Zyrtec

Generic Name: Cetirizine Hydrochloride
Class: Second Generation Antihistamines
VA Class: AH105
Chemical Name: [2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl] ethoxy]-acetic acid dihydrochloride
Molecular Formula: C₂₁H₂₅C_lN₂O₃•2ClH
CAS Number: 83881-52-1

Introduction

Second generation antihistamine; piperazine-derivative, carboxylic acid metabolite of hydroxyzine.^{1 2 3 11 12 20}

Uses for Zyrtec

Allergic Rhinitis

Self-medication for symptomatic relief of rhinorrhea, sneezing, lacrimation, itching eyes, and/or oronasopharyngeal itching associated with seasonal (e.g., hay fever) allergic rhinitis or other upper respiratory allergies.^{1 2 3 12 20 25 26 27 42 46 49 62 63 68 69 70 71}

Symptomatic relief of perennial (nonseasonal) allergic rhinitis.¹

May be used alone or in fixed combination with pseudoephedrine hydrochloride;^{1 63 69} use fixed-combination preparation only when both antihistamine and nasal decongestant activity are needed concurrently.⁶³

Chronic Idiopathic Urticaria

Self-medication for symptomatic relief of pruritus associated with chronic idiopathic urticaria (e.g., hives);^{1 2 3 12 20 28 29 46 72} not for prevention of chronic idiopathic urticaria or allergic skin reactions.⁷²

Zyrtec Dosage and Administration

Administration

Oral Administration

Administer orally without regard to food.^{1 2 3 12 14 20} May adjust time of administration for individual patient requirements.^{1 3}

Oral solution (syrup): Use only the measuring device (i.e., cup) provided by the manufacturer.^{70 72}

Chewable tablets: Administer with or without water.^{1 71}

Fixed combination cetirizine/pseudoephedrine tablets (Zyrtec-D): Swallow whole; do not break or chew.^{63 69}

Dosage

Available as cetirizine hydrochloride; dosage expressed in terms of the salt.¹

Pediatric Patients

Allergic Rhinitis

Seasonal

Self-medication in children 2 to <6 years of age: 2.5 mg once daily (as oral solution); may increase dosage to a maximum of 5 mg daily, given either as a 5-mg dose once daily or, alternatively, as a 2.5-mg dose every 12 hours.^{1 70} (See Pediatric Use under Cautions.)

Self-medication in children ≥6 years of age: 5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25 68 70 71} In clinical trials, most children ≥12 years of age received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

Self-medication in children ≥12 years of age: 5 mg every 12 hours (in fixed combination with 120 mg pseudoephedrine hydrochloride).^{63 69}

Perennial

Oral

Children 6 months to <2 years of age: 2.5 mg once daily (as oral solution).¹ In children 12–23 months of age, may increase dosage to a maximum of 5 mg daily, given as 2.5 mg every 12 hours.¹ (See Pediatric Use under Cautions.)

Children 2–5 years of age: 2.5 mg once daily (as oral solution);¹ may increase dosage to a maximum of 5 mg daily, given either as a 5-mg dose once daily (as chewable tablets or oral solution) or, alternatively, as a 2.5-mg dose every 12 hours (as oral solution).¹ (See Pediatric Use under Cautions.)

Children ≥6 years of age: 5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25} In clinical trials, most children ≥12 years of age received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

Children ≥12 years of age: 5 mg twice daily (every 12 hours) (in fixed combination with 120 mg pseudoephedrine hydrochloride).⁶³

Chronic Idiopathic Urticaria

Oral

Children 6 months to <2 years of age: 2.5 mg once daily (as oral solution).¹ In children 12–23 months of age, may increase dosage to a maximum of 5 mg daily, given as 2.5 mg every 12 hours.¹ (See Pediatric Use under Cautions.)

Children 2–5 years of age: 2.5 mg once daily (as oral solution);¹ may increase dosage to a maximum of 5 mg daily, given either as a 5-mg dose once daily (as chewable tablets or oral solution) or, alternatively, as a 2.5-mg dose every 12 hours (as oral solution).¹ (See Pediatric Use under Cautions.)

Self-medication in children ≥6 years of age: 5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25 72} In clinical trials, most children ≥12 years of age received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

Adults

Allergic Rhinitis

Seasonal

Oral

Self-medication: 5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25 68 70 71} In clinical trials, most patients received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

Self-medication: 5 mg twice daily (every 12 hours) (in fixed combination with 120 mg pseudoephedrine hydrochloride).^{63 69}

Perennial

Oral

5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25} In clinical trials, most patients received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

5 mg twice daily (every 12 hours) (in fixed combination with 120 mg pseudoephedrine hydrochloride).⁶³

Chronic Idiopathic Urticaria

Oral

Self-medication: 5 or 10 mg once daily (as chewable or conventional tablets or oral solution), depending on symptom severity.^{1 2 3 15 20 22 23 25 72} In clinical trials, most patients received an initial dosage of 10 mg daily; no additional benefit observed with 20-mg daily dosage.¹

Prescribing Limits

Pediatric Patients

Allergic Rhinitis

Oral

Children 12 months to <2 years of age: Maximum 5 mg daily.¹

Self-medication in children 2 to <6 years of age: Maximum 5 mg in 24 hours.⁷⁰ (See Pediatric Use under Cautions.)

Self-medication in children ≥6 years of age: Maximum 10 mg in 24 hours.^{68 70 71}

Self-medication in children ≥12 years of age: Maximum 10 mg daily (in fixed combination with 120 mg pseudoephedrine hydrochloride).⁶⁹ Fixed-combination preparation not recommended for children <12 years of age; contains 120 mg pseudoephedrine hydrochloride, which exceeds recommended single dose in such patients.⁶³

Children ≥12 years of age: In clinical trials, a 20-mg daily dosage did not provide additional clinical benefit.¹

Chronic Idiopathic Urticaria

Oral

Children 12 months to 5 years of age: Maximum 5 mg daily.¹

Self-medication in children ≥6 years of age: Maximum 10 mg in 24 hours.⁷²

Children ≥12 years of age: In clinical trials, a 20-mg daily dosage did not provide additional clinical benefit.¹

Adults

Allergic Rhinitis

Oral

Self-medication: Maximum 10 mg in 24 hours (alone or in fixed combination with 120 mg pseudoephedrine hydrochloride).^{68 69} In clinical trials, a 20-mg daily dosage did not provide additional clinical benefit.¹

Chronic Idiopathic Urticaria

Oral

Self-medication: Maximum 10 mg in 24 hours.⁷² In clinical trials, a 20-mg daily dosage did not provide additional clinical benefit.¹

Special Populations

Hepatic Impairment

Children <6 years of age: Use not recommended.¹

Adults and children ≥6 years of age: 5 mg once daily (as chewable or conventional tablets or oral solution).^{1 3}

Adults and children ≥12 years of age: 5 mg once daily (in fixed combination with 120 mg pseudoephedrine hydrochloride).⁶³

Renal Impairment

Children <6 years of age: Use not recommended.¹

Adults and children ≥6 years of age: 5 mg once daily (as chewable or conventional tablets or oral solution) in patients with impaired renal function (e.g., Cl_cr of 11–31 mL/minute) or those on hemodialysis (e.g., Cl_cr <7 mL/minute).^{1 3}

Adults and children ≥12 years of age: 5 mg once daily (in fixed combination with 120 mg pseudoephedrine hydrochloride) in patients with impaired renal function (e.g., Cl_cr of 11–31 mL/minute) or those on hemodialysis (e.g., Cl_cr <7 mL/minute).⁶³

Geriatric Patients

Self-medication in patients ≥65 years of age: 5 mg once daily (as chewable or conventional tablets or oral solution); do not exceed this amount in 24 hours.^{70 71 72}

Cautions for Zyrtec

Contraindications

• 
  

  Known hypersensitivity to cetirizine, hydroxyzine, or any ingredient in the formulation.^{1 3 63 68 69 70 71 72}

  
  

Warnings/Precautions

General Precautions

Prescribing and Dispensing Errors

Ensure accuracy of prescription; similarities in spelling, dosage intervals, and tablet strengths of Zyrtec and Zyprexa (olanzapine, an atypical antipsychotic agent) may result in errors.⁶⁵

CNS Effects

Risk of somnolence;^{1 2 3 5 6 27 28 39 41 42 43 49} caution required when performing hazardous activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle).^{1 3} (See Specific Drugs under Interactions.)

Use of Fixed Combinations

When used in fixed combination with pseudoephedrine hydrochloride (Zyrtec-D), consider the cautions, precautions, and contraindications associated with pseudoephedrine.^{63 69}

Specific Populations

Pregnancy

Chewable or conventional tablets or oral solution: Category B.¹

Fixed-combination cetirizine hydrochloride/pseudoephedrine hydrochloride: Category C.⁶³

Lactation

Distributed into milk.^{1 63} Use not recommended.^{1 3 57 63 68 69 70 71 72}

Pediatric Use

Chewable or conventional tablets or oral solution: Safety and efficacy not established in children <6 months of age; oral solution is the recommended formulation in children <2 years of age.¹

Fixed-combination cetirizine hydrochloride/pseudoephedrine hydrochloride: Safety and efficacy not established in children <12 years of age; use not recommended in this age group.⁶³

Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.^{66 67} Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.⁶⁶ Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of nonprescription cough and cold preparations to avoid overdosage.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.¹ No overall differences in safety relative to younger patients, but increased sensitivity cannot be ruled out.¹ Select dosage with caution because of age-related decreases in renal function; periodic monitoring of renal function recommended.^{1 3 20 39 46} Dosage adjustment recommended in patients ≥65 years of age.¹ (See Geriatric Patients under Dosage and Administration.)

Hepatic Impairment

Decreased clearance in patients with chronic hepatic impairment.^{1 3 20 39} Dosage adjustment necessary.^{1 3} (See Hepatic Impairment under Dosage and Administration.) Use not recommended in children <6 years of age with hepatic impairment.¹

Renal Impairment

Decreased clearance in patients with moderate renal impairment (Cl_cr of 11–31 mL/minute) or in those on hemodialysis.^{1 3 20 46 60} Dosage adjustment necessary.¹ (See Renal Impairment under Dosage and Administration.) Use not recommended in children <6 years of age with renal impairment.¹

Common Adverse Effects

Adults and children ≥12 years of age: somnolence, fatigue, dry mouth.¹ Insomnia reported with cetirizine hydrochloride-pseudoephedrine hydrochloride fixed combination.⁶³

Children 2–11 years of age: headache, pharyngitis, abdominal pain.¹

Children 6 months to 2 years of age: irritability, fussiness, insomnia, fatigue, malaise.¹

Interactions for Zyrtec

Metabolized minimally in the liver;² not known whether metabolized by CYP microsomal enzyme system.^{48 56 57} May have low potential for adverse drug interactions associated with metabolic enzyme systems.²

Drugs Affecting Hepatic Microsomal Enzymes

Concomitant administration with drugs known to inhibit CYP microsomal enzymes has not been associated with clinically important changes in ECG parameters (e.g., QT_c intervals).^{1 3 31 56}

Specific Drugs

Drug	Interaction	Comments
Azithromycin	No clinically important changes in ECG parameters observed with concomitant therapy; no clinically important interactions reported1 3 31 56
CNS depressants (e.g., alcohol, sedatives, tranquilizers)	Possible additive CNS effects (e.g., increased drowsiness)1 3 68 69 70 71 72	Avoid concomitant use1 3
Erythromycin	No clinically important changes in ECG parameters observed with concomitant therapy; no clinically important interactions reported1 3 31 56
Ketoconazole	Prolongation of QTc interval (with an increase of 17.4 msec) observed with concomitant administration; no clinically important interactions reported1 56 57	Not considered clinically important1 56 57
MAO	Potentiated pressor effects of sympathomimetic drugs (e.g., pseudoephedrine)63	Avoid concomitant use of fixed-combination preparation containing cetirizine hydrochloride and pseudoephedrine hydrochloride (Zyrtec-D) with an MAO inhibitor, or for 2 weeks after discontinuance of an MAO inhibitor63
Pseudoephedrine	No pharmacokinetic interactions observed1 3
Theophylline	Decreased clearance (16%) of cetirizine; disposition of theophylline not altered with concomitant administration1 3

Zyrtec Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed from the GI tract following oral administration,^{12 14 47 48} with peak plasma concentrations achieved in about 1 hour.^{1 2 3 4 14 39 46 47 48}

Bioavailability of chewable tablets or oral solution is comparable to that of conventional tablets.¹

Onset

Antihistaminic effect noted in 95% of adults and children at 1 hour.^{1 2 3 6 14 20 43}

Duration

Antihistaminic effect persists for about 24 hours.^{1 2 3 6 14 20 43}

Food

Food may decrease peak plasma concentrations and rate of absorption, but does not affect extent of absorption.^{1 2 3 12 20 63}

Distribution

Extent

Distribution into human body tissues not fully elucidated.^{1 3} Appears to be extensively distributed into many body tissues and fluids in animals; ³ brain cetirizine concentrations were <10% of those measured in plasma.²

Distributed into milk.¹

Plasma Protein Binding

Approximately 93%.^{1 3}

Elimination

Metabolism

Undergoes a low degree of first-pass metabolism in the liver; metabolized to limited extent by oxidative O-dealkylation to a metabolite with negligible antihistaminic activity.^{1 2 3 11 14 39 46 47 56 57}

Elimination Route

80% of a dose is excreted in urine, mainly as unchanged drug.^{1 2 4 12 14 20 39 46 47 48 57}

Half-life

Initial distribution half-life is about 3 hours;⁴⁸ terminal elimination half-life is about 8.3 hours.^{1 2 4 12 14 20 39 47 48 57}

Special Populations

In patients with chronic hepatic impairment or moderate renal impairment (e.g., Cl_cr of 11–31 mL/minute) or in those on hemodialysis, half-life is increased and clearance is decreased.^{1 3 20 39}

In geriatric patients (mean: 77 years of age), half-life is increased and clearance is decreased,¹ possibly due to age-related changes in renal function.^{1 3 20 39 46}

In pediatric patients, half-life is decreased and clearance is increased.¹

Stability

Storage

Oral

Tablets and Chewable Tablets

20–25°C (may be exposed to 15–30°C).^{1 63 68 71 72}

Solution

20–25°C (may be exposed to 15–30°C).¹ Also may be refrigerated at 2–8°C.¹

ActionsActions

• 
  

  Exhibits selective antagonism of peripheral histamine H₁-receptors.^{1 2 3 6 14 20 47 48}

  
  


• 
  

  Antihistaminic effect is comparable to that of astemizole (no longer commercially available in the US), clemastine, chlorpheniramine, diphenhydramine, hydroxyzine, loratadine, pyrilamine, and terfenadine (no longer commercially available in the US).^{2 3 20 43} Tolerance to antihistaminic effect usually does not occur.²

  
  


• 
  

  No appreciable anticholinergic or antiserotonergic effects in animal models,^{56 57} but dry mouth more common with cetirizine than placebo in clinical trials.^{1 3 20 28 41 49}

  
  

Advice to Patients

• 
  

  For self-medication, importance of taking only as directed and not exceeding recommended dosage.⁶⁹

  
  


• 
  

  Risk of somnolence;^{1 2 3 5 6 27 28 39 41 42 43 49} importance of exercising caution when performing activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle).^{1 68 69 70 71 72}

  
  


• 
  

  For self-medication with cetirizine in fixed combination with pseudoephedrine, importance of discontinuing therapy and contacting a clinician if symptoms do not improve within 7 days or are accompanied by fever, or if nervousness, dizziness, or sleeplessness occurs.⁶⁹

  
  


• 
  

  For self-medication for management of chronic idiopathic urticaria (e.g., hives), importance of understanding that cetirizine does not prevent hives.⁷² Importance of consulting a clinician before initiating therapy if hives are unusual in color, look bruised or blistered, or do not itch.⁷² Importance of discontinuing therapy and contacting a clinician if symptoms do not improve within 3 days or if hives have persisted for >6 weeks.⁷²

  
  


• 
  

  Importance of understanding that chronic idiopathic urticaria may present with other severe allergic reactions, including anaphylactic shock (e.g., trouble swallowing, swelling of the tongue, trouble speaking, wheezing or trouble breathing, dizziness or loss of consciousness, swelling in or around the mouth, drooling).⁷² These manifestations may occur when hives first appear or up to several hours later and can be life-threatening if not treated immediately.⁷² Importance of immediately seeking emergency help if anaphylactic shock occurs.⁷² If an epinephrine auto-injector has been prescribed, importance of carrying this device at all times; never use cetirizine as a substitute for the epinephrine auto-injector.⁷²

  
  


• 
  

  Importance of discontinuing the drug immediately and informing a clinician if an allergic or hypersensitivity reaction occurs.^{69 70 71}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.^{1 63}

  
  


• 
  

  Importance of patients with renal or hepatic impairment, heart disease, hypertension, thyroid disease, diabetes mellitus, glaucoma, or difficulty in urination resulting from prostate enlargement not undertaking self-medication without first consulting a clinician.^{69 70 71 72}

  
  


• 
  

  Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.^{1 63}

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Cetirizine Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Solution	5 mg/5 mL	Children's Zyrtec Hives Relief Syrup	McNeil
			Children's Zyrtec Syrup	McNeil
	Tablets, chewable	5 mg	Children's Zyrtec Chewables	McNeil
		10 mg	Children's Zyrtec Chewables	McNeil
	Tablets, film-coated	10 mg	Zyrtec	McNeil

Cetirizine Hydrochloride Combinations

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, extended-release	5 mg with Pseudoephedrine Hydrochloride 120 mg	Zyrtec-D	McNeil

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Cetirizine HCl 10MG Tablets (PERRIGO): 100/$18.99 or 300/$39.96

Cetirizine HCl 5MG Tablets (APOTEX): 100/$99.99 or 300/$253.98

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions February 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

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34. Proud D, Naclerio RM, Gwaltney JM et al. Kinins are generated in nasal secretions during natural rhinovirus colds. J Infect Dis. 1990; 161:120-3. [PubMed 2295843]

35. Proud D, Gwaltney JM Jr, Hendley JO et al. Increased levels of interleukin-1 are detected in nasal secretions of volunteers during experimental rhinovirus colds. J Infect Dis. 1994; 169:1007-13. [IDIS 329294] [PubMed 8169385]

36. Turner RB. Elaboration of interleukin 8 from fibroblast cells and human nasal epithelium in response to rhinovirus challenge. Program and abstracts of the thirty-fourth Interscience Conference on Antimicrobial Agents and Chemotherapy. Orlando, FL: 1994. Abstract No. B43.

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38. Lambert D, Hantzperg M, Danglas P et al. Double-blind comparative study of terfenadine and cetirizine in chronic idiopathic urticaria. Allerg Immunol. 1993; 25:235- 40.

39. Simons FER, Watson WTA, Minuk GY et al. Cetirizine pharmacokinetics and pharmacodynamics in primary biliary cirrhosis. J Clin Pharmacol. 1993; 33:949-54. [IDIS 320880] [PubMed 7693767]

40. Wasserfallen JB, Leuenberger P, Pécoud A. Effect of cetirizine, a new H₁ antihistamine, on the early and late allergic reactions in a bronchial provocation test with allergen. J Allergy Clin Immunol. 1993; 91:1189-97. [IDIS 315943] [PubMed 8099593]

41. Berkowitz RB, Dockhorn R, Lockey R et al. Comparison of efficacy, safety, and skin test inhibition of cetirizine and astemizole. Ann Allergy Asthma Immunol. 1996; 76:363- 8. [IDIS 3

Kuvan

Generic Name: Sapropterin Dihydrochloride
Class: Other Miscellaneous Therapeutic Agents
Chemical Name: (6R)-2-amino-6-[(1R, 2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-4(1H)-pteridinone dihydrochloride
Molecular Formula: C₉H₁₅N₅O₃ • 2HCl
CAS Number: 69056-38-8

Introduction

Synthetic dihydrochloride salt of naturally occurring tetrahydrobiopterin (BH₄); cofactor in the metabolism of phenylalanine.^{1 4 5 6}

Uses for Kuvan

Phenylketonuria

Used to reduce blood phenylalanine concentrations in patients with hyperphenylalaninemia associated with tetrahydrobiopterin (BH₄)-responsive phenylketonuria (PKU).^{1 4 5 6} Use in conjunction with a phenylalanine-restricted diet.¹ Designated an orphan drug by FDA for this use.³

Kuvan Dosage and Administration

General

• 
  

  Carefully monitor blood phenylalanine concentrations during therapy.¹ Measure blood phenylalanine concentrations after 1 week of treatment and periodically for up to 1 month to evaluate response to therapy.¹

  
  


• 
  

  Dietary phenylalanine intake must not be modified while response to sapropterin therapy is being evaluated so that the drug’s effect on phenylalanine concentrations can be accurately assessed.¹ (See Response to Treatment under Cautions.)

  
  

Administration

Oral Administration

Administer orally once daily with food, preferably at the same time each day.^{1 2}

Dissolve tablets in 4–8 ounces of water or apple juice and consume within 15 minutes of dissolution.^{1 2} Dissolution may take several minutes; stirring the mixture or crushing the tablets may increase rate of dissolution, but complete dissolution may not occur.^{1 2} If visible tablet fragments remain in the glass after mixture has been consumed, rinse the glass with additional water or apple juice then swallow the rinse to ensure that entire dose is consumed.^{1 2}

Take a missed dose as soon as possible, but avoid taking 2 doses on the same day.^{1 2}

Dosage

Available as sapropterin dihydrochloride; dosage expressed in terms of the salt.¹

Response to therapy is determined by change in blood phenylalanine concentrations.¹

Pediatric Patients

Phenylketonuria

Oral

Children ≥4 years of age: Initially, 10 mg/kg once daily.^{1 2 6 8} If blood phenylalanine concentrations do not decrease from baseline after 1 month of treatment, increase dose to 20 mg/kg once daily.^{1 6} If blood phenylalanine concentrations do not decrease after 1 month of treatment at 20 mg/kg once daily, consider the patient a nonresponder and discontinue therapy.^{1 6}

For responders, adjust dose within the range of 5–20 mg/kg once daily based on blood phenylalanine concentrations.¹

Dosages >20 mg/kg once daily not studied.¹

Adults

Phenylketonuria

Oral

Initially, 10 mg/kg once daily.^{1 2 6 8} If blood phenylalanine concentrations do not decrease from baseline after 1 month of treatment, increase dose to 20 mg/kg once daily.^{1 6} If blood phenylalanine concentrations do not decrease after 1 month of treatment at 20 mg/kg once daily, consider the patient a nonresponder and discontinue therapy.^{1 6}

For responders, adjust dose within the range of 5–20 mg/kg once daily based on blood phenylalanine concentrations.¹

Dosages >20 mg/kg once daily have not been studied.¹

Prescribing Limits

Pediatric Patients

Phenylketonuria

Oral

Safety and efficacy of dosages >20 mg/kg daily not established.¹

Adults

Phenylketonuria

Oral

Safety and efficacy of dosages >20 mg/kg daily not established.¹

Special Populations

No special population dosage recommendations at this time.¹

Cautions for Kuvan

Contraindications

• 
  

  Known severe hypersensitivity to sapropterin or any ingredient in the formulation.¹

  
  

Warnings/Precautions

Sensitivity Reactions

Consider risks and benefits of continued treatment if mild to moderate allergic reactions (e.g., rash) occur.¹ However, severe allergic reactions not reported in clinical trials.¹

Patient Evaluation and Monitoring

Treatment should be directed by clinicians knowledgeable in the management of patients with PKU.¹

Carefully monitor blood phenylalanine concentrations during therapy.¹ All patients should follow a phenylalanine-restricted diet; use of sapropterin does not eliminate the need for ongoing dietary management.¹

Prolonged elevations of phenylalanine can lead to severe cognitive, behavioral, and other neurologic complications (e.g., severe mental retardation, microcephaly, delayed speech, seizures).^{1 6} Long-term data not available on neurocognitive outcomes in patients receiving sapropterin.¹

Prolonged blood concentrations of phenylalanine that are too low have been associated with catabolism and protein breakdown.¹

Response to Treatment

Approximately 20–56% of patients with PKU respond to sapropterin.^{1 4} A therapeutic trial of the drug with close monitoring of blood phenylalanine concentrations is needed to identify responders.^{1 4 5 6} Response cannot be predicted based on laboratory testing (e.g., genetic testing).^{1 5} Discontinue treatment in patients who do not respond.^{1 8} (See Dosage under Dosage and Administration.)

Interactions

Concomitant use with certain drugs requires caution (e.g., methotrexate, PDE-5 inhibitors, levodopa).¹ (See Specific Drugs under Interactions.)

Specific Populations

Pregnancy

Category C.¹ Pregnant women are encouraged to enroll in manufacturer’s sapropterin pregnancy registry (The Maternal Phenylketonuria Observational Program [PKU MOMS Subregistry]), which monitors pregnant women and fetal outcomes of pregnant women exposed to sapropterin.^{1 7}

Lactation

Distributed into milk in rats; not known whether distributed into human milk.¹ Discontinue nursing or the drug.¹

Pediatric Use

Safety and efficacy not evaluated in children <4 years of age in clinical studies.¹ Blood phenylalanine concentrations should be frequently monitored to ensure adequate control.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently from younger patients.¹

Hepatic Impairment

Not studied in patients with hepatic impairment.^{1 8} Hepatic damage has been associated with impaired phenylalanine metabolism; careful monitoring is recommended.^{1 8}

Renal Impairment

Not studied in patients with renal impairment; monitor carefully.^{1 8}

Common Adverse Effects

Headache, diarrhea, abdominal pain, upper respiratory tract infection, pharyngolaryngeal pain, nausea, vomiting, rhinorrhea, nasal congestion, cough, pyrexia, contusion, rash, mild to moderate neutropenia.^{1 2}

Interactions for Kuvan

Inhibitors of Folate Metabolism

Possible decreased tetrahydrobiopterin (BH₄) concentrations with drugs that affect folate metabolism and their derivatives.¹ Use with caution.¹

Drugs Affecting Nitric Oxide-Mediated Vascular Relaxation

Possible additive vascular relaxation and reduction in BP.¹ Use with caution.¹

Specific Drugs

Drug	Interaction	Comments
Levodopa	Seizures, exacerbation of seizures, overstimulation, or irritability reported rarely in patients with neurologic disorders1	Use concomitantly with caution1
Methotrexate	Possible decreased BH4 concentrations due to inhibition of dihydropteridine reductase1	Use concomitantly with caution1
Phosphodiesterase inhibitors (e.g., sildenafil, tadalafil, vardenafil)	Possible hypotensive effect and additive vasorelaxation1	Use concomitantly with caution1

Kuvan Pharmacokinetics

Absorption

Onset

Phenylalanine concentrations decrease within 24 hours following a single dose; maximal reductions occur within 1 month with daily administration.¹

Duration

Phenylalanine concentrations remain stable over a 24-hour period following a single daily dose.¹

Food

Absorption comparable when tablets are dissolved in water or orange juice under fasted conditions.¹ Phenylalanine concentrations do not substantially increase with food intake following a single dose.¹

High-fat/high-calorie meal may increase absorption of sapropterin.¹

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.¹

Elimination

Half-life

Approximately 6.7 hours.¹

Special Populations

Pharmacokinetics unaffected by age within the range of 9–49 years of age; not studied outside this range.¹

Hepatic damage may impair phenylalanine metabolism.¹

Stability

Storage

Oral

Tablets

Tight containers at 20–25°C (may be exposed to 15–30°C).¹ Protect from moisture.¹

ActionsActions

• 
  

  Cofactor for phenylalanine hydroxylase (PAH), the enzyme that hydroxylates phenylalanine through an oxidative reaction to form tyrosine.^{1 4 5}

  
  


• 
  

  Enhances activity of residual PAH in patients with PKU, which improves the normal oxidative metabolism of phenylalanine and thus decreases blood phenylalanine concentrations in some patients with PKU.^{1 4 5}

  
  

Advice to Patients

• 
  

  Importance of providing patient or caregivers a copy of manufacturer’s patient information.¹

  
  


• 
  

  Importance of informing patients that not all patients with PKU will respond to therapy with sapropterin.^{1 2 6}

  
  


• 
  

  Importance of patients following a phenylalanine-restricted diet.^{1 2}

  
  


• 
  

  Importance of monitoring blood phenylalanine concentrations.^{1 2}

  
  


• 
  

  If a dose is missed, the missed dose should be taken as soon as possible.^{1 2} Two doses should not be taken on the same day.^{1 2}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 2}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant medical conditions .^{1 2}

  
  


• 
  

  Importance of informing clinicians of concomitant medical conditions.^{1 2}

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Sapropterin Dihydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, dispersible	100 mg	Kuvan	BioMarin

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. BioMarin Pharmaceutical Inc. Kuvan (sapropterin dihydrochloride) tablets prescribing information. Novato, CA; 2007 Dec.

2. BioMarin Pharmaceutical Inc. Kuvan (sapropterin dihydrochloride) tablets patient information. Novato, CA; 2007 Dec.

3. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD; 2008 May 16. From FDA website. Accessed 2008 Jul 22.

4. Burton BK, Grange DK, Milanowski A, et al. The response of patients with phenylketonuria and elevated serum phenylalanine to treatment with oral sapropterin dihydrochloride (6R-tetrahydrobiopterin): a phase II, multicentre, open-label, screening study. J Inherit Metab Dis. 2007; 30:700-7. [PubMed 17846916]

5. Levy HL, Milanowski A, Chakrapani A, et al. Efficacy of sapropterin dihydrochloride (tetrahydrobiopterin, 6R-BH4) for reduction of phenylalanine concentration in patients with phenylketonuria: a phase III randomised placebo-controlled study. Lancet. 2007; 370:504-10. [PubMed 17693179]

6. Anon. Sapropterin (Kuvan) for phenylketonuria. Med Lett Drugs Ther. 2008; 50:43-4. [PubMed 18509266]

7. BioMarin Pharmaceutical Inc. The Phenylketonuria Demographics, Outcomes, and Safety (PKUDOS) registry: information for patients. From Kuvan website. Accessed 2008 Oct 9.

8. BioMarin, Novato, CA: Personal communication.

More Kuvan resources

• Kuvan Side Effects (in more detail)
• Kuvan Use in Pregnancy & Breastfeeding
• Kuvan Drug Interactions
• Kuvan Support Group
• 0 Reviews for Kuvan - Add your own review/rating

• Kuvan Prescribing Information (FDA)


• Kuvan Advanced Consumer (Micromedex) - Includes Dosage Information


• Kuvan MedFacts Consumer Leaflet (Wolters Kluwer)


• Kuvan Consumer Overview

Compare Kuvan with other medications

• Phenylketonuria

Vitile XL Prolonged-release Tablets

1. Name Of The Medicinal Product

Vitile XL 30 mg Prolonged-release Tablets

2. Qualitative And Quantitative Composition

Each modified-release tablet contains gliclazide 30 mg.

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Modified-release tablet.

White, oval, biconvex 4.5 x 10.1 mm tablets marked “G” on one side.

4. Clinical Particulars

4.1 Therapeutic Indications

Non insulin-dependent diabetes (type 2) in adults when dietary measures, physical exercise and weight loss alone are not sufficient to control blood glucose.

4.2 Posology And Method Of Administration

Oral use.

For adult use only.

The daily dose may vary from 1 to 4 tablets per day, i.e. from 30 to 120 mg taken orally in a single intake at breakfast time.

The tablet(s) should be swallowed whole without chewing or crushing.

If a dose is forgotten, there must be no increase in the dose taken the next day.

As with any hypoglycaemic agent, the dose should be adjusted according to the individual patient's metabolic response (blood glucose, HbA_lc).

Initial dose

The recommended starting dose is 30 mg daily.

If blood glucose is effectively controlled, this dose may be used for maintenance treatment.

If blood glucose is not adequately controlled, the dose may be increased to 60, 90 or 120 mg daily, in successive steps. The interval between each dose increment should be at least 1 month except in patients whose blood glucose has not reduced after two weeks of treatment. In such cases, the dose may be increased at the end of the second week of treatment.

The maximum recommended daily dose is 120 mg.

Switching from gliclazide 80 mg tablets to Vitile XL 30 mg Prolonged-release Tablets

1 tablet of gliclazide 80 mg is comparable to 1 tablet of Vitile XL 30 mg Prolonged-release Tablets

Consequently the switch can be performed provided a careful blood monitoring.

Switching from another oral antidiabetic agent to Vitile XL 30 mg Prolonged-release Tablets

Vitile XL 30 mg Prolonged-release Tablets can be used to replace other oral antidiabetic agents.

The dosage and the half-life of the previous antidiabetic agent should be taken into account when switching to Vitile XL 30 mg Prolonged-release Tablets.

A transitional period is not generally necessary. A starting dose of 30 mg should be used and this should be adjusted to suit the patient's blood glucose response, as described above.

When switching from a hypoglycaemic sulfonylurea with a prolonged half-life, a treatment free period of a few days may be necessary to avoid an additive effect of the two products, which might cause hypoglycaemia. The procedure described for initiating treatment should also be used when switching to treatment with / Vitile XL 30 mg Prolonged-release Tablets i.e. a starting dose of 30 mg/day, followed by a stepwise increase in dose, depending on the metabolic response.

Combination treatment with other antidiabetic agents

Vitile XL 30 mg Prolonged-release Tablets can be given in combination with biguanides, alpha glucosidase inhibitors or insulin.

In patients not adequately controlled with Vitile XL 30 mg Prolonged-release Tablets, concomitant insulin therapy can be initiated under close medical supervision.

In the elderly (over 65 years)

Vitile XL 30 mg Prolonged-release Tablets should be prescribed using the same dosing regimen recommended for patients under 65 years of age.

In patients with mild to moderate renal insufficiency

The same dosing regimen can be used as in patients with normal renal function with careful patient monitoring. These data have been confirmed in clinical trials.

In patients at risk of hypoglycaemia

There is an increased risk of hypoglycaemia in following patients:

- undernourished or malnourished

- with severe or poorly compensated endocrine disorders (hypopituitarism, hypothyroidism, adrenocorticotrophic insufficiency)

- following withdrawal of prolonged and/or high dose corticosteroid therapy

- with severe vascular disease (severe coronary heart disease, severe carotid impairment, diffuse vascular disease).

It is recommended that the minimum daily starting dose of 30 mg is used.

Children and adolescents

There are no data and clinical studies available in children and adolescents below 18 years.

4.3 Contraindications

• known hypersensitivity to gliclazide or to any of the excipients, other sulfonylureas or sulfonamides

• type 1 diabetes

• diabetic pre-coma and coma, diabetic keto-acidosis

• severe renal or hepatic insufficiency: in these cases the use of insulin is recommended

• treatment with miconazole (see section 4.5)

• lactation (see section 4.6).

4.4 Special Warnings And Precautions For Use

Hypoglycaemia

This treatment should be prescribed only if the patient is likely to have a regular food intake (including breakfast). It is important to have a regular carbohydrate intake due to the increased risk of hypoglycaemia if a meal is taken late, if an inadequate amount of food is consumed or if the food is low in carbohydrate. Hypoglycaemia is more likely to occur during low-calorie diets, following prolonged or strenuous exercise, alcohol intake or if a combination of hypoglycaemic agents is being used.

Hypoglycaemia may occur following administration of sulfonylureas (see section 4.8). Some cases may be severe and prolonged. Hospitalisation may be necessary and glucose administration may need to be continued for several days.

Careful selection of patients, of the dose used, and clear patient directions are necessary to reduce the risk of hypoglycaemic episodes.

Factors which increase the risk of hypoglycaemia:

• patient refuses or (particularly in elderly subjects) is unable to co-operate

• malnutrition, irregular mealtimes, skipping meals, periods of fasting or dietary changes

• imbalance between physical exercise and carbohydrate intake

• renal insufficiency

• severe hepatic insufficiency

• overdose of Vitile XL 30 mg Prolonged-release Tablets

• certain endocrine disorders: thyroid disorders, hypopituitarism and adrenal insufficiency

• concomitant administration of alcohol or certain other medicines (see section 4.5).

Renal and hepatic insufficiency

The pharmacokinetics and/or pharmacodynamics of gliclazide may be altered in patients with hepatic insufficiency or severe renal failure. A hypoglycaemic episode occurring in these patients may be prolonged, so appropriate management should be initiated.

Patient information

The risks of hypoglycaemia, together with its symptoms, treatment and conditions that predispose to its development, should be explained to the patient and to family members.

The patient should be informed of the importance of following dietary advice, of taking regular exercise, and of regular monitoring of blood glucose levels.

Poor blood glucose control

Blood glucose control in a patient receiving antidiabetic treatment may be affected by any of the following: fever, trauma, infection or surgical intervention. In some cases, it may be necessary to administer insulin.

The hypoglycaemic efficacy of any oral antidiabetic agent, including gliclazide, is attenuated over time in many patients. This may be due to progression in the severity of the diabetes, or to a reduced response to treatment. This phenomenon is known as secondary failure which is distinct from primary failure, when an active substance is ineffective as first-line treatment. Adequate dose adjustment and dietary compliance should be considered before classifying the patient as secondary failure.

Laboratory tests

Measurement of glycated haemoglobin levels (or fasting venous plasma glucose) is recommended in assessing blood glucose control. Blood glucose self-monitoring may also be useful.

Treatment of patients with glucose-6-phosphate (G6PD)-deficiency with sulfonylurea agents can lead to haemolytic anaemia. Since gliclazide belongs to the chemical class of sulfonylurea drugs, caution should be used in patients with G6PD-deficiency and a non-sulfonylurea alternative should be considered.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

The following products are likely to increase the risk of hypoglycaemia

Contraindicated combination

- Miconazole (systemic route, oromucosal gel): increases the hypoglycaemic effect with possible onset of hypoglycaemic symptoms, or even coma.

Combinations which are not recommended

- Phenylbutazone (systemic route): increases the hypoglycaemic effect of sulfonylureas (displaces their binding to plasma proteins and/or reduces their elimination). It is preferable to use a different anti-inflammatory agent, or else to warn the patient and emphasise the importance of self-monitoring. Where necessary, adjust the dose during and after treatment with the anti-inflammatory agent.

- Alcohol: increases the hypoglycaemic reaction (by inhibiting compensatory reactions) that can lead to the onset of hypoglycaemic coma. Avoid alcohol or medicines containing alcohol.

Combinations requiring precautions for use

Potentiation of the blood glucose lowering effect and thus, in some instances, hypoglycaemia may occur when one of the following drugs is taken, for example:

Other antidiabetic agents (insulins, acarbose, biguanides), beta-blockers, fluconazole, angiotensin converting enzyme inhibitors (captopril, enalapril), H₂-receptor antagonists, MAOIs, sulfonamides, and nonsteroidal anti-inflammatory agents.

The following products may cause an increase in blood glucose levels

Combination which is not recommended

- Danazol: diabetogenic effect of danazol.

If the use of this active substance cannot be avoided, warn the patient and emphasise the importance of urine and blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic agent during and after treatment with danazol.

Combinations requiring precautions during use

- Chlorpromazine (neuroleptic agent): high doses (> 100 mg per day of chlorpromazine) increase blood glucose levels (reduced insulin release).

Warn the patient and emphasise the importance of blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with the neuroleptic agent.

- Glucocorticoids (systemic and local route: intra-articular, cutaneous and rectal preparations) and tetracosactrin: increase in blood glucose levels with possible ketosis (reduced tolerance to carbohydrates due to glucocorticoids).

Warn the patient and emphasise the importance of blood glucose monitoring, particularly at the start of treatment. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with glucocorticoids.

- Ritodrine, salbutamol, terbutaline: I.V.

Increased blood glucose levels due to beta-2 agonist effects.

Emphasise the importance of monitoring blood glucose levels. If necessary, switch to insulin.

Combination which must be taken into account

- Anticoagulant therapy (e.g. warfarin):

Sulfonylureas may lead to potentiation of anticoagulation during concurrent treatment.

Adjustment of the anticoagulant may be necessary.

4.6 Pregnancy And Lactation

Pregnancy

There is no experience with the use of gliclazide during pregnancy in humans, even though there are few data with other sulfonylureas.

In animal studies, gliclazide is not teratogenic.

Control of diabetes should be obtained before the time of conception to reduce the risk of congenital abnormalities linked to uncontrolled diabetes.

Oral hypoglycaemic agents are not suitable, insulin is the drug of first choice for treatment of diabetes during pregnancy. It is recommended that oral hypoglycaemic therapy is changed to insulin before a pregnancy is attempted, or as soon as pregnancy is discovered.

Lactation

It is not known whether gliclazide or its metabolites are excreted in breast milk. Other sulfonylureas have been found in milk. Given the risk of neonatal hypoglycaemia, the product is contra-indicated in breast-feeding mothers.

4.7 Effects On Ability To Drive And Use Machines

Patients should be made aware of the symptoms of hypoglycaemia and should be careful if driving or operating machinery, especially at the beginning of treatment.

4.8 Undesirable Effects

Based on the experience with gliclazide and with other sulfonylureas, the following undesirable effects have to be mentioned.

Hypoglycaemia

As for other sulfonylureas, treatment with Vitile XL 30 mg Prolonged-release Tablets can cause hypoglycaemia, if mealtimes are irregular and, in particular, if meals are skipped. Possible symptoms of hypoglycaemia are: headache, intense hunger, nausea, vomiting, lassitude, sleep disorders, agitation, aggression, poor concentration, reduced awareness and slowed reactions, depression, confusion, visual and speech disorders, aphasia, tremor, paresis, sensory disorders, dizziness, feeling of powerlessness, loss of self-control, delirium, convulsions, shallow respiration, bradycardia, drowsiness and loss of consciousness, possibly resulting in coma and lethal outcome.

In addition, signs of adrenergic counter-regulation may be observed: sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris and cardiac arrhythmia.

Usually, symptoms disappear after intake of carbohydrates (sugar). However, artificial sweeteners have no effect. Experience with other sulfonylureas shows that hypoglycaemia can recur even when measures prove effective initially.

If a hypoglycaemic episode is severe or prolonged, and even if it is temporarily controlled by intake of sugar, immediate medical treatment or even hospitalisation are required.

Gastrointestinal disturbances, including abdominal pain, nausea, vomiting, dyspepsia, diarrhoea and constipation have been reported. These can be avoided or minimised if gliclazide is taken with a meal.

The following undesirable effects have been more rarely reported:

- Blood and lymphatic system disorders: Changes in haematology are rare. They may include anaemia, leucopenia, thrombocytopenia, granulocytopenia. These are in general reversible upon discontinuation of gliclazide.

- Skin and subcutaneous tissue disorders: Rash, pruritus, urticaria, erythema, maculopapular rashes, bullous reactions.

- Hepatobiliary disorders: Raised hepatic enzyme levels (ASAT, ALAT, alkaline phosphatase), hepatitis (isolated reports). Discontinue treatment if cholestatic jaundice appears.

These symptoms usually disappear after discontinuation of treatment.

- Eye disorders: Transient visual disturbances may occur, especially on initiation of treatment, due to changes in blood glucose levels.

Class attribution effects

Cases of erythrocytopenia, agranulocytosis, haemolytic anaemia, pancytopenia and allergic vasculitis have been described for other sulfonylureas.

With sulfonylureas cases were also observed of elevated liver enzyme levels and even impairment of liver function (e.g. with cholestasis and jaundice) and hepatitis which regressed after withdrawal of the sulfonylurea or led to life-threatening liver failure in isolated cases.

4.9 Overdose

An overdose of sulfonylureas may cause hypoglycaemia.

Moderate symptoms of hypoglycaemia, without any loss of consciousness or neurological signs, must be corrected by carbohydrate intake, dose adjustment and/or change of diet. Strict monitoring should be continued until the doctor is sure that the patient is out of danger.

Severe hypoglycaemic reactions, with coma, convulsions or other neurological disorders are possible and must be treated as a medical emergency, requiring immediate hospitalisation.

If hypoglycaemic coma is diagnosed or suspected, the patient should be given a rapid I.V. injection of 50 ml of concentrated glucose solution (20 to 30%). This should be followed by continuous infusion of a more dilute glucose solution (10%) at a rate that will maintain blood glucose levels above 1 g/l. Patients should be monitored closely and, depending on the patient's condition after this time, the doctor will decide if further monitoring is necessary.

Dialysis is of no benefit to patients due to the strong binding of gliclazide to proteins.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: Sulfonamides, urea derivaties, ATC code: A10BB09

Gliclazide is a hypoglycaemic sulfonylurea oral antidiabetic active substance differing from other related compounds by an N-containing heterocyclic ring with an endocyclic bond.

Gliclazide reduces blood glucose levels by stimulating insulin secretion from the β-cells of the islets of Langerhans. Increase in postprandial insulin and C-peptide secretion persists after two years of treatment.

In addition to these metabolic properties, gliclazide has haemovascular properties.

Effects on insulin release

In type 2 diabetics, gliclazide restores the first peak of insulin secretion in response to glucose and increases the second phase of insulin secretion. A significant increase in insulin response is seen in response to stimulation induced by a meal or glucose.

Haemovascular properties

Gliclazide decreases microthrombosis, which may be involved in complications of diabetes, by two mechanisms:

• a partial inhibition of platelet aggregation and adhesion, with a decrease in the markers of platelet activation (beta thromboglobulin, thromboxane B₂).

• an action on the vascular endothelium fibrinolytic activity with an increase in tPA activity.

5.2 Pharmacokinetic Properties

Plasma levels increase progressively during the first 6 hours, reaching a plateau which is maintained from the sixth to the twelfth hour after administration.

Intra-individual variability is low.

Gliclazide is completely absorbed. Food intake does not affect the rate or degree of absorption.

The relationship between the dose administered ranging up to 120 mg and the area under the concentration time curve is linear.

Plasma protein binding is approximately 95%.

Gliclazide is mainly metabolised in the liver and excreted in the urine: less than 1% of the unchanged form is found in the urine. No active metabolites have been detected in plasma.

The elimination half-life of gliclazide varies between 12 and 20 hours.

The volume of distribution is around 30 litres.

No clinically significant changes in pharmacokinetic parameters have been observed in elderly patients.

A single daily dose of Vitile XL 30 mg Prolonged-release Tablets maintains effective gliclazide plasma concentrations over 24 hours.

5.3 Preclinical Safety Data

Preclinical data reveal no special hazards for humans based on conventional studies of repeated dose toxicity and genotoxicity. Long term carcinogenicity studies have not been done. No teratogenic changes have been shown in animal studies, but lower foetal body weight was observed in animals receiving doses 25-fold higher than the maximum recommended dose in humans.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Sodium hydrogen carbonate

Mannitol (E421)

Calcium hydrogen phosphate dihydrate

Hypromellose

Silica colloidal anhydrous

Magnesium stearate

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

2 years.

6.4 Special Precautions For Storage

Al/PVC-PVDC blister:

Do not store above 25°C.

HDPE container:

Do not store above 25°C.

Store in the original package in order to protect from moisture.

6.5 Nature And Contents Of Container

Clear aluminium/PVC-PVDC blisters.

White tablet containers (HDPE) closed with snap-on cap (LDPE) with a tamper evident ring.

Pack sizes:

Blisters: 10, 20, 28, 30, 56, 60, 90, 98, 100, 120, 180 modified-release tablets.

Tablet containers: 30, 100 and 180 modified-release tablets.

Not all pack sizes may be marketed.

6.6 Special Precautions For Disposal And Other Handling

No special requirements.

7. Marketing Authorisation Holder

Actavis Group PTC ehf

Reykjavikurvegur 76-78

Hafnarfjordur

IS-220

Iceland

8. Marketing Authorisation Number(S)

PL 30306/0229

9. Date Of First Authorisation/Renewal Of The Authorisation

09/04/2010

10. Date Of Revision Of The Text

09/04/2010

11 DOSIMETRY

(IF APPLICABLE)

12 INSTRUCTIONS FOR PREPARATION OF RADIOPHARMACEUTICALS

(IF APPLICABLE)

Tice BCG

Generic Name: bacillus of calmette and guerin vaccine, live (Intravesical route)

ba-SILL-us of KAL-met and GARE-in VAX-een, lyve

Intravesical route(Powder for Suspension)

Bacillus of calmette and guerin infections have been reported in health care workers and patients due to exposure to the vaccine during preparation and administration. Bacillus of calmette and guerin is capable of dissemination when administered by the intravesical route, and serious infections, including fatal infections, have been reported in patients receiving intravesical bacillus of calmette and guerin. THERACYS(R) and TICE(R) BCG contains live, attenuated mycobacteria and because of the potential risk for transmission, it should be prepared, handled, and disposed of as a biohazard material .

Commonly used brand name(s)

In the U.S.

• Theracys


• Tice BCG

Available Dosage Forms:

• Powder for Solution


• Powder for Suspension

Therapeutic Class: Vaccine

Uses For Tice BCG

Bacillus Calmette-Guérin (BCG) is used as a solution that is run through a tube (instilled through a catheter) into the bladder to treat bladder cancer. The exact way it works against cancer is not known, but it may work by stimulating the body's immune system.

BCG is to be administered only by or under the immediate supervision of your doctor.

Before Using Tice BCG

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

There is no specific information comparing use of BCG for treatment of cancer in children with use in other age groups.

Geriatric

This medicine has been tested and has not been shown to cause different side effects or problems in older people than it does in younger adults.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aclarubicin


• Adalimumab


• Aldesleukin


• Altretamine


• Amonafide


• Amsacrine


• Asparaginase


• Azacitidine


• Azathioprine


• Bleomycin


• Broxuridine


• Busulfan


• Capecitabine


• Carboplatin


• Carmustine


• Certolizumab Pegol


• Chlorambucil


• Cisplatin


• Cladribine


• Cyclophosphamide


• Cytarabine


• Cytarabine Liposome


• Dacarbazine


• Dactinomycin


• Daunorubicin


• Daunorubicin Citrate Liposome


• Decitabine


• Docetaxel


• Doxifluridine


• Doxorubicin Hydrochloride


• Doxorubicin Hydrochloride Liposome


• Edatrexate


• Eflornithine


• Epirubicin


• Estramustine


• Etanercept


• Etoposide


• Everolimus


• Fingolimod


• Floxuridine


• Fludarabine


• Fluorouracil


• Fotemustine


• Gallium Nitrate


• Gemcitabine


• Golimumab


• Hydroxyurea


• Idarubicin


• Ifosfamide


• Irinotecan


• Lomustine


• Mechlorethamine


• Melphalan


• Mercaptopurine


• Methotrexate


• Mitolactol


• Mitomycin


• Mitotane


• Mitoxantrone


• Mycophenolic Acid


• Oxaliplatin


• Paclitaxel


• Pegaspargase


• Pentostatin


• Pipobroman


• Pirarubicin


• Plicamycin


• Procarbazine


• Raltitrexed


• Rilonacept


• Rituximab


• Sirolimus


• Streptozocin


• Tacrolimus


• Teceleukin


• Tegafur


• Temsirolimus


• Teniposide


• Thioguanine


• Thiotepa


• Topotecan


• Treosulfan


• Trimetrexate


• Trofosfamide


• Uracil Mustard


• Ustekinumab


• Vinblastine


• Vincristine


• Vincristine Liposome


• Vindesine


• Vinorelbine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Abatacept


• Leflunomide

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Fever—Infection may be present and could cause problems

• Immunity problems—BCG treatment is less effective and there is a risk of infection

• Urinary tract infection—Infection and irritation of the bladder may occur

Proper Use of bacillus of calmette and guerin vaccine, live

This section provides information on the proper use of a number of products that contain bacillus of calmette and guerin vaccine, live. It may not be specific to Tice BCG. Please read with care.

Your doctor will ask you to empty your bladder completely before the solution is instilled into it.

Follow your doctor's instructions carefully about how long to hold the solution in your bladder:

• The solution should be held in your bladder for 2 hours. If you think you cannot hold it, tell your health care professional.


• During the first hour, your doctor may have you lie for 15 minutes each on your stomach, back, and each side.


• When you do empty your bladder, you should be sitting down.

It is important that you drink extra fluids for several hours after each treatment with BCG so that you will pass more urine. Also, empty your bladder frequently. This will help prevent bladder problems.

BCG is a live product. In other words, it contains active bacteria that can cause infection. Some bacteria will be present for several hours in urine that you pass after each treatment with BCG. Any urine that you pass during the first 6 hours after each treatment should be disinfected with an equal amount (usually about 1 cup) of undiluted household bleach. After the bleach is added to the urine, it should be allowed to sit for 15 minutes before it is flushed. If you have any questions about this, check with your doctor.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Precautions While Using Tice BCG

While you are being treated with BCG, and for 6 to 12 weeks after you stop treatment with it, avoid contact with people who have tuberculosis. If you think you have been exposed to someone with tuberculosis, tell your doctor.

While you are being treated with BCG and for a few weeks after you stop treatment with it, do not have any immunizations (vaccinations) without your doctor's approval.

Tice BCG Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

More common

• Blood in urine


• fever and chills


• frequent urge to urinate


• increased frequency of urination


• joint pain


• nausea and vomiting


• painful urination (severe or continuing)

Rare

• Cough


• skin rash

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Burning during first urination after treatment

After you stop using this medicine, it may still produce some side effects that need attention. During this period of time, check with your doctor immediately if you notice the following side effects:

• Cough


• fever

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Tice BCG side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Tice BCG resources

• Tice BCG Side Effects (in more detail)
• Tice BCG Use in Pregnancy & Breastfeeding
• Tice BCG Drug Interactions
• Tice BCG Support Group
• 0 Reviews for Tice BCG - Add your own review/rating

Compare Tice BCG with other medications

• Tuberculosis, Prophylaxis
• Urinary Tract Tumors

Cytra-2

Pronunciation: SIH-trik AS-id/SOE-dee-um SIH-trayt
Generic Name: Citric Acid/Sodium Citrate
Brand Name: Examples include Cytra-2 and Oracit

Cytra-2 is used for:

Treating metabolic acidosis and certain kidney problems (eg, kidney stones). It may also be used for other conditions as determined by your doctor.

Cytra-2 is an alkalinizing agent. It works by neutralizing excess acid in the blood and urine.

Do NOT use Cytra-2 if:

• you are allergic to any ingredient in Cytra-2


• you have aluminum toxicity, untreated Addison disease, low or no urine production, high blood potassium, congestive heart failure, heart damage, or severe kidney problems, or if you are dehydrated

Contact your doctor or health care provider right away if any of these apply to you.

Before using Cytra-2:

Some medical conditions may interact with Cytra-2. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you are taking aluminum salts (eg, aluminum hydroxide), amphetamines or lithium


• if you have a history of kidney disease, heart disease, electrolyte/mineral imbalances (eg, high potassium levels), Addison disease, or stomach problems (eg, ulcer disease)


• if you have high blood pressure, a urinary tract infection, or toxemia, or you are on a sodium-restricted diet

Some MEDICINES MAY INTERACT with Cytra-2. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Aluminum salts (eg, aluminum hydroxide) because the risk of severe aluminum toxicity may be increased


• Anorexiants (eg, phentermine) or sympathomimetics (eg, pseudoephedrine) because side effects may be increased by Cytra-2


• Lithium or tetracyclines (eg, doxycycline) because effectiveness may be decreased by Cytra-2

This may not be a complete list of all interactions that may occur. Ask your health care provider if Cytra-2 may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Cytra-2:

Use Cytra-2 as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Cytra-2 after meals and at bedtime, unless directed otherwise by your health care provider.


• Shake well before using.


• Use a measuring device marked for medicine dosing. Ask your pharmacist for help if you are unsure of how to measure your dose.


• Mix Cytra-2 with water before swallowing. Follow with additional water, if desired.


• If you miss a dose of Cytra-2, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Cytra-2.

Important safety information:

• LAB TESTS, including blood electrolyte and bicarbonate levels, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.


• Use Cytra-2 with caution in CHILDREN younger than 2 years of age because they may be more sensitive to its effects.


• PREGNANCY and BREAST-FEEDING: If you become pregnant while taking Cytra-2, discuss with your doctor the benefits and risks of using Cytra-2 during pregnancy. It is unknown if Cytra-2 is excreted in breast milk. If you are or will be breast-feeding while you are using Cytra-2, check with your doctor or pharmacist to discuss the risks to your baby.

Possible side effects of Cytra-2:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Diarrhea; loose stools; nausea; upset stomach; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); black, tarry stools; confusion; severe stomach pain; tingling of hands or feet; vomit that looks like coffee grounds; weakness.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Cytra-2 side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include diarrhea; nausea; seizures; vomiting.

Proper storage of Cytra-2:

Store Cytra-2 at room temperature, between 68 and 77 degrees F (20 and 25 degrees C), in a tightly closed container. Store away from heat, moisture, and light. Do not freeze. Keep Cytra-2 out of the reach of children and away from pets.

General information:

• If you have any questions about Cytra-2, please talk with your doctor, pharmacist, or other health care provider.


• Cytra-2 is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Cytra-2. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Cytra-2 resources

• Cytra-2 Side Effects (in more detail)
• Cytra-2 Use in Pregnancy & Breastfeeding
• Cytra-2 Drug Interactions
• Cytra-2 Support Group
• 0 Reviews for Cytra-2 - Add your own review/rating

• Cytra-2 Concise Consumer Information (Cerner Multum)

Compare Cytra-2 with other medications

• Urinary Alkalinization
• Urinary Tract Stones

Konsyl for Kids

Generic Name: psyllium (SIL ee um)

Brand Names: Fiberall, Genfiber, Hydrocil, Konsyl, Konsyl Orange Sugar-free, Konsyl-D, Konsyl-Orange, Laxmar, Laxmar Orange, Laxmar Sugar Free, Metamucil, Metamucil Berry Burst Smooth Texture Sugar Free, Metamucil Orange Coarse Milled Original Texture, Metamucil Orange Smooth Texture, Metamucil Orange Smooth Texture Sugar Free, Metamucil Unflavored Coarse Milled Original Texture, Metamucil Unflavored Smooth Texture Sugar Free, Natural Fiber Therapy, Perdiem Fiber Powder, Reguloid, V-Lax

What is Konsyl for Kids (psyllium)?

Psyllium is a bulk-forming fiber laxative. Psyllium works by absorbing liquid in the intestines and swelling to create a softer, bulky stool that is easier to pass.

Psyllium is used to treat occasional constipation or bowel irregularity. Psyllium may also be used to treat diarrhea and may help lower cholesterol when used together with a diet low in cholesterol and saturated fat.

Psyllium may also be used for other purposes not listed in this product guide.

What is the most important information I should know about Konsyl for Kids (psyllium)?

Laxatives may be habit-forming if they are used too often or for too long. This can lead to damage of intestinal nerves or muscle tissues. Do not take psyllium for longer than directed on the label or prescribed by your doctor. You should not take this product if you are allergic to psyllium, or if you have trouble swallowing, a sudden change in bowel habits that lasts longer than 2 weeks, severe nausea, vomiting, or stomach pain, or if you have ever had a skin rash while taking psyllium.

Also talk with your doctor before using psyllium if you have a colostomy or ileostomy, rectal bleeding, or a blockage in your intestines.

Stop using psyllium and call your doctor at once if you have choking or trouble swallowing, severe stomach pain or cramping, nausea or vomiting, constipation that lasts longer than 7 days, rectal bleeding, or itchy skin rash. Do not take psyllium for longer than 7 days in a row unless your doctor has told you to.

What should I discuss with my healthcare provider before taking Konsyl for Kids (psyllium)?

Laxatives may be habit-forming if they are used too often or for too long. This can lead to damage of intestinal nerves or muscle tissues. Do not take psyllium for longer than directed on the label or prescribed by your doctor. You should not take this product if you are allergic to psyllium, or if you have:

• 
  

  trouble swallowing;

  
  


• 
  

  a sudden change in bowel habits that lasts longer than 2 weeks;

  
  


• 
  

  severe nausea, vomiting, or stomach pain; or

  
  


• 
  

  if you have ever had a skin rash while taking psyllium.

  
  

If you have certain conditions, you may need a dose adjustment or special tests to safely use this product. Before you take psyllium, tell your doctor if you have:

• 
  

  a colostomy or ileostomy;

  
  


• 
  

  rectal bleeding; or

  
  


• 
  

  a blockage in your intestines.

  
  

Psyllium products may contain sugar, sodium, or artificial sweeteners. This may be of concern to you if you have diabetes, high blood pressure, or phenylketonuria (PKU). Check the product label if you have any of these conditions.

FDA pregnancy category B. Psyllium is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether psyllium passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take Konsyl for Kids (psyllium)?

Use this medication exactly as directed on the label, or as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended. Psyllium is intended to be used for a short time only.

Take psyllium with a full glass (at least 8 ounces) of water or another liquid. Taking psyllium without enough liquid may cause it to swell in your throat and cause choking. Drinking plenty of fluids each day while you are taking psyllium will also help improve bowel regularity.

The psyllium wafer must be chewed before you swallow it.

Do not swallow psyllium powder dry. It must be mixed with liquid. Place the psyllium powder into an empty glass and add at least 8 ounces of water or other liquid such as fruit juice. Stir this mixture and drink all of it right away.

If the powder and liquid mixture is too thick, add more liquid. After drinking the entire mixture, add a little more liquid to the same glass, swirl gently and drink right away to make sure you get the entire dose of psyllium.

Psyllium may be only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

It may take up to 3 days of using this medicine before your symptoms improve. For best results, keep using the medication as directed. Talk with your doctor if your symptoms do not improve after 2 or 3 days of treatment.

Do not take psyllium for longer than 7 days in a row unless your doctor has told you to. Store psyllium at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include nausea, vomiting, and stomach pain. Using a laxative too often or for too long may cause severe medical problems involving your intestines.

What should I avoid while taking Konsyl for Kids (psyllium)?

Avoid taking other oral (by mouth) medications within 2 hours before or after you take psyllium. Bulk-forming laxatives can make it harder for your body to absorb other medications, possibly making them less effective.

Avoid breathing in the dust from psyllium powder when mixing. Inhaling psyllium dust may cause an allergic reaction.

If you take psyllium as part of a cholesterol-lowering treatment plan, avoid eating foods that are high in fat or cholesterol. Your treatment will not be as effective in lowering your cholesterol if you do not follow a cholesterol-lowering diet plan.

Konsyl for Kids (psyllium) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using psyllium and call your doctor at once if you have a serious side effect such as:

• 
  

  choking or trouble swallowing;

  
  


• 
  

  severe stomach pain, cramping, nausea or vomiting;

  
  


• 
  

  constipation that lasts longer than 7 days;

  
  


• 
  

  rectal bleeding; or

  
  


• 
  

  itchy skin rash.

  
  

Less serious side effects may include:

• 
  

  bloating; or

  
  


• 
  

  minor change in your bowel habits.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Konsyl for Kids (psyllium)?

Tell your doctor about all other medications you use, especially:

• 
  

  a blood thinner such as warfarin (Coumadin); or

  
  


• 
  

  demeclocycline (Declomycin), doxycycline (Adoxa, Doryx, Oracea, Vibramycin), minocycline (Dynacin, Minocin, Solodyn, Vectrin), or tetracycline (Brodspec, Panmycin, Sumycin, Tetracap).

  
  

This list is not complete and there may be other drugs that can interact with psyllium. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

More Konsyl for Kids resources

• Konsyl for Kids Side Effects (in more detail)
• Konsyl for Kids Use in Pregnancy & Breastfeeding
• Konsyl for Kids Drug Interactions
• 0 Reviews for Konsyl for Kids - Add your own review/rating

• Konsyl Powder MedFacts Consumer Leaflet (Wolters Kluwer)


• Metamucil MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Konsyl for Kids with other medications

• Constipation
• Dietary Fiber Supplementation
• Irritable Bowel Syndrome

Where can I get more information?

• Your pharmacist can provide more information about psyllium.

See also: Konsyl for Kids side effects (in more detail)