Prevent an allergic reaction from happening at school.

Triprolidine Hydrochloride

Class: First Generation Antihistamines
ATC Class: R06AX07
VA Class: AH104
CAS Number: 6138-79-0
Brands: Allerfrim Syrup, Aprodine, Zymine Liquid, Zymine-D Liquid

Introduction

First generation antihistamine; an alkylamine derivative.a

Uses for Triprolidine Hydrochloride

Allergic and Nonallergic Rhinitis

Symptomatic relief of seasonal (e.g., hay fever) or perennial (nonseasonal) allergic rhinitis or nonallergic (vasomotor) rhinitis.101 102

Used in fixed combination with other agents (e.g., pseudoephedrine) for symptomatic relief of rhinorrhea, sneezing, oronasopharyngeal itching, lacrimation, itching eyes, and/or other symptoms (e.g., sinus congestion) associated with seasonal or perennial allergic rhinitis or nonallergic rhinitis.102 103 104 105

Slideshow: Top Prevention Tips - Springtime Allergies

Allergic Conjunctivitis

Symptomatic relief of allergic conjunctivitis caused by foods or inhaled allergens.101

Allergic Skin Disorders

Symptomatic treatment of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.101

Common Cold

Used in fixed combination with other agents (e.g., pseudoephedrine) for self-medication for symptomatic relief of sinus congestion and other symptoms associated with the common cold.103 104

Triprolidine Hydrochloride Dosage and Administration

Administration

Oral Administration

Administer orally as tablets or oral solution.101 102 103 104 a

Dosage

Available as triprolidine hydrochloride; dosage expressed in terms of the salt.101 102 103 104

Individualize dosage according to patient’s response and tolerance.a b

Fixed-combination preparations do not permit individual titration of dosages. When used in fixed combination with other agents (e.g., pseudoephedrine), select a dosage that is within the usual therapeutic range for each ingredient; dosage recommendations of triprolidine hydrochloride for adults and children when administered in fixed combinations are the same as when the drug is used as a single agent.a

Pediatric Patients

Allergic Conditions
Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, and Allergic Skin Disorders
Oral

Children 4 months to <2 years of age: 0.313 mg every 4–6 hours (as oral solution), not to exceed 1.252 mg in 24 hours.101 (See Pediatric Use Under Cautions.)

Children 2 to <4 years of age: 0.625 mg every 4–6 hours (as oral solution), not to exceed 2.5 mg in 24 hours.101

Children 4 to <6 years of age: 0.938 mg every 4–6 hours (as oral solution), not to exceed 3.75 mg in 24 hours.101

Allergic Rhinitis and Allergic Conjunctivitis

Self-medication in children 6 to <12 years of age: 1.25 mg every 4–6 hours (as tablets or oral solution), not to exceed 5 mg in 24 hours.103 104 105

Self-medication in children ≥12 years of age: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104 105

Common Cold
Oral

Self-medication in children 6 to <12 years of age: 1.25 mg every 4–6 hours (as tablets or oral solution), not to exceed 5 mg in 24 hours.103 104

Self-medication in children ≥12 years of age: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104

Adults

Allergic Conditions
Allergic Rhinitis and Allergic Conjunctivitis
Oral

Self-medication: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104 105

Common Cold
Oral

Self-medication: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104

Prescribing Limits

Pediatric Patients

Allergic Conditions
Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, and Allergic Skin Disorders
Oral

Children 4 months to <2 years of age: Maximum 1.252 mg in 24 hours.101

Children 2 to <4 years of age: Maximum 2.5 mg in 24 hours.101

Children 4 to <6 years of age: Maximum 3.75 mg in 24 hours.101

Allergic Rhinitis and Allergic Conjunctivitis

Self-medication in children 6 to <12 years of age: Maximum 5 mg in 24 hours.103 104 105

Self-medication in children ≥12 years of age: Maximum 10 mg in 24 hours.103 104 105

Common Cold
Oral

Self-medication in children 6 to <12 years of age: Maximum 5 mg in 24 hours.103 104

Self-medication in children ≥12 years of age: Maximum 10 mg in 24 hours.103 104

Adults

Allergic Conditions
Allergic Rhinitis and Allergic Conjunctivitis
Oral

Self-medication: Maximum 10 mg in 24 hours.105

Common Cold
Oral

Self-medication: Maximum 10 mg in 24 hours.103 104

Cautions for Triprolidine Hydrochloride

Contraindications

  • Use contraindicated in neonates and premature infants.102 a b (See Pediatric Use under Cautions.)

  • Women who are breast-feeding.102 (See Lactation under Cautions.)

  • Patients receiving MAO inhibitor therapy.102 (See Interactions.)

  • Patients with asthmatic attacks.b

  • Known hypersensitivity to triprolidine or any ingredient in the formulation.101 102

Warnings/Precautions

Warnings

Concomitant Diseases

Because of anticholinergic effects, use with extreme caution in patients with angle-closure glaucoma, pyloroduodenal obstruction, bladder-neck obstruction, and symptomatic prostatic hypertrophy.101 102 b

Use with extreme caution in patients with a history of bronchial asthma, increased IOP, hyperthyroidism, or cardiovascular disease (e.g., hypertension).101 102 b

CNS Effects

Risk of drowsiness.102 105 (See CNS Depressants under Interactions and also see Advice to Patients.)

Possible excitability (especially in children).105 (See Pediatric Use under Cautions.)

General Precautions

Use of Fixed Combinations

When used in fixed combination with other agents (e.g., pseudoephedrine), consider the cautions, precautions, and contraindications associated with all ingredients in the formulation.103 104 105 a

Duration of Therapy

When used for self-medication, discontinue therapy and consult a clinician if symptoms persist for >7 days or are accompanied by fever.105

Specific Populations

Pregnancy

Category C.101 102 106

Lactation

Distributed into milk.106 Some manufacturers suggest discontinuing nursing or the drug because of potential risk to nursing infants.101 102 a However, AAP considers triprolidine compatible with breast-feeding.106

Pediatric Use

Use not recommended in premature or full-term neonates.a b (See Contraindications.)

Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in children.b

Use in children <4 months of age not recommended. Children <6 years of age should receive triprolidine only under the direction of a clinician.103 104

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. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. 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 OTC cough/cold preparations to avoid overdosage.

Geriatric Use

Possible increased risk of dizziness, sedation, and hypotension in geriatric patients ≥60 years of age.102 b

Common Adverse Effects

Drowsiness,101 dry mouth,101 anorexia,101 nausea,101 vomiting,101 headache,101 dizziness,101 102 nervousness,101 blurred vision,101 polyuria,101 heartburn,101 dysuria,101 urinary retention.101

Interactions for Triprolidine Hydrochloride

Specific Drugs and Laboratory Tests

Drug or Laboratory Test

Interaction

Comments

CNS depressants (e.g., alcohol, hypnotics, sedatives, tranquilizers, tricyclic antidepressants)

Possible additive CNS depression101 102 105 b

Tricyclic antidepressants prolong and intensify anticholinergic effects of antihistamines101

Avoid concomitant use102 105

MAO inhibitors

MAO inhibitors prolong and intensify anticholinergic effects of antihistamines101 102 b

Avoid use with or for 2 weeks after discontinuance of MAO inhibitors105

Test, antigen or histamine

Inhalation-challenge testing with histamine or antigen: Possible suppression of test response

Antigen skin testing: Possible suppression of wheal and flare reactions

Triprolidine Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed.102

Therapeutic concentration achieved rapidly and usually maintained for 4–8 hours.102

Distribution

Extent

Distributed into milk.106 (See Lactation under Cautions.)

Elimination

Half-life

3–3.3 hours.101 102

Stability

Storage

Oral

Tablets

Tight, light-resistant containers at 15–30°C in a dry place.a

Solution

Tight, light-resistant containers at 15–30°C in a dry place;101 102 105 a do not freeze.a

Actions

  • Blocks H1-receptor sites, thereby preventing the action of histamine on the cell.101 102 b

  • Suppresses flare and pruritus that accompany the endogenous release of histamine.b

  • Has anticholinergic and sedative effects.102

  • Antihistamines do not block the stimulating effect of histamine on gastric acid secretion, which is mediated by H2-receptors of the parietal cells.b

Advice to Patients

  • Risk of drowsiness; avoid alcohol and use caution when driving or operating machinery.102 105

  • When used for self-medication, discontinue therapy and consult a clinician if symptoms persist for >7 days or are accompanied by fever.105

  • 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.101 102 Importance of patients already receiving another CNS depressant (e.g., sedative, tranquilizer) not undertaking self-medication without first consulting a clinician.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.101 102

  • Importance of informing patients of other important precautionary information.101 102 (See Cautions.)

Preparations

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

Many prescription cough, cold, and allergy preparations commercially available in the US have not been approved by the US Food and Drug Administration (FDA).500 Because of the potentially serious health risks associated with unapproved preparations, FDA announced on March 3, 2011, that it would take enforcement action (e.g., seizure, injunction, other judicial or administrative proceeding) against any currently marketed and listed unapproved cough, cold, and allergy preparation manufactured on or after June 1, 2011, or shipped on or after August 30, 2011.500 For additional information and for a complete list of unapproved cough, cold, and allergy preparations affected by this FDA notice, see FDA website ().

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Triprolidine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

1.25 mg/5 mL*

Triprolidine Hydrochloride Solution

Zymine Liquid

Vindex

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Triprolidine and Pseudoephedrine Hydrochlorides

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

1.25 mg/5 mL Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 30 mg/5 mL*

Allerfrim Syrup

Rugby

Triprolidine and Pseudoephedrine Hydrochlorides Solution

1.25 mg/5 mL Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 45 mg/5 mL*

Triprolidine and Pseudoephedrine Hydrochlorides Solution

Zymine-D Liquid

Vindex

Tablets

2.5 mg Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 60 mg*

Allerfrim

Rugby

Aprodine

Major

Triprolidine and Pseudoephedrine Hydrochlorides Tablets

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 1, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

101. Vindex Pharmaceuticals, Inc. Zymine (triprolidine hydrochloride) liquid prescribing information. Memphis, TN; 2005 Jul.

102. Vindex Pharmaceuticals, Inc. Zymine-D (triprolidine hydrochloride and pseudoephedrine hydrochloride) liquid prescribing information. Memphis, TN; 2005 Jul.

103. Major Pharmaceuticals. Aprodine (triprolidine hydrochloride and pseudoephedrine hydrochloride ) syrup product information. Livonia, MI. From Major Pharmaceutical website (). Accessed 2008 Jan 31.

104. Major Pharmaceuticals. Aprodine (triprolidine hydrochloride and pseudoephedrine hydrochloride ) tablets product information. Livonia, MI. From Major Pharmaceutical website (). Accessed 2008 Jan 31.

105. Rugby. Allerfrim (triprolidine hydrochloride and pseudoephedrine hydrochloride) syrup product information. Duluth, GA; 2004 Jul.

106. Triprolidine. In: Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:1639-40.

500. Food and Drug Administration. Drugs for human use; unapproved and misbranded oral drugs labeled for prescription use and offered for relief of symptoms of cold, cough, or allergy, enforcement action dates. Notice. [Docket No. FDA-2011-N-0100] Fed Regist. 2011; 76:11794-8.

a. AHFS Drug Information 2008. McEvoy GK, ed. Triprolidine Hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2008:24.

b. AHFS Drug Information 2008. McEvoy GK, ed. Antihistamines General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008:1-8.

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