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Triprolidine

Class: First Generation Antihistamines
ATC Class: R06AX07
VA Class: AH104
CAS Number: 6138-79-0
Brands: Zymine Liquid

Medically reviewed by Drugs.com on Oct 4, 2021. Written by ASHP.

Introduction

First generation antihistamine; an alkylamine derivative.

Uses for Triprolidine

Allergic and Nonallergic Rhinitis

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

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.

Allergic Conjunctivitis

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

Allergic Skin Disorders

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

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.

Triprolidine Dosage and Administration

Administration

Oral Administration

Administer orally as tablets or oral solution.

Dosage

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

Individualize dosage according to patient’s response and tolerance.

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.

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. (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.

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.

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.

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.

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.

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.

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.

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.

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.

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

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

Allergic Rhinitis and Allergic Conjunctivitis

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

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

Common Cold
Oral

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

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

Adults

Allergic Conditions
Allergic Rhinitis and Allergic Conjunctivitis
Oral

Self-medication: Maximum 10 mg in 24 hours.

Common Cold
Oral

Self-medication: Maximum 10 mg in 24 hours.

Cautions for Triprolidine

Contraindications

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

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

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

  • Patients with asthmatic attacks.

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

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.

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

CNS Effects

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

Possible excitability (especially in children). (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.

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.

Specific Populations

Pregnancy

Category C.

Lactation

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

Pediatric Use

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

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

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

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 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 agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 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.

Common Adverse Effects

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

Interactions for Triprolidine

Specific Drugs and Laboratory Tests

Drug or Laboratory Test

Interaction

Comments

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

Possible additive CNS depression

Tricyclic antidepressants prolong and intensify anticholinergic effects of antihistamines

Avoid concomitant use

MAO inhibitors

MAO inhibitors prolong and intensify anticholinergic effects of antihistamines

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

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 Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed.

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

Distribution

Extent

Distributed into milk. (See Lactation under Cautions.)

Elimination

Half-life

3–3.3 hours.

Stability

Storage

Oral

Tablets

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

Solution

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

Actions

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

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

  • Has anticholinergic and sedative effects.

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

Advice to Patients

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

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

  • 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. 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.

  • 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.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* 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 2022, Selected Revisions October 13, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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