Triprolidine (Monograph)

Brand name: Zymine Liquid
Drug class: First Generation Antihistamines

Medically reviewed by Drugs.com on Oct 3, 2023. Written by ASHP.

Introduction

First generation antihistamine; an alkylamine derivative.^a

Uses for Triprolidine

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}

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 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 m o} (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 m o}

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 m o}

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 m o}

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 m o}

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 m o}

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 m o}

Children 2 to <4 years of age: Maximum 2.5 mg in 24 hours.^{101 m o}

Children 4 to <6 years of age: Maximum 3.75 mg in 24 hours.^{101 m o}

Allergic Rhinitis and Allergic Conjunctivitis

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

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

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 m o}

Common Cold

Oral

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

Cautions for Triprolidine

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.^c Children <6 years of age should receive triprolidine only under the direction of a clinician.^{103 104 c}

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.^{r s} Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.^r Therefore, FDA recommended not to use such preparations in children <2 years of age;^t safety and efficacy in older children under evaluation.^{v x} 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.^{u v w x} 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.^{u v w} Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.^r

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

Drug Interactions

Specific Drugs and Laboratory Tests

Triprolidine 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.^{m n p q}

• 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.

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

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

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