VA Class:AH104

ATC Class:R06AX07

AHFS Class:

• First Generation Antihistamines 4:04

Generic Name(s):

• Triprolidine Hydrochloride

• Triprolidine and Pseudoephedrine Hydrochlorides

Associated Monographs

• Antihistamines General Statement

Triprolidine is an alkylamine-derivative, first generation antihistamine.

Triprolidine shares the actions and uses of other antihistamines.

Administration

Triprolidine hydrochloride preparations are administered orally.101,102,103,104

Dosage

Dosage of triprolidine hydrochloride should be individualized according to the patient's response and tolerance.

When triprolidine hydrochloride is used in fixed combination with pseudoephedrine hydrochloride, dosage recommendations for adults and children are the same as when the drug is used as a single agent.

For self-medication in adults and children 12 years of age and older, the usual dosage of triprolidine hydrochloride is 2.5 mg every 4-6 hours, not to exceed 10 mg in 24 hours.103,104,105 For self-medication in children 6 to younger than 12 years of age, the usual dosage is 1.25 mg every 4-6 hours, not to exceed 5 mg in 24 hours.103,104,105 Therapy should be discontinued if symptoms persist for more than 7 days or are accompanied by fever.105

Under the direction of a physician, children 4 to younger than 6 years of age may receive 0.938 mg every 4-6 hours, not to exceed 3.744 mg in 24 hours; children 2 to younger than 4 years of age may receive 0.625 mg every 4-6 hours, not to exceed 2.5 mg in 24 hours; and children 4 months to younger than 2 years of age may receive 0.313 mg every 4-6 hours, not to exceed 1.252 mg in 24 hours.101 (See Cautions: Pediatric Precautions.)

For further information on chemistry, pharmacology, pharmacokinetics, uses, cautions, acute toxicity, drug interactions, laboratory test interferences, and dosage and administration of triprolidine, see the Antihistamines General Statement 4:00.

Triprolidine shares the toxic potentials of other antihistamines, and the usual precautions of antihistamine therapy should be observed. (See Cautions in the Antihistamines General Statement 4:00.) When fixed combinations containing triprolidine hydrochloride and pseudoephedrine hydrochloride and/or other drugs are used, the precautions and contraindications associated with other drugs in the combination also must be considered.103,104,105

Pediatric Precautions

Like other antihistamines, triprolidine should be used with caution in infants and young children and should not be used in premature or full-term neonates. (See Cautions: CNS Effects and Pediatric Precautions, in the Antihistamines General Statement 4:00.) Use of the drug in children younger than 4 months of age is not recommended. Children younger than 6 years of age should receive triprolidine only under the direction of a clinician.

Overdosage and toxicity (including death) have been reported in children younger than 2 years of age receiving preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. There is limited evidence of efficacy for these preparations in this age group, and appropriate dosages (i.e., approved by the US Food and Drug Administration [FDA]) for the symptomatic treatment of cold and cough have not been established. Therefore, FDA stated that nonprescription cough and cold preparations should not be used in children younger than 2 years of a the agency continues to assess safety and efficacy of these preparations in older children. Meanwhile, 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 younger than 4 years of age. FDA recommends that parents and caregivers adhere to the dosage instructions and warnings on the product labeling that accompanies the preparation if administering to children and consult with their clinician about any concerns. Clinicians should ask caregivers about use of nonprescription cough and cold preparations to avoid overdosage. For additional information on precautions associated with the use of cough and cold preparations in pediatric patients, see Cautions: Pediatric Precautions in the Antihistamines General Statement 4:00.

Geriatric Precautions

Geriatric patients (60 years of age and older) may be particularly susceptible to dizziness, sedation, and hypotension.102

Mutagenicity and Carcinogenicity

Studies to determine the mutagenic and carcinogenic potentials of triprolidine have not been performed to date.

Pregnancy, Fertility, and Lactation

Pregnancy

There is inadequate experience with use of triprolidine in pregnant women to determine whether the potential for harm to the fetus exists. Reproduction studies in rats and rabbits using dosages up to 70 times the usual human dosage of the fixed-dose combination of triprolidine and pseudoephedrine (Actifed^®) have not revealed evidence of harm to the fetus. In an epidemiologic study in pregnant women, there was no evidence of increased risk of teratogenicity associated with use of triprolidine in fixed combination with pseudoephedrine during the first trimester, although a modest association could not be ruled out. There are no adequate and controlled studies to date using triprolidine in pregnant women, and the drug should be used during pregnancy only when clearly needed.

Fertility

Reproduction studies in rats and rabbits using dosages up to 70 times the usual human dosage of the fixed-dose combination of triprolidine and pseudoephedrine (Actifed^®) have not revealed evidence of impaired fertility

Lactation

Triprolidine is distributed into milk.106 Because of the potential for serious adverse reactions to antihistamines in nursing infants, some manufacturers state that a decision should be made whether to discontinue nursing or triprolidine, taking into account the importance of the drug to the woman.101,102 However, the American Academy of Pediatrics (AAP) considers triprolidine to be compatible with breast-feeding.106

Chemistry and Stability

Chemistry

Triprolidine is an alkylamine-derivative antihistamine. Triprolidine hydrochloride occurs as a white, crystalline powder with no more than a slight but unpleasant odor. The drug has solubilities of approximately 476 mg/mL in water and 556 mg/mL in alcohol at 25°C. Triprolidine has pK_as of 3.6 and 9.3.

Stability

Preparations containing triprolidine hydrochloride should be stored in tight, light-resistant containers at 15-30°C in a dry place;101,102,105 freezing of oral solutions should be avoided.

Please see the general statement for a list of references.