Tripelennamine

Medical uses

Where and when it is/was in common use, tripelennamine is used much like other mildly-anticholinergic antihistamines to treat conditions of the upper respiratory tract arising from illnesses and hay fever. It can be used alone or in combination with other agents to have the desired effect. Cough medicines of the general formula tripelennamine + codeine/dihydrocodine/hydrocodone ± expectorant ± decongestant(s) are popular where available. Among these are the Pyribenzamine cough syrups which contain codeine, with and without decongestants, listed in the 1978 Physicians' Desk Reference; the codeine-tripelennamine synergy is well-known and makes such mixtures more useful for their intended purposes.

Side effects

Tripelennamine is mildly sedating. Other side effects can include irritation, dry mouth, nausea, and dizziness.

Pharmacology

Pharmacodynamics

Tripelennamine acts primarily as an antihistamine, or H1 receptor antagonist. It has little to no anticholinergic activity, with 180-fold selectivity for the H1 receptor over the muscarinic acetylcholine receptors (for comparison, diphenhydramine had 20-fold selectivity for the H1 receptor). In addition to its antihistamine properties, tripelennamine also acts as a weak serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).

Pharmacokinetics

The elimination half-life of tripelennamine is 4 to 6 hours. In a clinical study, the half-life of tripelennamine following intramuscular injection of 50 to 100 mg was 2.9 to 4.4 hours.

History

Tripelennamine was patented in 1946 by Carl Djerassi and colleagues, working at CIBA in New Jersey.

Society and culture

Availability

Tripelennamine is available in the United States under the brand name PBZ OTC.

References

References

1. (2006). "Goldfrank's toxicologic emergencies". McGraw-Hill Professional.
2. (March 1987). "Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay". Jpn J Pharmacol.
3. (February 1994). "Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain". Naunyn-Schmiedeberg's Archives of Pharmacology.
4. (May 1996). "Potentiation of L-dopa-induced behavioral excitement by histamine H1-receptor antagonists in mice". Japanese Journal of Pharmacology.
5. (September 1999). "Effects of antihistamines on 3, 4-methylenedioxymethamphetamine-induced depletion of serotonin in rats". Synapse.
6. (June 1986). "The pharmacokinetics of pentazocine and tripelennamine". Clin Pharmacol Ther.
7. (April 2003). "Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view". Curr Drug Metab.
8. (1999). "Pharmaceutical Innovation: Revolutionizing Human Health". Chemical Heritage Foundation.
9. https://pbzotc.com/