MedlinePlus a601044 Molar mass 255.358 g/mol | Routes of
administration Oral, Intravenous CAS ID 91-81-6 | |
 | ||
AHFS/Drugs.com Multum Consumer Information ATC code D04AA04 (WHO) R06AC04 (WHO) Legal status In general: ℞ (Prescription only) Metabolism | ||
Tripelennamine (sold as Pyribenzamine by Novartis) is a drug that is used as an antipruritic and first-generation antihistamine. It can be used in the treatment of asthma, hay fever, rhinitis and urticaria, but is now less common as it has been replaced by newer antihistamines.
Contents
Medical uses
Where and when it is/was in common use, tripelennamine is used much like other mildly-anticholinergic antihistamines for treating 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 medicine of the general formula tripelennamine + codeine/dihydrocodine/hydrocodone ± expectorant ± decongestant(s) is quite popular where available. One example is the line of Pyribenzamine Cough Syrups which contains codeine and with and without decongestants listed in the 1978 Physicians' Desk Reference; the codeine-tripelennamine synergy is well-known and does make 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
Tripelennamine acts primarily as an antihistamine, or H1 receptor antagonist. It has little to no anticholinergic activity. In addition to its antihistamine properties, tripelennamine also acts as a weak serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). Because of its SRI properties, tripelennamine was used as the basis for the development of the selective serotonin reuptake inhibitor (SSRI) fluvoxamine (Luvox).
History
Tripelennamine was first synthesized in 1946 by Carl Djerassi, working in the laboratory of Charles Huttrer at Ciba, shortly after Djerassi got his B.S. It was his first patent.