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| Clinical data | |
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| Trade names | Pyribenzamine |
| AHFS/Drugs.com | Multum Consumer Information |
| MedlinePlus | a601044 |
| Routes of administration | Oral,intravenous |
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| Pharmacokinetic data | |
| Metabolism | Hepatichydroxylation andglucuronidation |
| Eliminationhalf-life | 4–6 hours[1] |
| Excretion | Renal |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.001.910 |
| Chemical and physical data | |
| Formula | C16H21N3 |
| Molar mass | 255.365 g·mol−1 |
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Tripelennamine, sold under the brand namePyribenzamine byNovartis, is a drug that is used as anantipruritic andfirst-generationantihistamine. It can be used in the treatment ofasthma,hay fever,rhinitis, andurticaria, but is now less common as it has been replaced by newer antihistamines. The drug was patented at CIBA, which merged with Geigy into Ciba-Geigy, and eventually becoming Novartis.
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 1978Physicians' Desk Reference; the codeine-tripelennamine synergy is well-known and makes such mixtures more useful for their intended purposes.
Tripelennamine is mildlysedating. Other side effects can include irritation,dry mouth,nausea, anddizziness.
Tripelennamine acts primarily as anantihistamine, orH1receptorantagonist. It has little to noanticholinergic activity, with 180-foldselectivity for the H1 receptor over themuscarinic acetylcholine receptors (for comparison,diphenhydramine had 20-fold selectivity for the H1 receptor).[2] In addition to its antihistamine properties, tripelennamine also acts as a weakserotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[3][4][5]
Theelimination half-life of tripelennamine is 4 to 6 hours.[1] In a clinical study, the half-life of tripelennamine followingintramuscular injection of 50 to 100 mg was 2.9 to 4.4 hours.[6][7]
Tripelennamine was patented in 1946 byCarl Djerassi and colleagues, working atCIBA in New Jersey.[8]
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Tripelennamine is available in theUnited States under the brand name PBZ OTC.[9]
