Pyribenzamine

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Tripelennamine
Systematic (IUPAC) name
N-benzyl-N',N'-dimethyl-N- pyridin-2-yl-ethane-1,2-diamine
Identifiers
CAS number 91-81-6 154-69-8 (monohydrochloride)
22306-05-4 (hydrochloride)
57116-36-6 (maleate)
6138-56-3 (citrate)
ATC code D04AA04 R06AC04
PubChem 5587
DrugBank APRD00689
Chemical data
Formula C16H21N3 
Mol. mass 255.358 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic hydroxylation and glucuronidation
Half life  ?
Excretion Renal
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

Tripelennamine (INN, also known as pyribenzamine) is a first generation pyridine antipruritic and antihistamine in the ethylenediamine class. It can be used in the treatment of asthma, hay fever, rhinitus and urticaria but is now less common as it has been replaced by newer antihistamines. This drug is sold in 50 mg tablets, which are usually green in colour. Tripellenamine is marketed by Novartis under the trade name Pyribenzamine.

Tripelennamine was first synthesized by Carl Djerassi, working in the laboratory of Charles Huttrer at Ciba, shortly after Djerassi got his BS. It was his first patent.

Side effects

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

Recreational use

Tripelennamine is sometimes abused recreationally in combination with the opiate pentazocine ("T's & Blues"), morphine ("Blue Velvet") and narcotic cough syrups. It is dangerous to combine an opiate with a sedating antihistamine via injection, although the use of antihistamines (usually by mouth) to reduce opioid requirements for pain relief is a well-known practice, which is done under medical supervision with tripelennamine, as well as hydroxyzine, cyclizine, promethazine, diphenhydramine, phenindamine, orphenadrine, meclizine, chlorpheniramine, cyproheptadine and others; this method is doubly useful when used with opioids which release a great deal of histamine when administered and therefore cause itching, redness of skin and other histamine-related effects.

Wikipedia content modification information:

  • This page was last modified on 5 June 2008, at 12:04.

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