Talk:Tripelennamine

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promethazine & codeine

The article mentions that promethazine increases codeine->morphine in liver. Codeine is converted into morphine via CYP2D6. Promethazine is an inhibitor of CYD2D6. I do not think that promethazine increases metabolism of codeine into morphine, if anything I think it would decrease that metabolic route. — Preceding unsigned comment added by 27.99.8.126 (talk) 05:44, 30 March 2016 (UTC)[reply]

recreational use section

per its tags, moving here til this can be cleaned of OR and reliably sourced

Recreational use

Tripelennamine by itself is a primary euphoriant manifesting anxiolytic, sedative, dopaminergic, and quasi-tricyclic-anti-depressant actions;[

benztropine, cyclobenzaprine
, etc. produce a characteristic mild to moderate euphoria by this mechanism, and alkylamines have elements of both. The relatively rapid onset of action by any route of administration is also part of the appeal.

Tripelennamine is used also for its tranquillizing effects, which are stronger than those of its close chemical relative

pyrilamine,[medical citation needed
] which is used in OTC day-time sedatives such as Compoz in many countries.

The most common recreational use of tripelennamine is as a potentiator of narcotic analgesics. It both strengthens the opioid effects overall and changes the side effect profile of the drug in question by adding warmth and other qualities.[

chlorpheniramine
. The above list includes drugs from all five major families of first-generation antihistamines, which attain a similar objective by somewhat differing means.

Tripelennamine is sometimes abused recreationally in combination with the benzomorphan class synthetic opioid pentazocine (Fortral, Talacen, Talwin) in a mixture known as "T's & Blues",[1] or morphine ("Blue Velvet"), by preparing an injection containing both agents; heroin may also be used like this. The local anesthetic effects of the antihistamine manifest in the case of intramuscular and subcutaneous injections. The US manufacturers of Talwin began adding naloxone to the tablets in the late 1970s as the practice of Ts and Blues spread—injecting a solution made from the pills delivers the antagonist which does not enter the system in significant amounts if the pills are swallowed. This changed the name of the product in question to Talwin NX. Talwin PX, available in Canada, and some other US versions as well as a large majority of pentazocine used in other countries does not contain the antagonist.

Tripelennamine is also used orally with the aforementioned drugs as well as paregoric, opium in all its forms including powdered opium and DTO (laudanum), narcotic cough syrups containing codeine and its derivatives, and analgesic preparations containing opioids with much the same impact, albeit taking longer to develop etc.

This use of tripelennamine with mixed

agonist–antagonist opioids such as pentazocine, phenazocine, dezocine, butorphanol (Stadol), buprenorphine (Temgesic, Subutex), nalbuphine (Nubain) and others has results that make it appear that the antihistamine changes the receptor-activation profile of these drugs in a way that makes them more euphoric, but it is unknown if tripelennamine operates in this way in a true, literal sense or if increased dopamine levels counteract the dysphoric action of antagonists and drugs affecting the kappa opioid receptor in particular, and to an unclear extent pure agonists with dysphoria-inducing metabolites such as pethidine (Dolantin, Demerol) and its relatives. The relatively small degree of additive anticholinergic action make non-parenteral analogues of Blue Velvet using opium-belladonna combinations feasible and all the more euphoric. Tripelennamine and drugs of the same type of course do not counteract the effects of the naloxone
which is added to pentazocine tablets in some countries to discourage injection.

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

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.

Like many of the first-generation antihistamines of the ethanolamine and alkylamine classes, tripelennamine and other members of its chemical class (ethylenediamines) produces a marginal to moderate euphoria; triepelennamine has a euphoriant effect with a relatively rapid onset and up to eight hours in duration.

The euphoric effect of tripelennamine makes these combinations more than the sum of their parts, and it is qualitatively and quantitatively different from that of the ethanolamine antihistamines such as

chlorpheniramine (Chlor-Trimeton), and dexchlorpheniramine (Polaramine), are therefore in between the ethanolamines and the ethylenediamines in this respect. Anticholinergics change the dopamine to acetylcholine ratio in the CNS, whereas this is much less prominent with tripelennamine, which causes an increase in the absolute levels of dopamine by means of reuptake inhibition without a lot of effect on acetylcholine. The opioid-potentiating effects of other antihistamines such as hydroxyzine, cyclizine
etc. appear to be directly due to additive sedation, and promethazine also has metabolic effects on codeine and the like, namely increasing the percentage of codeine that the liver converts to morphine in most people.

References

  1. PMID 1600804.{{cite journal}}: CS1 maint: multiple names: authors list (link
    )

- Jytdog (talk) 23:30, 3 April 2016 (UTC)[reply]

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