Meperidine is a synthetic opioid pain medication of the phenylpiperidine class.
Pethidine is indicated for the treatment of moderate to severe pain, and is delivered as a hydrochloride salt in tablets, as a syrup, or by intramuscular, subcutaneous, or intravenous injection.
Due to its toxic metabolite, it is more toxic than other opioids, especially during long-term use.
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TL;DR SYNTHESiS
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PHARMACOKINETICS
Meperidine is quickly hydrolysed in the liver to pethidinic acid and is also demethylated to norpethidine, which has half the analgesic activity of pethidine but a longer elimination half-life (8–12 hours). Accumulating with regular administration, or in kidney failure. Norpethidine is toxic and has convulsant and hallucinogenic effects.
The toxic effects mediated by the metabolites cannot be countered with opioid receptor antagonists such as naloxone or naltrexone, and are probably primarily due to norpethidine’s anticholinergic activity probably due to its structural similarity to atropine, though its pharmacology has not been thoroughly explored.
The neurotoxicity of pethidine’s metabolites is a unique feature of pethidine compared to other opioids. Pethidine’s metabolites are further conjugated with glucuronic acid and excreted into the urine.
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