Pethidine

Pethidine
ATC Code N02AB02
Formula C15H21NO2
Molar Mass (g·mol−1) 247,33
Physical State solid
Melting Point (°C) 30
PKS Value 8,59
CAS Number 57-42-1
PUB Number 4058
Drugbank ID DB00454
Solubility soluble in water (hydrochloride)

Basics

Pethidine is a synthetic opioid analgesic of the phenylpiperidine class. Pethidine is the prototype of a large family of analgesics that also includes, for example, fentanyl. Pethidine is indicated for the treatment of moderate to severe pain and is administered as a hydrochloride salt in tablets, as a syrup or by intramuscular, subcutaneous or intravenous injection.

Pharmacology

Pharmadynamics

Like morphine, pethidine exerts its analgesic effects by acting as an agonist at the μ-opioid receptor. Pethidine has structural similarities to atropine and other tropane alkaloids and may have some of their effects and side effects. In addition to these opioidergic and anticholinergic effects, it has a local anesthetic effect related to its interactions with sodium ion channels.

Pharmacokinetics

Pethidine is rapidly hydrolyzed in the liver to pethidic acid and also demethylated to norpethidine, which has half the analgesic activity of pethidine but a longer elimination half-life; it accumulates with regular administration or with decreased renal function. The metabolites of pethidine are further conjugated with glucuronic acid and excreted in the urine.

Toxicity

Side Effects

The adverse effects of pethidine are primarily those of opioids as a class: nausea, vomiting, dizziness, diaphoresis, urinary retention, and constipation. Because of the moderate stimulant effects mediated by dopamine and norepinephrine, sedation is less likely compared to other opioids. Unlike other opioids, it does not cause miosis due to its anticholinergic properties.

Overdose may cause muscle flaccidity, respiratory depression, obtundation, cold and clammy skin, hypotension, and coma.

Toxicological data

LD50 (rat, oral): 162 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017

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All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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