Pethidine
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| PsychonautWiki | TripSit | Pharmacology | DrugCentral | ||
|---|---|---|---|---|---|
| Classification | |||||
| Class / category | — | — | ≈ | ||
| Also known as | PethidineMeperidineDemerolDolantinDolcontral | pethidinemeperidine | — | — | ≈ |
| Safety | |||||
| Addiction potential | extremely addictive with a high potential for abuse | — | — | — | |
| Toxicity | high toxicitypotentially lethal when mixed with depressants like alcohol or benzodiazepines | — | — | — | |
| Dangerous interactions | — | — | — | ||
| Dose · Oral | |||||
| Threshold | 25 mg | — | — | — | |
| Light | 50–100 mg | 50–100 mg | — | — | = |
| Common | 100–200 mg | 100–200 mg | — | — | = |
| Strong | 200–400 mg | 200–400 mg | — | — | = |
| Duration | |||||
| Onset | 30–60 minutes | 30–60 minutes | — | — | = |
| Total | — | 4–6 hours | — | — | |
| After-effects | 2–10 hours | 2–10 hours | — | — | = |
| Pharmacology | |||||
| Receptor activity | — | — | Sodium-dependent serotonin transporterMu-type opioid receptorSodium-dependent dopamine transporterKappa-type opioid receptor | OPRM1GRIN3AOPRK1Oprd1KCNH2SLC6A3Slc6a4SLC22A1 | ≠ |
| Half-life | — | — | Initial distribution phase (t<sub>1/2 α</sub>) = 2-11 minutes; terminal elimination phase (t<sub>1/2 β</sub>) = 3-5 hours. In patients with hepatic dysfunction (e.g. liver cirrhosis or active viral hepatitis) the t<sub>1/2 β</sub> is prolonged to 7-11 hours. Plasma meperidine concentrations decline in a biphasic manner, with a half-life in the initial distribution phase (t1/2alpha) of 2-11 minutes and a half-life in the terminal elimination phase (t1/2beta) of 3-5 hours in individuals with normal renal and hepatic function. The elimination half-life is prolonged in patients with hepatic dysfunction, averaging about 7-11 hours in patients with liver cirrhosis or active viral hepatitis. After single rapid iv injection in man, 0.8 mg/kg, plasma meperidine concentration declined biexponentially with fast (alpha) and slow (beta) phases having half-lives in normal group of 0.19 hr and 3.2 hr (mean values), respectively. In cirrhotics half-life-alpha was not changed but half-life-beta increased to 7.0 hr. Pharmacokinetics of morphine, buprenorphine and pethidine were determined in 10 cats. ... Six received pethidine (5 mg/kg) intramuscularly. Jugular venous blood samples were collected at time points to 24 hr, and plasma morphine concentrations were measured by high performance liquid chromatograpy (HPLC), buprenorphine by radioimmunoassay (RIA) and pethidine by gas chromatography. ... For i.m. pethidine, elimination half-life /was/ 216.4 min ... . Following intravenous administration of meperidine in healthy individuals, the volume of distribution at steady state was 269 L (range, 198 to 333 L); plasma clearance was 1.06 L/min (range, 0.71 to 1.32), and the elimination half-life was 3.6 hours (range, 3.1 to 4.1). Liver disease, eg, cirrhosis, acute viral hepatitis, doubles the half-life. There is evidence that the disposition of meperidine varies between day and night, with the elimination half-life being shorter and the plasma clearance greater at night. This suggests that larger doses might be required at night. Bioavailability after oral administration is about 50% due to first-pass metabolism in the liver, but increases to 80% to 90% in patients with cirrhosis. The elimination half-life in the neonate is 22.7 hours. For more Biological Half-Life (Complete) data for Meperidine (7 total), please visit the HSDB record page. | — | |
| Protein binding | — | — | 60-80% bound to plasma proteins, primarily albumin and α<sub>1</sub>-acid glycoprotein. The presence of cirrhosis or active viral hepatitis does not appear to affect the extent of protein binding. | — | |
Dose at a glance
Each database's primary-route ladder on one shared scale — see where ranges line up or shift.
Duration at a glance
Total duration on one shared scale.
PsychonautWiki summary
Fatal overdose may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1] It is strongly discouraged to combine these substances, particularly in common to heavy doses.
TripSit summary
A phenylpiperidine opioid first synthesised by Otto Eisleb in 1939, better known by the names meperidine and pethidine. An analgesic, once widely prescribed it has since declined in usage due to the discovery of a toxic metabolite - norpethidine. Also reacts dangerously with many drugs.
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.