This article is about the analgesic drug also sold under the trade name Dolantin. For the anticonvulsant sold under the trade name Dilantin, see phenytoin.
Pethidine
Clinical data
Trade names
Demerol
Other names
Meperidine (USAN US)
Pregnancy category
AU: C
Dependence liability
High
Addiction liability
High[1]
Routes of administration
By mouth, IV, IM, IT,[2] SC, epidural[3]
ATC code
N02AB02 (WHO)
Legal status
Legal status
AU: S8 (Controlled drug)
BR: Class A1 (Narcotic drugs)[4]
CA: Schedule I
DE: Anlage III (Special prescription form required)
NZ: Class B
UK: Class A
US: Schedule II
UN: Narcotic Schedule I
Pharmacokinetic data
Bioavailability
50–60% (Oral), 80–90% (Oral, in cases of hepatic impairment)
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine class.[5][6][7][8][9][10] Synthesized in 1938[11] as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, in Germany.[12] Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines (piminodine, anileridine and others), the prodines (alphaprodine, MPPP, etc.), bemidones (ketobemidone, etc.) and others more distant, including diphenoxylate and analogues.[13]
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. For much of the 20th century, pethidine was the opioid of choice for many physicians; in 1975, 60% of doctors prescribed it for acute pain and 22% for chronic severe pain.[14]
It was patented in 1937 and approved for medical use in 1943.[15] Compared with morphine, pethidine was considered to be safer, carry a lower risk of addiction, and to be superior in treating the pain associated with biliary spasm or renal colic due to its putative anticholinergic effects.[7] These were later discovered to be inaccurate assumptions, as it carries an equal risk of addiction, possesses no advantageous effects on biliary spasm or renal colic compared to other opioids. Due to the neurotoxicity of its metabolite, norpethidine, it is more toxic than other opioids—especially during long-term use.[7] The norpethidine metabolite was found to have serotonergic effects, so pethidine could, unlike most opioids, increase the risk of triggering serotonin syndrome.[7][8]
^Bonewit-West K, Hunt SA, Applegate E (2012). Today's Medical Assistant: Clinical and Administrative Procedures. Elsevier Health Sciences. p. 571. ISBN 9781455701506. Archived from the original on 10 January 2023. Retrieved 20 August 2019.
^Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
^"Demerol, Pethidine (meperidine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 April 2014.
^Shipton E (March 2006). "Should New Zealand continue signing up to the Pethidine Protocol?" (PDF). The New Zealand Medical Journal. 119 (1230): U1875. PMID 16532042. Archived from the original (PDF) on 2014-04-08.
^ abcdLatta KS, Ginsberg B, Barkin RL (January–February 2002). "Meperidine: a critical review". American Journal of Therapeutics. 9 (1): 53–68. doi:10.1097/00045391-200201000-00010. PMID 11782820. S2CID 23410891.
^ abMacPherson RD, Duguid MD (2008). "Strategy to Eliminate Pethidine Use in Hospitals". Journal of Pharmacy Practice and Research. 38 (2): 88–89. doi:10.1002/j.2055-2335.2008.tb00807.x. S2CID 71812645.
^Mather LE, Meffin PJ (September–October 1978). "Clinical pharmacokinetics of pethidine". Clinical Pharmacokinetics. 3 (5): 352–368. doi:10.2165/00003088-197803050-00002. PMID 359212. S2CID 35402662.
^Cite error: The named reference AMH was invoked but never defined (see the help page).
^US 2167351 Piperidine compounds and a process of preparing them
^Michaelis M, Schölkens B, Rudolphi K (April 2007). "An anthology from Naunyn-Schmiedeberg's archives of pharmacology". Naunyn-Schmiedeberg's Archives of Pharmacology. 375 (2): 81–84. doi:10.1007/s00210-007-0136-z. PMID 17310263. S2CID 27774155.
^Reynolds AK, Randall LO (1957). Morphine and Allied Drugs. Toronto/London: University of Toronto Press/Oxford University Press. pp. 273–319.
^Kaiko RF, Foley KM, Grabinski PY, Heidrich G, Rogers AG, Inturrisi CE, Reidenberg MM (February 1983). "Central nervous system excitatory effects of meperidine in cancer patients". Annals of Neurology. 13 (2): 180–185. doi:10.1002/ana.410130213. PMID 6187275. S2CID 44353966.
^Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 52X. ISBN 9783527607495.
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine...
(normeperidine, pethidine intermediate B) is a 4-phenylpiperidine derivative that is both a precursor to, and the toxic metabolite of, pethidine (meperidine)...
Pethidine intermediate A is a 4-phenylpiperidine derivative that is a precursor to the opioid analgesic drug pethidine (meperidine). It is not known to...
United States. It is an analog of pethidine (meperidine) a Schedule II drug. Chemically, it is a reversed ester of pethidine which has about 70% of the potency...
compounds derived from MPPP, the reversed ester of the opioid analgesic pethidine, which were sold as designer drugs in the 1980s, but have been rarely...
(meperidinic acid, pethidine intermediate C) is a 4-phenylpiperidine derivative that is both a metabolite of and a precursor to pethidine (meperidine). It...
between the phenelzine she was taking prior to her hospital visit, and the pethidine administered by a resident physician. The lawsuits and regulatory investigations...
Oxpheneridine (carbamethidine) Pethidine (meperidine) Pethidine intermediate A Pethidine intermediate B (norpethidine) Pethidine intermediate C (pethidinic...
other opioids (e.g., codeine, oxycodone, hydrocodone, dihydromorphine, pethidine) all exert a similar influence on the cerebral opioid receptor system...
Piminodine (Alvodine) is an opioid analgesic that is an analogue of pethidine (meperidine). It was used in medicine briefly during the 1960s and 70s,...
or Lealgin), is an opioid analgesic which is structurally related to pethidine and is used clinically as a general anesthetic. Phenoperidine is an opioid...
preservative-free local anesthetic agents may be injected intrathecally. Pethidine also has local anesthetic properties, in addition to its opioid effects...
in the early 1950s in the USSR during research into the related drug pethidine. Trimeperidine has four structural isomers, of which two are active, the...
Acepromazine atropine diazepam Scopolamine Opioid analgesics, such as morphine, pethidine and buprenorphine. These drugs are used before the administration of an...
fentanyl, morphine, heroin and methadone (the notable exception being pethidine) Products containing nicotine such as cigarettes, chewing tobacco or gum...
intravenous opioid analgesia. Fentanyl or morphine are usually chosen. Pethidine (meperidine, brand name Demerol in the US) should be avoided, as large...
adequately to treatment with naloxone. It is equally as effective as pethidine in suppressing shivering after surgery. Doxapram has been used as a reversal...
listed in the convention); synthetic narcotics such as methadone and pethidine; and cannabis, coca, and cocaine. The Convention divides drugs into four...
a synthetic opioid drug with effects similar to those of morphine and pethidine (meperidine). The Parkinson-inducing effects of MPTP were first discovered...
subjects when compared to both methadone and pethidine. In comparison to equianalgesic doses of pethidine (Demerol), methadone was shown to produce less...
is less than that associated with other classes of opioids such as the pethidine class of synthetics in particular. Users of hydromorphone may experience...
when the latter is used by itself. The combination of levallorphan with pethidine (meperidine) was indeed used so frequently, a standardized formulation...
Oxycodone Oxymorphone Para-fluorofentanyl PEPAP PethidinePethidine intermediate A Pethidine intermediate B Pethidine intermediate C Phenadoxone Phenampromide...
first incident. In late 1973, he was hospitalized from the effects of a pethidine addiction. According to his primary care physician, George C. Nichopoulos...
Global Information
