Chemistry:Anileridine

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Short description: Analgesic drug
Anileridine
Clinical data
Trade namesLeritine
AHFS/Drugs.comMonograph
Routes of
administration
Tablets, injection
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding> 95%
MetabolismHepatic
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC22H28N2O2
Molar mass352.478 g·mol−1
3D model (JSmol)
Melting point83 °C (181 °F)
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Anileridine (trade name: Leritine) is a synthetic analgesic drug[1] and is a member of the piperidine class of analgesic agents[2] developed by Merck & Co. in the 1950s.[3] It differs from pethidine (meperidine) in that the N-methyl group of meperidine is replaced by an N-aminophenethyl group, which increases its analgesic activity.

Anileridine is no longer manufactured in the US or Canada.[4] Anileridine is in Schedule II of the Controlled Substances Act 1970 of the United States as ACSCN 9020 with a zero aggregate manufacturing quota as of 2014. The free base conversion ratio for salts includes 0.83 for the dihydrochloride and 0.73 for the phosphate.[5] It is also under international control per UN treaties.

Administration

As tablets or injection.[6]

Pharmacokinetics

Anileridine usually takes effect within 15 minutes of either oral or intravenous administration, and lasts 2–3 hours.[7] It is mostly metabolized by the liver.

See also

References

  1. ↑ "Pharmacology of ethyl-1-(4-aminophenethyl)-4-phenylisonipecotate, anileridine, a new potent synthetic analgesic". The Journal of Pharmacology and Experimental Therapeutics 119 (1): 26–34. January 1957. PMID 13417056. 
  2. ↑ "Anileridine as an anesthetic agent". The Journal of the Florida Medical Association. Florida Medical Association 44 (2): 143–5. August 1957. PMID 13449255. 
  3. ↑ Frank A Cutler Jr FA, Chemerda JM, "Substituted piperidines and methods for making same", US patent 2897204, issued 28 July 1959, assigned to Merck and Co Inc
  4. ↑ "Discontinued Prescription Drug Products". Canadian Pharmacists' Association. http://www.pharmacists.ca/content/hcp/tools/drugnews/discontinued.htm. 
  5. ↑ "Federal Register Notices: Quotas - 2014". Diversion Control Division, Drug Enforcement Agency. U.S. Department of Justice. 25 August 2014. http://www.deadiversion.usdoj.gov/fed_regs/quotas/2014/fr0825.htm. 
  6. ↑ "Pharmaceutical Information - LERITINE". RxMed. http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20%28General%20Monographs-%20L%29/LERITINE.html. 
  7. ↑ "Anileridine Consumer Information". MedicineNet. http://www.medicinenet.com/anileridine-oral_tablet/article.htm.