Long-acting derivative

Etidocaine is a long-acting derivative of lidocaine but is far more potent. It is effective for infiltration anesthesia, peripheral nerve block, and epidural and caudal blockade. 

Presently available hypnotic drugs for the treatment of transient, short-term, or chronic insomnia differ significantly in pharmacokinetic properties, including elimination half-life and presence of active metabolites. On the other hand, they have in common short absorption and distribution times. As a result, in most circumstances they induce sleep rapidly. According to their elimination half-life, hypnotics can be divided into short-, intermediate-, or long-acting derivatives. 

A repository 8-aminoquinohne derivative that would destroy the exo-ery-throcytic forms of P. vivax and P. malariae at a single dose would be useful either alone or in combination with other repository preparations [146]. Unfortunately, all attempts to date to synthesize long-acting derivatives of pamaquine, primaquine, and other 8-aminoquinolines have failed [36]. Pamaquine pamoate [148], primaquine pamoate, primaquine suraminate, and several dozen other relatively insoluble primaquine salts lacked significant repository activity in mice at doses ranging from 100 to 400 mg base/kg [36]. Further, hopes that A-[(6-methoxy-8-quinolylamino)alkyl]amides such as LVIa and b and LVIIa-c... 

Finally, attachment of a rather complex side chain to the para position of the benzene ring on the sulfonamide leads to the very potent, long-acting oral antidiabetic agent, glyburide (215). Preparation of this compound starts with the chlorosul-fonation of the acetamide of 3-phenethylamine (209). The resulting sulfonyl chloride (210) is then converted to the sulfonamide (211) and deacylated (212). Reaction with the salicylic acid derivative, 213, in the presence of carbodiimide affords the amide, 214. Condensation of that with cyclohexylisocyanate affords glyburide (215). ... 

Glowa J., Fantegrossi W., Lewis D., Matecka D., Rice K., Rothman R. Sustained decrease in cocaine-maintained responding in rhesus monkeys with l-[2]-bis(4-flourophenyl)methoxy[ethyl]-4-(3-hydroxy-3-phenylpropyl)piperazinyldecanoate, a long-acting ester derivative of GBR 12909. J. Med. Chem. 39 4689, 1996. 

Hsin, L.-W., Dersch, C.M., Baumann, M.H. et al. (2002) Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents chiral hydroxyl-containing derivatives of l-[2-[bis (4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and l-[2-(diphenylmethoxy)ethyl]-4-(3-phe-nylpropyl)piperazine. Journal of Medicinal Chemistry, 45 (6), 1321-1329. 

This hypothesis clearly contradicted a large body of clinical evidence that nitrates were effective. Some years later, using more sensitive and reliable analytical methods, this interpretation was shown to be incorrect, and the clinical utility of long-acting, oral organic nitrate derivatives affirmed. In 1967, one of the pharmacodynamically active metabolites of ISDN, IS-5N, was shown to be formed in vivo, and shortly thereafter it was introduced as a novel long-acting NO donor with improved bioavailability. 

Heart medication, betablockers, ACE-inhibitors, long acting nitro derivates, calcium channel blockers, angiotensin II antagonists... 

Lofentanil—another extremely potent fentanyl derivative that is 6,000 times stronger than morphine and is very long-acting (i.e., hours), so it is used only for prolonged surgical procedures and treatment of multiple trauma-related injuries. 

Zopiclone is widely used as a sedative-hypnotic. It is metabolized to an inactive N-desmethylated derivative and an active N-oxide compound, both of which contain chiral centres. S-Zopiclone has a 50-fold higher affinity for the benzodiazepine receptor site than the R-enantiomer. This could be therapeutically important, particularly if the formation and the urinary excretion of the active metabolite benefits the S-isomer, which appears to be the case. As the half-life of the R-enantiomer is longer than that of the S-form, it would seem advantageous to use the R-isomer in order to avoid the possibility of daytime sedation and hangover effects which commonly occur with long-acting benzodiazepine receptor agonists. 

Mesterolone is a non-17-alkylated derivative which is also has weak activity orally. Testosterone itself has little activity when taken orally and is used sublingually or as an implant. By esterification of testosterone formulations of long-acting testosterone derivatives in oily solutions for intramuscular injection were developed. 

Acedapsone is a derivative of dapsone that has little activity against M. leprae but is converted to an active dapsone metabolite. It is a long-acting intramuscular repository form of dapsone with a half-life of 46 days. It may prove useful in leprosy patients who cannot tolerate long-term oral dapsone therapy. 

OTC Afrin,Afrin 12-Hour, Ocuclear, Sinex 12 Hour Long-Acting Chemical Class Imidazoline derivative... 

Enalapril is an oral prodrug that is converted by hydrolysis to a converting enzyme inhibitor, enalaprilat, with effects similar to those of captopril. Enalaprilat itself is available only for intravenous use, primarily for hypertensive emergencies. Lisinopril is a lysine derivative of enalaprilat. Benazepril, fosinopril, moexipril, perindopril, quinapril, ramipril, and trandolapril are other long-acting members of the class. All are prodrugs, like enalapril, and are converted to the active agents by hydrolysis, primarily in the liver. 

Latanoprost, a stable long-acting PGF2E derivative, was the first prostanoid used for glaucoma. The success of latanoprost has... 

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