Alfentanil

A similar scheme via structures 53a, and would then afford alfentanil (55). 

Alfentanil, codein, dihydromorphine, etor-phine, fentanyl, heroin, hydromorphone, levo-methadone, morphine, oxycodone, pethidine, piritramide, remifentanil, sufentanil, tilidine, tramadol Buprenorphine, pentazocine Naloxone, naltrexone... 

Sufentanil, fentanyl, remifentanil, alfentanil, and morphine sulfate should be administered only by those specifically trained in the use of IV and epidural anesthetics Oxygen, resusdtative, and intubation equipment should be readily available. 

C12H15NO 3612-20-2) see Alfentanil Clebopride Fentanyl Fluspirilene Pipamperone "nnoridine Trifluperidol... 

C2H,0 64-17-5) see Actarit Alfentanil Alibendol Ainfenac sodium Beclobrate Candesartan cilexetil Chloral hydrate Dicycloverine Dimethadione Efonidipine hydrrxrhloride ethanol Eprazinone Ethambutol ... 

CijHijNjOi 95885-13-5) see Nefazodone hydrochloride l-ethyl-l,4-dihydro-5f/-tetrazol-5-one (C,H4N40 69048-98-2) see Alfentanil ethyldiisopropylamine... 

C3H5NO 109-90-0) see Alfentanil Cabergoline ethyl isocyanatoaeetate (C5H7NO3 2949-22-6) see Flumazenil ethyl isonicotinate... 

CHN 74-90-8) see L-Alanine Alfentanil Dimethadione Edetic acid Ibuprofen Indanorex Mecamylamine Molsidomine Nadoxolol D-Penicillamine Phensuximide L-Tryptophan Vetrabutine hydrogen peroxide... 

C,2oH2iiN20 61380-02-7) see Alfentanil iV-(4-methoxymethyl-4-piperidyl)propionaniIide (C15H24N2O2 61086-18-8) see Alfentanil Sufentanil 2-methoxy-5-(methylsulfonyl)benzoic acid (CgHioOjS 50390-76-6) see Tiapride 2-methoxy-10-[2-methyl-3-(p-toluenesulfonyloxy)propyi]-phenothiazine... 

C HiqOj 123-62-6) see Alclometasone dipropionate Alfentanil Alphaprodine Beclometasone Dextropropoxyphene Diethylstilbestrol dipropionate Fentanyl Propiram Sulindac Testosterone propionate propanol... 

Palm et al. [578] derived a two-way flux equation which is equivalent to Eq. (7.13), and applied it to the permeability assessment of alfentanil and cimeti-dine, two drugs that may be transported by passive diffusion, in part, as charged species. We will discuss this apparent violation of the pH partition hypothesis (Section 7.7.7.1). 

For weak acids, e.g., salicylic acid, the dependency on a pH gradient becomes complex since both the passive diffusion and the active transport process will be dependent on the proton concentration in the apical solution [61, 63, 98, 105] and a lowering of the pH from 7.4 to 6.5 will increase the apical to basolateral transport more than 20-fold. Similarly, for weak bases such as alfentanil or cimetidine, a lowering of the pH to 6.5 will decrease the passive transport towards the basolateral side [105]. The transport of the ionizable compound will, due to the pH partition hypothesis, follow the pKa curve. 

An example of N-dealkylation of an amine adjacent to a tertiary carbon can be found in the metabolism of synthetic opiod, alfentanil. The CYP3A4-catalyzed oxidation of the opiod alfentanil follows two major pathways (119) N-dealkylation to form no-ralfentanil and cleavage of the spiro center to generate N-phenylproprionamidc. Moreover,... 

V-phenyIpmprionamidc is found to come directly from alfentanil and not from noralfen-tanil. The mechanism of how the carbon-nitrogen of the spiro center is cleaved has not appeared in the literature. A possible mechanism would entail initial hydroxylation of a ring carbon adjacent to the piperdine nitrogen, followed by elimination of hydroxide to form the imine then rearrangement to the enamine, and finally elimination of the amide as indicated in Figure 4.56. 

FIGURE 4.56 Possible mechanism for the direct loss of A -phenylproprionainidc from alfentanil. 

Alfentanil—also known as Alfenta , it is very shortacting (5-15 minutes), 20-30 times more potent than morphine, and used for dental, diagnostic, and other minor surgical procedures. 

Alfentanil The curve rises from the origin until reaching a CSHT of 50 min at around 2 h of infusion. Thereafter the curve becomes horizontal. This demonstrates that alfentanil is also context insensitive for infusion durations of 2 h or longer. 

Fentanyl The most complex curve begins at the origin and is sigmoid in shape. It should cross the alfentanil line at 2 h duration and rise to a CSHT of 250 min after 6 h of infusion. Again, as the CSHT continues to rise, fentanyl does not become context insensitive. 

Morphine Diamorphine Codeine Pethidine Fentanyl Alfentanil Remifentanil... 

---