Mesantoin

D Mesantoin (Sandoz) wfm GB Mesantoin (Sandoz) wfm USA Mesantoin (Sandoz) wfm... 

Anticonvulsant Carbamazepine, ethosuximide, lamotrigine, mesantoin, phenytoin, trimefhadione, valproic acid... 

Hydantoins Ethotoin (Peganone) Fosphenytoin (Cerebyx) Mephenytoin (Mesantoin) Phenytoin (Dilantin) Primary effect is to stabilize membrane by blocking sodium channels in repetitive-firing neurons higher concentrations may also influence concentrations of other neurotransmitters (GABA, norepinephrine, others)... 

This category includes phenytoin (Dilantin), mephenytoin (Mesantoin), ethotoin (Peganone), and fosphenytoin (Cerebyx). Phenytoin is often the first... 

Isocorydine (1,2,10-trimethoxy-ll-hydroxyaporphine) was isolated for the first time by Maranon (422) and Go (423). Reynolds el al. (401) reported that its effect resembled that of bulbocapnine. Administration of N-methylisocorydinium chloride, a quaternary base isolated from Fagaro coco, results in apnea and finally in cardiac failure (424r-426). In rabbits it causes an increase in excitability whereas in rats it causes a decrease. The effect of mesantoine and coramine is to some extent antagonistic, which is contrary to the effect of lobeline and of the barbiturates. In rabbits and toads isocorydine diminishes the contractility and excitability of the skeletal muscles however, a curarelike effect was not observed. After intraperitoneal application to rats the recorded LD50 was 10.9 mg/kg. 

Recall from Section 1.9 that some molecules can exist as chiral enantiomers that are mirror images of each other. Although enantiomers may appear to be superficially identical, they may differ markedly in their metabolism and toxic effects. Much of what is known about this aspect of xenobiotics has been learned from studies of the metabolism and effects of pharmaceuticals. For example, one of the two enantiomers that comprise antiepileptic Mesantoin is much more rapidly hydroxylated in the body and eliminated than is the other enantiomer. The human cytochrome P-450 enzyme denoted CYP2D6 is strongly inhibited by quinidine, but is little affected by quinine, an optical isomer of quinidine. Cases are known in which a chiral secondary alcohol is oxidized to an achiral ketone, and then reduced back to the secondary alcohol in the opposite configuration of the initial alcohol. 

Mephenytoin has been extensively used for phenotyping purposes however, such use is not without practical problems. For example, sedation is often observed in PMs, especially those of small body size, e.g., children and Southeast Asians, following administration of a 100-mg dose usually used for phenotyping (178). Accordingly, a dose of 50-mg mephenytoin is often used to phenotype such individuals. A further complicating factor is that racemic mephenytoin (Mesantoin , Sandoz/Novartis, Basal, Switzerland) is not available in many parts of the world. For these reasons, other in vivo probes have been investigated. 

Trade names Epilan-Gerot Epilanex Mesantoin (Novartis) Indications Partial seizures Category Antiepileptic, hydantoin... 

Cantil, Trancolon Demerol, Dolantin, Dolestine, Dolosal, Opistan, Pethidine, Petidin mefloquine mefloquine methadone Epilan-Gerot, Epilanex, Mesantoin Mebaral, Prominal phytonadione meprobamate... 

Simultaneous amitriptyline, caffeine, clomipramine, codeine, desipramine, etbotoin, imip-ramine, lidocaine, mesantoin, metbsuximide, nirvanol, nortriptyline, oxeizepam, propranolol, quinidine... 

Extracted acetaminophen, amobarbital, butabarbital, chlordiazepoxide, diazepam, eth-chlorvynol, flurazepam, glutethimide, methaqualone, methypiylon, nitrazepam, pentobarbital, phenobarbital, phenytoin, primidone, salicgrlic acid, secobarbital, theophylline Simultaneous amitriptyline, caffeine, clomipramine, codeine, desipramine, ethotoin, imip-ramine, lidocaine, mesantoin, methsuximide, nirvanol, nortriptyline, oxazepam, procainamide, phenylpropanolamine, propranolol, quinidine... 

Also analyzed acetaminophen, alprazolam, amitriptyline, amoxapine, carbamazepine, chlordiazepoxide, chlorpromazine, chlorprothixene, clonazepam, demoxepam, desipra-mine, diphenhydreiniine, disop3n amide, doxepin, ethotoin, durazepam, glutethimide, hal-operidol, haloperidol, imipramine, lidocaine, lorazepam, loxapine, maprotiline, mesantoin, mesoridetzine, methaqualone, methotrimeprazine, nordiazepam, nortriptyline, oxazepam, pentazocine, perphenazine, phenacetin, phenobarbital, phen3doin, promazine, promethazine, propranolol, protriptyline, salicylic acid, thiothixene, trifluoperazine, trifluproma-zine, trimipramine... 

Ampicillin, cefotaxime, ceftazidine, ciprofloxacin, methicillin, sulfathiazole, sulfamethoxazole Carbamazepine, felbamate, mesantoin, phenytoin, valproic acid Cimetidine, ranitidine Amodiaquin, chloroquine, quinine Chlorpromazine, clozapine, mianserin... 

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