Trimethaphan Camsylate Miscellaneous

Further structural modification of classic antimuscarinic agents can be found in the drugs described next. Each of them has the typical bulky group characteristic of the usual anticholinergic molecule. One modification is represented by the diphenylmethylene moiety (e.g., diphemanil); a second, by a phenothiazine (e.g., ethopropazine); and a third, by a thioxanthene structure (e.g., methixene).

Diphemanil Methylsulfate, USP. Diphemanil methylsulfate, 4-(diphenylmethylene)-1, 1 -dimethylpiperidinium methylsulfate (Prantal), or diphemanil methylsulfate is a potent cholinergic blocking agent. In the usual dosage range, it acts as an effective parasympatholytic by blocking nerve impulses at the parasympathetic ganglia, but it does not invoke a sympathetic ganglionic blockade. It is claimed to be highly specific in its action on those innervations that activate gastric secretion and GI motility. Although this drug can produce atropine-like side effects, they rarely occur at recommended doses. The highly specific nature of its action on gastric functions makes the drug useful in the treatment of peptic ulcer, and its lack of atropine-like effects makes its use much less distressing than other anti-spasmodic drugs. In addition to its action in decreasing gastric hypermotility, diphemanil methylsulfate is valuable in hyperhidrosis in low doses (50 mg twice daily) or topically. The drug is not well absorbed from the GI tract, particularly in the presence of food, and should be administered between meals. The methylsulfate salt was chosen as the best, because the chloride is hygroscopic and the bromide and iodide ions have exhibited toxic manifestations in clinical use.


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