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20-September-2008 09:55:50 - Trimethaphan Trimethaphan Systematic IUPAC name decahydro-2-oxo-1,3-bisphenylmethyl- thieno1',2':1,2thieno3,4-dimidazol-5-ium Identifiers CAS number 7187-66-8 ATC code C02BA01 PubChem 23576 DrugBank APRD00044 Chemical data Formula C22H25N2OS Mol. mass 365.513 g/mol Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes Oral, IM, IV Trimethaphan is a drug that counteracts cholinergic transmission at the ganglion type of nicotinic receptors of the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous system. It acts as a non-depolarizing competitive antagonist at the nicotinic acetylcholine receptor, is short-acting, and is given intravenously. Contents 1 Effects 2 Therapeutic uses 3 Adverse effects 4 References Effects Trimethaphan is a sufonium compound and therefore carries a positive charge. Being charged, it cannot cross lipid cell membranes, such as those that comprise the blood-brain barrier. Due to this, trimethaphan does not have any effect on the central nervous system. The ciliary muscle of the eye functions to round the lens for accommodation and is controlled mainly by parasympathetic system input. With administration of a ganglion-blocking drug, the ciliary muscle cannot contract cycloplegia and the patient loses the ability to focus their eyes. Trimethaphan has a strong effect on the cardiovascular system. The size of blood vessels is primarily controlled by the sympathetic nervous system. Loss of sympathetic system input to the blood vessels causes them to get larger vasodilation which has the effect of lowering blood pressure. Postural hypotension is a common side effect of such drugs. Effects on the heart include a decreased force of contraction and an increase in heart rate tachycardia. Although it is important to note that this reflexive tachycardia can be diminished or undetected because Trimethaphan is also blocking the sympathetic ganglia innervating the heart. The motility of the gastrointestinal tract is regulated by the parasympathetic system, and blockage of this input results in diminished motility and constipation. Therapeutic uses The therapeutic uses of trimethaphan are very limited due to the competition from newer drugs that are more selective in their actions and effects produced. It is occasionally used to treat a hypertensive crisis and dissecting aortic aneurysm, to treat pulmonary edema, and to reduce bleeding during neurosurgery. Adverse effects The adverse effects are due to its nonselective ganglion block and are described in the Effects section above. The side effects are severe enough to limit this drugs use to emergency and acute situations. References Ganglion-blocking Drugs. Drug Benefits and Risks: International Textbook of Clinical Pharmacology. 2001. ISBN 0-471-89927-5 Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. 2004. ISBN 0-07-141092-9 v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Trimethaphan Categories: Anticholinergics Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 5 March 2008, at 07:22
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