TAILIEUCHUNG - CLINICAL PHARMACOLOGY 2003 (PART 23)

Acetylcholine is a widespread chemotransmitter in the body, mediating a broad range of physiological are two distinct classes of receptor for acetylcholine defined on the basis of their preferential activation by the alkaloids, nicotine (from tobacco) and muscarine (from a fungus, Amanita muscaria). Cholinergic drugs (acetylcholine agonists) mimic acetylcholine at all sites although the balance of nicotinic and muscarinic effects is variable. Acetylcholine antagonists (blockers) that block the nicotine-like effects (neuromuscular blockers and autonomic ganglion blockers) are described elsewhere (see Ch. 18). . | SECTION 5 CARDIO- RESPIRATORY AND RENAL SYSTEMS This page intentionally left blank SECTION 5 Cholinergic and antimuscarinic anticholinergic mechanisms and drugs SYNOPSIS Acetylcholine is a widespread chemotransmitter in the body mediating a broad range of physiological are two distinct classes of receptor for acetylcholine defined on the basis of their preferential activation by the alkaloids nicotine from tobacco and muscarine from a fungus Amanita muscaria . Cholinergic drugs acetylcholine agonists mimic acetylcholine at all sites although the balance of nicotinic and muscarinic effects is variable. Acetylcholine antagonists blockers that block the nicotine-like effects neuromuscular blockers and autonomic ganglion blockers are described elsewhere see Ch. 18 . Acetylcholine antagonists that block the muscarine-like effects . atropine are often imprecisely called more precise term antimuscarinic is preferred here. Cholinergic drugs Classification Sites of action Pharmacology Choline esters Alkaloids with cholinergic effects Anticholinesterases organophosphate poisoning Disorders of neuromuscular transmission myasthenia gravis Drugs which oppose acetylcholine Antimuscarinic drugs Cholinergic drugs cholinomimetics These drugs act on postsynaptic acetylcholine receptors cholinoceptors at all the sites in the body where acetylcholine is the effective neurotransmitter. They initially stimulate and usually later block transmission. In addition like acetylcholine they act on the noninnervated receptors that relax vascular smooth muscle in peripheral blood vessels. For myasthenia gravis both to diagnose edrophonium and to treat neostigmine pyridostigmine distigmine To stimulate the bladder and bowel after surgery bethanechol carbachol. distigmine To lower intraocular pressure in chronic simple glaucoma pilocarpine To bronchodilate patients with airflow obstruction ipratropium oxitropium To improve cognitive function in Alzheimer s .

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