Antimuscarinic And Ganglionic Drugs

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antimuscarinic drugs

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-all antimuscarinic drugs competitively block muscarinic receptors
-tertiary AM drugs have a negligible blocking activity at ganglionic Nn receptors, but quaternary have sig blocking

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organs affected at low doses of atropine

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-heart (M2 autorepctors on PNS terminals, lacrimal, salivary, and sweat glands

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organs affected at intermediate doses of atropine

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-same as low + heart (M2 receptors), sphincter muscle of iris, ciliary muscle, CNS (depression)

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organs affected at high doses of atropine

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-organs affected by lesser doses are affected to a greater degree
-smooth muscle of intestines, bronchi, and bladder as well as gastric glands are affected

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effects of antimuscarinics on CNS

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intermediate dose: mild vagal stim, "downer," despression of vesitubular function, reduction of parkinsonian tremor and rigidity
high doses: amnesia, malaise, restlessness, irritability, disorientation, hallucinations, delirium, then coma

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effects of antimuscarinics on CV system

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-SA node (low doses) decrease in HR (intermediate doses) tachy and abolished reflex vagal cardiac slowing
-atria: increase in coduction and automacticity, decrease in refractoriness
-vessels (high doses) dilation of cutaneous blood vessels

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effects of antimuscarinics on GI

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-decreased: gastric secretion, tone, amplitude of contractions, peristaltic activity, and secretions of intestinal tract
-relactioan of teh lower esophageal sphincter
-mild relaxation of gallbladder and bile ducts

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effects of antimuscarinics on genitourinary system

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-relaxation of pelves, calyces, and ureter
-decreased uretal parastalsis
-relaxation of detrusor muscles

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effects of antimuscarinics respiratory system

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-bronchial smooth muscle relaxation
-decrease tracheobronchial secretions
-decreased mucociliary clearance

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effects of antimuscarinics on eye

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-relaxation of sphincter of iris and sphincter muscle, hinders flow of aq humor, decreased secretion of lacrimal glands

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effects of antimuscarinics on skin

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decreased secretion of sweat glands

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pharmacokinetics of antimuscarinics

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-variable oral bioav
-tertiary amines distribute to all tissues, quaternary do not enter CNS
-50% of atropine and 90% of scopolamine metab'd by liver
-60% atropine excreted by kidney
-atropine and scopolamine half life of 3 hrs, glycopyrrole = 10 hours

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toxicity of antimuscarinics

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(allergic rxn) rashes, urticaria, fever
(acute poisoning) death from resp failure. treat sxs: vitals, diazepam for covulsions, temp control with ice bags and ETOH sponges

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therapeutic uses of antimuscarinics

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-in eye exams, prevent eye adhesions in irritation, stop diarrhea, colic, sialorrhea, motion sickness, enuresis, urge incontinence, bronchial asthma and COPD, cardiopulmonary resuscitation, sinus or nodal brady, AV block, pre op cardio, parkinsons,

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mechanism of nicotine

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-activates nicotinic receptors at autonomic ganglia, neuromuscular junction, some presynaptic nerve terms, adrenal medulla, CNS
-large doses cause depolarization blockade
=stims sensory receptors on mesentery, tongue, stomach, lung, skin, carotid/aortic bodies, pain receptors

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pharmacological effects of nicotine

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-CNS:stim of renshaw cells, +/- reticular formation, stim of respiratory and vasomotor centers, emetic center, chemoreceptor, AHD secretion, attention and memory, sedative-anxiolytic activity, cerebrospinal axis
-increade CO and HR, constrict skin/splanchnic vessels, dilate muscular vessels, increase bp, (cardiovascular collapse - toxic), anorexia, nausea, increase peristalisis and secretions, (paralytic ileus - toxic), increase resoirations, increase bronchoconstriction and secretions, (apnea - toxic), decreased diuresis, contraction of detrusor muscle, relaxation of trigone and internal sphincter, increase sweat, miosis, increase oxidases, platelet aggregation, loss of wt, hand tremors, skeletal muscle paralysis

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ganglionic blocking drugs

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-hexamethonium and mecamylamine
-competitive blockage of nicotinic receptors
-increase HR, decrease CO, venous tone, peripheral vascular resistance, increase skin blood flow, decrease splanchnic and renal blood flow
-may be useful to treat tourettes