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Autonomics-1.6
Pharmocology-Autonomics1.6/MuscarinicCholinergic
| Question | Answer |
|---|---|
| muscarinic agonist? | Ach |
| muscarinic antagonist? | atropine, pirenzepine |
| muscarinic receptor tissue? | autonomic ganglia, secretory glands, CNS, smooth muscle |
| Nn and Nm agonist? | nicotine |
| Nn antagonist? | Trimethaphan, nicotine |
| Nm antagonist? | Tubocurarine, pancuronuim, succinylcholine |
| Nn tissue? | autonomic ganglia, adrenal medulla, CNS |
| Nm tissue? | NMJ |
| what are the adrenergic receptors? | alpha1, alpha2, beta1, beta2, beta3 |
| alpha1 location? | postsynaptic effector cells, especially vascular smooth muscle, heart and papillary dilator muscle |
| alpha2 location? | presynaptic terminals (dec NT when stimulated), platlets, lipocytes, and some vascular smooth muscle. |
| beta1 location? | postsynaptic effector cells, especially the heart, lipocytes and juxtaglomerular cells |
| beta2 location? | postsynaptic effector cells, especially respiratory, uterine, GI and vascular smooth muscle, as well as skeletal muscle and liver. Also presynaptic NE. a little on the heart |
| beta3 location? | adipose tissue, mediate lipolysis when stimulated |
| muscarinic direct acting agonists? | alkaliod derivatives and choline esters-Ach prototype |
| alkaliod derivatives? | not susceptable to AchE degredation. muscarine, pilocarpine, arecoline |
| muscarine? | from the mushroom Amantia muscaria |
| pilocarpine? | can cause CV responses, used in opthalamic solution to cause miosis and contraction of ciliary muscle. eye undergoes spasm of accomodation and vision is fixed at a distance making it impossible to focus. Useful in open angle glaucoma. |
| side effects of pilocarpine? | diaphoresis (sweating) and salivation |
| Arecoline? | found in nuts of east india |
| choline esters? | Ach prototype: Ach, methacholine, carbichol, bethanechol (DuViod) |
| Ach? | nonselective, nicotinic and muscarinic receptors, short action, eye drops |
| Methacholine? | only for clinical use, test for athsma, historically used to tx tachycardia |
| carbachol? | limited to opthalamic use as miotic agent. less sensitive to atropine antagonism than other choline esters. |
| bethanechol (DuVoid)? | not susceptable to AchE degredation. No nicotinic action. Selet action on GI and urinary bladder. Used for postop urinary retention, postop abdominal distention, diabetic gastroparesis, esophegeal reflux, gastric atony following vagotomy. |
| when do you avoid bethanechol? | urinary tract obstruction |
| direct muscarinic agonists actions on CV system? | vasodialation, dec HR, dec conduction in SA and AV node, dec contraction |
| direct muscarinic agonists actions on vasculature? | relaxation on the endothelial cells of the vessels (not direct) |
| direct muscarinic agonists actions on the GI system? | increase tone, peristalsis, contractions, inc secretions. Unwanted N/V belching, cramps, defication |
| direct muscarinic agonists actions on the Urinary tract? | inc peristalsis, contract detrusor, inc void pressure, dec bladder capacity. relax trigone and external sphinctor. Inc micturation |
| direct muscarinic agonists actions on the eye? | miosis (contract smooth muscle of iris), cannot accomodate b/c cilliary muscle is contracted (near vision). Dec PANS allows ciliary to relax for far vision |
| direct muscarinic agonists actions on the respiratory system? | bronchial smooth muscle contracted, inc gland secretion. DO NOT give muscarinics in asthmatics |
| direct muscarinic agonists actions on the glands? | all glands stimulated (lacrimal, trachobronchial, salivary, digestive, exocrine) |
| SLUDGE = | (muscarinic agonists) salivation, lacramation, urination, defication, GI upset, emesis |
| Indirect acting muscarinic agonists? | AchE inhibitors. work on muscarinic and nicotinic receptors. |
| where do indirect muscarinic agonists target? | eye, skeletal muscle NMJ, GI tract, urinary bladder |
| reversivble indirect musc agonists? | carbamates to treat myasthenia gravis, alzheimers disease and glaucoma |
| irreversible indirect musc agonists? | organophosphates (atropine)used as toxic agents in insecticides and chemical warfare nerve gases |
| Hydrogen bonds? | edrophonium, easially reversible |
| intermediate bonds? | physostigmine, neostigmine and ambenonium, much slower |
| covalent bond? | much slower and long lasting |
| AchE reactivator? | pralidoxime, protopam(2-PAM) binds anionic site causing organophosphate to break off and regenerate AchE. Works best at NMJ than in the CNS. |
| edrophonium? | a carbamate, reversible (short acting) used to dx myasthenia, supraventricular tachycardia termination |
| physostigmine? | carbamate, reversible, used for glaucoma, CNS muscarine antagonist (atropine) antidote, reverse central anticholinergic syndrome due to OD with phenothiazine, antihistamines, tricyclic antidepressants |
| pyridostigmine? | carbamate, reversible, myasthenia treatment, NM block reversal |
| Neostigmine? | carbamate, reversible, paralytic ileus and bladder atony, myasthenia tx, NM block reversal |
| Ambenonium? | carbamate, reversible, Myasthenia tx |
| Demacarium? | carbamate, reversible, glaucoma |
| Tacrine, donepezil, rivastigmine, galantamine? | reversible, alzheimers dementia |
| echothiophate, isoflurophate? | organophosphate, irreversible, glaucome tx |
| effect of indirect acting cholinergic agents on eye? | miosis and constrict ciliary muscle for near vision only, no accomodation. If IC pressure elevated, it will fall b/c of facilitation of outflow, dec secretion |
| effect of indirect acting cholinergic agents on GI tract? | inc contraction, inc gastric secretion. cramps, diarrhea, defication. |
| effect of indirect acting cholinergic agents on NMJ? | short term (small doses): inc contrations because of inc time of Ach in synapse. Tx Myasthenia gravis. Long term (large doses): block NMJ transmission |
| effect of indirect acting cholinergic agents on vasculature? | less effect than direct bc only where vagal innervation exists. |
| therapudic uses for indirect acting cholinergic agents? | GI: paralytic ileus, bladder atony. Eye: glaucoma (physostigmine). neuromuscular: Myasthenia gravis (neostigmine, pyridostigmine, ambenonium) Alzheimers dementia (tacrine, rivastigmine, donepezil, galantamine) antimuscarinic intoxication (physostigmine) |
| Use indirect cholinergic agonists with caution in: | asthma, hyperthyroidism, Peptic Ulcer Disease, Hx of bradycardia, cardiac disease, hx of hypotension |
| contraindications for indirect cholinergic agonists: | urinary tract obstruction, GI obstruction, Ileus, closed angle glaucoma |
| muscarinic antagonists prototype? | atropine |
| tertiary amines? | atropine, scopolamine are naturally occuring, semi or synthetic include homatropine |
| Quaternary amines? | synthetic esters, reduce CNS action: propantheline, glycopyrolate, ipratropium. semi or synthetic include: methscopolamine, homatropine methylbromide and methantheline |
| MOA | reversible |
| what tissues do antimuscarinics affect at low doses? moderate? high? | low: salivary, bronchial, sweat glands, moderate: pupil, heart, high: GI and bladder |
| antimuscarinic agents actions? | Dry as a Bone, Blind as a Bat, Red and a Beet, and Mad as a Hatter (atropine poisoning) |
| atropine antimuscarinic effects in the CNS? | sedative action, large doses restlessness, disorientation, irratable, hallucinations, delirium. |
| scopolamine antimuscarinic effects on the CNS? | drowsiness, euphoria, fatigue, amnesia in a sensitive person. Anti-motion sickness action |
| antimuscarinics in CNS tx? | PD and extrapyramidal symptoms (EPS) |
| actions of antimuscarinics in the eye? | mydriasis and cycloplegia due to unopposed radial muscle induced dilation and paralysis of the ciliary muscle, dry sandy eyes, Inc IOC pressure in pts with narrow angle glaucoma. |
| Low atropine dose effect on the eye? | little effect, unable to focus to near vision. |
| actions of antimuscarinics on CV system? | theraputic doses produce tachycardia secondary to vagal blockade, little effect on BP, will antagonize exogenous choline esters. |
| Actions of antimuscarinics on respiratory system? | smooth muscle relaxation, bronchodiliation. Inhibit upper and lower tract secretions |
| Actions of antimuscarinics on GI? | atropine causes drying effect of oral mucosa (xerostomia). high dose affects acid output, GI tone and motility is delayed, possible constipation |
| Actions of antimuscarinics on GU? | smooth muscle relaxation, urinary retention especially in men with prostatic hypertrophy. |
| Actions of antimuscarinics on sweating? | atropine blocks sweating, especially due to choline agonists. |
| Tx uses of muscarinic antagonists in CNS? | PD and EPS (benztropine, trihexyphenidyl, procyclidine, biperiden) motion sickness prophylaxis (scopolamine) |
| Tx uses of muscarinic antagonists in eye? | mydriasis and sysloplegia induction (cyclopentolate, homatropine, tropicamide) |
| Tx uses of muscarinic antagonists in GI? | peptic ulcer disease and spastic colon (dicyclomine, glycopyrolate, methantheline, methscopolamine, propantheline, oxyphencyclimine) |
| Tx uses of muscarinic antagonists in CV? | symptomatic bradycardia and heart block (atropine) |
| Tx uses of muscarinic antagonists in respiratory? | COPD (ipratropium), |
| Tx uses of muscarinic antagonists in secretion? | antisecretory (dec GI motility, Urinary tract and biliary tract) (clindinium, hyosycamine) |
| Tx uses of muscarinic antagonists in UT? | antispasmodic and incontinence (flavoxate, oxybutnin, tolterodine) |
| contraindications for antimuscarinic Tx? | glaucoma, especially closed angle glaucoma, Hx of prostatic hyperplasia, gastric ulcer |
Created by:
lmh9p4
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