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Binds equally to M1, M2, and M3 receptors and Nicotinic Receptors. Quickly metabolized by cholinesterase. Given intra-ocular to cause miosis during eye surgery |
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(Miostat) Choline Ester. Binds M3>M1>M2 and also nicotinic receptors. Not readily metabolized by cholinesterase. Can be used as eye drops to treat glaucoma. |
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(Urecholine) Choline Ester, binds M3>M1>M2 but not Nicotinic. Not readily degraded by cholinesterase. Given PO to treat urinary retention. |
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(Salagen) Cholinergic Alkaloid. Activate M1, M2, and M3 receptors. Treats glaucoma or xerostomia (dry mouth). |
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Cholinergic Alkaloid found in certain mushrooms. Activates M1, M2, and M3 receptors. Symptoms of poisoning include sweating, salivation, nausea, vomiting, visual disturbances, bradycardia, tremors, convulsions, bronchospasm, and possibly coma. |
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Cholinesterase inhibitor. Treats ileus and urinary retention (postop), and Myasthenia Gravis. Also directly activates nicotinic receptors at NMJ. Doesn't reach CNS. Adv effects are convulsions, bradycardia, hypotension, fasciculations. |
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Cholinesterase inhibitor for treatment of glaucoma or atropine OD. Crosses BBB. |
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(Aricept) Cholinesterase inhibitor for diagnosis of myasthenia gravis (very short acting, about 2-10 minutes). |
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Cholinesterase inhibitor that preferentially acts on the CNS to slow progression of Alzheimer's. |
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Organophosphates (Parathion) |
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Irreversible cholinesterase inhibitor. OD can cause confusion, ataxia, convulsions, resp. paralysis, bradycardia, hypotension, miosis, paralysis. Treat by life support and giving atropine, diazepam, and cholinesterase reactivators. |
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Cholinesterase Reactivator (if enzyme did not undergo aging). Works best at NMJ, less at autonomic sites, and not at CNS. Adv effects are muscular weakness, dizziness, headache, nausea. |
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Low dose: activates D1 receptors causing vasodilation in renal, splanchnic, and coronary vessels. Int. Dose: activation of Beta receptors causing increased SV and HR. High dose: Vasoconstriction, nausea. Used to treat Cardiogenic, Neurogenic, or septic shock with poor renal perfusion. |
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Activates alpha and beta receptors causing increased systolic and decr diastolic BP with a net incr in mean BP and HR. Used to treat cardiac arrest and anaphylaxis |
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Mainly activates B1 and alpha receptors causing an increase in systolic and diastolic BP but a reflex decrease in HR. Used in spinal shock and in slowing absorption of local anesthetics. |
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Acts on beta receptors causing an increase in systolic BP, big decrease in diastolic BP, and big increase in HR. Used in emergencies when HR and contractility is low, V-tach, Beta blocker OD. |
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Alpha-1 agonist. Causes incr in BP with decr in HR. Treats postural hypotension, miosis, nasal congestion |
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Alpha-2 agonist (can activate Alpha-1 at high doses). Treat HTN, tobacco/alcohol/opiod withdraw, neuropathic pain, neuropsychiatric diisorders (Touretts, ADD, Autism), sedative. Adv effects: hypertensive crisis when withdrawn, sedation, xerostomia, constipation, sexual dysfxn, rashes. |
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Beta-1 agonist, increases heart contractility and conduction but not HR. Used for heart failure, cardiogenic shock, and stress testing. |
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Beta-2 agonist. Used to treat asthma, COPD, premature labor, and hyperkalemia Adverse effects: Tremor, tachycardia, hypotension, hypoxemia, hypokalemia, hyperglycemia |
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Stimulates release of NE, dopamine, and serotonin. Causes elevation of mood, ability to concentrate, peripheral effects similar to NE. Treats ADD, Narcolepsy OD causes agitation, hyperthermia, seizures, sympathetic overactivity. |
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Blocks reuptake of catecholamines. Central effects similar to amphetamines but shorter and more intense, peripheral effects similar to NE. |
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Releases stored catecholamines, treats nasal congestion, urinary incontinence, hypotension |
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Long acting Beta-2 agonist for treatment of COPD. Side effects are tremors, anxiety, muscle cramps, and palpitations. Paired with fluiticasone in Advair |
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Nonselective irreversible Alpha blocker. Causes vasodilation, enhanced release of NE (but its effects are diminished). For treating pheochromocytoma. Contraindications are urinary urge incontinence, angina, and orthostatic hypotension. |
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Alpha-1 receptor blocker. Treats BPH, overflow incontinence, HTN, Raynaud's, and heart failure. |
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(Flomax) Alpha-1 blocker, treats BPH and urinary obstruction |
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Nonselective Beta blocker. Decreases HR and contraction (Cardiac O2 demand lowered), lowers BP, some bronchoconstriction, decr. Aq humor production, less lipolysis and glycogenolysis (lowers blood sugar). Some local anesthetic activity |
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Nonselective Beta blocker. Some local anesthetic activity. Has partial beta agonist activity. |
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Nonselective Beta blocker. Lowers intraoccular pressure |
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Nonselective Beta blocker. Blocks uptake of K by SkM. Used to treat ventricular and supra-ventricular arrhythmias as well as A-fib/A-flutter |
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Beta-1 blocker. Hydrophillic so has higher bioavailability, lower clearance rate, and doesn't cross BBB. |
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(Lopressor) Beta-1 blocker. some local anesthetic activity |
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Beta-1 blocker. Parenteral administration only. |
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Alpha-Beta blocker. Blocks A1 and has partial agonist activity at B1 and B2. Reduces TPR with minimal effects on HR and CO. |
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Inhibits tyrosine hydroxylase (catecholamine synthesis). Treatment for pheochromocytoma. |
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Beta Receptor antagonists (general) |
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Definition
Mainly used for HTN, arrythmias, and angina. Also good for treating glaucoma, hyperthyroidism, CHF, tremor, pheochromocytoma, migranes, social phobias. |
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Indirect sympathetic activators, causes release of NE. |
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Anti-cholinergic Tertiary Amine. Treats visceral spasms, cholinesterase inhibitor OD, Cardiovascular problems, and used in opthamology |
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Anti-Cholinergic Tertiary Amine. For motion sickness, opthamology, and pre-anesthetic (to decrease bronchial secretions). |
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Anti-Cholinergic Tertiary Amine. For opthamology. |
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Anti-Cholinergic Tertiary Amine. Blocks only M3. For urge incontenence |
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(Cogentin) Anti-Cholinergic tertiary amine for Parkinson's |
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Anti-Cholinergic Quarternary Amine. For visceral spasms, heart disorders, preanesthetic |
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Anti-Cholinergic for treatment of bronchospasm disorders (Asthma and COPD) Combined with albuterol in Combivent |
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Definition
Activates nicotinic receptors at NMJ, CNS, autonomic ganglia, and adrenal medulla. Also stimulates chemoreceptors of carotid bodies, mechanoreceptors of lung, tongue, stomach and skin, thermoreceptors, and pain receptors. Moderate doses incr HR, CO, nausea, peristalsis, resp, bronchoconstriction, ADH release, sweating, miosis Large doses cause tachypnea, tachycardia, resp failure, headache, confusion, falling BP, and weakness. |
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Blocks Nn receptors. Causes incr HR, decreased PVR, hypotension. Used for severe hypertension |
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