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Autonomic Drugs
Autonomic Drugs Sem 3 Mini 1
46
Pharmacology
Professional
09/23/2011

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Term
Acetylcholine
Definition
Binds equally to M1, M2, and M3 receptors and Nicotinic Receptors. Quickly metabolized by cholinesterase.
Given intra-ocular to cause miosis during eye surgery
Term
Carbachol
Definition
(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.
Term
Bethanechol
Definition
(Urecholine) Choline Ester, binds M3>M1>M2 but not Nicotinic. Not readily degraded by cholinesterase. Given PO to treat urinary retention.
Term
Pilocarpine
Definition
(Salagen) Cholinergic Alkaloid. Activate M1, M2, and M3 receptors. Treats glaucoma or xerostomia (dry mouth).
Term
Muscarine
Definition
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.
Term
Neostigmine
Definition
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.
Term
Physostigmine
Definition
Cholinesterase inhibitor for treatment of glaucoma or atropine OD. Crosses BBB.
Term
Edrophonium
Definition
(Aricept) Cholinesterase inhibitor for diagnosis of myasthenia gravis (very short acting, about 2-10 minutes).
Term
Donepezil
Definition
Cholinesterase inhibitor that preferentially acts on the CNS to slow progression of Alzheimer's.
Term
Organophosphates (Parathion)
Definition
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.
Term
Pralidoxime
Definition
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.
Term
Dopamine
Definition
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.
Term
Epinephrine
Definition
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
Term
Norepinephrine
Definition
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.
Term
Isoproterenol
Definition
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.
Term
Phenylephrine
Definition
Alpha-1 agonist. Causes incr in BP with decr in HR. Treats postural hypotension, miosis, nasal congestion
Term
Clonidine/Apraclonidine
Definition
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.
Term
Dobutamine
Definition
Beta-1 agonist, increases heart contractility and conduction but not HR. Used for heart failure, cardiogenic shock, and stress testing.
Term
Albuterol
Definition
Beta-2 agonist. Used to treat asthma, COPD, premature labor, and hyperkalemia
Adverse effects: Tremor, tachycardia, hypotension, hypoxemia, hypokalemia, hyperglycemia
Term
Amphetamines
Definition
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.
Term
Cocaine
Definition
Blocks reuptake of catecholamines. Central effects similar to amphetamines but shorter and more intense, peripheral effects similar to NE.
Term
Ephedrine
Definition
Releases stored catecholamines, treats nasal congestion, urinary incontinence, hypotension
Term
Salmeterol
Definition
Long acting Beta-2 agonist for treatment of COPD. Side effects are tremors, anxiety, muscle cramps, and palpitations.
Paired with fluiticasone in Advair
Term
Phenoxybenzamine
Definition
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.
Term
Prazosin
Definition
Alpha-1 receptor blocker. Treats BPH, overflow incontinence, HTN, Raynaud's, and heart failure.
Term
Tamsulosin
Definition
(Flomax) Alpha-1 blocker, treats BPH and urinary obstruction
Term
Propanalol
Definition
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
Term
Pindolol
Definition
Nonselective Beta blocker. Some local anesthetic activity. Has partial beta agonist activity.
Term
Timolol
Definition
Nonselective Beta blocker. Lowers intraoccular pressure
Term
Sotalol
Definition
Nonselective Beta blocker. Blocks uptake of K by SkM. Used to treat ventricular and supra-ventricular arrhythmias as well as A-fib/A-flutter
Term
Atenolol
Definition
Beta-1 blocker. Hydrophillic so has higher bioavailability, lower clearance rate, and doesn't cross BBB.
Term
Metoprolol
Definition
(Lopressor) Beta-1 blocker. some local anesthetic activity
Term
Esmolol
Definition
Beta-1 blocker. Parenteral administration only.
Term
Labetalol
Definition
Alpha-Beta blocker. Blocks A1 and has partial agonist activity at B1 and B2. Reduces TPR with minimal effects on HR and CO.
Term
Metyrosine
Definition
Inhibits tyrosine hydroxylase (catecholamine synthesis). Treatment for pheochromocytoma.
Term
Beta Receptor antagonists (general)
Definition
Mainly used for HTN, arrythmias, and angina. Also good for treating glaucoma, hyperthyroidism, CHF, tremor, pheochromocytoma, migranes, social phobias.
Term
Tyramine
Definition
Indirect sympathetic activators, causes release of NE.
Term
Atropine
Definition
Anti-cholinergic Tertiary Amine. Treats visceral spasms, cholinesterase inhibitor OD, Cardiovascular problems, and used in opthamology
Term
Scopalamine
Definition
Anti-Cholinergic Tertiary Amine. For motion sickness, opthamology, and pre-anesthetic (to decrease bronchial secretions).
Term
Homatropine
Definition
Anti-Cholinergic Tertiary Amine. For opthamology.
Term
Darifenacin
Definition
Anti-Cholinergic Tertiary Amine. Blocks only M3. For urge incontenence
Term
Benztropine
Definition
(Cogentin) Anti-Cholinergic tertiary amine for Parkinson's
Term
Glycopyrrolate
Definition
Anti-Cholinergic Quarternary Amine. For visceral spasms, heart disorders, preanesthetic
Term
Ipratropium
Definition
Anti-Cholinergic for treatment of bronchospasm disorders (Asthma and COPD)
Combined with albuterol in Combivent
Term
Nicotine
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.
Term
Mecamylamine
Definition
Blocks Nn receptors. Causes incr HR, decreased PVR, hypotension. Used for severe hypertension
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