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Boards-Autonomic Drugs
Autonomic drugs from Kaplan Review
36
Pharmacology
Graduate
02/18/2012

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Term
Acetylcholine
Definition
M and N receptors; Short half life so no clinical use.
Term
Bethanechol
Definition
M; useful in ileus (postop/neurogenic), and urinary retention.
Term
Methacholine
Definition
M>N; Used to diagnose asthma (bronchial hyperreactivity)
Term
Pilocarpine
Definition
M; Can be used in glaucoma or as a tx. for xerostomia (dry mouth) as in Sjogren's syndrome. Also can be used to induce sweating in a CF suspected patient to measure Cl levels.
Term
Edrophonium
Definition
AchE inhibitor; used to dx. myasthenia; can differentiate myasthenia from a cholinergic crisis.
Term
Neostigmine, pyridostigmine
Definition
AchE inhibitor; quaternary amine (+ charge so no CNS entry). Useful to tx. ileus, urinary retention, myasthenia (long acting), and to reverse nondepolarizing NM blockers (cuarine).
Term
Physostigmine
Definition
AchE inhibitor; Tertiary amine (no charge so enters CNS). Used to treat glaucoma. Antidote in atropine overdose.
Term
Donepezil, tacrine
Definition
AchE inhibitor; Lipid soluble (CNS entry) and used to Tx. Alzheimer's disease. Area of action is the nucleus basalis of Meynert.
Term
Organophosphates (-phate in drug name)
Definition
AchE irreversible inhibitor; some members have clinical use (echothiophate in glaucoma), while others are used as insecticides (malathion, parathion) and as a nerve gas (sarin)
Term
Pralidoxime (2-PAM)
Definition
AchE re-activator; useful only before "aging" occurs which effectively irreversibly phosphorylates AchE.
Term
Atropine
Definition
M receptor antagonist; tertiary amine (enters CNS). Causes decreased secretions, mydriasis (w/ cycloplegia), hyperthermia, tachycardia, sedation, urinary retention/constapation, and behavioral excitation/hallucinations with increasing dose. Tx. AchE inhibitor OD.
Term
Tropicamide
Definition
M inhibitor; useful in ophthalmology to dilate pupils (topical)
Term
Ipratropium
Definition
M inhibitor; useful in asthma and COPD tx.. No CNS entry or change in mucus viscosity.
Term
Benzotropine, trihexyphenidyl
Definition
M inhibitor; lipid soluble (CNS entry) and can be used to tx. parkinsonism and in acute extrapyramidal symptoms induced by antipsychotics.
Term
Scopolamine
Definition
M inhibitor; used in motion sickness because CN VIII is predominantly controlled through Ach. Can cause sedation and anterograde amnesia.
Term
hexamethonium and mecamylamine
Definition
Nn blockers; act on ganglia. Reduce the predominant autonomic tone at a site. Can be used to differentiate a reflex from a drug induced tachycardia (prevents reflex tach or bradycardia).
Term
phenylephrine
Definition
a1 agonist; useful as a nasal decongestant and in ophthalmologic use.
Term
methoxamine
Definition
a1 agonist; used to tx paroxysmal atrial tachycardia by eliciting the vagal reflex to increased BP. Not commonly used today
Term
clonidine, methyldopa
Definition
a2 agonist; useful in mild to moderate hypertension by stimulating prejunctional receptors in the CNS to decrease sympathetic outflow.
Term
Isoproterenol
Definition
b1=b2 agonist; used to treat bronchospasm, heart block and bradyarrhythmias. Can cause flushing, angina and arrhythmias itself.
Term
Dobutamine
Definition
b1>b2 agonist; used in CHF because heart rate can be increased without causing too much edema due to vasodilation.
Term
albuterol and terbutaline
Definition
b2 agonist; useful in asthma.
Term
Ritodrine
Definition
b2 agonist; used in premature labor as a preventative measure. allows for the smooth muscle of the uterus to relax and to contract the sphincter.
Term
Salmeterol
Definition
b2 agonist; useful in asthma prophylactically because of its very slow onset of action.
Term
Norepinephrine
Definition
a1, a2, and b1 agonist. Causes a net increase in blood pressure with resulting reflex bradycardia (positive sloped tracing graph of hr vs. bp.) Reflex bradycardia can be prevented with hexamethonium or mecamilamine.
Term
epinephrine
Definition
a1, a2, b1, b2, agonist; the a2 action is largely irrelevant clinically. Has differing action at different doses: lower BP with increased pulse pressure and HR at low dose, increased pulse pressure, HR, and constant BP at medium dose, and increased BP and TPR at high dose with potential reflex bradycardia (similar to norepinephrine). Can distinguish high dose epinephrine from norepinephrine via administration of an a1 blocker to reverse the hypertension (unmasks b2 receptor activity).
Term
phenoxybenzamine
Definition
a1 and a2 antagonist; noncompetitive. DOC for pheochromocytome pre-surgery.
Term
phentolamine
Definition
a1 and a2 antagonist; competitive.
Term
prazosin, doxazosin, terazosin, tamsulosin.
Definition
a1 antagonist; usee with finesteride for BPH tx. allows for muscle relaxation. Also helps with hypertension which is also usually a problem in males with BPH.
Term
Acebutolol
Definition
B blocker; slightly B1 selective. Partial agonist reduces bradycardia side effect and can cause slight sedation. Also, as a partial agonists it causes no increase in blood lipids. Approved as a class II antiarrhythmic by the FDA.
Term
Atenolol
Definition
B blocker; slightly B1 selective. Water soluble so no sedation (no CNS entry).
Term
Metoprolol
Definition
B blocker; slightly B1 selective. Can cause some sedation, bradycardia, and increased blood lipids.
Term
Pindolol
Definition
B blocker; partial agonist. can cause some slight sedation but because it is a partial agonis it causes no increase in blood lipids.
Term
propranolol
Definition
B blocker; can be very sedative due to extensive CNS entry. Often used to treat anxiety disorders or tremors. Can cause an increase in blood lipids. Approved as a class II antiarrhythmic by the FDA.
Term
Timolol
Definition
B blocker; Can cause moderate sedation and increase in blood lipids. Useful in the treatment of glaucoma to block the action of NE at the ciliary epithelium in the eye (decreased aqueous humor formation).
Term
esmolol
Definition
B blocker; slightly B1 selective. Approved as a class II antiarrhythmic by the FDA.
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