Autonomic Drugs Flashcards by Esther Chung

Non-selective Alpha blockers?

Phenoxybenzamine (irreversible), phentolamine (reversible)

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What is phenoxybenzamine? Application? Tox?

Irreversible non-selective alpha blocker. Use preoperatively for pheochromocytomas to prevent hypertensive crisis
Toxicity: orthostatic hypotension, reflex tachycardia

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What is phentolamine? Application?

Reversible non-selective alpha blocker. Use for patients who are on MAO inhibitors who eat tyramine containing foods to prevent serotonin syndrome

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Alpha1 selective blockers?

(ending in -osin). Prazosin, terazosin, doxazosin, tamsulosin

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Alpha1 selective blockers used for? tox?

Prazosin, terazosin, doxazosin, tamsulosin. Urinary symptoms of BPH, hypertension (except tamsulosin).
Toxicity: 1st dose orthostatic hypotension, dizziness, headache

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Alpha2 blocker? what is it used for? Toxicity?

Mirtazipine. Used for depression. Toxicity: sedation, increased serum cholesterol, increased appetite.

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Effects of beta blockers on angina pectoris?

Decreases heart rate and contractility, resulting in decreased oxygen consumption

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Effects of beta blockers on MI? Which ones are frequently used

Metoprolol, carvedilol and bisoprolol. Decreases mortality

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Effects of beta blockers on SVT? Which ones are frequently used

Metoprolol and esmolol. Decreases AV conduction velocity (class II anti-arrhythmic)

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Effects of beta blockers on hypertension?

Decreases cardiac output, decreases renin secretion (due to beta 1 receptor blockade on JGA cells)

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Effects of beta blockers on CHF

Slows progression of chronic failure

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Effects of beta blockers on glaucoma? What drug is used?

timolol, betaxolol, carteolol. Decreases aqueous humor secretion synthesis

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Which beta blockers have beta1 selectivity

generally antagonists go from A TO M for beta 1 blocker activity (beta 1 for first HALF of alphabet)
Acebutolol (partial), atenolol, betaxolol, esmolol, metoprolol

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Which beta blockers are nonselective?

N through Z = beta 2, second half. Nadolol, pindolol (partial), propanolol, timolol

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What are carvedilol and labetalol

nonselective alpha AND beta antagonists.

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What is nebivolol?

beta 1 blockade for cardiac-selective blockade with stimulation of beta three receptors = which activate NO synthase in vasculature.

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What are the direct cholinomimetics?

Bethanechol, carbechol, pilocarpine, methacholine

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Bethanechol - application? Action?

Direct cholinomimetic
Application: Post-operative ileus, neurogenic ileus, urinary retention
Action: activates bowel and bladder smooth muscle. resistant to AchE. bethany call me (bethanchol) to activate your Bowels and Bladder

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Carbachol - application? Action?

Cholinomimetic

Application: glaucoma, pupillary constriction, and relief of ocular pressure. CARbon copy of acethyCHOLine

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Pilocarpine - application? Action?

Cholinomimetic
Application: Potent stimulator of tears, sweat, and saliva. Open and closed angle glaucoma.
Action: Contracts ciliary muscle (open angle glaucoma), pupillary sphincter muscle (closed angle glaucoma). resistant to AchE. you cry, drool sweat and your PILlOw

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Methacholine - application? Action

Cholinomimetic
Application: Challenge test for asthma diagnosis.
Action: Stimulates muscarinic receptors in airway when inhaled.

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Indirect cholinomimetics examples?

Anticholinesterases. Neostigmine, pyridostigmine, physostigmine, donepezil, rivastigmine, galantamine, edrophonium.

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Neostigmine - application and action?

Anticholinesterase
Application: Postoperative and neurogenic ileus, urinary retention, MG, reversal of NM blockade (post operative).
Action: increases endogenous Ach. NEO cns = NO cns penetration

Pyridostigmine - application and action?

Anticholinesterase
Increases endogenous ACh.
Application: MG (long acting), does not penetrate CNS
pyRIDostigmine gets RID of Mg

Physostigmine - application and action?

Anticholinesterase Application: Anticholinergic activity and toxicity (crosses BBB into CNS) Action: increases endogenous Ach. PHYSostimine PHYses atropine overdose.

Donepezil, rivastigmine, galantamine

Anticholinesterase | Applications: Alzheimers. increases endogenous Ach

Edrophonium

Historically, dx of MG. extremely short acting form of anticholienstrase.

Adverse effects of cholinomimetics in general?

Exacerbation of COPD, asthma and peptic ulcers

Cholinesterase inhibitor poisoning often due to? Causes what?

Often due to organophoshphates such as parathion that IRREVERSIBLY inhibit AchE Causes DUMBBELSS diarrhea, urination, miosis, bradycardia, bronchospasm, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation

organophosphate poisoning antidote?

Atropine (muscarininc antagonist) + pralidoxime (regenerates AchE if given early)

Example of muscarinic antagonist used in eye? Application?

Atropine, homatropine, tropicamide | Produces mydriasis and cycloplegia (paralysis of ciliary muscle/decreased accommadation)

Example of muscarinic antagonist used in CNS?

Benztropine - used for parkinsons PARK my BENZ

Example of muscarinic antagonist used in CNS for motion sickness

Scopolamine

Example of muscarinic antagonist used for COPD/asthma

ipratropium, tiotropium I PRAy i can breathe soon

Example of muscarinic antagonist used for GU? application?

oxybutynin. Reduces urgency in mild cystitis and reduces bladder spasms.

What is glycopyrrolate? Affects what organ system? Applications?

Muscarinic antagonist used in GI respiratory systems. | Parenteral: preop use to reduce airway secretions. Oral: drooling, peptic ulcer.

What is atropine? What is used for?

Muscarinic antagonist. used to treat bradycardia and for opthalmic applications.

What does atropine NOT block

nicotinic receptors, i.e., skeletal and cns excitation

What does atropine do for the 1) eye 2) airway 3) stomach 4) gut 5) bladder

1) mydriasis 2) decrease secretion 3) decrease acid secretion 4) decrease motility 5) decrease urgency in cystitis

Atropine Side effects can be remembered with what phrase?

HOT as a hare (increased body temperature due to DECREASED SWEATING), DRY as bone, BLIND as a bad (decreased ciliary muscle contraction => less accommodation => cycloplegia), MAD as a hatter Can cause acute angle closure glaucoma, urinary retention in men with prostatic hyperplasia, and hyperthermia in infants

What is jimson weed?

Garnders pupil (mydriasis) due to it's anticholinergic activity.

Epinephrine? what receptors does it work on? Application? what effects predominate at high doses

Beta>alpha | Applications: anaphylaxis, open angle glaucoma, asthma, hypotension. alpha effects predominate at high doses.

NE? What receptors does it work on? Application?

alpha1>alpha2>beta1 | Application: hypotension (decreases renal perfusion)

Isoproterenol? What receptors does it work on? Application?

Beta1=Beta2 | Applications: Electrophysiologic evaluation of tachyarrythmias. Can worse ischemia.

Dopamine? What receptors does it work on? Application?

D1=D2>beta>alpha | Unstable bradycardia, heart failure, shock; inotropic and chronotropic alpha effects predominate at high doses

Dobutamine? What receptors does it work on? Application?

Beta1>beta2, alpha. | Applications: heart failure (inotropic>chronotropic), cardiac stress testing

Phenylephrine? What receptors does it work on? Application?

Alpha1>alpha2 | Applications: hypotension (vasocontrictor), ocular procedures (mydriatic), rhinitis (decongestant)

Albuterol, salmeterol, terbutaline? What receptors does it work on? Application?

beta2>beta1 Albuterol for acute asthma, salmeterol for long-term asthma or COPD control, terbutaline to reduce premature uterine contractions

What are examples of indirect sympathomimetics?

Amphetamine, ephedrine and cocaine?

Amphetamine as indirect sympathomimetic - Effect? Applications

Effect: indirect general agonist, reuptake inhibitor, also releases stored catecholamines. Application: narcolepsy, obesity, ADD

Ephedrine as indirect sympathomimetic - Effect? Applications?

Effect: indirect general agonist, releases stored catecholamines. Application: nasal congestion, urinary incontinence, hypotension

Cocaine as indirect sympathomimetic indirect sympathomimetic - Effect? Applications?

Effect: indirect general agonist, reuptake inhibitor. Applications: causes vasoconstriction. local anesthesia. never give beta blockers if cocaine intoxication is suspected due to unopposed alpha1 activation and extreme hypertension

What are sympatholytics?

alpha2 agonists

What is clonidine? Application? Toxicity?

alpha 2 agonist - sympatholytic. Application: hypertensive urgency (limited situation, does not decrease renal blood flow. Used for ADHD, severe pain. Tox: CNS depression, bradycardia, hypotension, respiratory depression, small pupil size.

What is alpha methyldopa?

Alpha2 agonist/sympatholytic Application: hypertension in pregnancy/safe in pregancy Toxicity: direct coombs + hemolytic anemia, SLE like syndrome.