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72 Cards in this Set
- Front
- Back
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Common side effects of M agonists
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Sweating, salivation, lacrimal secretions
Nausea, vomiting, diarrhea Bladder tightness Blurred vision Bronchoconstriction |
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Bethanechol
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M agonist
Choline ester + quaternary amine Poor oral/BBB Used for stimulus of persistalsis in GI tract Treat urinary retention |
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M agonist contraindications
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Peptic ulcer
Coronary insufficiency |
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Pilocarpine
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M agonist
Alkaloid + tertiary amine Absorbed orally and BBB Treat dry mouth, glaucoma topically Side effect = sweating |
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Cevimeline
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M3 agonist - dry moth
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Carbachol
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N&M agonist
Diagnosis of asthma Choline ester |
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Nicotine toxic effects
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Nausea, vomiting, convulsions, constipation, flatulence
Sleep disturbance, nightmares, psychosis |
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Varencline
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Partial N agonist, reduce nicotine cravings
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Edrophonium
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ChE inhibitor, quarternary ammonium alcohol, IV
Very short duration Reversal of NMJ blockade after surgery Diagnosis of myasthenia gravis |
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Neostigmine
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ChE inhibitor, carbamate, quaternary amine
Poor oral, BBB, 30min-6hrs Treatment of myasthenia gravis Reveral of NMJ blockade after surgery |
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Donepezil
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ChE inhibitor
Carbamate, lipid soluble, Alzherimer's |
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Phyostigmine
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ChE inhibitor, carbamate
Tertiary amine, oral and BBB 30min-6hr Topical glaucoma treatment |
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Echothiophate
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ChE inhibitor, organophosphate
Long duration Not lipid soluble Glaucoma emergencies |
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Scopolamine
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M antagonist
Motion sickness patches Pre-anesthetic Enters CNS much easier than atrophine |
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Tolterodine
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Selective M3 antagonist
Low lipid solubility - no CNS effects Overactive bladder |
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Oxybutin
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M antagonist
Prevent bladder spam after prostate surgery |
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Diphenoxylate
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Used with atropine for diarrhea
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Glycopyrrolate
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Muscarinic antagonist
Block vagal response during visceral surgery Reduces side-effects of cholinergics in myasthenia gravis pts |
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Dicyclomine
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Muscarinic antagonist
Antispasmotic in GI tract |
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Solifenacin
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Selective M3 antagonist
Overactive bladder Less effect on salvation |
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Ipatropium
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Muscarinic antagonist
COPD and Asthma |
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Tropicamide
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Muscarinic antagonist
Pupil dilation and cyclopegia for eye exam |
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Ephedrine
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a&B agonist
longer duration and more bioavailable than epinephrine Increased HR, BP Cardiac arrest, complete heart block |
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Phenylephrine
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Selective a1 agonist
Nasal decongestant Pupil dilation for exam |
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Psuedoephedrine
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a1 agonist
Similar to phenylephrine, may be more effective |
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Clonidine
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a2 agonist
oral or transdermal patch Inhibits release of NE Treats: Hypertension, alcohol/drug addiction, menopausal hot flashes |
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Apraclonidine
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a2 agonist
Glaucoma |
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Dobutamine
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B1 agonist
Stress test |
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Albuterol
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B2 agonist
Asthma |
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Terbutaline
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B2 agonist
Rarely used for asthma but memorize it anyways |
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Ritrodine
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B2 agonist
Suppress premature labor |
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Amphetamine
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Increases release of NE and DA
CNS stimulation, decrease appetite, decrease need for sleep, increased activity, euphoria |
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Methylphenidate (Ritalin)
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Similar to amphetamine
ADHD - paradoxical decrease in activity |
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Cocaine
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Inhibits reuptake of NE and DA
Similar to amphetamine MI, stroke, arrythmias, psychosis, hypertension |
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Tyramine
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Increases release of catecholamines
Metabolized by MAO in liver/GI Norepinephrine-like effect Severe hypertensive crisis in pts taking MAOIs |
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Dopamine
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Vasodilation of renal vasculature, coronaries, mesenteric
At high doses - activate B1 receptors, increased HR and contractility |
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Fenodolpam
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D1 agonist
Short term BP reduction in sever hypertension |
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d-Tubocurarine
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Non-depolarizing competitive NMJ blocker
Prototype Slow onset, long duration Histamine release can cause vasodilation, bronchospasm, vagal response and ganglionic blockade |
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Pancuronium
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Non-depolarizing competitive NMJ blocker
Slow onset, long duration |
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Vecuronium
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Non-depolarizing competitive NMJ blocker
Faster onset, intermediate duration Metabolized by liver |
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Cisatracurium
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Non-depolarizing competitive NMJ blocker
Faster onset, intermediate duration Most commonly used - spontaneously hydrolyzed, no histamine release |
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Rocurium
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Non-depolarizing competitive NMJ blocker
Rapid onset, intermediate duration Intubation |
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Succinlycholine contraindications
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Patients with extensive soft tissue damage/burns
Rhabdomyolysis Spinal cord injuries with para- or quadriplegia Muscular dystrophy Children <8 unless emergency |
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Succinylcholine
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De-polarizing NMJ blocker
(see chart for a billion details) |
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Hexamethonium
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Ganglion blocker
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Adverse effects of succinylcholine
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Hyperkalemia --> cardiac arrest
Muscarinic/nicotinic cross stimulation --> bradycardia, arrythmias Fasiculations --> muscle pain, regurgitation Increased intraocular pressure |
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Mecamylamine
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Ganglion blocker
Not used clinically but makes for a fun review of autonomics! |
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Drug interactions of NMJ blockers
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Enhancing effects - inhaled/local anesthetics (isoflurane>NO), Aminoglycoside, Tetracycline, Ca-channel blockers
Succinylcholine + halothane = malignant hyperthermia |
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Phenoxybenzamine
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Irreversible alpha antagonist
Pheochromocyoma |
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Phentolamine
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Reversible alpha antagonist
Short-term treatment of hypertensive crisis Side effects - abdominal pain/gastric stimulation |
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Prazosin
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Reversible a1 antagonist
Hypertension, benign prostatic hyperplasia Short half-life, BID First dose phenomenom most pronounced |
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Terazosin
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Reversible a1 antagonist
Hypertension, benign prostatic hyperplasia (reduce size of prostate) Long half life, QD First dose phenomenom |
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Doxasozin
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Reversible a1 antagonis
tHypertension, benign prostatic hyperplasia (reduce size of prostate) Long half life, QD First dose phenomenom |
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Tamsulosin
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a1A antagonist in prostate
Benign prostatic hyperplasia Relaxes prostate, urinary sphincter, base of bladder Side affect: trouble ejaculating |
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Side affects of alpha antagonists
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Nasal congestion
Trouble ejaculating Postural hypotension Dizziness |
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Yohimbine
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a2 agonist
Increased NE, marketed for increased libido Dangerous for men w/hypertension |
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Metabolism of propanolol
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CYP
Extensive first pass metabolism 90% protein bound Half-life 3.5-6 hrs Increased metab - barbituates, smoking, phenytoin Decreased metab - cimetidine |
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Uses of propanolol
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Hypertension
Decreased morbidity post-MI, CHF Decreased angina, arrythmias Migraine prophylactic Hyperthyroidism Decrease portal vein pressure - cirrhosis Tremor |
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Propanolol
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Non-specific beta blocker
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Beta-blocker side effects
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Bronchoconstriction
Hypotension, bradycardia Sedation, depression Increased VLDL, decreased HDL Decreased ability to recover from hypoglycemia |
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Timolol
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Non-specific beta blocker
Can be used systemically like propanolol or topically for glaucoma Asthma = contraindication |
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Metropolol and Atenolol
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Selective B1 antagonists
Hypertension, post-MI, migraine Better exercise tolerance, reduced risk of hyperglycemia |
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Pindolol and Acetabulol
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Beta blockers with ISA (acetabulol specific for B1)
Hypertension, angina Less likely to cause bronchoconstriction or effect lipids |
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Esmolol
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Selective B1 antagonist
Very short duration, used in urgent situation or for critically ill |
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Betaxolol
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Selective B1 antagonist
Glaucoma, less likely to cause bronchoconstriction than timolol |
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Nebivolol
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Selective B1 antagonist
Most selective, fewer side effects Vasodilation via NO Reduces cholesterol, TAGs, blood glucose |
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Labetalol
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Combined alpha and beta blocker
Decrease in BP without compensatory increase in HR Chronic or emergency |
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Carvedilol
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Combined alpha and beta blocker
Decrease in BP without compensatory increase in HR Decreases effects of ROS and mitogenesis of VSMC Hypertension, CHF, post-MI |
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Guanethidine
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Taken into nerve terminal and displaces NE from vesicles, depleting NE stores
No longer used clinically |
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Reserpine
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Inhibits reuptake of amines depleting the stores of serotonin and NE
No longer used clinically |
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Metyrosine
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Inhibits dopamine and downstream NE and E synthesis
Pheochromocytoma |
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Glaucoma treatments
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Prostaglandin analogues
Beta-blockers - timolol, betaxolol a2 agonists - apraclonidine, brimonidine Carbonic anhydrase inhibitors Cholinergic agonists - pilocarpine, phyostigmine, echothiophate |
