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54 Cards in this Set

  • Front
  • Back
Acetylcholine
Endogenous Nicotinic and Muscarinic receptor agonist.
No clinical use since fast hydrolysis, broad activity.
Methacholine
M1 receptor agonist.
Diagnosis of bronchial hyperreactivity (triggers wheeze)
Bethanecol
Muscarinic receptor agonist.
Rx ileus (postop/neurogenic, *not in mechanical block) urinary retention
Pilocarpine
Muscarinic receptor agonist.
Rx glaucoma (topical), xerostoma (dry mouth, ex. in Sjogren's disease)
Edrophonium
AchE inhibitor.
Dx of myasthenia gravis (improves w/ drug) vs. cholinergic crisis (doesn't improve)
Short acting, so safe to use as test.
Physostigmine
AchE inhibitor.
tertiary amine (enters CNS).
Rx- glaucoma, antidote in atropine overdose
Neostigmine,
Pyridostigmine
AchE inhibitor.
quaternary amine (no CNS penetration)
Rx- ileus, urinary retention, myasthenia gravis, reverses nondepolarizing NMJ blockers (ex. curare)
Donezepil,
tacrine
AchE inhibitor.
lipid soluble (enters CNS)
Rx- Alzheimer's
Organophosphates
(sarin, malathion, parathion)
AchE inhibitor.
Suicide inhibitors of AchE, irreversible after "aging"
Pesticides (malathion, parathion) or chemical warfare nerve gas (sarin)
Atropine
Muscarinic antagonist.
Antispasmodic, antisecretory, antidiarrheal, management of AchE inhibitor OD
long half-life (24-36hrs)- not great for ophthamology
Tropicamide
M antagonist
Ophthamological dilation (topical)
Ipratropium
M antagonist
Asthma and COPD (inhalational)
No CNS entry
Scopolamine
M antagonist
Motion sickness. Side effects- sedation and short-term memory loss
Benztropine,
trihexyphenidyl
M antagonist
Rx for parkinsonism (primary or due to antipsychotic medications)
lipid-soluble (CNS penetrant)
Hexamethonium
Nicotinic neuronal receptor antagonist
wipe out entire ANS function
prevent baroreceptor reflex
Mecamylamine
Nicotinic neuronal receptor antagonist
wipe out entire ANS function
prevent baroreceptor reflex
Methyl-p-tyrosine
Inhibits tyrosine hydroxylase --> prevents formation of DOPA from tyrosine --> decreases Dopamine and NE synthesis
MAO inhibitors
prevent degradation of NE mobile pool --> increased potential for NE release via reuptake channel openers
NE Releasers
release NE from mobile pool into synapse
reserpine
prevents vesicle loading of NE, dopamine, serotonin
antipsychotic, anti-HTN
guanethidine
prevents NE vesicle release into synapse
alpha-1 receptors
Eye- radial muscle contraction --> mydriasis (dilation)
Vessels- contraction --> increased TPR, BP
Bladder- urinary retention
Male sex organs- ejaculation
Liver- increased glycogenolysis
Kidney- decreased renin release
alpha-2 receptors
Presynaptic nerve terminal- reduce neurotransmitter release (NE, etc.)
Platelets- increase aggregation
Pancrease- decrease insulin secretion
beta-1 receptors
Heart- increased conductance, HR, CO
Kidney- increase renin release
Eye- increase aqueous humor, increase IOP
beta-2 receptors
Blood vessels- vasodilation, decreased TPR, BP
Uterus- relaxation
Bronchioles- dilation
Pancreas- increased insulin secretion
Liver- increased glucose and lipid mobilization
Skeletal muscle- increased contractility (potentially tremors), increased glycogenolysis
phenylephrine
a1 agonist
nasal decongestant
ophthalmic- mydriasis w/o cycloplegia
methoxamine
a1 agonist
Rx paroxysmal atrial tachycardia via vagal reflex activation (like a chemical carotid massage)
clonidine
a2 agonist
Rx HTN via decreased CNS sympathetic signaling
like methyldopa
methyldopa
a2 agonist
Rx HTN via decreased CNS sympathetic signaling
like clonidine
Isoproterenol
nonselective B agonist
Rx bronchospasm (B2), heart block and bradyarrythmia (B1
Side effects- flushing (B2), angina, arrythmia (B1)
Dobutamine
B1>B2 agonist
Rx CHF via increased CO
Salmeterol,
Albuterol,
Terbutaline
B2 selective agonist
Asthma
salmeterol=slow-acting (prophylaxis only)
Ritodrine
B2 selective agonist
Prevent premature labor
Norepinephrine
a1, a2, B1 agonist
increases BP and HR, possibly eliciting reflex bradycardia
*no B2 effect!- can't decrease BP
Epinephrine (low dose)
a1, a2, B1, B2 (B1+B2 predominate at low dose)
increased HR, decreased BP
looks like isoproterenol
Epinephrine (medium dose)
a1, a2, B1, B2 (a1 and B2 cancel out, B1 predominates)
increased HR with no change in BP
looks like dobutamine
Epinephrine (high dose)
a1, a2, B1, B2 (a1 overshadows B2, a1 and B2 predominate)
increased HR and BP
Epinephrine reversal
addition of a1 antagonist to epinephrine changes response from hypertention to hypotension, maintain high HR
*addition of a1 antagonist to NE will bring BP back to baseline
Tyramine
NE releaser
interaction with MAOA inhibitors --> hypertensive crisis
(tyramine, amphetamines, ephedrine)
Amphetamines
NE releasers
interaction with MAOA inhibitors --> hypertensive crisis
(tyramine, amphetamines, ephedrine)
Ephedrine
NE releaser
interaction with MAOA inhibitors --> hypertensive crisis
(tyramine, amphetamines, ephedrine)
cocaine
NE reuptake inhibitor
increase NE in synapse (increased a1 and b1 responses)
tricyclic antidepressants
NE reuptake inhibitor
increase NE in synapse (increased a1 and b1 responses)
phentolamine
nonselective alpha antagonist
competitive inhibitor
Rx HTN
phenoxybenzamine
nonselective alpha antagonist
noncompetitive inhibitor
Rx pheochromocytoma, HTN
Prazosin, doxazosin, terazosin, tamsulosin
Selective a1 antagonist
Rx HTN, benign prostatic hyperplasia (manage urinary retention symptoms)
Yohimbine
Selective a2 antagonist
Rx- HTN, sexual dysfunction
Mirtazapine
Selective a2 antagonist
antidepressant, also causes weight gain
propanolol
nonselective beta antagonist
MI, HTN, CHF, glaucoma
CNS penetrant- sedative effect
atenolol
selective B1 antagonist
MI, HTN, CHF, glaucoma
not CNS penetrant
pindolol
nonselective B antagonist
MI, HTN, CHF, glaucoma
partial agonist- no hyperlipidemia (like acebutolol)
acebutolol
selective B1 antagonist
MI, HTN, CHF, glaucoma
parital agonist- no hyperlipidemia (like pindolol)
Labetalol, carvedilol
a1 and b antagonists
Rx CHF
sotalol
antiarrhythmic