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USMLE1 - Adrenergic/Cholenergics
USMLE1 - Adrenergic/Cholenergic Drugs.
55
Pharmacology
Professional
05/20/2010

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Cards

Term
Alpha 1 (G-protein class and fuctions)
Definition
Sympathetic; Gq; Increase VSMC tone, increase GI/GU sphincter tone, dilate pupils
Term
Alpha 2 (G-protein class and fuctions)
Definition
Sympathetic; Gi; Negative feedback by sympathetics, decrease Insulin
Term
Beta 1 (G-protein class and fuctions)
Definition
Sympathetic; Gs; Increase HR/contractility, Increase lipolysis, Increase Renin
Term
Beta 2 (G-protein class and fuctions)
Definition
Sympathetic; Gs; Increase HR/contractility, Increase lipolysis, Increase Insulin; Decrease VSMC/BSMC tone; Decrease Uterine tone
Term
M1 (G-protein class and fuctions)
Definition
Parasympathetic; Gq; CNS/Enteric NS
Term
M2 (G-protein class and fuctions)
Definition
Parasympathetic; Gi; Decrease HR, decrease contractility of atria
Term
M3 (G-protein class and fuctions)
Definition
Parasympathetic; Gq; Increase exocrine gladular secreation, Increase pupil size, Acomodation, Increase GI motility, Increase blader tone, Decrease VSMC tone
Term
D1 (G-protein class and fuctions)
Definition
Dopamine; Gs; Decrease Renal VSMC tone
Term
D2 (G-protein class and fuctions)
Definition
Dopamine; Gi; CNS NT
Term
H1 (G-protein class and fuctions)
Definition
Histamine; Gq; Puritis, pain, Increase Nasal/bronchial secreations, increase BSMC tone
Term
H2 (G-protein class and fuctions)
Definition
Histamine; Gs; Increase Gastric acid secretion
Term
V1 (G-protein class and fuctions)
Definition
Vasopresin; Gq; Increase VSMC tone
Term
V2 (G-protein class and fuctions)
Definition
Vasopresin; Gs; Increase aquaporins in collecting tubules
Term
Gq works by:
Definition
Activating Phospholipase C which converts Lipids to PIP2 to IP3/DAG. IP3 increase intracellular Ca levels, DAG activates Protein Kinase C
Term
Gs works by:
Definition
Activating Adenylyl Cyclase which converts ATP to cAMC. Increased cAMP Levels activate Protein kinase A
Term
Gi works by:
Definition
Inactivates Adenylyl Cyclase, reduces cAMP levels, therefore reduces Protein Kinase A levels
Term
Hemicholinium
Definition
Prevents Choline uptake, reduces ACh levels
Term
Vesamicol
Definition
Prevents ACh loading in vesicles, reduces ACh levels
Term
Botulinum
Definition
Prevents ACh loaded vesicles from fusing with plasma membrane, reduces ACh levels in synaptic cleft
Term
Metyrosine
Definition
Prevents Tyrosine conversion to DOPA (reduces DOPA/Dopanine/NE/Epi levels)
Term
Reserpine
Definition
Prevents NE loading into vesicles
Term
Guanethide
Definition
Prevents NE loaded vesicles from fusing with plasma membranes
Term
Amphetamines
Definition
Stimulates NE relsease, prevents NE uptake
Term
Cocaine
Definition
Prevents NE uptake
Term
TCAs
Definition
Prevents NE uptake
Term
Bethanechol
Definition
Cholenergic direct agonist,activates bowel/bladder smooth muscles
Term
Carbachol
Definition
ACh direct agonist; release of intraocular pressure
Term
Pilocarpine
Definition
Pile on the sweat/ears/saliva
Term
Metacholine
Definition
Used in Methacholine test for asthma. Sensitivity to small doses is positive.
Term
Neostigmine
Definition
AChE inhibitor; Myasthenia gravis, post OP neuromuscular block reversal; NO CNS
Term
Pyridostigmine
Definition
AChE inhibitor; Myasthenia gravis, NO CNS
Term
Edrophonium
Definition
AChE inhibitor; Diagnosis of Myasthenia gravis, very short acting
Term
Physiostigmine
Definition
AChE inhibitor; Glaucoma and atropine OD. Crosses CNS
Term
Echothiophate
Definition
AChE inhibitor; Glaucoma
Term
AChE inhibitor toxicity (Symptoms and Antedote)?
Definition
DUMBBELSS = Diarrhea, Urination, Miosis, Bronchospasm, Bradychardia, Excitation of muscles, Lacrimation, Sweating, Salivations. Antidote - Atropine
Term
Atropine
Definition
Muscurinic Antagonist; Increase Pupil diameter, cycloplegia, decrease nasal/bronchial secretions, decrease GU/GI motility. Blocks effects of AChE inhibitors. OD: Increase Temp, rapid pulse, dry mouth, dry flushed skin, constipation.
Term
Tropicamide
Definition
Increase pupil size, cycloplegia
Term
Benztropine
Definition
Muscarinic Antagonist; Used in Parkinsons, PARK my BENZ
Term
Scopolamine
Definition
Muscarinic Antagonist; Used in motion sickness.
Term
Ipratropium
Definition
Muscarinic Antagonist; I PRAY I can breath, Asthma, COPD
Term
Oxybutinin
Definition
Muscarinic Antagonist; Reduced urinary urgency
Term
Methscopolamine
Definition
Muscarinic Antagonist; used for peptic ulcers.
Term
Epinephrine selectivity?
Definition
all Alpha 1/2 and beta 1/2
Term
NE selectivity?
Definition
A1, A2>B1
Term
Isoproterenol selectivity?
Definition
B1=B1, IsoB
Term
Dopamine selectivity?
Definition
D1=D2>B>A
Term
Dobutamine selectivity?
Definition
B1>B2
Term
Phenylnephrine (selectivity)
Definition
A1>A2
Term
Selective B2 agonists
Definition
MAST: Metaproterenol, Albuterol, Salmeterol, Terbutaline, Ritodrine
Term
Clonidine/Alpla-methyldopa selectivity?
Definition
Central A2 agonists, decrease central adrenergic outflow
Term
Non selective Alpha blockers
Definition
Phenoxybenzamine (irreversible - used prior to pheochromocytoma surgery to negate effect of spilled chatecholamines)


Phentolamine (reversible)
Term
Selective A1 blockers?
Definition
Prozosin, terazosin, doxazosin
Term
Selective A2 blockers?
Definition
Mitazapine - for depression, sedation
Term
Nonselective B blockers
Definition
Propranolol, timolol, nadolol, pindolol, labitalol
Term
Selective B1 blockers
Definition
A BEAM of B1 blockers: Acebutalol, Betaxolol, Esmolol, Atenolol, Metoprolol
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