Term
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Definition
Non-specific BB
Prototype other non-specific BB's are compared to
High lipid solubility
Most effective when high renin
Can cause bronchospasms
Given post-MI, improves survival
Class II anti-arrhythmic -- reduce enhanced automaticity from catecholamines and ischemia, suppresses PVC's
Used for migraines |
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Definition
Non-specific BB
NO production, B-2 agonism |
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Definition
Non-specific BB
High lipid solubility |
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Term
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Definition
Non-specific BB
Intrinsic sympathomimetic activity
Effective with no effect on renin
Decrease HR and CO less than other BB |
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Term
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Definition
Non-specific BB
Open angle glaucoma eyedrops |
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Term
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Definition
B1-specific BB
Class II antiarrhythmic -- off label use, but most commonly used |
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Term
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Definition
B1-specific BB
Class II antiarrhythmic -- ventricular arrhythmias only
Intrinsic sympathomimetic activity
Decrease HR and CO less than other BB |
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Term
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Definition
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Term
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Definition
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Definition
B1-specific BB
Ca entry blockade |
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Term
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Definition
B1-specific BB
B2 agonist activity |
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Term
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Definition
B1-specific BB
Short half-life so given IV
Used for tachycardia/arrhythmia during and after surgery
Acute Tx of supraventricular arrhythmias, ischemia, postop HT |
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Term
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Definition
B1-specific BB
NO production
Favorable effects on carb and lipid metabolism -- drug of choice for HT and metabolic syndrome |
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Term
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Definition
Causes BAR-mediated drop in BP (BB's limit this)
Increase HR and systolic BP, decrease peripheral resistance and diastolic BP
Arrythmias
Parenteral or aerosol
Used in emergencies to stimulate HR in pt's w/ bradycardia or heart block |
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Term
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Definition
Non-specific BB
Class I antiarrythmic/membrane stabilizing
a-1 antagonism, Ca entry blockade, antioxidant activity, prevents lipid peroxidation
Mostly used w/ CHF and HT
Metabolized by CYP2D6 |
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Term
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Definition
Non-specific BB, 3rd generation
a-1 antagonism
Given IV for HT emergencies b/c blocks a-1 |
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Term
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Definition
a-1 specific aB
Used mainly for benign prostatic hyperplasia |
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Term
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Definition
a-1 specific aB
Used mainly for benign prostatic hyperplasia |
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Term
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Definition
a-1 specific aB
Used mainly for HT |
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Term
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Definition
Slight a-1 specific aB
Non-competitive/covalent
Used for HT in pheochromocytoma
Minor blockage of his/ser |
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Term
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Definition
Non-specific aB
Competitive
Small doses, a-2 action; large doses, a-1 action
Used for HT in pheochromocytoma |
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Term
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Definition
Cholinergic nicotinic receptor blocker
Competitive ACh inhibitor |
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Term
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Definition
Cholinergic nicotinic receptor blocker used for Tourette's syndrome
Competitive ACh inhibitor |
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Term
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Definition
a-2 agonist in RVLM
Can be given as patch
Can cause withdrawal HT
Can treat neuropathic pain and ADHD |
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Term
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Definition
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Definition
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Term
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Definition
a-2 agonist prodrug in RVLM
Chelated by Fe supplements
Longest half life of a-2 agonists
Contraindicated in pheochromocytoma -- interferes with catecholamine quantitation
Most common HT drug in used in pregnancy
Only current use is in preeclampsia
Na/H2O retention, positive Coombs |
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Term
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Definition
NE storage depletion -- binds vesicles (VMAT2) in central and peripheral adrenergic neurons
Long-lasting (days to weeks)
Metabolized to inactive products
Sedation, psychotic depression, worsens PUD or ulcerative colitis
Teratogenic, crosses into breast milk
Blocks uptake 2, NE/5-HT depleted |
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Term
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Definition
Blocks tyrosine hydroxylase and thus catecholamine synthesis
Treatment for pheochromocytoma |
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Term
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Definition
| Cholinergic nicotinic receptor blocker -- blocks channel after it opens |
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Term
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Definition
Increase HR and systolic BP, decrease diastolic BP (maybe) and peripheral resistance
Increases CO and O2 consumption
Can cause ventricular arrhythmias, cerebral hemorrhage, angina
Increase diastole duration and coronary BF
Used for hypersensitivity, local anesthetics, cardiac arrest
Not given orally |
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Term
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Definition
Vagal reflex causes bradycardia
Increase systolic and diastolic BP and peripheral resistance
CO unchanged or down, increased stroke volume and coronary BF
Chance of local necrosis |
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Term
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Definition
Does not cross BBB
Made and released in proximal tubule (natriuretic and diuretic)
IV infusion, short duration
Low dose: D1; vasodilation and improved GFR
Medium dose: D1, B1; NE release
High dose: a; vasoconstriction |
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Term
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Definition
Racemic mixture -- B1 agonist
Increase CO/contractility and stroke volume w/out HR change
For short-term Tx of cardiac decompensation
2 min. half life, given IV |
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Term
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Definition
Direct a1 agonist, no B activity
Vasoconstriction w/ reflex decrease in HR and CO
Control hypotension w/ regional or spinal anesthesia |
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Term
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Definition
Mixed activity, direct action at all a and B receptors
Orally active
Hypotension of analgesia
Increase HR and CO
Fatal arrhythmias |
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Term
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Definition
Low dose blockage of M1 pre-syn Ach receptors
High dose blockage of M2 nodal Ach receptors, increase HR
Little effect when no choline esters
Cutaneous vessel dilation at high dose
Prevents vagal reflex
Prevents bradycardia from parasympathomimetic drugs
Helps AV conduction |
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Term
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Definition
Vasodilation, decrease HR, decrease AV node conduction velocity, decrease atrial contractility
Increase Ki channels, block Ca channels (M2)
NO production in vasculature (M3) but vasoconstriction if endothelial damage |
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Term
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Definition
B1-specific BB
Best BB for HT
Glaucoma eyedrops |
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Term
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Definition
Vasodilates arterioles
Reflex increase in SNS, HR/contractility, renin release
Can get palpitations
Use with BB and diuretics (prevent reflex SNS and fluid retention)
IV for eclampsia
Autoimmune reactions |
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Term
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Definition
Vasodilates arterioles by opening K ATP channels
Reflex tachycardia/renin
Hirsutism (hair growth) = Rogaine |
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Term
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Definition
Vasodilates arterioles by opening K channels
Reflex tachycardia/renin
Hyperglycemia b/c inhibits insulin release |
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Term
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Definition
Vasodilates arterioles
Agonist of D1 receptors
Increases intraocular P (avoid in glaucoma) |
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Term
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Definition
Prodrug that forms NO/cGMP to dilate arteries and veins
Decreased pre- and afterload
Causes venous pooling
Emergency Tx for CHF and ventricular failure
Metabolized to cyanide |
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Term
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Definition
ACEI
Increases prostaglandin synthesis
Delays progression of renal disease in type I diabetes
Used post-MI to prevent LV dilation/remodeling |
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Term
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Definition
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Term
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Definition
| ACEI, lysine derivative of elalaprilat |
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Term
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Definition
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Term
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Definition
ARB prodrug
Competitive antagonist of thromboxane A2 receptor, blocks platelet aggregation
Increases excretion of uric acid (good for gout)
Inhibits cytochrome P450 system |
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Term
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Definition
ARB
Only 2% clearance by kidney |
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Term
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Definition
Renin inhibitor
Not used alone -- add ACEI and diuretic |
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Term
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Definition
Ca channel blocker -- phenylakylamine
Selective for myocardium
Slow AV conduction and SA firing, reduce contractility
Can cause AV block (esp. with BB), CHF, constipation
Tx for angina -- decreased HR, contractility, afterload, vasospasm (coronary vasodilation) |
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Term
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Definition
Ca channel blocker -- benzothiazepine
Intermediate selectivity b/t phenylakylamines and dihydropyridines
Less effect on vasodilation and contractility than verapramil
Slows AV conduction and SA firing, reduce contractility
Can cause AV block (esp. with BB), CHF
First pass not as bad (~50% bioavailability)
Tx for angina -- decreased HR, contractility, afterload, vasospasm (coronary vasodilation) |
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Term
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Definition
Ca channel blocker -- dihydropyridine
Selective for vasculature, dilate arteries more than veins
Can cause reflex tachycardia
Peripheral edema, GI irritation, can worsen angina
First pass not as bad (~50% bioavailability)
Tx for angina -- decreased afterload and vasospasm (coronary vasodilation) |
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Term
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Definition
Endothelin 1/2 (vasoconstrictor) receptor antagonist
Used for pulmonary artery HT
Severe liver toxicity, fetotoxicity |
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Term
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Definition
Sublingual, oral, transdermal
Metabolized to NO, venous dilation and coronary vasodilation
Decreased preload, BP and HR unchanged or slightly down/up
Hypotension, reflex SNS with high doses
Interaction w/ Sildenifil (Viagra) -- increase cGMP
Tolerance, give 8-12 hr nitrate free period
Anginal rebound w/ IV withdrawal |
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Term
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Definition
Used for chronic angina, does not relieve acute angina attacks
Fatty acid oxidase inhibitor, late Na current inhibitor
No effect on HR and BP
Increase in BUN/Cr, dizziness, headache, nausea, constipation
Don't use w/ CYP3A4 inhibitors
Increases digoxin [ ] by 50%
Benefits for increasing exercise tolerance and time to onset of angina, used in people who do not get revascularization |
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Term
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Definition
Class 1A antiarrhythmic
Drug-induced lupus, Torsades de Pointe
IV only, acute or short-term Tx only
Hepatic metabolism, bad for slow acetylators
Renal excretion of active metabolite, bad in kidney failure |
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Term
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Definition
Class 1A antiarrhythmic
Torsades de Pointe, diarrhea, autoimmune thrombocytopenia, proarrhythmia |
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Term
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Definition
Class 1A antiarrhythmic
Prominent vagolytic effect -- urinary retention, may worsen heart failure |
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Term
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Definition
Class 1B antiarrhythhmic
Preferentially binds partially depolarized cells
Blocks conduction at high rate
(VTach), so may cause asystole post-MI
Not effective for atrial arrhythmias
Extensive first pass (IV)
Rapid redistribution into fat tissue (loading dose)
CNS toxicity |
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Term
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Definition
Class 1C antiarrhythmic
Increased mortality post MI
Contraindicated in pt. w/ structural heart disease
Proarrhythmic effects
Only given with life-threatening arrhythmias in pt. w/ no structural heart disease |
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Term
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Definition
Class III antiarrhythmic
Analogue of thyroid hormone
Class I-IV antiarrhythmic action
EKG -- everything wide and long
IV has replaced lidocaine as choice for cardiac resuscitation
Very lipophilic, need loading dose
Inhibits Cyp34A
Causes pulmonary fibrosis, dermatitis, eye and thyroid problems |
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Term
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Definition
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