Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
68 Cards in this Set
- Front
- Back
How do sympathoplegics work?
|
They decrease sympathetic outflow from vasopressors, still sensitive to baroreceptor control (no postural changes)
|
|
What is the MOA of Methyldopa?
|
Analog of L-dopa, false analog of DA, NE -- Stimulates CNS alpha2 receptors: dec PVR, dec HR/CO, dec renal vascular resistance
|
|
What are the kinetics of methyldopa?
|
Delayed effect bc must go through gut to brain by aromatic aa transporters, Long lasting-- metabolites stored in nerve endings
|
|
What are the 3 toxicities of methyldopa? How long should it be used?
|
1) CNS - sedation! depression, nightmares, vertigo 2) Lactation- inc prolactin 3) POSITIVE Coombs (>12 mo's): hemolytic anemia, hepatitis, drug fever. Change drug after pregnancy
MOTHER-dopa |
|
When is methyldopa used?
|
Tx HTN in pregnancy
|
|
What is clonidine's MOA?
|
Partial agonist at alpha2 receptors in medulla: dec PVR, dec HR.
Dec BP while maintaining RBF (unlike methyldopa) May cause some vasoconstriction Dec circulating levels of catecholamines Also dec renin secretion by affecting sympathetic activity |
|
How is clonidine given?
|
Oral or PATCH/transdermal form
|
|
What are the toxicities of clonidine?
|
Rash at patch, CNS, REBOUND HTN: tachycardia -- need to wean off or tx with alpha/beta blockers
|
|
When is clonidine CI? What is its use?
|
Severe HTN bc partial agonist. Use for HTN.
|
|
What is the MOA of peripheral adrenergic neuronal blockers? What are the 2 drugs?
|
Lower BP by preventing release of NE from postsynaptic symp neurons.
Guanethidine, Reserpine |
|
What is the MOA of guanethidine?
|
Enters nerve ending, concentrates in vesicles and displaces NE to dec release of NE from endings (dec CO and PVR) -- Severe reflex RAAS.
guaNEthedine |
|
What drugs interfere with guanethedine?
|
Cocaine, Amphetamine, Tricyclic antidepressants, phenothiazines, phenoxybenzamine -- inhibit catecholamine reuptake pump (similar action)
|
|
What are the toxicities of guanethidine?
|
Sympathectomy: orthostatic hypotension, delayed ejaculation (sexual dysfunction)
|
|
Where is guanethidine CI? What is its use?
|
Pheochromocytoma and drug interactions: Sympathomimetics, leads to HTN. Used for severe HTN a long time ago (powerful!)
|
|
What is the MOA of reserpine?
|
Decreases uptake of amines into vesicles, deplete stores. NE, DA, 5HT. Lead to hypotensive effects (dec CO and PVR) with possible sedation, Parkinsonism
|
|
What are the toxicities of reserpine?
|
Minimal postural HTN, mental effects, diarrhea..
|
|
Where are beta blockers used?
|
HTN
Cardiac: Ischemic heart dz and angina, CHF, Arrythmias Kidneys (dec RBF): chronic kidney dz, diabetic nephropathy |
|
What are the toxicities of beta blockers?
|
Excess beta block: dec CO, heart block, bradycardia, bronchospasm, hypoglycemia, hyperkalemia during exercise, CNS depression, lipids, sexual dysfunction, postural hypotension
|
|
When do you use beta blockers?
|
Combine with vasodilators to block reflex tachycardia
LVH Reduce mortality after MI |
|
Where are beta blockers CI?
|
Caution with asthma, diabetes, COPD, PVD, depression, sinus bradycardia
|
|
What are possible properties of beta blockers that you should take into account?
|
Selective versus nonselective
Partial agonism Lipid solubility: CNS penetration |
|
What are some properties and uses of propanolol?
|
Nonselective beta blocker, dec renin production
Use in HTN, ischemic heart dz |
|
What are some properties and uses of metoprolol?
|
Selective beta blocker, cardioselective
Use in asthmatics if worried with propanolol |
|
What are the uses of nadolol and atenolol?
|
Nadolol-non, Atenolol-selective
Not use much due to renal failure, dose change bc excreted in urine |
|
What are the uses of betaxolol and bisoprolol?
|
Selective, long half-life
Use in pts with renal failure (metab in liver) |
|
What are the uses of pindolol, acebutolol and penbutolol?
|
Partial agonism: dec vascular resistance (partial beta2 agonism), doesn't reduce CO as much
Uses: HTN with CHF |
|
What are the uses of labetalol and carvedilol?
|
Comb beta and alpha1 blocker: dec vascular resistance w/o change in CO or HR bc agonist effects.
Labetalol: HTN emergency (IV), also PREGNANCY Carvedilol: Heart failure |
|
What is the use of esmolol?
|
Selective, rapid IV.
Use: intra/post-operative HTN, HTN crisis (tachycardia) |
|
What are the 3 selective alpha blockers for HTN?
|
Prazosin, Terazosin, Doxazosin
|
|
What is the MOA of selective alpha blockers?
|
Selective alpha1 blocker, dilates vessels, improve lipids.
|
|
What are the toxicities of alpha-blockers?
|
INC risk of HF when monotx, BAD.
Postural hypotension RAAS (must use with diuretic) First dose phenomenon (rapid fall in BP) -- start with low dose at bedtime Dizziness, palpitations, HA, lassitude Avoid reflex tachycardia with beta blockers |
|
What are the 2 nonselective alpha blockers?
|
phen = phentolamine, phenoxybenzamine
Phentolamine dx pheochromocytoma (short), phenoxybenzamine tx |
|
What are the effects of vasodilators and why are they not ideal?
|
Directly dilate arterioles, reflex tachycardia (beta blockers stop), RAAS (diuretics stop)
|
|
What are the 2 oral vasodilators? The 3 IV vasodilators?
|
Hydralazine, Minoxidil
Nitroprusside, Diazoxide, Fenoldopam |
|
What is the MOA and kinetics of hydralazine?
|
Dilates arterioles only, metab first pass by liver
Metab by acetylation: rapid/slow |
|
What toxicities do hydralazine cause?
|
LUPUS like syndrome: check ANA levels- rash, myalgia, arthralgia, fever
DOSE-dep and REVERSIBLE Also, HA, nausea, anorexia, palpitations, edema, angina from reflex tachycardia hydrALAzine - check ANA levels |
|
When can hydralazine be used?
|
Pregnancy!
|
|
What is the MOA of minoxidil? What are its uses?
|
Prodrug, opens K channels in SM, hyperpolarizes and relaxes vascular SM (only arterioles)
Severe HTN (use with loop diuretics, beta blockers to avoid reflex responses) |
|
What toxicities does minoxidil cause?
|
Compensatory tachycardia, angina, RAAS with possible pericardial effusion
Hirsuitism Postural hypotension MANoxidil is a vasodilator |
|
What is the MOA of sodium nitroprusside?
|
Release of NO stimulates guanylyl cyclase and increases cGMP, relax SM, dilate BOTH arterioles and venules (CO same)
|
|
What is the toxicity of sodium nitroprusside?
|
Renal failure: drug goes into RBC, release of CN, metabolized to THIOCYANATE -- cleared by kidney but accumulates. Weak, disoriented, psychosis, spasms, convulsions
|
|
When is sodium nitroprusside used?
|
HTN emergencies (IV) and severe HF -strong drug! Start on oral meds at same time so Nitroprusside minimized
|
|
What is the MOA and usage of diazoxide?
|
Open K channels, hyperpolarize and relax SM in arterioles
IV, not used long term or often bc profound hypotension and RAAS |
|
What is the MOA of fenoldopam?
|
D1 (dopa) agonist, causes dilation of peripheral arteries and natriuresis
fenolDOPAm |
|
What are the CI of fenoldopam? Toxicities? Uses?
|
Glaucoma (increases IOP!)
Also, reflex tachycardia, HA, flushing Use for HTN emergencies, postop HTN |
|
What is the MOA of Ca channel blockers?
|
Slow influx of Ca in smooth muscles: L-Type channel for CARDIAC and VASCULAR effects
Slow AV conduction, dec inotropy, slow SAN Relax/dilate vasculature |
|
What kind of effects do the dihydropyridines have mostly?
|
Vascular effects, more effective if high BP from SM contraction
Nefidipine, amlodipine, felodipine, isradipine, nicardipine, nisoldipine |
|
Which dihydropyridine causes reflex tachycardia and gum hypertrophy? Which dihydropyridine is best?
|
Nifedipine-bad choice. Use Amlodipine!
|
|
What is verapamil's main effect? What AE does it cause?
|
Phenylalkylamine Ca channel blocker-- primarily cardiac. Use for arrhythmias and slow heart
Causes constipation |
|
What is diltiazem's main effect?
|
Benzothiazepine Ca channel blocker -- intermediate effects on cardiac and vascular.
Use for ischemia, HTN, angina |
|
What are the toxicities of Ca channel blockers?
|
Inapprop cardiac effects (cardiac arrest, heart block, CHF) and inapprop vasodilation (HA, flushing, edema, postural hypotension)
|
|
What drug interactions do the Ca channel blockers diltiazem and verapamil have?
|
Beta-blockers worsen cardiac effects
Digitalis (slows heart) levels increase with use |
|
When are Ca channel blockers used? What advantages do these drugs have?
|
Monotx for NEW HTN
Combined with ACE inhibitors and diuretic to block RAAS and vasodilation Advantages: reverses LVH, lipid neutral, help vascular dz, preserve cerebral flow and GFR |
|
What two systems does Angiotensin-converting enzyme act on?
|
1) RAAS: Angiotensinogen (renin) -> Angiotensin I (ACE) -> Angiotensin II
2) Kinin: Kininogen (kallikrein) -> Bradykinin (ACE) -> inactive metabolites |
|
What are the effects of Angiotensin II? Bradykinin?
|
Stimulates autonomic ganglia to release Epi, NE (vasoconstriction)
Stimulates aldosterone (salt/water retention) Renal vasoconstriction Stimulates thirst and inc secretion of ADH, ACTH Mitogenic for vascular/cardiac muscle (LVH) Inc PG synthesis, vasodilation |
|
What pathologies and tx's lead to high renin states? What is the DOC?
|
Renal artery stenosis, intrinsic renal dz, malignant HTN
Certain HTN tx's: diuretics, vasodilators DOC: beta blockers can lower renin, Angiotensin inhibitors lower BP |
|
What are the 5 ACE Inhibitors?
|
Captopril, Lisinopril, Enalapril, Benazepril, Enalaprilat (IV)
|
|
What is the MOA of ACE inhibitors?
|
Block ACE: dec SVR, NO inc HR, promotes natriuresis
inc vasodilation by inhibiting degrad of bradykinin (may cause cough and angioedema) |
|
Which 2 ACE inhibitors are active without conversion in the liver (not prodrugs)?
|
Captopril, Lisinopril
|
|
Where are ACE inhibitors used?
|
HTN
Dec morbidity/.mortality in heart failure and LV dysfunction after MI Delay diabetic nephropathy |
|
What are the side effects of ACE inhibitors?
|
Hypotension, renal failure, Hyperkalemia (aldosterone -> Na/K/H antiporter), cough and angioedema (bc bradykinin)
|
|
What are the toxicities of ACE inhibitors?
|
Allergy to sulfhydral group - rash and fever
Dysgeusia (taste) |
|
Where are ACE inhibitors CI?
|
Pregnancy (instead use methyldopa, labetolol, hydralazine)
Chronic renal failure, SLE - marrow suppression |
|
What are the 3 angiotensin receptor blockers?
|
Losartan, Valsartan, Candesartan
|
|
What is the MOA of angiotensin receptor blockers and how is it different from ACE inhibitors?
|
Competitive antagonist or AT1 receptor, blocks AT II effects better without bradykinin dilation
|
|
What are the side effects of angiotensin receptor blockers?
|
Same as ACE inhibitors minus cough/angioedema
Hypotension, renal failure, Hyperkalemia (aldosterone -> Na/K/H antiporter) |
|
Where are ARBs CI?
|
Pregnancy
|
|
What drug reduces plasma renin activity?
|
Aliskiren (reduce entire RAAS)
|