Antihypertensive Flashcards
Thiazide, Hydrochlorothiazide, Chlorothialidone Type & indication
Often combined with BB’s, ACEI’s, ARBS, central-actors in fixed dose combinations for treatment of HTN
Thiazide, Hydrochlorothiazide, Chlorothialidone Contraindication
severe renal or cardiac insufficiency, hypokalemia, pregnancy
Thiazide, Hydrochlorothiazide, Chlorothialidone MOA
initial effect due to volume contraction, long term effect due to decreased peripheral resistance (prostaglandin)
Thiazide, Hydrochlorothiazide, Chlorothialidone Drug Action/Pd
Thiazide, K+ wasting, Ca2+ saver. Inhibits Na+ reabsorption-Inhibits Na/Cl cotransporter in distal tubule. Not as strong because most Na has already been pumped. Protective against kidney stones.
Thiazide, Hydrochlorothiazide, Chlorothialidone Adverse Effects
hyponatremia, hyperglycemia (watch diabetics), Increased LDL/HDL, Hypokalemia, Hyperuricemia, Impotence
Thiazide, Hydrochlorothiazide, Chlorothialidone Drug interactions
No NSAIDS (PG mechanism), No BB’s if diabetic or lipidy-worsen hyperlipidemia and hyperglycemia, No Digoxin or Quinidine or Steroids. No Carbamazapine/Chlorpropamide or Anticoagulants (prone to clots).
Thiazide, Hydrochlorothiazide, Chlorothialidone Notes
watch renal insufficiency w/thiazides.
Drug Name
Loop, Furosemide (Lasix)
Furosemide (Lasix) Type & indication
Loop Diuretic
Furosemide (Lasix) Contraindication
diabetics (if on sulfonylureas will get hyperglycemic), watch heart patients (interaction w/B-Block, Digoxin and Quinidine), no renal insufficiency (will potentiate hyperkalemia), hyperuricemia (can lead to GOUT)
Furosemide (Lasix) Drug Action/Pd
K+ wasting, Ca/Mg wasting, hypokalemia. Inhibits Na/K/Cl- transporter in loop of henle. Remember that Ca and Mg are linked to the K+ situation in loop of henle.
Furosemide (Lasix) Adverse Effects
Dehydation/hyponatremia, hypokalemia (K+ wasting), Impaired Diabetes Control, Increased LDL/HDL, OTOTOXICITY, hypomagnesemia, hypocalcemia.
Furosemide (Lasix) Drug interactions
No NSAIDs, No BB’s, No Digoxin or Quinidine or Steroids. No Aminoglycosides or Anticoagulants (increased bleed).
Spironolactone, Eplerenone Contraindication
hyperkalemia or in patients that can have a state causing hyperkalemia (diabetes, myeloma, renal dx, renal insuff)
Spironolactone, Eplerenone Drug Action/Pd
Aldo-R inhibitor, K+ Sparing. Collecting Tubule. Gets into cell via basolateral (blood) side-no transporter needed.
Spironolactone, Eplerenone Adverse Effects
Hyperkalemic metabolic acidosis (due to sparing of H+.) Gynecomastia, antiandrogenic effects (but not w/newer eplerenone)
Spironolactone, Eplerenone Drug interactions
No NSAIDS, ACE inhibitors or ARB’s (further mess with Aldosterone system), Don’t combine with RAS inhibitors
Spironolactone, Eplerenone Notes
note that man-boobs and anti-androgenic effects are only for older spironolactone.
Nifedipine Type & indication
Calcium channel blocker; good for ischemic heart disease (angina), chronic pulmonary disease, diabetes due to limited side effects.
Nifedipine Contraindication
liver failure (metabolism-pk), severe heart failure (need vasoconstriction to perfuse organs)
Nifedipine MOA
dihydropyridine
Nifedipine Drug Action/Pd
more selective action on vessels, least action on heart (is a dihydropyridine)
Nifedipine Adverse Effects
acute tachycardia (reflex to the vasodilation and decreased cardiac return), peripheral edema (arterioles dilate more than veins so fluid goes out of capillaries instead of into higher-pressure veins), flushing (sympa activation), headache (decreased return)
Nifedipine Notes
(Not the heart one) Dr. Samarel Sez: most cardiologists use diltiazem for treatment of angina b/c middle vasodilatory effects (hi vasodilation can lead to reflex tachy) and intermediate action in inotropy and chronotropy.
Diltiazem Type & indication
Calcium channel blocker; good for ischemic heart disease (angina), chronic pulmonary disease, diabetes due to limited side effects.
Diltiazem Contraindication
liver failure (metabolism), severe heart failure (need vasoconstriction to perfuse organs), negative inotropic effect could cause ischemia
Diltiazem MOA
non-dihydropyridine-has effects on AV node and contractility
Diltiazem Drug Action/Pd
intermediate action on vessels and heart. Blocks activated/inactivated Ca channels primarily in heart (use-dependent). Slows AV nodal conductions & increases refractoriness.
Diltiazem Adverse Effects
bradycardia (AV node), dizziness & headache (hypotensive effect from vasodilation), edema
Diltiazem Drug interactions
note that SHORT acting CCB’s cannot be used in patients with coronary ischemia (CAD) b/c they can have a heart attack!!
Diltiazem Notes
(D middle of the road) Dr. Samarel Sez: most cardiologists use diltiazem for treatment of angina b/c middle vasodilatory effects (hi vasodilation can lead to reflex tachy) and intermediate action in inotropy and chronotropy.
Verapamil Type & indication
Calcium channel blocker; good for ischemic heart disease (angina), chronic pulmonary disease, diabetes due to limited side effects.
Verapamil Contraindication
liver failure (metabolism), severe heart failure (need vasoconstriction to perfuse organs), negative inotropic effect could cause ischemia
Verapamil MOA
non-dihydropyridine-has effects on AV node and contractility
Verapamil Drug Action/Pd
more effect on heart than vessels, Blocks activated/inactivated Ca channels primarily in heart (use-dependent). Slows AV nodal conductions & increases refractoriness.
Verapamil Adverse Effects
constipation, bradycardia (AV node, reduced CO b/c of Ca block), dizziness & headache and edema
Verapamil Drug interactions
watch cardiac acting non-dihydropyridines in pts w/BB’s because they can get SEVERE BRADYCARDIA!
Verapamil Notes
(Very cardiac active) Dr. Samarel Sez: most cardiologists use diltiazem for treatment of angina b/c middle vasodilatory effects (hi vasodilation can lead to reflex tachy) and intermediate action in inotropy and chronotropy.
Clonidine Type & indication
sympathetic-induced HYPERTENSION
Clonidine
A2 agonist (but remember alpha-2 is hooked up to Gi) acute increase in BP initially (peripherally) and then reduced BP (centrally); has actions on vasculature & chol/adr nerve terminals
Clonidine Drug Action/Pd
A2 Agonist. Decreases sympathetic outflow from CNS
Clonidine Adverse Effects
side effects do with blocking sympathetics: sedation (12-35%), dry mouth (25-40%), bradycardia, dermatitis
Clonidine Drug interactions
CNS Depressants like barbituates, benzos, opioid analgesics… (because Clonidine causes some CNS depression.
Clonidine Notes
Caution patient about missing doses–withdrawal should be done slowly to prevent rebound hypertension. Major compensatory response is salt retention.
Methyldopa Type & indication
Hypertension in PREGNANCY (drug of choice)
Methyldopa Contraindication
Liver failure, or treatment with MAOI’s or L-Dopa for Parkinson’s
Methyldopa MOA
same MOA as A2 agonist Clonidine.
Methyldopa Drug Action/Pd
Prodrug which is converted to active form-is ALPHA 2 agonist
Methyldopa Adverse Effects
sedation, nightmares, movement disorders, hyperprolactinemia, Hemolytic Anemia (rare 1-5%)
Methyldopa Drug interactions
MAOI’s b/c drug competes w/Nepi for transport into vesicles, leading to Nepi buildup in cytoplasm and expulsion of Nepi into body, negating effects. L-dopa (parkinsons) b/c drug causes increased dopamine degredation.
Reserpine Type & indication
HTN-often combined with diuretics to use therapeutically b/c at low dose you don’t have depression side effect.
Reserpine Contraindication
DO NOT use as a MONOTHERAPY (alone).
Reserpine MOA
leaves monoamines susceptible to degredation by MAO
Reserpine Drug Action/Pd
PREsynaptic inhibition of Ntmission, indirect acting adrenergic blocking agent. Inhibits VMAT uptake of monoamines
Reserpine Adverse Effects
depression (not at lower doses), nasal congestion, bradycardia, sedation, diarrhea.
Reserpine Drug interactions
CNS depressants (sleeping meds especially) or MAOI’s
Reserpine Notes
note that dopamine is transported into vesicles, and this is the step that is blocked
Phentolamine Type & indication
Pheochromocytoma ; catecholamine extravasation (to save tissue from ischemia and death if NE/Epi is out of veins)
Phentolamine Contraindication
pts with poor cardiac blood flow or CAD (due to reflex tachycardia)
Phentolamine MOA
non-selective alpha antagonist (A1 & A2)
Phentolamine Adverse Effects
orthostatic hypotension, reflex tachy (can give B-Blocker to prevent from happening), nasal congestion (due to vasodilation of nasal vessels), decreases LDL & HDL
Phentolamine Notes
hypotensive side effects lessen after 1st dose
Prazosin Type & indication
Hypertension, selective A1 antagonist
Prazosin MOA
selective alpha-1 antagonist
Prazosin Drug Action/Pd
less reflex tachycardia b/c less A2 effects when compared to non-specifics, also large initial drop in blood pressure (pts level out). Does not impair exercise tolerance.
Prazosin Adverse Effects
orthostatic hypotension (syncopy), decreases LDL & HDL
Prazosin Notes
hypotensive side effects lessen after 1st dose
Propranolol, Nadolol Type & indication
Propranolol-mild to moderate HTN, is lipophilic, sometimes used with vasodilators. Nadolol-longer 1/2 life, better compliance, hydrophilic
Propranolol, Nadolol Contraindication
bradycardia or heart block; cardiogenic shock or heart failure, asthmatics or diabetics
Propranolol, Nadolol MOA
NONSELECTIVE BETA BLOCKERS (B1 & B2 block). (Propranolol is also a Type II anti-arrythmic.)
Propranolol, Nadolol Drug Action/Pd
Anti-HTN actions: decrease HR & contractility, decrease renin release; decrease sympathetic activation. Also inhibit aqueous humor production. Bronchospasm (inhibit B2)! Diabetics- decreased response to epi (liver B2)-don’t respond to hypoglycemia!
Propranolol, Nadolol Adverse Effects
lipophilic drug Propranolol-Chronic Fatigue, also insomnia, nightmares. Both have Bradycardia, increased triglycerides, decreased HDL’s, increased airway resistance (B2)
Propranolol, Nadolol Drug interactions
CCB’s (due to doubling up of reduced contracility and conduction)
Propranolol, Nadolol Notes
Nadolol has longer 1/2 life (20-24hr) so has once-daily dosing advantage over prototype propranolol.
Pindolol Type & indication
HYPERTENSION, especially if sympathetic activity is too high
Pindolol Contraindication
bradycardia or heart block; cardiogenic shock or heart failure, asthmatics or diabetics
Pindolol MOA
PARTIAL AGONIST, less bradycardia & lipid abnormalities than other B-Blocker types
Pindolol Drug Action/Pd
decrease heart rate & contractility and overall CO (B1), decrease renin release (less vasoconstriction via R-A-A system); decrease sympathetic activation.
Pindolol Adverse Effects
slightly lipophilic so may see Chronic fatigue, insomnia, nightmares.
Pindolol Drug interactions
CCB’s (due to doubling up of reduced contracility and conduction)
Pindolol Notes
Beneficial when sympathetic activity is too high
Sympatholytic Drugs:
idea is to decrease sympathetic mediated vasoconstriction (alphas), CO and Renin Release (Betas), (l) after name means lipophilic for B-Blockers, BB’s less effect in blacks or elderly
Metoprolol (l) Atenolol Type & indication
ANTI-HTN: HYPERTENSION, ANGINA, Arrythmias
Metoprolol (l) Atenolol Contraindication
bradycardia or heart block; cardiogenic shock or heart failure, asthmatics or diabetics*
Metoprolol (l) Atenolol MOA
Selective B1 BLOCKERS “cardioselective”, (these two are also used as Type II anti-arrythmic)
Metoprolol (l) Atenolol Drug Action/Pd
decrease heart rate & contractility and overall CO (B1), decrease renin release (less vasoconstriction via R-A-A system); decrease sympathetic activation. *Little effect on liver or lung so may be okay for diabetics or asthmatics.
Metoprolol (l) Atenolol Adverse Effects
less respiratory side effects b/c of cardioselectivity (B1), do have bradycardia, increased triglys
Metoprolol (l) Atenolol Drug interactions
CCB’s (due to doubling up of reduced contracility and conduction)
Labetolol (l) Type & indication
ANTI HTN: mild to severe HTN, used for Pheochromocytoma
Labetolol (l) Contraindication
bradycardia or heart block; cardiogenic shock or heart failure, asthmatics or diabetics
Labetolol (l) Drug Action/Pd
B-Blocker with A-Blocker activity
Labetolol (l) Adverse Effects
Due to alpha blocking, get more incidence of orthostatic hypotension (block of baroreceptor alpha response), same lipophilic effcts as above (fatigue)
Carvedilol (l) Type & indication
ANTI-HTN: mild to severe HTN, also used post-MI and for heart failure
Carvedilol (l) Contraindication
bradycardia or heart block; cardiogenic shock or heart failure, asthmatics or diabetics
Carvedilol (l) Drug Action/Pd
B-Blocker with A-Blocker activity
Carvedilol (l) Adverse Effects
Due to alpha blocking, get more incidence of orthostatic hypotension (block of baroreceptor alpha response), same lipophilic effcts as above (fatigue)
Hydralazine Type & indication
Vasodilation of small vessels, particularly arterioles: drug resistant HTN and emergencies
Hydralazine Contraindication
Severe angina or known CAD (see “Coronary steal”)
Hydralazine MOA
vasodilate arterioles
Hydralazine Drug Action/Pd
orally effective
Hydralazine Adverse Effects
tachycardia, angina aggrevation, fluid retention, nausea, vomiting, sweating flushing, lupus-like symptoms
Hydralazine Drug interactions
NSAID’s (can reduce effectiveness)
Hydralazine Notes
remember from Dr. Samarel’s lecture that drugs that work primarily on arterioles can produce coronary steal!
Minoxidil Type & indication
Vasodilation of small vessels, particularly arterioles: drug resistant HTN
Minoxidil Contraindication
Severe angina or known CAD (see “Coronary steal”)
Minoxidil MOA
vasodilate arterioles
Minoxidil Drug Action/Pd
orally effective
Minoxidil Adverse Effects
tachycardia, angina aggrevation, fluid retention, hypertrichosis (extra body hair), nausea, vomiting, sweating flushing, lupus-like symptoms
Minoxidil Notes
remember from Dr. Samarel’s lecture that drugs that work primarily on arterioles can produce coronary steal!
Nitroprusside Type & indication
Vasodilation of small vessels, particularly arterioles: emergencies
Nitroprusside MOA
arteriole & venous dilation; endothelium independent.
Nitroprusside Drug Action/Pd
immediate onset, brief duration. Can produce prompt vasodilation (w/reflex tachy) and can reduce BP in all pts, regardless of cause of HTN!
Nitroprusside Adverse Effects
nausea, vomiting, muscle twitch, cyanide poisioning
Nitroprusside Notes
you don’t give it orally b/c that converts it to cyanide!
Losartan Type & indication
Angiotensin R Blocker (ARB’s): non-peptide antagonist of ATII receptor
Losartan Contraindication
no ARB’s in pregnancy-renal damage to fetus (Dr. Fareed)
Losartan MOA
blocks renin-angiotensin-aldosterone system to lower BP
Losartan Adverse Effects
hyperkalemia. Less effective (just like ACEI’s) in salt-sensitive blacks.
Losartan Drug interactions
liver metabolism, so decrease dose if liver problem or hypovolumic
Losartan Notes
Better results with diuretic combo rather than increased dose!
Drug Name
Captopril
Captopril Type & indication
ACEI’s are Less effective in black patients you racist! ACEI’s: Reduces mortality post-MI and in HF pts, Reduces remodeling of heart post MI. Preserves renal function in diabetics
Captopril Contraindication
no ACE inhibitors in pregnancy due to renal damage of fetus (Dr. Fareed), bilateral renal stenosis
Captopril Drug Action/Pd
short t 1/2, need multiple daily doses, has active metabolites
Captopril Adverse Effects
hyperkalemia, dry cough, rash, angioedema (rare!). Risk of hyperkalemia if using K+ sparing drugs!
Captopril Drug interactions
ACE is also a kininase, so when you block it, you see increased bradykinin, which is a vasodilator and is thought to be what causes cough in people.
Enalapril Type & indication
ACEI’s are Less effective in black patients you racist! ACEI’s: Reduces mortality post-MI and in HF pts, Reduces remodeling of heart post MI. Preserves renal function in diabetics
Enalapril Contraindication
no ACE inhibitors in pregnancy due to renal damage of fetus (Dr. Fareed), bilateral renal stenosis
Enalapril Drug Action/Pd
prodrug that gets converted to active metabolite, longer 1/2 life, can dose 1-2x per day
Enalapril Drug interactions
Note you really want to give ACEI’s to post-MI, HF or Diabetics. BB’s also good post-MI. Remember that AT-II is a potent cardiomyocyte growth factor (hypertrophy) and fibroblast mitogen factor (hyperplasia)– ACEI prevents cardiac remodeling!!
Lisinopril Type & indication
ACEI’s are Less effective in black patients you racist! ACEI’s: Reduces mortality post-MI and in HF pts, Reduces remodeling of heart post MI. Preserves renal function in diabetics
Lisinopril Contraindication
no ACE inhibitors in pregnancy due to renal damage of fetus (Dr. Fareed), bilateral renal stenosis
Lisinopril Drug Action/Pd
more predictable onset and duration of action, has long 1/2 life for 1x dosing
Lisinopril Drug interactions
Note you really want to give ACEI’s to post-MI, HF or Diabetics. BB’s also good post-MI. Remember that AT-II is a potent cardiomyocyte growth factor (hypertrophy) and fibroblast mitogen factor (hyperplasia)– ACEI prevents cardiac remodeling!!
