CRS Drugs Flashcards
Captopril
ACE Inhibitor
Inhibits conversion of Angiotensin I to Angiotensin II
First line treatment for Hypertension, particularly for patients with DM & CKD.
AE: Cough, Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
Contraindications: Pregnancy, bilat renal art stenosis, hx of angioedema.
Enalapril
ACE Inhibitor
Inhibits conversion of Angiotensin I to Angiotensin II
First line treatment for Hypertension, particularly for patients with DM & CKD.
AE: Cough, Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
Contraindications: Pregnancy, bilat renal art stenosis, hx of angioedema.
Lisinopril
ACE Inhibitor
Inhibits conversion of Angiotensin I to Angiotensin II
First line treatment for Hypertension, particularly for patients with DM & CKD.
AE: Cough, Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
Contraindications: Pregnancy, bilat renal art stenosis, hx of angioedema.
Losartan
Angiotensin Receptor Blocker (ARB)
Blocks Angiotensin II receptors.
First line treatment for Hypertension as an alternative to ACE Inhibitors.
AE: Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
Contraindications: Pregnancy, bilat renal art stenosis
Valsartan
Angiotensin Receptor Blocker (ARB)
Blocks Angiotensin II receptors.
First line treatment for Hypertension as an alternative to ACE Inhibitors.
AE: Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
CI: Pregnancy, bilat renal art stenosis
Aliskiren
Renin Inhibitor
Inhibits Renin from converting Angiotensinogen into Angiotensin I
Alternative agent in treating hypertension.
AE: Hyperkalemia, Angioedema, Acute Renal Failure (in pt with bilat renal art stenosis), rash, fever, altered taste.
Verapamil
Calcium Channel Blocker. Non-dihydropyridine.
Blocks channels in both cardiac & vascular smooth muscle.
Used to treat angina, supraventricular tachyarrhythmias, hypertension, migraine, cerebral vasospasm.
Arrhythmias: Class IV, negative inotrope, negative chronotrope, negative dromotrope. Slow Phase 0 of SA node (inc PR). More effective against atrial arrhythmias.
AE: Constipation, negative inotropic effects, gingival hyperplasia, transient hypotension, CNS effects.
CI: pt with b blockers, 2nd or 3rd degree AV block, severe left vent diastolic dysfunction, digoxin, dofetilide, statins.
Diltiazem
Calcium Channel Blocker. Non-dihydropyridine.
Blocks channels in both cardiac & vascular smooth muscle.
Used to treat angina, supraventricular tachyarrhythmias, hypertension, cerebral vasospasm.
Arrhythmias: Class IV, negative inotrope, negative chronotrope, negative dromotrope. Slow Phase 0 of SA node (inc PR). More effective against atrial arrhythmias.
AE: Negative inotropic effects.
CI: Concomitant b blockers, 2nd or 3rd degree AV block, severe left vent diastolic dysfunction, digoxin, dofetilide, statins.
Amlodipine
Calcium Channel Blocker. Dihydropyridine.
Blocks channels in vascular smooth muscle leading to coronary & peripheral vasodilation.
AE: High doses can increase risk of MI (excess vasodilation causes reflex cardiac stimulation). Hypotension, peripheral edema, dizziness, headache, fatigue, gingival hyperplasia, flushing.
Nifedipine
Calcium Channel Blocker. Dihydropyridine.
Blocks channels in vascular smooth muscle leading to coronary & peripheral vasodilation.
AE: High doses can increase risk of MI (excess vasodilation causes reflex cardiac stimulation). Hypotension, peripheral edema, dizziness, headache, fatigue, gingival hyperplasia, flushing.
Furosemide
Loop Diuretic
Blocks Na/Cl/K cotransporter in ascending Loop of Henle.
Increases excretion of K, Ca, Mg. Increases renal blood flow, prostaglandin synthesis. Decreases renal vascular resistance.
AE: Ototoxic, hypokalemia, hypomagnesemia, allergic reactions.
Torsemide
Loop Diuretic
Blocks Na/Cl/K cotransporter in ascending Loop of Henle.
Increases excretion of K, Ca, Mg. Increases renal blood flow, prostaglandin synthesis. Decreases renal vascular resistance.
AE: Ototoxic, hypokalemia, hypomagnesemia, allergic reactions.
Bumetanide
Loop Diuretic
Blocks Na/Cl/K cotransporter in ascending Loop of Henle.
Increases excretion of K, Ca, Mg. Increases renal blood flow, prostaglandin synthesis. Decreases renal vascular resistance.
AE: Ototoxic, hypokalemia, hypomagnesemia, allergic reactions.
Hydrochlorothiazide
Thiazide Diuretic
Blocks Na/Cl cotransporter in distal tubule.
Increases excretion of K, Mg. Decreased excretion of Ca.
Useful in edema caused by mild-moderate HF, pre-menstrual edema, Diabetes insipidus.
First line treatment in htn with no co-morbidities. Second line in htn with all comorbidities except HF and MI.
AE: Metabolic alkalosis, hyperuricemia, hyperglycemia, hyperlipidemia, hypersensitivity, sexual dysfunction.
Chlorthalidone
Thiazide Diuretic
Blocks Na/Cl cotransporter in distal tubule.
Increases excretion of K, Mg. Decreased excretion of Ca.
Useful in edema caused by mild-moderate HF, pre-menstrual edema, Diabetes insipidus.
First line treatment in htn with no co-morbidities. Second line in htn with all comorbidities except HF and MI.
AE: Metabolic alkalosis, hyperuricemia, hyperglycemia, hyperlipidemia, hypersensitivity, sexual dysfunction.
Metolazone
Thiazide Diuretic
Blocks Na/Cl cotransporter in distal tubule.
Increases excretion of K, Mg. Decreased excretion of Ca.
Useful in edema caused by mild-moderate HF, pre-menstrual edema, Diabetes insipidus.
First line treatment in htn with no co-morbidities. Second line in htn with all comorbidities except HF and MI.
AE: Metabolic alkalosis, hyperuricemia, hyperglycemia, hyperlipidemia, hypersensitivity, sexual dysfunction.
Spironolactone
Aldosterone Antagonist (K sparing diuretic)
Aldosterone receptor antagonist in collecting tubule.
AE: Gastric upset & ulcers, antiandrogen effects, hyperkalemia, nausea lethargy + mental confusion.
Eplerenone
Aldosterone Antagonist (K sparing diuretic)
Aldosterone receptor antagonist in collecting tubule.
AE: Gastric upset & ulcers, antiandrogen effects, hyperkalemia, nausea lethargy + mental confusion.
Amiloride
Na Channel Inhibitor (K sparing Diuretic)
Blocks Na/K exchanger in collecting tubule.
Not efficacious alone, can prevent K loss associated with loop diuretics & thiazides.
AE: Hyperkalemia, leg cramps, GI upset, dizziness, pruritus, headache, visual changes.
Acetazolamide
Carbonic Anhydrase Inhibitor
Inhibit Carbonic Anhydrase in proximal tubule.
Cause metabolic acidosis, increases urinary pH.
AE: Metabolic acidosis, hyponatremia, hypokalemia, crystalluria, malaise, fatigue, depression, headache, GI upset, drowsiness paresthesia.
Mannitol
Osmotic Diuretic
Raises plasma osmotic pressure, draws H2O out of tissues and promotes diuresis. Does not directly affect Na excretion.
Increases urine flow in patients with renal failure. Reduce increased ICP & cerebral edema.
AE: Tissue dehydration, extracellular water expansion, don’t give in CHF or Pulmonary Edema.
Conivaptan
ADH Antagonist
Antagonist at ADH V1 and V2 receptor (collecting tubule). Decreases H2O reabsorption.
Used in euvolemic & hypervolemic hyponatremia, SIADH and some cases of CHF.
Potent inhibitor of CYP3A4.
AE: Infusion site reactions, thirst, Afib, GI & electrolyte disturbances, Nephrogenic Diabetes Insipidus.
Propranolol
Non-selective B blocker.
Used as add-on therapy to first-line agents in primary prevention patients. First-line therapy in patients with CAD, HF, post-MI.
Arrhythmia: Class II. Reduce incidence of arrhythmia after MI. Control of ventricular and supraventricular tachycardia.
AE: Bradycardia, hypotension, CNS effects.
CI: Acute CHF, severe bradycardia, heart-block, severe hyperactive airway disease.
Metoprolol
Selective B1 blocker
Used as add-on therapy to first line agents in primary prevention patients. First-line therapy in patients with CAD, HF, post-MI.
Arrhythmia: Class II. Reduce incidence of arrhythmia after MI. Control of ventricular and supraventricular tachycardia.
AE: Bradycardia, hypotension, CNS effects.
CI: Acute CHF, severe bradycardia, heart-block, severe hyperactive airway disease.
Atenolol
Selective B1 blocker
Used as add-on therapy to first line agents in primary prevention patients. First-line therapy in patients with CAD, HF, post-MI.
Arrhythmia: Class II. Reduce incidence of arrhythmia after MI. Control of ventricular and supraventricular tachycardia.
AE: Bradycardia, hypotension, CNS effects.
CI: Acute CHF, severe bradycardia, heart-block, severe hyperactive airway disease.
Pindolol
Non-selective B1 & B2 partial agonist
Used as add-on therapy to first line agents in primary prevention patients. First-line therapy in patients with CAD, HF, post-MI.
Prazosin
A1 antagonist
Lower PVR and arterial BP. No long-term tachycardia. Causes Na & H2O retention.
Side effect profile means they are used to treat BPH less than HTN.
AE: Orthostatic hypotension, short-term reflex tachycardia, dizziness, drowsiness, headache, lack of energy, nausea, palpitations.
Doxazosin
A1 antagonist
Lower PVR and arterial BP. No long-term tachycardia. Causes Na & H2O retention.
Side effect profile means they are used to treat BPH less than HTN.
AE: Orthostatic hypotension, short-term reflex tachycardia, dizziness, drowsiness, headache, lack of energy, nausea, palpitations.
Can increase rate of Congestive HF (specific to doxazosin)
Labetalol
Mixed a and b blocker
Safe in pregnancy. Does not cause reflex tachycardia.
Can be used to treat hypertensive emergency.
AE: Orthostatic hypotension. Contraindicated in COPD, asthma, 2nd or 3rd degree AV block or bradycardia.
Clonidine
Central A2 agonist
Acts on presynaptic a2 autoreceptors, reduces central sympathetic outflow.
Doesn’t lower Renal Blood Flow & GFR. Manage hypertension.
AE: Rebound hypertension with abrupt withdrawal (don’t use with b blockers). Drowsiness, dry mouth, dizziness, headache, sexual dysfunction.
Methyldopa
Central A2 agonist
Acts on presynaptic a2 autoreceptors, reduces central sympathetic outflow.
Doesn’t lower Renal Blood Flow & GFR. Manage hypertension. SAFE IN PREGNANCY.
AE: Rebound hypertension with abrupt withdrawal (don’t use with b blockers). Drowsiness, dry mouth, dizziness, headache, sexual dysfunction. NIGHTMARES, mental depression, vertigo, reversible lupus like syndrome, positive Coombs test, hemolytic anemia, hepatitis, drug fever.
Hydralazine
Direct Vasodilator
Directly vasodilates arterioles. Produces reflex tachycardia, increases plasma renin. Used as last-line hypertension therapy.
Treat PREGNANCY induced hypertensive emergencies.
AE: Fluid retention, reflex tachycardia, reversible lupus-like syndrome, headache, nausea, sweating, flushing, used with b blocker & thiazide.
Minoxidil
Direct Vasodilator
Directly vasodilates arterioles. Produces reflex tachycardia, increases plasma renin. Used as last-line hypertension therapy.
AE: Fluid retention, reflex tachycardia, used with b blocker & loop diuretic. Hypertrichosis (can be used to treat baldness)
Epoprostenol
Synthetic PGI2
Lowers peripheral, pulmonary & coronary resistance. Used in pulmonary HTN, given by continuous infusion.
AE: Flushing, headache, jaw pain, diarrhea, arthalgia.
Bosentan
Nonselective endothelin receptor blocker.
Blocks ETa and ETb responses to endothelin. Extremely unsafe in pregnancy (cat X).
Sildenafil
Phosphodiesterase Inhibitor
Increases cGMP, relaxes smooth muscle.
AE: Headache, flushing, dyspepsia, cyanopsia.
Contraindication: Nitrates
Sodium Nitroprusside
IV Vasodilator
Prompt vasodilation of peripheral arterial & venous SM. Reflex tachycardia.
Treat hypertensive crisis.
AE: Hypotension, goose bumps, abdominal cramping, nausea, vomiting, headache. Cyanide toxicity can be treated with Sodium Thiosulfate.
Fenoldopam
Peripheral D1 agonist
Evokes arteriolar dilation. Maintains or increases renal perfusion as lowers BP.
Safe for all hypertensive emergencies, particularly beneficial in pt with renal insufficiency.
Contraindication: Glaucoma
Nicardipine
Calcium Channel Blocker
Evokes reflex tachycardia. IV infusion for hypertensive emergency.
Nitroglycerin
Vasodilator through guanylyl cyclase activation
More effect on veins than arteries.
DOC for hypertensive emergencies in patients with cardiac ischemia & angina.
AE: Hypotension
Diazoxide
K channel opener
Prevents SM contraction and thus opens K channels.
AE: Hypotension, reflex tachy, Na & H2O retention.
Inhibits Insulin release & treats hypoglycemia secondary to insulinoma.
Phentolamine
Reversible non-selective alpha blocker
DOC for patients with catecholamine related emergencies.
Esmolol
B1 selective blocker
Short-acting.
Treat aortic dissection or post-op htn. IV treatment of acute arrhythmias in surgery or emergency situations.
Sacubitril
Neprilysin Inhibitor
Given together with Valsatran: ARNI
Prevents breakdown of BNP, bradykinin, Ag II
AE: Hypotension, Hyperkalemia, Teratogenic, worsens renal function, Cough
CI: Hx of angioedema with ACEI or ARB. Concomitant use of ACEI or ARB. Concomitant use of Aliskiren.
Isosorbide Dinitrate
Direct Vasodilator
Treatment of HFrEF. Used concurrently with Hydralazine in pt who cannot tolerate ACEI/ARB or African American pt.
CI: PDE5 inhibitors.
Dapagliflozin
SGLT2 Inhibitor
Decrease Glucose reabsorption in prox tubule –> inc Glucose in urine.
Mechanism of help in HFrEF unclear. Most effective in pt with DM2.
AE: UTI, volume depletion, inc serum creatinine, hyperkalemia, hypermagnesemia, hyperphosphatemia, hypotension.
Digoxin
Cardiac Glycoside
Inhibits Na/K ATPase leading to indirect inhibition of Na/Ca exchanger, leading to higher intracellular Ca.
Positive inotrope. Negative chronotrope. Negative dromotrope. Treat HF with afib.
AE: Arrhythmias, anorexia nausea & vomiting, headache, fatigue, confusion, blurred vision, altered color perception, halos around dark object.
Predisposing factors: Hypokalemia, quinidine/verapamil/amiodarone.
CI: Diastolic (HFpEF) or right-sided HF, uncontrolled HTN, bradyarrhythmias.
Vericiguat
Soluble guanylate cyclase stimulator
Vasodilator, decreases heart fibrosis/hypertrophy/inflammation. Increases renal blood flow.
AE: Hypotension, dizziness, nausea, abdominal discomfort, diarrhea, syncope.
CI: PDE5 inhibitors
Ivabradine
If current inhibitor
Decreases rate of SA/AV node depolarization, thus decreasing HR.
AE: Bradycardia, afib, sinus arrest, QT prolongation/Torsade de pointes.
CI: HFpEF, decompensated HF, Arrhythmia, heart block, hypotension & bradycardia, liver failure, use of CYP3A4 inhibitors (verapamil, diltiazem)
Inamrinone
PDE3 inhibitor
Increases myocardial cAMP. Positive inotrope. Systemic & Pulmonary vasodilator. Short term therapy for patients with intractable HF.
Milrinone
PDE3 inhibitor
Increases myocardial cAMP. Positive inotrope. Systemic & Pulmonary vasodilator. Short term therapy for patients with intractable HF.
Dopamine
Stimulates adrenergic & dopaminergic receptors.
Increases renal blood flow, cardiac stimulation.
Treat cardiogenic shock which persists after adequate fluid replacement.
Dobutamine
A1, B1, B2 agonist.
At therapeutic levels predominantly stimulates B1, potent inotrope with little chronotrope effect. Increases CO in acute treatment of HF.
Glucagon
Gs stimulator
Similar effects to b-agonists without the need of functioning b receptors.
Used as cardiac stimulant in managing b-blocker overdose.
Quinidine
Class IA Antiarrhythmic
Blocks fast inward Na channels. Slows phase 0 (inc QRS). Blocks K channels (Class 3 activity). Slows phase 3 (inc QT).
Suppress Supraventricular & Ventricular arrhythmias.
CYP2D6, CYP3A4, and P-glycoprotein inhibitor.
AE: Arrhythmias (Torsade De Pointes), SA/AV block, asystole, nausea, vomiting, diarrhea, thrombocytopenic purpura. VTach. Cinchonism (blurred vision, tinnitus, headache, psychosis)!, a-adrenergic blocker, antimuscarinic. Increase [digoxin].
CI: Complete heart block!, prolonged QT interval, hx of torsade de pointes, incomplete heart block, decomp HF, myocarditis, severe myocardial damage.
Procainamide
Class IA Antiarrhythmic
Blocks fast inward Na channels. Slows phase 0 (inc QRS). Blocks K channels (Class 3 activity). Slows phase 3 (inc QT).
Suppress Supraventricular & Ventricular arrhythmias.
Metabolized by CYP2D6 and acetylated to NAPA.
AE: Reversible lupus-like syndrome!, asystole, ventricular arrhythmias, CNS effects, hypotension, weak anticholinergic effects.
CI: Hypersensitivity, complete heart block, 2nd degree AV block, Lupus, Hx of torsade de pointes, HF, hypertension.
Disopyramide
Class IA Antiarrhythmic
Blocks fast inward Na channels. Slows phase 0 (inc QRS). Blocks K channels (Class 3 activity). Slows phase 3 (inc QT).
Suppress Supraventricular & Ventricular arrhythmias.
Strong antimuscarinic. Stronger negative inotrope than other Class IAs. Peripheral vasoconstrictor.
AE: Antimuscarinic effects (dry mouth, urinary retention, blurred vision, constipation). Hypotension, cardiac failure without pre-existing myocardial dysfunction.
Lidocaine
Class IB Antiarrhythmic
Block fast inward Na channels. Slows phase 0 (inc QRS). Shortens phase 3 (dec QT).
Acute treatment of ventricular arrhythmias. Treatment of digoxin arrhythmias.
IV only
AE: Drowsiness, slurred speech, agitation. Arrhythmias. Toxic doses: convulsions, coma.
Mexiletine
Class IB antiarrhythmic
Block fast inward Na channels. Slows phase 0 (inc QRS). Shortens phase 3 (dec QT).
Management of ventricular arrhythmias.
IV or oral. Orally active lidocaine derivative.
AE: Drowsiness, slurred speech, agitation. Arrhythmias. Toxic doses: convulsions, coma. GI side effects.
Flecainide
Class IC anti-arrhythmic
Markedly depresses Phase 0 (inc QRS). Prominent effects even at normal heart rate.
Treat severe ventricular & supraventricular arrhythmias, & prevent paroxysmal afib.
AE: Negative inotrope, CNS effects, GI effects, Arrhythmias & Vtach
CI: CHF, Structural Heart Disease!
Propafenone
Class IC Antiarrhythmic
Markedly depresses Phase 0 (inc QRS). Prominent effects even at normal heart rate. Also has b-blocking activity.
Treat severe ventricular & supraventricular arrhythmias, & prevent paroxysmal afib.
AE: Negative inotrope, CNS effects, GI effects, Arrhythmias & Vtach
CI: CHF, Structural Heart Disease!, COPD
Amiodarone
Class III Anti-arrhythmic
Has Class I, II, and IV effects, but III predominant.
Manage Vent & Supravent arrhythmias. DOC for Acute VTach refractory to shock. Low doses maintain normal sinus rhythm in afib.
Oral & IV. Very high VD and half-life, effects and AE may take 6 weeks to be achieved.
AE: Interstitial Pulmonary Fibrosis!, Blue Skin!, Av block, arrhythmias.
CI: Concomitant use of Digoxin, theophylline, warfarin, quinidine. Bradycardia, SA/AV block, hypotension, resp failure.
Sotalol
Class III antiarrhythmic
Also a potent non-selective B-blocker.
Treat life-threatening vent arrhythmias. Maintain sinus rhythm in pt with afib and aflutter who are currently in sinus rhythm.
AE: Same as b-blockers, Torsade De Pointes, arrhythmias (lowest rate of adverse effects).
CI: Renal impairment
Dofetilide
Class III anti-arrhythmic
Potent and pure K channel blocker. Prolong Phase 3 (inc QT). Phase 3 unaltered.
Convert Afib & Aflutter to normal sinus rhythm. Maintain normal sinus rhythm in pt with chronic afib/flutter.
AE: Vtach, Torsade De Pointes, CNS effects, chest pain.
Adenosine
Nucleoside (P1 receptor agonist)
High doses: Decreased conduction velocity & prolongs refractory period. Enhances K conductance, hyperpolarizes AV node.
DOC for abolishing acute supraventricular tachycardia.
AE: Flushing, burning, chest pain, hypotension, bronchoconstriction in asthmatics.
Magnesium
Functional Ca antagonist
Treat Torsade De Pointes, Digoxin arrhythmia, prophylaxis of arrhythmia in acute MI
Atropine
Anti-muscarinic
Treat bradyarrhythmias by decreasing vagal tone
Ranolazine
Na channel blocker
Blocks Na current of Na/Ca exchanger, decreases intracellular Ca level.
Produces myocardial relaxation and reduces myocardial O2 demand.
