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Practice Final

Beta-Blockers

Propranolol (Inderal LA/XL)

Indications: HTN, chronic stable angina, migraine prophylaxis AND treatment (off-label - thyroid storm, portal HTN)

Dosing: tablets, SR capsules, solution, IV; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 and 1A2 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 and β2 activity - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia; crosses the BBB (MOST lipophilic BB)

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take on empty stomach; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING); monitor in concomitant CHF for worsening sxs

Atenolol (Tenormin)

Indications: HTN, chronic stable angina

Dosing: renal dose adjustments; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 and β2 activity (only at high doses) - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia; does NOT cross BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING); monitor in concomitant CHF for worsening sxs

Metoprolol Tartrate (Lopressor)

Indications: HTN, chronic stable angina, AFib, post-MI

Dosing: IMMEDIATE RELEASE (BID dosing); tablets, IV; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing; when converting from MetTart <—> MetSucc, the doses are interchangeable

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take with food to increase absorption; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Metoprolol Succinate (Toprol XL)

Indications: HTN, chronic stable angina, HFrEF, post-MI

Dosing: EXTENDED RELEASE (initial dose: 12.5mg QD, target dose: 200mg QD); XL tablets; double dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing; when converting from MetTart <—> MetSucc, the doses are interchangeable

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take without regard to food; do NOT crush or chew - can score tablet; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Bisoprolol (Zebeta)

Indications: HTN, (off-label: HFrEF)

Dosing: renal dose adjustments (initial dose: 1.25mg QD, target dose: 100mg QD); double dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB; 50% hepatic + 50% renal elimination

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Nebivolol (Bystolic)

Indications: HTN

Dosing: titrate dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 substrate with active metabolite; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: the MOST β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB; 50% hepatic + 50% renal elimination

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Carvedilol (Coreg, SR)

Indications: HTN, HFrEF

Dosing: IR (initial dose: 3.125mg BID, target dose ≤ 85kg: 25mg BID, target dose > 85kg: 50mg BID) XR (initial dose: 10mg QD, target dose: 80mg QD); tablets, SR capsules; titrate dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1, β2, and α1 activity - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia - α1 antagonism is vascular smooth muscle ∴ increases vasodilation, increases HR and CO initially; crosses BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take with food to decrease absorption and avoid orthostasis; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Ranolazine (Ranexa)

Indications: chronic stable angina (2nd Line)

Dosing: XL tablets; hepatic dose adjustments (↓ dose 50% if cirrhosis)

Major Drug Interactions: strong CYP3A4 substrate - do NOT exceed 20mg simvastatin; moderate 3A4 inhibitors (diltiazem, verapamil) - do NOT exceed 500mg BID of ranexa; minor 2D6 substrate; Pgp inhibitors; digoxin; metformin

MOA: inhibits the late Na+ ion channels (INa) ∴ ↓ angina frequency

AEs: QTc prolongation, constipation, hypotension, dizziness, headache

Contraindications: strong 3A4 inhibitors/inducers; liver cirrhosis

Counseling/Patient Education: avoid grapefruit juice; do NOT crush or chew

Digoxin (Lanoxin)

Indications: HFrEF, AFib

Dosing: renal dose adjustments; 0.125-0.250mg QD - LD given for AFib before reducing to this MD; tablets, capsules, solution, injection

Major Drug Interactions: Pgp substrate (amiodarone, verapamil, diltiazem), diuretics

MOA: Na/K-ATPase inhibitor leading to myocardial Ca influx and increased contractility; increases vagal (parasympathetic) tone; positive inotrope, negative chronotrope

AEs: mild GI upset, bradycardia, CNS effects, digoxin toxicity (N/V, green/yellow halos, cardiac arrhythmias, low K/Mg and high Ca)

Warnings/Precautions: AV block, digoxin toxicity (DigiFab is antidote)

Contraindications: ventricular fibrillation

Counseling/Patient Education: caution use of OTC antacids, laxatives, anti-diarrheals

Monitor: draw serum concentrations at steady state (3-5 days), at least 6-8h after last dose (optimally 12-24h); HFrEF goal: 0.5-0.9 ng/mL, AFib goal: 0.8-2 ng/mL

Ivabradine (Corlanor)

Indication: decreases HF hospitalization in patients who are stable, symptomatic, have EF ≤ 35%, are in sinus rhythm with HR ≥ 70 BPM on max BB therapy or C/I to BB

decreases HR without affecting BP in HFrEF

Nitrates

Isosorbide Dinitrate IR/ER

Indications: angina, CAD, HF

Dosing: IR (TID with 4-5h break ∴ 8-1-6 schedule), ER (BID with 6h break ∴ 8-2 schedule); NITRATE-FREE INTERVALS (≥ 14h IR; > 18h ER)

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: venous vasodilator

AEs: headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: nitrate-free interval administration

Isosorbide Mononitrate (Imdur)

Indications: angina, CAD, HF

Dosing: IR (BID with 7h break ∴ 8-3 schedule), ER (once daily QAM); NITRATE-FREE INTERVALS (≥ 14h IR; > 18h ER)

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: venous vasodilator

AEs: headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: nitrate-free interval administration; do NOT crush XR tabs, swallow whole

Nitroglycerin (Nitrostat)

Indications: acute angina (off-label: 5-10min pre-activity)

Dosing: sublingual tablets; 3 tablets 5 minutes PRN (if no relief 3-5min after 1st tab, call 911)

Major Drug Interactions: ethanol, arterial vasodilators (C

CBs)

MOA: venous vasodilator

AEs: reflex tachycardia, headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: SIT DOWN before using; store in original amber vial; discard after 6-12 months

Hydralazine (Apresoline)

Indications: HTN (off-label: HFrEF ± nitrate)

Dosing: BID-QID

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: arterial vasodilator

AEs: fluid retention, reflex tachycardia, hypotension, dizziness, peripheral neuritis, blood dyscrasias

Warnings/Precautions: drug-induced lupus with long-term use (doses > 200mg/day)

Contraindications: CAD

Counseling/Patient Education: take with food; report any general fatigue/ body aches

Anti-Platelets

Clopidogrel (Plavix)

Indications: post-ACS, PCI, CVA

Dosing: 75mg daily

Major Drug Interactions: CYP2C19 substrate; NSAIDs; anticoagulants; PPIs (pantoprazole least likely to interact); fluoxetine

MOA: P2Y12 Inhibitor (thienopyridine); irreversibly bind and inhibit P2Y12 for the whole life of the platelet - indirectly acting ∴ needs to be metabolized to become active

AEs: bleeding, bruising

Warnings/Precautions: [BBW] CYP2C19 poor metabolizers (Asians)

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Prasugrel (Effient)

Indications: post-ACS, PCI

Dosing:

Major Drug Interactions: CYP3A4 and 2B6 substrate; NSAIDs; anticoagulants

MOA: more potent P2Y12 Inhibitor (thienopyridine); irreversibly bind and inhibit P2Y12 for the whole life of the platelet - indirectly acting ∴ needs to be metabolized to become active

AEs: bleeding, bruising

Warnings/Precautions: [BBW] avoid with age ≥ 75 unless DM s/p MI (high risk)

Contraindications: prior TIA/CVA, active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Ticagrelor (Brilinta)

Indications: ACS with PCI

Dosing:

Major Drug Interactions: CYP3A4 and Pgp substrate - avoid lovastatin/simvastatin > 40mg/day; NSAIDs; anticoagulants

MOA: P2Y12 Inhibitor (non-thienopyridine); reversibly bind and inhibit P2Y12 for the whole life of the platelet - directly acting ∴ doesn’t need to be metabolized to become active

AEs: dyspnea, bradyarrhythmias, hyperuricemia, bleeding, bruising

Warnings/Precautions: [BBW] ASA doses > 100mg/day decrease efficacy in patients with ACS

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Cilostazol (Pletal)

Indications: intermittent claudication

Dosing:

Major Drug Interactions: CYP3A4 and 2C19 substrate - diltiazem, MANY others

MOA: reversibly inhibits phosphodiesterase, PDE ↓ cAMP in ALL CELLS ∴ many downstream effects, PDE inhibitors ∴ induce vasodilation

AEs: headache, diarrhea, dizziness, palpitations, infection, rhinitis

Warnings/Precautions: tachycardia, hypotension, arrhythmia, hematologic effects

Contraindications: congestive HF of any severity

Counseling/Patient Education: avoid grapefruit juice; take on empty stomach; may take up to 12 weeks to see full effect

Anti-Coagulants

Warfarin (Coumadin)

Indications: valvular AFib, mechanical heart valves, VTE

Dosing: [initial] 5mg PO daily for first 1-2 days, then adjust based on INR, consider dropping starting dose to 2-3mg in elderly >60, low BW, HF, D/Is, low albumin, liver disease, decreased dose 10-20% may be required in eGFR <60; [maintenance] calculate total weekly dose and ↑/↓ by 5-20% (only when patient is within goal INR range), steady state usually achieved within 10-14 days; reversal (INR >10 + no big bleeds = PO Kcentra, any INR + big bleeds = IV Kcentra)

Major Drug Interactions: major CYP2C9 substrate - BAM-IF; NSAIDs; anti-platelets

↑ bleeding risk (no effect on INR): NSAIDs, SSRIs (serotonin is a platelet activator), thrombolytics, antiplatelets
INHIBITS METABOLISM: Bactrim, Amiodarone, Metronidazole, Itraconazole, Fluconazole (BAM-IF), ACUTE alcohol use
displacement from albumin: phenytoin, valproic acid, ethacrynic acid
↓ vitamin K producing bacteria in GI: any antibiotic... theoretically
INDUCES METABOLISM: azathioprine, carbamazepine, rifampin, St Johns Wort, cigarettes, CHRONIC alcohol use
inhibit absorption: cholestyramine

MOA: irreversibly binds VKORC1 in hepatocytes ∴ inhibits synthesis of vitamin K-dependent clotting factors (VII, IX, X, II [Protein C & S]); t1/2 40h

AEs: bleeding, bruising, Purple Toe Syndrome, Warfarin-Induced Skin Necrosis

Warnings/Precautions: risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: pregnancy, unsupervised patients with ↑ risk of noncompliance, active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Monitor: INR goal for AFib/VTE: 2-3, INR goal for mechanical mitral valve: 2.5-3.5; inpatient: check day 3, then every 1-2 days, outpatient: check every 3-5 days, recheck within 7-14 days of any dose adjustment, once stable, reduce checks to every 4-6 weeks

Enoxaparin (Lovenox)

Indications: VTE prophylaxis and treatment; ACS; AFib

Dosing: [dosed using ABW] VTE prophylaxis: 40mg SQ Q24H (CrCl <30 = 30mg SQ Q24H); VTE & AFib Treatment: 1mg/kg SQ Q12H (CrCl <30 = 1mg/kg SQ Q24H); ACS Treatment: (age <75 30mg bolus followed in 15 min by 1mg/kg SQ Q12H - max 100mg 1st 2 doses) (age ≥75 NO bolus, 0.75mg/kg SQ Q12H - max 75mg 1st 2 doses) (anyone CrCl <30 1mg/kg Q24H); reversal protamine sulfate

Major Drug Interactions: NSAIDs; anti-platelets

MOA: LMWH; indirect selective inhibitor of factor Xa & IIa via antithrombin (activating the inhibitor)

AEs: bleeding, bruising, osteoporosis/osteopenia

Warnings/Precautions: risk of spinal/epidural hematoma after neuraxial intervention, HIT; avoid in CrCl <15 and dialysis

Contraindications: hypersensitivity to pork; history of HIT within past 100 days; active bleeding, PUD

Counseling/Patient Education: report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Monitor: none required; anti-factor Xa levels drawn for pregnancy, weight <50kg or >155kg, CrCl <30 - draw 4-6h post-third or fourth dose; CBC; SCr

Dabigatran (Pradaxa)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE Treatment: 150mg PO BID (avoid in CrCl < 30); AFib Treatment: 150mg PO BID (CrCl <30 or CrCl 30-50 with dronedarone: 75mg PO BID) (avoid in CrCl <15 for stroke prevention in non-valv AFib); for VTE initiate after 5-10 days of parenteral anticoag; reversal Idarucizumab 5g [2.5g IV given ≤ 15 min apart]

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible direct thrombin inhibitor; hydrolyzed by esterases then glucuronidation to active isomers

AEs: dyspepsia, bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: pregnancy, active bleeding, PUD

Counseling/Patient Education: store/administer from original container (stable 4 months); swallow whole; avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Rivaroxaban (Xarelto)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE prophylaxis: 10mg PO daily, VTE Treatment: 15mg PO BID x21 days, then 20mg daily (CrCl < 30 C/I); AFib Treatment: 20mg daily with dinner (CrCl 15-50: 15mg daily with dinner, CrCl <15 C/I); for VTE initiate after 5-10 days of parenteral anticoag; reversal Andexanet alfa

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor; absolute bioavailability is dose-dependent (lower bioavailability with doses ≥ 15mg)

AEs: bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: CrCl <30, active bleeding, PUD

Counseling/Patient Education: doses ≥ 15mg should be taken in evening with food for best absorption - < 15mg can be taken without regard to food); avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Apixaban (Eliquis)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE prophylaxis: 2.5mg PO BID (begin 12-24h post-op, duration: hip (35 days), knee (12 days)); VTE Treatment: 10mg PO BID x7 days, then 5mg BID (dose adjust for age ≥ 80 and < 60 or SCr ≥ 1.5 - decrease to 2.5mg BID after 6 months to decrease risk); AFib Treatment: 5mg PO BID; for VTE initiate after 5-10 days of parenteral anticoag; reversal Andexanet alfa

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor

AEs: bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Edoxaban (Savaysa)

Indications: non-valvular AFib; VTE Treatment

Dosing: VTE & AFib

Treatment: 60mg PO daily (CrCl 15-50 or <60kg: 30mg daily, CrCl <15 or >95 C/I); for VTE initiate after 5-10 days of parenteral anticoag; no reversal

Major Drug Interactions: CYP3A4 and Pgp substrate - limit to 30mg/day when using specific Pgp inhibitors (verapamil, azithromycin, clarithromycin, erythromycin); NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor; absolute bioavailability is dose-dependent (lower bioavailability with doses ≥ 15mg)

AEs: dyspepsia, bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: active bleeding, PUD

Counseling/Patient Education: doses ≥ 15mg should be taken in evening with food for best absorption - < 15mg can be taken without regard to food); avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Diuretics

Furosemide (Lasix)

Indications: edema, HTN, ascites

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; t1/2 is 6h; oral bioavailability is 50%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Bumetanide (Bumex)

Indications: edema

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; bioavailability is 80-90%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Torsemide (Demadex)

Indications: edema, HTN

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; bioavailability is 80%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Hydrochlorothiazide

Indications: edema, HTN

Dosing: less effective at CrCl <30; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: acute closure glaucoma, hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Indapamide (Lozol)

Indications: edema, HTN

Dosing: if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients; common in elderly patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Chlorthalidone

Indications: edema, HTN

Dosing: preferred option for thiazides - CVD reduction; avoid with CrCl <10; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; t1/2 is 40-60h

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Metolazone (Zaroxolyn)

Indications: edema, HTN

Dosing: can use in CrCl <30; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients; mainly used inpatient bc of potency (outpatient use can cause electrolyte disturbances if not monitored); often used as a 2nd diuretic or dosed QOD

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: the most potent thiazide; inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Spironolactone (Aldactone)

Indications: HTN, HFrEF, primary aldosteronism, cirrhosis

Dosing: [initial] 12.5mg daily, [target] 25mg daily; not recommended CrCl <30

Major Drug Interactions: ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: non-selective aldosterone AND sex hormone antagonism; direct antagonism of aldosterone binding to mineralocorticoid receptors ∴ ↓ expression of ENaCs, K+ channels, and H+ATPase on lumen ∴ blocking reabsorption of Na+ and H2O into peritubular capillaries while maintaining serum K+

AEs: gynecomastia, hyperkalemia, renal insufficiency, nausea, impotence/dec. libido, breast tenderness, irregular menses, hyperuricemia, hyperchloremia metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout

Contraindications: hyperkalemia, renal insufficiency, anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

Eplerenone (Inspra)

Indications: HTN, HFrEF post-MI

Dosing: [initial] 25mg daily, [target] 50mg daily; not recommended CrCl <30

Major Drug Interactions: CYP3A4 substrate; ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: selective aldosterone antagonism; direct antagonism of aldosterone binding to mineralocorticoid receptors ∴ ↓ expression of ENaCs, K+ channels, and H+ATPase on lumen ∴ blocking reabsorption of Na+ and H2O into peritubular capillaries while maintaining serum K+

AEs: hyperkalemia, renal insufficiency, hyperuricemia, hyperchloremia metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout

Contraindications: hyperkalemia (serum K+ ≥5.5), CrCl ≤30, use of potent 3A4 inhibitors, HTN plus (T2DM with albuminuria or SCr >2 [men] >1.8 [women] or CrCl <50 or use of K+ supps), anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

Triamterene/HCTZ (Dyazide, Maxzide)

Indications: HTN, edema

Dosing: 37.5/25mg (Dyazide); 75/50mg (Maxzide); not recommended CrCl <30

Major Drug Interactions: ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: inhibits ENaC in collecting duct ∴ blocking reabsorption of Na+ and H2O while ↑ K+ in blood

AEs: hyperkalemia, renal insufficiency, hyperchloremic metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: kidney stones, [BBW] fluid & electrolyte losses; [BBW] hyperkalemia; DM, gout

Contraindications: hyperkalemia, renal insufficiency, anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

ACE-Inhibitors

Ramipril (Altace)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: [initial] 1.25-2.5mg daily; HFrEF target dose: 5mg BID

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Benazepril (Lotensin)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing:

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Enalapril (Vasotec)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: [initial] 2.5mg BID, [target] 10-20mg BID

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Lisinopril (Zestril)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: preferred in liver disease bc not hepatically metabolized (not a prodrug); [initial] 2.5-5mg daily; [target] 40mg daily - can dose BID for HTN

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

ARBs

KH

Practice Final

Beta-Blockers

Propranolol (Inderal LA/XL)

Indications: HTN, chronic stable angina, migraine prophylaxis AND treatment (off-label - thyroid storm, portal HTN)

Dosing: tablets, SR capsules, solution, IV; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 and 1A2 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 and β2 activity - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia; crosses the BBB (MOST lipophilic BB)

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take on empty stomach; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING); monitor in concomitant CHF for worsening sxs

Atenolol (Tenormin)

Indications: HTN, chronic stable angina

Dosing: renal dose adjustments; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 and β2 activity (only at high doses) - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia; does NOT cross BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING); monitor in concomitant CHF for worsening sxs

Metoprolol Tartrate (Lopressor)

Indications: HTN, chronic stable angina, AFib, post-MI

Dosing: IMMEDIATE RELEASE (BID dosing); tablets, IV; titrate q1-2 weeks to effect; taper off over 1-2 weeks if DCing; when converting from MetTart <—> MetSucc, the doses are interchangeable

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take with food to increase absorption; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Metoprolol Succinate (Toprol XL)

Indications: HTN, chronic stable angina, HFrEF, post-MI

Dosing: EXTENDED RELEASE (initial dose: 12.5mg QD, target dose: 200mg QD); XL tablets; double dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing; when converting from MetTart <—> MetSucc, the doses are interchangeable

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take without regard to food; do NOT crush or chew - can score tablet; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Bisoprolol (Zebeta)

Indications: HTN, (off-label: HFrEF)

Dosing: renal dose adjustments (initial dose: 1.25mg QD, target dose: 100mg QD); double dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB; 50% hepatic + 50% renal elimination

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Nebivolol (Bystolic)

Indications: HTN

Dosing: titrate dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 substrate with active metabolite; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: the MOST β1 selective - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation; crosses the BBB; 50% hepatic + 50% renal elimination

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Carvedilol (Coreg, SR)

Indications: HTN, HFrEF

Dosing: IR (initial dose: 3.125mg BID, target dose ≤ 85kg: 25mg BID, target dose > 85kg: 50mg BID) XR (initial dose: 10mg QD, target dose: 80mg QD); tablets, SR capsules; titrate dose q1-2 weeks to effect; taper off over 1-2 weeks if DCing

Major Drug Interactions: CYP2D6 substrate; drugs with additive HR-reducing effects; clonidine; non-DHP CCBs; NSAIDs

MOA: β1, β2, and α1 activity - β1 antagonism is the heart and kidneys ∴ slows HR, lowers BP, blocks heart remodeling, limits arrhythmias, induces vasodilation - partial β2 agonism is lungs and periphery ∴ bronchoconstriction, peripheral vasoconstriction, hypoglycemia - α1 antagonism is vascular smooth muscle ∴ increases vasodilation, increases HR and CO initially; crosses BBB

AEs: bradycardia, orthostatic hypotension, dizziness, withdrawal sxs with abrupt DC, CNS depression

Warnings/Precautions: COPD, DM, [BBW] for ischemic heart disease gradual tapering bc it can cause angina or MI if abruptly stopped!

Contraindications: asthma; severe bradycardia; 2nd/3rd degree heart block; cardiogenic shock; decompensated HF

Counseling/Patient Education: take with food to decrease absorption and avoid orthostasis; rise slowly from sitting/laying position (esp. 1st dose); take consistently to prevent rebound HTN; masks hypoglycemia sxs (EXCEPT SWEATING), monitor in concomitant CHF for worsening sxs

Ranolazine (Ranexa)

Indications: chronic stable angina (2nd Line)

Dosing: XL tablets; hepatic dose adjustments (↓ dose 50% if cirrhosis)

Major Drug Interactions: strong CYP3A4 substrate - do NOT exceed 20mg simvastatin; moderate 3A4 inhibitors (diltiazem, verapamil) - do NOT exceed 500mg BID of ranexa; minor 2D6 substrate; Pgp inhibitors; digoxin; metformin

MOA: inhibits the late Na+ ion channels (INa) ∴ ↓ angina frequency

AEs: QTc prolongation, constipation, hypotension, dizziness, headache

Contraindications: strong 3A4 inhibitors/inducers; liver cirrhosis

Counseling/Patient Education: avoid grapefruit juice; do NOT crush or chew

Digoxin (Lanoxin)

Indications: HFrEF, AFib

Dosing: renal dose adjustments; 0.125-0.250mg QD - LD given for AFib before reducing to this MD; tablets, capsules, solution, injection

Major Drug Interactions: Pgp substrate (amiodarone, verapamil, diltiazem), diuretics

MOA: Na/K-ATPase inhibitor leading to myocardial Ca influx and increased contractility; increases vagal (parasympathetic) tone; positive inotrope, negative chronotrope

AEs: mild GI upset, bradycardia, CNS effects, digoxin toxicity (N/V, green/yellow halos, cardiac arrhythmias, low K/Mg and high Ca)

Warnings/Precautions: AV block, digoxin toxicity (DigiFab is antidote)

Contraindications: ventricular fibrillation

Counseling/Patient Education: caution use of OTC antacids, laxatives, anti-diarrheals

Monitor: draw serum concentrations at steady state (3-5 days), at least 6-8h after last dose (optimally 12-24h); HFrEF goal: 0.5-0.9 ng/mL, AFib goal: 0.8-2 ng/mL

Ivabradine (Corlanor)

Indication: decreases HF hospitalization in patients who are stable, symptomatic, have EF ≤ 35%, are in sinus rhythm with HR ≥ 70 BPM on max BB therapy or C/I to BB

decreases HR without affecting BP in HFrEF

Nitrates

Isosorbide Dinitrate IR/ER

Indications: angina, CAD, HF

Dosing: IR (TID with 4-5h break ∴ 8-1-6 schedule), ER (BID with 6h break ∴ 8-2 schedule); NITRATE-FREE INTERVALS (≥ 14h IR; > 18h ER)

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: venous vasodilator

AEs: headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: nitrate-free interval administration

Isosorbide Mononitrate (Imdur)

Indications: angina, CAD, HF

Dosing: IR (BID with 7h break ∴ 8-3 schedule), ER (once daily QAM); NITRATE-FREE INTERVALS (≥ 14h IR; > 18h ER)

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: venous vasodilator

AEs: headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: nitrate-free interval administration; do NOT crush XR tabs, swallow whole

Nitroglycerin (Nitrostat)

Indications: acute angina (off-label: 5-10min pre-activity)

Dosing: sublingual tablets; 3 tablets 5 minutes PRN (if no relief 3-5min after 1st tab, call 911)

Major Drug Interactions: ethanol, arterial vasodilators (C

CBs)

MOA: venous vasodilator

AEs: reflex tachycardia, headaches (50%), dizziness, flushing, nausea

Warnings/Precautions: orthostatic hypotension, bradycardia, tachyphylaxis with daily/long-term use

Contraindications: concomitant use with PDE5i

Counseling/Patient Education: SIT DOWN before using; store in original amber vial; discard after 6-12 months

Hydralazine (Apresoline)

Indications: HTN (off-label: HFrEF ± nitrate)

Dosing: BID-QID

Major Drug Interactions: ethanol, arterial vasodilators (CCBs)

MOA: arterial vasodilator

AEs: fluid retention, reflex tachycardia, hypotension, dizziness, peripheral neuritis, blood dyscrasias

Warnings/Precautions: drug-induced lupus with long-term use (doses > 200mg/day)

Contraindications: CAD

Counseling/Patient Education: take with food; report any general fatigue/ body aches

Anti-Platelets

Clopidogrel (Plavix)

Indications: post-ACS, PCI, CVA

Dosing: 75mg daily

Major Drug Interactions: CYP2C19 substrate; NSAIDs; anticoagulants; PPIs (pantoprazole least likely to interact); fluoxetine

MOA: P2Y12 Inhibitor (thienopyridine); irreversibly bind and inhibit P2Y12 for the whole life of the platelet - indirectly acting ∴ needs to be metabolized to become active

AEs: bleeding, bruising

Warnings/Precautions: [BBW] CYP2C19 poor metabolizers (Asians)

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Prasugrel (Effient)

Indications: post-ACS, PCI

Dosing:

Major Drug Interactions: CYP3A4 and 2B6 substrate; NSAIDs; anticoagulants

MOA: more potent P2Y12 Inhibitor (thienopyridine); irreversibly bind and inhibit P2Y12 for the whole life of the platelet - indirectly acting ∴ needs to be metabolized to become active

AEs: bleeding, bruising

Warnings/Precautions: [BBW] avoid with age ≥ 75 unless DM s/p MI (high risk)

Contraindications: prior TIA/CVA, active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Ticagrelor (Brilinta)

Indications: ACS with PCI

Dosing:

Major Drug Interactions: CYP3A4 and Pgp substrate - avoid lovastatin/simvastatin > 40mg/day; NSAIDs; anticoagulants

MOA: P2Y12 Inhibitor (non-thienopyridine); reversibly bind and inhibit P2Y12 for the whole life of the platelet - directly acting ∴ doesn’t need to be metabolized to become active

AEs: dyspnea, bradyarrhythmias, hyperuricemia, bleeding, bruising

Warnings/Precautions: [BBW] ASA doses > 100mg/day decrease efficacy in patients with ACS

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Cilostazol (Pletal)

Indications: intermittent claudication

Dosing:

Major Drug Interactions: CYP3A4 and 2C19 substrate - diltiazem, MANY others

MOA: reversibly inhibits phosphodiesterase, PDE ↓ cAMP in ALL CELLS ∴ many downstream effects, PDE inhibitors ∴ induce vasodilation

AEs: headache, diarrhea, dizziness, palpitations, infection, rhinitis

Warnings/Precautions: tachycardia, hypotension, arrhythmia, hematologic effects

Contraindications: congestive HF of any severity

Counseling/Patient Education: avoid grapefruit juice; take on empty stomach; may take up to 12 weeks to see full effect

Anti-Coagulants

Warfarin (Coumadin)

Indications: valvular AFib, mechanical heart valves, VTE

Dosing: [initial] 5mg PO daily for first 1-2 days, then adjust based on INR, consider dropping starting dose to 2-3mg in elderly >60, low BW, HF, D/Is, low albumin, liver disease, decreased dose 10-20% may be required in eGFR <60; [maintenance] calculate total weekly dose and ↑/↓ by 5-20% (only when patient is within goal INR range), steady state usually achieved within 10-14 days; reversal (INR >10 + no big bleeds = PO Kcentra, any INR + big bleeds = IV Kcentra)

Major Drug Interactions: major CYP2C9 substrate - BAM-IF; NSAIDs; anti-platelets

↑ bleeding risk (no effect on INR): NSAIDs, SSRIs (serotonin is a platelet activator), thrombolytics, antiplatelets
INHIBITS METABOLISM: Bactrim, Amiodarone, Metronidazole, Itraconazole, Fluconazole (BAM-IF), ACUTE alcohol use
displacement from albumin: phenytoin, valproic acid, ethacrynic acid
↓ vitamin K producing bacteria in GI: any antibiotic... theoretically
INDUCES METABOLISM: azathioprine, carbamazepine, rifampin, St Johns Wort, cigarettes, CHRONIC alcohol use
inhibit absorption: cholestyramine

MOA: irreversibly binds VKORC1 in hepatocytes ∴ inhibits synthesis of vitamin K-dependent clotting factors (VII, IX, X, II [Protein C & S]); t1/2 40h

AEs: bleeding, bruising, Purple Toe Syndrome, Warfarin-Induced Skin Necrosis

Warnings/Precautions: risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: pregnancy, unsupervised patients with ↑ risk of noncompliance, active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Monitor: INR goal for AFib/VTE: 2-3, INR goal for mechanical mitral valve: 2.5-3.5; inpatient: check day 3, then every 1-2 days, outpatient: check every 3-5 days, recheck within 7-14 days of any dose adjustment, once stable, reduce checks to every 4-6 weeks

Enoxaparin (Lovenox)

Indications: VTE prophylaxis and treatment; ACS; AFib

Dosing: [dosed using ABW] VTE prophylaxis: 40mg SQ Q24H (CrCl <30 = 30mg SQ Q24H); VTE & AFib Treatment: 1mg/kg SQ Q12H (CrCl <30 = 1mg/kg SQ Q24H); ACS Treatment: (age <75 30mg bolus followed in 15 min by 1mg/kg SQ Q12H - max 100mg 1st 2 doses) (age ≥75 NO bolus, 0.75mg/kg SQ Q12H - max 75mg 1st 2 doses) (anyone CrCl <30 1mg/kg Q24H); reversal protamine sulfate

Major Drug Interactions: NSAIDs; anti-platelets

MOA: LMWH; indirect selective inhibitor of factor Xa & IIa via antithrombin (activating the inhibitor)

AEs: bleeding, bruising, osteoporosis/osteopenia

Warnings/Precautions: risk of spinal/epidural hematoma after neuraxial intervention, HIT; avoid in CrCl <15 and dialysis

Contraindications: hypersensitivity to pork; history of HIT within past 100 days; active bleeding, PUD

Counseling/Patient Education: report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Monitor: none required; anti-factor Xa levels drawn for pregnancy, weight <50kg or >155kg, CrCl <30 - draw 4-6h post-third or fourth dose; CBC; SCr

Dabigatran (Pradaxa)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE Treatment: 150mg PO BID (avoid in CrCl < 30); AFib Treatment: 150mg PO BID (CrCl <30 or CrCl 30-50 with dronedarone: 75mg PO BID) (avoid in CrCl <15 for stroke prevention in non-valv AFib); for VTE initiate after 5-10 days of parenteral anticoag; reversal Idarucizumab 5g [2.5g IV given ≤ 15 min apart]

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible direct thrombin inhibitor; hydrolyzed by esterases then glucuronidation to active isomers

AEs: dyspepsia, bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: pregnancy, active bleeding, PUD

Counseling/Patient Education: store/administer from original container (stable 4 months); swallow whole; avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Rivaroxaban (Xarelto)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE prophylaxis: 10mg PO daily, VTE Treatment: 15mg PO BID x21 days, then 20mg daily (CrCl < 30 C/I); AFib Treatment: 20mg daily with dinner (CrCl 15-50: 15mg daily with dinner, CrCl <15 C/I); for VTE initiate after 5-10 days of parenteral anticoag; reversal Andexanet alfa

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor; absolute bioavailability is dose-dependent (lower bioavailability with doses ≥ 15mg)

AEs: bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: CrCl <30, active bleeding, PUD

Counseling/Patient Education: doses ≥ 15mg should be taken in evening with food for best absorption - < 15mg can be taken without regard to food); avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Apixaban (Eliquis)

Indications: non-valvular AFib; VTE; DVT prophylaxis post knee/hip replacement

Dosing: VTE prophylaxis: 2.5mg PO BID (begin 12-24h post-op, duration: hip (35 days), knee (12 days)); VTE Treatment: 10mg PO BID x7 days, then 5mg BID (dose adjust for age ≥ 80 and < 60 or SCr ≥ 1.5 - decrease to 2.5mg BID after 6 months to decrease risk); AFib Treatment: 5mg PO BID; for VTE initiate after 5-10 days of parenteral anticoag; reversal Andexanet alfa

Major Drug Interactions: CYP3A4 and Pgp substrate; NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor

AEs: bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: active bleeding, PUD

Counseling/Patient Education: avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Edoxaban (Savaysa)

Indications: non-valvular AFib; VTE Treatment

Dosing: VTE & AFib

Treatment: 60mg PO daily (CrCl 15-50 or <60kg: 30mg daily, CrCl <15 or >95 C/I); for VTE initiate after 5-10 days of parenteral anticoag; no reversal

Major Drug Interactions: CYP3A4 and Pgp substrate - limit to 30mg/day when using specific Pgp inhibitors (verapamil, azithromycin, clarithromycin, erythromycin); NSAIDs; anti-platelets

MOA: reversible factor Xa inhibitor; absolute bioavailability is dose-dependent (lower bioavailability with doses ≥ 15mg)

AEs: dyspepsia, bleeding, bruising

Warnings/Precautions: advanced hepatic/renal impairment; risk of spinal/epidural hematoma after neuraxial intervention

Contraindications: active bleeding, PUD

Counseling/Patient Education: doses ≥ 15mg should be taken in evening with food for best absorption - < 15mg can be taken without regard to food); avoid grapefruit juice; report any unusual bleeding; inform all physicians/dentists of use - must be held several days before major procedures

Diuretics

Furosemide (Lasix)

Indications: edema, HTN, ascites

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; t1/2 is 6h; oral bioavailability is 50%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Bumetanide (Bumex)

Indications: edema

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; bioavailability is 80-90%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Torsemide (Demadex)

Indications: edema, HTN

Dosing: no max; furosemide 20mg IV = furosemide 40mg PO = torsemide 20mg IV/PO = bumetanide 1mg IV/PO

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NKCC2 cotransporter in thick ascending limb ∴ blocking reabsorption of Na+, Cl-, H2O, Mg2+, Ca2+ into the peritubular capillaries and K+ secretion into the tubular lumen (primarily K+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; bioavailability is 80%

AEs: hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypocalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, ototoxicity, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Hydrochlorothiazide

Indications: edema, HTN

Dosing: less effective at CrCl <30; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: acute closure glaucoma, hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Indapamide (Lozol)

Indications: edema, HTN

Dosing: if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients; common in elderly patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Chlorthalidone

Indications: edema, HTN

Dosing: preferred option for thiazides - CVD reduction; avoid with CrCl <10; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow; t1/2 is 40-60h

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Metolazone (Zaroxolyn)

Indications: edema, HTN

Dosing: can use in CrCl <30; if taken with loops, give thiazide 30 min prior to loop; preferable in African American patients; mainly used inpatient bc of potency (outpatient use can cause electrolyte disturbances if not monitored); often used as a 2nd diuretic or dosed QOD

Major Drug Interactions: digoxin, NSAIDs, lithium, dofetilide

MOA: the most potent thiazide; inhibit NCC cotransporter in distal convoluted tubule ∴ blocking reabsorption of Na+, Cl-, H2O into the peritubular capillaries and increasing reabsorption of Ca2+ (primarily Na+ wasting); also induces expression of COX2 ∴ increasing renal blood flow

AEs: hyperglycemia (high doses), hypokalemic metabolic acidosis, hyperuricemia, hypomagnesemia, hypercalcemia, hyponatremia, azotemia, xerostomia, dizziness/weakness, muscle cramps, photosensitivity

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout, sulfa allergy

Contraindications: anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Spironolactone (Aldactone)

Indications: HTN, HFrEF, primary aldosteronism, cirrhosis

Dosing: [initial] 12.5mg daily, [target] 25mg daily; not recommended CrCl <30

Major Drug Interactions: ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: non-selective aldosterone AND sex hormone antagonism; direct antagonism of aldosterone binding to mineralocorticoid receptors ∴ ↓ expression of ENaCs, K+ channels, and H+ATPase on lumen ∴ blocking reabsorption of Na+ and H2O into peritubular capillaries while maintaining serum K+

AEs: gynecomastia, hyperkalemia, renal insufficiency, nausea, impotence/dec. libido, breast tenderness, irregular menses, hyperuricemia, hyperchloremia metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout

Contraindications: hyperkalemia, renal insufficiency, anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

Eplerenone (Inspra)

Indications: HTN, HFrEF post-MI

Dosing: [initial] 25mg daily, [target] 50mg daily; not recommended CrCl <30

Major Drug Interactions: CYP3A4 substrate; ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: selective aldosterone antagonism; direct antagonism of aldosterone binding to mineralocorticoid receptors ∴ ↓ expression of ENaCs, K+ channels, and H+ATPase on lumen ∴ blocking reabsorption of Na+ and H2O into peritubular capillaries while maintaining serum K+

AEs: hyperkalemia, renal insufficiency, hyperuricemia, hyperchloremia metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: [BBW] fluid & electrolyte losses; DM, gout

Contraindications: hyperkalemia (serum K+ ≥5.5), CrCl ≤30, use of potent 3A4 inhibitors, HTN plus (T2DM with albuminuria or SCr >2 [men] >1.8 [women] or CrCl <50 or use of K+ supps), anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

Triamterene/HCTZ (Dyazide, Maxzide)

Indications: HTN, edema

Dosing: 37.5/25mg (Dyazide); 75/50mg (Maxzide); not recommended CrCl <30

Major Drug Interactions: ACEi/ARBs, K+ sparing meds, K+ supplements, digoxin, NSAIDs, lithium, dofetilide

MOA: inhibits ENaC in collecting duct ∴ blocking reabsorption of Na+ and H2O while ↑ K+ in blood

AEs: hyperkalemia, renal insufficiency, hyperchloremic metabolic acidosis, azotemia, xerostomia, dizziness/weakness, muscle cramps

Warnings/Precautions: kidney stones, [BBW] fluid & electrolyte losses; [BBW] hyperkalemia; DM, gout

Contraindications: hyperkalemia, renal insufficiency, anuria, severe electrolyte depletion

Counseling/Patient Education: take in AM with food or milk; avoid OTC laxatives

Monitor: check serum K+ in 3 days, at 1 week, and then monthly for 3 months after initiation

ACE-Inhibitors

Ramipril (Altace)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: [initial] 1.25-2.5mg daily; HFrEF target dose: 5mg BID

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Benazepril (Lotensin)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing:

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Enalapril (Vasotec)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: [initial] 2.5mg BID, [target] 10-20mg BID

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

Lisinopril (Zestril)

Indications: HTN, HFrEF, diabetic nephropathy, post-ACS

Dosing: preferred in liver disease bc not hepatically metabolized (not a prodrug); [initial] 2.5-5mg daily; [target] 40mg daily - can dose BID for HTN

Major Drug Interactions: K+ sparing meds, K+ supplements, NSAIDs, lithium, RAAS inhibitors, Entresto (36h washout period)

MOA: inhibit conversion of Angiotensin I to Angiotensin II ∴ ↓ BP and ↑ natriuresis; inhibits degradation of bradykinin ∴ cardioprotective!; ↑ renin production due to compensation for ↓ AngII effects; extra AngI metabolized and ↑ vasodilation ∴ cardioprotective!; NOT effective for primary aldosteronism (give MRA instead); also renoprotective!; ↓ TPR (arteriolar vasodilation); little effect on baroreceptors (∴ ↓ exercise & postural CV changes)

AEs: [higher risk in African Americans] dry cough, angioedema, hyperkalemia, renal dysfunction (30% increase in SCr after initiation), hypotension, dizziness

Warnings/Precautions: [BBW] fetal toxicity; bilateral renal artery stenosis; impaired renal function; breastfeeding moms; patients currently on aggressive diuretics, NSAID, and/or CHF

Contraindications: previous angioedema from ACEi or idiopathic/hereditary; pregnancy; concomitant use with aliskiren in patients with DM; concomitant use or within 36h of switching to or from Entresto

Counseling/Patient Education: take in the morning; report any facial swelling/difficulty breathing; dry cough; orthostasis counseling; avoid K+ supplements

ARBs

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