Cardio Flashcards
Heparin
Anticoagulant Surgical anticoag, unstable angina, thromb/isc stroke Complex with AT Inhibits factors 10a and 2a Indirectly inhibits 7a SE: Bleeding, HIT, osteoporosis, alopecia IV and subcu APTT
LMWH
Low molecule weight heparin Anticoagulant Prophy/Tx of DVT and ACS Complex with AT, inhibits 10a and 2a SE: Bleeding DO NOT GIVE TO HIT (still cross-rx) Subcu Better bioavailability and duration of action than hep
Fondaparinux
Anticoagulant Management of DVT Complex with AT, inhibits 10a and 2a SE: Bleeding Subcu
Argatroban
Anticoagulant Management of HIT Directly inhibits IIa SE: Bleeding DO NOT GIVE IN DIC IV
Bivalirudin
Anticoagulant Management in HIT Directly inhibits IIa SE: Bleeding IV
Hirudin
Anticoagulant Management of HIT DIrectly inhibits IIa SE: Bleeding IV
Antithrombin Concentrates
Anticoagulant DIC, sepsis, thrombophilia, hypercoagulable state Directly inhibits IIa NO ADVERSE EFFECTS IV
Protamine Sulfate
(anti-)Anticoagulant REVERSAL FOR HEPARIN SE: Bradycardia, hypotension IV Highly basic
Warfarin
Oral Anticoagulant
Tx of DVT and a.fib
Comp antag of vit K, factor 2,7,9,10 not synthesized
SE: Bleeding, necrosis
Contras: emergency (hep is faster), high vit K diet, PREGGOS, multiple drug interactions (potential warfarin/inc bleeding)
PT/INR
Vitamin K
Oral (anti)Anticoagulant
Hypoprothrombinemia, reverse effects of warfarin
Cofactor in synth of factor 2,7,9,10
SE: Hemolysis
Rivaroxaban
Oral anti-Xa Oral Anticoagulant Stroke prevention in a.fib, prophy/tx of DVT Inhibits factor Xa SE: Bleeding, liver toxicity
Apixaban
Oral anti-Xa Oral Anticoagulant Stroke prevention in a.fib Inhibits factor Xa SE: Bleeding, liver toxicity
Dabigatran
Oral Anticoagulant
Stroke prevention in a.fib
Inhibits thrombin
SE: Bleeding, liver toxicity
Aspirin
Antiplatelet drug ACS, stroke, arterial thrombosis COX inhibitor SE: bleeding, gastic irritation PO
Clopidogrel
Antiplatelet drug ACS, stroke, arterial thrombosis ADP receptor inhibitor SE: bleeding, TTP Prodrug, liver turns it into active metabolite PO
Prasugrel
Antiplatelet drug ACS, stroke, arterial thrombosis ADP receptor inhibitor SE: bleeding Better response than plavix, is also a prodrug PO
Ticagrelor
Antiplatelet drug ACS, stroke, arterial thrombosis ADP receptor inhibitor SE: bleeding Is not a pro drug, CAN BE USED IN LIVER FAILURE PO
NSAIDs
Antiplatelet drug Various diseases COX inhibitor Bleeding PO
Dipyridamole
Antiplatelet drug Arterial thrombosis, stroke Phosphodiesterase inhibitor (increases cAMP, blocks platelet aggregation response) SE: Bleeding Also a coronary vasodilator PO
Cilostazol
Antiplatelet drug Intermittent claudication Phosphodiesterase inhibitor SE: hypotension PO
Abciximab
Antiplatelet drug ACS/PCI GPIIb/IIIa inhibitor SE: Bleeding IV
Eptifibatide
Antiplatelet drug ACS/PCI GPIIb/IIa inhibitor SE: Bleeding IV
Tirofiban
Antiplatelet drug ACS/PCI GPIIb/IIIa inhibitor SE: Bleeding IV
Monteleukast (singulair)
Antiplatelet drug Asthma and seasonal allergies Leukotriene receptor inhibitor (dec. vasoconstriction, vascular permeability, inflammatory response) SE: Hypotension, behavioral changes PO
Zafirleukast
Antiplatelet drug Asthma Leukotriene receptor inhibitor (dec. vasoconstriction, vascular permeability, inflammatory response) SE: hypotension PO
Zieuton
Antiplatelet drug Asthma Lipoxygenase inhibitor (dec. vasoconstriction, vascular permeability, inflammatory response) SE: hypotension PO
Streptokinase
Thrombolytic agent Thrombolysis, stroke, MI, PE, DVT Fibrinolytic, activates plasmin SE: Bleeding Contra: INTRACRANIAL BLEEDING IV
Urokinase
Thrombolytic agent
Thrombolysis, stroke, MI, PE
tPA
Tissue plasminogen activator Thrombolytic agent Thrombolysis, stroke MI Fibrinolytic, activates plasmin SE: Bleeding Contra: INTRACRANIAL BLEEDING IV
EACA
Epsilon amino caproic acid (AMICAR) (anti) Thrombolytic agent Reversal of bleeding Anti-fibrinolytic, inhibits plasmin SE: Hypotension IV
Aprotonin
(anti) Thrombolytic agent Reversal of bleeding Anti-fibrinolytic SE: Graft thrombosis IV
Ancrod
Thrombolytic agent Fibrinolytic SE: allergic rxn Contra: INTRACRANIAL BLEEDING IV Derivative of snake venom
Tranexamic acid
(AMCHA) (anti) Thrombolytic agent Reversal of bleeding SE: retinopathy IV
Rosuvastatin (Crestor)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: CYP2C9 inhibitors inc [ ], gemfibrozil decreases OAT2P inc inc [STATIN]
Most potent
Atorvastatin (Lipitor)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: CYP34A inhibitors (increase risk of SE), GRAPEFRUIT JUICE, gemfibrozil (decreases OAT2P, inc inc [STATIN])
Simvastatin (Zocor)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: CYP34A inhibitors (increase risk of SE), GRAPEFRUIT JUICE, gemfibrozil (decreases OAT2P, inc [STATIN])
Pravastatin (Pravachol)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: gemfibrozil (decreases OAT2P, inc [STATIN])
Less rhabdo, no CYP 450, liver/renal excretion
Lovastatin (Mevacor)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: CYP34A inhibitors (increase risk of SE), GRAPEFRUIT JUICE, gemfibrozil (decreases OAT2P, inc [STATIN])
Fluvastatin (Lescol)
Anti-hyperlipidemic agent
STATIN
High LDL
Inhibits HMG-COA reductase, SREBP triggered, increased LDL-R expression and LDL CLEARANCE
SE: Muscle myalgia/myopathy, RHABDOMYOLYSIS, hepatitis
Contra: severe liver disease
Decrease LDL, decrease TG, increased HDL
Drug interaction: CYP2C9 inhibitors inc [ ], gemfibrozil decreases OAT2P inc inc [STATIN]
Least Potent
Cholestyramine
Anti-hyperlipidemic agent Bile Acid-Binding resin High LDL Prevents reabsorption of bile acids, inc. chol 7alpha-hydroxylase, dec. cholesterol, inc. LDL-R, inc. cholesterol clearance SE: INCREASE TG (can cause pancreatitis) Contra: TG > 400 mg/dL Decreases LDL Interferes with drug absorption (warfarin, phenobarb, digoxin, tetracycline) OK for kiddos and PREGGOS Impairs absorption of ADEK
Colestipol
Anti-hyperlipidemic agent Bile Acid-Binding resin High LDL Prevents reabsorption of bile acids, inc. chol 7alpha-hydroxylase, dec. cholesterol, inc. LDL-R, inc. cholesterol clearance SE: INCREASE TG (can cause pancreatitis) Contra: TG > 400 mg/dL Decreases LDL Interferes with drug absorption (warfarin, phenobarb, digoxin, tetracycline) OK for kiddos and PREGGOS Impairs absorption of ADEK
Colesevelam
Anti-hyperlipidemic agent Bile Acid-Binding resin High LDL Prevents reabsorption of bile acids, inc. chol 7alpha-hydroxylase, dec. cholesterol, inc. LDL-R, inc. cholesterol clearance SE: INCREASE TG (can cause pancreatitis) Contra: TG > 400 mg/dL Decreases LDL No drug interference OK for kiddos and PREGGOS
Ezetimibine
Anti-hyperlipidemic agent Inhibitor of Cholesterol Absorption High LDL Blocks NPCL1 chol abs. in GI, dec. hepatic chol, inc. LDL-R, inc. LDL clearance SE: Well-tolerate, flatulance, diarrhea Dec. LDL
Alirocumab
Anti-hyperlipidemic agent
Inhibitors of PCSK9
Hetero FH, high LDL not controlled with max STATIN, STATIN intolerance
Inhibits PCSK9, dec. LDL-R degredation by lysosome, inc. LDL clearance
SE: Unknown, too new
Decreased LDL
Injected subcu q 2 weeks
Evolocumab
Anti-hyperlipidemic agent
Inhibitors of PCSK9
Hetero FH, high LDL not controlled with max STATIN, STATIN intolerance
Inhibits PCSK9, dec. LDL-R degredation by lysosome, inc. LDL clearance
SE: Unknown, too new
Decreased LDL
Injected subcu q 2 weeks
Lomitapide
Anti-hyperlipidemic agent
Homo FH
Inhibits MTP (TG transfer protein) in GI and liver, dec. production of chylo/VLDL/LDL
SE: Hepatotoxicity
Contra: PREGGOS
Dec. chylo/VLDL/LDL
Drug interaction: is a CYP34A and P-gp inhibitor
Mipomersen
Anti-hyperlipidemic agent Homo FH Antisense oligo, specfici for apoB100, inc. expression apoB100, dec. VLDL/LDL SE: Hepatotoxicity Contra: mild/mod liver impairment Dec. VLDL/LDL
Niacin
Anti-hyperlipidemic agent
Hypertriglyceridema, high VLDL/LDL, low HDL
Many MoA: dec. lipolysis, inhibits DGAT2/VLDL synthesis, apoC3/inc LPL, inc. apoAI, dec.LP(a)/dec. thrombosis, dec. clots, dec. risk of MI/stroke)
SE: SKIN FLUSHING (tx with NSAIDs), GOUT, PEPTIC ULCERS, heperglycemia, hepatitis
Dec. TG/LDL, inc. HDL
MOST EFFECTIVE DRUG TO RAISE HDLs
Gemfibrozil
Anti-hyperlipidemic agent
Hypertriglyceridemia, high VLDL/LDL, low HDL
Dec. apoC3/inc. LPL expression/inc. FFA oxidation/dec. VLDL synthesis/inc.VLDL clearance, APOAI expression/inc.HDL
SE: GALLSTONES, hepatitis, myopathy, RHABDOMYOLYSIS
Contra: severe renal/hepatic disease
Drug interactions: strong protein binder so can knock warfarin/sulfas off, STATINs (inhibits OATP2 which increases [STATIN])
Fenofibrate
Anti-hyperlipidemic agent
Hypertriglyceridemia, high VLDL/LDL, low HDL
Dec. apoC3/inc. LPL expression/inc. FFA oxidation/dec. VLDL synthesis/inc.VLDL clearance, APOAI expression/inc.HDL
SE: GALLSTONES, hepatitis, myopathy, RHABDOMYOLYSIS (more common in Gem though)
Contra: severe renal/hepatic disease
Drug interactions: strong protein binder so can knock warfarin/sulfas off
L-NMMA
Nitric Oxide Inhibitor
Sepsis-related disorders
Binds arginine binding site in NOA
Non-selective NOS inhibitor
L-NAME
Nitric Oxide Inhibitor
Sepsis-related disorders
Binds arginine binding site in NOA
Non-selective NOS inhibitor
7-Nitroindazole
Nitric Oxide Inhibitor
Sepsis-related disorders
Binds arginine binding site in NOA
Partiall selective for NOS-1 in vivo
BBS-2
Nitric Oxide Inhibitor
Sepsis-related disorders
Inhibits iNOS dimerization
Weakly inhibits nNOS and eNOS
Hemoglobin
Nitric Oxide Inhibitor
Sepsis-related disorders
NO scavenger
NO (INOMAX)
NO Donor ACS Covalent modification of proteins SE: vasodilation Inhalation
Nitroglycerine
NO Donor
Pulmonary artery hypertension, exertional/variant/unstable angina
Rxs with vessel wall to increase [NO] in VSMC (causing venodilation)
SE: Orthostatic hypotension, reflex tachy, headache, nitrate tolerance
Contra: systemic hypotension
Sublingual
Hydralazine
NO Donor
Resistant/PREGGO Hypertension
NO donor, vasodilator
SE: Headache, nausea, vomiting, hypotension, tachycardia
Contra: long-term use
Drug interactions: NSAIDS REDUCE EFFECTIVENESS
PO
Sildenafil (Viagra)
NO Donor Hypertension Phosphodiesterase inhibitor SE: Hypotension, drug interactions (Nitro) PO
L-Arginine
NO Donor ACD, vascular disease NO Donor SE: Hypotension PO
Captopril
Vasoactive peptide
1stline drug in chronic chronic HTN, chronic CHF/a.fib
ACEI
SE: HYPERKALEMIA, rash, DRY COUGH, ANGIOEDEMA, severe stomach pain, chest pain, allergic reaction
Contra: PREGGOS, bilat renal stenosis
Drug interactions: exacerbates hyperK of K sparing drugs
PO
Short half life, multiple daily doses, active metabolites
PREVENTS LV REMODELING
Enalapril
Vasoactive peptide
1stline drug used in chronic HTN, chronic CHF/a.fib
ACEI
SE: HYPERKALEMIA, rash, DRY COUGH, ANGIOEDEMA, hypotension, severe stomach pain
Contra: PREGGOS, bilat renal stenosis
Drug interactions: exacerbates hyperK of K sparing drugs
PO
Converted to active metabolite, longer onset, longer t1/3, dose 1-2xday
PREVENTS LV REMODELING
Losartan
Vasoactive peptide
1stline drug used in chronic HTN, chronic CHF (esp if intolerant to ACEI)
Angiotensin receptor inhibitor (ARB)
SE: Diarrhea, insomnia, nasal congestion, HYPERKALEMIA
Contra: PREGGOS (causes renal failure)
Drug Interactions: K sparing drugs, hyperkalemic effects
PO
PREVENTS LV REMODELING
Valsartan
Vasoactive peptide Hypertension, chronic CHF (esp if intolerant to ACEI) Angiotensin receptor inhibitor (ARB) SE: stomach pain, nausea PO PREVENTS LV REMODELING
Icatibant
Vasoactive peptide Inflammatory responses Bradykinin receptor inhibitor SE: stomach pain, nausea PO
Aprotonin
Vasoactive peptide Inflammation Kallikrein inhibitor SE: MI, stroke, kidney failure IV
Desmopressin (DDAVP)
Vasoactive peptide Bleeding Vasopressin analogue SE: headache, stomach pain, nausea IV
Bosentan
Vasoactive peptide Pulmonary hypertension Endothelin receptor inhibitor SE: liver problems, stomach pain, nausea PO
Acetazolamide
Diuretic
Carbonic Anhydrase Inhibitor
Weak diuretic agent, inhibits CA in PROXIMAL TUBULE, reducing proximal HCO3 reabsorption
SE: Metabolic acidosis, hypokalemia (acute), CaPO3 stones, drowsiness, fatigue, CNS depression, paresthesia
Contra: cirrhosis
PO
Used in glaucoma, mountain sickness, raise urine pH
Organic ACID transporter
Dorzolamide
Diuretic
Carbonic Anhydrase Inhibitor
Weak diuretic agent, inhibits CA in PROXIMAL TUBULE, reducing proximal HCO3 reabsorption
SE: Metabolic acidosis, hypokalemia (acute), CaPO3 stones, drowsiness, fatigue, CNS depression, paresthesia
Contra: cirrhosis
PO
Used in glaucoma, mountain sickness, raise urine pH
Organic ACID transporter
Same as acetazolamide by 30x more potent
Methazolamide
Diuretic
Carbonic Anhydrase Inhibitor
Weak diuretic agent, inhibits CA in PROXIMAL TUBULE, reducing proximal HCO3 reabsorption
SE: Metabolic acidosis, hypokalemia (acute), CaPO3 stones, drowsiness, fatigue, CNS depression, paresthesia
Contra: cirrhosis
PO
Used in glaucoma, mountain sickness, raise urine pH
Organic ACID transporter
Same as acetazolamide, but 5x more potent
Dichlorphenamide
Diuretic
Carbonic Anhydrase Inhibitor
Weak diuretic agent, inhibits CA in PROXIMAL TUBULE, reducing proximal HCO3 reabsorption
SE: Metabolic acidosis, hypokalemia (acute), CaPO3 stones, drowsiness, fatigue, CNS depression, paresthesia
Contra: cirrhosis
PO
Used in glaucoma, mountain sickness, raise urine pH
Organic ACID transporter
Topic prep for ocular use (avoids systemic effects)
Mannitol
Osmotic diuretic
Tx or prevention of ARF
Reduce reabsorption of H2O and NaCl in proximal tubule
Contra: CHF, renal failure, pulmonary edema
SE: pulmonary edema, hyponatremia (in impaired renal function), hypernaturemia, nausea, vomiting, headache
No PO, IV only
Glycerol
Osmotic diuretic
Tx or prevention of ARF
Reduce reabsorption of H2O and NaCl in proximal tubule
Contra: CHF, renal failure, pulmonary edema
SE: pulmonary edema, hyponatremia (in impaired renal function), hypernaturemia, nausea, vomiting, headache
No PO, IV only
Urea
Osmotic diuretic
Tx or prevention of ARF
Reduce reabsorption of H2O and NaCl in proximal tubule
Contra: CHF, renal failure, pulmonary edema
SE: pulmonary edema, hyponatremia (in impaired renal function), hypernaturemia, nausea, vomiting, headache
No PO, IV only
Furosemide
Lasix
Loop diuretic
Acute pulmonary edema, HTN, CHF (in renal insufficiency), ARF, CRF, ascites, nephrotic syndrome
Inhibits Na/K/2Cl contransporter in TAL (reduces reabsorption of Na, K, Cl, Mg, Ca, and H2O), also renal vasodilation
SE: HYPOKALEMIA, hypomagnesemia, HYPONUTREMIA, HYPOVOLEMIA, hyperuricemia, metabolic alkalosis, OTOTOXICITY, diarrhea, INCREASED LDL/HDL
PO
Lots of drug interactions; AMINOGLYCOSIDES (ototoxicity), BB, digoxin, NSAIDs, quinidine, sulfas, steroids
Also used to treat hypercalcemia and hyperkalemia
Strong rebound aldosterone, increased Na reabsorption and thus K excretion downstreatm
Bumetanide
Loop diuretic
Acute pulmonary edema, HTN, CHF (in renal insufficiency), ARF, CRF, ascites, nephrotic syndrome
Inhibits Na/K/2Cl contransporter in TAL (reduces reabsorption of Na, K, Cl, Mg, Ca, and H20), also renal vasodilation
SE: Hypokalemia, hypomagnesemia, hyponutremia, HYPOVOLEMIA, hyperuricemia, metabolic alkalosis, OTOTOXICITY, diarrhea
PO
Lots of drug interactions; aminoglycosides, BB, digoxin, NSAIDs, quinidine, sulfas, steroids
40x more potent, shorter half life, 50% metabolized by liver
Torsemide
Loop diuretic
Acute pulmonary edema, HTN, CHF (in renal insufficiency), ARF, CRF, ascites, nephrotic syndrome
Inhibits Na/K/2Cl contransporter in TAL (reduces reabsorption of Na, K, Cl, Mg, Ca, and H20), also renal vasodilation
SE: Hypokalemia, hypomagnesemia, hyponutremia, HYPOVOLEMIA, hyperuricemia, metabolic alkalosis, OTOTOXICITY, diarrhea
PO
Lots of drug interactions; aminoglycosides, BB, digoxin, NSAIDs, quinidine, sulfas, steroids
Longer 1/2life than lasix, longer duration, better absorption, 80% metabolized by the liver
Ethacrynic acid
Loop diuretic
Acute pulmonary edema, HTN, CHF (in renal insufficiency), ARF, CRF, ascites, nephrotic syndrome
Inhibits Na/K/2Cl contransporter in TAL (reduces reabsorption of Na, K, Cl, Mg, Ca, and H20), also renal vasodilation
SE: WORSE SIDE EFFECTS, NEPHROTOXIC AND OTOTOXIC
PO
Lots of drug interactions; aminoglycosides, BB, digoxin, NSAIDs, quinidine, sulfas, steroids
Last resort, only used if sensitivity to others
Hydrochlorothiazide
Thiazide
HTN, edema dt CHF, hepatic cirrhosis, renal disease, kidney stones
Inhibits apical NaCl cotransport (into cell) in early DCT
SE: HYPOKALEMIA, hyponatremia, hypovolemia, hyperuricemia, hypercalcemia, METABOLIC ALKALOSIS, hypoerglycemia (insulin resistance), hyperlipidemia, hypersensitivity, interstitial nephritis
Drug interactions: anticoags, BB, carbamazepine/chloropropamide, digoxin, NSAIDs, quinidine, steroids
Also used to treat diabetes insipidus
Chlorothiazide
Thiazide
HTN, edema dt CHF, hepatic cirrhosis, renal disease, kidney stones
Inhibits apical NaCl cotransport (into cell) in early DCT
SE: HYPOKALEMIA, hyponatremia, hypovolemia, hyperuricemia, hypercalcemia, METABOLIC ALKALOSIS, hypoerglycemia (insulin resistance), hyperlipidemia, hypersensitivity, interstitial nephritis
Drug interactions: anticoags, BB, carbamazepine/chloropropamide, digoxin, NSAIDs, quinidine, steroids
1/10 potency, half life of 1.5 hours
Metolazone
Thiazide
HTN, edema dt CHF, hepatic cirrhosis, renal disease, kidney stones
Inhibits apical NaCl cotransport (into cell) in early DCT
SE: HYPOKALEMIA, hyponatremia, hypovolemia, hyperuricemia, hypercalcemia, METABOLIC ALKALOSIS, hypoerglycemia (insulin resistance), hyperlipidemia, hypersensitivity, interstitial nephritis
Drug interactions: anticoags, BB, carbamazepine/chloropropamide, digoxin, NSAIDs, quinidine, steroids
10x more potent, longer half life, most efficacious in renal insufficiency
Indapamide
Thiazide
HTN, edema dt CHF, hepatic cirrhosis, renal disease, kidney stones
Inhibits apical NaCl cotransport (into cell) in early DCT
SE: HYPOKALEMIA, hyponatremia, hypovolemia, hyperuricemia, hypercalcemia, METABOLIC ALKALOSIS, hypoerglycemia (insulin resistance), hyperlipidemia, hypersensitivity, interstitial nephritis
Drug interactions: anticoags, BB, carbamazepine/chloropropamide, digoxin, NSAIDs, quinidine, steroids
20x more potent, 1/2 life of 10-22 hours, metabolized by the liver
Chlorthalidone
Thiazide
HTN, edema dt CHF, hepatic cirrhosis, renal disease, kidney stones
Inhibits apical NaCl cotransport (into cell) in early DCT
SE: HYPOKALEMIA, hyponatremia, hypovolemia, hyperuricemia, hypercalcemia, METABOLIC ALKALOSIS, HYPERGLYCEMIA (insulin resistance), INCREASED LDL/HDL, hypersensitivity, interstitial nephritis, impotence
Contra: HYPOKALEMIA, PREGGOS
Drug interactions: anticoags, BB, carbamazepine/chloropropamide, digoxin, NSAIDs (will decrease prostaglandin effect), quinidine, steroids
Same potency, 1/2life of 44 hours
Spironolactone
K sparing diuretic/ chronic CHF
Chronic liver disease (tx second to hyperaldosteronisms from cirrhosis), prevent hypokalemia from other drugs, chronic CHF/a.fib
ARB: Blocks aldosterone on collective tubules (dec. Na reabsorption, spares K and H)
SE: HYPERKALEMIA, gynecomastia, hirsutism, menstrual irregularties, testicular atrophy
Drug interaction: ACI (hyperK, cardiac arrhyth), NSAIDs (hyperK), RAS inhibitors
Also used to treat primary hyperaldosteronism
PREVENTS LV REMODELING AND FIBROSIS!
Eplerenone
K sparing diuretic/ chronic CHF
Chronic liver disease (tx second to hyperaldosteronisms from cirrhosis), prevent hypokalemia from other drugs, chronic CHF/a.fib
Blocks aldosterone on collective tubules (MR receptor)
SE: HYPERKALEMIA
Drug interaction: ACI (hyperK, cardiac arrhyth), NSAIDs (hyperK), RAS inhibitors
NO ANTIANDROGENIC SE
PREVENTS LV REMODELING AND FIBROSIS!
Amiloride
K sparing diuretic
Prevent hypoK effects of other drugs
ENaC inhibitor: Reduce Na entry across luminal membrane of principal cells of DCT (decreases driving force for K efflux)
SE: HYPERKALEMIA, glucose intolerance in diabetics
Drug interaction: ACEI (hyperK, cardiac arrhyth), NSAIDs (hyperK), RAS inhibitors
Triamterene
K sparing diuretic
Prevent hypoK effects of other drugs
ENaC inhibitor: Reduce Na entry across luminal membrane of principal cells of DCT (decreases driving force for K efflux)
SE: HYPERKALEMIA, megaloblastic anemia in pts with liver cirrhosis
Drug interaction: ACEI (hyperK, cardiac arrhyth), NSAIDs (hyperK), RAS inhibitors
Liver metabolizes drug, ORGANIC BASE TRANSPORTER
Doxycycline
Diuretic ADH Antagonist SIADH, hyponutremia Prevent ADH-induced water reabsorption in principal cells of collecting tubule SE: Nephrotoxic Also used in CHF
Lithium
Diuretic ADH Antagonist SIADH, hyponutremia Prevent ADH-induced water reabsorption in principal cells of collecting tubule SE: Nephrotoxic Also used in CHF
Tolvaptan
Diuretic
ADH Antagonist
SIADH, hyponutremia
Prevent ADH-induced water reabsorption in principal cells of collecting tubule
SE: Hypernatremia, thirst, dry mouth, hypotension, dizziness
Also used in CHF
Conivaptan
Diuretic
ADH Antagonist
SIADH, hyponutremia
Prevent ADH-induced water reabsorption in principal cells of collecting tubule
SE: Hypernatremia, thirst, dry mouth, hypotension, dizziness
Also used in CHF, IV available for tx of euvolemic hyponatremia
Mozavaptan
Diuretic
ADH Antagonist
SIADH, hyponutremia
Prevent ADH-induced water reabsorption in principal cells of collecting tubule
SE: Hypernatremia, thirst, dry mouth, hypotension, dizziness
Also used in CHF
Procainamide
Anti-arrhythmic
Class IA (intermediate kinetics, prolonged AP)
A and V arrhyth, v.arryth post MI
Blocks Na and K channels, slows upstroke of AP, prolongs QRS, depresses SA/AV
SE: Torsades, hypotension, anticholinergic effects, lupus
PO, IV, IM
t1/2 3-4 hours, renally eliminated, NAPA metabolite
Quinidine
Anti-arrhythmic
Class IA (intermediate kinetics, prolonged AP)
A and V arrhyth, v.arryth post MI
Blocks Na and K channels, slows upstroke of AP, prolongs QRS, depresses SA/AV
SE: stronger antichol effects, cinchonism (headache, dizziness, tinnitus)
Rarely used b/c severe cardiac effects
Disopyramide
Anti-arrhythmic
Class IA (intermediate kinetics, prolonged AP)
V arrhyth only
SE: Greatest antichol effects (increases sinus rate and AV conduction), negative inotropic, atropine-like actions
Requires co-admin of drugs that slow conduction
Lidocaine
Anti-arrhythmic
Class IB (fast kinetics, reduction of AP duration)
V.arrhyth after MI, DRUG OF CHOICE for vtach and v fib after cardioversion
Na channel blockade, dec. AP duration, depression of conduction in depolarized (ischemic) cells
SE: least cardiotoxic class I, neurologic SE dt local anestheic properties
IV only
Extensive first pass liver metabolization, t1/2 is 1-2 hours
Prophy tx not recommended (can increase mortality)
Mexiletine
Anti-arrhythmic
Class IB (fast kinetics, reduction of AP duration)
V.arrhyth after MI, DRUG OF CHOICE for vtach and v fib after cardioversion
Na channel blockade, dec. AP duration, depression of conduction in depolarized (ischemic) cells
SE: least cardiotoxic class I, neurologic SE dt local anestheic properties
PO
t1/2 is 8-10 hours
Off label use for chronic pain
Flecainamide
Antiarrhythmic
Class IC (slow kinetics, no effect on AP duration)
Supravent arryth in otherwise normal hearts
Na and K channel blockade, no anticholinergic effects
CONTRA: V.TACH, MI, VENTRICULAR ECTOPY
Well absorbed, t1/2 is 20 hours, eliminated in liver and kidney
Propafenone
Antiarrhythmic
Class IC (slow kinetics, no effect on AP duration)
Supravent arryth in otherwise normal hearts
Na and K channel blockade, similar to propranolol but with weak BB
SE: arrhythmogenic, sinus bradycardia, bronchospasm (from BB), metallic taste, constipation
Propranolol
Antiarrhythmic
Class 2
Nonselective BB
Prevents recurrent infarction after MI, a.fib, a.flutter, AV nodal reentry
Inhibits sympathetics, reduce HR and pacemaker current, reduce conduction, decrease catecholamine DAD and EADs
SE: bradycardia, reduced exercise capacity, heart failure, hypotension, AV block, bronchospasm
Contra: sinus brady, partial AV block, asthma, COPD, diabetics
Can mask tachy symptoms of hypoglycemia
Esmolol
Antiarrhythmic Class 2 Cardioselective BB (B1) Acute supravent tachycardia IV only Short half-life
Amiodarone
Antiarrhythmic
Class 3 (prolongation of AP duration)
PO: recurrent v.tach/v.fib, a.fib
IV: out-of-hospital cardiac arrest, v.tach, v.fib
Blocks K, Na, Ca, B-receptors, prolongs AP refractoriness, slows conduction, suppresses abnormal automaticity, prolongs QT and QRS
SE: bradycardia, heart block, pulmonary FIBROSIS, hepatic toxicity, photodermatiis, blocks T4 to T3 (hypo/hyperthyroidisms)
PO, IV
30-0% bioavailable, lipohilic, accumulates in heart/lung/liver/cornea
Dronedarone
Antiarrhythmic
Class 3 (prolongation of AP duration)
A.fib, a.flutter
Blocks K, Na, Ca, B-receptors, prolongs AP refractoriness, slows conduction, suppresses abnormal automaticity, prolongs QT and QRS
SE: similar to amiodarone, without thyroid effects
Contra: severe heart failure
t1/2 is 24 hours
Structural analogue of amiodarone, designed to eliminate effects on thyroxine
Sotalol
Antiarrhythmic Class 3 (prolongation of AP duration) V and supraV arrhyth, maintenance of sinus rhythm in a.fib Nonselective BB, inhibits delayed rectifier and other K currents
Verapamil
Antiarrhythmic
Class 4 (Ca channel blockers)
Non-dihydropyridine
1stline HTN, Supravent arrhyth, reentry AV, slows ventricular rate in a.flutter/fib, exertional angina, variant angina
Blocks L-type Ca channels in heart, major effects in slow response tissues (SA/AV node), slows conduction, increases AV node refract, lowers HR, increases PR, vasodilation in periphery
SE: vasodilation, BRADYCARDIA, hypotension, fibrillation, LV dysfunction, CONSTIPATION, lassitude, nervousness, vasodilation, peripheral edema
Contra: Liver dysfunction, CONDUCTION DISTURBANCES, BB (use with caution)
PO
Metabolized in liver
Diltiazem
Antiarrythmic Class 4 (Ca channel blockers) Non-dihydropyridine 1stlineHTN and angina pectoris Blocks Ca channels in heart and periphery (vasodilation) SE: dizziness, headache, edema, BRADYCARDIA Contra: conduction disturbances Lower cardioselectivity than verapamil
Adenosine
Antiarrythmic
Class 4 (Ca channel blockers)
Conversion of paroxysmal supraven tachy to sinus rhyhtm
Increases K conductance, inhibits Ca currents, slows AV node, produces transient cardiac arrest
SE: Flushing and SOB
Contra: theophylline/caffeine (reduces effectiveness), potentiated by dipyridamole
Rapid IV bolus
t1/2 is seconds
Magnesium
Antiarrythmic Class 4 (Ca channel blockers) Digitalis induced arrhythmias with hypomg Unknown MoA IV
Potassium
Antiarrythmic
Class 4 (Ca channel blockers)
Maintain normal plasma K
Hyperkalemia: depolarizes resting membrane/slows conduction potential
Hypokalemia: decreases K permeability/enhances ectopic automaticity/lengthens AP duration (can lead to EADs)
IV, PO
Digitalis
Antiarrythmic
Class 4 (Ca channel blockers)
Cardiac glycoside
A.arrhyth, a.flutter, a.fib, acute CHF
Inhibits Na/K-ATPase, increases intracell Ca, causes (+) inotropy, increased AV refract, slows AV conduction
SE: DADs, yellow-green visual disturbances, anorexia, blurred vision, drowsiness, depression
Conta: aminodarone, verapamil, flecainide, hypokalemia/magnesemia
Long t1/2 (40 hours), eliminated by kidney, narrow therapeutic window
Nifedipine
Dihydropyridine
Ca channel antagonist, blocks L-type Ca channels in VSMC causes vasodilation/decreased contractility
1st line drug for uncomplicated HTN, used in diabetes and hyperlipidemia, anti-anginal
SE: ACUTE TACHY (reflex), headache, PERIPHERAL EDEMA, flushing, bradycardia, heart block, CHF, hypotension
Clonidine
Antihypertensive
Second line for HTN
a2 agonist (decreases sympathetic outflow from CNS)
SE: SEDATION, DRY MOUTH, bradycardia, DERMATITIS
Drug interactions: CNS depressants
Withdraw slowly to prevent REBOUND HTN
Guanfacine
Antihypertensive
Second line for HTN
a2 agonist (decreases sympathetic outflow from CNS)
SE: SEDATION, DRY MOUTH, bradycardia, DERMATITIS
Drug interactions: CNS depressants
Longer 1/2life, less chance of rebound HTN
Methyldopa
Antihypertensive
HTN in PREGGOS
a2-agonist, competes with L-DOPA for DOPA decarboxylase
SE: SEDATION, nightmares, movement disorders, hyperprolactinemia, anemia
Contra: Liver dx
Drug interactions: Levodopa
USED IN PREGGOS!
Reserpine
Antihypertensive
Resistant HTN
Depletes monoamine from storage vesciles
SE: sedation, diarrhea, DEPRESSION, bradycardia, NASAL CONGESTION
Drug interactions: CNS depressants, MAOIs
Phenoxybenzamine
Antihypertensive Rx for pheo before surg a-blocker SE: tachycardia Non-selective
Prazosin
Antihypertensive 2ndline for chronic HTN a-blocker SE: HYPOTENSION (first dose), dizziness, headaches, weakness Deacreases LDL/HDL
Terazosin
Antihypertensive
2ndline for chronic HTN
a1-blocker
Longer half life
Doxazosin
Antihypertensive
2ndline for chronic HTN
a1-blocker
Longer half life
Propranolol
Antihypertensive/Anti-anginal
HTN with angina, MI, or arrhythmia, post MI prophy
Nonselective B-blocker
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPAIRED EXERCISE TOLERANCE, INCREASED AIRWAY RESISTANCE, INSOMNIA, nightmares, CHRONIC FATIGUE, depression
CONTRA: CARDIOGENIC SHOCK, SINUS BRADY, ASTHMA, SEVERE HF, COPD
Drug interactions: CCB (reduced contractility and conduction)
Lipophilic
Nadolol
Antihypertensive/Anti-anginal
Long-term angina, post MI prophy
Nonselective B-blocker
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPAIRED EXERCISE TOLERANCE, INCREASED AIRWAY RESISTANCE
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug interactions: CCB (reduced contractility and conduction)
Longer half life than propranolol, hydrophilic
Pindolol
Antihypertensive
Long-term angina
Nonselective B-blocker
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPAIRED EXERCISE TOLERANCE, INCREASED AIRWAY RESISTANCE, INSOMNIA, nightmares, CHRONIC FATIGUE, depression
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug interactions: CCB (reduced contractility and conduction)
Les bradycardia than other BBs
Lipophilic
Metoprolol
Antihypertensive/Anti-anginal
HTHN, long term angina, post MI prophy, chronic CHF
B1-blocker
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPARIED EXERCISE TOLERANCE, INSOMNIA, nightmares, CHRONIC FATIGUE, depression
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug interactions: CCB (reduced contractility and conduction)
SOMEWHAT LIPOPHILIC
PREVENTS LV REMODELING
Atenolol
Antihypertensive/anti-anginal
Chronic HTN, angina, MI, arrhythmia, HF, post MI prophy
B1-blocker
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPARIED EXERCISE TOLERANCE
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug interactions: CCB (reduced contractility and conduction)
Hydrophilic
Excreted by kidney
Labetolol
Antihypertensive
Chronic HTN, pheo
Mixed a/B receptor blocker
SE: orthostatic HT, sexual dysfunction, BRADYCARDIA, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPAIRED EXERCISE TOLERANCE, INSOMNIA, nigtmares, CHRONIC FATIGUE, depression
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug indications: CCB (reduced contractility and conduction)
Lipophilic
Carvedilol
Antihypertensive
Chronic HTN, CHF, angina, post MI prophy
Mixed a/B blocker and NO generator
SE: BRADYCARDIA, impotence, INCREASED TG, DECREASED HDLS, HYPERGLYCEMIA, IMPAIRED EXERCISE TOLERANCE, INSOMNIA, nightmares, CHRONIC FATIGUE, depression
CONTRA: CARDIOGENIC SHOCK, SINUS BRADYCARDIA, ASTHMA, SEVERE HEART FAILURE
Drug interactions: CCB (reduced contractility and conduction)
Vasodilator
Lipophilic
PREVENTS LV REMODELING
Minoxidil
Antihypertensive
Resistant HTN
Vasodilator (similar to hydralazine)
SE: TACHYCARDIA, angina aggravation, fluid retention, nausea, vomiting, sweating, flushing, lupus, hypertrichosis
Nitroprusside
Antihypertensive Acute Hypertensive Crisis (BP >200) Vasodilator SE: Nausea, vomiting, muscle twitch, CYANIDE poisoning (from metabolites in long term use) Immediate onset, brief duration
Lisinopril
Antihypertensive/Diuretic
1stline drug used in chronic HTN, chronic CHF/a.fib
ACEI
SE: HYPERKALEMIA, rash, DRY COUGH, ANGIOEDEMA
Contra: PREGGOS, bilat renal stenosis
Drug interactions: exacerbates the hyperK effect of K sparing drugs
Water soluble, excreted unchanged by kidney, longer half life, allows 1x daily dosing
PREVENTS LV REMODELING
Isosorbide mononitrate
Anti-anginal
Exertional angina, variant angina, unstable angina
Reacts with vessel wall to increase [NO] in VSMC (causing venodilation)
SE: Orthostatic hypotension, reflex tachy, headache, nitrate tolerance
Contra: systemic hypotension
Isosorbide dinitrate
Anti-anginal
Exertional angina, variant angina, unstable angina
Reacts with vessel wall to increase [NO] in VSMC (causing venodilation)
SE: Orthostatic hypotension, reflex tachy, headache, nitrate tolerance
Contra: systemic hypotension
Nicardipine
Anti-anginal
Exertional angina, variant angina, unstable angina
CCB, blocks influx L-type Ca channels in VSMC, vasodilation and dec. contractility
SE: Bradycardia, heart block, CHF, hypotension, peripheral edema
Contra: advanced heart block, systemic hypotension, CHF
Prevents exercise-induced vasospastic angina
Amlodipine
Anti-anginal
Exertional angina, variant angina, unstable angina
CCB, blocks influx L-type Ca channels in VSMC, vasodilation and dec. contractility
SE: Bradycardia, heart block, CHF, hypotension, peripheral edema
Contra: advanced heart block, systemic hypotension, CHF
Prevents exercise-induced vasospastic angina
Ranolazine
Anti-anginal
Stable/exercise induce angina
pFOX inhibitor (inhibits FFA b-ox in cardiac myocytes, encourages glucose met pathway)
SE: Prolongs QT interval
Contra: Long QT syndrome
Drug Interactions: Drugs that prolong QT interval
Prevents exercise-induced myocardial ischemia, less lactic acid accumulation
Ivabradine
Anti-anginal
Chronic stable angina
If current inhibitor (in SA nodes, slows HR at rest and during exercise)
SE: Bradycardia, heart block, luminous phenomenon
Contra: Sick sinus syndrome
Drug interactions; CCB, verapamil, diltiazem
Prevents exercise-induced myocardial ischemia
Niseritide
ADCCHF in hospitalized patients
Activates VSM and renal BNP receptors, raises cGMP levels in VSMC and renal epithelial cells
Vasodilation to increase GFR, induces natriuresis (decreases Na reabsorption in distal tubule)
SE: hypotension, ventricular arrhythmias
Contra: Reduced LV filling pressure, systemic hypotension
Isoproterenol
CHF
B-Adrenergic
Low CO dt acute CHF, cardiogenic shock
Stimulates B receptor to increase myocardial cAMP
SE: arrhythmias, increased O2 consumption, angina
Contra: v. arrhyth, severe PVD
Dopamine
CHF
B-Adrenergic
Low CO dt acute CHF, cardiogenic shock
Stimulates B receptor to increase myocardial cAMP
SE: arrhythmias, increased O2 consumption, angina
Contra: v. arrhyth, severe PVD
Dobutamine
CHF
B-Adrenergic
Low CO dt acute CHF, cardiogenic shock
Stimulates B receptor to increase myocardial cAMP
SE: arrhythmias, increased O2 consumption, angina
Contra: v. arrhyth, severe PVD
Norepinephrine
CHF
B-Adrenergic
Low CO dt acute CHF, cardiogenic shock
Stimulates B receptor to increase myocardial cAMP
SE: arrhythmias, increased O2 consumption, angina, VASOCONSTRICTION
Contra: v. arrhyth, severe PVD
Inamrinone
CHF
ADCCHF in hospitalized patients (esp on BB)
Inhib. degredation of cAMP, inc. cAMP in cardiac muscle, inhib. degredation of cGMP in VSM, induce vasodilation
SE: arrhythmias, hypotension
Milrinone
CHF
ADCCHF in hospitalized patients (esp on BB)
Inhib. degredation of cAMP, inc. cAMP in cardiac muscle, inhib. degredation of cGMP in VSM, induce vasodilation
SE: arrhythmias, hypotension
LCZ696
ARB Chronic CHF, esp intolerant to ACEI Valsartan/sacubitril combo. Blocks AT receptor on VSM, prevents degredation of natriuretic peptides/bradykinin/adrenomedullin (causing vasodilation and reduction of ECF volume via NA excretion) SE: Hypotension, cough Contra: systemic hypotension
Bucindolol
BB
Chronic CHF
Nonselective and a1 blocker
SE: worsening CHF, bradycardia, heart block, depression, bronchospasm, peripheral vasospasm
Contra: acute exacerbation of chronic CHF, asthma, COPD, insulin-dependent diabetes mellitus
PREVENTS LV REMODELING
