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Cardio Drugs 1

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futuremdmba's version from 2017-11-04 13:20

Ischemia Drugs

Goals include:
Decrease O2 requirement (decrease HR, BP and contractility, preload and afterload)
Increase O2 delivery (decrease vasospasm)

Nitrates and Nitrites

Question Answer
MOA1. NO release into smooth muscle
2. guanylyl cyclase and cGMP increase
3. dephosphorylation of MLCK and cytosolic Ca2+ decrease
4. relaxation
Amyl NitriteObsolete; Ultra-short acting; Inhalation
Tx of cyanide poisoning (household fires)
Side effects: methemoglobinemia, reflex tachy, orthostatic hypertension, CNS effects, lethal synergism with Viagra
NitroglycerinShort-acting (not for maintenance); Onset 1-3mins, Duration 20-30mins
Tx: Stable and vasospastic angina, unstable angina
Side effects: Reflex tachy, throbbing headache, cutaneous flushing, OH, tolerance
Contra: Slidenafil (Viagra) due to excessive hypotension
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Calcium Channel Blockers

Question Answer
PharmacokineticsHigh first pass, high plasma protein binding, onset 30-60mins
PharmacodynamicsBlocks L-type voltage-gated Ca2+ channels and contraction
Negative inotropic and chronotropic effect (reduces current and delays recovery of current)
Dihydropyridine typesVascular selectivity; Positive effect on AV and SA nodes
Non-dihydropyridine typesCardiac selectivity; Negative effect on AV and SA nodes
Nifedipine (-dipines)Dihydropyridine type
Tx: Classic and Vasospastic angina, hypertensions
Side effects: Gingival hyperplasia, constipation, pretibial edema, nausea, flushing, dizziness
VerapamilNon-dihydropyridine type
Tx: Vasospastic angina, hypertension, supraventricular tachy, atrial fib, migraine
Side effects: Same as -dipines, gingival hyperplasia, heart failure, AV block, sinus node depression
Contra: Congestive heart failure due to negative inotropic effect
DiltiazemNon-dihydropyridine type
Tx: Same as verapamil
Side effects: Similar, but no gingival hyperplasia
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Beta Blockers

Question Answer
MOAdecreases HR and myocardial contractility, does not cause vasodilation
PharmacokineticsElimination 1/2 life = 5-30 mins
Liver excretion = lipophilic BBs
Renal excretion = low-lipophilic BBs
Propanolol (-olols)Blocks sympathetic effects, reduces renin release, titrated to achieve 55-60 bpm
Tx: Effort angina, hypertensions, arrhythmia, migraine, performance anxiety
Side effects: Beta-blockade, masks hypoglycemia, erectile dysfunction
Contra: Bronchospasm, Raynaud's, Prinzmetal angina (use CCB)
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Drug Combinations

Nitrates + BB = prevention of reflex tachy caused by nitrates alone
Nitrates + DHP CCB = decreased preload, decreased afterload (respectively); can lead to excessive hypotension and reflex tachy
NDHP CCB + BB = Not recommended
EffectNitrates AloneBB or CCB AloneNitrate + BB/CCB
HRReflex updowndown
Arterial pressuredowndowndown
EDVdownupno effect or down
ContractilityReflex updownno effect
Ejection timeReflex downnoneno effect
Net Myocardial O2 requireddowndowndown
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Other Ischemia Drugs

Question Answer
RanolazineBlocks inward Na current, decreases Ca influx, increases EDV
Tx: Stable angina
Side effects: Prolonged QT, shortened QT in long QT syndrome, nausea, constipation, dizziness
TrimetazidinepFOX inhibitor; causes metabolic shift to fatty acid oxid. which requires more O2 to produce ATP
Tx: stable angina
Side effects: Prolonged QT, torsades de points
IvabradineHyperpolarization-activatedcyclicnucleotide-gated(HCN) blocker (HCN)
FasudilRho kinase (ROCK) inhibitor; decreases coronary vasopasm for use in CAD (still in clinical trials)
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Anti-Coagulants

Types:
indirect thrombin inhibitors (via antithrombin) e.g. heparin and LMWH = parenteral
direct thrombin and factor X inhibitors
warfarin
Question Answer
Heparin (indirect)
- Large polysaccharide
- Water-soluble
parenteral, activates ATIII (inactivates thrombin, IIa, IXa, Xa)
Tx: Rapid DVT, pulmonary embolism, DOC anticoagulant in pregnancy, DIC, unstable angina, open-heart surgery
Side effects: Heparin-induced thrombocytopenia, bleeding, osteoporosis with chronic use
Monitor: aPTT; antidote is protamine sulfate
Enoxaparin (indirect)also tinzaparin, fondaparinux; binds ATIII and Xa (less thrombin effect)
Tx: DVT, PE, MI, unstable angina, AF
Side effects: Less HIT risk, bleeding
Monitor: none
Rivaroxaban (direct Xa)-xabans, oral, rapid onset, short 1/2 life
Tx: DVT, PE, prophylaxis for stroke in AF
Side effects: bleeding
Monitor: none
Lepirudin (direct thrombin)-rudins, argatroban
Tx: HIT, percutaneous coronary angioplasty (w/ aspirin)
Side effects: Bleeding, prolonging antibodies, anaphylactic reactions
Monitor: aPTT, renal insufficiency pt
Warfarin/Coumadinalso dicumarol, inhibits Vit.K epoxide reductase, narrow therapeutic window, rat poison
Tx: Long term DVT, post-MI, heart valve damage
Side effects: Bleeding, Skin necrosis (Protein C and S def.), Fetal warfarin syndrome (teratogen)
Contra: Pregnancy, antidote is Vit. K (slow) or FFP (fast)
Monitor: PT, INR
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Warfarin with CYP450 Drugs

FactorCYP450 InducerCYP450 Inhibitor
ClearanceIncreaseDecrease
Anticoagulant effectDecreaseIncrease
Prothrombin timeDecreaseIncrease
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Hepatic CYP450 Drugs

Question Answer
InducersEthanol, barbiturates, phenytoin, rifampicin, griseofulvin, carbamazepine, St. John's Wort/Smoking
InhibitorsIsoniazid, Sulfonamides, Cimetidine, Erythromycin, Grapefruit juice, Quinidine
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Thrombolytics

also called plasminogen activators or fibrinolytics
mainly used for MI, stroke, PE
contraindicated in bleeding
Question Answer
Alteplase
(-eplase's)
t-PA, converts plasminogen to plasmin, degrades fibrin
Tx: Acute MI, stroke (w/o bleed), PE
Side effects: Bleeding, cerebral hemorrhage, reperfusion arrhythmias
Antidote: aminocaproic acid
Increases PT and aPTT, no change platelet count, clot/fibrin selective
StreptokinaseFrom bacterial cultures, non-enzyme, complexes endogenous (non-fibrin bound) plasminogen
Side effects: Allergic reactions
Aminocaproic acidAntiplasin, also tranexamic acid, inhibits plasminogen activation
Tx: acute bleeding, hemophilia, intracranial aneurysms, menses, postoperative
Side effects: Thrombosis, hypotension, myopathy, diarrhea
Contra: DIC and genitourinary bleeding
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Anti-Platelets

Question Answer
AspirinCOX1/2 inhibitors, TXA2 reduction
Tx: MI, transient ischemia, cerebrovascular disease, inflammation
Side effects: GI toxicity, nephrotox, tinnitus, hypersensitivity (Samter's Triad = asthma, ASA sensitivity, nasal polyps), hyperventilation, aninon gap
Contra: D
Abciximab (GpIIb/IIIa)also tirofiban, eptifibatide
Tx: PCI, NSTEMI, unstable angina
Side effects: Bleeding, thrombocytopenia
Clodiprogel (ADP)also ticlodipine, prasugrel, ticagrelor
Tx: stroke, transient ischemia, unstable angina, PCI
Side effects: Leukocytopenia, neutropenia, bleeding, nausea, dyspepsia, TTP
Dipyridamole, CilostazolPDE III inhibitor, increases cAMP, decreases platelet aggregation, vasodilation
Tx: cardiac valve replacement, claudication
Side effects: headache, palpitations
Contra: heart failure
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Pro-Clotting

Question Answer
DesmopressinADH agonist
Tx: Hemophilia A, VWD
Side effects: Headache, nausea, flushing, hyponatremia, seizure
Recombinant Factor VIIaexternal coagulation factor activated
Tx: Hemophilia A and B, Factor VII def., Glanzmann's
Side effects: possible increase in thrombotic events
Vitamin KTx: Vit. K def., warfarin antidote, prevent hemorrhage in newborns
Side effects: Dyspnea, chest and back pain
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Anti-Hypertensives

Diuretics

ClassExamplesMOASide EffectsContraindication
Thiazide diureticsHydrochlorothiazideNa, K, H2O secretionHypoK/Na/Mg, HyperCa, metabolic acidosis, HyperUri/Lipid/GluGout
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Sympathoplegic Drugs

ClassExamplesMOASide EffectsContraindication
Beta blockers-olol
Non-selective = propanolol
Cardio-selective = Metoprolol, atenolol
Blocks beta receptors, decrease sympathetic effects on heartBradycardia, masks hypoglycemia, heart blocks, (impotence, rebound tachy and hypertension on withdrawal)Asthma/COPD (propanolol), heart blocks
a1 blockers-azosin
Prazosin, terazosin
Block a1 receptors causing vasodilationOrthostatic hypotension, palpitations, headache
Centrally-acting a2 agonistClonidine, methyldopaa-receptors in medulla, inhibits adrenergic outflow, decrease BPSedation, bradycardia (pt w/ SA node ab), dry mouth (clonidine), (rebound hypertension)
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Direct Vasodilators

ClassExamplesMOASide EffectsContraindication
DHP CCBAmlodipine, felodipineBlock Ca channels, arterial vasodilationVasodilation, headache, flushing, (orthostatic hypotension, peripheral edema, reflex tachy)Congestive heart failure
NDHP CCBDiltiazem, verapamilSame, slows AV nodal conduction (↓HR)Bradycardia, heart blocksDepressed LV function/heart failure, heart blocks
HydralazineFluid retention, lupus-like syndrome
MinoxidilFluid retention, hypertrichosis
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RAA Inhibitors

ClassExamplesMOASide EffectsContraindication
ACE Inhibitors-pril
Captopril, enalapril
Decrease ATII, arteriolar vasodilationDry cough, angioedema, hyperkalemia (rhinorrhea, proteinuria)Hyperkalemia, pregnancy, bilateral renal artery stenosis
ATII receptor blockersLosartanSame as prilsHyperkalemia, cough, angioedemaSame as prils
Direct renin inhibitorsAliskirenBlock renin binding, inhibit conversion ATogen to ATIHyperkalemia, Diarrhea, GERDSame as prils
Aldosterone receptor blockersSpirinolactoneNa and H2O excretion in collecting duct renal tubulesHyperkalemia, Gynecomastia, Impotence
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