Block 2 drugs Flashcards

Question

Ticagrelor (Brilinta)

Answer 1

Reversible P2Y12 blocker Metabolized by CYP3A4 Reduce risk of stroke, heart attack and death in patients with previous MI or angina Adverse: hemorrhage

Answer 2

GP IIb/IIIa receptor inhibitor Fab fragment of antibody targeting the GPIIb/IIIa Used with ASA and heparin to treat acute coronary thrombosis or during coronary angioplasty, reduces restenosis, recurrent MI Continuous infusion used in the perioperative setting Adverse: Major hemorrhagic event 10% of patients

Answer 3

Peptide inhibitor of fibrinogen binding site of GPIIb/IIIa receptor Used with ASA and heparin to treat acute coronary thrombosis or during coronary angioplasty, reduces restenosis, recurrent MI Continuous infusion used in the perioperative setting Adverse: Major hemorrhagic event 10% of patients

Answer 4

Inhibits thrombus formation due to inhibition of PDE (phosphodiesterase) Inhibits adenosine uptake Short duration of action, and is also a vasodilator Primary therapeutic use in combinatino with aspirin to prevent stroke: cerebrovascular ischemia Adverse: Not indicated for coronary disease due to "coronary steal": vasodilation redueces blood circulation to the heart Hypotension Increased bleeding risk

Answer 5

Act on clotting cascade to either inhibit pro-clotting factors or activate anti-clotting factors: -Direct thrombin inhibitors -HMW-Heparin -LMW-Heparin Prevent synthhesis of coagulation factors via vitamin K-Warfarin Rivaroxaban (Xarelto): factor Xa inhibitor Anticoagulant drugs typically reduce global clotting factor activity by 30-50% at therapeutic doses Cannot dissolve a thrombus that has already formed

Answer 6

Direct thrombin inhibitor standard oral twice daily Low molecular weight pro-drug, rapidly (approx 1 hr) converted to active form Dabigatran: competative inhibitor-binds to exosite 1 on thrombin preventing fibrinogen cleavage to mature fibrin Use: stroke prevention in patients with atrial fibrillation, equal efficacy to warfarin, less patient monitoring and adverse effects. Also for DVT and pulmonary embolism. Benefits: no patient monitoring/titration as with warfarin, rapid onset of action, less adverse drug reactions. Adeverse: Hemorrhage, heartburn, stomach upset, increase in risk of MI

Answer 7

Used in patients with thrombosis related to heparin-induced thrombocytopenia Derivatives: Lepirudin (Refludan): Single amino acid change

Answer 8

Reversible thrombin inhibitor | Used in patients with or at risk of heparin-induced thrombocytopenia

Answer 9

Reversible thrombin inhibitor Used in coronary angioplasty Adverse: increased bleeding risk

Answer 10

Inhibits clotting factors IXa, Xa, and thrombin bby greatly enhancing Antithrombin III activity (1000 fold) Not absorbed by GI tract due to large molecular weight therefore use IV and SC injection, im injection can cause hematomas Short half-life (approx 1 hr) means frequent injections or continuous infusion: not suitable in outpatient setting Adverse: heparin induced thrombocytopenia testing required to determine dose effect on coagulation overdose can be countered with protamin sulfate

Answer 11

Counteracts a HMW heparin overdose

Answer 12

Fractioned forms of HMW heparin: Dalteparin Inhibit Factor Xa by antithrombin, but not thrombin Use: Treat venous thromboembolism, thrombosis, pulmonary embolism, and unstable angina Neutralization of LMW heparin by protamine is incomplete Advantages over unfractionated heparin: Longer halflife (4 hrs) and faster absortion time Once daily SC injections administered in outpatient setting Lower risk of thrombocytopenia and osteoporosis less frequent monitoring required due to more predictable pharmacokinetic response

Answer 13

Penta-saccharide region of heparin Inhibit Factor Xa by antithrombin, but not thrombin Use: Treat venous thromboembolism, thrombosis, pulmonary embolism. Renal excretion, so not used accompanying renal disease Neutralizationof LMW heparin by protamine is incomplete Advantages over HMW and LMW heparin: Longer half life (20 hrs) and afster absortion time Once daily SC injections administered in outpatient setting Lower risk for thrombocytopenia

Answer 14

Blocks factor Xa Factor Xa is a component of the coagulation cascade, where the intrinsic and extrinsic pathways meet Indirectly, prevents the maturation of Thrombin Advantage over Warfarin: no titration prior to dosing Use:Preventing venous thromboembolism in patients following knee or hip replacement, and DVT Adverse:Increased bleeding risk

Answer 15

Most widely used oral antcoagulant with predictable pharmacokinetics, bioavailability and anticoagulant response: 1st used as rat poison from 1948. Indirect inhibition of clotting cascade: Blocks vitamin K epoxide reductase, lowering Vitamin K recycling and slowing maturation of prothrombin and clotting factors VII, IX, and X. Slow onset of action (8-12 hrs): existing mature clotting factors must be depleted; maximal effect 3-5 days after administration Use: Acute DVT, pulmonary embolism, venous thromboembolism, following acute MI, prothetic heart valve placement. Adverse: hemorrhage risk increases with intensity and duration of therapy Warfarin readily crosses the placenta, can cause hemorrhage at any time and developmental defects during 1st trimester Phytonadione (Vitamin K1) used to reverse warfarin associated bleeding ' Drug interactions: Patient history is crucial Increased potency: aspirin, Vitamin K deficiency, anabolic steroids, antibiotics, tamoxifen, oral hypoglycemics. Decreased potency: chronic alcohol abuse, oral contraceptives, corticosteroids, barbituates, increased hepatic synthesis of clotting factors, increased vitamin K intake, Cholestyramine metabolized by CYP2C9 induction eg barbituate, rifampicin inhibition-cimetidine

Answer 16

Effective only if used rapidly after onset of thrombosis Therapeutic uses in hospital: Acute ischemic stroke, MI, pulmonary embolism, severe deep venous thrombosis, ascending thrombophlebitis Inhibitors: aminocaproic acid: inhibits the conversion of plasminogen to plasmin (to treat thrombolytic overdose) Side effects: Hemorrhage, especially intracranial hemorrhage is the most serious Contraindications: Brain tumor or aneurysm, hemmorrhagic stroke, recent major surgery, active bleeding in GI or urinary tract, severe platelet shortage or coagulation disorder, severe uncontrolled hypertension

Answer 17

Catalyzes the conversion of inactive plasminogen to active plasmin for fibrin breakdown Acts throughout the circulation, not just at the clot Given iv asap after a heart attack to dissolve clots in the ateries of the heart wall Can cause allergic reaction or develop tolerance: typically only used for patients 1st heart attack, later heart attacks use tPA treament Associated with increased bleeding risk in acute ischemic stroke therefore not used in this setting

Answer 18

Endogenous thrombolytic: human gene cloned, expresses and purified using bacteria Preferentially activates plasminogen bound to fibrin, to target finbrinolysis to the formed thrombus and spare systemic activation tPA is effective in lysing thrombi during treatment of acute myocardial infarction. also for acute stroke accompanying low bleeding risk Derivatives: Reteplase (Retavase), Tenecteplase (TNKase)

Answer 19

Fragment of human tPA gene cloned and expressed in bacteria Increased plasma half-life allows convenient bolus dosing Acts on plasminogen only at the site of the clot (like tPA) Retepase lacks the major fibrin-binding domain, and less fibrin-specific than tPA

Answer 20

Second-generation thrombolytic; fragment of human tPA gene cloned, genetically expressed More clot-specific than tPA and has some resistance to plasminogen inhibitors

Answer 21

Sleep apnea, drug induced, chronic kidney disease, primary aldosteronism, renovascular disease, renovascular disease, chronic steroid therapy, Cushing's syndrome, pheochromocytoma, coarctation of the aorta, thyroid and parathyroid disease

Answer 22

Risk doubles with each 20 of SBP or 10 DBP

Answer 23

In office-Two readings, 5 minutes apart, sitting in chair, confirm elevated reading in contralateral arm Ambuatory BP monitoring- Indicated for elevation of "white-coat" HTN. Absence of 10-20% BP decrease during sleep may indicate increased CVD risk Self-measurement- Provides information on response to therapy. May help improve adherence to therapy and evaluate "white-coat" HTN

Answer 24

Obesity, Diet, Stress, lack of exercise, alcohol intake, cigarette smoking

Answer 25

normal BMI

Answer 26

Emphasizes: Fruits, vegetables, low fat dairy foods, and reduced sodium intake Includes whole grains, poultry, fish, nuts Reduced amounts of red meat, sugar, total and saturated fat, and cholesterol

Answer 27

CARDIAC OUTPUT-Stroke volume and heart rate | TOTAL PERIPHERAL RESISTANCE- vascular structure, vascular tone, blood volume

Answer 28

diuretics, agents affecting adrenergic function (sympatholytics), vasodilators, agents affecting the Renin Angiotensis Aldosterone System (RAAS)

Answer 29

THIAZIDES-Chlorothiazide, Hydrochlorothiazide LOOP DIURETICS-Furosemide, Bumetanide, Ethacrynic acid, Torsemide K+SPARING-Spironolactone, Triamterene, Amiloride

Answer 30

FIrst line treatment for uncomplicated hypertension Diuretics have been virtually unsurpassed in preventing the cardiovascular complications of hypertension Diuretics enhance the antihypertensive efficacy of multidrug regimens, can be useful in achieving BP control, and are more affordable than other anti-hypertensive agents

Answer 31

Initial therapy for isolated systolic hypertension

Answer 32

Elevation of plasma renin, angiotensin II, and aldosterone levels due to volume and sodium depletion

Answer 33

Potential drug interactions with thiazide and loop diuretics: Cardiac glycosides (ie, cardiotoxicity enhanced by hypokalemia) Acid drugs that compete for renal tubular secretion (penicilin) Loop diuretics-use for removal of edema (pulmonary edema) K+ sparing-often combined with K+wasting diuretics

Answer 34

Non-selective B1/2 antagonist (Propanolol) Selective B1 antagonist (Atenolol, Metoprolol) Neuronal Blockers (Reserpine, Guanethedine) CNS Alpha 2 agonist-(Clonidine) Slective alpha 1 andrenoceptor antagonists (Prazosin, Terazosin)

Answer 35

Block cardiac Beta 1 receptors==>decreases HR, CF and cardiac output Block renal Beta 1 receptors==>decreases plasma renin, ANG II and TPR (afterload) Use Beta blockers if MI; Benefits: Antiarrythmic, Anti-ischemic, Antiatherogenic, reverses cardiac remodeling

Answer 36

Decrease in sympathetic outflow==>decreases HR, TPR and MAP while producing diuresis and natriuresis Not routinely used for treatment of hypertension in elderly dude to marked CNS effects (sedation, confusion) and orthostatic hypertension

Answer 37

Block vascular Alpha 1 receptors==> vasodilation, decreased TPR and MAP Adeverse: Reflex tachycardia, orthostatic hypotension

Answer 38

Block neural synthesis/release of NE from sympathetic nerve terminals=> vasodilation, decreased TPR and MAP

Answer 39

Calcium channel blockers (CCBs) Nifedipine (Procardia; a dihydropyridine) Diltiazem Verapamil

Answer 40

Arterial smooth muscle-CCBs block L-type voltage gated calcium channels and therefore prevent calcium entry into arterial VSM==> vasodilation, decrease in TPR (afterload) and MAP Adverse: reflex tachycardia; ankle edema due to selective aterial vasodilation Cardiac tissue: "non-dihydropyridine" CCBs block calcium entry into monocytes ==>decrease in HR, CF and cardiac output Drug interaction: may precipitate AV block with other drugs that decrease AV node conduction (eg Beta blockers) Adverse:ankle edema CCBs do not affect plasma renin activity, GFR, salt and water excretion or body fluid composition

Answer 41

Direct acting vasodilator agents Hydralazine Minoxidil Sodium Nitroprusside (iv formulation only)

Answer 42

Arterial smooth muscle: Hydralazine and Minoidil have a direct, but unknown mechanism (potentially opeing ATP-sensive potassium channels in VSM cells) to cause selective relaxation of arterial smooth muscle==> therefore causing vasodilation, decrease in TPR (afterload) and MAP Sodium Nitroprusside is a nitrovasodilator. Metabolism of nitroprusside to nitric oxide leads to formation of cGMP and vasodilation. Uses: Hypertension, CHF Adverse: Reflex tachycardia Monoxidil-hirsutism (hair growth), ankle edema Sodium Nitroprusside-cyanide toxicity with increased dose/duration of use

Answer 43

``` Angiotensin Converting Enzyme inhibitors (ACEIs) captopril enalapril lisinopril ramipril Angiotensin AT1 Receptor Blockers (ARBs) Iosartan valsartan irbesartan candesartan azilsartan ```

Answer 44

ACEI and ARBS prevent formation of angiotensin II and activation of angiotensin AT1 receptors, respectively, thereby producing beneficial cardiorenal effects that include: Vasodilation (arterial and venous) Reduction in ventricular afterload and preload Natriuretic and diuretic efects Decrease in sympathetic activity Inhibition of cardiac and vascular hypertrophy Adverse: concurrent use of two of the following drugs together may result in hyperkalemia: ACEI, ARB, renin inhibitor, K+sparing diuretic Contraindicated in pregnant women: Use of ACEI and ARBS during the 2nd or 3rd trimester can cause injury and even death in the developing fetus. Adverse effects: ACE inhibitor-induced coughing and angioedema due to elevated plasma bradykinin levels

Answer 45

Adverse: Concurrent use of two of the following drugs together may result in hyperkalemia: ACEI, ARB, renin inhibitor, K+sparing diuretic

Block 2 drugs Flashcards

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