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Pathophysiology, Pharmacology, and Therapeutics > Exam 2 Medications > Flashcards

Exam 2 Medications Flashcards

1
Q

Atorvastatin (Lipitor)

A

Drug Class: HMG-CoA-reductase inhibitor (statin)

MOA: HMG-CoA reductase inhibitor

Indication: hypercholesterolemia, primary CHD prevention in at-risk patients, hypertriglyceridemia in pts with hypercholesterolemia

Onset: days. Peak: 2 weeks.

Elimination: hepatic via CYP3A4, excreted in bile and urine

Adverse Effects: myalgias, rhabdomyolysis, hepatotoxicity

Interactions: fibrates, CYP3A4 inhibitors, grapefruit juice

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2
Q

Ezetimibe (Zetia)

A

Drug Class: dietary cholesterol blocker

MOA: dietary inhibition of cholesterol at small intestine brush border; prevention of reabsorption of cholesterol secreted in bile

Indication: hypercholesterolemia (monotherapy or with statins)

Elimination: converted extensively to ezetimibe glucuronide (active metabolite) in intestinal wall and liver - excreted in bile

Adverse Effects: myalgia, myopathy, rhabdomyolysis, gallstones, hepatitis, pancreatitis, thrombocytopenia. Usually well-tolerated

Interactions: slightly increased liver damage with statins. Gallstones and myopathy with fibrate. Elevated levels with cyclosporine (and vice versa). Avoid in patients with hepatic impairment.

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3
Q

Gembifrozil (Lopid)

A

Drug Class: PPAR-alpha (peroxisome proliferator-activated alpha) agonist

MOA: agonism of PPAR-alpha to increase hepatic uptake and clearance of TGs from plasma

Indication: elevated TGs

Onset: several days

Elimination: liver metabolism, excreted in urine and feces (unusual to be excreted in both places)

Adverse Effects: rash, GI, gallstones, hepatotoxicity, myopathy. Contraindicated in severe kidney disease.

Interactions: statins (myopathy); warfarin (increased anticoagulant effects)

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4
Q

Omega-3 acid ethyl esters (Lovaza)

A

Drug Class: Omega-3 fatty acids

MOA: not well understood

Indication: elevated TGs

Elimination: liver via CYP450

Adverse Effects: burping, GI, taste changes. Caution with fish/shellfish allergy. Elevated ALT, can raise LDL (paradoxical).

Cautions: Discontinue before surgery (antiplatelet properties)

Interactions: antiplatelet or anticoagulant meds

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5
Q

Insulin

A

MOA: binds to insulin receptor to stimulate translocation of GLUT 4 to cell membrane

Indication: DM1, DM2, acute hyperglycemia

Onset/Peak/Duration: varies

Elimination: renal

Adverse Effects: hypoglycemia, lipohypertrophy, lipoatrophy, allergic reaction

Interactions: alcohol, oral hypoglycemic agents, B-blockers (hypoglycemia unawareness)

Administration: measured in units/mL; administered with insulin syringe
Routes: subQ (IM too fast)
Regular, rapid-acting can be IV
Only NPH can be mixed with rapid- and short-

Dosing:
insulin need increased by caloric intake, infection, stress, obesity, growth spurt, 2nd-3rd trimester
insulin need decreased by exercise, 1st trimester, immediate post-partum

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6
Q

Basal/Bolus

A

mimics natural insulin secretion rhythms (basal levels and spikes stimulated by glucose ingestion)

require carb counting and correction doses

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7
Q

Pramlintide (Symlin)

A

Drug Class: amylin amalog

MOA: Slows gastric emptying, promotes satiety, prevents postprandial hyperglycemia)

Indication: T1 and insulin-T2 patients as supplement

Onset/Duration: rapid onset/clearance

Elimination: renal

Adverse Effects: nausea, headache, hypoglycemia, caution of gastroparesis

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8
Q

Metformin (Glucophage)

A

Drug Class: biguanide

indication: first line T2DM

MOA: increase sensitivity of insulin receptors AND decrease liver gluconeogenesis

Onset/Duration: slow absorption, undetectable after 24 hrs

Elimination: renal, unchanged

Adverse Effects: A/N/V/D, lactic acidosis, avoid in hepatic/renal dysfxn, alcoholism

Interactons: alcohol, sulfonylureas, other DM meds

Caution: stop 48 hrs before radiologic procedure with IV contrast - need to make sure renal fxn is normal or else metformin can cause lactic acidosis

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9
Q

Glipizide (Glucotrol)

A

Drug Class: sulfonylurea

Indication: T2DM

MOA: stimulates insulin release by blocking ATP-sensitive K channels –> Ca++ influx and insulin release. SECRETAGOGUE (doesn’t require glucose)

Duration: 10-24 hrs

Elimination: hepatic metabolism, renal excretion

Adverse Effects: hypoglycemia, weight gain, hepatotoxicity, rash, avoid in pregnancy/lactation

Interactions: alcohol, B-blockers

Pt. Teaching: take w/ meals

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10
Q

Repaglinide (Prandin)

A

Drug Class: Meglitinide (glinides)

Indication: T2DM

MOA: secretagogue (same precautions)

Onset/Duration: rapid acting, rapid clearance, T1/2 = 1 hr

Elimination: hepatic metabolism, biliary excretion

Adverse Effects: hypoglycemia, weight gain

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11
Q

Acarbose (Precose)

A

Drug Class: a-Glucosidase inhibitor

Indication: T2DM

MOA: inhibit a-Glucosidase enzyme at GI brush border (inhibit carb absorption)

Onset/Duration: local in gut - take right before meals

Adverse Effects: abdominal distension, cramps, flatulence, diarrhea, hepatic dysfxn, caution if bowel obstruction

Interactions: metformin (GI effects amplified)

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12
Q

Secretagogue pt teaching

A

releases insulin regardless of food intake

eat with or right before meals

skip secretagogue if too sick to eat

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13
Q

Pioglitazone (Actos)

A

Drug Class: Thiazolidinedione (TZD)

Indication: T2DM

MOA: PPAR (peroxisome proliferator-activated receptor) gamma agonist; increases insulin sensitivity, decreases hepatic glucose production

Onset: well-absorbed from GI, peaks in 2 hrs, T1/2 = 3-7 hrs, metabolites T1/2 = 16-24 hrs

Elimination: hepatic metabolism, active/inactive metabolites formed via CYP2C8 pathway, renal/GI excretion

Adverse Effects: fluid retention, edema, HF

interactions: combo with insulin increases risk for hypoglycemia, CYP2C8 inhibitors and inducers

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14
Q

Sitagliptin (Januvia)

A

Drug Class: DPP-4 inhibitor

Indication: T2DM - 3rd line, usually in combo

MOA: inhibits DPP-4, increasing incretin action, increasing insulin synthesis and decreasing post-prandial glucagon (incretins require glucose presence)

Elimination: renal

Adverse Effects: low risk of hypoglycemia. headache, nasopharyngitis, upper resp. infection, rare pancreatitis, serious hypersensitivity rxns

Cautions: renal disease (reduce dose)

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15
Q

Canagliflozin (Invokana)

A

Drug Class: combo

Indication: T2DM

MOA: inhibits Sodium-glucose co-transporter-2 (SGLT2) in kidney. prevents reuptake of most filtered glucose (diruesed and not returned to circulation)

Metabolism: hepatic

Excretion: renal (do not give to pts with eGFR

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16
Q

Exenatide (Byetta)

A

Drug Class: combo (injectable)

Indication: T2DM

MOA: incretin-mimetic; synthetic analog of GLP-1; increases glucose-dependent insulin secretion AND decreased post-prandial glucagon, slows gastric emptying, suppresses appetite

Administer: injection, pen

Elimination: renal, unchanged

Adverse Effects: N/V/D, pancreatitis hypoglycemia w/ sulfonylureas, renal impairment, avoid in pregnancy

Interaction: slows absorption of oral drugs, give 1 hr before exenatide

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17
Q

Furosemide (Lasix)

A

Drug Class: loop diuretic

Indication: volume overload, edema. HTN and HF

MOA: loop diuretic - blocks Na and Cl reabsorption at TAL

Administer: slow IV push or slow IV drip (ototoxicity if too fast)

CV effect: decrease volume, afterload, preload

Onset/duration: oral - 30-60min/6-8 hr; IV - 2-5min/6 hr

Elimination: hepatic metabolism, renal excretion

Adverse Effects: volume depletion, dehydration, hypokalemia, ototoxicity

Interactions: antihypertensives, digoxin, NSAIDs, aminoglycoside antibiotics

Caution: sulfa allergy

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18
Q

Furosemide (Lasix) patient teaching

A

at low doses, K rich diet may be enough

at higher doses, K supplement needed (risk of dysrhythmias)

increased urination

  • don’t take overnight
  • easy access to bathroom/commode
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19
Q

Hydrochlorothiazide (HydroDiuril)

A

Drug Class: thiazide diuretic

Indication: HTN, edema

MOA: thiazide diuretic. blocks Na/Cl reabsorption at early DCT

CV effects: decrease blood volume, arterial resistance

Onset/duration: 1-2hr/6-12hr

Excretion: unchanged in urine

Adverse Effects: volume depletion, dehydration, hypotension, hypokalemia

Interactions: antihypertensives, digoxin, NSAIDs

Caution: sulfa allergy

20
Q

Spironolactone (Aldactone)

A

Drug Class: diuretic

Indication: HTN, edema, HF, off label for acne

MOA: blocks aldosterone action at late DCT and collecting ducts (salt/fluid excretion, K retention. in HF can block myocardial remodeling, myocardial fibrosis, SNS activation and vascular fibrosis promoted by aldosterone

Onset/Duration: 24-48hrs/48-72hrs (gene tranxn)

Adverse Effects: hyperkalemia, endocrine effects

Interactions: antihypertensives, ACE-inhibitors and ARBS, K supplements

21
Q

Lisinopril (Prinivil, Zestril)

A

Drug Class: ACE inhibitor (only one that is NOT a prodrug)

Indication: HTN, HF, MI, nephropathy

MOA: blocks conversion of Angiotensin I to Angiotensin II by inhibiting ACE, elevates bradykinin

CV effects: vasodilation, decrease afterload, preload, Na reabsorption, cardiac remodeling

Elimination: renal

Adverse Effects: cough, angioedema

Interactions: diuretics, antihypertensives, K supplements, K sparing diuretics

Contraindications: pregnancy, bilateral renal artery stenosis

22
Q

Losartan (Cozaar)

A

Drug Class: ARB

Indication: HTN, HF, diabetic nephropathy

MOA: blocks type-1 angiotensin II receptor in blood vessels, heart, adrenals

CV effects: dilation of arterioles and veins, prevention of cardiac remodeling induced by angiotensin II, decreased release of aldosterone

Onset: 6 hrs

Elimination: biliary and renal

Adverse Effects: hypotension, angioedema, rash

Interactions: diuretics, antihypertensives, K supplements

Contraindications: pregnancy, bilateral renal artery stenosis

23
Q

Aliskiren (Tekturna, Rasilez)

A

Drug Class: Cdirect renin inhibitor

Indication: HTN

MOA: inhibits conversion of angiotensinogen to angiotensin I; suppresses entire RAAS

poor bioavailability: 2.5%

Onset: 2 wks

Elimination: liver metabolism via CYP3A4; 25% unchanged

Adverse Effects: hyperkalemia, low incidence of cough and angioedema, GI effects

Interactions: furosemide irbesartan, atorvastatin, ketoconazole, CYP3A4 inhibitors

Contraindicated: pregnancy

24
Q

Prazosin (Minipress)

A

Drug Class: a1-adrenergic antagonist

Indication: HTN

MOA: dilates arterioles and veins

Onset/Duration: 1-2hrs/10hrs

Elimination: hepatic metabolism; excreted in bile and urine

Adverse Effects: orthostatic hypotension, reflex tachycardia - start low and go slow

25
Q

Metoprolol (Lopressor)

A

Drug Class: B1-adrenergic blockade

Indication: HTN, HF, angina, MI

MOA: cardioselective

CV Effect: decrease HR, contractility, AV conduction

IV in acute MI

Elimination: hepatic metabolism, renal excretion

Adverse Effects: bradycardia, hypoglycemic unawareness

Interactions: antihypertensives

Cautions: heart block and HF

Contraindications: bradycardia and AV block >1st degree

cannot be abruptly stopped - will cause rebound cardiac excitation

26
Q

Carvedilol (Coreg)

A

Drug Class: mixed B1 and a1 blockade

Indication: HF, HTN

MOA: B1 block: decreases HR, AV conduction, contractility, renin release
a1 block: vasodilation

Elimination: hepatic metabolism, renal excretion

Adverse Effects: bradycardia, dizziness, postural hypertension, worsening HF

27
Q

Clonidine (Catapres)

A

Drug Class: a2 activation

Indication: HTN

MOA: central (CNS) a2 activation in presynaptic cells in brainstem (decrease sympathetic outflow, activation of adrenergic receptors in vessels and heart by NE)

Elimination: hepatic metabolism, renal excretion

Adverse Effects: posture-independent hypotension, drowsiness, rebound HTN if abruptly withdrawn

Interactions: antihypertensives

Contraindication: pregnancy (fetal harm)

28
Q

Verapamil (Isoptin, Verelan, Calan)

A

Drug Class: CCB

Indication: angina, HTN, dysrhythmias (IV)

MOA: blocks Ca channels in vascular smooth muscle, myocardium, SA/AV nodes

IV considerations: slow, monitor BP and ECG, can cause serious cardiac side effects

Onset/Duration: 30 min/5hr

Elimination: hepatic metabolism

Adverse Effects: constipation, bradycardia

Interactions: digoxin, B-blockers, grapefruit juice

Caution: cardiac conduction disturbances, heart block

29
Q

Nifedipine (Adalat, Procardia)

A

Drug Class: CCB

Indication: angina, HTN

MOA: blocks Ca channels mostly in vascular smooth muscle cells

Onset/Duration: 20-30 min/24hr

Elimination: hepatic 1st pass effect, renal excretion

Adverse Effects: reflex tachycardia

Interaction with B-blockers

At high doses: loses selectivity and affects heart and blood vessels; toxic effect

30
Q

Nitroglycerin

A

Drug Class: venodilator

Indication: angina

MOA: vasodilation via NO

Elimination: hepatic inactivation

Adverse Effects: headache, orthostatic hypotension, cardiac vasospasm if patch/ointment withdrawn abruptly

Interactions: antihypertensives, phosphodiesterase Type 5 inhibitors (erectile dysfxn drugs)
–> life threatening hypotension

31
Q

Nitroglyerin patient teaching

A

for chest pain: 1 dose every 5 minutes x 3

patch must be of 10-12 hrs/day

never mix with erectile dysfxn drugs, ever

do not abruptly stop

change positions slowly to avoid orthostatic hypotension

store moisture-free at room temp in original container

wear gloves

32
Q

Hydralazine (Apresoline)

A

Drug Class: vasodilator

Indication: HTN, HF

MOA: stimulates release of NO from endothelium - acts on arterioles not veins

Onset/Duration: 30-45min/6hrs

Elimination: acetylation

Adverse Effects: reflex tachycardia, lupus-like rxn, increased blood volume

33
Q

Digoxin (Lanoxin)

A

Drug Class: cardiac glycoside

Indication: HF, a.fib

MOA: inhibits Na/K ATPase pump. positive inotrope

CV effects: increases myocardiocyte intracellular Ca –> inotropic effect (increase contractility)

increase arterial pressure –> decrease sympathetic drive on heart and vessels –> decrease HR, renin, preload

Requires serum monitoring

Elimination: renal

Adverse Effects: cardiac dysrhythmias, GI disturbances

Caution with hypokalemia

Digifab/Digibind = antibody (Fab antibody fragments)

Interactions: many

Does not prolong life

34
Q

Digoxin patient teaching

A

take exactly as prescribed

check pulse and rhythm before taking - hold if low or irregular

toxicity S/Sx: A/N/V, yellow/green haze of vision

know hypokalemia signs

35
Q

Aspirin

A

Drug Class: platelet de-aggregator

Indication: 1ary and 2ary prevention of MI, ischemic stroke, TIA, angina. acut MI

MOA: irreversibly inhibits COX (1>2)

Onset/Duration: 20min/for life of platelet

Elimination: hepatic then renal

Adverse Effects: bleeding, renal dysfxn, Reye syndrome

interactions: warfarin, anticoagulants, glucocorticoids, alcohol, ACE inhibitors, ARBS

36
Q

Clopidogrel (Plavix)

A

Drug Class: platelet de-aggregator

Indication: irreversible ADP receptor antagonist (prodrug) -reduce rate of stroke, MI, death in patients with recent history

MOA: inhibits platelet aggregation for life of platelet

Onset/Duration: 2hrs/7-10 days

Elimination: 1st pass metabolism. CYP2C19 converts prodrug to active form

Adverse Effects: dyspepsia, abdominal pain, diarrhea, rash

Interactions: proton-pump inhibitors (CYP2C19)

some people have a genetic variant in CYP2C19 that makes them more metabolizers

37
Q

Eptifibatide (Integrilin)

A

Drug Class: platelet de-aggregator

Indication: ACS managed medically or with PCI

MOA: GpIIB/IIIa inhibitor –> no receptor for fibrinogen –> platelet aggregation inhibited

IV ONLY
Used concurrently with aspirin and heparin

Onset/Peak: steady state by 4-6 hr

Elimination: renal clearance with plasma T1/2 = 2.5 hr

Adverse Effects: bleeding, thrombocytopenia

Interactions: antiplatelet drugs, heparin, thrombolytics, aspirin, NSAIDs

Contraindicated: major surgery, bleeding, hypertension, history of hemorrhagic stroke

38
Q

Warfarin (Coumadin)

A

Drug Class: anticoagulant

Indication: prevention of thrombosis associated with PE, prosthetic valves, a. fib

MOA: prevents active Vit. K regeneration (VKORC1 reductase) which reduces levels and functionality of Vit.K-dependent clotting factors (II, VII, IX, X)

Onset/Duration: 12 hrs, full effect days/ 2-5 days

Elimination: hepatic, renal/feces

Adverse Effects: bleeding, ecchymosis

Caution: category X drug

interactions: antiplatelet/coagulant agents, Vit. K, enzyme inhibitors-inducers, food components. Many drug interactions

Antidote: Vit. K

39
Q

Warfarin patient teaching

A

INR checks once a month (once a wk when titrating)

avoid drugs with bleeding risks

tell providers

safety precautions

maintain consistent intake of foods w/ vit.k

40
Q

Heparin

A

Drug Class: anticoagulant

Indication: treatment/prevention of thrombosis (MI, DVT, PE, stroke), prevention of postop venous thrombosis, open heart surgery, dialysis

MOA: increases antithrombin activity 1000x (which blocks thrombin and Xa)

IV or subQ. in UNITS

Onset/Duration: minutes/hrs

Elimination: hepatic, renal

Adverse Effects: bleeding, HIT

Interactions: antiplatelet agents

Caution in pts with bleeding risk

Antidote: protamine sulfate

41
Q

Heparin-induced thrombocytopenia

A

prothrombotic disorder caused by antibodies to complexes of platelet factor 4 and heparin

antibodies bind to PF4-heparin complexes on platelet surface and induce platelet activation

activated platelets release/express PF4 (positive feedback loop)

release of procoagulant platelet microparticles, thrombosis, platelet consumption, thrombocytopenia

can cause venous and arterial thromboses

42
Q

Enoxaparin (Lovenox)

A

Drug Class: anticoagulant

Indication: treatment/prevention of thrombosis

MOA: low-molecular weight heparin: increases anti-thrombin activity. preferentially inactivates Xa and not thrombin

Elimination: hepatic

Adverse Effects: bleeding

Interactions: antiplatelet agents, drugs that cause bleeding

Caution in patients with spina/epidural catheter

antidote: protamine sulfate

43
Q

Dabigatran Etexilate (Pradaxa)

A

Drug Class: anticoagulant

Indication: prevention of systemic embolism and stroke in pts with a.fib

MOA: competitive direct thrombin inhibitor (prodrug)

Administer intact capsule - breaking it increases bleeding risk

Onset/Peak/Duration: 30min/1-2hrs/24-36hrs

Elimination: P-glycoprotein substrate; glucuronidation to 4 active metabolites; renal elimination; dose adjustment in pts with reduced renal fxn

Adverse Effects: bleeding

Interaction: P-glycoprotein inducers/inhibitors

Contraindicated of active bleeding or mechanical prosthetic heart valve

No antidote

pt. teaching: keep in original bottle (unstable to moisture)

44
Q

Rivaroxaban (Xarelto)

A

Drug Class: anticoagulant

Indication: prevention/treatment of DVT; prevention of stroke in a.fib

MOA: Xa inhibitor

Peak: 2-4 hr

Elimination: P-glycoprotein substrate; some hepatic metabolism, urine and feces. avoid in renal impairment.

Adverse Effects: bleeding including spinal/epidural hematoma; increased risk of thrombotic stroke

Interaction: anticoagulants; P-glycoprotein/CYP3A4/5 inducers/inhibitors

Contraindicated if active bleeding

No antidote

45
Q

Alteplase (tPA) (Activase)

A

Drug Class: thrombolytic

Indication: acute MI, PE, ischemic stroke

MOA: activation of fibrin-bound plasminogen. identical to endogenous human tPA

T1/2 = 5 min

Adverse Effects: bleeding

Contraindications: prior hemorrhagic stroke, ischemic stroke in last 3 mo., brain cancer,

Caution: uncontrolled HTn, remote stroke, recent trauma, post surgery, active PUD, pregnancy, anticoagulants

Interactions: antiplatelet/anticoagulant agents

Pathophysiology, Pharmacology, and Therapeutics (7 decks)

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