Exam 2 Medications Flashcards
Atorvastatin (Lipitor)
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
Ezetimibe (Zetia)
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.
Gembifrozil (Lopid)
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)
Omega-3 acid ethyl esters (Lovaza)
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
Insulin
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
Basal/Bolus
mimics natural insulin secretion rhythms (basal levels and spikes stimulated by glucose ingestion)
require carb counting and correction doses
Pramlintide (Symlin)
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
Metformin (Glucophage)
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
Glipizide (Glucotrol)
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
Repaglinide (Prandin)
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
Acarbose (Precose)
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)
Secretagogue pt teaching
releases insulin regardless of food intake
eat with or right before meals
skip secretagogue if too sick to eat
Pioglitazone (Actos)
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
Sitagliptin (Januvia)
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)
Canagliflozin (Invokana)
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
Exenatide (Byetta)
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
Furosemide (Lasix)
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
Furosemide (Lasix) patient teaching
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
Hydrochlorothiazide (HydroDiuril)
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
Spironolactone (Aldactone)
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
Lisinopril (Prinivil, Zestril)
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
Losartan (Cozaar)
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
Aliskiren (Tekturna, Rasilez)
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
Prazosin (Minipress)
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
Metoprolol (Lopressor)
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
Carvedilol (Coreg)
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
Clonidine (Catapres)
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)
Verapamil (Isoptin, Verelan, Calan)
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
Nifedipine (Adalat, Procardia)
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
Nitroglycerin
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
Nitroglyerin patient teaching
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
Hydralazine (Apresoline)
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
Digoxin (Lanoxin)
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
Digoxin patient teaching
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
Aspirin
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
Clopidogrel (Plavix)
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
Eptifibatide (Integrilin)
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
Warfarin (Coumadin)
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
Warfarin patient teaching
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
Heparin
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
Heparin-induced thrombocytopenia
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
Enoxaparin (Lovenox)
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
Dabigatran Etexilate (Pradaxa)
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)
Rivaroxaban (Xarelto)
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
Alteplase (tPA) (Activase)
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
