Exam 1 (Intro & Cardio Drugs) Flashcards
Pharmacokinetics
drug movement throughout the body
Trough
lowest level of a drug concentration in the body keep above Min. Effective Conc.
Peak
highest level of drug concentration keep below toxicity conc.
bioavailability
fraction of active from of a drug that reaches systemic circulation
smaller bioavailability
= needs larger dosing to reach minimum effective concentration
absorption
movement of drug from site of administration to the blood
rate of absorption
= how soon effects will begin
distribution
movement of drug from blood into cells
3 types of distribution
- capillary beds = drugs pass easily
- blood brain barrier = very tight junctions, favor lipid soluble drugs
- placental drug transfer = diffusion
protein binding
- ALBUMIN
- binding is reversible
- some drugs have higher attract. to albumin == drug interactions
metabolism
- biotransformation of drug = alteration of drug structure
- occurs mostly in the liver
- drugs metabolized by same pathway == metabolism competition == dangerous
excretion
- movement of drug out of the body
- through urine, sweat, bile, saliva, breast milk, expired air
- KIDNEYS are the most important indicator
- GFR = drugs pass through capillary pores, large molecules (albumin) stay in blood
- passive tubular reabs. = polar/ionized drugs are removed through urine
half-life
- the time required for the drug in the body to decrease by 50%
- shorter HL = more frequent dosing to meet MEC
- longer HL = longer interval dosing w/o loss of MEC
minimun effective concentration
- plasma drug concentration required to prodcue desired/therapeutic response
3 ways drugs cross the cell membrane
- channels/pores (not common)
- transportation systems (selectivity)
- direct penetration of membrane (most drugs)
pharmacodynamics
- biochemical & physiological drug effects on the body & molecular mechanisms that produce these effects
dose reponse relationship
- relationship between administered dose size & response intensity (relative potency)
receptor interactions
- receptors are special chemical sites in the body that most drugs interact with (bind) == effects
- more selective = less side effects
agonists
- drugs that MIMIC body’s own regulatory molecules by activating receptors == produces maximal biological response
- ex: dobutamine mimics norepinephrine
antagonists
- drugs that BLOCK actions of endogenous regulators by preventing activation of receptors
- DOES produce pharmacological effect
- ex: antihistamines bind to histamine receptors == suppress allergy symptoms
therapeutic index
- falls between MEC & toxicity
- wider range/index = safer drug
plateau drug levels
- repeated admin. of same drug = increased drug lvl if 2nd dose is admin. prior to all of drug being eliminated
- When drug admin repeats w/ same dose == plateau will be reached in approx. 4 half-lives
- ex: if HL = 24 hrs, plateau = 96 hrs
loading dose
- to achieve plateau
- inital larger (loading) dose given, then smaller doses onces plateau is reached (maintenance dose)
kidney disease effects on tolerance
- decreased drug excretion == drug accumulation
liver disease effects on tolerance
- decreased drug metabolism == drug accumulation
tolerance
- decreased responsiveness = pt needs higher doses
BP classification
- <120 / <80: normal BP
- 120-129 / <80: elevated BP
- 130-139 / 80-89: stage 1 HTN
- 140+ / 90+: stage 2 HTN
- 180+ / 120+: HTN crisis
- GOAL FOR HTN PTS = 130/80
ECG changes for potassium lvls
- tall peaked T wave
- loss of P wave
- widened QRS w/ tall T wave
overall considerations for cardiovascular drugs
- BP goals
- consider holding when BP < 100/60
- assess recent BP prior to admin
- education = ortho. hypotension, fall risk, concurrent use of antiHTN drugs == additive effects on BP & HR
Loop Diuretics
- action = increases renal excretion of water and electrolytes
- uses = edema d/t HF, renal disease, hepatic impairment & HTN
- DRUGS = furosemide (Lasix)
- caution = thiazides, sulfonamides, anuria, ascites, acute pulmo edema, alcohol intolerance
- side effects = hypotension, dehydration, hypokalemia, hypovolemia, ototoxicity (iv rapid inf. w/ high dose)
- nursing = fluid status, monitor electrolytes, BP & HR, report hypokalemia, geriatric=r/f falls, IV rate = 20 mgs/min, may inc blood glucose (DM), admin early to avoid nocturia
- education = orthostatic hypoten, report weight gain of >3lbs/day, hydration, electrolyte imbalance s/s, K+ rich foods, report ototoxicity (vertigo, ringing, buzzing), photosensitivity
Thiazide Diuretics
- action = increases excretion of Na+ & water
- uses = same as loop, & estrogen therapy, glucocorticoid therapy
- DRUGS = hydrochlorothiazide
- caution = thiazides, sulfomaines, anuria
- S/E = same as loop
- nursing & education = same as loop
Aldosterone Antagonists: K+ Sparing Diuretics
- action = blocks action of aldosterone, retention of K+ & excretion of Na+
- uses = HF, HTN, edema (cirrhosis & nephrotic syn) primary aldosterone syndrome
- unlabelled uses = acne, hormone therapy for trans females
- DRUGS = spironolactone (Aldactone)
- caution = anuria, renal insuff., hyperkalemia, addison’s disease, current use of eplerenone
- S/E = metabolic acidiosis, HYPERkalemia, gynomastia (males), breast tender, inc. hair growth (females), thrombocytopenia
- interacts = ACE-I, NSAIDs, K+ supplmement, cyclosporine, antiHTN, alcohol, lithium & digoxin toxicity
- nursing = fluid status, BP, r/f falls, periodic ECF for prolonged therapy, skin rash (SJS), electrolytes (r/f HYPERkalemia)
- education = dizzniess, avoid salt-subs containing high K+, s/s of hyperkalemia, how to check BP weekly
s/s of HYPERkalemia
- fatigue
- muscle weakness
- paresthesia
- confusion
- dyspnea
- cardiac arrhythmias
Osmotic Diuretics
- action = inc. osmotic press. of GFR == excretion of water, electrolytes, & urea
- uses = IV: decrease intracranial pressure & cerebral edema, inhalation: cystic fibrosis
- caution = anuria, severe hypovol., active intracranial bleed, severe pulmo edema, renal impair. pts
- DRUGS = mannitol
- S/E = coma, chest pain, HF, blurred vision, electrolyte imbal, n/v, phlebitis @ IV site, rebound ICP
- interacts = nephrotic drugs & digoxin toxicity
- nusring = IV needs filter needle, assess fluid status, renal function, ICP readings, extravasation (fluid leaking into surrounding tissue) == may cause necrosis
Angiotensin-Converting Enzyme Inhibitor (ACE-I)
- action = blocks form. of angiotensin 2 == systemic vasodilator
- uses = HTN, HF
- DRUGS = lisinopril
- caution = hypotension, ACE-I, angioedema, pregnancy/lactation, caution with black pts (monotherapy = less effective)
- S/E = hypotension, renal impair, hyperkalemia, dizziness, cough, angioedema, 1st dose hypo
- interacts = diuretics, antiHTN, NSAIDs
- nursing = monitor for angioedema (swelling of face, extremities, eyes, lips, diff. swallow/breath), monitor BUN, CREA, K+, I/Os
- education = avoid salt subs w/ K+ or foods high in K+, ortho. hypoten, dizzy, hypoglycemia, notify ASAP for rash, angioedema, or dry cough, females w reproductive = need effective contraception
Angiotensin 2 Receptor Blockers (ARBs)
- action = blocks angiotensin 2 directly == secretion of water & Na+ & venous/arteriole dilation
- uses = HTN, diabetic neuropathy, stroke prevent.
- DRUGS = losartan
- caution = hypoten, bilateral renal artery stenosis, pregnancy/laction, caution with black pts
- S/E = hypoten, URI, back pain, HYPERkalemia, diarrhea, nasal congestion
- nursing = BP, angioedema, BUN, CREA, K+
- teachings = same as ACE-I
Angiotensin Receptor Neprilysin (ARNI)
- action = increase natriuretic peptides & suppress RAAS system
- DRUG = sacubitril (Entresto)
- caution = avoid w/ pregnancy/lactation
- suspension form of med is available
Direct Renin Inhinitors
- action = inhibits renin == decreased angiotensin 2 formation
- DRUG = aliskiren
- caution = hypotension, DM, pregnancy/lactation, cyclosporine, ACE/ARBS
- S/E = hypoten, renal impair, HYPERkalemia, reflux, diahrrea, angioedema
- interacts = high fatty meals decrease absorption
- nursing = BP, angioedema, BUN, CREA, K+,
Calcium Channel Blockers (CCB)
- action = prevents calcium from entering cell == dilation & decreased arterial pressure, decreases HR (SA node), decreases conduction (AV node)
- 2 families: dihydropyridines (nifedipine) & non-dyhydropyridines (verapamil & diltiazem)
- uses = HTN, angina / nifedipine unlabeled uses = migraine, HF, cardiomyopathy / verapamil & diltiazem = SVT & rapid vent. rates in a-fib
- caution = grapefuit juice, st. johns wort, sick sinus syndrome, SBP < 90, lactation
- S/E = reflex tachycar, bradycar, hypoten, arrhyth, HF, headache, SJS, syncope
- interacts = NSAIDs, digoxin, BB, fentanyl, nitrates, alcohol, GRAPEFRUIT JUICE
- nursing = BP, HR, HOLD IF <50bpm / SBP <90, edema, fluid status, angina pain, r/f falls
- IV push verapamil & diltiazem undiluted OVER 2 minutes / continuous infusion = titrate to HR & BP
Andrenergic Antagonists
- action = arteriole & vein dilation
- uses = HTN, BPH
- DRUGS = prazosin
- S/E = ortho. hypoten, reflex tachycar, nasal congestion, 1st dose hypoten
- education = take inital dose @ bed time, hypotension precautions
Central-Acting Alpha2 Agonists
- action = act w/ CNS == decrease adren. receptors of heart & periph. vascular sys === decrease CO and BP & HR
- uses = HTN, severe cancer pain, ADHD
- unlabelled uses = migraines, flushing w/ menopause
- DRUGS = clonidine, guanfacine, methyldopa
- S/E = rebound HTN (from abruptly d’c), sedation, dizziness, dry mouth, constipation
- education = DON’T stop abruptly, hypoten precaut, larger doses @ bedtime
- methyldopa = safe for pregnancy!!!
Beta-Andrenergic Antagonists: Beta-Blockers
- action - block beta receptors of heart == decrease HR, contraction force, AV impulse
- 3 categories: non selective (block B1 & B2), cardioselective (block B1), 3rd gen (B w/ vasodilation action
- DRUGS = non-select (propranolol), cardioselect (metoprolol & atenolol), 3rd gen (carvedilol & labetalol)
- uses = HTN, cardiac dysrhythmias, MI, HF, hyperthyroidism
- S/E = non-select (bronchocontriction = avoid in pts w/ asthma, hypoglycemia = caution in pts w/ DM) / cardioselec (bradycardia, rebound cardiac excit w/ abrupt withdrawal
- caution = uncomp. HF, pulm. edema, cardio shock
- nursing = abrupt d’c may cause life-threat dysryth, monitor BP, HR, ECG, assess angina, hold if HR < 50 bpm or hyponten < 100/60
- education = ortho. hypoten, how to check BP weekly, pulse daily, may inc cold sensitivity
Hypertensive Emergency Drug
- DRUG = Nitropusside
- action = vasodilator
- caution = dec. cerebreal perf., renal/hepatic disease, r/f thiocyanate & cyanide accumulation)
- nursing = cyanide toxicity (lactic acidosis, hypoxemia, tachycar, altered LOC, seizure, almond breath odor), thiocyanate tox (tinnitus, hyperreflexia, confusion, weakness), monitor continuous VS & ECG
- IV solution may be brown, protect from light, discard after 24hrs
Cyclooxygenase Inhibitors
- action = inhibits enzymes needed for platelet synthesis, anaglesia, inhibits prostglandins = reduce fever & inflam
- uses = analgesia, reduce inflam, reduce fever, reduce incidence of MI
- DRUGS = aspirin, salicylates, NSAIDs
- caution = other NSAIDs, bleeding disorders, thrombocytopenia, avoid in OB over 30 wks, avoid in peds = r/f Reyes syndrome
- S/E = GI bleed, dyspepsia, n/v, hepatotoxicity, hypersensitivity
- nursing = may inc r/f hypersens. w/ pts w/ asthma, allergies, nasal polyps, prolonged bleeding for 7 days
- education = take w/ food to avoid gastric irrita., report unusal bleeding, black tarry stool or fever lasting >3 days, avoid alc & other NSAIDs, few days of acetaminophen/NSAIDs may cause neuropathy
- usually hold 1 week prior to surgery
Glycoprotein Inhibitors
- action = binds to platelet receptors = preventing fibrin from binding
- uses = dec r/f reocclusion after coronary artery revascularization, accelerates re-perfusion in pts undergoing thrombolytic therapy
- DRUGS = eptifibatide, tirofiban
- caution = active bleeding hx w/i 30 days, severe uncntrl HTN, major surg. w/i 6 wks, sever renal impair, hx of hemorrhagic stroke
- S/E = BLEEDING (GI, intracranial), hematuria, hematomas, thrombocytopenia, dec BP
- nursing = BLEEDING risk, assess cath site, monitor PTT, dont remove arteriole sheath if PTT < 45 sec
ADP inhibitors
- action = inhibits platelet aggregation by irreversibly inhibiting binding of ATP to plat. receptors
- uses = STEMI, non-STEMI, establish PAD, recent MI/stroke
- DRUGS = clopidogrel
- SAME NURSING & S/E & TEACHING: bleeding precautions
Arteriole Vasodilators
- action = inhibits cAMP == decrease PTT aggregation & vasodilation
- uses = intermittent claudation reduction of symptoms (PAD)
- DRUGS = cilostazol
- caution = HF
- nursing & education = avoid grapefruit juice, dizziness precautions, avoid smoking (vasoconstrictor), assess intermittent claud., admin on empty stomach
Vitamin K inhibitors
- action = interf. w/ hepatic syn. of vit. K dependent clotting factors
- uses = prophylaxsis & tx of venous thrombus, pulmo embolism, a-fid, mngmt of MI
- DRUGS = warfarin
- caution = active ulcer disease, uncntrl HTN, pregnancu, bleed/open wounds, recent brain/eye/spinal surg, severe liver/kidney impair.
- S/E = fever, bleeding, dermal necrosis, calciphylaxis (Ca build up in fat/skin/vessels) hepatitis
- nursing = high alter drug, assess r/f bleeding/hemorrhage, monitor INR, PT, CBC
- education = notify of missed dose, DON’T double dose, admin late afternoon/evening, avoid foods high in Vit K, cran juice, & alc
- avoid w oral contra, st johns wort, vit k foods (green veggies)
INR levels
- normal = 0.8-1.2
- therapeutic lvls = 2-3
- r/f emboli = 2.5-3.5
unfractionated heparin
- action = @ low doses (prevents conversion of prothrom - throm) @ high doses (neutralize throw
- uses = prevent thrombin formation, prevent extension of existing thrombus
- caution = severe thrombocytopenia, uncntrl bleed, liver/kidney disease, hx of heparin induced thrombocyt.
- S/E = alopecia (long-tern use), HYPERkalemia, anemia, bleeding,
- nursing = bleeding, monitor PTT, CBC, K+
- HIGH ALERT = bleeding
- admin = SQ 45-90 degree, alternate injection sites, DON’T massage, DON’T aspirate, IV = loading dose, no other meds in heparin infusion
Low Molecular Weight heparin
- same as heparin, but more predictable pharm. profile
- Uses = prevent VTE, DVT, PE
- DRUGS = enoxaparin, lovenox, dalteparin
- caution = same, & pork products, & benzyl alcohol
- S/E = alopecia (LT), HYPERkalemia, anemia, bleeding
- nursing = CAN’T be used w/ unfr. hep., used IV only for STEMI, DON’T expel air bubble
activated factor XA inhibitor
- action = binds to antithrombin 3 == preventing thrombus
- uses = prevent/tx DVT & PE
- DRUG = fondaparinux
- nursing = d’c med if PTT <100k, DON’T expel air bubble, inject SQ into R/L anterolateral abd wall, bleeding precautions
Direct Oral Anticoagulants (DOACs)
- action = direct thrombin inhitors / direct factor Xa inhibitors
- DRUGS = thrombin (dabigatran (pradaxa)) / Xa (apixaban (Eliquis))
- rapid onset, doesn’t req. routine blood monitor
- uses = dec r/f throbotic seq. (stroke, sys embolism), resolution of PE & DVT
- caution = st. johns wort, bleeding preautions
- acetode for factor xA inhibit = andexant alpha
thrombolytics
- ONLY DRUG CLASS THAT BREAKS FORMED CLOTS
- tissue plasminogen activator (TPA)
- uses = acute MI, ischemic stroke, acute massive PE
- DRUGS = alteplase, activase
- nursing = serious r/f bleeding, direct pressure up to 30 min, monitor VS, aPT, INR, Hgb, Hct, fibrinogen
- may use proton pump inhibitor to prevent GI bleed
LDL / HDL
- LDL = stores cholesterol in blood (bad)
- HDL = regulates LDL storage & promotes excretion (good)
HMG-CoA reductase inhibitors
- action = inhib HMG-CoA (enzyme that catalyzes cholesterol synthesis) == dec LDL & inc HDL
- uses = primary hypercholesterolemia, mix dyslipidemia, primary prevent of cornary heart disease
- DRUG = atorvastatin (Lipitor, Atorvaliq)
- caution = active liver disease, elevation of AST/ALT
- S/E = rash, abd cramp, flatus, heartburn, RHABDOMLYSIS (severe muscle dengen)
- nursing = serum cholesterol & TG, diet hx, LFTs, liver disease = d’c, CREA kinase >10 = d’c
- education = AVOID grapefruit, dont double dost, not a cure, diet health, notify for muscle pain, tender, weak or liver disease s/s
Bile-acid seqestrants
- action = inc LDL hepatocyte receptors == dec LDL lvls by 20%, improves glycemic control w DM2
- uses = adjunct w/ diet, usually combo w/ statins == dec LDL by 50%
- DRUGS = colesevelam, cholestyramine, cloestipol
- caution = bowel obstruct, TG>500, hx pracreatits d/t hyperTGemia
- S/E = constipation, n/v, bloat, may inc fat absop = dec uptake of fat sol vitamins
- admin 1-2 / day WITH food
Fibrates (fibric acid derivates)
- action = inhibits periph lipolysis, dec TG liver production, inc HDL
- uses = MOST effective drug for dec TG lvls
- DRUGS = gemfibrozil, fenofibrate
- caution = hepat/renal impair, gall baldd disease, current use of simuastatin
- S/E = abd pain, diahrrea, epi pain, rash, gallstones, myopathy
- interacts = warfarin == r/f bleeding
- nursing = monitor INR, r/f rhabod w/ statins
PCSK9 inhibitors
- made from hamster ovary cells
- action = PCSK9 protein binds to LDL receptors w/i liver == clear LDL from blood
- DRUGS = alirocumab
- SQ inj
- S/E = inj site reaction, confusion, hypersensitivity (angioedema, vasculitis)
- nursing = EXPENSIVE drug, may not be covered, solution should be room temp for use, solution = clear/pale yellow, admin 300mg as 150mg @ diff sites
- DON’T admin if solution is cloudy/has precipitate
Organic Nitrates
- action = promote vasodilation of conoary arteries, dec preload pressure, dec myocard O2 consump
- uses = mngmt of angina pectoris, adjunct tx of HF, MI
- DRUGS = nitroglycerin, isosorbide dinitrate, mononitrate
- caution = inc ICP, anemia, hypovol, PDE-5 inhib
- S/E = hypotension, tachy reflex, dizzy, headache
- nursing = asses angina, BP, HR, ECG (IV), IV must be diluted & special tube
education = dont miss/double doses, take 1st dose sitting, headahce common, keep tabs away from heath & replace every 6mo after opening
Ranolazine
- action = dec accumulation of Na+ & Ca+ in myocardial cells
- uses = 1st new antiangial drug in 25 yrs
- caution = CYP3A inhib, CCB (except amoldipine), hep impair, lactation
- S/E = QT prolongation, inc BP, TORSADES, acute renal failure
- nursing/education = no grapefruit, monitor renal function, ECG, fall risk
Sodium channel blockers
- action = slows impulse conduction in atria, ventricles & His-Purkinje system
- 1A DRUGS: quinidine, disopyramide = uses: restore/maintain sinus rhythm w a-fib/a-flutter, tx of malaria = S/E: hypotension, torsades, GI issues, agranulocytosis = nursing: admin w/ full glass of water on empty stomach (or w/ food if GI irrit), monitor ECG, HR, BP serum quinidine lvls = 2-6(good), >8mcg(toxic)
- 1B DRUGS: lidocaine (IV), mexiletine, phenytoin = uses: IV-vent. arrhy, IM-local anesth, transderm-pain = S/E: cardiac arrest, seizure, anaphylaxis, agran = nursing: serum lidocaine - 1.5-5mcg, toxicity = confusion, SOB, dizzy, n/v, tinnitus, tremors
- oral lidocaine can numb = may decrease swallowing
- 1C DRUGS: propafenone (oral), flecainide = uses: tx vent arrhy, a-fib/flutter, PSVT = S/E: dizzy, arrhythmia, altered tase, constipation, agran = nursing = K+ lvls, ECG, HR, BP *may prolong QT interval
classes of antidysrhthmic drugs
- 1 = sodium channel blockers
- 2 = beta blockers
- 3 = potassium channel blockers
- 4 = calcium channel blockers
- Others = Digoxin
potassium channel blockers
- action = prolongs AP refract period = dec adrenergic stim = slows sinus rate (PR&QT int)
- uses = tx of life-threat ventricular arrhythmias
- DRUGS = amiodarone
- S/E: corneal microdeposits, ARDS, Pulmo fibrosis, hyperthyroidism, HF, blue discoloration
- nursing = ECG, report bradycardia, BP, assess lungs, K+ lvls, assess thyroid
- education = avoid grapefuit, notify of all meds (st john wort) monitor pulse daily, photosensitivity, s/e may not appear until days/weeks/mo later
Digoxin
- dangerous drug d/t narrow TI
- action = inhibits Na/K ATPase == prolong refractory period of AV/SA node
- uses = HF, fib, paroxysmal atrial tachycardia
- caution = vent tachy, av block, ELECTROLYTES, renal impairment, obesity
- S/E: arrhy, Brady, anorexia, n/v, fatigue
- interacts = loop/thiazide, ACE-I & ARBS, dopamie, antacids, quinidine
- nursing = HIGH ALERT, continuous ECG, monitor AP pulse for 1 min, hold med if <60bpm, IV push over 5 min
- digoxin toxicity = abd pain, anorexia, n/v, visual issues, bradycardia
- hold if HR <60 or >100