95 terms

Pharm Exam 2

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Morphine MOA
agonizes opioid receptor, mimics endogenous opioid peptide
Morphine actions
pain relief, drowsiness, mental clouding, anxiety reduction, sense of well-being
morphine pharmacokinetics
administered by several routes: oral, IM, IV, SC, epidural and intrathecal
fentanyl
other strong opioid agonist (100x the potency of morphine)
2 strong opioid agonists
morphine and fentanyl
3 moderate to strong opioid agonists
codeine, oxycodone, hydrocodone
Codeine, Oxycodone, Hydrocodone MOA
-opioid agonist
-schedule 2 and used for severe pain (5-10 on pain scale)
Codeine, Oxycodone, Hydrocodone actions
-similar to morphine in most respects
-produces analgesia, sedation, euphoria
-can cause respiratory depression, constipation, urinary retention, cough suppression and miosis
differences between morphine and codeine/oxycodone/hydrocodone
-3 moderate produce less analgesia and respiratory depression than morphine
-3 have somewhat lower potential for abuse
naxolone (narcan) MOA
-opioid antagonist (mu and kappa)
-drugs that block the effects of opioid agonists
principal uses of narcan
-treat opioid overdose
-relief of opioid-induced constipation
-reversal of post-op opioid effects
agonist-antagonist opioids MOA
acts as agonist at kappa receptor and antagonist as mu receptor
cannabis/marijuana (THC/dronabinol (marinol)) MOA
activates cannaboid receptors in the brain
cannabis/marijuana actions
suppression of emesis, appetite stimulation, relief of neuropathic pain
1st generation NSAIDS-aspirin MOA
inhibit cox-1 and cox-2
-irreversible action
aspirin action
-used to treat inflammatory disorders (rheumatoid arthritis, osteoarthritis, bursitis)
-alleviate mild to moderate pain
-suppress fever
-relive dysmenorrhea
-suppress inflammation but have risk of serious harm
-GI bleeding
-cardioprotective (inhibits platelets)
non aspirin 1st generation NSAIDS (ibuprofen/advil) MOA
-inhibit cox-1 and cox-2 (more cox-2)
-inhibition is reversible (unlike with aspirin)
non aspirin 1st generation NSAIDS action
-aspirin-like drug with fewer GI, renal and hemorrhagic effects than aspirin
-principal indications: rheumatoid arthritis an osteoarthritis
-doesn't protect against MI, stroke, or platelet aggregation
second generation NSAIDs celecoxib (Celebrex) MOA
inhibits Cox-2
second generation NSAIDs action
-suppresses inflammation
-relieves pain
-no help in reducing MI/stroke
-affect BP so never give during peri or post operative period
second generation NSAIDS uses
-osteoarthritis
-rheumatoid arthritis
-acute pain
-dysmenorrhea
acetaminophen (Tylenol) MOA
unknown COX inhibitor
-inhibits prostaglandin synthesis in CNS
Tylenol therapeutic uses
-analgesic, antipyretic
-doesn't have any anti-inflammatory or anti-rheumatic actions
-not associated with Reye's syndrome
aspirin MOA
-platelet aggregate inhibit
-inhibit cyclooxyrgenase action
aspring therapeutic uses
-ischemic stroke/TIA
-chronic and acute angina
-coronary stenting
-acute or past MI
-primary prevention of MI
aspirin adverse effects
bleeding, GIB, hemorrhagic stroke
clopidogrel (plavix) MOA
-antiplatelet drug
-adenosin diphosphate receptor antagonist
-prodrug
clopidogrel therapeutic uses
-prevents blockage of coronary artery stents
-reduces thrombotic events in patients with acute coronary syndromes
clopidogrel adverse effects
-similar to aspirin (bleeding, GI bleed, hemorrhagic stroke)
don't give clopidogrel to people taking what?
-most proton pump inhibitors due to cytochrome P450
-use with caution in combination with other drugs that promote bleeding
tirofiban (aggrastat) MOA
-antiplatelet drug
-glycoprotein 2b/3a inhibitor
-inhibits main bridge between coagulation pathway
Tirofiban (Aggrastat) therapeutic uses
-unstable angina
-PTA/stent procedures
-MI
Tirofiban Adverse Effects
-bleeding
-thrombocytopenia
-rash
-HA
-nausea
unfractionated heparin MOA
-enhances antithrombin 3
-rapid-acting anticoagulant
-administered by injection or IV only
fractionated heparin therapeutic uses
-preferred anticoagulant during pregnancy if rapid anticoagulant is required because it is polar (harder to cross the placenta)
-pulmonary embolism (PE)
-ischemic stroke evolving
-massive deep venous thrombosis
-NOT GIVEN for hemorrhagic strokes
low molecular weight heparin (heparin derivative-lovenox/enoxaprin) MOA
-inactivates factor Xa
-potentiates action of antithrombin 3
heparin derivative therapeutic uses
-prevention of DVT following surgery (knee, hip replacement)
-treatment of established DVT
heparin and its derivative's antidote
protamine sulfate
warfarin (Coumadin) MOA
-vitamin K antagonist
-inhibiting factors 7, 8, 10 and prothrombin
-PO only
warfarin (Coumadin) therapeutic uses
-not useful in emergencies (long half life)
-long-term prophylaxis of thrombosis
-prevention of venous thrombosis and associated pulmonary embolism
-prevention of thromboembolism (in patients with prosthetic heart valves)
-prevention of thrombosis during atrial fibrillation
atrial fibrillation
-impulse isn't getting back and forth the way it's supposed to
-atria don't contract efficiently
-blood can get left behind and pool
-anticoagulants can be in effective in people with chronic afib
warfarin (Coumadin) antidote
vitamin k for hypoprothrombinemia
warfarin adverse effects
-Hemorrhage (vit. K for toxicity)
-Fetal hemorrhage & teratogenesis from use during pregnancy
-use during lactation
-99% protein bound
direct thrombin inhibitors MOA (dibigatran, etexilate, pradaxa)
-direct inhibition of thrombin
-oral prodrug undergoes conversion to dabigatran
advantages of direct thrombin inhibitors
-no monitoring of INR
-little risk of adverse interactions
-uniform dose regardless of age or weight
adverse effects of direct thrombin inhibitors
-prodrug so doesn't work in liver failure patients
-bleeding
-GI disturbances
-must stop 1-2 days before surgery
direct thrombin inhibitors therapeutic uses
-prevent stroke and systemic embolism in patients with nonvalvular afib
direct factor Xa inhibitor (rivaroxaban/Xarelto) MOA
-acts directly to inhibit Xa without using antithrombin 3
-PO
advantages of direct factor Xa inhibitor
-safer than thrombin inhibitors
direct factor Xa inhibitor therapeutic uses
-prophylaxis
-less severe pre-formed thrombus
-cancer related thromboembolism
adverse effects of direct factor Xa inhibitor
-bleeding
-thrombocytopenia
-agranulocytosis
-steven-johnson syndrome (severe rash)
thrombolytic drugs (alteplase/tPa) MOA
-promote conversion of plasminogen to plasmin
-route is IV
major adverse effect of thrombolytic drugs
-bleeding (minor oozing to life-threatening amount)
-bleeding in recent wounds, needle puncture sites, invasive procedure sites
-anticoagulants increase the risk for hemorrhage
-blood replacement may need to be considered
therpeutic uses of tPA (alteplase)
-must be given 4-6 hours within onset of symptoms
-acute coronary thrombosis (acute MI)
-acute ischemic stroke
-acute massive pulmonary emboli
adverse effects of tPA
-bleeding
-excessive fibrinolysis can be reverse with IV aminocaproic acid (amicar)
ACE-I MOA (lisinopri, enalopril, captopril, zestril) MOA
-blocks conversion of angiotensin 1 to angiotensin 2 and produces a net dilation
-blocks stimulation of aldosterone release from adrenal gland which blocks sodium retension
-dilates blood vessels
-reduces blood volume
-increase bradykinin
ACE-I uses
-hypertension
-heart failure
-MI
-diabetic and non diabetic nephropathy
-preventio of MI
-stroke
-prevent death in patents at high CV risk
ACE-I adverse effects
-first dose hypotension
-fetal injury
-cough
-angioedema
-hyperkalemia
-dysgeusia and rash (captopril)
-renail failure (contraindication)
-neutropenia (captopril) and agranulocytosis
ARBs MOA
-blocks vasoconstriction by antagonizing the effects of angiotensin 2 at the receptor site
-decreases peripheral vascular resistance
ARBs therapeutic uses
-hypertension
-heart failure
-diabetic nephropathy
-MI
-stroke prevention
-migraine headache
ARB adverse effects
-angioedema
-fetal harm
-renal failure (contraindicated)
Direct Renin Inhibitors (aliskiren/tekturna) MOA
-binds tightly with renin and inhibits the cleavage of angiotensinogen into angiotensin (direct renin inhibitor)
-suppressed the entire RAAS
DRI uses
hypertension only
DRI side effects
-well-tolerated
-angioedema, cough (rare), diarrhea, hyperkalemia (with combination), fetal injury and death (similar to ACE and ARBs)
does the adverse effect of cough from ACE inhibition occur right away?
usually, but it can occur later in treatment (first 2 weeks more often)
which drug works highest on RAAS cascade?
aliskiren (tekturna)
which drug is listed as a diuretic and as a RAAS system drug?
spironolactone (aldactone)
what considerations do all of the RAAS drugs have in common?
they all have the potential of causing hyperkalemia and have risks for pregnancy
CCB MOA
blockade at...
-peripheral arterioles causing dilation and reduced arterial pressure
-arteries arterioles of the heart and increase coronary perfusion
-SA node and reduces heart rate
-AV node and decreases AV nodal conduction
-myocardium and causes decreased force of contraction
DHP CCBs (nifedipine) uses
-best choice for hypertension of the CCBs
-angina
-migraines
-selective
non-DHP CCBs (Verapamil, Diltiazem) uses
-nonselective
-best choice for CAD
-decreases HR, contractility, workload, and BP
-use for angina, cardiac dysrhythmias, and migraines
CCB side effects
-bradycardia
-hypotension
-headache, dizziness, light-headedness
-reflex tachycardia
-fatigue
-peripheral edema
-constipation (verapamil)
fishing of the skin (nifedipine)
-AV block
thiazide diuretics MOA
(hydrochlorothiazide HCTZ)
-inhibits sodium and chloride reabsorption
-increases urine volume
-reduces blood volume
-reduces arterial resistance
thiazide diuretics adverse effects
-electrolyte imbalance especially Na, Cl, and K (monitor these, BUN and Cr)
-hypokalemia (not usually profound here)
-hypotension
-dry mouth
-uric acid retention (gout)
high ceiling (loop) diuretics (furosemide-lasix) MOA
-inhibit chloride and sodium reabsorption in ascending loop of Henle
loop diuretic uses
-acute edema
-hypertension
-renal impairment
loop diuretic adverse effects
-dry mouth
-hypotension
-pronounce hypokalemia
-ototoxicity (especially from things also being taken like gentamycin)
potassium sparing diuretics (spironolactone) MOA
promote sodium excretion but retain potassium in the distal tubule
potassium sparing diuretics uses
-available PO
-hypertension, edema
-heart failure
-counteract K wasting effects
potassium sparing diuretics adverse effects
-hyperkalemia
-electrolyte abnormalities
beta 1
decreases heart rate and force, decreases renin secretion
beta 2
increases airway and vascular resistance
beta adrenergic blockers (propranolol and metoprolol) MOA
-blocks beta 1 in heart (some are selective)
-blocks beta 2 in smooth muscle and other places (some are not selective)
-beta 1 can lose selectivity at higher doses
beta blocker uses
-hypertension
-angina
-cardiac dysrhythmias
-MI
-migraines
-stage fright
-HF
beta blocker side effects
-fluid retention or worsening of HF
-fatigue
-hypotension
-bronchospasm from beta 2 receptor inhibition
-bradycardia or heart block
-inhibition of glycogenolysis
alpha 1 blockers
-prazosin, doxazosin
-reduces essential hypertension
-reduces benign prostatic hyperplasia
adverse effects of alpha 1 blockers
-orthostatic hypotension really bad
-blockage of alpha receptors on vein
-reduces muscle tone in the venous wall
-upon standing, blood pools in the veins
-return of blood to the heart reduced
-cardiac output decreases-blood pressure drops
-ALWAYS dangle feet first
-reflex tachycardia
-nasal congestion
-inhibition of ejaculation
-sodium retention and increased blood volume
alpha 2 clonidine MOA
-selective activation of alpha 2 receptors in the CNS
-reduces sympathetic outflow to blood vessels and the heart
-reduced norepinephrine
alpha 2 clonidine effects
-bradycardia and a decrease in CO
-minimal orthostatic hypotension
alpha 2 clonidine adverse effects
-drowsiness
-xerostomia
-rebound hypertension (withdraw slowly over 2-4 days)
-not recommended during pregnancy
-constipation
-impotence
-gynecomastia
-CNS effects
alpha 2 methyldopa adverse effects
-positive Coombs test and hemolytic anemia
-hepatotoxicity (hepatitis, jaundice, and rarely fatal hepatic necrosis)
-xerostomia, sexual dysfunction, orthostatic hypotension, CNS effects
alpha 2 methyldopa therapeutic use
-hypertension
-no longer first line, but good for pregnancy
-lowers BP by acting at site within the CNS
-causes alpha 2 activation
-taken up into brainstem and converted into alpha 2 agonist (prodrug for brain)
-vasodilation, not cardio-suppression
-lowers BP in supine and standing subjects
vasodilator (hydralazine) MOA
selective dilation of arterioles
vasodilator hydralazine therapeutic uses
-essential hypertension
-hypertensive crisis
-heart failure
hydralazine (vasodilator) adverse effects
-postural hypotension is minimal
-reflex tachycardia
-increased blood volume
-systemic lupus erythematosus like syndrome
-headache, dizziness, weakness and fatigue