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Exam Two
Pharm Exam Two
97
Nursing
Undergraduate 3
10/23/2011

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Term
ADRENERGIC RESPONSES TO STIMULATION
Definition
see following
Term
Cardiovascular: Blood Vessels
Definition
receptor: alpha one
response: constriction

receptor: beta two
response: dilation
Term
Cardiovascular: Cardiac Muscle
Definition
receptor: beta one
response: increased contractility
Term
Cardiovascular: AV Node
Definition
receptor: beta one
response: increased heart rate
Term
Cardiovascular: SA Node
Definition
receptor: beta one
response: increased heart rate
Term
Endocrine: Pancreas
Definition
receptor: beta one
response: decrease insulin release
Term
Endocrine: Liver
Definition
receptor: beta two
response: glycogenolysis
Term
Endocrine: Kidney
Definition
receptor: beta two
response: increased renin secretion
Term
GI: Muscle
Definition
receptor: beta two
response: decreased motility
Term
GI: Sphincter
Definition
receptor: alpha one
response: constriction
Term
Genitourinary: Bladder Sphincter
Definition
receptor: alpha one
response: constriction
Term
Genitourninary: Penis
Definition
receptor: alpha one
response: ejaculation
Term
Genitourinary: Uterus
Definition
receptor: alpha one
response: contraction

receptor: beta two
response: relaxation
Term
Respiratory: Bronchial Muscles
Definition
receptor: beta two
response: dilation
Term
Ocular: Pupillary Muscles of Iris
Definition
receptor: alpha one
response: mydriasis
Term
Adrenergic Catecholamines
Definition
substances that can produce a sympathomimetic response

endogenous: epinephrine, norepinephrine, dopamine

synthetic: isoprotenerol, dobutamine, phenylephrine

hint: mostly end in "ine"
Term
Category: Adrenergic Agonist Agent
Definition
classification: alpha/beta adrenergic

prototype: epinephrine

route: IV
onset of action: <2 min
peak: rapid
half-life: <5 min
duration: 5-30 min

route: subcut
onset of action: 5-10 min
peak: 20 min
half-life: variable
duration: unknown

NOTE: EPINEPHRINE ACTIVATES ALL ADRENERGIC RECEPTORS
Term
Adrenergic Agonist Agent Indications (epinephrine)
Definition
increase BP
restore cardiac function in an arrest
delay absorption of local anesthetic
overcome AV block
bronchial dilation in asthma
Tx of choice in anaphylactic shock
Term
Adrenergic Agonist Agent Side Effects
Definition
hypertensive crisis
dysrhythmias
angina pectoris
necrosis following extravasation
hyperglycemia
Term
Beta Adrenergic Agonist Response
Definition
bronchial, GI, and uterine smooth muscle relaxation

glycogenolysis

cardiac stimulation
Term
Alpha-Adrenergic Side Effects
Definition
CNS: headache, restlessness, excitement, insomnia, euphoria

CV: palpitations (dysrhythmias), tachycardia, vasoconstriction, hypertension

other: anorexia, dry mouth, nausea, vomiting, taste changes (rarely occurs)
Term
Beta-Adrenergic Side Effects
Definition
CNS: mild tremors, headache, nervousness, dizziness

CV: increased heart rate, palpitations (dysrhythmias), fluctuating blood pressure

other: sweating, nausea, vomiting, muscle cramps
Term
Dopaminergic Receptors
Definition
an additional adrenergic receptor

stimulated by dopamine

causes dilation of renal, mesenteric, coronary, and cerebral blood vessels, resulting in increased blood flow
Term
Category: Vasoactive Sympathomimetics
Definition
category: pressors, inotropes

prototypes: dobutamine, dopamine, epinephrine, isoproterenol, norepinephrine

route: IV
onset of action: 2-5 min
peak: rapid
half-life: <2 min
duration: 10 min

also fall under the category of inotropic drugs with vasopressors
Term
Vasoactive Sympathomimetics Indications (dopamine)
Definition
shock
heart failure
acute renal failure
Term
Vasoactive Sympathomimetics Mechanism of Action (dopamine)
Definition
dose dependent receptor specificity
low doses act on dopaminergic receptors only
high doses act on both dopaminergic and beta 1 receptors
very high doses activate alpha 1 receptors as well
Term
Vasoactive Sympathomimetics Side Effects
Definition
CV: tachycardia, dysrhythmias, angina

respiratory: dyspnea

integumentary: extravasation
Term
Beta Blocker Actions
Definition
B1 affects the heart

B2 affects the lungs
Term
Beta Blocker Mode of Action
Definition
beta receptors are on the surface of cells, innervated by the SNS, and mediate certain physiologic responses to adrenaline

beta receptor blockers block the activity of a beta receptor, decrease heart rate and force of contractions, and lower high blood pressure
Term
Category: Antihypertensives
Definition
classification: alpha antagonists

prototypes: phentolamine (Regitine), doxazosin (Cardura), terazosin (Hytrin), prazosin (Minipress), ergotamine tartrate (Ergostat), phenoxybenzamine HCI (Dibenzyline), tolazoline (Priscoline)

hint: mostly end in amine or zosin
Term
Alpha Blocker Indications
Definition
treat vascular headaches (migraines)
control post-partum bleeding
treat hypertension
treat BPH
Term
Beta Blocker Indications
Definition
antiangina
cardioprotective
class II antidysrhythmic
antihypertensive
treatment of migraine headaches
glaucoma (topical use)
Term
Alpha Blocker Mechanism of Action
Definition
interrupt SNS stimulation
results in vasodilation, reduced BP, miosis, reduced smooth muscle tone
Term
Beta Blocker Mechanism of Action (cardioselective B1)
Definition
reduces SNS stimulation of the heart
decreases heart rate
prolongs SA node recovery
slows conduction rate through the AV node
decreases myocardial contractility, thus decreasing myocardial oxygen demand
Term
Beta Blocker Mechanism of Action (nonspecific B1 and B2)
Definition
effects on heart: same as cardioselective
effects on bronchioles: constriction, resulting in narrowing of airways and shortness of breath
effects on blood vessels: mild vasoconstriction
Term
Alpha Blocker Pharmacokinetics (phentolamine)
Definition
route: subcut
onset of action: immediate
peak: 2 min
half-life: unknown
duration: 15-30 min
Term
Category: Antihypertensives
Definition
classification: beta blockers

non-cardio selective prototypes: carvedilol (Coreg), labetolol (Trandate), propanolol (Inderal), sotalol (Betapace)

cardioselective prototypes: atenolol (Tenormin), metoprolol (Lopressor), esmolol (Brevibloc)

hint: end in olol
Term
Beta Blocker Phamacokinetics (carvedilol)
Definition
route: po
onset of action: 20-120 min
peak: 1-4 hours
half-life: 6-8 hours
duration: 8-24 hours
Term
Beta Blocker Phamacokinetics (labetalol)
Definition
route: IV
onset of action: 2-5 min
peak: 5-15 min
half-life: 2.5-8 hours
duration: 2-4 hours

route: po
onset of action: 20-120 min
peak: 1-4 hours
half-life: 2.5-8 hours
duration: 8-24 hours
Term
Beta Blocker Pharmacokinetics (propanolol)
Definition
route: IV
onset of action: 2 min
peak: 1-4 hours
half-life: 3-5 hours
duration: 3-6 hours

route: po
onset of action: 1-2 hours
peak: 1- 4 hours
half-life: 3-5 hours
duration: 6-12 hours
Term
Beta Blocker Pharmacokinetics (sotalol)
Definition
route: po
onset of action: 1-2 hours
peak: 2.5-4 hours
half-life: 12 hours
duration: 8-16 hours
Term
Beta Blocker Pharmacokinetics (atenolol)
Definition
route: IV
onset of action: immediate
peak: <5 min
half-life: 6-7 hours
duration: <12 hours

route: po
peak:2-4 hours
half-life: 6-7 hours
duration: 24 hours
Term
Beta Blocker Pharmacokinetics (metaprolol)
Definition
route: IV
onset of action: 1 min
peak: 20 min
half-life: 3-8 hours
duration: 5-8 hours

route: po
onset of action: 1 hour
peak: 2-4 hours
half-life: 3-8 hours
duration: 10-20 hours
Term
Beta Blocker Pharmacokinetics (esmolol)
Definition
route: IV
onset of action: immediate
peak: 6 min
half-life: 9 min
duration: 15-20 min
Term
Alpha Blocker Side Effects
Definition
CV: palpitations, orthostatic hypotension, tachycardia, edema, dysrhytmias, chest pain

CNS: dizziness, headache, drowsiness, anxiety, depression, vertigo, weakness, numbness, fatigue

GI: nausea, vomiting, diarrhea, constipation, abdominal pain

other: incontinence, nosebleed, tinnitus, dry mouth, pharyngitis, rhinitis
Term
Beta Blocker Side Effects
Definition
blood: agranulocytosis, thrombocytopenia

CV: AV block, bradycardia, heart failure, peripheral vascular insufficiency

CNS: dizziness, mental depression, lethargy, hallucinations

GI: nausea, dry mouth, vomiting, diarrhea, cramps, ischemic colitis

other: impotence, rash, alopecia, bronchospasm
Term
Alpha/Beta Blocker Toxicity
Definition
acute overdose of po meds:
empty patients stomach immediately
induce emesis with syrup of ipecac
gastric lavage

acute overdose of IV meds:
treat symptoms (decreased BP/seizures)
Term
Adrenergic Blocking Agents Nursing Implications
Definition
assess for allergies and history of COPD, hypotension, cardiac dysrhythmias, bradycardia, HF, or other cardiovascular problems (any preexisting condition that might be exacerbated by the use of these agents might be a contraindication to their use)

remember that alpha blockers may precipitate hypotension

remember that beta blockers may precipitate bradycardia, hypotension, heart block, HF, and bronchoconstriction

avoid OTC medications because of possible interactions (antacids, antimuscarinics/anticholinergics, diuretics and cardiovascular drugs, neuromuscular blocking agents, oral hypoglycemic agents)

monitor for side effects such as hypotension, tachycardia (alpha blockers), bradycardia, heart block, HF, increased airway resistance, fatigue, lethargy, depression, insomnia, vivid nightmares

monitor for therapeutic effects such as decreased chest pain in patients with angina, return to normal BP and pulse, other specific effects depending on the use
Term
Beta Blocking Agents Nursing Implications
Definition
rebound hypertension of chest pain may occur if this medication is discontinued abruptly

patients should notify their physician if they become ill and unable to take medication

inform patients that they may notice a decrease in their tolerance for exercise; dizziness and fainting may occur with increased activity (notify physician if this occurs)

patients should report weight gain of more than two in a week, edema of the feet and ankles, shortness of breath, excessive fatigue or weakness, syncope or dizziness to their physician
Term
Category: Antihypertensive
Definition
classification: angiotensin converting enzyme inhibitor

prototypes: captopril (Capoten), lisinopril (Zestril), enalapril (Vasotec), quinapril (Acupril)

route: PO
onset of action: varies with drug
peak: varies with drug
half-life: varies with drug
duration: varies with drug
Term
ACEI Indications
Definition
hypertension
HF (either alone or in combination with diuretics or other agents)
slows progression of left ventricular hypertrophy after an MI
renal protective effects in patients with diabetes
drugs of choice in hypertensive patients with HF
Term
Category: Antihypertensives
Definition
classification: angiotensin II receptor blocking agents

prototypes: iosartan (Cozaar, Hyzaar), valsartan (Diovan)

route: po
onset of action: varies with drug
peak: varies with drug
half-life: varies with drug
duration: varies with drug

hint: sartan
Term
ARB Indications
Definition
hypertension
adjunctive agents for the treatment of HF
may be used alone or with other agents such as diuretics
used primarily in patients who cannot tolerate ACEI
Term
ARB Mechanism of Action
Definition
allow angiotensin I to be converted to angiotensin II, but block the receptors that receive angiotensin II

block vasoconstriction and release of aldosterone
Term
ARB Side Effects
Definition
upper respiratory infections
headache
may cause occasional dizziness, inability to sleep, diarrhea, dyspnea, heartburn, nasal congestion, back pain, fatigue

hyperkalemia much less likely to occur
Term
Category: Antihypertensive
Definition
classification: calcium channel blocker

prototypes: verapamil (Calan), nifedipine (Procardia), dilatizem (Cardizem)

route: po
onset of action: varies with drug
peak: varies with drug
half-life: varies with drug
duration: varies with drug
Term
CCB Action
Definition
blocks calcium access to cells causing decreased decreased contractility, decreased conductivity of the heart, and decreased demand for oxygen
Term
CCB Side Effects
Definition
decreased blood pressure
bradycardia
may precipitate AV block
headache
abdominal discomfort (nausea, vomiting)
peripheral edema
Term
CCB Side Effects by System
Definition
CV: hypotension, palpitations, bradycardia

GI: constipation, nausea

other: rash, flushing, peripheral edema, dermatitis
Term
CCB Indications
Definition
angina
hypertension
dysrhytmias
migraine headaches
raynaud's disease
Term
CCB Nursing Implications
Definition
blood levels should be monitored to ensure they are therapeutic

oral CCBs should be taken before meals and as ordered

patients should be encouraged to limit caffeine intake

extended release formulas should never be crushed or chewed
Term
Category: Antilipemic
Definition
classification: HMG-CoA reductase inhibitors

prototypes: atrovastatin (Lipitor), lovastatin (Mevacor), pravastatin (Pravachol), rosuvastatin (Crestor), simvastatin (Zocor)

route: po
onset of action: 0.5 hours
peak: 1-2 hours
half-life: 7-14 hours
duration of action: unknown

hint: all end in astatin
Term
HMG-CoA Inhibitor Reductase Indications
Definition
hypercholesterolemia
primary and secondary prevention of CV events
post-MI therapy
diabetes
Term
HMG-CoA Reductase Inhibitor Mechanism of Action
Definition
inhibition of HMG-CoA reductase = lower cholesterol biosynthesis

increased number of LDL receptors on hepatocytes = remove more LDL from blood

decreased production of aliprotein B-100 = decreased production of VLDLs
Term
HMG-CoA Reductase Inhibitor Side Effects
Definition
CNS: headache

skin: rash

GI: dyspepsia, cramps, flatulence, constipation, abdominal pain
Term
HMG-CoA Reductase Inhibitor Adverse Effects
Definition
hepatotoxicity: liver function tests every six months while on treatment

myopathy: rhabdomyolisis (mostly with rosuvastatin)

peripheral neuropathy: linkage to muscle weakness and tingling in hands and feet (reversible with stopping treatment)

link to parkinson's disease: being studied, no direct linkage proven yet
Term
HMG-CoA Reductase Inhibitor Drug Interactions
Definition
most other lipid-lowering drugs (except bile acid sequestrants)

drugs that inhibit CYP3A4 (macrolid antibiotics, azole antifungal drugs, HIV protease inhibitors, amiodarone, cyclosporine, grapefruit juice) increase levels of statins

pregnancy category x

dosing should be once daily in the evening (endogenous cholesterol synthesis increases during the night)
Term
Category: Antilipemic
Definition
classification: nicotinic acid (vitamin B3)

prototypes: nicotinic acid (Niacin), nia-bid, niaspan, slo-niacin

route: po
onset of action: rapid
peak: 30-60 min
half-life: 45 min
duration: unknown

hint: look for nia
Term
Nicotinic Acid Indications
Definition
hyperlipidemia
hypertriglyceridemia
Term
Nicotinic Acid Mechanism of Action
Definition
inhibit lipolysis in adipose tissue

increase activity of lipoprotein lipase

decrease esterification of triglycerides (conversion of triglycerides in liver to storage form)

lower LDLs and higher HDLs by lower metabolism of cholesterol and triglycerides
Term
Nicotinic Acid Adverse Effects
Definition
skin: flushing, itching (intense flushing initially can be pretreated with aspirin; also decreased with SR version of niacin)

GI: abdominal discomfort

hepatotxicity: most likely with slo-niacin/less likely with niaspan

hyperglycemia: occurs most commonly in patients with DM

gouty arthritis: competes for renal excretion with uric acid leading to increased levels of uric acid

can raise blood levels of homocysteine

may increase risk for CHD
Term
Category: Antilipemic
Definition
classification: bile acid sequestrants

prototypes: cholestyramine (Questram), colestipol (Colestid), colesevelam (Welchol) (newer drug tablet form only, used before Questram and Colestid, used if intolerant to statins)

route: po
onset of action: unknown
peak: unknown
half-life: unknown
duration: unknown

hint: look for cole
Term
Bile Acid Sequestrants Indications
Definition
hyperlipidemia
hyperglycemia in patients with DM
Term
Bile Acid Sequestrants Mechanism of Action
Definition
bind bile preventing resorption of bile acids from small intestine to lower LDLs (bile acids necessary for the absorption of cholesterol in the small intestine)

increase LDL receptors on hepatocytes
Term
Bile Acid Sequestrants Side Effects
Definition
GI: heartburn, nausea, belching, bloating, constipation
Term
Bile Acid Sequestrants Adverse Effects
Definition
bleeding, headaches, tinnitus, burnt odor to urine
Term
Category: Antilipemic
Definition
classification: cholesterol absorption inhibitor

prototype: ezetimibe (Zetia)

route: po
onset of action: unknown
peak: 4-12 hours
half-life: 22 hours
duration: unknown
Term
Cholesterol Absorption Inhibitor Indications
Definition
hyperglycemia: approved for monotherapy and combined use with statins (slightly increases risk for liver damage)
Term
Cholesterol Absorption Inhibitor Mechanism of Action
Definition
selectively inhibits absorption of cholesterol and other sterols from the small intestine, resulting in lower total cholesterol, LDL, alipoprotein B, and triglycerides
Term
Ezetimibe (Zetia) Adverse Effects
Definition
myopathy
rhabdomyolysis
hepatitis
pancreatitis
thrombocytopenia
Term
Ezetimibe (Zetia) Drug Interactions
Definition
statins
fibrates
bile-acid sequestrants
cyclosporine
Term
Category: Antilipemic
Definition
classification: fibric acid derivates (fibrates)

prototypes: gemfibrozil (Lopid), fenofibrate (Tricor), fenofibric acid (TriLipix)

route: po
onset of action: several days
peak: 1-2 hours
half-life: 1.3-1.5 hours
duration: unknown

hint: look for fibr
Term
Fibric Acid Derivative Indications
Definition
hypertriglyceridemia
Term
Fibric Acid Derivative Mechanism of Action
Definition
activate lipoprotein lipase which is responsible for breakdown of cholesterol

also suppress release of fatty acids from adipose tissue

inhibit triglyceride production in liver

increase secretion of cholesterol into bile for excretion
Term
Fibric Acid Derivative Acverse Effects
Definition
rash, GI disturbances, gallstones, myopathy, liver injury (hepatotoxic)
Term
Fibric Acid Derivative Interactions
Definition
displaces warfarin from plasma albumin

measure INR frequently
Term
Category: Antianginal
Definition
classification: nitrates

prototypes: nitroglycerin (Nitro-bid, Nitrol), isosorbide dinitrate (Isordil, Sorbitrate, Dilatrate SR), isosorbide mononitrate (Imdur, Monokate, ISMO)

hint: look for bide and nitrate
Term
Nitrates Pharmacokinetics (nitroglycerin)
Definition
route: sublingual
onset of action: 2-3 min
peak: unknown
half-life: 1-4 min
duration: 0.5-1 hour
Term
Available Forms of Nitrates
Definition
sublingual
buccal
chewable tablets
oral capsules/tablets
IV solutions
ointments
transdermal patches
translingual sprays
Term
Nitrates Indications
Definition
treat stable, unstable, and vasospastic angina
prevent angina attacks
Term
Nitrate Mechanism of Action
Definition
dilate all blood vessels:
dilation of coronaries --> redistribution of oxygenated blood flow to ischemic areas
dilation of veins --> reduction in venous return --> decreased left ventricular end diastolic pressure --> decreased preload

dose dependent arterial vasodilator effect
Term
Nitrate Side Effects
Definition
CNS: headache (usually diminishes over time)

CV: tachycardia, postural hypotension

blood: methemoglobin

skin: rash

other: tolerance may develop
Term
Nitrate Drug Interactions
Definition
hypotensive drugs
phosphodiesterase type 5 inhibitors
beta blockers, verapamil, and diltiazem
Term
Ranolazine
Definition
belongs to the first new class of antianginal agents approved in more than 25 years

benefits modest and greater in men that women

does not reduce heart rate, blood pressure, or vascular resistance

can prolong QT; multiple drug interactions

not a first line drug therapy (combine with first-line agents for inadequate response to other first-line medications)
Term
Category: Inotropic
Definition
classification: phosphodiesterase inhibitors (PDI)

prototypes: inamrinone (Inodilator), milrinone (Primacor)

route: IV
onset of action:5-15 minutes
peak: immediately
half-life: 2-3 hours
duration: 8-10 hours
Term
PDI Indications
Definition
short term management of heart failure
Term
PDI Mechanism of Action
Definition
inhibit action of phosphodiesterase = increase in intracellular cAMP specifically in the cardiac muscle --> positive inotropic affect and vasodilation

increased Ca+ available for cardiac contraction = greater force of contraction

may increase heart rate = positive chronotropic response
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