Pharmacology Exam 1

Front 1

origin of the word "pharmacology"

Back 1

"pharmacon" = Greek for drugs or medicine
"logia" = Latin for knowledge and its study

Front 2

Pharmacodynamics

Back 2

actions of a drug on the body

Front 3

Pharmacokinetics

Back 3

actions of the body on the drug

Front 4

toxicology

Back 4

study of undesirable effects of chemical agents on living things

Front 5

pharmacogenetics

Back 5

study of relationship of genetic factors to variations in drug response

Front 6

Pharmacognosy

Back 6

recognition of natural compounds with pharmacologic activity in plants

Front 7

aqueous vs. lipid solubility

Back 7

aqueous solubility of a drug is often a function of the electrostatic charge; lipid solubility is inversely proportional to its charge

Front 8

weak acid vs. weak base

Back 8

when protonated, a weak base is polar and therefore more water-soluble; when protonated, a weak acid is less polar and less water-soluble

Front 9

Henderson-Hasselbalch equation

Back 9

used for determining how to accelerate the excretion of a drug from the body (ex: overdose)

Front 10

intrathecal administration

Back 10

direct injection into intrathecal space (spinal canal); for drugs that cannot cross the BBB

Front 11

topical vs. transdermal administration

Back 11

topical - local effect; slowest of all routes
transdermal - systemic effect; also slow

Front 12

the five major lipoprotein classes

Back 12

chylomicrons, LDL, VLDL, HDL, Lp(a)

Front 13

Antihyperlipedemic agents

Back 13

Nicotinic acid
Bile acid sequestering resins - Cholestyramine, Colesevelam, Colestipol
HMG CoA reductase inhibitors
Fibric acid derivatives
Cholesterol absorption inhibitors
Alli

Front 14

Nicotinic acid

Back 14

reduces LDL, VLDL, TG's;
raises HDL by unknown mechanism;
greater response in women than in men;
niacin flush, concurrent pruritus, headaches, pain

Front 15

Bile acid sequestering resins (BASR'S)

Back 15

not absorbed systemically;
interfere with reuptake of bile acids, stimulating cholesterol synthesis; does not raise plasma cholesterol levels b/c new cholesterol is shunted to bile-acid synthesis pathway; hepatocytes increase uptake of LDL

Front 16

Cholestyramine (Questran) and Coelstipol (Cholestid)

Back 16

BASR's - salts of basic anion exchange resins; can reduce bioavailability of other drugs

Front 17

Colesevelam (WelChol)

Back 17

BASR; oral; reduces LDL; less potential for reducing bioavailability than Cholestyramine and Colestipol

Front 18

HMG CoA reductase inhibitors

Back 18

end in "statin"
inhibits cholesterol formation in hepatocyte; hepatocytes increase uptake of LDL;

Front 19

adverse effects of HMG CoA reductase inhibitors

Back 19

toxicity to skeletal muscles, rhabdomyolysis, inflammation of hepatocy, increase in plasma transaminases (SGOT, SGPT), elevation of muscle and liver enzymes
Absolute C.I. = Pregancy

Front 20

Fibric acid derivatives

Back 20

reduce serum TG levels; name contains "fibr"

Front 21

Gemfibrozil (Lopid)

Back 21

a fibric acid derivative;
inhibits peripheral lipolysis, decreasing hepatic production of TGs;
inhibits synthesis and increases clearance of apoB, a carrier for VLDL;
structurally related to Clofibrate but more effective

Front 22

Clofibrate (Atromid-S)

Back 22

reduces synthesis of VLDL,
less effective than Gemfibrozil;
INCREASES MORTALITY - NON CARDIOVASCULAR CAUSES

Front 23

Fenofibrate (Tricor, Lofibra)

Back 23

activates peroxisome proliferator activated receptors, which alter transcription of genes for lipoprotein metabolism;
induces lipoprotein lipase, decreases production of apoCIII;
not safe during pregancy

Front 24

Ezetimibe (Zetia)

Back 24

cholesterol absorption inhibitor;
increases HDL;
adverse effects similar to statin monotherapy;
can be used in combo with statins
act at brush border of small intestine

Front 25

Anticoagulants

Back 25

Heparin, Enoxaparin, Tinzaparin (DVT), Fondaparinux, Pentosan, Antithrombin III, Warfarin (oral), Lepirudin, Argatroban, Bivalirudin

Front 26

Platelet inhibitors

Back 26

Aspirin, Dipyridamole, Ticlopidine, Abciximab, Eptifibatide, Tirofiban, Clopidogrel, Cilostazol

Front 27

Thrombolytic agents

Back 27

tPA (Alteplase), Anistreplase, Streptokinase, Urokinase, Tenecteplase (TNK-tPA)

Front 28

Heparin

Back 28

present in mammalian tissues, esp. mast cell granules;
activates the neutralizing activity of antithrombin III, which neutralizes the activated forms of clotting factors;

Front 29

Administration of heparin

Back 29

must be administered parenterally; sufficient amount administered to prolong the PTT to twice normal

Front 30

Reversal of heparin action

Back 30

using protamine sulfate; isolated from fish sperm; for immediate reversal of anticoagulation

Front 31

thrombocytopenia

Back 31

below normal count of platelets; side effect of heparin use (heparin induced thrombocytopenia (HIT))

Front 32

Lepirudin (Refludan)

Back 32

recombinant form of hirudin (natural anticoagulant); safe to use in patients with HIT

Front 33

Argatroban (Acova)

Back 33

intravenous thrombin inhibitor; safe to use in patients with HIT;
eliminated by liver (unlike Lepirudin) and can therefore be used in patients with end-stage renal disease

Front 34

Bivalirudin (Angiomax)

Back 34

analog of hirudin;
treatment for unstable angina and acute MI;
substitute for heparin in patients with a history of HIT undergoing angioplasty

Front 35

Ancrod (Viprinex)

Back 35

from venom of Malayan pit viper; being investigated as alternative to heparin for patients with HIT

Front 36

Danaparoid

Back 36

LMWH; used in management of HIT

Front 37

Low Molecular Weight Heparins (LMWH)

Back 37

Enoxaparin, Dalteparin, Danaproid, Tinzaparin, Fondaparinux

Front 38

characteristics of LMWH's

Back 38

prevent deep venous thrombosis (DVT);
inhibit factor X;
less effect on antithrombin III than heparin does;
more predictable anticoagulant response, better bioavailability

Front 39

Fondaparinux (Arixtra)

Back 39

LMWH; prevention of DVT and pulmonary embolism; inhibits targeted step in coag cascade (factor Xa); does not inhibit thrombin (IIa)

Front 40

Pentosan (Elmiron)

Back 40

weak anticoagulant derived from plants (rather than animal source like heparin); used for relief of pain from interstitial cystitis

Front 41

Warfarin (Coumadin)

Back 41

vitamin K antagonist; indirect anticoagulant b/c it does not affect coagulation in vitro; affects mostly factor VII; prolongs PT by 1.5 to 2.5 times normal

Front 42

reversal of Warfarin action

Back 42

vitamin K administration (slow); transfusion with fresh frozen plasma (immediate), but has risk of viral hepatitis

Front 43

Aspirin

Back 43

irreversibly inhibits COX, inhibiting synthesis of PG's and TXA2, preventing platelet aggregation; rapid effect

Front 44

Ticlopidine (Ticlid)

Back 44

inhibits ADP pathway involved in platelets binding to fibrinogen and each other;
prevents thrombolytic stroke and transient ischemic attacks

Front 45

Dipyridamole (Persantine)

Back 45

used to prevent angina; coronary vasodilator; used in combo with aspirin as well as warfarin; inhibits phosphodiesterase, keeping cAMP levels high, which inhibits TXA2 synthesis

Front 46

Abciximab (Reopro)

Back 46

monoclonal against platelet IIb/IIIa receptors - prevents fibrin binding;
reduces actue MI when used with heparin more than heparin alone

Front 47

Eptifibatide (integrilin) and Tirofiban (Aggrastat)

Back 47

like Abciximab, but shorter half-life

Front 48

Clopidogrel (Plavix)

Back 48

analogue of Ticlopidine; blocks ADP pathway (fibrin binding)

Front 49

Cilostazol (Pletal)

Back 49

vasodilatory platelet aggregation inhibitor;inhibits aggregation caused by ADP, arachadonic acid, collagen, EPI, thrombin, stress; inhibits phosphodiesterase type III, which prevents degradation of cAMP in platelets and vascular tissue

Front 50

Alteplase, tPA, TPA (Activase), Reteplase (Retavase, r-PA)

Back 50

converts plasminogen to plasmin; tissue plasminogen activator (tPA) binds fibrin on clot surface; fibrinogen binds tPA-fibrin complex and activates plasminogen; expensive, intravenous

Front 51

Streptokinase (Kabikinase, Streptase)

Back 51

indirectly activates plasminogen by complexing with it; this increases protease activity that converts it to plasmin; not specific to clot-bound fibrin; less expensive

Front 52

Anistreplase

Back 52

Streptokinase + recombinant human plasminogen, improves kinetics; expensive

Front 53

Urokinase, Saruplase

Back 53

single chain serine protease that directly degrades fibrin and fibrinogen

Front 54

Tenecteplase (TNK-tPA, TNKase)

Back 54

administered for treatment of acute MI;
modified form of tPA; longer half life than Alteplase

Front 55

Garlic and ginger

Back 55

inhibit thromboxane synthesis

Front 56

Re-entry phenomenon

Back 56

when a pathway for the spread of electrical impulse from the pacemaker is blocked, re-entry causes the re-excitation of ventricular muscle; most common cause of arrhythmia

Front 57

Class I anti-arrhythmic drugs

Back 57

same mechanism as local anesthetics - block Na+ channels

Front 58

Quinidine

Back 58

Class IA;
toxic potential, now being replaced by verapamil;
binds to open Na+ channel, preventing Na+ entry;
Adverse: can cause AV or SA block, can cause ventricular tachycardia

Front 59

Procainamide

Back 59

Class IA;
mechanism similar to quinidine;
adverse: causes lupus-like syndrome, CNS side effects (psychosis)

Front 60

Disopyramide

Back 60

Class IA;
similar action to quinidine;
can cause negative inotropic effect and peripheral vasoconstriction; reduces contractility in patients with left ventricular dysfunction; anticholinergic effects

Front 61

Mexiletine and Tocainide

Back 61

Class IB; similar action as Lidocaine;
may cause cardiovascular depression and allergies;
Mexiletine used for life-threatening ventricular arrhythmias; Tocainide can cause agranulocytosis and other fatal hematological effects

Front 62

Flecainide (Tambocor)

Back 62

Class IC;
slowly dissociates from Na channels;
diminishes phase 0 upstroke in Purkinje and myocardial fibers; slows conduction but low effects on duration of AP or refraction;
used only in refractory tachycardia (not fibrillation)

Front 63

Class II anti-arrhythmic drugs

Back 63

beta-blockers;
diminish phase IV depolarization

Front 64

Esmolol (Brevibloc)

Back 64

short-acting Class II;
used in emergency situations; selective for beta 1 receptor;
administered via continuous IV infusion

Front 65

Propranolol and Metoprolol

Back 65

prophylactics for patients who had MI to prevent arrhythmia;
adverse: depression of cardiac output

Front 66

Class III anti-arrhythmic drugs

Back 66

Amiodarone, Ibutilide, Dofetilide, Bretylium, Sotalol

Front 67

action of Class III drugs

Back 67

reduce outward K current during repolarization; prolog duration of AP without changing phase 0 of depol. or resting potential;
prolong effective refractory period;
can induce arrhythmias

Front 68

Ibutilide (Corvert)

Back 68

slows repolarization, prolongs AP;
promotes influx of Na thru slow Na channels;
recommended for atrial flutter and fibrillation;
prior to this, cardioversion was used for rapid conversion of flutter/fibrillation to normal rhythm; ONLY AGENT INDICATED FOR RAPID CONVERSION OF ATRIAL ARRHYTHMIAS

Front 69

Dofetilide (Tikosyn)

Back 69

Class III K channel blocker;
reserved for highly symptomatic patients - conversion and maintenance of normal rhythm from flutter/fibrillation;
more potent than Sotalol

Front 70

Sotalol (Betapace)

Back 70

beta-blocker with class II and class III properties;
used in trt of atrial arrhythmias or life-threatening ventricular arrhythmias;
can be pro-arrhythmic so should not be used in mild cases

Front 71

Bretylium (Bretylol)

Back 71

K channel blocker; raises voltage necessary to induce ventricular fibrillation;
high incidence of adverse effects - not first-line trt

Front 72

Amiodarone (Cordarone, Pacerone)

Back 72

used primarily instead of Bretylium; K channel blocker; antianginal as well as antiarrhythmic;
has weak Class I action; has Class II action;
alpha and beta blocker;
adverse - blue skin (b/c of iodine)

Front 73

Class IV drugs

Back 73

Ca channel blockers
Verapamil
Diltiazem
Bepridil

Front 74

Verapamil (Calan, Isoptin) and Diltiazem (Cardizem, Dilacor)

Back 74

useful in angina, hypertension, and supraventricular tachyarrhythmias;
more effective than digoxin;

Front 75

Bepridil (Vascor)

Back 75

labeled for angina, not arrhythmias, but has Class I activity (blocks fast Na channels)

Front 76

Nifedipine and dihydropyridines

Back 76

peripheral Ca channel blockers - not effective for cardiac arrhythmias b/c they decrease arterial pressure

Front 77

Adenosine (Adenocard)

Back 77

used in management of re-entrant paroxysmal supraventricular tachycardias (assoc with Wolff-Parkinson-White syndrome);
good substitute for verapamil b/c effects are transient;
causes K to flow out, hyperpolarizing the atrial tissues, reducing duration of AP, does not affect upstroke

Front 78

Digoxin

Back 78

used to manage ventricular effects in atrial fibrillation and flutter; shortens refractory period; diminishes conduction velocity in Purkinje fibers

Front 79

toxic levels of Digoxin

Back 79

cause ectopic ventricular beats resulting in ventricular tachycardia and fibrillation; treated by lidocaine

Front 80

Antianginal agents

Back 80

Organic Nitrates
Beta-1 receptor blockers
Ca channel blockers
Antithrombotic and Antiplatelet agents
FA oxidation inhibitors

Front 81

Classic angina

Back 81

aka typical, exertional or atherosclerotic;
obstruction of large coronary arteries; caused by exercise, exertion, emotion, eating

Front 82

Variant angina

Back 82

occurs at rest, during sleep sometimes;
coronary artery spasm reduces blood flow

Front 83

Mixed angina

Back 83

combo of typical and variant;
pain at rest as well as during exercise; myocardial oxygen demand as well as spasm induced reduction of blood flow in coronary artery

Front 84

Unstable angina

Back 84

can be deadly;
pre-infarction syndrome - high propensity of accelerating to MI

Front 85

Silent angina

Back 85

ischemia without symptoms

Front 86

Organic Nitrates (examples)

Back 86

Amyl Nitrate
Nitroglycerin
Isosorbide dinitrate
Isosorbide-5-mononitrate
Erythrityl tetranitrate
Pentaerythritol

Front 87

Organic Nitrates - mechanism

Back 87

relax vascular s.m. by converting to NO, which activates guanylate cyclase, producing cGMP, causing dephosphorylation of myosin light chain

Front 88

Organic Nitrates - effect on myocardial oxygen requirements

Back 88

reduce oxygen demand by decreasing venous return to heart

Front 89

organic nitrates - tolerance

Back 89

tolerance develops rapidly; must have "nitrate-free interval" to overcome

Front 90

Amyl nitrate

Back 90

administration: inhalation;
vasodilatory; useful in the case of CN poisoning;
rarely used for angina b/c it is expensive, causes headaches and tachycardia;
street names: "Amy" and "poppers"

Front 91

Isosorbide dinitrate (ISDN)

Back 91

long-acting oral organic nitrate; can also be used to treat CHF;
administered orally - low bioavailability (22%); sublingually - 60%; sustained-release - 75%

Front 92

Beta-adrenergic blocking agents - actions

Back 92

suppress activation of the heart; NOT USEFUL IN VASOSPASTIC (VARIANT/MIXED) ANGINA;
also reduce BP (antihypertensive);
reduce myocardial oxygen consumption

Front 93

Beta-blockers - examples

Back 93

Non-selective:
Propranolol, Timolol, Nadolol, Pindolol

Selective for beta 1
Bisoprolol, Atenolol, Metoprolol

Front 94

Pindolol (Visken)

Back 94

oral;
intrinsic sympathomimetic activity (ISA)
VASODILATORY BETA-BLOCKER - partial agonist for beta-2

Front 95

Beta-blockers, mechanism

Back 95

beta1 blockage causes fall in cardiac output; beta 2 blockage counters this by increasing vascular resistance; non-selective blockers produce more modest decrease in BP than do selective beta1 antagonists

Front 96

Propranolol

Back 96

nonselective beta blocker;
can block beta 2 receptors in bronchial muscle, inducing bronchospasm;
has negative chronotropic effect that decreases HR and a negative inotropic effect that decreases cardiac output

Front 97

Verapamil

Back 97

for angina, hypertension, supraventricular tachyarrhythmias; class IV antiarrhythmic - more effective than digoxin;
least selective of the Ca blockers; decreases HR and oxygen demand; vasodilatory effect on vascular s.m.;
crosses placenta; constipation

Front 98

Diltiazem (Cardizem, Dilacor, Diltia)

Back 98

used for variant angina, stable and unstable angina, hypertension, supraventricular tachycardia, control of ventricular rate in atrial fibrillation and flutter; less pronounced cardiac effect than Verapamil

Front 99

Nifedipine (Adalat, Procardia, Afeditab, Nifedical)

Back 99

a dihydropyridine; higher affinity for vascular Ca channels than cardiac Ca channels; vasodilators with minimal effect on cardiac conduction; but useful for variant angina;
more prominent vasodilatory effects than Diltiazem and Verapamil; short half-life

Front 100

Nifedipine - adverse effects

Back 100

peripheral edema; flushing, weakness, headache, syncope, hypotention, lightheadedness

Front 101

Antiplatelet and Antithrombotic agents

Back 101

Aspirin - reduces mortality in case of unstable or chronic stable angina;
irreversible COX inhibitor
Heparin, Warfarin

Front 102

Ranolazine (Ranexa)

Back 102

Partial fatty acid oxidation (PFox) inhibitor; shifts heart metabolism from FA oxid. to glycolysis which uses less oxygen, reducing myocardial demand

Front 103

Drugs used in Heart Failure

Back 103

Inotropic agents
Diuretics
Vasodilators
Ca channel antagonists
Beta adrenergic receptor antagonists

Front 104

Congestive Heart Failure (CHF)

Back 104

heart is unable to pump blood at a volume adequate to meet the metabolic needs of the organs

Front 105

treating CHF

Back 105

increase cardiac output, reduce blood volume, reduce afterload

Front 106

physiological responses to CHF

Back 106

increased adrenergic activity - greater HR, force of contraction, vasoconstriction;
retention of fluids - release of renin, angiotensin II, and aldosterone;
hypertrophy of cardiac muscle
ALL FURTHER HEART FAILURE

Front 107

Cardiac glycosides

Back 107

inotropic agents; ex: Digoxin;
enhance cardiac muscle contractility, increase CO;
LOW THERAPEUTIC INDEX (toxic/effective dose)

Front 108

Cardiac glycosides - mechanism

Back 108

inhibit Na/K ATPase, leading to increase of Na in cardiac cells; Na/Ca exchanger brings Ca in, increasing cardiac force;
Ca is released from SR -- sustained contraction

Front 109

renal function and Digoxin

Back 109

in the aged, digoxin tolerance and exretion are compromised due to diminished renal clearance, reduction in lean body mass

Front 110

Electrolyte effect on uptake of Digoxin

Back 110

Hyperkalemia reduces myocardial concentration of digoxin; Hypokalemia increases it

Front 111

drugs that increase Digoxin concentration in plasma

Back 111

Quinidine - competes for excretion;
Verapamil, Amiodarone, K-sparing diuretics, corticosteroids

Front 112

Digoxin toxicity

Back 112

ectopic beats, first degree AV block;
antidote - antidigoxin immunotherapy

Front 113

Digoxin gems

Back 113

increases left ventricular ejection fraction; now replaced by ACE inhibitors as first-line therapy for CHF due to systolic dysfunction

Front 114

Digoxin vs. Verapamil/Diltiazem

Back 114

Verapamil and Diltiazem more effective for controlling ventricular rate during atrial fibrillation or flutter

Front 115

Digoxin vs. Ca channel blockers

Back 115

Ca antagonists preferred for trt of supraventricular arrhythmias due to re-entry

Front 116

Beta-AGONISTS

Back 116

positive inotropic effects; vasodilation;
Dobutamine and Dopamine

Front 117

Dobutamine

Back 117

beta-agonist; inotropic agent
increases cAMP levels, which leads to phosphorylation of Ca channels, increasing myocardial Ca entry and contraction

Front 118

Dopamine vs. Dobutamine

Back 118

Dobutamine does not affect dopaminergic receptors; Dboutamine is primarily selective for beta-1, but also has some beta-2 and alpha-1 agonist properties; Dobutamine is synthetic

Front 119

Phsophodiesterase inhibitors - examples

Back 119

Milrinone (Primacor) and Inamrinone (Inocor)

Front 120

Milrinone (Primacor)

Back 120

PDE inhibitor - increases intracell cAMP levels -- increased contractility; may not be beneficial to CHF; may cause arrhythmia -- used only for acute heart failure

Front 121

Inamrinone (Inocor)

Back 121

formerly Amrinone;
inotropic and vasodilatory effects;
IV admin;
short-term management of CHF;
can increase morbidity/mortality

Front 122

Vasodilators

Back 122

Nitroprusside, nitroglycerin, hydralazine, isosorbide dinitrate

Front 123

Vasodilators - action

Back 123

used in sever CHF;
decreases preload (volume of blood that fills in diastole) and afterload (pressure that must be overcome for heart to pump into arteries)

Front 124

Hydralazine

Back 124

vasodilator
drug of choice in pateitns with fatigue and low left ventricular output;

Front 125

ACE inhibitors

Back 125

also vasodilators, but more effective than others;
agents of choice in CHF;
ex: Captopril, Enalapril, Benazepril, Lisinopril;
can be used in combo with diuretics; fetotoxic

Front 126

ARB's - Valsartan

Back 126

mainly used for hypertension;
angiotensin II antagonist, blocks AT1 receptor (selectively);
can treat CHF in patients who are intolerant to ACE inhibitors;
reduces left ventricular hypertrophy

Front 127

Smooth muscle relaxants

Back 127

nitrates; for patients who are intolerant to ACE inhibitors

Front 128

Diuretics

Back 128

relieve pulmonary congestion and peripheral edema;
decrease plasma volume and therefore venous return (preload); K-sparing diuretics need to be monitored if patient is taking ACE inhibitors

Front 129

Beta blockers

Back 129

Bisoprolol, Carvedilol, Metoprolol, Atenolol

Front 130

Carvedilol

Back 130

alpha- and nonselective beta-blocker; affects beta receptors more; antioxidant as well

Front 131

Labetalol (Normodyne, Trandate)

Back 131

affect alpha-1 receptors more than beta; management of hypertension;
a vasodilatory beta blocker

Front 132

beta blocker mechanism

Back 132

attenuation of adverse effects of catecholamines, upregulation of beta receptors, decreased heart rate, reduced remodeling

Front 133

Nesiritide (BNP, Natricor)

Back 133

IV preparation of human B-type natriuretic peptide - produced in ventricles of heart;
produces balanced arterial and venous dilation;
acute trt of decompensated CHF;
more potent and longer-lasting than ANP