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Pharmacology > Pharm block 2 > Flashcards

Pharm block 2 Flashcards

1
Q

classes of diuretics

A

carbonic anhydrase inhibitors (acetazolamide); osmotic diuretics (mannitol); loop diuretics (furosemide - K+-wasting); thiazides (hydrochlorothiazide - K+-wasting); K+-sparing diuretics (triamterene/amiloride; spironolactone); natriuretic peptides (nesiritide)

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2
Q

carbonic anhydrase inhibitor drugs

A

acetazolamide; related: dorzolamide (topical, eye)

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3
Q

carbonic anhydrase inhibitors pk

A

oral, iv; excreted via proximal tubule

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4
Q

carbonic anhydrase inhibitors renal pd

A

indirectly blocks bicarb reabsorption; alkalinisation of urine; metabolic acidosis; inc K+ secretion downstream; inc NaCl reabsorption (-> tachyphylaxis)

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5
Q

carbonic anhydrase inhibitors intra-ocular pd

A

block NaHCO3 secretion; dec aqueous humor formation

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6
Q

carbonic anhydrase inhibitors choroid plexus pd

A

dec rate of cerebrospinal fluid formation

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7
Q

carbonic anhydrase inhibitors uses

A

glaucoma - topical dorzolamide, systemic acetazolamide in emergencies; urinary alkalinisation - inc excretion of weak acids (uric acid, cysteine, aspirin) (theoretical); mountain sickness - choroid (cerebral edema, respiratory alkalosis)

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8
Q

carbonic anhydrase inhibitors adverse effects

A

metabolic acidosis; kidney stones; renal K+-loss; CNS toxicity (drowsiness, paresthesias)

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9
Q

carbonic anhydrase inhibitors contraindications

A

hepatic cirrhosis (reversal of NH4+ -> trapping acidic urine by alkalinisation) - NH4+ -> hepatic encephalopathy

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10
Q

mannitol characteristics

A

non-absorbable, non-metabolizable sugar

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11
Q

mannitol pk

A

MUST be IV; excreted via glomerular filtration

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12
Q

mannitol pd

A

retains h2o in tubule; some inc in natriuresis

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13
Q

mannitol uses

A

water diuresis (when preferred to Na excretion); maintain tubular flow (non-responders -> test dose); reduce intra-cranial/-ocular pressure

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14
Q

mannitol adverse effects

A

EC volume expansion (-> CHF, pulmonary edema); dehydration, hypernatremia

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15
Q

loop diuretics

A

FUROSEMIDE; bumetanide; torsemide; ethacrynic acid

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16
Q

loop diuretics pk

A

oral, iv, instant onset

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17
Q

loop diuretics pd

A

inhibit Na/K/Cl symporter in thick ascending limb -> directly affects blood flow

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18
Q

furosemide uses

A

EMERGENCIES; edematous conditions (acute pulmonary edema, acute CHF); acute hypercalcemia/hyperkalemia; acute renal failure - adjust oliguria, inc K secretion (flushing tubules -> non-oliguric renal failure); anion overdose (combine w/saline - bromide, fluoride, iodide); forced diuresis; (hypertension, CHF - second line for refractory cases; short-term)

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19
Q

furosemide adverse effects

A

HYPOKALEMIA; hypokalemic metabolic alkalosis; ototoxicity; hyperuricemia (->gouty attack); hypomagnesaemia; allergic rxns (sulfonamide moiety)

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20
Q

furosemide contraindications

A

other ototoxic drugs (aminoglycoside antibiotics)

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21
Q

thiazide diuretics - hydrochlorothiazide pd

A

inhibition of NaCl symporter in distal convoluted tubule; UNLIKE LOOP diuretics -> inc Ca reabsorption

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22
Q

hydrochlorothiazide pk

A

usually oral

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23
Q

hydrochlorothiazide adverse effects

A

similar to loop diuretics (less pronounced); hypokalemia, hypokalemic metabolic acidosis; hyperuricemia; hypernatriuria; impaired carb tolerance, hyperlipidemia; allergic rxns

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24
Q

hydrochlorothiazide uses

A

hypertension - inexpensive, proven, effective, safe, one daily dose, no dose titration needed; congestive heart failure; nephrolithiasis from IDIOPATHIC HYPERCALCIURIA (normal serum Ca!) - intestinal Ca-hyperabsorbers, renal ca/PO4 leakers; nephrogenic diabetes insipidus

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25
Q

metolazone pk

A

oral (65% bioavail)

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26
Q

metolazone pd

A

similar to thiazide diuretics; also effective when GFR<30ml/min;

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27
Q

metolazone uses

A

hypertension; edema; use instead of other thiazides in combo treatment of FUROSEMIDE RESISTANCE

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28
Q

K+-sparing diuretics - triamterene, amiloride pk

A

triamterene - hepatic metabolism, renal excretion; amiloride - renal excretion

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29
Q

triamterene, amiloride pd

A

mild inc in NaCl excretion via effects in late distal tubule/collecting duct

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30
Q

triamterene, amiloride adverse effects

A

HYPERKALEMIA (muscle weakness, fatigue, arrhythmia) esp in combo w/ACE inhibitors; metabolic acidosis; triamterene - acute renal failure (w/indomethacin), kidney stones

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31
Q

K+-sparing diuretics - spironolactone pk

A

prodrug of canreonate - IV

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32
Q

spironolactone pd

A

aldosterone antagonist -> delayed effect; mild inc in NaCl excretion in the late distal tubule, collecting duct

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33
Q

spironolactone adverse effects

A

HYPERKALEMIA esp. in combo w/ACE inhibitors; metabolic acidosis; gynecomastia

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34
Q

natriuretic peptide - nesiritide characteristics

A

B-type; in cardiac ventricles, released in response to myocardial distenstion; drug from E. coli; counterregulation of RAAS

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35
Q

nesiritide pk

A

IV peptide drug

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36
Q

nesiritide pd

A

activate guanylyl cyclase -> vascular smooth muscle relaxation; interlinked antagonisms for renin, ATII, aldosterone, ADH - inc GFR, dec Na reabsorption

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37
Q

nesiritide uses

A

acute severe heart failure

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38
Q

five classes of antihypertensive drugs

A

diuretics, beta-andrenoceptor antagonists (beta-blockers), Ca-channel blockers, angiotensin inhibitors (ACE inhibitors, AT1 blockers), alpha-adrenergic blockers

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39
Q

centrally-acting antihypertensive drugs

A

clonidine, methyldopa, reserpine

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40
Q

vasodilators

A

nitrates, nitroprusside, dihydralazine

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41
Q

classification of blood pressure for adults

A

normal =160/>=100

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42
Q

(reserpine) characteristics

A

rauwolfia alkaloid; obsolete but good model drug

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43
Q

(reserpine) pk

A

oral; effects persist for up to 6 weeks (intolerable)

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44
Q

(reserpine) pd

A

depletes biogenic amines from neuronal vesicles by inhibition of reuptake, CNS/periphery

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45
Q

(reserpine) uses

A

none

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46
Q

(reserpine) adverse effects

A

denervation of sympathetic system -> parasympathetic system prevails; nasal congestion, hypersecretion (bad for asthmatics); bronchoconstriction; mental depression (suicidal thoughts); parkinsonism; ulcerogenic

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47
Q

clonidine characteristics

A

alpha2 sympathomimetic drug; 2nd choice for treating hypertension; interesting off-label uses

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48
Q

clonidine pk

A

oral, iv, transdermal patch

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49
Q

clonidine pd

A

centrally mediated hypotensive effects - alpha2 agonist -> dec CO, relax capacitance of vessels, dec peripheral resistance -> renal blood flow maintained; may have initial hypertensive episode; pronounced rebound after prolonged use

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50
Q

clonidine uses

A

2nd line treatment of hypertension

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51
Q

clonidine adverse effects

A

high doses -> bradycardia, AV-block, fxn’l cardiac failure, dry mouth, drowsiness, sedation, constipation

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52
Q

clonidine other clinical uses

A

symptomatic treatment of w/drawal syndromes (heroin, alcohol, benzodiazepines); prevent/treat alcoholic delirium; postmenopausal syndrome; refractory diarrhea (short bowel syndrome); adjunct in analgo-sedation (->dexmedetomidine)

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53
Q

methyldopa characteristics

A

centrally acting antihypertensive safe in PREGNANCY

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54
Q

methyldopa pk

A

oral

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55
Q

methyldopa pd

A

centrally mediated hypotensive effects comparable, not identical, to clonidine

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56
Q

methyldopa adverse effects

A

mostly like clonidine; Coombs test may turn positive

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57
Q

alpha1-blockers

A

prazosin, terazosin, doxazosin

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58
Q

prazosin, terazosin, doxazosin pk

A

oral, iv

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59
Q

prazosin, terazosin, doxazosin pd

A

blockade of alpha1-receptors in arterioles/venules; no effect on inhibitory feedback for NE release (selective for alpha1)

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60
Q

prazosin, terazosin, doxazosin adverse effects

A

first dose phenomenon (hypotension, syncope) -> give initial dose at bedtime; orthostatic hypotension; tests for antinuclear factor (ANF) may turn positive (reflex tachy)

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61
Q

choice of diuretic drug in hypertension

A

CHOICE: thiazides (hydrochlorothiazide); 2nd line: K+-sparing - amiloride, triamterene, spironolactone; for GFR <30ml/min or refractory hypertension - loop diuretic (furosemide) or thiazide (METOLAZONE)

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62
Q

rules for routine use of thiazides

A

low dose, take in morn; combo w/k-sparing diuretic if hypokalemia a problem (watch for hyperkalemia); keep pt on dry weight but may cause dehydration -> mental confusion, aggravate COPD, peripheral arterial occlusive disease; important adverse effects - hypokalemia, hyperuricemia, impaired glucose tolerance, hyperlipidemia

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63
Q

beta-adrenoceptor antagonists (beta-blockers)

A

propranolol (non-selective); atenolol, metoprolol (beta1>beta2); pindolol (partial agonist); labetalol (alpha, beta-blocker, beta2 agonist); carvedilol (alpha/beta blocker); esmolol (beta1>beta2, short-acting, emergencies)

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64
Q

beta-blockers characteristics

A

beta1 selectivity is relative -> NEVER use for asthma, COPD; use in CHF is tricky - use tiny doses

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65
Q

unselective beta-blockers contraindications

A

pregnancy; diabetes; beta1-blockers can be considered; asthma, COPD, PAD, SA/AV abnormalities

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66
Q

alpha1-blockers vs. beta-blockers

A

alpha1-blockers don’t affect insulin-sensitivity -> minimal changes in CO -> don’t cause cold extremity syndrome; beta-blockers don’t cause orthostatic hypotension

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67
Q

calcium channel blockers

A

VERAPAMIL, diltiazem, nifedipine (and dihydropyridines); huge advantage over beta-blockers bc can give to diabetics, asthmatics, in pregnancy, COPD

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68
Q

verapamil, diltiazem, nifedipine pk

A

oral, iv, bound by serum proteins

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69
Q

verapamil, diltiazem, nifedipine pd

A

block L-type ca channels -> “cardiodepressant” (antiarrhythmic), arteriolar vasodilation

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70
Q

nifedipine (dihydropyridine) adverse effects

A

due to excessive vasodilation -> dizziness, headache, REFLEX TACHY, peripheral edema, constipation

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71
Q

verapamil, diltiazem adverse effects

A

bradycardia, slow SA/AV conduction

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72
Q

MI risk with antihypertensive drug therapy

A

short-acting, fast acting Ca channel blockers nifedipine, diltiazem and verapamil was associated w/inc risk of MI

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73
Q

second generation Ca channel blockers - long-acting

A

AMLODIPINE (standard - no inc risk of MI), felodipine, nisoldipine

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74
Q

second generation Ca channel blockers - slow onset

A

AMLODIPINE, felodipine

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75
Q

second generation Ca channel blockers - increased vascular selectivity

A

nisoldipine

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76
Q

second generation Ca channel blockers - increased potency

A

isradipine

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77
Q

interaction Ca channel-blockers and beta-blockers

A

beta blockers can potentiate the vasodilating effects of ca-channel blockers; 1+1=3

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78
Q

angiotensin inhibitors

A

ACE - inhibitors; ATII (AT1 subtype)-blockers

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79
Q

ACE-inhibitors

A

CAPTOPRIL, enalapril, enalaprilat, lisinopril, benzaepril, fosinopril, moexipril, quinapril, ramipril; all used for hypertension, some also for CHF

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80
Q

ATII (AT1)-blockers

A

losartan (hypertension, CHF); valsartan (hypertension)

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81
Q

ACE inhibitors - captopril pk

A

oral

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82
Q

captopril pd

A

ATII antagonism (ACE inhibition) -> dec vasoconstriction/NE release/ aldosterone secretion

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83
Q

bradykinin-related ACE inhibition pd

A

keeps bradykinin active -> vasodilation -> no reflex tachy, no significant change in CO, no h2o/na retention, some dec of sympathetic tone

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84
Q

captopril adverse effects

A

hypotension, dry cough, bronchospasm, skin rashes, angioneurotic edema, neutropenia, leukopenia, taste perversion, hyperkalemia, proteinuria

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85
Q

captopril contraindications

A

renal artery stenosis, renal failure; history of angioedema (asthma, COPD); pregnancy (oligohydramnion)

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86
Q

captopril toxicity

A

hypotension w/o marked tachy

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87
Q

captopril unwanted interactions

A

NSAIDs inhibit bradykinin pathway - dec antihypertensive response; K-sparing diuretics aggravate hyperkalemia; hypersensitivity to other drugs can be aggravated; inc plasma levels of digoxin, lithium

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88
Q

captopril therapeutically exploited interactions

A

K-wasting diuretics yield over-additive antihypertensive effect

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89
Q

ACE inhibitors - enalapril/enalaprilat characteristics

A

enalapril is prodrug of enalaprilat

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90
Q

enalapril pk

A

oral

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91
Q

enalaprilat pk

A

iv - hypertensive emergencies

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92
Q

enalapril, enalaprilat pd compared to captopril

A

longer duration of action

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93
Q

enalapril, enalaprilat adverse effects compared to captopril

A

no sulfhydryl-group -> no taste perversion

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94
Q

ACE inhibitors - others

A

most are prodrugs; fosinopril, moexipril - hepatic elminiation,, others renal;

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95
Q

ACE-inhibitors uses

A

hypertension; chf; MI; progressive renal disease in diabetic nephropathy (hyper-and normo-tensive pt’s)

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96
Q

losartan characteristics

A

angiotensin II subtype 1 blocker (AT1 blocker)

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97
Q

losartan pk

A

oral

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98
Q

losartan pd

A

LIKE ACE-inhibitors -> dec vasocontriction, dec NE release, dec aldosterone secretion; UNLIKE ACE inhibitors -> NO effect on bradykinin

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99
Q

losartan adverse effects

A

like ACE inhibitors (except bradykinin-related ae’s) - no/less cough, no angioedema

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100
Q

losartan contraindications

A

renal artery stenosis, renal failure, pregnancy

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101
Q

single drug therapy of hypertension

A

THIAZIDE or BETA BLOCKER or ca channel blocker or ACE inhibitor (or alpha1 blocker)

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102
Q

combination therapy of hypertension

A

thiazide w/beta-blocker, ca channel blocker, or ACE inhibitor; ca channel blocker w/beta-blocker or ACE inhibitor

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103
Q

triple therapy of hypertension

A

combo therapy with furosemide or clonidine

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104
Q

positive criteria for selection of antihypertensive drugs - diuretics

A

old age, black race, chf, chronic renal failure (loop diuretics)

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105
Q

positive criteria for selection of antihypertensive drugs - beta-blockers

A

youth, white, post-MI, migraine, senile tremor, atrial fibrillation (to control ventricular rate), paroxysmal supraventricular tachy

106
Q

positive criteria for selection of antihypertensive drugs - long-acting ca channel blockers

A

old age, black race, migraine

107
Q

positive criteria for selection of antihypertensive drugs - ACE inhibitors

A

youth, white race, type I diabetes w/nephropathy, impotence from other drugs; NOT IN PREGNANCY

108
Q

positive criteria for selection of antihypertensive drugs - AT1-blockers

A

same as ACE inhibitors but can’t be used due to hypersensitivity/cough; NOT IN PREGNANCY

109
Q

positive criteria for selection of antihypertensive drugs - alpha-blockers

A

prostatism, diabetes mellitis, dyslipidemia

110
Q

Traditional treatment of CHF

A

inotropic - muscle changes

111
Q

vasodilators used for chf

A

hydralazine - arterioles; minoxidil - arterioles; nitrates - veins/venules; ACE inhibitors - arterioles, veins

112
Q

treating a symptom - fatigue

A

rest, positive inotropes

113
Q

treating a symptom - edema

A

salt restriction, diuretics, digitalis

114
Q

treating a symptom - dyspnea

A

diuretics (loop)

115
Q

treating a symptom - congestion

A

nitrovasodilators, diuretics

116
Q

treating a symptom - poor cardiac contractility

A

positive inotropes, digitalis

117
Q

treating a symptom - increased pre/afterload

A

ACE inhibitors, ang-blockers, veno/vasodilators

118
Q

treating a symptom - cardiac tissue remodeling

A

ACE inhibitors, ang-blockers, beta-blockers, spironolactone

119
Q

treating a symptom - irreversible heart failure

A

heart transplantation

120
Q

cardiac glycosides

A

digoxin, digitoxin

121
Q

problems with cardiac glycosides

A

narrow therapeutic margin; complicated/unfavorable pk; sensitivity varies b/n pt’s, could change during therapy; severe, lethal ae’s

122
Q

digoxin cardiac effects

A

inc myocardial contractility; dec sinus HR (- chronotropic effect) mainly due to vagal nerve input to SA node; dec AV conduction velocity - prolong refractory period in AV (- dromotropic effect); inc automaticity/excitability in atria, purkinje, ventricles

123
Q

digoxin possible therapeutic benefits

A

inc CO; improve tissue perfusion; improve diuresis -> resorption of edema; dec sympathetic tone, vasoconstrction; dec peripheral resistance (afterload); dec preload; dec myocardial overdistension; improve working efficiency -> favorable; improve symptoms, but NO DEC IN DEATHS

124
Q

digoxin adverse effects

A

arrhythmia: tachyarrhythmia (premature ventricular contractions, ventricular fibrillation - low K+), bradyarrhythmia (non/paroxysmal atrial tachy, AV-block - high K+); GI - anorexia, nausea, vomiting, diarrhea; CNS - headache, malaise, neuralgias, delirium (Van Gogh Starry Night)

125
Q

digoxin precipitating factors for adverse effects

A

hypo/hyperkalemia; drug accumulation/overdose; hypomagnesemia, hypercalcemia; hyperthyreosis; abnormal renal fxn; respiratory disease; acid-base imbalances

126
Q

digoxin toxicity treatment

A

w/draw drug; monitor plasma dig, K levels, ECG; adjust electrolyte status; ventricular tachyarrhythmia - lidocaine, mg2+, adjust K to high normal

127
Q

severe digoxin toxicity

A

associate with hyperkalemia -> bradyarrhythmias, suppressed automaticity -> temp pacemaker; digitalis antibodies (digoxine immune fab, digibind)

128
Q

digoxin indications

A

chf grade NYHA III/IV; antiarrhythmic therapy for atrial flutter/fibrillation

129
Q

digoxin non-indications

A

ineffective in myocarditis, corpulmonale; uncontrolled hypertension; bradyarrhythmias; non-responders or intolerance (severe ae’s)

130
Q

ACE inhibitors uses

A

hypertension, chf, MI, progressive renal disease

131
Q

ACE inhibitors uses - CHF

A

prevent/delay progression of heart failure (can’t improve ejection fraction); dec incidence of sudden death, MI; dec hospitalization; improve quality of life

132
Q

ACE inhibitors uses - MI

A

dec mortality when started in periinfarction period (no later than 16 days post MI)

133
Q

how to use a beta-blocker

A

start low (10%dose, go slow); clinical assessment b4 every inc in dose (NYHA III - outpatient, NYHA IV - hospitalize); late onset of benefit (3mths - 12/18mths); give w/diuretics, ACE inhibitors, digitalis (keep as constant as possible, manages side effects); only method that can INCREASE EJECTION FRACTION

134
Q

managing side effects of beta-blockers in treating CHF

A

give w/diuretics, ACE inhibitors, digitalis; try to maintain beta-blocker, consider: sedation, hypotension (to reduce diuretics, ACE inhibitors), edema (inc diuretic), bradycardia, AV-block (dec digitalis)

135
Q

Last resort treatments

A

inotropic drugs for acute cardiac failure; keep pt alive for few more days/weeks - dopamine (low dose, act on dopamine receptors in kidney); dobutamine (iv; acts on alpha/beta receptors, inc CO w/o affecting HR); amrinone/milrinone (inc myocardial cAMP by inhibiting PDE III, inc contractile system sensitivity to ca; vaso/venodilation -> potentiates effect of dobutamine -> kills pt)

136
Q

Class I antiarrhythmic drugs - fast channel blockers (Na)

A

quinidine, lidocaine, flecainide

137
Q

Class II antiarrhythmic drugs - beta-blockers (Ca)

A

propranolol (beta antagonist), atenolol (beta1 antagonist), esmolol (short-acting beta1 antagoinst), sotalol (beta antagonist, k-channel blocker)

138
Q

Class III antiarrhythmic drugs - inhibitors of repolarization (K)

A

prolong AP, ERP; amiodarone, bretylium (indirect sympatholytic, antihypertensive), sotalol, ibutilide (emergencies), dofetilide (like sotalol, less ae’s)

139
Q

Class IV antiarrhythmic drugs - calcium channel blockers (Ca)

A

verapamil, diltiazem

140
Q

unclassified antiarrhythmic drugs

A

adenosine, atropine, digoxin, magnesium

141
Q

main factors promoting arrhythmias

A

ischemia/hypoxia; acid-base imbalance; inc autonomic input; drug toxicity (digitalis, antiarrhythmic drugs); overstretching cardiac fibers (chf); impaired tissue (MI survivors)

142
Q

all arrhythmias result from:

A

disturbance in impulse formation, conduction, or combo of both

143
Q

delayed afterdepolarization

A

result of ischemia, anything that affects cAMP (E/NE, theophylline), digitalis, tachy

144
Q

early afterdepolarization

A

result of brady, hypokalemia, action potential delaying drugs

145
Q

principles to therapy of cardiac arrhythmias

A

eliminate/minimize precipitating factors; define arrhythmia type (brady/tachy? ventricular/supraventricular?); minimize risks of doing drug therapy -> most cause arrhythmias!

146
Q

goals of therapy of cardiac arrhythmias

A

terminate ongoing arrhythmia; prevent recurrence

147
Q

class IA antiarrhythmic drugs

A

inhibits Na AND k channels -> prolonged repolarization; quinidine, procainamide, disopyramide

148
Q

class IB antiarrhythmic drugs

A

accelerated repolarization; lidocaine (used for resuscitation), mexiletine, tocainide (phenytoin)

149
Q

class IC antiarrhythmic drugs

A

little effect - rarely used; flecainide, propafenone

150
Q

quinidine pk

A

oral, IM, BID, QID (iv - watch for arrhythmia, hypotension)

151
Q

quinidine pd

A

na channel block in ACTIVATED STATE -> dec vmax in phase 0; block K channels -> prolong AP; antimuscarinic (low doses) -> inc AV-conduction (paradoxically); alpha-blocker (high conc)

152
Q

quinidine cardiac effects

A

block Na channels in ACTIVATED STATE -> dec automaticity; dec conduction/excitability; recovering from blockade - slower in depolarized than polarized tissue; RESULT: prolonged refractory period esp in depolarized tissue; block K channels - dec max re-entry frequency -> prolong AP, ERP

153
Q

quinidine EKG effects

A

prolong QRS (delays conduction in bundle of His, purkinje); prolong QT, alter T-wave (delays repolarization); variable prolongation of PR (slows AV conduction)

154
Q

quinidine cardiac adverse effects

A

dec CONTRACTILITY (- inotrope); paradoxical inc sinus rate, av-conduction (antimuscarinic actions) -> remove protective av-block -> ventricular tachy; torsade des pointes - polymorphic ventricular tachy -> could kill, self-limiting (quinidine syncope); excessive dec conduction -> toxic (AVB, asystolia) - serum K > 5, quinidine > 5

155
Q

quinidine extracardiac pd

A

antimalarial (2nd line, CHOICE for falciparum malaria); hypotensive (alpha-blocker)

156
Q

quinidine extracardiac adverse effects

A

GI disturbances; CNS - cinchonism (overdose of cinchona) - headache, dizziness, tinnitus

157
Q

quinidine extracardiac drug interactions

A

compete for CYP450 w/digoxin, verapamil, others

158
Q

quinidine use

A

supraventricular arrhythmias - paroxysmal supraventricular tachy, wolff-parkinson-white syndrome, convert atrial flutter/fibrillation to sinus rhythm as adjunct/2nd-line treatment; do not use w/o prior digitlization

159
Q

procainamide characteristics

A

amide of procaine; protected from enzymatic hydrolysis; less cns effects

160
Q

procainamide pk

A

oral; iv arrythmia, hypotension

161
Q

procainamide pd

A

LIKE quinidine; block na channels in activated state, block K channels; antimuscarinic (less than quinidine); alpha-sympatholytic

162
Q

procainamide adverse effects

A

cardiac/GI - like quinidine; cns - mental confusion, psychosis, less frequent than w/lidocaine; hypersensitivity (much more often w/quinidine), lupus-like syndrome (reversible), 70% w/ANAs; hypotension; antimuscarinic - aggravates glaucoma, urinary retention

163
Q

procainamide uses

A

indications similar to quinidine -> try other if one doesn’t work; 2nd choice after lidocaine for sustained ventricular arrhythmias w/acute MI; oral - sustained release for prolonged therapy; iv - infusion, ECG-monitoring, control plasma levels

164
Q

class IB - lidocaine characteristics

A

amide local anaesthetic

165
Q

lidocaine pk

A

ONLY iv

166
Q

lidocaine pd

A

block IN/ACTIVATED na channels -> more pronounced effect in tissues w/long plateaus (purkinje, ventricular) and depolarized tissue; little effect on K-channels -> shorten AP duration (effect depolarized, arrhythmogenic tissue)

167
Q

lidocaine cardiac adverse effects

A

exacerbate arrhythmias; SA-standstill in pt’s w/MI

168
Q

lidocaine cns adverse effects

A

paresthesias; toxic - convulsions, coma (very high doses)

169
Q

lidocaine drug interactions

A

agents that interfere w/hepatic perfusion, microsomal metabolism

170
Q

lidocaine uses

A

CHOICE for ventricular tachy, fibrillation after cardioversion; suppress arrhythmia assoc w/depolarization (post MI, dig toxicity); NOT for prolonged prophylactic use post-MI

171
Q

mexiletine characteristics

A

orally active congeners of lidocaine

172
Q

mexiletine pk

A

oral

173
Q

mexiletine pd

A

same as lidocaine

174
Q

mexiletine adverse effects

A

frequent w/therapeutic doses; cns - nausea, tremor, blurred vision, lethargy; allergic - rash, fever, agranulocytosis

175
Q

(phenytoin) characteristics

A

antiepileptic drug similar to phenobarbital

176
Q

(phenytoin) pk

A

oral, iv

177
Q

(phenytoin) pd

A

same as lidocaine

178
Q

(phenytoin) adverse effects

A

cns - sedation, nystagmus, vertigo, loss of mental accuity; gingival hyperplasia

179
Q

class IC - flecainide, propafenone characteristics

A

very slow dissociation from na channel during recovery; use in life-threatening, refractory arrhythmia; flecainide CAST - inc mortality in post MI pt’s treated for premature ventricular contractions -> use ONLY oral for atrial arrhythmias in hearts otherwise uncompromised

180
Q

class II prototype drug - propranolol cardiovascular effects

A

dec SA freq -> sinus brady; dec automaticity in purkinje; prolong ERP of AV-node; suppress ectopic ventricular depolarizations; - inotrope; diverse hemodynamic effects

181
Q

propranolol cardiovascular adverse effects

A

hypotension, aggravation of chf, asystolia

182
Q

propranolol uses

A

dec risk of sudden death in post MI; control supraventricular tachy; exercise/stress-precipitated ventricular arrhythmias; ischaemic heart disease, angina pectoris

183
Q

class III - amiodarone pk

A

2 weeks to reach steady state; 30-120 days half life

184
Q

amiodarone pd

A

block INACTIVATED na channels - most pronounced in tissues w/long plateaus (purkinje, ventricular), depolarized; block k-channels; weak ca channel, beta blocker

185
Q

amiodarone adverse effects

A

can deposit in tissues (slowly reversible) -> pulmonary fibrosis, corneal deposits, photodermatitis, skin discoloration; cns - paresthesias, tremor, ataxia, headache; thyroid dysfxn; GI/liver toxicity

186
Q

amiodarone drug interactions

A

digoxin, theophylline, warfarin, quinidine

187
Q

class III - sotalol characteristics

A

racemic mix used

188
Q

sotalol pk

A

oral, iv

189
Q

sotalol pd

A

block k-channels; beta blocker

190
Q

sotalol adverse effects

A

same as beta blockers; proarrhythmic (torsades des pointes)

191
Q

sotalol uses

A

treat/prophylaxis of severe ventricular tachyarrhythmias, atrial arrhythmias

192
Q

ca channel blockers - verapamil, diltiazem characteristics

A

block L-type ca-channels in in/activated states; most pronounced effect on AV-conduction

193
Q

verapamil, diltiazem uses

A

re-entrant supraventricular tachy; dec ventricular rate in atrial fib, flutter; ischaemic heart disease, angina pectoris; hypertension

194
Q

adenosine characteristics

A

ubiquitous auto/para/endocrine compound

195
Q

adenosine pk

A

iv infusion

196
Q

adenosine pd

A

purine-p1 receptor agonist; inc k-conductance, inhibits cAMP-mediated ca influx -> hyperpolarization, esp in av-node

197
Q

adenosine uses

A

conversion of narrow complex paroxysmal ventricular tachy (PSVT)

198
Q

adenosine adverse effects

A

transient (short t1/2) -> flushing, av-block III, chest pain, atrial fib, bronchoconstriction esp in asthmatics

199
Q

miscellaneous antiarrhythmics

A

potassium; magnesium (ca-antagonist - treat torsades des pointes, dig-induced arrhythmia, prevent arrhythmia in acute MI); digoxin (slow av conduction); atropine (bradyarrhythmia -> dec vagal tone)

200
Q

drug therapy for atrial fibrillation

A
  • dromotropic agents -> digoxin, verapamil/diltiazem, beta-blockers; induce/maintain sinus rhythm - block fast action potentials (class IA, IC, III antiarrhythmics)
201
Q

angina treatment drugs

A

nitrates, beta-blockers, ca-channel blockers

202
Q

angina combination treatment

A

nitrate + beta-blocker

203
Q

nitrates

A

nitroglycerine, isosorbide dinitrate (ISDN), isosorbide mononitrate (ISMN)

204
Q

nitrates pd

A

relax smooth muscles, including vascular; fast relaxation of venous tone -> inc capacitance, dec preload; slowly dec arteriolar resistance -> dec myocardial O2 demand

205
Q

nitrates pk

A

nitroglycerine - subligual, buccal, transderma, iv; NOT oral

206
Q

nitrates adverse effects

A

vasodilation -> headache, flushing; hypotension -> reflex tachy, dizziness, weakness, cerebral ischaemia; nitrate tolerance

207
Q

nitrates uses

A

acute/anticipated attacks of angina; prolonged preventative therapy (ISMN, ISDN); paroxysmal nocturnal dyspnea in chf; spasmolytic in colic pain (biliary, renal, intestinal)

208
Q

factors that induce nitrate tolerance

A

prolonged nitrate exposure (patch, sustained release, iv); large doses; frequent dosing

209
Q

factors that prevent nitrate tolerance

A

intermittent dosing; small doses; infrequent dosing; nitrate-free intervals

210
Q

sodium nitroprusside characteristics

A

ferrocyanide compound; limit use to only some hours

211
Q

sodium nitroprusside pd

A

direct NO donator -> immediate vasodilation

212
Q

sodium nitroprusside pk

A

iv infusion; protect from light, converted to cyanide, then thiocyanide

213
Q

sodium nitroprusside uses

A

ICU/emergencies; controlled hypotension in surgery; some of severest cardiac failure

214
Q

sodium nitroprusside precautions

A

borderline systolic BP; myocardial ischaemia w/o heart failure; hepatic/renal insufficiency

215
Q

sodium nitroprusside adverse effects

A

nausea, vomiting, headache, cns disturbances

216
Q

sodium nitroprusside toxicity

A

cyanide intoxication

217
Q

ca channel blockers

A

verapamil, diltiazem, nifedipine (and dihydropyridines)

218
Q

verapamil, diltiazem, nifedipine pk

A

oral, iv

219
Q

verapamil, diltiazem, nifedipine pd

A

block L-type ca channels -> cardiodepressant, arteriolar vasodilation

220
Q

verapamil, diltiazem, nifedipine adverse effects

A

dihydropyridines (excessive vasodilation) -> dizziness, headache, peripheral edema, reflex tachy; verapamil, diltiazem -> brady, slow SA/AV conduction

221
Q

beta blockers for angina

A

propranolol, atenolol, metoprolol

222
Q

beta blockers effects on angina

A

dec severity/freq in exertional angina; somewhat effective in unstable angina; cardioprotective in post MI (beta1 selective); ineffective in vasospastic angina - may worsen condition

223
Q

antihyperlipidemic drugs

A

hmg coa reductase inhibitors (statins); niacin; fibrates; bile-acid binding agents; cholesterol absorption inhibitors; combination drug therapy

224
Q

statins

A

lovastatin, sinvastatin, pravastatin, atorvastatin, fluvastatin, rosuvastatin

225
Q

statins characteristics

A

CHOICE, most efficacious for inc LDL (hypercholesterolemia)

226
Q

statins pk

A

cyp450

227
Q

statins pd

A

inhibit hmg coa reductase (HMG analogs) -> inc LDL receptor expression (homozygotes for FH -> no LDL receptors -> no response); modest dec TGs; small inc HDL

228
Q

statins adverse effects of monotherapy

A

myopathy, myositis w/rhabdomyolysis; inc transaminase, liver enzymes

229
Q

statins adverse effects of combo therapy

A

interactions (cyp450); myopathy, myositis, rhabdomyolysis; inc risk of overdose of ther drugs

230
Q

statins contraindications

A

pregnancy/lactation, hepatic disease, muscular disease

231
Q

statin combinations

A

w/bile acid binding agent or cholesterol absorption inhibitor (more dec LDL); w/niacin - inc risk of myopathy; w/fibrates - inc risk of rhabdomyolysis (gemfibrozil)

232
Q

bile-acid binding agents

A

cholestyramine, colestipol, colesevelam

233
Q

cholestyramine, colestipol, colesevalem characteristics

A

2nd choice for lipid reduction; ensure ample fluid intake to avoid constipation

234
Q

cholestyramine, colestipol, colesevalem pd

A

cationic resins - bind to negatively charged bile acids in sm intestine -> prevent reabsorption -> inc conversion of cholesterol to bile acids; inc LDL receptor

235
Q

cholestyramine, colestipol, colesevalem pk

A

oral, fat soluble -> not absorbed/met’d; uncomfortable to ingest; completely excreted in feces

236
Q

cholestyramine, colestipol, colesevalem interactions

A

acidic drugs, coumadin, vitamin c; dec absorption of fat-soluble vit’s, drugs (digoxin, warfarin, antiretrovirals, cyclosporin)

237
Q

cholestyramine, colestipol, colesevelam uses

A

type IIa/b hyperlipidemias; only w/isolated inc in LDL; hypercholesterolemia in young (s w/biliary obstruction (pancreatic carcinoma)

238
Q

cholestyramine, colestipol, colesevalem adverse effects

A

GI - constipation, nausea, bloating, flatulence

239
Q

cholestryamine, colestipol, colesevalem combinations

A

w/statins or niacin -> more dec LDL

240
Q

cholestyramine, colestipol, colesevalem contraindications

A

can upregulate vldl, TG synth -> caution in pt’s w/hypertriglyceridemia

241
Q

niacin

A

nicotinic acid, vitamin b3

242
Q

nicotinic acid, vitamin B3 characteristics

A

most effective agent to inc hdl

243
Q

nicotinic acid, vitamin b3 pd

A

dec vldl, ldl, tg; inhibits lipolysis in adipose; dec FA’s -> dec triacylglycerol synth (req’d for vldl); inc HDL

244
Q

nicotinic acid, vitamin b3 pk

A

oral; converted to nicotinamide -> used in NAD; niacin/metabolites excreted in urine

245
Q

nicotinic acid, vitamin b3 uses

A

when statin contraindicated; familial hyperlipidemias; combo w/statins for severe hypercholesterolemias

246
Q

nicotinic acid, vitamin b3 adverse effects

A

cutaneous flush, pruritus (vasodilator); hyperuricemia; hepatotoxicity; impaired insulin sensitivity (caution diabetics); combo w/statin -> inc risk of myopathy

247
Q

fibrates

A

fenofibrate, gemifibrozil

248
Q

fenofibrate, gemfibrozil pk

A

oral; bound to albumin

249
Q

fenofibrate, gemfibrozil pd

A

dec vldl, tg’s; inc hdl; modest dec ldl; binds, activates PPARalpha (hepatocytes, sk muscle, macrophages, heart);

250
Q

fenofibrate, gemfibrozil uses

A

hypertriglycerolemias; CHOICE for dysbetalipoproteinemia; pt’s not responding to diet/other drugs

251
Q

fenofibrate, gemfibrozil adverse effects

A

mild GI; CHOLELITHIASIS; myositis

252
Q

fenofibrate, gemfibrozil interactions

A

compete w/coumarin (warfarin) for plasma binding sites -> potentiates anticoagulant activity

253
Q

fenofibrate, gemfibrozil contraindications

A

PREGNANCY safety not established

254
Q

cholesterol absorption inhibitors

A

ezetimibe, plant sterols

255
Q

ezetimibe, plant sterols pd

A

dec ldl (small dec tg’s, small inc hdl); inhibit absorption of dietary, biliary cholesterol; inhibit hepatic vldl synth; upregulation of ldl receptor

256
Q

ezetimibe, plant sterols pk

A

oral; met in sm intestine, liver

257
Q

ezetimibe, plant sterols uses

A

complementary to statins or in combo when statins inadequate; hypercholesterolemia when statin CI’d

258
Q

ezetimibe, plant sterols adverse effects

A

diarrhea, ab pain, headache, rash, angioedema

259
Q

ezetimibe, plant sterols contraindications

A

pregnancy, lactation

260
Q

omega-3 fatty acids - fish oils characteristics

A

dec tg’s

261
Q

fish oils pd

A

dec tg synth; inc fa oxidation

262
Q

fish oils uses

A

tg > 500mg/dL

Pharmacology (15 decks)

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