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Flashcards in Pharm 10.2 Deck (67)
1

selective Beta 1 blockers

Acebutolol, atenolol, metoprolol

2

betablockers - ISA - intrinsic sympathomimmetic activity

Acebutolol, Pindolol

3

beta blockers with sedation effects

most except Atenolol

4

beta blockers that increase blood lipids

most except Acebutolol and Pindolol

5

Propanolol administration

oral is well absorbed, undergoes extensive first pass metabolism

6

Propanolol and BBB

Propranolol is lipophilic so it inters the BBB

7

Propanolol excretion

excreted in urine as glucuronide metabolites

8

nonselective beta blockers on inotropy

dec force of contration - negative inotropy

9

nonselective beta blockers on chronotropy

dec rate of contraction - negative chronotropy

10

nonselective beta blockers on SA and AV nodes

supress SA and AV nodal activity -- bradycardia

11

overall effect of beta blockers on the heart

dec heartrate, SV, and CO, decBP in hypertensiv ppl -->reflex peripheral vasoconstriction

12

Why is Propranolol useful in angina

dec cardiac work so dec O2 consumption

13

Propranolol on blood vessels

blocks B2 mediate vasodialation

14

nonselective beta blockers and BP

does not dec BP in normal ppl, but decreases BP in hypertensive ppl (both systolic and diastolic)

15

nonselective beta blockers and postural hypotension

no postural hypotension because no effect on alpha 1 adrenergic receptors

16

Propranolol and the Kidney

decrease renin release from kidney (beta 1 action) -- very useful property in reducing compensatory BP elevation

17

beta blockers are often combined with

a diuretic in treatment of HTN

18

Propranolol and respiratory tract

bronchoconstriction and can precipitate bronchial asthma (Beta 2 action)

19

Beta 2 blocker contraindications

bronchial asthma

20

beta blockers and the eyes

dec IOT due to inc aqueous humor production

21

Propranolol and the CNS

sedation, lethargy, depression, forgetfulness, sleep disturbances (dreams and nightmares) worse in lipophilic agents

22

Propranolol and skeletal muscle

antaganizes the epinephrine induced tremmors (muscle spindle controling tremors is under beta 2 control)

23

Propranolol metabolic effects

blocks epinephrine induced glycogenolysis --> fasting hypoglycemia; decrease insuline release (beta 2 block) after meal causing hyperglycemia

24

why should propranolol be used with caution in diabetics

bc it masks the warning sympathetic signes and symptoms such as swating, palpitations (tachycardia) induced by hypoglycemia

25

what is a warning sign of hypoglycemia

tachycardia --this is masked by beta blockers

26

therapeutic uses of Propranolol

hypertension, Angina (except Prinzmetal's angina), MI (prophylactic use post-MI), Cardiac arrhythmias (Class II: Propranolol, Acebutolol, Esmolol), Migraine (prophylactically), Hyperthyroidism, Pheochromocytoma, Performance anxiety, Essential tremors, Glaucoma (Timolol), CHF, Hypertrophic cardiomyopathy, marfan syndrome and aneurysms

27

Beta blockers and hyperthyroidism

chance of thyroid storm increases during surgical removal of theyroid so betablockers beore surgery is desirable

28

CHF and beta blockers

dec sympathetic discharge and NE release dec CHF mortality

29

hypertrophic cardiomyopathy and betablockers

dec syncope, arrhythmias, and sudden death

30

Marfan syndrome and aneurysms and betablockers

alone or combined with ACEI/ARB dec aneurismal dialation by dec TGFbeta activity

31

beta blocker adverse CVS effects

bradycardia, AV block, abrupt discontinuation of propranolol can precipitate angina, arrhythmia, and hypertension ---should be withdrwan gradually after long term use

32

beta blockers adverse respiratory effects

causes bronchoconstriction, should not be used in asthmatic and COPD patients

33

beta blockers adverse metabolic effects

fasting hypoglycemia, increases blood lipid levels (LDLs and TGs)

34

beta blockers and other adverse effects

sexual dysfunction, fatigue and exercise intolerance

35

betablockers are contraindicated in

asthmatics, COPD, diabetics, Raynaud's disease, Prinzmetal angina

36

beta blockers with Digitalis and verapamil

additive depression of SA and AV node --> cardiac arrest

37

beta blockers and insuline/oral hypoglycemics

aggravate hypglycemic effects, mask warning signes (tremor and tachycardia)

38

betablockers and indomethacin and other NSAIDs

annul antihypertensive actions of betablockers

39

betablockers and cimetidine

inhibits metabolism of Propranolol

40

Timolol

potent nonselective betablocker, reduces the production of aqueous humor in the eye and hence used topically for the treatment of chronic open-angle glaucoma

41

nadolol

very long duration, same actions as propranolol (nonselective)

42

selective beta 1 antagonists

acebutolol, atenolol, esmolol, metoprolol

43

selective beta 1 antagonists can be used

in hypertensive patients with asthma and COPD bc they do not cause bronchoconstriction at therapeutic doses

44

selective beta 1 antagonists actions

decrease BP in hypertensive pts, inc exercise tolerance in angina, no bronchoconstriction effect, no effect on PR, no effect on CHO metabolism

45

therapeutic uses of beta 1 blockers

HTN (esp if they have pulm dysfuntion or diabetes), Angina, MI

46

beta1 blocker adverse effects

bradycardia

47

Atenolol

selective beta 1 blocker

48

Atenolol properties

lower lipid solubility, less CNS entry, excreted unchanged in the urine

49

Atenolol uses

HTN, Angina, MI

50

Metoprolol administered

orally/ IV for HTN, Angina, MI

51

Vasodialating beta blockers (less adverse effects)

labetalol, carvedilol, nevibolol, celiprolol

52

labetalol

beta blocker with additional alpha 1 blockade

53

carvedilol

nonselective beta blocker, alpha 1 blocker, ca-channel blocker, antioxidant

54

carvedilol halflife

7 hours

55

Nevibolol

cardioselective, anti-oxidant, beta 3 sitmulation causing NO production (effective in black ppl)

56

Celiprolol

Cardioselective, beta 1 blocker, beta 2 agonist, NO production

57

betablocker responsivness and ethnicity

chinese>white>black

58

American SNP asscociated with better survival in CHF patients treated with beta blockers

ADRB1gly389gly > ARDB1arg389gly

59

Esmolol

shortest acting beta 1 blocker, IV administration to treat acute supraventricular tachycardia

60

beta 1 blockers with ISA

pindolol, acebutolol

61

beta1 blockers with ISA cause

less bradycardia (beta1) and slight vasodialation or bronchodialation (beta2), act partial agonists

62

beta 1 blockers with ISA uses

HTN with moderate bradycardia in DM , CHO metabolism is less affected

63

beta blocker with K+ channel block

sotalol - used as antiarrhythmic (class 3)

64

alpha and beta blockers

labetalol, carvedilol

65

actions of Labetalol and carvedilol

peripheral vasodialation dec BP -- used in HTN emergency

66

benefits of labetolol and carvedilol

does not cause reflex bradycardia

67

cons of labetolol and carvedilol

same contraindications as nonselective beta blockers