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Pharmacology part 3 > Adrenergic blockers > Flashcards

Adrenergic blockers Flashcards

1
Q

first beta-blocker

A

propranolol

  • mainly blocks beta-1 in heart
  • also blocks renin release:juxtaglomerular cells have beta-1
  • large individual variation in effect
  • NON-selective, also blocks beta-2
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2
Q

timolol

A

non-selective

-no blockage of Na channels

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3
Q

Pindolol

A

partial agonist

  • less HR and BP
  • angina, hypertension with bradycardia
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4
Q

Beta-1 selective

A

atenolol
metoprolol
-less effects on lungs

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5
Q

metoprolol

A

good for asthma and in preventing cardiovascular problems (in hypertension)

  • excreted in urine, T1/2 of 5 hours
  • extended release preparation used
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6
Q

atenolol

A

metabolized in liver (2C9),

half-life: 6 hours

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7
Q

most popular drug of all cardiovascular drugs

A

beta-blockers, used for

  • angina
  • hypertension
  • cardiac arrhythmias: especially with strong sympathetic component
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8
Q

beta blocker use with angina

A

beta blockers decrease HR and force-> decrease work

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9
Q

beta blocker use with hypertension

A

initially decrease BP and decrease CO

-no postural hypertension

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10
Q

beta blockers _______ during surgery

A

pheochromocytoma

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11
Q

prophylaxis of migraine

A
  • affects about 15% of population-> women twice as much as men
  • beta-blockers: decrease pulse pressure
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12
Q

prevent recurrence of

A

heart attacks

  • decrease incidence of death
  • especially good after MI
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13
Q

beta-1 blockers in

A

hyperdynamic circulatory state

  • excessive increase HR in emotional situations
  • used prior to dental procedures, football games, musical performances, etc
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14
Q

glaucoma

A

beta blockers well tolerated
-inhibits formations of aqueous humor
Mostly Beta-2 receptors in eye

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15
Q

drugs of choice in glaucoma

A

PG analogs, increase outflow through accessory uveoscleral pathway

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16
Q

precautions in use of beta blockers

A
  • Asthma (not so bad with beta-1 specific drugs), beta-2 bad to block
  • CNS depression
  • Poor circulation
  • Diabetes
  • Rebound tachycardia
17
Q

precautions in use of beta blockers: CNS depression

A

may be caused by beta-blockers especially those with high lipid solubility ( pindolol, propranolol)
-dont use in patients with history of depression

18
Q

precautions in use of beta blockers: poor circulation

A

decreases CO leads to tiredness, numbness, tingling, muscle ache

  • dont use in pregnancy
  • decrease exercise tolerance
19
Q

precautions in use of beta blockers: diabetes

A

block beta-2 to inhibit mobilization of liver glycogen

-increases effect of insulin

20
Q

precautions in use of beta blockers: rebound tachycardia

A

cessation of therapy

-taper dose over period of weeks

21
Q

Alpha blockers

A

competitive alpha-1 blockers

-some also block alpha-2

22
Q

clinical use of alpha blockers

A

prostatic hypertrophy

improve urine flow

23
Q

tamusolin (Flomax)

A

specific for alpha-1 receptors

-less effect on blood vessels (1B)

24
Q

alpha blockers for increase in BP

A

dilates arteries and veins

  • prasosin T1/2 3 hours
  • terazosin T1/2 12 hours

phentolamine (older drug), nonspecific
-alpha1/alpha2= 4/1
can cause tachycardia, used to block necrosis by injected sympathomimetics

25
Q

precautions and side effects of alpha-1 blockers

A
  • postural hypotension
  • nasal stuffiness
  • impaired sex function-> failure of ejaculation
26
Q

Ergot alkaloids 1st known adrenergic blockers

A

-powerful alkaloids which can cause gangrene due to toxic effect on blood vessels, can also cause angina, hallucinations, abortions

27
Q

Ergot alkaloids

A

alpha-blockers: not part of clinical actions, not even side effects
-have partial agonist activity on alpha-1 and 5HT1D receptors
-Main effect: prolonged contraction smooth muscle
acts mainly on capacitance blood vessels, uterine smooth muscle also contracted

28
Q

what is Ergot used in?

A

Migraine

  • relieves painful throbbing with each heart beat
  • taken at start of headache
  • erotamine even more effective when taken with caffeine
29
Q

mild migraine

A

aspirin

30
Q

moderate migraine

A

ergot

31
Q

severe migraine

A

beta blockers

32
Q

what else of ergot alkaloids used for

A

post partum bleeding

  • much bleeding occurs when placenta tears away from uterine wall
  • ergot alkaloids contract uterus and stop bleeding
  • agonists or partial agonists on 5HT/alpha-1 receptors
  • ergonovine

Pharmacology part 3 (13 decks)

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