Adrenergic blockers

Question 1

first beta-blocker

Answer 1

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

Question 2

timolol

Answer 2

non-selective

-no blockage of Na channels

Question 3

Pindolol

Answer 3

partial agonist

• less HR and BP
• angina, hypertension with bradycardia

Question 4

Beta-1 selective

Answer 4

atenolol
metoprolol
-less effects on lungs

Question 5

metoprolol

Answer 5

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

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

Question 6

atenolol

Answer 6

metabolized in liver (2C9),

half-life: 6 hours

Question 7

most popular drug of all cardiovascular drugs

Answer 7

beta-blockers, used for

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

Question 8

beta blocker use with angina

Answer 8

beta blockers decrease HR and force-> decrease work

Question 9

beta blocker use with hypertension

Answer 9

initially decrease BP and decrease CO

-no postural hypertension

Question 10

beta blockers _______ during surgery

Answer 10

pheochromocytoma

Question 11

prophylaxis of migraine

Answer 11

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

Question 12

prevent recurrence of

Answer 12

heart attacks

• decrease incidence of death
• especially good after MI

Question 13

beta-1 blockers in

Answer 13

hyperdynamic circulatory state

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

Question 14

glaucoma

Answer 14

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

Question 15

drugs of choice in glaucoma

Answer 15

PG analogs, increase outflow through accessory uveoscleral pathway

Question 16

precautions in use of beta blockers

Answer 16

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

Question 17

precautions in use of beta blockers: CNS depression

Answer 17

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

Question 18

precautions in use of beta blockers: poor circulation

Answer 18

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

• dont use in pregnancy
• decrease exercise tolerance

Question 19

precautions in use of beta blockers: diabetes

Answer 19

block beta-2 to inhibit mobilization of liver glycogen

-increases effect of insulin

Question 20

precautions in use of beta blockers: rebound tachycardia

Answer 20

cessation of therapy

-taper dose over period of weeks

Question 21

Alpha blockers

Answer 21

competitive alpha-1 blockers

-some also block alpha-2

Question 22

clinical use of alpha blockers

Answer 22

prostatic hypertrophy

improve urine flow

Question 23

tamusolin (Flomax)

Answer 23

specific for alpha-1 receptors

-less effect on blood vessels (1B)

Question 24

alpha blockers for increase in BP

Answer 24

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

Question 25

precautions and side effects of alpha-1 blockers

Answer 25

- postural hypotension - nasal stuffiness - impaired sex function-> failure of ejaculation

Question 26

Ergot alkaloids 1st known adrenergic blockers

Answer 26

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

Question 27

Ergot alkaloids

Answer 27

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

Question 28

what is Ergot used in?

Answer 28

Migraine - relieves painful throbbing with each heart beat - taken at start of headache - erotamine even more effective when taken with caffeine

Question 29

mild migraine

Answer 29

aspirin

Question 30

moderate migraine

Answer 30

ergot

Question 31

severe migraine

Answer 31

beta blockers

Question 32

what else of ergot alkaloids used for

Answer 32

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