Pharm REVERSE -adnrenergic antagonists

Question 1

drugs that disrupt the synthesis, storage or release of norepinephrine

Answer 1

What is the mechanism of adrenergic neuron blockers?

Question 2

1) Guanethidine
2) Guanadrel
3) Reserpine

Answer 2

Which drugs are Adrenergic neuron blockers? (3)

Question 3

Inhibits norepinephrine release and depletes neuronal amine stores

Answer 3

What is the mechanism of Guanethidine and Guanadrel? (2)

Question 4

Severe hypertension

Answer 4

What is the therapeutic use of Guanethidine and Guanadrel?

Question 5

Guanethidine is a polar compound that does not enter the CNS

Answer 5

What is the difference between Guanethidine and Guanadrel?

Question 6

NET - therfore they are inhibited by tricyclic antidepressants that inhibit NET

Answer 6

How are Guanethidine and Guanadrel taken up into the cell?

Question 7

Many side effects: orthostatic hypotension, interferes with sexual function, diarrhae, muscle weakness, edema

Answer 7

What are the side effects of Guanethidine and Guanadrel?

Question 8

It inhibits he vesicular monamine oxidase transporter 2 (VMAT2) therby inhibiting the synthesis of norepinephrine

Answer 8

What is the mechanism of Reserpine?

Question 9

diffusion (does not need VMAT2)

Answer 9

How does Reserpine get into the cell?

Question 10

treats essential hypertension - rarely used

Answer 10

What is the therapeutic use of Reserpine?

Question 11

Many CNS side effects, depression, suicide, sedation

Other side effects: diarrhae, orthostaic hypo-tension, increased gastric acid secretion

Answer 11

What are the side effects of Reserpine?

Question 12

Slow onset and Long acting

Answer 12

What is Reserpine’s length of onset and how long does it last?

Question 13

Agents produce their major actions by inhibiting alpha and beta receptors. Both exogenously administered as well as endogenously released catecholamines are blocked

Answer 13

What is the mechanism of adrenergic receptor blockers?

Question 14

1) Phenoxybenzamine
2) Phentolamine
3) Prazosin
4) Tamsulosin

Answer 14

What drugs are alpha adrenergic receptor antoganists? (4)

Question 15

irreversible inhibition of a₁ and a₂

Answer 15

Phenoxybenzamine

Question 16

Irreversible antagonist via covalent bonding with receptor. New receptors need to be synthesized, so it is very long lasting

Answer 16

What is the mechanism of Phenoxybenzamine?

Question 17

produces vasodilation proportional to the degree of sympathetic tone

Answer 17

What is the effect of Phenoxybenzamine?

Question 18

Competitive reversible antagonist of a₁ and a₂

Answer 18

phentolamine

Question 19

Therapies:

1) pheochromocytoma
2) To reverse or shorten the duration of soft-tissue anesthesia produced by combined local anesthetic and sympathomimetic

Answer 19

Phenoxybenzamine

Question 20

Therapies:

1) hypertension
2) pheochromocytoma
3) to reverse or shorten the duration of soft tissue anesthesia produced by combined local anesthetic and sympathomimetic

Answer 20

Phentolamine?

Question 21

Side effects:

1) tachycardia and salt/water retention (edema)
2) Orthostatic hypotension

Answer 21

phenoxybenzamine and phentolamine

Question 22

competitive blocker of a₁ receptors

Answer 22

Prazosin

Question 23

Effects:

1) minimal tachycardia
2) decreases vascular tone in resistance (arterioles) and capacitance (veins)
3) produce favorable lipid profile: low LDL, high HDL

Question 24

Therapys:

1) hypertension
2) short-term treatment of congestive heart failure (because of preload and afterload reducing agent)
3) Benign prostatic hyperplasia (BPH) - relaxes a₁ mediated contraction of prostate and bladder neck that contributes to resistance to urine flow

Answer 24

Prazosin

Question 25

Side effects

1) “first dose” phenomenon - hypotension and syncope 30-90 minutes after first dose
2) presistent orthostatic hypotension
3) salt and water retention (edema)

Answer 25

prazosin

Question 26

a₁ receptor antagonist with ome selectivity for a_1A versus a_1B (favors a_1A receptor blockage in prostate)

Answer 26

Tamsulosin

Question 27

Therapeutic use:

Effective for treatement of BPH with little effect on blood pressure

Not approved for treatmenet of hypertension

Answer 27

Tamsulosin

Question 28

1) Propranolol
2) Timolol
3) Metoprolol
4) Atenolol

Answer 28

What are the non-selective beta adrenergic receptor antagonists?

Question 29

Competitive reversible blockade of both B₁ and B₂ receptors

Answer 29

Propranolol and Timolol

Question 30

Therapeutic use:

Hypertension

Angina

cardiac arrhythmias due to excess catecholamines or that respond to a reduction in heart rate/AV conduction velocity

Acute myocardial infarction

migraine prophylaxis

Answer 30

Propanolol

Question 31

Side effects

Cardiac depression, bradycardia/heart block

May increase airway resistance

Mask sympoms of hypoglycemia

sedation, impotence, nightmares

Answer 31

Propranolol

Question 32

Patients with shouldn’t recieve what drug:

Asthma

CHF

bradyarrhythmias, AV block

insulint-dependentdiabetes prone to hypoglycemic episodes

hypotension

vasopastic angina

Answer 32

Propranolol

Question 33

Therapeutic use:

Similar to propranolol along with treatment of wide angle glaucoma

Answer 33

Timolol

Question 34

Competitive, reversible B₁ receptor blocker

Answer 34

Metoprolol

Question 35

Therapeutic use:

Similar to propranolol - also used to treate heart failure

Answer 35

metoprolol

Question 36

B₁ receptor antagonist

Answer 36

Atenolol and metoprolol

Question 37

Similar to propranolol (except for migraine prophylaxis)

Answer 37

Atenolol

Question 38

Therapys

Essential hypertension and hypertensive emergencies

Answer 38

Labetalol

Question 39

Competitive antagonist of a₁ receptor and both B receptors (non-selective)

Answer 39

Labetalol and Carvedilol

Question 40

1) anti-oxidant properties and anti-inflammatory effects
2) blocks L-type calcium channels at higher doses

Answer 40

Carvedilol

Question 41

Therapeutic use:

1) CHF
2) Hypertension
3) Acute MI

Answer 41

Carvedilol