Pharmacology - chapter 7 - Adrenergic antagonists

Question 0

phenoxybenzamine therapeutic uses?

Answer 0

pheochromocytoma, raynauds disease, frostbite, acrocyanosis.

Question 1

Phenoxybezamine?

Answer 1

Irreversible & noncompetitive inhibitor of alpha-1 and alpha-2 receptors.

Question 2

Phentolamine?

Answer 2

competitive block of alpha-1 & alpha-2 receptors used to treat hypertensive crisis.

Question 3

Prazosin, Terazosin, Doxazosin, Tamsulosin and Alfuzosin ?

Answer 3

Selcetive competitive blockers of the lpha-1 receptor.

Question 4

Tamsulosin & alfuzosin therapeutic uses?

Answer 4

Benign Prostatic hyperplasia

Question 5

Prazosin, Terazosin and Doxazosin therapeutical use?

Answer 5

used to treat hypertension. By inhibiting alpha-receptors these drugs inhibit vasoconstriction = vasodilates. They also bind alpha receptors in adipose tissue and in liver, improving lipidprofiles and glucose metabolism in hypertensive patients.

Question 6

What is “first-dose” effect?

Answer 6

E.g. Prazosin, terazosin and doxazosin may produce a orthostatic hypotensive response when the first dose is administered.

Question 7

How to avoid “first-dose” response?

Answer 7

lower the first dose to 1/3rd or 1/4th of normal dose, and give drug at bedtime.

Question 8

5alpha-reductase?

Answer 8

convert testosterone to dihydrotestosterone

Question 9

Finasteride and dutasteride?

Answer 9

5 alpha-reductase inhibitors used to treat benign prostatic hyperplasia

Question 10

A humongously horribly disastrous sideeffect of Finasteride and duasteride?

Answer 10

sexual dysfunction

Question 11

Yohimbine?

Answer 11

Found as a component of the bark of the yohimbe tree. It’s a selective competitive alpha2-blocker. Works at the level of the CNS to increase sympathetic outflow.

Question 12

All clinically available beta blockers are… ?

Answer 12

competitive antagonists

Question 13

with exception of labetalol and carvediol, the name of all beta blosker end in …..?

Answer 13

“-olol”

Question 14

Propranolol?

Answer 14

Beta-1 and beta-2 blocker

Question 15

Effects of propanolol?
1 cardiovascular
2 respiratory
3 kidney
4 glucose

Answer 15

1 cardiovascular - lowers CO with negative iono-and chronotrophic effects. Prevents beta-2 mediated vasodilation = vasoconstriction.
2 respiratory - bronchoconstriction
3 decreased renal perfusion increses Na-retention.
4 glucose - beta-blockade leads to decreased glycogenolysis and glucagon secretion.

Question 16

Conditions where you never treat with propranolol?

Answer 16

Asthma or COPD patients.

Question 17

beta blockers in asthmatic diabetes patient?

Answer 17

use cardioselective betablockers

Question 18

Drugs that inhibit or interfere with propranolol?

Answer 18

cimentidine, fluoxetine, paroxetine and ritonavir

Question 19

drugs that stiulate or induce metabolism of propanolol?

Answer 19

barbiturates, phenytoin and rifampin

Question 20

Timolol and nadolol?

Answer 20

Noselective beta antagonists that are more potent than propanolol.

Question 21

Beta blockers and glaucoma?

Answer 21

Beta blockers are effective in treating glaucoma. The decrease the intraocular pressure by lowering the secretion of aqueous humor by the ciliary body.

Question 22

Acetubulol, atenolol, metoprolol, bisoprolol, betaxolol, nebivolol og esmolol?

Answer 22

Beta1 selective antagonists.

Question 23

beta-1 cardioselectivity and dose-relationship?

Answer 23

cardiospecificity is most pronounced at low doses, and lost with increased doses.

Question 24

pindolol and acebutolol?

Answer 24

beta-1 antagonists with slight intrinsic agonist activity.

Question 25

Labetalol and carvediol?

Answer 25

antagonists of both alpha and beta adrenergic receptors. Good drugs for treating hypertensive patients for whom increased TPR is undesirable.

Question 26

Reserpine?

Answer 26

plant alkaloid that block Mg/ATP-dependent transport of biogenic amines, norepinephrine, dopamine and serotonine.

Question 27

Guanethidine?

Answer 27

blocks release of stored norepinephrine as well as displacing norepinephrine from storage vesicles.

Question 28

Cocaine?

Answer 28

blocks reuptake of epinephrine, norepinephrine, serotonine and dopamine by inhibiting monoamine reuptake and thereby potentiating their effects.

Question 29

Drug of choice in pheocromocytoma?

Answer 29

Phenoxybenzamine - a nonselective noncompetetive alpha blocker that manage the hypertesive crisis that can be seen in pheocromocytoma.

Question 30

The only irreversible alpha blocker out there is …. ?

Answer 30

phenoxybezamine

Question 31

selective alpha1 blockers are primarily used in these to conditions?

Answer 31

hypertension & BPH

drugs would be prazosin, doxazosin, terazosin and tamsulosin

Question 32

Where do these two drugs work?

1 Yohimbine
2 Mirtazapine

Answer 32

1 Yohimbine is an alpha2 blocker
2 Mirtazapine is also an alpha2 blocker, frequently used in treating depression. Adverse effect with miratazapine is weight gain.

Question 33

Three conditions where you avoid betablockers?

Answer 33

1 Diabetes
2 Asthmatics
3 People with pripheral vascular diseases, esp. prinzmetals angina.

Question 34

Which beta blockers are beta1 selective?

Answer 34

All drugs that start with the letters A through M are beta1 selective.

Question 35

what beta blocker have the strongest sedative effect?

Answer 35

propranolol

Question 36

why add diuretics and beta blockers to patients recieving alpha1 blockers?

Answer 36

beta blockers to counter a reflex tachycardia

diuretics because of increased RAAS activity

Question 37

why are alpha blockers used in BPH?

Answer 37

symtomatic management of BPH by relaxing the trigone sphincter. A bonus is that the alpha blocker treat the comorbid condition of hypertension

Question 38

Three main places where beta1 receptors are located?

Answer 38

1 Heart
2 Kidney
3 Eye(aqueous humor production)

Question 39

What is the best drug to counter act a overdose of beta blockers?

Answer 39

Glucagon, due to the fact that glucagon interacts with Gs protein and increases intracellular cAMP.

Question 40

Beta blocker that do not have a sedative effect?

Answer 40

Atenolol

Question 41

The only beta blocker that can be used in thyrotoxicosis?

Answer 41

Propranolol, because it is the only beta blocker that inhibits deiodinase - conversion of T4 to T3

Question 42

Pilocarpine, echothiophate and timolol are all used to treat…. ?

Answer 42

Closed angle glaucoma. Pilocarpine and echothiophate are cholinomimetics that produce miosis, whereas timolol make beta1 blockade that reduce the production of aqueous humor.

Question 43

alpha1 selective agents: first dose precautions?

Answer 43

First dose should be small and taken right before bed, due to the fact that selective alpha1 blockers are associated with an exaggerated orthostatic hypotensive response(pooling of blood in the veins reduce the venous return).

Question 44

Three beta blockers with partial agonist activity(ISA)?

Answer 44

1 Acebutolol
2 Labetalol
3 Pindolol