adrenoceptor blockers

Question 1

 All active by
 Oral route
 Parenteral route

Answer 1

alpha blocking drugs

Question 2

IRREVERSIBLE LONG-ACTING

	Prototype
	Only slightly alpha1 selective
	Short elimination half life
	Long duration of action (48 hours)
	Binds covalently to the alpha receptors

Answer 2

PHENOXYBENZAMINE

Question 3

DoA of PHENOXYBENZAMINE

Answer 3

48 hours)

Question 4

REVERSIBLE SHORT-ACTING

•	Prototype
•	Nonselective (alpha1=alpha2)
	Duration of action
	Oral (2-4 hours)
	IV (20-40 minutes)

Answer 4

PHENTOLAMINE

Question 5

ALPHA1 SELECTIVE

 Prototype
 Selective reversible alpha1 blocker
 Duration of action 8-24 hours
 Doxasozin, terazosin and tamsulosin

Answer 5

PRAZOSIN

Question 6

• Prototype
• Selective alpha2 competitive blockers
• Used primarily in research application

Answer 6

YOHIMBINE, RAUWOLSCINE

Question 7

NONSELECTIVE BLOCKERS

 Most important effects are on the ??

Answer 7

CVS system

Question 8

 Predictable result of the use of an agonist in a patient who has received
an alpha-blocker
 Reversal in the BP effect of large doses of epinephrine
 From pressor response (alpha receptors) to a depressor response (beta receptors)
 Not observed with phenylephrine or NE because they lack sufficient beta2 effects

Answer 8

EPINEPHRINE REVERSAL

Question 9

 Block alpha1 receptors much more effectively

 Cause much less tachycardia than the nonselective blockers when reducing BP

Answer 9

SELECTIVE ALPHA1 BLOCKERS

Question 10

• Tumor that secretes cathecolamines

Answer 10

pheochromocytoma

Question 11

type of BLOCKERS

• Severe hypertension caused by overdose with drugs of abuse such as amphetamine, cocaine, or phenylpropanolamine

Answer 11

NONSELECTIVE ALPHA

Question 12

type of BLOCKERS
 Prazosin, doxazosin, and terazosin are used in hypertension
 Used together with tamsulosin for urinary hesitancy and prevention of urinary retention with benign prostatic hyperplasia

Answer 12

SELECTIVE ALPHA

Question 13

Prazosin, doxazosin, and terazosin Used together with ? for urinary hesitancy and prevention of urinary retention with benign prostatic hyperplasia

Answer 13

tamsulosin

Question 14

• TOXICITY of alpha blockers

•

Answer 14

Main manifestation is orthostatic hypotension

Question 15

 Competitive pharmacologic antagonists
 Propranolol is the prototype
 Developed for chronic oral use
• Bioavailability and duration of action vary widely

Answer 15

BETA BLOCKING DRUGS

Question 16

Beta1 receptor selectivity

Answer 16

Acebutolol
Atenolol
Esmolol
Metoprolol

Question 17

Advantage when treating patients with asthma

Answer 17

Beta1 receptor selectivity

PARTIAL AGONIST ACTIVITY

Question 18

Nonselective beta-blockers

Answer 18

 Nadolol
 Propranolol
 Timolol
 Pindolol

Question 19

 Combined alpha and beta-blockers
 Optically active


Answer 19

Labetalol

 Carvedilol

Question 20

PARTIAL AGONIST ACTIVITY
 ”Intrinsic sympathomimetic activity”

 May be an advantage in treating patients with asthma
 At maximum dose, can cause some bronchodilatation

Answer 20

Pindolol
 Acebutolol
 Labetalol

Question 21

 ”Membrane stabilizing ability”
 Disadvantage when a beta-blocker is used topically in the eye because it decreases protective reflexes and increases the risk of corneal ulceration

Answer 21

LOCAL ANESTHETIC ACTIVITY

Question 22

LOCAL ANESTHETIC ACTIVITY

Answer 22

	Acebutolol
	Labetalol
	Metoprolol
	Propranolol 	
	Pindolol

Question 23

• Short-acting ester

* Used only parenterally

Answer 23

ESMOLOL

Question 24

4. Longest acting beta-blocker

Answer 24

NADOLOL

Question 25

 Less lipid soluble |  Enter the CNS to a lesser extent

Answer 25

ACEBUTOLOL, ATENOLOL and NADOLOL

Question 26

 EFFECTS of beta blockers in CVS

Answer 26

 Decrease BP  Antagonize renin secretion  (-) inotropic effect  (-) chronotropic effect

Question 27

 EFFECTS of beta blockers in RESPIRATORY

Answer 27

Bronchoconstriction | Increase airway resistance

Question 28

EFFECTS of beta blockers in EYE

Answer 28

* Decrease intraocular pressure | * Decrease production of aqueous humor

Question 29

EFFECTS of beta blockers inMETABOLIC AND ENDOCRINE

Answer 29

* Reduce insulin secretion | * Caution for insulin dependent DM

Question 30

 CLINICAL USES of beta blockers

Answer 30

```  Open-angle glaucoma  Hypertension  Angina • Arrhythmias • Chronic heart failure • Pheochromocytoma ```

Question 31

TOXICITY in CVS

Answer 31

1. CVS 1. Bradycardia 2. AV blockade 3. Heart failure

Question 32

TOXICITY in RESPIRATORY

Answer 32

1. Worsen the asthma

Question 33

TOXICITY in CNS

Answer 33

1. Sedation 2. Fatigue 3. Sleep alteration 4. Depression 5. Psychosis

Question 34

TOXICITY in CNS

Answer 34

1. Sedation 2. Fatigue 3. Sleep alteration 4. Depression 5. Psychosis

Question 35

Conversion of the pressor response to epinephrine (typical of large doses) to a blood pressure–lowering effect; caused by α blockers, which unmask the β2 effects of epinephrine

Answer 35

Epinephrine reversal

Question 36

Partial agonist action by adrenoceptor blockers; typical of several β blockers (eg, pindolol, acebutolol)

Answer 36

Intrinsic sympathomimetic | activity (ISA)

Question 37

Local anesthetic action; typical of several β blockers (eg, propranolol)

Answer 37

Membrane-stabilizing | activity (MSA)

Question 38

Hypotension that is most marked in the upright position; caused by venous pooling (typical of α blockade) or inadequate blood volume (caused by blood loss or excessive diuresis)

Answer 38

Orthostatic hypotension

Question 39

A tumor consisting of cells that release varying amounts of norepinephrine and epinephrine into the circulation

Answer 39

Pheochromocytoma

Question 40

Drugs used in glaucoma. | Beta blockers

Answer 40

Timolol, others

Question 41

Drugs used in glaucoma | Prostaglandins

Answer 41

Latanoprost, others

Question 42

Drugs used in glaucoma. | Cholinomimetics

Answer 42

Pilocarpine, physostigmine

Question 43

Drugs used in glaucoma. Alpha agonists Nonselective:

Answer 43

epinephrine

Question 44

Drugs used in glaucoma. | Alpha2-selective agonists

Answer 44

Apraclonidine, brimonidine

Question 45

Drugs used in glaucoma. | Carbonic anhydrase inhibitors

Answer 45

Acetazolamide, dorzolamide

Question 46

Drugs used in glaucoma. | Osmotic agents

Answer 46

Mannitol

Question 47

Clinical Applications | Pheochromocytoma, antidote to overdoseof α agonists

Answer 47

Phentolamine

Question 48

Clinical Applications Pheochromocytoma, carcinoid, mastocytosis, Raynaud’s phenomenon

Answer 48

phenoxybenzamine

Question 49

Clinical Applications Hypertension, benign prostatic hyperplasia

Answer 49

PRAZOSIN

Question 50

Clinical Applications Obsolete use for erectile dysfunction • research use

Answer 50

YOHIMBINE

Question 51

``` Clinical Applications Angina, arrhythmias (treatment and prophylaxis), hypertension, thyrotoxicosis, tremor, stage fright, migraine ```

Answer 51

PROPRANOLOL