Drugs competitively block adrenergic receptors

Relative

affinity for 1 and / or 2 receptors Some of them have ' Intrinsic sympathomimetic activity ISA

Some

have membrane stabilizing effect ( LA or quinidine like effect ) Some have high lipid solubility; with central depressant effect

Non selective
Propranolol Pindolol

Selective 1

B-blockers

Atenolol Metoprolol

Combined & blocker

labetalol &carvedilol

B-blockers

Lipophilic

Hydrophilic

Lipophylic
oral absorption Complete

Hydrophilic
Irregular

Liver metabolism
T 1/2

Yes
Short

No
Long

CNS side effects

High

low

Lipophylic
Propranolol Timolol

Hydrophilic
Atenolol Acebutalol

Labetalol Carvedilol

The

prototype of beta blockers. It has equal affinity for 1 & 2 It has NO ISA . It possess local anesthetic action

Heart
- ve chronotropic , - ve inotropic - ve dromotropic COP, work & O2 consumption. automatcity & excitability

vasoconstriction ( B2 blocking)
blood supply to organs

1. COP (1- blocking effect). 2. Block rennin release, so Ag II & aldosteron (1- effect). 3. NE release from Nerve terminals. 4. central sympathetic outflow. 5.Ressetting of baroreceptor

Bronchoconstriction in susceptible patients (2- blocking effect).

Hypoglycemia due to decrease both glycogenolysis & glucagon secretion 2. Inhibit lipolysis 3. Sodium retention : BP in renal perfusion Na+ retention& plasma volume.
1.

Propranolol depresses CNS reduce tremors due to anxiety

1. Hypertension.

2. Angina pectoris 3. Cardiac arrhythmia. 4. Myocardial infarction 5. Hyperthyrodism

6. Open-angle Glaucoma (chronic): Timolol 7. Prophylaxis of Migraine headache 8. Management of familial tremors & anxiety 9. Pheochromocytoma with -blockers (never alone)

1-Block of cardiac 1-receptors:

-ve

inotropic heart failure (treated by digitalis). -ve chronotropic bradycardia (Treated by atropine). -ve dromotropic heart failure. Hypotension.

2. Blockade of 2: Bronchospasm and asthma. Hypoglycemia (symptomless hypoglycemic coma). Vasoconstriction (cold extremities). Coronary vasoconstriction.

Exacerbates angina, tachycardia, may lead to arrhythmias Rebound hypertension. .

 Bronchial asthma. Type I diabetes mellitus. Peripheral vascular disease.

Heart block, severe HF, massive MI.

Drug interactions
Pharmacokinetic Pharmacodynamic Interactions Interactions 1. Hepatic enzyme 1. Anti-diabetic drugs inhibitors as: e.g. insulin. cimetidine & isoniazid 2. Hepatic enzyme 2. Verapamil (calcium inducers as: channel blocker) barbiturates, phenytoin, & rifampin 3. Non-steroidal antiinflammatory drugs

Drugs

Selectivity

PA activity

LA activity

Lipid solubility

T (h)

Propranolol Pindolol

1 , 2 1 , 2

+ Weak

High Moderate

4-6 3-4

Atenolol Acebutalol

1 1

Low Low

6-9 3-4

Labetalol
Carvedilol

1, 1
1 , 1

+
-

+
-

Moderate
Moderate

5
6-8