Beta Adrenergic Blockers

Also known as sympatholytic drugs. They produce competitive antagonism

of beta-adrenoceptors in the autonomic nervous system. This prevents the
“flight or fight” response induced by adrenaline and noradrenaline.

MODE OF ACTION:
LOWERS MYOCARDIAL OXYGEN DEMAND BY

A. REDUCING HEART RATE

B. REDUCING BLOOD PRESSURE
C. REDUCING MYOCARDIAL CONTRACTILITY
 Types

• There are three main sub-types of beta-adrenoceptors:

• Beta1-adrenoceptors (75%) are located in the heart (selective)

• Beta 2-adrenoceptors are located in vascular and bronchial smooth
muscle
• Beta 3-adrenoceptors are located on adipocytes and are thought to be
involved with fatty acid metabolism
 Classification
Non Selective act both on beta 1 and beta 2 adrenergic receptors.
• Propranolol, sotalol, timolol, pindolol, labetalol,carvedolol (1st
generation)
Selective that act only on Beta 1
 Metoprolol, atenolol, bisoprolol, acebutolol (2nd generation)
 3rd generation having alpha blocking activity
Pharmacokinetics
• Absorption
• Most of the drugs in this class are well absorbed after oral
administration; peak concentrations occur 1–3 hours after ingestion.
• Sustained-release preparations of propranolol and metoprolol are
available
• Distribution and Clearance
• The β antagonists are rapidly distributed and have large volumes of
distribution. Propranolol and penbutolol are quite lipophilic and readily
cross the blood-brain barrier. Most β antagonists have half-lives in the
range of 3–10 hours.
Pharmacodynamics of the Beta-Receptor
Antagonist Drugs
• Effects on the Cardiovascular System
• Beta-blocking drugs given chronically lower blood pressure in patients
with hypertension. The mechanisms involved are not fully understood
but probably include suppression of renin release and effects in the
CNS. These drugs do not usually cause hypotension in healthy
individuals with normal blood pressure. So it is useful
• Angina
• Myocardial infarction
• chronic heart failure
Effects on the Respiratory Tract
• Blockade of the β2 receptors in bronchial smooth muscle may lead to
an increase in airway resistance, particularly in patients with asthma.
Consequently, these drugs should generally be avoided in patients with
asthma.
Effects on the Eye
• Beta-blocking agents reduce intraocular pressure, especially in
glaucoma. The mechanism usually reported is decreased aqueous
humor production
Metabolic and Endocrine Effects

• Beta-receptor antagonists such as propranolol inhibit sympathetic

nervous system stimulation of lipolysis.

• glycogenolysis in the human liver is at least partially inhibited after

β2-receptor blockade. Glucagon is the primary hormone used to
combat hypoglycemia so they should be used with caution in insulin-
dependent diabetic patients.
• The chronic use of β-adrenoceptor antagonists has been associated with
increased plasma concentrations of very-low-density lipoproteins (VLDL)
and decreased concentrations of HDL cholesterol. Both of these changes
are potentially unfavorable in terms of risk of cardiovascular disease

• Effects Not Related to Beta-Blockade

• Local anesthetic action, also known as “membrane-stabilizing” action, is a

prominent effect of several β blockers. This action is the result of typical
local anesthetic blockade of sodium channels.
CLINICAL PHARMACOLOGY OF THE BETA-
RECEPTOR–BLOCKING DRUGS
• Hypertension
• The β-adrenoceptor–blocking drugs have proved to be effective and
well tolerated in hypertension
• Ischemic Heart Disease
• Beta-adrenoceptor blockers reduce the frequency of anginal episodes
and improve exercise tolerance in many patients with angina These
actions are due to blockade of cardiac β receptors, resulting in
decreased cardiac work and reduction in oxygen demand.
• Cardiac Arrhythmias
• Beta antagonists are often effective in the treatment of both
supraventricular and ventricular arrhythmias

• Hyperthyroidism
• Excessive catecholamine action is an important aspect of the
pathophysiology of hyperthyroidism, especially in relation to the
heart. The β antagonists are beneficial in this condition. Propranolol
has been used extensively in patients with thyroid storm (severe
hyperthyroidism
 Neurologic Diseases
• Propranolol reduces the frequency and intensity of migraine
headache. Other β-receptor antagonists with preventive efficacy
include metoprolol and probably also atenolol, timolol, and nadolol.
The mechanism is not known.
• Since sympathetic activity may enhance skeletal muscle tremor, so β
antagonists have been found to reduce certain tremors
• The somatic manifestations of anxiety may respond dramatically to
low doses of propranolol, particularly when taken prophylactically.
For example, benefit has been found in musicians with performance
anxiety (“stage fright”).
• Propranolol may contribute to the symptomatic treatment of alcohol
withdrawal in some patients.
Adverse effects
• Bradycardia
• CNS effects include mild sedation, vivid dreams, and rarely,
depression
• Discontinuing the use of β blockers in any patient who develops
psychiatric depression should be seriously considered if clinically
feasible.