3. Beta receptors are membrane bound G protein
coupled receptors which function primarily by increasing
or decreasing intracellular production of second
messenger cAMP.
4. 3 types:
Beta 1 receptors:
Beta 2 receptors:
Beta 3 receptors:
located on adipose
tissue.
5.
6. “PROPRANOLOL”
Pharmacokinetics:
• Well absorbed orally.
• Low bioavailibility due to high first pass metabolism
in liver.
• Lipophilic in nature so can penetrate into brain easily.
• Metabolism depend on hepatic blood flow.
• Bioavalability is increased when taken just after
meal.
7. Pharmacological actions:
Cardiovascular system:
Dec. heart rate-antianginal
Dec. force of contraction-antihypertensive
Membrane stabilizing action-antiarrhythmics
Reduces ill influence of NA on heart-
cardioprotective.
8. Blood vessels:
Blocks vasodilation and fall in BP evoked by
isoprenaline.
TPR initially increased (inhibition of vasodilation)-
little change in BP
On continue treatment resistant vessels gradually
adopt to chronically reduced CO-TPR dec.
Reduce NA release due to block of presynaptic
beta action
Dec. renin release from kidney
9. Respiratory system:
Blocking beta 2 in broncial smooth muscle can
cause life threating broncho-constriction in
asthmatics.
CNS:
Beside decreasing central sympathetic outflow
causes sedation litharge disturbance in sleep after
long term use.
Suppresses anxiety.
10. Metabolic effects:
In normal person it has min. effect on basal blood
glucose-long term use dec. insulin.
Hyperlipidemia-inc. VLDL,TG,CH,LDL.
Inhibits glycogenolysis in heart,skeletel muscle an in
liver
Skeletal muscle:
Inhibit adrenergically provoked tremor.
Fatigue-reduce blood flow.
Eye:
Dec. secretion of aqueous humor-dec. IOT.
11. Adverse effects:
Bradycardia
Plasma lipid is altered .
Worsens in asthama.
Impaired carbohydrate tolerance.
HTN
Angina-sudden death
Cold extremities
12. Drug interaction
digitalis,verapamil causes additive depression of
SA node and AV conduction leading to cardic
arrest.
Enzyme induces-phenytion,rifampicin, smoking
dec. its plasma conc.
Cimetidine and hydralazine may increase its
bioavalibility.
Warning signals of hypoglycemia mediated
through sympathatic stimulation is supressed-
hypoglucemic coma.
13. More potent in blocking Beta 1- cardiac receptors.
Pharmacokinetics:
Completely absorbed orally.
Do not cross BBB.
Daily dose is sufficient because of longer duration
of action.
Have low lipid solubility.
14. Use:
Atenolol is used in angina and the most
commonly used beta blocker for hypertension.
15. Intravenous
It has been used to terminate:
Peroximal supraventricular tachycardia.
Episodic atrial fibrillation
Adrenergically mediated arrhythmia
Arrhythmia during anaesthesia.
Intra operative,postoperative hypertension.
In early treatment of myocardial infarction.
16. Both alpha and beta blocker.
Given as an I.V bolus or infusion in hypertensive
emergencies.
Actions:
reduce BP.
Used in hypertensive emergency.
Does not alter serum lipid/blood glucose level,
does not cause reflex tachycardia.
Adverse effects:
Orthostatic, hypotension ,dizziness