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FIRAS MOHAMMED ALI 1ST GRP

DEFINITION- Those pharmacological substance that inhbit the action of adrenergic recetors r called adr.antagonist TYPES- They are of 2 types of alpha and beta blockers Alpha blockers r more specifically divided into alpha1 and alpha 2 Beta blockers r divided into nonspecific, beta1, beta2, beta3 selective drugs

GENRAL EFFECTS OF THE DRUG Alpha receptor causes lowering of peripheral vasucular resistance and blood pressure. They also cause orthostatic hypotension and reflex tachycardia. Hypotension is due to antagonism of symapathetic activity. OTHER EFFECTS- In eye alpha receptor blocker elicits miosis. Alpha 1 receptor tat r in base of bladder, blocks and decrease the resistance to the flow of urine.

PHENOXYBENZENE- It binds covelently to alpha recertor causing irreversible blockade. This drug inhibits the action of norepinephrine reuptake and blocks histamine, acetylcholine and serotonin receptors. It causes fall in blood pressure, wen symphatetic tone is high. It is given orally. PHENATOLAMINE It is a potent competitive antagonist at both alpha 1 aplha 2 recetors. It reduces per. Resistance through blockade

of alpha 1 receptors and possibly alpha 2 receptors on vasucular smooth muscle. Its cardiac stimulation is due to antangonism of presynaptic alpha 2 receptors and symphathetic activation from baroflex mechanisms. It has minor inhibitory effects at seratonin receptors and agonist at muscarinic and H1 and H2 receptors. PRAZOSIN-its highly selective for alpha 1 recptor its relaxes arterial and venous vascular smooth muscle,and smooth muslce of prostate,due to blockage of alpha 1 receptor.its given by oral admistration and 50% of drug is metaboliged.the half life is noramally 3 hours.

TERAZOSIN its reversible alpha 1 selective antagonist.its has high bioavability.bt its extensively metaboliged in liver,with only samll fraction of unchanged drug exreated in urine.its effective in hypertension,also approved for use in men with urinary symptoms due to benign a prostatic hyperplasia.the half of terazosin is 9 to 12 hours. DOXAZOSIN-its has moderate bioavability and extensivly metaboliged with very littekl parent drug excreated in urine.it is more efficacious in treatment of hypertension and BPH.the half life is 22 hours.

TAMSULOSIN-It is competitive alpha 1 antagonist. It has high bioavailibility and half life of 9-15 hrs. It has greater potency in inhibiting contraction in prostate smooth muscle. ALFUZOSIN - It is alpha 1 selective quinazoline derivative that is uesd for BPH. It has bioavailibility of 60% and half life of 5hrs YOHIMBINE It is indole alkaloid apha 2 selective antagonist . It is sometimes used in teatment of orthostatic hypertension because it promotes n.epinephrine release through blockade of pressynaptica alpha 1 receptors.

Phenoxybenzene is used in treatment of pheochromocytoma. Alpha receptor antagonist are useful in preoperative management of this disease. Alpha receptor antagonists have limited management in hypertensive emergencies. Members of prazosin family alpha 1 selective antagonist are useful n mild to moderate systemic hypertension. Individuals with raynauds phenomenon and other conditions involving reversible vasospasm benefit from drugs prazosin and phenoxybenzene.

Prazosin and doxazosin, terazosin are all eficacious with patients of BPH, and also with patients with hypertension. Drug combination of phentoalmine with smooth muscle relaxants are injected directly into penis with patients of erectile dysfunction. Alpha 2 antagonists are given for treatment of physiatric depression.

Beta receptor antagonist drugs are categorized in nonselective, selective. Nonselective blocks all beta receptors. Beta blocking drugs lower blood pressure in patients with hypertension. They are very valuable in treating of angina and chronic heart failure. Beta 1 blocking drugs antagonize release of renin caused by symphathetic nervous system. Beta blocking drugs reduces intraocular pressure especially in glaucoma.

PREPRANOLOL It is ptototypical beta blocing nonselective drug. It has negligible effects on alpha and muscarinic receptors. It diminishes cardiac output resluting in ve inotropic and chronotropic effects. It is used with diuretic to prevent Na+ retention. It is administered carefully with insulin-dependant diabetic patients. It is contraindicated in patients with asthama bcoz blocking of beta receptors in bronchioles can lead to contraction of smooth muscle.

METAPROLOL,ATENOLOL- They are members of beta 1 selective drug. These drugs are safer in pateints who experince bronchioconstriction in response to propranlol. However in patients like COPD, the benefits may exceeds the risk, eg in in patients with myocardial infarction. NADOLOL,TIMLOL,LEVOBUNOLOL- They r all members of nonselective drugs, have very long duration of action. It has excellent ocular hypotensive effects when administerd topically in eye for eg treatment of open angle glaucoma.

LABETALOL- It is reversible beta blocker with concurrent alpha 1 blocking actions. It is useful in treatment with hypertensive patients in whom increased peripheral resistance is undesirable(in old men) PINDLOL,ACEBUTOLOL,CARTEOID- They members of partial beta agonist. They are effective in major cardiovascular applications of eta blocking group. They are less likely to cause badycardia and abnrmalities in plasma lipids than other antagonists. Pindolol,perhaps as a result of actions on cerotonin signaling,may protenciatiot actoin of traditional anti depressent medications. Celiprolol is a beta one selective antagonist with a modest capacity to activate beta to receptors.

CARVEDILOL,BUCINDOLOL-they are members of non selecive beta recptors antagonist with capacity to block alpha one receptors. Carwedilol antagonizes actions of catacolomines more potentely at beta receptors then at alpha one receptors. The drugs have half life of 6-8hrs. Carvedilol inhibits vascular smooth muscles mitogenesis indipendently of adrinoreceptor block age. These drugs also clinically benefits in chronic heart failiure.

The beta adrinoceptor blocking drugs have prove to be affective in hypertension. The drug is oftn used with either a dieuretic or a vasodilator. Labetalol a competative alpha and beta antagonist is a effective in hypertension. Beta adrinoceptor blockers reduce the frequency of anginal episodes and emproved execise tollerence in pations with angina. These actions relate to blockage of cardiac beta receptor resulting in decrease cardiac work and reduction in oxygen demand

Multiple large scale prospective studies indicate that long term use of timolol,propranolol,metoprolol in patienc who have had a myocardial infarction prolongs survival. In additions these antagonist are strongly indiacted in a cute face of myocardial infarction. They are often effective in treatment of both suprave ntricular and ventricular arrhythmias,by increasing atriovetricular nodal refractoryperiod,beta antagonist slow ventricular response in atrial flutter and fibrilations. These drugs can also reduce ventricular ectopic beats.

Beta receptors antagonist have been found to increase stroke volume in patience ith obstructive cardiomayopathy. They are also useful in desecting aortic aneurysm to decrease the rate of development of cistolic pressure. Beta antagonist are benefecient in treatment of hyperthyroidism. Propranalol hav been used in patience with thyroied storm.

Bradycardia is the most common adverse effect of beta blocking drugs. Some patience report coolness of hand and feet in winter. Central nervous system effect include mild sedation,vived dreams and rarely depression.
Patients with ischemic heart disease and renovascular hypertension may at increase risk if beta blockage is suddenly intruppted due to involment of up regulation of no of beta receptors.

Beta to receptor blockage associated with non selective agents causes worsening of preexsisting asthama and other form of airway obstructions without having these coniquences in normal individual. Beta receptor blockage depresses mayocrdial contactality and excitibility.

What is glaucoma? It is a major cause of blindness,the primary manifetation is increased intraoccular pressure not associated with symptons. Without treatment increased intraoccular pressure results in damage to retina and optic nerve. Types of glaucomaThere are two types of glaucoma open angle form and closed angle. Closed angle form is associated with shallow anterior chamber,

in which a dilated iris can occlude the outflow dranage pathway at an angle the cornia and ciliary body. This form is associted with accute pain, which must be controlled by surgical removal of part of iris. The open angle form is a chrnic condition and tretment is largely pharmacological. Treatment of open angle is done by protaglandins analogs and beta blockers.

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