Adrenergic Antagonists: Uses & Effects

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.ft043{font-size:18px;line-height:21px;font-family:CairoFont-2-0;color:#000000;} differences th ird  ge ne rat ion lipid soluble third generation of B blockers(non selective with aditional action) Adrenergic Antagonists Irreversible Reversible PhenoxyBenzamine toxicity mechnism of action  therapeutic use receptor antagonist phentolamine Tolazine Prazosine Terazosine a blocker postural hypotension and tachy cardia nasal congestion sedation, fatigue and headache antagonise both a1 and a2 receptor essential hypertension of pheochromocytoma Therapeutic Use mechnism of action  antagonise both a1 and a2 receptor toxicity postural hypotension nasal congestion headache Tachy cardia  Arrythmias in O2 >>myocardial ischemia inNE stimulate Histamine Hcl by acting on H2 receptor which cause peptic ulcer hypertensi on cri si s due to  pheochromocytoma abrupt wi thdrawal of cloni di ne upregulation of NE receptors  used in pulmonary hypertension in newborn infants with Respiratory Distress Syndrome it has high affinity to a1 receptor >>so produce less tachy cardia than phentolamine and phenoxybenzamine therapeutic uses side effects mild to moderate hypertension Congestive heart failure(as it shows relative absence of tachycardia) BPH>>Benign Prostatic Hyperblasia>>as it antagonise a1 receptor in sphicter of urianary bladder peripheral vascular diseases>>raynaud’s phenomenon prinzmetal Angina م ه م ي ن   ج د ا postural hypotension in the initial dose(first dose phenonmenon) after rapid increase in the dose after addition of another antihypertensive drug the same as prazosine but it is differnet in 3 items long duration of action 18h>>one dosw per day os enough has more bioviability less potent Mixed a and B blockers Labetalol Carvedilol B Blockers neuron blockers Guanithidine Reserbine inhibit Oxygen free raducals  used in essential hypertension(pheochromocytoma),and in hypertension during prenancy produce less tachy cardia used in treatment of hypertension selective a1 and non selective B so used in chronic heart failure mechanism of action  it crosses the nerve ,concentrate in the vesicles and replace NE,then NE is destructed by MAO enzyme >>so it inhibits its release pharmacokinetics onset 1-2 weeks duration(half life) s days and persists after stop of the therapy don’t cross the CNS(not lipid soluble) so No central effects like reserpine(nightmares,mental depression or sedation) therapeutic uses hypertension toxicity postural hypotenstion diarrhea compensatory sodium and water retention>>due to NE decrease mechanism of action  Toxicity  destroy storage vesicle and blocks ability of this vesicle to take up and store NE and Dpamine therapeutic uses hypertension CNS Effect (Sedation,nightmare mental depression) postural hypotension Extrapyremidal effect as parkinson’s disease >>>due to decrease  in Dopamine mild diarrhea, gastro intestinal cramps and increase in gastric Acid secretions  not used in peptic ulcer Generations used in chronic heart failure (with metoprolol>>second generation) increase Insulin effect inpatients with insulin resistence (prefered in diabetes) not used nowadays for treatment of hypertention due to its side effects and only used for refractory hypertension Refractory hypertension Prinzmetal Angina Classical Angina Selective B1 Blocker First generation (Non selective B Blockers) toxicity contradications Mechanism of action  Blocks B1 Blocks B2 vascular supply for active musles>>due to V.C vascular supply for Extremities >>peripheral vascular disease(Cold extremities)  contractility&excitability may cause haert failure heart rate(Brady Cardia) may be life threatining in patients with AV Block (partial or complete) AV Conduction prolonged antagonism up regulation of B receptors and increase its sensitivity has withdrawl symptoms therapeutic uses not used in bronchial athsma not used in prinzmetal angina not used alone in pheochromocytoma Heart heart failure >>>Exacerbate especialy in patients with compensated heart failure Brady cardia may be life threatining in patients with AV Block (partial or complete) Sudden Withdrawal effects tachy cardia&arrythmais Angina so withdrawal must be gradual over several weeks  bronchus bronchospasm in patients with bronchial asthma not normal patients hypo glycemia in diabetes as it CNS effects augments hypoglycemic effect of insulin and oral hypoglycemic mask signs of hypoglycemia vascular supply for active musles>>due to V.C vascular supply for Extremities >>peripheral vascular disease(Cold extremities)  Blocks B2 NE effect on ANS causes mental depression sleep disturbance sedation Drug Allergy rash and fever Heart Hypertension CNS Glaucoma ischemic heart diseases Obstructive hypertrophic cardiomyopathy dissecting aortic aneurysm chronic heart failure cardiac work heart rate with anti arrythmic action prolong survival of myocardial infarction patient myocardial O2 demand used in cardiac arrhythmais like supraventricular tachy cardia supra ventricular arrhythmais atrail fibrillation metoprolol carvidolol systolic pressure myocardial contraction by slowing heart rate primary hypertension pheo chromocytoma only given with a blockers if given alone it exaggerate the effect of catecholamines Hyper thyrodism portal hypertension diminish portal vein pressure in patients withb cirrhosis Essential tremors  Anxiety migrane and headache mechanism is UNKNOUN Propranolol low dose of Propranolol Blocks B receptors in part inhibits peripheral conversion of thyroxine to triiodothyronine(active form of thyroid hormone) as sympathetic activity may enhance the skeletal muscle tremor IOP >>by blockin B2 receptor in the ciliary Body of the eye thyroid hormone increase expression of B receptors Propranolol is used in anxiety and hyper throdism no block of B2 so no hypoglycemia (B2 is important in liver recovery from hypo glycemia) No peripheral vascular disease safer to use in patients with bronchial asthma therapeutic uses arrhythmais Hypertension angina pectoris EX: metoprolol,atenolol,esmolol Refractory Hypertension: blood pressure that remains uncontrolled in spite of maximal medical therapy (more than 5 antihypertensive drug) so we use prazosine as a blocker But b blockers cause coroonary spasm