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  Timolol

Pharmacokinetics | Indications | Routes of Administration and Dosage | Contra Indications | Precautions | Interactions


Systems Cardiovascular and Peripheral Vascular System
Category Non selective B-blocker


Pharmacokinetics

It is well absorbed after oral administration, extensively metabolised in the liver with little unchanged drug appearing in the urine. Its bioavailability is 50%.



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Indications

Timolol is used in the treatment of hypertension, to relieve angina and in IHD patients to help prevent additional Myocardial Infarction, to correct cardiac arrhythmias, in hyperthyroidism. It has a membrane stabilising effect in large doses. It causes decreased automaticity, conduction velocity and increases the refractory period to nerve impulses in nerve conduction. As a result, they decrease the heart's need for blood and oxygen by reducing its workload. They also help to maintain the cardiac rhythm.



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Routes of Administration and Dosage

Oral dosage (tablets): For hypertension: Adults: 10 mg two times a day. It can be increased upto 60 mg per day taken as a single dose or in divided doses. For treatment after a MI: Adults: 10 mg two times a day. For preventing migraine headaches: Adults : 10 mg two times a day. It may be increased upto 30 mg once a day or in divided doses.



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Contra Indications

Timolol is contraindicated in Sinus bradycardia, heart blocks, untreated cardiac failure, cardiogenic shock, severe arterial disorder, hypoglycaemia, severe haemorrhage and asthma.



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Precautions

Precaution should be taken during abrupt reduction in dosage, pregnancy, lactation, elderly, IHD,CCF, renal or hepatic dysfunction.



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Interactions

It may increase the risk of serious allergic reaction to these drugs: Aminophylline, Caffeine, Oxitriphylline, Theophylline: the effects of both these drugs and beta-blockers may be reduced; in addition, theophylline levels in the body may be increased, especially in patients who smoke. Oral antidiabetics or Insulin: There is an increased risk of hyperglycemia ; beta-blockers may cover up certain symptoms of hypoglycemia such as increases in pulse rate and blood pressure, and may make the hypoglycemia last longer. Calcium channel blockers: bepridil, diltiazem, felodipine, flunarizine, isradipine, nicardipine, nifedipine, nimodipine, verapamil, clonidine, guanabenz : Effects on blood pressure may be increased. Adverse effects may occur if clonidine, guanabenz, or a beta-blocker is stopped suddenly after use together. Adverse cardiac effects may occur when beta-blockers are used with calcium channel blockers. Cocaine : Cocaine may block the effects of beta-blockers; in addition, there is an increased risk of Hypertension, tachcardia, and possibly cardiac disorders if cocaine is used while taking a beta-blocker. With Monoamine oxidase (MAO) inhibitors: Taking beta-blockers within 2 weeks of taking monoamine oxidase (MAO) inhibitors may cause severe hypertension.



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Pharmacokinetics | Indications | Routes of Administration and Dosage | Contra Indications | Precautions | Interactions

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