Metoprolol is a cardioselective β1-adrenergic blocking agent used for acute myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. It may also be used for supraventricular and tachyarrhythmias and prophylaxis for migraine headaches. Metoprolol is structurally similar to bisoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At low doses, metoprolol selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Unlike propranolol and pindolol, metoprolol does not exhibit membrane-stabilizing or intrinsic sympathomimetic activity. Membrane-stabilizing effects are only observed at doses much higher than those needed for β-adrenergic blocking activity. Metoprolol possesses a single chiral centre and is administered as a racemic mixture. Film-coated tablet Peach coloured, round shaped [diameter 8.1 mm], film-coated tablets, debossed with 'C over 74' on one side and deep score line on the other side. Metoprolol tartrate is indicated in adults for: • Hypertension. • Tachycardiac arrhythmia, particularly supraventricular tachycardia. • Prevention of cardiac death and re-infarction after the acute phase of myocardial infarction. Combination therapy with another antihypertensive agent may also be considered to further reduce blood pressure. Patients with renal impairment The rate of elimination is insignificantly affected by renal function and therefore no dose adjustment is needed. This may be increased, if necessary, to 200 mg daily in single or divided doses. Patients with hepatic impairment Usually metoprolol can be given at the same dose to patients with cirrhosis of the liver as to patients with normal hepatic function. A dose reduction should only be considered when there are signs of severely impaired hepatic function (i.e. Elderly patients There are no adequate data from the use in patients above the age of 80. However, caution is advised in elderly patients as a fall in blood pressure or excessive bradycardia may have more pronounced effects. Paediatric population: There is limited data on the use of metoprolol in children and adolescents, therefore the use of Metoprolol tartrate is not recommended. - Hypersensitivity to metoprolol, other beta blockers or to any of the excipients listed in section 6.1. - Patients with unstable or acute decompensated heart failure (pulmonary oedema, hypoperfusion or hypotension), in which case continuous or periodical intravenous inotropic β receptor agonist therapy is indicated. - Manifest and clinically significant sinus bradycardia (heart frequency Beta blockers must be administered with caution to asthmatics.
When you get a new prescription, the first thing your doctor does (after choosing the drug) is decide on the dose. What most people don’t think about: Your doctor’s dosing decision is crucial—getting even slightly more of a medication than you need can greatly increase your risk for side effects. Correct dosing, however, can lessen (or even eliminate) side effects. Each year in the US, drug side effects are estimated to cause more than one million hospitalizations and more than 100,000 deaths. Yet many doctors reflexively prescribe “average” doses without checking recommendations for optimal dosing based on such factors as age, sex and body weight. For example, a 100-pound woman might be given the same dose as a 200-pound man…and a 75-year-old may be given the same dose as a healthy college student. It’s not hard to guess who is more likely to have preventable side effects. It is lipid soluble and has a high first pass hepatic metabolism resulting in the need for high oral doses (100-200 mg/day) compared to intravenous doses of 2.5 to 5 mg, titrated to effect. It is roughly half as potent as propranolol, and maximum β1-blockade effect is achieved at 0.2 mg/kg. Atenolol is also β1 selective, is lipophilic, and has an elimination half-life of 6 hours. Even so, the effect of an oral dose of 25 to 100 mg lasts 24 hours. In a recent study, perioperative blockade with atenolol resulted in a reduced short- and long-term mortality in high-risk patients having noncardiac surgery compared with , one of the most often-prescribed beta blockers, the role of CYP2D6 genetic polymorphisms in its pharmacokinetics seems to be well established. CYP2D6 catalyzes O-demethylation and, even more specifically, α-hydroxylation of the drug (On the basis of the considerable impact of the CYP2D6 polymorphism on the disposition of CYP2D6 substrates, it has often been suggested that CYP2D6 PM are more susceptible to adverse effects than EM at standard doses of Another beta blocker, the racemate carvedilol, which has been approved as an adjunctive therapy in the treatment of heart failure, is known to be stereoselectively metabolized by cytochrome P450 enzymes (). CYP2D6 polymorphism has been shown to alter the stereoselective disposition of carvedilol with PM demonstrating an impaired clearance of the R-enantiomer; thus, the PM were affected by a more pronounced α1-blockade, which might outweigh the beneficial β1-blocking effects ().
The maintenance dose is 100 mg of metoprolol tartrate twice a day in the. associated with bradycardia, hypotension and stroke including fatal outcome in. One of the biggest issues in managing high blood pressure is medication compliance. Would dying from an overdose of propranolol be painful. Can someone die of an overdose on ibuprofen?