Metoprolol (Tartrate)

Metoprolol (Tartrate) is a cardioselective β-blocking agent with intrinsic sympathomimetic activity. Metoprolol (Tartrate) is approximately equipotent to propranolol in inhibiting β1 receptors such as those in heart but 50 to 100 fold less potent than propranolol in blocking β2 receptors. Drugs that blocks the β1 receptor have been developed to eliminate the unwanted bronchoconstrictor effects (β2) of propranolol seen among the asthmatic patients. Metoprolol antagonizes β1 receptors at doses 50 to 100 times less than those required to block β2 receptors. This cardioselectivty is more pronounced at low doses and is lost at high doses. It lowers the blood pressure in hypertension. It slows the heart rate. Metoprolol (Tartrate) is prepared by chemical synthesis and the racemate is used clinically. Metoprolol (Tartrate) is adminsitered orally and intravenously.

Brands

MEROL-XL MEROL-XL MEROL MEROL MEROL MEROL BETALOC-ZOK METOCARD METSU XL REFIT LOPRESOR MEPRESOR MEPRESOR MEPRESOR MEPROL TOPROL AKSOPRESSOR METOLOL CARSEL CARSEL CARSEL CARSEL CARSEL PLUS CARSEL PLUS METCARD METOSCOT FYNKARD MEGATOP METAPRESSOR

Adult Dose

Dose: 5 mg
Single Dose: 5 (5)
Frequency: As recommended.
Route: IV
Instructions: For Cardiac Arrythmia rate is 2mg/min may be repeated at intervals of 5 min to a total dose of 10-15 mg .Maintainence therapy dose should not exceed than 50 mg (PO) given 3 times a day ,4 to 6 hrz after IV therapy

Neonatal

Paedriatic

Dose: 2.5 to 4 mg/kg
Single Dose: 3.2 (3.25)
Frequency: 12 hourly
Route: Oral
Instructions: -

Characteristics

. It is of Synthetic origin and belongs to Amino propanolol. It belongs to Beta-1 adrenergic antagonist pharmacological group on the basis of mechanism of action and also classified in Beta Blocker, Beta1 Selective pharmacological group.The Molecular Weight of Metoprolol (Tartrate) is 684.80. Its pKa is 9.5.

Contraindications

Metoprolol (Tartrate) is contraindicated in conditions like Cardiogenic shock,Bradycardia,Atrioventricular block,Refractory heart failure.

Effects

The severe or irreversible adverse effects of Metoprolol (Tartrate), which give rise to further complications include Agranulocytosis, Hyperglycemia, Severe bradycardia.Metoprolol (Tartrate) produces potentially life-threatening effects which include Myocardial depression. which are responsible for the discontinuation of Metoprolol (Tartrate) therapy.The signs and symptoms that are produced after the acute overdosage of Metoprolol (Tartrate) include Bradycardia, Hypotension.The symptomatic adverse reactions produced by Metoprolol (Tartrate) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Fatigue, Nausea, Vomiting, Alopecia, Diarrhea, Dyspnea, Pruritus, GI upset, Elevation of liver enzymes, Hyperpigmentation, Sleep pattern disturbances, Lassitude, Musculoskeletal pain, Xerosis, Extremities coolness.

Indications

Metoprolol (Tartrate) is primarily indicated in conditions like Angina, Cardiac arrhythmia, Hypertension, Hyperthyroidism (adjunct), Maintenance of recurrent duodenal ulcers, Migraine prophylaxis, Myocardial infarction, Prevention of relapse in duodenal ulcer, Severe or recurrent duodenal and gastric ulcertion, Surgery, To prevent recurrence of neural tube defect, and can also be given in adjunctive therapy as an alternative drug of choice in Thyrotoxicosis.

Interactions

Metoprolol (Tartrate) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlprazolamAmiodarone (HCl)Amiodarone inhibit first pass hepatic metabolism of metoprolol leads to bradycardia,cardiac arrest and ventricular fibrillation due to additive slowing in AV conduction.ModerateCheck for patient response and hemodynamic ststus is advised.AspirinHigh doses of salicylates alter the antihypertensive effect of beta-blockers by inhibiting the synthesis of prostaglandinMinorMonitor the altered antihypertensive response whenever salicylate is introduced or discontinued.BenorylateCholine Magnesium TrisalicylateCimetidine (HCl)Cimetidine inhibit hepatic CYP450 and/or renal tubular secretion thus increases plasma concentration of metoprolol.ModeratePatient response and tolerance should be monitor.Clonidine (HCl)Metoprolol may enhance the rebound hypertensive effect of Clonidine (HCl).This effect can occur when the Clonidine Hcl is abruptly withdrawn. ModerateIf possible, withdraw metoprolol several days before slowly withdrawing. clonidine. Consider the use of labetalol in place of clonidine, as it has both alpha- and beta-blocking activity. Use a cardioselective beta-blocker (such should pose less risk than nonselective agents). Monitor closely for acute rise in blood pressure.Clorazepate (K)Both agents acts additively thus increases hypotensive and/or CNS depressant effects.ModerateClosely monitor for hypotension and excessive or prolonged CNS depression.Dexamphetamine (Sulphate)Diltiazem (HCl)Diltiazem may enhance the hypotensive effect of metoprolol. Bradycardia and signs of heart failure have also been reported.Diltiazem may decrease the metabolism, via CYP isoenzymes, of metoprolol.ModerateThough usually safe and effective during concomitant use, monitor bradycardia, hypotension, or signs of heart failure during concomitant use of Metoprolol and Diltiazem. phthalmic beta-blockers are of little concern.DiphenhydramineFluoxetine (HCl)Fluoxetin may potentiate the pharmacological effect of metoprolol by inhibiting metabolic clearence result in development of bradycardia, hypotension, and complete heart block.ModerateClosely monitor the cardiac function of patient and adjust the dose of metoprolol accordingly.Fluvoxamine (Maleate)Fluvoxamine may potentiate the pharmacological effect of metoprolol by inhibiting metabolic clearence result in development of bradycardia, hypotension, and complete heart block.ModerateClosely monitor the cardiac function of patient and adjust the dose of metoprolol accordingly.IndomethacinIndomethacin may attenuate the anihypertensive effect of metoprolol by inhibiting renal prostaglandin synthesis.ModerateClosely monitor for altered antihypertensive response.Insulin Lispro ProtamineIoxaglateLimited data suggest that patients receiving beta blockers may have an increased risk of severe hypotensive and/or hypersensitivity reactions to parenteral iodinated contrast media. In addition, the treatment of allergic/anaphylactoid reactions in these patients may be more difficult. The mechanism is unknown.ModeratePatients who have received beta blockers should be closely monitored for adverse reactions to iodinated contrast media. If anaphylaxis occurs, clinicians should be aware that beta blockers may attenuate the response to epinephrine. Thus, larger doses of epinephrine may be necessary to overcome the bronchospasm, although such large doses can also cause excessive alpha adrenergic stimulation resulting in hypertension, reflex bradycardia, heart block, and possible potentiation of bronchospasm. Alternative treatments recommended include vigorous supportive care (e.g., fluids) and the use of parenteral beta agonists for bronchospasm and norepinephrine for hypotension.Metformin (HCl)Metoprolol increases the hypoglycemic effect by inhibiting hepatic glycogenolysis and insulin secretion.ModerateClosely monitor the blood glucose level on regular basis.Mibefradil (Di HCl)NaproxenNaproxen may attenuate the anihypertensive effect of metoprolol by inhibiting renal prostaglandin synthesis.ModerateClosely monitor for altered antihypertensive response.NifedipineCombined use of metoprolol with nifedipine decrease the rate, conduction and contractility of heart particularly in patients of ventricular or conduction abnormalities.by decreasing peripheral vascular resistance.ModerateDosage regimen should be adjusted accordingly. Closely monitor the hemodynamic effect and tolerance of patient.NitroprussideShould not be use concurrently without doctor or pharmacist approval.Pentobarbitone (Na)Propafenone (HCl)Combined use of both drugs increases Plasma conc of former agentPropoxyphenePropoxyphene increases the serum level of metoprolol by inhibiting CYP450 2D6 first-pass metabolism and decreasing hepatic clearence.ModerateReduce the dose of metoprolol. Closely monitor for hypotension, heart failure, brady cardia, arrythmia and mental status.PropylthiouracilHyperthyroidism may cause an increased clearance of beta blockers with a high extraction ratio. A dose reduction of beta-adrenergic blockers may be needed when a hyperthyroid patient becomes euthyroid.QuinidineQuinidine increases the serum level of metoprolol by inhibiting first-pass metabolism and by decreasing hepatic clearence.Quinidine and metoprolol have negative inotropic effect on heart so this combination may become beneficial when used to treat atrial fbrillation.ModerateClosely monitor for orthostatic hypotension, cardiac arrythmia, bradycardia and heart failure. Dose of metoprolol should be decreased accordingly.RanolazineRanolazine 750 mg twice daily increased the plasma concentrations of a single dose of immediate-release metoprolol (100 mg), a CYP2D6 substrate, by 1.8-fold. The exposure to other CYP2D6 substrates, such as tricyclic antidepressants and antipsychotics, may be increased during coadministration with ranolazine, and lower doses of these drugs may be requiredSertraline (HCl)Sertraline may potentiate the pharmacological effect of metoprolol by inhibiting metabolic clearence result in development of bradycardia, hypotension, and complete heart block.ModerateClosely monitor the cardiac function of patient and adjust the dose of metoprolol accordingly.Tocainide (HCl)Verapamil (HCl) These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Interfrence

Risks

Drug should not be given to Paediatrics, Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Storage

Inj Store at room temperature, Below 30°C. Do not Freeze. Protect from Sunlight. Tab Store Between 15°C-25°C. Protect from Sunlight and Moisture.

Warnings

Metoprolol should be used with caution in diabetic patients and patients with liver or kidney disease or during pregnancy.

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