Eslo-Met-2.5 & 5 Tablets
Therapy Area
Cardiology
Composition
Eslo Met 2.5
Each modified release uncoated bilayered tablet contains :
S (-) Metoprolol Succinate 23.75 mg
equivalent to S (-) Metoprolol Tartrate 25 mg
(As prolonged release)
S (-) Amlodipine Besylate IP equivalent to S (-) Amlodipine 2.5 mg
(As immediate release)
Excipients q.s.
Colour : Lake of Indigo Carmine
Eslo Met 5
Each modified release uncoated bilayered tablet contains :
S (-) Metoprolol Succinate 23.75 mg
equivalent to S (-) Metoprolol Tartrate 25 mg
(As prolonged release)
S (-) Amlodipine Besylate IP equivalent to S (-) Amlodipine 5 mg
(As immediate release)
Excipients q.s
Colour : Lake of Quinoline Yellow
Description
S (-) Metoprolol is a selective β1-receptor blocker and it is the active form of the racemate Metoprolol. The β1 receptor affinity of S (-) Metoprolol is about 500 times greater than that of R (+) Metoprolol. S (-) Amlodipine is a dihydropyridine calcium channel blocker with vasodilating properties. S (-) Amlodipine is 1000 times more potent than the R (+) isomer in binding to the dihydropyridine receptor. S (-) Amlodipine is the active form of the racemate Amlodipine.
Mechanism of Action
S (-) Metoprolol is a selective β1-receptor blocking agent. Blockade of β1-receptors results in reduction of heart rate, cardiac output and blood pressure. The beneficial effects of β-blocking agents in angina are related primarily to their hemodynamic effects i.e. decreased heart rate, blood pressure, and contractility-which decrease myocardial oxygen requirement.
S (-) Amlodipine is a dihydropyridine calcium channel antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. S (-) Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. Reduction in the peripheral vascular resistance benefits the patients with angina of effort. In cardiac muscle, blockade of calcium channel results in reduction in the contractility of the heart and decrease in sinus node pacemaker rate and decrease in atrioventricular node conduction velocity. Cardiac output is also reduced. The reduction in cardiac mechanical function reduces the oxygen requirement in patients with angina. Reduction in coronary arterial tone has been demonstrated in patients with variant angina.
Pharmacokinetics
In humans absorption of S (-) Metoprolol is rapid and complete. Metoprolol is eliminated by several pathways, including benzylic hydroxylation (alphahydroxylation) which accounts for ~ 10% of the dose. This pathway is stereoselective for S (-) Metoprolol. The major pathway is O-demethylation that favours R (+) Metoprolol and accounts for 65% of the dose of racemic Metoprolol.
Administration of S (-) Amlodipine 2.5 mg as a single dose in the fasting state produced maximum plasma concentration (Cmax) of 8.30 ± 1.071 ng/ml in 2.73 ± 0.88 hours (Tmax). The mean AUC0-t value (t=48 hours) of S (-) Amlodipine (2.5 mg) was 95.33 ± 14.45 ng-hour/ml. The AUC0-∞value recorded was 140.91± 28.06 ng-hour/ml.
Indications
Eslo Met is indicated for the treatment of essential hypertension and angina pectoris in adults.
Contraindications
In patients who have shown hypersensitivity to any component of the product or to other beta-blockers or calcium channel blockers.
In atrioventricular block of second or third degree, patients with unstable decompensated cardiac heart failure (pulmonary oedema, hypoperfusion or hypotension), patients with continuous or intermittent inotropic therapy acting through beta-receptor agonism, marked clinically relevant sinus bradycardia, sick-sinus syndrome, cardiogenic shock and severe peripheral arterial circulatory disorder
S (-) Metoprolol should not be given to patients with suspected acute myocardial infarction as long as the heart rate is <45 beats/min, the PQ-interval is >0.24sec orthe systolic blood pressure is<100mmHg.
Dosage and Administration
One tablet to be taken once daily, orally. The dose may be titrated as per requirement.
Overdosage
In case of Eslo Met overdosage, unabsorbed drug should removed by induction of emesis and / or gastric lavage.
Potential signs and symptoms associated with overdosage of S (-) Metoprolol are bradycardia, hypotension, bronchospasm and cardiac failure. There is no specific antidote. Symptoms of S (-) Metoprolol overdosage should be treated with atropine, vasopressors, β2-stimulating agents and drugs for cardiac failure.
Overdose with S (-) Amlodipine may result in excessive peripheral vasodilatation. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported. The patient should be closely monitored, and the treatment should be symptomatic and supportive. Management depends on the time since ingestion and the severity of the symptoms. Serum electrolytes and creatinine should be monitored frequently.
Warnings and Precautions
Intravenous administration of calcium antagonists of the verapamil-type should not be given to patients treated with beta-blockers
Patients suffering from heart failure should have their decompensation treated both before and during treatment. Abrupt interruption of the medication is to be avoided.
Sudden withdrawal of beta blockade is hazardous, especially in high-risk patients, and may aggravate chronic heart failure as well as increase the risk of myocardial infarction and sudden death. Any withdrawal of the product should therefore, if possible, be made gradually over at least two weeks when the dose is reduced by half in each step, down to the final dose. The final dose should be given for at least four days before discontinuation. If symptoms occur, a slower withdrawal rate is recommended.
Though clinical studies in patients with normal liver function have shown that there is no elevation in the hepatic enzymes with the use of S (-) Amlodipine, caution should be taken while administering S (-) Amlodipine to patients with hepatic and renal impairment.
Special Population
Pregnant women & Nursing Mothers
No data available; the product should be administered only when the potential benefits outweighs the risk to the patient.
Children
Safety and effectiveness not established.
Adverse Effects
Gingival Hypertrophy & Alopecia have been reported with S (-) Amlodipine use. On the basis of clinical data available, the following adverse events have been reported in less than 2% of patients with S (-) Amlodipine : vertigo (0.05%), tachycardia (0.05%), cough (0.05%), headache (0.43%), difficulty in breathing (0.1%), and facial puffiness (0.05%). Fatigue, dry mouth, dizziness, dyspnoea and mild rash have been reported with S (-) Metoprolol.
Storage
Store below 30°C. Protect from light & moisture
Keep out of reach of children
Presentation:
Eslo Met 2.5 : A blister strip of 10 tablets.
Eslo Met 5 : A blister strip of 10 tablets.
