Metoprolol Amlodipine 50mg 5mg Tablet - Manufacturers & Suppliers - Third Party Contract Manufacturing - PCD Pharma Franchise
Metoprolol is a selective beta-1 blocker commonly employed as the succinate and tartrate derivatives depending if the formulation is designed to be of immediate release or extended-release. The possibility of the generation of these formulations comes from the lower systemic bioavailability of the succinate derivative.
Amlodipine is a medication which is used for lowering of blood pressure and also causes prevention of chest pain. It lowers the blood pressure by relaxing the blood vessels.
Indications
Metoprolol is indicated for the treatment of angina, heart failure, myocardial infarction, atrial fibrillation, atrial flutter and Atenelol is used in hypertension
Mechanism of action
Metoprolol is a beta-1-adrenergic receptor inhibitor specific to cardiac cells with negligible effect on beta-2 receptors. This inhibition decreases cardiac output by producing negative chronotropic and inotropic effects without presenting activity towards membrane stabilization nor intrinsic sympathomimetics
Amlodipine
It inhibits the movement calcium ions in vascular smooth cells and cardiac muscle. It binds to dihydropyridine and nondihydropyridine binding sites. This causes decreased heart muscle heart muscle contractility. It also causes a reduction in peripheral vascular resistance and reduction in blood pressure. It also acts as inhibitor of acid sphingomyelinase which is involved in signal transduction and programmed cell death.
Dosage
As prescribed by the physician.
Pharmacology
Metoprolol
Absorption
When metoprolol is administered orally, it is almost completely absorbed in the gastrointestinal tract.1 The maximum serum concentration is achieved 20 min after intravenous administration and 1-2 hours after oral administration. The bioavailability of metoprolol is of 100% when administered intravenously and when administered orally it presents about 50% for the tartrate derivative and 40% for the succinate derivative.
Distribution
The reported volume of distribution of metoprolol is 4.2 L/kg
Excretion
Metoprolol is mainly excreted via the kidneys. From the eliminated dose, less than 5% is recovered unchanged
Amlodipine
Absorption
The drug is slowly and completely absorbed in the GI tract. The peak plasma concentration of the drug is archived in 6-12hrs. The bioavailability is 64-90% which is not affected by food.
Distribution
About 97.5% of the drug is bound to plasma protein. The drug is metabolized by liver.
Excretion
The drug metabolites are excreted in urine.
Precautions
• Check with your doctor right away if you are having chest pain or discomfort, dilated neck veins, extreme fatigue, irregular breathing or heartbeat, shortness of breath, swelling of the face, fingers, feet, or lower legs, or weight gain. Do not suddenly stop taking this medicine without first checking with your doctor
Amlodipine can cause hypotension
• It increases angina and can cause myocardial infarction
• Patients with hepatic failure
Contraindications
• pheochromocytoma
• diabetes
• low blood sugar
• depression
• myasthenia gravis, a skeletal muscle disorder
• complete heart block
• second degree atrioventricular heart block
• sick sinus syndrome
• sinus bradycardia
• sudden and serious symptoms of heart failure called acute decompensated heart failure
• Raynaud's phenomenon, a condition where blood vessels constrict too much with coldness or stress
• peripheral vascular disease
Introduction