Topress is a selective beta1-blocker. Topress reduces or inhibits the agonistic effect on the heart of catecholamines (which are released during physical and mental stress). This means that the usual increase in heart rate, cardiac output, cardiac contractility and blood pressure, produced by the acute increase in catecholamines, is reduced by Topress. Topress interferes less with Insulin release and carbohydrate metabolism than do non-selective beta-blockers. Topress interferes much less with the cardiovascular response to hypoglycaemia than do non-selective beta-blockers.
ln the management of hypertension and angina pectoris. Cardiac arrhythmias, especially supraventricular tachyarrhythmias. Adjunct to the treatment of hyperthyroidism. Early intervention with Topress in acute myocardial infarction reduces infarct size and the incidence of ventricular fibrillation. Pain relief may also decrease the need for opiate analgesics. Topress has been shown to reduce mortality when administered to patients with acute myocardial infarction.
Topress is also used to associated treatment for these conditions: Angina Pectoris, Atrial Fibrillation, High Blood Pressure (Hypertension), Migraine, Myocardial Infarction, Tachycardia, Supraventricular, Thyroid Crisis, Acute hemodynamically stable Myocardial infarction, Chronic heart failure with reduced ejection fraction (NYHA Class II), Chronic heart failure with reduced ejection fraction (NYHA Class III)
|Metoprolol Other Names||(RS)-Metoprolol, DL-metoprolol, Metoprolol|
Metoprolol is not highly bound to plasma proteins and only about 11% of the administered dose is found bound. It is mainly bound to serum albumin.
|Therapeutic Class||Beta-adrenoceptor blocking drugs, Beta-blockers|
|Manufacturer||Eskayef Bangladesh Ltd|
|Last Updated:||June 23, 2021 at 11:23 am|
Hypertension: Total daily dosage Topress 100-400 mg to be given as a single or twice daily dose. The starting dose is 100 mg (two Topress-50 tablets) per day. This may be increased by 100 mg per day at weekly intervals. lf full control is not achieved using a single daily dose, a b.i.d. regimen should be initiated. Combination therapy with a diuretic or other anti-hypertensive agent may also be considered.
Angina: Usually Topress 50 mg (one Topress-50 tablet) to 100 mg (two Topress-50 tablets) twice or three times daily.
Cardiac arrhythmias: Topress 50 mg (one Topress-50 tablet) b.i.d or t.i.d should usually control the condition. It necessary the dose can be increased up to 300 mg per day in divided doses. Following the treatment of an acute arrhythmia with Topress injection, continuation therapy with Topress tablets should be initiated 4-6 hours later. The initial oral dose should not exceed 50 mg t.i.d.
Hyperthyroidism: Topress 50 mg (one Topress-50 tablet) four times a day.The dose should be reduced as the euthyroid state is achieved.
Myocardial infarction: Orally, therapy should commence 15 minutes after the last injection with 50 mg every 6 hours for 48 hours. Patients who fail to tolerate the full intravenous dose should be given half the suggested oral dose. Maintenance – The usual maintenance dose is 200 mg daily given in divided doses. Elderly’ There are no special dosage requirements in otherwise healthy elderly patients. Signidcant hepatic dysfunction: A reduction in dosage may be necessary.
Arrhythmias: By intravenous injection, up to 5 mg at a rate of 1-2 mg/minute, repeated after 5 minutes if necessary, total dose 10-15 mg.
In surgery: By slow intravenous injection 2-4 mg at induction or to control arrhythmias developing during anaesthesia; 2 mg doses may be repeated to a maximum of 10 mg.
Myocardial Infarction: Early intervention within 12 hours of infarction, by intravenous injection 5 mg every 2 minutes to a maximum of 15 mg, followed after 15 minutes by 50 mg by mouth every 6 hours for 48 hours; maintenance 200 mg daily in divided doses.
Impaired Renal Function: Dose adjustment is not needed in patients with impaired renal function.
Impaired Hepatic Function: Dose adjustment is not normally needed in patients suffering from liver cirrhosis because Topress has low protein binding (5-10%). When there are signs of serious impairment of liver function (e.g. shunt-operated patients), a reduction in dose should be considered.
Elderly: Dose adjustment is not needed.
Bradycardia, bronchospasm, hypotension, headache, fatigue, sleep & gastro-intestinal disturbances, dizziness, vertigo, visual disturbances etc.
The second or third dose should not be given if the heart rate is <40 beats/minute, the P-R interval is > 0.26 seconds and the systolic blood pressure is <90 mmHg or if there is any aggravation of dyspnoea or cold sweating. Intravenous administration of calcium antagonists of the Verapamil-type should not be given to patients treated with beta-blockers. When treating patients with suspected or definite myocardial infarction, the haemodynamic status of the patient should be carefully monitored after each of the three 5 mg intravenous doses. Use in Pregnancy: As with most medicines, Topress should not be given during pregnancy and lactation unless its use is considered essential. As with all antihypertensive agents, beta-blockers may cause side effects (e.g. bradycardia) in the foetus and in the newborn and breast-fed infant. Use in Lactation: The amount of Topress ingested via breast-milk seems to be negligible as regards beta-blocking effect in the infant if the mother is treated with Topress doses within the normal therapeutic range.
Plasma level of Topress may be raised by co-administration of compounds metabolished by CYP2D6 e.g. Antiarrhythmics, antihistamines, H2 receptor antagonists, antidepressants, antipsychotics and COX-2 inhibitors. The plasma conc. of Topress is lowered by Rifampicin.
- Avoid alcohol.
- Avoid natural licorice.
- Take with food.
Volume of Distribution
The reported volume of distribution of metoprolol is 4.2 L/kg. Due to the characteristics of metoprolol, this molecule is able to cross the blood-brain barrier and even 78% of the administered drug can be found in cerebrospinal fluid.
The immediate release formulations of metoprolol present a half-life of about 3-7 hours.
The reported clearance rate on patients with normal kidney function is 0.8 L/min. In cirrhotic patients, the clearance rate changes to 0.61 L/min.
Pregnancy & Breastfeeding use
Topress should not be used in pregnancy or lactating mothers unless the physician considers that the benefit outweighs the possible hazard to the fetus or infant.
2nd or 3rd degree AV block, sick sinus syndrome, hypotension, decompensated heart failure, sinus bradycardia, severe peripheral arterial circulatory disorders, cardiogenic shock, severe asthma and bronchospasm, untreated phaeochromocytoma, Prinzmetal's angina, metabolic acidosis.
Renal Impairment: No dosage adjustment needed.
Hepatic Impairment: Reduce dose.
Poisoning due to an overdose of metoprolol may lead to severe hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impairment of consciousness, coma, nausea, vomiting, cyanosis, hypoglycaemia and, occasionally, hyperkalaemia. The first manifestations usually appear 20 minutes to 2 hours after drug ingestion. Treatment: Treatment should include close monitoring of cardiovascular, respiratory and renal function, and blood glucose and electrolytes. Further absorption may be prevented by induction of vomiting, gastric lavage or administration of activated-charcoal if ingestion is recent. Cardiovascular complications should be treated symptomatically, which may require the use of sympathomimetic agents (e.g. noradrenaline, metaramionl), atropine or inotropic agents (e.g. dopamine, dobutamine). Temporary pacing may be required for AV block. Glucagon can reverse the effects of excessive B-blockade, given in a dose of 1-10 mg intravenously. Intravenous B2-stimulants e.g. terbutaline may be required to relieve bronchospasm. Topress cannot be effectively removed by haemodialysis.
Store in a cool, dry place protected from light. Keep out of reach of children.