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ETC / RX - Cardiovascular system - Vedicard

COMPOSITION:

VEDICARD® 3.125: Each film coated caplet contains:

  • Active ingredient: Carvedilol 3.125 mg.
  • Other ingredients: Flowlac 100, microcrystalline cellulose, crospovidon, magnesium stearate, colloidal anhydrous silica, opadry II white.

VEDICARD® 6.25: Each film coated caplet contains:

  • Active ingredient: Carvedilol 6.25 mg.
  • Other ingredients: Flowlac 100, microcrystalline cellulose, crospovidon, magnesium stearate, colloidal anhydrous silica, opadry II blue.

VEDICARD® 12.5: Each film coated caplet contains:

  • Active ingredient: Carvedilol 12.5 mg.
  • Other ingredients: Flowlac 100, microcrystalline cellulose, crospovidon, magnesium stearate, colloidal anhydrous silica, opadry II white, quinoline yellow lake.

VEDICARD® 25: Each film coated caplet contains:

  • Active ingredient: Carvedilol 25 mg.
  • Other ingredients: Flowlac 100, microcrystalline cellulose, crospovidon, magnesium stearate, colloidal anhydrous silica, opadry II orange.

PHARMACODYNAMICS:

Carvedilol is a nonselective β-adrenergic blocking agent with selective α1-adrenergic blocking activity.

Carvedilol has two main antihypertensive metabolism of actions. One is vasodilation, primarily through selective alpha1- receptor blockade, therefore reducing the peripheral vascular resistance. Carvedilol also has nonselective beta-adrenoreceptor blocking activity. The selective effect and beta-receptors occur at the same dose. It also has calcium channel blocking activity. Clinical studies have proved that combination alpha1-receptor blocker and beta-receptor blocker may slightly reduce frequence of heart or unchange in taking a rest, remain ejection fraction and blood flow in the kidney and periphery.


PHARMACOKINETICS:

Carvedilol is well absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism in the liver; the absolute bioavailability is about 25%. Peak plasma concentrations occur 1 to 2 hours after an oral dose. It has high lipid solubility. Carvedilol is more than 98% bound to plasma proteins. It is extensively metabolised in the live, primarily by the cytochrome P450 isoenzymes CYP2D6 and the metabolites are excreted mainly in the bile. The elimination half-life is about 6 to 10 hours. Carvedilol has been shown to accumulate in breast milk.


INDICATIONS:

Congestive Heart Failure

Treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin, in conjunction with other drugs.

Hypertension

Management of essential hypertension. It can be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics


ADMINISTRATION AND DOSAGE:

Carvedilol should be taken with food to slow the rate of absorption and reduce the incidence of side effects.

Dosage must be individualized and closely monitored by a physician during up-titration.

Congestive Heart Failure

The recommended starting dose of Carvedilol is 3.125 mg twice daily for two weeks. If this dose is tolerated, it can then be increased to 6.25 mg twice daily. Dosing should then be doubled every 2 weeks to the highest level tolerated by the patient.

The maximum recommended dose is 25 mg twice daily in patients weighting less than 85 kg and 50 mg twice daily in patients weighting more than 85 kg.

Hypertension

The recommended starting dose of Carvedilol is 6.25 mg twice daily. If this dose is tolerated, the dose should be maintained for 7 to 14 days, and then increased to 12.5 mg twice daily if needed. This dose should also be maintained for 7 to14 days and can then be adjusted upward to 25 mg twice daily if tolerated and needed. Total daily dose should not exceed 50 mg. The full antihypertensive effect of Carvedilol is seen within 7 to 14 days.


CONTRAINDICATIONS:

  • Patients with hypersensitivity to any ingredient of this drug.
  • Patients with NYHA class IV decompensated cardiac failure, bronchial asthma or related bronchospastic conditions, second-or third-degree AV block, sick sinus syndrome (unless a permanent pacemaker is in place), cardiogenic shock or severe bradycardia.
  • Patients with severe hepatic impairment.
  • Pregnancy and lactation.

WARNINGS AND PRECAUTIONS:

  • Hepatic injury may be occurred during therapy. If the patient has laboratory evidence of liver injury or jaundice, carvedilol should be stopped and not restarted.
  • Hypotension and postural hypotension may occur in congestive heart failure patients receiving carvedilol. Thus, treatment should be initiated with low dose. Dosage should then be increased slowly as directed in administration and dosage section.
  • Caution should be taken in the administration of carvedilol to patients (1) suspected of having pheochromocytoma, (2) suspected of having Prinzmetal’s variant angina, (3) peripheral vascular disease, (4) diabetes and hypoglycemia, (5) thyrotoxicosis.
  • Safety and efficacy in patients younger than 18 years of age have not been established.

SIDE EFFECTS:

Allergy, malaise, vertigo, peripheral edema, postural hypotension, SGPT increased, SGOT increased, hypoglycemia, somnolence and impotence.

In case of an unexpected reaction, consult your physician.


INTERACTIONS:

  • Concomitant administration of carvedilol with reserpine and monoamine oxidase inhibitors may deplete catecholamines.
  • Concomitant administration of carvedilol with clonidine may potentiate the lowering effects of blood pressure and heart rate.
  • Digoxin concentrations are increased when digoxin and carvedilol are administered concomitantly.
  • Interactions of carvedilol with strong inhibitors of CYP2D6 such as quinidine, fluoxetine and paroxetine have not been studied, but these drugs would be expected to increase blood levels of the R(+) enantiomer of carvedilol.
  • Isolated cases of conduction disturbance have been observed when carvedilol is co-administered with diltiazem.
  • Carvedilol may enhance the blood-sugar-reducing effect of insulin and oral hypoglycemics.
  • Rifampicin may reduce plasma concentration of carvedilol.

OVERDOSAGE:

Symptoms: Overdosage may cause cardiac disorders, central nervous system poisoning, bronchospasm, hypoglycemia and hyperkalemia. The commonly cardiac symptoms include hypotension and bradycardia. AV block, in ventricular conductivity disorder and heart shock may occur after massive overdose. Effect on the central nerve includes convulsion, unconsciousness and apnea.

Management: Patients should be treated convulsion, hypotension, hyperkalemia and hypoglycemia. If bradycardia and hypotension resist atropine, iso-proterenol, or pacemaker, glucagon may be used. If peripheral vasodilation dominates, it may be necessary to administer adrenaline or noradrenaline with continuous monitoring of circulatory conditions.


PRESENTATION:

Box of 1 blister x 10 film coated caplets.

Storage: Store at temperature from 150C to 300C.

Shelf-life: 36 months from manufacturing date. Do not use after expiry date.

Quality Specification: Manufacturer’s.