And Medicine Blog And Medicine is a Popular Medicine Blog
  • CARDIVAS 6.25 mg, 12.5 mg Carvedilol Tablets Side effects

    For the use of a Registered Medical Practitioner or a Hospital or a Laboratory only.

    CARDIVAS 6.25 / CARDIVAS 12.5

    Carvedilol Tablets 12.5 mg and 6.25 mg

    CARDIVAS 12.5: Each film coated tablet conta.ns carvedilol INN 12.5 mg. Cardivas 6.25: Each film coated tablet contains carvedilol BP 6.25 mg.

    CARDIVAS 6.25 / CARDIVAS 12.5

    Clinical Pharmacology

    Carvedilol is a vasodilating non-selective beta-blocking agent with antioxidant properties. Carvedilol reduces the peripheral vascular resistance through vasodilation and suppresses ths renin-angiotensin-aldosterone system through beta-blockade. The activity of plasma renin is reduced and fluid retention is rare. Carvediloi, has no intrinsic sympathomimetic activity and like propranolol. it has rtembrane stabilising properties. Carvedilol is a racemate of two stereoisomers. Beta-blockade is attributed to the S(-) enantiomer; in contrast, both enantiomers exhibit the same alphal-blocking activity. Carvedilo! is a potent antioxidant, a scavenger of reactive oxygen radicals and an anti-proliferative agent.

    The absolute bioavai’ability of carvedilol is approximately 25% in humans. Bioavailability is stereo-selective. 30% for the R-form and 15% for the S-form. Serum levels peak at approximately 1 hour after an oral dose. Carvedilol is highly lipophilic, approximately 98% to 99% is bound to plasma proteins. The first pass effect after oral administration is approximately 60-75%. The average elimination half-life ranges from 6 to 10 hours.

    Indications

    Hypertension, angina, and as adjunct to diuretics, digcxn or ACE inhibitors in symptomatic chronic heart failure.

    *  In patients with marked fluid retention or overload requiring intravenous inotropic support.

    *  Patients with obstructive airways disease, liver dysfunction.

    * Hypersensitivity to carvediiol or any other constituent of the tablets.

    *  history of bronchospasm or asthma, 2nd and 3rd degree A-V heart block, severe bradycardia, cardiogemc shock, sick sinus syndrome (including sino-atrial   block),   severe   hypotension,    metabolic   acidosis   and phaeochromocytoma < unless adequately controlled by alpha blockade).

    In chronic heart failure patients, worsening cardiac failure or fluid retention occur during up-titration of carvedilol. If such symptoms occur, the dose of diuretic should be adjusted and dose of carvedilol should ;.ot be advanced until clinical stability resumes. Occasionally it may be necessary to lower the carvedilol dose or temporarily discontinue it. In hypertensive patients who have chronic heart failure controlled with digoxin. diuretics and an ACE inhibitor, carvediloi shouid be used with caution since both digoxin and carvedilol may slow AV conduction. In patients with diabetes, the use of carvedilol may be associated with worsening control of blood glucose Therefore, regular monitoring of blood glucose is required in diabetics when carvedilol is initiated or up-titrated and hypogiycaemic therapy adjusted accorumgly.

    In chronic heart failure patients, renal function should be monitored during up titration of carvedilol and the drug discontinued or dosage reduced if worsening of renal failure occurs. Wearers of contact lenses should be advised of the possibility of reduced lacrimation. Discontinuation of carvedilol should be gradual in patients with ischaemic heart disease, as it has beta-blocking activity. Carvedilol may mask the symptoms of thyrotoxicosis. If carvedilol induces bradycardia, with a decrease in pulse rate to less than 55 beats per minute, the dosage of carvedilol should be reduced. Care should be taken in administering carvedilol to patients with a history of serious hypersensitivity reactions and in those undergoing.

    desensitization therapy as beta-blockers may increase both the sensitivity towards allergens and the seriousness of anaphylactic reactions. In patients suffering from the peripheral circulatory disorder Raynaud’s phenomenon, there may be exacerbation of symptoms. Patients with a history of psoriasis associated with beta-blocker therapy should be given carvedilol only after considerations of the risk-benefit ratio. Caution should be taken in the administration of carvedilol to patients suspected of having phaeochromocytoma or to patients suspected of having Prinzmetal’s variant angina. In patients with a tendency to bronchospastic reactions, respiratory distress can occur as a result of a possible increase in airway resistance.

    There is no adequate experience with carvedilo! in pregnant women. With other alpha and beta blocking agents, effects have included perinatal and neonatal distress (bradycardia, hypotension, respiratory depression, hypoglycemia, hypothermia). There is and increased risk of cardiac and pulmonary complications in the neonate in the postnatal period. Carvedilol should not be used in pregnancy or in breast feeding mothers unless the anticipated benefits outweigh the potential risks. It is not known whether carvedilol is excreted in human milk. Breast feeding is therefore not recommended during the administration of carvedilol.

    Drug Interactions

    Carvediloi may potentiate the effect of other concomitantly administered drugs that are anti-hypertensive in action (e.g. alphal-receptor antagonists) or have hypotension asjaart of their adverse effect profile. Patients taking an agent with beta-blocking properties and a drug that can deplete catecholamines (e.g. reserpine and monoamine oxidase inhibitors) should be observed closely for signs of hypotension and/or severe bradycardia. Isolated cases of conduction disturbance have been observed when carvedilol and diltiazem were given concomitantly. Therefore, careful monitoring of ECG and blood pressure should be undertaken when co-administering calcium channel blockers of the verapamil or diltiazem type, or class I antiarrhythmic drugs. These types of drugs should not be co-administered intravenously in patients receiving carvedilol. The effects of insulin or oral hypoglycaemics may be intensified. Trough plasma digoxin levels may be increased in hypertensive patients co-administered carvedilol and digoxin. Concomitant administration of carvedilol and cardiac glycosides may prolong AV conduction time.

    When treatment with carvedilol and clonidine together is to be terminated, carvedilol should be withdrawn first, several days before gradually decreasing the dosage of clonidine. Care may be required in those receiving inducers of mixed function oxidases e.g. rifampicin, as serum levels of carvedilol may be reduced or inhibitors of mixed function oxidases e.g. cimetidine, as serum levels may be increased. During general anaesthesia, attention shouid be paid to the potential synergistic negative inotropic effects of carvedilol and anaesthetic drugs. It is recommended that cyclosporin concentrations be monitored closely after initiation of carvedilol therapy and that the dose of cyclosporin be adjusted as appropriate.

    Side effects

    The commonly reported adverse events with carvedilol were weight increase, hypercholesterolaemia, hyperglycaemia, hypoglycaemia, dizziness, headache, asthenia, fatigue, bradycardia, postural hypotension, oedema, nausea, diarrhoea, vomiting, dermatitis, increased sweating, vision abnormalities, asthma, dyspnoea, gastro-intestinal upset, abdominal pain, pain in the extremities and reduced lacrimation.

    Dosage and Administration

    The tablets should be taken with fluid. For chronic heart failure patients,

    carvedilol should be given with food.

    Symptomatic chronic heart failure

    Adults: The recommended dose for the initiation of therapy is 3.125mg.

    twice a day for two weeks. If this dose is tolerated, the dosage should be increased subsequently, at intervals of not less than two weeks, to 6.25mg twice daily, followed by 12.5mg twice daily and thereafter 25mg twice daily. Dosing should be increased to the highest level tolerated by the patient. The recommended maximum daily dose is 25mg given twice daily for all patients with severe CHF and for patients with mild to moderate CHF weighing less than 85kg. In patients with mild or moderate CHF weighing more than 85kg, the recommended maximum dose is 50mg twice daily. If carvedilol is discontinued for more than two weeks, therapy should be recommenced at 3.125mg twice daily and up titrated in line with the above dosing recommendation.

    The dose of carvedilol should not be increased in any patient with deteriorating heart failure since last visit or with signs of decompensate or unstable chronic heart failure. The dosage must be titrated to individual requirements. For those patients receiving diuretics and/or digoxin and/or ACE inhibitors, dosing of these other drugs should be stabilized prior to initiation of carvedilol treatment.

    Elderly: Same as Adults. Hypertension

    Adults: Once daily dosing is recommended. The recommended dose for initiation of therapy is 12.5mg once a day for the first two days. Thereafter the recommended dosage is 25mg once a day. Although this is an adequate dose in most patients, if necessary the dose may be titrated up to a recommended daily maximum dose of 50mg given once a day or in divided doses. Dose titration should occur at intervals of at least two weeks.

    Elderly: An initial dose of 12.5mg daily is recommended. This has provided satisfactory control in some cases. If the response is inadequate the dose may be titrated up to the recommended daily maximum dose of 50mg given once a day or in divided doses.

    Angina

    Adults: The recommended dose for initiation^ therapy is 12.5mg twice a day for the first two days. If needed, the dose can be further increased up to 25 mg twice a day.

    Elderly: The recommended maximum daily dose is 50mg given in divided doses.

    Renal Impairment: No dose adjustment is anticipated as long as systolic blood pressure is above lOOmmHg.

    Hepatic Impairment: Carvediiol is contra-indicated in patients with hepatic dysfunction.

    Storage

    Store in a cool dry place, protected from the light.

    Cardivas 12.5: Each Box containing 3 x 10′s tablets in Alu-Poly strip pack. Cardivas 6.25: Each Box containing 5 x 10′s tablets in Alu-Alu blister pack.

    1 Comment

One Response to “CARDIVAS 6.25 mg, 12.5 mg Carvedilol Tablets Side effects”

  1. Helen Leo said on

    Is there a interaction between 12.5 MG Carvedilol and the sun? I started breaking out in hives after I started taking this medication whenever I would go out in the sun. Thank you for your help. Helen Leo.

Leave a Reply