pms-Carvedilol

Carvedilol

In combination w/ diuretics & an ACE inhibitor, w/ or w/o digitalis, for the treatment of mild, moderate or severe heart failure of ischemic or non-ischemic origin to increase survival & reduce the combined risk of all-cause mortality & CV or non-CV hospitalizations.

Individualized dosage. Initially 3.125 mg bd for 2 wk, can be increased to 6.25, 12.5 & 25 mg bd over successive intervals of at least 2 wk if tolerated. Maintain patients on the highest tolerated dose. Max recommended dose: 25 mg bd.

Should be taken with food.

Hypersensitivity. Patients w/ decompensated cardiac failure requiring IV inotropic therapy w/ sympathomimetic agents; bronchial asthma or related bronchospastic conditions; 2nd or 3rd degree AV block, or sick sinus syndrome (unless a permanent pacemaker is in place); cardiogenic shock; severe hypotension; severe bradycardia; primary obstructive valvular heart disease; mental incapacity, unless closely supervised by an appropriate caregiver; clinically manifest hepatic impairment.

Treatment discontinuation should be done gradually to avoid deterioration. Reports of skin rashes & conjunctival xerosis. Worsening cardiac failure may occur during initiation & up-titration. Control cardiac failure for at least 4 wk before treatment initiation. High risk of hypotension & postural hypotension during treatment initiation & 1st 30 days of dosing corresponding to the up-titration period. Can precipitate or aggravate symptoms of arterial insufficiency in patients w/ peripheral vascular disease. Use w/ caution in patients w/ primary regurgitative valvular disease. May provoke chest pain in patients w/ Prinzmetal's angina. Discontinue treatment if severe sinus bradycardia occurs. May enhance hypoglycemia in patients prone to this condition. Regularly monitor blood glucose when carvedilol is initiated, adjusted or discontinued. May mask the clinical signs of continuing hyperthyroidism or complications. Use w/ caution in patients w/ pheochromocytoma. Perform laboratory testing at the 1st symptom/sign of liver dysfunction. Stop & do not restart treatment if there is laboratory evidence of liver injury or jaundice. Increased difficulty in treating an allergic-type reaction in patients on β-blockers; administer epinephrine w/ caution. Possibility of reduced lacrimation in patients wearing contact lenses. Periodic ophth examinations are advisable while on treatment. Potential for pronounced hypotension during anesth. Monitor renal function in patients at risk of renal failure during up-titration & discontinue or reduce dose if worsening of renal function occurs. Patients w/ bronchospastic disease should not receive β-blockers. Pregnancy. Do not breastfeed during treatment. Elderly.

Dizziness, upper resp infection. Mild to moderate heart failure: Fatigue, dyspnea, cardiac failure, chest pain. Severe heart failure: Hypotension.

Decreased AUC & C_max w/ rifampin. Increased AUC w/ cimetidine. Increased blood levels of carvedilol R(+) enantiomer w/ strong CYP2D6 inhibitors eg, quinidine, fluoxetine, paroxetine, & propafenone. Additive effects w/ other antihypertensive agents. Possible hypotension &/or marked bradycardia w/ catecholamine-depleting agents. Conduction disturbance w/ antiarrhythmics & Ca channel blockers. Increased peak conc of digoxin. Potentiated BP & heart rate lowering effects w/ clonidine. Increased conc of cyclosporine. Potentiated bradycardic effects w/ fingolimod. Possible blunting of reflex tachycardia produced by nitroglycerin. Enhanced blood sugar reducing effect of insulin & oral hypoglycemics. Possible drug interaction w/ TCAs. Increased AUC w/ grapefruit juice (CYP3A4 & CYP1A2 inhibitor).

Beta-Blockers

C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.

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