Cardekim

Management of HTN, angina pectoris & heart failure.

HTN Initially 12.5 mg once daily, increased after 2 days to 25 mg once daily; or initially 6.25 mg bid, increased after 1-2 wk to 12.5 mg once daily. Dose may be increased further if necessary at interval of at least 2 wk to 50 mg once daily or in divided doses. Elderly 12.5 mg once daily. Angina pectoris Initially 12.5 mg bid, increased after 2 days to 25 mg bid. Heart failure Initially 3.125 mg bid for 2 wk, may then be increased if tolerated to 6.25 mg bid. Dose should be increased if tolerated at intervals of at least 2 wk to max 50 mg bid for patient >85 kg or 25 mg bid for patient <85 kg.

Should be taken with food.

Patients w/ history of a serious hypersensitivity reaction (eg, SJS, anaphylactic reaction, angioedema). Bronchial asthma or related bronchospastic conditions. 2nd- or 3rd-degree AV block. Sick sinus syndrome. Severe bradycardia (unless a permanent pacemaker is in place). Patients w/ cardiogenic shock or who have decompensated heart failure requiring use of IV inotropic therapy. Patients w/ severe hepatic impairment.

Patients w/ history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Carefully observe patients & advise to limit physical activity to min when discontinuation of treatment is planned; discontinue carvedilol over 1-2 wk whenever possible. Reports of bradycardia in hypertensive patients, heart failure patients, & MI patients w/ left ventricular dysfunction. Starting w/ a low dose, administration w/ food, & gradual up-titration should decrease likelihood of syncope or excessive hypotension. Worsening heart failure or fluid retention may occur during up-titration; if such symptoms occur, increase diuretics & do not advance carvedilol dose until clinical stability resumes. Not to be given to patients w/ bronchospastic disease (eg, chronic bronchitis & emphysema); however, may be used w/ caution in patients who do not respond to, or cannot tolerate, other antihypertensive agents. May mask some of the manifestations of hypoglycemia, particularly tachycardia, & may potentiate insulin-induced hypoglycemia & delay recovery of serum glucose levels; caution patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents about these possibilities. Monitor blood glucose when carvedilol dosing is initiated, adjusted, or discontinued. Caution in patients w/ peripheral vascular disease; suspected of having pheochromocytoma or Prinzmetal's variant angina. Rarely, use in patients w/ heart failure has resulted in deterioration of renal function; monitor renal function during up-titration in patients w/ risk factors & discontinue drug or reduce dose if worsening of renal function occurs. Take particular care when anesth agents which depress myocardial function (eg, ether, cyclopropane, & trichloroethylene) are used if treatment w/ carvedilol is to be continued perioperatively. β-adrenergic blockade may mask clinical signs of hyperthyroidism eg, tachycardia; abrupt w/drawal of β-blockade may be followed by an exacerbation of the symptoms of hyperthyroidism or may precipitate thyroid storm. Initiate α-blocking agent prior to the use of any β-blocking agent in patients w/ pheochromocytoma. Avoid situations (eg, driving or hazardous tasks), where injury could result should syncope occur, during initiation of therapy. Use during pregnancy only if potential benefit justifies potential risk to the fetus. Decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother.

Dizziness, headache; cardiac failure; hypotension; genital edema; asthenia. Bronchitis, pneumonia, URTI, UTI; anemia; wt increase, hypercholesterolemia, impaired blood glucose control (hyperglycemia, hypoglycemia) in patients w/ pre-existing diabetes; depression, depressed mood; visual impairment, decreased lacrimation, eye irritation; bradycardia, edema, hypervolemia, fluid overload; orthostatic hypotension, disturbances of peripheral circulation (cold extremities, peripheral vascular disease, exacerbation of intermittent claudication & Raynaud's phenomenon); dyspnea, pulmonary edema, asthma in predisposed patients; nausea, diarrhea, vomiting, dyspepsia, abdominal pain; pain in extremities; renal failure & renal function abnormalities in patients w/ diffuse vascular disease &/or underlying renal insufficiency, micturition disorders; pain.

Potentially increased blood levels of the R(+) enantiomer of carvedilol w/ potent CYP2D6 inhibitors eg, quinidine, fluoxetine, paroxetine, & propafenone. Hypotension &/or severe bradycardia w/ drugs that can deplete catecholamines eg, reserpine & MAOIs. May potentiate BP- & heart rate-lowering effects w/ clonidine. Modest increases in mean trough conc of cyclosporine in renal transplant patients suffering from chronic vascular rejection. Increased risk of bradycardia w/ digitalis glycosides. Increased conc of digoxin. Reduced plasma conc w/ rifampin. Increased AUC w/ cimetidine. Increased conc of S(-)-enantiomer of carvedilol w/ amiodarone (CYP2C9 & P-gp inhibitor). β-blocking properties may be enhanced w/ other CYP2C9 inhibitors (eg, fluconazole) resulting in further slowing of the heart rate or cardiac conduction. Conduction disturbance (rarely w/ hemodynamic compromise) w/ diltiazem. May enhance blood sugar-reducing effect of insulin & oral hypoglycemics.

Beta-Blockers

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

Rx