Indications/Uses
Management of hypertension and angina pectoris and as an adjunct to standard therapy in symptomatic heart failure.
Dosage/Direction for Use
The physician will determine the amount of the daily dose and the length of time for which it must be taken. Do not interrupt or stop taking Duobloc without first checking with the doctor.
Essential Hypertension: Treatment should begin with 12.5 mg daily for the first 2 days. After that treatment can continue with 25 mg once daily. If the effect is insufficient, the dose may be increased to 25 mg twice daily for 14 days at the earliest. A single dose of 25 mg or total daily dose of 50 mg should not be exceeded.
Chronic Stable Angina: The recommended dose for initiation of therapy is 12.5 mg twice a day for the first 2 days. Thereafter, the recommended dosage is 25 mg twice daily. If necessary, the dosage may subsequently be increased at the intervals at least 2 weeks up to the recommended maximum daily dose of 100 mg given in divided doses (twice daily).
Administration
Should be taken with food.
Contraindications
Patients with hypersensitivity to carvedilol or any component of Duobloc. Unstable or decompensated heart failure. Clinically manifest liver dysfunction. As with other α-blockers, Duobloc must not be used in patients with: 2nd- and 3rd-degree atrioventricular (AV) block (unless a permanent pacemaker is in place), severe bradycardia (<50 bpm), sick sinus syndrome (including sinoatrial block), severe hypotension (systolic blood pressure <85 mmHg), cardiogenic shock, history of bronchospasm or asthma, history of other obstructive lung disorder.
Special Precautions
Chronic Heart Failure: In chronic heart failure patients, worsening cardiac failure or fluid retention may occur during up-titration of Duobloc. If such symptoms occur, diuretics should be increased and the dose should not be advanced until clinical stability resume. Occasionally, it may be necessary to lower the dose or, in rare cases, temporarily discontinue it. Such episodes do not preclude subsequent successful titration of Duobloc. It should be used with caution in combination with digitalis glycosides, as both medicines slow AV conduction.
Adverse Reactions
Dosage may need to be reduced in severe hepatic impairment (Hepatic: Hyperbilirubinemia, increased liver function tests), liver function abnormalities are reversible on stopping treatment. Liver function should be monitored regularly.
Drug Interactions
Increased risk of myocardial depression when combined with verapamil, diltiazem and class I antiarrhythmics. May reduce requirement for hypoglycemic therapy.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacokinetics: Absorption: Rapid; food decreases the rate but the extent of absorption; administration with food minimizes risks of orthostatic hypotension.
Metabolism: First-pass metabolism, extensively metabolized primarily by aromatic ring oxidation and glucuronidation (2% excreted unchanged); 3 active metabolites (4-hydroxyphenyl metabolite is 13 times more potent than parent drug); plasma concentrations in the elderly and those with cirrhotic liver disease are 50% and 4-7 times higher, respectively.
Bioavailability: 25-35%.
Half-Life: 7-10 hrs.
Elimination: Primarily via bile into feces.
MedsGo Class
Beta-Blockers