Each film coated tablet contains Carvedilol 12.5 or 25 mg.
Carvedilol is a nonselective β-adrenergic blocking agent with a1-blocking activity.
Chemically it is (±)-1-(Carbazol-4-yloxy)-3-[(2-(o-methoxyphenoxy) ethyl] amino]-2-propanol.
Pharmacology: Drug Mechanism: Carvedilol is used for treating high blood pressure and congestive heart failure. Carvedilol blocks receptors of the adrenergic nervous system, the system of nerves in which epinephrine (adrenalin) is active. Nerves from the adrenergic system enter the heart and release an adrenergic chemical (norepinephrine) that attaches to receptors on the heart's muscle and stimulates the muscle to beat more rapidly and forcefully. By blocking the receptors, carvedilol reduce the heart's rate and force of contraction and thereby reduces the work of the heart. Carvedilol also blocks adrenergic receptors on arteries and causes the arteries to relax and the blood pressure to fall. The drop in blood pressure further reduces the work of the heart since it is easier to pump blood against a lower pressure.
Pharmacokinetics: Absorption: Following oral administration, carvedilol is rapidly absorbed. The maximum serum concentration is reached after approximately 1 hr. Approximately 98-99% of carvedilol is bound to plasma proteins. Carvedilol is a lipophilic compound, the distribution volume is approximately 2 L/kg and is during long-term treatment.
Elimination: The average elimination half-life of carvedilol ranges from 6-10 hrs. Plasma clearance is approximately 590 mL/min. Elimination is mainly biliary. The primary route of excretion is via the feces. A minor part is eliminated via the kidneys in the form of various metabolites.
Bioavailability: The absolute bioavailability of carvedilol in humans is approximately 25%. Food does not affect the extent of bioavailability, although the time to reach maximum plasma concentrations is prolonged.
In patients with impaired liver function, bioavailability is raised to as much as 80% due to a reduced first-pass effect.
It is used in the management of hypertension and angina pectoris, and as an adjunct to standard therapy in symptomatic heart failure. It is also used to reduce mortality in patients with left ventricular dysfunction following myocardial infarction.
The doctor will determine the amount of the daily dose and the length of time for which it must be taken. Unless otherwise prescribed, 1 tablet Carvedilol daily.
Treatment should begin with 1/2 tablet Carvedilol (=12.5 mg) daily for the first two (2) days. After that treatment can continue with 1 tablet Carvedilol daily.
Do not increase the dose unless directed by the doctor. If the effect is insufficient, the doctor may increase the dose to 1 tablet Carvedilol twice daily after 14 days at the earliest. A single dose of 25 mg or a total daily dose of 50 mg should not be exceeded.
Carvedilol should be used cautiously in patients who use diuretics or who are elderly or have cirrhosis, asthma, peripheral vascular disease, hyperthyroidism, prinzmetal's variant.
Carvedilol should not be used during pregnancy and lactation or in children because of a lack of experience in these cases.
The most common side effects of carvedilol are dizziness, edema (fluid accumulation), decreased heart rate, diarrhea and postural hypotension (a rapid decrease in blood pressure when going from the seated to the standing position that causes light-headedness and/or fainting). Taking carvedilol with food minimizes the risk of postural hypotension.
Other common side effects of Carvedilol are irregular heart rhythm, and abnormalities of vision.
Wearers of contact lens should be aware of the possibility or reduced lacrimation.
Carvedilol can mask early warning symptoms of hypoglycemia (low blood sugar) such as tremors and increased heart rate. (These symptoms are caused by activation of the adrenergic nervous system, which is blocked by the carvedilol). Therefore, diabetics taking medications that lower blood sugar such as insulin or oral anti-diabetic medications may need to increase the frequency with which they monitor their blood sugar.
Carvedilol taken with calcium channel blockers such as diltiazem or verapamil may trigger an irregular heart rhythm or an increase in blood pressure.
Reserpine, monoamine oxidase inhibitors and clonidine, because they have similar mechanisms of action as carvedilol, may greatly accentuate the effects of carvedilol and cause a steep decline a blood pressure and/or heart rate. Close monitoring of blood pressure and heart rate may be needed.
Carvedilol may cause an increase in digoxin blood levels. Therefore, in patients receiving digoxin, the digoxin blood level should be monitored if carvedilol is started, adjusted or discontinued.
Rifampin can sharply decrease the carvedilol blood level. Therefore, in patients taking rifampin, the dose of carvedilol may need to be increased.
Carvedilol shares a common pathway for elimination by the liver with several other drugs such as quinidine, fluoxetine, paroxetine, or propafenone. Use of these drugs may block the elimination of carvedilol. No studies have been done to confirm these effects on the elimination of carvedilol, however, carvedilol blood levels may be increase (along with the risk for carvedilol's side effects) if patients are taking any of these drugs.
Carvedilol may increase the levels in the blood of cyclosporin, and the dose cyclosporin may need to be adjusted when the two drugs are used together.
Since the tablets may discolor when exposed to light, it is recommended that they be kept in their closed boxes. Store at temperature not exceeding 30°C.
C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
Cardipres film-coated tab 12.5 mg
30's (P330/box, P11/film-coated tab)
Cardipres film-coated tab 25 mg
30's (P525/box, P17.5/film-coated tab)