CARLIV [Carvedilol] 12.5 mg Tablets
CARLIV
instructions for medical use of the medicinal product
Tradename
Carliv, Carliv
International non-proprietary name
carvedilol, carvedilol
Compound
Each film-coated tablet contains:
active ingredient: carvedilol 12.5 mg
excipients: corn starch, dextrin, sucrose, sodium starch glycolate , disodium edetate, povidone, magnesium stearate, talc
Each film-coated tablet contains:
active substance: carvedilol 25 mg
excipients: corn starch, dextrin, sucrose, sodium starch glycolate , disodium edetate, povidone, magnesium stearate, talc
Dosage form
Tablets.
Pharmacotherapeutic group
Alpha and beta blocker .
Pharmacological properties
Pharmacodynamics
Carvedilol has a combined non-selective β1-, β2- and α1-blocking action. It does not have its own sympathomimetic activity, it has membrane-stabilizing properties. Due to the blockade of β-adrenergic receptors of the heart, blood pressure, cardiac output and heart rate may decrease. Carvedilol inhibits the RAAS by blocking the β-adrenergic receptors of the kidneys, causing a decrease in plasma renin activity. By blocking α-adrenergic receptors, carvedilol can cause peripheral vasodilation, thereby reducing systemic vascular resistance. The combination of blockade of β-adrenergic receptors and vasodilation has the following effects: in patients with arterial hypertension - a decrease in blood pressure; in patients with coronary artery disease - anti-ischemic and antianginal action; in patients with left ventricular dysfunction and circulatory failure - favorably affects hemodynamic parameters, increases the ejection fraction of the left ventricle and reduces its size.
Pharmacokinetics
Carvedilol is rapidly absorbed from the gastrointestinal tract. It has a high lipophilicity. Cmax in the blood is reached after 1-1.5 hours. T1 / 2 is 6-10 hours. It binds to plasma proteins by 95-99%. The bioavailability of the drug is 24-28%. Eating does not affect bioavailability. Metabolized in the liver with the formation of a number of active metabolites - 60-75% of the adsorbed drug is metabolized during the "first pass" through the liver. Metabolites have a pronounced antioxidant and adrenoceptor blocking effect. Excretion of the drug from the body occurs through the gastrointestinal tract.
In case of impaired renal function, the pharmacokinetic parameters of carvedilol do not change significantly.
In patients with impaired liver function, the systemic bioavailability of carvedilol is increased by reducing metabolism during the "first pass" through the liver. Carvedilol crosses the placental barrier and is excreted in breast milk.
Indications for use
• arterial hypertension (in monotherapy and in combination with diuretics);
• chronic heart failure (as part of combination therapy);
• IHD: stable angina.
Contraindications
• acute and decompensated chronic heart failure requiring intravenous administration of inotropic agents;
• severe liver failure;
• AV-blockade II-III st.;
• severe bradycardia (less than 50 bpm);
• sick sinus syndrome;
• arterial hypotension (systolic blood pressure less than 85 mm Hg);
• cardiogenic shock;
• bronchial asthma;
• chronic obstructive pulmonary disease;
• age up to 18 years (efficacy and safety have not been established);
• hypersensitivity to carvedilol or other components of the drug.
Dosage and administration
Inside, regardless of the meal. The tablets are swallowed whole, without chewing, with water.
Arterial hypertension
The initial dose is 6.25-12.5 mg 1 time / day in the first two days of treatment. Then - 25 mg 1 time / day. In case of insufficiency of the antihypertensive effect after 2 weeks of therapy, the dose can be increased by 2 times. The maximum recommended dose of the drug is 50 mg 1 time / day (possibly divided into 2 doses).
Chronic heart failure
The dose is selected individually, under the close supervision of a physician. The recommended initial dose is 3.125 mg 2 times / day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times / day, then up to 12.5 mg 2 times / day, then up to 25 mg 2 times / day. The dose should be increased to the maximum that is well tolerated by the patient. In patients weighing less than 85 kg, the target dose is 50 mg/day; in patients weighing more than 85 kg, the target dose is 75-100 mg / day.
ischemic heart disease
The initial dose is 12.5 mg 2 times / day in the first two days of treatment. Then - 25 mg 2 times / day. If the antianginal effect is insufficient, after 2 weeks of therapy, the dose can be increased by 2 times. The maximum recommended daily dose of the drug is 100 mg divided into 2 doses.
Special instructions and precautions
With caution, the drug is prescribed for bronchospastic syndrome, chronic bronchitis, emphysema, AV blockade of the 1st degree, unstable angina pectoris, in the treatment of alpha1-blockers or alpha2-adrenomimetics, with the combined use of MAO inhibitors, depression, myasthenia gravis, renal failure.
Patients with severe heart failure (greater than NYHA grade III), electrolyte imbalance, low blood pressure (less than 100 mm Hg), or elderly patients should be under close medical supervision within 2 hours after the first dose or after taking the first increased dose, due to the risk of developing a sudden drop in blood pressure, orthostatic hypotension and syncope. The risk of these complications can be reduced by prescribing the drug in small initial doses and taking it with meals.
The drug is not recommended for use in patients with low blood pressure.
In patients with heart failure, if their initial SBP is less than 100 mm Hg. Art. or there are concomitant diseases - ischemic heart disease, peripheral vascular disease or impaired renal function, you should check the condition of the urinary system more often, because. treatment may affect kidney function (usually temporarily). If inhibition of renal function is observed, the dose of the drug should be reduced or treatment should be discontinued.
Like other beta-blockers, Carliv may mask the symptoms of hypoglycemia and adversely affect carbohydrate metabolism. Accordingly, during treatment, patients with diabetes require special attention and more frequent measurement of blood sugar.
Treatment with Carliv may mask symptoms of hyperthyroidism. With the sudden withdrawal of the drug, an increase in thyrotoxicosis is likely and a thyrotoxic crisis is possible.
Treatment with the drug in patients with established pheochromocytoma should not be initiated until appropriate therapeutic blockade of alpha-adrenergic receptors.
Treatment with Carliv in patients with psoriasis requires a benefit/risk assessment, as may exacerbate the disease or cause symptoms.
The use of the drug may reduce the sensitivity of allergic tests.
When using Karliva, general anesthesia should be carried out with caution using drugs with a negative inotropic effect (ether, cyclopropane, trichlorethylene). Before extensive surgical interventions, a gradual withdrawal of the drug is recommended.
Care must be taken when using the drug in case of severe metabolic acidosis.
Drinking alcohol should be avoided while using Carliv.
Stop treatment should be gradual, reducing the dose.
Carliv can cause bradycardia, with a decrease in heart rate (below 55 beats per minute), the dose of the drug should be reduced.
Caution is necessary when prescribing the drug to patients with peripheral vascular disease (including Raynaud's syndrome), since beta-blockers can increase the symptoms of arterial insufficiency.
Non-selective beta-blockers may cause pain in patients with Prinzmetal's angina. In such cases, the drug should be administered with caution.
Influence on the ability to drive vehicles and mechanisms
It is not recommended to drive a car at the beginning of therapy and when increasing the dose of the drug. You should refrain from other activities associated with the need for a high concentration of attention and quick psychomotor reactions.
Use during pregnancy and during breastfeeding
Contraindicated in pregnancy and during breastfeeding .
Interaction with other drugs
With the combined use of carvedilol with agents that deplete catecholamine reserves (reserpine, MAO inhibitors), severe bradycardia and arterial hypotension are possible.
Calcium channel blockers (verapamil, diltiazem) and antiarrhythmic drugs (especially class I) while taking carvedilol can provoke severe arterial hypotension and heart failure. In / in the introduction of these drugs in conjunction with taking carvedilol is contraindicated.
With alpha- and beta-adrenergic agonists, hypertension, severe reflex bradycardia and asystole may occur, as well as a decrease in the beta-blocking effect of carvedilol.
Clonidine and carvedilol may enhance each other's ability to lower blood pressure and heart rate. When used together, the withdrawal should be made gradually: carvedilol is first excluded, then, after a few days, clonidine can be gradually stopped.
With the simultaneous use of carvedilol with digoxin, AV conduction slows down.
Insulin and oral hypoglycemic agents increase the hypotensive effect of carvedilol and mask the symptoms of hypoglycemia. Therefore, in patients with diabetes, regular monitoring of blood sugar levels is recommended.
Nitrates and antihypertensive drugs (clonidine, guanethidine, alpha-methyldopa, guanfacine, etc.) enhance the hypotensive effect of carvedilol and reduce heart rate.
Means for anesthesia increase the negative inotropic effect and the hypotensive effect of carvedilol.
Drugs affecting the central nervous system (hypnotics, tranquilizers, tricyclic antidepressants and ethyl alcohol) and carvedilol mutually reinforce each other's effects.
NSAIDs reduce the hypotensive effect of carvedilol due to a decrease in PG production.
When carvedilol is co-administered with ergotamine, the vasoconstrictor effect of ergotamine must be taken into account.
Xanthine derivatives (aminophylline, theophylline) reduce the beta-adrenergic blocking effect of carvedilol.
Inhibitors of microsomal oxidation (cimetidine) increase, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol.
With the simultaneous use of cyclosporine, the concentration of the latter increases (correction of the daily dose of cyclosporine is recommended).
Side effect
From the nervous system: dizziness, headache (usually not strong and at the beginning of treatment), loss of consciousness, myasthenia gravis (more often at the beginning of treatment), increased fatigue, depression, sleep disturbance, paresthesia.
On the part of the organ of vision: blurred vision, decreased tearing.
From the side of the cardiovascular system: bradycardia, orthostatic hypotension, AV block II-III stage, rarely - peripheral circulatory disorders, progression of heart failure (during the period of increasing doses), edema of the lower extremities, angina pectoris, a pronounced decrease in blood pressure.
From the digestive system: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of hepatic transaminases.
From the hemopoietic system: rarely - thrombocytopenia, leukopenia.
From the side of metabolism: weight gain, impaired carbohydrate metabolism.
From the respiratory system: shortness of breath and bronchospasm (in predisposed patients).
From the urinary system: rarely - impaired urination, impaired renal function.
From the musculoskeletal system: myalgia, arthralgia.
Allergic reactions: skin allergic reactions.
Other: exacerbation of psoriasis, nasal congestion, flu-like syndrome, sneezing, pain in the limbs, intermittent claudication.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms: decrease in blood pressure (accompanied by dizziness or fainting), bradycardia. Shortness of breath due to bronchospasm and vomiting may occur. In severe cases, cardiogenic shock, respiratory failure, confusion, and conduction disturbances are possible.
Treatment is symptomatic. It is advisable to use intravenous m-anticholinergics (atropine), adrenomimetics (epinephrine, norepinephrine). It is necessary to monitor and correct vital signs, if necessary - in the intensive care unit.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 30 0 C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the packaging.
Holiday conditions
Released by prescription.
Release form
14 tablets in an aluminum foil blister. 2 blisters with instructions for use in a cardboard box.