KARVEDIGAMMA
Active material: Karvedilol
When ATH: C07AG02
CCF: Beta1-,beta2-adrenoblokator. Alpha1-adrenoblokator
When CSF: 01.01.01.01.02
Manufacturer: WÖRWAG PHARMA GmbH & Co. KG (Germany)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Pills, Film-coated white, oblong; on one side – stamping “12.5”, risks on both sides.
| 1 tab. | |
| karvedilol | 12.5 mg |
Excipients: microcrystalline cellulose, lactose monohydrate, krospovydon, povidone, colloidal silicon dioxide, magnesium stearate, Opadry II White YS-22-18096 (Titanium dioxide, polydextrose, Valium 3br, gipromelloza 6sp, triэtiltsitrat, gipromelloza 50SP, macrogol-8000).
10 PC. – blisters (3) – packs cardboard.
DESCRIPTION OF ACTIVE SUBSTANCES.
Pharmacological action
The antihypertensive agent of the group of alpha- and beta-blockers without intrinsic sympathomimetic activity. blocks α1-, b1– и b2-adrenoreceptory. The blockade of β1-adrenoceptor moderately reduces the conductivity, strength and heart rate, without causing severe bradycardia. The blockade of α1-adrenoceptor causes dilation of peripheral blood vessels. The blockade of β2-adrenoceptor may slightly raise the tone of the bronchi, Some microvascular, as well as the tone and peristalsis.
Pharmacokinetics
Once inside quickly and almost completely absorbed from the gastrointestinal tract. Cmax plasma levels reached within 1 no. Bioavailability is 25%.
Plasma protein binding – 98-99%. Vd – about 2 l / kg. It penetrates through the placental barrier, excreted in breast milk. Treated effect “first pass” through the liver. Metabolites have a pronounced anti-oxidant and adrenoblokirutm action.
T1/2 – 6-10 no. Plasma clearance – 590 ml / min. Displayed, primarily, the bile.
In patients with impaired liver function may increase the bioavailability before 80%.
Testimony
Arterial hypertension.
Angina.
Congestive heart failure (in a combination therapy).
Dosage regimen
Is the inside. The initial dose – 12.5 mg 1 time / day, then increase the dose to 25 mg 1 time / day. If necessary, the dose can be increased 1 once every 2 of the week; the maximum dose – 50 mg / day. Elderly patients may be an effective dose 12.5 mg / day.
Side effect
Cardio-vascular system: at the beginning of treatment (first dose effect) and with increasing doses episodes possible excessive decrease of blood pressure (These phenomena are usually on their own and the patient's condition is stable without special correction); with the further application of carvedilol is also possible bradycardia; rarely observed violations of peripheral blood flow, angina, AV блокада, episodes of intermittent claudication; in some cases – increasing incidence of heart failure.
From the central and peripheral nervous system: possible weakness, fatiguability, headache; in some cases – sleep disorders, mental depression, paresthesia.
From the digestive system: tone and increase intestinal motility; in some cases – change transaminase activity in blood plasma.
Allergic reactions: rarely – an allergic rash, itch.
Dermatological reactions: hives, reaction, resembling lichen planus, the appearance of psoriatic lesions or worsening of pre-existing psoriasis.
The respiratory system: in some cases – nasal congestion.
From the hematopoietic system: in some cases – thrombocytopenia, leukopenia.
Contraindications
AV-blockade II and III degrees, vыrazhennaya bradycardia, heart failure decompensation, shock, bronchial asthma, chronic lung diseases with BOS syndrome history, hepatic failure, pregnancy, lactation, Hypersensitivity to carvedilol.
Pregnancy and lactation
Carvedilol is contraindicated during pregnancy and lactation (breast-feeding).
Although there is no direct evidence of embryo- or fetotoksicheskoe action carvedilol, it is known, it crosses the placenta and is excreted in breast milk. blockade of α- and β-adrenergic receptors in the fetus or neonate can induce prenatal or neonatal distress syndrome, proyavlyayuschyysya bradycardia, respiratory depression, hypothermia and hypoglycemia.
Cautions
To use caution in patients with coronary artery disease and heart failure. Before treatment with carvedilol in heart failure should conduct appropriate therapy to eliminate the symptoms of decompensation.
When applying kardvedilola in patients with coronary artery disease may decrease myocardial oxygen demand (by blocking the β1-adrenoreceptorov). In this connection, the abolition of carvedilol should be done gradually in order to avoid the development of angina attacks.
In patients with endocrine disorders Carvedilol may mask the symptoms of hyperthyroidism, and the early signs of acute hyperglycemia (what must be avoided in patients with insulin-dependent diabetes mellitus).
During the period of treatment is not recommended the use of alcohol.
Clinical experience with carvedilol in pediatrics missing.
Effects on ability to drive vehicles and management mechanisms
Early treatment, as well as by increasing the dose of carvedilol in the treatment should refrain from driving and other activities, related to high concentration and psychomotor quick reactions.
Drug Interactions
While the use of carvedilol antiarrhythmics, for narcosis, antihypertensive drugs, antianginal drugs, other beta-blockers (incl. as eyedrops) there is a risk of unwanted drug interactions.
With simultaneous application of CYP2D6 isozyme inhibitors amplification theoretically possible actions of carvedilol.
With simultaneous application of CYP2D6 isoenzyme inducers system may decrease the action of carvedilol.
While the use of verapamil, diltiazem for the on / in the introduction of the possibility of severe hypotension.
In an application with digoxin may increase the concentration of digoxin in the blood plasma and increased risk of bradycardia and AV-conduction disturbances.
While applying insulin, oral hypoglycemic agents may increase the risk of hypoglycaemia.
While the use of clonidine possible bradycardia, hypotension, conduction disorders. In the case of sudden clonidine patients, receiving carvedilol, possible sharp rise in blood pressure.
If you are applying with rezerpinom, MAO inhibitors, there is a risk of severe hypotension and bradycardia.
When applied simultaneously with rifampicin decreased AUC and Cmax carvedilol plasma.
Fluoxetine inhibits CYP2D6 CYP, which leads to the inhibition of metabolism of carvedilol and its cumulation. This can enhance the effect cardiodepressive (incl. ʙradikardiju). fluoxetine and, mainly, its metabolites are characterized by a long T1/2, so the likelihood of drug interaction is preserved even after a few days after fluoksetina.
While the use of cimetidine increases AUC carvedilol without changing its Cmax plasma.
At simultaneous application with cyclosporine may increase (Low to moderate) the concentration of cyclosporine in the blood plasma.
While the use of derivatives of ergotamine possible deterioration of peripheral circulation.
