Kordafen
Producer: JSC Himfarm Republic of Kazakhstan
Code of automatic telephone exchange: C08CA05
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent - mg nifedipine 10, 0.
Excipients: potato starch, lactoses monohydrate, cellulose microcrystallic, gelatin, talc, magnesium stearate.
Structure of a cover: gipromelloza, macrogoal 6000, titanium dioxide (Е 171), talc, propylene glycol, dye varnish quinolinic yellow (Е 104).
Pharmacological properties:
Pharmacokinetics. Absorption. Nifedipine quickly and almost completely (90%) is soaked up from a digestive tract. The phenomenon of primary passing through a liver is characteristic of nifedipine, about 45-75% of a peroral dose get in not changed look into blood, Cmax is reached in 0,5-2 h. Food reduces nifedipine absorption speed, but does not influence amount of the absorbed drug. Biological availability of nifedipine increases at patients with cirrhosis.
Distribution. Nifedipine contacts proteins of a blood plasma for 92-98%. Linkng with proteins decreases at patients with a liver or renal failure. Less than 5% get through a blood-brain barrier, a fetoplacental barrier and is allocated with breast milk. Drug does not kumulirutsya.
Metabolism. Drug will quickly and completely be transformed in a liver to inactive metabolites. Metabolism is carried out mainly by oxidation of dihydropyridine and one of methyl groups in oxymethyl, and also by hydrolysis of radio group in carboxyl.
Removal. At patients with normal function of kidneys and a liver the elimination half-life of nifedipine makes 2-5 hours. About 80% of nifedipine are removed in the form of metabolites with urine (less than 1% in an invariable look), the rest – with bile.
At patients with a liver failure time of removal of drug increases.
Pharmacodynamics. Кордафен® (derivative dihydropyridine) treats group of antagonists of calcium. Drug does not influence concentration of calcium ions in blood serum. The mechanism of effect of drug consists in braking of receipt of calcium ions in cells of a myocardium and in cells of smooth muscles of blood vessels.
Drug reduces contractility of preferential smooth muscles of vessels, than a myocardium.
Expanding blood vessels, Kordafen® reduces the peripheric resistance of vessels, arterial pressure of blood. Thereby reducing the need of a myocardium for oxygen and stenocardia symptoms.
Indications to use:
- vasospastic stenocardia (Printsmetal's stenocardia, alternative stenocardia)
- Reynaud's syndrome
Route of administration and doses:
The tablets Kordafen® are intended for intake.
Adults: a usual dose of 10 mg 3 times a day.
In case of need it is possible to raise a dose to 20 mg 3 times a day under control of arterial pressure of blood. The maximum daily dose makes 60 mg.
Drug can be accepted irrespective of meal. Tablets should be swallowed entirely, washing down with a small amount of liquid.
Features of use:
Кордафен® can strengthen symptoms of coronary heart disease, including cause displays of an acute myocardial infarction in the patients beginning treatment with drug or raising a dose of drug or at its prolonged use that is probably connected with its action - aritmogenny, decrease in blood supply of a myocardium, and also insignificant negative inotropic effect.
At patients, treated beta-blockers, it is not necessary to interrupt suddenly treatment with these means (prior to therapy of Kordafenom®) owing to emergence of a withdrawal and strengthening of symptoms of coronary insufficiency.
Кордафен® it is necessary to apply carefully at patients with heart failure or an aortostenosis (especially, receiving beta-blockers as Kordafen® can accelerate display of the existing heart failure) a mitral stenosis, the hypertrophic cardiomyopathy expressed by bradycardia or tachycardia, heavy disturbances of cerebral circulation, a myocardial infarction with a left ventricular failure, a liver and renal failure, to the patients accepting cardiac glycosides and elderly people.
Кордафен®, reducing peripheric resistance, can cause hypotonia. Therefore, it is necessary to control arterial pressure during an initial stage of treatment and after each increase in a dose of drug.
Кордафен® in shape with bystry release it is not necessary to apply to the long treatment of an idiopathic hypertensia and other diseases demanding use of drug in the dose exceeding 60 mg a day.
At prolonged use development of tolerance and a withdrawal is possible.
If during treatment of Kordafenom® the patient needs to carry out surgical intervention under the general anesthesia, it is necessary to warn the anesthesiologist, about administration of drug.
At patients with abnormal liver functions and/or kidneys it is necessary to avoid use of drug in high doses.
Cases of increase in a liver and stagnation of bile were noted. At reception of high doses of Kordafena® increase in activity of transaminases of a liver, emergence of an intra hepatic cholestasia is possible. At patients with cirrhosis time of removal of Kordafena® can increase up to 7 days.
Laboratory tests. Кордафен®, like other drugs from group of antagonists of calcium, reduces aggregation of thrombocytes of in vitro. At some patients drug increased a bleeding time that is connected probably with braking of transport of calcium ions a cellular cover of thrombocytes.
The patients accepting Kordafen® can have a false positive reaction of Koombs, hemolitic anemia.
Owing to a lowering of arterial pressure of Kordafen® can limit ability of control of automobiles and service of the mechanical equipment.
Side effects:
Manifestation of side effect depends on a drug dose.
- skin itch, small tortoiseshell, dieback
- face reddening, feeling of heat
- weakness, drowsiness
- nausea, dryness of a mucous membrane of an oral cavity, increase in appetite, diarrhea or lock; seldom - a hyperplasia of gums (bleeding, morbidity, puffiness), at long reception - abnormal liver functions (an intra hepatic cholestasia, increase in activity of "hepatic" transaminases)
- muscular spasms, tremor, paresthesias
- peripheral hypostases
- nervousness, changeable mood
- reflex tachycardia, tranzitorny hypotonia, emergence of attacks of stenocardia, myocardial infarction, development or aggravation of heart failure, arrhythmia, ventricular arrhythmia
- anemia, leukopenia, thrombocytopenia
- the complicated breath, cough, a fluid lungs
- hyperemia of mucous membranes of a nose, pharyngitis
Interaction with other medicines:
APF inhibitors, antagonists of receptors of angiotensin-II, diuretics, nitrates, Cimetidinum (to a lesser extent ranitidine), tricyclic antidepressants, inhalation anesthetics.
At use with Kordafenom® the hypotensive effect amplifies.
Prazozinum and other alpha adrenoblockers. Suppresses metabolism of Prazozinum and other alpha adrenoblockers owing to what strengthening of hypotensive effect is possible.
Beta-blockers. At simultaneous use of Kordafena® with beta-blockers hypotension and heart failure is possible.
Sympathomimetics, NPVS, are oestrogenic. Sympathomimetics, NPVS (suppression of a sitez of PG in kidneys and Na delay + and liquids in an organism), estrogen (a liquid delay in an organism) reduce hypotensive effect of Kordafena®.
Nitrates. At a combination to nitrates strengthening of tachycardia is noted.
Calcium drugs. Drugs of calcium can reduce effect of blockers of calcium channels.
The quinidine and other medicines causing lengthening of an interval of Q-T. Кордафен® lowers concentration of quinidine in a blood plasma, after nifedipine cancellation perhaps sharp increase in its concentration in blood, and also at combined use of a kordafen with the quinidine or other medicines causing lengthening of an interval of Q-T the risk of considerable lengthening of an interval of Q-T is increased.
Amiodaronum and quinidine. Blockers of slow calcium channels strengthen negative inotropic effect of Amiodaronum and quinidine.
Foxglove glycosides. Кордафен® increases the level of glycosides of a foxglove in blood serum therefore in an initiation of treatment these drugs it is necessary to control concentration of glycosides to avoid their overdose.
Theophylline. Кордафен® increases theophylline level in blood serum.
Indirect anticoagulants, anticonvulsants, NPVS, quinine, salatsilata, Sulfinpyrazonum. Кордафен® can force out from communication with proteins derivatives of coumarin and an indandion (thereby increasing a prothrombin time), anticonvulsants, NPVS, quinine, salicylates, Sulfinpyrazonum owing to what their plasma concentration can increase.
Inductors of microsomal enzymes of a liver. Inductors of microsomal enzymes of a liver (rifampicin, etc.) reduce concentration of nifedipine.
Vincristinum. Nifedipine reduces removal of Vincristinum from an organism.
Cimetidinum, ranitidine and famotidine. Cimetidinum applied together with Kordafenom® increases concentration of nifedipine in blood serum. The mechanism of this interaction is connected with braking by Cimetidinum of function of the R-450 cytochrome of a liver which is responsible for nifedipine metabolism. At the same time, simultaneous use of Kordafena® with famotidine and ranitidine has no significant effect on nifedipine metabolism.
Alcohol. Alcohol increases biological availability of nifedipine.
Contraindications:
- hypersensitivity to nifedipine or excipients
- ventricular tachycardia
- heavy heart failure
- heavy arterial hypotension (systolic the ABP is lower than 90 mm hg)
- the expressed aortal or subaortal stenosis
- the first 4 weeks after a myocardial infarction
- unstable stenocardia and heavy attacks of stenocardia
- pregnancy and period of a lactation
- children's and teenage age up to 18 years (there are no proofs of safety)
Overdose:
Symptoms: strengthening of symptoms of side effects, including - hypotonia, bradycardia.
Treatment: symptomatic at a serious poisoning carry out a gastric lavage, appoint absorbent carbon. An antidote are calcium salts. The hemodialysis is inefficient.
Storage conditions:
To store in the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children!
Issue conditions:
According to the recipe
Packaging:
On 10 tablets place in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.
On 5 planimetric packagings together with the instruction on a medical use in the state and Russian languages put in a pack from a cardboard.
