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Kardiket retard

Kardiket retard (Kardiket retard)

international and chemical name: isosorbide dinitrate; 1, 4, 3, 6-diangidro-D-sorbidu dinitrate;

Main physical and chemical characteristics: white tablets; an upper surface – plainly, with a facet and the distribution line; the lower surface - convex;

Structure. 1 tablet retard includes 20 mg, 40 mg or 60 mg of isosorbide of dinitrate;

other components: lactoses monohydrate, talc, magnesium stearate, polyvinyl acetate, potato starch.

Form of production of medicine. Tablets of the prolonged action.

Farmakoterapevtichesky group. Vazodilatatora, that are applied in cardiology. Code of automatic telephone exchange C01D A08.

Effect of the medicine.

Action mechanism

Like all organic nitrates, isosorbide dinitrate (_SDN) works as the donor of nitrogen oxide (NO). NO leads to relaxation of unstriated muscles of vessels by stimulation of guanylate cyclase and further increase in concentration of an intracellular cyclic guanilatmonofosfat (tsGMF). Thus it is stimulated (tsGMF) - a dependent protein kinase and thereof changes phosphorylations of different proteins in a cell of an unstriated muscle. In turn it leads to dephosphorylation of easy chains of a myosin and decrease in a kontraktilnost.

Pharmacodynamics

_SDN causes relaxation of unstriated muscles of vessels that conducts to a vazodilatation. The phlebectasia promotes venous "deposition" of blood and reduces venous to return to heart; thus the diastolic pressure and volume (preloadings) decreases ventricular final.

Impact on arteries, and at the highest doses – on arterioles to lead to decrease in the system vascular resistance (afterload). It in turn improves function of heart.

To lead influence both on preloadings, and on afterloads to decrease in consumption by oxygen heart.

Besides, _SDN causes redistribution of a blood-groove to subendocardial departments of heart in the conditions of atherosclerotic defeat. The last effect, perhaps, is explained by the selection dilatation of large coronary vessels. Dilatation collateral arteries, caused by nitrates, can improve perfusion of a myocardium at a stenosis of vessels. Besides, nitrates counteract emergence and eliminate coronary spasms.

At patients with congestive heart failure nitrates improve a hemodynamics at rest and at a tension.

Pharmacokinetics

In a digestive tract of _SDN it is released from the tablet prolonged actions slowly within several hours. Absorption of active ingredient high. Bioavailability at reception – 22% (effect of "the first passing" through a liver). Therapeutic concentration is reached in 30 minutes, the maximum concentration (Cmax) – 1 hour. Linkng with proteins of a blood plasma – 30%. The elimination half-life makes 12 hours of _SDN is metabolized in a liver with formation of isosorbide-2-mononitrate (T1/2 – 1,5 – 2 hours) and isosorbide-5-mononitrate (T1/2 - 4 – 6 hour). Both metabolites have pharmacological activity. It is removed by kidneys (generally in the form of metabolites).

Indications for use.

Treatment and prevention of stenocardia (including after a myocardial infarction);

treatments of heavy chronic heart failure in a combination with glycosides, diuretics, APF inhibitors.

Way of use and dose in the absence of other recommendations to apply irrespective of reception of food, without chewing and washing down with enough water. When it is necessary to halve a tablet, it should be put on a firm surface the line of a break up and to press on a tablet a thumb. A tablet it is easy to be divided into 2 halves.

Kardiket retard 20: on 1 tablet 2 times a day. The friend / should accept the following dose not earlier, than in 6 – 8 hours after reception of the first dose. At the increased need for nitrodrugs it is possible to increase a daily dose to 1 tablet 3 times a day, with an interval of 6 hours (about the 6th, 12th hour, and, the last dose – about the 18th hour).

Kardiket retard 40: on 1 tablet once a day or on ½ tablets 2 times a day. The friend / should accept the following dose not earlier, than in 6 – 8 hours after reception of the first dose. At the increased need for nitrodrugs it is possible to increase a daily dose to 1 tablet 2 times a day; it is recommended to accept the last dose about the 18th hour.

Kardiket retard 60: on 1 tablet once a day. At the increased need for nitrodrugs it is possible to increase a daily dose to 1 tablet 2 times a day. The friend / should accept the following dose not earlier, than in 6 – 8 hours after reception of the first dose.

Treatment should be begun with the smallest doses, slowly increasing a dose to necessary. The maximum daily dose makes 120 mg. Duration of a course of treatment is defined individually. Drug is appointed for long use which cannot be stopped sharply.

There are no certificates about need to change dosages for patients of advanced age.

Side effect. Undesirable effects can be defined as very frequent (≥1/10), frequent (≥1/100, <1/10), not frequent (≥1/1 000, <1/100), liquid (≥1/10 000, <1/1 000) or very liquid (<1/10 000).

At Kardiket's use retard the undesirable phenomena provided below can be observed.

Heart. Frequent: reflex tachycardia; not frequent: strengthening of symptoms of stenocardia, lowering of arterial pressure.

Vascular system. Frequent: hypotension in a standing position, including orthostatic reactions; not frequent: a collapse (which sometimes is followed by bradycardia and a syncopal state).

At use of organic nitrates reported about heavy hypotensive reactions that were followed by nausea, vomiting, feeling of concern, pallor and the raised potovydeleniye.

Digestive tract. Not frequent: nausea, vomiting; very liquid: heartburn.

The general state. Frequent: feeling of weakness.

Nervous system. Very frequent: a headache ("nitrate the main pain") that gradually decreases at further administration of drug;

frequent: dizziness, drowsiness.

Skin and hypodermic fabric. Not frequent: allergic skin reactions (for example rash), reddening;

very liquid: vascular hypostasis, in some cases – exfoliative dermatitis.

Note. During therapy by Kardiket retard there can be temporary an anoxemia through relative redistribution of a blood-groove in alveolar zones with hypoventilation. Separately, at patients with coronary heart disease it can lead to a myocardium hypoxia.

Contraindications.

Drug is contraindicated

at hypersensitivity to isosorbide of dinitrate, other nitrate connections or to any excipient;

at an acute circulatory unefficiency (shock, a collapse);

at cardiogenic shock (if the corresponding receptions do not support the sufficient level of end diastolic pressure);

at hypertrophic obstructive cardiomyopathy;

at chronic cardial compression;

at a cardiac tamponade;

at heavy hypotension (the systolic blood pressure is lower than 90 mm hg);

During therapy by nitrates it is impossible to apply phosphodiesterase inhibitors, for example sildenafit.

Overdose.

Overdose symptoms

90 mm lowered a blood pressure ≤ hg.

Pallor.

The strengthened potovydeleniye.

Weak pulse fillings.

Tachycardia.

Faints (including orthostatic reactions when changing position of a body).

Headache.

Weakness.

Nausea.

Vomiting.

Diarrhea.

Concerning patients who accepted other nitrates, it is reported about methemoglobinemia cases. During biotransformation of isosorbide of dinitrate nitrite ions are released that can cause a methemoglobinemia and cyanosis with a further tachypnea, feeling of alarm, a loss of consciousness and a cardiac standstill. It is not possible to exclude possibilities of this collateral reactions at dinitrate isosorbide overdose.

Overdoses can increase the intracranial pressure which sometimes causes cerebral symptoms.

General measures:

to stop intake of drug;

general measures which apply in case of the hypotension caused by nitrates:

to give to the patient of horizontal position with the hung head at a low headboard;

to provide intake of oxygen;

to increase the circulating volume;

to carry out special antishock therapy (the patient has to is in an intensive care unit).

Special measures

There is no specific antagonist of vasodilating effect of isosorbide of dinitrate. As hypotension that develops at overdose, is result of a venodilatation and an arterial hypovolemia, therapy has to be directed to increase in volume of the circulating blood (see. "Systemic effects"). Sometimes happens to give to the patient of horizontal position enough. Sometimes it is necessary to make intravenous infusion physiological (or similar to it) solution. Use of adrenaline in such situation is not recommended (exceeds harmful effect over positive).

Treatment of a methemoglobinemia

Vidnovlyuvalna therapy with vitamin C, methylene blue or toluydinsiny – behind the choice;

oxygen uses (in case of requirement);

artificial ventilation, blood replacement (in case of requirement).

hemodialysis (in case of requirement).

Resuscitation measures:

in case of signs of an apnoea or blood circulation immediately use resuscitation actions.

Features of use.

Kardiket retard should be applied with special care and under the supervision of the doctor

at low filling pressures (for example at an acute myocardial infarction, dysfunction of a left ventricle (left gastric insufficiency);

at an aortal and/or mitral stenosis;

at orthostatic dysfunction;

at anemia;

at renal (hepatic) failure;

to patients of advanced age;

at surgical interventions;

at closed-angle glaucoma;

at a craniocereberal injury, a hemorrhagic stroke and other diseases, followed by the increased intracranial pressure.

Described tolerance development (decrease in efficiency), and also cross tolerance to the others of drugs of nitrate type (decrease in effect if the patient before that accepted other nitrate). For prevention decrease or loss of effect should avoid long reception of large doses (120 mg a day).

Patients who are on a maintenance therapy Kardiketom retard have to be informed that they cannot accept drugs which contain phosphodiesterase inhibitors (for example sildenafit), because of risk of development of not controlled hypotension.

Because drug includes lactose, it patients cannot appoint absorption of glucose and a galactose with such rare genetic diseases as intolerance of a galactose, hereditary laktozo-deficit of Lapp, disturbance.

Because drug includes sucrose, patients cannot appoint drug with such rare genetic diseases as intolerance of fructose, disturbance absorption of glucose and a galactose, sakharozo-izomaltazny insufficiency.

Period of pregnancy and lactation.

The adequate and controlled researches at pregnant women are absent. Kardiket retard should be applied during pregnancy only on an urgent need if the advantage of use exceeds potential risk, and at continuous supervision of the doctor.

It is unknown, or dinitrate with milk of the person is removed isosorbide. As many drugs are allocated thus, it is not recommended to appoint Kardiket retard to women who nurse.

Influence on ability to manage motor transport and mechanisms.

Kardiket retard can cause change of reaction to it a step that it will influence ability to take active participation in traffic or to work with exact mechanisms. This action amplifies at a combination with alcohol.

Experience of use of Kardiket retard for treatment of children is absent.

Interaction with other medicines. Hypotensive action of Kardiket retard can amplify at simultaneous use with anti-hypertensive drugs, for example with beta-blockers, blockers of calcium channels, vazodilatator, neuroleptics and cyclic antidepressants, and also at alcohol intake. Hypotensive action of Kardiket retard to lodge at a concomitant use with phosphodiesterase inhibitors (for example with sildenafily), and it can bring to unsafe for life of cardiovascular complications. Patients who are on therapy by Kardiket retard should not apply phosphodiesterase inhibitors (for example sildenafit). In case of requirement sildenafit it is necessary to accept not earlier, than in 72 hours after Kardiket's reception retard.

There were messages that simultaneous use of Kardiket retard and dihydroergotamine can lead to increase in concentration of dihydroergotamine in blood and thus strengthen its hypertensive action.

Conditions and periods of storage. To store in the place, unavailable to children. To store at a temperature not above 25 °C.

Period of validity – 5 years.

 
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