Composition, form of production and packaging
Capsules retard gelatin, white, size 1; the contents of the capsules are white or almost white granules.
1 caps.
isosorbide-5-mononitrate 60 mg
Excipients: ethylcellulose, corn starch, sucrose, talc.
The composition of the capsule shell: gelatin, titanium dioxide.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Peripheral vasodilator with predominant effect on venous vessels. Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in cGMP (mediator of vasodilation).
Reduces the need for myocardium in oxygen by reducing preload and postload (reduces the final diastolic volume of the left ventricle and reduces the systolic tension of its walls). Possesses coronary dilatation.
Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of circulation and regression of symptoms with pulmonary edema. Promotes redistribution of coronary blood flow in the area with reduced blood circulation. Increases tolerance to physical activity in patients with IHD, angina pectoris.
It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.
The possibility of developing cross-tolerance to other nitrates is not ruled out.
After a break in the application, the sensitivity to the drug is quickly restored.
PHARMACOKINETICS
Suction and distribution
When ingested quickly and completely absorbed from the digestive tract. Bioavailability is 90-100%. C max is reached after 8 hours. Binding to plasma proteins is less than 4%.
Metabolism and excretion
Isosorbide-5-mononitrate is almost completely metabolized in the liver with the formation of inactive metabolites.
T 1/2 is 4-5 hours. It is almost completely excreted in the urine in the form of metabolites, 2% is excreted unchanged.
INDICATIONS
- prevention of angina attacks in patients with ischemic heart disease;
- treatment of chronic heart failure (as part of combination therapy).
DOSING MODE
Olikard 40 retard appoint 1 caps. 1 time / day. If necessary, the dose of the drug can be increased to 2 caps / day. In this case, the drug should take 1 caps. 2 times / day.To maintain the therapeutic effect, it is necessary to take the drug a second time not later than 6 hours after the first dose.
Olikard 60 retard appoint 1 caps. 1 time / day.
Capsules should be taken without chewing and washing down with a sufficient amount of liquid (a glass of water).
SIDE EFFECT
From the side of the cardiovascular system: "nitrate" headache, marked decrease in blood pressure and / or orthostatic arterial hypotension, which can be accompanied by reflex tachycardia, dizziness, sensation of weakness, short-term hyperemia of the skin; rarely - a bradycardia, a collapse; in some cases - increased symptoms of angina on the background of severe arterial hypotension.
From the side of the digestive system: nausea, vomiting.
Allergic reactions: cutaneous manifestations.
Dermatological reactions: exfoliative dermatitis.
CONTRAINDICATIONS
- acute circulatory failure (shock, vascular collapse);
acute myocardial infarction;
- cardiogenic shock (if by means of intra-aortic counterpulsation or with the help of preparations having a positive inotropic effect, it is not possible to provide a sufficiently high final diastolic pressure in the left ventricle);
- severe arterial hypotension (systolic blood pressure below 90 mm Hg) and hypovolemia;
- simultaneous reception sildenafil;
- children's and adolescence under 18 years (effectiveness not established);
- hypersensitivity to isosorbide-5-mononitrate, the components of the drug and other nitro compounds.
PREGNANCY AND LACTATION
The use of Olikard retard during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be applied to the drug with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be applied to the drug with severe hepatic insufficiency.
SPECIAL INSTRUCTIONS
With caution should be used in idiopathic hypertrophic subaortal stenosis, constrictive pericarditis and cardiac tamponade, low values ​​of perfusion pressure, incl. with acute myocardial infarction or lack of left ventricle of the heart, aortic and / or mitral stenosis, orthostatic hypotension, diseases accompanied by increased intracranial pressure, severe anemia, angle-closure glaucoma, marked renal and hepatic insufficiency.
Olikard retard is not intended for arresting an acute attack of angina pectoris, acute myocardial infarction.
To prevent the development of tolerance to the drug Olikard retard should avoid its continuous intake in high doses.
Impact on the ability to drive vehicles and manage mechanisms
Since Olikard retard can cause a decrease in the ability to concentrate, patients taking the drug should be careful when engaging in potentially dangerous activities requiring increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: marked decrease in blood pressure, collapse, reflex tachycardia, headache, weakness, dizziness, skin flushing, nausea, vomiting and diarrhea. Large amounts of nitrite ion can cause methaemoglobinemia, cyanosis, dyspnea and tachypnea.
At very high doses of the drug, an increase in intracranial pressure with cerebral symptoms may develop.
In chronic overdose, an elevated level of methemoglobin is detected.
Treatment: gastric lavage. If there is a marked decrease in blood pressure and / or shock, plasma replacement therapy should be performed; in exceptional cases, infusion of norepinephrine and / or dopamine may be administered.
The use of epinephrine (adrenaline) and related compounds is contraindicated.
At methemoglobinemia enter: ascorbic acid - 1 g IV; 1% solution of methylthioninium chloride (methylene blue) - 1-2 mg / kg (up to 50 ml) in / in; conduct oxygen therapy, hemodialysis, blood transfusion.
DRUG INTERACTION
With the simultaneous use of the drug Olikard retard with antihypertensive drugs, vasodilators, antipsychotics, tricyclic antidepressants, procainamide, quinidine, beta-adrenoblockers, slow calcium channel blockers, dihydroergotamine, sildenafil and ethanol, hypotensive effect may increase.
With the combination of Olikarda retard with amiodarone, propranolol, blockers of slow calcium channels (including verapamil, nifedipine), the antianginal effect may increase.
Under the influence of adrenostimulants, alpha-adrenoblockers (including dihydroergotamine), it is possible to reduce the antianginal effect of Olicard retard (excessive decrease in blood pressure and, consequently, coronary perfusion).
Olikard retard with simultaneous application reduces the effect of vasopressor drugs.
With the combined use of olikarda retard with m-holinoblokatorami (atropine) increases the likelihood of increased intraocular pressure.
With the simultaneous application of Olikard retard, the concentration of dihydroergotamine in the blood plasma increases.
Barbiturates accelerate metabolism and reduce the concentration of isosorbide-5-mononitrate in blood plasma.
Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide-5-mononitrate in the digestive tract.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
