Isoket - instructions for use, doses, side effects, contraindications

Active substanceIsosorbide dinitrateIsosorbide dinitrate

Similar drugsTo uncover

Dinisorb

concentrate d / infusion

Isacardin®

spray n / az.

Isacardin®

concentrate d / infusion

Isoket®

concentrate d / infusion

YUSB Farma SpA Italy

Isoket®

spray locally

Cardicet®

pills inwards

YUSB Pharma GmbH Germany

Nitrosorbide

pills inwards

Nitrosorbide

pills inwards

Nitrosorbide

pills inwards

Nitrosorbide

pills inwards

UPDATE OF PFC, CJSC Russia

Dosage form: & nbspfrompre-dosed

Composition:

100 grams of dispensed spray contain:

Active substance: isosorbide dinitrate 2.946 g;

Excipients: Macrogol 400 17.668 g, ethanol 100% 79.386 g

One bottle contains: 12.7 g (15.0 ml) of the drug solution and 3.3 g (3.8 ml) of the excess solution of the preparation;

16.0 g (18.8 ml) of the drug solution contained 471 mg of isosorbide dinitrate.

1 dose (42.45 mg solution of the drug) contains 1.25 mg isosorbide dinitrate.

Description:

Transparent, colorless solution with the smell of alcohol.

Pharmacotherapeutic group:Vasodilating agent - nitrate

ATX: & nbsp

C.05.A.E.02 Isosorbide dinitrate

C.01.D.A.08 Isosorbide dinitrate

Pharmacodynamics:

Isosorbide dinitrate is a peripheral vasodilator with a predominant effect on venous vessels. The mechanism of action is associated with the release of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase,resulting in an increase in the level of cyclic guanosine monophosphate (a mediator of vasodilation). Reduces the need for myocardium in oxygen by reducing preload (reduces course the 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 coronary heart disease, angina pectoris. It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.

Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored.

Pharmacokinetics:

After spraying on the oral mucosa, the effect manifests itself in 1-3 minutes and lasts 90 - 120 minutes.

Absorption is high. Bioavailability through oral mucosa - 60%. Connection with blood plasma proteins - 30%.The half-life is 30-60 minutes. Metabolised in the liver to two active metabolites of isosorbide-2-nitrate and isosorbide-5-nitrate, have half-lives of 1.5 to 2 hours or 4 to 6 hours, respectively.

The drug is excreted by the kidneys (almost completely in the form of metabolites).

Indications:

- Cessation of angina attacks.

- Preventing attacks of angina pectoris.

- Acute myocardial infarction.

- Acute left ventricular failure.

Contraindications:

- Hypersensitivity to isosorbide dinitrate, other nitro compounds or other components of the drug.

- Acute vascular insufficiency (vascular collapse).

- Severe arterial hypotension (systolic blood pressure below 90 mm Hg, diastolic blood pressure - below 60 mm Hg).

- Cardiogenic shock if correction of the end diastolic pressure of the left ventricle with intra-aortic counterpulsation or preparations with a positive inotropic effect is not possible.

- Deficiency of glucose-6-phosphate dehydrogenase.

- Hemorrhage in the brain.

- Hypertrophic obstructive cardiomyopathy.

- Constrictive pericarditis.

- Cardiac tamponade.

- Severe hypovolemia.

- Simultaneous administration of inhibitors of phosphodiesterase-5 (for example, sildenafil, vardenafil or tadalafil), as they potentiate the antihypertensive effect of nitrates.

- Simultaneous reception with a stimulator of soluble guanylate cyclase by rhyociguate.

- Severe anemia.

- Severe aortic and subaortic stenosis, severe mitral stenosis.

- Age to 18 years (efficacy and safety of use not established).

Carefully:

- Low filling pressure of the left ventricle, including acute myocardial infarction, left ventricular dysfunction (eg, left ventricular failure). It is necessary to avoid a decrease in systolic blood pressure of less than 90 mm Hg. Art.

- With aortic and / or mitral stenosis of mild to moderate degree.

- Propensity to orthostatic disorders of vascular regulation.

- Diseases that are accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral injury).

- Elderly age.

- Closed-angle glaucoma (risk of increased intraocular pressure).

- Severe kidney failure.

- Severe hepatic insufficiency (risk of methaemoglobinaemia).

- Hypothyroidism.

- Inadequate and malnutrition.

Pregnancy and lactation:

Fertility

There is no data on the effect of Isoket® on human fertility.

Pregnancy

Adequate and well-controlled clinical studies of the safety of isosorbide dinitrate during pregnancy have not been conducted. In studies of reproductive toxicity conducted in rats and rabbits at doses reaching the level of maternal toxicity, there was no evidence of harmful effects of isosorbide dinitrate on the fetus. Since in animal studies it is not always possible to reproduce the effect of the drug on humans.

The use of Isoket® in pregnancy is possible only strictly according to the doctor's prescription and in the event that the intended benefit to the mother exceeds the possible risk to the fetus and / or the child. In this case, careful monitoring of the condition of the pregnant woman and fetal development is carried out.

Breastfeeding period

There is information about the penetration of nitrates into breast milk, but the exact content of isosorbide dinitrate in breast milk has not been determined. Also, a possible risk of methaemoglobinaemia in infants was reported,so if you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Isoket® Spray is used to spray on the oral mucosa. At the first application and in the event that, after the last application of the Isoket® Spray has passed more than a day, the first dose is released into the air, because it may not be complete. To ensure the necessary effect, it is necessary to press the sprayer continuously and until the end. Do not inhale the spray. When using Isoket® Spray, avoid contact with eyes and skin.

Mode of application:

- Bring the Izoket^®Spray close to the mouth, holding it vertically.

- Take a deep breath.

- Exhale.

- Inject 1 dose (by pressing the nebulizer) into the mouth (this may cause a slight burning of the tongue).

- After taking 1 dose, close your mouth and breathe through your nose within 30 seconds.

Use the information above if your doctor has not given you other advice. Please adhere to the described application conditions, otherwise Isoket® Spray may not have the desired effect.

To stop an attack of angina or before a physical or emotional load that can cause an attack,It is necessary to inject the spray into the mouth 1-3 times with an interval of 30 seconds between injections against the background of a delay in breathing. A single dose of 3 injections to stop an attack can be increased only at the urging of a doctor. In acute myocardial infarction or acute left ventricular failure (taken only under the control of blood pressure (BP), heart rate and medical supervision) at the beginning of 1-3 doses at intervals of 30 s, in the absence of effect for 10 min, one additional dose (only under the supervision of a doctor).

Application the elderly patients

Elderly patients do not need dose adjustment.

Application the children

The effectiveness and safety of isosorbide dinitrate in children have not been established.

Side effects:

Possible side effects are given below for body systems and frequency of occurrence (classification of the World Health Organization): very often (more than 1/10), often (more than 1/100 and less than 1/10), infrequently (more than 1/1000 and less than 1 / 100), rarely (more than 1/10000 and less than 1/1000), very rarely (less than 1/10000), the frequency is unknown (the frequency can not be estimated from available data).

From the central nervous system

Often: headaches ("nitrate" headaches) at the beginning of the treatment, which, as a rule, disappear with further use of the drug.

Often: drowsiness, slight dizziness.

Frequency unknown: blurred vision, inhibition (especially at the beginning of treatment), cerebral ischemia.

From the side of the cardiovascular system

Often: tachycardia, orthostatic hypotension.

Infrequently: "paradoxical" enhancement of angina attacks, collapse (sometimes accompanied by bradyarrhythmia and syncope).

Frequency unknown: marked decrease in blood pressure.

From the gastrointestinal tract

Infrequently: nausea, vomiting.

Rarely: heartburn.

Disturbances from the skin and subcutaneous tissues

Infrequently: skin allergic reactions (including rash), "tides" of blood to the skin of the face.

Rarely: angioedema, Stevens-Johnson syndrome.

Frequency unknown: exfoliative dermatitis.

General violations and violations at the site of introduction

Often: asthenia, burning in the tongue.

Frequency unknown: dryness of the oral mucosa.

Prolonged use of the drug may cause transient hypoxemia due to the relative redistribution of blood flow inhypoventilation alveolar sites (in patients with coronary heart disease - can lead to myocardial hypoxia).

Overdose:

Symptoms: marked decrease in blood pressure (less than 90 mm Hg), pallor, increased sweating, "threadlike" pulse, tachycardia, postural dizziness, throbbing headache, asthenia, nausea, vomiting, diarrhea; increased intracranial pressure (with high doses), methemoglobinemia.

Treatment:

In light cases: transfer of the patient to the "lying" position with raised legs or the lowered head end of the bed;

In more severe cases: with a pronounced decrease in blood pressure - replenishment of circulating blood volume (BCC), administration of norepinephrine (noradrenaline) or other vasoconstrictors (epinephrine (epinephrine) is not recommended); with methemoglobinemia - ascorbic acid 1 g inside or 0.1-0.15 ml / kg 1% solution in the form of sodium salt (not more than 50 ml), oxygen therapy, mechanical ventilation, hemodialysis.

Interaction:

The use of isosorbide dinitrate with antihypertensive agents (for example, beta-adrenoblockers, diuretics, blockers of "slow" calcium channels,inhibitors of angiotensin-converting enzyme), neuroleptics, tricyclic antidepressants, ethanol and ethanol-containing agents can lead to a pronounced decrease in blood pressure.

When used simultaneously with procainamide, quinidine, an antihypertensive effect is also possible.

Simultaneous use of Isoket® with a soluble guanylate cyclase stimulant rhyociguate can cause the development of arterial hypotension.

With simultaneous use with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect.

Under the influence of sympathomimetics, alpha-adrenoblockers (dihydroergotamine and others), the severity of the antianginal effect can be reduced (excessive reduction of blood pressure, and as a consequence - coronary perfusion).

With simultaneous application with dihydroergotamine, an increase in the concentration and increase in the action of dihydroergotamine is possible.

When combined with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure.

Simultaneous use of Isoket® and phosphodiesterase-5 inhibitors (including sildenafil, tadalafil, vardenafil) is contraindicated in view of the possibility of a marked decrease in blood pressure.

Sapropterin is a cofactor of nitric oxide synthase. It is advisable to use caution while using sapropterine-containing medications with all vasodilating agents whose action is associated with nitric oxideNO), including classical donators NO (eg, nitroglycerine, isosorbide dinitrate, isosorbide-5 mono nitrate) and others.

It should be borne in mind that the data given also apply to those cases when the drug was taken recently.

Special instructions:

Each time the sprayer is pressed, an equal amount of solution is sprayed in the form of minute droplets. It easily penetrates the mucous membrane of the mouth and in a few seconds falls into the bloodstream.

Isoket® spray does not contain freon, is environmentally friendly. Another advantage is the transparency of the bottle, which makes it possible to notice the need for replacement in time.

During the therapy, it is necessary to monitor blood pressure and heart rate.

Avoid abrupt discontinuation of the drug, reduce the dose gradually. Frequent use and in high doses can cause the development of tolerance, in this case it is recommended to cancel for 24-48 hours, or after 3-6 weeks of regular admission, to take a break for 3-5 days, replacing Isoket® spray with other antianginal drugs for this time.

Treatment with Isoket® should not be performed in patients who received phosphodiesterase-5 inhibitors immediately before taking it (for example, sildenafil, tadalafil, vardenafil).

The solution contains about 85 percent ethanol.

During the treatment of Isoket® spray should be avoided the use of alcohol.

Please store Isoket® Spray at room temperature and check the spray gun from time to time. This is especially necessary with a long break in its application. On the label of the spray bottle, below, there is an arrow. When the level of liquid in the bottle reaches the upper edge of the arrow, you need to purchase the next bottle of spray.

Further use of such a bottle is also possible, as long as with slight inclination the tip of the suction tube is still immersed in the liquid.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (risk of drowsiness). This effect is exacerbated by alcohol.

Form release / dosage:

Spray dosed, 1.25 mg / dose.

Packaging:

For 15 ml of concentrate in a bottle of brown transparent glass with a nozzle for fixing the cap, a metering pump with a rigidly fixed sprayer made of white plastic (spray head) and a red protective cap.

Each bottle together with instructions for use is placed in a cardboard pack.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012496 / 02

Date of registration:28.03.2007 / 08.08.2017

Expiration Date:Unlimited

Representation: & nbspAlvils, OOOAlvils, OOO

Information update date: & nbsp23.10.2017

Illustrated instructions

Instructions

Isoket® (Isoket®)