Mono Rohm ретард

General characteristics. Structure:

Active agent: isosorbide mononitrate - 40 mg or 60 mg;

Excipients: sugar krupka [sucrose, starch syrup], ethyl cellulose, stearic acid, talc.

Structure of the capsule:

capsules No. 2 (dosage of 40 mg) - titanium dioxide, dye quinolinic yellow, dye an azoruby, dye iron oxide red, dye a sunset yellow, gelatin;
capsules No. 1 (dosage of 60 mg) - dye blue patent, gelatin, titanium dioxide.

Description: Capsules firm gelatinous No. 2 of henna-red color - for a dosage of 40 mg. Capsules firm gelatinous No. 1 with a lid of blue color and korpuksy white color - for a dosage of 60 mg. Contents of capsules - pellets of white or almost white color.

Pharmacological properties:

Pharmacodynamics. Isosorbide mononitrate - a peripheral vazodilatator with preferential influence on venous vessels. Has vasodilating and anti-anginal effect. Reduces preloading (due to expansion of peripheral veins) and an afterload (owing to decrease in the general peripheric vascular resistance), reduces a myocardium potrebyonost in oxygen, expands coronary arteries and improves a coronary kroyovotok, promotes its redistribution to ischemic areas, reduces the koyonechny diastolic volume of a left ventricle and reduces the systolic tension of its walls.

Increases tolerance to an exercise stress at patients with the coronary heart disease (CHD), reduces pressure in a small circle of blood circulation.

Isosorbide mononitrate causes relaxation of muscles of bronchial tubes, urinary tract, muscles of a gall bladder, biliary tract and a gullet, and also small and large intestine, including sphincters.

Nitrates act on molecular level by means of formation of nitrogen of oxide (N0) and a cyclic guanozinmonofosfat who mediates relaxation of smooth muscles of internals.

Expands vessels of a brain, a firm meninx that can be followed by a headache. As well as to other nitrates, cross tolerance develops. After cancellation (a break in treatment) sensitivity to it is quickly recovered.

The anti-anginal effect is shown in 30 minutes and 2-6 hours proceed.

Pharmacokinetics. After isosorbide intake mononitrate is quickly and completely absorbed from the digestive tract (DT). Bioavailability makes from 90-100% and does not depend on meal. Communication with proteins of a blood plasma - less than 4%.

Therapeutic concentration of isosorbide of mononitrate in blood is reached in 30 minutes and makes 250 ng/ml, within the 4th hour - 414 ng/ml, within the 12th hour - 199 ng/ml (i.e. decrease in concentration slow).

Concentration in a blood plasma is directly proportional to the accepted dose. Time of achievement of the maximum concentration makes 8 h.

Isosorbide mononitrate is almost completely metabolized in a liver (is not exposed to effect of "the first passing") with formation of inactive metabolites by a denitrovaniye to isosorbide or by means of conjugation with glucuronic acid and obrazovayoniy inactive 2 glucuronides.

2% - in not changed look are removed by kidneys, mainly, in the form of metabolites. The elimination half-life makes 4-5 hours.

Indications to use:

Prevention of attacks of stable stenocardia at patients with coronary heart disease, including after the postponed myocardial infarction; treatment of chronic heart failure (as a part of a combination therapy).

Route of administration and doses:

Inside, capsules are swallowed entirely, washing down with water.

Frequency of reception and duration of treatment are established by the doctor individually. Treatment is recommended to begin with a dose of drug MONO ROHM RETARD 40 mg of 1 times a day, if necessary - with a dose of drug MONO ROHM RETARD of 60 mg of 1 times a day. In some cases the dose can be increased to 2 capsules (80 mg) in 2 receptions a day. For achievement of full therapeutic effect the second capsule of drug MONO ROHM RETARD of 40 mg (at a daily dose of 80 mg) has to be accepted not later than че­рез 8 hours. The maximum daily dose makes 120 mg.

Features of use:

Drug MONO ROHM RETARD should not be used for stopping of bad attacks of stenocardia and an acute myocardial infarction!

During therapy by drug MONO ROHM RETARD control of the ABP and heart rate is necessary.

It is necessary to avoid sharp drug withdrawal (to reduce a dose gradually). At prolonged use tolerance development in this connection, cancellation for 24-48 hours is recommended is possible or after 3-6 weeks of regular administration of drug to do a break for 3-5 days, having replaced with this time drug MONO ROHM RETARD with other anti-anginal drugs.

Use of drug MONO ROHM RETARD can lead to a tranzitorny anoxemia due to redistribution of a blood-groove in the hypoventilated alveolar segments. It can be an ischemia releaser at patients with an ischemic heart disease. During treatment it is necessary to exclude the use of ethanol (alcohol).

Influence on ability to manage vehicles and to work with mechanisms

During treatment drug MONO ROHM RETARD is not recommended to be managed vehicles and to be engaged in potentially dangerous types of activity demanding bystry psychomotor reaction.

Side effects:

From cardiovascular system: in an initiation of treatment the "nitrate" headache is possible; the expressed decrease in the ABP; orthostatic hypotension, сопровождающая­ся reflex tachycardia, block, dizziness, weakness; seldom at the expressed arterial hypotension - strengthening of symptoms of stenocardia (paradokyosalny reaction); in some cases - a collapse, sometimes with a bradyarrhythmia and a faint.

From the alimentary system: nausea, vomiting, emergence of feeling of easy burning of language, dryness of a mucous membrane of an oral cavity is possible.

From the central nervous system: drowsiness, a sight illegibility, decline in the ability to bystry mental and motor reactions (especially in an initiation of treatment).

Allergic reactions: perhaps tranzitorny erubescence, skin rash.

Others: tolerance development, and also cross tolerance with other nitro compounds at prolonged continuous treatment by high doses of isosorbide of a moyononitrat. To prevent decrease or loss of efficiency, it is necessary to avoid continuous reception of high doses of drug.

In some cases - exfoliative dermatitis.

Interaction with other medicines:

At simultaneous use with other vazodilatator, beta adrenoblockers, inhibitors of an angiotensin-converting enzyme (APF), blockers of "slow" calcium channels (BMKK), diuretics, neuroleptics, tricyclic antidepressants, ethanol, phosphodiesterase 5 inhibitors (sildenafit, vardenafit, tadalafit) possibly strengthening of hypotensive effect of drug MONO ROHM RETARD. At simultaneous use with dihydroergotamine increase in a kontsenyotration of dihydroergotamine in a blood plasma is possible. Reduces effect of vazopressor.

The therapeutic effect of Norepinephrinum (noradrenaline) decreases at simultaneous uses with nitro compounds.

Barbiturates accelerate metabolism and reduce concentration of isosorbide of mononitrate in a blood plasma.

At a combination with Amiodaronum, propranolol, BMKK (verapamil, nifedipine, etc.) strengthening of anti-anginal action is possible.

The adsorbents knitting and enveloping means reduce mononitrate isosorbide absorption from a GIT.

At simultaneous use with m-holinoblokatorami (atropine, etc.) the risk of increase in intraocular pressure increases.

Under the influence of beta-adrenergic agonists, alpha adrenoblockers (dihydroergotamine and others) decrease in expressiveness of anti-anginal effect (tachycardia and excessive decrease in the ABP) is possible.

Contraindications:

hypersensitivity to organic nitrates or other components of drug
acute disorders of blood circulation (shock, collapse)
acute myocardial infarction with the expressed arterial hypotension
cardiogenic shock if rather high end diastolic pressure in a left ventricle by use of intra aortal counterpulsation or due to introduction of the means having positive inotropic effect is not provided
toxic fluid lungs
anemia (severe form)
the expressed arterial hypotension (the systolic arterial pressure (AP) less than 90 mm hg, diastolic the ABP less than 60 mm hg)
concomitant use of inhibitors of phosphodiesterase 5 (sildenafit, tadalafit, vardenafit as they exponentiate hypotensive effect of nitrates)
age up to 18 years (efficiency and safety are not established)
patients with rare hereditary diseases: intolerance of fructose and syndrome of disturbance of absorption of a glucose/galactose or insufficiency of invertase/isomaltase

With care:
hypertrophic subaortic stenosis, chronic cardial compression, cardiac tamponade
low filling pressure at an acute myocardial infarction, a left ventricular failure. It is not necessary to allow decrease in the systolic/diastolic ABP less than 90 mm hg.
aortal and/or mitral stenosis
tendency to orthostatic disturbances of vascular regulation
at glaucoma (risk of increase in intraocular pressure)
heavy renal failure
abnormal liver functions (risk of development of a methemoglobinemia)
hemorrhagic stroke
hyperthyroidism
the diseases which are followed by the increased intracranial pressure
the postponed craniocereberal injury
the raised digestive tract peristaltics
sprue

Pregnancy and period of a lactation

For safety reasons MONO ROHM RETARD can be applied at pregnancy and in the period of a lactation only strictly on doctor's orders, after careful assessment of advantage to mother and possible risk to a fruit and/or the child as not enough data of its use for pregnant women and nursing mothers. If the nursing mother nevertheless accepts MONO ROHM RETARD, it is necessary to establish observation of the child regarding development of possible undesirable effects of drug use.

Overdose:

Symptoms: the expressed decrease in the ABP with an orthostatic vazodilatation, reflex tachycardia and a headache. There can be a weakness, dizziness, a dermahemia, nausea, vomiting, diarrhea. In high a dose (more than 20 mg/kg of body weight) it is necessary to expect emergence of a methemoglobinemia, cyanosis, диспноэ and a tachypnea because of education nitrite ions owing to mononitrate isosorbide metabolism.

At very high doses of drug intracranial pressure with cerebral symptoms can increase. At chronic overdose increase in a methemoglobin comes to light.

Treatment: gastric lavage, reception of absorbent carbon.

At the expressed decrease in the ABP - to give to the patient horizontal position with the raised legs and to hold events for completion of the volume of the circulating blood (VCB); in exceptional cases for improvement of blood circulation it is possible to carry out infusions of Norepinephrinum (noradrenaline) and/or a dopamine.

Use of Epinephrinum (adrenaline) and related to it connections contraindicated. At a methemoglobinemia:

1. Ascorbic acid - 1 g in or in the form of sodium salt in/in - 0,1 - 0,15 ml/kg of 1% of solution to 50 ml,

2. Oxygenotherapy, hemodialysis, exchange hemotransfusion.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children! A period of validity - 3 years. Not to use after the period of validity specified on packaging!

Issue conditions:

According to the recipe

Packaging:

Capsules of the prolonged action of 40 mg and 60 mg.

On 10 capsules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 2 blister strip packagings together with the application instruction place in a pack cardboard.