Mesaton - instructions for use, dose, side effects, contraindications

Alpha-1 adrenostimulant, which has little effect on the beta-adrenoreceptors of the heart; is not catecholamine (contains only one hydroxyl group in the aromatic nucleus). It causes a narrowing of arterioles and an increase in blood pressure (with a possible reflex bradycardia).Compared with norepinephrine and epinephrine, it lowers blood pressure less sharply, but it acts longer (it is less susceptible to the action of catechol-O-methyltransferase); does not cause an increase in the minute volume of blood.

The action begins immediately after the introduction and lasts for 5-20 minutes (after intravenous administration), 50 minutes (with subcutaneous injection), 1-2 hours (after intramuscular injection).

Pharmacokinetics:

Metabolised in the liver and gastrointestinal tract (without the participation of catechol-O-methyltransferase). It is excreted by the kidneys in the form of metabolites.

Indications:

Parenteral - arterial hypotension, shock conditions (including traumatic, toxic), vascular insufficiency (including against a background of vasodilator overdose), as a vasoconstrictor during local anesthesia.

Intranasal - vasomotor and allergic rhinitis.

Contraindications:

Hypersensitivity to the drug; hypertrophic obstructive cardiomyopathy, pheochromocytoma, ventricular fibrillation.

Carefully:

Metabolic acidosis, hypercapnia, hypoxia, atrial fibrillation, closed angle glaucoma, arterial hypertension, hypertension in a small circle of blood circulation, hypovolemia, severe stenosis of the aortic aorta, acute myocardial infarction, tachyarrhythmia, ventricular arrhythmia; (including history) - arterial thromboembolism, atherosclerosis, obliterating thromboangiitis (Buerger's disease), Raynaud's disease, vascular tendencies to spasms (including with frostbite), diabetic endarteritis, thyrotoxicosis, diabetes mellitus, porphyria, deficiency of glucose-6-phosphate dehydrogenase, joint use of monoamine oxidase inhibitors, general anesthesia (fluorotane), renal dysfunction, elderly age, under 18 years of age (efficacy and safety not established).

Pregnancy and lactation:

Adequate and strictly controlled studies in humans and animals have not been conducted on the effect of the drug on pregnant women, there are no data on the allocation of the drug to breast milk, so that during pregnancy and during breastfeeding the drug can be administered with caution, only under strict indications and under the supervision of a doctor , evaluating the benefit / risk ratio.

Dosing and Administration:

Intravenously slowly, with the collapse - 0,1-0,3-0,5 ml of 1% solution, diluting in 20 ml of 5% dextrose solution or 0.9% solution of sodium chloride. If necessary, repeat the introduction.

Intravenously drip - 1 ml of a 1% solution in 250-500 ml of a 5% solution of dextrose.

Subcutaneously or intramuscularly, adults - 0,3-1 ml of 1% solution 2-3 times a day; children older than 15 years with arterial hypotension during spinal anesthesia - 0.5-1 mg / kg.

To narrow the vessels of the mucous membranes and reduce the inflammatory phenomena, they are lubricated or buried (the concentration of the solution is 0.125%, 0.25%, 0.5%, 1%).

With local anesthesia, add 0.3-0.5 ml of a 1% solution to 10 ml of an anesthetic solution.

Higher doses for adults: subcutaneously and intramuscularly: single - 10 mg, daily - 50 mg; intravenously: single - 5 g, daily - 25 mg.

Side effects:

From the cardiovascular system: increased blood pressure, palpitation, ventricular fibrillation, arrhythmia, bradycardia, cardialgia.

From the central nervous system: dizziness, fear, insomnia, anxiety, weakness, headache, tremor, paresthesia, seizures, cerebral hemorrhage;

Other: pallor of the skin of the face, ischemia of the skin at the injection site,in isolated cases, necrosis and the formation of a scab during tissue ingestion or hypodermic injections, allergic reactions are possible.

Overdose:

Symptoms: ventricular extrasystole, short paroxysms of ventricular tachycardia, a sense of heaviness in the head and extremities, a significant increase in blood pressure.

Treatment: intravenous administration of alpha-blockers (phentolamine) and beta-adrenoblockers (for violations of the heart rhythm).

Interaction:

Mesaton reduces the antihypertensive effect of diuretics and antihypertensive drugs (methyldopa, mekamilamin, guanadrel, guanethidine). Phenothiazines, alpha-adrenoblockers (phentolamine), furosemide and other diuretics reduce the hypertensive effect.

Inhibitors of monoamine oxidase (furazolidone, procarbazine, selegiline), oxytocin, ergot alkaloids, tricyclic antidepressants, methylphenidate, adrenostimulants enhance the pressor effect and arrhythmogenicity of phenylephrine.

Beta-adrenoblockers reduce cardiostimulating activity, against the background of reserpine - possible arterial hypertension (as a result of depletion of catecholamine stores in adrenergic endingsincreased sensitivity to adrenomimetics). Inhalational anesthetics (chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial and ventricular arrhythmia, as sharply increase the sensitivity of the myocardium to sympathomimetics.

Ergometrine, ergotamine, methylergomethrin, oxytocin, doxapram increase the severity of the vasoconstrictor effect.

Reduces the antianginal effect of nitrates, which, in turn, can reduce the pressor effect of sympathomimetics and the risk of arterial hypotension (simultaneous use is possible depending on the achievement of the necessary therapeutic effect).

Thyroid hormones increase (mutually) the effect and the associated risk of coronary insufficiency (especially in coronary atherosclerosis).

Special instructions:

During the treatment period, the parameters of the electrocardiogram, blood pressure, minute blood volume, blood circulation in the extremities and at the injection site should be monitored.

In patients with arterial hypertension in the case of drug-induced collapse, it is sufficient to maintain systolic blood pressure at a level below the usual 30-40 mm Hg. Art.

Before or during the therapy of shock conditions, correction of hypovolemia, hypoxia, acidosis and hypercapnia is mandatory.

A sharp increase in blood pressure, pronounced bradycardia or tachycardia, persistent cardiac arrhythmias require discontinuation of treatment.

To prevent and re-lower blood pressure after drug discontinuation, the dose should be reduced gradually, especially after prolonged g infusion.

Infusion is resumed if the systolic blood pressure drops to 70-80 mm Hg.

It should be borne in mind that the use of vasoconstrictors during labor to correct arterial hypotension or as an additive to local anesthetics against the background of stimulating generic activities (vasopressin, ergotamine, ergometrine, and metergergometrin) may lead to a persistent increase in arterial pressure in the postpartum period.

With age, the number of adrenoreceptors sensitive to phenylephrine decreases. Monoamine oxidase inhibitors, increasing the pressor effect of sympathomimetics, can cause the onset of headaches, arrhythmias, vomiting, hypertensive crisis,therefore, when patients take monoamine oxidase inhibitors in the preceding 2-3 weeks, the doses of sympathomimetics should be reduced.

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

During therapy, you should not engage in hazardous activities that require rapid motor and mental reactions (including driving).

Form release / dosage:

Solution for injection, 10 mg / ml.

Packaging:

For 1 ml in ampoules, enclosed 10 pieces together with instruction for use and scarifier ampoule or disk cutting ceramic in a pack of cardboard.

If there are fracture rings or break points on the ampoule, the ampoule scarifier or ceramic cutting disc is not put into the pack.

Storage conditions:

Keep in a place protected from light and inaccessible to children, at a temperature of no higher than 25 ° C.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N016059 / 01

Date of registration:24.09.2009

The owner of the registration certificate:EXPERIMENTAL FACTORY ГНЦЛС, ООО EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

Manufacturer: & nbsp

EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

Information update date: & nbsp19.09.2015

Illustrated instructions

Instructions

Mesatone (Mesaton)