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

Phenylephrine - alpha1-adrenostimulant, slightly affecting the beta-adrenoreceptors of the heart; It is not catecholamine because it contains only one hydroxyl group in the aromatic nucleus. It causes a narrowing of arterioles and an increase in blood pressure (BP) (with a possible reflex bradycardia), but it lasts longer,because it is less prone to the action of catechol-o-methyltransferase.

Does not cause an increase in the minute volume of blood.

After intravenous administration, the effect of the drug develops immediately and lasts for 5-20 minutes. With subcutaneous and intramuscular injection, the drug starts in 10-15 minutes and lasts for 1-2 hours after administration.

Pharmacokinetics:

After intramuscular injection, it is rapidly absorbed into the systemic circulation. The volume of distribution after a single injection is 340 liters. Connection with blood plasma proteins low. Almost completely metabolized in the liver by monoamine oxidase (without the participation of catechol-o-methyltransferase). The final half-life is about 3 hours. It is excreted by the kidneys in the form of metabolites.

Indications:

- Acute hypotension;

- Vascular insufficiency in case of an overdose with vasodilators;

- Shock (traumatic, toxic);

- As a vasoconstrictor for local anesthesia.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- Diseases accompanied by obstruction of the outflow tract of the left ventricle (severe aortic stenosis, hypertrophic cardiomyopathy);

- Pheochromocytoma;

- Arterial hypertension of any severity;

- Ventricular fibrillation;

- Deficiency of glucose-6-phosphate dehydrogenase;

- Porphyria;

- Thyrotoxicosis;

- Closed-angle glaucoma;

- Acute myocardial infarction;

- Use simultaneously with monoamine oxidase (MAO) inhibitors and within 14 days after discontinuation of therapy with MAO inhibitors;

- Halotane or cyclopropane anesthesia;

- Pregnancy and the period of breastfeeding;

- Age to 18 years.

Carefully:Coronary heart disease (especially after a recent myocardial infarction), angina pectoris, coronary thrombosis, mesenteric and other visceral or peripheral vessels, diabetes mellitus, pulmonary hypertension, ventricular arrhythmias, occlusive vascular disease: arterial thromboembolism, atherosclerosis, thromboangiitis obliterans (Buerger's disease), Raynaud's disease, the propensity of blood vessels to spasms with frostbite, diabetic endarteritis, thyroid dysfunction, metabolic acidosis, hypercapnia, hypoxia, advanced age, renal and / or hepatic impairment, use in patients with prostate disease who have an increased risk of urinary retention.

Pregnancy and lactation:

Adequate and strictly controlled studies of the use of the drug during pregnancy and during breastfeeding were not conducted.

In animals in late pregnancy phenylephrine caused a delay in fetal growth and stimulated earlier onset of labor.

The use of Mesaton during pregnancy and during breastfeeding is contraindicated.

Data on the isolation of phenylephrine in breast milk are absent.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Mesaton is administered intravenously, subcutaneously or intramuscularly.

When collapse a single dose for intravenous administration is 0.1 -0.5 ml of a 1% solution of Mezaton.

With intravenous administration, a single dose is diluted in 20 ml of a 5% solution of dextrose (glucose) or 0.9% sodium chloride solution and injected slowly. If necessary (if systolic blood pressure drops to 70-80 mm Hg), the introduction is repeated. The interval between repeated intravenous administration of the drug should be at least 15 minutes.

The drug is allowed to be injected intravenously, for which 1 ml of a 1% solution of Mezaton is diluted in 250-500 ml of a 5% solution of dextrose (glucose).The initial rate of administration is 180 μg per minute; Further, the rate of administration is reduced to 30-60 μg per minute.

With intramuscular and subcutaneous administration, a single dose is 0.3-1.0 ml of a 1% solution of Mezaton.

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

After a prolonged intravenous infusion, the dose of the drug should be gradually reduced to prevent the development of the "withdrawal" syndrome (repeated decrease in blood pressure).

Higher doses for intramuscular and subcutaneous injection: single dose - 10 mg, daily - 50 mg. The highest dose for intravenous administration: single dose - 5 mg, daily - 25 mg.

Incompatibility

The drug should not be mixed with other drugs in the same container.

Side effects:

According to the World Health Organization, the undesirable effects are classified according to their frequency of development as follows: Often (> 10% of appointments); often (> 1% and <10%); infrequently (> 0.1% and <1%); rarely (> 0.01% and <0.1%); rarely (<0,01 %); frequency unknown (insufficient data to estimate the frequency of development).

From the cardiovascular system: rarely - increase or decrease in blood pressure, palpitations, bradycardia, tachycardia, ventricular arrhythmias (especially when used in high doses), angina pectoris, frequency unknown - pulmonary edema, cardiac arrest.

From the side of the central nervous system: very rarely - Insomnia, nervousness, tremor, anxiety, increased excitability, confusion, irritability and headache, dizziness, cerebral hemorrhage, paresthesia, weakness.

From the side of the organ of vision: very rarely - pain in the eyes, mydriasis.

From the urinary system: very rarely - dysuria, urinary retention.

From the digestive system: often - nausea, vomiting, frequency unknown - increased salivation.

From the respiratory system: rarely - dyspnoea.

Allergic reactions: rarely - skin rash, hives.

Other: pallor of the skin of the face, sensation of tingling and cooling of limbs, increased sweating, hyperglycemia.

In some cases, necrosis and the formation of a scab is possible when ingested in tissue or with subcutaneous injections.

Overdose:

Symptoms: headache, a significant increase in blood pressure, reflex bradycardia, ventricular extrasystole, short paroxysms of ventricular tachycardia, a sense of heaviness in the head and limbs. With a significant overdose, confusion, hallucinations and convulsions may occur.

Treatment: intravenous administration of short-acting alpha-blockers (phentolamine in a dose of 5-60 mg intravenously for 10-30 minutes) and beta-blockers (for heart rhythm disturbances).

Interaction:

Phenylephrine reduces the antihypertensive effect of diuretics and antihypertensives, beta-blockers (risk of hypertension and cardiovascular disorders).

Neuroleptics, phenothiazide derivatives reduce the hypertensive effect of the drug. MAO inhibitors, oxytocin, ergot alkaloids, tricyclic antidepressants, methylphenidate, adrenomimetics enhance the pressor effect and the arrhythmogenic effect of phenylephrine.

Beta-adrenoblockers reduce the cardiostimulating activity of the drug. Application of the drug against the background of the previous application of reserpine may cause the development of hypertensive crisisdue to depletion of catecholamine stores in adrenergic endings and an increase in sensitivity to adrenomimetics. Inhalational anesthetics (including chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial and ventricular arrhythmias (including ventricular fibrillation), since they sharply increase the sensitivity of the myocardium to sympathomimetics. Ergometrine, ergotamine, methylergomethrin, oxytocin, doxapram increase the severity of the vasoconstrictor effect.

Phenylephrine reduces the antianginal effect of nitrates, which, in turn, can reduce the pressor effect of Mesatone and the risk of arterial hypotension (simultaneous use is allowed depending on the achievement of the necessary therapeutic effect).

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

The pressure effect of phenylephrine hydrochloride is increased in patients receiving tricyclic antidepressants.

Phenylephrine, when used concomitantly with digoxin or other cardiac glycosides, increases the risk of cardiac rhythm and myocardial infarction. The use of Mesaton during birth for the correction of arterial hypotension against the background of the use of funds that stimulate labor activity (vasopressin, ergotamine, ergometrine, metergergometrin), can cause a persistent increase in blood pressure in the postpartum period.

Special instructions:

During treatment, 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 by 30-40 mm Hg. A sharp increase in blood pressure, pronounced bradycardia or tachycardia, persistent heart rhythm disturbances require discontinuation of treatment.

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

The drug is used with caution in arterial hypertension in a small circle of blood circulation, hypovolemia, ventricular arrhythmia.

In the elderly, the number of adrenoreceptors sensitive to phenylephrine decreases.

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

During the treatment period, 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.

Form release / dosage:

Solution for injection 10 mg / ml.

Packaging:

1 ml per ampoule of neutral glass.

10 ampoules together with the instruction for use are placed in a box of cardboard.

5 ampoules per contour cell packaging made of polyvinyl chloride film.

For 1 or 2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004206

Date of registration:21.03.2017

Expiration Date:21.03.2022

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp06.04.2017

Illustrated instructions

Instructions

Mesatone (Mesaton)