Mesaton, 10 mg/ml 1 ml 10 pcs

PharmacoDynamics

Phenylephrine is an alpha1-adrenergic stimulant that slightly affects the beta-adrenoceptors of the heart; it is not a catecholamine because it contains only one hydroxyl group in the aromatic core. Causes narrowing of the arterioles and an increase in arterial pressure (BP) (with possible reflex bradycardia), but is more prolonged because it is less prone to the action of catechol()-methyltransferase.

It does not cause an increase in the minute blood volume.

After intravenous administration, the action of the drug develops immediately and lasts for 5-20 minutes. When administered subcutaneously and intramuscularly the action of the drug starts 10-15 min and lasts 1-2 hours after injection.

Pharmacokinetics

After intramuscular administration the drug is quickly absorbed into the systemic blood flow. Volume of distribution after single administration is 340 l. Binding to plasma proteins is low. It is almost completely metabolized in the liver by monoaminoxidase (without catechol()-methyltransferase). The terminal elimination half-life is about 3 hours. It is excreted by the kidneys as metabolites.

Indications

Acute arterial hypotension;

Vascular insufficiency in overdose of vasodilators;

Shock (traumatic, toxic);

As a vasoconstrictor during local anesthesia.

Active ingredient

Composition

Active ingredient:

Phenylephrine hydrochloride – 10 mg

Excipients:

Glycerol (distilled glycerin) – 60 mg;

water for injection – up to 1 ml

How to take, the dosage

Mesaton is administered intravenously, subcutaneously or intramuscularly.

In case of collapse, the single dose when administered intravenously is 0.1-0.5 ml of 1% solution of Mesaton.

In intravenous administration the single dose is diluted in 20 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution and slowly injected by trickle. If necessary (if systolic BP decreases to 70-80 mmHg), the injection is repeated. The interval between repeated intravenous injections of the drug shall be at least 15 minutes.

The drug can be administered intravenously by drop infusion for which 1 ml of 1% solution of Mesaton is diluted in 250-500 ml of 5% dextrose (glucose) solution. The initial infusion rate is 180 micrograms per minute; later the infusion rate is reduced to 30-60 micrograms per minute.

In intramuscular and subcutaneous administration, the single dose is 0.3-1.0 ml of 1% Mesaton solution

In local anesthesia they add 0.3-0.5 ml of 1% solution of Mesaton per 10 ml of anesthetic solution.

After prolonged intravenous infusion, the drug dose should be reduced gradually to prevent development of “withdrawal” syndrome (repeated BP reduction). The highest dose with intramuscular and subcutaneous administration: single dose – 10 mg, daily – 50 mg. The highest dose with intravenous injection: single dose – 5 mg, daily – 25 mg.

Interaction

Phenylephrine reduces the antihypertensive effect of diuretics and hypotensive agents, beta-adrenoblockers (risk of arterial hypertension and cardiovascular disorders).

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

Beta-adrenoblockers decrease the cardiac stimulatory activity of the drug.

The use of the drug against prior use of reserpine may cause development of a hypertensive crisis due to depletion of catecholamine stores in adrenergic endings and increased sensitivity to adrenomimetics.

Inhaled anesthetics (including chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial and ventricular arrhythmias (including ventricular fibrillation) because they dramatically increase myocardial sensitivity to sympathomimetics. Ergometrine, ergotamine, methylergometrine, oxytocin, doxapram increase the severity of the vasoconstrictor effect.

Phenylephrine decreases the antianginal effect of nitrates, which in turn may decrease the pressor effect of Mesaton@ and the risk of arterial hypotension (simultaneous use is permitted depending on achieving the desired therapeutic effect).

The thyroid hormones mutually increase drug efficacy and associated risk of coronary artery disease (especially in coronary atherosclerosis).

The presorptive 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 disturbances and myocardial infarction.

The use of Mesaton during labor to correct arterial hypotension against the background of the use of labor-promoting agents (vasopressin, ergotamine, ergometrine, methylergometrine) may cause persistent BP increase in the postpartum period.

Special Instructions

The electrocardiogram, BP, minute blood volume, blood flow in the extremities and at the injection site should be monitored during treatment.

In patients with arterial hypertension in case of drug-induced collapse, it is sufficient to maintain systolic BP at 30-40 mm Hg lower than normal. A sharp increase in BP, marked bradycardia or tachycardia, persistent cardiac rhythm disturbances require treatment discontinuation.

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

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

The number of adrenoreceptors sensitive to phenylephrine decreases in the elderly.

Impact on the ability to drive vehicles, machinery During treatment, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity to any of the ingredients of the drug;

Diseases accompanied by left ventricular outflow tract obstruction (severe aortic stenosis, hypertrophic cardiomyopathy);

Pheochromocytoma;

Artial hypertension of any severity;

Ventricular fibrillation;

Glucose-b-phosphate dehydrogenase deficiency;

Porphyria;

Thyrotoxicosis;

Closed angle glaucoma;

Acute myocardial infarction;

p> Use concomitantly with monoamine oxidase inhibitors (MAOIs) and for 14 days after stopping therapy with MAOIs;

Halothane or cyclopropane anesthesia;

Pregnancy and breastfeeding;

Age under 18 years of age.

With caution

Coronary heart disease (especially after a recent MIOCAP heart attack), angina pectoris, coronary, mesenteric and other visceral or peripheral vascular thrombosis, diabetes mellitus, pulmonary hypertension, ventricular arrhythmias, occlusive vascular disease: arterial thromboembolism, atherosclerosis, obliterating thrombangiitis (Buerger’s disease), Raynaud’s disease, susceptibility of vessels to frostbite spasm, diabetic endarteritis, thyroid dysfunction, metabolic acidosis, hypercapnia, hypoxia, older age, renal and/or liver function disorders, use in patients with prostate disease who have an increased risk of urinary retention.

Side effects

Adverse reactions (ARs) are categorized according to the MedDRA Dictionary classification of organ and organ system lesions and the frequency of development of WHO ARs: very common: (2 1/10); frequent: (2 1/100 and < 1/10); infrequent: (2 1/1000 and < 1/100); rare: (2 1/10000 and < 1/1000); very rare: (< 1/10000); frequency unknown (the incidence cannot be determined from available data).

Immune system disorders: rare – allergic reactions (skin rash, urticaria).

Endocrine system disorders: frequency is unknown – hyperglycemia. Metabolic and nutritional disorders: frequency unknown – increased sweating.

Nervous system disorders: very rare – insomnia, nervousness, tremor, anxiety, increased excitability, confusion, irritability and headache, dizziness, brain hemorrhage, paresthesia, weakness.

Visual organ disorders: very rare – eye pain, mydriasis.

Cardiac disorders: rare – feeling of palpitations, bradycardia, tachycardia, ventricular arrhythmias (especially when used in high doses), angina pectoris, frequency unknown – pulmonary edema, cardiac arrest.

Vascular disorders: rare – increase or decrease in blood pressure, frequency is unknown – pale skin, tingling sensation and coldness of the extremities.

Disorders of the respiratory system, thorax and mediastinum: rarely – dyspnea.

Gastrointestinal tract disorders: frequently nausea, vomiting, frequency unknown – increased salivation.

Renal and urinary tract disorders: very rare – dysuria, urinary retention.

General disorders and disorders at the site of administration: necrosis and scab formation in case of ingestion or subcutaneous injections are possible in some cases.

Overdose

Symptoms: headache, significant increase in blood pressure, reflex bradycardia, ventricular extrasystole, short paroxysms of ventricular tachycardia, feeling of heaviness in the head and extremities. In significant overdose, confusion, hallucinations and seizures may occur.

Treatment: intravenous administration of short-acting alpha-adrenoblockers (phentholamine at a dose of 5-60 mg intravenously for 10-30 minutes) and beta-adrenoblockers (for heart rhythm disorders).

Pregnancy use

There have been no adequate and strictly controlled studies on the use of the drug during pregnancy and during breastfeeding.

In animals during late pregnancy, phenylephrine caused fetal growth retardation and stimulated early labor.

The use of MesatoneThe adverse reactions (ARs) are categorized according to the MedDRA Dictionary classification of organ and organ system lesions and the frequency of development of WHO ARs: very common: (2 1/10); frequent: (2 1/100 and <1/10); infrequent: (2 1/1000 and <1/100); rare: (2 1/10000 and <1/1000); very rare: (<1/10000); frequency unknown (the incidence could not be determined from available data).

Immune system disorders: rare – allergic reactions (skin rash, urticaria).

Endocrine system disorders: frequency is unknown – hyperglycemia. Metabolic and nutritional disorders: frequency unknown – increased sweating.

Nervous system disorders: very rare – insomnia, nervousness, tremor, anxiety, increased excitability, confusion, irritability and headache, dizziness, brain hemorrhage, paresthesia, weakness.

Visual organ disorders: very rare – eye pain, mydriasis.

Cardiac disorders: rare – feeling of palpitations, bradycardia, tachycardia, ventricular arrhythmias (especially when used in high doses), angina pectoris, frequency unknown – pulmonary edema, cardiac arrest.

Vascular disorders: rare – increase or decrease in blood pressure, frequency is unknown – pale skin, tingling sensation and coldness of the extremities.

Disorders of the respiratory system, thorax and mediastinum: rarely – dyspnea.

Gastrointestinal tract disorders: frequently nausea, vomiting, frequency unknown – increased salivation.

Renal and urinary tract disorders: very rare – dysuria, urinary retention.

General disorders and disorders at the injection site: necrosis and scab formation possible in individual cases if ingested or injected subcutaneously. contraindicated during pregnancy and during breastfeeding.

There are no data on excretion of phenylephrine into the breast milk.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Similarities