Magnesium sulfate

General characteristics. Structure:

Active ingredient: 250 mg of magnesium of sulfate in 1 ml of solution.

Excipients: driving for injections.

Pharmacological properties:

Pharmacodynamics. At parenteral administration renders anticonvulsant, antiarrhytmic, anti-hypertensive, spasmolytic action, in high doses oppresses nervously - muscular transfer, has tokolitichesky effect, suppresses a respiratory center. Mg2 + is physiological антагонистрм Sa2 + and is capable to force out it from places of binding. Regulates exchange processes, mezhneyronalny transfer and muscular irritability, interferes with receipt of Sa2 + through a presynaptic membrane, reduces quantity of acetylcholine in a peripheral nervous system and the central nervous system (CNS). Relaxes smooth muscles, reduces the arterial pressure (AP) which is (preferential increased) strengthens a diuresis.

Anticonvulsant action - Mg2 reduces, release of acetylcholine from neuromuscular synapses, suppressing at the same time neuromuscular transmission, has the direct oppressing effect on TsNS.

Antiarrhytmic action - Mg2 + reduces excitability of cardiomyocytes, recovers ionic balance, stabilizes cellular membranes, breaks Na+ current, the slow entering current of Sa2 + and unilateral current of K+.

The cardiotyre-tread effect is caused by expansion of coronary arteries, decrease in the general peripheric vascular resistance and aggregation of thrombocytes.

Tokolitichesky action - Mg2 + oppresses sokratitelny ability of a myometrium (decrease in absorption, binding and distribution of Sa2 + in cells of smooth muscles), strengthens a blood stream in a uterus as a result of expansion of its vessels.

Is an antidote at poisonings with salts of heavy metals.

System effects develop almost instantly later intravenous (in) introductions.

Action duration at in introduction - 30 min.

Pharmacokinetics. Equilibrium concentration - 2-3,5 mmol/l. Gets through hematoencephalic and placental barriers, creates in breast milk of concentration, the concentration twice exceeding in a blood plasma.

Removal is carried out by kidneys, the speed of renal excretion is proportional to concentration in a blood plasma and to the level of glomerular filtering.

Indications to use:

Arterial hypertension (including hypertensive crisis with the wet brain phenomena), polymorphic ventricular tachycardia (pirouette type), a convulsive syndrome (for suppression of spasms at an eclampsia; for the prevention of spasms at a heavy preeclampsia; for removal of strong reductions of a uterus), poisoning with salts of heavy metals (mercury, arsenic, tetraethyllead), a hypomagnesiemia, (including raised - the need for magnesium and acute hypomagnesiemia - tetany).

Route of administration and doses:

Intravenously. Doses are specified taking into account therapeutic effect and concentration of ions of magnesium in blood serum.

Preeclampsia and eclampsia. The dose is established individually depending on a clinical situation. A saturation dose - 2-4, in 5-20 min. (infusion). The Maintenance dose-1-2 of in an hour.

Uterus tetany. A saturation dose - 4 g in 20 min. (infusion). A maintenance dose - at first - 1-2 g an hour, later - 1 g an hour (it is possible to enter kapelno 24-72 h).

Hypomagnesiemia. At newborns. A daily dose - 0,2-0,8 mg/kg in/in slowly.

At adults. Easy. Solution of magnesium of sulfate is applied parenterally if the peroral way of administration of drugs of magnesium (because of nausea is impossible or inexpedient; vomitings, the broken resorption in a stomach, etc.). Daily dose of-1-2 in oil. This dose is entered once or into 2-3 receptions. The injection site should be changed.

Heavy. An initial dose - 5 g intravenously slowly in 1 l of infusion solution. Dose depending on concentration of drug in blood serum.

Prevention of a hypomagnesiemia at the patients receiving only parenteral food. If in nutrient solutions there is no magnesium, it is added in addition. A daily dose - l, 5-4 g. Usually, v1 l of solution of parenteral food add 1 g of magnesium of sulfate.

The maximum urgent dose of magnesium of sulfate adult - 40 g.

At hypertensive crises enter - in/in (slowly!!) 5-20 ml 250 mg/ml of solution of magnesium of sulfate.

For stopping of arrhythmias in/in enter 1-2 g within about 5 minutes, perhaps repeated introduction.

Doses of magnesium of sulfate are specified in grams. To them there corresponds the amount of solution: 1 g - 4 ml (250 mg/ml); 2 g - 8 ml (250 mg/ml); - 3 g - 12 ml (250 mg/ml); 4 g - 16 ml (250 mg/ml); 5 g - 20 ml (250 mg/ml); 10 g - 40 ml / (250 mg/ml); 15 g - 60 ml (250 mg/ml); 20 g - 80 ml (250 mg/ml); 30 g - 120 ml (250 mg/ml);> 40 g-160 of ml (250 mg/ml).

Sulfate magnesium solution in ampoules is diluted with injection solutions: 0,9% of sodium of chloride or 5% of a dextrose (glucose).

Features of use:

Pregnancy and lactation. To take during pregnancy and a lactation with caution.

Magnesium sulfate should be applied carefully that there was no toxic concentration of drug: Elderly people usually should apply the reduced dose as at them function of kidneys is reduced. Patients with a renal failure (if clearance of creatinine more than 20 ml/min.) and an oliguria do not; to receive more than 20 g of magnesium of sulfate (81 mmol of Mg2+) during 48 h, it is not necessary to enter magnesium sulfate in/in too quickly. Control of maintenance of ions of magnesium in blood serum (there have to be not higher than 0,8-1,2 mmol/l), a diuresis (not less than 100 ml / 4 h), respiration rates (not less than 16 in min.), arterial pressure is recommended.

At administration of magnesium of sulfate it is necessary to have, the calcium solution prepared for in/in introductions, for example, 10% gluconate calcium solution. In need of magnesium, simultaneous in/in introductions, and calcium, they are entered into different veins. At use of magnesium of sulfate results radiological, researches to which technetium is applied can be distorted.

Influence on ability to manage vehicles and mechanisms. Influence of drug on ability to manage vehicles and mechanisms was not studied.

Side effects:

Precursory symptoms and symptoms of a gipermagniyemiya: bradycardia, a diplopia, sudden "inflow" of blood to the person, a headache, the expressed decrease in the ABP, nausea, short wind, a speech smazannost, vomiting, an adynamy.

Gipermagniyemiya signs; the concentration of ions of magnesium ranged as increase in blood serum: decrease in deep tendon jerks (2-3,5 mmol/l), lengthening of an interval of PQ and expansion of the QRS complex on the electrocardiogram (2,5 - 5 mmol/l), loss of deep tendon jerks (4-5 mmol/l), oppression of a respiratory center (5-6,5 mmol/l), disturbance of conductivity of heart (7,5 mmol/l), a cardiac standstill (12,5 mmol/l).

Besides, hyperhidrosis uneasiness, deep / sedation/polyuria, uterus atony.

Interaction with other medicines:

Patients who together with magnesium sulfate apply also other medicines have to report about it to the doctor.

Strengthens effect of other medicines, the oppressing TsNS.

Cardiac glycosides increase risk of disturbance. conductivity and an atrioventricular block (especially at simultaneous in administration of salts of calcium).

Muscle relaxants and nifedipine strengthen neuromuscular blockade.

At combined use of magnesium of sulfate for parenteral administration with others., vazodilatator strengthening of hypotensive effect is possible.

Barbiturates, narcotic analgetics, hypotensive medicinal, means increase probability of oppression of a respiratory center;

Breaks absorption of antibiotics of group of tetracycline, weakens - effect of streptomycin and Tobramycinum. Salts of calcium reduce effect of magnesium of sulfate.

Pharmaceutical it is incompatible (forms a deposit) with calcium drugs, ethanol (in high concentration), carbonates, hydrocarbonates and phosphates of alkaline metals, salts of arsenic acid, barium, strontium, clindamycin phosphate, a gadrokortazona of sodium succinate, polymyxin B sulfate, Procainum a hydrochloride, salicylates and tartrates.

At concentration of ions of magnesium higher than 10 mmol/ml in mixes for full parenteral food are possible division of fatty emulsions.

Contraindications:

Hypersensitivity to drug components; atrioventricular block (AV blockade); heavy chronic renal failure (if clearance of creatinine less than 20 ml/min.); arterial hypotension; the states connected with deficit of calcium and oppression of a respiratory center; the expressed bradycardia; the predrodovy period (in 2 hours prior to childbirth).

With care. A myasthenia, a chronic renal failure (if clearance of creatinine more - 20 ml/min.), diseases of a respiratory organs, acute inflammatory diseases, digestive tract, advanced age, pregnancy, the lactation period, children's age.

Overdose:

Symptoms: disappearance. knee jerk, nausea, vomiting, sharp decrease in the ABP, bradycardia, respiratory depression and TsNS.

Treatment: it is necessary in/in to enter slowly solution of Calcii chloridum or calcium of a gluconate - 5-10 ml of 10%, carry out an oxygenotherapy, inhalation of Carbogenum, artificial breath / peritoneal dialysis or a hemodialysis, symptomatic therapy.

Storage conditions:

At a temperature from 15 to 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the expiration specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous administration of 250 mg/ml in ampoules on 5 ml or 10 ml. On 10 ampoules with the application instruction, a knife ampoule or the scarificator ampoule in a pack or a box from a cardboard. When packaging the ampoules having a ring of a break or a point for opening the knife ampoule or the scarificator ampoule is not put. On 5 ampoules in cassette planimetric packaging. On 2 cassette planimetric packagings with the application instruction in a pack from a cardboard.