Magnesium sulfate
Producer: JSC Himfarm Republic of Kazakhstan
Code of automatic telephone exchange: B05XA05
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active agent – magnesium of sulfate of 1,25 g.
Excipient – water for injections.
Pharmacological properties:
Pharmacokinetics. System effects develop in 1 h after intramuscular introduction and almost instantly later intravenous. Duration of preservation of effect makes about 30 min. at introduction to a vein and 3-4 h at intramuscular introduction. Concentration of ions of magnesium in a blood plasma normal averages 0,84 mmol/l, 25-35% of this quantity are in the state connected with proteins. Well gets through a placenta and a blood-brain barrier, in milk creates concentration twice the exceeding concentration in a blood plasma.
It is removed with urine (at the same time strengthens a diuresis) by filtering, the speed of renal excretion is proportional to concentration in a blood plasma. 93-99% of magnesium are exposed to the return reabsorption in proximal and distal renal tubules.
Pharmacodynamics. At parenteral administration renders sedative, diuretic, arteriodilatiruyushchy, anticonvulsant, antiarrhytmic, hypotensive, spasmolytic, in high doses - kurarepodobny (the oppressing influence on neuromuscular transmission), tokolitichesky, somnolent and narcotic actions, the respiratory center suppresses. Magnesium is the "physiological" blocker of slow calcium channels (BSCC) and is capable to force out it from places of binding. Regulates exchange processes, mezhneyronalny transfer and muscular irritability, interferes with intake of calcium through a presynaptic membrane, reduces quantity of acetylcholine in a peripheral nervous system and the central nervous system (CNS). Relaxes smooth muscles, the ABP reduces (preferential raised), strengthens a diuresis.
Anticonvulsant action - magnesium reduces release of acetylcholine from neuromuscular synapses, suppressing at the same time neuromuscular transmission, has the direct oppressing effect on TsNS.
Antiarrhytmic action - magnesium reduces excitability of cardiomyocytes, recovers ionic balance, stabilizes cellular membranes, breaks sodium current, the slow entering current of calcium and unilateral current of potassium.
The cardiotyre-tread effect is caused by expansion of coronary arteries, decrease in the general peripheric resistance of vessels (GPRV) and aggregation of thrombocytes.
Tokolitichesky action - magnesium oppresses sokratitelny ability of a myometrium (decrease in absorption, binding and distribution of calcium 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 in/in and in 1 h after introduction in oil. Action duration at in introduction - 30 min., at in oil - 3-4 h.
Indications to use:
- a convulsive syndrome (for example, at acute nephrite at children)
- hypomagnesiemia, including prevention (defective or unbalanced food, reception of contraceptives of diuretics, muscle relaxants, alcoholism)
- the increased need for magnesium
- polymorphic ventricular tachycardia (pirouette type)
- arterial hypertension in early stages
- hypertensive crisis with the wet brain phenomena
- an angina of exertion, cardiac arrhythmias (supraventricular and caused by therapy by antiarrhytmic or diuretic means, glucocorticoids or cardiac glycosides)
- eclampsia, encephalopathy, epileptic syndrome
- ischuria
- poisoning with salts of heavy metals mercury, arsenic, tetraetilsvinetsy, soluble salts of barium (antidote)
- the increased need for magnesium (pregnancy, a growth period, the recovery period, stresses, excessive sweating)
- acute hypomagnesiemia (tetany signs, dysfunction of a myocardium)
- threat of premature births
Route of administration and doses:
The drug is administered intramusculary or intravenously slowly (the first 3 ml – within 3 min.). At intravenous administration the patient has to be in a prone position.
The adult appoint 1,25-5,0 g (5-20 ml of 25% of solution) 1-2 times a day. At poisonings as an antidote intravenously enter 0,25-1,0 g (5-10 ml in the form of 5-10% of solution).
When stopping arrhythmias enter intravenously slowly 1,0-2,0 g (4-8 ml of 25% of solution) within 1-2 min., then pass to the supporting infusional introduction within 2 hours. For this purpose 10 ml of 25% of solution dissolve in 200 ml 5% of glucose or potassium - the polarizing mix and enter with a speed of 3-20 mg/min. (5-30 caps/min.).
At treatment of late toxicosis, a preekslampsiya and eclampsia use administration of magnesium of sulfate according to Richard's scheme: originally 4,0 g (16 ml of 25% of solution) intravenously slowly within 3-4 min., in 4 hours repeat intravenous administration in the same dose and in addition enter intramusculary 5,0 g (20 ml of 25% of solution). In the subsequent each 4 hours repeat intramuscular administration of magnesium of sulfate in a dose of 4,0-5,0 g (16-20 ml of 25% of solution). Instead of Richard's scheme perhaps intravenous drop administration of 5,0 g of magnesium of sulfate (20 ml of 25% of solution) in cultivation on 400 ml of 0,9% of solution of sodium of chloride or 5% of glucose with a speed of 9-25 mg/min. (15-40 caps/min.).
To children for stopping of spasms appoint at the rate of 20-40 mg/kg (0,08 - 0,16 ml/kg of 25% of solution) intramusculary.
Duration of treatment is established by the attending physician.
Features of use:
In need of magnesium, simultaneous in/in administrations of salts, and calcium they are entered into different veins.
Sulfate magnesium use for stopping of the epileptic status is possible (as a part of complex therapy).
Patients with a heavy renal failure should not receive more than 20 g of magnesium of sulfate (81 mmol of Mg2+) during 48 h, patients with an oliguria or a heavy renal failure should not enter magnesium sulfate in/in too quickly. Control of concentration 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/mines) is recommended, to the ABP.
At parenteral use it is necessary to observe extra care not to create toxic concentration of drug. Elderly patients often need a dose decline (weakening of function of kidneys).
Solution for injections can be also used for intake (as HP laxative).
At pregnancy apply with care, only in cases when the expected therapeutic effect exceeds potential risk for a fruit. In need of use in the period of a lactation, breastfeeding should be stopped.
Influence on ability to manage motor transport or other mechanisms is not established.
Side effects:
- bradycardia, disturbance of endocardiac conductivity
- feeling of inflows of heat, perspiration, diplopia
- hypotension, muscular weakness, headache
- deep sedation, oppression of tendon jerks
- asthma
- polyuria
- hypoventilation up to аплоэ.
Interaction with other medicines:
Strengthens effect of other medicines, the oppressing TsNS.
Cardiac glycosides increase risk of disturbance of conductivity and AV of blockade (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 other vazodilatator strengthening of hypotensive effect is possible.
Barbiturates, narcotic analgetics, the hypotensive medicines (M) 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 sodium hydrocortisone succinate, polymyxin B sulfate, Procainum a hydrochloride, salicylates and tartrates. At concentration of magnesium higher than 10 mmol/ml in mixes for full parenteral food are possible division of fatty emulsions.
Contraindications:
- the expressed bradycardia or an atrioventricular block
- the expressed renal failures (clearance of creatinine less than 20 ml/min.)
- hypersensitivity and gipermagniyemiya
- acute inflammatory diseases of a gastro intestinal path
- the predrodovy period (for 2 h before childbirth)
- lactation period.
Overdose:
Symptoms: disappearance of a knee jerk, nausea, vomiting, sharp decrease in the ABP, bradycardia, respiratory depression and TsNS.
Treatment: in/in slowly, solution of Calcii chloridum or calcium of a gluconate - 5-10 ml of 10%, carry out an oxygenotherapy, inhalation of Carbogenum, an artificial respiration, peritoneal dialysis or a hemodialysis, symptomatic therapy.
Storage conditions:
To store in the dry, protected from light place, at a temperature not above 30 °C. To store in the place, unavailable to children!
Issue conditions:
According to the recipe
Packaging:
Solution for injections of 25% 5 ml in ampoules of neutral glass.
On 5 ampoules pack into a blister strip packaging.
