• Rating:
  • Manufacturer:
  • Model:
    1396
  • Available:
    In stock
  • Availability date:
    2020-07-30
  • Dosage form:
    solution
  • In stock:
    496 Items

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Composition:


active ingredient: methocarbamol;


1 ml of the solution for injection contains metocarbamol 100 mg;


excipients: polyethylene glycol 300, sodium hydrosulfite (E 223), concentrated hydrochloric acid, water for injection.


Dosage form. Solution for injection.


Basic physical and chemical properties: transparent colorless solution.


Pharmacotherapeutic group. Muscle relaxants with a central mechanism of action. Carbamic acid esters. ATX code M03B A03.


Pharmacological properties.


Pharmacodynamics.


Metocarbamol is a central-acting muscle relaxant with sedative properties. It does not directly relax tense skeletal muscles in humans. The mechanism of action has not been established, but it may be associated with general depression of the central nervous system (CNS). Its action is manifested by relieving pain, reducing muscle spasms and increasing the mobility of the affected muscle. Pain relief is caused by changes in the perception of pain. Unlike neuromuscular blockers, metocarbamol does not affect nerve conduction, neuromuscular transmission, or muscle excitability.


Metocarbamol has a long-term blocking effect on polysynaptic reflex pathways at doses that do not significantly change transmission through monosynaptic reflex arcs, and interrupts pathological impulses from areas of muscle damage. It does not have a direct effect on the mechanism of contraction of striated muscles, motor synapse or nerve fiber.


Pharmacokinetics.


In healthy volunteers, the plasma clearance of metocarbamol ranges from 0.20 to 0.80 L/H/kg, the average Half-Life is from 1 to 2 hours, and binding to plasma proteins is in the range from 46 to 50 %.


Methocarbamol is metabolized by dealkylation and hydroxylation, and conjugation is also possible. All metabolites of metocarbamol are excreted in the urine. A small amount of unchanged Methocarbamol is also excreted in the urine.


Special groups of patients.


Elderly people.


The mean Half-Life of Methocarbamol in healthy elderly volunteers (mean age 69 (± 4) years) was slightly longer than in healthy young volunteers (mean age 53.3 (± 8.8)) years), healthy population (1.5 (± 0.4) hours vs. 1.1 (± 0.27) hours, respectively). The proportion of bound Methocarbamol in older volunteers is slightly lower than in younger volunteers (41-43% vs. 46-50%, respectively).


Patients with impaired renal function.


The clearance of metocarbamol in 8 patients with impaired renal function during maintenance hemodialysis was reduced by approximately 40% compared to 17 healthy volunteers, although the average half-life in these two groups was similar (1.2 (± 0.6) vs. 1.1 ( ± 0.3 hours, respectively).


Patients with impaired liver function.


In 8 patients with secondary cirrhosis caused by alcohol abuse, the average total clearance of metocarbamol was reduced by approximately 70% compared to that obtained in 8 healthy volunteers of the same age and with the same body weight.


The mean elimination Half-Life (± SD) in patients with cirrhosis and healthy volunteers was 3.38 (± 1.62) hours and 1.11 (± 0.27) hours, respectively. The percentage of metocarbamol bound to plasma proteins decreased to about 40-45% compared to 46-50% in healthy volunteers.


Clinical characteristics.


Indications.


To relieve the discomfort associated with acute pain in diseases of the musculoskeletal system as a supplement to the regime of limited physical activity (muscle rest), physical therapy and other activities.


Contraindications.


It should not be prescribed to patients with kidney diseases or suspected of their existence, due to the presence of polyethylene glycol 300 in the drug, which increases the existing acidosis and urinary retention in patients with impaired renal function.


Hypersensitivity to metocarbamol or to any of the excipients of the drug.


Interactions with other drugs and other types of interactions.


Metocarbamol may inhibit the action of pyridostigmine bromide, so it should be used with caution in patients with Myasthenia gravis receiving anticholinesterase agents.


Since metocarbamol may have a general CNS suppression effect, patients receiving injectable metocarbamol should be warned about the combination of effects with alcohol and other CNS depressants.


Impact on laboratory results


Metocarbamol may cause color interference in some 5-hydroxyindolacetic acid (5-HYOC) screening tests using nitrosonaphthol reagent and in vanillylmygdalic acid (IUD) urine screening tests using the Gitlow method.


Application features.


Caution should be exercised when using the injectable form in patients with epilepsy or suspected epilepsy.


As with other medications that are administered intravenously or intramuscularly, the dose should be carefully monitored and the injection rate should be observed. The rate of administration should not exceed 3 mL per minute, that is, two ampoules of 5 ml should be administered for approximately 3 minutes. Since the injectable drug metocarbamol is hypertensive, vascular extravasation should be avoided. A horizontal position of the patient will reduce the likelihood of adverse reactions.


The blood that enters the syringe does not mix with the hypertonic solution. This phenomenon is observed for many other intravenous drugs. Blood can be injected together with Methocarbamol, or the injection can be stopped after the plunger reaches the blood, depending on what the doctor prefers.


The drug contains sodium hydrosulfite, which can rarely cause hypersensitivity reactions and bronchospasm.


Use during pregnancy or lactation.


Pregnancy


Studies of the effect of metocarbamol on animals have not been conducted. Data on possible adverse effects on fetal development are insufficient. Very rarely, intrauterine and congenital abnormalities have been reported due to intrauterine exposure to metocarbamol. Therefore, injectable Methocarbamol should not be used in pregnant women, especially in the early stages of pregnancy, and in women planning pregnancy, except when, according to the doctor's assessment, the potential benefit outweighs the possible risk.


Breast-feeding period


Metocarbamol and / or its metabolites are excreted in animal milk. However, there are no data on the excretion of its metabolites in human breast milk. Caution should be exercised when prescribing metocarbamol to women who are breast-feeding.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


The patient should be warned that metocarbamol may cause drowsiness or dizziness, which may impair the ability to drive vehicles or maintain other mechanisms.


There may be deterioration of mental and/or physical abilities that are necessary to perform dangerous tasks, such as operating machinery and equipment, or driving a car. Patients should be warned about the risks associated with operating machinery and equipment, including driving a car, until they are sure that metocarbamol therapy does not adversely affect their ability to engage in such activities.

Dosage and administration.


It is intended for intravenous and intramuscular use only. The total dose for adults should not exceed 30 ml per day for no more than 3 consecutive days, with the exception of tetanus treatment. If the patient's condition requires continued treatment with metocarbamol, such a course can be repeated after a 48-hour break. The dosage and frequency of injections should be based on the severity of the condition and the response to treatment.


For the most severe cases or in the postoperative state, additional doses of 1 gram can be repeated every 8 hours, up to a maximum of 3 g per day for no more than 3 consecutive days.


Instructions for intravenous use.


Metocarbamol solution can be administered undiluted directly into a vein at a maximum rate of 3 mL/min. One ampoule is used as a single dose. It can also be added to an intravenous dropper of 0.9% sodium chloride solution or up to 5% dextrose solution. The drug should not be diluted in more than 250 ml.


AFTER MIXING, DO NOT PUT THE FINISHED SOLUTION FOR INTRAVENOUS INFUSION IN THE REFRIGERATOR. Care should be taken to prevent vascular extravasation of this hypertonic solution, as thrombophlebitis may occur. It is best to keep the patient in a horizontal position during and for at least 10-15 minutes after the injection.


Instructions for intramuscular use.


If intramuscular administration is provided, no more than 5 ml should be injected into each gluteal area. If necessary, the injection can be repeated at intervals of 8 hours.


It is not recommended for subcutaneous administration.


Special instructions for use in tetanus.


There is clinical evidence that Methocarbamol may have a beneficial effect on the control of neuromuscular manifestations of tetanus. However, this does not replace the usual wound treatment procedure, the use of tetanus antitoxin, penicillin, tracheotomy, fluid balance control, and symptomatic treatment. Injectable metocarbamol should be added to the course of treatment as soon as possible.


For adults. Insert 10 ml or 20 ml directly into the tube of the pre-inserted needle. An additional 10 ml or 20 ml can be added to the infusion solution so that the total initial dose is 30 ml. This procedure should be repeated every 6 hours if necessary.


For children. The recommended minimum starting dose is 15 mg/kg or 500 mg/m2. If necessary, this dose can be repeated every 6 hours. The total dose should not exceed 1.8 g/m2 for 3 consecutive days. Maintenance doses can be administered by injection into a tube or by intravenous infusion with an appropriate amount of fluid (see instructions for intravenous use).


Children.


The safety and efficacy of injectable Methocarbamol in pediatric patients has not been established, except in cases of tetanus (see the section "dosage and administration").


Overdose.


Information on the acute toxicity of Methocarbamol is limited. Overdose of metocarbamol is often combined with alcohol or other drugs that depress the central nervous system, and includes the following symptoms: nausea, drowsiness, blurred vision, hypotension, convulsions and coma. In the post-marketing period, deaths were reported from overdose of metocarbamol or when it was used together with other drugs that depress the central nervous system, alcohol or psychotropic drugs.


Treatment


Overdose care includes symptomatic and supportive treatment. Supportive measures include ensuring airway patency, monitoring urine output and vital signs of the body, and, if necessary, intravenous fluids. The effectiveness of hemodialysis in case of overdose is unknown.


Adverse reactions.


The following adverse reactions have been reported with metocarbamol (some of them may be associated with excessively rapid intravenous injection):


From the body as a whole: anaphylactic reaction, angioedema, fever, headache.


From the cardiovascular system: bradycardia, redness (hot flashes), hypotension, loss of consciousness, thrombophlebitis.


In most cases, the return to consciousness occurred independently. In other cases, epinephrine, injectable steroids, and/or injectable antihistamines were used for Acceleration.


From the digestive system: dyspepsia, jaundice (including cholestatic jaundice), nausea and vomiting.


From the blood and lymphatic system: leukopenia.


Immune system disorders: hypersensitivity reactions.


Nervous system disorders: amnesia, confusion, diplopia, fainting or pre-fainting, drowsiness, insomnia, mild muscle discoordination, nystagmus, lethargy, convulsions (including epileptic seizures), dizziness.


Seizures have been reported during intravenous administration of metocarbamol in patients suffering from epilepsy, one of the causes of which may be mental trauma from the procedure. Despite reports of successful discontinuation of epileptiform seizures with metocarbamol, it is not recommended to use it in patients with epilepsy.


From the skin: itching, rash, urticaria.


From the sensory organs: blurred vision, conjunctivitis, nasal congestion, metallic taste.


Other: pain and flaking at the injection site.

Tags: Dorsum® [Metocarbomol]