Miotolid (Solution) Instructions for Use

Marketing Authorization Holder

S.C. Rompharm Company S.R.L. (Romania)

Manufactured By

S.C. Rompharm Company S.R.L. (Romania)

ATC Code

M03BX04 (Tolperisone)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Tolperisone (Rec.INN registered by WHO)

Dosage Form

Miotolid

Solution for intramuscular injection 100 mg+2.5 mg

Dosage Form, Packaging, and Composition

Solution for intramuscular injection

1 ml – ampoules (5 pcs.) – cardboard packs – By prescription

Clinical-Pharmacological Group

Centrally acting muscle relaxant

Pharmacotherapeutic Group

Centrally acting muscle relaxants; other centrally acting muscle relaxants

Pharmacological Action

A combined agent, the action of which is determined by the properties of its constituent components.

Tolperisone hydrochloride is a centrally acting muscle relaxant. It has a membrane-stabilizing, local anesthetic effect, inhibits the conduction of nerve impulses in primary afferent fibers and motor neurons, which leads to the blocking of spinal mono- and polysynaptic reflexes. It presumably mediates the blocking of neurotransmitter release by inhibiting the influx of calcium ions into synapses. It inhibits excitation conduction along the reticulospinal pathway in the brainstem. Independently of its effect on the CNS, it enhances peripheral blood flow. A weak antispasmodic and antiadrenergic effect of tolperisone may play a role in the development of this effect.

Lidocaine hydrochloride has a local anesthetic action; when used in recommended doses, it does not have a systemic effect.

Pharmacokinetics

Tolperisone hydrochloride

Tolperisone is extensively metabolized in the liver and kidneys. It is excreted in the urine almost exclusively (>99%) as metabolites. The pharmacological activity of the metabolites is unknown. T_1/2 after IV administration is about 1.5 hours.

Lidocaine hydrochloride

Absorption is complete (the rate of absorption depends on the site of administration and the dose). Time to reach C_max in plasma after IM administration is 30-45 minutes. Plasma protein binding is 50-80%.

It is rapidly distributed in tissues and organs. It penetrates the blood-brain barrier and the placental barrier, and passes into breast milk (40% of the concentration in maternal plasma). It is metabolized in the liver (90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and cleavage of the amide bond with the formation of active metabolites. It is excreted in the bile (part of the dose undergoes reabsorption in the gastrointestinal tract) and by the kidneys (up to 10% unchanged).

Indications

Hypertonia and spasm of striated muscles arising from organic diseases of the CNS (including damage to the pyramidal tracts, multiple sclerosis, stroke, myelopathy, encephalomyelitis), the musculoskeletal system (including spondylosis, spondyloarthrosis, cervical and lumbar syndromes, arthrosis of large joints); restorative treatment after orthopedic and trauma surgeries.

As part of complex therapy: for obliterating vascular diseases (obliterating atherosclerosis, diabetic angiopathy, obliterating thromboangiitis, Raynaud’s disease, diffuse scleroderma); for diseases arising from disorders of vascular innervation (acrocyanosis, intermittent angioneurotic dysbasia).

ICD codes

Dosage Regimen

Administer Miotolid by intramuscular injection only. Do not administer intravenously.

For adults, the usual dose is 100 mg tolperisone hydrochloride and 2.5 mg lidocaine hydrochloride (contents of one 1 ml ampoule) twice daily.

Inject deeply into the gluteal muscle. Alternate injection sites between left and right sides.

The maximum daily dose is 200 mg tolperisone hydrochloride (two 1 ml ampoules). Do not exceed this dose.

The duration of treatment is determined by the physician based on clinical response and the underlying condition.

Use with caution in patients with hepatic impairment or renal impairment. No specific dose adjustment is required for these populations.

This medication is contraindicated in children and adolescents under 18 years of age.

Adverse Reactions

From the hematopoietic system very rarely – anemia, lymphadenopathy.

From the immune system rarely – hypersensitivity reactions, anaphylactic reactions; very rarely – anaphylactic shock.

From metabolism infrequently – anorexia; very rarely – polydipsia.

Psychiatric disorders infrequently – insomnia, sleep disorders; rarely – loss of activity, depression.

From the nervous system infrequently – headache, dizziness, drowsiness; rarely – attention deficit syndrome, tremor, convulsions, loss of sensation, sensory disorders, lethargy.

From the organ of vision rarely – visual perception disorders.

From the organ of hearing and labyrinthine disorders rarely – tinnitus, vertigo.

From the cardiovascular system infrequently – arterial hypotension; rarely – angina pectoris, tachycardia, palpitations; very rarely – bradycardia, flushing.

From the respiratory system rarely – dyspnea, epistaxis, tachypnea.

From the digestive system infrequently – gastrointestinal discomfort, diarrhea, dry mouth, dyspepsia, nausea; rarely – epigastric pain, constipation, flatulence, vomiting, liver function disorders.

From the skin and subcutaneous tissues rarely – allergic dermatitis, sweating, skin itching, urticaria, skin rash.

From the musculoskeletal system infrequently – muscle weakness, myalgia, limb pain; rarely – limb discomfort; very rarely – osteopenia.

From the urinary system rarely – enuresis, proteinuria.

General disorders and administration site conditions often – injection site redness; infrequently – asthenia (weakness), malaise, fatigue; rarely – feeling of drunkenness, feeling of heat, irritability, thirst; very rarely – chest discomfort.

Laboratory and instrumental data rarely – decreased blood pressure, increased bilirubin concentration, impaired liver function tests, decreased platelet count, increased white blood cell count; very rarely – increased creatinine level.

Contraindications

Hypersensitivity to the components of the drug, severe myasthenia gravis; pregnancy, breastfeeding period; children and adolescents under 18 years of age.

With caution, the drug should be used in renal and hepatic insufficiency (dose adjustment is not required).

Use in Pregnancy and Lactation

Use during pregnancy is indicated only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

During treatment, the issue of discontinuing breastfeeding should be decided.

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

With caution should be used in hepatic insufficiency (dose adjustment is not required).

Use in Renal Impairment

With caution should be used in renal insufficiency (dose adjustment is not required).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

Effect on ability to drive vehicles and mechanisms

Caution must be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

There are no data on the interaction of this drug with other drugs that limit the use of the drug.

Although tolperisone does affect the CNS, the drug does not cause a sedative effect, so it can be used in combination with sedatives, hypnotics and drugs containing ethanol.

It does not enhance the effect of ethanol on the CNS.

It enhances the effect of NSAIDs, so when used concomitantly, a dose reduction of the latter may be required.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.