Tolperizon (Tablets) Instructions for Use

Instructions
Dosage forms

ATC Code

M03BX04 (Tolperisone)

Active Substance

Tolperisone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Centrally acting muscle relaxant

Pharmacotherapeutic Group

Muscle relaxants; centrally acting muscle relaxants; other centrally acting muscle relaxants

Pharmacological Action

Centrally acting muscle relaxant. The reduction of pathologically increased skeletal muscle tone is explained by the ability of tolperisone to suppress spinal polysynaptic reflexes and its inhibitory effect on the caudal part of the reticular formation.

It has central N-cholinoblocking properties. It does not have a significant effect on the peripheral parts of the nervous system. It has a weak antispasmodic and vasodilating effect.

Indications

Spinal and cerebral palsies (hypertonia, muscle spasm, spinal automatism; limb contractures).

Diseases accompanied by dystonia, rigidity, muscle spasm; obliterating arterial diseases: obliterating atherosclerosis of limb vessels, diabetic angiopathy, obliterating thromboangiitis (Buerger’s disease), Raynaud’s syndrome.

Consequences of disorders of vascular innervation (acrocyanosis, intermittent angioneurotic dysbasia).

Extrapyramidal disorders (postencephalitic and atherosclerotic parkinsonism).

Postthrombotic disorders of lymph circulation and venous circulation, trophic leg ulcer, infantile spastic paralysis (Little’s disease), epilepsy, encephalopathy of vascular origin; hypertonia combined with a violation of muscle tone of another type.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
G21.3	Postencephalitic parkinsonism
G21.4	Vascular parkinsonism
G24	Dystonia (including dyskinesia)
G40	Epilepsy
G80	Cerebral palsy
G81.1	Spastic hemiplegia
G82.1	Spastic paraplegia
G82.4	Spastic tetraplegia
G93.4	Unspecified encephalopathy
I73.0	Raynaud's syndrome
I73.1	Obliterative thromboangiitis [Buerger's disease]
I73.8	Other specified peripheral vascular diseases
I73.9	Peripheral vascular disease, unspecified (including intermittent claudication, arterial spasm)
I79.2	Peripheral angiopathy in diseases classified elsewhere (including diabetic angiopathy)
I87.0	Postthrombotic syndrome
L98.4	Chronic skin ulcer, not elsewhere classified
R25.2	Cramp and spasm

ICD-11 code	Indication
4A44.8	Thromboangiitis obliterans
7A82	Sleep related leg cramps
8A00.23	Vascular parkinsonism
8A00.2Y	Other specified secondary parkinsonism
8A02.Z	Dystonic disorders, unspecified
8A6Z	Epilepsy or epileptic seizures, unspecified
8D2Z	Cerebral palsy, unspecified
8E47	Encephalopathy, not elsewhere classified
8E4A.0	Paraneoplastic or autoimmune disorders of the central nervous system, including brain and spinal cord
8E63	Post-cardiopulmonary bypass encephalopathy
BD42.0	Raynaud's disease
BD42.1	Raynaud's syndrome
BD42.Z	Raynaud's phenomenon, unspecified
BD4Z	Chronic obliterative arterial diseases, unspecified
BD53.Y	Other specified secondary involvement of arteries and arterioles
BD5Z	Diseases of arteries or arterioles, unspecified
BD74.Z	Chronic venous insufficiency of lower extremities, unspecified
EA40	Tropical phagedenic ulcer
EF60	Ischemic ulceration of the skin
EG00	Dilation of skin vessels of the extremities
EM0Z	Unspecified skin disorder
MB40.7	Acroparesthesia
MB47.3	Convulsion or spasm
MB50.1	Spastic tetraplegia
MB53.2	Spastic hemiplegia
MB56	Paraplegia
ME60.2	Ulcerative skin lesion of unspecified nature

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Administer tablets orally with a full glass of water during or after a meal to minimize potential gastrointestinal discomfort.

Initiate therapy with an initial dose of 50 mg taken two to three times daily.

Gradually titrate the dosage upward based on individual patient tolerance and therapeutic response.

The standard maintenance dose for adults is 150 mg two to three times daily.

The maximum total daily dose should not exceed 450 mg.

For intramuscular administration, inject 100 mg twice daily; administer deep into the muscle.

For intravenous administration, inject 100 mg once daily as a single, slow injection.

Adjust the dosage regimen carefully in patients with hepatic impairment or renal insufficiency.

Closely monitor elderly patients for adverse effects; a lower maintenance dose may be sufficient.

Abrupt discontinuation of therapy is not recommended; taper the dose gradually under medical supervision.

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

Adverse Reactions

Possible headache, myasthenia, arterial hypotension, nausea, vomiting, gastralgia, allergic reactions (anaphylactic shock, bronchospasm, urticaria, erythematous rashes, skin itching).

Contraindications

Myasthenia gravis, pregnancy, lactation period, children and adolescents under 18 years of age, hypersensitivity to tolperisone.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Pediatric Use

Contraindicated in children under 1 year of age.

Special Precautions

Effect on the ability to drive vehicles and operate machinery

Use with caution in patients whose activities require increased attention and speed of psychomotor reactions.

Drug Interactions

The effect of tolperisone is enhanced when used concomitantly with drugs for general anesthesia, peripheral muscle relaxants, psychoactive drugs, and with clonidine.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Tolperizon Renewal [Obnovlenie Pfc, JSC (Russia)]
Film-coated tablets 50 mg: 10, 20, 30, 40 or 50 pcs.
Film-coated tablets 150 mg: 10, 20, 30, 40 or 50 pcs.

Marketing Authorization Holder

Obnovlenie Pfc, JSC (Russia)

Dosage Forms

	Tolperisone Renewal	Film-coated tablets 50 mg: 10, 20, 30, 40 or 50 pcs.
		Film-coated tablets 150 mg: 10, 20, 30, 40 or 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, with a characteristic odor, round, biconvex; surface roughness is allowed; the core on the cross-section is white or almost white.

	1 tab.
Tolperisone (as hydrochloride)	50 mg

Excipients: microcrystalline cellulose PH101, lactose monohydrate, croscarmellose sodium, hypromellose (hydroxypropyl methylcellulose), citric acid monohydrate, magnesium stearate; shell composition: hypromellose (hydroxypropyl methylcellulose) (E464), titanium dioxide (E171), macrogol 4000 (polyethylene glycol 4000) (E1521).

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.

Film-coated tablets white or almost white, with a characteristic odor, round, biconvex; surface roughness is allowed; the core on the cross-section is white or almost white.

	1 tab.
Tolperisone (as hydrochloride)	150 mg

Tolperizon Velpharm [Elzapharm, LLC (Russia)]
Film-coated tablets 50 mg: 20, 30, 40, 50, 60, 70, 80, 90, or 100 pcs.
Film-coated tablets 150 mg: 20, 30, 40, 50, 60, 70, 80, 90, or 100 pcs.

Marketing Authorization Holder

Elzapharm, LLC (Russia)

Manufactured By

Velpharm, LLC (Russia)

Velpharm-M, LLC (Russia)

Dosage Forms

	Tolperisone Velpharm	Film-coated tablets 50 mg: 20, 30, 40, 50, 60, 70, 80, 90, or 100 pcs.
		Film-coated tablets 150 mg: 20, 30, 40, 50, 60, 70, 80, 90, or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex, with a characteristic odor. The core on the cross-section is white or almost white.

	1 tab.
Tolperisone hydrochloride	50 mg

Excipients: microcrystalline cellulose 101, lactose monohydrate (milk sugar), croscarmellose sodium (primellose), hypromellose (oxypropyl methylcellulose), citric acid monohydrate, magnesium stearate.
Dry mixture for film coating contains: hypromellose, titanium dioxide, macrogol or hypromellose (oxypropyl methylcellulose), titanium dioxide, macrogol 6000 (polyethylene glycol 6000, polyethylene oxide 6000).

10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (7) – cardboard packs.
10 pcs. – contour cell packaging (8) – cardboard packs.
10 pcs. – contour cell packaging (9) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
20 pcs. – jars (1) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
40 pcs. – jars (1) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
60 pcs. – jars (1) – cardboard packs.
70 pcs. – jars (1) – cardboard packs.
80 pcs. – jars (1) – cardboard packs.
90 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.