Tolperisone
Obolensky OP
1440 Items
2019-09-19
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Clinical Pharmacology
Tolperisone OBL - muscle relaxant, has a selective inhibitory effect on the caudal part of the reticular formation of the brain, has central holinoblokiruyuschimi properties.
It has no effect on the peripheral parts of the nervous system, has a weak antispasmodic and vasodilating effect.
Indications
- spinal and cerebral paralyzes (hypertonus, muscle spasm, spinal automatism; limb contracture).
- diseases with dystonia, rigidity, muscle spasm; arterial disease obliterans: obliterating atherosclerosis of the limb vessels, diabetic angiopathy, thromboangiitis obliterans (Buerger's disease), Raynaud's syndrome.
- effects of disorders of vascular innervation (acrocyanosis, "intermittent" angioedema).
- extrapyramidal disorders (post-encephalic and atherosclerotic parkinsonism).
- postthrombotic disorders of lymph circulation and venous circulation, trophic ulcer of the leg, children spastic paralysis (Little disease), epilepsy, vascular genesis encephalopathy; hypertonus in combination with a violation of muscle tone of another type.
Composition
1 tablet contains: Tolperisone hydrochloride - 50 mg.
Excipients: citric acid, lactose monohydrate (milk sugar), hyprolose (hydroxypropylcellulose), crospovidone, stearic acid.
Shell auxiliaries: Opadry II (Series 85) [polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide].
Tolperisone is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Obolensky OP | Russia | pills | |
| Mydocalm | Gedeon Richter | Hungary | pills |
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Dosage and Administration
Inside
For adults, the initial dose of 50 mg 2-3 times a day, with a gradual increase to 150 mg 2-3 times a day.
The duration of the course of treatment depends on the severity and nature of the course of the disease.
Adverse reactions
- headache,
- myasthenia gravis
- decrease in blood pressure
- nausea,
- vomiting
- gastralgia,
- allergic reactions (anaphylactic shock, bronchospasm, urticaria, erythematous rash, pruritus).
Contraindications
- hypersensitivity (including to lidocaine),
- myasthenia gravis
- children's age (up to 1 year).
Drug interactions
Drugs for general anesthesia, peripheral muscle relaxants, psychoactive drugs, clonidine enhance the effect.
Pregnancy and Lactation
Contraindicated during pregnancy and lactation.
Special instructions
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.
Overdosage
Symptoms: respiratory depression and cardiac activity, lowering blood pressure.
Treatment: symptomatic.
- Brand name: Mydocalm
- Active ingredient: Tolperisone
- Dosage form: pills, film coated.
- Manufacturer: Obolensky OP
- Country of Origin: Russia
- Synthesis of 3H-tolperisone
- Tolperisone: Evaluation of the Lidocaine-Like Activity by Molecular Modeling
- Gas—liquid chromatographic method for the determination of tolperisone in human plasma: pharmacokinetic and comparative bioavailability studies
- NMR analysis, protonation equilibria and decomposition kinetics of tolperisone
- Simultaneous determination of tolperisone and lidocaine by high performance liquid chromatography
- Simultaneous micellar LC determination of lidocaine and tolperisone
- High performance thin layer chromatographic determination of tolperisone hydrochloride
- Synthesis and resolution of a Tolperisone metabolite
- Synthesis, resolution and absolute configuration of a tolperisone metabolite
- Synthesis of some tolperisone metabolites in racemic and optically active form
- Prophylactic tolperisone for post-exercise muscle soreness causes reduced isometric force – a double-blind randomized crossover control study
- Comprehensive studies of Tolperisone·HCl-cyclodextrin complexes
- Optimization of the reversed-phase high-performance liquid chromatographic separation of the enantimers of a cationic chiral drug (tolperisone) on a heptakis(6-azido-6-deoxy) perphenylcarbamated β-cyclodextrin column
- HPLC Determination of tolperisone in human plasma
- A randomized, double-blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke
- Tolperisone: A Typical Representative of a Class of Centrally Acting Muscle Relaxants with Less Sedative Side Effects
- LC-UV Assay of Tolperisone HCl from Sustained Release Matrix Tablets
- A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms
- Fatal tolperisone poisoning: Autopsy and toxicology findings in three suicide cases
- Efficacy and tolerance of repeated oral doses of tolperisone hydrochloride in the treatment of painful reflex muscle spasm: results of a prospective placebo-controlled double-blind trial
- Determination of tolperisone in human plasma by liquid chromatography/tandem mass spectrometry for clinical application
- Tolperisone disappoints in phase IIb study in spasticity
- PP136—Genetic polymorphism of CYP2D6 significantly affects the pharmacokinetics of tolperisone
- PP124—Pharmacokinetics of tolperisone in relation to CYP2C19 genotypes
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