Muscle pain is the scourge of our time. Neck and lower back discomfort from sitting, the effects of trauma – all this creates discomfort and affects the quality of life. The modern pharmaceutical market offers different ways to solve the problem. The most effective in the fight against muscle pain are myorelaxants – especially in combination with NSAIDs and non-pharmacological methods of action (LFC, massage).
The experts of our magazine have studied the myorelaxants presented by pharmaceutical companies and identified two popular products among them – Midocalm and Tolperizone. They are similar in composition, dosage, beneficial effect and indications. We found that Midocalm is an original drug with a good evidence base and accumulated practical experience of use. Tolperizone is a generic, and its effectiveness may be lower. A detailed comparison of drugs is presented in the article.
Form release and composition: is there a difference?
The active substance of both drugs is tolperizone hydrochloride. This is a muscle relaxant of central action. Released in the pharmacy strictly by prescription.
Myorelaxant release forms are different:
Midocalm is available in tablets (50 and 150 mg) and solution for injection (10%). Manufactured by Gedeon Richter (Hungary).
Tolperizone is presented in tablets (50 mg) and solution for injection (10%). Produced in Russia.
The cost of the drugs varies. The original Midocalm is more expensive – a pack of 50 mg tablets (30 pieces) will cost 300-400 rubles. Tolperizone is one and a half times cheaper. Often patients buy a cheap muscle relaxant, but it is not always justified. Why this is the case – let’s figure it out.
How myorelaxants work?
Before we talk about the effects of tolperisone, it is worth considering the types of myorelaxants:
Central action. They affect motor neurons in the central nervous system – structures of the brain and spinal cord.
Peripheral action. They work at the junction of muscle fibers and nerve endings – the neuromuscular synapses. Does not affect the CNS.
Mydocalm and Tolperizone are central muscle relaxants. Their mechanism of action is not fully understood. Previously, scientists believed that such drugs only block the conduct of signals along the reflex arc. No signal – the muscles don’t work and relax. Today we know: the action of muscle relaxants is more complex and is associated with such aspects:
They stabilize the membranes of neurons (nerve cells);
inhibit impulse conduction in sensory and motor fibers;
Disrupt impulse conduction along reflex arcs;
Block sodium channels and inhibit calcium influx into synapses.
It reduces pain and normalizes muscle tone.
Tolperisone also increases peripheral blood flow. This is possible due to the weak antispasmodic and vasodilator action of the drug. Does not affect the peripheral nervous system.
So, tolperizone has a triple action:
will stop the pain;
Relieves muscle spasm;
improves blood circulation.
Myorelaxant breaks the vicious circle of “pain – muscle spasm – pain” that occurs in many diseases of the spine, joints, and peripheral nerves. When combined with other medications, it effectively deals with the resulting problem and improves quality of life.
Pharmacokinetics of original Midocalm is well studied. The drug is quickly absorbed after oral administration and peaks in 0.5-1 hour. Its bioavailability is low – about 20%. Remains effective for 6-8 hours, so it is prescribed several times a day. Is metabolized in the liver and kidneys and excreted in the urine as metabolites.
Generic Tolperizone according to WHO recommendations must be a full analogue of the original – that is, have biological and therapeutic equivalence. In other words, it should distribute in the body exactly the same way, have a similar effect in the same dosage. But in Russia, the requirements for generics are softer – it is enough that the copy is biologically equivalent to the original – that is, it spreads in the tissues at the same rate.
We suggest that Tolperizone also reaches its maximum effect after 0.5-1 hour and lasts for 6-8 hours. Whether its therapeutic effect will be comparable to the original is unknown. This requires a full cycle of clinical studies, which the manufacturer is not required to do.
50 years of practical use: evaluation of the effectiveness of the drugs
Myorelaxants have been used in medicine since the 70s. Experience shows that Tolperizone is effective and meets expectations. Its positive effect has been confirmed by clinical trials:
Increased muscle tone is a symptom found in many neurological and orthopedic conditions. Clinical trials show that prescribing muscle relaxants together with analgesics significantly increases the effectiveness of therapy and reduces drug dosages.
Centrally acting myorelaxants are recommended for the treatment of osteoarthritis of the hip joint. Studies conducted in 2014-2017 showed: tolperizone is effective in patients with a predominant arthritic component (pain, swelling, stiffness of movement in the joint).
Myorelaxants are indicated in the complex therapy of nonspecific low back pain. The authors of the study recommend using tolperizone together with nonsteroidal anti-inflammatory drugs to enhance the effect.
All of this applies to tolperizone, the active ingredient in both drugs. And here is what they write in the medical literature about the original Midocalm:
A multicenter research project was completed in 2013. It involved 13 countries, 284 cities, 2,090 medical facilities and more than 35,000 patients. The effectiveness of Midocalm for pain relief in muscle spasms was demonstrated.
The positive effects of Midocalm after a stroke were shown. A randomized, double-blind, placebo-controlled trial has confirmed that Midocalm normalizes muscle tone, relieves pain, accelerates rehabilitation and improves quality of life.
A Parus clinical trial has confirmed that Midocalm has analgesic and muscle relaxant effects. Results are noticeable on the third day after the start of therapy and reach a maximum on the 10th day. Control ultrasound showed improvement and even restoration of blood flow in the tissues. The authors emphasize: the drug does not have a sedative effect and does not affect blood pressure, which distinguishes it from other muscle relaxants.
In the Russian-language literature, Midocalm is claimed as one of the best remedies for the treatment of back pain associated with muscle spasm. The authors note that the drug is effective in the treatment of acute lumbar pain. The prescribed myorelaxant relieves unpleasant symptoms, speeds recovery and reduces the period of disability.
Mydocalm in injectable form is recommended for rapid pain relief. Intramuscular injection of the drug is proven to reduce pain after only 1.5 hours. The authors of the study claim: Midocalm not only relieves the condition, but also gets rid of kinesiophobia – the fear of movement against the background of the disease.
Trial of generic Tolperizone was completed in 2018. A multicenter randomized placebo-controlled trial showed: the combination therapy of Tolperizone + NSAIDs is significantly better than the treatment with non-steroidal anti-inflammatory drugs alone. The authors suggest starting treatment with injectable forms of Tolperisone and then switching to tablets.
When muscle relaxants are prescribed?
The indications for both drugs are similar. They are prescribed where it is necessary to relieve increased muscle tone:
Organic CNS pathology: stroke, multiple sclerosis, encephalomyelitis, etc.;
Musculoskeletal system disorders: arthrosis of large joints (hip, knee, shoulder), spondyloarthrosis, osteochondrosis, etc.;
Rehabilitation after surgery in traumatology and orthopedics;
Vascular obliterating diseases: Raynaud’s disease, diabetic angiopathy, scleroderma, etc.;
impaired vascular innervation;
Encephalopathy (brain damage) with muscle dystonia (including Little’s disease).
Myorelaxants are usually used in combination with other drugs – anti-inflammatory, analgesics, vasodilators. As monotherapy, tolperizone is not as effective.
Mydocalm and Tolperizone tablets are prescribed after meals. Must not be chewed, only swallowed whole with water. The regimen of administration is determined by the doctor, taking into account the age and condition of the patient. The pills are usually taken 2 to 3 times a day.
Intramuscular muscle relaxants are usually prescribed at the beginning of therapy. After achieving the desired effect, the patient is switched to tablets.
Precautions
Studies show: in 84% of cases, tolperizone causes mild side effects. Serious adverse reactions are almost never observed. There is evidence that the original Midocalm less often leads to side effects, but this remains a controversial issue.
The instructions for use of both drugs state the following possible reactions:
headache;
Muscle weakness;
Decrease in arterial pressure;
Nausea and vomiting;
discomfort and pain in the abdomen;
Allergic reactions: red and itchy skin, bronchospasm, anaphylactic shock.
The risk of side effects increases with increasing the dosage of the drug. In therapeutic doses, unwanted reactions are rare.
Mydocalm and Tolperizone are not used:
In pregnancy and during breastfeeding;
For myasthenia gravis – muscle weakness.
Mydocalm is approved in children – from the age of 3 years. Tolperisone is prescribed only for adults – from 18 years of age.
The instructions for use state that Midocalm does not affect the speed of psychomotor reactions. For Tolperisone it is stated: do not use in patients whose activities require concentration and quick reactions (e.g., when driving a car). Since the active ingredient is the same, practitioners advise caution.
Conclusions
Briefly on the important stuff:
Mydocalm and Tolperizone contain the same active substance and are central muscle relaxants. They are prescribed for increased muscle tone against a background of neurological pathology, in diseases of the musculoskeletal system and other similar conditions.
Midocalm is the original drug, Tolperizone is its analogue (generic). The efficacy of the original has been confirmed by randomized clinical trials. Generic, according to recent data, is not inferior in effectiveness, but more often causes adverse reactions.
Midocalm is approved for use in children over 3 years of age. Tolperisone is prescribed to adults only.
Choosing a myorelaxant, be sure to consult a doctor. There’s a reason these drugs are only available at the pharmacy with a prescription. Uncontrolled use of the drug threatens the development of severe reactions and can seriously undermine health.
