Grandaxin

Grandaxin, also known as Tofisopam, is a drug that belongs to the group of benzodiazepines, used in medicine as an anxiolytic and muscle relaxant. It is used to reduce anxiety and muscle tension, as well as improve sleep.

The main effect of Grandaxin is its ability to reduce anxiety by influencing chemical transmissions in the brain, which leads to a decrease in the excitability of the nervous system. It also has a muscle relaxant effect, helping to relax muscles and reduce muscle tension.

Grandaxin is often prescribed in cases of anxiety disorders, panic attacks accompanied by severe anxiety, as well as myofascial pain syndrome and other conditions accompanied by muscle tension and pain.

It is available in oral tablet form and is usually taken several times a day, depending on individual needs and doctor's recommendations.

Indications Grandaxina

1. Anxiety Disorders: Grandaxin is often prescribed to reduce anxiety symptoms in patients with a variety of anxiety disorders, including generalized anxiety disorder, panic disorder, and social phobic disorder.
2. Muscle tension: The drug is used to relieve muscle tension and spasms. This is especially helpful for patients with myofascial pain syndrome or other conditions characterized by muscle tension.
3. Insomnia: Grandaxin may help improve sleep quality in patients with anxiety disorders or other mental health problems that may make it difficult to fall asleep.
4. Associated symptoms in neurological diseases: Grandaxin is sometimes used to reduce anxiety and muscle tension in patients with neurological diseases such as Parkinson's disease or migraines.

Release form

Grandaxin is usually available in the form of tablets for oral administration. Tablets may have different dosages depending on medical practice and manufacturer's instructions.

Pharmacodynamics

1. Anxiolytic effect:

   • Grandaxin has an effect on anxiolytic receptors in the central nervous system, such as benzodiazepine type A (GABA-A) receptors.
   • This leads to an increased inhibitory effect of the neurotransmitter gamma-aminobutyric acid (GABA) on the brain, which helps reduce anxiety.

2. Miorelaxant effect:

   • Grandaxin also has a muscle relaxant effect, which manifests itself in a decrease in muscle tension.
   • This effect may be useful in treating conditions involving muscle tension or spasms.

3. Anticonvulsant effect:

   • Unlike some other benzodiazepines, Grandaxin has a pronounced anticonvulsant effect.
   • It may be useful in treating various forms of seizures and epilepsy.

4. Comparatively low level of sedation:

   • Compared to some other benzodiazepines, Grandaxin usually has a lower level of sedation, which allows patients to remain lucid when using it.

Pharmacokinetics

1. Absorption: Tofisopam is usually well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are usually reached 1-2 hours after administration.
2. Distribution: It is well distributed in body tissues, including the central nervous system, where it exerts its pharmacological effects.
3. Metabolism: Tofisopam is metabolized in the liver to form active metabolites. The main metabolite, 7-hydroxy-tofisopam, has pharmacological activity. Metabolism occurs through the processes of hydroxylation and demethylation.
4. Excretion: Metabolites and part of the unchanged tofisopam are excreted from the body, mainly through the kidneys, both in the form of conjugates and unchanged. The half-life of tofisopam is about 5-8 hours.
5. Factors influencing pharmacokinetics: Various factors, such as age, gender, functional state of the liver and kidneys, can affect the pharmacokinetics of tofisopam and its metabolites.
6. Interactions: Grandaxin may interact with other drugs, especially with other centrally acting agents and alcohol. Concomitant use of Grandaxin with alcohol and other central nervous system depressants should be avoided, as this may lead to increased sedative effects.

Dosing and administration

1. Dosage:

   • The usual starting dose of Grandaxin for adults is 50-100 mg per day, divided into 2-3 doses.
   • The maximum daily dose is usually 300 mg.
   • The dosage for children and adolescents may be less and is determined by the doctor in accordance with their weight and age.

2. Method of application:

   • Grandaxin tablets should be taken orally, i.e. Through the mouth, with a small amount of water.
   • It is better to take the tablets with food to reduce possible side effects on the stomach.

3. Duration of treatment:

   • The duration of taking Grandaxin is determined by the doctor and depends on the nature and severity of the symptoms, as well as the patient’s response to treatment.
   • Discontinuation of use should be carried out gradually under the supervision of a physician to avoid the possible occurrence of withdrawal syndrome.

Use Grandaxina during pregnancy

The use of Grandaxin (Tofizopam) during pregnancy may potentially carry risks for the development of the fetus, especially in the first trimester, when the main organs and systems are formed. There is limited data on the safety of using this drug during pregnancy. However, a study conducted in Hungary found no significant risks of congenital anomalies when using Tofizopam during pregnancy. The study found no statistically significant differences in the incidence of birth defects between groups receiving and not receiving benzodiazepines during the critical period for the development of major congenital anomalies (Erős et al., 2002).

However, due to insufficient data and potential risks, the use of Grandaxin during pregnancy should only occur under strict indications and under close medical supervision.

Contraindications

1. Hypersensitivity: People with a known hypersensitivity to tofisopam or to any of the ingredients of the drug should not use Grandaxin.
2. Myasthenia gravis: Grandaxin may increase muscle weakness in patients with myasthenia gravis, so its use in this case may be contraindicated.
3. Liver impairment: Patients with severely impaired liver function should use Grandaxin with caution and under medical supervision, as it is metabolized in the liver.
4. Pregnancy and breastfeeding: Data on the safety of Grandaxin during pregnancy and breastfeeding are limited, so its use during this period should only be carried out on the recommendation of a doctor.
5. Children: The safety and effectiveness of Grandaxin in children have not been sufficiently studied, so its use in children may require consultation with a doctor.
6. Acute carbon chamber glaucoma: The use of Grandaxin may be contraindicated in patients with acute carbon chamber glaucoma due to a possible increase in intraocular pressure.
7. Alcohol intake: The use of Grandaxin in combination with alcohol or other centrally acting drugs, such as sedatives, may increase central nervous system depression and the risk of side effects.

Side effects Grandaxina

• The most commonly reported side effects are moderate to mild symptoms such as nausea and headache. These symptoms usually occur with high doses and resolve on their own after dose reduction (Szegö et al., 1993).
• Grandaxin has low toxicity and causes mild side effects, which makes it preferable for long-term use compared to other tranquilizers (Szegö et al., 1993).
• In some cases, allergic reactions are possible, which require discontinuation of the drug and seeking medical help.

It is also important to note that Grandaxin does not cause physical or mental dependence, making it a safe option for long-term treatment of anxiety disorders.

Overdose

1. Central suppression: Because Grandaxin acts as a central depressant, overdose may result in significant central nervous system depression, which may manifest as profound sedation, drowsiness, syncope, or coma.
2. Respiratory depression: One of the most dangerous consequences of an overdose of Grandaxin is respiratory depression, in which breathing becomes shallow, slow or completely absent. This can lead to hypoxia and serious complications.
3. Hypotension: Overdose can cause a decrease in blood pressure, which can lead to dizziness, loss of consciousness and even collapse.
4. Muscle weakness and ataxia: Overdose can lead to increased muscle relaxant effects of the drug, which manifests itself in muscle weakness, ataxia (impaired coordination of movements) and loss of body control.
5. Coma: In severe cases of overdose, coma may develop, a state of loss of consciousness from which the person may not awaken without medical attention.

Interactions with other drugs

1. Alcohol and other centrally acting drugs:

   • Interaction with alcohol and other drugs that depress the central nervous system, such as hypnotics, sedatives, or antidepressants, may result in increased sedation and an increased risk of unwanted side effects such as drowsiness and inhibition.

2. Medicines affecting the cardiovascular system:

   • Grandaxin may enhance the cardiovascular depressant effects of other drugs, such as antihypertensive drugs or drugs for the treatment of arrhythmias.

3. Drugs metabolized through the cytochrome P450 system:

   • Grandaxin can affect the activity of enzymes of the cytochrome P450 system, which can change the metabolism of other drugs and lead to changes in their concentration in the blood. For example, this may be important when using Grandaxin simultaneously with antidepressants, antiarrhythmic drugs or antiepileptic drugs.

4. Drugs affecting the pH of the gastrointestinal tract:

   • Medicines that change the acidity of gastric contents, such as antacids, may affect the rate and completeness of Grandaxin absorption from the gastrointestinal tract.

5. Drugs affecting liver and kidney function:

   • Since Grandaxin is metabolized in the liver, medications that affect the function of this organ may alter its metabolic pathway and excretion from the body.