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, and to improve sleep.

Grandaxin's main action is its ability to reduce anxiety by affecting 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 as an oral tablet and is usually taken several times a day, depending on individual needs and your doctor's recommendations.

Indications Grandaxin.

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 useful 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 interfere with sleep.
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 migraine.

Release form

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

Pharmacodynamics

1. Anxiolytic action:

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

2. Muscle relaxant 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 action:

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

4. Relatively low level of sedation:

   • Compared to some other benzodiazepines, Grandaxin is generally characterized by a lower level of sedation, which allows patients to maintain clarity of consciousness while using it.

Pharmacokinetics

1. Absorption: Tofisopam is generally 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 the tissues of the body, 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 via hydroxylation and demethylation processes.
4. Excretion: Metabolites and some unchanged tofisopam are excreted from the body, primarily via the kidneys, both as conjugates and unchanged. The half-life of tofisopam is approximately 5-8 hours.
5. Factors affecting pharmacokinetics: Various factors such as age, gender, liver and kidney function may influence 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 lower and is determined by the doctor according to their weight and age.

2. Directions for use:

   • 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 Grandaxin administration 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 treatment should be done gradually under medical supervision to avoid possible withdrawal symptoms.

Use Grandaxin. during pregnancy

Use of Grandaxin (Tofisopam) during pregnancy may potentially pose risks to fetal development, particularly in the first trimester when major organs and systems are being formed. There is limited data on the safety of this drug during pregnancy. However, a study conducted in Hungary did not find significant risks of congenital anomalies with the use of Tofisopam during pregnancy. The study did not find statistically significant differences in the incidence of birth defects between the 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, Grandaxin should only be used during pregnancy for strict indications and under close medical supervision.

Contraindications

1. Hypersensitivity: People with 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 failure: Patients with severe liver dysfunction 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 be carried out only on the recommendation of a doctor.
5. Childhood: 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 angle-chamber glaucoma: The use of Grandaxin may be contraindicated in patients with acute angle-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 developing side effects.

Side effects Grandaxin.

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

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

Overdose

1. Central Depression: 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 effects of Grandaxin overdose is respiratory depression, in which breathing becomes shallow, slow, or absent. This can lead to hypoxia and serious complications.
3. Hypotension: Overdose may cause a drop in blood pressure, which may lead to dizziness, loss of consciousness, and even collapse.
4. Muscle weakness and ataxia: Overdose may result in increased muscle relaxant effects of the drug, resulting in muscle weakness, ataxia (impaired coordination of movements) and loss of body control.
5. Coma: In severe cases of overdose, a coma, a state of unconsciousness from which a person may not awaken without medical attention, may develop.

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 sluggish reactions.

2. Medicines that affect the cardiovascular system:

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

3. Drugs metabolized via the cytochrome P450 system:

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

4. Drugs that affect the pH of the gastrointestinal tract:

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

5. Drugs that affect liver and kidney function:

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