tofisopam

Action and Spectrum

Actions and Spectrum: 

• Anxiolytic Effects: tofisopam is primarily prescribed to relieve symptoms of anxiety and tension. It acts as an anxiolytic by modulating the brain’s GABA (gamma-aminobutyric acid) receptors, although its mechanism of action differs from traditional benzodiazepines. tofisopam is believed to have anxiolytic effects without causing sedation or significant impairments in cognitive function. It is suitable for individuals needing anxiety relief without the drowsiness associated with other anxiolytic medications. 
• Antispasmodic Effects: tofisopam also has antispasmodic properties, which help relax muscles and relieve muscle tension.  

This makes it worthwhile when muscle spasms or tension contribute to symptoms such as irritable bowel syndrome (IBS) and specific pain syndromes. 

• Cognitive Function: Unlike traditional benzodiazepines, which can impair cognitive function and memory, tofisopam is thought to have a more favorable cognitive profile. It may have fewer adverse effects on memory and cognitive tasks, which can be particularly beneficial for individuals who need anxiety relief while maintaining mental clarity. 
• Lack of Sedation: tofisopam is often favored when sedation is undesirable. It tends to have less sedative effect than many other anxiolytic medications, allowing individuals to remain alert and functional during treatment. 
• Limited Risk of Dependence: While tofisopam is derived from the benzodiazepine class of drugs, it is generally considered to have a lower risk of dependence and withdrawal symptoms than traditional benzodiazepines. However, it is not entirely free from the potential for dependence, and it should still be used cautiously and under medical supervision. 
• Duration of Action: tofisopam has a relatively short duration of action, which means it may need to be taken multiple times daily to maintain its therapeutic effect.

Drug Interaction

Adverse Reaction

Frequency not defined 

Rash 

Epigastric pain 

Nausea 

Extreme liveliness 

Aggressiveness 

Hyperactivity 

Itching 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Acute narrow-angle glaucoma 
• Severe liver impairment  
• Pregnancy  
• Breastfeeding 

Cautions: 

• Renal impairment 
• Elderly patients 
• Substance abuse 
• Driving and operating machinery 
• Drug interactions 

Pregnancy / Lactation

Pregnancy consideration:  

tofisopam is contraindicated during pregnancy. 

Breastfeeding warnings:  

It is unknown whether the drug is excreted in breast milk. 

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

• Anxiolytic Effects: 

tofisopam is primarily used to relieve symptoms of anxiety and tension. It has anxiolytic properties, meaning it can reduce feelings of anxiety and emotional tension. 

• Muscle Relaxation: 

tofisopam also has muscle relaxant properties. It helps in reduction of muscle tension and spasms, making it useful in conditions with muscle-related symptoms, like irritable bowel syndrome (IBS) and certain pain syndromes. 

• Cognitive Effects: 

tofisopam is believed to have a more favorable cognitive profile than traditional benzodiazepines. It is thought to have fewer adverse effects on memory and cognitive function, which can be particularly beneficial for individuals who need anxiety relief while maintaining mental clarity. 

Pharmacodynamics: 

• Sedation and Drowsiness: Unlike many other anxiolytic medications, tofisopam tends to have less sedative effect. It is associated with lower levels of sedation and drowsiness, allowing individuals to remain alert and functional during treatment. 
• Duration of Action: tofisopam has a relatively short duration of action. Its pharmacodynamic effects are not long-lasting, which can require multiple daily dosages to maintain therapeutic benefits. 
• Dependence and Withdrawal: tofisopam has a lower risk of dependence and withdrawal symptoms than traditional benzodiazepines. Its unique pharmacodynamic profile may contribute to this reduced potential for dependence. 
• Individual Variability: Individual responses to tofisopam can vary with any medication. Factors such as age, liver function, concurrent medications, and the specific condition being treated can influence how tofisopam affects different individuals. 

Pharmacokinetics: 

Absorption 

tofisopam is administered orally, typically in tablet form. 

Absorption of tofisopam is relatively rapid, with the drug entering the systemic circulation. 

Distribution 

tofisopam is distributed throughout the body, and its distribution is influenced by factors such as its lipophilicity (affinity for fat tissues), plasma protein binding, and tissue permeability. 

Metabolism 

tofisopam undergoes hepatic metabolism, primarily in the liver. 

It is metabolized into several metabolites, including 2-pyridylacetic acid (2-PAA) and 2-(2-pyridyl) ethanol (2-PE). 

Elimination and Excretion 

tofisopam and its metabolites are primarily eliminated via renal excretion, with the kidneys significantly removing the drug from the body. 

The elimination half-life of tofisopam can vary between individuals but is typically in the range of 2 to 4 hours. This means it takes this amount of time for half of the drug to be cleared from the body. 

Adminstartion

Administration: 

tofisopam is typically administered orally in the form of tablets. The dosing and administration instructions may vary based on the specific brand of tofisopam and your healthcare provider’s recommendations. tofisopam can be taken with or without food, as it is not significantly affected by food intake. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tofisopam 

Pronounced as: to-fi-so-pam 

Why do we use tofisopam? 

tofisopam is primarily used for its anxiolytic (anti-anxiety) and muscle relaxant properties. It is prescribed to address various conditions and symptoms related to anxiety and muscle tension. Here are some common reasons why tofisopam may be used: 

• Anxiety Disorders: tofisopam is primarily prescribed to relieve symptoms of anxiety and tension. It can treat generalized anxiety disorder (GAD) and other anxiety-related disorders. It helps reduce feelings of anxiety, worry, and emotional tension. 
• Muscle Tension and Spasms: tofisopam has muscle relaxant properties. It can help relax muscles and alleviate muscle tension and spasms. This can benefit conditions associated with muscle-related symptoms, such as pain or stiffness. 
• Gastrointestinal Disorders: Some gastrointestinal conditions, such as irritable bowel syndrome (IBS), can be exacerbated by anxiety and stress. tofisopam may help manage anxiety-related gastrointestinal symptoms, such as abdominal pain and discomfort. 
• Adjunct to Physical Therapy: tofisopam may be prescribed as an adjunct to physical therapy or other treatments for musculoskeletal conditions. It can help enhance the effectiveness of physical therapy by reducing muscle tension and promoting relaxation. 
• Preoperative Anxiety: In some cases, tofisopam may alleviate preoperative anxiety and tension in individuals undergoing surgery. It can help reduce preoperative apprehension. 
• Cognitive Function: tofisopam is believed to have a more favorable cognitive profile than traditional benzodiazepines. It may have fewer adverse effects on memory and cognitive tasks, making it suitable for individuals who need anxiety relief while maintaining mental clarity. 
• Limited Sedation: tofisopam has less sedative effect than other anxiolytic medications. This allows individuals to remain alert and functional during treatment.