brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM) Benzodiazepine ( 2,3-benzodiazepine, unlike traditional 1,4-benzodiazepines)

Nextril commonly prescribed for

(Bold for FDA approved)

How Nextril works

• Binds to benzodiazepine receptors on the GABA-A ligand-gated chloride channel complex

• Modulates receptor activity without enhancing GABAergic transmission

• Reduces excessive neuronal activity in the limbic system, including the amygdala, providing anxiolytic effects

• Minimal sedative effects due to selective modulation rather than broad GABA potentiation.

How long until Nextril works

• Provides relief within a few hours of the first dose for anxiety symptoms

• Maximal therapeutic benefit may be achieved within a few days to a week with regular use

Notable Side Effects

• Drowsiness, fatigue, dizziness

• Headache

• Dry mouth

• Mild gastrointestinal disturbances (nausea, abdominal discomfort)

• Muscle weakness

• Hypersensitivity reactions (rash, itching, swelling) (Rare)

• Risk of dependence and withdrawal symptoms with prolonged use (Rare)

• Cognitive impairment (memory problems, concentration issues) (Rare)

Life Threatening Side Effects

• Severe allergic reactions (anaphylaxis)

• Respiratory depression when combined with other CNS depressants

• Hepatic or renal dysfunction (in patients with pre-existing conditions)

weight gain

unusual

sedation

not usual

What to do about Nextril side effects

• Wait

• Wait

• Wait

• Lower the dose

• Take largest dose at bedtime to avoid sedative effects during the day

• Switch to another agent

usual dosage range

• Generalized Anxiety Disorder (GAD): 50-100 mg/day, typically in divided doses. Start at a lower dose (50 mg) and increase as needed based on individual response, with a maximum of 100 mg/day. Panic Disorder: 50-100 mg/day, with the dose adjusted according to response. Usually taken once daily or divided into two doses.

Dosage Forms

• Tablet 50mg, 100mg

long term use

• ofisopam may maintain its efficacy for anxiety and related conditions over time, but response can vary between patients. Dose adjustments may be needed based on therapeutic outcomes.

• While the risk of dependence with tofisopam is lower compared to benzodiazepines, prolonged use, especially beyond 12 weeks, may still increase the risk, particularly in patients with a history of substance abuse.

habit forming

• The risk of dependence and tolerance is lower compared to traditional benzodiazepines, long-term use may still lead to psychological dependence, especially in patients with a history of substance abuse.

Renal Impairment

• Dose should be reduced

Hepatic Impairment

• Dose should be reduced

Cardiac Impairment

• Can be used to treat anxiety associated with acute myocardial infarction

Elderly

• Should receive lower doses and be monitored

Children and Adolescents

• Safety and efficacy in children and adolescents are not well-established; lower doses are recommended if used, and close monitoring is necessary.

• Limited data on its use in children and adolescents; not commonly prescribed for this population.

• Long-term effects of tofisopam in children and adolescents are unknown.

Pregnancy

• Possible increased risk of birth defects when benzodiazepines, including tofisopam, are taken during pregnancy.

• Tofisopam is not generally recommended as treatment for anxiety during pregnancy, particularly during the first trimester, due to potential risks.

• Drug should be tapered if discontinued to minimize withdrawal effects.

• Infants whose mothers received tofisopam late in pregnancy may experience withdrawal effects or neonatal flaccidity.

Breast Feeding

• Tofisopam may pass into breast milk in small amounts.

• It is recommended to either discontinue the drug or use bottle feeding during treatment.

• Potential effects on the nursing infant include feeding difficulties, sedation, and weight loss; therefore, close monitoring is advised if breastfeeding is continued.