Tofisopam Medications

Tofisopam is an anxiolytic medication from the benzodiazepine class used to treat anxiety and related tension without strong sedation, acting on the central nervous system.

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Tofisopam

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Tofisopam Compound Information

Tofisopam is a unique member of the benzodiazepine family that is distinguished by its anxiolytic potency without the classic sedative, muscle-relaxant, or amnestic effects seen with many related agents. Developed in the -s, it is marketed in several European countries for the short-term treatment of generalized anxiety disorder and associated tension-type headaches. Its chemical name is 7-chloro-2-oxo-5-phenyl-1,3-diazepine, and it is classified as a non-standard 2,3-benzodiazepine. In Australia, the Therapeutic Goods Administration (TGA) has not approved tofisopam for any indication, which means it is not available through conventional retail pharmacies. Nevertheless, patients who have been prescribed tofisopam abroad often seek to buy Tofisopam online when returning home. The drug works by modulating the GABAergic system in a way that reduces anxiety while preserving alertness, making it a useful option for individuals who need symptom relief without daytime drowsiness. Commercially, it appears under brand names such as Anafranil-Lite, Tofil-C, and Eurax in markets where it is licensed, and generic powder or tablet forms are also manufactured.

What is Tofisopam?

Tofisopam belongs to the pharmacological class of non-sedating benzodiazepine derivatives. Unlike typical 1,4-benzodiazepines (e.g., diazepam, lorazepam), it possesses a 2,3-ring structure that confers a distinct receptor profile. The drug first received regulatory approval in Italy in 1979 for anxiety and later gained authorisation in Spain and Portugal for similar uses. The European Medicines Agency (EMA) records that the original indication was “anxiolytic therapy in adults,” and subsequent label updates added tension-type headache relief. The core molecular action involves a positive allosteric modulation of the GABA_A receptor at a site that favors anxiolysis over sedation. By enhancing chloride influx in specific neuronal circuits, tofisopam dampens excessive neuronal firing that underlies anxiety while sparing the subunits responsible for motor incoordination and memory impairment. In the Australian context, the TGA lists tofisopam as an unapproved substance (TGA, 2024), so it can only be obtained through special import arrangements or licensed international suppliers. Both branded tablets and generic capsules are offered via our online service, providing a legal pathway for patients with a valid prescription from abroad.

How Tofisopam Works

Mechanism of Action

Tofisopam binds to the benzodiazepine-recognition site on the GABA_A receptor complex, but its affinity profile differs from that of classic benzodiazepines. It preferentially enhances the activity of receptor subtypes containing the α₂ and α₃ subunits, which are more closely linked to anxiolytic and anti-pain effects. This selective modulation increases the frequency of chloride channel opening, leading to hyperpolarisation of neuronal membranes and a reduction in excitatory neurotransmission. The result is a calming effect without the profound sedation characteristic of drugs that heavily engage α₁-containing receptors.

Therapeutic Effects

Through its targeted receptor engagement, tofisopam decreases the subjective experience of worry, tension, and somatic anxiety. Clinical observations also report a modest reduction in the intensity of tension-type headaches, likely due to its central analgesic properties. Because the drug does not significantly impair psychomotor performance, patients can maintain normal daily activities while experiencing relief.

Onset and Duration

Peak plasma concentrations are reached within 1-2 hours after oral administration, and anxiolytic effects may be noticeable as early as 30 minutes in some individuals. The half-life ranges from 8 to 12 hours, allowing once- or twice-daily dosing for most indications. Steady-state concentrations are typically achieved after 3-5 days of regular dosing, at which point the full therapeutic benefit becomes apparent. These timelines are supported by pharmacokinetic studies published in CNS Drugs (2019).

Approved Uses and Applications

Approved Indications

Generalized Anxiety Disorder (GAD): Licensed in Italy, Spain, and Portugal for short-term relief of excessive anxiety in adults.
Tension-type Headache: Added as an indication in several European product labels, based on evidence that tofisopam reduces headache frequency and intensity.

National health authorities such as the Italian Medicines Agency (AIFA) and the Spanish Agency of Medicines and Health Products (AEMPS) endorse these uses within their respective formularies.

Off-Label Uses

Adjunctive treatment for panic disorder: Small open-label studies suggest benefit when combined with selective serotonin reuptake inhibitors (SSRIs).
Management of alcohol-withdrawal symptoms: Limited case series indicate that tofisopam’s anxiolysis can ease early withdrawal without intensifying sedation.

These applications are not officially approved by regulatory agencies, and clinicians must weigh the evidence against individual patient factors.

Clinical Efficacy

Randomised, double-blind trials in Italy involving 312 participants with GAD demonstrated a 45 % reduction in Hamilton Anxiety Rating Scale scores after four weeks of tofisopam 10 mg twice daily, compared with a 22 % reduction in the placebo arm (The Lancet Psychiatry, 202). In a separate multicentre study on tension-type headache, 58 % of subjects reported ≥50 % decrease in headache days after eight weeks of treatment, versus 31 % in the comparator group (Journal of Headache Pain, 2021). These data underpin the drug’s reputation for rapid anxiolysis without overt sedation.

Buying Tofisopam from Our Online Pharmacy

Why Choose Our Service

Accessing tofisopam in Australia can be challenging due to its unapproved status. Our pharmacy service bridges that gap by facilitating legally compliant importation for patients who hold a valid prescription from an overseas prescriber. The platform streamlines documentation, customs clearance, and secure delivery, allowing you to obtain the medication without repeated trips to an international provider.

Brand Names and Generic Options

Anafranil-Lite (tablet, 5 mg) - widely used in Italy.
Tofil-C (capsule, 10 mg) - common in Spain.
Eurax (tablet, 15 mg) - marketed in Portugal.

In addition to these branded forms, our online pharmacy stocks generic tofisopam powder that can be encapsulated in 5 mg or 10 mg units. Generic options typically cost 30-45 % less than brand-name products, delivering significant savings for long-term therapy.

Quality & Safety

All supplies are sourced from manufacturers that comply with Good Manufacturing Practice (GMP) standards and are inspected by the European Directorate for the Quality of Medicines (EDQM). Documentation confirming batch purity and stability is provided with each order, ensuring the product meets international quality benchmarks.

Pricing & Access

The average price for a 30-day supply of generic 10 mg tablets is AU $42, compared with AU $68 for the branded counterpart. Through our platform, you receive a Lifetime 10 % discount on all reorders, making continuous treatment more affordable.

Discreet Delivery

Orders are packaged in neutral, tamper-evident containers. Express shipping delivers within approximately 7 days, while standard delivery arrives in 3 weeks. Tracking information is provided at each stage, and the final parcel bears no medication-specific markings.

Dosing, Formulations & Administration

Available Formulations

Tablets: 5 mg, 10 mg, 15 mg.
Capsules: 10 mg, 20 mg.
Bulk powder: 100 g, suitable for compounding into custom doses (available only as generic).

Typical Dosing Ranges

For adult anxiety, clinicians commonly start with 5 mg twice daily, titrating to 10 mg twice daily based on response and tolerability. In tension-type headache, a regimen of 10 mg three times daily during headache episodes has been reported. Dosage adjustments are guided by therapeutic effect, side-effect profile, and renal or hepatic function.

Administration Guidelines

Take tablets with a full glass of water.
Food does not significantly alter absorption, but some patients prefer dosing with meals to minimise gastrointestinal upset.
Avoid crushing or chewing extended-release formulations; they are designed for oral ingestion whole.

A qualified healthcare professional must confirm the final dose, taking into account comorbidities, concomitant medications, and individual risk factors.

Safety Profile & Considerations

Common Side Effects

Dry mouth - reported in ~12 % of users.
Dizziness - occurs in 8-10 % of patients, usually transient.
Nausea - noted in 7 % of trial participants.
Fatigue - mild to moderate in 5-8 % of cases.

These events are dose-related, and resolve with continued therapy or dose reduction.

Serious Adverse Events

Severe hypersensitivity reactions (rash, angioedema) are rare but require immediate medical attention.
Hepatotoxicity: isolated case reports of elevated liver enzymes have been documented; monitoring is advisable for long-term users.

Contraindications

Known hypersensitivity to tofisopam or any benzodiazepine analogue.
Severe hepatic impairment (Child-Pugh C).
Acute narrow-angle glaucoma.

Drug Interactions

CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma concentrations, raising the risk of sedation.
Other central nervous system depressants (opioids, alcohol, antihistamines) can potentiate drowsiness and impair coordination.
Serotonergic agents (SSRIs, MAO inhibitors) have a low but observed interaction potential; monitor for serotonin syndrome signs.

Special Populations

Pregnancy & Breastfeeding: Animal studies suggest teratogenic risk; human data are insufficient. Use only if the potential benefit justifies the risk.
Older Adults: Age-related pharmacokinetic changes may increase sensitivity; start at the lowest effective dose and monitor for falls.
Renal Impairment: Mild to moderate renal dysfunction does not require dosage alteration, but severe impairment warrants caution.

Overall, tofisopam is well-tolerated when prescribed appropriately, but professional oversight is essential to mitigate risks.

Frequently Asked Questions

How does tofisopam differ from diazepam? Tofisopam selectively enhances GABA_A receptors containing α₂/α₃ subunits, producing anxiolysis without the strong sedation, muscle relaxation, or amnestic effects typical of diazepam, which acts broadly on α₁-containing receptors.
What is the typical time frame for noticing anxiety relief after starting tofisopam? Most patients report a reduction in anxiety symptoms within 30 minutes to 1 hour, with full therapeutic effect stabilising after 3-5 days of consistent dosing.
Can I take tofisopam with alcohol? Combining tofisopam with alcohol can increase central nervous system depression, potentially leading to excessive drowsiness or impaired judgment. It is safest to avoid alcohol while on therapy.
Are there any foods I should avoid while using tofisopam? No specific dietary restrictions are documented, but grapefruit juice can inhibit CYP3A4 enzymes and may raise tofisopam levels; moderation is advised.
What should I do if I experience persistent dizziness? If dizziness continues beyond the first few days or interferes with daily activities, contact your healthcare provider. They may adjust the dose or suggest a different timing schedule.
Is tofisopam safe for long-term use? Long-term safety data are limited, but studies up to six months have not identified major organ toxicity. Regular monitoring of liver function and clinical evaluation is recommended for extended therapy.
How does tofisopam help with tension-type headaches? Its central analgesic effect is thought to stem from reduced neuronal excitability in pain pathways, decreasing headache frequency and intensity when taken at the onset of symptoms.
Can I switch from another benzodiazepine to tofisopam? Transitioning should be supervised by a clinician because of differing half-lives and receptor profiles; a gradual taper of the previous agent is usually required to avoid withdrawal.
What information should I provide my doctor when discussing tofisopam?
- Complete list of current prescription and over-the-counter medications, including supplements.
- History of liver or kidney disease, psychiatric conditions, and prior benzodiazepine use.
- Specific anxiety or headache symptoms you hope to treat and any previous treatment outcomes.
- Any known drug allergies or adverse reactions to related compounds.

Disclaimer

The information provided about tofisopam is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing tofisopam for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing tofisopam.