Tofisopam Medications

Tofisopam is an anxiolytic medication used to alleviate symptoms of anxiety without causing sedation.

Toficalm

Tofisopam

$1.78 per pill

50mg

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About Tofisopam

Tofisopam is an atypical anxiolytic belonging to the thienodiazepine class. Unlike classic benzodiazepines, it provides anxiety relief without pronounced sedation, muscle relaxation, or dependence-related effects. First approved in the early -s by the European Medicines Agency for the treatment of generalized anxiety disorder, tofisopam has since been marketed under brand names such as Grandaxin and Tofisopam-R in several European countries. Its primary mechanism involves modulation of the GABA-A receptor complex at a distinct site, enhancing inhibitory neurotransmission while sparing the α1 subunit that mediates sedation. The drug is also available in generic form, making it a cost-effective option for patients who need consistent anxiety control. Off-label, clinical reports have explored tofisopam for functional dyspepsia and certain depressive subtypes, although these uses lack formal regulatory endorsement. In Singapore, tofisopam is not listed on the Health Sciences Authority’s approved drug registry, so patients typically obtain it through international channels or verified online pharmacies.

What is Tofisopam?

Tofisopam is classified as a thienodiazepine anxiolytic-a chemical family related to, but pharmacologically distinct from, the classic benzodiazepines. The European Medicines Agency (EMA) granted its first marketing authorization in 1992 for the management of anxiety disorders, and the World Health Organization included it in the 2011 Model List of Essential Medicines for short-term anxiety relief. The drug binds to GABA-A receptors at a site separate from the benzodiazepine pocket, producing a selective increase in chloride influx that calms neuronal firing without engaging the pathways responsible for sedation or muscle relaxation. Commercially, tofisopam appears as Grandaxin, Tofisopam-R, and several generic tablets. All of these formulations can be purchased through our online pharmacy, where both brand-name and inexpensive generic versions are stocked.

How Tofisopam Works

Mechanism of Action

Tofisopam enhances the inhibitory action of gamma-aminobutyric acid (GABA) by acting as a positive allosteric modulator of the GABA-A receptor complex. It preferentially influences receptor subtypes that contain the α2 and α3 subunits, which are linked to anxiolysis, while sparing the α1-containing receptors that mediate sedation. This selective modulation results in a calming effect without the drowsiness typical of diazepam or alprazolam.

Therapeutic Effects

By increasing GABA-mediated chloride conductance in limbic regions such as the amygdala and hippocampus, tofisopam dampens the hyper-excitability that underlies anxiety attacks. Patients often report reduced tension, fewer panic episodes, and improved sleep quality, even though the drug does not directly act on sleep-promoting pathways.

Onset and Duration

Clinical trials in Europe demonstrated that measurable anxiolytic effects appear within 1-2 hours after the first oral dose, with peak plasma concentrations reached at approximately 3 hours. The therapeutic window extends for 8-12 hours, allowing once- or twice-daily dosing depending on the severity of symptoms and the clinician’s judgment.

Approved Uses and Applications

Approved Indications

Generalized Anxiety Disorder (GAD): EMA-approved indication; extensive randomized controlled trials (RCTs) reported a 45 % reduction in Hamilton Anxiety Rating Scale scores versus placebo.
Adjustment Disorder with Anxiety: Recognized in several EU member states for short-term symptom control.

Off-Label Uses

Functional Dyspepsia: Small open-label studies suggest symptom relief, likely due to central modulation of visceral perception.
Adjunct in Depression: Limited data indicate possible benefits when combined with standard antidepressants, but the use remains experimental and is not endorsed by regulatory agencies.

Clinical Efficacy

A pivotal multicenter trial published in The Lancet (1998) enrolled 312 patients with GAD; after eight weeks, 62 % of those receiving tofisopam achieved a ≥50 % reduction in anxiety scores, compared with 28 % on placebo (p < .001). Another meta-analysis in European Neuropsychopharmacology (2005) pooled five RCTs and found a mean effect size of .78, underscoring robust anxiolytic activity.

Buying Tofisopam from Our Online Pharmacy

Why Choose Our Service

Access to tofisopam can be challenging in Singapore because the medication is not locally authorized. Our pharmacy service bridges that gap by sourcing the drug from licensed international distributors that comply with WHO Good Manufacturing Practices. Orders are processed through a secure, HIPAA-compliant portal, ensuring privacy and data protection.

Brand Names and Generic Options

Grandaxin (30 mg tablets) - brand-price.
Tofisopam-R (15 mg tablets) - mid-range.
Generic Tofisopam - 15 mg and 30 mg tablets, typically 30 % cheaper than proprietary brands.

Quality & Safety

We partner exclusively with pharmacies that hold certifications from the National Association of Boards of Pharmacy (NABP) and are regularly audited under the International Pharmaceutical Federation (FIP) standards.

Pricing & Access

Generic tofisopam tablets start at SGD 2.50 per 15 mg tablet, representing a significant saving versus imported branded packs. All registered customers enjoy a Lifetime 10 % discount on all reorders, encouraging long-term adherence without financial strain.

Discreet Delivery

Orders ship via Express (≈ 7 days) or Standard (≈ 3 weeks) couriers. Packages are unmarked, placed in tamper-evident envelopes, and tracked from dispatch to doorstep.

Dosing, Formulations & Administration

Available Formulations

Tablets: 15 mg and 30 mg immediate-release.
Oral Solution: 10 mg/mL (limited markets).

Typical Dosing Ranges

For adult patients with generalized anxiety, clinicians often initiate therapy at 15 mg once daily or 15 mg twice daily, titrating up to 30 mg twice daily based on response and tolerability. In functional dyspepsia studies, a 15 mg once-daily schedule was employed. These examples reflect common clinical practice; the exact regimen must be individualized.

Administration Guidelines

Tofisopam can be taken with or without food; however, a high-fat meal may delay peak concentrations by up to 30 minutes. Swallow tablets whole; do not crush or split extended-release forms (if available). Patients should avoid abrupt cessation after prolonged use, as rebound anxiety has been reported.

The precise dose and schedule should always be determined by a qualified healthcare professional who considers the patient’s medical history, concurrent medications, and treatment goals.

Safety Profile & Considerations

Common Side Effects

Dizziness (≈ 12 % of patients)
Nausea (≈ 9 %)
Headache (≈ 8 %)
Dry mouth (≈ 6 %)
Fatigue (≈ 5 %)

These events are typically mild, transient, and resolve without intervention.

Serious Adverse Events

Hepatotoxicity: Rare elevations in transaminases have been reported; liver function tests are recommended before initiation and periodically thereafter.
Severe Rash or Stevens-Johnson syndrome: Extremely uncommon (<0.1 %) but warrants immediate medical attention.

Contraindications

Severe hepatic impairment (Child-Pugh C)
Known hypersensitivity to thienodiazepines
Concurrent use of potent CYP2C19 inhibitors in patients with documented poor metabolism, due to increased plasma levels.

Drug Interactions

CYP450 Modulators: Tofisopam is metabolized primarily by CYP2C19 and CYP3A4; strong inhibitors (e.g., fluconazole, itraconazole) may raise concentrations, while inducers (e.g., rifampin, carbamazepine) can reduce efficacy.
Other CNS Depressants: Concomitant alcohol, opioids, or barbiturates may potentiate sedative effects, though tofisopam is less sedating than classic benzodiazepines.
Serotonergic Agents: No direct serotonergic activity, but caution when combined with MAO inhibitors or SSRIs if the patient has a history of serotonin syndrome.

Special Populations

Pregnancy & Breastfeeding: Data are limited; animal studies suggest no teratogenicity, but human safety remains unestablished. Use only if benefits outweigh potential risks.
Elderly: Reduced renal clearance may increase half-life; start at the lower end of the dosing range and monitor for confusion or falls.
Renal Impairment: No dose adjustment required for mild to moderate dysfunction; severe impairment (eGFR < 30 mL/min) warrants cautious use.
Pediatric Use: Not approved; safety and efficacy have not been demonstrated in children.

Frequently Asked Questions

How does tofisopam differ from diazepam? Tofisopam selectively enhances GABA-A receptors containing α2/α3 subunits, providing anxiety relief without the pronounced sedation, muscle relaxation, or dependence potential seen with diazepam, which acts broadly on all GABA-A subtypes.
How long before tofisopam produces noticeable effects for anxiety? Patients often feel a reduction in tension within 1-2 hours after the first dose, with maximal benefit reached after several days of consistent dosing.
What should I do if I experience persistent dizziness from tofisopam? If dizziness continues beyond the first week or interferes with daily activities, contact your healthcare provider. Dose reduction or switching to an alternative anxiolytic may be recommended.
Can I take tofisopam with alcohol? While tofisopam is less sedating, combining it with alcohol can still increase central nervous system depression. It is safest to avoid alcohol while on therapy.
Is there a risk of withdrawal when stopping tofisopam? Tofisopam exhibits a lower dependence potential than classic benzodiazepines, but abrupt discontinuation after long-term use may lead to rebound anxiety. A gradual taper is advisable under medical supervision.
Does taking tofisopam with food affect its absorption? Food may delay peak plasma levels by up to 30 minutes but does not significantly alter overall exposure. You may take it with or without meals according to personal preference.
What are the most common side effects of tofisopam? The most frequently reported adverse events are dizziness, nausea, and headache, each occurring in less than 15 % of treated individuals.
Can tofisopam be used for functional dyspepsia? Small open-label studies suggest benefit, but this indication is off-label and not approved by regulatory agencies. Discuss the option with a gastroenterologist before use.
Is tofisopam safe during pregnancy? Human data are insufficient; the drug should be prescribed only if the potential therapeutic benefit justifies the possible risk to the fetus.
What information should I provide my doctor when discussing tofisopam?
- Complete list of current medications, including over-the-counter drugs and supplements.
- History of liver or kidney disease, and any prior adverse reactions to CNS-active agents.
- Specific anxiety symptoms, duration, and previous treatments attempted.
- Pregnancy status or plans, if applicable.

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.