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Disulfiram | CAS No: 97-77-8 | GMP-certified suppliers
A medication that supports chronic alcoholism management by helping maintain abstinence and providing reliable therapeutic value for alcohol dependence programs in key North American markets.
Therapeutic categories
Primary indications
- For the treatment and management of chronic alcoholism
Product Snapshot
- Disulfiram is an oral small‑molecule product supplied mainly as tablets, including soluble and effervescent forms
- It is used for the management of chronic alcoholism in long-term treatment programs
- It is an approved API in the United States and Canada
Clinical Overview
Pharmacologically, disulfiram exerts its primary effect through irreversible inhibition of aldehyde dehydrogenase. This blocks the second step of ethanol metabolism and can elevate circulating acetaldehyde concentrations five- to tenfold compared with drinking alone. Disulfiram does not accelerate ethanol clearance. Sensitivity to alcohol typically increases with continued therapy rather than diminishing, indicating absence of tolerance to its pharmacodynamic action. Disulfiram also exhibits competitive binding to the peripheral benzodiazepine receptor, although the clinical relevance of this interaction for alcohol withdrawal symptoms remains insufficiently characterized.
Absorption and metabolic disposition vary, with biotransformation producing diethyldithiocarbamate and downstream sulfur-containing metabolites. These compounds can interact with cytochrome P450 pathways, notably CYP2E1 inhibition and CYP3A substrate behavior. Disulfiram and its metabolites have been associated with potential QTc prolongation and may lower seizure threshold. Use in the presence of hepatic dysfunction or concurrent hepatotoxic drugs warrants caution due to the risk of hepatic injury. Additional considerations include interactions with antiparasitic and insecticidal agents derived from related thiocarbamate chemistry, although clinical relevance varies by formulation.
Disulfiram is marketed under several long-established prescription brands for alcohol dependence treatment. For API procurement, suppliers should provide consistent control of thiuram disulfide content, impurity profiling aligned with pharmacopeial specifications, and validated stability data to support formulation and regulatory submissions.
Identification & chemistry
| Generic name | Disulfiram |
|---|---|
| Molecule type | Small molecule |
| CAS | 97-77-8 |
| UNII | TR3MLJ1UAI |
| DrugBank ID | DB00822 |
Pharmacology
| Summary | Disulfiram irreversibly inhibits mitochondrial aldehyde dehydrogenase, causing acetaldehyde accumulation during ethanol metabolism and producing aversive physiologic effects that deter alcohol consumption. It also inhibits dopamine beta‑hydroxylase and can bind peripheral benzodiazepine receptors, though the clinical relevance of these actions is unclear. The drug’s pharmacodynamic profile centers on creating heightened sensitivity to ethanol without affecting its overall elimination rate. |
|---|---|
| Mechanism of action | Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake causing an accumulation of acetaldehyde in the blood producing highly unpleasant symptoms. Disulfiram blocks the oxidation of alcohol through its irreversible inactivation of aldehyde dehydrogenase, which acts in the second step of ethanol utilization. In addition, disulfiram competitively binds and inhibits the peripheral benzodiazepine receptor, which may indicate some value in the treatment of the symptoms of alcohol withdrawal, however this activity has not been extensively studied. |
| Pharmacodynamics | Disulfiram produces a sensitivity to alcohol which results in a highly unpleasant reaction when the patient under treatment ingests even small amounts of alcohol. Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake, the concentration of acetaldehyde occurring in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. Accumulation of acetaldehyde in the blood produces a complex of highly unpleasant symptoms referred to hereinafter as the disulfiram-alcohol reaction. This reaction, which is proportional to the dosage of both disulfiram and alcohol, will persist as long as alcohol is being metabolized. Disulfiram does not appear to influence the rate of alcohol elimination from the body. Prolonged administration of disulfiram does not produce tolerance; the longer a patient remains on therapy, the more exquisitely sensitive he becomes to alcohol. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine beta-hydroxylase | Humans | inhibitor |
| Aldehyde dehydrogenase, mitochondrial | Humans | inhibitor |
ADME / PK
| Absorption | Disulfiram is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose). |
|---|---|
| Metabolism | Hepatic. |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility, typically formulated as conventional or effervescent tablets using solubility‑enhancing excipients.
- Lipophilic thiuram disulfide structure can exhibit hydrolytic and reductive instability; protect from moisture and reducing environments during manufacture and storage.
- Food does not affect absorption, but formulations must avoid alcohol‑containing excipients due to disulfiram–ethanol reactions.
Regulatory status
| Lifecycle | The API is approaching a mature market phase, with key patent protections either expired or nearing expiry. Products remain available in the US and Canada, supporting continued but largely established market activity. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The originator product is Antabuse, with multiple generic manufacturers now active, indicating that the molecule is long off‑patent and widely available. Current market presence is concentrated in the US and Canada, with no major branded activity noted in the EU. The established generic landscape suggests mature competition and broad supply coverage. |
|---|
Safety
| Toxicity | LD<sub>50</sub>=8.6g/kg (orally in rats). Symptoms of overdose include irritation, slight drowsiness, unpleasant taste, mild GI disturbances, and orthostatic hypotension. |
|---|
- Exhibits low acute oral toxicity in rodents (LD50 ≈ 8
- 6 g/kg), but high‑dose exposure may provoke mucosal irritation and central nervous system depression
- Overexposure can manifest as mild gastrointestinal disturbances and transient orthostatic hypotension
Disulfiram is a type of Substances for alcohol addiction
Pharmaceutical API Subcategory: Substances for Alcohol AddictionSubstances for alcohol addiction are a vital subcategory within the pharmaceutical active pharmaceutical ingredients (APIs) market. These substances play a crucial role in the development of medications and therapies designed to address alcohol addiction, a prevalent and serious health issue worldwide.
APIs for alcohol addiction typically consist of specific chemical compounds that target the neurochemical pathways involved in addiction. These substances act on the central nervous system to modulate brain functions, reducing cravings and withdrawal symptoms associated with alcohol dependence.
Common API substances utilized in the treatment of alcohol addiction include naltrexone, acamprosate, and disulfiram. Naltrexone acts by blocking the brain's opioid receptors, thereby decreasing the pleasurable effects of alcohol consumption and reducing cravings. Acamprosate works by stabilizing the chemical balance in the brain, reducing the distressing symptoms experienced during alcohol withdrawal. Disulfiram, on the other hand, creates an unpleasant reaction when alcohol is consumed, acting as a deterrent for individuals trying to abstain from alcohol.
Pharmaceutical companies and research organizations are continuously exploring innovative API substances and formulations to improve the effectiveness and tolerability of alcohol addiction treatments. The development of new substances often involves rigorous clinical trials to ensure their safety and efficacy.
The market for substances targeting alcohol addiction is driven by the increasing awareness of the detrimental effects of excessive alcohol consumption and the growing demand for effective treatment options. By providing pharmaceutical APIs tailored to this subcategory, manufacturers contribute to combating alcohol addiction and supporting individuals on their journey towards recovery.
Disulfiram (Substances for alcohol addiction), classified under Anti-addiction agents
Anti-addiction agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment and management of various forms of addiction. These agents target the neurochemical pathways in the brain that are involved in addiction and dependence, offering therapeutic interventions to individuals struggling with substance abuse disorders.
One prominent group of anti-addiction agents includes opioid receptor antagonists, such as naltrexone and naloxone. These APIs bind to opioid receptors in the brain, blocking the euphoric effects of opioids and reducing cravings. By doing so, they help individuals overcome opioid addiction and prevent relapse.
Another essential class of anti-addiction agents are nicotine receptor agonists, like varenicline. These APIs target nicotine receptors in the brain, reducing the pleasurable sensations associated with smoking and alleviating nicotine withdrawal symptoms. This aids in smoking cessation efforts and enhances long-term abstinence rates.
Furthermore, anti-addiction agents may also encompass APIs used in the treatment of alcohol addiction, such as disulfiram and acamprosate. Disulfiram inhibits the breakdown of alcohol in the body, leading to unpleasant reactions when alcohol is consumed, thus discouraging its use. Acamprosate, on the other hand, helps normalize brain activity disrupted by chronic alcohol use, reducing cravings and promoting abstinence.
In conclusion, anti-addiction agents are a critical category of pharmaceutical APIs used to combat addiction and substance abuse disorders. By targeting specific neurochemical pathways, these agents provide valuable support in overcoming addiction, preventing relapse, and improving the overall well-being of individuals affected by substance abuse.
Disulfiram API manufacturers & distributors
Compare qualified Disulfiram API suppliers worldwide. We currently have 5 companies offering Disulfiram API, with manufacturing taking place in 5 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Corden Pharma | Producer | Germany | Italy | CoA, GMP, USDMF | 45 products |
| PCI SYNTHESIS | Producer | Unknown | Unknown | CoA, USDMF | 4 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS | 64 products |
| Productos Aditivos SA | Producer | Spain | Spain | CoA, GMP, ISO9001, MSDS, USDMF | 3 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
When sending a request, specify which Disulfiram API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Disulfiram API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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