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Trazodone | CAS No: 19794-93-5 | GMP-certified suppliers
A medication that treats major depressive disorder and is used off-label for anxiety, insomnia, alcohol dependence, and various neuropsychiatric conditions with broad neurotransmitter effects.
Therapeutic categories
Primary indications
- Trazodone is indicated for the treatment of major depressive disorder (MDD)
- It has been used off-label for adjunct therapy in alcohol dependence, and off-label to treat anxiety and insomnia
- It may also be used off-label to treat symptoms of dementia, Alzheimer’s disease, schizophrenia, eating disorders, and fibromyalgia due to its effects on various neurotransmitter receptors
Product Snapshot
- Trazodone is available predominantly as oral tablets and capsules, with formulations including immediate release, extended release, film-coated, and injectable solutions
- It is primarily used for the treatment of major depressive disorder, with off-label applications in alcohol dependence adjunct therapy, anxiety, insomnia, and other neuropsychiatric conditions
- Trazodone holds approved status in key regulatory markets including the US and Canada
Clinical Overview
Pharmacodynamically, trazodone exerts antidepressant effects by modulating serotonergic neurotransmission and is noted for sedative properties that benefit insomnia associated with depression. It acts by inhibiting serotonin reuptake while antagonizing several receptor subtypes, including serotonin 5-HT2A/2C, histamine H1, and alpha-1 adrenergic receptors. This multimodal receptor activity differentiates it from other antidepressants that typically target a narrower receptor spectrum. Notably, trazodone may prolong the cardiac QT interval, and caution is warranted in patients with cardiovascular risks. Central nervous system depressant effects can impair cognition, alertness, and memory, especially in elderly patients.
The mechanism of action involves serotonin reuptake inhibition coupled with receptor antagonism at 5-HT1A, 5-HT1C, 5-HT2A/2C, histaminergic, and alpha-1 adrenergic receptors, contributing to its clinical efficacy and side effect profile. It is metabolized primarily by cytochrome P450 enzymes CYP3A4 and CYP2D6, serving as both a substrate and weak inhibitor of CYP2D6, which may lead to drug-drug interactions. Pharmacokinetic details include moderate bioavailability and distribution throughout the central nervous system consistent with its therapeutic targets.
Safety considerations for trazodone include the risk of priapism, a rare but serious adverse event requiring urgent medical attention due to possible permanent tissue damage. QT prolongation mandates ECG monitoring in susceptible individuals. Sedation and cognitive impairment necessitate caution in activities requiring mental alertness.
Trazodone has been in clinical use since its FDA approval in 1981 under various brand names worldwide. Given its complex pharmacology and potential for interaction, pharmaceutical sourcing teams should ensure APIs meet stringent purity standards and are accompanied by comprehensive analytical characterization. Supplier qualification should include verification of batch-to-batch consistency, absence of harmful impurities, and compliance with current Good Manufacturing Practices (cGMP) to support regulatory submissions and ensure patient safety.
Identification & chemistry
| Generic name | Trazodone |
|---|---|
| Molecule type | Small molecule |
| CAS | 19794-93-5 |
| UNII | YBK48BXK30 |
| DrugBank ID | DB00656 |
Pharmacology
| Summary | Trazodone is primarily indicated for major depressive disorder and functions through the inhibition of serotonin reuptake and antagonism of multiple serotonin receptor subtypes, including 5-HT2A and 5-HT2C. It also blocks histamine H1 and alpha-1 adrenergic receptors, contributing to its sedative properties. These combined pharmacodynamic effects modulate neurotransmitter activity implicated in mood regulation and sleep. |
|---|---|
| Mechanism of action | The mechanism of action of trazodone is not fully understood, however, it is known to inhibit the reuptake of serotonin and block both histamine and alpha-1-adrenergic receptors. Despite the fact that trazodone is frequently considered a selective serotonin reuptake inhibitor, several reports have shown that other mechanisms including antagonism at serotonin 5-HT1a, 5-HT1c, and 5-HT2 receptor subtypes may occur. The strongest antagonism of trazodone is reported to occur at the serotonin 5-HT21c receptors, preventing serotonin uptake. In addition to acting on serotonin receptors, trazodone has been shown to inhibit serotonin transporters. The antidepressant effects of trazodone result from the inhibition of receptor uptake, which normally decreases circulating neurotransmitters, contributing to depressive symptoms. |
| Pharmacodynamics | Trazodone treats depressed mood and other depression-related symptoms and shows benefit in the treatment of insomnia due to its sedating effects. It is known to prolong the cardiac QT-interval. Memory, alertness, and cognition may be decreased by trazodone, especially in elderly patients due to its central nervous system depressant effects. A note on priapism Trazodone has been associated with the occurrence of priapism, a painful and persistent incidence of penile tissue erection that is unrelievable and can cause permanent neurological damage if left untreated. Patients must be advised to seek immediate medical attention if priapism is suspected. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
| 5-hydroxytryptamine receptor 2C | Humans | agonist |
| Sodium-dependent serotonin transporter | Humans | inhibitor |
ADME / PK
| Absorption | Trazodone is rapidly absorbed in the gastrointestinal tract after oral administration, with a bioavailability ranging from 63-91% and an AUC0−t of 18193.0 ng·h/mL. Food may impact absorption in a variable fashion, and may sometimes lead to decreases in the Cmax of trazodone. In the fed state in 8 healthy volunteers, the Cmax was measured to be 1.47 +/- 0.16 micrograms/mL, and in the fasted state, was measured at 1.88 +/- 0.42 micrograms/mL. The average Tmax after a single dose of 300 mg was 8 hours. Food may increase absorption by up to 20%. |
|---|---|
| Half-life | The plasma elimination half-life was markedly prolonged (13.6 versus 6 hours) elderly volunteers in the fasted state when compared with younger volunteers. Another study of 8 healthy individuals taking a single dose of trazodone indicated a terminal elimination half-life of 7.3 +/- 0.8 hr. A two-phase pattern of trazodone elimination has been reported. Initially, the half-life is reported to range from 3 to 6 hours and the second phase of elimination to range from 5 to 9 hours. |
| Protein binding | The plasma protein binding of trazodone is 89-95% according to in vitro studies. |
| Metabolism | Trazodone is heavily metabolized and activated in the liver by CYP3A4 enzyme to the active metabolite, m-chlorophenylpiperazine (mCPP). The full metabolism of trazodone has not been well characterized. Some other metabolites that have been identified are a dihydrodiol metabolite and carboxylic acid. |
| Route of elimination | Less than 1% of an oral dose is excreted unchanged in the urine. In a pharmacokinetic study, about 60-70% of radiolabeled was excreted urine within 48 hours. Approximately 9-29% was found to be excreted in feces over a range of 60 to 100 hours. According to the FDA medical review, the kidneys are responsible for 70 to 75% of trazodone excretion. About 21% of trazodone is reported to be excreted by the fecal route and 0.13% of the parent drug is eliminated in the urine as unchanged drug. |
| Volume of distribution | A single-dose pharmacokinetic study of 8 volunteers taking trazodone determined a volume of distribution of 0.84 +/- 0.16 L/kg. The FDA medical review of trazodone reports a volume of distribution of 0.47 to 0.84 L/kg. |
| Clearance | A decrease in total apparent clearance (5.1 versus 10.8 L/h) was seen elderly volunteers in the fasted state when compared with younger volunteers. Another pharmacokinetic study determined the total body clearance of trazodone to be 5.3 +/- 0.9 L/hr in 8 healthy patients taking a single dose of trazodone. |
Formulation & handling
- Trazodone is primarily formulated for oral administration in solid dosage forms such as tablets and capsules, including extended-release variants.
- Injectable formulations are also available for intramuscular and intravenous routes, requiring sterile handling conditions.
- The compound has moderate water solubility and logP, indicating consideration for solubility enhancement in formulation development and should be administered shortly after a light meal to optimize absorption.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has primary patent protection in the United States extending until March 2029, with some earlier patents having expired by 2020. The API is marketed in both the US and Canada, indicating a mature market with ongoing patent coverage in key regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The supply landscape for trazodone includes multiple manufacturers, with both originator and generic companies actively producing the API. Branded products have a presence primarily in the US and Canadian markets, supported by various packagers to facilitate distribution. Patent expirations between 2020 and 2029 indicate ongoing and potential future opportunities for generic competition. |
|---|
Safety
| Toxicity | The oral LD50 of trazodone is 690 mg/kg in rats. An overdose of trazodone may result in central nervous system, cardiac, respiratory effects. Signs and symptoms may include dyspnea, bradycardia, hypotension, mental status changes, lack of coordination, and coma, among others. In addition, an overdose may result in priapism, a persistent unrelievable penile tissue erection that may cause permanent damage if not treated promptly. No specific antidote exists for a trazodone overdose. If an overdose occurs, consider the possibility that trazodone may have been combined with other drugs. Contact a poison control center in case of overdose for the most current management guidelines. Dialysis does not accelerate trazodone clearance. |
|---|
- Handle trazodone with caution due to potential central nervous system, cardiac, and respiratory toxicity in cases of overdose
- Avoid exposure routes that may lead to systemic absorption
- High oral doses demonstrate significant acute toxicity (LD50 690 mg/kg in rats)
Trazodone is a type of Selective Serotonin Reuptake Inhibitors (SSRIs)
Selective Serotonin Reuptake Inhibitors (SSRIs) are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used for the treatment of various mental health disorders, particularly depression and anxiety. SSRIs work by inhibiting the reuptake of serotonin, a neurotransmitter that plays a crucial role in regulating mood, emotions, and well-being.
These medications are designed to selectively target the serotonin transporter proteins in the brain, preventing the reabsorption of serotonin into the presynaptic neuron. By blocking the reuptake process, SSRIs increase the concentration of serotonin in the synaptic cleft, enhancing its availability for binding to postsynaptic receptors. This ultimately leads to an improved transmission of serotonin signals between neurons.
The mechanism of action of SSRIs helps to alleviate symptoms of depression and anxiety by stabilizing mood, reducing feelings of sadness, enhancing motivation, and promoting a sense of calmness. The exact therapeutic effects and onset of action may vary depending on the specific SSRIs used.
SSRIs have gained popularity due to their favorable safety profile and efficacy in treating a range of mental health conditions. Common SSRIs include fluoxetine, sertraline, citalopram, and escitalopram. These medications are typically available in oral dosage forms, such as tablets or capsules.
It's important to note that SSRIs should be prescribed and monitored by healthcare professionals, as they can have potential side effects and interactions with other medications. Individuals considering SSRIs should consult with their healthcare provider to determine the most appropriate treatment option for their specific needs.
Trazodone API manufacturers & distributors
Compare qualified Trazodone API suppliers worldwide. We currently have 8 companies offering Trazodone API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Fermion | Producer | Finland | Finland | Other, BSE/TSE, CoA, GDP, GMP, MSDS, USDMF | 29 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Intas Pharma | Producer | United Kingdom | Unknown | CoA, USDMF | 30 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Piramal Pharma Solutions | Producer | India | India | CoA, USDMF | 44 products |
| Sharon Bio-Medicine | Producer | India | India | CoA, GMP, WC | 12 products |
| SPC Life Sciences Pvt Ltd... | Producer | India | India | CoA | 5 products |
When sending a request, specify which Trazodone 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.).
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