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Desipramine | CAS No: 50-47-5 | GMP-certified suppliers
A medication that provides symptomatic relief in depressive syndromes and is used off-label for neuropathic pain, anxiety disorders, and ADHD management.
Therapeutic categories
Primary indications
- For relief of symptoms in various depressive syndromes, especially endogenous depression
- It has also been used to manage chronic peripheral neuropathic pain, as a second line agent for the management of anxiety disorders (e
- G
- Panic disorder, generalized anxiety disorder), and as a second or third line agent in the ADHD management
Product Snapshot
- Desipramine is an oral small molecule available in multiple tablet and film-coated tablet formulations
- It is primarily indicated for depressive syndromes and also used in neuropathic pain, anxiety disorders, and ADHD management
- The product holds approved and investigational status in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, desipramine functions as a secondary amine TCA and is the active metabolite of imipramine. Its principal mechanism of action involves selective inhibition of norepinephrine reuptake at neuronal synapses, resulting in increased noradrenergic neurotransmission. It also inhibits serotonin reuptake, albeit to a lesser extent compared to tertiary amine TCAs. Chronic administration leads to down-regulation of cerebral cortical beta-adrenergic receptors and sensitization of postsynaptic serotonergic receptors, enhancing serotonergic transmission which is thought to underpin its antidepressant effects. Clinical benefits typically manifest within 2 to 4 weeks of initiation, with some patients requiring up to 8 weeks.
Absorption and metabolism details include hepatic biotransformation predominantly through cytochrome P450 enzymes including CYP2D6 and CYP3A4 subfamilies. Desipramine exhibits moderate inhibitory effects on several cytochrome P450 isoforms, which may influence drug interactions. Elimination is mainly renal, and the compound has a narrow therapeutic index necessitating careful dose titration and monitoring.
Safety considerations highlight a spectrum of anticholinergic, sedative, and cardiovascular effects due to antagonism of muscarinic, histamine-H1, and alpha-1 adrenergic receptors, though desipramine presents fewer anticholinergic and sedative side effects relative to tertiary amine TCAs. It may pose risk for QTc prolongation and should be used cautiously in patients with cardiac conditions. Like other TCAs, it lowers the seizure threshold and requires vigilance for toxicity, including overdose risk.
From an API sourcing perspective, quality assurance should focus on stringent control of polymorphic forms, impurity profiles, and compliance with pharmacopeial standards. Consistency in potency, stability, and adherence to Good Manufacturing Practice (GMP) are essential due to the narrow therapeutic window and potential for significant clinical effects.
Identification & chemistry
| Generic name | Desipramine |
|---|---|
| Molecule type | Small molecule |
| CAS | 50-47-5 |
| UNII | TG537D343B |
| DrugBank ID | DB01151 |
Pharmacology
| Summary | Desipramine is a tricyclic antidepressant that primarily inhibits the reuptake of norepinephrine, with secondary effects on serotonin reuptake, enhancing synaptic neurotransmitter levels in the central nervous system. Chronic administration leads to down-regulation of beta-adrenergic receptors and sensitization of serotonergic receptors, resulting in increased serotonergic transmission. Its pharmacological profile includes affinity for multiple adrenergic and muscarinic receptor subtypes, contributing to its therapeutic effects in depressive disorders and certain off-label uses. |
|---|---|
| Mechanism of action | Desipramine is a tricyclic antidepressant (TCA) that selectively blocks reuptake of norepinephrine (noradrenaline) from the neuronal synapse. It also inhibits serotonin reuptake, but to a lesser extent compared to tertiary amine TCAs such as imipramine. Inhibition of neurotransmitter reuptake increases stimulation of the post-synaptic neuron. Chronic use of desipramine also leads to down-regulation of beta-adrenergic receptors in the cerebral cortex and sensitization of serotonergic receptors. An overall increase in serotonergic transmission likely confers desipramine its antidepressant effects. Desipramine also possesses minor anticholinergic activity, through its affinity for muscarinic receptors. TCAs are believed to act by restoring normal levels of neurotransmitters via synaptic reuptake inhibition and by increasing serotonergic neurotransmission via serotonergic receptor sensitization in the central nervous system. |
| Pharmacodynamics | Desipramine, a secondary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is the active metabolite of imipramine, a tertiary amine TCA. The acute effects of desipramine include inhibition of noradrenaline re-uptake at noradrenergic nerve endings and inhibition of serotonin (5-hydroxy tryptamine, 5HT) re-uptake at the serotoninergic nerve endings in the central nervous system. Desipramine exhibits greater noradrenergic re-uptake inhibition compared to the tertiary amine TCA imipramine. In addition to inhibiting neurotransmitter re-uptake, desipramine down-regulates beta-adrenergic receptors in the cerebral cortex and sensitizes serotonergic receptors with chronic use. The overall effect is increased serotonergic transmission. Antidepressant effects are typically observed 2 - 4 weeks following the onset of therapy though some patients may require up to 8 weeks of therapy prior to symptom improvement. Patients experiencing more severe depressive episodes may respond quicker than those with mild depressive symptoms. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium-dependent noradrenaline transporter | Humans | inhibitor |
| Sodium-dependent serotonin transporter | Humans | inhibitor |
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
ADME / PK
| Absorption | Desipramine hydrochloride is rapidly and almost completely absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism. Peak plasma concentrations are attained 4 - 6 hours following oral administration. |
|---|---|
| Half-life | 7-60+ hours; 70% eliminated renally |
| Protein binding | 73-92% bound to plasma proteins |
| Metabolism | Desipramine is extensively metabolized in the liver by CYP2D6 (major) and CYP1A2 (minor) to 2-hydroxydesipramine, an active metabolite. 2-hydroxydesipramine is thought to retain some amine reuptake inhibition and may possess cardiac depressant activity. The 2-hydroxylation metabolic pathway of desipramine is under genetic control. |
| Route of elimination | Desipramine is metabolized in the liver, and approximately 70% is excreted in the urine. |
Formulation & handling
- Desipramine is a small molecule suitable for oral tablet formulations with multiple coating options to support stability and patient acceptability.
- The compound has low water solubility and high logP, indicating formulation strategies should address bioavailability challenges.
- Administration with food is recommended to minimize gastrointestinal irritation; alcohol and caffeine intake should be limited during treatment.
Regulatory status
| Lifecycle | The API is currently marketed in Canada and the US, with key patents expiring between 2024 and 2026, indicating a transition towards increased generic competition and market maturity. Lifecycle management efforts are ongoing to sustain product presence post-patent expiry. |
|---|
| Markets | Canada, US |
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Supply Chain
| Supply chain summary | Desipramine's supply chain involves multiple packagers, indicating a broad manufacturing base predominantly focused on the US and Canadian markets. The presence of branded products by originator companies such as Sanofi-Aventis suggests established global reach, primarily in North America. Given the extensive list of generic packagers and the absence of recent patent protection, generic competition is well-established in these regions. |
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Safety
| Toxicity | Male mice: LD50 = 290 mg/kg, female rats: LD50 = 320 mg/kg. Antagonism of the histamine H<sub>1</sub> and α<sub>1</sub> receptors can lead to sedation and hypotension. Antimuscarinic activity confers anticholinergic side effects such as blurred vision, dry mouth, constipation and urine retention may occur. Cardiotoxicity may occur with high doses of desipramine. Cardiovascular side effects in postural hypotension, tachycardia, hypertension, ECG changes and congestive heart failure. Psychotoxic effects include impaired memory and delirium. Induction of hypomanic or manic episodes may occur in patients with a history of bipolar disorder. Withdrawal symptoms include GI disturbances (e.g. nausea, vomiting, abdominal pain, diarrhea), anxiety, insomnia, nervousness, headache and malaise. |
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- Handle with care to avoid exposure due to potential cardiotoxicity and CNS effects at high doses
- Use appropriate protective measures to prevent contact, as antimuscarinic and antihistamine receptor antagonism may cause systemic adverse effects upon absorption
- Monitor and control environmental release to mitigate risks of sedation, hypotension, and psychotropic effects associated with the compound
Desipramine is a type of Tricyclic antidepressants
Tricyclic antidepressants (TCAs) are a class of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the treatment of various mental health disorders, especially depression and anxiety. TCAs derive their name from their unique molecular structure, which consists of three interconnected rings.
These antidepressants work by inhibiting the reuptake of neurotransmitters such as serotonin and norepinephrine in the brain, thereby increasing their availability and improving mood regulation. Some commonly prescribed TCAs include amitriptyline, imipramine, and nortriptyline.
The efficacy of TCAs in managing depressive symptoms is well-documented, making them a popular choice among healthcare professionals. Additionally, they exhibit analgesic properties, making them useful in treating chronic pain conditions like neuropathic pain and migraines.
It is important to note that TCAs are associated with a range of side effects, including dry mouth, drowsiness, constipation, and blurred vision. Moreover, they require careful monitoring due to their potential for drug interactions, particularly with monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake inhibitors (SSRIs).
Despite the availability of newer classes of antidepressants, TCAs remain an essential component of the treatment arsenal for various mental health disorders. Their well-established efficacy, along with ongoing research and development in the field, ensures that TCAs will continue to play a significant role in managing these conditions in the foreseeable future.
Desipramine (Tricyclic antidepressants), classified under Antidepressants
Antidepressants are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of depression and other mood disorders. These medications work by balancing the levels of certain chemicals in the brain called neurotransmitters, such as serotonin, norepinephrine, and dopamine.
There are several types of antidepressants available, each with its own mechanism of action and efficacy. Selective serotonin reuptake inhibitors (SSRIs) are commonly prescribed as a first-line treatment for depression. They prevent the reabsorption of serotonin, resulting in increased serotonin levels in the brain. Examples of popular SSRIs include fluoxetine, sertraline, and escitalopram.
Tricyclic antidepressants (TCAs) are another class of antidepressants that work by blocking the reuptake of both serotonin and norepinephrine. They are generally used when SSRIs are ineffective or not well-tolerated. Amitriptyline, nortriptyline, and imipramine are commonly prescribed TCAs.
Other antidepressants include serotonin-norepinephrine reuptake inhibitors (SNRIs), atypical antidepressants, and monoamine oxidase inhibitors (MAOIs). SNRIs, such as venlafaxine and duloxetine, inhibit the reuptake of both serotonin and norepinephrine. Atypical antidepressants, including bupropion and mirtazapine, have diverse mechanisms of action, targeting multiple neurotransmitters. MAOIs, such as phenelzine and tranylcypromine, work by inhibiting the enzyme monoamine oxidase, which breaks down neurotransmitters.
It is important to note that antidepressants may have various side effects and require close monitoring by healthcare professionals. Dosages and treatment duration vary based on individual needs and response. Antidepressants are typically prescribed as part of a comprehensive treatment plan that may include psychotherapy and lifestyle modifications.
In conclusion, antidepressants are a vital category of pharmaceutical APIs used to manage depression and related mood disorders. They act on neurotransmitters in the brain to alleviate symptoms and improve overall well-being. It is crucial to consult with a healthcare provider to determine the most suitable antidepressant and monitor its effects.
Desipramine API manufacturers & distributors
Compare qualified Desipramine API suppliers worldwide. We currently have 2 companies offering Desipramine API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Lundbeck Pharma | Producer | Italy | Italy | CoA, USDMF | 15 products |
| PCAS | Producer | France | Unknown | CoA, USDMF | 29 products |
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