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Amoxapine | CAS No: 14028-44-5 | GMP-certified suppliers
A medication that provides relief from neurotic, reactive, endogenous, and psychotic depression symptoms, including cases with anxiety or agitation.
Therapeutic categories
Primary indications
- For the relief of symptoms of depression in patients with neurotic or reactive depressive disorders as well as endogenous and psychotic depressions
- May also be used to treat depression accompanied by anxiety or agitation
Product Snapshot
- Amoxapine is available as an oral tablet and solution formulation
- It is primarily indicated for the treatment of various forms of depression, including neurotic, reactive, endogenous, psychotic, and depression with anxiety or agitation
- Amoxapine is approved for use in the US and Canadian markets
Clinical Overview
Pharmacologically, amoxapine functions primarily by inhibiting the reuptake of norepinephrine and serotonin (5-HT), thereby enhancing serotonergic neurotransmission. It differs structurally and mechanistically from other TCAs such as amitriptyline and imipramine and exhibits additional dopamine receptor antagonism. This dopaminergic blockade potentially contributes to its antipsychotic properties. The drug is not a monoamine oxidase inhibitor. Amoxapine’s pharmacodynamic profile includes blockade of histamine H1, alpha-1 adrenergic, and muscarinic receptors, contributing to sedation, hypotension, and anticholinergic side effects respectively.
The precise mechanism underlying its clinical efficacy remains incompletely defined, though animal studies demonstrate reduced uptake of norepinephrine and serotonin and modulation of dopamine receptor responses. Clinical studies suggest a relatively rapid onset of antidepressant action compared to other TCAs.
Regarding absorption, distribution, metabolism, and excretion (ADME), amoxapine is metabolized primarily by cytochrome P450 CYP2D6 enzymes and acts as both a substrate and inhibitor of CYP2D6. This interaction warrants attention to potential drug-drug interactions and individualized dosing strategies. Given its narrow therapeutic index, careful monitoring is recommended.
Safety considerations include a profile characteristic of TCAs: anticholinergic effects (dry mouth, constipation, urinary retention), sedation, hypotension, and the potential for QTc interval prolongation. Amoxapine may lower seizure threshold and has neurotoxic potential at higher doses. It requires cautious use in populations susceptible to cardiovascular, neurological, or hepatic conditions.
Notable uses include treatment of depressive disorders resistant to other antidepressants and management of psychotic depression due to its dopaminergic antagonism. Several branded formulations exist globally under regulatory approval.
For API procurement, sourcing should prioritize suppliers who comply with stringent quality standards, including GMP certification and documented control of polymorphic forms. Verification of impurity profiles, batch-to-batch consistency, and stability under defined storage conditions is essential given amoxapine’s narrow therapeutic index and complex metabolism.
Identification & chemistry
| Generic name | Amoxapine |
|---|---|
| Molecule type | Small molecule |
| CAS | 14028-44-5 |
| UNII | R63VQ857OT |
| DrugBank ID | DB00543 |
Pharmacology
| Summary | Amoxapine is a tricyclic antidepressant that primarily inhibits the reuptake of norepinephrine and serotonin, enhancing monoaminergic neurotransmission. It also acts as an antagonist at multiple dopamine, adrenergic, serotonin, histamine, muscarinic acetylcholine, and GABA receptors, contributing to its pharmacodynamic profile. These combined effects target depressive symptoms and associated anxiety or agitation. |
|---|---|
| Mechanism of action | Amoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). |
| Pharmacodynamics | Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class, chemically distinct from the dibenzodiazepines, dibenzocycloheptenes, and dibenzoxepines. It has a mild sedative component to its action. The mechanism of its clinical action in man is not well understood. In animals, amoxapine reduced the uptake of nor-epinephirine and serotonin and blocked the response of dopamine receptors to dopamine. Amoxapine is not a monoamine oxidase inhibitor. Clinical studies have demonstrated that amoxapine has a more rapid onset of action than either amitriptyline or imipramine |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium-dependent serotonin transporter | Humans | inhibitor |
| Sodium-dependent noradrenaline transporter | Humans | inhibitor |
| Dopamine D2 receptor | Humans | antagonist |
ADME / PK
| Absorption | Rapidly and almost completely absorbed from the GI tract. Peak plasma concentrations occur within 1-2 hours of oral administration of a single dose. |
|---|---|
| Half-life | 8 hours |
| Protein binding | In vitro tests show that amoxapine binding to human plasma proteins is approximately 90%. |
| Metabolism | Amoxapine is almost completely metabolized in the liver to its major metabolite, 8-hydroxyamoxapine, and a minor metabolite, 7-hydroxyamoxapine. Both metabolites are phamacologically inactive and have half-lives of approximately 30 and 6.5 hours, respectively. |
| Route of elimination | 60-69% of a single orally administered dose of amoxapine is excreted in urine, principally as conjugated metabolites. 7-18% of the dose is excrete feces mainly as unconjugated metabolites. Less than 5% of the dose is excreted as unchanged drug in urine. |
| Volume of distribution | Widely distributed in body tissues with highest concentrations found in lungs, spleen, kidneys, heart, and brain. Lower concentrations can be detected in testes and muscle. |
Formulation & handling
- Amoxapine is a small molecule compound primarily formulated for oral administration as tablets with varying strengths.
- Oral formulations should be taken with food to reduce gastrointestinal irritation; alcohol consumption should be avoided due to interaction risks.
- Ophthalmic solutions are also available, indicating sensitivity to formulation sterility and aseptic handling procedures for conjunctival use.
Regulatory status
| Lifecycle | The API's key patents have expired in both the US and Canada, resulting in a mature market with widespread generic availability. Product competition is established, reflecting a stabilized lifecycle phase. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Amoxapine includes multiple originator companies, such as Sandoz, Watson Laboratories, and Lederle Laboratories, reflecting a diversified supply base. Branded products are primarily available in the US and Canadian markets, with multiple brand samples indicating established presence. Given the absence of recent patent activity and the presence of several manufacturers, the product likely faces generic competition or is positioned for such competition. |
|---|
Safety
| Toxicity | Toxic manifestations of amoxapine overdosage differ significantly from those of other tricyclic antidepressants. Serious cardiovascular effects are seldom if ever observed. However, CNS effects, particularly grand mal convulsions, occur frequently, and treatment should be directed primarily toward prevention or control of seizures. Status epilepticus may develop and constitutes a neurologic emergency. Coma and acidosis are other serious complications of substantial amoxapine overdosage in some cases. Renal failure may develop two to five days after toxic overdose in patients who may appear otherwise recovered. Acute tubular necrosis with rhabdomuolysis and myolobinurla is the most common renal complication in such cases. This reaction probably occurs in less than 5% of overdose cases, and typically in those who have experienced multiple seizures. |
|---|
- Amoxapine exhibits a high incidence of CNS toxicity in overdose, including frequent grand mal seizures and potential development of status epilepticus
- Cardiovascular toxicity is rarely observed even in substantial overdose scenarios
- Delayed renal failure due to acute tubular necrosis with rhabdomyolysis can occur, typically 2–5 days post-overdose and often associated with multiple seizure events
Amoxapine 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.
Amoxapine (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.
Amoxapine API manufacturers & distributors
Compare qualified Amoxapine API suppliers worldwide. We currently have 1 companies offering Amoxapine API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
When sending a request, specify which Amoxapine 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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