Name: | Amoxapine |
---|---|
PubChem Compound ID: | 2170 |
Description: | The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both. It also blocks dopamine receptors. |
Molecular formula: | C17H16ClN3O |
Molecular weight: | 313.781 g/mol |
Synonyms: |
NCGC00015004-02; NCGC00015004-01; AMOXEPINE; EU-0100116; Prestwick1_000102; 14028-44-5; Demolox; SPBio_001150; KBio1_000236; DIBENZ(b,f)(1,4)OXAZEPINE, 2-CHLORO-11-(1-PIPERAZINYL)-.
show more » |
Name: | Amoxapine |
---|---|
Name (isomeric): | DB00543 |
Drug Type: | small molecule |
Description: | The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both. It also blocks dopamine receptors. |
Synonyms: |
Amoxepine
|
Brand: | Defanyl, Ascendin, Demolox, Asendis, Moxadil |
Category: | Neurotransmitter Uptake Inhibitors, Adrenergic Uptake Inhibitors, Dopamine Antagonists, Antidepressive Agents, Second-Generation, Serotonin Uptake Inhibitors |
CAS number: | 14028-44-5 |
Indication: | 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. |
---|---|
Pharmacology: |
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...
show more » |
Mechanism of Action: | Amoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). |
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. |
Protein binding: | In vitro tests show that amoxapine binding to human plasma proteins is approximately 90%. |
Biotransformation: | 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. |
Half Life: | 8 hours |
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. |
Affected organisms: | Humans and other mammals |
Food interaction: |
| ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Drug interaction: |
|