Amoxepine

Amoxepine Uses, Dosage, Side Effects, Food Interaction and all others data.

Amoxepine, the N-demethylated derivative of the antipsychotic agent loxapine, is a dibenzoxazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amoxapine does not affect mood or arousal, but may cause sedation. In depressed individuals, amoxapine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amoxepine may be used to treat neurotic and reactive depressive disorders, endogenous and psychotic depression, and mixed symptoms of depression and anxiety or agitation.

Amoxepine 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. Amoxepine is not a monoamine oxidase inhibitor. Clinical studies have demonstrated that amoxapine has a more rapid onset of action than either amitriptyline or imipramine

Amoxepine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Amoxepine
Availability	Prescription only
Generic	Amoxapine
Amoxapine Other Names	Amoxapin, Amoxapina, Amoxapine, Amoxapinum, Amoxepine, Desmethylloxapin
Related Drugs	Rexulti, sertraline, trazodone, Lexapro, Zoloft, citalopram, Cymbalta
Type
Formula	C₁₇H₁₆ClN₃O
Weight	Average: 313.781 Monoisotopic: 313.098189856
Protein binding	In vitro tests show that amoxapine binding to human plasma proteins is approximately 90%.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Amoxepine is a tricyclic antidepressant used in the treatment of neurotic or reactive depressive disorders and endogenous or psychotic depression.

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.

Amoxepine is also used to associated treatment for these conditions: Depression, Depression, Endogenous, Depression, Reactive, Neurotic depression, Psychotic Depression

How Amoxepine works

Amoxepine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).

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.

Food Interaction

Avoid alcohol.
Take with food. Food reduces irritation.

Amoxepine Alcohol interaction

[Moderate] GENERALLY AVOID:

Concomitant use of ethanol and a tricyclic antidepressant (TCA) may result altered TCA plasma levels and efficacy, and additive impairment of motor skills, especially driving skills.

Acute ethanol ingestion may inhibit TCA metabolism, while chronic ingestion of large amounts of ethanol may induce hepatic TCA metabolism.

Patients should be advised to avoid alcohol during TCA therapy.

Alcoholics who have undergone detoxification should be monitored for decreased TCA efficacy.

Dosage adjustments may be required.

Amoxepine Drug Interaction

Major: citalopram, citalopram, escitalopram, escitalopram, vilazodone, vilazodoneModerate: aripiprazole, aripiprazole, amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, lorazepam, lorazepam, lurasidone, lurasidone, albuterol, albuterol, lisdexamfetamine, lisdexamfetamineUnknown: cholecalciferol, cholecalciferol

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.

Elimination Route

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

Elimination Route

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.