Amoxapine

2-chloro- 11 -(1- piperazinyl) dibenz [b, f] [ 1,4] oxazepine (IUPAC)

N06AA17

Tricyclic antidepressant

Attention

Template: Infobox chemical / molecular formula search available

Amoxapine is one of the dibenzazepine derivatives ( dibenzoxazepines ) and is used as a drug from the group of tricyclic antidepressants.

  • 2.1 Therapeutic indications (indications )
  • 2.2 Adverse reactions (side effects)
  • 2.3 Interaction with other drugs

Pharmacology

Pharmacodynamics

Amoxapine inhibits esp. the resumption of the neurotransmitter norepinephrine. In addition, it acts as a weak serotonin reuptake inhibitors at the same time blocking of the 5-HT2 receptor. One of its major metabolite, 7 - Hydroxyamoxapin, acts as an antagonist at the D2 receptor. It also has anticholinergic and antihistaminic activity at the H1 receptor. Of the effects and side effects, it corresponds to the imipramine type.

Pharmacokinetics

Amoxapine is absorbed relatively quickly, making it unfolds after 90 minutes, the maximum ( Tmax). Bioavailability is 90%. It is almost completely metabolized by the CYP450 enzyme system and excreted mainly by the kidney. However, the half -life of eight hours for its active metabolites Hydroxyamoxapin 8 at 30 hours. In clinical studies, it was found that the antidepressant effect of amoxapine unfolds faster than amitriptyline or imipramine.

Clinical information

Areas of application (indications )

Amoxapine is indicated for the treatment of depression, bipolar disorders and panic disorders. Therapeutically useful doses range from 200 to 300 mg everyday, can possibly be increased to 600 mg.

It has also been shown that amoxapine can be used for the treatment of schizophrenia. In studies, it proved as effective as haloperidol and risperidone. Here, the extrapyramidal syndrome occurred less frequently and should have been the prolactin levels less often increased. In the negative symptoms of schizophrenia, it should work better than haloperidol.

Adverse effects (side effects)

Common adverse reactions (<1% ) are: anxiety, nervousness, confusion, nausea, increased appetite, headache, debility, insomnia, nightmares, tremor, ataxia, palpitations, edema, rash, prolactin elevation, increased sweating. A very rare but dangerous side effect is the neuroleptic malignant syndrome.

Interactions with other drugs

It has been observed that drugs that inhibit the cytochrome P450 2D6 enzyme that hinder the breakdown of amoxapine, so that the dose must be reduced.

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