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Amoxapine, sold under the brand name Asendin among others, is a tricyclic antidepressant (TCA). It is the N- demethylated metabolite of loxapine. Amoxapine first received marketing approval in the United States in 1992 (approximately 30 to 40 years after most of the other TCAs were introduced in the United States).
Contents
1 Medical uses
2 Contraindications
2.1 Lactation
3 Side effects
4 Overdose
5 Pharmacology
5.1 Pharmacodynamics
5.2 Pharmacokinetics
6 Society and culture
6.1 Brand names
7 See also
8 References
Medical uses
Amoxapine is used in the treatment of major depressive disorder. Compared to other antidepressants it is believed to have a faster onset of action, with therapeutic effects seen within four to seven days.
Contraindications
As with all FDA -approved antidepressants it carries a black-box warning about the potential of an increase in suicidal thoughts or behaviour in children, adolescents and young adults under the age of 25.
Severe cardiovascular disorders (potential of cardiotoxic adverse effects such as QT interval prolongation)
Uncorrected narrow angle glaucoma
Acute recovery post- myocardial infarction
Its use is also advised against in individuals concurrently on monoamine oxidase inhibitors or if they have been on one in the past 14 days and in individuals on drugs that are known to prolong the QT interval (e.g. ondansetron, citalopram, pimozide, sertindole, ziprasidone, haloperidol, chlorpromazine, thioridazine, etc.).
Lactation
Its use in breastfeeding mothers not recommended as it is excreted in breast milk and the concentration found in breast milk is approximately a quarter that of the maternal serum level.
Side effects
Adverse effects by incidence:
Note: Serious (that is, those that can either result in permanent injury or are irreversible or are potentially life-threatening) are written in bold text.
Very common (>10% incidence) adverse effects include:
Constipation
Dry mouth
Sedation
Common (1–10% incidence) adverse effects include:
Anxiety
Ataxia
Blurred vision
Confusion
Dizziness
Headache
Fatigue
Nausea
Nervousness/restlessness
Excessive appetite
Rash
Increased perspiration (sweating)
Tremor
Palpitations
Nightmares
Excitement
Weakness
ECG changes
Oedema. An abnormal accumulation of fluids in the tissues of the body leading to swelling.
Prolactin levels increased. Prolactin is a hormone that regulates the generation of breast milk. Prolactin elevation is not as significant as with risperidone or haloperidol.
Uncommon/Rare (100,000
Human
H 4
6,310
Human
mACh
1,000
Human
Values are K i (nM). The smaller the value, the more strongly the drug binds to the site.
Amoxapine possesses a wide array of pharmacological effects. It is a moderate and strong reuptake inhibitor of serotonin and norepinephrine, respectively,
7-Hydroxyamoxapine, a major active metabolite of amoxapine, is a more potent dopamine receptor antagonist and contributes to its neuroleptic efficacy,
Pharmacokinetics
Amoxapine is metabolised into two main active metabolites: 7-hydroxyamoxapine and 8-hydroxyamoxapine.
Amoxapine
7-hydroxyamoxapine
8-hydroxyamoxapine
Compound
t 1/2 (hr)
t max (hr)
C SS (ng/mL)
Protein binding
V d
Excretion
Amoxapine
8
1-2
17-93 ng/mL (divided dosing), 13-209 ng/mL (single daily dosing)
90%
0.9-1.2 L/kg
Urine (60%), feces (18%)
8-hydroxyamoxapine
30
5.3 (single dosing)
158-512 ng/mL (divided dosing), 143-593 ng/mL (single dose)
?
?
?
7-hydroxyamoxapine
6.5
2.6-5.4 (single dosing)
?
?
?
?
Where:
– t 1/2 is the elimination half life of the compound.
– t max is the time to peak plasma levels after oral administration of amoxapine.
– C SS is the steady state plasma concentration.
– protein binding is the extent of plasma protein binding.
– V d is the volume of distribution of the compound.
Society and culture
Brand names
Brand names for amoxapine include (where † denotes discontinued brands):
Adisen ( KR )
Amolife ( IN )
Amoxan ( JP )
Asendin† (previously marketed in CA, NZ, US )
Asendis† (previously marketed in IE, UK )
Défanyl ( FR )
Demolox ( DK †, IN, ES †)
Oxamine ( IN )
Oxcap ( IN )
See also
Loxapine

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