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Loxapine (several trade names worldwide
Loxapine may be metabolized by N -demethylation to amoxapine, a tetracyclic antidepressant.
Contents
1 Medical uses
2 Precautions
3 Side effects
4 Pharmacology
5 See also
6 References
7 External links
Medical uses
The US Food and Drug Administration (FDA) has approved loxapine inhalation powder for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.
A brief review of loxapine found no conclusive evidence that it was particularly effective in patients with paranoid schizophrenia.
Precautions
This drug is unrelated to the habit-forming benzodiazepines, and misuse is rare. The risks and side effect profile are comparable to other antipsychotics.
Side effects
Further information: Typical antipsychotic
Note: Percentages given after possible adverse effects refer to the incidence of said adverse effects, according to DrugPoint.
Common side effects of loxapine (≥1% incidence) when inhaled include
Taste sense altered (14%)
Sedated (12%)
Pharyngitis (3%)
Common side effects of orally-administered loxapine include
Constipation
Dry mouth
Akathisia
Dizziness
Intense sleeping
Slurred speech
Extrapyramidal symptoms (dose-dependent. At lower dosages its propensity for causing extrapyramidal side effects appears to be similar to that of atypical antipsychotics
Blurred vision
Urinary retention
Somnolence (which appears to be moderate in severity compared to other antipsychotic drugs )
Dyspnoea
Nasal congestion
Rare side effects include
Paralytic ileus
Agranulocytosis
Leukopenia
Thrombocytopenia
Hepatocellular liver damage
Neuroleptic malignant syndrome
Seizure
Tardive dyskinesia
Stroke
Transient ischaemic attack
Death
Pharmacology
Loxapine (and metabolite)
Site
LOX
AMX
5-HT 1A
2,460
ND
5-HT 1B
388
ND
5-HT 1D
3,470
ND
5-HT 1E
1,400
ND
5-HT 2A
6.6
0.5
5-HT 2C
13
2 (rat)
5-HT 3
190
ND
5-HT 5A
780
ND
5-HT 6
31
50
5-HT 7
88
40 (rat)
α 1A
31
ND
α 1B
53
ND
α 2A
151
ND
α 2B
108
ND
α 2C
80
ND
β 1
>10,000
ND
β 2
>10,000
ND
M 1
120
ND
M 2
445
ND
M 3
211
ND
M 4
1,270
ND
M 5
166
ND
D 1
54
ND
D 2
11
21
D 3
19
21
D 4
8.4
21
D 5
75
ND
H 1
2.2–4.9
7.9–25
H 2
208
ND
H 3
55,000
>100,000
H 4
5,050–8,710
6,310
SERT
>10,000
58
NET
5,700
16
DAT
>10,000
58
Values are K i (nM). The smaller the value, the more strongly the drug binds to the site.
The data in the table to the right was obtained from the PDSP Ki database and they are for binding towards human cloned proteins (receptor and transporter) unless otherwise specified.
See also
Amoxapine
Clotiapine

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