Perphenazine
2 - { 4 - [ 3 - (2 -chloro- 10H - phenothiazin -10 -yl ) propyl] piperazin-1 -yl} ethanol
N05AB03
White, light-sensitive crystals
- Neuroleptics
- Antiemetics
94-100 ° C
278-281 ° C ( 133 Pa )
Water: 28.3 mg · l -1 ( 24 ° C)
Attention
318 mg · kg -1 ( LD50, rat, oral)
Template: Infobox chemical / molecular formula search available
Perphenazine is a drug selected from the group of phenothiazines which is used in the treatment of psychoses. Perphenazine was put on the market in 1957. Due to the availability of newer antipsychotic drugs, however, it is increasingly rare application. In the CATIE study perphenazine was used as reference substance to the atypical neuroleptics.
- 2.1 Mechanism of action ( pharmacodynamics )
- 2.2 Absorption and distribution in the body ( pharmacokinetics )
- 3.1 Chemical Information
Clinical information
Areas of application (indications )
Application areas include acute psychosis, such as schizophrenia, with delusions, hallucinations, catatonic syndromes, delirium and other organic psychosis, agitation.
Perphenazine may also be indicated for the treatment of vomiting when other treatment measures are not feasible or have failed.
Posology and method of administration
The dosage is up to three times a day 4 to 8 mg. Perphenazine can be used for long-term treatment, but this increases the risk of tardive dyskinesia.
Contraindications ( contraindications)
Although the drug the group of phenothiazines belongs to the spectrum of the contraindications were more similar to haloperidol.
Use during pregnancy and lactation
The application in the first trimester is considered to be contraindicated in the second or third trimester, the indication should be very strictly set.
Adverse effects (side effects)
As a drug of the group of phenothiazines the spectrum of side effects is very similar to that of chlorpromazine.
Pharmacological properties
Mechanism of action ( pharmacodynamics )
Perphenazine at equivalent doses is 10 - more potent than chlorpromazine Vergleichsneuroleptikum to 15 times, and is therefore regarded as so-called highly potent neuroleptic. Perphenazine also acts as FIASMA ( functional inhibitors of acid sphingomyelinase ).
Uptake and distribution in the body ( pharmacokinetics )
Bioavailability is 40%, the plasma half-life 8-12 hours. Perphenazine is therefore usually administered two to three times daily with dose focal point in the evening due to the sedative and hypotensive effect. Perphenazine is metabolized by the liver.
Other Information
Chemical information
In perphenazine is a phenothiazine with a piperazinylalkyl side chain on ring 2 perphenazine therefore has a chemical structure in common with the first ever discovered neuroleptic, the chlorpromazine.