Fluoropipamide
Fluoropipamide Uses, Dosage, Side Effects, Food Interaction and all others data.
Fluoropipamide is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. It was developed by Janssen Pharmaceutica in 1961 and started its first round of clinical trials in 1963 .
In an effort to improve haloperidol's pharmacological effects, Janssen discovered that pipamperone, an agent whose pharmacological profile was distinct from haloperidol and all other known antipsychotic drugs at this time, had significant anti-tryptamine activity. Some studies suggest pipamperone was the first atypical antipsychotic. Interestingly, when risperidone was created, Janssen suggested it was a more potent version of pipamperone. Synthesized in the year 1984, risperidone’s pharmacological properties were similar to pipamperone’s in that both block more serotonin more potently than dopamine .
Fluoropipamide is an antipsychotic medication that has sedative effects, which may be beneficial in the management of agitation and disordered sleep . Fluoropipamide, showing antidopaminergic and anti-serotonergic properties, has been noted for its anti-agitation effects and for its ability to normalize sleep rhythms in psychiatric patients . One study showed that pipamperone increased the expression of D4 (dopaminergic) receptors, explaining its helpfulness in decreasing positive psychotic symptoms, such as delusions and hallucinations .
Trade Name | Fluoropipamide |
Generic | Pipamperone |
Pipamperone Other Names | Carpiperone, Floropipamide, Fluoropipamide, Pipamperona, Pipamperone |
Type | |
Formula | C21H30FN3O2 |
Weight | Average: 375.488 Monoisotopic: 375.232205381 |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Treatment of chronic psychoses and states of aggressiveness of various origins .
How Fluoropipamide works
Fluoropipamide binds mainly to 5-HT2A receptors, with a nearly equal affinity to D4 receptors and a moderate affinity for 5-HT2C, D2, D3, 1- and 2B-adrenoceptors .
This drug is a selective 5-HT2A, D1 and D4 antagonist . Extrapyramidal adverse effects also appear to be limited in pipamperone treatment compared to traditional antipsychotic medications due to its high receptor selectivity .
Fluoropipamide has a 15-fold higher affinity for D4 than D2 receptors. It has been suggested that D4 receptors may play a role in the modulation of GABAergic neuronal activity by dopamine .
Toxicity
Ld50 in rats, 48 mg/kg . Prolonged Qtc interval. Monitoring with regular ECGs is recommended .
Half Life
17-26h
Elimination Route
Mainly via the kidneys
Innovators Monograph
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