Pipamperone (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
,
USAN
280px, "Samguk Sagi" Book 04. Silla's Records. In 512, Usan-guk(于山國)was Ulleungdo(鬱陵島)
Usan-guk, or the State of Usan, occupied Ulleung-do and the adjacent islands during the Korean Three Kingdoms period. According to th ...
,
BAN), also known as carpiperone and floropipamide or fluoropipamide, and as floropipamide hydrochloride (
JAN
Jan, JaN or JAN may refer to:
Acronyms
* Jackson, Mississippi (Amtrak station), US, Amtrak station code JAN
* Jackson-Evers International Airport, Mississippi, US, IATA code
* Jabhat al-Nusra (JaN), a Syrian militant group
* Japanese Article Num ...
), is a
typical antipsychotic
Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics ma ...
of the
butyrophenone
Butyrophenone is an organic compound with the formula C6H5C(O)C3H7. It is a colorless liquid.
The butyrophenone structure—a ketone flanked by a phenyl ring and a butyl chain—forms the basis for many other chemicals containing various sub ...
family used in the treatment of
schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ...
and as a sleep aid for depression. It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.
Pipamperone was discovered at
Janssen Pharmaceutica
Janssen Pharmaceuticals is a pharmaceutical company headquartered in Beerse, Belgium, and wholly-owned by Johnson & Johnson. It was founded in 1953 by Paul Janssen.
In 1961, Janssen Pharmaceuticals was purchased by New Jersey-based American ...
in 1961, and entered
clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
s in the
United States
The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territorie ...
in 1963.
Pharmacology
![Pipamperon neuraxpharm 40mg by Danny S](https://upload.wikimedia.org/wikipedia/commons/a/a1/Pipamperon_neuraxpharm_40mg_by_Danny_S._-_001.JPG)
Pipamperone acts as an
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
of the
5-HT2A,
5-HT2B,
5-HT2C D2,
D3,
D4,
α1-adrenergic,
and
α2-adrenergic receptors.
It shows much higher
affinity
Affinity may refer to:
Commerce, finance and law
* Affinity (law), kinship by marriage
* Affinity analysis, a market research and business management technique
* Affinity Credit Union, a Saskatchewan-based credit union
* Affinity Equity Par ...
for the 5-HT
2A and D
4 receptors over the D
2 receptor (15-fold in the case of the D
4 receptor, and even higher in the case of the 5-HT
2A receptor),
being regarded as "highly selective" for the former two sites at low doses.
Pipamperone has low and likely insignificant affinity for the
H1 and
mACh receptors, as well as for other
serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...
and
dopamine receptor
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through diffe ...
s.
Pipamperone is considered to have been a forerunner to the
atypical antipsychotic
The atypical antipsychotics (AAP), also known as second generation antipsychotics (SGAs) and serotonin–dopamine antagonists (SDAs), are a group of antipsychotic drugs (antipsychotic drugs in general are also known as major tranquilizers and ne ...
s, if not an atypical antipsychotic itself, due to its prominent
serotonin antagonism.
It is also used to normalise mood and sleep patterns and has antianxiety effects in neurotic patients.
Antidepressant effects
Low-dose pipamperone (5 mg twice daily) has been found to accelerate and enhance the
antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
effect of
citalopram
Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and socia ...
(40 mg once daily), in a combination (citalopram/pipamperone) referred to as PipCit (code name PNB-01).
See also
*
Clozapine
Clozapine is a psychiatric medication and is the first atypical antipsychotic (also called second-generation antipsychotic). It is primarily used to treat people with schizophrenia and schizoaffective disorders who have had an inadequate respo ...
*
Melperone
Melperone (Bunil ( PT), Buronil ( AT, BE, CZ, DK, FL†, NL†, NO†, SE), Eunerpan ( DE)) is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. It first ...
*
Pimozide
Pimozide (sold under the brand name Orap) is an antipsychotic drug of the diphenylbutylpiperidine class. It was discovered at Janssen Pharmaceutica in 1963. It has a high potency compared to chlorpromazine (ratio 50-70:1). On a weight basis i ...
*
Piritramide
*
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions ...
References
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Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (fo ...
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{{Adrenergic receptor modulators
{{Dopamine receptor modulators
{{Serotonin receptor modulators
5-HT2A antagonists
5-HT2B antagonists
5-HT2C antagonists
Alpha-1 blockers
Alpha-2 blockers
Carboxamides
Belgian inventions
Butyrophenone antipsychotics
D2 antagonists
D3 antagonists
D4 antagonists
Janssen Pharmaceutica
Fluoroarenes
Piperidines
Typical antipsychotics