Clocapramine (Clofekton, Padrasen), also known as 3-chlorocarpipramine, is an
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 ...
of the
iminodibenzyl class which was introduced in
Japan in 1974 by
Yoshitomi for 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 wi ...
.
In addition to
psychosis
Psychosis is a condition of the mind that results in difficulties determining what is real and what is not real. Symptoms may include delusions and hallucinations, among other features. Additional symptoms are incoherent speech and behavior ...
, clocapramine has also been used to augment
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 ...
s in the treatment of
anxiety
Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil
Turmoil may refer to:
* ''Turmoil'' (1984 video game), a 1984 video game released by Bug-Byte
* ''Turmoil'' (2016 video game), a 2016 indie oil tycoon video ...
and
panic
Panic is a sudden sensation of fear, which is so strong as to dominate or prevent reason and logical thinking, replacing it with overwhelming feelings of anxiety and frantic agitation consistent with an animalistic fight-or-flight reac ...
.
Clocapramine has been reported to act as an
antagonist of the
D2,
5-HT2A,
α1-adrenergic, and
α2-adrenergic receptors, and does not inhibit the
reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of trans ...
of either
serotonin or
norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad ...
.
It has also been shown to have
affinity for the
σ receptors.
Clocapramine's affinity for the 5-HT
2A receptor is greater than that for the D
2 receptor and it has a lower propensity for inducing
extrapyramidal symptoms compared to
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 m ...
s, thus underlying its ''atypical'' nature.
Clinical trials
In several
clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s, clocapramine has been compared to other
neuroleptic
Antipsychotics, also known as neuroleptics, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of oth ...
agents. Against
haloperidol
Haloperidol, sold under the brand name Haldol among others, is a typical antipsychotic medication. Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychos ...
, though there was no significant difference in efficacy at the end of the study, clocapramine tended to be superior in alleviating
motor retardation,
alogia, and
thought disorder, and also produced fewer
side effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...
s.
Against
sulpiride, clocapramine demonstrated more favorable effects in the treatment of both
positive and
negative symptom
Signs and symptoms are the observed or detectable signs, and experienced symptoms of an illness, injury, or condition. A sign for example may be a higher or lower temperature than normal, raised or lowered blood pressure or an abnormality showi ...
s, including motor retardation,
delusion
A delusion is a false fixed belief that is not amenable to change in light of conflicting evidence. As a pathology, it is distinct from a belief based on false or incomplete information, confabulation, dogma, illusion, hallucination, or some o ...
s,
hallucination
A hallucination is a perception in the absence of an external stimulus that has the qualities of a real perception. Hallucinations are vivid, substantial, and are perceived to be located in external objective space. Hallucination is a combinati ...
s, and
social isolation
Social isolation is a state of complete or near-complete lack of contact between an individual and society. It differs from loneliness, which reflects temporary and involuntary lack of contact with other humans in the world. Social isolation ...
, though it produced more side effects.
Against
timiperone
Timiperone, sold under the brand name Tolopelon, is a typical antipsychotic of the butyrophenone class which is marketed in Japan for the treatment of schizophrenia. It is similar in chemical structure to benperidol, but has a thiourea group ...
, clocapramine showed lower efficacy against both positive and negative symptoms and produced more side effects such as
dyskinesia
Dyskinesia refers to a category of movement disorders that are characterized by involuntary muscle movements, including movements similar to tics or chorea and diminished voluntary movements. Dyskinesia can be anything from a slight tremor o ...
,
insomnia
Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy ...
,
constipation
Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the bowel moveme ...
, and
nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...
.
Clocapramine has been implicated in at least one fatality, a suicide in which there were two self-inflicted stab wounds and an
overdose
A drug overdose (overdose or OD) is the ingestion or application of a drug or other substance in quantities much greater than are recommended. of clocapramine as well as three other antipsychotics was taken.
The stab wounds could not explain the death, and thus, it was attributed to multiple drug toxicity instead.
See also
*
Carpipramine
*
Mosapramine
*
Penfluridol (typical antipsychotic)
References
{{Tricyclics
Atypical antipsychotics
Carboxamides
Chloroarenes
Dibenzazepines
Piperidines