Zuclopenthixol
Encyclopedia
Zuclopenthixol also known as zuclopentixol, is a typical antipsychotic
drug
of the thioxanthene
class. It was introduced in 1962 by Lundbeck
.
Zuclopenthixol is the cis-isomer
of clopenthixol
.
It is also used in the treatment of acute bipolar mania.
may be helpful for tremor and stiffness, while diazepam
may be helpful for akathisia. 100 mg of zuclopenthixol decanoate is roughly equivalent to 20 mg of flupentixol decanoate or 12.5 mg of fluphenazine
decanoate.
In acutely psychotic and agitated inpatients, 50 - 200 mg of zuclopenthixol acetate may be given for a calming effect over the subsequent three days, with a maximum dose of 400 mg in total to be given. As it is a long-acting medication, care must be taken not to give an excessive dose.
In oral form zuclopenthixol is available in 10, 25 and 40 mg tablets, with a dose range of 20–60 mg daily.
of D1 and D2 receptors, though it also has some antihistamine
effects, among other properties.
Other side effects are similar to many other typical antipsychotics, namely extrapyramidal symptoms
as a result of dopamine blockade in subcortical areas of the brain. This may result in symptoms similar to those seen in Parkinsons Disease and include a restlessness and inability to sit still known as akathisia
, a slow tremor and stiffness of the limbs. Zuclopenthixol is thought to be more sedating than the related flupentixol
, though possibly less likely to induce extrapyramidal symptoms than other typical depots. As with other dopamine antagonists, zuclopenthixol may sometimes elevate prolactin
levels; this may occasionally result in amenorrhoea
or galactorrhoea in severe cases. Neuroleptic malignant syndrome
is a rare but potentially fatal side effect. Any unexpected deterioration in mental state with confusion and muscle stiffness should be seen by a physician.
Typical antipsychotic
Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis...
drug
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
of the thioxanthene
Thioxanthene
Thioxanthene is a chemical compound in which the oxygen atom in xanthene is replaced with a sulfur atom. It is also related to phenothiazine. Several of its derivatives are used as typical antipsychotics in the treatment of schizophrenia and other psychoses....
class. It was introduced in 1962 by Lundbeck
Lundbeck
H. Lundbeck A/S is a Danish international pharmaceutical company engaged in the research and development, production, marketing, and sale of drugs for the treatment of disorders in the central nervous system , including depression, schizophrenia, Alzheimer’s disease, Parkinson’s disease,...
.
Zuclopenthixol is the cis-isomer
Isomer
In chemistry, isomers are compounds with the same molecular formula but different structural formulas. Isomers do not necessarily share similar properties, unless they also have the same functional groups. There are many different classes of isomers, like stereoisomers, enantiomers, geometrical...
of clopenthixol
Clopenthixol
Clopenthixol , also known as clopentixol, is a typical antipsychotic drug of the thioxanthene class. It was introduced by Lundbeck in 1961....
.
Uses/Forms
Zuclopenthixol is available in three major preparations:- As zuclopenthixol decanoate (Clopixol), it is a long acting intramuscular injection. Its main use is as a long acting injection given two or three times weekly to people with schizophreniaSchizophreniaSchizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
who have a poor compliance with medication and suffer frequent relapses of illness. In some countries this can be mandated by Court order for a lengthy period of time, sometimes years, at the request of the psychiatrist. There is some evidence it may be more helpful in managing aggressive behaviour.
- As zuclopenthixol acetate (Clopixol, Acuphase), it is a shorter acting intramuscular injection used in the acute sedation of psychotic inpatients. The effect peaks at 48–72 hours providing 2–3 days of sedation.
- As zuclopenthixol dihydrochloride (Clopixol), it is a tablet used in the treatment of schizophrenia in those who are compliant with oral medication.
It is also used in the treatment of acute bipolar mania.
Dosing
As a long acting injection, zuclopenthixol decanoate comes in a 200 mg and 500mg ampoule. Doses can vary from 50 mg 4 weekly to the maximum licensed dose of 600 mg weekly. In general, the lowest effective dose to prevent relapse is preferred. The interval may be shorter as a patient starts on the medication before extending to 3 weekly intervals subsequently. The dose should be reviewed and reduced if side effects occur, though in the short term an anticholinergic medication benztropineBenztropine
Benzatropine , also known as benztropine , is an anticholinergic marketed under the trade name Cogentin which is used in the treatment of Parkinson's disease, parkinsonism, akathisia, and dystonia.- Indications :...
may be helpful for tremor and stiffness, while diazepam
Diazepam
Diazepam , first marketed as Valium by Hoffmann-La Roche is a benzodiazepine drug. Diazepam is also marketed in Australia as Antenex. It is commonly used for treating anxiety, insomnia, seizures including status epilepticus, muscle spasms , restless legs syndrome, alcohol withdrawal,...
may be helpful for akathisia. 100 mg of zuclopenthixol decanoate is roughly equivalent to 20 mg of flupentixol decanoate or 12.5 mg of fluphenazine
Fluphenazine
Fluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia and acute manic phases of bipolar disorder. It belongs to the piperazine class of phenothiazines....
decanoate.
In acutely psychotic and agitated inpatients, 50 - 200 mg of zuclopenthixol acetate may be given for a calming effect over the subsequent three days, with a maximum dose of 400 mg in total to be given. As it is a long-acting medication, care must be taken not to give an excessive dose.
In oral form zuclopenthixol is available in 10, 25 and 40 mg tablets, with a dose range of 20–60 mg daily.
Pharmacology
Zuclopenthixol mainly acts by antagonismReceptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
of D1 and D2 receptors, though it also has some antihistamine
Antihistamine
An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
effects, among other properties.
Side effects
Chronic administration of zuclopenthixol (30mg/kg/day for two years) in rats resulted in small, but significant, increases in the incidence of thyroid parafollicular carcinomas and, in females, of mammary adenocarcinomas and of pancreatic islet cell adenomas and carcinomas. An increase in the incidence of mammary adenocarcinomas is a common finding for D2 antagonists which increase prolactin secretion when administered to rats. An increase in the incidence of pancreatic islet cell tumours has been observed for some other D2 antagonists. The physiological differences between rats and humans with regard to prolactin make the clinical significance of these findings unclear.Other side effects are similar to many other typical antipsychotics, namely extrapyramidal symptoms
Extrapyramidal symptoms
The extrapyramidal system can be affected in a number of ways, which are revealed in a range of extrapyramidal symptoms , also known as extrapyramidal side-effects , such as akinesia and akathisia .Extrapyramidal symptoms are various movement disorders such as acute dystonic reactions,...
as a result of dopamine blockade in subcortical areas of the brain. This may result in symptoms similar to those seen in Parkinsons Disease and include a restlessness and inability to sit still known as akathisia
Akathisia
Akathisia, or acathisia, is a syndrome characterized by unpleasant sensations of inner restlessness that manifests itself with an inability to sit still or remain motionless...
, a slow tremor and stiffness of the limbs. Zuclopenthixol is thought to be more sedating than the related flupentixol
Flupentixol
Flupentixol , also known as flupenthixol , marketed under brand names such as Depixol and Fluanxol, is a typical antipsychotic drug of the thioxanthene class...
, though possibly less likely to induce extrapyramidal symptoms than other typical depots. As with other dopamine antagonists, zuclopenthixol may sometimes elevate prolactin
Prolactin
Prolactin also known as luteotropic hormone is a protein that in humans is encoded by the PRL gene.Prolactin is a peptide hormone discovered by Henry Friesen...
levels; this may occasionally result in amenorrhoea
Amenorrhoea
Amenorrhoea , amenorrhea , or amenorrhœa, is the absence of a menstrual period in a woman of reproductive age. Physiological states of amenorrhoea are seen during pregnancy and lactation , the latter also forming the basis of a form of contraception known as the lactational amenorrhoea method...
or galactorrhoea in severe cases. Neuroleptic malignant syndrome
Neuroleptic malignant syndrome
Neuroleptic malignant syndrome is a life- threatening neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs...
is a rare but potentially fatal side effect. Any unexpected deterioration in mental state with confusion and muscle stiffness should be seen by a physician.