Zuclopenthixol (marketed as
Cisordinol,
Clopixol or
Acuphase) is a
typical antipsychoticTypical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis...
neuroleptic
drugA 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
thioxantheneThioxanthene is a molecule in which the oxygen atom in xanthene is replaced with a sulfur atom. Various thioxanthene derivatives are used in the treatment of schizophrenia and psychosis...
group. It mainly acts by
antagonismA 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 D
1 and D
2 dopamineDopamine is a neurotransmitter occurring in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this phenethylamine functions as a neurotransmitter, activating the five types of dopamine receptors — D
1, D
2, D
3, D
4, and...
receptorsDopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system . The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors....
, though it also has some
antihistamineAn H
1 antagonist is a histamine antagonist of the H
1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
activity. It is produced and marketed by
LundbeckH. 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 psychiatric and neurological disorders, particularly fast-working, non-addictive anti-depressants for people who need to function...
pharmaceutical company.
It is available in three forms:
- As zuclopenthixol decanoate (Clopixol), it is a long acting intramuscular injection.
Zuclopenthixol (marketed as
Cisordinol,
Clopixol or
Acuphase) is a
typical antipsychoticTypical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis...
neuroleptic
drugA 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
thioxantheneThioxanthene is a molecule in which the oxygen atom in xanthene is replaced with a sulfur atom. Various thioxanthene derivatives are used in the treatment of schizophrenia and psychosis...
group. It mainly acts by
antagonismA 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 D
1 and D
2 dopamineDopamine is a neurotransmitter occurring in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this phenethylamine functions as a neurotransmitter, activating the five types of dopamine receptors — D
1, D
2, D
3, D
4, and...
receptorsDopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system . The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors....
, though it also has some
antihistamineAn H
1 antagonist is a histamine antagonist of the H
1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
activity. It is produced and marketed by
LundbeckH. 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 psychiatric and neurological disorders, particularly fast-working, non-addictive anti-depressants for people who need to function...
pharmaceutical company.
It is available in three forms:
- As zuclopenthixol decanoate (Clopixol), it is a long acting intramuscular injection. Its main use is as a long acting injection given two or three weekly to people with schizophrenia
Schizophrenia , from the Greek roots skhizein and phrēn, phren- is a psychiatric diagnosis that describes a mental disorder characterized by abnormalities in the perception or expression of reality...
who have a poor compliance with medication and suffer frequent relapses of illness. In some countries this can be involuntary under Community Treatment Orders. 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 tablets), it is a tablet used in the treatment of schizophrenia
Schizophrenia , from the Greek roots skhizein and phrēn, phren- is a psychiatric diagnosis that describes a mental disorder characterized by abnormalities in the perception or expression of reality...
in those who are compliant with oral medication.
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 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
akathisiaAkathisia, 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
flupentixolFlupentixol or flupenthixol , marketed as Depixol and Fluanxol, is a typical antipsychotic drug. It is a thioxanthene, and therefore closely related to the phenothiazines...
, though possibly less likely to induce extrapyramidal symptoms than other typical depots. As with other dopamine antagonists, zuclopenthixol may sometimes elevate
prolactinProlactin or Luteotropic hormone is a peptide hormone discovered by Dr. Henry Friesen, primarily associated with lactation. In breastfeeding, the act of an infant suckling the nipple stimulates the production of prolactin, which fills the breast with milk via a process called lactogenesis, in...
levels; this may occasionally result in
amenorrhoeaAmenorrhoea , 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 amenorrhea method...
or galactorrhoea in severe cases.
Neuroleptic malignant syndromeNeuroleptic malignant syndrome is a neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs. It generally presents with muscle rigidity, fever, autonomic instability and cognitive changes such as delirium, and is associated with elevated creatine...
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.
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 in side effects occur, though in the short term an anticholinergic medication
benztropineBenztropine mesilate , benztropine mesylate, or benztropine marketed as Cogentin, is an anticholinergic drug principally used for the treatment of:*Drug-induced parkinsonism, akathisia and acute dystonia;*Parkinson disease; and...
may be helpful for tremor and stiffness, while
diazepamDiazepam , first marketed as Valium by Hoffmann-La Roche, is a benzodiazepine derivative drug. It possesses anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnestic properties. It is commonly used for treating anxiety, insomnia, seizures, muscle spasms, restless legs...
may be helpful for akathisia. 100 mg of zuclopenthixol decanoate is roughly equivalent to 20 mg of flupentixol decanoate or 12.5 mg of
fluphenazineFluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia and acute manic phases of bipolar disorder...
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.