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Zuclopenthixol

April 14, 2024

Zuclopenthixol (brand names Cisordinol, Clopixol and others), also known as zuclopentixol, is a medication used to treat schizophrenia and other psychoses. It is classed, pharmacologically, as a typical antipsychotic. Chemically it is a thioxanthene. It is the cis-isomer of clopenthixol (Sordinol, Ciatyl).[3] Clopenthixol was introduced in 1961, while zuclopenthixol was introduced in 1978.

Zuclopenthixol
Clinical data
Trade namesClopixol
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
  • AU: C
Routes of
administration		Oral, IM
Drug classTypical antipsychotic
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • BR: Class C1 (Other controlled substances)[2]
  • UK: POM (Prescription only)
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability49% (oral)
Protein binding98%
MetabolismLiver (CYP2D6 and CYP3A4-mediated)
Elimination half-life20 hours (oral), 19 days (IM)
ExcretionFeces
Identifiers
  • cis-(Z)-2-(4-(3-(2-chloro-9H-thioxanthen-9-ylidene)propyl)piperazin-1-yl)ethanol
CAS Number
PubChem CID
  • 5311507
DrugBank
  • DB01624 Y
ChemSpider
  • 4470984 Y
UNII
  • 47ISU063SG
KEGG
  • D03556 Y
ChEBI
  • CHEBI:51364 N
ChEMBL
  • ChEMBL53904 Y
CompTox Dashboard (EPA)
  • DTXSID3048233
ECHA InfoCard100.053.398
Chemical and physical data
FormulaC22H25ClN2OS
Molar mass400.97 g·mol−1
3D model (JSmol)
  • Interactive image
  • Clc2cc1C(\c3c(Sc1cc2)cccc3)=C/CCN4CCN(CCO)CC4
  • InChI=1S/C22H25ClN2OS/c23-17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)27-22)5-3-9-24-10-12-25(13-11-24)14-15-26/h1-2,4-8,16,26H,3,9-15H2/b18-5- Y
  • Key:WFPIAZLQTJBIFN-DVZOWYKESA-N Y
 NY (what is this?)  (verify)

Zuclopenthixol is a D1 and D2 antagonist, α1-adrenergic and 5-HT2 antagonist.[4] While it is approved for use in Australia, Canada, Ireland, India, New Zealand, Singapore, South Africa and the UK it is not approved for use in the United States.[5][6]

Medical uses edit

Available forms edit

Zuclopenthixol is available in three major preparations:

  • As zuclopenthixol decanoate (Clopixol Depot, Cisordinol Depot), it is a long-acting intramuscular injection. Its main use is as a long-acting injection given every two or three weeks to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness.[7] There is some evidence it may be more helpful in managing aggressive behaviour.[8]
  • As zuclopenthixol acetate (Clopixol-Acuphase, Cisordinol-Acutard), 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.[9]
  • As zuclopenthixol dihydrochloride (Clopixol, Cisordinol), it is a tablet used in the treatment of schizophrenia in those who are compliant with oral medication.[10]

It is also used in the treatment of acute bipolar mania.

Dosing edit

As a long-acting injection, zuclopenthixol decanoate comes in a 200 mg and 500 mg ampoule. Doses can vary from 50 mg 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 benztropine 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 2, 10, 25 and 40 mg tablets, with a dose range of 20–60 mg daily.[11]


Side effects edit

Chronic administration of zuclopenthixol (30 mg/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.

Withdrawal syndrome: Abrupt cessation of therapy may cause acute withdrawal symptoms (eg, nausea, vomiting, or insomnia). Symptoms usually begin in 1 to 4 days of withdrawal and subside within 1 to 2 weeks.[12][13]

Other permanent 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 Parkinson's disease and include a restlessness and inability to sit still known as akathisia, a slow tremor and stiffness of the limbs.[10] Zuclopenthixol is thought to be more sedating than the related flupentixol, though possibly less likely to induce extrapyramidal symptoms than other typical depots.[7] 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.

Zuclopenthixol decanoate induces a transient dose-dependent sedation. However, if the patient is switched to maintenance treatment with zuclopenthixol decanoate from oral zuclopenthixol or from i.m. zuclopenthixol acetate the sedation will be no problem. Tolerance to the unspecific sedative effect develops rapidly.[14]

Very common Adverse Effects (≥10% incidence) [15]
Common (1–10%) [15]
Uncommon (0.1–1%)[15]
Rare (0.01–0.1%)[15]
Very rare (<0.01%)[15]

Pharmacology edit

Pharmacodynamics edit

 
Cisordinol 10 mg tablet

Zuclopenthixol antagonises both dopamine D1 and D2 receptors, α1-adrenoceptors and 5-HT2 receptors with a high affinity, but has no affinity for muscarinic acetylcholine receptors. It weakly antagonises the histamine (H1) receptor but has no α2-adrenoceptor blocking activity [citation needed].

Evidence from in vitro work and clinical sources (i.e. therapeutic drug monitoring databases) suggests that both CYP2D6 and CYP3A4 play important roles in zuclopenthixol metabolism.[16]

Pharmacokinetics edit

Pharmacokinetics of long-acting injectable antipsychotics
Medication Brand name Class Vehicle Dosage Tmax t1/2 single t1/2 multiple logPc Ref
Aripiprazole lauroxil Aristada Atypical Watera 441–1064 mg/4–8 weeks 24–35 days ? 54–57 days 7.9–10.0
Aripiprazole monohydrate Abilify Maintena Atypical Watera 300–400 mg/4 weeks 7 days ? 30–47 days 4.9–5.2
Bromperidol decanoate Impromen Decanoas Typical Sesame oil 40–300 mg/4 weeks 3–9 days ? 21–25 days 7.9 [17]
Clopentixol decanoate Sordinol Depot Typical Viscoleob 50–600 mg/1–4 weeks 4–7 days ? 19 days 9.0 [18]
Flupentixol decanoate Depixol Typical Viscoleob 10–200 mg/2–4 weeks 4–10 days 8 days 17 days 7.2–9.2 [18][19]
Fluphenazine decanoate Prolixin Decanoate Typical Sesame oil 12.5–100 mg/2–5 weeks 1–2 days 1–10 days 14–100 days 7.2–9.0 [20][21][22]
Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12.5–100 mg/1–4 weeks 2–3 days 4 days ? 6.4–7.4 [21]
Fluspirilene Imap, Redeptin Typical Watera 2–12 mg/1 week 1–8 days 7 days ? 5.2–5.8 [23]
Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20–400 mg/2–4 weeks 3–9 days 18–21 days 7.2–7.9 [24][25]
Olanzapine pamoate Zyprexa Relprevv Atypical Watera 150–405 mg/2–4 weeks 7 days ? 30 days –
Oxyprothepin decanoate Meclopin Typical ? ? ? ? ? 8.5–8.7
Paliperidone palmitate Invega Sustenna Atypical Watera 39–819 mg/4–12 weeks 13–33 days 25–139 days ? 8.1–10.1
Perphenazine decanoate Trilafon Dekanoat Typical Sesame oil 50–200 mg/2–4 weeks ? ? 27 days 8.9
Perphenazine enanthate Trilafon Enanthate Typical Sesame oil 25–200 mg/2 weeks 2–3 days ? 4–7 days 6.4–7.2 [26]
Pipotiazine palmitate Piportil Longum Typical Viscoleob 25–400 mg/4 weeks 9–10 days ? 14–21 days 8.5–11.6 [19]
Pipotiazine undecylenate Piportil Medium Typical Sesame oil 100–200 mg/2 weeks ? ? ? 8.4
Risperidone Risperdal Consta Atypical Microspheres 12.5–75 mg/2 weeks 21 days ? 3–6 days –
Zuclopentixol acetate Clopixol Acuphase Typical Viscoleob 50–200 mg/1–3 days 1–2 days 1–2 days 4.7–4.9
Zuclopentixol decanoate Clopixol Depot Typical Viscoleob 50–800 mg/2–4 weeks 4–9 days ? 11–21 days 7.5–9.0
Note: All by intramuscular injection. Footnotes: a = Microcrystalline or nanocrystalline aqueous suspension. b = Low-viscosity vegetable oil (specifically fractionated coconut oil with medium-chain triglycerides). c = Predicted, from PubChem and DrugBank. Sources: Main: See template.

History edit

Zuclopenthixol was introduced by Lundbeck in 1978.[27]

References edit

  1. ^ "Clopixol (Zuclopenthixol Hydrochloride) Film-coated tablets". Australian Product Information. Australia: The Therapeutics Goods Administration. from the original on 2018-06-15. Retrieved 2013-08-08.
  2. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). from the original on 2023-08-03. Retrieved 2023-08-16.
  3. ^ Sneader, Walter (2005). Drug discovery: a history. New York: Wiley. p. 410. ISBN 0-471-89980-1. from the original on 2023-04-29. Retrieved 2020-10-07.
  4. ^ Christensen AV, Arnt J, Hyttel J, Larsen JJ, Svendsen O (April 1984). "Pharmacological effects of a specific dopamine D-1 antagonist SCH 23390 in comparison with neuroleptics". Life Sciences. 34 (16): 1529–1540. doi:10.1016/0024-3205(84)90607-6. PMID 6144029.
  5. ^ Green AI, Noordsy DL, Brunette MF, O'Keefe C (January 2008). "Substance abuse and schizophrenia: pharmacotherapeutic intervention". Journal of Substance Abuse Treatment. 34 (1): 61–71. doi:10.1016/j.jsat.2007.01.008. PMC 2930488. PMID 17574793.
  6. ^ Sweetman, Sean C., ed. (2009). "Anxiolytic Sedatives Hypnotics and Antipsychotics". Martindale: The complete drug reference (36th ed.). London: Pharmaceutical Press. pp. 1040–1. ISBN 978-0-85369-840-1.
  7. ^ a b da Silva Freire Coutinho E, Fenton M, Quraishi SN (1999). "Zuclopenthixol decanoate for schizophrenia". The Cochrane Database of Systematic Reviews. 1999 (2). John Wiley and Sons, Ltd.: CD001164. doi:10.1002/14651858.CD001164. PMC 7032616. PMID 10796607. from the original on 2007-06-13. Retrieved 2007-06-12.
  8. ^ Haessler F, Glaser T, Beneke M, Pap AF, Bodenschatz R, Reis O (2007). "Zuclopenthixol in adults with intellectual disabilities and aggressive behaviours". British Journal of Psychiatry. 190 (5): 447–448. doi:10.1192/bjp.bp.105.016535. PMID 17470962.
  9. ^ Lundbeck P/L (1991). "Clopixol Acuphase 50 mg/mL Injection Clopixol Acuphase 100 mg / 2 mL Injection". Lundbeck P/L. from the original on 2007-06-09. Retrieved 2007-06-12.
  10. ^ a b Bryan EJ, Purcell MA, Kumar A (November 2017). "Zuclopenthixol dihydrochloride for schizophrenia". The Cochrane Database of Systematic Reviews. 2017 (11): CD005474. doi:10.1002/14651858.CD005474.pub2. PMC 6486001. PMID 29144549.
  11. ^ "Clopixol 2 mg film-coated tablets - Summary of Product Characteristics (SmPC) - (emc)". www.medicines.org.uk. from the original on 2023-03-28. Retrieved 2023-03-28.
  12. ^ [1]
  13. ^ [2]
  14. ^ "Summary of Product Characteristics" (PDF). (PDF) from the original on 2017-03-28. Retrieved 2017-03-28.
  15. ^ a b c d e "TGA eBS - Product and Consumer Medicine Information Licence". from the original on 2018-06-15. Retrieved 2013-08-08.
  16. ^ Davies SJ, Westin AA, Castberg I, Lewis G, Lennard MS, Taylor S, Spigset O (2010). "Characterisation of zuclopenthixol metabolism by in vitro and therapeutic drug monitoring studies". Acta Psychiatrica Scandinavica. 122 (6): 445–453. doi:10.1111/j.1600-0447.2010.01619.x. PMID 20946203. S2CID 41869401.
  17. ^ Parent M, Toussaint C, Gilson H (1983). "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation". Current Therapeutic Research. 34 (1): 1–6.
  18. ^ a b Jørgensen A, Overø KF (1980). "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum. 279: 41–54. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472.
  19. ^ a b Reynolds JE (1993). "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. pp. 364–623.
  20. ^ Ereshefsky L, Saklad SR, Jann MW, Davis CM, Richards A, Seidel DR (May 1984). "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry. 45 (5 Pt 2): 50–9. PMID 6143748.
  21. ^ a b Curry SH, Whelpton R, de Schepper PJ, Vranckx S, Schiff AA (April 1979). "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology. 7 (4): 325–31. doi:10.1111/j.1365-2125.1979.tb00941.x. PMC 1429660. PMID 444352.
  22. ^ Young D, Ereshefsky L, Saklad SR, Jann MW, Garcia N (1984). Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.). 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists. Dallas, Texas.
  23. ^ Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (November 1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung. 20 (11): 1689–98. PMID 4992598.
  24. ^ Beresford R, Ward A (January 1987). "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs. 33 (1): 31–49. doi:10.2165/00003495-198733010-00002. PMID 3545764.
  25. ^ Reyntigens AJ, Heykants JJ, Woestenborghs RJ, Gelders YG, Aerts TJ (1982). "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry. 17 (4): 238–46. doi:10.1159/000468580. PMID 7185768.
  26. ^ Larsson M, Axelsson R, Forsman A (1984). "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate". Current Therapeutic Research. 36 (6): 1071–88.
  27. ^ William Andrew Publishing (22 October 2013). Pharmaceutical Manufacturing Encyclopedia. Elsevier. pp. 1102–. ISBN 978-0-8155-1856-3. from the original on 14 January 2023. Retrieved 27 September 2017.

April 14, 2024
zuclopenthixol, brand, names, cisordinol, clopixol, others, also, known, zuclopentixol, medication, used, treat, schizophrenia, other, psychoses, classed, pharmacologically, typical, antipsychotic, chemically, thioxanthene, isomer, clopenthixol, sordinol, ciat. Zuclopenthixol brand names Cisordinol Clopixol and others also known as zuclopentixol is a medication used to treat schizophrenia and other psychoses It is classed pharmacologically as a typical antipsychotic Chemically it is a thioxanthene It is the cis isomer of clopenthixol Sordinol Ciatyl 3 Clopenthixol was introduced in 1961 while zuclopenthixol was introduced in 1978 ZuclopenthixolClinical dataTrade namesClopixolAHFS Drugs comInternational Drug NamesPregnancycategoryAU CRoutes ofadministrationOral IMDrug classTypical antipsychoticATC codeN05AF05 WHO Legal statusLegal statusAU S4 Prescription only 1 BR Class C1 Other controlled substances 2 UK POM Prescription only In general Prescription only Pharmacokinetic dataBioavailability49 oral Protein binding98 MetabolismLiver CYP2D6 and CYP3A4 mediated Elimination half life20 hours oral 19 days IM ExcretionFecesIdentifiersIUPAC name cis Z 2 4 3 2 chloro 9H thioxanthen 9 ylidene propyl piperazin 1 yl ethanolCAS Number53772 83 1 Y 85721 05 7 acetate 64053 00 5 decanoate PubChem CID5311507DrugBankDB01624 YChemSpider4470984 YUNII47ISU063SGKEGGD03556 YChEBICHEBI 51364 NChEMBLChEMBL53904 YCompTox Dashboard EPA DTXSID3048233ECHA InfoCard100 053 398Chemical and physical dataFormulaC 22H 25Cl N 2O SMolar mass400 97 g mol 13D model JSmol Interactive imageSMILES Clc2cc1C c3c Sc1cc2 cccc3 C CCN4CCN CCO CC4InChI InChI 1S C22H25ClN2OS c23 17 7 8 22 20 16 17 18 19 4 1 2 6 21 19 27 22 5 3 9 24 10 12 25 13 11 24 14 15 26 h1 2 4 8 16 26H 3 9 15H2 b18 5 YKey WFPIAZLQTJBIFN DVZOWYKESA N Y N Y what is this verify Zuclopenthixol is a D1 and D2 antagonist a1 adrenergic and 5 HT2 antagonist 4 While it is approved for use in Australia Canada Ireland India New Zealand Singapore South Africa and the UK it is not approved for use in the United States 5 6 Contents 1 Medical uses 1 1 Available forms 1 2 Dosing 2 Side effects 3 Pharmacology 3 1 Pharmacodynamics 3 2 Pharmacokinetics 4 History 5 ReferencesMedical uses editAvailable forms edit Zuclopenthixol is available in three major preparations As zuclopenthixol decanoate Clopixol Depot Cisordinol Depot it is a long acting intramuscular injection Its main use is as a long acting injection given every two or three weeks to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness 7 There is some evidence it may be more helpful in managing aggressive behaviour 8 As zuclopenthixol acetate Clopixol Acuphase Cisordinol Acutard 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 9 As zuclopenthixol dihydrochloride Clopixol Cisordinol it is a tablet used in the treatment of schizophrenia in those who are compliant with oral medication 10 It is also used in the treatment of acute bipolar mania Dosing edit As a long acting injection zuclopenthixol decanoate comes in a 200 mg and 500 mg ampoule Doses can vary from 50 mg 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 benztropine 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 2 10 25 and 40 mg tablets with a dose range of 20 60 mg daily 11 Side effects editChronic administration of zuclopenthixol 30 mg 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 Withdrawal syndrome Abrupt cessation of therapy may cause acute withdrawal symptoms eg nausea vomiting or insomnia Symptoms usually begin in 1 to 4 days of withdrawal and subside within 1 to 2 weeks 12 13 Other permanent 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 Parkinson s disease and include a restlessness and inability to sit still known as akathisia a slow tremor and stiffness of the limbs 10 Zuclopenthixol is thought to be more sedating than the related flupentixol though possibly less likely to induce extrapyramidal symptoms than other typical depots 7 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 Zuclopenthixol decanoate induces a transient dose dependent sedation However if the patient is switched to maintenance treatment with zuclopenthixol decanoate from oral zuclopenthixol or from i m zuclopenthixol acetate the sedation will be no problem Tolerance to the unspecific sedative effect develops rapidly 14 Very common Adverse Effects 10 incidence 15 Dry Mouth Somnolence Akathisia Hyperkinesia HypokinesiaCommon 1 10 15 Tachycardia Heart palpitations Vertigo Accommodation disorder Abnormal vision Salivary hypersecretion Constipation Vomiting Dyspepsia Diarrhoea Asthenia Fatigue Malaise Pain at the injection site Increased appetite Weight gain Myalgia Tremor Dystonia Hypertonia Dizziness Headache Paraesthesia Disturbance in attention Amnesia Abnormal gait Insomnia Depression Anxiety Abnormal dreams Agitation Decreased libido Nasal congestion Dyspnoea Hyperhidrosis PruritusUncommon 0 1 1 15 Hyperacusis Tinnitus Mydriasis Abdominal pain Nausea Flatulence Thirst Injection site reaction Hypothermia Pyrexia Abnormal liver function tests Decreased appetite Weight loss Muscle rigidity Trismus Torticollis Tardive dyskinesia Hyperreflexia Dyskinesia Parkinsonism Syncope Ataxia Speech disorder Hypotonia Convulsion Migraine Apathy Nightmares Libido increased Confused state Ejaculation failure Erectile dysfunction Female orgasmic disorder Vulvovaginal Dryness Rash Photosensitivity Pigmentation disorder Seborrhoea Dermatitis Purpura Hypotension Hot flushRare 0 01 0 1 15 Thrombocytopenia Neutropenia Leukopenia Agranulocytosis QT prolongation Hyperprolactinaemia Hypersensitivity Anaphylactic reaction Hyperglycaemia Glucose tolerance impaired Hyperlipidaemia Gynaecomastia Galactorrhoea Amenorrhoea Priapism Withdrawal symptomsVery rare lt 0 01 15 Cholestatic hepatitis Jaundice Neuroleptic malignant syndrome Venous thromboembolismPharmacology editPharmacodynamics edit nbsp Cisordinol 10 mg tabletZuclopenthixol antagonises both dopamine D1 and D2 receptors a1 adrenoceptors and 5 HT2 receptors with a high affinity but has no affinity for muscarinic acetylcholine receptors It weakly antagonises the histamine H1 receptor but has no a2 adrenoceptor blocking activity citation needed Evidence from in vitro work and clinical sources i e therapeutic drug monitoring databases suggests that both CYP2D6 and CYP3A4 play important roles in zuclopenthixol metabolism 16 Pharmacokinetics edit vte Pharmacokinetics of long acting injectable antipsychotics Medication Brand name Class Vehicle Dosage Tmax t1 2 single t1 2 multiple logPc RefAripiprazole lauroxil Aristada Atypical Watera 441 1064 mg 4 8 weeks 24 35 days 54 57 days 7 9 10 0Aripiprazole monohydrate Abilify Maintena Atypical Watera 300 400 mg 4 weeks 7 days 30 47 days 4 9 5 2Bromperidol decanoate Impromen Decanoas Typical Sesame oil 40 300 mg 4 weeks 3 9 days 21 25 days 7 9 17 Clopentixol decanoate Sordinol Depot Typical Viscoleob 50 600 mg 1 4 weeks 4 7 days 19 days 9 0 18 Flupentixol decanoate Depixol Typical Viscoleob 10 200 mg 2 4 weeks 4 10 days 8 days 17 days 7 2 9 2 18 19 Fluphenazine decanoate Prolixin Decanoate Typical Sesame oil 12 5 100 mg 2 5 weeks 1 2 days 1 10 days 14 100 days 7 2 9 0 20 21 22 Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12 5 100 mg 1 4 weeks 2 3 days 4 days 6 4 7 4 21 Fluspirilene Imap Redeptin Typical Watera 2 12 mg 1 week 1 8 days 7 days 5 2 5 8 23 Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20 400 mg 2 4 weeks 3 9 days 18 21 days 7 2 7 9 24 25 Olanzapine pamoate Zyprexa Relprevv Atypical Watera 150 405 mg 2 4 weeks 7 days 30 days Oxyprothepin decanoate Meclopin Typical 8 5 8 7Paliperidone palmitate Invega Sustenna Atypical Watera 39 819 mg 4 12 weeks 13 33 days 25 139 days 8 1 10 1Perphenazine decanoate Trilafon Dekanoat Typical Sesame oil 50 200 mg 2 4 weeks 27 days 8 9Perphenazine enanthate Trilafon Enanthate Typical Sesame oil 25 200 mg 2 weeks 2 3 days 4 7 days 6 4 7 2 26 Pipotiazine palmitate Piportil Longum Typical Viscoleob 25 400 mg 4 weeks 9 10 days 14 21 days 8 5 11 6 19 Pipotiazine undecylenate Piportil Medium Typical Sesame oil 100 200 mg 2 weeks 8 4Risperidone Risperdal Consta Atypical Microspheres 12 5 75 mg 2 weeks 21 days 3 6 days Zuclopentixol acetate Clopixol Acuphase Typical Viscoleob 50 200 mg 1 3 days 1 2 days 1 2 days 4 7 4 9Zuclopentixol decanoate Clopixol Depot Typical Viscoleob 50 800 mg 2 4 weeks 4 9 days 11 21 days 7 5 9 0Note All by intramuscular injection Footnotes a Microcrystalline or nanocrystalline aqueous suspension b Low viscosity vegetable oil specifically fractionated coconut oil with medium chain triglycerides c Predicted from PubChem and DrugBank Sources Main See template History editZuclopenthixol was introduced by Lundbeck in 1978 27 References edit Clopixol Zuclopenthixol Hydrochloride Film coated tablets Australian Product Information Australia The Therapeutics Goods Administration Archived from the original on 2018 06 15 Retrieved 2013 08 08 Anvisa 2023 03 31 RDC Nº 784 Listas de Substancias Entorpecentes Psicotropicas Precursoras e Outras sob Controle Especial Collegiate Board Resolution No 784 Lists of Narcotic Psychotropic Precursor and Other Substances under Special Control in Brazilian Portuguese Diario Oficial da Uniao published 2023 04 04 Archived from the original on 2023 08 03 Retrieved 2023 08 16 Sneader Walter 2005 Drug discovery a history New York Wiley p 410 ISBN 0 471 89980 1 Archived from the original on 2023 04 29 Retrieved 2020 10 07 Christensen AV Arnt J Hyttel J Larsen JJ Svendsen O April 1984 Pharmacological effects of a specific dopamine D 1 antagonist SCH 23390 in comparison with neuroleptics Life Sciences 34 16 1529 1540 doi 10 1016 0024 3205 84 90607 6 PMID 6144029 Green AI Noordsy DL Brunette MF O Keefe C January 2008 Substance abuse and schizophrenia pharmacotherapeutic intervention Journal of Substance Abuse Treatment 34 1 61 71 doi 10 1016 j jsat 2007 01 008 PMC 2930488 PMID 17574793 Sweetman Sean C ed 2009 Anxiolytic Sedatives Hypnotics and Antipsychotics Martindale The complete drug reference 36th ed London Pharmaceutical Press pp 1040 1 ISBN 978 0 85369 840 1 a b da Silva Freire Coutinho E Fenton M Quraishi SN 1999 Zuclopenthixol decanoate for schizophrenia The Cochrane Database of Systematic Reviews 1999 2 John Wiley and Sons Ltd CD001164 doi 10 1002 14651858 CD001164 PMC 7032616 PMID 10796607 Archived from the original on 2007 06 13 Retrieved 2007 06 12 Haessler F Glaser T Beneke M Pap AF Bodenschatz R Reis O 2007 Zuclopenthixol in adults with intellectual disabilities and aggressive behaviours British Journal of Psychiatry 190 5 447 448 doi 10 1192 bjp bp 105 016535 PMID 17470962 Lundbeck P L 1991 Clopixol Acuphase 50 mg mL Injection Clopixol Acuphase 100 mg 2 mL Injection Lundbeck P L Archived from the original on 2007 06 09 Retrieved 2007 06 12 a b Bryan EJ Purcell MA Kumar A November 2017 Zuclopenthixol dihydrochloride for schizophrenia The Cochrane Database of Systematic Reviews 2017 11 CD005474 doi 10 1002 14651858 CD005474 pub2 PMC 6486001 PMID 29144549 Clopixol 2 mg film coated tablets Summary of Product Characteristics SmPC emc www medicines org uk Archived from the original on 2023 03 28 Retrieved 2023 03 28 1 2 Summary of Product Characteristics PDF Archived PDF from the original on 2017 03 28 Retrieved 2017 03 28 a b c d e TGA eBS Product and Consumer Medicine Information Licence Archived from the original on 2018 06 15 Retrieved 2013 08 08 Davies SJ Westin AA Castberg I Lewis G Lennard MS Taylor S Spigset O 2010 Characterisation of zuclopenthixol metabolism by in vitro and therapeutic drug monitoring studies Acta Psychiatrica Scandinavica 122 6 445 453 doi 10 1111 j 1600 0447 2010 01619 x PMID 20946203 S2CID 41869401 Parent M Toussaint C Gilson H 1983 Long term treatment of chronic psychotics with bromperidol decanoate clinical and pharmacokinetic evaluation Current Therapeutic Research 34 1 1 6 a b Jorgensen A Overo KF 1980 Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics III Serum levels Acta Psychiatrica Scandinavica Supplementum 279 41 54 doi 10 1111 j 1600 0447 1980 tb07082 x PMID 6931472 a b Reynolds JE 1993 Anxiolytic sedatives hypnotics and neuroleptics Martindale The Extra Pharmacopoeia 30th ed London Pharmaceutical Press pp 364 623 Ereshefsky L Saklad SR Jann MW Davis CM Richards A Seidel DR May 1984 Future of depot neuroleptic therapy pharmacokinetic and pharmacodynamic approaches The Journal of Clinical Psychiatry 45 5 Pt 2 50 9 PMID 6143748 a b Curry SH Whelpton R de Schepper PJ Vranckx S Schiff AA April 1979 Kinetics of fluphenazine after fluphenazine dihydrochloride enanthate and decanoate administration to man British Journal of Clinical Pharmacology 7 4 325 31 doi 10 1111 j 1365 2125 1979 tb00941 x PMC 1429660 PMID 444352 Young D Ereshefsky L Saklad SR Jann MW Garcia N 1984 Explaining the pharmacokinetics of fluphenazine through computer simulations Abstract 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists Dallas Texas Janssen PA Niemegeers CJ Schellekens KH Lenaerts FM Verbruggen FJ van Nueten JM Marsboom RH Herin VV Schaper WK November 1970 The pharmacology of fluspirilene R 6218 a potent long acting and injectable neuroleptic drug Arzneimittel Forschung 20 11 1689 98 PMID 4992598 Beresford R Ward A January 1987 Haloperidol decanoate A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis Drugs 33 1 31 49 doi 10 2165 00003495 198733010 00002 PMID 3545764 Reyntigens AJ Heykants JJ Woestenborghs RJ Gelders YG Aerts TJ 1982 Pharmacokinetics of haloperidol decanoate A 2 year follow up International Pharmacopsychiatry 17 4 238 46 doi 10 1159 000468580 PMID 7185768 Larsson M Axelsson R Forsman A 1984 On the pharmacokinetics of perphenazine a clinical study of perphenazine enanthate and decanoate Current Therapeutic Research 36 6 1071 88 William Andrew Publishing 22 October 2013 Pharmaceutical Manufacturing Encyclopedia Elsevier pp 1102 ISBN 978 0 8155 1856 3 Archived from the original on 14 January 2023 Retrieved 27 September 2017 Retrieved from https en wikipedia org w index php title Zuclopenthixol amp oldid 1215879481, 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