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Not to be confused with clonazepam or clonidine.
Mr. Ibrahem/Clozapine
Skeletal formula of clozapine
Stick-and-ball model of the clozapine molecule
Clinical data
Trade namesClozaril, Leponex, Versacloz, others [1]
AHFS/ Drugs.com Monograph
MedlinePlus a691001
License data
Pregnancy
category
  • AU: C
Routes of
administration		 By mouth, intramuscular injection
Drug class Atypical antipsychotic [2]
Legal status
Legal status
Pharmacokinetic data
Bioavailability60 to 70%
Metabolism Liver, by several CYP isozymes
Elimination half-life4 to 26 hours (mean value 14.2 hours in steady state conditions)
Excretion80% in metabolized state: 30% biliary and 50% kidney
Identifiers
  • 8-Chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Chemical and physical data
FormulaC18H19ClN4
Molar mass326.83 g·mol−1
3D model ( JSmol)
Melting point183 °C (361 °F)
Solubility in water0.1889 [3] mg/mL (20 °C)
  • CN1CCN(CC1)C2=Nc3cc(ccc3Nc4c2cccc4)Cl
  • InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3 checkY
  • Key:QZUDBNBUXVUHMW-UHFFFAOYSA-N checkY
   (verify)

Clozapine, sold under the brand name Clozaril among others, [1] is an atypical antipsychotic medication. [2] It is mainly used for schizophrenia that does not improve following the use of other antipsychotic medications. [2] In those with schizophrenia and schizoaffective disorder it may decrease the rate of suicidal behavior. [2] It is more effective than typical antipsychotics, particularly in those who are treatment-resistant. [5] [6] [7] It is used by mouth, [2] or by injection into a muscle. [8]

Clozapine is associated with a relatively high risk of low white cells (agranulocytosis), a condition of suppressed immunity which may result in death. [2] To decrease this risk, it is recommended that the white blood cell count be regularly monitored. [2] Other serious risks include seizures, inflammation of the heart, high blood sugar levels, constipation, and in older people with psychosis as a result of dementia, an increased risk of death. [2] [9] [10] Common side effects include drowsiness, increased saliva production, low blood pressure, blurred vision, and dizziness. [2] The potentially permanent movement disorder tardive dyskinesia occurs in about 5% of people. [9] Its mechanism of action is not entirely clear. [2]

Clozapine was first made in 1956, and sold commercially in 1972. [11] [12] It was the first atypical antipsychotic. [13] It is on the World Health Organization's List of Essential Medicines. [14] It is available as a generic medication. [2] The wholesale cost in the developing world is between US$0.05 and US$2.10 per day as of 2014. [15]

References

  1. ^ a b Cite error: The named reference brands was invoked but never defined (see the help page).
  2. ^ a b c d e f g h i j k l m n "Clozapine". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved 1 December 2015.
  3. ^ Hopfinger A, Esposito EX, Llinas A, Glen RC, Goodman JM (2009). "Findings of the Challenge To Predict Aqueous Solubility". Journal of Chemical Information and Modeling. 49 (1): 1–5. doi: 10.1021/ci800436c. PMID  19117422.
  4. ^ Cite error: The named reference WHO2020DDD was invoked but never defined (see the help page).
  5. ^ Leucht S, Cipriani A, Spineli L, Mavridis D, Orey D, Richter F, et al. (September 2013). "Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta-analysis". Lancet. 382 (9896): 951–62. doi: 10.1016/S0140-6736(13)60733-3. PMID  23810019.
  6. ^ Essali A, Al-Haj Haasan N, Li C, Rathbone J (January 2009). "Clozapine versus typical neuroleptic medication for schizophrenia". The Cochrane Database of Systematic Reviews (1): CD000059. doi: 10.1002/14651858.CD000059.pub2. PMC  7065592. PMID  19160174.
  7. ^ Siskind D, McCartney L, Goldschlager R, Kisely S (November 2016). "Clozapine v. first- and second-generation antipsychotics in treatment-refractory schizophrenia: systematic review and meta-analysis". The British Journal of Psychiatry. 209 (5): 385–392. doi: 10.1192/bjp.bp.115.177261. PMID  27388573.
  8. ^ Hewitt, Jed; Haste, Jules (April 2017). "Protocol for the use of intramuscular (IM) clozapine injection" (PDF). Sussex Partnership NHS Foundation Trust. Archived (PDF) from the original on 29 August 2021. Retrieved 2019-03-15.
  9. ^ a b Hartling L, Abou-Setta AM, Dursun S, Mousavi SS, Pasichnyk D, Newton AS (October 2012). "Antipsychotics in adults with schizophrenia: comparative effectiveness of first-generation versus second-generation medications: a systematic review and meta-analysis". Annals of Internal Medicine. 157 (7): 498–511. doi: 10.7326/0003-4819-157-7-201210020-00525. PMID  22893011.
  10. ^ "Clozaril, Fazaclo ODT, Versacloz (clozapine): Drug Safety Communication - FDA Strengthens Warning That Untreated Constipation Can Lead to Serious Bowel Problems". FDA. 28 January 2020. Archived from the original on 24 February 2020. Retrieved 30 January 2020.
  11. ^ Haidary, HA; Padhy, RK (January 2019). "Clozapine". PMID  30571020. {{ cite journal}}: Cite journal requires |journal= ( help)
  12. ^ Crilly J (March 2007). "The history of clozapine and its emergence in the US market: a review and analysis". History of Psychiatry. 18 (1): 39–60. doi: 10.1177/0957154X07070335. PMID  17580753.
  13. ^ Li JJ, Corey JJ, eds. (2013). "Chapter 7: CNS Drugs". Drug discovery practices, processes, and perspectives. Hoboken, N.J.: John Wiley & Sons. p. 248. ISBN  9781118354469. Archived from the original on 10 September 2019. Retrieved 30 August 2017.
  14. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl: 10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  15. ^ "Clozapine". International Drug Price Indicator Guide. Archived from the original on 22 January 2018. Retrieved 2 December 2015.
Retrieved from " https://en.wikipedia.org/?title=User:Mr._Ibrahem/Clozapine&oldid=1233778152"
From Wikipedia, the free encyclopedia
Not to be confused with clonazepam or clonidine.
Mr. Ibrahem/Clozapine
Skeletal formula of clozapine
Stick-and-ball model of the clozapine molecule
Clinical data
Trade namesClozaril, Leponex, Versacloz, others [1]
AHFS/ Drugs.com Monograph
MedlinePlus a691001
License data
Pregnancy
category
  • AU: C
Routes of
administration		 By mouth, intramuscular injection
Drug class Atypical antipsychotic [2]
Legal status
Legal status
Pharmacokinetic data
Bioavailability60 to 70%
Metabolism Liver, by several CYP isozymes
Elimination half-life4 to 26 hours (mean value 14.2 hours in steady state conditions)
Excretion80% in metabolized state: 30% biliary and 50% kidney
Identifiers
  • 8-Chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Chemical and physical data
FormulaC18H19ClN4
Molar mass326.83 g·mol−1
3D model ( JSmol)
Melting point183 °C (361 °F)
Solubility in water0.1889 [3] mg/mL (20 °C)
  • CN1CCN(CC1)C2=Nc3cc(ccc3Nc4c2cccc4)Cl
  • InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3 checkY
  • Key:QZUDBNBUXVUHMW-UHFFFAOYSA-N checkY
   (verify)

Clozapine, sold under the brand name Clozaril among others, [1] is an atypical antipsychotic medication. [2] It is mainly used for schizophrenia that does not improve following the use of other antipsychotic medications. [2] In those with schizophrenia and schizoaffective disorder it may decrease the rate of suicidal behavior. [2] It is more effective than typical antipsychotics, particularly in those who are treatment-resistant. [5] [6] [7] It is used by mouth, [2] or by injection into a muscle. [8]

Clozapine is associated with a relatively high risk of low white cells (agranulocytosis), a condition of suppressed immunity which may result in death. [2] To decrease this risk, it is recommended that the white blood cell count be regularly monitored. [2] Other serious risks include seizures, inflammation of the heart, high blood sugar levels, constipation, and in older people with psychosis as a result of dementia, an increased risk of death. [2] [9] [10] Common side effects include drowsiness, increased saliva production, low blood pressure, blurred vision, and dizziness. [2] The potentially permanent movement disorder tardive dyskinesia occurs in about 5% of people. [9] Its mechanism of action is not entirely clear. [2]

Clozapine was first made in 1956, and sold commercially in 1972. [11] [12] It was the first atypical antipsychotic. [13] It is on the World Health Organization's List of Essential Medicines. [14] It is available as a generic medication. [2] The wholesale cost in the developing world is between US$0.05 and US$2.10 per day as of 2014. [15]

References

  1. ^ a b Cite error: The named reference brands was invoked but never defined (see the help page).
  2. ^ a b c d e f g h i j k l m n "Clozapine". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved 1 December 2015.
  3. ^ Hopfinger A, Esposito EX, Llinas A, Glen RC, Goodman JM (2009). "Findings of the Challenge To Predict Aqueous Solubility". Journal of Chemical Information and Modeling. 49 (1): 1–5. doi: 10.1021/ci800436c. PMID  19117422.
  4. ^ Cite error: The named reference WHO2020DDD was invoked but never defined (see the help page).
  5. ^ Leucht S, Cipriani A, Spineli L, Mavridis D, Orey D, Richter F, et al. (September 2013). "Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta-analysis". Lancet. 382 (9896): 951–62. doi: 10.1016/S0140-6736(13)60733-3. PMID  23810019.
  6. ^ Essali A, Al-Haj Haasan N, Li C, Rathbone J (January 2009). "Clozapine versus typical neuroleptic medication for schizophrenia". The Cochrane Database of Systematic Reviews (1): CD000059. doi: 10.1002/14651858.CD000059.pub2. PMC  7065592. PMID  19160174.
  7. ^ Siskind D, McCartney L, Goldschlager R, Kisely S (November 2016). "Clozapine v. first- and second-generation antipsychotics in treatment-refractory schizophrenia: systematic review and meta-analysis". The British Journal of Psychiatry. 209 (5): 385–392. doi: 10.1192/bjp.bp.115.177261. PMID  27388573.
  8. ^ Hewitt, Jed; Haste, Jules (April 2017). "Protocol for the use of intramuscular (IM) clozapine injection" (PDF). Sussex Partnership NHS Foundation Trust. Archived (PDF) from the original on 29 August 2021. Retrieved 2019-03-15.
  9. ^ a b Hartling L, Abou-Setta AM, Dursun S, Mousavi SS, Pasichnyk D, Newton AS (October 2012). "Antipsychotics in adults with schizophrenia: comparative effectiveness of first-generation versus second-generation medications: a systematic review and meta-analysis". Annals of Internal Medicine. 157 (7): 498–511. doi: 10.7326/0003-4819-157-7-201210020-00525. PMID  22893011.
  10. ^ "Clozaril, Fazaclo ODT, Versacloz (clozapine): Drug Safety Communication - FDA Strengthens Warning That Untreated Constipation Can Lead to Serious Bowel Problems". FDA. 28 January 2020. Archived from the original on 24 February 2020. Retrieved 30 January 2020.
  11. ^ Haidary, HA; Padhy, RK (January 2019). "Clozapine". PMID  30571020. {{ cite journal}}: Cite journal requires |journal= ( help)
  12. ^ Crilly J (March 2007). "The history of clozapine and its emergence in the US market: a review and analysis". History of Psychiatry. 18 (1): 39–60. doi: 10.1177/0957154X07070335. PMID  17580753.
  13. ^ Li JJ, Corey JJ, eds. (2013). "Chapter 7: CNS Drugs". Drug discovery practices, processes, and perspectives. Hoboken, N.J.: John Wiley & Sons. p. 248. ISBN  9781118354469. Archived from the original on 10 September 2019. Retrieved 30 August 2017.
  14. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl: 10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  15. ^ "Clozapine". International Drug Price Indicator Guide. Archived from the original on 22 January 2018. Retrieved 2 December 2015.
Retrieved from " https://en.wikipedia.org/?title=User:Mr._Ibrahem/Clozapine&oldid=1233778152"

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