ବାଇକାଲୁଟାମାଇଡ

ଉଇକିପିଡ଼ିଆ‌ରୁ
ବାଇକାଲୁଟାମାଇଡ
Clinical data
PronunciationBicalutamide:
/baɪkəˈluːtəmaɪd/ bye-kə-LOO-tə-myde[୨]
Casodex:
/ˈkeɪsoʊdɛks/ KAY-soh-deks[୩]
Trade namesCasodex, Cosudex, Calutide, Calumid, Kalumid, others
SynonymsICI-176,334; ZD-176,334
AHFS/Drugs.commonograph
MedlinePlusa697047
data
Pregnancy
category
  • AU: D
  • US: X (Contraindicated)
Routes of
administration		By mouth[୧]
Drug classNonsteroidal antiandrogen
ATC code
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityWell-absorbed; absolute bioavailability unknown[୬]
Protein bindingRacemate: 96.1%[୧]
(R)-Isomer: 99.6%[୧]
(Mainly to albumin)[୧]
MetabolismLiver (extensively):[୪][୫]
• Hydroxylation (CYP3A4)
• Glucuronidation (UGT1A9)
Metabolites• Bicalutamide glucuronide
• Hydroxybicalutamide
• Hydroxybicalutamide gluc.
(All inactive)[୪][୧][୭][୮]
Elimination half-lifeAcute: 5.8 days[୯]
Chronic: 7–10 days[୧୦]
ExcretionFeces: 43%[୪]
Urine: 34%[୪]
Identifiers
  • (RS)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
ECHA InfoCard100.126.100 Edit this at Wikidata
Chemical and physical data
FormulaC18H14F4N2O4S
Molar mass430.373 g/mol
3D model (JSmol)
ChiralityRacemic mixture (of (R)- and (S)-enantiomers)
Melting point191 to 193 °C (376 to 379 °F) (experimental)
Boiling point650 °C (1,202 °F) (predicted)
Solubility in water0.005 mg/mL (20 °C)
  • O=C(Nc1cc(c(C#N)cc1)C(F)(F)F)C(O)(C)CS(=O)(=O)c2ccc(F)cc2
  • InChI=1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25) checkY
  • Key:LKJPYSCBVHEWIU-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

ବାଇକାଲୁଟାମାଇଡ (ଇଂରାଜୀ ଭାଷାରେ Bicalutamide, ବିକ୍ରୟ ନାମ କାସୋଡେକ୍ସ/ Casodex) ଏକ ଆଣ୍ଡ୍ରୋଜେନ ବିରୋଧୀ (antiandrogen) ଔଷଧ ଯାହା ପ୍ରୋସ୍ଟେଟ କର୍କଟ ରୋଗର ଚିକିତ୍ସା ନିମନ୍ତେ ଦିଆଯାଏ ।[୧୧] ମେଟାସ୍ଟାସିସ (metastatic) ହୋଇଥିବା ପ୍ରୋସ୍ଟେଟ କର୍କଟ ରୋଗରେ ବା ଓର୍କିଡେକ୍ଟୋମି (surgical removal of the testicles) କରାଯାଇଥିଲେ ଏହା ଗୋନାଡୋଟ୍ରପିନ-ରିଲିଜିଙ୍ଗ ହରମୋନ ଆନାଲଗ (gonadotropin-releasing hormone (GnRH) analogue) ସାଥିରେ ଦିଆଯାଏ ।[୧୨][୧୧][୧୩] ମହିଳାଙ୍କର ଅତ୍ୟଧିକ ବାଳ ବୃଦ୍ଧି (excessive hair growth) ହୋଇଥିଲେ ବାଇକାଲୁଟାମାଇଡ ଦିଆଯାଏ,[୧୪] ଟ୍ରାନ୍ସଜେଣ୍ଡର ମହିଳାଙ୍କର (transgender women) ହରମୋନ ଥେରାପିର (hormone therapy) ଏହା ଉପାଦାନ ଥାଏ,[୧୫] ପ୍ରିଆପିଜ୍ମ (priapism) ପ୍ରତିଷେଧ ନିମନ୍ତେ ଦିଆଯାଏ,[୧୬] ଓ ବାଳକମାନଙ୍କର ସମୟ ପୂର୍ବ ଯୌବନ ପ୍ରାପ୍ତି (early puberty) ରୋଗମାନଙ୍କ ନିମନ୍ତେ ଏହା ଦିଆଯାଏ ।[୧୭] ଏହି ଔଷଧ ପାଟିରେ (by mouth) ଦିଆଯାଏ ।[୧୧]

ଏହାର ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ସ୍ତନ ବୃଦ୍ଧି (breast enlargement), ସ୍ତନ ଯନ୍ତ୍ରଣା (breast tenderness) ଓ ଦେହ ଲାଲ ପଡ଼ିଯିବା (hot flashes) ଦେଖାଯାଏ ।[୧୧] ପୁରୁଷମାନଙ୍କର ମହିଳାତ୍ୱ (feminization) ପ୍ରକାଶ ପାଏ ଓ ସେମାନେ ଯୌନ କ୍ରିୟାହୀନ (sexual dysfunction) ହୋଇଯାଆନ୍ତି ।[୧୮] ମହିଳାମାନଙ୍କର ଅଳ୍ପ ପ୍ରତିକ୍ରିୟା ହେଲେ ମଧ୍ୟ ଏହା ବ୍ୟବ‌ହାର କରିବାକୁ ଏଫଡିଏ (Food and Drug Administration ବା FDA) ମନା କରେ ।[୧୯][୧୧] ଗର୍ଭାବସ୍ଥାରେ ଶିଶୁର କ୍ଷତି ହୋଇପାରେ ।[୧୧] ପ୍ରାୟ ୧% ଲୋକଙ୍କର ବାଇକାଲୁଟାମାଇଡ ଯୋଗୁ ଟ୍ରାନ୍ସାଆମିନେଜ ସ୍ତର ବୃଦ୍ଧି (elevated liver enzyme) ପାଏ ।[୨୦][୨୧] ଏହା ଯୋଗୁ କ୍ୱଚିତ୍ ଯକୃତ୍ ବିଷକ୍ରିୟା (liver damage),[୧୧] ଓ ଫୁସଫୁସ ବିଷକ୍ରିୟା (lung toxicity) ଦେଖାଯାଇପାରେ ।[୬] ଯକୃତ ପରିବର୍ତ୍ତନ ଓ କ୍ଷତି ସଙ୍କଟ କମ୍ ଥିଲେ ମଧ୍ୟ ଚିକିତ୍ସା ସମୟରେ ଲିଭର ଫଙ୍କସନ ଟେଷ୍ଟ (monitoring of liver enzyme) କରିବାକୁ ଉପଦେଶ ଦିଆଯାଏ ।[୧୧]

ଆଧାର[ସମ୍ପାଦନା]

  1. ↑ ୧.୦ ୧.୧ ୧.୨ ୧.୩ ୧.୪ Cockshott ID (2004). "Bicalutamide: clinical pharmacokinetics and metabolism". Clinical Pharmacokinetics. 43 (13): 855–878. doi:10.2165/00003088-200443130-00003. PMID 15509184. These data indicate that direct glucuronidation is the main metabolic pathway for the rapidly cleared (S)-bicalutamide, whereas hydroxylation followed by glucuronidation is a major metabolic pathway for the slowly cleared (R)-bicalutamide.
  2. ↑ Finkel, Richard; Clark, Michelle Alexia; Cubeddu, Luigi X. (2009). Pharmacology. Lippincott Williams & Wilkins. pp. 481–. ISBN 978-0-7817-7155-9. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  3. ↑ Sifton DW, PDR Staff (2002). PDR Drug Guide for Mental Health Professionals. Thomson/PDR. ISBN 978-1-56363-457-4.
  4. ↑ ୪.୦ ୪.୧ ୪.୨ ୪.୩ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; LemkeWilliams2008 ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
  5. ↑ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; GrosseCampeau2013 ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
  6. ↑ ୬.୦ ୬.୧ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; Dart2004 ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
  7. ↑ Dole EJ, Holdsworth MT (1997). "Nilutamide: an antiandrogen for the treatment of prostate cancer". The Annals of Pharmacotherapy. 31 (1): 65–75. doi:10.1177/106002809703100112. PMID 8997470. page 67: Currently, information is not available regarding the activity of the major urinary metabolites of bicalutamide, bicalutamide glucuronide, and hydroxybicalutamide glucumnide.
  8. ↑ Schellhammer PF (September 2002). "An evaluation of bicalutamide in the treatment of prostate cancer". Expert Opinion on Pharmacotherapy. 3 (9): 1313–28. doi:10.1517/14656566.3.9.1313. PMID 12186624. The clearance of bicalutamide occurs pre- dominantly by hepatic metabolism and glucuronidation, with excretion of the resulting inactive metabolites in the urine and faces.
  9. ↑ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; Skidmore-Roth2013 ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
  10. ↑ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; JordanFurr2010 ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
  11. ↑ ୧୧.୦ ୧୧.୧ ୧୧.୨ ୧୧.୩ ୧୧.୪ ୧୧.୫ ୧୧.୬ ୧୧.୭ "Bicalutamide". The American Society of Health-System Pharmacists. Retrieved 8 December 2016.
  12. ↑ Wass, John A.H.; Stewart, Paul M. (28 July 2011). Oxford Textbook of Endocrinology and Diabetes. OUP Oxford. pp. 1625–. ISBN 978-0-19-923529-2. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  13. ↑ Shergill, Iqbal; Arya, Manit; Grange, Philippe R.; Mundy, A. R. (2010). Medical Therapy in Urology (in ଇଂରାଜୀ). Springer Science & Business Media. p. 40. ISBN 9781848827042. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  14. ↑ Williams, Hywel; Bigby, Michael; Diepgen, Thomas; Herxheimer, Andrew; Naldi, Luigi; Rzany, Berthold (22 January 2009). Evidence-Based Dermatology. John Wiley & Sons. pp. 529–. ISBN 978-1-4443-0017-8. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  15. ↑ Gooren, LJ (31 March 2011). "Clinical practice. Care of transsexual persons". The New England Journal of Medicine. 364 (13): 1251–7. doi:10.1056/nejmcp1008161. PMID 21449788.
  16. ↑ Yuan J, Desouza R, Westney OL, Wang R (2008). "Insights of priapism mechanism and rationale treatment for recurrent priapism". Asian Journal of Andrology. 10 (1): 88–101. doi:10.1111/j.1745-7262.2008.00314.x. PMID 18087648.
  17. ↑ Jameson, J. Larry; De Groot, Leslie J. (25 February 2015). Edndocrinology: Adult and Pediatric. Elsevier Health Sciences. pp. 2425–2426, 2139. ISBN 978-0-323-32195-2. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  18. ↑ Elliott S, Latini DM, Walker LM, Wassersug R, Robinson JW (2010). "Androgen deprivation therapy for prostate cancer: recommendations to improve patient and partner quality of life". The Journal of Sexual Medicine. 7 (9): 2996–3010. doi:10.1111/j.1743-6109.2010.01902.x. PMID 20626600.
  19. ↑ Shapiro, Jerry (12 November 2012). Hair Disorders: Current Concepts in Pathophysiology, Diagnosis and Management, An Issue of Dermatologic Clinics. Elsevier Health Sciences. pp. 187–. ISBN 1-4557-7169-4. {{cite book}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
  20. ↑ "Casodex® (bicalutamide) Tablets" (PDF). FDA.
  21. ↑ Wellington K, Keam SJ (2006). "Bicalutamide 150mg: a review of its use in the treatment of locally advanced prostate cancer" (PDF). Drugs. 66 (6): 837–50. doi:10.2165/00003495-200666060-00007. PMID 16706554.
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