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ବାଇକାଲୁଟାମାଇଡ

ଉଇକିପିଡ଼ିଆ‌ରୁ
(Bicalutamideରୁ ଲେଉଟି ଆସିଛି)
ବାଇକାଲୁଟାମାଇଡ
Clinical data
PronunciationBicalutamide:
/baɪkəˈluːtəmaɪd/ bye-kə-LOO-tə-myde[୧]
Casodex:
/ˈkeɪsoʊdɛks/ KAY-soh-deks[୨]
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[୩]
    Drug classNonsteroidal antiandrogen
    ATC code
    Legal status
    Legal status
    • ℞ (Prescription only)
    Pharmacokinetic data
    BioavailabilityWell-absorbed; absolute bioavailability unknown[୪]
    Protein bindingRacemate: 96.1%[୩]
    (R)-Isomer: 99.6%[୩]
    (Mainly to albumin)[୩]
    MetabolismLiver (extensively):[୫][୬]
    • Hydroxylation (CYP3A4)
    • Glucuronidation (UGT1A9)
    Metabolites• Bicalutamide glucuronide
    • Hydroxybicalutamide
    • Hydroxybicalutamide gluc.
    (All inactive)[୫][୩][୭][୮]
    Elimination half-lifeAcute: 5.8 days[୯]
    Chronic: 7–10 days[୧୦]
    ExcretionFeces: 43%[୫]
    Urine: 34%[୫]
    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 ।[୪] ଯକୃତ ପରିବର୍ତ୍ତନ ଓ କ୍ଷତି ସଙ୍କଟ କମ୍ ଥିଲେ ମଧ୍ୟ ଚିକିତ୍ସା ସମୟରେ ଲିଭର ଫଙ୍କସନ ଟେଷ୍ଟ (monitoring of liver enzyme) କରିବାକୁ ଉପଦେଶ ଦିଆଯାଏ ।[୧୧]

    ଆଧାର

    [ସମ୍ପାଦନା]
    1. ↑ 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)
    2. ↑ Sifton DW, PDR Staff (2002). PDR Drug Guide for Mental Health Professionals. Thomson/PDR. ISBN 978-1-56363-457-4.
    3. 1 2 3 4 5 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.
    4. 1 2 ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; "Dart2004" ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
    5. 1 2 3 4 ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; "LemkeWilliams2008" ନାମରେ ଥିବା ଆଧାର ଭିତରେ କିଛି ଲେଖା ନାହିଁ ।
    6. ↑ ଆଧାର ଭୁଲ: ଅଚଳ <ref> ଚିହ୍ନ; "GrosseCampeau2013" 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. 1 2 3 4 5 6 7 8 "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. Archived from the original (PDF) on 2016-08-28. Retrieved 2017-09-12.
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