Bicalutamide


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Advanced prostate cancer
Adult: In combination with luteinizing-hormone releasing hormone (LHRH) analogue therapy or surgical castration: 50 mg once daily, to be started at the same time as treatment with LHRH analogue or surgical castration, or alternatively, started at least 3 days before LHRH therapy.

Oral
Locally advanced prostate cancer
Adult: As monotherapy or adjuvant therapy to surgery or radiotherapy in patients with high recurrence risk cases: 150 mg once daily, continued for at least 2 years or until disease progression.

Oral
Locally advanced, non-metastatic prostate cancer
Adult: In patients whom surgical castration or other medical intervention is inappropriate: 150 mg once daily, continued for at least 2 years or until disease progression.
Cách dùng
May be taken with or without food.
Chống chỉ định
Females. Children. Pregnancy and lactation. Concomitant use of terfenadine, astemizole, or cisapride.
Thận trọng
Patient with history of or risk factors for QT prolongation, heart failure, frequent electrolyte abnormalities; alcohol abuse, family history or risk factors for osteoporosis; diabetes. Moderate to severe hepatic impairment.
Phản ứng phụ
Significant: QT prolongation, gynaecomastia, breast pain, anaemia, hepatitis, increased liver enzymes, hypersensitivity reactions (e.g. angioneurotic oedema, urticaria); decreased bone mineral density (prolonged use); loss of glycaemic control and decreased glucose tolerance (in combination with LHRH agonists in diabetic patients). Rarely, photosensitivity reactions.
Cardiac disorders: Cardiac failure, chest pain.
Gastrointestinal disorders: Abdominal pain, constipation, nausea, dyspepsia, flatulence, diarrhoea.
General disorders and administration site conditions: Asthenia.
Investigations: Increased weight.
Metabolism and nutrition disorders: Decreased appetite, oedema.
Nervous system disorders: Dizziness, somnolence.
Psychiatric disorders: Depression.
Renal and urinary disorders: Haematuria.
Reproductive system and breast disorders: Erectile dysfunction, decreased libido.
Skin and subcutaneous tissue disorders: Dry skin, alopecia, hirsutism or hair regrowth, pruritus, rash.
Vascular disorders: Hot flush.
Potentially Fatal: Severe liver injury. Rarely, interstitial lung disease.
Thông tin tư vấn bệnh nhân
Avoid excessive exposure to sunlight or UV light and utilise adequate sun protection (e.g. wear protective clothing, use of sunscreen).
Monitoring Parameters
Monitor LFT at baseline and regularly during the 1st 4 months of therapy, then periodically thereafter; CBC, electrolyte, ECG, echocardiograms, LH, prostate specific antigen, serum testosterone periodically; blood glucose (in diabetic patients), PT and INR (in patients receiving warfarin). Monitor for signs and symptoms of liver dysfunction.
Tương tác
Increased risk of haemorrhage with anticoagulants e.g. coumarin. Increased risk of QT interval prolongation or torsade de pointes with class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic drugs, methadone, moxifloxacin, or antipsychotics. May increase serum levels of ciclosporin and Ca channel blockers.
Potentially Fatal: May increase exposure of drugs with narrow therapeutic index such as terfenadine, astemizole, and cisapride.
Tác dụng
Description: Bicalutamide is a nonsteroidal antiandrogen. It inhibits the action of androgens by binding to the cytosol androgen receptors in the target tissue without activating gene expression resulting in regression of prostatic tumours.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 31 hours ([R]-enantiomer).
Distribution: Plasma protein binding: 96%.
Metabolism: Undergoes extensive stereospecific metabolism in the liver; the (R)-enantiomer (active) primarily undergoes oxidation to inactive metabolites followed by glucuronidation and the (S)-enantiomer (inactive) primarily undergoes glucuronidation.
Excretion: Via urine and faeces. Elimination half-life: Approx 1 week ([R]-enantiomer).
Đặc tính

Chemical Structure Image
Bicalutamide

Source: National Center for Biotechnology Information. PubChem Database. Bicalutamide, CID=2375, https://pubchem.ncbi.nlm.nih.gov/compound/Bicalutamide (accessed on Jan. 21, 2020)

Bảo quản
Store below 30°C.
Phân loại MIMS
Phân loại ATC
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
References
Anon. Bicalutamide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/11/2020.

Bicalutamide Tablet (Accord Healthcare Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/11/2020.

Buckingham R (ed). Bicalutamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

Casodex 150 mg Film Coated Tablets (AstraZeneca). MIMS Singapore. http://www.mims.com/singapore. Accessed 05/11/2020.

Casodex 150 mg Film-Coated Tablets (AstraZeneca UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 04/11/2020.

Casodex 50 mg Film Coated Tablets (AstraZeneca). MIMS Singapore. http://www.mims.com/singapore. Accessed 05/11/2020.

Casodex 50 mg Film-Coated Tablets (AstraZeneca UK). MHRA. https://products.mhra.gov.uk/. Accessed 04/11/2020.

Casodex Tablet 50 mg (AstraZeneca Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2020.

Joint Formulary Committee. Bicalutamide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

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