Beclometasone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Inhalation/Respiratory
Asthma prophylaxis
Adult: As aerosol or dry powd inhaler: Initially, 100-200 mcg daily for mild cases; 200-400 mcg daily for moderate cases; 400-800 mcg daily for severe cases. All doses are given in 2 divided doses. Usual maintenance dose: 400-800 mcg daily in 2 divided doses, titrated to the lowest effective dose. Max: 800 mcg (up to 2 mg may be necessary in severe cases) daily in divided doses.
Child: ≥6 yr 100 mcg in 2-4 divided doses, titrated to the lowest effective dose for maintenance. Max: 200 mcg daily.

Nasal
Treatment and prophylaxis of allergic and non-allergic rhinitis
Adult: As spray: 100 mcg into each nostril bid, or 50 mcg in each nostril 3-4 times daily. Max: 400 mcg daily. 50 mcg in each nostril bid may be used as prophylaxis.
Child: ≥6 yr Same as adult dose.

Oral
Ulcerative colitis
Adult: As modified-release tab: 5 mg once daily in the morning, before or after breakfast, for mild to moderate cases. Max duration: 4 wk.

Topical/Cutaneous
Corticosteroid-responsive dermatoses
Adult: 0.025% cream: Apply a thin film to affected area(s) 1-3 times daily, or as directed based on severity.
Chống chỉ định
As primary treatment of status asthmaticus or acute episodes of asthma requiring intensive measures (inhalation).
Thận trọng
Patient w/ bacterial (e.g. active or quiescent pulmonary TB), fungal, parasitic, and viral (e.g. chickenpox, measles, ocular herpes simplex) infection, DM, gastro-duodenal ulcer, serious arterial HTN, myasthenia gravis, MI, osteoporosis, hypoadrenalism, glaucoma, cataract, seizure disorder, depression, previous steroid-related psychosis, recent nasal septal ulcers, trauma, and surgery. Renal and hepatic (e.g. cirrhosis) impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Oral candidiasis, hoarseness, cough, epistaxis, irritation and dryness of nose and throat, unpleasant taste and smell, nasopharyngitis, rhinitis, sneezing, paradoxical bronchospasm w/ wheezing, dyspnoea; hypersensitivity (e.g. rash, urticaria, pruritus, erythema, angioedema); impaired wound healing; headache, vertigo, tremor; adrenal suppression. Rarely, Cushing’s syndrome, decreased bone mineral density, psychomotor hyperactivity, aggression, irritability, anxiety, depression, sleep disorder, suicidal ideation.
Thông tin tư vấn bệnh nhân
Rinse mouth thoroughly after inhalation.
Monitoring Parameters
Monitor growth annually during long term use in childn. Assess for ocular changes, signs and symptoms of adrenal insufficiency, and oral candidiasis.
Tác dụng
Description: Beclometasone (as diproprionate) is a prodrug w/ potent glucocorticoid and weak mineralocorticoid activity. It controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes, reduces fibroblast activity, and reverses capillary permeability and lysosomal stabilisation at the cellular level to prevent or control inflammation.
Onset: W/in a few days up to 2 wk.
Pharmacokinetics:
Absorption: Readily absorbed from the resp and GI tract. Absolute bioavailability: 44% (nasal). Time to peak plasma concentration: 0.5 hr (inhalation).
Distribution: Rapidly distributed to all body tissues. Volume of distribution: 20 L. Plasma-protein binding: 87%.
Metabolism: Undergoes hydrolysis by pulmonary esterases to major active metabolite, beclometasone-17-monopropionate (17-BMP), during absorption; subsequently undergoes metabolism in the liver by CYP3A4 enzyme to less active metabolites, beclometasone-21-monopropionate (21-BMP) and beclometasone. Undergoes first-pass metabolism in the liver and/or GI tract (oral).
Excretion: Via faeces (60% mainly as metabolites) and urine (<10-12% as free and conjugated metabolites). Elimination half-life: 0.5 hr.
Đặc tính

Chemical Structure Image
Beclometasone

Source: National Center for Biotechnology Information. PubChem Database. Beclomethasone, CID=20469, https://pubchem.ncbi.nlm.nih.gov/compound/Beclomethasone (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-30°C. Nasal/inhalation aerosol: Do not puncture. Protect from heat or open flame.
Phân loại ATC
R03BA01 - beclometasone ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
R01AD01 - beclometasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
D07AC15 - beclometasone ; Belongs to the class of potent (group III) corticosteroids. Used in the treatment of dermatological diseases.
A07EA07 - beclometasone ; Belongs to the class of corticosteroids acting locally. Used in the treatment of intestinal inflammation.
References
Anon. Beclomethasone (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2016.

Anon. Beclomethasone (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2016.

Bausch & Lomb NZ Ltd. QVAR Autohaler and Inhaler data sheet 2 April 2015. Medsafe. http://www.medsafe.govt.nz/. Accessed 06/09/2016.

Beclomethasone. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 06/09/2016.

Buckingham R (ed). Beclometasone Dipropionate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2016.

Buckingham R (ed). Interactions of Corticosteroids. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2016.

Joint Formulary Committee. Beclometasone Dipropionate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Beclomethasone Dipropionate (EENT). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/09/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Beclomethasone Dipropionate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/09/2016.

Mylan New Zealand Limited. Alanase Aqueous Nasal Spray data sheet 16 June 2015 . Medsafe. http://www.medsafe.govt.nz/. Accessed 06/09/2016.

QNASL Aerosol, Metered (Teva Respiratory, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/09/2016.

QVAR Aerosol, Metered (Teva Respiratory, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/09/2016.

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