Peringatan Keamanan

The oral LD₅₀ in rats is >3750 mg/kg.MSDS

The acute toxicity of beclometasone dipropionate is low. The only harmful effect that follows inhalation of large amounts of the drug over a short period of time is suppression of hypothalamic-pituitary-adrenal (HPA) function. Chronic: The excessive use of beclometasone dipropionate over a long period could lead to adrenal suppression.

Beclomethasone dipropionate

DB00394

small molecule approved investigational

Deskripsi

Beclomethasone dipropionate is a second-generation^A179842 synthetic corticosteroid and diester of beclomethasone, which is structurally similar to dexamethasone.^L6871 It is a prodrug of an active metabolite beclomethasone 17-monopropionate (17-BMP)^A179839 which acts on the glucocorticoid receptor to mediates its therapeutic action. Beclomethasone dipropionate itself posesses weak glucocorticoid receptor binding affinity and is rapidly converted into 17-BMP upon administration.^A179839 Formulations for oral inhalation, intranasal, and topical use are available for beclomethasone dipropionate. Beclomethasone dipropionate became first available in a pressurized metered-dose inhaler in 1972 and later in a dry powder inhaler and an aqueous nasal spray.^A179839 Due to its anti-inflammatory, antipruritic, and anti-allergy properties, beclomethasone dipropionate is used in various inflammatory conditions, such as asthma, allergic rhinitis, and dermatoses to reduce symptoms. When inhaled, it is proposed that beclomethasone dipropionate remains active locally in the lung without causing significant side effects associated with systemic corticosteroids.^A180010 Compared to earlier corticosteroids such as dexamethasone and prednisolone, beclomethasone dipropionate is reported to be less irritating to the nasal mucosa with a longer duration of action when administered intranasally.^A179848

Struktur Molekul 2D

Berat 521.042

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous administration, the half life of beclomethasone dipropionate was 0.5 hours while the half life of the active metabolite 17-BMP was 2.7 hours. Following oral and intranasal administration, the half life of 17-BMP was 8.8 and 5.7 hours, respectively.[A179839]

Volume Distribusi Following intravenous administration, the steady-state volume of distribution was 20 L for beclomethasone dipropionate and 424 L for the active metabolite, beclomethasone-17-monopropionate.[A179839]

Klirens (Clearance) Following intravenous administration, the clearance of beclomethasone dipropionate and 17-BMP were 150 L/h and 120 L/h, respectively.[A179839]

Absorpsi

Following oral inhalation of 320 mcg of beclomethasone dipropionate (BDP), the Cmax was 88 pg/mL and it was reached after 0.5 at post-administration. The mean Cmax of the major and most active metabolite, beclomethasone-17-monopropionate (17-BMP), was 1419 pg/mL at 0.7 hour post-dosing.^L6871 In another pharmacokinetic study, the AUC of BDP and 17-BMP were 6660 and 6185 pgxh/mL, respectively. The Cmax was 35356 pg/mL for BDP and 2633 pg/mL for 17-BMP, and and the median time to reach these concentrations (Tmax) was 0.2 hours. In the same study, the AUC of 17-BMP following oral and intranasal administration were 10158 and 3660 pgxh/mL, respectively. The Cmax of 17-BMP following oral and intranasal administration were 703 and 310 pg/mL, respectively, and the Tmax was 4 hours. The total bioavailability of 17-BMP following oral and intranasal administration were 41% and 44%, respectively.^A179839

Metabolisme

During absorption, beclomethasone dipropionate is undergoes rapid and extensive hydrolysis mediated by esterases CYP3A to form beclomethasone-17-monopropionate (17-BMP), beclomethasone-21-monopropionate (21-BMP), and beclomethasone (BOH). 17-BMP is the major active metabolite with the most potent anti-inflammatory activity.^L6871 About 95% of the total beclomethasone dipropionate administered via oral inhalation undergoes presystemic conversion to form 17-BMP in the lung.^A179839

Rute Eliminasi

Regardless of the route of administration, beclomethasone dipropionate and its metabolites are predominantly excreted in the feces, with less than 10% of the drug and its metabolites being excreted in the urine.^L6871 ^L6880

Interaksi Obat

1246 Data

Denosumab	The risk or severity of adverse effects can be increased when Denosumab is combined with Beclomethasone dipropionate.
Peginterferon alfa-2a	The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Beclomethasone dipropionate.
Interferon alfa-n1	The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Beclomethasone dipropionate.
Interferon alfa-n3	The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Beclomethasone dipropionate.
Peginterferon alfa-2b	The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Beclomethasone dipropionate.
Interferon gamma-1b	The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Beclomethasone dipropionate.
Interferon alfa-2a	The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Beclomethasone dipropionate.
Gemtuzumab ozogamicin	The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Beclomethasone dipropionate.
Pegaspargase	The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Pegaspargase.
Interferon beta-1b	The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Beclomethasone dipropionate.
Interferon alfacon-1	The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Beclomethasone dipropionate.
Rituximab	The risk or severity of adverse effects can be increased when Rituximab is combined with Beclomethasone dipropionate.
Basiliximab	The risk or severity of adverse effects can be increased when Basiliximab is combined with Beclomethasone dipropionate.
Muromonab	The risk or severity of adverse effects can be increased when Muromonab is combined with Beclomethasone dipropionate.
Ibritumomab tiuxetan	The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Beclomethasone dipropionate.
Tositumomab	The risk or severity of adverse effects can be increased when Tositumomab is combined with Beclomethasone dipropionate.
Alemtuzumab	The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Beclomethasone dipropionate.
Alefacept	The risk or severity of adverse effects can be increased when Alefacept is combined with Beclomethasone dipropionate.
Efalizumab	The risk or severity of adverse effects can be increased when Efalizumab is combined with Beclomethasone dipropionate.
Antithymocyte immunoglobulin (rabbit)	The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Beclomethasone dipropionate.
Interferon alfa-2b	The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Beclomethasone dipropionate.
Daclizumab	The risk or severity of adverse effects can be increased when Daclizumab is combined with Beclomethasone dipropionate.
Phenylalanine	The risk or severity of adverse effects can be increased when Phenylalanine is combined with Beclomethasone dipropionate.
Cladribine	The excretion of Cladribine can be decreased when combined with Beclomethasone dipropionate.
Carmustine	The risk or severity of adverse effects can be increased when Carmustine is combined with Beclomethasone dipropionate.
Amsacrine	The risk or severity of adverse effects can be increased when Amsacrine is combined with Beclomethasone dipropionate.
Bleomycin	The risk or severity of adverse effects can be increased when Bleomycin is combined with Beclomethasone dipropionate.
Chlorambucil	The risk or severity of adverse effects can be increased when Chlorambucil is combined with Beclomethasone dipropionate.
Raltitrexed	The risk or severity of adverse effects can be increased when Raltitrexed is combined with Beclomethasone dipropionate.
Mitomycin	The risk or severity of adverse effects can be increased when Mitomycin is combined with Beclomethasone dipropionate.
Bexarotene	The risk or severity of adverse effects can be increased when Bexarotene is combined with Beclomethasone dipropionate.
Floxuridine	The risk or severity of adverse effects can be increased when Floxuridine is combined with Beclomethasone dipropionate.
Tioguanine	The risk or severity of adverse effects can be increased when Tioguanine is combined with Beclomethasone dipropionate.
Dexrazoxane	The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Beclomethasone dipropionate.
Streptozocin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Streptozocin.
Trifluridine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Trifluridine.
Gemcitabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Gemcitabine.
Epirubicin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Epirubicin.
Chloramphenicol	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Chloramphenicol.
Lenalidomide	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Lenalidomide.
Altretamine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Altretamine.
Zidovudine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Zidovudine.
Oxaliplatin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Oxaliplatin.
Fluorouracil	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Fluorouracil.
Propylthiouracil	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Propylthiouracil.
Pentostatin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pentostatin.
Linezolid	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Linezolid.
Clofarabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Clofarabine.
Pemetrexed	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pemetrexed.
Mycophenolate mofetil	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mycophenolate mofetil.
Tretinoin	The metabolism of Tretinoin can be increased when combined with Beclomethasone dipropionate.
Dacarbazine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Dacarbazine.
Temozolomide	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Temozolomide.
Penicillamine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Penicillamine.
Azacitidine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Azacitidine.
Carboplatin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Carboplatin.
Dactinomycin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Dactinomycin.
Azathioprine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Azathioprine.
Hydroxyurea	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Hydroxyurea.
Mycophenolic acid	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mycophenolic acid.
Topotecan	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Topotecan.
Mercaptopurine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mercaptopurine.
Thalidomide	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Thalidomide.
Melphalan	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Melphalan.
Fludarabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Fludarabine.
Flucytosine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Flucytosine.
Capecitabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Capecitabine.
Procarbazine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Procarbazine.
Arsenic trioxide	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Arsenic trioxide.
Idarubicin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Idarubicin.
Estramustine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Estramustine.
Mitoxantrone	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mitoxantrone.
Lomustine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Lomustine.
Eculizumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Eculizumab.
Decitabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Decitabine.
Nelarabine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Nelarabine.
Stepronin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Stepronin.
Hydroxychloroquine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Hydroxychloroquine.
Castanospermine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Castanospermine.
Vorinostat	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Vorinostat.
2-Methoxyethanol	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with 2-Methoxyethanol.
Brequinar	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Brequinar.
Pirfenidone	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pirfenidone.
Interferon alfa	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Interferon alfa.
Glatiramer	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Glatiramer.
Briakinumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Briakinumab.
Human interferon omega-1	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Human interferon omega-1.
Mepolizumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mepolizumab.
Abetimus	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Abetimus.
Belatacept	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Belatacept.
Bendamustine	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Bendamustine.
Pralatrexate	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pralatrexate.
Wortmannin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Wortmannin.
Eribulin	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Eribulin.
Belimumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Belimumab.
Teriflunomide	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Teriflunomide.
Carfilzomib	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Carfilzomib.
Dimethyl fumarate	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Dimethyl fumarate.
Obinutuzumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Obinutuzumab.
Vedolizumab	The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Vedolizumab.

Target Protein

Glucocorticoid receptor NR3C1

Referensi & Sumber

Synthesis reference: Taub, D., Wendler, N.L. and Slates, H.L.; US.Patent 3,345,387; October 3, 1967; assigned to Merck & Co., Inc.

Artikel (PubMed)

PMID: 11421996
Daley-Yates PT, Price AC, Sisson JR, Pereira A, Dallow N: Beclomethasone dipropionate: absolute bioavailability, pharmacokinetics and metabolism following intravenous, oral, intranasal and inhaled administration in man. Br J Clin Pharmacol. 2001 May;51(5):400-9. doi: 10.1046/j.0306-5251.2001.01374.x.
PMID: 6381025
Brogden RN, Heel RC, Speight TM, Avery GS: Beclomethasone dipropionate. A reappraisal of its pharmacodynamic properties and therapeutic efficacy after a decade of use in asthma and rhinitis. Drugs. 1984 Aug;28(2):99-126. doi: 10.2165/00003495-198428020-00002.
PMID: 8750396
Edwards TB: Effectiveness and safety of beclomethasone dipropionate, an intranasal corticosteroid, in the treatment of patients with allergic rhinitis. Clin Ther. 1995 Nov-Dec;17(6):1032-41.
PMID: 9854452
Barnes PJ: Anti-inflammatory actions of glucocorticoids: molecular mechanisms. Clin Sci (Lond). 1998 Jun;94(6):557-72.
PMID: 16604091
Barnes PJ: How corticosteroids control inflammation: Quintiles Prize Lecture 2005. Br J Pharmacol. 2006 Jun;148(3):245-54. doi: 10.1038/sj.bjp.0706736.
PMID: 9373450
Grebe SK, Feek CM, Durham JA, Kljakovic M, Cooke RR: Inhaled beclomethasone dipropionate suppresses the hypothalamo-pituitary-adrenal axis in a dose dependent manner. Clin Endocrinol (Oxf). 1997 Sep;47(3):297-304.
PMID: 9563370
Dluhy RG: Clinical relevance of inhaled corticosteroids and HPA axis suppression. J Allergy Clin Immunol. 1998 Apr;101(4 Pt 2):S447-50.
PMID: 4753325
Wilcox JB, Avery GS: Beclomethasone dipropionate corticosteroid inhaler: a preliminary report of its pharmacological properties and therapeutic efficacy in asthma. Drugs. 1973;6(2):84-93. doi: 10.2165/00003495-197306020-00002.

Menampilkan 8 dari 10 artikel.

Link

Contoh Produk & Brand

Produk: 88 • International brands: 25

Produk

Alti-beclomethasone Dipropionate Inhaler 50mcg/md

Aerosol, metered • 50 mcg / act • Respiratory (inhalation) • Canada • Generic • Approved
Apo-beclomethasone Nasal Spray

Suspension • 50 mcg / act • Nasal • Canada • Generic • Approved
Beclodisk - Pwr Inh 100mcg/blister

Powder • 100 mcg / blister • Respiratory (inhalation) • Canada • Approved
Beclodisk - Pwr Inh 200mcg/blister

Powder • 200 mcg / blister • Respiratory (inhalation) • Canada • Approved
Beclodisk Pwr 100mcg/blister

Powder • 100 mcg / blister • Respiratory (inhalation) • Canada • Approved
Beclodisk Pwr 200mcg/blister

Powder • 200 mcg / blister • Respiratory (inhalation) • Canada • Approved
Becloforte 250mcg/aem

Aerosol, metered • 250 mcg / act • Respiratory (inhalation) • Canada • Approved
Becloforte Inhaler - Aem Inh 250mcg/aem

Aerosol, metered • 250 mcg / act • Respiratory (inhalation) • Canada • Approved

Menampilkan 8 dari 88 produk.

International Brands

Aerobec — Teva
Aldecin — Schering-Plough
Anceron
Andion
Beclacin — Mayado Seiyaku
Becloforte — GlaxoSmithKline
Beclomet — Orion
Beclorhinol — Chiesi
Becloval
Beclovent — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.