Peringatan Keamanan

The oral LD₅₀ of fludrocortisone in rats is >1g/kg.^L9055 Acute overdosage of fludrocortisone is likely to result in symptoms consistent with its adverse effect profile. Patients receiving a single large dose should be treated with plenty of water by mouth and should undergo monitoring of serum electrolytes, particularly potassium and sodium, and be treated appropriately for any developing imbalances.L8974,L8977

Fludrocortisone

DB00687

small molecule approved investigational

Deskripsi

Fludrocortisone is a synthetic mineralocorticoid used in conjunction with hydrocortisone to replace missing endogenous corticosteroids in patients with adrenal insufficiency.A187169,A187187 It is functionally similar to aldosterone, the body's primary endogenous mineralocorticoid, and is structurally analogous to cortisol, differing only by a fluorine atom at the 9-position of the steroid structure - this fluorination is thought to be crucial to fludrocortisone's significant mineralocorticoid potency.^A5423

Struktur Molekul 2D

Berat 380.4504

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) The plasma half-life of fludrocortisone has been variably reported to be between 1-3.5 hours,[A187159,A187169,A187181] though prescribing information gives an approximate half-life of 18-36 hours.[L8974]

Volume Distribusi The apparent volume of distribution of fludrocortisone is 80-85 L.[A187169,A187159] Distribution into CSF appears minimal - the observed ratio of CSF drug concentration versus plasma drug concentration is 1:6.[L8977]

Klirens (Clearance) Population pharmacokinetics have estimated the plasma clearance of fludrocortisone to be 40.8 L/h.[A187169]

Absorpsi

Absorption of fludrocortisone following oral administration is rapid and complete.L8977,A187169,A187181,A187159 Pharmacokinetic studies have estimated the C_max to be 0.0012 to 0.20 ?g/L with a T_max between 0.5 and 2 hours.A187169,A187181 The AUC_0-? of fludrocortisone after oral administration has been variably estimated to be between 1.22 to 3.07 ?g.h/L.A187169,A187181

Metabolisme

There exists is a paucity of information regarding the specific metabolic pathway in vivo of fludrocortisone. The 9?-fluorination of fludrocortisone appears to greatly simplify its metabolism as compared to other corticosteroids^A187162 - while oxidation via 11-hydroxysteroid dehydrogenases has been observed,^A187144 this reaction is greatly impaired as the fluorine moiety appears to confer "protection" from 11?-oxidation by these enzymes. The reduction in 11?-oxidation is thought to be one of the reasons behind fludrocortisone's profound mineralocorticoid potency.^A5423 An in vitro study generated only two metabolites following incubation in human liver microsomes and cytosol, namely 20?-dihydrofluorocortisol and 6?-hydroxyfluorocortisol, and did not explore in detail the potential enzymes responsible for this reaction.^A187162 Given that fludrocortisone is a corticosteroid, a class of medications known to be metabolized by the CYP3A family,^A14813 and is not recommended to be given with strong inhibitors/inducers of CYP3A,^L8974 it is likely that the CYP3A family of enzymes contributes in some way to its metabolism (though this information does not appear to have been specifically elucidated for fludrocortisone).

Rute Eliminasi

Approximately 80% of an administered dose of fludrocortisone shows up in the urine, with the other 20% likely eliminated via fecal or biliary route.L8977,A187181

Interaksi Makanan

1 Data

1. Limit salt intake. Excessive intake of salt can result in hypertension and edema.

Interaksi Obat

1037 Data

Denosumab	The risk or severity of adverse effects can be increased when Denosumab is combined with Fludrocortisone.
Peginterferon alfa-2a	The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Fludrocortisone.
Interferon alfa-n1	The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Fludrocortisone.
Interferon alfa-n3	The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Fludrocortisone.
Peginterferon alfa-2b	The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Fludrocortisone.
Interferon gamma-1b	The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Fludrocortisone.
Interferon alfa-2a	The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Fludrocortisone.
Aldesleukin	The risk or severity of adverse effects can be increased when Aldesleukin is combined with Fludrocortisone.
Gemtuzumab ozogamicin	The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Fludrocortisone.
Pegaspargase	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fludrocortisone.
Interferon beta-1b	The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Fludrocortisone.
Interferon alfacon-1	The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Fludrocortisone.
Rituximab	The risk or severity of adverse effects can be increased when Rituximab is combined with Fludrocortisone.
Basiliximab	The risk or severity of adverse effects can be increased when Basiliximab is combined with Fludrocortisone.
Muromonab	The risk or severity of adverse effects can be increased when Muromonab is combined with Fludrocortisone.
Ibritumomab tiuxetan	The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Fludrocortisone.
Tositumomab	The risk or severity of adverse effects can be increased when Tositumomab is combined with Fludrocortisone.
Alemtuzumab	The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fludrocortisone.
Alefacept	The risk or severity of adverse effects can be increased when Alefacept is combined with Fludrocortisone.
Efalizumab	The risk or severity of adverse effects can be increased when Efalizumab is combined with Fludrocortisone.
Antithymocyte immunoglobulin (rabbit)	The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Fludrocortisone.
Interferon alfa-2b	The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Fludrocortisone.
Daclizumab	The risk or severity of adverse effects can be increased when Daclizumab is combined with Fludrocortisone.
Phenylalanine	The risk or severity of adverse effects can be increased when Phenylalanine is combined with Fludrocortisone.
Bortezomib	The risk or severity of adverse effects can be increased when Bortezomib is combined with Fludrocortisone.
Cladribine	Fludrocortisone may increase the immunosuppressive activities of Cladribine.
Carmustine	The risk or severity of adverse effects can be increased when Carmustine is combined with Fludrocortisone.
Amsacrine	The risk or severity of adverse effects can be increased when Amsacrine is combined with Fludrocortisone.
Bleomycin	The risk or severity of adverse effects can be increased when Bleomycin is combined with Fludrocortisone.
Chlorambucil	The risk or severity of adverse effects can be increased when Chlorambucil is combined with Fludrocortisone.
Raltitrexed	The risk or severity of adverse effects can be increased when Raltitrexed is combined with Fludrocortisone.
Mitomycin	The risk or severity of adverse effects can be increased when Mitomycin is combined with Fludrocortisone.
Bexarotene	The risk or severity of adverse effects can be increased when Bexarotene is combined with Fludrocortisone.
Vindesine	The risk or severity of adverse effects can be increased when Vindesine is combined with Fludrocortisone.
Floxuridine	The risk or severity of adverse effects can be increased when Floxuridine is combined with Fludrocortisone.
Tioguanine	The risk or severity of adverse effects can be increased when Tioguanine is combined with Fludrocortisone.
Vinorelbine	The risk or severity of adverse effects can be increased when Vinorelbine is combined with Fludrocortisone.
Dexrazoxane	The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Fludrocortisone.
Sorafenib	The risk or severity of adverse effects can be increased when Sorafenib is combined with Fludrocortisone.
Streptozocin	The risk or severity of adverse effects can be increased when Streptozocin is combined with Fludrocortisone.
Trifluridine	The risk or severity of adverse effects can be increased when Trifluridine is combined with Fludrocortisone.
Gemcitabine	The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fludrocortisone.
Teniposide	The risk or severity of adverse effects can be increased when Teniposide is combined with Fludrocortisone.
Epirubicin	The risk or severity of adverse effects can be increased when Epirubicin is combined with Fludrocortisone.
Chloramphenicol	The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Fludrocortisone.
Lenalidomide	The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fludrocortisone.
Altretamine	The risk or severity of adverse effects can be increased when Altretamine is combined with Fludrocortisone.
Zidovudine	The risk or severity of adverse effects can be increased when Zidovudine is combined with Fludrocortisone.
Oxaliplatin	The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Fludrocortisone.
Cyclophosphamide	The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Fludrocortisone.
Vincristine	The risk or severity of adverse effects can be increased when Vincristine is combined with Fludrocortisone.
Fluorouracil	The risk or severity of adverse effects can be increased when Fluorouracil is combined with Fludrocortisone.
Propylthiouracil	The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Fludrocortisone.
Pentostatin	The risk or severity of adverse effects can be increased when Pentostatin is combined with Fludrocortisone.
Methotrexate	The risk or severity of adverse effects can be increased when Methotrexate is combined with Fludrocortisone.
Vinblastine	The risk or severity of adverse effects can be increased when Vinblastine is combined with Fludrocortisone.
Linezolid	The risk or severity of adverse effects can be increased when Linezolid is combined with Fludrocortisone.
Imatinib	The risk or severity of adverse effects can be increased when Imatinib is combined with Fludrocortisone.
Clofarabine	The risk or severity of adverse effects can be increased when Clofarabine is combined with Fludrocortisone.
Pemetrexed	The risk or severity of adverse effects can be increased when Pemetrexed is combined with Fludrocortisone.
Mycophenolate mofetil	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mycophenolate mofetil.
Daunorubicin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Daunorubicin.
Irinotecan	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Irinotecan.
Etoposide	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Etoposide.
Dacarbazine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Dacarbazine.
Temozolomide	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Temozolomide.
Penicillamine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Penicillamine.
Azacitidine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Azacitidine.
Carboplatin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Carboplatin.
Dactinomycin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Dactinomycin.
Cytarabine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Cytarabine.
Azathioprine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Azathioprine.
Doxorubicin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Doxorubicin.
Hydroxyurea	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Hydroxyurea.
Mycophenolic acid	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mycophenolic acid.
Topotecan	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Topotecan.
Mercaptopurine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mercaptopurine.
Thalidomide	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Thalidomide.
Melphalan	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Melphalan.
Fludarabine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Fludarabine.
Flucytosine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Flucytosine.
Capecitabine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Capecitabine.
Procarbazine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Procarbazine.
Arsenic trioxide	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Arsenic trioxide.
Idarubicin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Idarubicin.
Estramustine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Estramustine.
Mitoxantrone	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mitoxantrone.
Lomustine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Lomustine.
Docetaxel	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Docetaxel.
Eculizumab	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Eculizumab.
Decitabine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Decitabine.
Nelarabine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Nelarabine.
Stepronin	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Stepronin.
Hydroxychloroquine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Hydroxychloroquine.
Castanospermine	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Castanospermine.
Vorinostat	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Vorinostat.
2-Methoxyethanol	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with 2-Methoxyethanol.
Brequinar	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Brequinar.
Pirfenidone	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Pirfenidone.
Belinostat	The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Belinostat.

Target Protein

Androgen receptor AR

Mineralocorticoid receptor NR3C2

Glucocorticoid receptor NR3C1

Referensi & Sumber

Synthesis reference: U.S. Patent 2,957,013

Artikel (PubMed)

PMID: 907708
Agarwal MK, Coupry F, Philippe M: Physiological activity and receptor binding of 9 alpha fluorohydrocortisone. Biochem Biophys Res Commun. 1977 Sep 23;78(2):747-53. doi: 10.1016/0006-291x(77)90242-x.
PMID: 6274900
Lan NC, Graham B, Bartter FC, Baxter JD: Binding of steroids to mineralocorticoid receptors: implications for in vivo occupancy by glucocorticoids. J Clin Endocrinol Metab. 1982 Feb;54(2):332-42. doi: 10.1210/jcem-54-2-332.
PMID: 12466373
Diederich S, Eigendorff E, Burkhardt P, Quinkler M, Bumke-Vogt C, Rochel M, Seidelmann D, Esperling P, Oelkers W, Bahr V: 11beta-hydroxysteroid dehydrogenase types 1 and 2: an important pharmacokinetic determinant for the activity of synthetic mineralo- and glucocorticoids. J Clin Endocrinol Metab. 2002 Dec;87(12):5695-701. doi: 10.1210/jc.2002-020970.
PMID: 28435101
Abboud R, Akil M, Charcosset C, Greige-Gerges H: Interaction of glucocorticoids and progesterone derivatives with human serum albumin. Chem Phys Lipids. 2017 Oct;207(Pt B):271-278. doi: 10.1016/j.chemphyslip.2017.04.007. Epub 2017 Apr 21.
PMID: 13746120
SANDBERG AA, SLAUNWHITE WR Jr, CARTER AC: Transcortin: a corticosteroid-binding protein of plasma. III. The effects of various steroids. J Clin Invest. 1960 Dec;39:1914-26. doi: 10.1172/JCI104216.
PMID: 7846738
Mitsky VP, Workman RJ, Nicholson WE, Vernikos J, Robertson RM, Robertson D: A sensitive radioimmunoassay for fludrocortisone in human plasma. Steroids. 1994 Sep;59(9):555-8. doi: 10.1016/0039-128x(94)90074-4.
PMID: 8157723
Oelkers W, Buchen S, Diederich S, Krain J, Muhme S, Schoneshofer M: Impaired renal 11 beta-oxidation of 9 alpha-fluorocortisol: an explanation for its mineralocorticoid potency. J Clin Endocrinol Metab. 1994 Apr;78(4):928-32.
PMID: 8274419
Abel SM, Back DJ, Maggs JL, Park BK: Cortisol metabolism by human liver in vitro--IV. Metabolism of 9 alpha-fluorocortisol by human liver microsomes and cytosol. J Steroid Biochem Mol Biol. 1993 Dec;46(6):833-9. doi: 10.1016/0960-0760(93)90326-r.

Menampilkan 8 dari 12 artikel.

Textbook

ISBN: 978-0-7020-3471-8
32. (2012). In Rang and Dale's Pharmacology (7th ed.). Edinburgh: Elsevier/Churchill Livingstone.

Link

Contoh Produk & Brand

Produk: 28 • International brands: 7

Produk

Florinef

Tablet • 0.1 mg • Oral • Canada • Approved
Florinef Acetate

Tablet • 0.1 mg/1 • Oral • US
Florinef Acetate

Tablet • .1 mg/1 • Oral • US • Approved
Florinef Acetate 0.1mg

Tablet • .1 mg / tab • Oral • Canada • Approved
Fludrocortisone Acetate

Tablet • 0.1 mg/1 • Oral • US • Generic • Approved
Fludrocortisone Acetate

Tablet • 0.1 mg/1 • Oral • US • Generic • Approved
Fludrocortisone Acetate

Tablet • 0.1 mg/1 • Oral • US • Generic • Approved
Fludrocortisone Acetate

Tablet • 0.1 mg/1 • Oral • US • Generic • Approved

Menampilkan 8 dari 28 produk.

International Brands

Adixone — Genopharm
Astonin — Merck
Cortineff — Polfa Pabianice
Florinef Acetaat — Bristol-Myers Squibb
Florinefe — Bristol-Myers Squibb
Fludrocortison — Bristol-Myers Squibb
Lonikan — Merck

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.