Betamethasone

Identification

Summary

Betamethasone is a systemic corticosteroid used to relieve inflammation in various conditions, including but not limited to allergic states, dermatologic disorders, gastrointestinal diseases, and hematological disorders.

Brand Names
Betaderm, Betaloan Suik, Beteflam, Betnesol, Celestoderm, Celestone Soluspan, Dermacinrx Therazole Pak, Diprolene, Diprosalic, Diprosone, Dovobet, Enstilar, Fucibet, Lotriderm, Lotrisone, Luxiq, Marbeta, Rivasone, Rolene, Rosone, Sernivo, Taclonex, Valisone-G, Wynzora
Generic Name
Betamethasone
DrugBank Accession Number
DB00443
Background

Betamethasone is a long-acting corticosteroid with immunosuppressive and antiinflammatory properties.11 It can be used topically to manage inflammatory skin conditions such as eczema, and parenterally to manage several disease states including autoimmune disorders.11 Betamethasone has potent glucocorticoid activity and negligible mineralocorticoid activity.11

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 392.4611
Monoisotopic: 392.199902243
Chemical Formula
C22H29FO5
Synonyms
  • 16β-Methyl-1,4-pregnadiene-9α-fluoro-11β,17α,21-triol-3,20-dione
  • 9-Fluoro-16β-methylprednisolone
  • 9α-Fluoro-16β-methylprednisolone
  • beta-Methasone alcohol
  • Betadexamethasone
  • Betametasona
  • Betamethasone
  • Bétaméthasone
  • Betamethasonum
External IDs
  • NSC-39470
  • SCH 4831
  • SCH-4831

Pharmacology

Indication

As a member of the corticosteroid family, betamethasone is indicated for the treatment of several inflammatory conditions. As topical monotherapy, betamethasone is indicated to relieve pruritic and inflammatory symptoms of corticosteroid-responsive-dermatoses.12,14,15 Betamethasone can be used topically in combination with a vitamin D analog such as calcipotriene to treat plaque psoriasis.16 The corticosteroid is also available as an injectable suspension and can be used to manage a range of inflammatory conditions including endocrine disorders, gastrointestinal disorders, and rheumatic disorders among other conditions.13

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor inhibiting pro-inflammatory signals, while promoting anti-inflammatory signals.1 Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces.1 Patients who require long-term treatment with a corticosteroid should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.1

Mechanism of action

Glucocorticoids inhibit neutrophil apoptosis and demargination, and inhibit NF-Kappa B and other inflammatory transcription factors.1 They also inhibit phospholipase A2, leading to decreased formation of arachidonic acid derivatives.1 In addition, glucocorticoids promote anti-inflammatory genes like interleukin-10.1

Corticosteroids like betamethasone can act through nongenomic and genomic pathways.3 The genomic pathway is slower and occurs when glucocorticoids activate glucocorticoid receptors and initiate downstream effects that promote transcription of anti-inflammatory genes including phosphoenolpyruvate carboxykinase (PEPCK), IL-1-receptor antagonist, and tyrosine amino transferase (TAT).3 On the other hand, the nongenomic pathway is able to elicit a quicker response by modulating T-cell, platelet and monocyte activity through the use of existing membrane-bound receptors and second messengers.3

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
Absorption

The absorption and potency of any topical corticosteroid including betamethasone depends on the vehicle in which the steroid is delivered. For example, betamethasone dipropionate 0.05% ointment is classified as a highly potent topical steroid, while betamethasone dipropionate 0.05% cream or lotion is considered to be moderately potent.4

There are several structural modifications that can determine the potency of a topical corticosteroid. For example, corticosteroids containing a halogen at specific carbons, or that contain esters are more potent due to enhanced lipophilicity.5 As such, there is a marked difference between topical products containing betamethasone dipropionate vs. betamethasone valerate. Betamethasone dipropionate contains 2 esters which enhances its potency, while betamethasone valerate has only one ester and is less potent.5

It should be noted that the use of occlusive dressings with topical steroids significantly increases the absorption, increasing the risk for adverse effects.14

Volume of distribution

In a study that included Indian women of reproductive age, the volume of distribution following a single intramuscular dose of betamethasone phosphate was 94,584±23,539 mL(s).9

Protein binding

Betamethasone valerate binds to serum albumin and corticosteroid-binding globulin.7,8

Metabolism

The metabolism of betamethasone yields 6 metabolites.10 The metabolic processes include 6β hydroxylation, 11β-hydroxyl oxidation, and reduction of the C-20 carbonyl group followed by removal of the side chain.10

Route of elimination

Corticosteroids are eliminated predominantly in the urine.2

Half-life

In a study that included Indian women of reproductive age, the half-life following a single intramuscular dose of betamethasone phosphate was 10.2 ± 2.5 hours.9

Clearance

In a study that included Indian women of reproductive age, the CL/F following a single intramuscular dose of betamethasone phosphate was 6,466 ± 805 mL/hour.9

Adverse Effects
Adverseeffects
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Toxicity

Chronic high doses of glucocorticoids can lead to the development of cataracts, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.6 Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.6

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Betamethasone can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Betamethasone is combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Betamethasone.
AbirateroneThe metabolism of Betamethasone can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Betamethasone.
AcarboseThe risk or severity of hyperglycemia can be increased when Betamethasone is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Betamethasone is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Betamethasone is combined with Acemetacin.
AcenocoumarolBetamethasone may increase the anticoagulant activities of Acenocoumarol.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Betamethasone is combined with Acetohexamide.
Interactions
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Food Interactions
No interactions found.

Products

Products2
Drug product information from 10+ global regions
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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
IngredientUNIICASInChI Key
Betamethasone acetateTI05AO53L7987-24-6AKUJBENLRBOFTD-QZIXMDIESA-N
Betamethasone benzoate877K0XW47A22298-29-9SOQJPQZCPBDOMF-YCUXZELOSA-N
Betamethasone dipropionate826Y60901U5593-20-4CIWBQSYVNNPZIQ-XYWKZLDCSA-N
Betamethasone sodium phosphate7BK02SCL3W151-73-5PLCQGRYPOISRTQ-LWCNAHDDSA-L
Betamethasone valerate9IFA5XM7R22152-44-5SNHRLVCMMWUAJD-SUYDQAKGSA-N
International/Other Brands
Bentelan (Defiante) / Betnovate (GlaxoSmithKline) / Celestamine (Schering-Plough) / Diprosone (Schering-Plough) / Procort / Rinderon (Shionogi Seiyaku)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Beben Gel 0.025%Gel0.025 %TopicalParke Davis Division, Warner Lambert Canada Inc.1973-12-311999-04-08Canada flag
Betacort Scalp Lotion 0.1%Liquid.1 %TopicalIcn Pharmaceuticals1981-12-312005-04-26Canada flag
Betaderm Crm 0.05%Cream0.05 %TopicalTaro Pharmaceuticals, Inc.1979-12-31Not applicableCanada flag
Betaderm Crm 0.1%Cream0.1 %TopicalTaro Pharmaceuticals, Inc.1979-12-31Not applicableCanada flag
Betaderm Lotion 0.1%Lotion0.1 %TopicalTaro Pharmaceuticals, Inc.1979-12-31Not applicableCanada flag
Betaderm Ont 0.05%Ointment0.05 %TopicalTaro Pharmaceuticals, Inc.1979-12-31Not applicableCanada flag
Betaderm Ont 0.1%Ointment0.1 %TopicalTaro Pharmaceuticals, Inc.1988-12-31Not applicableCanada flag
Betagel - 0.1%Gel.1 %TopicalUcb Inc1996-12-061998-04-21Canada flag
Betamethasone DipropionateOintment0.5 mg/1gTopicalA S Medication Solutions1984-09-04Not applicableUS flag
Betamethasone DipropionateOintment0.5 mg/1gTopicalPreferred Pharmaceuticals Inc.2017-04-172019-06-19US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BetamethasoneCream0.5 mg/1gTopicalImpax Generics2004-01-232017-06-30US flag
Betamethasone DipropionateCream0.5 mg/1gTopicalA-S Medication Solutions2008-09-23Not applicableUS flag
Betamethasone DipropionateOintment0.5 mg/1gTopicalPhysicians Total Care, Inc.1994-04-27Not applicableUS flag
Betamethasone DipropionateCream0.5 mg/1gTopicalCosette Pharmaceuticals, Inc.2018-10-12Not applicableUS flag
Betamethasone DipropionateLotion, augmented0.5 mg/1mLTopicalTeligent Pharma, Inc.2018-02-14Not applicableUS flag
Betamethasone DipropionateOintment0.5 mg/1gTopicalH.J. Harkins Company, Inc.2015-01-04Not applicableUS flag
Betamethasone DipropionateCream0.5 mg/1gTopicalA-S Medication Solutions2018-10-12Not applicableUS flag
Betamethasone DipropionateOintment0.5 mg/1gTopicalActavis Pharma, Inc.1997-02-01Not applicableUS flag
Betamethasone DipropionateCream0.5 mg/1gTopicalPreferreed Pharmaceuticals Inc.1987-02-032011-02-15US flag
Betamethasone DipropionateCream0.5 mg/1gTopicalGolden State Medical Supply, Inc.1992-04-30Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ซาโนเบท ครีมCream0.1 %w/wบริษัท โอสถ อินเตอร์ แลบบอราทอรีส์ จำกัด จำกัด2007-03-26Not applicableThailand flag
เบต้าเนทCream0.05 %w/wห้างหุ้นส่วนจำกัด โรงงานเลิศสิงห์เภสัชกรรม1997-06-05Not applicableThailand flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Amolg ABetamethasone valerate (0.61 mg/1g) + Gentamicin sulfate (1 mg/1g)CreamTopicalOASIS TRADING2018-11-15Not applicableUS flag
BECLODERM NBetamethasone valerate (0.04 g) + Clotrimazole (1 g) + Neomycin sulfate (0.5 g)CreamTopicalQUIMICA PATRIC LTDA.2010-04-122015-09-16Colombia flag
BELOGENT %0,05+%0,1 KREM, 15 GBetamethasone dipropionate (0.05 %) + Gentamicin sulfate (0.1 %)CreamTopicalFARMA-TEK İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
BELOGENT %0,05+%0,1 KREM, 30 GBetamethasone dipropionate (0.05 %) + Gentamicin sulfate (0.1 %)CreamTopicalFARMA-TEK İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
BELOGENT %0,05+%0,1 MERHEM, 15 GBetamethasone dipropionate (0.05 %) + Gentamicin sulfate (0.1 %)OintmentTopicalFARMA-TEK İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
BELOGENT %0,05+%0,1 MERHEM, 30 GBetamethasone dipropionate (0.05 %) + Gentamicin sulfate (0.1 %)OintmentTopicalFARMA-TEK İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
BEMETH - NBetamethasone (0.1 G/100G) + Neomycin sulfate (0.5 G/100G)CreamTopicalบริษัท โอสถ อินเตอร์ แลบบอราทอรีส์ จำกัด จำกัด2002-08-28Not applicableThailand flag
BERIMON FORTEBetamethasone (0.25 MG) + Dexchlorpheniramine maleate (4 MG) + Phenylephrine hydrochloride (10 MG)Capsuleบริษัท พอนด์ เคมีคอล จำกัด2018-11-01Not applicableThailand flag
BERIMON NASAL CAPSULEBetamethasone (0.25 MG) + Dexchlorpheniramine maleate (2 MG) + Phenylephrine hydrochloride (10 MG)CapsuleNasalห้างหุ้นส่วนสามัญนิติบุคคล โรงงานเภสัชกรรมพอนด์เคมีคอลประเทศไทย2018-09-20Not applicableThailand flag
BERIMON NASAL CAPSULEBetamethasone (0.25 MG) + Dexchlorpheniramine maleate (2 MG) + Phenylephrine hydrochloride (10 MG)CapsuleNasalบริษัท พอนด์ เคมีคอล จำกัด2018-12-06Not applicableThailand flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Amolg ABetamethasone valerate (0.61 mg/1g) + Gentamicin sulfate (1 mg/1g)CreamTopicalOASIS TRADING2018-11-15Not applicableUS flag
Betalido KitBetamethasone sodium phosphate (3 mg/1mL) + Betamethasone acetate (3 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitInfiltration; Intra-articular; Intralesional; Intramuscular; Perineural; TopicalAsclemed Usa, Inc.2014-06-13Not applicableUS flag
Betalido KitBetamethasone sodium phosphate (3 mg/1mL) + Betamethasone acetate (3 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitInfiltration; Intra-articular; Intralesional; Intramuscular; Perineural; TopicalAsclemed Usa, Inc.2014-06-13Not applicableUS flag
Betaloan SUIKBetamethasone sodium phosphate (3 mg/1mL) + Betamethasone acetate (3 mg/1mL)Injection, suspensionIntra-articular; Intralesional; IntramuscularAsclemed Usa, Inc.2010-04-28Not applicableUS flag
Betaloan SUIKBetamethasone sodium phosphate (3 mg/1mL) + Betamethasone acetate (3 mg/1mL)Injection, suspensionIntra-articular; Intralesional; IntramuscularAsclemed Usa, Inc.2010-04-28Not applicableUS flag
Betamethasone Combo 6mg/mL PFBetamethasone acetate (3 mg/1mL) + Betamethasone sodium phosphate (3 mg/1mL)Injection, suspensionEpidural; Intramuscular; Intraspinal; IntrathecalUs Compounding, Inc2013-12-202015-09-11US flag
Betamethasone Combo 6mg/mL PFBetamethasone acetate (3 mg/1mL) + Betamethasone sodium phosphate (3 mg/1mL)Injection, suspensionEpidural; Intramuscular; Intraspinal; IntrathecalUs Compounding, Inc2013-12-202015-09-11US flag
Betamethasone Combo 7mg/mLBetamethasone acetate (3 mg/1mL) + Betamethasone sodium phosphate (4 mg/1mL)Injection, suspensionIntramuscularUs Compounding, Inc2013-12-202015-09-11US flag
Betamethasone Combo 7mg/mLBetamethasone acetate (3 mg/1mL) + Betamethasone sodium phosphate (4 mg/1mL)Injection, suspensionIntramuscularUs Compounding, Inc2013-12-202015-09-11US flag
Betamethasone Dipropionate 0.05% / Minoxidil 5%Betamethasone dipropionate (0.05 g/100g) + Minoxidil (5 g/100g)SolutionTopicalSincerus Florida, LLC2019-05-01Not applicableUS flag

Categories

ATC Codes
R01AD06 — BetamethasoneD07BC01 — Betamethasone and antisepticsS01BA06 — BetamethasoneS01BB04 — Betamethasone and mydriaticsS01CB04 — BetamethasoneH02AB01 — BetamethasoneC05AA05 — BetamethasoneS03CA06 — Betamethasone and antiinfectivesD07XC01 — BetamethasoneD07AC01 — BetamethasoneA07EA04 — BetamethasoneS02BA07 — BetamethasoneR03BA04 — BetamethasoneS03BA03 — BetamethasoneS01CA05 — Betamethasone and antiinfectivesD07CC01 — Betamethasone and antibiotics
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
Alternative Parents
Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 11-beta-hydroxysteroids / 17-hydroxysteroids / 3-oxo delta-1,4-steroids / Halogenated steroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols
show 8 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 9-halo-steroid / Alcohol / Aliphatic homopolycyclic compound
show 23 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:3077)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
9842X06Q6M
CAS number
378-44-9
InChI Key
UREBDLICKHMUKA-DVTGEIKXSA-N
InChI
InChI=1S/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15-,16-,17-,19-,20-,21-,22-/m0/s1
IUPAC Name
(1R,2S,3aS,3bS,9aS,9bR,10S,11aS)-9b-fluoro-1,10-dihydroxy-1-(2-hydroxyacetyl)-2,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES
[H][C@@]12C[C@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C

References

Synthesis Reference

Fernando AHUMADA AYALA, "SKIN-CARE PREPARATIONS CONTAINING MUPIROCIN AND BETAMETHASONE DIPROPIONATE." U.S. Patent US20100063015, issued March 11, 2010.

US20100063015
General References
  1. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
  2. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
  3. Uva L, Miguel D, Pinheiro C, Antunes J, Cruz D, Ferreira J, Filipe P: Mechanisms of action of topical corticosteroids in psoriasis. Int J Endocrinol. 2012;2012:561018. doi: 10.1155/2012/561018. Epub 2012 Nov 5. [Article]
  4. Spada F, Barnes TM, Greive KA: Comparative safety and efficacy of topical mometasone furoate with other topical corticosteroids. Australas J Dermatol. 2018 Aug;59(3):e168-e174. doi: 10.1111/ajd.12762. Epub 2018 Feb 7. [Article]
  5. Mehta AB, Nadkarni NJ, Patil SP, Godse KV, Gautam M, Agarwal S: Topical corticosteroids in dermatology. Indian J Dermatol Venereol Leprol. 2016 Jul-Aug;82(4):371-8. doi: 10.4103/0378-6323.178903. [Article]
  6. Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [Article]
  7. Pontremoli C, Barbero N, Viscardi G, Visentin S: Insight into the interaction of inhaled corticosteroids with human serum albumin: A spectroscopic-based study. J Pharm Anal. 2018 Feb;8(1):37-44. doi: 10.1016/j.jpha.2017.07.003. Epub 2017 Jul 5. [Article]
  8. Simard M, Underhill C, Hammond GL: Functional implications of corticosteroid-binding globulin N-glycosylation. J Mol Endocrinol. 2018 Feb;60(2):71-84. doi: 10.1530/JME-17-0234. Epub 2017 Dec 22. [Article]
  9. Jobe AH, Milad MA, Peppard T, Jusko WJ: Pharmacokinetics and Pharmacodynamics of Intramuscular and Oral Betamethasone and Dexamethasone in Reproductive Age Women in India. Clin Transl Sci. 2020 Mar;13(2):391-399. doi: 10.1111/cts.12724. Epub 2019 Dec 13. [Article]
  10. Butler J, Gray CH: The metabolism of betamethasone. J Endocrinol. 1970 Mar;46(3):379-90. doi: 10.1677/joe.0.0460379. [Article]
  11. Authors unspecified: Corticosteroids . [Article]
  12. FDA Approved Drug Products: Diprosone (Betamethasone dipropionate) ointment [Link]
  13. FDA Approved Drug Products: Celestone Soluspan (betamethasone sodium phosphate and betamethasone acetate) injectable suspension [Link]
  14. DIPROLENE® (augmented betamethasone dipropionate) ointment, for topical use - FDA Label [Link]
  15. FDA Approved Drug Products: Luxiq (betamethasone valerate) Foam [Link]
  16. FDA Approved Drug Products: Enstilar (calcipotriene and betamethasone dipropionate) foam [Link]
  17. Celestone Soluspan Product Insert (Injectable) [File]
Human Metabolome Database
HMDB0014586
KEGG Drug
D00244
PubChem Compound
9782
PubChem Substance
46505155
ChemSpider
9399
BindingDB
73823
RxNav
1514
ChEBI
3077
ChEMBL
CHEMBL632
ZINC
ZINC000003876136
Therapeutic Targets Database
DAP001043
PharmGKB
PA164754818
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Betamethasone
FDA label
Download (37.5 KB)
MSDS
Download (71.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentDeQuervain's Tendinopathy1
4Active Not RecruitingTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4CompletedOtherPsoriasis Vulgaris (Plaque Psoriasis)1
4CompletedPreventionHand Eczema1
4CompletedPreventionNeonatal Distress1
4CompletedPreventionPreterm Delivery1
4CompletedSupportive CareAdherence1
4CompletedTreatmentAlopecia Areata (AA)1
4CompletedTreatmentBack Pain Lower Back / Stenosis, Spinal1
4CompletedTreatmentBack pain / Neck Pain1

Pharmacoeconomics

Manufacturers
  • Schering corp sub schering plough corp
  • Parke davis div warner lambert co
  • Parke davis pharmaceutical research div warner lambert co
  • Altana inc
  • Glenmark generics inc usa
  • Perrigo new york inc
  • Taro pharmaceuticals usa inc
  • Tolmar inc
  • Schering corp
  • Savage laboratories inc div altana inc
  • Actavis mid atlantic llc
  • E fougera div altana inc
  • Pharmaderm div altana inc
  • Teva pharmaceuticals usa inc
  • Alpharma us pharmaceuticals division
  • Taro pharmaceuticals inc
  • Teva pharmaceuticals usa
  • Watson laboratories inc
  • Connectics corp
  • Tj roaco ltd
  • Pharmafair inc
  • Stat trade inc
Packagers
  • Accra Pac Inc.
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • American Regent
  • A-S Medication Solutions LLC
  • C.O. Truxton Inc.
  • Clint Pharmaceutical Inc.
  • Contract Pharm
  • Crown Laboratories Inc.
  • Darby Dental Supply Co. Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • DPT Laboratories Ltd.
  • E. Fougera and Co.
  • Faithful Friends Homeopathic Inc.
  • Genesis Pharmaceutical Inc.
  • Glenmark Generics Ltd.
  • Hikma Pharmaceuticals
  • Major Pharmaceuticals
  • Martin Surgical Supply
  • Mason Distributors
  • Medisca Inc.
  • Merit Pharmaceuticals
  • Nycomed Inc.
  • Palmetto Pharmaceuticals Inc.
  • Patheon Inc.
  • Perrigo Co.
  • Pharmaforce Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Qualitest
  • Quality Care
  • Rebel Distributors Corp.
  • SAL Pharma
  • Sandoz
  • Savage Labs
  • Schering Corp.
  • Stat Rx Usa
  • Stiefel Labs
  • Taro Pharmaceuticals USA
  • Teva Pharmaceutical Industries Ltd.
  • Tolmar Inc.
  • Warrick Pharmaceuticals Corp.
Dosage Forms
FormRouteStrength
Injection, solutionParenteral1.5 MG/2ML
Injection, solutionParenteral4 MG/2ML
OintmentOphthalmic
Solution / dropsAuricular (otic); Ophthalmic
SyrupOral
Tablet
GelTopical0.025 %
OintmentOphthalmic
SprayNasal50 mcg/1dose
TabletOral
CreamTopical1 mg/g
Tablet
Cream
CapsuleOral1 MG
CapsuleOral2 MG
InjectionIntramuscular; Intravenous4 mg/2ml
Injection, solutionIntramuscular; Intravenous1.5 MG/2ML
Injection, solutionIntramuscular; Intravenous4 MG/2ML
OintmentCutaneous
Ointment
Capsule
CapsuleNasal
EmulsionTopical
KitInfiltration
GelConjunctival
OintmentConjunctival
Solution / dropsConjunctival
Suspension / dropsConjunctival
Suspension / dropsConjunctival0.5 %
LiquidTopical.1 %
SuspensionIntramuscular5 mg
SolutionOral1 mg/g
GelTopical.1 %
Cream
SuspensionIntra-articular; Intralesional; Intramuscular
KitInfiltration; Intra-articular; Intralesional; Intramuscular; Perineural; Topical
CreamCutaneous
CreamTopical0.05 g
CreamTopical0.064 g
SuspensionIntra-articular; Intralesional; Intramuscular5 mg
SolutionIntramuscular; Intravenous8 mg
SolutionIntramuscular; Intravenous4 mg
OintmentTopical61.728 mg
OintmentTopical0.05 g
CreamTopical100 mg
CreamTopical0.1 g
TabletOral0.5 MG
TabletOral1 MG
Injection, solutionParenteral4 MG/1ML
Injection, suspensionEpidural; Intramuscular; Intraspinal; Intrathecal
Injection, suspensionIntramuscular
CreamTopical.64 mg/1g
CreamTopical0.5 mg/1g
CreamTopical0.64 mg/1g
Cream, augmentedTopical0.5 mg/1g
GelTopical.50 mg/1g
GelTopical0.5 mg/1g
GelTopical0.64 mg/1g
LotionTopical0.5 mg/1mL
Lotion, augmentedTopical0.5 mg/1mL
OintmentTopical0.05 mg/1g
OintmentTopical0.5 mg/1g
Ointment, augmentedTopical0.5 mg/1g
SolutionTopical
LotionTopical0.64 mg/1mL
Injection, solutionEpidural; Intramuscular; Intraspinal; Intrathecal12 mg/1mL
CreamTopical0.1 %
CreamTopical1 mg/1g
CreamTopical1.2 mg/1g
LotionCutaneous1 mg/1mL
LotionTopical1 mg/1mL
OintmentTopical1 mg/1g
OintmentTopical1.2 mg/1g
LotionTopical1.22 mg / g
CreamTopical.05 %
CreamTopical.64 mg / g
LotionTopical.64 mg / g
OintmentTopical.64 mg / g
SolutionIntra-articular; Intralesional; Intramuscular; Intravenous8 mg
PatchTopical0.1 % w/w
Plaster
Tablet, effervescentOral
Solution / drops; suspension / dropsNasal
Solution / dropsAuricular (otic); Ophthalmic.1 %
LiquidAuricular (otic); Ophthalmic0.1 %
TabletTopical0.1 mg
EnemaRectal5 mg / 100 mL
TabletOral.5 mg / tab
Tablet, effervescentOral0.5 mg / evt
CreamTopical
OintmentTopical
SolutionTopical
CreamTopical.1 %
LotionTopical0.1 g
Lotion
LotionTopical.1 %
OintmentTopical.1 %
Aerosol, foamCutaneous0.1 %
OintmentCutaneous
SprayNasal
Spray, suspensionNasal
InjectionIntra-arterial; Intradermal; Intralesional; Intramuscular
GelTopical
InjectionIntra-articular; Intralesional; Intramuscular
Injection, suspensionParenteral
OintmentTopical0.1 %
SprayTopical
Injection, solution
SolutionOral0.6 mg/5mL
Solution / dropsOral
Tablet, coated
InjectionIntralesional; Intramuscular
Tablet, extended releaseOral1 mg
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Soft tissue
SuspensionIntra-articular; Intrabursal; Intradermal; Intramuscular
SyrupOral12 mg
TabletOral2 mg
CreamTopical
PatchTopical
Gel
Aerosol, foamTopical1 mg/g
InsertVaginal
KitTopical
LotionTopical0.5 mg/1g
Injection
Ointment
Ointment0.5 mg/g
CreamOphthalmic
CreamTopical0.05 % w/w
GelTopical
LotionTopical0.05 % w/w
OintmentTopical0.05 %
OintmentTopical0.05 % w/w
SolutionOral0.5 mg/g
SolutionTopical0.05 %
OintmentTopical0.05 %w/w
CreamTopical0.05 %
Suspension
InjectionIntradermal; Intralesional
SuspensionIntramuscular
LiquidAuricular (otic); Ophthalmic
GelCutaneous
CreamTopical0.05 g/100g
OintmentTopical0.05 g/100g
Cream1 MG/G
EmulsionTopical1 MG/G
LotionTopical
Ointment1 MG/G
SolutionTopical0.5 MG/G
Aerosol, foamTopical
Aerosol, foamCutaneous
CreamCutaneous
SolutionAuricular (otic); Ophthalmic
Solution / dropsOphthalmic
SuspensionParenteral
SyrupOral0.01 g
LotionTopical
Aerosol, foamTopical0.12 %
Aerosol, foamTopical1.2 mg/1g
KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Topical
CreamTopical1 MG
LotionAuricular (otic); Ophthalmic
OintmentAuricular (otic); Ophthalmic
Tablet, film coated
LotionTopical.05 %
SolutionAuricular (otic)
Solution / dropsAuricular (otic)
CreamTopical0.1 % w/w
CreamTopical0.5 MG/G
KitIntra-articular; Intralesional; Intramuscular
Injection, suspensionIntra-articular; Intralesional; Intramuscular
CreamTopical0.5 mg / g
LotionTopical.5 mg / g
OintmentTopical.5 mg / g
CreamTopical.5 mg / g
OintmentTopical.05 %
SprayTopical0.5 mg/1g
SolutionCutaneous
SolutionOral0.1 %
EmulsionTopical0.1 %
Ointment0.1 %
Injection, solutionParenteral
OintmentTopical
Spray, meteredTopical
SuspensionTopical
LotionTopical0.05 %
LotionTopical0.1 %
LotionTopical0.1 % w/w
Solution / dropsOphthalmic
InjectionIntradermal; Intralesional; Intramuscular
Cream0.2 %w/w
Tablet, film coated0.5 mg
Cream0.1 %w/w
EmulsionTopical
Tablet0.6 mg
Cream0.05 %w/w
Ointment0.05 %w/w
Prices
Unit descriptionCostUnit
Luxiq 0.12% Foam 100 gm Can325.17USD can
Luxiq 0.12% Foam 50 gm Can174.7USD can
Diprolene 0.05% Lotion 60ml Bottle148.19USD bottle
Diprolene 0.05% Ointment 50 gm Tube147.41USD tube
Diprolene AF 0.05% Cream 50 gm Tube147.02USD tube
Betamethasone Dipropionate Aug 0.05% Ointment 45 gm Tube118.42USD tube
Diprolene 0.05% Gel 50 gm Tube103.99USD tube
Betamethasone Dipropionate Aug 0.05% Lotion 60ml Bottle100.64USD bottle
Betamethasone Dipropionate Aug 0.05% Cream 50 gm Tube88.66USD tube
Betamethasone Dipropionate Aug 0.05% Gel 50 gm Tube88.26USD tube
Diprolene 0.05% Lotion 30ml Bottle78.79USD bottle
Betamethasone acetate powd78.03USD g
Diprolene 0.05% Ointment 15 gm Tube69.38USD tube
Diprolene AF 0.05% Cream 15 gm Tube69.38USD tube
Betamethasone Dipropionate Aug 0.05% Ointment 15 gm Tube58.83USD tube
Betamethasone sod phos powder56.61USD g
Diprolene 0.05% Gel 15 gm Tube49.99USD tube
Betamethasone dp powder48.96USD g
Betamethasone valerate powd47.89USD g
Maxivate 0.05% Cream 45 gm Tube44.99USD tube
Betamethasone Dipropionate 0.05% Lotion 60ml Bottle40.4USD bottle
Betamethasone Dipropionate Aug 0.05% Cream 15 gm Tube39.62USD tube
Betamethasone Dipropionate Aug 0.05% Gel 15 gm Tube39.46USD tube
Betamethasone Dipropionate 0.05% Ointment 45 gm Tube19.67USD tube
Betamethasone Dipropionate 0.05% Cream 45 gm Tube18.9USD tube
Betamethasone Valerate 0.1% Lotion 60ml Bottle16.99USD bottle
Betamethasone Valerate 0.1% Ointment 45 gm Tube15.87USD tube
Beta-Val 0.1% Lotion 60ml Bottle14.99USD bottle
Betamethasone Dipropionate 0.05% Ointment 15 gm Tube13.51USD tube
Betamethasone Dipropionate 0.05% Cream 15 gm Tube12.99USD tube
Betamethasone Valerate 0.1% Cream 45 gm Tube12.99USD tube
Beta-Val 0.1% Cream 45 gm Tube12.99USD tube
Betamethasone Valerate 0.1% Cream 15 gm Tube11.99USD tube
Betamethasone Valerate 0.1% Ointment 15 gm Tube11.99USD tube
Beta-Val 0.1% Cream 15 gm Tube11.99USD tube
Betnesol (5 mg/100Ml) 5 mg/enm Enema9.51USD enema
Celestone soluspan 6 mg/ml8.08USD ml
Betamethasone ac-sp 6 mg/ml vial7.68USD ml
Luxiq 0.12% foam5.01USD g
Diprolene af 0.05% cream4.19USD g
Lotrisone 1-0.05% Lotion2.89USD ml
Lotrisone cream2.71USD g
Betamethasone dp aug 0.05% crm2.17USD g
Diprolene Glycol 0.05 % Glycol Cream0.54USD g
Diprolene Glycol 0.05 % Glycol Ointment0.54USD g
Ratio-Topilene 0.05 % Glycol Cream0.54USD g
Ratio-Topilene 0.05 % Glycol Ointment0.54USD g
Diprolene Glycol 0.05 % Glycol Lotion0.49USD g
Ratio-Topilene 0.05 % Glycol Lotion0.49USD g
Prevex B 0.1 % Occlusive Cream0.4USD g
Beta-val 0.1% cream0.32USD g
Ratio-Ectosone Regular 0.1 % Lotion0.3USD g
Ratio-Ectosone Mild 0.05 % Lotion0.23USD g
Diprosone 0.05 % Ointment0.23USD g
Ratio-Topisone 0.05 % Ointment0.23USD g
Diprosone 0.05 % Cream0.21USD g
Diprosone 0.05 % Lotion0.21USD g
Ratio-Topisone 0.05 % Cream0.21USD g
Ratio-Topisone 0.05 % Lotion0.21USD g
Betamethasone va 0.1% cream0.14USD g
Betaderm Regular 0.1 % Ointment0.1USD g
Ratio-Ectosone Regular 0.1 % Cream0.1USD g
Valisone Scalp 0.1 % Lotion0.1USD g
Betaderm Regular 0.1 % Cream0.09USD g
Ratio-Ectosone Scalp 0.1 % Lotion0.09USD g
Betaderm Mild 0.05 % Ointment0.07USD g
Betaderm Mild 0.05 % Cream0.06USD g
Ratio-Ectosone Mild 0.05 % Cream0.06USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6126920No2000-10-032016-03-01US flag
US7078058No2006-07-182017-05-24US flag
US6753013No2004-06-222020-01-27US flag
US6787529No2004-09-072020-01-27US flag
US9119781Yes2015-09-012031-12-10US flag
US9439911No2016-09-132030-08-31US flag
US9433630No2016-09-062030-08-31US flag
US9655907No2017-05-232030-08-31US flag
US9364485No2016-06-142030-08-31US flag
US9775851No2017-10-032030-08-31US flag
US9877974No2018-01-302030-08-31US flag
US10130640Yes2018-11-202031-12-10US flag
US10179137No2019-01-152030-08-31US flag
US9566286No2017-02-142031-06-10US flag
US10617698No2011-06-102031-06-10US flag
US10660908No2011-06-102031-06-10US flag
US10688108No2011-06-102031-06-10US flag
US10682364No2011-06-102031-06-10US flag
US10716799No2011-06-102031-06-10US flag
US10265265No2007-09-272027-09-27US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)178°Chttp://www.chemspider.com/Chemical-Structure.20490.html
boiling point (°C)568.2°Chttp://www.chemspider.com/Chemical-Structure.9399.html
water solubility66.5 mg/L (at 25 °C)EPA
logP1.138http://www.chemspider.com/Chemical-Structure.9399.html
logS-3.77ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0505 mg/mLALOGPS
logP1.93ALOGPS
logP1.68ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)12.42ChemAxon
pKa (Strongest Basic)-3.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area94.83 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity102.49 m3·mol-1ChemAxon
Polarizability40.81 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.992
Blood Brain Barrier+0.9781
Caco-2 permeable+0.8304
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor INon-inhibitor0.8112
P-glycoprotein inhibitor IINon-inhibitor0.8134
Renal organic cation transporterNon-inhibitor0.7971
CYP450 2C9 substrateNon-substrate0.8733
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7315
CYP450 1A2 substrateNon-inhibitor0.938
CYP450 2C9 inhibitorNon-inhibitor0.9106
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9247
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9169
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9399
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.1482 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9558
hERG inhibition (predictor II)Inhibitor0.5091
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0ab9-0239000000-6da1b4bf9567b7486622
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05i4-2930000000-bc11f96b96bcca3051a8
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dj-3960000000-a7dc9d06200fd3114dc2

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. Tanigawa K, Nagase H, Ohmori K, Tanaka K, Miyake H, Kiniwa M, Ikizawa K: Species-specific differences in the glucocorticoid receptor transactivation function upon binding with betamethasone-esters. Int Immunopharmacol. 2002 Jun;2(7):941-50. [Article]
  2. Aida K, Shi Q, Wang J, VandeBerg JL, McDonald T, Nathanielsz P, Wang XL: The effects of betamethasone (BM) on endothelial nitric oxide synthase (eNOS) expression in adult baboon femoral arterial endothelial cells. J Steroid Biochem Mol Biol. 2004 Aug;91(4-5):219-24. [Article]
  3. Johnstone JF, Bocking AD, Unlugedik E, Challis JR: The effects of chorioamnionitis and betamethasone on 11beta hydroxysteroid dehydrogenase types 1 and 2 and the glucocorticoid receptor in preterm human placenta. J Soc Gynecol Investig. 2005 May;12(4):238-45. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Matsunaga T, Maruyama M, Matsubara T, Nagata K, Yamazoe Y, Ohmori S: Mechanisms of CYP3A induction by glucocorticoids in human fetal liver cells. Drug Metab Pharmacokinet. 2012;27(6):653-7. doi: 10.2133/dmpk.dmpk-12-nt-018. Epub 2012 May 22. [Article]
  2. Academic disertation [Link]
  3. Celestone monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Paakki P, Kirkinen P, Helin H, Pelkonen O, Raunio H, Pasanen M: Antepartum glucocorticoid therapy suppresses human placental xenobiotic and steroid metabolizing enzymes. Placenta. 2000 Mar-Apr;21(2-3):241-6. doi: 10.1053/plac.1999.0471. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
  2. Matsunaga T, Maruyama M, Matsubara T, Nagata K, Yamazoe Y, Ohmori S: Mechanisms of CYP3A induction by glucocorticoids in human fetal liver cells. Drug Metab Pharmacokinet. 2012;27(6):653-7. doi: 10.2133/dmpk.dmpk-12-nt-018. Epub 2012 May 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Matsunaga T, Maruyama M, Matsubara T, Nagata K, Yamazoe Y, Ohmori S: Mechanisms of CYP3A induction by glucocorticoids in human fetal liver cells. Drug Metab Pharmacokinet. 2012;27(6):653-7. doi: 10.2133/dmpk.dmpk-12-nt-018. Epub 2012 May 22. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Pontremoli C, Barbero N, Viscardi G, Visentin S: Insight into the interaction of inhaled corticosteroids with human serum albumin: A spectroscopic-based study. J Pharm Anal. 2018 Feb;8(1):37-44. doi: 10.1016/j.jpha.2017.07.003. Epub 2017 Jul 5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Steroid binding
Specific Function
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name
SERPINA6
Uniprot ID
P08185
Uniprot Name
Corticosteroid-binding globulin
Molecular Weight
45140.49 Da
References
  1. Simard M, Underhill C, Hammond GL: Functional implications of corticosteroid-binding globulin N-glycosylation. J Mol Endocrinol. 2018 Feb;60(2):71-84. doi: 10.1530/JME-17-0234. Epub 2017 Dec 22. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [Article]

Drug created on June 13, 2005 13:24 / Updated on September 28, 2021 07:54