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Betamethasone

D07A - Corticosteroids, plain ATC D07CC01 Small molecule approved 1961 Oral Topical

JFDA label: Topizone Cream

Mechanism of Action

Agonist of Glucocorticoid receptor — Glucocorticoid receptor agonist

TargetActionGene / class
Glucocorticoid receptor efficacy AGONIST NR3C1

Indications

Approved

  • Eye Diseases — eye inflammation
  • Hemorrhoids — hemorrhoid
  • Lung Diseases, Obstructive — Airway obstruction
  • Nasal Obstruction — Nasal congestion

Off-label

  • Bronchiolitis
  • Carpal Tunnel Syndrome
  • Cough
  • Dermatitis, Atopic
  • Dry Eye Syndromes
  • Eczema
  • Glaucoma
  • Gout
  • Hyaline Membrane Disease
  • Hypersensitivity
  • Lichen Planus, Oral
  • Macular Edema
  • Melanoma
  • Neck Pain
  • Orbital Pseudotumor
  • Pharyngitis
  • Pregnancy
  • Premature Birth
  • Psoriasis
  • Respiratory Distress Syndrome
  • Respiratory Distress Syndrome, Newborn
  • Retinal Vein Occlusion
  • Rhinitis, Allergic, Seasonal
  • Sciatica
  • Tachypnea

Contraindications

Source: openFDA

  • Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is contraindicated in patients who are hypersensitive to any components of this product. Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura. Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Endocrine disorders (2)

Common Adrenal suppression (systemic / prolonged topical) · Cushing's syndrome (systemic)

Metabolism and nutrition disorders (1)

Common Hyperglycaemia (systemic)

Skin and subcutaneous tissue disorders (3)

Very Common Skin thinning / atrophy (topical)

Common Striae (topical) · Telangiectasia (topical, face)

Musculoskeletal and connective tissue disorders (1)

Common Osteoporosis (systemic long-term)

Infections and infestations (1)

Common Immunosuppression / opportunistic infections

Dosing

Source: openFDA

Benzyl alcohol as a preservative has been associated with a fatal “Gasping Syndrome” in premature infants and infants of low birth weight. Solutions used for further dilution of this product should be preservative-free when used in the neonate, especially the premature infant. The initial dosage of parenterally administered Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension may vary from 0.25 to 9 mg per day depending on the specific disease entity being treated. However, in certain overwhelming, acute, life-threatening situations, administrations in dosages exceeding the usual dosages may be justified and may be in multiples of the oral dosages. It Should Be Emphasized That Dosage Requirements Are Variable and Must Be Individualized on the Basis of the Disease Under Treatment and the Response of the Patient. After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. Situations which may make dosage adjustments necessary are changes in clinical status secondary to remissions or exacerbations in the disease process, the patient’s individual drug responsiveness, and the effect of patient exposure to stressful situations not directly related to the disease entity under treatment. In this latter situation it may be necessary to increase the dosage of the corticosteroid for a period of time consistent with the patient’s condition. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly. In the treatment of acute exacerbations of multiple sclerosis, daily doses of 30 mg of betamethasone for a week followed by 12 mg every other day for 1 month are recommended (see PRECAUTIONS, Neuro-psychiatric section). In pediatric patients, the initial dose of betamethasone may vary depending on the specific disease entity being treated. The range of initial doses is 0.02 to 0.3 mg/kg/day in three or four divided doses (0.6 to 9 mg/m 2 bsa/day). For the purpose of comparison, the following is the equivalent milligram dosage of the various glucocorticoids: Cortisone, 25 Triamcinolone, 4 Hydrocortisone, 20 Paramethasone, 2 Prednisolone, 5 Betamethasone, 0.75 Prednisone, 5 Dexamethasone, 0.75 Methylprednisolone, 4 These dose relationships apply only to oral or intravenous administration of these compounds. When these substances or their derivatives are injected intramuscularly or into joint spaces, their relative properties may be greatly altered. If coadministration of a local anesthetic is desired, Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension may be mixed with 1% or 2% lidocaine hydrochloride, using the formulations which do not contain parabens. Similar local anesthetics may also be used. Diluents containing methylparaben, propylparaben, phenol, etc., should be avoided, since these compounds may cause flocculation of the steroid. The required dose of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is first withdrawn from the vial into the syringe. The local anesthetic is then drawn in, and the syringe shaken briefly. Do not inject local anesthetics into the vial of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension. Bursitis, Tenosynovitis, Peritendinitis In acute subdeltoid, subacromial, olecranon, and prepatellar bursitis, one intrabursal injection of 1 mL Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension can relieve pain and restore full range of movement. Several intrabursal injections of corticosteroids are usually required in recurrent acute bursitis and in acute exacerbations of chronic bursitis. Partial relief of pain and some increase in mobility can be expected in both conditions after one or two injections. Chronic bursitis

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension should not be administered intravenously. Serious Neurologic Adverse Reactions with Epidural Administration Serious neurologic events, some resulting in death, have been reported with epidural injection of corticosteroids. Specific events reported include, but are not limited to, spinal cord infarction, paraplegia, quadriplegia, cortical blindness, and stroke. These serious neurologic events have been reported with and without use of fluoroscopy. The safety and effectiveness of epidural administration of corticosteroids have not been established, and corticosteroids are not approved for this use. General Rare instances of anaphylactoid reactions have occurred in patients receiving corticosteroid therapy (see ADVERSE REACTIONS ). In patients on corticosteroid therapy subjected to any unusual stress, hydrocortisone or cortisone is the drug of choice as a supplement during and after the event. Cardio-Renal Average and large doses of corticosteroids can cause elevation of blood pressure, salt and water retention, and increased excretion of potassium. These effects are less likely to occur with the synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation may be necessary. All corticosteroids increase calcium excretion. Literature reports suggest an apparent association between use of corticosteroids and left ventricular free wall rupture after a recent myocardial infarction; therefore, therapy with corticosteroids should be used with great caution in these patients. Endocrine Corticosteroids can produce reversible hypothalamic pituitary adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment. Metabolic clearance of corticosteroids is decreased in hypothyroid patients and increased in hyperthyroid patients. Changes in thyroid status of the patient may necessitate adjustment in dosage. Infections General Patients who are on corticosteroids are more susceptible to infections than are healthy individuals. There may be decreased resistance and inability to localize infection when corticosteroids are used. Infection with any pathogen (viral, bacterial, fungal, protozoan, or helminthic) in any location of the body may be associated with the use of corticosteroids alone or in combination with other immunosuppressive agents. These infections may be mild to severe. With increasing

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

Local injections, such as for tendinitis, would not be expected to cause any adverse

Chemistry & Properties

2D structure
FormulaC22H29FO5
Molecular weight392.47 g/mol
IUPAC name(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one
CAS378-44-9
PubChem CID9782
InChIKeyUREBDLICKHMUKA-DVTGEIKXSA-N
logP1.9 (XLogP 1.9)
Polar surface area94.83 Ų
H-bond acceptors / donors5 / 3
Drug-likeness (QED)0.67
Lipinski violations0
SMILESC[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life2.591 h
Volume of distribution1.116 L/kg
Protein binding71.6%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP2C8Inhibitor
CYP3A4Substrate

Receptor binding (top 1)

TargetActionAffinity
Glucocorticoid receptor (NR3C1) Agonist pIC50 8.1

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1A2 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Adalimumab major
Bacillus calmette-guerin substrain tice live antigen major
Baricitinib major
Bempedoic acid major
Brexucabtagene autoleucel major
Bupropion major
Certolizumab pegol major
Cinoxacin major
Ciprofloxacin major
Cladribine major
Deferasirox major
Delafloxacin major
Desirudin major
Desmopressin major
Dinutuximab major
Enoxacin major
Etanercept major
Fingolimod major
Gatifloxacin major
Gemifloxacin major
Golimumab major
Grepafloxacin major
Infliximab major
Iohexol major
Iopamidol major
Leflunomide major
Levofloxacin major
Lomefloxacin major
Measles virus vaccine live attenuated major
Mifepristone major
Moxifloxacin major
Mumps virus strain B level jeryl lynn live antigen major
Nalidixic acid major
Natalizumab major
Norfloxacin major
Ofloxacin major
Ozanimod major
Rotavirus vaccine major
Rubella virus vaccine major
Siponimod major

Showing 40 of 100+.

Registered Products (44)

BrandForm / strengthPackAgentCitizen (JOD)
Betasone Ointment Ointment 0.1 %w/w 15 g tube pack varies Professional Drug Store 0.590
Betaroid Ointment Ointment 0.1 %w/w 15 g tube pack varies JERASH PHARMACEUTICALS LTD.CO/JORDAN 0.740
Betaval-N Ointment Ointment (as 17-valerate) 0.1 %, ( as sulphate) 0.5 % 15 g tube The Arab Pharmaceutical Manufactruing Co. 0.760
Vasone Ointment Ointment (as valerate) USP 0.1 % w/w 15 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 0.800
Betaval Cream Cream 0.1 % 15 g tube pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 0.810
Betaval Ointment Ointment 0.1 % 15 g tube pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 0.810
Betaval-N Cream Cream 0.1 %, 0.5 % 15 g tube pack varies The Arab Pharmaceutical Manufactruing Co. 0.810
Bitnoval Skin Cream Cream As Valerate 0.1 % 15 g tube Amman Pharmaceutical Industries Co 0.810
Vasone Cream Cream (as valerate) USP 0.1 % 15 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 0.810
Bitnoval Oint Ointment (as valerate)0.1 % 15 gm Amman Pharmaceutical Indusries 0.890
Betaval-N Ointment Ointment (as 17-valerate) 0.1 %, (as sulphate) 0.5 % 30 g tube The Arab Pharmaceutical Manufactruing Co. 1.100
Betasone Ointment Ointment 0.1 %w/w 30 g tube pack varies Professional Drug Store 1.120
OPHTAMESONE Eye/Ear/Nasal Drops Ophthalmic Solution 0.1 % 10 ml Dar Al Dawa Development and Investment Co Ltd/Jordan 1.190
Beprosalic Ointment Ointment 0.05 %, 2 % 15 g tube Reda Jardaneh Drug Store 1.310
Betaval Cream Cream 0.1 % 30 g tube pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 1.350
Betaval Ointment Ointment 0.1 % 30 g tube pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 1.350
Betaval-N Cream Cream 0.1 %, 0.5 % 30 g tube pack varies The Arab Pharmaceutical Manufactruing Co. 1.350
Betaroid Ointment Ointment 0.1 %w/w 30 g tube pack varies JERASH PHARMACEUTICALS LTD.CO/JORDAN 1.400
Citadone 0.6mg/5ml Oral Solution Solution 0.6 mg/5 ml 100 ml UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 1.560
Fusibact-B Cream Cream 1.0 mg, 20 mg 15 g tube شركة مستودع ادوية الايمان 2.080
Betnovate Cream Cream 0.122 %w/w 30 g tube Suleiman Tannous & Sons Co. Ltd 2.160
Betnovate Ointment Ointment 0.1 % 30 g tube Suleiman Tannous & Sons Co. Ltd 2.160
Betnovate Scalp Application Lotion 0.122 %w/w 30 ml Suleiman Tannous & Sons Co. Ltd 2.250
Salibet Ointment Ointment 0.05 %, 3 % 30 g tube شركة مستودع ادوية الايمان 2.280
Betafucin skin cream Cream (Valerate)0.1 %, 2 % 15 g tube Amman Pharmaceutical Indusries 2.300
Topizone Cream Cream 0.1 %, 2 % 15 g tube Pharma International Company/ Jordan 2.300
Ezaderm Cream Cream 0.1 %, 2 % 15 gm UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 2.310
Sunnymethasone Ampoule 14 mg/2 ml 1 amp Mohamad Zreiqat Drug Store 2.380
Demancortil Ampoule 4 mg per 2 ml, 10 mg per 2 ml 1 amp Al-Omawai Drug Store 2.530
Uciderm B Cream Cream 0.1 %, 2 % 15 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 2.580
DIPROSONE Cream 0.5 mg 30 g tube Adatco Drug Store 2.690
Dermocid C Cream 1 mg/1gm, 20 mg/1gm 15 gm Dar Al Dawa Development and Investment Co Ltd/Jordan 2.710
Zydex-B Cream Cream (as Valerate)0.1 %, 2 % 15 g tube Sukhtian Group 2.710
FUCICORT Cream (as Valerate)1 mg/g, 20 mg/g 15 gm Khoury Drug Store 2.970
DIPROSALIC Ointment Ointment 0.5 mg, 30 mg/g 30 g tube Adatco Drug Store 3.250
DIPROFOS Injection Injection 2 mg/ml, 5 mg/ml 1 ampoule Adatco Drug Store 3.970
Tebeta Vial 4 mg/ml 3 vial MS PHARMA/JORDAN 4.020
Gentazole-B Cream Betamethasone Dipropionate 0.064 %WW, Clotrimazole 1.00 %WW, Gentamicin Sulphate 0.1 %WW (30 GM) / TUB Sana Pharmaceutical Industry Co. 4.800
Daivobet Ointment Ointment 0.5 mg/g, 50 mcg/g 15 g tube pack varies Khoury Drug Store 8.870
Beta-cal Gel Gel as Dipropionate 0.05 %, as Monohydrate 0.005 % 30 GM JERASH PHARMACEUTICALS LTD.CO/JORDAN 9.810
Daivobet Gel Gel 0.5 mg/g, 50 mcg/g 30 gm pack varies Khoury Drug Store 10.900
Psoriano Ointment Ointment 0.5 mg/g (as dipropionate), 50 mcg/g (as monohydrate) 30 GM/1 TUB SANA PHARMACEUTICAL INDUSTRY/JORDAN 14.000
Beta-cal Ointment Ointment 50 mcg/g, 0.5 mg/g 30 g tube JERASH PHARMACEUTICALS LTD.CO/JORDAN 14.730
Daivobet Ointment Ointment 0.5 mg/g, 50 mcg/g 30 g tube pack varies Khoury Drug Store 16.890