Betamethasone
JFDA label: Topizone Cream
Mechanism of Action
Agonist of Glucocorticoid receptor — Glucocorticoid receptor agonist
| Target | Action | Gene / 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
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
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
Local injections, such as for tendinitis, would not be expected to cause any adverse
Chemistry & Properties
| Formula | C22H29FO5 |
|---|---|
| Molecular weight | 392.47 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 |
| CAS | 378-44-9 |
| PubChem CID | 9782 |
| InChIKey | UREBDLICKHMUKA-DVTGEIKXSA-N |
| logP | 1.9 (XLogP 1.9) |
| Polar surface area | 94.83 Ų |
| H-bond acceptors / donors | 5 / 3 |
| Drug-likeness (QED) | 0.67 |
| Lipinski violations | 0 |
SMILES
C[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)COBiology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 2.591 h |
| Volume of distribution | 1.116 L/kg |
| Protein binding | 71.6% |
| BBB penetrant | No |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2C8 | Inhibitor | — |
| CYP3A4 | Substrate | — |
Receptor binding (top 1)
| Target | Action | Affinity |
|---|---|---|
| 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 drug | Severity | Management |
|---|---|---|
| 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)
| Brand | Form / strength | Pack | Agent | Citizen (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 |