Hydrocortisone

H02A - Corticosteroids for systemic use, plain ATC S02CA03 Small molecule approved 1952 Oral Parenteral Topical Natural product

JFDA label: Otosporin Ear / Drops

Mechanism of Action

Agonist of Glucocorticoid receptor — Glucocorticoid receptor agonist

Target	Action	Gene / class
Glucocorticoid receptor efficacy	AGONIST	NR3C1

Indications

Approved

Adrenal Hyperplasia, Congenital — classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency
Adrenal Insufficiency — adrenocortical insufficiency
Arthritis, Juvenile — juvenile idiopathic arthritis
Arthritis, Psoriatic — psoriatic arthritis
Arthritis, Rheumatoid — rheumatoid arthritis
Asthma — asthma
Bursitis — bursitis
Colitis, Ulcerative — ulcerative colitis
Conjunctivitis, Allergic — allergic conjunctivitis
Crohn Disease — Crohn's disease
Dermatitis — dermatitis
Dermatitis, Atopic — atopic eczema
Dermatitis, Seborrheic — seborrheic dermatitis
Endocrine System Diseases — endocrine system disease
Exanthema — exanthem
Eye Diseases — eye inflammation
Hemorrhoids — hemorrhoid
Herpes Labialis — Herpes Labialis
Inflammation — inflammation
Leukemia — leukemia
Lymphoma — lymphoma
Nasal Obstruction — Nasal congestion
Neoplasms — cancer
Osteoarthritis — osteoarthritis
Otitis Externa — otitis externa
Pneumonia — pneumonia
Pruritus — Pruritus
Psoriasis — psoriasis vulgaris
Serum Sickness — type III hypersensitivity reaction disease
Skin Diseases — skin disease
Spondylitis — spondylitis
Tenosynovitis — tenosynovitis

Off-label

Addison Disease
Adrenal Cortex Neoplasms
Aging
Alcoholism
Alopecia Areata
Anemia, Refractory
Anemia, Refractory, with Excess of Blasts
Atrial Fibrillation
Borderline Personality Disorder
Bronchopulmonary Dysplasia
Central Nervous System Neoplasms
Eczema
Granuloma, Pyogenic
Heart Arrest
Heart Failure
Hypotension
Hypoxia
Inflammatory Bowel Diseases
Influenza, Human
Leukemia, Biphenotypic, Acute
Leukemia, Erythroblastic, Acute
Leukemia, Lymphoid
Leukemia, Mast-Cell
Leukemia, Megakaryoblastic, Acute
Leukemia, Monocytic, Acute
Leukemia, Myeloid, Acute
Leukemia, Myelomonocytic, Acute
Leukemia, Myelomonocytic, Chronic
Liver Cirrhosis
Lymphohistiocytosis, Hemophagocytic
Lymphoma, Large B-Cell, Diffuse
Melanoma
Memory Disorders
Multiple Myeloma
Myelodysplastic Syndromes
Myeloproliferative Disorders
Myocardial Infarction
Neoplasms, Plasma Cell
Opioid-Related Disorders
Oral Submucous Fibrosis
Pain
Pancreatitis
Phobic Disorders
Pneumonia, Viral
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Prostatic Neoplasms
Prostatic Neoplasms, Castration-Resistant
Sepsis
Severe Acute Respiratory Syndrome
Shock, Septic
Wounds and Injuries

Contraindications

Source: openFDA

Cortifoam ® is contraindicated in patients who are hypersensitive to any components of this product. Local contraindications to the use of intrarectal steroids include obstruction, abscess, perforation, peritonitis, fresh intestinal anastomoses, extensive fistulas and sinus tracts. Absolute

Dosing

Source: openFDA

The usual dose is one applicatorful once or twice daily for two or three weeks, and every second day thereafter, administered rectally. Directions for use, below and on the carton, describe how to use the aerosol container and applicator. Satisfactory response usually occurs within five to seven days marked by a decrease in symptoms. Symptomatic improvement in ulcerative proctitis should not be used as the sole criterion for evaluating efficacy. Sigmoidoscopy is also recommended to judge dosage adjustment, duration of therapy, and rate of improvement. 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. Directions For Use (1) Shake foam container vigorously for 5-10 seconds before each use. Do not remove container cap during use of the product. (2) Hold container upright on a level surface and gently place the tip of the applicator onto the nose of the container cap. CONTAINER MUST BE HELD UPRIGHT TO OBTAIN PROPER FLOW OF MEDICATION. (3) Pull plunger past the fill line on the applicator barrel. (4) To fill applicator barrel, press down firmly on cap flanges, hold for 1 – 2 seconds and release. Pause 5 – 10 seconds to allow foam to expand in applicator barrel. Repeat until foam reaches fill line. Remove applicator from container cap. Allow some foam to remain on the applicator tip. A burst of air may come out of container with first pump. (5) Hold applicator firmly by barrel, making sure thumb and middle finger are positioned securely underneath and resting against barrel wings. Place index finger over the plunger. Gently insert tip into anus. Once in place, push plunger to expel foam, then withdraw applicator. CAUTION: Do not insert any part of the aerosol container directly into the anus. Apply to anus only with enclosed applicator. (6) After each use, applicator parts should be pulled apart for thorough cleaning with warm water. The container cap and underlying tip should also be pulled apart and rinsed to help prevent build-up of foam and possible blockage.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

General Do not insert any part of the aerosol container directly into the anus. Contents of the container are under pressure. Do not burn or puncture the aerosol container. Do not store at temperatures above 120°F. Because Cortifoam ® is not expelled, systemic hydrocortisone absorption may be greater from Cortifoam ® than from corticosteroid enema formulations. If there is not evidence of clinical or proctologic improvement within two or three weeks after starting Cortifoam ® therapy, or if the patient's condition worsens, discontinue the drug. Rare instances of anaphylactoid reactions have occurred in patients receiving corticosteroid therapy (see ADVERSE REACTIONS ). Cardio-renal 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 hypothalamicpituitary 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 doses of corticosteroids, the rate of occurrence of infectious complications increases. Corticosteroids may also mask some signs of current infection. Fungal infections Corticosteroids may exacerbate systemic fungal infections and therefore should not be used in the presence of such infections unless they are needed to control drug

Pregnancy & Lactation

Pregnancy

Lactation

No Data Hale L3

Maternal use of hydrocortisone as an enema would not be expected to cause any adverse

Chemistry & Properties

Formula	C21H30O5
Molecular weight	362.47 g/mol
IUPAC name	(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
CAS	50-23-7
PubChem CID	5754
InChIKey	`JYGXADMDTFJGBT-VWUMJDOOSA-N`
logP	1.78 (XLogP 1.6)
Polar surface area	94.83 Å²
H-bond acceptors / donors	5 / 3
Drug-likeness (QED)	0.70
Lipinski violations	0

SMILES

C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2[C@@H](O)C[C@@]2(C)[C@H]1CC[C@]2(O)C(=O)CO

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB -0.22)

Enzyme interactions

Enzyme	Role	Detail
CYP3A4	Substrate	—

Receptor binding (top 1)

Target	Action	Affinity
GPR33 (GPR33)	None	pKd 7.9

Transporters

BCRP (Inhibitor)BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)OATP (Inhibitor)OATP1A2 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OCT1 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)OAT3 (Substrate)OATP1A2 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Adalimumab	major
Amiodarone	major
Arsenic trioxide	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
Dofetilide	major
Dronedarone	major
Droperidol	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

Showing 40 of 100+.

Registered Products (32)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Alfacort Cream	Cream 1 %	15 g tube pack varies	Professional Drug Store	0.810
Alfacort Ointment	Ointment 1 %	15 g tube pack varies	Professional Drug Store	0.810
Nystaform Oint	Ointment 1 g, 3 g, 1 g	20 g tube	AL-Faiasel Drug Store	0.930
Otosporin Ear / Drops	Eye/Ear Drops 10 mg/ml, 3400 IU, 10000 IU	5 ml	Suleiman Tannous & Sons Co. Ltd	0.940
Hydrocort Skin Cream	Cream 1 %	15 g tube pack varies	Amman Pharmaceutical Indusries	1.000
Hydrocort Skin Ointment	Ointment 1 %	15 g tube pack varies	Amman Pharmaceutical Indusries	1.000
Hydrocortisone Sodium Succinate 100mg powder vila IV & IM injection	Powder for Injection 100 mg	1 amp pack varies	Reda Jardaneh Drug Store	1.000
Dermocort Cream	Cream 1 %, 3 %	20 g tube	Petra Drug Store	1.060
Topicort Cream	Cream 1 %	30 g tube	Hayat Pharmaceutical Industries CO.PLC/JORDAN	1.300
TERRACORTRIL E/E OINTMENT	Ointment 10 mg, 5 mg, 10000 IU	3.5 g tube	Sabbagh Drug Store	1.320
TERRACORTRIL E/E SUSP	Suspension 5.7 mg, 11.400 IU, 17 mg	5 ml	Sabbagh Drug Store	1.350
candicort cream	Cream 1 %, 2 %	15 g tube	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	1.460
Mycoten-HC Cream	Cream 1 %, 1 %	15 g tube	Sukhtian Group	1.480
Zona	Cream 0.1 %	30 gm	Pharma International Company/ Jordan	1.500
Alfacort Cream	Cream 1 %	30 g tube pack varies	Professional Drug Store	1.540
Alfacort Ointment	Ointment 1 %	30 g tube pack varies	Professional Drug Store	1.540
Hydrosone Inj	Powder for Injection 100 mg	One Vial pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	1.720
Hydrosone 100mg with	Vial 100 mg	1 vial pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	1.740
MYCOHEAL-HC CREAM	Cream 1 %, 2 %	15 g tube	Dar Al Dawa Development and Investment Co Ltd/Jordan	1.740
Daktacort cream	Cream 10 mg/g, 20 mg/g	15 g tube	Al-Amad Drug Store	1.810
Crotaphil-H Cream	Cream 10 %, 0.25 %	25 g tube	PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN	1.820
SOLU-CORTEF A.O.V INJ	Powder for Injection 100 mg	2 ml	Khoury Drug Store	2.020
Aquax-H Cream	Cream 0.1 %	30 g tube	PELLA PHARMACEUTICALS CO.LTD/JORDAN	2.310
Locoid Scalp Lotion	Lotion 0.1 %	30 ml	Shawi & Rushedat Drug Store	2.610
Zydex-HC Cream	Cream 2 %, 1 %	15 g tube	Sukhtian Group	2.990
Fucidin H Cream	Cream 20 mg/g, 10 mg/g	15 g tube	Khoury Drug Store	3.740
Hydrocortisone Medis	Vial Hydrocortisone Na-Succinate 100 mg	10 vial	Professional Drug Store	8.060
Hydrocortisone Medo Vial	Vial 100 mg	10 vial pack varies	Khoury Drug Store	9.950
Hydrosone 20 Tablets	Tablet 20 mg	100 tab	Hikma Pharmaceuticals Co.Ltd/Jordan	12.000
HYDROCORTISONE Sodium Succinate	Tablet 100 mg	50 vial	Reda Jardaneh Drug Store	61.080
Hydrocortisone Sodium Succinate 100mg powder vila IV & IM injection	Powder for Injection 100 mg	100 vial pack varies	Reda Jardaneh Drug Store	85.000
Hydrocortisone Medo Vial	Vial 100 mg	100 vial pack varies	Khoury Drug Store	90.510