Cortisone

Mechanism :

It is a corticosteroid with glucocorticoid and mineralocorticoid properties.

It exerts its anti-inflammatory effect by suppressing the migration of polymorphonuclear neutrophils (PMNs) and fibroblasts, decreasing capillary permeability and modifying transcription and therefore the rate of synthesis of mediators of inflammation.

Owing to its mineralocorticoid property, cortisone acts on the distal renal tubule and causes sodium resorption and excretion of hydrogen and potassium. It also interferes with absorption of calcium from gut and increases excrection of calcium via kideny.

Indication :

• Tuberculous meningitis concurrently with AKT
• Nephrotic syndrome: To induce diuresis or remission
• Haematological disorders: Autoimmune haemolytic anaemia, Erythroblastopenia, Congenital Hypoplastic Anaemia
• Asthma exacerbation
• Trichinosis with neurologic or myocardial involvement
• Respiratory inflammatory conditions: Loeffler’s syndrome, Aspiration pneumonitis, Berylliosis
• Anaphylaxis and anaphylactoid reactions
• Inflammatory dermatological conditions: Atopic dermatitis, Bullous dermatitis herpetiformis, contact dermatitis, Stevens Johnson Syndrome
• Steroid-responsive ophthalmic disorders
• Juvenile rheumatoid arthritis, juvenile idiopathic arthritis
• Acute leukaemia of childhood: Palliative management

Contraindications :

1.  Hypersensitivity to corticosteroids
2.  Systemic fungal infection
3.  Cerebral malaria
4.  Administration of live virus vaccines if receiving immunosuppressive doses
5.  Caution in :

- Active or latent Tuberculosis

- Varicella, measles exposure

- Congestive heart failure

- Seizure disorder

- Thyroid disorder

- Ocular HSV

- Hypertension

- Renal impairment

       6. Avoid abrupt cessation 

Dosing :

Adverse Effect :

Serious reactions: 

• Growth suppression if long term use

• Cushing syndrome

• Increase in intracranial pressure

• Seizures

• Steroid psychosis

• Increased risk of infections

• Pseudotumour cerebri

• Hypokalemic alkalosis

• Peptic Ulcer Disease, GI perforation

• Pancreatitis

• Adrenal Insufficiency if abrupt withdrawal

Common Reactions 

• Weight Gain

• Hirsutism

• Cushingoid appearance

• Oedema

• Impaired wound healing

• Insomnia

• Cataract

• Petechiae, Ecchymosis

Interaction :

Glucocorticoids are substrates of CYP3A4 enzyme and therefore any drug which affects this enzyme system will interact with glucocorticoids. 

1. CYP3A4 Inducers + Glucorticoids = Decreased exposure and efficacy

- Antiseizure: Phenytoin, Phenobarbital, Fosphenytoin, Carbamazepine

- Antimicrobials: Efavirenz, Etravirine, Rifampin, Rifabutin, Nafcilin, Rifapentine

2. CYP3A4 Inhibitors + Glucorticoids: Increased exposure and toxicity

- Antimicrobials: Clarithromycin, telithromycin

- Antifungal: Ketoconazole, Itraconazole, Voriconazole

- Antiviral: Atazanavir, Darunavir, Ritonavir, Lopinavir, Fosamprenavir, Indinavir, Nelfinavir, Saquinavir, Telaprevir

- Estrogens

- Immunosuppressants: Cyclosporine, Tacrolimus, Everolimus

3. Others 

Contraindicated

- All live vaccines

- Mifepristone: Increased risk of hypokalemia

- Desmopressin: Increased risk of hypertension, hyponatremia

- Talimogene laherparepvec: Increased risk of disseminated herpes

Alternate use recommended

- Other corticosteroids: Prednisone, Dexamethasone

- Amphotericin: Increased risk of hypokalemia, arrythmias

- Ceritinib: It may increase the levels of cortisone and thus its side effects

- Furosemide: Cortisone may decrease the efficacy of Furosemide, increased risk of hypokalemia

- Melatonin: It may hamper with immunosuppressive therapy

- Midodrine: Increased risk of hypertension

 Natalizumab: Increased risk of serious infections

- Nevirapine: Increased risk of skin rash

Monitor closely

- Warfarin: Cortisone may increase anticoagulant effect, monitor INR if concomitant use

- Fluoroquilones: Increased risk of tendinopathy

- Oral Hypolgycaemic drugs: Glucose dyregulation, monitor blood glucose closely

- NSAIDs: Increased risk of peptic ulcer disease