Usage
Oral corticosteroids are prescribed for a wide range of medical conditions, including inflammatory and autoimmune disorders, allergic reactions, asthma, certain cancers, and adrenal insufficiency. They are classified as anti-inflammatory, immunosuppressive, and anti-allergic agents. These medications work by mimicking the effects of cortisol, a hormone naturally produced by the adrenal glands. They suppress the immune system and reduce inflammation by inhibiting the production of inflammatory mediators.
Alternate Names
Oral corticosteroids are often referred to simply as “steroids.” Some examples include: Prednisone, Prednisolone, Methylprednisolone, Dexamethasone, Cortisone, and Hydrocortisone. Brand names vary depending on the specific corticosteroid and the manufacturer.
How It Works
Pharmacodynamics: Corticosteroids exert their effects by binding to glucocorticoid receptors in the cytoplasm of cells. This complex then translocates to the nucleus, where it modulates gene expression. This leads to decreased production of inflammatory mediators like prostaglandins, leukotrienes, and cytokines, as well as decreased activity of immune cells.
Pharmacokinetics: Oral corticosteroids are generally well-absorbed from the gastrointestinal tract. They are metabolized primarily in the liver and excreted by the kidneys. The half-life of different corticosteroids varies, ranging from a few hours (e.g., hydrocortisone) to several days (e.g., dexamethasone). Specific cytochrome P450 (CYP) enzymes are involved in their metabolism.
Mode of Action: Corticosteroids act by suppressing the immune system and reducing inflammation. They achieve this through multiple mechanisms, including:
- Inhibition of phospholipase A2: This enzyme is crucial for the production of arachidonic acid, a precursor to inflammatory mediators.
- Decreased production of cytokines: These signaling molecules play a key role in inflammation and immune responses.
- Suppression of leukocyte migration: Corticosteroids reduce the movement of white blood cells to sites of inflammation.
- Inhibition of gene transcription: Corticosteroids can modulate the expression of genes involved in inflammation.
Dosage
Dosage guidelines for oral corticosteroids vary depending on the specific medication, the condition being treated, and the patient’s individual characteristics.
Standard Dosage
Adults:
The initial adult dosage can range from 5 mg to 60 mg daily, depending on the specific corticosteroid and the indication. Higher doses may be necessary for certain conditions. The dose may be given once daily, in divided doses, or on alternate days.
Children:
Pediatric dosages are typically based on body weight, usually 0.14 to 2 mg/kg per day, divided into three or four doses.
Special Cases:
- Elderly Patients: Start with lower doses and monitor closely for side effects.
- Patients with Renal Impairment: Dosage adjustments may be necessary depending on the degree of impairment.
- Patients with Hepatic Dysfunction: Dosage adjustments may be required.
- Patients with Comorbid Conditions: Careful monitoring is essential in patients with diabetes, hypertension, osteoporosis, and other conditions.
Clinical Use Cases
Dosage recommendations for specific clinical use cases should be determined by the treating physician based on the patient’s individual needs.
- Intubation: Corticosteroids may be used to reduce inflammation in the airways.
- Surgical Procedures: High doses may be given perioperatively to suppress the immune response and reduce inflammation.
- Mechanical Ventilation: Corticosteroids can help improve lung function.
- Intensive Care Unit (ICU) Use: High doses may be used to manage critical illness.
- Emergency Situations: Corticosteroids can be life-saving in conditions like anaphylaxis and adrenal crisis.
Dosage Adjustments
Dosage adjustments are often needed based on individual patient factors, including renal or hepatic dysfunction, comorbid conditions, and drug interactions.
Side Effects
Common Side Effects:
Increased appetite, weight gain, fluid retention, mood changes, difficulty sleeping, increased blood sugar, increased risk of infection.
Rare but Serious Side Effects:
Osteoporosis, avascular necrosis, cataracts, glaucoma, peptic ulcers, Cushing’s syndrome, adrenal suppression.
Long-Term Effects:
Prolonged use can lead to significant side effects, including osteoporosis, adrenal insufficiency, and increased risk of infections.
Adverse Drug Reactions (ADR):
Severe allergic reactions, adrenal crisis, psychosis, gastrointestinal bleeding.
Contraindications
Systemic fungal infections, hypersensitivity to corticosteroids. Relative contraindications include uncontrolled infections, diabetes, hypertension, osteoporosis, and peptic ulcer disease.
Drug Interactions
Corticosteroids can interact with several medications, including NSAIDs, anticoagulants, antidiabetic agents, and certain antibiotics. They can also interact with CYP450 enzyme inducers and inhibitors. Alcohol, smoking, and grapefruit juice can affect corticosteroid metabolism.
Pregnancy and Breastfeeding
Corticosteroids are generally considered safe during pregnancy, but prolonged use or high doses may pose risks to the fetus. They are excreted in breast milk and may affect the nursing infant.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, modulating gene expression and suppressing inflammation and immune responses.
- Side Effects: Range from common side effects like increased appetite and weight gain to serious side effects like osteoporosis and adrenal suppression.
- Contraindications: Systemic fungal infections, hypersensitivity.
- Drug Interactions: Numerous drug interactions, including NSAIDs, anticoagulants, and CYP450 modulators.
- Pregnancy & Breastfeeding: Generally safe during pregnancy but should be used with caution; excreted in breast milk.
- Dosage: Varies depending on the condition and patient; typically 5-60 mg daily for adults.
- Monitoring Parameters: Blood pressure, blood sugar, bone density, electrolyte levels.
Popular Combinations
Corticosteroids are often used in combination with other medications, depending on the condition being treated.
Precautions
- General Precautions: Monitor for side effects, adjust dosage based on patient response.
- Specific Populations: Exercise caution in elderly patients, patients with renal or hepatic impairment, and pregnant or breastfeeding women.
- Lifestyle Considerations: Advise patients on diet, exercise, and stress management.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for ORAL CORTICOSTEROIDS, PLAIN?
A: The recommended dosage varies depending on the specific corticosteroid, the condition being treated, and the individual patient. Adult dosages can range from 5 mg to 60 mg or more per day. Pediatric dosages are based on body weight.
Q2: What are the most common side effects of oral corticosteroids?
A: Common side effects include increased appetite, weight gain, fluid retention, mood changes, difficulty sleeping, and increased blood sugar.
Q3: What are the long-term risks of oral corticosteroid use?
A: Long-term use can lead to osteoporosis, adrenal suppression, increased risk of infections, cataracts, glaucoma, and other serious side effects.
Q4: Are oral corticosteroids safe during pregnancy?
A: They are generally considered safe during pregnancy, but prolonged use or high doses may pose risks to the fetus.
Q5: How should oral corticosteroids be discontinued?
A: Long-term use should be tapered gradually to avoid adrenal insufficiency.
Q6: What are the signs of an allergic reaction to oral corticosteroids?
A: Signs of an allergic reaction include rash, itching, swelling, dizziness, and difficulty breathing.
Q7: Can oral corticosteroids interact with other medications?
A: Yes, they can interact with numerous medications, including NSAIDs, anticoagulants, and certain antibiotics.
Q8: What should patients be advised about lifestyle modifications while taking oral corticosteroids?
A: Patients should be advised on healthy diet, regular exercise, stress management, and adequate calcium and vitamin D intake.
Q9: What monitoring is necessary during long-term oral corticosteroid therapy?
A: Regular monitoring of blood pressure, blood sugar, bone density, and electrolyte levels is important. Regular eye exams are also advised.
