Usage
Oral corticosteroids are prescribed for a wide range of medical conditions, including inflammatory and autoimmune disorders, allergic reactions, asthma, adrenal insufficiency, and certain cancers. They are classified as corticosteroids, a class of steroid hormones. 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.
Alternate Names
Oral corticosteroids are often referred to simply as steroids. Specific generic names include prednisone, prednisolone, dexamethasone, methylprednisolone, cortisone, and hydrocortisone. Brand names vary depending on the specific drug and manufacturer. Examples include Rayos, Orapred, Medrol, and Deltasone.
How It Works
Pharmacodynamics: Corticosteroids exert their effects by binding to glucocorticoid receptors in the cytoplasm of target cells. This complex then translocates to the nucleus, modulating gene expression. The resulting changes influence various physiological processes, including immune response, metabolism, and inflammation. They inhibit inflammatory mediators, suppress cell-mediated immunity, and reduce vascular permeability.
Pharmacokinetics: Oral corticosteroids are generally well-absorbed from the gastrointestinal tract. Metabolism primarily occurs in the liver, with subsequent excretion through the kidneys. The half-life varies depending on the specific drug, ranging from a few hours (e.g., hydrocortisone) to several days (e.g., dexamethasone).
Mode of Action: Corticosteroids suppress inflammation by inhibiting the production of inflammatory cytokines, prostaglandins, and leukotrienes. They also decrease the infiltration of inflammatory cells into tissues. Additionally, they induce apoptosis in lymphocytes and eosinophils, further reducing immune activity. Specific receptor binding involves glucocorticoid receptors. Elimination pathways are primarily renal, with a small portion excreted in bile.
Dosage
Dosage guidelines vary considerably based on the specific condition, disease severity, patient response, and corticosteroid used.
Standard Dosage
Adults:
The initial dose can range from 5 mg to 60 mg per day for prednisone, depending on the indication. Higher doses may be used in certain situations. The dose is typically tapered down to the lowest effective maintenance dose.
Children:
Pediatric dosing is calculated based on body weight (e.g., 0.14 mg/kg to 2 mg/kg per day of prednisolone) or body surface area. The total daily dose is usually divided into three or four smaller doses throughout the day.
Special Cases:
- Elderly Patients: Start with a lower dose due to increased sensitivity to side effects.
- Patients with Renal Impairment: Dosage adjustment may be needed depending on the degree of impairment and specific drug.
- Patients with Hepatic Dysfunction: Some corticosteroids (e.g., cortisone, prednisone) require hepatic activation, so patients with liver dysfunction may require dosage adjustments.
- Patients with Comorbid Conditions: Close monitoring is necessary in patients with diabetes, hypertension, osteoporosis, and other conditions, as corticosteroids can exacerbate these.
Clinical Use Cases
Dosing is highly individualized based on the specific clinical situation and patient needs. Guidelines are based on the equivalent dose of prednisone.
- Intubation/Surgical Procedures/Mechanical Ventilation/ICU Use/Emergency Situations: Higher doses are often used initially, with subsequent tapering as the condition stabilizes.
Dosage Adjustments
Dose adjustments are often based on clinical response, tolerance, and the development of adverse effects. Drug interactions and comorbidities should be considered. Patients with renal or hepatic impairment may require dose reductions.
Side Effects
Common Side Effects:
Increased appetite, weight gain, fluid retention, mood changes, insomnia, increased risk of infection, elevated blood sugar, and gastrointestinal upset.
Rare but Serious Side Effects:
Osteoporosis, avascular necrosis, cataracts, glaucoma, peptic ulcers, Cushing’s syndrome, adrenal suppression, and psychiatric disturbances.
Long-Term Effects:
The long-term use of oral corticosteroids can lead to a variety of complications, including osteoporosis, diabetes, hypertension, and increased susceptibility to infections.
Adverse Drug Reactions (ADR):
Severe allergic reactions, adrenal crisis, and psychosis.
Contraindications
Absolute contraindications include systemic fungal infections and hypersensitivity to the specific drug. Relative contraindications include active infections, uncontrolled diabetes, severe hypertension, osteoporosis, and recent myocardial infarction.
Drug Interactions
Corticosteroids can interact with various medications, including NSAIDs, anticoagulants, antidiabetic agents, and certain antibiotics. They can also induce or inhibit CYP450 enzymes, affecting the metabolism of other drugs. Alcohol, grapefruit juice, and smoking can also influence corticosteroid metabolism.
Pregnancy and Breastfeeding
Corticosteroids are generally considered safe during pregnancy, especially in lower doses. However, prolonged use of high doses may be associated with a slightly increased risk of cleft palate or low birth weight. They are excreted in breast milk, but the amount is usually considered low and generally safe for infants.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, modulating gene expression and influencing immune response, metabolism, and inflammation.
- Side Effects: Range from common effects like weight gain and mood changes to serious effects like osteoporosis and adrenal suppression.
- Contraindications: Systemic fungal infections, hypersensitivity.
- Drug Interactions: NSAIDs, anticoagulants, antidiabetics, antibiotics.
- Pregnancy & Breastfeeding: Generally safe in low doses.
- Dosage: Highly variable, based on indication and patient response.
- Monitoring Parameters: Blood pressure, blood glucose, bone density, electrolyte levels.
Popular Combinations
Corticosteroids are often combined with other medications depending on the condition being treated. Examples include combinations with bronchodilators for asthma or with immunosuppressants for autoimmune disorders.
Precautions
General precautions include monitoring for side effects, adjusting doses for specific populations, and screening for underlying medical conditions. Lifestyle considerations include limiting alcohol intake and avoiding smoking.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for ORAL CORTICOSTEROIDS, PLAIN?
A: Dosage varies widely depending on the specific drug, indication, and patient factors. Consult specific drug information for guidance.
Q2: What are the most serious side effects of long-term corticosteroid use?
A: Osteoporosis, diabetes, hypertension, adrenal suppression, increased susceptibility to infections, cataracts, and glaucoma.
Q3: How should corticosteroids be discontinued after prolonged use?
A: Tapering the dose gradually is crucial to prevent adrenal insufficiency.
Q4: Can corticosteroids be used during pregnancy?
A: Generally safe, especially in lower doses. Consult a physician for individual guidance.
Q5: What are the signs of an adrenal crisis?
A: Severe weakness, fatigue, abdominal pain, vomiting, low blood pressure, and loss of consciousness. Requires immediate medical attention.
Q6: How do corticosteroids interact with other medications?
A: They can interact with NSAIDs, anticoagulants, antidiabetics, and certain antibiotics. Consult a comprehensive drug interaction resource.
Q7: What are the main contraindications for corticosteroid use?
A: Systemic fungal infections and hypersensitivity to the specific drug.
Q8: What are the key monitoring parameters during corticosteroid therapy?
A: Blood pressure, blood glucose, bone density, and electrolyte levels.
Q9: Can patients drink alcohol while taking oral corticosteroids?
A: While not absolutely contraindicated, moderate alcohol consumption is recommended. Excessive alcohol use can exacerbate certain side effects.
