Prednisone

BRAND NAMES

1. Deltasone 

2. Rayos (delayed-release formulation) 

3. Sterapred 

4. Predone

5. Cortan

6. Delta-dome

7. Fernisone

8. Meticorten

9. Orasone

10. Paracort

11. Prednicen-m

12. Servisone

MECHANISM OF ACTION

Prednisone works by mimicking the effects of natural glucocorticoid hormones produced by the adrenal glands. After administration, it is converted in the liver to its active form, prednisolone, which then enters cells and binds to intracellular glucocorticoid receptors.

PHARMACOKINETICS

Absorption

Prednisone is well absorbed from the gastrointestinal tract after oral administration, with high bioavailability. Peak plasma concentrations are typically reached within 1–2 hours for immediate-release formulations, while delayed-release forms take longer.

Distribution

Prednisone (after conversion to prednisolone) is widely distributed throughout body tissues, with an apparent volume of distribution of approximately 0.4–1 L/kg. It is moderately bound to plasma proteins, mainly albumin and corticosteroid-binding globulin, and can readily cross cell membranes to exert its effects in various organs and tissues.

Metabolism

Prednisone is a prodrug that is rapidly converted in the liver to its active form, prednisolone, primarily by hepatic enzymes. Prednisolone then undergoes further metabolism in the liver through reduction and conjugation reactions to form inactive metabolites.

Elimination

Prednisone, after conversion to prednisolone, is eliminated primarily by the kidneys in the form of inactive metabolites produced in the liver. Only a small fraction is excreted unchanged in the urine.

PHARMACODYNAMICS

Prednisone exerts its effects by acting as a glucocorticoid receptor agonist, producing potent anti-inflammatory and immunosuppressive actions. After conversion to prednisolone, it binds to intracellular glucocorticoid receptors and alters gene transcription, leading to decreased production of inflammatory mediators such as cytokines, prostaglandins, and leukotrienes. It also inhibits the accumulation and activity of immune cells like lymphocytes, macrophages, and neutrophils at sites of inflammation. Additionally, prednisone reduces capillary permeability and stabilizes cell membranes, which helps limit swelling and tissmaue dage.

ADMINISTRATION

Prednisone is primarily administered orally in the form of tablets, delayed-release tablets, or oral solutions. It is usually taken once daily, preferably in the morning with food to reduce gastrointestinal irritation and to mimic the body’s natural cortisol rhythm. The dosage and duration vary depending on the condition being treated and the patient’s response. In some cases, alternate-day therapy may be used to minimize side effects during long-term treatment. For prolonged use, the dose is often gradually tapered rather than stopped abruptly to prevent adrenal insufficiency.

DOSAGE AND STRENGTH

Prednisone is available in a variety of strengths to allow flexible dosing based on the condition being treated. Common tablet strengths include 1 mg, 2.5 mg, 5 mg, 10 mg, 20 mg, and 50 mg. Oral solutions are also available in concentrations such as 5 mg/5 mL.

The dosage varies widely depending on the indication, severity, and patient response. For adults, typical doses may range from 5 mg to 60 mg per day, though higher doses can be used in severe conditions. In children, dosing is usually based on body weight (e.g., 0.1–2 mg/kg/day).

DRUG INTERACTIONS

Prednisone can interact with a wide range of medications due to its effects on metabolism, immune function, and electrolyte balance. Drugs such as NSAIDs (e.g., ibuprofen, aspirin) increase the risk of gastrointestinal ulceration and bleeding when used with prednisone.

FOOD INTERACTIONS

Prednisone does not have major direct food–drug interactions, but food can influence its tolerability and side effects. It is recommended to take prednisone with food or milk to reduce gastrointestinal irritation such as nausea, indigestion, or gastric ulcer risk. Diets high in sodium (salt) may worsen fluid retention and increase blood pressure, so salt intake is often limited during long-term therapy.

CONTRAINDICATIONS

Prednisone is contraindicated in patients with a known hypersensitivity to prednisone or any of its components. It should generally be avoided in patients with systemic fungal infections unless appropriate anti-infective therapy is also being given, as it can worsen infection due to its immunosuppressive effects.

SIDE EFFECTS

• Increased appetite and weight gain 

• Fluid retention (edema) 

• Mood changes (irritability, anxiety, depression) 

• Insomnia (difficulty sleeping) 

• Indigestion or stomach irritation 

• Elevated blood glucose levels (hyperglycemia) 

• Increased risk of infections (immunosuppression) 

• Osteoporosis (bone thinning) with long-term use 

• Muscle weakness 

• Hypertension (high blood pressure)

OVER DOSE

Prednisone overdose is uncommon and is usually related to excessive or prolonged use rather than a single acute ingestion. It results in exaggerated glucocorticoid effects, leading to symptoms such as severe fluid retention, hypertension, marked hyperglycemia, mood disturbances (anxiety, agitation, or psychosis), and increased susceptibility to infections due to immune suppression.

TOXICITY

Prednisone toxicity is usually associated with prolonged use of high doses rather than acute overdose. Excess glucocorticoid exposure can lead to Cushing’s syndrome–like features such as severe weight gain, moon face, central obesity, muscle wasting, hypertension, hyperglycemia, and fluid retention.