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Prednisolone belongs to the steroid or corticosteroid class of medications. It is one of the most commonly used medications to treat a wide range of medical problems, including allergies, joint inflammation, respiratory issues, some blood disorders, collagen diseases, certain eye diseases, cancer, endocrine issues, intestinal problems, and edema caused by certain ailments. It lowers the levels of compounds that cause inflammation and allergies. 

It can also help to minimize organ rejection following transplantation. It can cure a variety of allergic reactions and inflammation in the body. It also lowers the immune system, which may help cure autoimmune illnesses such as rheumatoid arthritis, in which the immune system mistakenly targets tissues. In 1955, it obtained FDA approval.

BRAND NAMES:

Bubbli-Pred – It contains the active ingredients of prednisolone. It is available in the form of tablets used to treat allergies, asthma, cancer, blood disorders, eye diseases, and immune system disorders.

Flo-Pred - It contains the active ingredients of prednisolone. It is available in the form of oral suspension.

Millipred – It contains the active ingredients of prednisolone. It is available in the form of tablets and oral solutions.

Orapred – It contains the active ingredients of prednisolone. It is available in the form of oral disintegrating tablets. 

MECHANISM OF ACTION:

Corticosteroids bind to the glucocorticoid receptor, causing changes in gene expression that have numerous downstream effects over hours to days. Long-term high doses of glucocorticoids bind to the mineralocorticoid receptor, increasing sodium levels while decreasing potassium levels. Lower doses of corticosteroids have an anti-inflammatory effect, whereas higher doses are immunosuppressive. Corticosteroids have short-term effects such as lowering vasodilation and capillary permeability, as well as decreased leukocyte migration to inflammatory sites.

PHARMACOKINETICS:

Absorption: After administration of oral prednisolone is approximately 70% bioavailability. It reaches a Cmax of 113-1343ng/ml with a Tmax of 1.0-2.6 hours.

Distribution: The volume of distribution of posaconazole is 0.22-0.7K/Kg

Metabolism: Intracellular metabolism by 11β-HSD controls the availability of prednisolone for binding to the glucocorticoid and mineralocorticoid receptors. Two types of 11 β-HSD are present in the body. 11β-HSD-1 acts primarily as a reductase and converts the inactive prednisone into the active prednisolone. 11β-HSD-2 acts primarily as an oxidase and converts prednisolone to prednisone, thereby protecting the mineralocorticoid receptor from occupation by cortical and prednisolone.

Excretion: Prednisolone is excreted through urine.

PHARMACODYNAMICS:

Corticosteroids have a broad therapeutic window because patients often require doses that are several times higher than what the body produces naturally. Patients using corticosteroids should be advised about the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.

DOSAGE AND ADMINISTRATION:

Prednisolone comes as a tablet, an orally disintegrated tablet, a solution, and a suspension to take orally with food.

  • Prednisolone tablets are available in oral solutions with the strength of 5mg, 10mg, 15mg, 20mg, and 25mg/ml.
  • These are available in tablets with a strength of 5mg.
  • This is also available in oral disintegrating tablets with the strengths of 10mg, 15mg, and 30mg.

 

DRUG INTERACTIONS:

Drug interaction with prednisolone may include

  • Tuberculosis – rifampicin and isoniazid
  • Blood thinner – aspirin and warfarin
  • Anti-epilepsy drugs- carbamazepine, phenobarbital and phenytoin
  • Anti-cholinergic drugs – amitriptyline
  • Myasthenia gravis – neostigmine
  • Anti-diabetic drugs – insulin
  • HIV medications – cobicistat 
  • NSAIDs – ibuprofen, naproxen
  • Diuretics – thiazides, furosemide, ethacrylic acid.
  • Asthma drugs - theophylline, salbutamol, terbutaline, salmeterol and formoterol
  • Antibiotics – amphotericin B

CONTRAINDICATIONS:

Prednisolone is contraindicated in the presence of systemic fungal infections. It is also contraindicated with the administration of immune suppressive prednisone dose. And also contraindicated with patients with documented hypersensitivity to the drug or components of the formulations.

SIDE EFFECTS:

Side effects of prednisolone may include

  • Nausea
  • Changes in personality
  • Headache
  • Extreme changes in mood
  • Thinning hair
  • Acne
  • Increased sweating
  • Increased appetite
  • Irregular or absent menstrual periods.
  • Vision problems
  • Seizures
  • Vision problems
  • Muscle weakness
  • Sudden weight gain
  • Rash
  • Depression
  • Difficulty breathing
  • Itching
  • hives

OVERDOSE:

An overdose of prednisolone may cause gastrointestinal disturbance, insomnia, and restlessness. 

The symptoms of overdose may include

  • Burning skin
  • Deafness
  • Dry skin
  • Depression
  • Increased appetite
  • Muscle weakness
  • Nausea and vomiting

TOXICITY:

An overdose of oral prednisolone can be treated with gastric lavage or vomiting, as well as supportive and symptomatic therapy. Chronic overdose can be treated by reducing the dose or treating patients on alternate days.

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Prednisolone