Prednisolone Pharmacology


About Prednisolone
Systemic synthetic Glucocorticoid, Immunosuppressant.
Mechanism of Action of Prednisolone
The drug exerts it`s pharmacological action by penetrating and binding to cytoplasmic receptor protein and causes a structural change in steroid receptor complex. This structural change allows it`s migration in to the nucleus and then binding to specific sites on the DNA which leads to transcription of specific m-RNA and which ultimately regulates protein synthesis. It exerts more selective glucocorticoid action with little mineralocorticoid actions.
The drug exerts anti-inflammatory and immunosuppressant actions as follows: - 1) Induce lipocortins in macrophages, endothelium, and fibroblasts which inhibits phospholipase A2 and thus decreases the production of Prostaglandins, leukotriens (LT), and platelet activating factor, 2) Causes negative regulation of genes for cytokines in macrophages, endothelial cells and lymphocytes and thus decreases the production of interleukins (IL-1, IL-2, IL-3, IL-6), TNF-a, GM-CSF (granulocyte macrophage colony stimulating factor), Gama interferon and suppresses fibroblast proliferation and T-lymphocyte functions and interferes chemo taxis. 3) Decreases the production of acute phase reactants from macrophages and endothelial cells and interferes complement function. 4) Decreases the production of ELAM-1(Endothelial leukocyte adhesion molecule-1) and ICAM-1(intracellular adhesion molecule-1) in endothelial cells. 5) Inhibit IgE mediated histamine and LT-C4 release from basophiles and the effects of antigen-antibody reaction is not mediated 6) Reduces the production of collagenase and stromolysin and thus prevents tissue destruction

Pharmacokinets of Prednisolone
Absorption: Well absorbed orally, Distribution: Drug is rapidly removed from blood and distributed in to muscle, liver, kidney, skin, and intestine. It crosses the placenta and also secreted in breast milk, Metabolism: Metabolized in liver in to inactive metabolites by glucuronide and sulfate conjugation. Excretion: Metabolites are excreted mainly through urine and a small amount is excreted through faeces.
Onset of Action for Prednisolone
2 to 4 days
Duration of Action for Prednisolone
Half to 3days
Half Life of Prednisolone
18 to 36hours
Side Effects of Prednisolone
1.Susceptibility to infection
2.Peptic ulcer
7.Atrophy of adrenal cortex(on prolonged therapy)
8.Suppression of adrenocorticotropic hormone
9.Cushing`s syndrome
10.Inhibition of growth in children
12.Behavioral disturbances
13.Thromboembolic disorders
17.Muscle wasting
18.Gastrointestinal discomfort
19.Increased appetite
20.Delayed wound healing
25.Heart failure
27.Posterior sub capsular cataract
29.Increased intracranial pressure

Contra-indications of Prednisolone
1.Hypersensitivity to the drug
2.Peptic ulcer
3.Systemic Infections
4.Fungal infections
5.Live vaccines

Special Precautions while taking Prednisolone
1.Avoid sudden discontinuation of the drug
4.Ocular herpes simplex
5.Primary glaucoma
6.Peptic ulcer
7.Primary psychosis and psychoneurosis
8.Recent myocardial infarction
9.Heart failure
10.Diabetes mellitus
16.Myasthenia gravis
17.Renal impairment
18.Hepatic impairment
19.Non specific Ulcerative colitis
21.Recent intestinal anastomosis
23.Thromboembolic disorders

Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution.
Neonates: Contraindicated
Indications for Prednisolone
1.Allergic conditions
3.Inflammatory conditions
4.Rheumatic disorders
5.Autoimmune diseases
7.Inflammatory bowel disease
9.Acute gout

Interactions for Prednisolone
Barbiturates: Decrease pharmacologic of prednisolone.
Oral contraceptives: May increase concentration of prednisolone.
Oestrogens: May decrease the clearance of prednisolone.
Ketoconazole: Increases efficacy of prednisolone.
Rifampicin: Decreases efficacy.
Prednisolone affects the actions of the following:
Anticholinesterases: Effects may be antagonised in myasthenia gravis.
Cyclosporine: May lead to enhanced toxicity.
Digitalis glycosides: May lead to enhanced toxicity.
Isoniazid: Decreased serum levels of isoniazid.
Salicylates: Decreased serum levels of salicylate.
Diuretics: May cuase hypokalaemia and increased hyperglycaemia.
Non-depolarising muscle relaxants: Altered response.
Somatrem: Growth promoting effect inhibited.
Theophyllines: Altered response of either agent.
IUCD: contraceptive failure.
Lab. Tests:
a) Increases serum cholesterol levels.
b) Increases urine glucose levels.
c) Decreases Thyroid I131 uptake; Decreases T3 serum levels.
d) Decreases serum potassium.
Typical Dosage for Prednisolone
Oral: 10 to 60mg/day; depending up on the severity of the condition and patient`s response.
Children: 0.15 to 2mg/kg/day in 4 to 6 divided doses; depending up on the severity of the condition and patient`s response.
I.M. or I.V.: 2 to 30mg 12th hourly
Intra-articular: 5 to 25mg Prednisolone acetate.

Schedule of Prednisolone
Storage Requirements for Prednisolone
Store at room temperature below 30 degree C. Protect from light and moisture. Keep out of reach of children.
Effects of Missed Dosage of Prednisolone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.

Effects of Overdose of Prednisolone
Provide symptomatic treatment and supportive measures.

Home Delivery for Prednisolone in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including prednisolone.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for prednisolone and other medicines and health products. Home delivery services for prednisolone may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take prednisolone only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for prednisolone before they complete the sale. You can get this information while placing the order for prednisolone with the pharmacy.

Prednisolone is a generic medicine name and there are several brands available for it. Some of the brands for prednisolone might be better known than prednisolone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have prednisolone in stock, you can ask for one of the branded alternatives for prednisolone.