Methylprednisolone

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A Medico-Marketing PPS on Methylprednosolone

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  • 1. Methylprednisolone Shilpa Garg
  • 2. Introduction Glucocorticoids are a class of steroid hormones  characterised by an ability to bind with the glucocorticoid receptor (GR) and trigger similar effects.  Glucocorticoids are distinguished from mineralocorticoids and sex steroids by their specific receptors, target cells, and effects.  Glucocorticoids have potent anti-inflammatory and immunosuppressive properties  Glucocorticoids are produced in the adrenal glands.  Mineralocorticoids are a class of steroid hormones characterised by their similarity to aldosterone and their influence on salt and water balance.
  • 3. Comparative Steroid Potencies Glucocorticoid Mineralocorticoid Duration of action (t1/2 in Name potency potency hours) Hydrocortisone (Cortisol) 1 1 8 Cortisone acetate 0.8 0.8 oral 8, intramuscular 18+ Prednisone 3.5-5 0.8 16-36 Prednisolone 4 0.8 16-36 Methylprednisolone 5-7.5 0.5 18-40 Dexamethasone 25-80 0 36-54 Betamethasone 25-30 0 36-54 Triamcinolone 5 0 12-36 8 puffs 4 times a day Beclometasone equals 14 mg oral - - prednisone once a day Fludrocortisone acetate 15 200 - Deoxycorticosterone acetate 0 20 - (DOCA) Aldosterone 0.3 200-1000 -
  • 4. Introduction Pharmacologically speaking, there  isn't a lot of difference between methylprednisolone and prednisolone. Methylprednisolone is slightly more potent in glucocorticoid activity than prednisolone, so it's thought to be stronger than prednisolone
  • 5. Methylprednisolone Methylprednisolone is a potent  corticosteroid with an anti- inflammatory activity at least five times that of hydrocortisone.  An enhanced separation of glucocorticoid and mineralocorticoid effect results in a reduced incidence of sodium and water retention.
  • 6. Pharmacokinetics Corticosteroids are absorbed from the  gastro-intestinal tract.  In the circulation they are extensively bound to plasma proteins and are metabolised mainly in the liver but also in the kidney and are excreted in the urine.
  • 7. Indications Methylprednisolone is indicated for conditions requiring glucocorticoid activity such as:  Endocrine disorders ◦ Primary and secondary adrenal insufficiency ◦ Congenital adrenal hyperplasia Rheumatic disorders  ◦ Rheumatoid arthritis ◦ Juvenile chronic arthritis ◦ Ankylosing spondylitis
  • 8. Indications Collagen diseases/arteritis  ◦ Systemic lupus erythematosus ◦ Systemic dermatomyositis (polymyositis) ◦ Rheumatic fever with severe carditis ◦ Giant cell arteritis/ polymyalgia rheumatica Dermatological diseases  ◦ Pemphigus vulgaris
  • 9. Indications Allergic states  ◦ Severe seasonal and perennial allergic rhinitis ◦ Drug hypersensitivity reactions ◦ Serum sickness ◦ Allergic contact dermatitis ◦ Bronchial asthma
  • 10. Indications Ophthalmic diseases  ◦ Anterior uveitis (iritis, iridocyclitis) ◦ Posterior uveitis ◦ Optic neuritis Respiratory diseases  ◦ Pulmonary sarcoid ◦ Fulminating or disseminated tuberculosis (with appropriate antituberculous chemotherapy) ◦ Aspiration of gastric contents
  • 11. Indications Neoplastic diseases  ◦ Leukaemia (acute and lymphatic) ◦ Malignant lymphoma Gastrointestinal diseases  ◦ Ulcerative colitis ◦ Crohn's disease
  • 12. Indications Haematological disorders  ◦ Idiopathic thrombocytopenic purpura ◦ Haemolytic anaemia (autoimmune) Miscellaneous  ◦ Tuberculous meningitis (with appropriate anti-tuberculous chemotherapy) ◦ Transplantation
  • 13. Dosage & Administration Recommended initial daily dosage  Rheumatoid arthritis ◦ severe 12-16 mg ◦ moderately severe 8-12 mg ◦ moderate 4-8 mg ◦ children 4-8 mg Systemic dermatomyositis: 48 mg  Systemic lupus erythematosus: 20-100 mg  Acute rheumatic fever: 48 mg until ESR  normal for one week.  Allergic diseases: 12-40 mg
  • 14. Dosage & Administration Bronchial asthma up to 64 mg single  dose/alternate day up to 100 mg maximum.  Ophthalmic diseases:12-40 mg  Haematological disorders and leukaemias: 16-100 mg  Malignant lymphoma: 16-100 mg  Ulcerative colitis: 16-60 mg
  • 15. Dosage & Administration Crohn's disease up to 48 mg per day  in acute episodes.  Organ transplantation up to 3.6 mg/kg/day  Pulmonary sarcoid: 32-48 mg on alternate days.  Giant cell arteritis/polymyalgia rheumatica: 64 mg  Pemphigus vulgaris: 80-360 mg
  • 16. Contraindications Methylprednisolone is contraindicated  where there is ◦ known hypersensitivity to components ◦ and in systemic infection unless specific anti-infective therapy is employed.
  • 17. Warnings & Precautions Pregnancy  The ability of corticosteroids to cross the placenta varies between individual drugs, however, methylprednisolone does cross the placenta.  Administration of corticosteroids to pregnant animals can cause abnormalities of foetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development.
  • 18. Warnings & Precautions Lactation  Corticosteroids are excreted in small amounts in breast milk, however, doses of up to 40 mg daily of methylprednisolone are unlikely to cause systemic effects in the infant.  Infants of mothers taking higher doses than this may have a degree of adrenal suppression, but the benefits of breastfeeding are likely to outweigh any theoretical risk.
  • 19. Side Effects Bloody or black, tarry stools   Confusion, excitement, restlessness, a false sense of well-being  Eye pain, decreased or blurred vision, or bulging eyes  Fever, sore throat, sneezing, cough, or other signs of infection, wounds that will not heal  Frequent passing of urine  Increased thirst  Irregular heartbeat  Menstrual problems  Muscle cramps or weakness
  • 20. Side Effects Nausea, vomiting   Pain in hips, back, ribs, arms, shoulders, or legs  Pain, redness, swelling, or infection at the injection site  Rounding of face  Skin problems, acne, thin and shiny skin  Stomach pain  Swelling of feet or lower legs  Unusual bruising, pinpoint red spots on the skin  Unusual tiredness or weakness  Weight gain or weight loss  Mental depression, mood swings, mistaken feelings of self-importance or of being mistreated
  • 21. Drug Interactions Following drug(s) may interact with methylprednisolone  ◦ Acetazolamide ◦ Antiinflammatory drugs (NSAIDs, such as ibuprofen) ◦ Barbiturate medicines for inducing sleep or treating seizures ◦ Erythromycin ◦ Female hormones, including contraceptives or birth control pills ◦ Itraconazole ◦ Liver virus vaccines, and other toxoids and vaccines ◦ Phenytoin ◦ Rifabutin ◦ Rifampin ◦ Warfarin
  • 22. Glossary of Medical Terms Polymyalgia: pain involving many  muscles  Hyperplasia: abnormal increase in the number of normal cells in normal arrangement in an organ or tissue  Ankylosing spondylitis: Arthritis of the spine, resembling rheumatoid arthritis and leading to fusion of the vertebrae.
  • 23. Glossary of Medical Terms Systemic lupus erythematosus: an  autoimmune disease that can be life threatening. Patients may have a distinctive pattern of facial redness and oral lesions.  Carditis: Inflammation of the muscle tissue of the heart.  Dermatomyositis : A chronic inflammatory disease of skin and muscle which is associated with patches of slightly raised reddish or scaly rash.
  • 24. Glossary of Medical Terms Sarcoid: fleshy tumor.   Aspiration : withdrawal of fluid from the body by means of suction using an aspirator.  Lymphoma : malignant tumor of lymph nodes.  Giant cell arteritis: A serious disease characterized by inflammation of the walls of the blood vessels (vasculitis). The vessels affected by the inflammation are the arteries (hence the name quot;arteritisquot;). Giant cell arteritis can lead to blindness and/or
  • 25. Glossary of Medical Terms Polymyalgia rheumatica: Its a  disorder of the muscles and joints characterized by pain and stiffness, affecting both sides of the body, and involving the shoulders, arms, neck, and buttock areas.  Pemphigus vulgaris : One of a group of chronic, relapsing autoimmune skin diseases that cause blisters and erosions of the skin and mucous membranes.
  • 26. Glossary of Medical Terms Idiopathic thrombocytopenic purpura: A  blood disorder characterized by the destruction of blood platelets due to the presence of antiplatelet autoantibodies. (Autoantibodies are antibodies directed against the patient's own cells, in this disorder, the patient's own platelets.) Thrombocytopenia refers to a decrease in platelets (also known as thrombocytes). Purpura pertains to the visible hallmarks: purplish areas in the skin and mucous membranes (such as the mouth lining) where bleeding has occurred as a result of decreased platelets.
  • 27. Glossary of Medical Terms Uveitis: Involves all inflammatory  processes of the middle layers of the eye, also called the uveal tract or uvea. The uvea includes the iris (colored part of the eye), choroid (a thin membrane containing many blood vessels) and ciliary body (the part of the eye that joins these together).