A Medico-Marketing PPS on Methylprednosolone

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).