MECHANISM OF ACTION –
As a synthetic glucocorticoid (GC), its lipophilic structure allows for easy passage through the cell membrane where it then binds to its respectively glucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, formation of the GC/GCR complex causes dissociation of chaperone protein from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus. This process occurs within 20 minutes of binding. Once inside the nucleus,the homodimer GC/GCR complex binds to specific DNA binding-sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to synthesis of anti-inflammatory proteins while binding to negative GREs block the transcription of inflammatory genes.
PHARMACOLOGICAL ACTION –
1-Inhibit glucose utilization by peripheral tissue.
2-Promote lipolysis.
3-Enhance renal excretion of calcium.
4-Secretion of gastric acid and pepsin is increased.
USES –
1. Acute adrenal insufficiency.
2. Addison’s disease
3. Congenital adrenal hyperplasia
4. Arthritis
5. Autoimmune diseases
6. Bronchial asthma
7. Cerebral edema.
SIDE EFFECTS –
1-Increase appetite, weight gain, nausea
2-Increase risk of infection
3-Cardiovascular events in children
4-Dermatological effects including reddening of face, bruising/ skin discoloration, impaired wound healing, thinning of skin, skin rash, fluid build up and abnormal hair growth.
5-Menstrual abnormalities
6-Less response to hormones especially during stressful instances such as surgery or illness.
7-Change in electrolytes: rise in BP, increase sodium and low potassium leading to alkalosis.
8-GI system effects: Swelling of stomach lining, reversible increase in liver enzymes and risk of stomach ulcer
9-Muscular and skeletal abnormalities such as muscle weakness and loss, osteoporosis, long bone fractures, tendon rupture and back fractures.
DRUG-DRUG INTERACTION –
1-Prednisolone + moxifloxacin = can increase the risk of tendinitis and tendon rupture.
2-Prednisolne + Bupropion = may increases the chances of seizures.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.230
As a synthetic glucocorticoid (GC), its lipophilic structure allows for easy passage through the cell membrane where it then binds to its respectively glucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, formation of the GC/GCR complex causes dissociation of chaperone protein from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus. This process occurs within 20 minutes of binding. Once inside the nucleus,the homodimer GC/GCR complex binds to specific DNA binding-sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to synthesis of anti-inflammatory proteins while binding to negative GREs block the transcription of inflammatory genes.
PHARMACOLOGICAL ACTION –
1-Inhibit glucose utilization by peripheral tissue.
2-Promote lipolysis.
3-Enhance renal excretion of calcium.
4-Secretion of gastric acid and pepsin is increased.
USES –
1. Acute adrenal insufficiency.
2. Addison’s disease
3. Congenital adrenal hyperplasia
4. Arthritis
5. Autoimmune diseases
6. Bronchial asthma
7. Cerebral edema.
SIDE EFFECTS –
1-Increase appetite, weight gain, nausea
2-Increase risk of infection
3-Cardiovascular events in children
4-Dermatological effects including reddening of face, bruising/ skin discoloration, impaired wound healing, thinning of skin, skin rash, fluid build up and abnormal hair growth.
5-Menstrual abnormalities
6-Less response to hormones especially during stressful instances such as surgery or illness.
7-Change in electrolytes: rise in BP, increase sodium and low potassium leading to alkalosis.
8-GI system effects: Swelling of stomach lining, reversible increase in liver enzymes and risk of stomach ulcer
9-Muscular and skeletal abnormalities such as muscle weakness and loss, osteoporosis, long bone fractures, tendon rupture and back fractures.
DRUG-DRUG INTERACTION –
1-Prednisolone + moxifloxacin = can increase the risk of tendinitis and tendon rupture.
2-Prednisolne + Bupropion = may increases the chances of seizures.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.230
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