Prednisolone (For Asthma)

Chemical

Synthetic glucocorticoid

Use

Asthma

Presentation

Tablets

Route/Dose

5 – 60mg / day

MoA

  • Glucocorticoid receptor AGONIST
  • Binds corticoreceptor-ligand complex
  • Translocates itself into cell nucleus
  • Alters protein DNA transcription
  • Inhibits phospholipase A2 (which breaks down phospholipids to give arach. Acid)
  • ↓Arach acid
  • ↓PG/leukotriene/IL production
  • ↓inflam cascade, ↓oedema, ↓capillary leakiness
  • (↓airway hyperresponsiveness)

PD

Resp

  • Contract engorged vessels of bronchial mucosa
  • Potentiate B2 agonist effects
  • Inhibit infiltration of asthmatic airways by LC, eosinophils, MCs

GI

  • ↑risk of peptic ulcers
  • ↓Ca2+ absorption

Renal

  • Na+ retention, K+ excretion

CVS

  • +ve inotropy & VC by ↑no. of α1 & β adrenoreceptors

Metabolic

  • Gluconeogenesis
  • Inhibit use of peripheral glucose
  • ↑lipolysis
  • ↓amino acid → protein

Immune

  • Blocks neutrophil & macrophage recruitment
  • Blocks lymphokines
  • Inhibits all stages of inflammatory process

PK

A

Rapidly & completely, PO or PR

80 – 100% bioavailability

D

PPB 90%

VD 0.35 – 0.7L/kg

M

Liver hydroxylation → conjugation

E

10% doses unchanged in urine

t ½ B 2.5 – 5hrs

Adverse Effects