Acute Porphyria Drug Database

D07XA02 - Prednisolone
Propably not porphyrinogenic
PNP

Rationale
Conclusive pharmacokinetic evidence not compatible with CYP-inducing capacity in clinical use. Being ligand to glucocorticoid nuclear receptor giving rise to endogenous protective glucose production. Feedback inhibition of adrenal androgen production will add to a protective effect. No reports of porphyrogenic side effects in clinical use, but well documented evidence of tolerance in acute porphyria.
Chemical description
1,2-dehydrohydrocortisone(M=360). Synthetic corticosteroid with dominant glucocorticoid activity. Administered as watersoluble sodiumsuccinate ester.
Therapeutic characteristics
Shock conditions. Antiallergic, antipruritic, immunosuppressive and antiinflammatory properties. Five times stronger antiinflammatory effect than hydrocortisone. The slower metabolism of synthetic corticosteroids with their lower plasma-protein binding affinity may account for their increased potency compared with the natural corticosteroid. Less potent pituitary suppressant activity than e.g. dexamethasone. Predominant glucocorticoid activity, after activating the nuclear glucocorticoid receptor increasing the expression of the genes for the key gluconeogenetic enzymes PEPCK and G6P, elevating blood glucose and initiating antiporphyrogenic insulin release.
Hepatic exposure
Irrelevant.
Metabolism and pharmacokinetics
Microsomal CYP-oxidation mainly in the liver. Biological half life 12-36 hours. Slower metabolism compared with the natural hormones. As a ligand to glucocorticoid nuclear receptor, prednisolon may participate in PXR activation and subsequent ALAS1 induction. Inducer of gluconeogenetic enzymes. Substrate of CYP3A4, the metabolism affected by CYP-inducers as well as by CYP3A4 inhibitors. No effects on the elimination rate of other CYP-metabolized drugs. Systemic effects in rectal administration.
Personal communication
Skadberg, patient report (n=1): tolerated. Others, patient report (n=2): tolerated.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.

References

  1. Scientific articles
  2. Pascussi et al Ann Rev Pharmacol 2008; 48:1-32. #3270
  3. Thunell. Genomic approach to acute porphyria. Physiol Res 2006. PMID 17298222. #3285
  4. Moreau et al. Mol Pharmaceutics 2008; 5:35-41. PMID 27885969. #3286
  5. Drug reference publications
  6. Martindale #3258
  7. Other sources
  8. National Formularies ( Norwegian and Swedish ). #3284

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