Prednisolone

Prednisolone
ATC Code A01AC04, A07EA01, C05AA04, D07AA03, D07XA02, D10AA06, H02AB06, R01AD02, S01BA04, S01CB02, S02BA03, S03BA02
Formula C21H28O5
Molar Mass (g·mol−1) 360,44
Physical State solid
Melting Point (°C) 239
CAS Number 50-24-8
PUB Number 5755
Drugbank ID DB00860
Solubility sparingly soluble in water

Basics

Prednisolone is a drug in the glucocorticoid group used to treat certain types of allergies, inflammatory diseases, autoimmune diseases, and cancers. These include the treatment of rheumatoid arthritis, dermatitis, eye inflammation, asthma, and multiple sclerosis. It is administered in the form of tablets, injection into a vein, as a skin cream and as eye drops.


Pharmacology

Pharmacodynamics

Prednisolone acts because of its structural similarity to endogenous glucocorticoids. Unbound, it can penetrate the membrane of the cell and then bind with high affinity to intracellular glucocorticoid receptors.

The anti-inflammatory (anti-inflammatory) effect is achieved by interfering with the so-called arachidonic acid metabolism. Prednisolone causes fewer prostaglandins and leukotrienes to be produced at the end of this metabolism. These are significantly involved in the inflammatory process of the human body.

Prednisolone has an anti-allergic effect by preventing the release of histamine and simultaneously reducing the number and activity of certain B and T lymphocytes.

Pharmacokinetics

Bioavailability is about 70% and maximum plasma concentration is reached after about 1-3 hours. Plasma protein binding can vary widely and is usually between 60 and 90%. Prednisolone is metabolized in the liver and 98% is excreted by the kidneys. The half-life is 2-4 hours.

Toxicity

Side effects

Side effects for short-term use include nausea and fatigue.

More severe side effects include psychiatric problems, which may occur in about 5% of people.

Common side effects with long-term use include bone loss, weakness, yeast infections, and easy bruising.

While short-term use in the later part of pregnancy is safe, long-term use or use in early pregnancy is occasionally associated with harm to the baby and therefore should not be used during this time.

Toxicological data

LD50 (rat, oral): 120 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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