Betamethasone

Betamethasone
ATC Code A01AC05, A07EA04, C05AA05, D07AC01, D07XC01, H02AB01, R01AD06, R03BA04, S01BA06, S01CB04, S02BA07, S03BA03
Formula C22H29FO5
Molar Mass (g·mol−1) 392,46
Physical State solid
Melting Point (°C) 232
CAS Number 378-44-9
PUB Number 9782
Drugbank ID DB00443
Solubility practically insoluble in water

Basics

Betamethasone is a drug from the group of glucocorticoids. It is used to treat a number of conditions including rheumatic conditions such as rheumatoid arthritis and systemic lupus erythematosus, skin conditions such as dermatitis and psoriasis, allergic conditions such as asthma and angioedema, Crohn's disease, cancers such as leukaemia, and in combination with fludrocortisone for adrenal insufficiency. It can be taken by mouth, injected into a muscle, or applied to the skin in the form of a cream or solution. Betamethasone is available by prescription only.

Pharmacology

Pharmacodynamics

Betamethasone 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. Betamethasone 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.

Betamethasone 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

The absorption and potency of betamethasone is highly dependent on the salt used. By attaching a specific salt, certain properties such as solubility and rate of absorption can be controlled. The metabolism of betamethasone yields 6 metabolites. Metabolic processes include 6β-hydroxylation, 11β-hydroxyl oxidation, and reduction of the C-20 carbonyl group followed by removal of the side chain. Corticosteroids are predominantly excreted in the urine. The half-life of betamethasone is about 10-12 hours.

Toxicity

Side effects

  • Euphoria
  • Depression
  • inhibition of adrenal activity
  • Hypertension
  • excessive hair growth (hypertrichosis)
  • Ecchymosis
  • Skin irritations

Prolonged use of this medicine on large areas of skin, broken or rough skin, folds of skin or under airtight dressings may, in rare cases, result in the absorption of enough corticosteroid to cause systemic side effects, such as a decrease in the production of natural hormones by the adrenal glands.

Serious side effects include increased risk of infection, muscle weakness, severe allergic reactions, and psychosis.

Toxicological data

LD50 (mouse, oral): > 4500 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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