methylprednisolone aceponate

Action and Spectrum

Actions and Spectrum:  

Actions:  

Methylprednisolone aceponate has an effective action against inflammatory processes since it suppresses the accumulation of macrophages, leukocytes and other cells to the area of inflammation. It also inhibits the formation of inflammatory mediators such as the prostaglandins and leukotrienes by inhibition of the enzyme phospholipase A2.

Drug Interaction

Adverse Reaction

Adverse reaction 

Frequency not defined 

Itching

Dryness of skin

Allergic skin reactions

Black Box Warning

Black Box Warning  

None

Contraindication / Caution

Contraindication/Caution:  

Atrophic skin diseases

Perioral dermatitis

Hypersensitivity

Postvaccination skin reactions

Acne vulgaris

Viral diseases

Rosacea

Pregnancy / Lactation

Pregnancy & breastfeeding: 

Pregnancy consideration:   

No data is available regarding the administration of the drug during pregnancy.

Breastfeeding warnings:   

No data is available regarding the excretion of drugs in breast milk.

Pregnancy category:  

• Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester.
• Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
• Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
•  Category D: Adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.
• Category N: No data for the drug under this category is available.

Pharmacology

Pharmacology:  

Methylprednisolone aceponate inhibits the formation of inflammatory mediators such as the prostaglandins and leukotrienes by inhibition of the enzyme phospholipase A2.

Pharmacodynamics: 

It has an effective action against inflammatory processes since it suppresses the accumulation of macrophages, leukocytes and other cells to the area of inflammation.

Pharmacokinetics:  

Absorption 

Methylprednisolone aceponate when applied topically it has minimal systemic absorption with a total percutaneous absorption of less than 1% due to its lipophilic nature.

Distribution 

Due to limited absorption, it is rapidly metabolized in the skin to methylprednisolone 17-propionate as a potent anti-inflammatory compound with higher affinity for intracellular corticosteroid receptors.

Metabolism 

It hydrolyzes to methylprednisolone 17-propionate which is inactivated by conjugation with glucuronic acid and primarily excreted in the liver.

Elimination & Excretion 

Its inactive metabolites are primarily excreted through urine with in a 16-hour elimination half-life. The primary metabolite methylprednisolone 17-propionate is mostly eliminated through renal pathways.

Adminstartion

Administration:  

Methylprednisolone aceponate 0.1% is a potent glucocorticosteroid used to treat eczema in adults and children. Its anti-inflammatory activity makes it comparable to betamethasone valerate, hydrocortisone butyrate, and prednicarbate. 90% of patients show improvement or remission after 3-4 weeks with tolerability generally good. More clinical experience is needed to determine potential additional benefits over other glucocorticosteroids.

Patient Information Leaflet

Patient information leaflet  

Generic Name: methylprednisolone aceponate

Why do we use methylprednisolone aceponate?  

The drug is synthetic corticosteroids. It is effective in various skin conditions such as dermatitis, and in eczema. It is also used on situations like sunburn since it is an anti-inflammatory drug, and it provides a soothing effect to the skin.
Methylprednisolone aceponate has roles in other classes of diseases such as different types of eczema including contact and degenerative eczema.