Topical Glucocorticoids: Dermocorticoids

Products

Dermocorticoids are commercially available in the form of creams, ointments, lotions, gels, pastes, foams, scalp applications, shampoos, and solutions, among others. Numerous drugs are available, including many combination preparations. Hydrocortisone was the first active ingredient to be used in the 1950s. Today, dermocorticoids are among the most important drugs in dermatology.

Effects

Glucocorticoids have anti-inflammatory, antiallergic, immunosuppressive, antiproliferative, vasoconstrictive, and antipruritic properties. The effects are based on binding to intracellular glucocorticoid receptors in the cytoplasm of cells. The resulting complex interacts with DNA and promotes protein expression. In addition, the agents also exert extragenomic effects.

Structure and properties

Topical corticosteroids are derived from endogenous glucocorticoids and have a steroid backbone. To modify their properties, they are halogenated (chlorinated, fluorinated), alkylated (methylated), anellated, and esterified, among others. This alters potency, lipophilicity, pharmacokinetics, and absorption into the skin. Some glucocorticoids are prodrugs that are hydrolyzed in the skin by esterases and thereby activated. A good example of these modifications is fluticasone propionate, which is fluorinated, methylated, and esterified with propionic acid.Caution: designations such as fluticasone propionate and fluticasone furoate do not represent drug salts but esters with a covalent bond. Therefore, these suffixes (e.g., -propionate, -furoate) cannot be omitted.

Active ingredients

Dermal glucocorticoids are divided into drug classes according to their potency. Some of the drugs listed are combination preparations. Class I: Weakly potent:

Class II: moderately potent:

Class III: Strongly effective:

  • Betamethasone valerate (e.g., Betnovate).
  • Desoximetasone (out of commerce)
  • Fluocinolone acetonide (Synalar)
  • Diflucortolone valerate (Travocort)
  • Fluocinonide (Topsym)
  • Halometasone (Sicorten plus)
  • Methylprednisolone aceponate (Advantan)
  • Mometasone furoate (Elocom)
  • Fluticasone propionate (Cutivate)
  • Prednicarbate (Prednitop)

Class IV: Very potent:

By the way, groundhog ointments are natural cortisone ointments. The marmot fat contains, among other things, hydrocortisone (class I).

Indications

Dermocorticodes are administered for the treatment of eczematous, inflammatory, hyperproliferative, pruritic, and allergic skin conditions. Examples include eczema, psoriasis, atopic dermatitis, seborrheic dermatitis, insect bites, sunburn, lupus erythematosus, and scalp inflammation (selection).

Dosage

According to the SmPC. The drugs are usually applied once to a maximum of twice daily. Because of the potential for adverse effects, dermocorticoids should be used for as short a time as possible and applied only thinly. The duration of application is dictated by the professional information. If dermocorticoids are needed for a longer period of time, breaks in therapy must be taken or cortisone-free skin care products must be applied in the meantime. Topical glucocorticoids should not be applied over large areas and should not be overdosed. Caution should be exercised when applying them to the face, genital region, and intertriginous areas of the body because the active ingredients are more easily absorbed into the body there.

Contraindications

Contraindications include (selection):

  • Hypersensitivity
  • Rosacea
  • Perioral dermatitis
  • Acne
  • Itching without inflammation
  • Skin ulcers
  • Viral infections, e.g. a herpes infection, shingles.
  • Bacterial skin infections (as monotherapy).
  • Skin fungal infections (as monotherapy).
  • Use in infants, children, during pregnancy and lactation: see SmPC.

For full precautions, see the drug label.

Interactions

Some glucocorticoids are substrates of CYP450 isozymes. Systemic exposure may increase with CYP inhibitor therapy. The excipients of creams and ointments may interfere with the safety of latex condoms when used in the genital area. Occlusion (e.g., bandages, patches, diapers) may increase absorption into the body.

Adverse effects

Possible adverse effects include:

  • Local skin reactions, such as a burning sensation, pain, itching, irritation, redness
  • Hypersensitivity reactions, contact allergy.
  • Infectious diseases due to immunosuppressive effects.
  • Systemic side effects of glucocorticoids (e.g., NNR suppression, rare, especially with overdose), see under cortisone tablets.
  • Tachyphylaxis
  • Rebound after rapid discontinuation

In the event of improper use, i.e. overdose, persistent occlusion and too long a period of use, the skin can be damaged. This manifests itself, for example, in a thinning of the skin (skin atrophy), skin striae (striae distensae), pigmentation disorders, increased hairiness and telangiectasia. There is also a risk of systemic cortisone side effects. However, when used as directed, the widespread “cortisone scare” is unfounded. See also under medication overuse.