DERMATOLOGY

Medications in Dermatology

Corticosteroids

  • Potency: Ointment >creams- occlusive nature of an ointment enhances absorption of the corticosteroid.
  • Creams
    • more preservatives and excipients than ointments, and so are more likely to cause hypersensitivity or irritation.
    • A cream base may be used for an acute weeping rash.
  • gel or lotion
    • hair-bearing areas
  • Stubborn dermatoses
    • benefit from occlusion, such as plastic wrap, occlusive dressings or gloves, applied overnight with appropriate securing in place.
  • absorption
    • greatest at thin skin of eyelids, genitals and skin creases: use a mild corticosteroid.
    • least at  thick skin of palms and soles: use apotent corticosteroid.
    • the limbs and trunk: moderately potent corticosteroid
  • For Candida infection
    • (e.g. secondary infection of irritant napkin dermatitis)
    • mix 1% hydrocortisone in equal quantities with an antifungal preparation such as nystatin.
Generic nameFormulation
Group I Mild
Desonide 0.5%Lotion
Hydrocortisone 0.5%, 1%Cream, ointment
Group II Moderately potent
Betamethasone valerate 0.02%Cream
Betamethasone valerate 0.05%Cream, ointment
Clobetasone butyrate 0.05%Cream
Triamcinolone acetonide 0.02%, 0.05%Cream, ointment
Group III Potent
Betamethasone valerate 0.1%Cream, ointment
Betamethasone dipropionate 0.05%Cream, ointment, lotion
Methylprednisolone aceponate 0.1%Cream, ointment, fatty ointment, lotion
Mometasone furoate 0.1%Cream, ointment, lotion, hydrogel
Group IV Very potent
Betamethasone dipropionate 0.05% (in optimised vehicle)Cream, ointment
Clobetasol propionate 0.05%Cream*, ointment*, lotion*, shampoo

Overall, the choice of potency will largely be guided by the following factors:

  • patient: age (infant, child or adult) and lesion location
  • lesion: type and severity of lesion (as described in Table 2)
  • topical medication: molecular structure, percentage and formulation/vehicle
  • method of application: occlusive dressing increases potency with better efficacy and effect, and wet dressing intensifies the effect by improved permeability of topical medication.
Common skin conditions treatable with topical corticosteroid (TCS) agents
Mild (low) potency TCS
 
Dermatitis (face, eyelids, napkin area)IntertrigoPerianal inflammation
Mild-to-moderate potency TCS
 
Atopic dermatitisAsteatotic eczemaContact dermatitisDry nummular eczemaPerianal inflammation (severe)Intertrigo (short term)Scabies (after scabicide)Seborrhoeic dermatitis
Moderate-to-potent/ultrapotent TCS
 
Atopic dermatitis (severe)Alopecia areataContact dermatitis (severe)Eczema of hyperkeratotic, exudative nummular, hand and feetGranulomatous skin disorders – Granuloma annulare, Necrobiosis lipoidica, and sarcoidosisLupus erythematosusLichen – simplex chronicus, planus and sclerosusPemphigus and pemphigoidPsoriasisStasis dermatitisVitiligo

Topical corticosteroid application

  • advice of applying TCS agents ‘sparsely’ is no longer applicable
  • instead, ‘liberally’ is encouraged. 
  • Type
    • ointment : is preferred for dry, scaly and mucocutaneous lesions
      • (eg on the lips and genitals)
    • Cream: wet/oozing lesions
    • liquid (solution, lotion) for hairy areas (eg scalp), where cream or ointment is unable to reach the areas of affected skin
  • moisturisers/emollients
    • It is highly recommended to use adjunct moisturisers/emollients following application of TCS agents to affected areas. 
    • The moisturiser can be applied locally or to the whole body to ease pruritus and irritation by maintaining optimum skin moisture. 
    • The moisture alone is also useful as a steroid-sparing agent in trivial dermatitis. 
    • Diluting the topical steroid with moisturiser does not change the potency of the medicine.
  • Timing
    • Application is usually encouraged in the evening/night after bathing to avoid incidental removal of the medication as a result of day-to-day activities. 
    • In terms of frequency, a once-daily regimen is generally recommended for better compliance. 
    • Twice-daily application may be considered for the initial week(s) for certain severe lesions, reducing to daily or alternate-day application depending on the response.
  • occlusive dressing
    • An occlusive dressing with appropriate cover, such as a tubular bandage or plastic wrap, is favourable for severe and thick/keratotic/lichenified lesions. 
    • Occlusion with a non-irritant glove or sock can also be used for lesions of the hand or foot, respectively. 
  • duration
    • The duration of treatment depends on the type and intensity of the lesion
  • Amount
    • The required dose (amount) is guided by location and extent of the lesion.
    • The fingertip unit (FTU) is a useful general guide for the amount of topical agent
    • A child aged six years with face and neck involvement requires 2 FTU (1 g) daily, and a 15 g tube of topical corticosteroid (TCS) would last two weeks.
    • An adult with one leg and foot involvement requires 8 FTU (4 g) daily, and two tubes of 15 g TCS or one tube of 30 g would last one week.
  • General Rule that
    • 30 g
      • – will cover the adult body once
      • – will cover hands twice daily for 2 weeks
      • – will cover a patchy rash twice daily for 1 week
    • that 200 g will cover a quite severe rash twice daily for 2 weeks

Adverse effects

  • Topical steroids have
    • anti-inflammatory effects
    • immunosuppressive effects
    • antiproliferative effects
  • Adverse effects
    • skin thinning (atrophy)
    • stretch marks (striae) in armpits or groin area
    • enlarged or broken capillaries (telangiectasia)
    • easy bruising and tearing of the skin
    • localised increased hair thickness and length (hypertrichosis)
    • acne-like changes
    • colour change of the skin
    • periorificial dermatitis
    • steroid rosacea
    • pustular psoriasis
    • contact dermatitis
    • pigment alteration
    • Red Skin syndrome
      • ‘topical corticosteroid withdrawal’
      • rare adverse reaction resulting from inappropriate topical corticosteroid use in some conditions (eg periorificial dermatitis, rosacea, some psoriasis conditions) and when treating certain areas of the body (eg genital area).
      • can also be associated with an exacerbation of the original skin condition
      • Symptoms include
        • papulopustular rashes
        • red burning skin
    • hypothalamic–pituitary–adrenal axis suppression is extremely rare, Nevertheless, it is necessary to be mindful of systemic absorption
      • iatrogenic Cushing’s syndrome
      • growth retardation
      • cataract
      • glaucoma
    • susceptible individuals :
      • young children and elderly patients with thin skin, higher-potency TCS agents
Red Skin Syndrome
  • Adverse events are generally reversible by cessation of medication
  • methylprednisolone aceponate and mometasone furoate are associated with lesser local and systemic adverse effects than older formulations of TCS because of their lipophilic structure and pharmacokinetics.
  • Mild-to-moderate-potency steroids and short-term use of potent topical steroids are safe in pregnancy and lactation according to a systematic review 

Keratolytic agents

  • are acids that disrupt the adhesions between the keratinocytes thus causing shedding of these layers. 
  • used for exfoliative procedures/ keratolytic peels
  • used in acne, roughness and mild dyspigmentation
  • Clinical results take time and repeated treatments to become apparent.
  • ex:
    • Urea
    • Salicylic acid
      • range from 0.5% up to 30%
      • Salicylic acid 2-3% _ Betamethasone 0.05% (Diprosalic®) = Psoriasis, Hyperkeratotic eczema
      • Salicylic acid 15-27% (Duofilm®)  =   Viral warts, Corns
      • Salicylic acid 2%, Coal tar solution 12%, Sulphur 4% (Coco-Scalp) = Seborrhoeic dermatitis Dandruff, Scalp psoriasis
      • Salicylic acid 0.5% oil-free acne wash (Neutrogena®) = Acne
    • Lactic acid
    • Fruit acids (alpha hydroxy acids)
    • Propylene glycol
    • Jessner’s solution – 14% each of resorcinol, salicylic acid, and lactic acid, mixed in ethanol.

side effects

  • Moderate or severe skin irritation (particularly if not present before use of this medicine)
  • Flushing
  •  warm skin and reddening of skin.
  • True allergy to topical salicylic acid is rare, however serious reactions including anaphylaxis have been reported.

Precautions 

  • do not use any of the following preparations on the affected area
    • Alcohol containing preparations
    • Any other medicated topical agents, e.g. benzoyl peroxide, topical retinoids, calcipotriol
    •  Abrasive soaps and cleansers
    • Cosmetics or soaps that dry the skin or are designed to peel/exfoliate

Coal tar 

  • It appears to have antimicrobial, antipruritic (reduce itching) and keratoplastic (normalise keratin growth in the skin and reduce scaling) effects.
  • used for treat the scaling, itching and inflammation of
    • Scalp psoriasis
    • Palmoplantar pustulosis  
    • Plaque psoriasis
    • Atopic dermatitis
  • Products:
    • Coconut Oil Compound Ointment (Coco-Scalp™) for scalp psoriasis
    • Egopsoryl TA Gel™ to apply to psoriasis plaques
    • Polytar Emollient and Liquid for bathing
    • Shampoos such as Polytar™, Sebitar™, Ionil T™ and Fongitar™
  • The use of coal tar is declining as newer compounds effective against the different forms of psoriasis are replacing it. 
  • However, it still has the advantages of being low cost and causing less systemic toxicity as compared with more modern therapies.
  • general tips for using coal tar products.
    • Apply it at bedtime if possible to avoid the daytime inconvenience of the smell and staining
    • Leave on skin for at least 2 hours unless otherwise directed by your doctor
    • If treating the scalp, apply with a downward stroke in the same direction as hair growth
    • Cover or wrap with bandages to help the preparation stay in place and prevent staining. Do not use plastic wrap as this may cause irritation and infection
    • Do not apply to infected, blistered, raw or oozing areas of the skin
    • After applying coal tar preparations, protect the treated area from direct sunlight and do not use a sunlamp unless otherwise directed by your doctor.

Vitamin A 

is also called retinol. Natural and synthetic compounds derived from retinol are known as retinoids and include:

  1. First generation
    • Isotretinoin, Retinol, Retinal, Tretinoin, Alitretinoin are modifications of natural retinoids which do not act selectively
  2. Second generation
    • Acitretin is an oral retinoid in which a benzene ring is replaced by a cyclohexane ring
  3. Third generation
    • Adapalene, tazarotene, and bexarotene are polyaromatic retinoids with selective activity for the retinoid receptors
  4. Fourth generation 
    • Trifarotene is highly specific for the skin retinoid (RAR-γ) receptor

Topical retinoids

  • Types and uses
    • adapalene, isotretinoin, tretinoin, trifarotene
      • Mild – moderate Acne vulgaris and its complications
        • Applied to the face once daily at bedtime
        • effective first-line treatment for comedonal and inflammatory acne
        • not recommended as monotherapy for severe acne (pustules,deep nodules, cysts)
        • It may take 12 weeks or longer before improvement is seen.
        • useful to treat post-inflammatory hyperpigmentation as they inhibit melanosome transfer and facilitate melanin dispersal. 
        • They are particularly recommended for the treatment of acne in skin of colour.
      • Photodamage and photoageing
        • If used longterm (>6 months) topical tretinoin can reduce freckling, solar lentigines, fine wrinkling, solar comedones, sun-induced skin fragility, and actinic keratoses
      • Melasma
        • active ingredient in skin bleaching cream to treat melasma.
      • Darier disease
    • Alitretinoin
      • Kaposi sarcoma  
    • Bexarotene
      • Cutaneous T-cell lymphoma
    • Tazarotene
      • Facial acne
      • Postinflammatory hyperpigmentation in dark skin
      • Chronic plaque psoriasis
      • Photodamage
  • Contraindications
    • Hypersensitivity or allergy to retinoids or excipients
    • Some topical retinoids are contraindicated for use in pregnancy
  • Precautions
    • Topical retinoids can make eczema worse because of their drying effect – (erythema, peeling, dry skin)
    • Topical retinoids can cause photosensitivity
    • women of childbearing age must use effective contraception due to the teratogenic effects of retinoids.
    • not recommended for use by young children
    • Not suitable to treat large areas of the body such as extensive acne over the back or chest
    • Can be irritating if applied close to the eyes or lips. Adapalene is the least irritating topical retinoid, and tretinoin the most

Oral retinoids

  • Acitretin
  • Alitretinoin
  • Bexarotene (a rexinoid)
  • Isotretinoin
  • Vitamin A (retinol)

In acne, isotretinoin:

  1. Reduces sebum production
  2. Shrinks the sebaceous glands
  3. Reduces follicular occlusion
  4. Inhibits the growth of bacteria
  5. Has anti-inflammatory properties.

Used for:

  • for the treatment
    • acne
    • severe follicular conditions
      • Rosacea. Seborrhoea, hidradenitis suppurativa, scalp folliculitis.
    • acute promyelocytic leukaemia
    • severe psoriasis (pustular psoriasis, erythrodermic psoriasis, and palmoplantar psoriasis) palmoplantar keratoderma
    • pityriasis rubra pilaris
    • Darier disease
    • lichen planus
    • lichen
    • cutaneous lupus erythematosus.

Acne dose: Isotretinoin

  • 0.1 to over 1 mg/kg body weight OR lower dosages, unrelated to body weight (eg, 10 mg/day)
  • side effects of isotretinoin are dose dependent; at 1 mg/kg/day, nearly all patients will have some side effects, whereas, at 0.1 mg/kg/day, most patients will not
  • Some patients may only need a small dose once or twice a week
  • treatment may be completed in a few months or continue for several years.
  • courses have often been restricted to 16–30 weeks (4–7 months) to minimise the risk of teratogenicity

Adverse effects 

  • teratogenicity (category X)
    • malformations include craniofacial, central nervous system, cardiovascular, and thymic
    • Blood donation by males and females on isotretinoin is not allowed in case the blood is used for a pregnant woman.
  • Mucocutaneous effects:
    • cheilitis, dryness of the oral mucosa, epistaxis, xerophthalmia, xerosis, fingertip fissuring, hair loss, nail fragility, periungual granuloma, paronychia
  • Musculoskeletal effects:
    • myalgia, arthralgia, bone pain, premature fusion of the epiphyses, skeletal hyperostosis, calcification of tendons and ligaments
  • Neurological effects:
    • headaches, raised intracranial pressure
  • Ophthalmologic effects:
    • nyctalopia (loss of night vision)
  • Gastrointestinal/metabolic effects:
    • nausea, abdominal pain, diarrhoea, elevated liver enzymes and lipids (triglycerides and cholesterol).
  • Psychiatric effects:
    • depression, irritability/aggression, suicidality, and sleep disturbances. Retinoid-associated depression and suicidality are debatable due to the lack of valid/scientific study
  • Commercial pilots may be subject to flying restrictions if they take isotretinoin
  • High dose isotretinoin in very young children has been associated with
    • premature epiphyseal closure, leading to shorter stature (this is not seen in the low dose used for the treatment of acne)

Calcipotriol

  • Calcipotriol is a vitamin-D derivative
  • 1% as powerful as the natural hormone calcitriol (also known as 1,25 dihydroxycholecalciferol).
  • Calcipotriol is also available in combination with betamethasone propionate as a
    •  gel or ointment (Daivobet)
    • foam (Enstilar).
  • used for
    • used mainly for psoriasis
    • moderately or very effective for about 80% of patients
    • patches become less scaly and thick, but red patches often persist despite continued treatment.
  • Plaques of severe psoriasis before and after six weeks use of calcipotriol ointment:
Psoriasis pre-calcipotriolPsoriasis post-calcipotriol
  • Also used in
    • Morphoea
    • Palmoplantar pustulosis
    • Ichthyosis
    • Palmoplantar keratoderma
    • Grover disease
    • Disseminated superficial porokeratosis and linear porokeratosis
    • Benign familial pemphigus
    • Pityriasis rubra pilaris
    • Acanthosis nigricans
    • Epidermal naevus.

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