TOPICALS

THERAPY IN
DERMATOLOGY

Dr Anis Bt Omar
Jabatan Dermatologi, HRPZ2
TOPICALS THERAPY
 Topical formulations are applied directly to
the skin

 Advantages :

 An increased dose of medication is applied

where it is needed
 There are reduced side effects and toxicity to
other organs compared to systemic medications.
DISADVANTAGES

 Time-consuming
 Complicated

eg: several different formulations have been

prescribed
 Messy and uncomfortable.
 Topical formulations are made up in a
vehicle, or base which may be optimised for
a particular site of the body or type of skin
condition

 designed to be moisturising or to maximise

the penetration of an active ingredient,
often a medicine, into or through the skin.
VEHICLES OF FORMULATIONS

 Topicals formulation contain an active

ingredients + vehicles
 Vehicle usually contains water, oil, alcohol or
propylene glycol mixed with preservatives,
emulsifiers, absorption promoters
and fragrances.
 The amount of the active ingredient which
is absorbed through the skin depends on the
following factors:

 Skin thickness (thin skin)

 Skin barrier function (disrupted skin)
 where there is occlusion (skin folds, under
dressings, or when a greasy ointment is used)
 Small molecules
 Lipophilic compounds
 Higher concentrations of the active ingredient
QUANTITY OF TOPICAL
FORMULATIONS

 The vehicle
 The thickness of the application
 The total area to be treated
 The frequency of the application
 The duration of the treatment course.
 FINGER TIP UNIT

Finger tip unit (FTU) = 500mg = treat 2% BSA

One fingertip unit covers one side of 2 flat
hands
 RULE OF NINE
 It takes 20–30 g of cream or ointment to
cover an adult's total body once.
SOLUTION
 Water or alcoholic lotion containing a
dissolved powder.
LOTION
 Usually considered thicker than a solution.
 More likely to contain oil as well as water or
alcohol.
 A shake lotion separates into parts with time
so needs to be shaken into suspension before
use.
Less greasy
Easy to apply over a large area
Suitable for areas with hair
Evaporation of water gives a
cooling effect (calamine lotion)
CREAM
 Thicker than a lotion
 Maintaining its shape.
 Requires preservative to extend shelf life.
 Often moisturising.
 Good for acute & subacute lesions
OINTMENT
 Semi-solid, water-free or nearly water-free
(80% oil).
 Greasy, sticky, emollient,
protective, occlusive.
 No need for preservative, so
contact allergy is rare.
 May include a hydrocarbon (paraffin), wool
fat, beeswax, macrogols, emulsifying wax,
cetrimide or vegetable oil (olive oil, arachis
oil, coconut oil).
 Good for thick chronic lesions, palms, sole
GEL
 Aqueous or alcoholic monophasic semisolid
emulsion, often based on cellulose and
liquefies upon contact with skin.
 Often includes preservatives and fragrances.
PASTE
 A concentrated suspension of oil, water and
powder.
AEROSOL FOAM/SPRAY
 A solution with pressurised propellant.
POWDER
 Solid, for example, talc (a mineral) or corn
starch (vegetable).
 Additional absorbent property
COLLOID
 Liquid preparation that forms a flexible film
when dry
 Eg opsite spray ( to seal off minor cuts and
wound)
PAINT/LACQUER
 Solutions of one or more ingredients intended for
application with a brush leaving a film of drug on
skin surface
 Eg podophyllin paint, castellani’s paint, nail
lacquer
PROPER USE OF TOPICALS
 Aim:
 achieve efficacy

 minimize risk of side effects

 Duration of use:
 Intermittent

 Short term

 Long-term
STRATEGIES
Potent agents used for short-term to
achieve response followed by long-term
intermittently use
or moderate potency agents
Continuous long term treatment- use
the least potent agent that can achieve
disease control or transitioned to an
agent with the lowest long-term risk
TOPICAL CORTICOSTEROID
 Cornerstone of treatment in the majority
of dermatological diseases

 Mechanisms of action
 anti-inflammatory

 anti-proliferative

 immunosuppressive

 vasoconstrictive
CORTICOSTEROID POTENCY

( DERMOVATE )

(ELOMET)
(PURE)
(EUMOVATE)

(BVC 1:2)

(1% HCT CREAM)

WHAT IS AVAILABLE ?
WHICH CORTICOSTEROID?

 Appropriate potency and vehicle

 Consider:
 disease severity

 site

 age of the patient

 patient preference
TOPICAL STEROID SELECTION-
POTENCY
 Super potent
 For severe dermatoses, chronic lichenified ,

hyperkeratotic over non-facial and non-intertriginous

 Scalp, palms, soles and extensor surface

 Medium to high potency

 Mild – moderate ; non-facial and non-intertriginous

areas

 Low potency
 Can be used on large areas and thinner skin

 Face, eyelids, genital and intertriginous areas

 In infant , elderly
TOPICAL CORTICOSTEROID SELECTION -
VEHICLE
 Vehicle influences the absorption and potency of the drug

Ointments
 for infiltrated, lichenified lesions
 enhance penetration of the drug by means of occlusive
effect

Creams
 acute and subacute dermatoses
 Face and intertriginous areas

Addition of propylene glycol

 increases the solubility of corticosteroids in the vehicle
 Increased potency
TOPICAL CORTICOSTEROID
SELECTION - ABSORPTION
 Absorption varies with respect to anatomical
location

 Variable thickness of the stratum corneum and

its lipid composition

 Groin, axillae, neck, and face have increased

absorption and thus more likely to develop local
side effects

 Penetration varies between eyelid and plantar

skin about 300-fold
ABSORPTION
 Defective epidermal barrier
 in atopic dermatitis, penetration of topical
corticosteroids is 2x - 10x greater than that
through healthy skin

 Skin of delicate sites

 eyelids is much more likely to atrophy from
even mild-potency topical corticosteroids
DURATION OF TREATMENT
 Duration of use:
 Potent corticosteroids, limit use to 2- 4
weeks
 The optimal end point for use of the less

potent agents is not known

 Continuous use for longer periods

 Increased risk of cutaneous side effects and
systemic absorption
 Gradual reduction in potency, frequency of

use following clinical response

 In general:
 Super potent : 2-4 weeks
 Potent and medium : 6-8 weeks

 Stop treatment once skin condition resolves

 If not improved, refer dermatologist

SIDE EFFECTS OF CORTICOSTEROID
 Cutaneous
 Atrophy
 Telangiectasia

 Striae

 Steroid rosacea

 Steroid acne

 Perioral dermatitis

 Folliculitis

 Purpura
 Systemic side effect:

 Hypothalamic-pituitary-adrenal (HPA) axis

suppression
 Cushing’s syndrome

 Osteonecrosis of the femoral head

 Cataracts

 Glaucoma
LOCAL CUTANEOUS SIDE EFFECTS

 more frequent than systemic side effects

 commonly at steroid-sensitive sites (face
and intertriginous areas)
 areas treated for long duration
 may cause contact dermatitis
SYSTEMIC SIDE EFFECTS
 Greatest risk
 high-potency agents used over a large surface
for a prolonged period
 occlusion

 widespread, extended use of mid-potency

agents

 Limit continuous use of potent agents to:

 twice a day application / bd
 up to 2-4 weeks

 no more than 50 g/wk

REBOUND

 Disease recurs worse than the pretreatment

baseline
 After topical corticosteroid is discontinued
 Occur most typically when treatment is
abruptly discontinued
 To avoid rebound: taper with gradual
reduction both potency and frequency
TACHYPHYLAXIS

 Loss of effectiveness with continued use

 May affect long-term efficacy
PRACTICAL TIPS:
ACUTE LESIONS
 Inflamed, oozing (wet), painful, red
 e.g Cellulitis, acute contact dermatitis

 Use mild gentle treatment

 Wet dressings, dabs, soaks

 Normal saline or KMNO4

 Use only mild topical steroids

eg 1% Hydrocort cream, BVC1:4

 Creams better than ointments

 Avoid irritants such as coal tar, dithranol,

calcipotriol
CHRONIC LESIONS

 Dry, very scaly, thick

 e.g. Psoriasis, lichenified chronic eczema

 Liberal use of moisturiser is important

 Frequency can be more often 3-4x per day
 e.g. Aqueous cream, Ung Emulsificans, vaseline
 Ointments work better than creams
 eg BVO Vs BVC
EMOLLIENTS
Occlusives
 which provide a layer of oil on the surface of
the skin to slow water loss and thus increase
the moisture content of the stratum corneum

Humectants
 which are substances introduced into the
stratum corneum to increase its water
holding capacity
AVAILABLE EMOLLIENT
 Aqueous cream
 Aqueous in Glycerin
 Vaseline (white soft paraffin)
 Emulsificant ointment (Ung emulsificant
ointment)
 10% Urea cream
KERATOLYTICS
 Soften and facilitate exfoliation of epidermal
cells
 Salicylic acid cream / ointment
 used to treat psoriasis, seborrheic dermatitis,
acne, and warts
 Adverse effects : burning
 if large areas are covered, systemic toxicity
 Lactic acid
 Alpha hydroxy acids
 Urea cream
 used to treat plantar keratodermas and ichthyosis
COAL TAR
 obtained by the destructive distillation of
bituminous coal at very high temperatures
 main groups of compounds :48%
hydrocarbons, 42% carbon and 10% water
 mixed with other ingredients, such as
salicylic acid and sulphur
 to make lotions, creams, ointments and
shampoos
 treat the scaling, itching and inflammation
of psoriasis, eczema, and seborrheic
dermatitis.
 Advantages:low cost and less systemic
toxicity
 antimicrobial
 antipruritic (reduce itching)
 keratoplastic (normalise keratin growth in
the skin and reduce scaling) effects.
 s/e:mild stinging or skin irritation
 discolour bleached, tinted, light blond or
grey hair
 photosensitivity
 Ung cocois co :
Coal tar+ sulphur+ salicylic
acid

LIQUOR PICIS CARBONIS

BENZOYL PEROXIDE
 Both antibacterial and comedolytic
properties
 s/e: skin irritation, bleaching of hair and
colored fabric
TOPICAL RETINOIDS
 Vitamin A derivatives
 Used for acne, fine wrinkles and
hyperpigmentation
 Common s/e:
 Erythema, burning and scaling

 Don’t apply together with BPO as it oxidizes

tretinoin

 Adapalene gel -> synthetic naphthoic acid

derivative with retinoid activity
TOPICAL ANTIBIOTICS
 To reduce number of
Propionibacterium.acnes and reduce
inflammation.
 Clindamycin, erythromycin

 Do not use as monotherapy – to prevent

resistance. Often combined with BPO

 Fusidic acid/mupirocin – cover gram +ve

bacteria
 Neomycin – can cause contact dermatitis
 Neomycin
 Fusidic acid
 Mupirocin
 Chloramphenicol

 Clindamycin
 Erythromycin
 Metronidazole
TOPICAL ANTIFUNGALS

 Fungi static (stop fungal from growing) vs

fungi cidal (kill the fungi)

 Fungi static – imidazole, polyenes

 Fungicidal - allylamines
 Imidazoles
 Miconazole
 Clotrimazole

 Ketoconazole

 Polyene
 Nystatin

 Allylamines
 Terbinafine
IMMUNOMODULATORS
 Topical calcineurin inhibitor
 Tacrolimus
 Pimecrolimus

 Used to treat atopic eczema, vitiligo and

psoriasis

 Topical imiquimod
 Genital warts
COMBINATION
TOPICALS
 Steroid + anti-fungal
 Steroid + antibiotic
 Steroid + keratolytic
 Steroid + vit D analogue
 Antibiotic + keratolytic
TAKE HOME MESSAGE
 Efficacy topical steroid depend on potency,
vehicle and site location.
 Depend on type of skin lesion
 Site effect of corticosteroid
 striae, atrophy, telangiectasia, acne

 Topical antifungal : preferred for superficial

fungal infection