TOPICALLY APPLIED

CORTICOSTEROIDS
 Topical Preparations: Products which are
designed for application to the skin -
either by
simply spreading them over the skin or by
rubbing them in.
 Dermatological preparations: are

employed for the treatment of diseased

or injured skin. Diseased, injured or
inflamed skin proves more permeable
than intact skin.
 Percutaneous topical
preparations: are intended for
use on intact skin and they
produce their effects either
locally or systemically.
Topically used
corticosteroids
 The most potent and effective anti-
inflammatory medications available
 They are the therapy of choice in most
inflammatory diseases, pruritic
eruptions (dermatitis),
hyperproliferative disorders (psoriasis),
infiltrative disorders (sarcoidosis)
 Effectiveness of the drugs is due to their
anti-inflammatory activity. (Explain the
mechanism of action?)
 They have the ability to inhibit
cell division
 In dermatologic diseases
characterized by increased cell
turnover e.g. psoriasis, the anti
mitotic effect of steroids is
important factor
Anti-inflammatory action of
corticosteroids

PHARMACOLOGY FOR HEALTHCARE PROFESSIONALS

Analogues of topical steroids and their
efficacy

 Hydrocortisone (HC) is the

prototype. (Active or not?)
 Prednisolone &

Methylprednisolone are active as

HC
 9-α-flourinated compounds like

dexamethasone &
Betamethasone (As
hydrocortisone)
 Attaching 5-carbon valerate to
the 17 hydroxy position to
betamethasone  300 times
active as hydrocortisone
 Acetonide derivatives of

fluorinated steroids  potent

topical drugs
 21-derivatives of acetonide  5-

fold increase
 Intrinsic activity of topical
corticosteroids is dependent on
chemical modification of the
molecule like F at C9, carbon
valerate chain at C17
 Betamethasone + 5- carbon
valerate chain at 17 position  > 300
times as active as hydrocortisone
Advantages of topical
corticosteroids

 Wide spectrum against skin

diseases
 Rapid action in small amounts

 Ease of use (topical application)

 Absence of pain or odor

 Relative lack of sensitization

 Prolonged stability
 Compatibility with almost all

commonly used topical

medications
 Rare systemic untoward

systemic side effects

Factors affecting the effectiveness of
topical corticosteroids

 . Drug potency
1. Active form (e.g. prednisone &
prednisolone), Binding to a
glucocorticoid receptor
2. Addition of halogen atom (e.g.
fluoride)
3. Vehicle (Oint., cream, lotion, etc)
4. Added drug (salicylic acid, urea)
 2. Percutaneous penetratio
Percutaneous Drug
Absorption
All topical preparations must make their
way into the skin before they can exert
effects.
 Percutaneous absorption
involves:
 Dissolution of the drug in its vehicle,
 Diffusion of the drug from the vehicle

to the surface of the skin, and

 The actual penetration of the drug

through the different layers of the

skin.
 Percutaneous absorption may be
effected by the following routes:
 Transcellular diffusion
 Diffusion through channels between

the epidermal cells

 Diffusion through sebaceous ducts
 Diffusion through the hair follicles
 Diffusion through the sweat ducts
Factors affecting trans-dermal
absorption of corticosteroids

 Site of steroid application. (See the next

diagram)
 Hydration
 Long term occlusion of impermeable film.
(▲100 times)
 Inflamed skin. (Health status of skin)
 Dosage form: ointment > cream and lotion.
 Increasing the concentration of applied
cortisone.
 Lipophilicity of the corticosteroids
 Solubility of cortisone in the
vehicle.
1. Intra lesional injection.
 In diseases that are very responsive

 apply low to minimum efficacy

corticosteroids.
 In less responsive diseases  apply

high efficacy preparations +

occlusion or both, when remission
occurs shift to low efficacy
 Absorption of steroids is dependent
on the site of their application (the
times = the concentration of
absorbed steroid relative to the
percentage of concentration of the
absorbed hydrocortisone). Skin is
thinnest on the eyelids at 0.05 mm
and the thickest on the palms and
soles at 1.5 mm.
Classification of topical steroids
according to their potency

Hydrocortisone 1% < Betamethasone valerate 0.1%

< Clobetasole propionate 0.05%
 Lowest efficacy corticosteroids: Mild
 Who: infant, child, adult
 Areas: Face, folds , genitals, extensive
areas of the skin
 Examples
 Hydrocortisone (0.25 - 2.5 %).
 Dexamethasone (0.1%, 0.04%).

Low efficacy corticosteroids: (Mild
to moderate)
Who: infant, child, adult

2-25 times as
Potency:
hydrocortisone
Sites:Face, folds, genitals,
Examples:
Betamethasone valerate (0.01%)
Triamcinolone acetonide (0.025%)
 . Intermediate efficacy corticosteroids:
Moderately potent
 Potency: Up to 100 times as hydrocortisone
 Who: Adult & Child & Extensive area of the
skin
 Examples:
 Hydrocortisone valerate (0.2%)

(Betnovate)
 Betamethasone valerate (0.1 %).

 Triamcinolone acetonide (0.1 %).

(Kenacort)
 High efficacy corticosteroids: Potent
Who: Adults
Potency: Up to 150 times as
hydrocortisone
Areas: Localized thick lesions
Examples:
 Betamethasone dipropionate

(0.05%) (diprolone)
 Triamcinolone acetonide (0.5%).

 Flucinolone acetonide (0.2%).

 . Highest efficacy corticosteroids:
(Very Potent)
Who: Adult
Potency: Up to 600 times
hydrocortisone
Areas: Resistant & Localized
thick lesions (palm)
Examples:
 Clobetasole propionate 0.05%

(Dermovate)
1. Begin with high efficacy compound
then maintain on that with less
efficacy
2. Use the less potent corticosteroids
e.g. 1% hydrocortisone on scrotum,
groin, axillae, eyelids, face.
Which preparation? cream or
ointment, lotion or gel

 As with moisturizers, the type of steroid

formulation most suitable depends on the
characteristics of disease and the area of
skin affected.
 Lotions and gels are most suitable for

hairy areas of skin.

 Creams are better for moist, weeping

areas of skin, while

 Ointments are most suitable for drier,

scaly areas
Dermatological disorders responsive
to topical corticosteroids

 . Highly responsive disorders:

 1- Atopic dermatitis.
 2- Seborrheic dermatitis.

 3- Lichen simplex chronicus.

 4- Pruritus ani.

 5- Later phase of allergic contact &

irritant dermatitis.
 6- Stasis dermatitis.

 7- Psoriasis (genitalia and face).

Dermatological disorders responsive
to topical corticosteroids

. Less responsive disorders:

1. Discoid lupus erythematosus
2. Psoriasis of palms and soles
3. Necrobiosis lipoidica diabeticorum
4. Sarcoidosis
5. Lichen striatus
6. Vitiligo
7. Granuloma annulare
Least responsive disorders: (Intra lesion
injection required):
1. Kelosis
2. Hypertrophic scars
3. Hypertrophic lichen planus
4. Alopecia areata
5. Acne cysts
6. Prurigo nodularis
Corticosteroids
 Action
 Corticoid depresses formation,

release and activity of endogenous

mediators of inflammation,
including
PGs,
kinins,
histamine,
liposomal enzymes and
complement system. Also
Corticosteroids
 Leads to:
 Inhibit. lymphoid proliferation
 Lyses of either suppressor or helper

T cells
 Monocyte- macrophage system

inhibit chemotaxis
 Inhibit. of IL6 & IL1, IL2, TNF, PAF,

leukotriens, PGS.
 Inhibits the antibody response
 Decrease amount of antibody
Topical steroids: Adverse
effects
.Systemic: Extremely rare e.g. if TS >50
gm clobetasol propionate or 500 gm of
hydrocortisone/week
 Potential suppression of pituitary-

adrenal axis  Occlusion, surface area,

amount, duration, concentration, Type
(Clobetasol), Infants, children, liver
failure
 Growth retardation in children.

 Iatrogenic Cushing's syndrome.

 When: Too long, too much, too often, too
old, too young, too extensive, face, folds,
genitalia.
 What are the adverse effects of steroid ê
occlusion?
Infection, folliculitis, miliaria,▼ heat
change, ▲sunburn, atrophy, striae
Occlusive dressings (airtight dressings) 
absorption of the steroid and may 
also the chances of side effects
 . Local: Rare if TS used correctly

1. Skin atrophy, striae (stretch marks),

telangiectases,
2. Easy bruising and tearing of skin
(purpura, ecchymosis).
3. Pustules & Papules.
4. Peri-oral dermatitis (rash around
mouth)
Insusceptibility to skin infection, Mask
superficial infections, worsen fungal infections.
1. Tachyphylaxis

2. Hypo-pigmentation.

3. Hyper-trichosis. (Excessive abnormal hair

growth)
4. Glaucoma & cataract. (when used around the

eye)
5. Allergic contact dermatitis. (leg ulcers,

stasis )
1.
Questions for revision:
2. What are the precautions of using topical
corticosteroids in children and infants?
3. On which basis you choose the dosage form of
corticosteroids? e.g. occlusion
4. How frequent you apply the topical corticosteroids
per day. Why?
5. What is your opinion about using topical steroids in
pregnancy and lactation?
Contraindications to topical
corticosteroids

1.Untreated skin infections (bacterial,

fungal, or viral)
2. Acne rosacea

3. Peri-oral dermatitis

4. Potent corticosteroids are contra-

indicated in widespread plaque
psoriasis.
How can you minimize the side
effects of topical steroids?

 Potency: use the least potent steroid

whenever possible
 Frequency: ≱ Once or Twice daily

 Amount: use steroid sparingly by using

FTU. How? (1, 2, 3, 6, 7 FTU)

 Duration, not for prolonged periods –

change to less potent with recovery

 Surface area: Broad area—least potent,

and least amount, reduce frequency

 Areas of skin: take care of areas that
absorb more (like face and genitalia)
 Occlusion: Precautions with occlusion

 Once the lesion responded, reduce or

stop the steroid & maintain on a mild

one
 Never use the steroid as moisturizers
 Getting the dose right - the fingertip
unit
 One fingertip unit (FTU) is the amount

of topical steroid that is squeezed out

from a standard tube along an adult's
fingertip. (This assumes the tube has
a standard 5 mm nozzle) A finger tip
is from the very end of the finger to
the first crease in the finger.
Intralesional
corticosteroids
Definition:
Injection of small amounts of
corticosteroids into coetaneous
lesions (Relatively insoluble
steroids)
Examples:
Triamcinolone acetonide,
triamcinolone diacetate,
betamethasone acetatephosphate)
Advantages:
1. High concentration

2. Prolonged depot (3-4 weeks)

3. No systemic side effects

Treated diseases: Acne cysts,

Alopecia areata, keloids, nail
disorders, Prurigo nodularis
Methods: Insulin syringe (1ml/30 G),
Air powered gun ( pyogenic
Infection & Viral hepatitis). Dose
1mg/injection site of triamcinolone
(Conc. 10mg/ml- Dose Vol. 0.1ml)
Adverse efects:
1. No systemic. Why?

2. Local: Atrophy, hypo-pigmentation,

hair growth, infection, ulceration.
THE END