Dermatologic

Pharmacology
1. Topical
2. Intralesional
3. Systemic
Oral
Parenteral
1. Topical
Transdermal patch
Semisolid Preparation:
Ointment, cream
Gel, etc
 local application for
localized effects
 local application for
systemic absorption
and consequent
systemic effects
 direct contact with
underlying pathologic
process
no first pass metabolism
form a drug depot that
slowly release the active
ingredient of the drug
Oral
capsules, tablets
syrup, oral suspension
Parenteral
IV, IM, SC
Three Routes of Drug Penetration Through the Skin:

1. through intact stratum corneum

2. through sweat ducts
3. through the sebaceous follicle
1. Low molecular mass (600da)
2. Adequate solution in oil and water
3. High partition coefficient
1. Establishment of a
concentration gradient which
provides the driving force for
drug movement across the skin
2. Release of drug from the
vehicle (partition coefficient)
3. Drug diffusion across the layers
of the skin (diffusion coefficient)
1. Dosage
amount of drug should be sufficient to
cover affected body surface
approximately 30 g is required to cover
the whole body surface
Sufficient contact time
2. Regional Anatomic Variation
permeability is generally inversely
proportional to the thickness of stratum
corneum
drug penetration is higher on the face, in
intertriginous areas or skin sites with
opposing surfaces e.g. axilla, groin and
inframammary areas
vulnerable to drug related toxicity
3. Integrity of the skin
intact skin provides a formidable barrier for
passage of drugs
disrupted epidermal layer allows
drug to readily pass (compromised barrier
function)
e.g. inflammation
abnormal stratum corneum (i.e. psoriasis)
4. Hydration
increase in the water content of the
stratum corneum due to inhibition of
transepidermal loss of water
increases drug penetration
hydration causes swelling of the stratum
corneum making it more permeable to
drug molecules
4. Hydration
Methods of Hydration:
4.1. Occlusion with an Impermeable
film
4.2. Application of Lipophilic Occlusive
vehicles e.g. Ointments
Occlusive Dressing
5. Vehicle
solvent through which most drugs for
topical administration is incorporated
markedly influence ability of drug to
penetrate the outer layers of the skin
6. Age
drug penetration is generally greater in
infants and in elderly because they
have thinner stratum corneum
children have a greater ratio of surface
area to mass than adults, so greater
systemic absorption of topical drugs
7. Lipid Solubility of Drug
lipid soluble compounds diffuse
through lipids within the stratum
corneum
1. Dimethyl sulfoxide (DMSO)
penetrate deeply into the skin without
damaging it and carry other
compounds deeper into the biologic
system
predominantly used vehicle for topical
analgesics, anti-inflammatory and
anti-oxidant
2. Propylene glycol
vehicle for organic compounds
also an effective Humectant and
increases the water content of the
stratum corneum
Keratolytic at 40-70%
concentration
3. Urea
also possess hygroscopic
property
makes cream and lotion less
greasy
4. Liposomes
are concentric spherical shells of
phospholipids in an aqueous medium that
may enhance percutaneous absorption
penetrate compromised epidermal barriers
more efficiently
variations in size, charge and lipid content
can influence liposome function
5. Microgels
are polymers that may enhance
solubilization of certain drugs to
enhance penetration and decrease
irritant effects
1. Easy to apply and remove
2. Non-irritating, inexpensive
3. Odorless, non greasy
4. Cosmetically pleasing
5. Active drug must be stable in the vehicle
6. Active drug must be readily released once
in contact with the skin
1. Powder Talc , Starch
consist of very fine particle size which
covers a large surface area of the body
absorb moisture and reduce friction
soothing and cooling effect
adhere poorly to the skin
1. Powder Talc , Starch
Types:
1. body powders
dusting powder, talcum powder, face
powder
2. medicated powders
used for prickly heat or preventing
microbial growth on skin
2. Ointment
semisolid preparation intended for external
application to the skin or mucous
membranes
creates and oily residue o the skin ing effect
increase hydration of
stratum corneum
2. Ointment
occlusive effect prolong and enhance
drug penetration
not suitable for weeping lesions
useful in chronic, dry lesions
anhydrous nature does not require
preservatives
2. Ointment
Typical ointment bases:
1. Petrolatum
2. Polyethylene glycol
3. Lanolin
good skin penetration and
adherence to surfaces
Ointments
3. Creams
classified as water-in-oil or
oil-in-water formulations
less messy and less occlusive than
ointments
dry quickly
3. Creams
contain water so prone to bacterial or
fungal contamination
drying effect
preferred form for exudative
dermatoses and for use under wet
dressings
Creams
4. Emollient
substances in liquid form that soften and
soothe the skin
component of lipstick, lotion and other
cosmetic products
4. Emollient
essential component is lipid
Three different types of emollient
1. Oil in water emulsion cream
2. Water in oil emulsion ointment
3. Water free preparation fatty ointment
4. Emollient
provides a layer of oil on the surface of the skin to slow
water loss and thus increase the moisture content of the
stratum corneum
4. Emollient
also known as:
Moisturizer
Lubricant
Vanishing cream
4. Emollient
employed as protective and as skin
softening agent
also serve as vehicles for more
active drugs
5. Lotion
5. Lotion
usually applied to external body
surfaces e.g. skin with bare hands
used to soften and smoothen skin or
used to deliver medications to the
skin
less viscous than cream or ointment
5. Lotion
medicated lotions may contain:
Antibiotics
Antifungals
Corticosteroids
Antiseptics
Skin Whitening
Antipruritics
5. Lotion
applied thinly on external body
surface such as the skin, scalp
cover a larger body surface area
applied to the skin more frequently
without rubbing
6. Gels
sticky, jelly-like semisolids or solids
prepared from high molecular weight
polymers in an aqueous or alcoholic
base
liquefies upon contact with the skin
6. Gels
Two Kinds of Gels:

1. Alcoholic gels
hand sanitizers
best suited for acute
exudative, pruritic
eruptions
6. Gels
Two Kinds of Gels:

2. Non-alcoholic gels
hair gels, sunscreens
more lubricating best suited for dry
scaly lesions in the scalp
7. Liniment
viscous liquids containing
substances possessing analgesic,
soothing or stimulating properties
should be rubbed when applied to
the skin to release active drug
should not be applied to broken skin
7. Liniment
similar viscosity as lotion
8. Astringent
forms a protein precipitate which
serve as a protective coat allowing
new tissues to generate underneath
check oozing discharge or bleeding
in skin and mucous membrane by
coagulating protein
8. Astringent
commonly used to reduce extent of
weeping dermatitis
e.g.
Zinc oxide
Burrows solution
8. Astringent
9. Humectants
substances that diffuse into the
stratum corneum and attract water
substances that promote water
retention due to their hygroscopicity
e.g. glycerine, urea, pyrrolidone
carboxylic acid (PCA), sorbitol
10. Collodion
liquid preparations consisting of a
solution of proxylin in a mixture of
ether and alcohol
painted on the skin and allowed to
dry to leave a flexible film over the
site of application
10. Collodion
used to seal minor cuts and
wounds or as a means to hold a
dissolved drug in contact with the
skin for prolonged periods
10. Collodion
11. Paste
stiff preparations containing a high
proportion of finely powdered solids
such as Zinc oxide, calcium
carbonate or starch
forms an unbroken, relatively water
impermeable film on the skin surface
less occlusive and messy than
ointments
11. Paste
suitable for subacute or chronic
dermatoses
useful for local application of
irritating drugs
Mode of administration:
1. Local
Topical
Intralesional
2. Systemic
Oral
Intramuscular
Intravenous
Corticosteroid
Mechanism of action:
 Anti-inflammatory
inhibition of Phospholipase A2

Immunosuppression
classification of Topical Corticosteroids in
order of decreasing potency
more potent steroid is used initially
followed by a less potent agent
twice daily application is sufficient
more frequent application does not improve
response
Class 1 - Highest Potency
Clobetasol propionate 0.05%
Betamethasone dipropionate in
optimized vehicle 0.05%
Class 2 - High Potency
Fluocinonide 0.05%
Betamethasone dipropionate 0.05%
Class 1
Betamethasone dipropionate cream,
ointment 0.05% (in optimized vehicle)*
Clobetasol propionate cream, ointment
Diflorasone diacetate ointment 0.05%
Halobetasol propionate ointment 0.05%
Class 2
Amcinonide ointment 0.1%
Betamethasone dipropionate ointment 0.05%*
Desoximetasone cream, ointment 0.25%, gel
0.05%
Diflorasone diacetate ointment 0.05%
Fluocinonide cream, ointment, gel 0.05%
Halcinonide cream, ointment 0.1%
Class 3
Betamethasone dipropionate cream 0.05%*
Betamethasone valerate ointment 0.1% \
Diflorasone diacetate cream 0.05%
Fluticasone proprionate 0.005%
Mometasone furoate 0.1%
Triamcinolone acetonide ointment 0.1%,
cream 0.5%
Class 4
Amcinonide cream 0.1%
Desoximetasone cream 0.05%
Fluocinolone acetonide cream 0.2%*
Fluocinolone acetonide ointment 0.025%*
Flurandrenolide ointment 0.05%, tape 4 mg/cm2
Hydrocortisone valerate ointment 0.2%
Triamcinolone acetonide ointment 0.1%
Mometasone furoate cream, ointment 0.1%
Class 5
Betamethasone dipropionate lotion 0.05%*
Betamethasone valerate cream, lotion 0.1%
Fluocinolone acetonide cream 0.025%
Flurandrenolide cream 0.05%
Hydrocortisone butyrate cream 0.1%
Hydrocortisone valerate cream 0.2%
Triamcinolone acetonide cream, lotion 0.1%*
Triamcinolone acetonide cream 0.025%
Class 6
Aclometasone dipropionate cream, ointment
0.05%
Desonide cream 0.05%
Fluocinolone acetonide cream, solution
0.01%*
Class 7
Dexamethasone sodium phosphate cream
0.1%
Hydrocortisone cream, ointment, lotion
0.5%, 1.0%, 2.5%*
Methylprednisolone aceponate cream,
ointment 1 mg/g
Prednisolone cream 5 mg/g
1. Type of skin lesions
2. Location of the skin lesions
3. Severity of skin lesions
4. Age of the patient
5. Duration of treatment
If its dry, wet it.

If its wet, dry it.

 Low-Med Potency High Potency
Type of lesion Thin, acute Chronic,
hyperkeratotic,
lichenified, endurated
Site areas with thin recalcitrant lesion in
stratum corneum face and
intertrigneous areas
Palms and soles
Extent or size of Large areas Smaller areas
lesion
Age of patient Young and elderly Adults
Duration of treatment longer not > 3 weeks;
longer for recalcitrant
lesions
Ointment
is the most effective preparation for
treating thick, fissured, lichenified skin
lesions
choice for dry dermatoses
the occlusive nature enhances
corticosteroid penetration
Creams
preferred for acute and subacute
dermatoses
used in moist skin and in intertriginous
areas
preferred for weeping or wet lesions
Lotions
preferred for lesions:
in hairy areas
involving large body surface areas
 face and intertriginous areas (axilla, groin,
perineum, and inframammary area) has
thin stratum corneum
susceptible to local and systemic adverse
effects
recalcitrant lesions of the face or
intertriginous areas may require more
potent corticosteroids or a longer duration
of treatment
 use the lowest potency corticosteroid
that is effective, especially in infants and
children
use of topical corticosteroids under
plastic wrap, tight-fitting clothing, or
under diapers may increase absorption
several fold
apply very thinly
Use in pregnancy
Topical corticosteroids may cause fetal
abnormalities in animals if used in large
amounts, with occlusive dressing, for prolonged
periods of time, or if the more potent agents are
used
but fetal abnormalities have not been
documented in human beings.
 used for severe dermatologic conditions
such as:
allergic contact dermatitis to plants
e.g. poison ivy
life-threatening vesicolobullous dermatoses
e.g. pemphigus vulgaris
bullous pemphigoid
 usually given in the morning to coincide
with circadian rhythm of endogenous
steroid secretion
chronic administration predispose to greater
side effects
with chronic therapy, need to taper dose
gradually before stopping treatment
Impaired wound
healing
Bruising
Skin
thinning
Striae