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PHARMACOLOGY

OF MEDICATIONS
FOR SKIN DISEASE

LECTURER : DR. NANA NOVIA JAYADI, SPKK

This teaching material is copyrighted.


No part of this work may be reproduced, including photocopied, without written permission of Universitas Pelita
Harapan
Learning Objective

 The basic therapeutic regimen for various skin


condition.
 Understand the principles therapy in
dermatology.
 Know the 2 main drugs, antihistamine and
corticosteroid, used for skin diseases.
 Recognize the management of steroid treatment.
MEDICATION FOR SKIN
DISEASE

Medication • Topical
for skin • Systemic
disease • Intralesion

• Radiotherapy
• Phototherapy
Other • Laser
modalities • Cryotherapy
• Electrosurgery
• Surgery
TOPICAL THERAPY
Active substance:
(corticosteroids,
antiobiotics, etc)

+
Vehicle:
(cream, lotion, gel,
etc)
TOPICAL THERAPY

Advantages
• Drug deliverd in high concentration in skin
• Minimal systemic side effects

Disadvantages
• Time consuming
• Messy
• Confusing
• Local side effects
Pharmakokinetics of Topical
Therapy
Drug factors Host factors
 Percutaneous  Site
penetration
 Age
 Percutaneous
 Hydration of skin
absorption
 Temperature of skin
 Vehicle
 Skin barrier (stratum
 Topical formulation
corneum)
 Quantity
 Frequency
 Drug reaction
Stratum corneum
• Barier to percutaneous
drug delivery

• Consist of of 50%
ceramides, 35% cholesterol
and 15% free fatty acids.

• 2 major component 
corneocyte & extraseluler
lipid (“brick & mortar”)

• Compound applied
topically migrate through
passive diffusion
Routes of percutaneous absorption :
 The transepidermal  interceluler & intracellular (transcellular)
 Transappendageal (via hair follicles, sweat & sebaceous glands,
pillosebaceous apparatus).

Diseases of the skin may have altered stratum corneum (increased,


decreased, or absent)  changing barrier function
Increased in:
• Traumatised skin, inflamed skin
• Denaturing st. corneum  solvents,
surfactants, alcohol
• Penetration enhancers  propylene
glycol, urea, ozones, salicylic acid
• Occlusion  increases temperature,
hydration, reduces wash off
I. Occlusion
• Enhanced drug penetration
• Via closed, airtight dressings,
greasy ointments
• Increase hydration & temperature
• Limits rub off/wash off
II. Frequency of application
• Likely has a little effect on increasing
topical drug efficacy
• One daily application is enough for most
topical steroid
• Non spesific emollient or protective
effect of creams and ointments are likely
enhanced by more frequent application
III. Quantity of application
•The fingertip unit (FTU)
is a useful guide to
estimate how much
topical drugs to use
•Represents
approximately 0.5g of 1 Fingertip unit (FTU)

cream or ointment
IV. Adherence
• Often overlooked aspect of medication efficacy

Tachyphylaxis  decrease prologed regimens. in drug response


when used over periode of time

Rebound effect  worsening of preexisting dermatoses who


have been using topical potent corticosteroid for
“Facilitates drug delivery by bringing the substance in
contact with skin”

 Inactive part of topical preparation


 To enhance the beneficial effects of the
medication
 Beneficial non-specific effect: cooling ,
protective, emollient, occlusive, or
astringent properties
Can be devided into:
•Liquid
•Powder
•Ointment
•Cream
•Gel
•Paste
•Linimen
1.Liquids

 Can be devided into:


a. Solutions  aqueous solution (e.g
aluminium acetate, Burrow’s solution
b. Tincture  hydroalcoholic solution
(alcohol concentration ± 50%)

 Effect : cleansing, drying, cooling,


astringent, vasoconstriction
2. Solutions

a. Compress (open and closed)


b. Bath
c. Full bath
3. Powder

 Absorb moisture, decrease friction, cooling, mild,


anti-inflammation & anti pruritic
 Adhere poorly to the skin  limited to cosmetic &
hygiene purposes
 Used in the intertriginous area, dry & superficial
dermatoses
 Basic material : talcum venetum
 Most contain zinc oxide (antiseptic, astringent, &
antipruritic)
4. Ointment

 Semisolid preparation, Petrolatum-based vehicle


 Used for glaborous skin
 Capable of providing occlusion, hydration, &
lubrication
 Drug potency is often increased by this vehicle
due to its ability to enhance permeability
 Devided into 5 categories: hydrocarbon bases &
absorption bases (ointment) , emulsion w/o or o/w
(cream), watersoluble bases (gel)
5. Cream
Can be used for hairy skin

A. Water in oil emulsion (W/O)


 Two phase systems  involving one or more
immiscible liquids dispersed in another (with the
assistance of 1 or more emulsifying agent.
 < 25% water, oil as as dispersion medium
 Less greasy, spread easily on the skin
 Provide protective film of oil that remains on the
skin as an emollient, while slow evaporation of
the water provides a cooling effect
B. Oil in water emulsions (O/W):
 Water may comprise up to 80% formulation
 Most commonly chosen to deliver a dermatologic
drug
 Spread very easily, water washable, less greasy,
easily removed from the skin and clothing
 Contain preservative (e.g. Paraben) to inhibit thw
growth of molds
 Contain humectant (an agent that draws moisture
into the skin)  glycerin, propylene glycol or
polyethilen glycol

 The oil phase may contain cetyl/stearyl alcohol to


impart stability and velvety smooth feel upon
application

 After application, the aqueous phase evaporates,


leaving a small hydrating layer of oil and a
concentrated deposit of the drug.
6.Gel

 Water soluble bases


 Consist polyethylene glycols (PEG)
 Water soluble, will not support the growth
of mold (no preservative)
 Will be useful if dermatologist desires a
high surface concentration and low
percutaneous absorption of the drug
 Suitable for facial and hairy areas
7. Pastes

 Incorporation of high concentration of powders into an


ointment
 “stiffer” than the original ointment
 Function: to localize the effect of a drug that may be
staining or irritating & act as an impermeable barriers
that serve as protectants or sunblock
 Less greasy, more drying, less occlusive
8. Linimen

 Mixture
of liquids, powder and
ointment
 Indication: subacute dermatoses
 Contraindication: madidans
dermatoses
 Aluminium  Selenium dissulfide
acetate
 Sulphure
 Acetic acid
 Ter
 Benzoic acid
 Urea
 Salicylic acid
 Antiseptic
 Camphora
 Topical
 Menthol corticosteroid
 Podophylin
Binding to specific receptor in celluler cytoplasm &
modulating the transcription of multiple genes 
suppresion of the production of inflammatory substance &
inhibit the recruitment of inflammatory cells

Most frequently prescribed of all dermatologic drug


products

Effects:

• anti-inflammatory
• immunosuppresive
• antiproliferative
• vasoconstriction
Principles when initiating topical steroid
therapy:

• Lowest potency to sufficiently control disease


• Prolonged use of an insufficient potency agent
should be avoided (max 2-4 weeks)
• When large surface area involved  low to
medium potency recommended
• Low potency should be used on the face and
intertriginous area
 Very potent corticosteroids, frequently under
occlusion, are usually required for hyperkeratotic
or lichenified dermatoses nad for involvement of
palms and soles

 High potency and medium potency should be


avoided in young children other than for short
term application
Local side effects:
 Skin atrophy
 Acneiform eruptions
 Hypertrichosis
 Pigmentary changes
 Development of infections
 Allergic reactions
Systemic side effects :
 Occular effects
Glaucoma, vision loss
 Suppression of the hypothalamic-pituitary-
adrenal (HPA) axis
Has been decribed with the use of potent
topiical corticosteroid  iatrogenic
Cushing syndrome, corticosteroid related
Addison crises
 Metabolic side effects
Increased glucose production and
decreased glucose use induced
hyperglycemia  diabetes mellitus
Continuing use of topical steroid:
 Highly potent formulation should be used
for short periods (2-3 weeks) or intermittently
 Once disease control is partially
achieved less potent compound should
be initiated
 Reduce frequency of application once
disease control is partially achieved
 Topical steroid shoud be avoided on
ulcerated, atrophic skin or skin with
coexistent infectious dermatoses
 Sudden discontinuation after prolonged used
should be avoided
 Special guidelines should be followed when
treating certain body area or certain populations
 Laboratory test should be considered if systemic
absorption is suspected.
Reference

1. Wolff K, Goldsmith LA, Katz SI, Gilchrest BA, Paller AS,


Leffell DJ, penyunting. Fitzpatrick’s dermatology in
general medicine. Edisi ke-8. New York: Mc Graw Hill
Inc; 2012.

2. Menaldi SLSW, Bramono K, Indriatmi W.penyunting. Ilmu


penyakit kulit dan kelamin, edisi ke-7. Jakarta: Badan
Penerbit FKUI. 2015.

3. James WD, Berger TG, Elston DM, penyunting. Andrew’s


disease of the skin clinical dermatology. Edisi ke-10.
USA: Elsevier Inc., 2006.

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