DERMATOLOGY

PHARMACOLOGY
1. INTRODUCTION
Skin functions:
• Protection
• Thermoregulation
• Immune responsiveness
• Biochemical synthesis
• Sensory detection
• Social and sexual communication
2. Role of the skin in pharmacokinetics
• Drug absorption
- nature of drug ] control rate of
- behaviour of vehicle] drug
- status of skin ] absorption
• Barriers
- stratum corneum
- membrane of epidermal cells
- basement membrane at dermal-
epidermic junction
• Drug once in dermis  circulation
• Metabolism
- 1% metabolizing activity
• Excretion
- by sweat glands
3. Vehicles
• Ointments – semisolid fatty preparations
• Creams – emulsion of oil in water or H2O
in oil
• Pastes – thick, semi-occlusive ointment
• Powders – adsorbent
• Gels- semi-solid colloidal solutions or
suspension
Uses:
• Lotions – main component is water
• Direct application
• Lotions, linctures for
- acute inflammation with oozing
- vesiculation
- crusting
• Creams, ointment for
- chronic inflammation with scaling
- lichenification
• Tinctures, lotions, gels, aerosols for
- scalp and hairy areas
• Dusting powders – folds of skin
4. Drugs
(a) Emollients
- soften, soothe, lubricate and protect skin
surface
- are fats, oils or waxes into which active
medicinal agents are incorporated
examples, olive oil, cocoa butter, lanolin, rose
water ointment, glycerine
(b) Astringents
- precipate proteins forming a protection scab
under which healing takes place
Examples: Calamine, ZNO, tannic acid
(c) Protectives
(i) powder
- insoluble, chemically inert
- finely ground substances
- prevent friction and contact with irritation
- examples: ZnO, starch, Mg silicate
(ii) Mechanical
- provide occlusive protection from
external environment
- e.g Zn gelatin
(d) Keratolytics
- soften keratin
- cause disquamation of superficial
layers of epithelium
- examples: Benzoic acid, salicylic acid
propylene glycol
(e) Caustics
- stronger irritation, act on protoplasm
- destroy living tissue like warts, corns
- examples: caustic potash, caustic
soda, salicylic acid (10-50%)
(f) Irritation/counter – irritants
(i) Irritants – cause hyperemia, inflammation e.g
canthridins
(ii) Counter-irritants – cause local tissue reaction by
injuring protoplasm e.g iodine
(g) Retinoids
- act via intracellular receptors (RAR, RXR)
1st generation:
Retinol
* Tretinoin
* Isotretinoin
2nd generation
• Etretinate
• Acitrein
3rd generation
• Arotinoid
Actions:
- Stabilize lysosomes, RNA polymerase
activity, PGE2 concentrations
- Regulate cellular proliferation
- Modulate immune function
Clinical uses:
• Tretinoin – treat acne, photoaged skin
• Isotretinoin – treat severe acne
• Etretinate – treat psoriasis
Adverse effects:
Teraogenecity, dry skin, epidermal fragility,
visual disturbances, hair thining, myalgia,
arthralgia raised liver enzymes, allergic
vsaculitis, acne fulminans
(h) Antiinflammatory drugs
Topical glucocorticoids
Examples:
- Hydrocortisone 0.1% - mild potency
- Betamethasone valerate – moderate
- Beclomethasone – potent
- Clobetasol proplanate – very potent
Clinical uses: eczema, vitiligo, alopecia
areata, keloids, dermatosus periphigus
Adverse effects: atrophy, pustules, papules,
steroid rosacea (chronic vascular &folicular dilation), perioral
dermatitis, steroid acne, glaucoma,
hypopigmentation, hypertrichosis

• Systematic glucocorticoids
- Short term therapy – contact dermatitis,
atopic dermatitis
- Long term therapy – collagen vascular
disease
ANTIMICROBIAL DRUGS
Antibiotics  Bacitracin, Gramidin - Gram +ve
microorganism
*Topical  Polymixine B - Pseudomonas,
 Neomycin, E.coli
Gentamycin E.coli, Proteus, Klebsiella
 Systemic  Tetracyclines - P. acnes
 erythromycin
* Antifungals
 Topical  Azoles e.g Clotrimazole - Dermatophytes,
Preps Econazole, Miconazole yeast, C.albicans
 Allylamines e.g Naftifine - Dermatophytes
Terbinafine
 Polyene antibiotics - C.albicans
e.g Nystatin
Oral preps  Griseofulvin - Dermatophytes (nails,
scalp, ringworms
 Azoles e.g - Dermatophytes
Itraconazole,
Fluconazole,
Ketoconazole - Dermatophytes
* Antivirals Acyclovir, valacyclovir - Herpes viral infection
(herpes simplex, herpes genitalis)
* Ectoparasiticides Lindane - pediculosis capitis or
pubis
Crotamiton - scabies
Permethrin - Mange, P.humans
Benzyl benzoate - scabies, pedicutosis
Treatment of acne
• Keratolytic agents e.g salicycliacid, benzyl
peroxide – 1st line of therapy
• Topical antibacterial drugs
- Clindamycin  P.acnes
- Erythromcin  P.acnes
- Tetracyclines (topicycline, meclocycline)
- metronidazole  acne rosacea
• Systemic antibiotics
- Tetracycline  indicated in children over
12 years
 - Erythromycin  children below 12 years
NB: Antibiotic resistance to Propionibacterium
acne is high
• Retinoids e.g Tretinoin , Isotretinoin effective
against acne vulgaris
J. Drugs affecting pigmentation
• Hydroquinone
- produces reversible depigmentation of skin
- inhibits melanocyte metabolic process
- uses: Rx. Freckles,
K. Sunscreens
- reduce the amount of UV radiation reaching
the skin or block it altogether
(i) Physical sunscreens (reflectant)
- e.g ZnO, calamine, titannic dioxide
- barrier to UVA, UVB
- are opaque
(ii) Absorbent sunscreens (chemical)
- UVA protection – Benzophenones,
Dibenzopheniones
- UVB protection – aminobenzoic acid,
aminobenzoates, cinnamates, salicylates,
camphos
M. Antipruritic agents
• Antihistamine (H1) e.g hydroxyzine,
chlorpromazine, trimeprazine – for
generalized pruritus
• Topical hydrocortisone, calamine,
astringents tannic acid for localized pruritus
• Doxepin HCL 5% cream to treat pruritus
asociated with atopic dermatitis or lichen
simplex chronicus
• Pramoxine HCL cream – useful in mild
eczematous dermatitis
N. Trichogenic agents
• Minoxidal
- stimulates hair growth
- used in treating androgenic alopecia
- side effects: allergic contact dermatitis,
irritation
• Finasteride (5 – reductase inhibitor)
- promotes hair growth
- Rx. Androgenic alopecia
-  libido, erectile dysfunction
O. Miscellaneous drugs
* Antiseborrhea agents
- Chloroxine shampoo
- Ketocanozole shampoo
- Coal tar shampoo
- SeleNium sulfide shampoo
* Dapsone, antimetabolites
* Antimalarials, cyclosporine
Dermal adverse drug reactions
Drug skin reaction
Aspirin & other salicylates Urticaria
Furosemide purpuric rash
Glutethimide generalized erythema
Gold salts generalized exfoliative
erythroderma
Penicillin Severe erythema
Neomycin, creams/cosmetics contact dermatitis
Coal for preps, psoralens ] photosensitivity
Demeclocycline ] reactions
Doxycyline ]
Topical corticosteroids ] irritant or allergic
Topical antihisamines ] contact dermatitis
Topical antimicrobials ]
Corticosteroids, androgens Acne
DRUGS AND CONNECTIVE TISSUE
DISORDERS

Immunosuppressive agents
• Introduction
• Inhibition of immune response
- nonspecific inhibition: inhibit by their
cytotoxic action e.g azathioprine,
cyclophosphamide, methotrexate
- specific inhibition – inhibit activation or
actions of specific cells e.g glucocorticoids,
cyclosporine, tacrolimus
Uses: to treat disease that reflect
imbalances in immune system e.g
- systemic lupus erythematosis (SLE)
- Systemic sclerosis (scleroderma)
- Polyarteritis nodosa
- Temporal arteritis
- Polymyositis, dermatomyositis
- Rheumatoid arthritis
- Inflammatory bowel disease
Drugs Therapeutic Adverse Effects
• Glucocorticoids RA, SLE Osteoporosis
- antiinflammatory polymyositis cataracts
& immunologic dermatomyositis ulcers
effects vasculitis cushing syndrome
Transplantation

• Cyclophos- SLE, vasculitis myelosuppression

phamide alopecia,
- alkylating agent hemorrhagic
Cytotoxic cystitis, gonadal
failure
Drugs Therapeutic Adverse Effects
• Methotrexate RA, SLE myelosuppression
- antimetabolite polymyositispneumonitis
- Folic acid dermatomyositis hepatotoxicity
antagonist
- Cytotoxic
• Azathioprine SLE, RA Myelosuppression
cytotoxic polymyositisGIT symptoms
transplantation hepatotoxicity
Clycosporine RA, SLE Renal toxicity
- selective immune transplantation  BP
Suppressant psoariasis hepatotoxicity
uveitis
Drugs Therapeutic Adverse Effects
• Gold salts RA dermatitis, GIT
- antiinflammatory disturbances
effects, proteinuria
• Penicillamine RA Dermatitis, GIT
Chelating agent sclerodema symptoms,
protenuria
NSAIDS Inflammation GIT, kidney, CNS
- antiinflammatory hemopoietic
Effects, analgesic adverse effects
antipyretic
Systematic lupus erythematosus (SLE)
NB: Use antiinflammatory and
immunosuppressive drugs
Mild SLE:
NSAIDS: Glucocorticoids (low dose);
antimalarials; methotrexate
Severe SLE: Glucocorticoids (high dose);
Azathioprine; cyclophosphamide
Investigational: Cyclosporine; immune
globulin