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pa S4 Lec 2: Dermatologic Pharmacology by Leonardo A. Torres, FPSECP,
January 26, 2011
Je FPSP, FPSA, RBA-ABI
ANTIBACTERIAL AGENTS
s
vi
DERMATOLOGIC VEHICLES
a
• Topical medications usually consist of active I. Topical Antibacterial Preparations
M ingredients incorporated in a vehicle that
vs facilitates cutaneous application • Topical antibacterial agents may be useful in:
Re 1) Preventing infections in clean wounds
ai Important considerations in vehicle selection: 2) Early treatment of infected dermatoses and
M 1) Solubility of the active agent in the vehicle wounds
n 2) Rate of release of the agent from the vehicle 3) Reducing colonization of the nares by
3) Ability of the vehicle to hydrate the stratum staphylococci
corneum, thus enhancing penetration 4) Axillary deodorization
Re
F. 4) Stability of the therapeutic agent in the vehicle 5) Management of acne vulgaris
co 5) Interactions, chemical and physical, of the
Ri vehicle, stratum corneum, and active agent • The efficacy of antibiotics in these topical
F. applications is not uniform
ul • Dermatologic formulations may be classified as • Some contain corticosteroids in addition to
Pa tinctures, wet dressings, lotions, gels, aerosols, antibiotics
vs powders, pastes, creams, foams, and ointments • In the treatment of secondarily infected dermatoses,
which are usually colonized with streptococci,
• Ability of the vehicle to retard evaporation from staphylococci, or both, combination therapy may
Vi
ne the surface of the skin: tinctures and wet prove superior to corticosteroid therapy alone
le dressings <<< ointments • Antibiotic-corticosteroid combinations may be useful
Ar in treating diaper dermatitis, otitis externa, and
a • acute inflammation with oozing, impetiginized eczema
ň vesiculation, and crusting • The pathogens isolated from most infected
Ni - best treated with drying preparations such as dermatoses are group A β-hemolytic streptococci,
g tinctures, wet dressings, and lotions Staphylococcus aureus, or both
• The pathogens present in surgical wounds will be
• chronic inflammation with xerosis, scaling,
an
those resident in the environment
ad and lichenification
D - best treated with more lubricating preparations
er such as creams and ointments
h
ac • scalp and hairy areas A. BACITRACIN
e - tinctures, lotions, gels, foams, and aerosols peptide antibiotic

•
T
• intertriginous areas active against:
- gram-positive organisms such as streptococci,
ar
- emulsified vanishing-type creams
be pneumococci, and staphylococci
co - most anaerobic cocci, neisseriae, tetanus bacilli,
Ri and diphtheria bacilli
ie • compounded in an ointment base alone or in
ck combination with neomycin, polymyxin B, or
Ni both
ad • use in the anterior nares may temporarily
Gl decrease colonization by pathogenic
Je staphylococci
nz • microbial resistance may develop following
prolonged use
Ay
h ADR:
at • bacitracin-induced contact urticaria syndrome,
K including anaphylaxis, occurs rarely
o • allergic contact dermatitis (frequent) and
Jh immunologic contact urticaria (rare)
h • poorly absorbed through the skin, so systemic
a toxicity is rare

B. GRAMICIDIN
n
e
Gi
o Page 1 of 15
Ed
e
ll
ce
k
ar
M
el peptide antibiotic F. NEOMYCIN
h aminoglycoside antibiotic
ac • active against: water-soluble and are excreted primarily in the
R - gram-positive organisms such as streptococci, urine
” pneumococci, and staphylococci
“G - most anaerobic cocci, neisseriae, tetanus bacilli, Clinical Use:
and diphtheria bacilli • active against gram-negative organisms,
including E coli, proteus, klebsiella, and
n
• available only for topical use, in combination
h
with other antibiotics such as neomycin, enterobacter
Jo
polymyxin, bacitracin, and nystatin • available in numerous topical formulations,
n both alone and in combination with polymyxin,
Ia ADR: bacitracin, and other antibiotics
a • systemic toxicity limits this drug to topical use • also available as a sterile powder for topical
n use
Ni C. MUPIROCIN
ADR:
• most gram-positive aerobic bacteria, including • renal failure may permit accumulation, with
methicillin-resistant S aureus (MRSA), are possible nephrotoxicity, neurotoxicity, and
sensitive to mupirocin ototoxicity
• frequently causes sensitization, particularly if
• effective in the treatment of impetigo
applied to eczematous dermatoses or if
contagiosa caused by S aureus and group A β-
compounded in an ointment vehicle
hemolytic streptococci
• when sensitization occurs, cross-sensitivity to
streptomycin, kanamycin, paromomycin, and
ADR:
gentamicin is possible
• intranasal mupirocin in Bactroban Nasal
ointment for eliminating nasal carriage of S G. GENTAMICIN
aureus may be associated with irritation of aminoglycoside antibiotic
mucous membranes caused by the water-soluble and are excreted primarily in the
polyethylene glycol vehicle urine

D. RETAPAMULIN Clinical Use:

• effective in the treatment of uncomplicated

• active against gram-negative organisms,
including E coli, proteus, klebsiella, and
superficial skin infection caused by group A β-
enterobacter
hemolytic streptococci and S aureus, excluding
• available as an ointment or cream
MRSA
• generally shows greater activity against P
• topical retapamulin 1% ointment is indicated aeruginosa than neomycin
for use in adult and pediatric patients, 9
• more active against staphylococci and group A
months or older, for the treatment of impetigo
β-hemolytic streptococci
• recommended treatment regimen is twice-daily
application for 5 days • widespread topical use of gentamicin,
especially in a hospital environment, should be
ADR: avoided to slow the appearance of gentamicin-
resistant organisms.
• well tolerated with only occasional local
irritation of the treatment site
ADR:
• renal failure may permit accumulation, with
E. POLYMYXIN B SULFATE possible nephrotoxicity, neurotoxicity, and
peptide antibiotic ototoxicity

II. TOPICAL ANTIBIOTICS IN ACNE

• effective against gram-negative organisms,
including Pseudomonas aeruginosa,
Escherichia coli, enterobacter, and klebsiella
• most strains of proteus and serratia are
resistant, as are all gram-positive organisms
ADR:
• total daily dose should not exceed 200 mg in
order to reduce the likelihood of neurotoxicity
and nephrotoxicity
• hypersensitivity (uncommon)
• Several systemic antibiotics that have traditionally
been used in the treatment of acne vulgaris have
been shown to be effective when applied topically
• Currently, four antibiotics are so utilized: clindamycin
phosphate, erythromycin base, metronidazole, and
sulfacetamide
• The effectiveness of topical therapy is less than that
achieved by systemic administration of the same
antibiotic

Page 2 of 15
• Therefore, topical therapy is generally suitable only • topical use during pregnancy and by nursing
in mild to moderate cases of inflammatory acne mothers and children is not recommended
(teratogenic)
A. Clindamycin (1%)
• against Propionibacterium acnes E. MINOCYCLINE (ORAL)
• the water-based gel and lotion formulations are
well tolerated and less likely to cause irritation • systemic therapy for those with more extensive
• also available in fixed-combination topical gels disease and acne that is resistant to topical
with benzoyl peroxide (BenzaClin, Duac), and therapy
with tretinoin (Ziana) • Side effects: dizziness and
hyperpigmentation of the skin and mucosa,
ADR: serum-sickness-like reactions, and drug-
• rare cases of bloody diarrhea and induced lupus erythematosus.
pseudomembranous colitis
• vaginal candidiasis is a common
• the hydroalcoholic vehicle and foam
complication
formulation (Evoclin) may cause drying and
irritation of the skin, with complaints of burning
and stinging
D. Sodium Sulfacetamide
• allergic contact dermatitis (uncommon)
MOA:
B. Erythromycin (3%)
• inhibition of P. acnes by competitive inhibition
In topical preparations, erythromycin base
of p-aminobenzoic acid utilization
rather than a salt is used to facilitate penetration
Clinical Use:
MOA: inhibitory effects on P. acnes
• topical sulfacetamide is available alone as a
10% lotion (Klaron) and as a 10% wash
• development of antibiotic-resistant strains of
(Ovace), and in several preparations in
organisms, including staphylococci is a possible
combination with sulfur for the treatment of
complication of topical therapy
acnevulgaris and acne rosacea
• topical water-based gel is less drying and may
be better tolerated CI:
• also available in a fixed combination • in patients having a known hypersensitivity to
preparation with benzoyl peroxide sulfonamides
(Benzamycin) for topical treatment of acne
vulgaris OTHER ACNE PREPARATIONS
ADR:
• local burning sensation at the time of A. RETINOIC ACID ( a.k.a RETINOIN ) &
application and drying and irritation of the skin DERIVATIVES (0.05% Cream)
• allergic hypersensitivity (uncommon)
Acid form of Vitamin A
C. Metronidazole Treatment of acne vulgaris
MOA:
MOA:
• inhibitory effects of metronidazole on Demodex • Stabilizes lysosomes, increases ribonucleic acid
brevis polymerase activity, increases prostaglandin E2,
• alternately, the drug may act as an anti- cAMP, and cGMP levels, and increases the
inflammatory agent by direct effect on incorporation of thymidine into DNA.
neutrophil cellular function • Its action in acne decreased cohesion
between epidermal cells and increased epidermal
Clinical Use: cell turnover.
• topical metronidazole is effective in the
treatment of rosacea ADR: erythema and dryness

ADR:
• adverse local effects of the water-based gel B. ADAPALENE
formulation (MetroGel) include dryness,
burning, and stinging • derivative of naphthoic acid that resembles
• caution should be exercised when applying retinoic acid in structure and effects
metronidazole near the eyes to avoid excessive • most effective in patients with mild to moderate
tearing acne vulgaris.
CI:

Page 3 of 15
 C. TAZAROTENE o dermatophytosis and candidiasis
(cream)
• acetylenic retinoid o seborrheic dermatitis (shampoo)
• Clinical Use: treatment of mild to moderately severe • Topical antifungal-corticosteroid fixed
facial acne combinations
o Clotrimazole-betamethasone
D. ISOTRETINOIN dipropionate (cream)

• synthetic retinoid currently restricted to the oral ADR

treatment of severe cystic acne that is • stinging, pruritus, erythema, local irritation,
recalcitrant to standard therapies local contact dermatitis(uncommon)
• used for Cystic acne
B. Ciclopirox Olamine (cream, lotion)
ADR: • synthetic broad-spectrum antimycotic agent
 dryness and itching of the skin and mucous
membranes. • dermatophytes, candida species, and P.
 headache, orbiculare
 corneal opacities,
• mild to moderate onychomycosis (fingernails,
 pseudotumor cerebri,
toenails)
 IBD
 Anorexia, alopecia, muscle and joint pains
 Teratogenic
MOA
E. BENZOYL PEROXIDE (2.5-5% Cream)
• inhibit the uptake of precursors of
• antimicrobial activity against P acnes and its macromolecular synthesis (cell membrane)
peeling and comedolytic effects
C. Allylamines:
• Treatment of acne vulgaris. Safe to use in Pregnancy.
1. Naftifine hydrochloride (1% cream or gel)
ADR: Contact Sensitization
• allylamine
F. AZELAIC ACID (15-20% cream/gel)
• dermatophytes and yeast(less active)
• antimicrobial activity against P acnes as well as
in vitro inhibitory effects on the conversion of
testosterone to dihydrotestosterone.
• treatment of acnevulgaris (in the form of MOA
Azelex) and acne rosacea (Finacea). Best
Treatment for Males • inhibition of squalene epoxidase (ergosterol
synthesis)
ANTIFUNGAL AGENTS
I. Topical Antifungal Preparations
ADR
A. Topical Azole Derivatives: Imidazoles
• local irritation, burning sensation, and
Include clotrimazole, econazole, ketoconazole, erythema
miconazole, oxiconazole, and sulconazole
• mucous membrane contact should be avoided
Clinical Use:
• against dermatophytes (epidermophyton, 2. Terbinafine (1% cream and lotion)
microsporum, and trichophyton) and yeast
• Candida albicans and Pityrosporum • allylamine (activity similar to naftifine)
orbiculare(tinea versicolor)
• Miconazole (cream, lotion); Clotrimazole • dermatophyte infections
(cream, lotion, vaginal cream, tablets)
o in vulvovaginal candidiasis • Onychomycosis
• Econazole (cream); Oxiconazole (cream,
lotion); Sulconazole (cream, solution) • For fingernail (6wks) and toenail (12wks)
• Ketoconazole infections

Page 4 of 15
 • mild nausea, diarrhea, and occasional vomiting
(oral)
ADR
• allergic contact hypersensitivity, which is
• erythema, dryness, and stinging uncommon (topical)

• eyes and mucous membrane contact should be

avoided
2. Amphotericin B
• serious hepatic toxicity, liver failure, death
• systemic mycoses

• cutaneous candida infections (lesser extent)

D. Butenafine (1% cream, solution, powder, powder
aerosol)

• benzylamine (structurally related to ADR: a temporary yellow staining of the skin (cream)
allylamines)
II. Oral Antifungal Agents
MOA
A. Griseofulvin
• inhibition of squalene epoxidase (ergosterol
synthesis) • dermatophyte infections

E. Tolnaftate (synthetic) • infections of the scalp (4-6 wks), glabrous

(nonhairy) skin (3-4 wks), fingernails (6
• effective topically against dermatophyte months), toe nails (8-18 months)
infections caused by epidermophyton,
microsporum, and trichophyton • detected in the stratum corneum

• active against P. orbiculare, but not to candida • high concentration in outermost layers

• cross sensitivity to penicillin (because derived

from penicillin mold)
ADR
• can alter Coumarin anticoagulant activity
• irritation or allergic contact sensitization (rare)

F. Polyenes: Nystatin & Amphotericin B

MOA:
• C. albicans infections
• inhibition of hyphal cell wall synthesis and
• Inaffective against dermatophytes mitosis

• paronychial and intertriginous candidiasis • effects on nucleic acid synthesis

• interferes with microtubules of the mitotic

spindle and with cytoplasmic microtubules
1. Nystatin
• active only against growing cells
• cutaneous and mucosal candida infections

• oral candidiasis (thrush) – oral or vaginal tablet

ADR:
• Recurrent or recalcitrant perianal, vaginal,
vulvar, anddiaper area candidiasis – oral • headaches, nausea, vomiting, diarrhea,
photosensitivity, peripheral neuritis, mental
• Vulvovaginal candidiasis – vaginal tablet confusion

CI
ADR: • Porphyria, hepatic failure, hypersensitivity,
leucopenia, proteinuria

Page 5 of 15
B. Oral Azole Derivatives • against members of the herpesvirus family
(HSV 1 and 2)
1. Ketoconazole
MOA:
• first imidazole derivative used
• phosphorylated by herpes simplex virus-coded
• treatment in glabrous skin and cutaneous
thymidine kinase, the resultant triphosphate
infections
interferes with herpesvirus DNA polymerase
• chronic mucocutaneous candidiasis and viral DNA replication

• chromomycosis A. Antiviral Agents

• Tinea versicolor 1. Valacyclovir (Oral)

• tinea capitis • L-valyl ester of acyclovir

• For Genital herpes, orolabial herpes and zoster

ADR:

• Nausea, pruritus, gynecomastia, hepatitis

2. Acyclovir (topical, 5% ointment)

• acyclic guanosine derivative with clinical

2. Triazoles: activity against HSV-1, HSV-2, and VZV

• topical: herpes labialis

a. Fluconazole

mucocutaneous candidiasis, dermatophyte 3. Famcyclovir (Oral)

infection
• active against HSV-1, HSV-2, VZV, EBV, and
HBV

b. Itraconazole • effective tx for genital herpes, herpes labialis

and zoster
Onychomycosis

c. Voriconazole 4. Penciclovir (topical, 1% cream)

• active metabolite of famciclovir

ADR: • recurrent orolabial herpes simplex virus

infection in immunocompetent adults
• Arrhythymias, depression and rhabdomyolysis
(combined tx)

CI of oral azoles ADR:

• midazolam or triazolam – result in elevated • Pruritus, mild pain with transient stinging or
plasma conc – prolong hypnotic and sedative burning.
effect
B. Docosanol (10% cream)
• HMG-CoA inhibitors – rhabdomyolysis
• inhibits fusion between the plasma membrane
TOPICAL ANTIVIRAL AGENTS and the HSV envelope, thereby preventing viral
entry into cells and viral replication

Page 6 of 15
 • for herpes labialis

MOA:

C. Trifluridine (1% ophthalmic) • agents inhibit T lymphocyte activation

• prevent the release of inflammatory

cytokines and mediators from mast cells in
• inhibits viral DNA synthesis in HSV-1, HSV-2, vitro after stimulation by antigen-IgE
CMV complexes
• effective in treating keratoconjunctivitis and
recurrent epithelial keratitis due to HSV-1 or ADR:
HSV-2
• burning sensation
D. Immunomodulators: HPV 6, 11

Imiquimod
ECTOPARASITICIDES
• external genital and perianal
warts in adults

• actinic keratoses on the face A. PERMETHRIN (2-5% cream)

and scalp
• Treatment of Scabies and Pediculosis
• primary basal cell carcinomas • Washed after 14 hours
on the trunk, neck, and extremities
ADR:
• 3 times per week and left on • Transient Burning, Stinging, Pruritis
the skin for 6–10 hours prior to washing, for
16 weeks B. LINDANE (Hexachlorocyclohexane):
Shampoo/lotion

• Treatment of pediculosis capitis or pubis.

MOA: Also for Scabies but there is concern for its
toxicity.
• stimulate peripheral mononuclear cells • Wash after 12 hrs
to release interferon-α
Contraindication:
• stimulate macrophages to produce • In premature infants and in patients with
interleukins-1, -6, -8, and tumor necrosis known seizure disorders
factor-α
ADR:
• Neurotoxicity and hematotoxicity in infants,
children and pregnant women
ADR:
C. CROTAMITON (cream/lotion)
• pruritus, erythema, and superficial
erosion. • Scabicide with anti pruritic properties. Can be
used as alternative to Lindane.

Contriaindication:
E. Immunosuppressive: • Contraindicated in acutely inflamed skin or to
the eyes or mucous membranes

ADR:
Tacrolimus (0.03%,0.1% ointment) & • Allergic contact hypersensitivity and Primary
Pimecrolimus (1% cream) Irritation

• macrolide D. SULFUR (5% cream)

immunosuppressants for mild to moderate
atopic dermatitis • Scabicide
• Safe for Infants & Pregnant women

Page 7 of 15
 • has an unpleasant odor and stains on skin These DNA photoproducts may inhibit DNA
synthesis.
E. MALATHION (0.5% lotion)

• Treatment of Pediculosis only ADR: Cataracts and skin cancer.

• Wash/comb only after 4-6 hours
SUNSCREENS/SUNBLOCKS

MOA: A. PABA esters (p-aminobenzoic acid)

• organophosphate cholinesterase inhibitor 1. Benzophenones: Oxybenzone, Dioxybenzone

and Sulisobenzone
• broader spectrum of absorption from 250 to
AGENTS AFFECTING PIGMENTATION 360 nm
A. REDUCING AGENTS: DEPIGMENTATION
2. Dibenzoylmethane: Parasol and Eusolex
1. HYDROQUINONE, MONOBENZONE, & • absorb wavelengths throughout the longer UVA
MEQUINOL range, 320 to 400 nm, with maximum
absorption at 360 nm
• Reduce Hyperpigmentation of skin • for individuals with polymorphous light
• Topical hydroquinone and mequinol- temporary eruption, cutaneous lupus erythematosus, and
lightening drug-induced photosensitivity
• Monobenzone causes irreversible
depigmentation 3. Terephthalylidene dicamphorsulfuric acid
• Monobenzone and Mequinol combination with (Greater UVA protection)
steroid topical + retinoic acid • absorb ultraviolet light in the ultraviolet B
(UVB) wavelength range from 280 to 320 nm
MOA: • less prone for phtodegradation
• SPF is measure of Effectiveness in absorbing
erythrogenic ultraviolet light. Minimum : 15%
• Inhibition of the enzyme Tyrosinase, thus
interfering with the biosynthesis of Melanin.
ADR: Skin Aging, Photocarcinogenesis
• Monobenzone may be toxic to melanocytes
resulting to loss of these cells
ANTI-PSORIASIS
Side effects: local irritation (Hydroquinone and
Monobenzone)
• percutaneous absorption may take place A. ACITRETIN Oral 25-50mg
because monobenzone causes
hypopigmentation at sites distant from the • For the Treatment of Psoriasis especially
area of application pustular forms.

2. L-Glutathione Contraindication:
• In Pregnancy, Consumption of Ethanol, Blood
B. OXIDISING AGENTS: REPIGMENTATION Donation

1. TRIOXSALEN Oral UVA irradiation & ADR: Teratogenic, Hepatotoxicity

METHOXSALEN Oral
• They are Psoralens that need to
photoactivated to produce effect
• Trioxsalen for Vitiligo
• Methoxsalen for Psoriasis
MOA:
• Psoralens intercalate with DNA and, with
subsequent UVA irradiation, cyclobutane
adducts are formed with pyrimidine bases.
B. TAZAROTENE (0.1% gel/cream)
be
MOA:
• The active metabolite, tazarotenic acid, binds
to retinoic acid receptors, resulting in modified
gene expression.
• may have anti-inflammatory and
antiproliferative actions.
ADR: burning or stinging sensation (sensory
irritation), peeling, erythema, localized edema of
the skin (irritant dermatitis)
C. CALCIPOTRIENE (0.005% ointment)

Page 8 of 15
 • a synthetic vitamin D3 derivative
• treatment of plaque-type psoriasis vulgaris of 2. INFLIXIMAB
moderate severity.
ADR: MOA:
burning, itching, and mild irritation • binds to the soluble and transmembrane forms
dryness and erythema of the treatment area of TNF-α and inhibits binding of TNF-αwith its
receptors
D. T-CELL MODULATORS:
Contraindication & ADR: SAME AS ETANERCEPT!
1. ALEFACEPT IV/IM
3. ADALIMUMAB
MOA:
• immunosuppressive that interferes with MOA:
lymphocyte activation, and causes a reduction • binds specifically to TNF-α and blocks its
in subsets of CD2 T lymphocytes and interaction with cell surface TNF receptors
circulating total CD4 and CD8 T-lymphocyte
counts. Contraindication & ADR: SAME AS ETANERCEPT!
• treatment of adult patients with moderate to
severe chronic plaque psoriasis
F. IMMUNOSUPPRESIVES (Mentioned in Lecture)
Contraindications:
1. CYCLOSPORINE
• In patients with CD4 counts are below 250 2. METHOTREXATE = anti thymidylate synthetase
cells/L
• In patients with clinically significant infection
ANTI-INFLAMMATORY STEROID TOPICALS
2. EFALIZUMAB Subcutaneous

MOA: A. TOPICAL CORTICOSTEROIDS

• Immunospuresive recombinant humanized • Minimally absorbed after application to normal
IgG1 kappa isotype monoclonal antibody that skin
binds to the CD11a subunit of leukocyte • Long-term occlusion with an impermeable film
function antigen-1. This binding affects the enhances penetration
activation, adhesion, and migration of T • Marked regional anatomic variation in
lymphocytes. corticosteroid penetration
• Ointments have better activity compared with
Contraindication: Not to be given with other creams or lotions
immunosuppressive medications • Increasing concentration increase penetration
(not proportionately)
ADR: severe immune-mediated thrombocytopenia
• Intralesional injection(0.1mL) of relatively
insoluble corticosteroids often effective for
E. ANTI-TNF ALPHA:
lesions unresponsive to topical forms
*HYDROCORTISONE
1. ETANERCEPT Subcutaneous
- natural glucocorticosteroid of the adrenal cortex
MOA: - original topical glucocorticosteroid
• binds selectively to TNFα and β and blocks * PREDNISOLONE, METHYLPREDNISOLONE
interaction with cell surface TNF receptors that - as active topically as hydrocortisone
play a role in the inflammatory process of * DEXAMETHASONE, BETAMETHASONE
plaque psoriasis. - fluorinated steroids
- no advantage over hydrocortisone
Clinical Use: Treatment of Psoriatic Arthritis *TRIAMCINOLONE, FLUOCINOLONE
- acetone derivatives of the fluorinated steroids
Contraindication:
• In Patients with TB risk - with distinct efficacy advantage topically
• Not to be used concurrently with other
immunosuppressive
MOA:
ADR:
• Sepsis • Induction of phospholipase A2 inhibitory proteins 
• Pneumonia inhibit release of arachidonic acid  control
• Lymphoma biosynthesis of potent mediators of inflammation
(e.g. prostaglandins and leukotrienes).

Page 9 of 15
*Arachidonic acid is released from membrane phospholipids HYDROCORTISONE
by phospholipase A 2. INTERMED
MOMETASONE
• Inhibit the production by multiple cells of factors that TRIAMCINOLONE
LOW
are critical in generating the inflammatory response FLUMETHASONE
METHYLPREDNISOLONE
• Antimitotic: useful in psoriasis and other LOWEST
DEXAMETHASONE
dermatological diseases associated with increased
cell turnover
B. TAR COMPOUNDS

* Inflammation: characterized by extravasation and infiltration

Clinical Uses:
of leukocytes into the affected tissue, mediated by a
series of interactions of the adhesion molecules of both • Psoriasis
the WBC and the endothelial cells, inhibited by • Dermatitis
glucocorticosteroids • Lichen simplex chronicus
• Chronic lichenified dermatitis: particularly
ADR: useful as tx due to its phenolic constituents
endowing it with antipruritic properties
• potentially suppress pituitary-adrenal axis
- Iatrogenic Cushing’s syndrome
* Alternative to topical corticosteroids in subacute and chronic
stages of dermatitis and psoriasis
• Applying potent TCs in extensive areas for
prolonged periods increases likelihood of
systemic effects
- Growth retardation among children ADR:
• Irritant folliculitis: discontinue therapy for 3-5 d
• Local effects (skin): • Phototoxicity
 Atrophy: wrinkled “cigarette • Allergic Contact Dermatitis
paper” appearance
Contraindications:
 Prominent telangiectases
 Tendency to develop purpura, • Acute dermatitis with vesiculation and oozing:
ecchymosis irritated by even weak tar preparations
 Rosacea • Patients previously exhibiting sensitivity to
 Perioral dermatitis them

 Steroid acne KERATOLYTIC & DESTRUCTIVE AGENTS

 Hypopigmentation
 Hypertrichosis A. SALICYLIC ACID (3-6% sol./gel)
 Glaucoma – increased intraocular
pressure
 Allergic Contact Dermatitis MOA: Solubilize cell surface proteins that keep stratum
(ACD): Patch test with high corneum intact  desquamation of
concentrations of corticosteroids (i.e. 1% keratotic debris
in petrolatum) for confirmation
ADR:
* Patch testing performed with: • Salicylism and death
- 1 g pf topical SA: raise serum salicylate not
Hydrocortisone valerate/butyrate
>0.5 mg/dL plasma (threshold: 30-50 mg/dL)
Tixocortol pivalate
Budesonide • Urticarial and erythema multiforme reactions,
anaphylaxis: in allergic patients
Contraindications: • Local irritation, acute inflammation, ulceration
Hypersensitivity: some develop generalized with use of high concentrations
flare with adreno-corticotropic hormone or oral
prednisone Special Precaution:
• Particular care when using it on the extremities
Efficacy Drugs of patients with diabetes or peripheral vascular
BETAMETHASONE dse (PVD)
HIGHEST
CLOBETASOL
FLUOCINONIDE B. PROPYLENE GLYCOL 10-70% sol. (from ppt), 40-
HIGH 70% (Katzung)
DIFLORASONE

Page 10 of 15

• Percutaneously absorbed: oxidized by liver to
lactate and pyruvate  utilized in general body
metabolism
• Effective keratolytic agent for the removal of
hyperkeratotic debris
MOA:
• Effective humectant: increases H2O content of
stratum corneum  develops osmotic gradient
through stratum corneum  draws H2O out
from the inner layers  increases hydration of
outermost layers
Clinical Uses:
• Ichthyosis
• Palmar and plantar keratodermas
• Psoriasis
• Pityriasis rubra pilaris
• Keratosis pilaris
• Hypertrophic lichen planus
ADR: Allergic contact dermatitis
C. UREA (20% cream, lotion)
• Local adverse effects: inflammation, erosions,
burning pain, itching
• Conjunctivitis: with eye contact
Contraindications: Pregnancy: teratogenic, fetotoxic
E. FLUOROURACIL (5-FU) (5-6% top.)
MOA: Inhibits thymidilate synthetase activity,
interfering with DNA and RNA synthesis
Clinical Use: Actinic keratosis
ADR:
• Pain, Pruritus, Burning sensation,Tenderness
• Residual postinflammatory hyperpigmentation
• Allergic contact dermatitis
F. NSAIDS: DICLOFENAC (3% gel)
Clinical Use:
• Actinic keratosis: moderate effectiveness
ADR:
• Anaphylactoid reactions

MOA: Contraindications: Known aspirin hypersensitivity

• Humectant: increases H2O content of stratum
corneum G. AMINOLEVULINIC ACID (ALA) (20% sol.)
• Keratolytic: involve alterations in prekeratin
and keratin  increase solubilization MOA
• Break H-bonds that keep stratum corneum * ALA: endogenous precursor of photosensitizing
intact
porphyrin metabolites
Cinical Use:
• Ichthyosis vulgaris • Protoporphyrin IX (PpIX) accumulates in the
cell (with addition of photodynamic illuminator,
• Hyperkeratosis of palms and soles
BLU-U, 18 h after)  formation of superoxide
• Xerosis
and hydroxyl radicals (cytotoxic) 
• Keratosis pilaris
photosensitization of actinic keratoses

Clinical Use: Actinic keratosis

Special Precautions: Cytotoxic on sunlight

D. PODOPHYLLUM & PODOFILOX (0.5% sol.)

ANTIPRURITIC AGENTS
MOA: Cytotoxic  prevents normal assembly of the
mitotic spindle and arrests epidermal mitoses in A. DOXEPIN (5% cream)
metaphase
MOA:
Clinical Use: • Unknown but may relate to the potent H1- and
H2-receptor anatagonist properties of
• Condyloma acuminatum (genital warts)
dibenzoxepin tricyclic compounds
ADR:
Clinical Use: Atopic dermatitis, Lichen simplex
• Hepato-, neuro- (visual and auditory
chronicus
hallucinations, delusions, disorientation,
confusion and delirium), and nephrotoxic
• Neuropathy with diminished tendon reflexes ADR:

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 • Allergic contact dermatitis, Marked burning and
stinging of treatment site

Contraindications:
• Untreated narrow-angle glaucoma
• Tendency to urinary retention

B. PRAMOXINE (1% cream, lotion, gel)

• Topical anesthetic can provide temporary relief
from pruritus associated with mild eczematous
dermatoses
MOA
• Decreases neuronal membrane's permeability
to sodium ions  initiation and conduction of
nerve impulses are blocked depolarization of
the neuron inhibited

Clinical Use: Mild eczematous dermatitis

ADR: Transient burning and stinging

ANTI-SEBORRHEA AGENTS

The following lists topical formulations for the

treatment of seborrheic dermatitis. These are of
variable efficacy and may necessitate concomitant
treatment with topical corticosteroids for severe cases.

1. Betamethasone valerate foam (Luxiq)

2. Chloroxine shampoo (Capitrol)
3. Coal tar shampoo (Ionil-T, Pentrax, Theraplex-
T, T-Gel)- Anti- inflammatory
ADR: Allergic contact dermatitis
4. Fluocinolone acetonide shampoo (FS Shampoo)
5. Ketoconazole shampoo (Nizoral)
6. Selenium sulfide shampoo (Selsun, Exsel)
7. Zinc pyrithione shampoo (DHS-Zinc, Theraplex-
Z)

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Page 13 of 15
Drug Mechanism of Action Clinical Use Adverse Drug Reactions / Contraindications
TRICHOGENIC
AGENTS
Minoxidil (Rogaine) Unknown • Effective in reversing the • Cessation of treatment will lead to hair loss in 4-6
progressive months.
miniaturization of terminal • Percutaneous absorption in normal scalp is minimal
scalp hairs associated with BUT possible systemic effects on BP should be
androgenic alopecia monitored in patients with cardiac disease.
• Vertex balding more
responsive than frontal
balding
• Effect not permanent
Finasteride (Propecia) • 5α-reductase inhibitor • Oral: promotes hair • Decreased libido
Oral: 1 mg/ day for 3-6 • Blocks the conversion growth, prevents further • Ejaculation disorders
months of testosterone to hair loss • Erectile dysfunction
dihydrotestosterone • Treatment for at least 3-6 • ADRs will resolve in most men who remain on
(the androgen months is necessary. therapy and in all men who discontinue with the
responsible for • Continued treatment drug
androgenic alopecia in necessary to sustain • C/I: pregnant women (chance of hypospadia in
genetically benefit. male fetus)
predisposed men) • No data to support use in
women with androgenic
alopecia
Drug Mechanism of Action Clinical Use Adverse Drug Reactions / Contraindications
ANTI-TRICHOGENIC
AGENTS
Eflornithine (Vaniqa) • Irreversible inhibitor • Topical: reduce hair • Stinging
Oral: 2x a day for 6 of ornithine growth in ~30% of women • Burning
months, return after 8 decarboxylase • Hair growth observed to • Folliculitis
weeks (catalyst of rate- return to pre-treatment
limiting step in levels 8 weeks after
biosynthesis of discontinuation.
polyamines)

Drug Mechanism of Action Clinical Use Adverse Drug Reactions / Contraindications

ANTI-NEOPLASTIC
AGENTS
Alitretinoin (Panretin) • Topical formulation of 9-
cis-retinoic acid
• Treatment of cutaneous
lesions in patients with
AIDS-related Kaposi’s
sarcoma
Bexarotene (Targretin) • Member of a subclass • Oral/topical gel: treatment
of retinoids that of cutaneous T-cell
• Intense erythema, edema and vesiculation
• Should not concurrently use products containing
deet, a common component of insect repellant
products
• Teratogenicity
• May increase levels of triglyceride and cholesterol

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 selectively binds and lymphoma
activates retinoid X
receptor subtypes
Vorinostat (Zolinza) • Histone deacetylase • Treatment of cuteneous T- • Pulmonary embolus
inhibitor cell lymphoma in patients • Deep vein thrombosis
with progressive, • Thrombocytopenia
persistent or recurrent • Anemia
disease on or after two • GI disturbances
systemic therapies

MISCELLANEOUS MEDICATIONS

Drug or Group Conditions

Alitretinoin AIDS-related Kaposi's sarcoma
Antihistamines Pruritus (any cause), urticaria
Antimalarials (H- Lupus erythematosus, Photosensitization
chloroquine)
Antimetabolites Psoriasis, pemphigus, pemphigoid
Becaplermin Diabetic neuropathic ulcers
Bexarotene Cutaneous T cell lymphoma
Chlorhexidine Antiseptic wash (oral/vaginal)
Corticosteroids Pemphigus, pemphigoid, lupus erythematosus, allergic contact dermatoses, and certain other dermatoses
Cyclosporine, Psoriasis. Pemphigus
Methotrexate
Dapsone Dermatitis herpetiformis, erythema elevatum diutinum, pemphigus, pemphigoid, bullous lupus erythematosus
Denileukin diftitox Cutaneous T cell lymphoma
Etanercept Psoriatic arthritis
Interferon-alpha Melanoma, viral warts
Mycophenolate Mofetil Bullous disease
Thalidomide Erythema nodosum leprosum

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