Dermatopharmacology

1. DERMATO-
PHARMACOLOGY
Presenter – Dr. Sneha Dange, Jr2
Dept. of Pharmacology,
GMC, Nagpur

2. OVERVEIW
 Introduction of skin structure
 Principles of topical drug application
 Antimicrobial agents
 Antifungal agents
 Antiviral agents
 Drugs for infestation
 Immunosuppressants & immunomodulators
 Miscellaneous agents
 Recent advances
2

3. INTRODUCTION
 Skin is the largest organ of the human body
 The prevalence of skin diseases in the general population in different
geographic regions of India varies from 7.9% to 60%
Adults (>18 years) constitute about 80.9% & among 59.9% males
Overall, infections of the skin and subcutaneous tissue are the most
common (32.6%) followed by the disorders of skin appendages (19.8%),
dermatitis, eczema (18.8%), (16.7%) acne
Psoriasis, urticaria, melasma, and vitiligo in 3.4%, 3.4%, 3.6%, and 3.3%
patients, respectively
3

4. SKIN STRUCTURE
4
Epidermis –
o Multilayered, keratinising,
stratified, squamous
epithelium
o Lipid rich stratum
corneum prevents water
loss (Absorbtion)
Dermis –
o Thick, vascular, consist of
skin appendages, sweat
gland, sebaceous gland
(metabolism)

5. PRINCIPLES OF TOPICAL DRUG
APPLICATION
Topical drug treatment aim at providing high concentration of the
drug at the site of application with minimal systemic absorption
However, therapeutic effects depends on properties of drug,
vehicle used & skin lesions
Absorption of drug depends on-
 Lipid solubility of the preparation
 State of hydration of stratum corneum
 Drug concentration in the vehicle
 Thickness of the skin
 Quantity applied
 Presence of inflamed skin
 Use of occlusive dressing
5

6. FORMULATIONS
6
OINTMENT
• Solid or liquid
dispersed in
nonaqueous base
• Anhydrous to <
20% water
• preventing loss of
heat and water
• Greasy texture, so
less cosmetically
favorable
• Preparation is
difficult to wash
off
• Not easily
spreadable
CREAM
• Emulsions of water
in oil (oily creams)
or oil in water
(vanishing creams)
• 20%–80% water
• Less hydrating
than ointments
• effective in both
dry and
weepy/exudative
• less greasy, less
viscous, and more
spreadable
GEL
• Water-soluble
emulsion
• polyethylene glycols,
alcoholic solvent
• Concentrates drug at
surface after
evaporation
• Cosmetically favorable
• Easy to apply and wash
off, especially to hair-
bearing areas
• Nongreasy
• Provides cooling
sensation
LOTION
• Lotion-suspended
drug
• Solution-dissolved
drug base (aqueous
or alcoholic)
• Provide cooling
effect
• Easy to apply to
hair-bearing areas
• Spreads rapidly
• Less hydrating than
ointments or creams
• Exudative
dermatoses
• Hair-bearing areas

7. FORMULATIONS
7
Demulcents
-are inert substances
which sooth inflamed
or denuded mucosa or
skin by preventing
contact with
air/irritants in the
surroundings
-gum acacia, gum
tragacanth,
Glycyrrhiza,
Methylcellulose,
Propylene glycol,
Glycerine
Emollients
-bland oily
substances which
sooth and soften skin
-form an occlusive
film over the skin,
preventing
evaporation, thus
restoring elasticity
of cracked and dry
skin
-Olive oil, arachis oil,
sesame oil, cocoa
butter, hard and soft
paraffin, liquid
paraffin, wax
Adsorbants-
-finely powdered,
inert, insoluble
solids capable of
binding to their
surface (adsorbing)
noxious and irritant
substances
-physical
protection to the
skin n mucosa
-Magnesium/zinc
stearate, Talc,
Calamine, boric
acid, starch
Astringents-
-are substances
that prectpitate
proteins, but do
not penetrate
cells, so affect
superficial layer
only
-Tannic acid and
tannins, Ethano l
and methanol at
50 90%, zinc
oxide
Irritants and
counterirritants
-sensory nerve
endings & induce
inflammation
-produce cooling
sensation, warmth,
pricking, tingling,
hyperaesthesia
,numbness, local
vasodilatation
-Camphor,
Eucalyptus oil,
Menthol, Capsicum

8. GLUCOCORTICOIDS
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Immunosuppressive and anti-inflammatory properties
Selected on the basis of its potency, the site of involvement & severity of
disease
More potent steroid is used initially, followed by a less potent agent
More frequent application does not improve response
Only non-fluorinated glucocorticoids should be used on the face,axillae or
groin
Intralesional preparations (insoluble triamcinolone acetonide & triamcinolone
hexacetonide) - solubilize gradually & so prolonged duration of action

9. GLUCOCORTICOIDS
Long-term occlusion is an effective method of enhancing penetration & absorption
Prednisolone and methylprednisolone same as hydrocortisone
9α-fluorinated dexamethasone and betamethasone no advantage over hydrocortisone
Triamcinolone and fluocinolone, the acetonide derivatives of the fluorinated steroids-
distinct efficacy in topical therapy
Betamethasone is not very active, but attaching 5-carbon valerate chain to the 17-
hydroxyl position results in a compound which is 300 times active than hydrocortisone
9

10. 10
Class I Class II Class III
• Betamethasone
dipropionate cream,
ointment
0.05% (augmented)
• Clobetasol propionate
cream, ointment 0.05%
• Halobetasol propionate,
ointment 0.05%
• Diflorasone diacetate,
ointment 0.05%
• Betamethasone
dipropionate, ointment
0.05%
• Fluocinonide, cream,
ointment, gel 0.05%
• Amcinonide, ointment 0.1%
• Desoximetasone, cream,
ointment 0.25%,,gel 0.05%
• Diflorasone diacetate,
ointment 0.05%
• Halcinonide, cream,
ointment 0.1%
• Betamethasone valerate,
ointment 0.1%
• Betamethasone
dipropionate, cream 0.05%
• Triamcinolone acetonide,
ointment 0.1%, cream 0.5%
• Diflorasone diacetate,
cream 0.05%
Potency of Topical Corticosteroids

11. 11
Class IV Class V Class VI Class VII
• Hydrocortisone
valerate, ointment
0.2%
• Mometasone
furoate, cream,
ointment 0.1%
• Triamcinolone
acetonide,
ointment 0.1%
• Fluocinolone
acetonide, cream
0.2%
• Fluocinolone
acetonide,
ointment 0.025%
• Betamethasone
dipropionate, lotion
0.05%
• Betamethasone
valerate, cream,
lotion 0.1%
• Hydrocortisone
valerate, cream
0.2%
• Hydrocortisone
butyrate, cream
0.1%
• Fluocinolone
acetonide, cream
0.025%
• Fluocinolone
acetonide, cream,
solution 0.01%
• Alclometasone
dipropionate,
cream, ointment
0.05%
• Desonide, cream
0.05%
• Hydrocortisone,
cream, ointment,
lotion 0.5%, 1%,
2.5%
Potency of Topical Corticosteroids

12. ANTIMICROBIAL AGENTS
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 Numerous organisms (Staphylococcus aureus and Streptococcus pyogenes) causes
cutaneous infections ranging from benign to life-threatening
 Treatment depend on the depth of cutaneous involvement, immune status of the
patient, causative organism, and local antibiotic resistance patterns
Topical –
 Mupirocin
 Retapamulin
 Bacitracin & Gramicidin
 Polymyxin B
 Neomycin, Gentamicin
 Silver sulfadiazine
 Mafenide
Systemic –
 Penicillins & cephalosporins
 Clindamycin, doxycycline,
trimethoprim sulfamethoxazole
 Vancomycin, linezolid,
quinupristin, dalfopristin,
daptomycin (MRSA)
 Dalbavancin, oritavancin,
telavancin, tedizolid,
ceftaroline

13. 13
Topical agent MOA Indication
Mupirocin (2%
ointment or cream)
Inhibits protein synthesis by binding to
bacterial isoleucyl-tRNA synthetase
S. Aureus and S. Pyogenes,
Impetigo twice daily-5 days
Retapamulin (ointment
1%)
Selectively inhibits bacterial protein
synthesis by interacting at 50S subunit of
bacterial ribosomes
Same +
Anaerobes
For 9 months & above
Bacitracin & gramicidin Peptide antibiotic Gram-positive organisms
Polymyxin B Peptide antibiotic Gram-negative organisms
Neomycin, gentamicin Aminoglycoside antibiotics
(Neomycin alone and in combination with
polymyxin, bacitracin)
Gram-negative organisms
Gentamicin-(p aeruginosa than
neomycin), staphylococci & group A
β-hemolytic streptococci
Silver sulfadiazine
Mafenide (5% solution)
Binds -bacterial DNA & inhibits replication
Sulfonamide
Gram-positive bacteria + MRSA,
Gram-negative bacteria,
p.aeruginosa
Partial-thickness burns

14. ANTIFUNGAL AGENTS
Topical –
Azoles derivatives
Ciclopirox olamine
Tavaborole
Allylamines
Butenafine
Tolnaftate
Nystatine & Amphotericine B
Oral –
Azole derivatives
Terbutaline
Griseofulvin
14

15. 15

16. ANTIFUNGAL AGENTS
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17. TOPICAL AZOLES
17
 Once/twice daily application for 2–3 week
 Antifungal-corticosteroid - more rapid symptomatic
improvement
 Systemic therapy (terbinafine, fluconazole,
itraconazole, griseofulvin ) - more extensive cutaneous
involvement or a poor response to topical therapy

18. ANTIFUNGAL AGENTS
18
Topical antifungal MOA Indication
Tavaborole (5%
solution)
Blocks fungal protein synthesis by
inhibiting aminoacyl-transfer
ribonucleic acid synthetase
Toe-nails onychomycosis
Naftifine, Terbinafine
(1% or 2% gel)
Inhibition of squalene epoxidase Tinea, Pityriasis
versicolor
Butenafine (1% cream)
(benzylamine)
Inhibition of squalene epoxidase Tinea, Pityriasis
versicolor
Tolnaftate 1% cream, powder, topical solution Tinea, Pityriasis
versicolor
Ciclopirox 8% topical solution/lacquer, 1%
shampoo, 0.77% gel
Onychomycosis
Tinea, seborrheic
dermatitis
Nystatin
Amphotericin B
Topical,
IV
mucosal candidiasis,
systemic mycoses

19. ANTIFUNGAL AGENTS
19
Systemic antifungal MOA Indication Remark
Fluconazole(100 mg
daily)
Itraconazole (200 mg
daily )
Inhibit conversion of
lanosterol to ergosterol
Mucocutaneous
Candidiasis,
dermatophytosis,
Onychomycosis
Half-life of 30 hours
Ventricular dysfunction
Midazolam, triazolam, or HMG-
COA inhibitors is
contraindicated
Terbinafine
(250 mg daily)
Inhibition of squalene
epoxidase
6 weeks for
fingernail
onychomycosis
12 weeks for
toenail
Hepatic dysfunction
Griseofulvin (500 mg
daily)
Inhibit mitosis in fungal
cells
Recalcitrant
infections tinea
6 months fingernail
onychomycosis
8-18 months for
toenail
Microsized, ultramicrosized
reducing the particle size of
the increases drug absorption

20. ANTIVIRAL AGENTS
20
Agent Treatment
Genital Herpes
Acyclovir, oral 400 mg tid × 7–10 days or 200 mg 5 times daily
Famciclovir, oral 250 mg tid × 7–10 days
Valacyclovir, oral 1000 mg bid × 10 days
Orolabial herpes
Acyclovir, oral 400 mg tid × 7–10 days
or 200 mg 5 times daily
Famciclovir, oral 500 mg tid × 7–10 days
Valacyclovir oral 1 g bid × 7–10 days
Acyclovir topical (5% cream)
Docosanol, topical (10% cream)
Penciclovir, topical (1% cream)
Zoster infection Acyclovir, oral 800 mg 5 times daily × 7–10 days
Famciclovir, oral 500 mg tid × 7 days
Valacyclovir, oral 1 g tid × 7 days
Warts caused by HPV
 Keratolytic salicylic acid
 Topical podophylline 15-20% solution
 Trichloroacetate, phenol, formaldehyde 5%
 Silver nitrate for cauterise warts

21. SCABIES
Itch mite Sarcoptes scabiei
burrow superficial layer - tunnel-
lays eggs
Drugs used –
 Sulphur
 Benzyl benzoate
 Permethrin
 Gamma benzene hexachloride
(GBH/Gamma
BHC/gammaxene/lindane)
 Ivermectin
 Monosulphiram
Pediculus humanus affects scalp,
body, pubic area
Drugs used –
 Permethrin 1%
 Malathion 0.5%
 Dicophane (DDT) 2%
 Gamma benzene hexachloride 1%
cream, 2% shampoo
PEDICULOSIS
21
DRUGS FOR INFESTATION

22. Drugs for infestation contd..
 Sulphur – 5% children, 10% adults, 0.5% neonates
Oldest remedy, irritant, stains cloths, unpleasant odour, cheap but obsolete
Possible alternative for infants & pregnant woman
Benzyl benzoate – 25% emulsion
Highly scabicidal & drug of choice
5% lotion for pediculosis in 6months & older children
Treatment repeated after 7 days
Permethrin –
1% pediculosis 10mins, 5% cream for scabies for 8-14hrs
Only 2% dose is absorbed
Does not have disadvantages like gammexane & is safe
22

23. Drugs for infestation contd..
23
 Gamma benzene hexachloride (GBH/Gamma BHC/gammaxene/lindane)
1% lotion for scabies – over body below neck & left for 12hrs avoid contact with
eyes
Odourless, non irritant
Neurotoxic – avoided in infants, childrens
Ivermectin – (resistant cases)
0.5% lotion for pediculosis 6 months & older children
Single dose 200mcg/kg for scabies repeat after 2 weeks – highly effective
Malathion 0.5% (resistant cases)
Rapidly pediculocidal, applied for 8-12 hrs n repeated 7-9 days later
Well tolerated no systemic side effects

24. Drugs for infestation contd..
24
 Dicophane (DDT) 10%
10% dusting powder for pediculosis corporis & pubis
Adequate residual effect for larvae which hatch later
Spinosad
0.9% for 10 mins in 4years & older patients for pediculosis
Derived from fermentation of a soil Actinomyces bacterium
Crotamiton
10% lotion – 2 application 24 hr apart
Effective alternative to lindane for scabies

25. IMMUNOSUPPRESSANTS &
IMMUNOMODULATORS
Imiquimod -
 Stimulate peripheral mononuclear cells to release interferon alpha & stimulate
macrophages to produce interleukins-1, -6, and -8, and tumor necrosis factor-a (TNF-a)
 5% cream - for external genital and perianal warts in adults, actinic keratoses on the
face and scalp, superficial BCC on the trunk, neck, and extremities
Tacrolimus & Pimecrolimus –
 Inhibit T-lymphocyte activation and prevent the release of inflammatory– cytokines
and mediators from mast cells
 Tacrolimus 0.03% ointment and Pimecrolimus 1% cream are approved for use in children
older than 2 years of age, adult for mild to moderate atopic dermatitis
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26. 26
Methotrexate Dihydrofolate reductase inhibitor moderate-to-severe psoriasis
Fluorouracil Blocks methylation in DNA
synthesis
multiple actinic keratoses, superficial BCCs
Cyclophosphamide Alkylates and cross-links DNA advanced CTCL
Mechlorethamine
hydrochloride
Alkylating agent Topically for CTCL
Carmustine Cross-links in DNA and RNA Topically for CTCL
Vinblastine Inhibits microtubule formation Intralesional Kaposi sarcoma and advanced
CTCL
Bleomycin Induction of DNA strand breaks off label intralesionally for squamous cell
carcinoma and recalcitrant warts
Azathioprine Purine synthesis inhibitor pemphigus vulgaris, bullous pemphigoid,
atopic dermatitis, chronic actinic
dermatitis, LE, psoriasis
Mycophenolate mofetil Inosine monophosphate
dehydrogenase inhibitor
corticosteroid-sparing agent
Cyclosporine Calcineurin inhibitor psoriasis
Sirolimus mTOR inhibitor tuberous sclerosis complex, pachyonychia
congenita, complex vascular anomalies

27. MISCELLANEOUS AGENTS
# Keratolytic agents
# Antiseborrhic agents
# Agents affecting pigmentation
# Trichogenic & antitrichogenic
agents
# Antipruritic agents
# Acne preparations
# Agents for psoriasis
# Irritant & counterirritants
27

28. KERATOLYTIC AGENTS
 Salicylic acid
 Propylene glycol
 Urea
 Podophyllum resin & podofilox
 Sinecatechins
 Fluorouracil
 Ingenol mebutate
28

29. KERATOLYTIC AGENTS
Salicylic acid –
Solubilize cell surface proteins that keep the stratum corneum intact -
0.5%-2% acne vulgaris, 6% ointment dandruff, seborrheic dermatitis, psoriasis, >6%
destructive to tissues
Limit - total amount of salicylic acid applied and the frequency of application
Urticarial, anaphylactic reactions, erythema multiforme, local irritation
 Propylene glycol –
An excellent vehicle for organic compounds
Only minimal amounts is absorbed
With 6% salicylic acid - ichthyosis, palmar and plantar keratodermas, psoriasis,
pityriasis rubra pilaris, keratosis pilaris & hypertrophic lichen planus
Keratolytic agent at 40–70% concentrations
29

30. KERATOLYTIC AGENTS
 Urea –
As a humectant at 2–20% in creams and lotions, feels less greasy
Keratolytic at 20% – involved in alterations in prekeratin and keratin – solubilization
30–50% - nail plate for softening the nail prior to avulsion
Podophyllum resin & podofilox -
Are cytotoxic agents - epidermal mitoses are arrested in metaphase
25% concentration in tincture of benzoin - condyloma acuminatum 2–3 hours
0.5% solution or gel (Condylox) - genital condylomas
Toxic symptoms with excessively large application - nausea, vomiting, alterations in
sensorium, muscle weakness, neuropathy with diminished tendon reflexes, coma & death
30

31. KERATOLYTIC AGENTS
Sinecatechins-
15% ointment - topical for external genital and perianal warts in immunocompetent
patients 18 years and older 3times daily not to exceed 16 weeks of therapy
Fluorouracil –
Inhibits thymidylate synthetase activity – interfere synthesis of DNA
Available in 0.5%, 1%, 2%, 4%, and 5% concentrations
Topically for multiple actinic keratoses.
Ingenol mebutate 0.015% gel
Aminolevulinic acid (ALA) 20% topical actinic keratoses
Topical 3% gel of diclofenac
31

32. ANTISEBORRHIC AGENTS
 Ketoconazole 2%
 Salicylic acid 2% aqueous cream
 Corticostroid topical
 Selenium sulphide 2.5%
 Zinc pyrithione 1%
 Sulphur 2%
 Coal tar
32

33. ANTISEBORRHIC AGENTS
33
Common action of these drugs is due to antipityrosporal,
cytostatic, anti-inflammatory activity & antiseptic
activity
Chronic & recurrent cases treatment continue for long
time
Topical steroids (hydrocortisone 1%) as effective as
azoles

34. AGENTS AFFECTING PIGMENTATION
Melanising Agents
Hydroquinone
Monobenzone
Mequinol
Demelanising Agents
Trioxsalen
Methoxsalen
34

35. AGENTS AFFECTING PIGMENTATION
35
Melanising Agents
Hydroquinone –
inhibit tyrosinase thus melanine synthesis,
temporary lightening
2-4% in freckles, post-inflammatory
pigmentation, melasma of pregnancy & due
to OCP
Monobenzone –
Monobenzyl ether of hydroquinone
Causes total, irreversible depigmentation
Mequinol –
Monomethyl ether
Temporary lightening
Demelanising Agents
Trioxsalen –
psoralens used for the repigmentation
in vitiligo
0.6mg/kg 2-3 times/week 2hr before
5-10 min sunlight
Time increased by 2 min daily, max
dose 80mg/day
C/I in porphyria & SLE
Methoxsalen –
Topically 0.1-1% lotion ,oral 20mg/day
for vitiligo
Followed by sunlight/UV exposure
Can cause acute vesicular
photosensitivity reactions

36. SUNSCREENS – Topical medications useful in protecting
against sunlight, absorbs UV light
UVB (280-320nm) – erythema, sunburn, tanning
UVA (320-400nm) – ageing & cancer
SPF (sun protection factor) – is effectiveness in absorbing UV light,
minimal erythema dose with & without sunscreen in a group of normal
36
PABA, its esters & benzophenone (oxy,
dioxy, sulisobenzone) absorbs B region
Dibenzoylmethanes absorbs UVA range
(SLE, drug induced photosensitivity)
Ecamsule – better
Sunshades -reflects UV light
Zinc oxide
Titanium dioxide
Calamine

37. TRICHOGENIC & ANTITRICHOGENIC AGENTS
37
 Minoxidil
 Finasteride
 Bimatoprost
 Eflornithine

38. TRICHOGENIC & ANTITRICHOGENIC AGENTS
38
 Minoxidil – (2-5% solution twice daily)
 Increses blood flow which increses elongation & normalization of hair follicles
 Androgenic alopecia
 Cessation of treatment – hair loss in 4-6months
 Finasteride –(1mg/day for 3-6months)
 5a reductase inhibitor that blocks conversion of testosterone to dihydrotestosterone
 Useful in only men with androgenic alopecia
 Promotes hair growth & prevents further hair loss
 Bimatoprost – prostaglandin analogue 0.03% for hypotrichosis of eyelashes
 Eflornithine –
 Irreversible inhibitor of ornithine decarboxylase for hair growth
 Topical preparation reduces facial hairs in 6 months in women but return back in 8
weeks after treatment stops

39. ANTIPRURITIC AGENTS
39
Doxepin –
Topical 5% cream - utilized in the treatment of pruritus associated with atopic
dermatitis or lichen simplex chronicus
Mechanism of action is unknown but may relate to the potent H1- and H2-receptor
antagonist properties
C/I - untreated narrow-angle glaucoma, tendency to urinary retention
Pramoxine -
1% cream, lotion, or gel used for temporary relief from pruritus associated with mild
eczematous dermatoses

40. AGENTS FOR ACNE
40
 Cleanser – soaps
 Comedolytics – local tretinoin
 Exfoliants(peeling agent) – salicylic
acid
 Sebostatics – oral isotretinoin
 Hormones – cyproterone acetate,
estrogen
 Antibacterial agents –
Local – erythromycin, clindamycin,
azelaic acid, BPO
Systemic –tetracycline, erythromycin,
minocycline, cotrimoxazole
 Mild cases without inflammation –
(topical) tretinoin, adapalene, salicylic
acid, BPO
 Mild cases with inflammation –topical
antibiotics, BPO, or combination of
erythromycin, clindamycin, BPO for 4-
6weeks
 Sever cases with inflammation –
 Topical tretinoin + systemic antibiotics,
 Multinodular cystic acne oral isotretinoin,
 Women reproductive age group COC,
cyproterone acetate

41. AGENTS FOR ACNE
41
Retinoic acid/tretinoin/all-trans-retinoic acid –
Potent comedolytic, promotes lysis of keratinocytes
Increases epidermal cell turnover, prevent photoageing of skin
0.025--0.05% gel or cream for 6- 10 weeks
Adapalene (0.1% gel) -
Synthetic tretinoin- like drug which binds directly to nuclear retinoic acid
receptor
Modulates keratinization and differentiation of follicular
Anti-inflammatory, comedolytic, but less irritating than tretinoin
Tazarotene (0.1% gel) –
Topical retinoid for acne & psoriasis

42. AGENTS FOR ACNE
42
Isotretinoin/13-cis-retinoic acid (1–2 mg/kg) -
 Synthetic retinoid for oral treatment of severe cystic acne that is recalcitrant
to standard therapies (20 weeks)
 Cheilitis, dryness, epistaxis, pruritus, conjunctivitis, paronychia, rise in serum
lipids and intracranial tension, and musculoskeletal symptoms & teratogenic
 So reserved for unresponsive cases of severe acne
Benzoyl peroxide (2.5% or 5%)
 Antimicrobial activity against P acnes & comedolytic effects
 Fixed-combination formulations with 3% erythromycin / 1% clindamycin/ 0.1%
adapalene is available
Azelaic acid (15-20%) –
 A straight-chain saturated dicarboxylic acid effective for
acne vulgaris & acne rosacea

43. AGENTS FOR ACNE
43
Antibiotics –
Topical - Clindamycin, erythromycin & Nadifloxacin - effective against P.acnes
than BPO
Useful in inflamed papules rather than non-inflamed comedones
Systemic - doxycycline (100-200mg) is preferred, minocycline, erythromycin
(500-1000mg) for 4-6 weeks then tapered
long-term systemic antibiotic therapy has risk (intracranial hypertension
after use of tetracyclines for > 2 months)
Cyproterone acetate –
Sebaceous glands are androgen dependent so COC pills can be given for 3-4
months
Cyproterone acetate is potent antiandrogen in place of OC pills

44. AGENTS FOR PSORIASIS
44
 Topical –
Emollients
Keratolytic agents
Cytostatic agents
Glucocorticoids
Calcipotriols, tacalcitol
Retinoids
 Phototherapy –
UVB irradiation with or
without coal tar
UVA irradiation with
psoralens
 Systemic –
Etretinate, acitretin
Immunosuppressants
(methotrexate,
cyclosporine,
mycophenolate mofetil)
Biologic agents
Systemic steroids

45. AGENTS FOR PSORIASIS
45
 Topically applied emollients, keratolytics - symptomatic relief
 Topical corticosteroids are the primary drugs used
 Effective in mild-to-moderate disease & initially even in severe cases
 Most patients respond within 3 weeks
 Therapy is started with a high potency steroid which is substituted
by either weekly application or by a milder preparation
 Systemic therapy with corticosteroids and immunosuppressants is
reserved for severe and refractory case
Psoriasis –
An immunological disorder manifesting as localized or
widespread erythematous scaling lesions or plaques
Excessive epidermal proliferation
Periodic flareups are common
Drug therapy depends on type, location & extend of
lesions
Drugs can diminish the lesions, but can not cure

46. AGENTS FOR PSORIASIS
46
Topical
Corticosteroids
Vit D
analogues
Dithranol Coal tar Retinoids
Calcineurin
Inhibitor
Systemic therapy
 Methotrexate
 Cyclosporine
 Acitretin
 Fumaric acid esters
 Hydroxycarbamide
(hydroxyurea)
 Apremilast
 Tofacitinib

47. AGENTS FOR PSORIASIS
47
 Calcipotriol -
 A synthetic vit D analogue effective topically in plaque psoriasis
 Binds to the intracellular vit D receptor in epidermal keratinocytes and
suppresses their proliferation
 Respond in 4-8 weeks & efficacy is comparable to a moderate potency topical
steroid
 Tazarotene (0.05-0. 1%) gel -
 Synthetic retinoid, a prodrug hydrolysed to tezarotenic acid that exerts
antiproliferative, anti-inflammatory action by binding to the intracellular
retinoic acid receptor
Coal tar – (3% ointment)
 Crude preparation containing many phenolic compounds exerts a phototoxic
action on the skin when exposed to light (UVA) & retards epidermal turnover
 It induces resolution of lesions in majority of cases, but relapses arc common

48. AGENTS FOR PSORIASIS
48
 Dithranol
 Synthetic derivative of chrysarobin, extracted from bark of araroba tree
 Antiproliferative and pro‐apoptotic effects on keratinocytes
 Calcineurin Inhibitors- Tacrolimus (0.03% and 0.1% ointment) and
Pimecrolimus (1% cream)
 Narrow‐band UVB (290–320 nm)
 Induces apoptosis of T cells
 Causes cutaneous immunomodulation by increasing vit D
 Reduces epidermal hyperproliferation
 Induction of keratinocyte apoptosis
 PUVA photochemotherapy -Psoralens + UVA (320-400 nm)
 Psoralens bind to DNA - Activated by UVA - Permanent DNA damage

49. AGENTS FOR PSORIASIS
49
Systemic therapy
 Methotrexate - First line systemic agent in plaque psoriasis
 Cyclosporine - Uncommonly recommended for maintainance treatment
 Acitretin - binds to nuclear receptors of the steroid superfamily &
Reduces keratinocyte proliferation
 Hydroxycarbamide (hydroxyurea) - Used infrequently
 Apremilast – decrease pro-inflammatory mediators & increase
inflammatory mediators
 Tofacitinib - Inhibitor of Janus kinases JAK1 and JAK3, Approved for
psoriatic arthritis

50. AGENTS FOR PSORIASIS
50
TNF‐α
inhibitors
Infliximab
Etanercept
Adalimumab
Certolizumab pegol
Golimumab
IL‐12/IL‐23
p40
inhibitors
Ustekinumab
IL‐17
inhibitors
Brodalumab
Ixekizumab
Secukinumab
IL‐23
inhibitors
Guselkumab
Tildrakizumab
Risankizumab
Biological therapy

51. REFERENCES
 Matthew J. Sewell, Craig N. Burkhart, and Dean S. Morrell, Chapter 70
Dermatological Pharmacology, Goodman & Gilman's the pharmacological basis
of therapeutics. New York: McGraw-Hill: 13th edition;1271.
 Dirk B. Robertson, MD & Howard I. Maibach, MD, Chapter 61 Dermatologic
Pharmacology, Bertram G. Katzung Basic & Clinical Pharmacology 14th
Edition; 1068.
 Pharmacotherapy of common skin disorders and skin pretectives, chapter 69,
Pharmacology and Pharmacotherapeutics, R.S.Satoskar, Nirmala N.Rege,
Raakhi K.Tripathi, Sandhya K. Kamat, 26th edition.
51

52. REFERENCES
 Jain S, Barambhe MS, Jain J, Jajoo UN, Pandey N. Prevalence of skin
diseases in rural Central India: A community-based, cross-sectional,
observational study. J Mahatma Gandhi Inst Med Sci 2016;21:111-5.
 Deepak Dimri, Venkatashiva Reddy B, Amit Kumar Singh, "Profile of Skin
Disorders in Unreached Hilly Areas of North India", Dermatology Research
andPractice, vol. 2016, ArticleID 8608534, 6 pages, 2016. https://doi.org/1
0.1155/2016/8608534
52

53. THANK YOU..!!