DermatopharmacologyDermatopharmacology

Prof Werner SinclairProf Werner Sinclair

Department of DermatologyDepartment of Dermatology

University of the Free StateUniversity of the Free State

Outcomes for this LectureOutcomes for this LectureAfter this lecture the student should be able to:After this lecture the student should be able to:

  

Name the most important characteristics and uses of the following antifungals: Name the most important characteristics and uses of the following antifungals:

GriseofulvinGriseofulvin

TerbinafineTerbinafine

KetoconazoleKetoconazole

FluconazoleFluconazole

ItraconazoleItraconazole

Topical imidazole creamsTopical imidazole creams

Discuss the characteristics and uses of the different strengths and formulations of Discuss the characteristics and uses of the different strengths and formulations of topical steroids topical steroids

Name the indications for and most important side-effects of chloroquineName the indications for and most important side-effects of chloroquine

Discuss the indications and use of topical retinoidsDiscuss the indications and use of topical retinoids

Discuss the origin, characteristics of and indications for mupirocin Discuss the origin, characteristics of and indications for mupirocin

Discuss the use of tetracyclines in dermatology Discuss the use of tetracyclines in dermatology

Name the uses of the different types of antihistamines (sedating vs non-sedating) in Name the uses of the different types of antihistamines (sedating vs non-sedating) in dermatologydermatology

Name the indications for and side-effects of anti-androgens and imiquimodName the indications for and side-effects of anti-androgens and imiquimod

Drugs To Be DiscussedDrugs To Be Discussed11

Antifungals: GriseofulvinAntifungals: Griseofulvin TerbinafinTerbinafin FluconazoleFluconazole ItraconazoleItraconazole KetoconazoleKetoconazole

Corticosteroids: TopicalCorticosteroids: Topical SystemicSystemic

ChloroquineChloroquine

Drugs To Be DiscussedDrugs To Be Discussed22

Retinoids: Topical Retinoids: Topical SystemicSystemic

Benzoyl peroxideBenzoyl peroxideShampoosShampoosBarriersBarriersAntibiotics: TopicalAntibiotics: Topical

SystemicSystemicAntivirals: AcyclovirAntivirals: Acyclovir

PodophyllinPodophyllinAntiscabies: Benzoyl benzoateAntiscabies: Benzoyl benzoate

Drugs To Be DiscussedDrugs To Be Discussed33

AntihistaminesAntihistamines

Anti-androgensAnti-androgens

ImiquimodImiquimod

AntifungalsAntifungals

GriseofulvinGriseofulvin

TerbinafinTerbinafin

FluconazoleFluconazole

ItraconazoleItraconazole

KetoconazoleKetoconazole

GriseofulvinGriseofulvin

Only active against dermatophytes Only active against dermatophytes (keratolytic fungi)(keratolytic fungi)

FungistaticFungistatic

Absorbed with fatty food (milk)Absorbed with fatty food (milk)

Very safe in childrenVery safe in children

10 – 20 mg per kg per day10 – 20 mg per kg per day

TerbinafinTerbinafin

Only active against dermatophytesOnly active against dermatophytes

FungicidalFungicidal

Tablets and creamTablets and cream

Some severe immunological side-effects Some severe immunological side-effects

FluconazoleFluconazole

Broad spectrumBroad spectrum

FungistaticFungistatic

Convenient once per week dosageConvenient once per week dosage

Can be used in neonatesCan be used in neonates

Used for: Candida Used for: Candida

CryptococcusCryptococcus

ItraconazoleItraconazole

Very broad spectrumVery broad spectrum

FungistaticFungistatic

To be taken with mealsTo be taken with meals

Capsules and suspension availableCapsules and suspension available

Used for: Any fungal infectionUsed for: Any fungal infection

Not better than terbinafin for Not better than terbinafin for

dermatophytesdermatophytes

KetoconazoleKetoconazole

Broad spectrumBroad spectrumFungistaticFungistaticTo be taken with mealsTo be taken with mealsTablets, cream and shampoo availableTablets, cream and shampoo availableUsed for: Seborrheic dermatitisUsed for: Seborrheic dermatitis

Pityriasis versicolorPityriasis versicolor CandidiasisCandidiasis

Side-effects: Liver toxicitySide-effects: Liver toxicity P450 inducerP450 inducer

Imidazole CreamsImidazole Creams

Variety available

Similar spectra

Little to choose

Price deciding factor

E.g.. Ketoconazole, econazole, clotrimazole

CorticosteroidsCorticosteroids

TopicalTopical

SystemicSystemic

Topical CorticosteroidsTopical Corticosteroids

3 Strengths3 Strengths

Fluorinated vs Non-fluorinated Fluorinated vs Non-fluorinated

Ointments, Creams, Lotions, ShampoosOintments, Creams, Lotions, Shampoos

Topical CorticosteroidsTopical Corticosteroids

Ointments: More potentOintments: More potent

Penetrates deeperPenetrates deeper

More atrophy More atrophy

Used for: Dry lesionsUsed for: Dry lesions

Thick lesions Thick lesions

Thick skinThick skin

Topical CorticosteroidsTopical Corticosteroids

Creams: Less potentCreams: Less potent

Penetrates lessPenetrates less

Less atrophyLess atrophy

Used for: Acute, thin lesionsUsed for: Acute, thin lesions

Moist lesionsMoist lesions

Thin skin (Face, skin folds)Thin skin (Face, skin folds)

Topical CorticosteroidsTopical Corticosteroids

Lotions: Least potent, least atrophy Lotions: Least potent, least atrophy

Used for: Hairy areas (scalp)Used for: Hairy areas (scalp)

Wet lesions (Watery solutions)Wet lesions (Watery solutions)

Topical CorticosteroidsTopical Corticosteroids

Shampoos Shampoos

Clobetasol: Used for psoriasis of the scalpClobetasol: Used for psoriasis of the scalp

Systemic CorticosteroidsSystemic Corticosteroids

Prednisone / PrednisolonePrednisone / Prednisolone

Potent, fast acting anti-inflammatoryPotent, fast acting anti-inflammatory

CheapCheap

Side-effects: Short term: Almost noneSide-effects: Short term: Almost none

Long term: SevereLong term: Severe

Used once daily, in the morningUsed once daily, in the morning

ChloroquineChloroquine

Indications: Cutaneous lupus erythematosusIndications: Cutaneous lupus erythematosus

Porphyria cutanea tardaPorphyria cutanea tarda

Side-effects: Corneal deposits (Temporary)Side-effects: Corneal deposits (Temporary)

Maculopathy (Permanent)Maculopathy (Permanent)

OtherOther

RetinoidsRetinoids

Topical: TretinoinTopical: Tretinoin

AdapaleneAdapalene

TazaroteneTazarotene

Comedolytic, anti-inflammatoryComedolytic, anti-inflammatory

Indications: Acne (All forms)Indications: Acne (All forms)

Anti-agingAnti-aging

OtherOther

RetinoidsRetinoids

Systemic: IsotretinoinSystemic: Isotretinoin

AcitretinAcitretin

Indications: AcneIndications: Acne

PsoriasisPsoriasis

LymphomasLymphomas

Many othersMany others

Side-effects, etc: See acne lecture Side-effects, etc: See acne lecture

Benzoyl peroxideBenzoyl peroxide

Comedolytic, antisepticComedolytic, antiseptic

Gel / CreamGel / Cream

Superficial, inflammatory acne vulgarisSuperficial, inflammatory acne vulgaris

ShampoosShampoos

Ketoconazole: Seborrheic dermatitisKetoconazole: Seborrheic dermatitis

Pityriasis versicolorPityriasis versicolor

((Not for tinea capitisNot for tinea capitis))

Coal tar (LPC): PsoriasisCoal tar (LPC): Psoriasis

Povidone iodine (Betadine)Povidone iodine (Betadine)

Selenium sulfide (Selsun)Selenium sulfide (Selsun)

Zinc pyrithioneZinc pyrithione

BarriersBarriers

Zinc/Castor oil BP: Nappy rashZinc/Castor oil BP: Nappy rash

AntibioticsAntibiotics

Topical: Topical: MupirocinMupirocin Fucidic acidFucidic acid GentamycinGentamycin ErythromycinErythromycin ClindamycinClindamycin

Systemic: Systemic: TetracyclinesTetracyclines (oxytetracycline, (oxytetracycline, doxycycline, minocycline, lymecycline)doxycycline, minocycline, lymecycline)

PenicillinsPenicillins (amoxycillin, cloxacillin, (amoxycillin, cloxacillin, amoxycillin-clavulanic acidamoxycillin-clavulanic acid

Erythromycin Erythromycin

MupirocinMupirocin

Manufactured by Pseudomonas bacteriaManufactured by Pseudomonas bacteria

Broad spectrumBroad spectrum

Esp effective against StaphylococciEsp effective against Staphylococci

Ointment and creamOintment and cream

No systemic useNo systemic use

Reserved for short term useReserved for short term use

TetracyclinesTetracyclines

Bacteriostatic antibiotics, potent anti- Bacteriostatic antibiotics, potent anti-

inflammatory effectsinflammatory effects

Used widely in acne, rosacea, bullous diseasesUsed widely in acne, rosacea, bullous diseases

Oxytetracycline: RosaceaOxytetracycline: Rosacea

Lymecycline: Drug of choice for acneLymecycline: Drug of choice for acne

Minocycline: Acne in white patients (pigmentation)Minocycline: Acne in white patients (pigmentation)

Doxycycline: Acne in black patients (phototoxicity)Doxycycline: Acne in black patients (phototoxicity)

PenicillinsPenicillins

Cloxacillin, Flucloxacillin, Amoxycillin-Cloxacillin, Flucloxacillin, Amoxycillin-Clavulanic acid: Staph infectionsClavulanic acid: Staph infections

Amoxycillin, erythromycin: Strep infectionsAmoxycillin, erythromycin: Strep infections

AntiviralsAntivirals

Acyclovir: Cream, tablets and IVAcyclovir: Cream, tablets and IVUsed for: Herpes simplex 1 and 2Used for: Herpes simplex 1 and 2

Herpes zosterHerpes zoster (Cream useless on skin)(Cream useless on skin)

Side-effects: Practically none Side-effects: Practically none

Podophyllin: 25% in TBCo: Used for Podophyllin: 25% in TBCo: Used for condylomata acuminata and verrucaecondylomata acuminata and verrucae

AntiscabiesAntiscabies

Benzoyl benzoateBenzoyl benzoate

Only effective treatment for scabies Only effective treatment for scabies

Method of use: See lecture on skin Method of use: See lecture on skin infectionsinfections

AntihistaminesAntihistamines

Sedating: PromethazineSedating: Promethazine

ChlorpheniramineChlorpheniramine

Hydroxyzine (AteraxHydroxyzine (Aterax®®))

AntihistaminesAntihistamines

Sedating: PromethasineSedating: Promethasine

ChlorpheniramineChlorpheniramine

Hydroxyzine (AteraxHydroxyzine (Aterax®®) )

Used for: Atopic dermatitisUsed for: Atopic dermatitis

Acute urticariaAcute urticaria

Other forms of night-time pruritusOther forms of night-time pruritus

AntihistaminesAntihistamines

Sedating: PromethasineSedating: Promethasine ChlorpheniramineChlorpheniramine Hydroxyzine (AteraxHydroxyzine (Aterax®®) )

Used for: Atopic dermatitisUsed for: Atopic dermatitis Acute urticariaAcute urticaria Other forms of night-time pruritusOther forms of night-time pruritus

Side-effects: Sedation (NB: Driving)Side-effects: Sedation (NB: Driving) Photo-allergy (not hydroxyzine)Photo-allergy (not hydroxyzine) Dry mouthDry mouth

AntihistaminesAntihistamines

Non-sedating: LoratidineNon-sedating: Loratidine

CetirizineCetirizine

DesloratidineDesloratidine

LevocetirizineLevocetirizine

Used for: Acute and chronic urticariaUsed for: Acute and chronic urticaria

Allergic rhinitis Allergic rhinitis

Side-effects: Almost none Side-effects: Almost none

Anti-androgensAnti-androgens

Cyproterone acetateCyproterone acetate Progestogen, blocks 5Progestogen, blocks 5αα-reductase-reductase 2mg in Diane-35®2mg in Diane-35® 10mg in Androcur10mg in Androcur Used mostly for acneUsed mostly for acne Side-effects: Depression, weight gainSide-effects: Depression, weight gain

DrosperinoneDrosperinone Ingredient of YasminIngredient of Yasmin®®

Imiquimod (AldaraImiquimod (Aldara®)®)

Topical immunostimulantTopical immunostimulant

Used for condylomata acuminataUsed for condylomata acuminata

Superficial spreading basal cell CASuperficial spreading basal cell CA

Side-effects: Severe local inflammationSide-effects: Severe local inflammation