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 Lecture
After 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:
   Griseofulvin   Griseofulvin
   Terbinafine   Terbinafine
   Ketoconazole   Ketoconazole
   Fluconazole   Fluconazole
   Itraconazole   Itraconazole
   Topical imidazole creams   Topical imidazole creams
Discuss the characteristics and uses of the different strengths and formulations oftopical steroidsDiscuss the characteristics and uses of the different strengths and formulations oftopical 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 mupirocinDiscuss the origin, characteristics of and indications for mupirocin
Discuss the use of tetracyclines in dermatologyDiscuss the use of tetracyclines in dermatology
Name the uses of the different types of antihistamines (sedating vs non-sedating) indermatologyName the uses of the different types of antihistamines (sedating vs non-sedating) indermatology
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 Discussed1Drugs To Be Discussed1
Antifungals: GriseofulvinAntifungals: Griseofulvin
                       Terbinafin                       Terbinafin
                       Fluconazole                       Fluconazole
                       Itraconazole                       Itraconazole
                       Ketoconazole                       Ketoconazole
Corticosteroids: TopicalCorticosteroids: Topical
                             Systemic                             Systemic
ChloroquineChloroquine
Drugs To Be Discussed2Drugs To Be Discussed2
Retinoids: TopicalRetinoids: Topical
                    Systemic                    Systemic
Benzoyl peroxideBenzoyl peroxide
ShampoosShampoos
BarriersBarriers
Antibiotics: TopicalAntibiotics: Topical
                      Systemic                      Systemic
Antivirals: AcyclovirAntivirals: Acyclovir
                   Podophyllin                   Podophyllin
Antiscabies: Benzoyl benzoateAntiscabies: Benzoyl benzoate
Drugs To Be Discussed3Drugs To Be Discussed3
AntihistaminesAntihistamines
Anti-androgensAnti-androgens
ImiquimodImiquimod
AntifungalsAntifungals
GriseofulvinGriseofulvin
TerbinafinTerbinafin
FluconazoleFluconazole
ItraconazoleItraconazole
KetoconazoleKetoconazole
GriseofulvinGriseofulvin
Only active against dermatophytes(keratolytic fungi)Only active against dermatophytes(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-effectsSome 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: CandidaUsed for: Candida
                   Cryptococcus                   Cryptococcus
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
                                       dermatophytes                                       dermatophytes
KetoconazoleKetoconazole
Broad spectrumBroad spectrum
FungistaticFungistatic
To be taken with mealsTo be taken with meals
Tablets, cream and shampoo availableTablets, cream and shampoo available
Used for: Seborrheic dermatitisUsed for: Seborrheic dermatitis
                   Pityriasis versicolor                   Pityriasis versicolor
                   Candidiasis                   Candidiasis
Side-effects: Liver toxicitySide-effects: Liver toxicity
                         P450 inducer                         P450 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
StrengthsStrengths
Fluorinated vs Non-fluorinatedFluorinated vs Non-fluorinated
Ointments, Creams, Lotions, ShampoosOintments, Creams, Lotions, Shampoos
  
Topical CorticosteroidsTopical Corticosteroids
Ointments: More potentOintments: More potent
                     Penetrates deeper                     Penetrates deeper
                     More atrophy                     More atrophy
Used for:   Dry lesionsUsed for:   Dry lesions
                     Thick lesions                     Thick lesions
                     Thick skin                     Thick skin
Topical CorticosteroidsTopical Corticosteroids
Creams: Less potentCreams: Less potent
                  Penetrates less                  Penetrates less
                  Less atrophy                  Less atrophy
Used for: Acute, thin lesionsUsed for: Acute, thin lesions
                  Moist lesions                  Moist lesions
                  Thin skin (Face, skin folds)                  Thin skin (Face, skin folds)
  
Topical CorticosteroidsTopical Corticosteroids
Lotions: Least potent, least atrophyLotions: 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
ShampoosShampoos
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: Severe                        Long term: Severe
Used once daily, in the morningUsed once daily, in the morning
ChloroquineChloroquine
Indications: Cutaneous lupus erythematosusIndications: Cutaneous lupus erythematosus
                       Porphyria cutanea tarda                       Porphyria cutanea tarda
Side-effects: Corneal deposits (Temporary)Side-effects: Corneal deposits (Temporary)
                         Maculopathy (Permanent)                         Maculopathy (Permanent)
                         Other                         Other
RetinoidsRetinoids
Topical: TretinoinTopical: Tretinoin
                 Adapalene                 Adapalene
                 Tazarotene                 Tazarotene
Comedolytic, anti-inflammatoryComedolytic, anti-inflammatory
Indications: Acne (All forms)Indications: Acne (All forms)
                      Anti-aging                      Anti-aging
                      Other                      Other
RetinoidsRetinoids
Systemic: IsotretinoinSystemic: Isotretinoin
                   Acitretin                   Acitretin
Indications: AcneIndications: Acne
                      Psoriasis                      Psoriasis
                      Lymphomas                      Lymphomas
                      Many others                      Many others
Side-effects, etc: See acne lectureSide-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 versicolor                           Pityriasis versicolor
                           (Not for tinea capitis)                           (Not 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: MupirocinTopical: Mupirocin
                 Fucidic acid                 Fucidic acid
                 Gentamycin                 Gentamycin
                 Erythromycin                 Erythromycin
                 Clindamycin                 Clindamycin
Systemic: Tetracyclines (oxytetracycline,doxycycline, minocycline, lymecycline)Systemic: Tetracyclines (oxytetracycline,doxycycline, minocycline, lymecycline)
                    Penicillins (amoxycillin, cloxacillin,amoxycillin-clavulanic acid                    Penicillins (amoxycillin, cloxacillin,amoxycillin-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 effects                                               inflammatory 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-Clavulanic acid: Staph infectionsCloxacillin, Flucloxacillin, Amoxycillin-Clavulanic acid: Staph infections
Amoxycillin, erythromycin: Strep infectionsAmoxycillin, erythromycin: Strep infections
AntiviralsAntivirals
Acyclovir: Cream, tablets and IVAcyclovir: Cream, tablets and IV
Used for: Herpes simplex and 2Used for: Herpes simplex and 2
                   Herpes zoster                   Herpes zoster
              (Cream useless on skin)              (Cream useless on skin)
Side-effects: Practically noneSide-effects: Practically none
Podophyllin: 25% in TBCo: Used forcondylomata acuminata and verrucaePodophyllin: 25% in TBCo: Used forcondylomata acuminata and verrucae
AntiscabiesAntiscabies
Benzoyl benzoateBenzoyl benzoate
Only effective treatment for scabiesOnly effective treatment for scabies
Method of use: See lecture on skininfectionsMethod of use: See lecture on skininfections
AntihistaminesAntihistamines
Sedating: PromethazineSedating: Promethazine
                   Chlorpheniramine                   Chlorpheniramine
                   Hydroxyzine (Aterax®)                   Hydroxyzine (Aterax®)
AntihistaminesAntihistamines
Sedating: PromethasineSedating: Promethasine
                   Chlorpheniramine                   Chlorpheniramine
                   Hydroxyzine (Aterax®)                   Hydroxyzine (Aterax®)
Used for: Atopic dermatitisUsed for: Atopic dermatitis
                   Acute urticaria                   Acute urticaria
                   Other forms of night-time pruritus                   Other forms of night-time pruritus
  
AntihistaminesAntihistamines
Sedating: PromethasineSedating: Promethasine
                   Chlorpheniramine                   Chlorpheniramine
                   Hydroxyzine (Aterax®)                   Hydroxyzine (Aterax®)
Used for: Atopic dermatitisUsed for: Atopic dermatitis
                   Acute urticaria                   Acute urticaria
                   Other forms of night-time pruritus                   Other forms of night-time pruritus
Side-effects: Sedation (NB: Driving)Side-effects: Sedation (NB: Driving)
                        Photo-allergy (not hydroxyzine)                        Photo-allergy (not hydroxyzine)
                        Dry mouth                        Dry mouth
AntihistaminesAntihistamines
Non-sedating: LoratidineNon-sedating: Loratidine
                          Cetirizine                          Cetirizine
                          Desloratidine                          Desloratidine
                          Levocetirizine                          Levocetirizine
Used for: Acute and chronic urticariaUsed for: Acute and chronic urticaria
                   Allergic rhinitis                   Allergic rhinitis
Side-effects: Almost noneSide-effects: Almost none
Anti-androgensAnti-androgens
Cyproterone acetateCyproterone acetate
       Progestogen, blocks 5α-reductase       Progestogen, blocks 5α-reductase
       2mg in Diane-35®       2mg in Diane-35®
       10mg in Androcur       10mg in Androcur
       Used mostly for acne       Used mostly for acne
       Side-effects: Depression, weight gain       Side-effects: Depression, weight gain
DrosperinoneDrosperinone
       Ingredient of Yasmin®       Ingredient of Yasmin®
Imiquimod (Aldara®)Imiquimod (Aldara®)
Topical immunostimulantTopical immunostimulant
Used for condylomata acuminataUsed for condylomata acuminata
                  Superficial spreading basal cell CA                  Superficial spreading basal cell CA
Side-effects: Severe local inflammationSide-effects: Severe local inflammation