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Table 652 Vehicles for Topically Applied Drugs CREAM Physical basis Oil in water emulsion OINTMENT Water

in oil GEL/FOAM Water-soluble emulsion LOTION/SOLUTION/FOAM Solution-dissolved drug base Lotion-suspended drug Aerosol propellant with drug Foam drug with surfactant as foaming agent and propellant May be aqueous or alcoholic

Solubilizing medium Pharmacological advantage Advantages for patient

>31% water (up to 80%) Leaves concentrated drug at skin surface Spreads and removes easily No greasy feel

<25% water Protective oil film on skin Spreads easily Slows water evaporation Gives a cooling effect Avoid intertriginous areas Greasy to very greasy Stains clothes Moderate to high Increases skin moisture Needs surfactants to prevent phase separation Hydrocarbon (VASELINE)

Contains water- soluble polyethylene glycols Concentrates drug at surface after evaporation Nonstaining Greaseless Clear appearance Foams well for scalp and other hairy locations Needs preservatives High alcohol can be drying

Low residue on scalp

Locations on body Disadvantages Occlusion Composition issues

Most locations Needs preservatives Low Requires humectants (glycerine, propylene glycol, polyethylene glycols) to keep moist when applied Oil phase with long-chain alcohol for stability and smooth feel Has absorption bases hydrophilic petrolatum

Solutions and foams are well accepted on scalp

Microspheres or microsponges can be formulated in gels

Mechanism of Action for Selected Cytotoxic and Immunosuppressive Drugs Methotrexate Azathioprine Fluorouracil Cyclophosphamide Carmustine Cyclosporine Tacrolimus Pimecrolimus Mycophenolate mofetil Imiquimod Vinblastine Bleomycin Dapsone Thalidomide Dihydrofolate reductase inhibitor Purine synthesis inhibitor Blocks methylation in DNA synthesis Alkylates and cross-links DNA Cross-links in DNA and RNA Calcineurin inhibitor Calcineurin inhibitor Calcineurin inhibitor Inosine monophosphate dehydrogenase inhibitor Interferon-alpha induction Inhibits microtubule formation Induction of DNA strand breaks Inhibits neutrophil migration, oxidative burst Cytokine modulation

Mechlorethamine hydrochloride Alkylating agent

Table 658 Recommended Cutaneous Antifungal Therapy CONDITION Tinea corporis, localized Tinea corporis, widespread Tinea pedis Onychomycosis Candidiasis, localized Tinea versicolor, localized Tinea versicolor, widespread TOPICAL THERAPY ORAL THERAPY Azoles, allylamines Azoles, allylamines Azoles Azoles, allylamines Ketoconazole, itraconazole, fluconazole Griseofulvin, terbinafine, itraconazole, fluconazole Griseofulvin, terbinafine, itraconazole, fluconazole Griseofulvin, terbinafine, itraconazole, fluconazole Ketoconazole, itraconazole, fluconazole

Candidiasis, widespread and mucocutaneous

Biological Agents Commonly Used in Dermatology DRUG Structural class Components ALEFACEPT EFALIZUMAB ADALIMUMAB Human monoclonal antibody ETANERCEPT Receptor-antibody fusion protein p75 TNF receptor and Fc IgG1 INFLIXIMAB Chimeric monoclonal antibody Variable region of mouse monoclonal antibody on human IgG1

Receptor- antibody Humanized monoclonal fusion protein antibody LFA-3 and Fc IgG1

Complementarity IgG1 determining region of mouse monoclonal antibody on human IgG1 CD11a subunit of LFA-1 TNFSC SC

Binding site Method of administration Dosing for psoriasis

CD2 IM

TNFSC

TNFIV 5 mg/kg at weeks 0, 2, and 6, then every 6-8 weeks

15 mg weekly x 12 0.7 mg/kg first week, weeks, stop 12 then 1 mg/kg weekly weeks, then repeat

80-mg loading dose, then 40 mg 50 mg twice weekly x 3, biweekly months then 50 mg weekly

FDA indications

Moderate- severe psoriasis

Moderate-severe psoriasis;

Moderate-severe psoriasis; moderate-severe psoriatic arthritis; adult and juvenile rheumatoid arthritis; ankylosing spondylitis; Crohn's disease B 53%

Moderate-Severe psoriasis; moderate- severe arthritis; adult and juvenile rheumatoid arthritis; ankylosing spondylitis B 47%

Severe psoriatic moderatesevere psoriatic arthritis; adult rheumatoid arthritis; Ankylosing spondylitis; ulcerative colitis; Crohn's disease B 76-80%

Pregnancy category Efficacy in psoriasisa

B 28-33%

C 27-39%

Agents Used for the Treatment of Pruritus Pruritoceptive Pruritus: Itch originating in the skin due to inflammation or other cutaneous disease EmollientsRepair of barrier function Coolants (menthol, camphor, calamine)Counter-irritants CapsaicinCounter-irritant AntihistaminesInhibit histamine-induced pruritus Topical steroidsDirect anti-pruritic and anti-inflammatory effects Topical immunomodulatorsAnti-inflammatories PhototherapyReduced mast cell reactivity and anti-inflammatory effects ThalidomideAnti-inflammatory through suppression of excessive tumor necrosis factor-

Neuropathic Pruritus: Itch due to disease of afferent nerves CarbamazepineBlockade of synaptic transmission and use-dependant sodium channels GabapentinSuppresses neuronal hyperexcitability by inhibiting voltage-dependant calcium channels Topical anesthetics (EMLA, benzocaine, pramoxine)Inhibit nerve conduction via decreased nerve membrane permeability to sodium Neurogenic Pruritus: Itch that arises from the nervous system without evidence of neural pathology ThalidomideCentral depressant Opioid-receptor antagonists (naloxone, naltrexone)Decrease opioidergic tone Tricyclic antidepressantsDecrease pruritus signaling through alteration in neurotransmitter concentrations Selective serotonin reuptake inhibitors (SSRIs)Decrease pruritus signaling through alteration in neurotransmitter concentrations Psychogenic Pruritus: Itch due to psychological illness Anxiolytics (alprazolam, clonazepam, benzodiazepines)Relieve stress-reactive pruritus Antipsychotic agents (chlorpromazine, thioridazine, thiothixene, olanzapine)Relieve pruritus with impulsive qualities Tricyclic antidepressantsRelieve depression and insomnia related to pruritus SSRIsRelieve pruritus with compulsive qualities

Potency of Selected Topical Glucocorticoids

CLASS OF DRUGa GENERIC NAME, FORMULATION 1

TRADE NAME

Betamethasone dipropionate cream, ointment 0.05% (in optimized vehicle) DIPROLENE Clobetasol propionate cream, ointment 0.05% Diflorasone diacetate, ointment 0.05% Halobetasol propionate, ointment 0.05%
TEMOVATE PSORCON ULTRAVATE CYCLOCORT DIPROSONE, TOPICORT FLORONE, MAXIFLOR LIDEX, LIDEX-E, FLUONEX HALOG, HALOG-E DIPROSONE, BETATREX,

Amcinonide, ointment 0.1% Betamethasone dipropionate, ointment 0.05% Desoximetasone, cream, ointment 0.25%, gel 0.05% Diflorasone diacetate, ointment 0.05% Fluocinonide, cream, ointment, gel 0.05% Halcinonide, cream, ointment 0.1%

others

Betamethasone dipropionate, cream 0.05% Betamethasone valerate, ointment 0.1% Diflorasone diacetate, cream 0.05% Triamcinolone acetonide, ointment 0.1%, cream 0.5%

others

others others

FLORONE, MAXIFLOR ARISTOCORT A, CYCLOCORT TOPICORT LP SYNALAR-HP SYNALAR

Amcinonide, cream 0.1% Desoximetasone, cream 0.05% Fluocinolone acetonide, cream 0.2% Fluocinolone acetonide, ointment 0.025% Flurandrenolide, ointment 0.05%, tape 4 Hydrocortisone valerate, ointment 0.2% g/cm
2

CORDRAN

WESTCORT

Triamcinolone acetonide, ointment 0.1% Mometasone furoate, cream, ointment 0.1% 5 Betamethasone dipropionate, lotion 0.05% Betamethasone valerate, cream, lotion 0.1% Fluocinolone acetonide, cream 0.025% Flurandrenolide, cream 0.05% Hydrocortisone butyrate, cream 0.1% Hydrocortisone valerate, cream 0.2% Triamcinolone acetonide, cream, lotion 0.1% Triamcinolone acetonide, cream 0.025% 6 Alclometasone dipropionate, cream, ointment 0.05% Desonide, cream 0.05% Fluocinolone acetonide, cream, solution 0.01% 7 Dexamethasone sodium phosphate, cream 0.1% Hydrocortisone, cream, ointment, lotion 0.5%, 1.0%, 2.5%

KENALOG, ARISTOCORT ELOCON DIPROSONE, BETATREX, SYNALAR CORDRAN SP LOCOID WESTCORT KENALOG ARISTOCORT ACLOVATE TRIDESILON, DESOWEN SYNALAR DECADRON HYTONE, NUTRICORT, PENECORT

others

others

Class 1 is most potent; class 7 is least potent.