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Skin Drugs
Skin Drugs
54
Pharmacology
Professional
03/26/2012

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Term
Bacitracin
Definition
Antibiotic, inhibits dephos of bactoprenol which transfers peptidoglycan subunits to the cell wall (cell wall synth)
Decreases concentration of Staph, suppresses infection of wounds, and can be dissolved in saline to irrigate joints or pleural cavity.
Term
Clindamycin
Definition
Antibiotic, binds the 50S ribosome subunit. Works against Propionibacterium acnes (acne infection).
Adv effects of skin irritation or bloody diarrhea/pseudomembraneous colitis (rare, due to systemic absorption)
Term
Erythromycin
Definition
Antibiotic, binds the 50S ribosome subunit. Eliminates P. acnes.
Resistance by active efflux of drug, enzyme inactivation, or mod of receptor binding site.
Adv effects: development of resistant bac, skin reactions.
Term
Gentamycin
Definition
Antibiotic, binds to 30S sub of ribosome
Effective against Gm- bac, especially Pseudomonas and also Staph and Strep. Treats infected wounds, burns, and IV cath infections.
Not for widespread use.
Term
Gramicidin
Definition
Antibiotic, forms stationary ion channels through the cell mem of susceptible bac.
Topical admin for some bac.
Term
Metronidazole
Definition
Kills Demodex brevis (paracitic face mite). Causes loss of DNA helical structure and strand breakage. Also inhibits neutrophil function (anti-inflammatory, Rx rosacea).
Adv effects: skin rxns, avoid eyes, dont give in pregnancy.
Term
Mupirocin
Definition
Antibiotic, inhibits isoleucyl tRNA synthase. Treats Staph skin infections and nasal carriage (effective against MRSA).
Resistance due to point mutations of target enzyme (low level) or plasma encoded alternate enzyme (high level)
Used only in small areas to avoid development of resistance.
Term
Neomycin
Definition
Antibiotic, binds to 30S subunit of ribosome.
Effective against Gm- bacteria (E. coli, Klebsiella, Enterobacter). Treats infected surfaces.
Can cause cross-sensitivity to other drugs. Not for widespread use.
Term
Sodium Sulfacetamide
Definition
Antibiotic, inhibits PABA (an int in bac folate synth) utilization. Effective against P. acnes.
Adv effects: local rxn, sulfur allergy.
Term
Acyclovir
Definition
Antiviral, Anti herpes. Oral/topical
Requires phos by viral thymidine kinase to become active. Also some anti-VZV effect (10x less potent)
Irreversibly binds viral DNA template during replication and causes termination.
Resistance: mutated thymidine kinase, mutated DNA Pol, low levels of thymidine kinase
Adverse effects: renal tox (crystallopathy if not well hydrated and given IV), neurotox (IV admin)
Term
Docosanol
Definition
Antiviral, topical cream treats herpes infection. Inhibits fusion of viral membrane with host cell (preventing entry of virus)
Term
Penciclovir
Definition
Antiviral, Anti-herpes
Topical admin
For recurrent herpes labalis infection
Adv effect: application site rxn
Term
Imiquimod
Definition
Antiviral, treats genital warts, topical admin. Also treats primary basal cell carcinoma.
Stimulates release of IFN-alpha, TNF-alpha, IL-1, 6, and 8.
Adv effect: local rxn, fatigue, flu-like symptoms
Term
Tacrolimus
Definition
Macrolide Immunosuppressant, forms complex with FK506 bp and inhibits calcineurin. Treats atopic dermatitis
Adv effects: burning sensation on application with prolonged use, Black Box warning b/c of teratogenic effects in animals
Do not use with occlusive dressings
Term
Pimecrolimus
Definition
Macrolide immunosupppressant, forms complex with FK506 bp and inhibits calcineurin. Treats atopic dermatitis.
Adv effects: burning sensation on application with prolonged use, Black Box warning b/c of teratogenic effects in animals
Don't use with occlusive dressings
Term
Hydroquinone
Definition
Inhibits tyrosinase, blocking the formation of melanin, causes temporary lightening of the skin.
Term
Monobenzone
Definition
Inhibits tyrosinase, blocking the formation of melanin, causes irreversible depigmentation due to death of melanocytes.
Adv effects: depigmentation of sites distant from area of application
Term
Mequinol
Definition
Inhibits tyrosinase, blocking the formation of melanin, causes temporary lightening of the skin
Term
Trioxsalen
Definition
For repigmentation. Oral and topical admin. Photoactivation by two mechanisms: Type 1 (O2 independent addition to pyrimidine bases) and Type 2 (O2 dependent creation of radical oxygen species) Stimulates melanocyte pigmentation and anti-inflammatory.
Treats vitiligo (requires many treatments)
Adv effects: GI and CNS disturbances, bronchoconstriction, CHF, photoaging, skin cancer
Term
Methoxsalen
Definition
For repigmentation. Oral and topical admin. Photoactivation by two mechanisms: Type 1 (O2 independent addition to pyrimidine bases) and Type 2 (O2 dependent creation of radical oxygen species) Stimulates melanocyte pigmentation and anti-inflammatory.
Treats psoriasis vitiligo (both require many treatments). Also treats T-Cell Leukemia by Extracorporeal Photopheresis (blood has drug added, exposed to light, then returned to Pt)
Adv effects: GI and CNS disturbances, bronchoconstriction, CHF, photoaging, skin cancer.
Term
Adapalene
Definition
Acne medication (retinoid), Reduces hyperkeratinization that leads to microcomedone formation, the
initial lesion of acne. Requires several months of therapy
Term
Tretinoin
Definition
Acne treatment (retinoid), Reduces hyperkeratinization that leads to microcomedone formation, the
initial lesion of acne.
Requires several months of therapy.
Term
Isotretinoin
Definition
Retinoid, treats moderate-severe acne vulgaris. Normalizes keratinization in sebaceous follicle, decr sebum synth, decr P. acnes. High doses treat skin cancer.
Adv effects: Can cause cheilosis and dry mucus membranes
DONT give in pregnancy
Term
Tazarotene
Definition
Retinoid, treats acne and psoriasis (along with corticosteroids) Effective in some basal cell carcinomas.
Adv effects: skin irritation
Term
Azelaic Acid
Definition
Antimbac against P. acnes and inhibits testosterone conversion to DHT. Tx for acne vulgaris and acne rosacea.
Term
Benzoyl Peroxide
Definition
Tx for acne, releases free radicals which oxidize bac proteins in sebaceous glands. Enters skin unchanged then is converted to active benzoic acid.
Term
Acitretin
Definition
Retinoid (blocks retinoic acid receptor (RAR) and Retinoid X Receptor (RXR), treats psoriasis, needs 3-6 months of therapy.
Adv effects: dry skin and mucus mem, hair thinning
Term
Alefacept
Definition
Fusion protein consisting of the extracellular CD2-binding portion of the (LFA-3) linked to the Fc portion of human IgG. Blocks CD2 receptor preventing psoriasis associated activation of T-cells.
Treats moderate-severe plaque psoriasis.
Adv effects: incr risk of malignancy, lymphopenia. CD4 T-Cell levels should be monitored.
Term
Efalizumab
Definition
Recombinant IgG antibody, blocks LFA-1 on T-Cell, blocking its interaction with the APC and preventing T-cell activation.
Treatment of Psoriasis.
Adv effects: thrombocytopenia, rebound psoriasis on discontinuation.
Term
Calcipotriene
Definition
Vitamin D analog. Similar effects as the retinoids. Treatment of psoriasis.
Adv effects: hypocalcemia and hypercalciurea.
Term
Adalimumab
Definition
TNF inhibitor for treatment of psoriasis
Term
Etanercept
Definition
TNF inhibitor for treatment of psoriasis
Term
Infliximab
Definition
TNF inhibitor for treatment of psoriasis
Term
Methotrexate
Definition
Treatment of moderate-severe psoriasis and a lot of other skin conditions including cutaneus T-Cell lymphoma.
Inhibits Dihydrofolate Reductase, blocking DNA synthesis and repair.
Term
Azathioprine
Definition
Treatment of psoriasis and other inflammatory skin disorders. Purine antimetabolite: converted to mercaptopurine.
Term
Cyclosporine
Definition
Tx of Psoriasis. Calcineurin inhibitor
Term
Mycophenolate Mofetil
Definition
Tx of psoriasis and auto-immune blistering disorders. Inhibits inosine monophosphate deH which is involved in de novo guanosine synth. Inhibits B and T cell prolif since they are dependent on de novo synth path
Term
Coal Tar
Definition
Antipuretic, good alternative to topical corticosteroids. Treats psoriasis, dermatitis, and lichen simplex chronicus.
Avoid use in acute dermatitis with vesiculation and swelling.
Term
Salicylic acid
Definition
Keratolytic compound, MOA poorly understood. May solubilize cell surface proteins that keep the stratum corneum intact resulting in desquamation.
Adv effects: salicylism in children, not good for extremities of diabetics.
Term
Propylene Glycol
Definition
Keratolytic agent, increases water content of the stratum corneum.
Term
Urea
Definition
Causes alterations in keratin leading to increased solubilization, increased water content of the stratum corneum, and keratolytic effects.
Term
Podophyllum Resin
Definition
Binds to microtubules of mitotic spindle causing cytotoxic effect. Effective against condyloma acuminatum (Genital warts). Should be washed off 2-3 hours after application.
Adv effects: excessive application can cause muscle weakness, neuropathy, coma , and death. Dont give if pregnant.
Term
Fluorouracil
Definition
Inhibits thymidylate synthase. Treats acne keratitis. Must avoid excessive exposure to sunlight while taking it.
Term
Aminolevulinic Acid
Definition
Induces type 2 photochemical rxn causing formation of radical oxygen species.
Treats precancerous actinic keratosis, acne, and thin non-melanoma skin cancers.
MUST avoid sunlight or bright indoor lights for at least 40 hours after application.
Term
Methylaminolevulinate
Definition
Induces type 2 photochemical rxn causing formation of radical oxygen species.
Treats precancerous actinic keratosis, acne, and thin non-melanoma skin cancers.
MUST avoid sunlight or bright indoor lights for at least 40 hours after application.
Term
Vorinostat
Definition
Inhibits histone deacetylase enzymes, inhibiting gene expression, blocking cell growth and activating apoptosis.
Treats persistent T-cell lymphoma.
Adv effects: pulm edema, DVT, anemia
Term
Cyclophosphomide
Definition
Alkylating Agent, converted to active nitrogen mustard that forms a bridge between 2 strands of DNA and blocks transcription and translation
MOR: incr activity of enzymes that reseal DNA strand breaks.
Toxicity: nephrotoxic, hemorrhagic, permanent amenorrhea and azoospermia, can cause leukemia, cardiotoxic, bladder toxic.
Antidote is Mesna
Term
Denileukin Diftitox
Definition
Diptheria toxin fragment bound to IL-2. Binds IL-2 receptor on T-cell and is internalized and blocks protein synthesis through interaction with EF2. Induces apoptosis.
Useful in cutaneus T-Cell lymphoma where >20% of cells express CD25
Adv effects: hypersensitivity rxn
Term
Vinblastine
Definition
Treats Kaposi's sarcoma and cutaneous T-cell lymphoma.
Term
Bleomycin
Definition
Treats warts and Kaposi's sarcoma
Term
Doxorubicin
Definition
Treats Kaposi's Sarcoma
Term
Dapsone
Definition
Treats Leprosy and autoimmune skin conditions. Antagonist of PABA and folic acid synthesis of M. leprae. Also anti-inflammatory
Term
Thalidomide
Definition
Treats multiple myeloma and cutaneous manifestations of leprosy.
NOT for pregnancy, women of childbearing age. Must go through special STEPS program to admin.
Term
Capsaicin
Definition
Active component of hot chili peppers. Stimulates and desensitizes Vanilloid Receptor (Gated channel activated by noxious stimuli). Causes depletion of Substance P.
Used to treat post-theraputic neuralgia and pain of diabetic neuropathy.
Dont give in cardiovascular or cerebrovascular disease.
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