Exam 1 Flashcards
Formulations that are drying and best for oozing/crusting presentations
Tinctures, wet dressings, and lotions
Formulations that are moisturizing and best suited to xerodermic conditions
Creams & ointments
Emulsion of water and fat; lipid is biggest component
Cream
Emulsion of fat and water but with more water, less fat
Lotion
Emulsion of petroleum jelly and water; very thick & messy
Ointment
lotion or gel that is aerosolized; beneficial for scalp conditions
Foam
Emulsion of water and a thickener (polymer or starch)
Gel
Mixing a powder with a liquid creates a
Paste
Dry, mostly w/ cornstarch as the base in the US
Powder
Aqueous base of water and drug
Solution
Solution that contains alcohol; used when drug isn’t water soluble
Tincture
Common reasons to use a TCS
Atopic and contact derm, psoriasis, localized urticaria/hives
Side effects of systemic steroids?
Hyperglycemia, HTN, iatrogenic Cushing’s, HPA-axis inhibition
Super/Very Potent TCS
Clobetasol propionate 0.05% cream/ointment
Brand: Temovate & Clobex
Potent TCS
Mometsone furoate 0.1% ointment (Elocon)
Betamethasone dipropionate 0.05% lotion (Diprolene)
Mild potency TCS
Triamcinolone acetonide 0.25% cream
Least potent TCS
Hydrocortisone acetate (1% or 2.5% cream or lotions)
MOA of tacrolimus (Protopic) and pimecrolimus (Elidel) - what type of drugs are these?
Topical immunosuppressants
Bind to and inhibit calcineurin; inhibits T-cell activation
Topical antipuritics
Pramoxine, Doxepin (zonalon as topical, Sinequan oral), Diphenhydramine (topical benadryl)
Topical antipuritic that is a tricyclic antidepressant; Plasma levels may be similar whether given oral or topical - anticholinergic effects, sedation, drug interactions
Doxepin (zonalon)
Antihistamine that is given as a topical antipuritic. Plasma levels may approach that of oral use if used chronically - anticholinergic effects, sedation
Diphenhydramine (Topical Benadryl)
Peptide abx available topically, covers G+ bacteria
Inhibits transporting NAG/NAM across cell membrane
Poorly absorbed, well tolerated
Bacitracin
Peptide abx available topically, covers G- bacteria
Binds LPS, disrupts cell membrane
Poorly absorbed, well tolerated
Polymyxin B
aminoglycosides available topically, covers G- bacteria
Binds to 30S ribosomal subunit
Poorly absorbed, may lead to sensitization
Neomycin, Gentamicin
What 3 antibiotics are in Neosporin?
Bacitracin, Polymyxin B, and Neomycin
Antibiotic active against G+ cocci (Strep, Staph, including MSSA and MRSA)
Inhibits isoleucyl-tRNA synthetase, inhibiting protein synthesis
Used for impetigo as well as other superficial infx caused by susceptible organisms
Mupirocin (Bactroban)
Topical antibiotic
Binds 50S ribosomal subunit
Similar in spectrum and use as mupirocin, but not specifically approved for MRSA
Retapamulin (Altabax)
Systemic antibiotics for skin infections
Penicillins (amoxi/clav, dicloxacillin)
Cephalosporins (cephalexin, cefprozil, cefuroxime, cefpodoxime, ceftriaxone)
Fluoroquinolones (ciprofoxacin, levofloxacin, moxifloxacin)
Others: clindamycin, daptomycin, linezolid, tigecycline, TMP/SMX, vancomycin
MOA, common/serious SE, coverage of Penicillins
Binds to and inhibits PBP, inhibiting peptidoglycan synthesis
SE: hypersensitivity MC, rash, serum sickness, SJS, renal toxicity, diarrhea
Amoxi/Clav covers B-lactamase + organisms, G+ staph and strep, Haemophilis, Listeria, E. coli, Shigella, Salmonella
Dicloxacillin covers B-lactamase + organisms and staph
MOA, common/serious SE, coverage of Cephalosporins
MOA: PBP inhibition (same as pcn)
SE: hypersensitivity (MC), bleeding (MTT side chain in Cefotetan), N/V/D, obstructive biliary toxicity w/ Ceftriaxone, C. diff, Disulfiram-like rxn
Coverage: higher gen = broader spectrum; don’t cover LAME,
Cephalexin - staph/strep
Cefprozil, Cefuroxime - Enterobacteria (E. coli, Klebsiella) and Bacteroides fragilis
Ceftriaxone, Cefpodoxime - Gram - rods, pcn-resistant Strep pneumo
MOA, common/serious SE, coverage of Fluoroquinolones
MOA: targets DNA gyrase in G- and Topoisomerase IV in G+
SE: QT interval, insulin resistance, CNS - myasthenia gravis, N/V/D, cartilage toxicity in pregnancy and children, drug interactions w/ cations, CYP1A2 inhibition
Covers Gram- such as Enterbacteriaceae, Haemophilus, Moraxella, and Pseudomonas
Cipro and moxifloxacin can cover G+ and anaerobes
Not as broad spectrum, significantly inhibit p450 enzymes, almost totally regulated to topical treatment (*1 exception)
Imidazoles (Ketoconazole*, clotrimazole, econazole, miconazole, oxiconazole, sertaconazole, sulconazole)
Tend to be broader spectrum with less drug interactions; almost all used systemically
Triazoles (*Efinaconazole, *terconazole, fluconazole, itraconazole, posaconazole, voriconazole)
MOA of Azole-antifungals
Inhibits lanosterol-14a-demethylase (needed to convert lanosterol to ergosterol)
Toxicity of systemic azole-antifungals
Nausea, abdominal discomfort, hepatotoxicity, drug interactions, avoid in pregnancy
Orally (Nizoral)
Foam for Seb derm (Extina)
Shampoo for dandruff (Nizoral AD)
Topical use well tolerated
Ketoconazole
Side effects of systemic ketoconazole
Hepatotoxicity common, strong p450 inhibition (drug interactions), inhibits synthesis of androgens, estrogens, progestins, cortisol, and aldosterone
Clotrimazole, Butoconazole, Econazole, Luliconazole, Miconazole, Oxiconazole, Sertaconazole, Sulconazole, Tioconazole
Imidazole Antifungals
Used topically for tineas and vaginal candidiasis
Imidazole antifungals
Used orally for tinea, onychomycosis, or serious systemic infections
Negative inotrope - avoid in heart failure
Itraconazole (Sporanox)
Used orally or IV. Less drug interactions than itraconazole. Used for candidiasis (thrush, vulvovaginal, or systemic) or other systemic fungal infx, including fungal meningitis
Fluconazole (Diflucan)
Used orally or parenterally; similar # of drug interactions as fluconazole; Often chosen as prophylaxis against fungal infx in high-risk patients; Used for oropharyngeal and esophageal candidiasis in AIDS patients
Posaconazole (Noxafil)
Used for vaginal candidiasis
Terconazole (Terazol) or Fluconazole (Diflucan)
Used topically for onychomycosis (only indication); used daily for a year & cures 15% of cases
Efinaconazole (Jublia)
MOA of Allylamines & Tolnaftate
Inhibits squalene epoxidase (enzyme involved in ergosterol synthesis); ergosterol decreases, squalene increases, which is likely toxic
Orally for onychomycosis and other dermatophyte infx - most effective for onychomycosis
Topically for minor tineas
Toxicity (Systemic): GI, increased liver enzymes, hepatotoxicity
Terbinafine (Lamisil)
Allylamines & Use
Naftifine (Naftin), Butenafine (Mentax), Tolnaftate (Tinactin), Terbinafine (Lamisil)
Have good activity against dermatophytes and Candida
MOA of Griseofulvin (Gris-PEG)
Deposits into keratin (skin & nails), binds to fungal microtubules and inhibits mitosis
Use of Griseofulvin
Orally for dermatophyte type infections; Not considered first-line - usually requires months of tx and high relapse rates