Kruse Flashcards
Topical ANTIBIOTICS for acne
- Clindamycin and Erythromycin
- Should NOT be used as monotherapy because combo (with retinoids, benzoyl peroxide) decreases resistance
Topical Antifungal agents
- Azoles
- Ciclopirox olamine
- Allylamines: Terbinafine, naftifine
- Butenafine
- Tolnaftate
- Nystatin
- Amphotericin B
MOA of Allylamines
- inhibits squalene epoxidase, a key enzyme in ergosterol biosynthesis
- effective for topical treatment of tinea corporis, tinea cruris, and tinea pedia
What antifungal used as an oral suspension for treatment of thrush
Nystatin
What is the antifungal with broad antifungal activity but rarely used topically and has a cumulative organ toxicit
Amphotericin B
what are the oral Antifungal agents
- Azoles: drug-Drug interaction (P450 inhibitor)
- Griseofulvin
- Terbinafine
what is the MOA for the antiviral agents
- converted to pharmacologically active triphosphate metabolites and inhibit viral DNA synthesis and viral replication
- Topical: modest benefit for herpes labialis
- Systemic: most effective in treating herpes labialis, also used systemically for HSV and VZV
Immunomodulators used in treatment of Actinic Keratoses
- Imiquimod
- Tacrolimus and pimecrolimus
which immunomodulators are useful in the treatment of atopic dermatitis and psoriasis but traditionally used to prevent heart, liver, and kidney allograft rejection due to potent immunosuppressive activity (oral forms)
- Tacrolimus
- Pimecrolimus
MOA of Tacrolimus and Pimecrolimus
-inhibit T lymphocyte activation and prevent release of inflammatory cytokines and mediators from mast cells
other Acne preparations
-Retinoic acid and derivatives Topicals -Retinoic acid -Adapalene -Tazarotene
Oral: Isotretinoin
- Benzoyl peroxide
- Azelaic acid
common adverse events of topical retinoics for acne
- erythema, mild peelin, dryness
- Avoid or minimize sun exposure (enhanced reactivity to UV radiationg with increased risk of severe sunburn)
what is the MOA of Isotretinoin (oral retinoid preparation)?
what is it used for?
- Reduces sebaceous gland size and reduces sebum production
- Use restricted to the treatment of unmanageable severe cystic acne, disorders of keratinization, psoriasis, and cutaneous and extracutaneous malignant neoplasms
MAO of Benzoyl Peroxide
- prodrug converted to benzoic acid within the epidermis and dermis
- MAO: releases free-redical oxygen which oxidizes bacterial proteins in the sebaceous follicles decreasing the number of anaerobic bacteria and decreasing irritating-type free fatty acids
- antimicrobial against P. acnes
- avoid contact with eyes and mucous membranes
MOA of Azelaic acid
- antimicrobial activity against P. acnes as well as in vitro inhibitory effects on the conversion of testosterone
- 6-8 weeks to clinical improvement
- also used to treat hyperpigmentation
Drugs for Psoriasis
- UV light: photochemotherapy (PUVA), psoralen followed by UVA radiation
- Topical: Emollients, corticosteroids, vitamin D analogs (calcipotriene and calcitriol), Tar, Tazarotene, Calcineurin inhibitors
- systemic therapy
Systemic therapy options for psoriasis (usually
reserved for pts with more than 10% body surface area involvement or less extensive but debilitating disease
- methotrexate: inhibits diydrofolate reductase
- Acitretin: systemic retinoid
- Cyclosporine: inhibits calcineurin (phosphatase that enhances cytokine transcription) and thereby inhibits transcription of IL-1 and 2 receptors, blocks T cell activation
- Alefacept
- TNF inhibitors
- Ustekinumab
MOA of emollients
keep skin moist and minimizes itching and tenderness
MOA of vitamin D analogs
hypoproliferative effects on keratinocytes
MOA of Alefacept
- immunosuppressive dimeric fusion protein that consst of extracellular CD2-binding portion of the human leukocyte function antigen-3 linked to Fc portion of human IgG1
- interferes with lymphocyte activation
- Discontinue when CD4 counts remain below 250
what are the TNF inhibitos used for psoriasis
- Etanercept
- Infliximab
- Adalimumab
highlights for the TNF inhibitors
- can cause serious life threatening infections, exacerbate CHF, and cause demyelinating disease in predisposed pts
- evaluate for tuberculosis risk factors and latent disease prior to initiating therapy
- Possible association b/t the use of TNF blockers and the development of LYMPHOMA
MOA of Ustekinumab
- Targets and interferes with the proinflammatory cytokines IL-1 and IL-23
- possible link with major adverse cardiovascular events
when are systemic corticosteroids given?
-severe dermatological illnesses such as allergic contact dermatitis to plants (poison ivy, poison oak) and for life threatening vesiculobullous dermatoses (pemphigus vulgaris, bullous pemphigoid)
what are the low to medium efficacy topical corticosteroids?
used for what?
- Hydrocortisone (lowest)
- Betamethasone valerate (low)
- Hydrocortisone valerate (intermediate)
-seborrheic dermatitis
what are the high efficacy topical corticosteroids?
used for what?
- Betamethasone dipropionate
- Clobetasol propionate (highest)
-Psoriasis of palms and soles, sarcoidosis, vilitigo, pemphigus
what are the Keratolytic agents
- Salicylic aci
- Fluorouracil
highlights for Fluorouracil
- Fluorinated pyrimidine antmetabolite resembling uracin used in the topical treatment of multiple actinic keratosis
- MAO: inhibits thymidylate synthetase and blocks the synthesis of DNA and RNA
what are the first generaion H1-receptor blockers?
highlights?
- diphenhydramine
- have some anticholinergic activity and are sedating, making them useful for control of pruritis
2nd gen H1 receptor antagonists?
highlight?
- cetirizine, loratadine, desloratadine, fexofenadine hydrochloride
- lack anticholinergic side effects and are nonsedating because they do no cross the blood brain barrier
- Metabolized by CYP3A4 and 2D6 and should NOT be coadministered with med that inhibit these like Imidazole antifungals or macrolides
Trichogenic agents (hair growth)
- Minoxidil
- Finasteride
what must be monitors when giving Minoxidil
-blood pressure in pts with cardiac disease
what is finasteride used for?
MOA?
- treatment of androgenic alopecia and BPH
- competitive and selective inhibitor of type 2 isoenzyme of steroid 5a-reductase; blocks conversion of testosterone to DHT in prostate
adverse effects of finasteride
- decreased libido
- ejaculation disorders, erectile dysfunction
what must be obtained 2 weeks before starting Isotretinoin for acne
-pregnancy test . .teratogen
