Dermatologic Pharm Flashcards
Topical Corticosteroids
- produce anti-inflammatory response in skin
- used to systematic relief of itching
- classified based on potency
- used for eczema and psoriasis
- low potency on thin skin
- high potency on thick skin
Adverse effects of topical steroids
- high potency steroids increase chance of systemic effect and can permanently thin skin
- local effects are more often seen in topical applications (atrophy, steroid acne,hypopigmentation, hypertrichosis, allergic contact dermatitis)
Imiquimod (Aldara)
-topical steroid
-immunomodulator
MOA: stimulates immune system to make interferon and interleukin to get rid of skin lesion
Spectrum: genital/perianal warts, actinic keratoses on face and scalp, superficial basal cell of trunk, neck, and extremities
Adverse effects: local itching and redness
Tacrolimus (Protopic) and Pimecrolimus (Elidel)
-topical steroid
-immunomodulator
MOA: T-cell activation leads to activation of calcineurin. Calcineurin activates gene prodcution to produce IL-2 activating immune response
-Calcineurin inhibitor
-used for moderate to severe atopic dermatitis
-short term or intermittent tx
-not for continuous long term use
-not for kids under 2 years old
-Adverse effects: burning, itching, redness.
-BBW: skin cancer and lymphomas
Ectoparasiticides
- topical steroid
- kill parasites
- Permethrin (Elimite)
- Ivermectin (SKLice)
- Malathion (Ovide)
- Lindane (Kwell)
- Crotamiton (Eurax)
- typically have to treat more than once (7-10 days after original tx)
- Concern is drug systemically absorbed
Permethrin (Elimite & Nix)
- topical steroid
- Ectoparasiticides
- spectrum: pediculus humanus (lice), pthirus pubis (crabs), sarcoptes scabiei (scabies)
- lice/crabs: apply and leave on for 10 minutes
- scabies: hleave on for 8-14 hours
- Adverse effects: burning, pruritis
Ivermectin (Sklice)
- topical steroid
- Ectoparasiticides
- used in pt over 6 months of age for head lice
- scabies
- apply to dry hair and rinse off after 10 minutes
- adverse reactions: conjunctivitis, eye irritation, dandruff, dry skin, skin burning sensation
Malathion (Ovide)
- topical steroid
- tx of pediculus humanus capitis (head lice and their ova)
- mildly effective for scabies
- thoroughly cover and moisten hair, allow it to dry (8-12 hr)
- repeat in 7-9 days
- adverse effects: irritation of scalp and skin
Lindane (Kwell)
- topical steroid
- kills lice (shampoo)
- Important difference: more systemic absorption, concentrates in brain, increased risk of neurotoxicity (seizures and death)
- okay for small area (lice tx), but not okay for larger area (scabies)
- BBW: do not give to infants, children, and pregnant women
- Adverse effect: skin irritation
Topical Immunomodulators
- modify the immune system in the skin
- not systemic so less adverse reactions
- Imiquidmod and Tacrolimus/Pimecroliumu
Crotamiton (Eurax)
- topical steroid
- used for scabies
- apply to the neck down once daily and repeat next day
- repeat this cycle again in 1 week if needed
- adverse effect: skin irritation
Topical Acne drugs
- retinoids (tretinoin, adapalene, tazarotene)
- benzoyl peroxice
- azelaic acid (Finacea)
- salicylic acid
- topical antibiotics (erythromycin, clindamycin, gentamicin, sodium sulfacetamide)
Systemic acne drugs
Istretinoin (acutane)
Oral antibiotics for acne
- tetracycline
- minocycline
- doxycycline
Tretinoin
- topical tx for acne
- topical form of vitamin A
- cream and gel form
- MOA: decreases cohesion between epidermal cells and comedones and stimulates turnover of follicular epithelial cells (cells shed more easily from the dermis)
- adverse effects: skin irritation (worse over first 4-6 weeks)
- don’t use around eyes, nose, and mouth
- try cream before gel
Retinoids
- topical acne tx
- promotes dermal collagen synthesis, new blood vessel formation, and thickening of epidermis (decreased wrinkles)
- derivatives: Adapalene (Differin) and Tazarotene (Tazorac)
- Adapalene is less irritating then tretinoin
Benzoyl Peroxide
- topical acne tx
- MOA: antibacterial and comedolytic properities and generates free radicles that oxidize proteins in Cuitbacterium ances cell wall
- adverse effects: bleaching of hair and skin irritation
- synergistic with clindamycin or erythromycin
Azelaic acid (Azelex or Finacea)
- same drug, but different brand names
- Azelex marketed for acne vulgaris
- Finacea marketed for rosacea
- MOA: not know, but possess antimicrobial activity
- mild to moderate acne
Topical Antibotics
- Clindamycin, Erythromycin, Sodium Sulfacetamide
- MOA: reduces number of Cutibacterium acnes
- combining with retinoids or benzyol peroxice increase efficacy (work in different ways)
- combining also decreases antibiotic resistance
- Adverse effects: drying and stinging of skin
Clindamycin, erythromycin, and sodium sulfacetamide MOA
-inhibit protein synthesis at 50s subunit
Isotretinoin (Accutane)
- systemic acne tx
- vitamin A derivatives (like retinoids, but PO)
- MOA: reduces sebaceous gland size and reduces sebum production
- Adverse reactions: hypervitaminosis A, dryness and itching of mucous membranes, depression
- Teratogen
- only prescribed by dermatologist
- severe cystic acne
systemic antibiotic acne tx
- reduces number of cutibacterium acnes
- combining with benzoyl peroxide increases efficacy
- can be more effective, but has more side effects
- Tetracycline, erythromycin, minocycline, and doxycycline (mino and doxy most common)
- Clindamycin uses topically, but not orally due to c.diff risk
Minocycline and Doxycycline MOA
Inhibit protein synthesis at 30s subunit
Acne pharmacology
- takes 6-8 weeks to work
- most tx irritates skin
- need to be careful with sun exposure
- want drying effect so use lotions or gels and maybe some creams
- avoid ointments
Mild acne
benzoyl peroxide or topical retinoid
Moderate acne
combination of benzoyl peroxide + topical retinoid/topcial antibiotics
Severe acne
combination therapy with oral antibiotics, topical retinoid, and benzoyl peroxide/topical antibotics
Tazarotene (Tazorac)
- topical drug for psoriasis
- retinoid (vitamin A derivative)
- can be teratogen
- MOA: binds to retinoic acid receptor to reduce keratinocyte proliferation rate
- helps normalize cell differentiation, prohibits formation of cornified envelope
- ADR: irritates skin, phytosensitivity
Calcipotriene (Dovonex)
- topical drug for psoriasis
- Vitamin D derivative
- increased vitamin D receptors and inhibit epidermal proliferation and stimulation
Calcipotriene/betamethasone (Taclonex)
-ADR: hypercalcemia, irritates skin
Topical tx for psoriasis
- Tazarotene (Tazorac)
- Calcipotriene (Dovonex)
- Calcipotriene/betamethasone (Taclonex)
- topical steroids: betamethasone, desoximetasone, flucinolone, halboetasol
Systemic tx for psoriasis
- Methotrexate
- Acitretin (Soritane)
Methotrexate
- systemic tx for psoriasis
- used for symptomatic control of psoriasis that is unresponsive to other therapies
- MOA: interferes with DNA synthesis, repair, and cellular replication
Acitretin (Soritane)
- systemic tx for severe psoriasis
- dermatologist prescribed
- MOA: blocks retinoid receptors to inhibit IL-6 resulting in anti-inflammatory, anti-proliferative, and keratinocyte differentiation in epithelium
ending mab
- monoclonal antibody
- biologics
- systemic tx for psoriasis
Occlusion
- prevents the evaporation of water from the skin to increase the moisture level of the skin
- wrapping area in plastic, vehicle of the drug (most common way), patches
Types of vehicles
- Tinctures: drug dispersed in alcohol based liquid
- lotions: drug suspended in liquid, need to shake to disperse drug
- gels: semisolid system, drug evenly dispersed
- creams: drug evenly dispersed in a semisolid base that spreads easily
- ointments: drug evenly dispersed in semisolid base that is less easy to spread
- most to least drying: tinctures, gels, lotions, creams, ointments
Transdermal delivery drugs
- applied for a systemic effect
- generally not for disease of skin
- Pros: delivered reliably, relatively pain free, avoid first pass effect (good bioavailability), maintenace drugs due to increased pt compliance
- Cons: takes several days to see effect, difficult to titrate dose
Transdermal patches info
- don’t cut patch as it destroys delivery system
- when removed there is still drug in the patch - don’t touch surface
- keep out of reach of children as they think they are stickers
Clinical uses of topical antibiotics
- prevention
- treatment: mild active skin infection in early stage only
- decreasing nasal carriage of stap (MRSA)
- Acne
Topical antibiotics
-OTC combinations: Neosportin (bacitracin, polymyxin B, neomycin) and polysporin (bactracin, polymyxin B)
Bacitracin
- topical antibiotic
- MOA: inhibits peptidoglycan chain synthesis for bacterial cell wall synthesis
- useful for G+ staph infections
Polymyxin B
- topical antibiotic
- MOA: increasing bacterial cell membrane permeability leading to death of the cell (cell lysis)
- useful for G-
Neomycin
- topical antibiotic
- aminoglycoside
- MOA: inhibits protein synthesis at 30s ribosomal subunit
- Usual for G-
Topical antibiotics tx
- tx for mild active skin infection in early stage only
- Standard of care for an active skin infection is oral antibiotics
- Can combine with Retapamulin and Mupriocin for cases such as Impetigo
Retapamulin (Altabax)
- used with topical antibiotics
- MOA: inhibit protein sysnthsis at 50s subunit
- kills strep and staph but NOT MRSA
- only use if methicillin-susceptible strains only
Mupirocin (bactroban)
- MOA: inhibits bacterial protein and RNA synthesis
- Kills MRSA
- decreases nasal carriage of MRSA
Antifungals
- takes 2-3 weeks for full effect
- apply once or twice a day
- 3 types: dermatophates, candida, malassezia furfur
Common fungal infections
- onchomycosis: toe/finger nail
- Tinea Pedis: feet
- Tinea Cruris: jock itch
- Tinea Corporis: ringworm
- Tina Capitis: fungal scalp infection
Topical Antifungals
- Azoles
- Ciclopirox (Penlac)
- Tolnaftate (Tinactin)
- Naftifine (Naftin)
- Terbinafine (Lamisil)
- Nystatin
Topical Azoles (Imidazoles)
- Efinaconazole (Jublia) - nail lacquer
- Ketoconazole - cream, gel, shampoo
- Econazole - cream, foam
- Itraconazole (Sporonox): capsule
- Fluconazole (Diflucan): tablet, suspension, IV
- Miconazole (Lotrimin, Monistate): cream, powder, ointment
- good at killing a 3 fungus
- often found in combination with corticosteroids
- ADR: itching, redness, stinging
Ciclopriox (Loprox)
- topical fungal that kills dermatophytes, candida, and malassezia furfur
- MOA: inhibits transport of essential elements of fungal cells, disrupt DNA, RNA, and protein synethesis
- Indications: onychomycosis, seborrheic dermatitis of scalp, tindea pedis, cruris, corporis
- ADR: application site reaction (erythema, pruritus, burning)
Tolnaftate (Tinactin)
- topical fungal (cream or powder)
- kills dermatophytes, but no candida
- ADR: pruritus (rarely)
- recurrenes can occur more often
- doesn’t work on palms or soles of feel as well as azoles
Naftifine (Naftin) and Terbinafine (Lamisil)
- grouped together as they are allylamines
- topical fungal (cream/powder)
- MOA: inhibits squalene epoxidase (enzyme necessary for fungi biosythesis) which leads to deficiency in ergosterol and subsequent fungal death
- good for dermatophytes (tineas)
- no candida coverage
- ADR: dry skin, erythema, pruritus, burning
Nystatin
- topical fungal (cream, ointment, powder, suspension)
- kills candida, but not dermatophytes
- MOA: binds to sterols in fungal cell membrane leading to leakage of cellular contents and cell death (tears holes in cell membrane)
- well tolerated
Oral antifungal groups
- Oral azoles
- Terbinafine
- Griseofulvin
Oral Azoles
- antifungal
- Fluconazole (Diflucan) and itraconazole (Sporanox)
- effective for skin, less so for nails
- do not give with statins, midazolam, or triazolam
- 34A inhibitor
Fluconazole (Diflucan)
- oral azole
- very long half life
- can give every day or every other day
- used for dermatophytes and candidia (espeially vaginal yeast infections)
Itraconazole (Sporanox)
- oral azole
- last long time in skin and nails
- can be used for nail infection, but has a lot of ADR including liver dysfunction
- can give for 3 months which is a relatively short course of therapy
- Monitor AST/ALT - hepatotoxic
- avoid in heart failure -excarbates
Terbinafine (Lamisil)
- oral antifungal is effective, but can give topically
- answer for nail infections
- not to be used for a long time
- 6 weeks for fingernails and 12 weeks for toenails
- Need to check liver function tests periodically
- ADR: headache, n/v, taste disturbances, increased liver enzymes
Griseofulvin
- oral antifungal
- tx of dermatophyte infections not adequately treated by topical therapy
- MOA: interferes with microtubule function - disrupting mitosis
- uses: infection of hair/scalp (4-6 weeks), skin infection (3-4 weeks), nails (6-18 months)
- ADR: teratogenic, headache, nausea, diarrhea, photosensivity, leukopenia, hepatotoxicity, may get reaction if allergic of pcn
- not used much in US