Pharmacology for Derm Flashcards
Soap Substitutes
-Milder, less drying than soap
-Cleanse and moisturize
-Available OTC
-Cetaphil
Emollients
-Come in creams, lotions, ointments, gels
-Mechanism of Action
- Forms a protective layer (occlusion) on skin that slows water loss and “holds” in the skin’s natural moisture (humectant). Replaces lost lipids in the skin by penetrating between the skin cells below the surface.
- Moisturizes (lubrication)
- Softens the skin
- Decreases scaling
- Reduces pruritus
-Petrolatum, lanolin, mineral oil, dimethicone, fatty acids, ceremides (structural lipids), zinc oxide, Eucerin
-Can have additives such as humectants (glycerin, proplyene glycol)
-draws in moisture from the air
Adverse effects
-Generally well tolerated
-Burning, rash, erythema, allergic reaction
Directions for use
-Apply on clean, moist skin (water improves effectiveness)
-Applying an occlusive bandage will increase absorption
-Avoid eyes, nose, mouth and genital areas
-Requires multiple applications daily for effective results
Additives for Emollients
-exfoliate
-Lac-Hydrin
-Glycolic acid
-Topical urea (Carmol-40)
-Helps epidermal cells form keratin that is softer and less susceptible to cracking
-Best for maintenance therapy on noninflamed skin
-Apply once daily (best at night)
Keratolyric Agents
-Available in creams, lotions, shampoos, gels
-Water helps to increase effectiveness with some products
Mechanism of Action
-Softens and exfoliates
- Helps to retain moisture
- “Soften and destroy the stratum corneum by increasing endogenous hydration that causes the cornified epithelium (horny layer) of the skin to swell, soften, and desquamate”
Uses
-Treatment of psoriasis, acne
-Removal of warts, corns
-Salicylic acid (Duoplant, Acnex, Clear away wart removal, Dermarest)
-Podofilox (Condylox)
Adverse effects
-Allergic reaction, skin irritation, burning, erythema
-Salicylate toxicity (N/V, tinnitus, dizziness)
Drug interactions
Other salicylates or aspirin containing products
Anticoagulants
Corticosteroids
Diuretics (may increase salicylate concentrations)
Sulfa (may increase keratolytic effect)
Methotrexate (increase methotrexate levels, protein binding)
Debriding Agents
Mechanism of Action:
Topical agents that removes foreign material, necrotic tissue by enzymatic reactions without damaging new granulation tissue, allows for faster healing
-Collagenase, Accuzyme, Panafil
Adverse effects
Erythema, systemic bacterial infections (rare, monitor comorbidities, debilitated patients)
Drug interactions
Decreased effectiveness with detergents, heavy metals (mercury, silver), povidone iodine
-seen in tx of burn patients
Apply once daily
Scabicides
- Permethrin (Elimite) (first line)
- Lindane (Kwell)
- Ivermectin (Stromectol)
Permethrin (Elimite)
SCABACIDE
*Most common TOPICAL Agent
Dosing: Permethrin (Elimite) 5% cream (60g)
Mechanism of Action
Alters parasite cell membrane function
Directions for Use
Apply from neck down, leave on overnight then wash off
May repeat in 14 days
Important to tell patients itching may persist after effective treatment
Adverse effects
Burning, pruritus, erythema, paresthesias
Lindane (Kwell)
SCABACIDE
*NOT first line tx
Lindane (Kwell) 1% lotion, 1% shampoo
Mechanism of Action
Directly absorbed into parasites and ova and inhibits neurotransmission
Directions for Use
Apply from neck down, leave on for 8 hours, wash off
Do not use on broken or significantly wet skin (increases absorption)
Retreatment not recommended
Adverse effects
Black Box: may be associated with neurologic toxicities
Do not use in seizure disorders, infants, pregnant women
Ivermectin (Stromectol)
SCABACIDE
-Oral
Mechanism of Action
Causes parasite paralysis and death through increasing nerve and muscle cell membrane permeability
Directions for Use
Take 200mcg/kg orally as a single dose
May repeat in 10 days
Adverse Effects
Orthostatic hypotension, tachycardia, seizures, SJS, asthma exacerbation, hepatitis, headache, fever, pruritus, edema, conjunctivitis, ocular irritation
*Steven-Johnson Syndrome
Pediculosides
- Pyrethroids (first line)
- Ivermectin (Sklice)
- Malathion (Ovide)
Pyrethroids
PEDICULOSIDE
*First line tx
- OTC lotions/shampoos
- RID (pyrethrin 0.33%), Nix (permethrin 1%)
Mechanism of Action
Block parasite nerve cell membrane function
*Does not kill nits
Directions for Use
Apply to freshly washed and towel dried hair
Apply liberally, leave on for 10 minutes, wash off
Repeat in 7 to 10 days if necessary
Contraindicated if allergic to ragweed or chrysanthemums (RID)
Adverse Effects
Skin irritation
Ivermectin (Sklice)
PEDICULOCIDE
-Topical application
Mechanism of Action
Causes parasite paralysis and death through increasing nerve and muscle cell membrane permeability
Directions for Use
Apply to dry hair, leave on for 10 minutes, then wash with warm water
Adverse Effects
Conjunctivitis, ocular irritation, seborrhea, burning
Malathion (Ovide)
PEDICULOCIDE
Mechanism of Action
Inhibits cholinesterase in parasite
Directions for Use
Apply on dry hair, saturate, leave on for 8 to 12 hours, wash off
May repeat in 7 to 10 days
Adverse effects
Skin and scalp irritation
Acne Treatment
(overview of options)
-Topical retinoids
-Topical antibiotics
-Benzoyl peroxide
-Sulfacetamide
-Erythromycin
-Other topical agents
Azelaic acid (Azelex, Finacea)
Salicylic acid
Dapsone gel
List of Topical Retinoids
Adapalene (Differin)
Adapalene/benzyl peroxide (Epiduo)
Tretinoin topical (Atralin, Avita, RetinA)
Tazarotene (Tazorac)
Topical Retinoids
(indications, MoA, adverse effects, etc)
Indications
Mild to moderate acne
Sun damaged skin
wrinkles
Mechanism of Action
Derivative of vitamin A, causes epithelial cells to grow and die more quickly, prevents the formation of new comedones, has anti-inflammatory and exfoliating properties
Directions for Use
Apply once daily at bedtime
Wash skin and allow to dry thoroughly, 30 minutes before tretinoin application
Topical clindamycin decreases irritation of tretinoin, apply tretinoin 5 min prior to topical clindamycin
Topical benzoyl peroxide increases efficacy of tretinoin
Adverse effects
Stinging, dryness, scaling, erythema, warmth, photosensitivity, pruritus
Precautions
Not for use in under 12 years of age
Do not use in eczema or sunburned skin
Pregnancy class C
Gel preparations are flammable
Drug interactions
Topical astringents, abrasive soaps, sulfur, salicylic acid
Medications that may increase photosensitivity: sulfonamides, fluoroquinolones, thiazides, tetracyclines, St John’s wort
Avoid excessive intake of vitamin A (cod liver oil)
Oral Retinoids
(name, MoA, side effects, etc)
-Isotretinoin (Sotret, Claravis, Amnesteem)
Indication
Refractory acne
Mechanism of Action
Unknown, causes normalization of epidermal differentiation, reduces sebum secretion
Directions for Use
0.5mg to 1mg/kg/day divided twice daily for 20 to 24 weeks
Adverse effects
Black Box :Teratogenic (requires 2 forms of contraceptive, only dispensed through special registry program)
Cheilitis, dry skin, increase triglycerides, LFTs, hair shedding, peeling , pseudotumor cerebri, SJS, suicidal attempts, neutropenia, photosensitivity
Drug interactions
Tretinoin, vitamin A, tetracyclines(papilledema), carbamazepine
Benzoyl Peroxide
-Comes in a wash/cream (OTC)
-Benzac AC, Desquam-E
Mechanism of Action
-Antibacterial activity against propionibacterium acnes (free radicals oxide bacterial proteins) (also thought to reduce bacterial resistance)
-Keratolytic
-Comedolytic
Directions for Use
Apply once or twice daily 30 minutes after washing skin
Start with lowest concentration
Adverse Effects
Skin irritation, dryness, erythema, peeling
May bleach hair, skin and clothes
Precaution
Avoid alcohol or other agents that may be irritating to skin
Pregnancy class C
Develop tolerance
List of Topical Antibiotics
- Clindamycin
- Erythromycin
- Sulfacetamide
Topical Clindamycin
antibiotic
Formulations: gel, lotions, foams, pads, solutions
Mechanism of Action
-Binds to the 50S ribosomal subunit blocking protein synthesis
-Anti-inflammatory, comedolytic
Directions for Use
-Apply thin layer twice daily
-Increased efficacy with benzyl peroxide
-Pregnancy class B
Adverse effects
-Burning, erythema, pruritus, peeling, dryness, rash, GI/diarrhea
Topical Erythromycin
Antibiotics
Formulations: lotions, gels, solutions, pads
Mechanism of Action
Binds to the 50S ribosomal subunit blocking protein synthesis
Directions for Use
Apply thin layer twice daily
Increased effective with benzyl peroxide
Pregnancy class B
Adverse effects
Burning, peeling, dryness, pruritus, erythema
Topical Sulfacetamide
Antibiotic
Indications: acne, dandruff, seborrhiec dermatitis
Mechanism of Action
Inhibits bacterial dihydropteroate synthetase therefore inhibiting folate synthesis
Directions for Use
Apply thin layer twice daily
Avoid with sulfa allergy
Pregnancy class _C_
Adverse Effects
Erythema multiforme, Stevens-Johnson syndrome, erythema, pruritus, skin irritation, burning
Azelaic Acid (topical agent)
“Other Topical Agents”
-Azelex, Finacea
Indications: Acne, rosacea
Mechanism of action
Unknown, thought to have antibacterial, anti-inflammatory and keratolytic/comedolytic actions
Directions for Use
Not for use in less than 12 years of age
Apply thin layer to clean/dry skin twice daily
Pregnancy class B
Adverse effects
Less irritation than tretinoin or benzyl peroxide, pruritus, burning, erythema, hypopigmentation, hypertrichosis
Dapsone
“Other Topical Agents”
-Aczone
Indications: Acne, leprosy
Mechanism of Action
Unknown, thought to have antibacterial, anti-inflammatory activity
Directions for Use
Apply thin layer twice daily
Pregnancy class C
Zinc increases penetration into skin
Adverse effects
Facial edema, seizures, depression, GI, burning, erythema, peeling, yellow/orange color of skin and hair with gel
Drug interactions
Trimethoprim
Types of Treatment of Psoriasis
-Topical
-Phototherapy
-Systemic Agents
Nonbiologic
Biologic
Topical Treatment of Psoriasis
-Corticosteroids
-Topical retinoids
-Salicylic acid
-Coal tar
- Vitamin D analogues
- Anthralin
- Calcineurin inhibitors
- Moisturizers
Vitamin D analogues
- topical treatment of psoriasis
- Calcipotriene (Calcitrene, Dovonex, Sorilux)
Mechanism of Action
Binds to Vit D receptors blocking cell proliferation, mechanism not well understood.
Side Effects
hypercalcemia, burning, itching
Drug Interactions
Calcium supplementation
Anthralin
topical treatment of psoriasis
Mechanism of Action
antimitotic; slows the reproduction of skin cells; normalizes DNA
Side Effects
stains anything and everything; skin irritation
Calcineurin inhibitors
topical treatment of psoriasis
- Tacrolimus (Prograf)
- Pimecrolimus (Elidel)
Mechanism of Action
Immunosuppressant; inhibition of T lymphocyte activation; decreases inflammation and plaque production
Phototherapy
treatment of psoriasis
-Sunlight
Mechanism of Action: kills activated T cells in the skin decreasing inflammation and scaling
Side Effects: skin damage
-Ultraviolet (UVB) radiation
-Artificial light source (Broadband, narrow band, Goeckerman (coal tar and UVB)
Side Effects: burns
Topical psoralen plus ultraviolet A (topical PUVA)
Mechanism of Action: utilizes a “light-sensitizing” medication then UVA light
Treatment of Psoriasis
Systemic: Nonbiological Agents (medications)
-Methotrexate (Trexall)
-Cyclosporine (Sandimmune)
-Acitretin (Soriatane)
-Apremilast (Otezla)
Treatment of Psoriasis
Systemic Biological Agents
Adalimumab (Humira)
Alefacept (Amevive)
Etanercept (Enbrel)
Infliximab (Remicade)
Ustekinumab (Stelera)
Mechanism of Action: decreases inflammation through inhibition of tumor necrosis factor; thought to be disease modifying
Side Effects: malignancy, infections, CHF
Drug-interactions: live vaccines
Antiherpes/Antivaricella Agents
- Acyclovir (Zovirax)
- Famciclovir (Famvir)
- Valacyclovir (Valtrex)
- Penciclovir (Denavir)
- Docosanol (Abreva) OTC
- Trifluridine ophthalmic (Viroptic)
Acyclovir
(Uses, MoA, pharmacokinetics, dosage, & side effects)
ANTIHERPES/ANTIVARICELLA AGENT
- Uses: genital herpes, herpes labialis, herpes zoster, varicella, HSV encephalitis (IV)
- Ineffective against latent virus
- Acyclic guanosine derivate
-
Mechanism of Action
- Requires 3 phosphorylation steps
- Converted to monophosphate derivative by virus-specified thymidine kinase
- Selective activation of acyclovir
- Active metabolites accumulates only in infected cells
- Converted to di and triphosphate compounds by the host’s cellular enzymes
- Converted to monophosphate derivative by virus-specified thymidine kinase
- Triphosphate inhibits viral DNA synthesis (acts as a chain terminator)
- Incorporates into the viral DNA & inhibits DNA polymerase
- Requires 3 phosphorylation steps
-
Pharmacokinetics
- Accumulates in renal failure
- Oral bioavailability 15-30%
- Distributes widely in body fluids including CSF, breast milk amniotic fluid & placenta
- Half-life 3 hours
-
Dosage and Administration
- IV, oral, topical
- Dosed 5 times a day (300mg dosed 3 times a day)
- Suppression 400mg twice daily for 1 year
-
Side Effects
- Topical preparations
- Mucosal irritation and transient burning
- Oral preparations
- Nausea, diarrhea, rash, headache, renal insufficiency, neurotoxicity, thrombocytopenia
- IV
- Renal insufficiency (crystalline nephropathy), CNS side effects
- Topical preparations
Valacyclovir
(Uses, MoA, pharmacokinetics, dosage, & side effects)
- Uses: herpes zoster, genital herpes, herpes labialis, prevents CMV in post transplant patients
- L-valyl ester of acyclovir
-
Mechanism of Action
- rapidly converted to acyclovir after oral administration
- Inhibits DNA synthesis
-
Pharmacokinetics
- Serum levels are 3-5x greater than acyclovir IV or oral
- Half-life 3 hours
-
Dosage and Administration
- oral
- VZV- 1 gram three times a day for 7 days
- HSV- 1 gram twice daily for 10 days (500mg twice daily for recurrent)
- Suppression- 1000mg once daily 6 months
-
Side Effects
- TTP, hemolytic-uremic syndrome (in high doses), headache, GI intolerance (nausea, abdominal pain), photosensitivity
Penciclovir
ANTIHERPES/ANTIVARICELLA
•Uses: topically for herpes labialis
- Acyclic guanine nucleoside
- Active metabolite of famciclovir
•Mechanism of Action
- Inhibitor of viral DNA synthesis
- Initially phosphorylated by viral thymidine kinase
- Less potent than acyclovir but present in higher concentration and longer periods of time in infected cells
•Dosage and Administration
•Topical 1 % cream, applied every 2 hours while awake for 4 days
Famciclovir
ANTIHERPES/ANTIVARICELLA
- Uses: herpes zoster, genital herpes (treatment and suppression), herpes labialis, EBV
- Diacetyl ester prodrug of 6 deoxy-penciclovir
-
Mechanism of Action
- Rapidly converted to by first pass metabolism to penciclovir
- Inhibits viral DNA synthesis
-
Pharmacokinetics
- 70% bioavailability
- Half-life 10 hours (up to 20 hours)
- Prolonged in renal impairment
-
Dosage and Administration
- Oral
- 500mg three times daily for 7 days
- Suppression 250mg twice daily for 1 year
-
Side Effects
- Headache, nausea, fatigue, confusion, erythema multiforme, jaundice, thrombocytopenia
Dacosanol
ANTIHERPES/ANTIVARICELLA
- Uses: herpes labialis
-
Mechanism of Action
- Inhibits fusion between the plasma membrane and HSV envelope
- Prevents viral entry into cells and subsequent viral replication
-
Dosage and Administration
- 10% topical cream
- Applied 5 times a day
-
Side Effects
- Skin irritation
TYPES OF ANTIFUNGALS
- Polyenes
- Amphotericin B (Amphotec, Amphocin, Abelcet, AmBisome)
•Nystatin (Mycostatin)
- Antimetabolites
- Flucytosine
•I**midazoles
- Ketoconazole (Nizoral)
- Miconazole (Monistat)
- Clotrimazole (Lotrimin, Mycelex, gyne-lotrimin)
•**Triazoles
- Itraconazole (Sporanox)
- Fluconazole (Diflucan)
- Voriconazole (Vfend)
•Posaconazole (Noxafil)