Pharmacology for Derm Flashcards

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1
Q

Soap Substitutes

A

-Milder, less drying than soap

›-Cleanse and moisturize

›-Available OTC

›-Cetaphil

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2
Q

Emollients

A

-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

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3
Q

Additives for Emollients

A

›-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)

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4
Q

Keratolyric Agents

A

›-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)

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5
Q

Debriding Agents

A

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

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6
Q

Scabicides

A
  • Permethrin (Elimite) (first line)
  • Lindane (Kwell)
  • Ivermectin (Stromectol)
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7
Q

Permethrin (Elimite)

A

›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

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8
Q

Lindane (Kwell)

A

›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

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9
Q

›Ivermectin (Stromectol)

A

›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

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10
Q

Pediculosides

A
  • Pyrethroids (first line)
  • Ivermectin (Sklice)
  • Malathion (Ovide)
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11
Q

›Pyrethroids

A

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

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12
Q

›Ivermectin (Sklice)

A

›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

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13
Q

›Malathion (Ovide)

A

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

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14
Q

Acne Treatment

(overview of options)

A

›-Topical retinoids

›-Topical antibiotics

-Benzoyl peroxide

›-Sulfacetamide

›-Erythromycin

›-Other topical agents

›Azelaic acid (Azelex, Finacea)

›Salicylic acid

›Dapsone gel

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15
Q

List of Topical Retinoids

A

›Adapalene (Differin)

Adapalene/benzyl peroxide (Epiduo)

Tretinoin topical (Atralin, Avita, RetinA)

Tazarotene (Tazorac)

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16
Q

Topical Retinoids

(indications, MoA, adverse effects, etc)

A

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)

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17
Q

Oral Retinoids

(name, MoA, side effects, etc)

A

-›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

18
Q

Benzoyl Peroxide

A

-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

19
Q

List of Topical Antibiotics

A
  • Clindamycin
  • Erythromycin
  • Sulfacetamide
20
Q

Topical Clindamycin

A

›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

21
Q

Topical Erythromycin

A

›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

22
Q

Topical Sulfacetamide

A

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

23
Q

Azelaic Acid (topical agent)

A

“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

24
Q

Dapsone

A

“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

25
Q

Types of Treatment of Psoriasis

A

›-Topical

›-Phototherapy

›-Systemic Agents

›Nonbiologic

›Biologic

26
Q

Topical Treatment of Psoriasis

A

›-Corticosteroids

›-Topical retinoids

›-Salicylic acid

›-Coal tar›

  • Vitamin D analogues
  • Anthralin
  • Calcineurin inhibitors
  • Moisturizers
27
Q

›Vitamin D analogues

A
  • 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

28
Q

›Anthralin

A

topical treatment of psoriasis

Mechanism of Action

antimitotic; slows the reproduction of skin cells; normalizes DNA

›Side Effects

stains anything and everything; skin irritation

29
Q

›Calcineurin inhibitors

A

topical treatment of psoriasis

  • Tacrolimus (Prograf)
  • Pimecrolimus (Elidel)

›Mechanism of Action

Immunosuppressant; inhibition of T lymphocyte activation; decreases inflammation and plaque production

30
Q

Phototherapy

A

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

31
Q

Treatment of Psoriasis

Systemic: Nonbiological Agents (medications)

A

›-Methotrexate (Trexall)

›-Cyclosporine (Sandimmune)

›-Acitretin (Soriatane)

›-Apremilast (Otezla)

32
Q

Treatment of Psoriasis

Systemic Biological Agents

A

›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

33
Q

Antiherpes/Antivaricella Agents

A
  • Acyclovir (Zovirax)
  • Famciclovir (Famvir)
  • Valacyclovir (Valtrex)
  • Penciclovir (Denavir)
  • Docosanol (Abreva) OTC
  • Trifluridine ophthalmic (Viroptic)
34
Q

Acyclovir

(Uses, MoA, pharmacokinetics, dosage, & side effects)

A

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
    • Triphosphate inhibits viral DNA synthesis (acts as a chain terminator)
      • Incorporates into the viral DNA & inhibits DNA polymerase
  • 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
35
Q

Valacyclovir

(Uses, MoA, pharmacokinetics, dosage, & side effects)

A
  • 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
36
Q

Penciclovir

A

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

37
Q

Famciclovir

A

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
38
Q

Dacosanol

A

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
39
Q

TYPES OF ANTIFUNGALS

A
  • 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)

40
Q
A