Dermatological Agents Flashcards

1
Q

how are drugs deliver in dermatological diseases

A

Concentration gradient
Partition coefficient
Diffusion coefficient

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2
Q

what are the physiological factors of drug delivery in dermatological diseases

A
  • thickness of stratum corneum
  • degree of hydration
  • temperature
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3
Q

what is the equation for Percutaneous Absorption

A

J=Cveh x K x D/x

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4
Q

what are most dermatological drugs incorporated into

A

vehicles

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5
Q

what are vehicles

A

vehicles bring the drug into contact with the skin

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6
Q

the type of vehicle used greatly influences what

A

drug’s absorption

-vehicles themselves can have a beneficial or harmful effect on the skin

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7
Q

see slide 5

A

see slide 5

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8
Q

what are the general guidelines for topical therapy

A

-dosage
-regional anatomic variation
altered barrier function
-hydration
-vehicle

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9
Q

what are topical glucocorticoids

A

-are grouped into 4-7 classes in order for decreasing potency

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10
Q

modifications of topical glucocorticoids are based on what

A

hydroxylation, methylation, fluorination or esterificaition are made to increase lipid solubility and potency, and decrease mineralcorticoid effect

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11
Q

relative potency of topical glucocortioics are based on what

A

vasoconstrictor assay, psoriasis bioassy, or relief of experimentally induced-erythema or inflammation

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12
Q

what is the mechanism of action of steroids

A
  • penetrate cell membrane and bind to a cytoplasmic receptor- heat shock protein complex
  • the heat shock protein is released and the hormone receptor complex is transported to the nucleus
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13
Q

steroids interact with —- and regulate their expression

A

glucocorticoid response elements on various genes and other regulatory proteins

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14
Q

what type of therapeutic use do topical steroids have

A

anti-inflammatory and immunosuppressive effects

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15
Q

MOA of topical steroids

A

-decrease adhesion, migration and function of macrophages, PMS and other lymphocytes

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16
Q

topical steroids block production and release of what

A
  • various cytokines and acute phase reactants

- suppress growth factor induced DNA synthesis and fibroblast proliferation

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17
Q

describe the anti-inflammatory effects of topical steroids

A

-antimitotic; anti-inflammatory; reduce capillary permeability; local vasoconstriction; secondary anti-pruitic effects

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18
Q

how do you choose a topical steroid

A

ask yourself the following

  1. what condition are you trying to treat? (acute vs. chronic)
  2. what potentcy do youw ant to use?
  3. what part of the body are you treating? (thin vs. thick skin)
  4. minimize the risk of the SE
  5. what vehicle/Formulation do you want to use? (ointment, cream, gel, lotion, or foam?)
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19
Q

how are topical steroids strengths classified

A

classified into 4-7 potency groups
Group 1 = ultra high potency
Group 7 = lowest potency

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20
Q

absorption and potency of topical steroids are increased with what

A

fluorination, occlusion and application of thinner skin

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21
Q

lower potency are used for

A

infants, young children; elderly
high skin penetration areas
long-term/chronic therapy

22
Q

higher potency are used for

A

Acute lesions/flare-ups
skin penetration poor
short-term control

23
Q

where can steroids be applied from thickest to thinnest areas

A
palmar, plantar, nails
dorsum of hands & feet
lower arms & legs
upper arms & legs
eyelids*, face*, chest, & back
mucous membranes*, scrotum*, submammary area*, axillary & perineal flexures*

*Fluorinated steroids generally avoided on these areas

24
Q

what are ointments more potent

A

bc they tend to be more occlusive

25
Q

what are ointments used for

A
  • dry, fissured & lichenfied skin due to moisturizing effect

- palms and soles

26
Q

what are creams used for

A
  • weeping lesions due to drying nature

- used in intertriginous areas due to high moisture in these areas

27
Q

what are gels, locations and foams used for

A
  • suitable for scalp or regions with hair
  • little moisturizing benefit
  • penetration enhancers (eg. propylene glycol) often used which can be irritating
28
Q

what is the purpose of occlusive dressings

A
  • increase hydration of skin thus enhancing drug penetration

- increasing drug penetration increases risk of systemic adverse effects

29
Q

what are occlusive dressings

A

wrapping medicated areas with occlusive dressings

30
Q

what are the occlusive dressings commonly used

A

Saran Wrap, vinyl gloves, cotten gloves

31
Q

what are the different types of skin infections

A
  • bacterial, fingal, viral or parasitic in origin

- systemic therapy may be required

32
Q

what drugs are used against surface bacterial infections

A

topical antibiotics are used

33
Q

what are the therapeutic uses of topical antibiotics

A
  • prevent infections in clean wounds
  • for early treatment of infected dermatoses and wounds
  • reduce colonization of the nares by Staphylococci
  • to treat acne
34
Q

what are the different OTC Topical Antibiotics

A

Bacitracin: Gram (+)
Neomycin: Gram (-), some Gram (+)
Polymixin: Gram (-)

Polysporin® (bacitracin + polymixin)
Neosporin® (all three)

35
Q

what is the MOA of mupirocin

A

-inhibits bacterial enzymes necessary for protein and RNA synthesis

36
Q

what is the spectrum of activity of Mupirocin

A
  • effects gram (+) and some gram (-) bacteria

- broader spectrum of activity that OTC products

37
Q

what is the functional role of Retinoids

A
  • vision
  • cell proliferation and differentiation
  • bone growth
  • immunity; tumor suppression
38
Q

what is the MAO of Retinoids

A

-effects gene expression via 2 families of receptors (RARs; RXRs)

39
Q

what are the different types of Retinoids

A
Tretinoin* (acne; photodamaged skin)
Isotretinoin# (acne vulgaris)
Alitretinoin* (Kaposi’s sarcoma)
Acitretin# (psoriasis)
Adapalene* (acne)
Tazarotene* (acne; psoriasis; photoaging)
Bexarotene*# (cutaneous T-cell lymphoma)
40
Q

Retinoid Toxicity

A
  • acute toxicity similar to Vit. A intoxication
  • dry skin, nosebleeds, conjunctivitis, reduced night vision, hair loss, MSK pain, mucocutaneous abnormalities, “retinoid dermatitis” and mood alterations
  • oral retinoids are potent teratogens
41
Q

what is the goal of acne treatment

A
  1. correct abnormalities of follicular maturation (unplug pores)
  2. decrease sebum production
  3. decrease P.acnes colonization
  4. decrease inflammation
42
Q

see slide 28-31

A

see slide 28-31

43
Q

what are the Atopic Dermatitis

A

Glucocorticoids
Antihistamines
Immunosuppressants

44
Q

what topical agents can be used to treat Pruritus

A

antihistamines
emollient creams and lotions
menthol
camphor pramoxine; doxepin; capsaicin; tar

45
Q

what systemic agents are used to treat pruritus

A

antihistamines; doxepinl glucocorticoids

46
Q

what physical modalities are used to treat Pruritus

A

PUVA; acupuncture, electrical stimulation

47
Q

what immunosuppressants are used for Eczema

A

Tacrolimus and Pimecrolimus

48
Q

what is the MOA of Tacrolimus and Pimecrolimus

A
  • inhibits production of interleukins, interferons, other antigen-stimulated products in T cells
  • inhibit release of pre-formed mediators from skin mast cells and basophils, breastfeeding
49
Q

how long should Tacrolimus and Pimecrolimus be used for

A

short term and intermittent long-term therapy for eczema

50
Q

what topical agents are used for Psoriasis

A
Glucocorticoids
Calcipotriene (Vit D analog)
Tazarotene (retinoid)
Anthralin
Coal tar
51
Q

what systemic agents are used to treat Psoriasis

A

Methotexate
Acitretin
Immunosuppressants (cyclosporine; mycophenlate)
Biologic agents (alefacept; efalizumab; etanercept, adalimumab; infliximab)