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Choosing Topical Corticosteroids (PowerPoint)

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Choosing Topical Corticosteroids (PowerPoint) Powered By Docstoc
					DERM:
Topical steroids scabies
Acne             alopecia
Rosacea
Antifungals
Immunomodulators



      Topical Corticosteroids

                        Nursing 7755
                          Fall 2010
                     Debkfp@hotmail.com   1
                    Topical corticosteroids
MOA:
Vasoconstriction
Anti-inflammation
                               Cell
Decrease epidermal
proliferation

Inhibit phospholipase
A2 which reduces skin
levels of pro-inflam
   kinines:
Arachidonic acid
   (Omega-6, ’s
   inflammation)
Prostaglandins
   (’s vascular dilation)
Leukotrienes
   (inflammatory
   response)
                                              2
    lichen planus                    USE: erythema,
                                     scaling & pruritus
       Quic kTime™ and a                                                                      QuickTime™ and a
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                                          lichen sclerosis                                atopic dermatitis
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                                                                                                  Qui ckTi me™ an d a
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 lichen simplex chronicus
                                               psoriasis                              nummular eczema

                                            Qu i ckTi me ™ an d a
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                                                                                   asteatotic dermatitis
                                                                                                       3
Severe ezcema
                                                           Uses, cont.
                                    alopecia areata
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                                                                          discoid lupus
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 severe poison ivy
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                                                                                                                 4
Systemic:                SE’s
•Suppression of
HPA axis                Cushinoid features
•Hyperglycemia
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              Steroid induced Acne
                                                        5
                                    SE

                                                            Long-term use :
                                                            • Local tissue
                                                              atrophy w/ striae
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                                                            • Masking bacterial
                                                              or fungal infx
                                                            • Skin fragility    6
      Choosing a topical steroid
• many topical steroids available
• different vehicles
• differ in potency and formulation

• Weaker: thin-skinned, sensitive areas
  – axillae, groin, perianal, breast folds, face, eyelids

• Moderate:
  – trunk, arms, legs

• Strong: thick-skinned areas
  – palms, soles, certain dermatitis such as lichen planus
                                                             7
    and psoriasis
Altering Corticosteroids In 1952
basic cyclopentanophenanthrene nucleus ..
  three 6-carbon rings (A, B, C) + a single 5-
  carbon ring (D




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numerous modifications:




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• alterations affect potency, pharmacodynamic




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  activity, adverse reaction risk
• potency is significantly increased by
  modifications at:
• C-6a or C-9a Fluorination
• C-21 Halogenation
• C-17. C-21 Esterification
• Double bond between C-1 and C-2 on ring A.
                                                                                    8
        Ointments                        QuickTime™ and a
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• Most effective
• Ointment have oily/greasy base (ie:petroleum jelly)
• Greasy texture persists on the skin surface
• Translucent
• Best lubrication, penetration
• Best for dry or thick, hyperkeratotic lesions
• Not recommended for areas where skin touches
  skin or acute vesicular or weeping rashes
• poor pt satisfaction / compliance b/c grease
                                                                   9
             Creams                                   QuickTime™ and a
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• most often prescribed
• water suspended in oil                                   QuickTime™ and a
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• white color/ less greasy/ vanish into the skin
• good lubricating/ emollient qualities
• USE:
   – most skin areas, useful where skin touches skin (groin,
     rectal area, armpits )
   – acute exudative inflammation b/c of drying effect w/
     repeated use
• generally less potent than ointments of the same medication,
• often contain preservatives (cause irritation, stinging, allergic
  reaction)
                                                                                 10
                 Lotions and gels
 •   Solution or lotion : bases contain water, alcohol,
 •    other chemicals
 •   Clear or milky appearance                                 Quic kT ime™ and a
                                                                 dec om pres sor

 •   least greasy & occlusive
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 •   drying effect on an oozing lesion
 •   useful for use on the scalp b/c no residue
 •   can cause stinging and drying           Foams: Use:
Gels: mixture of propylene glycol          hairy areas
(drying) & water                           expensive
•Clear color, nongreasy,                   drying
•jelly-like consistency
                                                        Quic kTim e™ and a
• Use: exudative inflammation(poison                      decompress or
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ivy)
"wet" rashes ,scalp                        Cordran tape                           11
                  Potency
• There are seven groups of topical steroid
  potency, ranging from ultra high potency
  (group I) to low potency (group VII).

• Fluorinated topical steroids are generally
  more potent than others
  – IE: triamcinolone acetonide (contains fluoride
    ion) is 100x more potent than nonfluorinated
    HC

                                                     12
     Potency: 7 groups-- I: High-> VII:low
I :Ultra High
Betamethasone dipropionate 0.05%      Gel, oint (Diprolene)
Clobetasol propionate   0.05% cr, oint, sol, foam(Temovate,
                                                    Olux)
Halobetasol propionate     0.05%         cr, oint. (Ultravate)


II: High
Betamethasone dipropionate 0.05%         AF cream, lotion
                                         (DiproleneAF)
Fluocinonide               0.05%         gel, cream, oint, sol
                                         (derma-smoothe, Lidex)
Mometasone fuorate         0.1%          lotion oint (Elecon)


                                                                 13
                                       Potency
III: Medium to high
Betamethasone dipropionate     0.05%          cream
Betamethasone valerate         0.05% 0.1% lotion oint
Fluticasone     propionate     0.05%          oint
Triamcinolone acetonide 0.1% oint, 0.5% cream
IV: Medium
Betamethasone benzoate         0.025%       oint
Betamethasone valerate         0.12%        Luxiq foam
Fluocinolone acetonide         0.025%       oint
Fluticasone    propionate      0.05%        cream
Hydrocortisone valerate        0.2%         oint
Triamcinolone acetonide        0.1           cream

                                                         14
                                    Potency
V:Medium Low
Betamethasone dipropionate   0.05% lotion
Betamethasone valerate       0.01% 0.05% 0.1% cream
Fluticasone    acetonide     0.025% cream
Hydrocortisone valerate      0.2%   cream
Triamcinolone acetonide      0.1%   lotion
VI :Low
Fluticasone   acetonide      0.01% cream/ solution
Triamcinolone acetonide      0.1%   cream (Aristocort)


VII: Least potent
Hydrocortisone               1%, 2.5% cr, lotion, oint
Dexamethasone                0.1% gel, aerosol,cream
                                                         15
Methylprednisolone acetate   0.25%, 1% cream oint
           Combo product
• Lotrisone, Mycolog II: potent steroid plus
  antifungal




                                               16
             Application tips

• Children/elderly:
  – avoid potent fluorinated compounds
• Face:
  – only non-fluorinated
  – mild unless severe dematitis
• Better to use super-potent briefly than mild
  – ineffective long term


                                             17
   Frequency of Administration
• QD or BID application
• No improved result for more frequent
  administration
• Chronic application can induce
  tachyphylaxis (tolerance)
• Max 3wks for ultra-high-potency steroids



                                             18
          Amount of application
• Titrate to the minimal amt needed
• Prevent tachyphylaxis:
  – 1wk on, 1wk off or 3d on,4d off
  – taper off
  – hi potent for flare, low for control.
• Amount: does not affect penetration or potency
  – Thick application is wasted
  – Only thin layer in intimate contact w/ skin is absorbed
• Absorption: Thin to thick stratum corneum:
  mucous membranes -> scrotum-> eyelids-> face->
  torso-> extremities-> palm,soles, elbows, knees
• Inflamed skin: less barrier, better absorption  19
       Dosing-
        FTU
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                                                                     20
                   Occlusion

• Occlusion: determines penetration
• Occlusion: ’s hydration-> ’s penetration-> ’s
  potency
• Intertriginous: touching skin acts like occlusive
  dssg (axillae, inguinal)
• Create Occlusion: non-breathing saran wrap,
  held by tape, sock, Ace; leave on all noc
  – ie plastic shower cap; cordran tape rubber gloves,
    baggies, sauna suits.

                                                         21
•
                          Application tips
    Stratum corneum acts as
    reservoir
    – continues to release med.
    – So apply qd
• Decreasing epidermal
  barrier:                                QuickTime™ and a
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    – Soaking to hydrate stratum
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      corneum--> better
      penetration;
    – Wrinkling ’s skins surface
      area to accomodate water it
      absorbs
    – Smearing: after soaking,
      smear onto wet skin to trap
      absorbed water                                                    22
                                            Sulfacetamide
   Acne meds topical                            -Klaron
                                                -Plexion
Azelaic acid       •Clindamycin Top             -Rosac
   – Azelex            –CleocinT                -Rosanil
   – Finacea           –Clindagel               -Rosula
                       –Clindamax               -Sulfacet R
                       –Evoclin
Dapsone            •Clindamycin/BPO           RETINOIDS:
   – Aczone
                       –Acanya                •Adapalene
                       –BenzaClin
                                                  –Differin
Benzoyl peroxide       –Duac
                                              •Adapalene/BPO
   – Benzac AC     •Clindamycin/tretinoin
                                                  –Epiduo
                       –Ziana
   – Benzac W                                 •Tazarotene
   – Brevoxyl                                     -Tazorac
   – Desquam E     •Erythromycin top          •Tretinoin Topical
                                                  –Atralin
   – Desquam X         –Akne-mycin
                                                  –Avita
   – Triaz         •Erythro/BPO
                                                  -RetinA
                       –Benzamycin
   – ZoDerm                                       -RetinA micro
                                                              23
       Acne…                        BENZOYL PEROXIDE
                                Works as peeling agent
                                •’s cell sloughing/ skin turnover
                                •Loosens follicular plug

         papular                Works as direct antimicrobial
                                against p.acnes..
Forms:Soap, lotion, cream,      •BPO is decomposed on skin by cysteine->
wash, gel:more stability,       •Liberating free Oxygen radicals->
more potent; alcohol or water   •That oxidize bacterial proteins
based, alcohol base more
drying, irritating              Apply sparingly,to dry skin, 30”after
•1-10%                          washing, the lowest concentration, taper
                                up,qod->tid
                                               Preg: C
•5 &10% not signif. more                       SE: initial dryness, irritation;
effective than 2.5%                            develops tolerance 1+wk;
•2.5% is better tolerated       Misc:Reduces anbx
•Add 10%urea:moisturizing       resistance if used w/anbx;               24
                                bleach fabrics
         Topical Anbx                Clindamycin:anti-inflam,
                                     comedolytic
                                     •Gel, lotion, sol, foam, pads
           pustular                  •BID; better w/ BPO
                            cystic   •SE: rash, GI/diarrhea
                                     •Preg B




                                     Erythromycin:
Sulfacetamide:sulfa anbx             •blocks cell wall synthesis
 inhibits folate synthesis           •1%-4% w/ w/o zinc
SE: local irritation, burning,       (enhances penetration)
itching erythema, SJS                •Gel, lotion, solution , pads
Avoid w/sulfa allergy                •SE: erythema, dryness
Apply thin film BID                  •Apply bid, Preg B
Preg C                               •W/ BPO more effective25
        Topical Acne cont.
    antibacterial / anti-inflammatory
                                               Dapsone (leprosy)
              Azelaic acid:           antibacterial, anti-inflammatory
found in wheat, rye, barley.                        Adv. Rx:
Naturally produced by Malassezia      Facial edema, depression,
furfur (AKA Pityrosporum ovale), a    psychosis, tonic clonic sz,
normal skin yeast.                    sinusitis, Abd pain, pancreatitis,
                                      vomiting
            MOA: unknown
                                                     Apply:
Antibacterial: (Propionibacterium     pea-sized amt, thin layer BID;
acnes & Staphylococcus epi)           reevaluate if no improvement
Keratolytic / comedolytic:            after 12wk
Normalizes lining of hair follicle.                    SE:
Antiinflammatory                      Yellow/orange color of skin &
Reduces pigmentation: melasma,        hair w/ dapsone gel + top.BPO
actinic lentigines.                                    DI:
                  USE:                trimethoprim
                                                      Preg:
>12yr, clean/dry skin BID
                                      C
                   SE:                              Monitor:
skin irritant, hypopigmentation       CBC
                 Preg: B                                              26
       Topical…..Retinoids                            Uses:
             MOA:                           •1st w/ mild/mod
Vitamin A derivative                        infammatory or
• Anti-inflammatory                         pustular acne,
• Exfoliating
• Comedolytic:’s cell                      •fine wrinkles
   turnover in follicular wall,             •hyperpigmentation
   ’s cohesiveness of cells                •tactile roughness
’s stratum corneum cell layers
   from 14 to 5                                    SE:
                                    *Irritation          Stinging
              Apply:                *Dryness             Pruritus
• qhs/qohs, 30”after washing        *Erythema            Burning
• Initial flare / results 8-12wk    *Photosensitivity
                                    Hypertriglyceridemia ??
• Apply 3-5”prior to top clinda             AGE: Not <12yr
  Enhances penetration (&SE)           Preg: C (po teratogenic)
  of topical clinda.
                                    DI: Substrate of minor:CYP2A6,
• Synergistic w/ BPO;                    2B6, major 2C8,2C9
  use BPO qam/tretinoin HS,            Inhibits weak CYP2C9
  enhance efficacy w/ less             Induces weak CYP2E1 27
  irritation                       OCPs (’s progestin concentration)
                                                               RETINOIDS:
             Retinoids…                                        •Tretinoin Topical
                                                                    –Atralin
                                                                    –Avita
Tretinoin:…
                                                                    -RetinA
Solution:           (most irritation) 0.05% solution
                                                                    -RetinA micro
Gels:                  0.01% and 0.025% gels
                                                               •Adapalene
Gel microsphere:       0.04%, 0.1%
                                                                    –Differin
Creams: (least irritation)
                                                               •Adapalene/BPO
                       0.025% cream (mild, sensitive skin)
                                                                    –Epiduo
                       0.05% cream (mod, sensitive skin)
                                                               •Tazarotene
                       0.1% creams (mod, nonsensitive skin)
                                                                    -Tazorac

Adapalene: 3rd gen retinoid: 0.1% gel, crm, alcoholic sol, pledgets, 0.3% gel
•0.1% gel better tolerable than tretinoin 0.025% gel
•More selective binding for retinoid acid receptor in epidermis

Tazarotene: prodrug, synthetic retinoid, converted to active form of tazarotenic acid
after application; selective binding to RARs
•0.1%, 0.05% gel & crm
•more effective than 0.025% tretinoin gel, 0.1%, microsphere, adapalene 0.1% gel
•SE: peri-lesional irritation                                                     28
                      Acne meds oral
                                                       www.ipledgeprogram.com
• Isotretinoin $$$
   –   Accutane        tier 3/na                       Black Box: teratogenicity
                                                       (2 forms of birth control)
   –   Amnesteem       t1
   –   Claravis        t1                              SE: depression/ suicide etc
   –   Sotret          t1                               CBC changes
                                                        Rashes (SJS)
• doxycycline 100mg qd..$free                           Pseudotumor cerebri
   –   Adoxa          t3            SE:
                                                       Common Rx:
                                    Yeast
   –   Doryx          t3            Caution<8yr        Chelitis, dry skin, pruritus
   –   Monodox        t3            Tooth discolor     Conjunctivitis, photosensitivity
                                    Photosensitivity   Hypertrigs
   –   Oracea         t3            GI upset           Hair loss
• minocycline         t1 50mg 1-3x/d
                                                       Visual disturbances
       $15/30
                           Separate from dairy      Monitoring:
   – Solodyn     t3        Avoid <8yr; Preg D       Check LFTs, trigs, Hcg qmo
                           Monitor CBC, LFT, BUN/CR                          29
                    Rosacea
•acneiform disorder of middle-
aged & older adults
•characterized by vascular dilation
of central face
•(nose, cheek, eyelids, forehead.)




The disease is chronic; control rather than cure is the
goal of therapy.                                     30
                      ROSACEA
Topical antibiotics & BPO relieve inflammation

• Sodium sulfacetamide 10%/sulfur 5 % lotion
• Clindamycin      1% solution, gel, lotion
• Erythromycin     2% solution BID, somewhat less effective
  than other anbx

• Benzoyl peroxide 2.5% QD/BID, increasing to 5 or 10 %,
                   Effect: 4-6wk

 For papular and pustular lesions :
                         thin layer, entire involved area, QD/BID
 •Metronidazole: w/ or w/o short course of oral antibiotics.
 QD:1% gel (30g) qd
 BID: 0.75% cream (45g), lotion (59mL), 0.75% gel (28.4g)
       “Metrocream”        “MetroLotion” “Metrogel”
 •Azelaic acid: sl more effective/more irritating
  20% cream (30 g) BID; 15% gel BID “Azelex”, “Finacea”
    Combination products
    (eg, benzoyl peroxide + erythromycin “Benzamycin”
                                                                31
         benzoyl peroxide + clindamycin) “Benzaclin” ”Duac”
 IMADAZOLES                     POLYENE           Topical Antifungals
miconazole                   nystatin/triamcinolone
  Zeasorb AF                       •Mycolog II
                                                              OTHER
  Micatin otc                nystatin topical
  Neosporin AF OTC                 •Mycostatin        selenium sulfide OTC
  Monistat derm                    •Nyanyc                Selsun
   Fungoid tincture0tc             •Pedi Dri              Selsun blue OTC
  Lotrimin AF Spray OTC                               phenol:
miconazole/petrolatum/           ALLYLAMINES              OTC: castellani Paint
zn oxide                   butenafine                     modified
  Vusion                       Mentax
                               Lotrimin ultra otc      tolnaftate
ketoconazole
                           terbinafine                      LamisilAF otc
   Extina
                                Lamisil AT otc              Tinactin
   Nizoral AD OTC
                           naftifine                   ciclopirox
   Nizoral
                                Naftin                     Penlac Nail Lacquer
   Xolegel
                                                           Loprox
oxiconazole        clotrimazole/betameth.              Gentian violet otc
     Oxistat           Lotrisone
clotrimazole      Econazole
    Mycelex         Spectazole
                                                                             32
                Oral antifungals
Imidazole, triazole,                  Echinocandin
thiazole antifungals
                                      anidulafungin
Imidazole:                                     Eraxis
ketoconazole    Polyene antifungals   caspofungin
clotrimazole                                   Cancidas
                  Amphotericin B      micafungin
     Mycelex              Abelcet              Mycamine
Triazoles:                AmBisome
                          Amphocin          other
fluconazole
                          Amphotec
     Difucan      Nystatin            griseofulvin:
itraconazole                             Grifulvin V.
     Sporonox                            Gris-PEG
voriconazole
                       Allylamines    flucytosine
     Vfend                               Ancobon
                        terbinafine     (Antimetabolite)
posaconazole
     Noxafil               Lamisil                         33
                     antifungals
USE: fungal infections ie:

candidiasis        tinea pedis       tinea corporis




                       KOH..hyphae


                                                 34
              Polyene antifungals
• bind with ergosterol in the fungal cell membrane,
• causes the cell to leak
•Animal cells contain cholesterol instead of ergosterol
and so are much less susceptible.
                                         •at therapeutic doses,
                                         some amphotericin B
                                         may bind to animal
                                         membrane
                                         cholesterol,
                                         increasing the risk of
                                         human toxicity.
                                         •IV Amphotericin B is
                                         nephrotoxic.
                                                           35
Imidazole, triazole, and thiazole antifungals

.. inhibit the enzyme lanosterol 14 α-demethylase; the
    enzyme necessary to convert lanosterol to ergosterol.


Different mechanism of inhibition of the CYP450 enzyme.
•Imidazole: N3 of the Imidazole compound binds to CYP450,
•Triazole: N4 of the Triazoles bind to CYP450
•Triazoles have higher specificity for the CYPP450 than
Imidzoles, thus more potent than Imidazoles.




                                                            36
                   Allylamines

 …inhibit squalene epoxidase, another enzyme
 required for ergosterol synthesis.
                        OTHER
Griseofulvin binds to polymerized microtubules and inhibits
fungal mitosis

DI’s: CYP3A4, increased concentration w/
CCBs, immunosuppressants, chemo drugs,
benzodiazepines, tricyclic antidepressants,
macrolides, SSRIs.                                            37
           Topical Immuno-modulators:
   Protopic 0.03% or 0.1% ointment & Elidel 1% cream

MOA: “Calcineurin” Inhibitor
    Inhibits T-lymphocytes & pro- inflammatory
    cytokines in inflamed dermis
PK:
Protopic substrate of CYP3A4 (major)
  inhibits CYP3A4 (weak), min. absorbed
Elidel:substrate of CYP3A4 (minor)
USE:Adult: Apply small amt 0.03% or 0.1% oint. BID
rub in gently & completely. Reeval 6 wk.
Child ≥2 years: use 0.03%
SE: HA, burning,
                    Black box warning ?malignancies
                    lymphoma and skin malignancy       38
              Aldara.. Immuno-modulator
 activates the body's own immune system.
 (cytokines, including interferon-alpha and others)
 no direct antiviral activity
 not chemodestructive or cytotoxic.
USE: Perianal warts/condyloma acuminata:
Apply a thin layer 3 x/wk on alternative days @hs
and leave on skin for 6-10 hours. Remove by
washing with mild soap and water.x<16wk.

Actinic keratosis: Apply 2x/wk x 16 weeks); apply
HS, leave on x8hr

Common warts (unlabeled use) Apply qhs.

Superficial basal cell carcinoma: Qhs 5d/wk x 6
wks. Treatment area should include a 1 cm margin
of skin around the tumor. Leave on skin for 8 hours.

Peds: >12yr                                            39
                           Lice/Scabies
  SCABIES:sx onset 2-6wk but contagious.
  Rx all household members, sexual contacts, prolonged direct skin-to-
  skin contact within the preceding month
  RX: scabicides kill mites; some kill mite eggs.


Scabicide lotion or cream:
•apply to clean body, neck -> toes.
•infants /young children:apply entire head / neck
•leave on for the recommended time then wash
•decontaminate bedding, clothing, towels used w/i
3d prior to rx, washing in hot water / drying in a
hot dryer, dry-cleaning, or seal in a plastic bag x
72hrs.

 •Mites :survive 2-3d away from human skin.
 •Sx due to hypersensitivity reaction to mites & feces (scybala),
 •Itching may continue x several wks
 •If itching > 2- 4 wks after treatment-> retreat
                                                                    40
                     Lice treatment
• Topical pediculicides:
   PYRETHROIDS (permethrin, pyrethrins), malathion, lindane, benzyl
     alcohol.

   –   Pyrethroids OTC Lotions (RID) 1% concentration of permethrin.
   –   neurotoxic to lice, low mammalian toxicity,
   –   Wash hair/towel dry hair, Saturate scalp x10”,rinse w/ water
   –   A second treatment is indicated in 7 to 10 days,
   –   Prescription strength permethrin (5%) available, not more
       effective than OTC

   – Malathion Rx lotion 0.5%
   – with terpineol was most effective at killing head lice, compared
     with pyrethroids and lindane
   – Apply x 8-12 hr. Repeat if lice noted 7-19d.

                                                                        41
                              Lice rx.
Benzyl alcohol 5% lotion
2009, FDA approved 6mo+
• MOA: asphyxiation of lice through obstruction of their respiratory
  sphericles.
• Apply x 10”, saturation of scalp / hair, rinsed off with water.
• Repeat in 7d
• SE: irritation of skin, scalp, eyes, transient numbness at the site of
  application.

Lindane shampoo is not a drug of first choice because it has been
   associated with rare neurologic adverse effects and widespread
   resistance.
• insecticide that inhibits neurotransmission in parasitic arthropods.
   AE: seizures, death BLACK BOX

Spinosad fermentation product of the soil bacterium
   Saccharopolyspora spinosa, may be a promising future treatment.
   MOA: compromises the CNS of lice-> paralysis.
After treatment, lice free 85% spinosad, 44% permethrin.
                                                                           42
                           Skin lesions…
Actinic Keratoses: clone of abnormal squamous cells caused by UV light-
induced gene alteration.
carcinoma in situ, can develop into SCC (1:1000risk/yr) or BCC
Risk : age, skin color, sun exposure.
IDENTIFY: Small flat, rough papules, red, scaly patches, papules, or plaques,
sun exposed areas.
Seborrheic kerotosis:common epidermal tumors,
benign proliferation of immature keratinocytes
Age:50+,1-100s, autosomal dominant, sudden
appearance of multiple seb k’sw/ skin tags &
acanthosis nigricans=?malignancies;”stuck on”




AKs :erythematous base, hyperkeratotic, hard or
spine-like, irregular vs
SebKs: smooth, sometimes soft hyperkeratosis, no
erythematous base
Rx:Liquid nitrogen, destructive treatment of choice
                                                                          43
    topical 5-fluorouracil or imiquimod
            Rx: Imiquimod, 5-FU
Imiquimod/Aldara: topical immune response
  modifier stimulates local cytokine induction
Imiquimod 5% cream; 2-3x/wk x 12-16wk
complete resolution of AKs in 50% of pts, placebo 5%
AE: local erythema, scabbing, flaking.
Topical 5-fluorouracil: inhibits DNA synthesis, causes
inflammation w/ destruction of lesion
APPLY: 1-2% face, 5% elsewhere; x 2-4wk
2wk for inflammation to subside after dc’d.
4-6wk for skin to progress through erythema,
blistering, necrosis w/ erosion, re-epithelialization.
ALT: apply Bid until superficial ulceration occurs (2-
3wk). Then:low potency topical corticosteroid cream
BID to reduce inflammation until healed                44
EFFICACY: 50% for 100 % clearance of AKs
         Liquid nitrogen, LN2

• nitrogen in a liquid state
  at a very low temp.
• cryogenic fluid which can
  cause rapid freezing on
  contact with living tissue




                                45
           Skin cancers…
Squamous cell carcinoma: (SCC): common
•malignant proliferation of epidermal keratinocytes
•Locally invasive, usually curative.
•Rarely metastasizes
•Appearance: sun exposed areas; firm, flesh colored
or erythematous papules or plaque
•60% start as AK             Basal cell carcinoma (BCC)
                             common skin cancer arising from
                             basal layer of epidermis
                             •Low metastatic potential
                             •Most common: southern 55-70yo
                             cauc. female
 Malignant Melanoma: aggressive, spread
 unpredictable, any organ
 •M/F White: back, extremities
 •Asians/Blacks: mucous membranes,soles, palms;
                                                           46
 •Risk: sun exposure, skin type, fam. hx, changing moles
    Minoxidil: Rogaine (po), Mintop etc, (top)
      xxxxxxx   HX: initial use: HTN

                •“Minoxidil may cause increased growth or
                darkening of fine body hairs. If this is
                bothersome, consult your doctor. When the
                medication is discontinued, the hair will
                return to normal within 30 to 60 days.”
                                          xxxxxxxxx




•02/13/96 : patent expired
•2007 foam-based formulation of 5%

                                                      47
                      Minoxidil: MOA
MOA: Unknown
Vasodilator: speculated that dilating blood vessels &
  opening K+ channels-->
  allows more O2, blood & nutrients to the follicle.

This causes follicles in the telogen phase to shed, usually
  soon to be replaced by new, thicker hairs (new anagen
  phase)

 Anagen: growth phase
 (2-3yrs)
 Catagen: regressing phase
 (2-3 wk)
 Telogen: resting phase
 (3mo)
                                                              48
       Minoxidil…effectiveness, indication
One study: healthy males 18-50yr w/ androgenic alopecia..
 5% sol. x 32wks:  non-vellus hair counts avg 39 hairs/cm2
 Placebo:           5 hairs/cm2

INDICATION: androgenic alopecia, indicated top of head only
           effective w/ large area
           effectiveness younger men (18-41yr)




     Androgenic alopecia              Alopecia areata


          When DC: changes disappear w/i months          49
                             Minoxidil…SE
Common:
eye burning/irritation                            itching
redness / irritation at treated area              unwanted hair growth
Alcohol dries scalp--> dandruff
hair loss!! hairs already in telogen phase shed early, before beginning new
   anagen phase



Severe SE: Severe allergic rx:
rash         hives        itching      SOB
peripheral edema                       angioedema
tachycardia chest tightness /pain vertigo/syncope
unexplained wt gain
                            highly toxic to cats -> death                50
                    Minoxidil…application
Maximum effect: solution contact w/ scalp 4hrs
                 min. 40”..less effective
Apply 1-2x/d for maintenance
                                       Dihydrotestosterone (DHT) is an
Minoxidil vasodilates..does not        androgen, synthesized primarily in
  reduce DHT or the enzyme             the prostate gland, testes, hair
  responsible for its                  follicles, and adrenal glands by the
  accumulation around the hair         enzyme 5α-reductase
  follicle, 5-alpha reductase,
  which are the main causes of      There are 2 “5-alpha reductase inhibitors”
                                     finasteride/Proscar
  male pattern baldness in           dutasteride/Avodart
  genetically susceptible           for BPH
  individuals.
               THUS.. When treatment is stopped, the DHT already
               accumulated around the follicle has its expected effect,
               and the follicle usually shrinks again and eventually dies.
                                                                         51
                         Propecia: MOA
                  Finasteride / Proscar / Propecia / generic
“Synthetic anti-androgen”
• Testosterone produced in
   testicles/adrenals
• Majority is bound to sex
   hormone-binding globulin
   (SHBG)
   (protein produced in liver, that
   transports testosterone in
   blood, prevents metabolism, &
   prolongs half-life)
• Once unbound from SHBG,
   free testosterone enters cells
•In scalp, skin, prostate, testosterone is converted into dihydrotestosterone
(DHT) by enzyme 5-alpha reductase.
•DHT is a more powerful androgen than testosterone (has a much higher
affinity for the androgen receptor), so by converting testosterone to DHT, 5-
alpha reductase amplifies the androgenic effect of testosterone in the
                                                                           52
tissues
                        propecia
•Finasteride inhibits 5-alpha reductase thus blocks conversion
of testosterone into the more powerful androgen DHT.
•This reduces androgenic activity in the scalp, treating hair loss
at its hormonal source.
• 1992 FDA approved Proscar for BPH
• 1997 FDA approved Propecia for male pattern baldness
  (MPB)
• 5-yr study, men w/ mild-mod hair loss, 1mg/d, 2/3regrew
  hair(hair counts). 48% visible growth, 42% no further loss
• all in placebo, lost hair.
• Most successful in the crown
• DC: loss 6-12mo
• Caution: pregnant women
• ineffective for hair loss in Fe
                                                               53
             Propecia … side effects

•   impotence            1.1% to 18.5%
•   abnl ejaculation     7.2%
•    ejaculatory volume 0.9% - 2.8%
•   abnl sexual function 2.5%
•   gynecomastia         2.2%
•   erectile dysfunction 1.3%
•   ejaculation disorder 1.2%
•   testicular pain
•   Resolution w/ dc

                                         54
                                    Misc…
  Witch Hazel: astringent, vasoconstrictor
  USE: contact dermatitis, hemorrhoids acne
 Emollients: soften and soothe skin
 3 basic properties:
 ▪Occlusion - provide a layer of oil on skin surface to
 slow water loss and thus  the moisture content of
 the stratum corneum
 ▪Humectant -  water-holding capacity of SC
 ▪Lubrication - add a slip or glide across the skin.
 IE: mineral oil, lanolin, fatty acids, cholesterol, squalene,
 and structural lipids such as ceremides

Ceramides (1-7):barrier function of the skin.
Stratum Corneum has 3 types of lipids:ceramides,cholesterol, FFAs
Eczematous skin have fewer ceramides in SC.
Psoriatic skin: same # ceramides as nl skin but less 1,3,4,5,6, & more 2.
al lipids have to be replaced at a proper ratio to restore barrier function
                                                                          55
                           Misc…
Kelo-cote: topical silicone gel for mgmt
  & prevention of scars (keloids)



  Lac-hydrin, Amlactin 12% lactic acid
  Apply bid, solution/cream
  Use: xerosis
  MOA: humectant
                                                Keratosis
                                                pilaris


                          ichthyosis vulgaris

                                                       56
                       Misc…
Burow's solution: aluminium acetate dissolved in water.
invented mid-1800s by Karl August Burow, ophthalmologist.
MOA:         astringent / antibacterial properties
USES:        skin conditions: insect bites, rhus derm,
             swelling, allergies. bruises.
APPLY:       cold compresses over the affected area.
AVAILABLE: OTC , Domeboro tablets to dissolve in water

Zovirax/acyclovir / 5% ointment,cream / Abreva 10% OTC
MOA:       inhibits DNA synthesis and viral replication
Apply      5 times/day for 4 days
USE:       Rx of herpes labialis (cold sores)
Preg       B
Absorption:minimal systemic
                                                      57
Excretion: Urine
Debkfp@hotmail.com

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