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DERM: Topical steroids scabies Acne alopecia Rosacea Antifungals Immunomodulators. Topical Corticosteroids . Nursing 7755 Fall 2010 Debkfp@hotmail.com. Topical corticosteroids. MOA: Vasoconstriction Anti-inflammation Decrease epidermal proliferation. Cell. Inhibit phospholipase

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topical corticosteroids

DERM:

Topical steroids scabies

Acne alopecia

Rosacea

Antifungals

Immunomodulators

Topical Corticosteroids

Nursing 7755

Fall 2010

Debkfp@hotmail.com

topical corticosteroids2
Topical corticosteroids

MOA:

Vasoconstriction

Anti-inflammation

Decrease epidermal proliferation

Cell

Inhibit phospholipase

A2 which reduces skin

levels of pro-inflam kinines:

Arachidonic acid

(Omega-6, ’s inflammation)

Prostaglandins

(’s vascular dilation)

Leukotrienes

(inflammatory response)

use erythema scaling pruritus
USE: erythema, scaling & pruritus

lichen planus

lichen sclerosis

atopic dermatitis

lichen simplex chronicus

nummular eczema

psoriasis

asteatotic dermatitis

uses cont
Uses, cont.

Severe ezcema

alopecia areata

discoid lupus

severe poison ivy

slide5
SE’s
  • Systemic:
  • Suppression of HPA axis
  • Hyperglycemia

Cushinoid features

Steroid induced Acne

slide6
SE

Long-term use :

  • Local tissue atrophy w/ striae
  • Thinning of epidermis w/ telangiectasias & purpura
  • Masking bacterial or fungal infx
  • Skin fragility
choosing a topical steroid
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 and psoriasis
altering corticosteroids in 1952
Altering Corticosteroids In 1952

basic cyclopentanophenanthrene nucleus .. three 6-carbon rings (A, B, C) + a single 5-carbon ring (D

numerous modifications:

  • alterations affect potency, pharmacodynamic 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.
ointments
Ointments
  • 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 acutevesicular or weeping rashes
  • poor pt satisfaction / compliance b/c grease
creams
Creams
  • most often prescribed
  • water suspended in oil
  • 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)
lotions and gels
Lotions and gels
  • Solution or lotion: bases contain water, alcohol,
  • other chemicals
  • Clear or milky appearance
  • least greasy & occlusive
  • drying effect on an oozing lesion
  • useful for use on the scalp b/c no residue
  • can cause stinging and drying

Foams: Use:

hairy areas

expensive

drying

  • Gels: mixture of propylene glycol (drying) & water
  • Clear color, nongreasy,
  • jelly-like consistency
  • Use: exudative inflammation(poison ivy)
  • "wet" rashes ,scalp

Cordran tape

potency
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
potency 7 groups i high vii low
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)

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)

potency14
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

potency15
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

Methylprednisolone acetate0.25%, 1% cream oint

combo product
Combo product
  • Lotrisone, Mycolog II: potent steroid plus antifungal
application tips
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
frequency of administration
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
amount of application
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
dosing ftu
Dosing-FTU

2 FTU = 1gm

occlusion
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.
application tips22
Application tips
  • Stratum corneum acts as reservoir
    • continues to release med.
    • So apply qd
  • Decreasing epidermal barrier:
    • Soaking to hydrate stratum corneum--> better penetration;
    • Wrinkling ’s skins surface area to accomodate water it absorbs
    • Smearing: after soaking, smear onto wet skin to trap absorbed water
acne meds topical

Sulfacetamide

    • -Klaron
    • -Plexion
    • -Rosac
    • -Rosanil
    • -Rosula
    • -Sulfacet R
Acne meds topical
  • Clindamycin Top
    • CleocinT
    • Clindagel
    • Clindamax
    • Evoclin
  • Clindamycin/BPO
    • Acanya
    • BenzaClin
    • Duac
  • Clindamycin/tretinoin
    • Ziana
  • Erythromycin top
    • Akne-mycin
  • Erythro/BPO
    • Benzamycin

Azelaic acid

  • Azelex
  • Finacea

Dapsone

  • Aczone

Benzoyl peroxide

  • Benzac AC
  • Benzac W
  • Brevoxyl
  • Desquam E
  • Desquam X
  • Triaz
  • ZoDerm
  • RETINOIDS:
  • Adapalene
    • Differin
  • Adapalene/BPO
    • Epiduo
  • Tazarotene
    • -Tazorac
  • Tretinoin Topical
    • Atralin
    • Avita
    • -RetinA
    • -RetinA micro
slide24

BENZOYL PEROXIDE

  • Works as peeling agent
  • ’s cell sloughing/ skin turnover
  • Loosens follicular plug
  • Works as direct antimicrobial against p.acnes..
  • BPO is decomposed on skin by cysteine->
  • Liberating free Oxygen radicals->
  • That oxidize bacterial proteins
  • Applysparingly,to dry skin, 30”after washing, the lowest concentration, taper up,qod->tid
Acne…

papular

  • Forms:Soap, lotion, cream, wash, gel:more stability, more potent; alcohol or water based, alcohol base more drying, irritating
  • 1-10%
  • 5 &10% not signif. more effective than 2.5%
  • 2.5% is better tolerated
  • Add 10%urea:moisturizing

Preg: C

SE: initial dryness, irritation;

develops tolerance 1+wk;

Misc:Reduces anbx resistance if used w/anbx;

bleach fabrics

topical anbx

Clindamycin:anti-inflam, comedolytic

  • Gel, lotion, sol, foam, pads
  • BID; better w/ BPO
  • SE: rash, GI/diarrhea
  • Preg B
Topical Anbx

pustular

cystic

  • Erythromycin:
  • blocks cell wall synthesis
  • 1%-4% w/ w/o zinc (enhances penetration)
  • Gel, lotion, solution , pads
  • SE: erythema, dryness
  • Apply bid, Preg B
  • W/ BPO more effective

Sulfacetamide:sulfa anbx

inhibits folate synthesis

SE: local irritation, burning, itching erythema, SJS

Avoid w/sulfa allergy

Apply thin film BID

Preg C

topical acne cont antibacterial anti inflammatory
Topical Acne cont.antibacterial / anti-inflammatory

Azelaic acid:

found in wheat, rye, barley.

Naturally produced by Malassezia furfur (AKA Pityrosporum ovale), a normal skin yeast.

MOA: unknown

Antibacterial: (Propionibacterium acnes & Staphylococcus epi)

Keratolytic / comedolytic: Normalizes lining of hair follicle.

Antiinflammatory

Reduces pigmentation: melasma, actinic lentigines.

USE:

>12yr, clean/dry skin BID

SE:

skin irritant, hypopigmentation

Preg: B

Dapsone (leprosy)

antibacterial, anti-inflammatory

Adv. Rx:

Facial edema, depression,

psychosis, tonic clonic sz,

sinusitis, Abd pain, pancreatitis,

vomiting

Apply:

pea-sized amt, thin layer BID;

reevaluate if no improvement

after 12wk

SE:

Yellow/orange color of skin &

hair w/ dapsone gel + top.BPO

DI:

trimethoprim

Preg:

C

Monitor:

CBC

topical retinoids

Uses:

  • 1st w/ mild/mod infammatory or pustular acne,
  • fine wrinkles
  • hyperpigmentation
  • tactile roughness
Topical…..Retinoids

*Use with BPO

or top anbx

MOA:

Vitamin A derivative

  • Anti-inflammatory
  • Exfoliating
  • Comedolytic:’s cell turnover in follicular wall,

’s cohesiveness of cells

’s stratum corneum cell layers from 14 to 5

Apply:

  • qhs/qohs, 30”after washing
  • Initial flare / results 8-12wk
  • Apply 3-5”prior to top clinda Enhances penetration (&SE) of topical clinda.
  • Synergistic w/ BPO;

use BPO qam/tretinoin HS, enhance efficacy w/ less irritation

SE:

*Irritation Stinging

*Dryness Pruritus

*Erythema Burning *Photosensitivity

Hypertriglyceridemia ??

AGE: Not <12yr

Preg: C (po teratogenic)

DI:Substrate of minor:CYP2A6, 2B6, major 2C8,2C9

Inhibits weak CYP2C9

Induces weak CYP2E1

OCPs (’s progestin concentration)

retinoids

RETINOIDS:

  • Tretinoin Topical
    • Atralin
    • Avita
    • -RetinA
    • -RetinA micro
  • Adapalene
    • Differin
  • Adapalene/BPO
    • Epiduo
  • Tazarotene
    • -Tazorac
Retinoids…

Tretinoin:…

Solution: (most irritation) 0.05% solution

Gels: 0.01% and 0.025% gels

Gel microsphere: 0.04%, 0.1%

Creams: (least irritation)

0.025% cream (mild, sensitive skin)

0.05% cream (mod, sensitive skin)

0.1% creams (mod, nonsensitive skin)

  • 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
acne meds oral
Acne meds oral

www.ipledgeprogram.com

Black Box: teratogenicity

(2 forms of birth control)

SE: depression/ suicide etc

CBC changes

Rashes (SJS)

Pseudotumor cerebri

Common Rx:

Chelitis, dry skin, pruritus

Conjunctivitis, photosensitivity

Hypertrigs

Hair loss

Visual disturbances

Monitoring:

Check LFTs, trigs, Hcg qmo

  • Isotretinoin $$$
    • Accutane tier 3/na
    • Amnesteem t 1
    • Claravis t 1
    • Sotret t 1
  • doxycycline 100mg qd..$free
    • Adoxa t3
    • Doryx t3
    • Monodox t3
    • Oracea t3
  • minocycline t1 50mg 1-3x/d $15/30
    • Solodyn t3

SE:

Yeast

Caution<8yr

Tooth discolor

Photosensitivity

GI upset

Separate from dairy

Avoid <8yr; Preg D

Monitor CBC, LFT, BUN/CR

rosacea
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.

rosacea31
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”

benzoyl peroxide + clindamycin) “Benzaclin” ”Duac”

topical antifungals
Topical Antifungals

IMADAZOLES

POLYENE

  • miconazole
  • Zeasorb AF
  • Micatin otc
  • Neosporin AF OTC
  • Monistat derm
  • Fungoid tincture0tc
  • Lotrimin AF Spray OTC
  • miconazole/petrolatum/ zn oxide
  • Vusion
  • ketoconazole
  • Extina
  • Nizoral AD OTC
  • Nizoral
  • Xolegel
  • oxiconazole
    • Oxistat
  • clotrimazole
  • Mycelex
  • nystatin/triamcinolone
    • Mycolog II
  • nystatin topical
    • Mycostatin
    • Nyanyc
    • Pedi Dri

OTHER

butenafine

Mentax

Lotrimin ultra otc

terbinafine

Lamisil AT otc

naftifine

Naftin

  • selenium sulfide OTC
    • Selsun
    • Selsun blue OTC
  • phenol:
    • OTC: castellani Paint modified

ALLYLAMINES

  • tolnaftate
    • LamisilAF otc
    • Tinactin
  • ciclopirox
  • Penlac Nail Lacquer
  • Loprox
  • Gentian violet otc

clotrimazole/betameth.

Lotrisone

Econazole

Spectazole

oral antifungals
Oral antifungals

Imidazole, triazole,

thiazole antifungals

Echinocandin

anidulafungin

Eraxis

caspofungin

Cancidas

micafungin

Mycamine

  • Imidazole:
  • ketoconazole
  • clotrimazole
    • Mycelex

Polyene antifungals

Amphotericin B

Abelcet

AmBisome

Amphocin

Amphotec

Nystatin

  • Triazoles:
  • fluconazole
    • Difucan
  • itraconazole
    • Sporonox
  • voriconazole
  • Vfend
  • posaconazole
  • Noxafil

other

griseofulvin:

Grifulvin V.

Gris-PEG

flucytosine

Ancobon

(Antimetabolite)

Allylamines

terbinafine

Lamisil

antifungals
antifungals

USE: fungalinfections ie:

candidiasis

tinea pedis

tinea corporis

KOH..hyphae

polyene antifungals
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.
imidazole triazole and thiazole antifungals
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.
allylamines
Allylamines

…inhibit squalene epoxidase, another enzyme required for ergosterol synthesis.

OTHER

Griseofulvin binds to polymerizedmicrotubules and inhibits fungal mitosis

DI’s: CYP3A4, increased concentration w/ CCBs, immunosuppressants, chemo drugs, benzodiazepines, tricyclic antidepressants, macrolides, SSRIs.

topical immuno modulators
Topical Immuno-modulators:

Protopic0.03% or 0.1% ointment& Elidel1% 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

aldara immuno modulator
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

lice scabies
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
lice treatment
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.
lice rx
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.

skin lesions
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

topical 5-fluorouracil or imiquimod

rx imiquimod 5 fu
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

EFFICACY: 50% for 100 % clearance of AKs

liquid nitrogen ln 2
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
skin cancers
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;
  • Risk: sun exposure, skin type, fam. hx, changing moles
minoxidil rogaine po mintop etc top
Minoxidil: Rogaine (po), Mintop etc, (top)
  • 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.”

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

minoxidil effectiveness indication
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)

Alopecia areata

Androgenic alopecia

When DC: changes disappear w/i months

minoxidil se
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

minoxidil application
Minoxidil…application

Maximum effect: solution contact w/ scalp 4hrs

min. 40”..less effective

Apply 1-2x/d for maintenance

Minoxidil vasodilates..does notreduceDHT or the enzyme responsible for its accumulation around the hair follicle, 5-alpha reductase, which are the main causes of male pattern baldness in genetically susceptible individuals.

Dihydrotestosterone (DHT) is an androgen, synthesized primarily in the prostate gland, testes, hair follicles, and adrenal glands by the enzyme 5α-reductase

There are 2 “5-alpha reductase inhibitors”

finasteride/Proscar

dutasteride/Avodart

for BPH

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.

propecia moa finasteride proscar propecia generic
Propecia: MOAFinasteride / 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 androgeniceffect of testosterone in the tissues
propecia
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
propecia side effects
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
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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

slide56
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

slide57
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

Excretion: Urine

slide58

The end!!

Debkfp@hotmail.com