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KCSU17 Derm > Derm Pharm > Flashcards

Derm Pharm Flashcards

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1
Q

Absorption is enhanced when

A

Stratum corners is thinner (scrotum, face, axilla)

Skin integrity is compromised

Temperature increased

Increased hydration

Increased concentration

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2
Q

The more ____ the vehicle, the more hydrated the skin is

A

Occlusive

More hydrated skin = more absorption of drug

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3
Q

Rank the vehicles from best absorption to worst

A

Ointment –> cream —> lotion –> gels (worst)

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4
Q

Creams

A

Semisolid emulsions of oil

Easily washed off with water

Middle ground potentcy

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5
Q

Ointments

A

Water suspended in oil, excellent lubricant

Decreases water loss, enhances absorption

MOST potent due to occlusive effect

Patient acceptance is low (greasy) and not good in hair areas

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6
Q

Lotions

A

Powder in water so you must shake before use

Cooling and drying but least potent

Useful in large hair areas

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7
Q

MOA of topical corticosteroids

A

Act against inflammation at cellular level

Inhibition of formation, release, and activity of mediators of inflammation –> decreases inflammation

Inhibits the migration of macrophages and leukocytes (reverses vascular dilation and permability)

Antimitotic effect on epidermal cells

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8
Q

When topical agents are applied to skin (Big Macs)

A

Inhibit migration of macrophages and leukocytes to reverse vascular dilation and permeability

Decreases edema, pruritis, edema

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9
Q

Absorption of topical corticosteroids increases with:

A

Increased hydration

Breaks in skin

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10
Q

Metabolism of topical corticosteroids

A

Primarily in the liver

Some in the skin

Elimination is primarily in the kidney

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11
Q

Potency of topical corticosteroids is dependent upon

A
  1. Characteristics of the drug (fluorinated to make more potent)
  2. Concentration of the drug
  3. Vehicle for delivery
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12
Q

General approach to topical corticosteroids

A

Start with lower potency, less occlusive vehicles (creams) then titrate up

Thin film of preparation

Only low-mid potency for children and short duration

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13
Q

What corticosteroids should be used on the face?

A

Non fluorinated/low potency areas

Used in all areas with thin stratum corneum

High potency can be used for BREIF periods

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14
Q

Lowest efficacy corticosteroid (concentration)

A

Hydrocortisone (0.25-2.5%)

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15
Q

Low efficacy corticosteroid (concentration)

A

Triamcinolone actinide/Aristocort Kenalog (0.025%)

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16
Q

Intermediate efficacy corticosteroid (concentration)

4

A

Hydrocortisone valerate/Westcort (0.1%)

Flurandrenolide/Cordran (0.025%)

Desonide/Desowen (0.05%)

Triamcinolone acetonide/kenalog (0.1%)

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17
Q

High efficacy corticosteroid (concentration)

3

A

Fluocinonide/Lidex (0.05%)

Triamcinolone acetonide/Kenalog (0.5)

Desoximetasone/Topicort (0.25%)

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18
Q

Highest efficacy corticosteroid (concentration)

A

Clobetasole propionate/Temovate (0.05%)

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19
Q

Intralesional corticosteroids

A

Preparations that are insoluble upon injection and solubility gradually

Ex. Triamcinolone acetonide/Kenalog-10

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20
Q

Triamcinolone acetonide

A

Intradermal

Limited to 1.0mg per injection site

Multiple sites can be injected

Greater volume of corticosteroid injected results in greater likelihood of systemic absorption/effects

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21
Q

Adverse reactions to topical corticosteroids

A
  1. HPA suppression
  2. Excessive absorption = Cushing’s disease, hyperglycemia, and hypokalemia

Under most conditions systemic absorption is very minimal and therefore these ADRs are minimal

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22
Q

When do we worry about systemic involvement of topical corticosteroids

A
  1. High potency agents in occlusive preparations
  2. Large amounts of topical over large area of the body
  3. Topical corticosteroids over breaks in the skin
  4. Topical corticosteroids in pediatric patients
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23
Q

Most significant ADR Topical corticosteroids

A

Skin thinning/atrophy

Secondary infection due to immunosuppression

Tolerance (reversible if used cyclically)

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24
Q

Pathogens from most dermatological concerts are

A

Group A b-hemolytic streptococcus

Staphylococcus aureus

We try to cover these but also take into account regional patterns of resistance (Antibiogram)

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25
Q

Topical antibiotics

A
  1. Bacitracin
  2. Gramicidin
  3. Polymixin B sulfate
  4. Aminoglycosides (Gentamicin)
  5. Mupirocin
  6. Metronidazole
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26
Q

bacitracin and gramicidin

A

Peptide antibiotics

Activity against pretty much everything (anaerobes and gram positives)

Minimally absorbed thru skin but have significant toxicity if given oral/systemically

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27
Q

Bacitracin MOA

A

Inhibits bacterial cell wall synthesis

Prevents transfer of mucopeptides into the growing cell wall

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28
Q

Gramicidin

A

Interferes with bacterial protein synthesis by binding to 30s ribosomal subunits

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29
Q

Polymixin B sulfate

A

Peptide antibiotic

Detergent (attaches and disrupts cellular bacterial membranes)

Gram -
No activity against gram +, proteus or serration

Often used in combo

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30
Q

Neomycin

A

Aminoglycosides

Interferes with bacterial protein synthesis (30S ribosomal subunit)

Gram negatives

Minimally absorbed from skin, can cause sensitization

** NUMBER 2 LEADING CAUSE OF CONTACT DERMATITIS

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31
Q

Gentamicin

A

Aminoglycosides

Increased activity against P. Aeruginosa compared with neomycin

Increased activity against staph and group A strep when compared to Neomycin

Interferes with bacterial protein synthesis (30s ribosomal subunit)

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32
Q

Gentamicin ADME

A

Can serum levels

Esp. When applied to large areas of denuded (burn lesions)

Possible to see accumulation in patients with renal impariment = toxicity

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33
Q

Mupirocin

A

Bactroban

Inhibits protein synthesis

Active against Gram + and Gram - aerobic bacteria

MRSA

Used intranasally for prophylaxis post op infections

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34
Q

ADME, ADR, Use

Mupirocin

A

Minimally absorbed through the skin

Can cause adverse drug reactions

For nasal colonization: 1/2 tube in ea. Nares (bid x 5d)

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35
Q

Metronidazole

A

Treatment of rosacea

Demodex brevis inhibition

Acts as an anti-inflammatory agent

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36
Q

Approach to treating mild-moderate acne (and agents)

A

Agents that correct defect in keratinization by producing exfoliation

  1. Salicylic acid
  2. Benzoyl peroxide
  3. Topical retinoids
  4. Topical antibiotics
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37
Q

Salicylic acid

A

Keratolytic (softens layer)

Reduced cohesion of corneocytes

Shedding of epidermal cells

Breakdown of keratin

Can cause burning, reddening, local skin peeling

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38
Q

Benzoyl peroxide

A

Pro-Active

Bactericidal agent

Stratum corneum and concentrates in pilosebaceous unit

Slowly releases oxygen acts against gram-positive and gram-negative anaerobic bacteria, yeast, and fungi

Decreases sebum production and consequently free fatty acids which decrease inflammation

Wash or apply ONCE daily and begins to work 8-12 weeks after starting

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39
Q

ADRs of Benzoyl peroxide

A

Dry skin – marked peeling and erythema

Benzoyl peroxide will bleach clothing

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40
Q

Normal epithelial differentiation is dependent upon which vitamin?

A

Vitamin A

Therefore most powerful peeling agents are vitamin-A related

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41
Q

Retinoid

Topical agents

Oral:

A

Retinoid Retin-A

Adapalene/Differin

Tazarotene/Tazorac

ALSO oral: Isotretinoin (Claravis, amnesteem)

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42
Q

Retinoids MOA

A

Act to reduce obstruction within the follicle

Useful in comedian and inflammatory acne

Normalize abnormal keratinocyte desquamation

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43
Q

Indications for oral Retinoid

A

Severe recalcitrant nodular acne

Acne vulgaris

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44
Q

Retinoid topical use

A

Apply in concentration that causes slight erythema with mild peeling

Apply once in evening at bedtime

Thin

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45
Q

1/3 rule

A

1/3 of patients have success with Retinoid

1/3 of patients will have to do combo Benzoyl and Retinoid

1/3 ill have to go right back on

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46
Q

IPledge program

A

Isoretinoin is teratogen (causes spontaneous abortion and life threatening congenital malformations )

THEREFORE it can only be prescribed by a iPLEDGE provider and dispensed by and iPLEDGE pharmacy and given to an iPLEDGE patient

Must be on 2 forms of contraceptive

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47
Q

Clindamycin

A

Cleocin T/Evoclin

MOA: binds to 50s ribosomal subunit, interferes with protein synthesis

Less irritating if water based gel

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48
Q

Clindamycin ADR

A

Cases of drug being systemically absorbed to levels that cause bloody diarrhea and pseudomembranous colitis (RARE for other topical agents)

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49
Q

Erythromycin

A

Binds to P site of 500s ribosomal subunit

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50
Q

Which medications should not be used as mono therapy for acne?

A

Clindamycin and e-mycin

Due to risk of increasing resistance

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51
Q

Sulfacetamide

A

Topical

Inhibition of P. Canes via PABA utilization

Warning: hypersensitive to sulfa

52
Q

Oral antibiotics used for acne

A

Tetracycline
Doxycycline
Minocycline

These three are very affective but can’t give to pregnant ladies or children

Erythromycin
Hormonal agents

53
Q

Tetracyclines

A

Bacteriostatic

Inhibits protein synthesis (30 and 50s subunits)

Minocycline > Doxycycline > Tetracycline

Can cause vertigo, photosentivity

54
Q

Erythromycin

A

Limited to those who cant use tetracycline (i.e. Pregnant women or children under 8)

55
Q

Hormonal agents

A

Used to treat acne

Oral contraceptives (some have FDA approval specifically for acne, but all of them have same effects)

Appear to control inflammatory component of acne (control the androgen levels)

56
Q

Topical Antifungal agents

A

azole derivatives
Ciclopirox/Loprox
Naftin/Lamisil
Tolnaftate/tinactin

57
Q

Topical azole derivatives

A

Alters cell membrane permeability

58
Q

Ciclopirox

A

Topical antifungal

Loprox

Broad spectrum

Activity against dermatophytes, candida species and P. orbiculare

Available as a nail polish for onychomycosis (low cure rate)

59
Q

Naftin

A

Aka lamisil

Topical antifungal

Activity against dermatophytes and P. Orbiculare but NOT candida

60
Q

Oral antifungal agents

A

Useful in treatment of systemic mycosis

Treatment may take up to a year for oral antifungal treatment

Take with acidic beverage then run to sweat it out

61
Q

Herpes simplex type 1 and 2

A

Spread by intimate contact, shedding to succeptible host

Viral replication continues local inflammation and cell lysis lead to distinct vesicles

62
Q

Varicella zoster

A

Direct contact, droplets and airborne transmission

Infects via respiratory tract

Disseminated vascular rash after 10-14 days

Stress can play a role in deactivation (also age and immunosuppresion)

63
Q

Oral antivirals

A

Acyclovir
Valacyclovir
Famciclovir

64
Q

Acyclovir

A

HSV 1, HSV 2, varicella

Decrease duration of acute infection for HSV 2

Decreased number of lesions in varicella

65
Q

Valacylovir

A

Useful for recurrent HSV outbreaks

Activity against varicella and herpes zoster

66
Q

Famciclovir

A

Recurrent HSV outbreaks, herpes zoster

67
Q

Topical antivirals

A

Zovirax
Denavir
Abreva

68
Q

Zovirax

A

Acyclovir

Topical antiviral

Management of inital herpes episodes

69
Q

Denavir

A

Penciclovir

Treatment of recurrent herpes labialis (HSV) on lips and face

“Cold sore”

70
Q

Abreva

A

OTC treatment of cold sores

71
Q

Immunomodulators

A

imiquimod
Tacrolimus/Protopic
Pimelcrolimus/Elidel

72
Q

Imiquimod MOA

A

Aldabra/Zyclara

TLR-7 agonist that induces cytokines and chemokines with antiviral and immunomodulating effects (attacks the cells in question)

73
Q

Imiquimod indications

A

Condylomata acuminata
Molluscum contagiosum
DNA viral infections

WARTS
ACTINIC keratosis
Superficial basal cell carcinoma (also includes skin around the tumor)

74
Q

Protopic and Elidel MOA

A

Suppresses cellular immunity by inhibiting T cell activation

Therefore prevents release of inflammatory cytokines and mediators

75
Q

Psoriasis treament overview

A

Limited disease = topical therapy

More than 20% of body = complex and/or systemic therapy

76
Q

Emollients

A

Psoriasis topical treatment

Used during therapy free periods to minimize dryness

Hydrate stratum corneum and minimize evaporation of water

Decrease binding forces of horny layer and enhance desquamation and eliminate scaling

Mild vasoconstrictor

77
Q

Keratolytics

A

Remove scale, smooth skin and decrease hyperkeratosis

Salicylic acid is MC used (2-10%)

78
Q

Keratolytics MOA

A

Decrease corneocyte to corneocyte cohesion producing exfoliating action

79
Q

Salicylic acid/Keratolytics ADRs

A

Local irritation

Application to large areas can result in salicylism (n/v/tinnitus/hyperventilation)

80
Q

Corticosteroid

Psoriasis efficacy

A

Clears psoriasis in 25% of patients within 3-4 weeks

50% of patients experience 75% clearing (mostly gone)

81
Q

High potency corticosteroids for psoriasis

A

Used for finite periods of time when local therapy is possible

Esp. For thick, chronic psoriatic plaques

Clobetasol proprionate (0.05%)

82
Q

Intermediate potency corticosteroid for psoriasis

A

CAN be used on face if needed for limited amount of time

83
Q

Low potency corticosteroid for psoriasis

A

Safest for long term use, face and thin skin areas, young children and infants

Hydrocortisone 1%

84
Q

corticosteroid for psoriasis

Advantage

A

Prompt relief
Convenient and acceptable

Disadvantage is that it cant be used on face

85
Q

corticosteroid for psoriasis

Useage

A

Daily or twice daily

More effective the more often it is used but continuous application for more than a month is discouraged

When lesions flatten then use intermittently

86
Q

Calcipotrience

MOA

A

Dovonex

Topical vitamin D3 analog

  • Suppress keratinocyte proliferation
  • Anti-inflammatory effects
  • Decrease IL-2 production
87
Q

Dovonex

Efficacy

A

Calcipotriene

Most patients see improvement b it not clearing of lesions

Similar results to corticosteroids but it takes longer to work

88
Q

Calcipotriene ADRs

A

Systemic absorption is small but can still effect body so urine calcium excretion must be monitored

89
Q

Tazarotene

A

Normalized abnormal keratinocyte dififerntiation

Reduces hyperproliferation

Decreased inflammation

Psoriasis

90
Q

Tazarotene

Advantage

A

Anti-psoriatic effects last for longer amount of time when compared to corticosteroid

91
Q

Tazarotene ADR

A

Teratogenic (topical are not shown to cause this but must tell patient)

92
Q

Topical, 1st line agents in psoriasis (4)

A
  1. Keratolytics
  2. Corticosteroids
  3. Calcipotriene
  4. Tazarotene
93
Q

Topical second line agents for psoriasis (3)

A
  1. Coal tar
  2. Anthralin
  3. immunomodulators
94
Q

Coal tar

A

Mixture of hydrocarbons formed from distillation of bituminous coal

Not popular bc it takes a lot of time and has cosmetic disadvantages (messy, stains skin and close has odor)

Typically used at bed time (shampoo or cream) can be used with UVB

95
Q

Anthralin

A

Reduction of mitotic rate and proliferation of epidermal cell by inhibiting synthesis of nuclear protein from inhibits of DNA synthesis to affected areas

Concurrent application of petrolatum ointment around the lesion minimizes irritation

96
Q

Anthralin

Advantage

A

Effective for widespread plaques

Produces long remission

97
Q

Anthralin disadvantage

A

Staining of skin, clothes

Irritation to normal skin and flex urges

Can precipitate generalized psoriasis

98
Q

T or F

Immunomodulators are FDA approved for psoriasis

A

FALSE

They are only approved for atopic dermatitis

Can cause lymphoma and skin cancer

99
Q

1st Line psoriasis systemic therapy agents

A

Acitretin/Soriatane

Methotrexate

Remicaid

100
Q

Acitretin

A

Soriatane

Used in severe, recalcitrant psoriasis

Unknown MOA

101
Q

Acitretin

Pharmacokinetics

A

Absorption is optimal if given with food

Mostly all of it is bound to albumin in the blood

Achieves steady state plasma concentration in 3 weeks

102
Q

Acitretin

ADRs

A

Hyperlipidemia

Liver enzyme elevation and hepatitis

Known teratogen (must not be pregnant/intend on getting pregnant in 3 years bc of accumulation in adipose)

103
Q

Acitretin Drug interactions

A

Interferes with contraceptive effects in single progesterone agents

Must not be used in concurrent ingestion of alcohol = longer half life (harming liver more and more)

104
Q

Methotrexate

A

Rhumatrex/Trexall

Immunosuppressive

Produces anti-psoriatic effects (lower dose than chemo patients)

105
Q

Methotrexate MOA in psoriasis

A

Inhibits dihydrofolate reductase (needed for AA, pyrimidines and purine synthesis)

Inhibits epidermal cell proliferation

Inhibits replication and function of T and B cells and suppresses cytokines secretion

Causes prolonged remission and Many patients have improvement

106
Q

Methotrexate ADR

A

Hepatotoxic *can cause fibrosis and cirrhosis)

Bone marrow depletion

Nausea

Diarrhea

107
Q

Methotrexate

Relative CIs

A

Decreased renal function

Pregnancy or breast feeding

Must delay conception for one full ovulatory cycle or 3 months in men

NSAID and aminoglycoside use can reduce clearance of MTX and cause toxic levels

108
Q

Remicade

A

Infliximab

Chimeric monoclonal Ab that binds to soluble and transmembrane forms of TNF-alpha and inhibits it binding with receptors

IV infusion only

Modulates expression of adhesion mollyecuels responsible for leukocyte migration and cytokines serum levels

THEREFORE IT BLOCKS INFLAMMATORY AND IMMUNE RESPONSES

109
Q

Entercept

A

Enbrel

Reduces signs and symptoms and inhibits progression of structural damage of active arthritis in patients with psoriatic arthritis

Can be used in combo with MTX

110
Q

Enbrel MOA

A

Binds to TNF and blocks interaction with cell surface receptors

Blocks inflammatory and immune responses

SQ injection, half life of 102 hours and peaks at 69 hrs

111
Q

Alefacept

A

Amevive

Interferes with lymphocyte activate and proliferation

May increase risk of malignancies and increased risk of infection

112
Q

Efalizumab

Indication, MOA

A

Plaque psoriasis

Blocks T cell activation

AKA raptiva

113
Q

Adalimumab

A

AKA Humira

Immunomodulator used for mod-severe plaque psoriasis

Blocks TNF-alpha

114
Q

Psoriasis immunomodulatory drugs (5)

A

Etanercept/Enbrel

Alefacept/Amevive

Infliximab/Remicade

Efalizumab/Raptiva

Adalimumab/Humira

115
Q

Scabies 1st line treatment

A

Permethrin 5% topical cream

Elimite

116
Q

Elimite

MOA

A

Scabies

Acts on nerve cell membrane of mite to disrupt sodium channel that regulates membrane polarization

Causes paralysis and death of the parasite

117
Q

Alternative treatments

Scabies

A

Lindane 1% lotion/shampoo

Ivermectin/stromectol

Crotamiton 10% /Eurax

Malathion 0.5%/Oviedo

118
Q

Lindane 1%

A

Scabies alternative treatment

Lotion or shampoo

Directly absorbed by parasites and ova thru exoskeleton

Simulates nervous system resulting in seizure and death of parasite arthropod

Wet or warm skin increase risk of systemic absorption (therefore neurotoxicity of patient)

119
Q

Ivermectin

A

Stromectol

Binds CHLORIDE ion channel in nerve and muscle cells

Causes hyperpolarization and death of parasite

2nd line agent for scabies

120
Q

Eurax

A

Crotamiton 10%

Scabies 2nd line if Permtehrin failed

121
Q

Ovide

A

Malathion 0.5%

Excessive stimulation of cholinergic receptors in CNS and PNS causing cell death

122
Q

1st line Pedicuolosis capitis

A

Permethrin 1% topical

Acts on sodium channel nerve cell membrane to result in paralysis and death

Apply to scalp and behind ears, nape of neck

Must reapply if lice are seen 7 days after initial treatment

123
Q

2nd line agent of Lice

A

Natroba/Spinosad

Topical Ivermectin

Benzoyl Alcohol

124
Q

Natroba

A

derived from fermentation of Bactria in soil (Saccharopolyspora Spinosa) causing neuronal excitation that causes paralysis and death

125
Q

Topical Ivermectin

MOA

A

Binds to chloride ion channel in nerve and muscle cells

Causes hyperpolarization of nerve or muscle cell

Death of parasite

Used in lice (2nd line)

126
Q

Benzyl Alcohol

LICE MOA

A

Asphyxiation of lice

KCSU17 Derm (12 decks)

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