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DEENT Exam 4 > Acne Pharmacology > Flashcards

Acne Pharmacology Flashcards

1
Q

Benzoyl Peroxide Products

A

Acne: Clearasil, Fostex, Oxy-10

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2
Q

Benzoyl Peroxide MOA

A

Keratolytic

Converted to benzoic acid which is a potent oxidizing agent in the skin

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3
Q

Benzoyl Peroxide Pharmacological effect

A

Loosens keratinocytes(reduces plugs)

Increases turnover rate of keratinocytes (fall off the skin faster)

Prevents closure of follicles

Antibacterial activity against P. acnes

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4
Q

Benzoyl Peroxide Side Effects

A

Drying and peeling of the skin

Burning, blistering, scaling, and edema

Bleaching

No known systemic side effects – metabolized before it gets through the skin and becomes inactive

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5
Q

Sulfur Products

A

Acne: Fostril, Liquimat, combination products

(can also be used for scabies0

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6
Q

Sulfur MOA

A

Keratolytic

Forms hydrogen sulfide when applied to skin

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7
Q

Sulfur Pharmacological Effect

A

Causes inflammation which promotes peeling and unblocking of plugs

*Has antibacterial properties due to inactivation of bacterial enzymes

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8
Q

Sulfur Side Effects

A

Redness, skin irritation, peeling, odor (forms hydrogen sulfide) and comedogenic (may cause/worsen acne due to inflammatory action)

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9
Q

Salicylic Acid MOA

A

Keratolytic
Lowers skin pH increasing hydration of keratin which facilitates the loosening and removal of the keratinized skin cells (keratinocytes that are stuck together loosen and fall off)

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10
Q

Salicylic Acid Pharmacological Effect

A

Promote the shedding of the stratum corneum

The effects range from peeling to desquamation (removal of layers of skin)

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11
Q

Salicylic Acid Concentrations

A

3 to 6% - skin conditions like dandruff, acne and psoriasis

6% - may cause skin damage

Up to 40% wart and corn removal(Compound W, Duofilm, Freezone)

For wart removal – must protect the skin around it (use vasoline around the area that you are trying to remove)

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12
Q

Salicylic Acid Side Effects

A

Irritation and inflammation of normal skin

Bleaching

Salicylism (overdose – tinnitis or ringing in the ears, change in pH: acid/base imbalance, rapid breathing, psychological disorders: altered mental function)

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13
Q

Keratolytics

A

Benzoyl Peroxide
Sulfur
Salicylic Acid

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14
Q

Acne Antibiotics MOA

A

EXCEPT metronidazole

Reduces P. acnes by inhibiting protein synthesis in the bacterial cell

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15
Q

Acne Antibiotics

A 
Tetracycline
Minocycline
Doxycycline
Clindamycin
Erythromycin
Metronidazole
Azelaic Acid
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16
Q

Acne Antibiotic Pharmacological Effect

A

Decreases the percentage of free fatty acids (by inhibition of lipases)

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17
Q

Tetracycline unique MOA

A

Decreases keratin in the sebaceous pores (keratinocytes are less sticky and plugs are not formed)

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18
Q

Tetracycline products

A

Achromycin
Sumycin
Topicycline

Was used for many different types of infections, now used almost exclusively for the skin

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19
Q

Tetracycline Side Effects

A

NOT UNDER 16
-GI - N/V/D
-Pseudomembraneous colitis
-Bones and teeth are discolored and growth is impaired in the young
-Photosensitivity in fair skinned people (sunburn easier – use higher SPF or stay out of the sun)
-Increased incidence of superinfections (kill the fungus/yeast normally present, bad stuff grows, pseudomembranous colitis, thrush)
Little use of topical tetracycline (it phosfloreses – face will be bright yellow under blue-light conditions)

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20
Q

Tetracycline special warnings

A

NOT under 16

Should not be given with metal-containing products (contain Ca, Mg, Fe) – milk, MV, antacids – ions bind to the tetracycline and inactivate them

Tetracycline likes the + ions so it binds to teeth

Will look like bone cancer on an X-ray

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21
Q

Minocycline products

A

Minocin

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22
Q

Doxycycline products

A

Vibramycin

23
Q

Minocycline and Doxycycline

A

May be more efficacious than tetracycline

-More lipid soluble

24
Q

Minocycline and Doxycycline Side Effects

A

Ototoxicity and darkening of skin and teeth

May cause hearing difficulty (ototoxicity)

25
Q

Clindamycin Products

A

Cleocin
Cleocin T
C/T/S

26
Q

Clindamycin Side Effects

A

Oral:
(Mostly likely to cause) Pseudomembranous colitis – the worst diarrhea (bloody, pussy, smelly) – caused by Clostridium difficile; c dif can be lethal

N/V/D

Impaired liver function

Neutropenia (fewer neutrophils produced) - rare

Topical: (used topical more than oral)
Dryness or peeling of the skin

Contact dermatitis

27
Q

% of topical clindamycin dose absorbed systemically

A

10%

28
Q

Erythromycin products

A 
E-mycin 
Ery-tab 
A/T/S 
Erycette 
T-Stat
Ery-Sol
Benzamycin
29
Q

Erythromycin Side Effects

A

Oral side effects:
N/V/D
epigastric pain
**Orally has many drug interactions – inhibitor of CYP3A4 (main drug metabolizing enzyme)

Topical side effects:
Burning and drying especially when combined with benzoyl peroxide
(used topically because it is hard on stomach)

30
Q

Metronidazole Products

A

Flagyl

Metrogel

31
Q

Metronidazole MOA

A

Antibiotic (rosacea)
reduced by low-redox potential electron transport proteins

The reduction product disrupts DNA by inhibition of nucleic acid

used for rosacea

32
Q

Metronidazole Side Effects

A
  • N/V/D
  • Peripheral neuropathy with prolonged use
  • Disulfuram reaction - headache, copious vomiting, hypotension and possible death
  • Local effects include burning, stinging and drying
  • Found to be carcinogenic in animals.
33
Q

Metronidazole Pharmacological Effects

A
  • Inhibits growth of Demodex brevis
  • Suppression of skin bacteria does not appear to play a major role in the mechanism of action of the drug in treatment of inflammatory lesions of rosacea
  • Inactive in vitro against Propionibacterium acnes
  • Bactericidal, amebicidal, and trichomonacidal
  • Has direct anti-inflammatory effects and effects on neutrophil motility, lymphocyte transformation, and some aspects of cell-mediated immunity
34
Q

Azelaic Acid Products

A

Azelex

35
Q

Azelaic Acid MOA

A

Antibiotic: inhibits bacterial protein synthesis

And keratolytic

36
Q

Azelaic Acid Pharmacological Effect

A

–Antimicrobial action

Reduction in the thickness of the stratum corneum (less chance of producing a plug, also good for wrinkles)

37
Q

Azelaic Acid Side Effects

A

Pruritis, burning, stinging and tingling
Erythema, dryness and rash

Many side effects go away with continued use

38
Q

Retinoids

A

Vitamin A derivatives

Retinoids combines Retinol, Retinal, Retinic Acid

The “GOLD STANDARD”

Necessary for cell growth, differentiation and homeostasis of epithelial cells, the reproduction system and vision

Deficiency results in hyperplastic and keratotic skin (toad skin)

High and low doses give the same effect on skin, eyes and birth defects

39
Q

Retinoids include

A

Tretinoin
Isotretinoin
Adapalene

40
Q

Tretinoin products

A

Retin-A,
Renova,
Avita,
Retin-A Micro

41
Q

Tretinoin MOA

A

Direct mechanism:
Homo- or heterodimer retinoid-receptor complexes bind to RARE and alter protein transcription (affects the growth of the skin cells)

Indirect mechanism:
One receptor complex binds a transcription factors preventing it from binding to TRE on the DNA (reduced inflammation)

42
Q

Tertinoin Pharmacological Effects

A

Effects on keratinocytes:

  • Decreases proliferation (decrease in the number of cells)
  • Promotes differentiation (goes through the life cylce faster = maturation)
  • Increases the turnover (the skin cells fall off)
  • Reduces the cohesiveness (reduced stickiness = reduced plugs)
  • The change in protein transcription has anti-inflammatory and anti-proliferative activity
  • Reduces the thickness of the stratum corneum (reduce the amount of wrinkles)
43
Q

Tretinoin Side Effects

A

-Blistering, peeling, crusting, burning and edema of the skin – highly likely
Will go away with use

  • Can increase photosensitivity – use sunblock
  • There are no known systemic side effects, but they are teratogenic

Note: Acne will get worse before it gets better (and it will get better…good drug) stick with it
Do not give to patients with eczema
Do not give in pregnancy-teratogenic

44
Q

Adapalene products

A

Differin

45
Q

Adapalene MOA

A

Same as other retinoids except:
Specifically, binds to RAR beta and gamma (most prominent) receptors only

Binds to 2 of the subtypes instead of 3
Gamma is predominant in skin (but no gamma only drug exists yet)

46
Q

Adapalene Pharmacological Effects

A

Same as Tretinoin:

Effects on keratinocytes:

  • Decreases proliferation (decrease in the number of cells)
  • Promotes differentiation (goes through the life cylce faster = maturation)
  • Increases the turnover (the skin cells fall off)
  • Reduces the cohesiveness (reduced stickiness = reduced plugs)
  • The change in protein transcription has anti-inflammatory and anti-proliferative activity
  • Reduces the thickness of the stratum corneum (reduce the amount of wrinkles)
47
Q

Adapalene Side Effects

A

erythema, scaling, dryness, pruritis and burning

48
Q

Isotretinoin Products

A

Accutane

49
Q

Isotretinoin MOA

A

Same as others

50
Q

Isotretinoin Pharmacological Effects

A

Decreases sebaceous gland size – less sebum produced

Decreases sebum production – less blockage, less food for P. acnes

Reduces inflammation – inhibits the release of prostaglandins from macrophages

Reduces keratinization – less sticky = less likely to form plug

Superb acne drug – one course can lead to long term or permanent remission of acne

51
Q

Isoretinoin Side Effects

A

Dermatological:

Common -
Inflammation of the lips (90%), epitaxis – bloody nose (80%), itching of the skin and nose (80%),
xerosis (dry mouth), conjunctivitis
xerophthalmia (dry eyes – may be unable to wear contact lenses)

Less common (3 – 8 weeks after therapy) - Skin rash, peeling of skin from palms and soles, photosensitization and alopecia (hair loss)

Really hard to take
Will look worse before it looks better

52
Q

Isotretinoin Other Side Effects

A

Arthralgia (15%)
Pain or stiffness of muscles, bones & joints as a result of calcification and hyperostoses (bones grow)

Closure of epiphyses plate causing premature stoppage in growth (Not as much of an effect in people)

Persistent headache
Pseudotumor cerebri (benign increase in intracranial pressure) – check eyes
Drug should be discontinued and patient should be checked for papilledema with retinal hemorrhages - permanent

CNS
Lethargy and fatigue
Depression, psychosis and suicidal ideation with attempts(especially in teenagers – major reason why people want it removed from the market)

Ophthalmic effects
Conjunctivitis
Burred or tunnel vision, diplopia (double vision)
Reduction of night vision with sudden onset (rare)
Optic neuritis, cataracts, papilledema (rare)

Blood lipids
Increased triglycerides and plasma cholesterol levels occurring in 25% of patients – worry about this in older patients  can cause pancreatitis
Reduces HDL levels
Use cautiously in obese, diabetic or alcoholic patients (already have high triglycerides; at risk for developing pancreatitis)

53
Q

Retinoids in pregnancy

A

Contraindicated: Teratogenic

Mechanism of action:
Retinoids are called morphogens which are signaling molecules that control the spatial pattern of differentiation

*Birth defects included hydrocephalus, microcephaly, facial malformation, cleft palate, abnormal formation of outer ear, facial dysmorphia, microphthalmia and cardiovascular defects (FYI)

iPledge system: must have neg. pregnancy test every month before getting drug

Cannot donate blood while on this medication (1 month from stopping drug) – due to potential that the blood could be given to a female who is pregnant

Birth defects are most common in 1st trimester

Women start med on 2nd day of menstrual cycle to ensure they are not pregnant

54
Q

Retinoid potential market removal

A

Birth defects
Teen suicide
50% greater risk of Crohn’s Disease

DEENT Exam 4 (6 decks)

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