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Dermatology > Drugs 2 > Flashcards

Drugs 2 Flashcards

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1
Q

Rifampin Use

A

TB, MRSA, S. epi
prophylactically for meningitis by meningococci or H. influenzae
Leprosy

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2
Q

Clindamycin Mechanism

A

inhibit protein synthesis, bind to 50S
close to erythromycin site so don’t give together
Cidal or static dep. on conc.

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3
Q

Clindamycin Resistance

A

-occurs slow, stepwise
-decreased affinity of drug for ribosome
(methylation by erm-encoded genes provided resistance)

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4
Q

Clindamycin Use

A

anaerobes- gram +/-
peptostreptococci, actinomyces
bacteroides fragilis
gram + cocci - MRSA, Group A Strep

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5
Q

Clindamycin Pharm

A

-rapid/near complete oral abs
-rate delayed by food
-acid stable
penetrated bone and abscesses, not CSF or intracellular
goes into placenta and is found in breast milk
Liver metabolized
Excretion: bile/urine

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6
Q

Clindamycine Toxicity

A

Pseudomembranous colitis from Clostridium difficile (severe colitis)- give metronidazole or vancomycin

  • GI disturbances-diarrhea
  • Hypersensitivity
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7
Q

Clindamycine Uses

A

Bacteroides fragilis (outside CNS)
prophylaxis if patient is allergic to penicillin
With pyrimethamine-toxoplasmosis in patients with AIDS
With primaquine for Pneumocystis jiroveci pheumonia
-oral infections

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8
Q

Mupirocin Mechanism

A

Inhibits protein mRNA synthesis, binds reversibly to staphylococcal isoleucyl tRNA synthetase
-bacteriostatic/cidal depending on concentration

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9
Q

Mupirocin Use

A 
gram +
straph, strep, MRSA
topical: impetigo
ointment is polyethylene glycol: cause renal failure
MRSA carriage treatment
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10
Q

Bacitracin Mechanism

A

Polypeptide Antibiotic
Inhibits bacterial cell wall synthesis-inhibits movement of peptidoglycan building blocks of cell wall from inside to outside the cell membrane by inhibiting dephosphorylation of the isoprenyl pyrophosphate carrier protien

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11
Q

Bacitracin Use

A

Gram + cocci and bacilli

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12
Q

Bacitracin Toxicity

A 
Severe nephrotoxicity with parenteral use
topically ointment (neomycin & polymyxin)
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13
Q

Dapsome Mechanism

A

Folic acid antagonist - bacteriostatic

inhibit 2nd messenger pathway

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14
Q

Dapsone Toxicity

A

“Dapsone/Sulfone Sundrome”

  • hemolysis, methemoglobinemia, hepatitis, cholestatic jaundice, peripheral neuropathy, hypoalbuminemia, psychosis, leukopenia, agranulocytosis
  • maculopapular rash, lymphadenopathy
  • Stevens-Johnson syndrome
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15
Q

Dapsone Use

A

LEPROSY

  • acne vulgaris
  • dermatitis herpetiformis

-actinomycotic mycetoma, granuloma annulare, ITP, malaria prophylaxis, pneumocystis (prophylaxis), polychondritis, pyoderma gangrenosum, subcorneal pustular dermatosis, toxoplasmosis prophylaxis

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16
Q

Rifampin Mechanism

A

Inhibits bacterial and mycobacterial RNA synthesis

  • beta-subunit of DNA-dependent RNA polymerase
  • eukaryotic cells unaffected
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17
Q

Rifampin Pharm

A

good for rapid/slow dividing
Hepatic metabolism/elimination
CYP inducer
Give no less than twice weekly

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18
Q

Rifampin Toxicity

A

Increased hepatic enzymes, liver toxicity
Hard to manage diabetes
-Hemolysis, hemoglobinuria, hematuria, renal insufficiency/failure
-Fever, chills, myalgias
Red/Orange body fluid

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19
Q

Rifampin Use

A

TB

LEPROSY

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20
Q

Clofazimine Mechanism

A

preferential binding to mycobacterial guanine in DNA

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21
Q

Clofazimine Pharm

A 
lipophilic
hepatic elimination (unchanged)
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22
Q

Clofazimine Toxicity

A 
anti-inflammatory/immunosuppression
staining body/body fluid-tanning/bronzing skin
sweat, urine, poop-brown black
effects babys through breast milk
-must monitor the blook
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23
Q

Clofazimine Use

A

Leprosy

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24
Q

Minocycline Mech

A

inhibits 30S subunit
cidal
Cat D

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25
Q

Minocycline Use

A

leprosy

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26
Q

Thalidomide Mechanism

A 
inhibits Nf(kappa)B transcriptional upregulation & TNF-alpha production 
-blocks leukocyte migration
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27
Q

Thalidomide Toxicity

A

Teratogen
-increase in plasma HIV viral load
somnolence>rash>headache
peripheral neuropathy

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28
Q

Thalidomide Use

A

leprosy

29
Q

Adalimumab Mechanism

A

IgG1 monoclonal antibody, binds to TNF-alpha

30
Q

Adalimumab Use

A

SC

psoriasis, arthritis, spondylitis, crohn’s

31
Q

Adalimumab Toxicity

A

Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB
Don’t give with immunsuppressives/vaccines

32
Q

Etanercept Mechanism

A

Receptor-ab fusion protein: p75 TNF receptor and Fc IgG1

binds to TNF alpha

33
Q

Botulinum Toxin Mechanism

A

Purified protein complex from Clostridium botulinum
BIND: heavy chain portion binds to cell membrane via an unidentified high-affinity “acceptor” molecule
INTERNALIZING: endocytosis
BLOCKING: light chain cleaves protein (SNAP25) that enables fusion of Ach vesicles with cell membrane, blocks release of pain neuropeptides
SPROUTING: new nerve endings sprout and reconnect the muscle, renewing neuromuscular “coupling”

34
Q

Botulinum Toxin Pharm

A
  • local injection
  • cause muscular paralysis-blocks muscarinic and nicotinic receptors
  • used for cosmetic smoothing of wrinkles
  • migraine headache
35
Q

Botulinum Toxin Toxicity

A
  • systemic - respiratory arrest and death
  • typical anticholinergic effects: dry mouth, discomfort/pain at injection, tiredness, headache, neck pain, eye problems: double vision, blurred vision, decrease sight, drooping/swelling eyelids, dry eyes
  • Albumin containing: allergy
36
Q

Glycopyrrolate Mechanism

A

off label for sweating

systemic antimuscarinic agents, don’t cross BBB

37
Q

Propranolol Mechanism

A

reduce sympathetic CNS stimulation - emotional stability improved
-off label for sweating

38
Q

Diltiazem Mechanism

A

blocks Ca2+ channels involved in secretion process

off-label for sweating

39
Q

Etanercept use

A

SC

psoriasis, arthritis, spondylitis,

40
Q

Etanercept Toxicity

A

Contraindication: Sepsis
Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB
Don’t give with immunsuppressives/vaccines

41
Q

Infliximab Mechanism

A

Chimeric monoclonal ab
(cariable region of mouse monoclonal ab on human IgG1)
binds TNF-alpha

42
Q

Infliximab Use

A

IV

psoriasis, arthritis, spondylitis, colitis, Chrohn’s

43
Q

Infliximab Toxicity

A

Contraindication: CHF, murine protein, hypersensitivity
Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB
Don’t give with immunsuppressives/vaccines

44
Q

Ustekinumab Mechanism

A

binds to p40 subunit integral to IL-12 and IL-23 activation (overexpressed in psoriasis plaques)
-disrupts IL-12 and IL-23 signal transduction (suppresses formatin of pro-inflammatroy Th1 and Th17 cells)

45
Q

Ustekinumab Toxicity/Use

A

psoriasis

  • increase risk of infection & neoplasm
  • live vaccination contraindicated
  • test for latent TB before
  • Anaphylactic rxns reported
46
Q

Calcipotriene Mechanism

A

-topical, binds to vit D receptor; complex associates with RXR-alpha and binds DNA vit D response elements (modulation of epidermal differentiation and inflammation

47
Q

Calcipotriene Use

A

psoriasis

48
Q

Clacipotriene Toxicity

A 
topical irritant (reduced by concurrent corticosteroids)
hypercalcemia/calciurea with XS dose
-abdominal pian, constipation, depression, fatigue, hypertension, anorexia, weight loss, muscle weakness, N/V thirst
-susceptibility to UV cancer
49
Q

Calcitriol Mechanism

A

hormonally active form of vit D3
better tolerated in intertiginous and sensitive areas of skin
-comparable safety to calcipotriene
PSORIASIS

50
Q

Benzoyl Peroxide

A

-topical pro-drug converted in skin to benzoic acid
-free radical liberation lethal fro nearby p. acnes
toxicity: drying of skin, marked peeling, erythema, irritation
-contact dermatitis (rash), pruitus, blistering, crusting or swelling, cool compresses or topical corticosteroids
-often with microbials like clindamycin, erythromycine, adapalene (helps prevent resistance)
avoid eyes and mucous membranes
-may bleach hair and colored fabrics

51
Q

Salicylic Acid

A

Topical keratolytic: causes desquamation of horny layer of skin
-for hyperkeratotic skin disorders common/plantar warts, psoriasis, calluses, corns
-acne
Toxicity: irritation, increase risk of salicylism (if people have renal/hepatic impairment)
Neonatal toxicity via breast milk/contact toxicity from drug on chest

52
Q

Adapalene Mechanism

A

Retinoid: selectively binds to nuclear retinoic acid receptor RAR beta and gamma, inhibits keratinocyte differentiation
-exfoliation and anti-inflammatory effects
Acne

53
Q

Isotretinoin Mechanism

A

converted inside cell to metabolites that are agonists of RAR -
-induces apoptosis in glands including sebaceous
Oral
Acne

54
Q

Tretinoin Mechanism

A

targets RAR to effect cell differentiation and proliferation

Acne

55
Q

Toxicity: Adapalene, Isotretinoin, Tretinoin

A

dry skin, nose bleeds, loss of vision, hair loss
(vit A toxicity)
Isotretinoin: Oral Teratogen
Adapalene, Tretinoin: Topical - red, burn, sting, increased UV sensitivity

56
Q

Tazorotene Mechanism

Acitretin Mechansim

A

RAR agonist - promotes cell differentiation
Acne & Psoriasis
Topical - red, burn, sting, increased UV sensitivity

57
Q

Hydrocortisone
Beclomethasone
Clobetasol Proprionate

A

-anti-inflammatory, antipruritic, vasoconstrictive
-increse lipocortins production, decrease inflammatory mediators
mild-hydro
moderate-beclo
very potent-clobetasol

58
Q

Amorolfine

A

Inhibits ergosterol synthesis

  • topical only, limits absorption
  • may irritate if skin abrasions, hypersensitivity
59
Q

Ciclopirox

A

poorly understood, loss of function of catalase/ peroxidase
topical only
-may irritate if skin abrasions, hypersensitivity
onchomycosis topical, local tinea (topical)

60
Q

Naftifine

A

-gram +/- bactericidal
-anti-inflammatory via inhibition of inflammatory mediators: prostaglandins, leukotrienes, histamine (vasoconstriction)
Topical-hepatic meta, renal elim
CAT B
CAN’T use with topical azoles (inhibits sterol production at earlier point than azoles-no effect)
-no systemic drug interactions

61
Q

Fluconazole

A

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, a CYP enzyme needed to convert lanosterol to ergosterol
CYP2C9
QT prolongation, liver toxic, CAT D
High CSF
for: Tenia widespread, onychomycosis (oral)

62
Q

Posaconazole

A

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, a CYP enzyme needed to convert lanosterol to ergosterol
CYP3A4
QT prolongation, liver toxic, CAT C

63
Q

Terbinafine

A

Inhibits squalene epoxidase, decreased ergosterol synthesis
-well tolerated (long half-life, rare hepatotoxicity)
-transient lymphopenia & neutropenia with oral
avoid for immunosuppressed (infection)
routine CBC
-CAT B

for: Tenia widespread, onychomycosis (oral)
      Tenia local (topical)
64
Q

Itraconazole

A

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, a CYP enzyme needed to convert lanosterol to ergosterol
CYP3A4
weakens heart, liver toxic, CAT C
for: Tenia widespread, onychomycosis (oral)

65
Q

Voriconazole Mechanism

A

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, a CYP enzyme needed to convert lanosterol to ergosterol
CYP2C19
QT prolongation, liver toxic, CAT D

66
Q

Cephalosporins

A

beta-lactame that inhibit cell wall synthesis
MRSA, enterococci
-hypersensitivity, Vit K deficiency

67
Q

Vancomycin

A

-Inhibits cell wall mucopeptide by binding D-ala D-ala portion of cell wall precursors
Gram +
Nephrotoxicity, Ototoxicity, Thrombophlebitis “flushing”

68
Q

Trimethoprim/Sulfamethaxazole

A

-Inhibits bacterial dihydrofolate reductase
-block folate acid synthesis
Toxicity: Megaloblastic anemia, leukopenia, granulocytopenia

Dermatology (9 decks)

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