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Drugs 2 Flashcards

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
Minocycline Use
leprosy
26
Thalidomide Mechanism
``` inhibits Nf(kappa)B transcriptional upregulation & TNF-alpha production -blocks leukocyte migration ```
27
Thalidomide Toxicity
Teratogen -increase in plasma HIV viral load somnolence>rash>headache peripheral neuropathy
28
Thalidomide Use
leprosy
29
Adalimumab Mechanism
IgG1 monoclonal antibody, binds to TNF-alpha
30
Adalimumab Use
SC | psoriasis, arthritis, spondylitis, crohn's
31
Adalimumab Toxicity
Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB Don't give with immunsuppressives/vaccines
32
Etanercept Mechanism
Receptor-ab fusion protein: p75 TNF receptor and Fc IgG1 | binds to TNF alpha
33
Botulinum Toxin Mechanism
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
Botulinum Toxin Pharm
- local injection - cause muscular paralysis-blocks muscarinic and nicotinic receptors - used for cosmetic smoothing of wrinkles - migraine headache
35
Botulinum Toxin Toxicity
- 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
Glycopyrrolate Mechanism
off label for sweating | systemic antimuscarinic agents, don't cross BBB
37
Propranolol Mechanism
reduce sympathetic CNS stimulation - emotional stability improved -off label for sweating
38
Diltiazem Mechanism
blocks Ca2+ channels involved in secretion process | off-label for sweating
39
Etanercept use
SC | psoriasis, arthritis, spondylitis,
40
Etanercept Toxicity
Contraindication: Sepsis Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB Don't give with immunsuppressives/vaccines
41
Infliximab Mechanism
Chimeric monoclonal ab (cariable region of mouse monoclonal ab on human IgG1) binds TNF-alpha
42
Infliximab Use
IV | psoriasis, arthritis, spondylitis, colitis, Chrohn's
43
Infliximab Toxicity
Contraindication: CHF, murine protein, hypersensitivity Black Box: infection:fungal,mycobacterial, viral, noeplasia, TB Don't give with immunsuppressives/vaccines
44
Ustekinumab Mechanism
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
Ustekinumab Toxicity/Use
psoriasis - increase risk of infection & neoplasm - live vaccination contraindicated - test for latent TB before - Anaphylactic rxns reported
46
Calcipotriene Mechanism
-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
Calcipotriene Use
psoriasis
48
Clacipotriene Toxicity
``` 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
Calcitriol Mechanism
hormonally active form of vit D3 better tolerated in intertiginous and sensitive areas of skin -comparable safety to calcipotriene PSORIASIS
50
Benzoyl Peroxide
-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
Salicylic Acid
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
Adapalene Mechanism
Retinoid: selectively binds to nuclear retinoic acid receptor RAR beta and gamma, inhibits keratinocyte differentiation -exfoliation and anti-inflammatory effects Acne
53
Isotretinoin Mechanism
converted inside cell to metabolites that are agonists of RAR - -induces apoptosis in glands including sebaceous Oral Acne
54
Tretinoin Mechanism
targets RAR to effect cell differentiation and proliferation | Acne
55
Toxicity: Adapalene, Isotretinoin, Tretinoin
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
Tazorotene Mechanism | Acitretin Mechansim
RAR agonist - promotes cell differentiation Acne & Psoriasis Topical - red, burn, sting, increased UV sensitivity
57
Hydrocortisone Beclomethasone Clobetasol Proprionate
-anti-inflammatory, antipruritic, vasoconstrictive -increse lipocortins production, decrease inflammatory mediators mild-hydro moderate-beclo very potent-clobetasol
58
Amorolfine
Inhibits ergosterol synthesis - topical only, limits absorption - may irritate if skin abrasions, hypersensitivity
59
Ciclopirox
poorly understood, loss of function of catalase/ peroxidase topical only -may irritate if skin abrasions, hypersensitivity onchomycosis topical, local tinea (topical)
60
Naftifine
-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
Fluconazole
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
Posaconazole
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
Terbinafine
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
Itraconazole
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
Voriconazole Mechanism
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
Cephalosporins
beta-lactame that inhibit cell wall synthesis MRSA, enterococci -hypersensitivity, Vit K deficiency
67
Vancomycin
-Inhibits cell wall mucopeptide by binding D-ala D-ala portion of cell wall precursors Gram + Nephrotoxicity, Ototoxicity, Thrombophlebitis "flushing"
68
Trimethoprim/Sulfamethaxazole
-Inhibits bacterial dihydrofolate reductase -block folate acid synthesis Toxicity: Megaloblastic anemia, leukopenia, granulocytopenia

Dermatology (9 decks)

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