Folate & DNA synthesis inhibitors Flashcards

1
Q

What principle is used for Anti-folates?

A

Bacteria can’t produce folic acid exogenously; must be made from PABA

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2
Q

Sulfonamide - MOA

A

Inhibit dihydropteroate synthase

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3
Q

Trimethoprim - MOA

A

Inhibit dihydrofolate reductase

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4
Q

Cotrimoxazole - MOA

A

Combination of Sulfonamide & Trimethoprim

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5
Q

Are Sulfonamide & Trimethoprim bacteriostatic/cidal?

A

Both bacteriostatic, but if combine = bactericidal

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6
Q

Anti-folates - PK

A

Good oral

Good CSF - TMP > SMZ

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7
Q

Sulfonamide - Spectra

A

Gram +ve & -ve

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8
Q

Trimethoprim - Spectra

A

Same as sulfonamides; given when allergic to sulfonamides

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9
Q

Cotrimoxazole - Spectra

A

MRSA

Can be used in immunocompromised pts

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10
Q

Anti-folates - SE

A
GI
Allergy (sulfa)
Photosensitivity
Renal
Hyperkalemia
BM suppression (give folinic acid if pregnant, malnourished)
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11
Q

Sulphonamides - DDI

A

1) Enhance oral anticoags
2) Potentiate sulfonylurea hypoglycemic agents & hydantoin anticonvulsants
Since 2) is via albumin displacement = cause Kernicterus

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12
Q

Trimethopirm - DDI

A

Enhance Warfarin
Increase Methotrexate
Increase half-life of Phenytoin

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13
Q

Name 2 groups of DNA synthesis inhibitors

A

Fluoroquinolones & Nirofurantoin

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14
Q

Fluoroquinolones - MOA

A

Inhibit DNA gyrase

High conc - inhibit Topoisomerase IV

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15
Q

Fluoroquinolones - PK

A

Good oral

Good CSF

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16
Q

Fluoroquinolones - Dosing

A

Can give OD if renal fx okay

17
Q

Fluoroquinolones - Spectra

A
Broad spec
Gram +ve - Strep pneu
Anaerobe
Atypical
Gram -ve - P.aeruginosa
18
Q

Fluoroquinolones - Clinical

A

2nd line - TB

19
Q

Fluoroquinolones - SE

A
GI
CNS - Seizures
Hypersensitivity
QT prolongation (Moxifloxacin > Ciprofloxacin, Levofloxacin
Joint swelling
Tendonitis & tendon rupture
20
Q

Nitrofurantoin - MOA

A

Bacterial nitrofuran reductase -> reduce parent drug into reactive intermediate -> damage bacterial DNA

21
Q

Nitrofurantoin - Spectra

A

Narrower than FQ
Gram +ve - MRSA
Gram -ve - E.coli

22
Q

Nitrofurantoin - PK

A

Good oral

Alkaline urine reduces anti-microbial activity

23
Q

Nitrofurantoin - SE

A

GI
Hypersensitivity
Pulmonary interstitial fibrosis - esp elderly
Blood dyscrasias, Hemolysis in infants & G6PD-deficient
Colors urine brown

24
Q

Fluoroquinolones - DDI

A
Theophylline
NSAIDs
Warfarin
Antacids - decr FQ absn
CYP inhibitor - incr FQ
25
Q

Nitrofurantoin - DDI

A

Antacids - decr absn of NF

26
Q

Metronidazole - MOA

A

Nitroreductase -> Cytotoxic metabolites -> Bind to DNA

27
Q

Metronidazole - Spectra

A

Cannot use on Aerobes bc they lack Nitroreductase
C.difficile
Amebiasis
H.pylori

28
Q

Metronidazole - SE/CI

A

BM suppression

CI: 1st trimester

29
Q

Metronidazole - DDI

A

Warfarin

Alcohol - disulfiram reaction