ABs that are inhibitors of Nucleic Acid Synthesis Flashcards

1
Q

what are the 3 ABs that are inhibitors of nucleic acid synthesis

A

sulfonamides, trimethoprims, and rifampin

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2
Q

MoA of sulfonamide?
static or cidal
selectivity?
spectrum: gram - or gram +

A

Sulfonamides are competitive inhibitors of dihydropteroate synthase this inhibiting synthesis of folic acid
static!!
act on both gram - AND gram +
selective against bacteria bc humans don’t produce their folate that get it from diet

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3
Q

what are the clinical uses of sulfonamides?

A

UI, toxoplasmosis, Malaria, prophylactic

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4
Q

Sulfonamides
absorption:
distribution/ excretion:
Toxicity

A
sulfonamides
taken orally 
crosses BBB 
excreted really
dose related and dose unrelated toxicities
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5
Q

what are the dose related toxicities of sulfonamides

A

Crystalluria- take with lots of water!
hemolytic anemia
GI upset
Kernicterus- displaces albumin bound bilirubin, in newborns this will allow bilirubin to cross BBB leading to encephalopathy

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6
Q

what are the dose UNRELATED toxicities of sulfonamides

A

hypersensitivity- Stevens Johnson syndrome

photosensitivity

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7
Q

What is the special note about sulfonamides?

A

DO NOT use in newborns! causes kernicterus- bilirubin passing BBB and causing encephalopathy

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8
Q

What AB is a inhibitor of dihydrofolate reductase, a structural analog of ptreridine?
static or cidal? MoA

A

trimethoprim, MoA = inhibitor of folic acid synthesis

STATIC!

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9
Q

Trimethoprim spectrum?

clinical uses?

A

trimethoprim is effective against gram - and gram + = broad spectrum
clinically used for: UI, prostatitis, Pneuomocystis jarovecil (in AIDS pts)
TX for community acquired MRSA

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10
Q

Community acquire MRSA can be treated with what?

A

trimethoprim

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11
Q

Trimethoprim toxicities a mild but can result in what
absorption:
distribution:

A

Trimethoprim taken orally, penetrates CNS, excreted renally, can cause blood Dyscrasias
and can cause anemias

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12
Q

What AB bind to and inhibits RNA polymerase?
is this drug static or cidal?
Route of admin?

A

rifampin
CIDAL!
taken orally

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13
Q

Rifampin is used to treat what and how?

Spectrum of rifampin?

A

Rifampin is used in combo with other drugs as 1st line of defense against TB
Spectrum: M tuberculosis and some staphylcocci

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14
Q

Rifampin is used to treat TB, what else it is used to treat?

A

Rifampin is used to resistant staph infections, meningitis

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15
Q

What is important to tell pts when taking Rifampin about the distribution of the drug?

A

Rifampin causes urine, feces, saliva, sputum, and tears to turn red orange

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16
Q

What is important about the metabolism of Rifampin?

A

Potent inducer of hepatic microsomal enzymes and INC metabolism and dec half life of HIV protease and non nucleoside reverse transcriptase inhibitors. So pts with HIV given Rifabutin (analog of rifampin)

17
Q

Metabolism of Rifampin

A

liver p450 enzyme mediated deacetylation

18
Q

toxicity of rifampin?

A

liver damage - jaundice- effected by p450!