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Cology 2 Exam 2 > The -lides > Flashcards

The -lides Flashcards

1
Q

How do macrolides work?

A

Binds the 50s subunit to interfere with the initiation coplex (50s and 30s don’t come together)

Interferes with transfer of t-RNA complex from A to P site to prevent elongation

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2
Q

Name the macrolides

A

Erythromycin
Clarithromycin
Azithromycin

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3
Q

What do macrolides work against?

A 
Gram + cocci, bacilli
Chlamydia
Legionella
H influenzae
H pylori
Respiratory infections
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4
Q

What is the difference between the macrolides

A

Erythromycin was discovered from streptomyces erythreus

Clarithromycin has an OCH3 group
Azithromycin has an N-CH3 group

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5
Q

How are macrolides admnistered?

A

Enteric coated tablets bc they are inactivated by acid

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6
Q

True or False: Macrolides cross the BBB

A

False

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7
Q

True or False: Macrolides are safe in pregnancy

A

False - they cross the placenta

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8
Q

How are macrolides excreted?

A

Biliary excretion

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9
Q

What toxicities do you worry about with macrolides?

A

Cholestatic hepatitis
Sensitivity reactions
GI disturbances
Tinnitus, hearing loss (reversible!)

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10
Q

True or False: Hearing loss from macrolides is reversible

A

True

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11
Q

What is Erithromycin used for?

A

Can also be used to stimulate GI tract after surgery (can be used to treat gastroparesis)

Also used for pertussis

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12
Q

Which macrolides can cause QT prolongation? When?

A

Erithromycin

When given with antihistamines, ketoconazole?

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13
Q

Which macrolides can inhibit CYP3A4? What drug levels does this affect?

A

Erithromycin and azithromycin

Affects theophylline, warfarin, digoxin levels

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14
Q

What is clarithromycin used for?

A

H pylori
Community pneumonia
Mycobacterium avium - intracellular

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15
Q

What is azithromycin used for?

A

H influenzae
Community pneumonia
Mycobacterium avium-intracellular

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16
Q

What causes resistance with macrolides?

A

Active transport out of the bacteria

Decreased binding to ribosomes

Increased metabolism by esterases

50s ribosomal mutations

17
Q

How do ketolides work?

A

Binds 50s subunit; interferes with initiation complex

Interferes with transfer of peptide t-RNA complex from A to P site

Prevents elongation

18
Q

Name the ketolides

A

Telithromycin

19
Q

What is telithromycin?

A

A ketolide; semi-synthetic derivative of erythromycin

20
Q

How do ketolides differ from macrolides?

A

Less metabolic and efflux mediated resistance than macrolides

21
Q

What is telithromycin used for?

A

Community acquired pneumonia in adults over 18 ONLY

22
Q

What was the FDA debacle with telithromycin?

A

In 2001 FDA panel tried to approve it for community acquired pneumonia, bronchitis, and sinusitis

FDA approved in 2004

February 2007 withdrew approval due to hepatotoxicity! BAD

23
Q

Which agent has a black box warning for myasthenia gravis?

A

Telithromycin

24
Q

What are the toxicities associated with telithromycin?

A

Hepatotoxicity (leading to death or liver transplants)

Visual disturbances due to slow accomidation, anticholinergic effects

GI distress

QT prolongation, arrhythmias

Black box warning in myasthenia gravis

25
Q

Drug interactions with telithromycin?

A

CYP3A4 inhibitor so don’t use with statins (can cause rhabdomyolsis)

26
Q

What is clindamycin?

A

A lincosamide; drug of choice for lung abscess and anaerobic lung and pleural space infections

27
Q

How do lincosamides work?

A

Binds 50S subunit; interferes with transfer of peptide t-RNA complex from site A to P site

Prevents elongation

28
Q

What is clindamycin used for?

A

Gram+, anaerobic, penicillin resistant staph and strep

Drug of choice for lung abscess and anaerobic lung and pleural space infections

Also used in necrotizing fasciitis because it inhibits toxin production (caused by streptococcus pyogenes)

29
Q

Which drug is used for necrotizing fasciitis?

A

Clindamycin; it inhibits toxin production, doesn’t actually kill the bacteria

30
Q

What toxicities are associated with clindamycin?

A

Diarrhea (20%) - c diff
Skin rash (stevens johnson syndrome)
Can inhibit neuromuscular transmission, potentiates NM blockers

31
Q

What resistance occurs with clindamycn?

A

Altered metabolism to increase methylation

Cology 2 Exam 2 (18 decks)

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