Protein synthesis inhibitors Flashcards by Melissa Ring

What are the main categories of protein synthesis inhibitors

Aminoglycosides
lincosamides
oxazolidinone
Macrolides
Streptogramins
tetracyclines

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What drugs are considered aminoglycosides

Gentamicin
Amikacin
Tobramycin

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What type of drugs are considered lincosamides

Clindamycin

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What type of drugs are considered oxazolidinones

Linezolid

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What type of drugs are considered Macrolides

Azithromycin
Clarithromycin
Erythromycin

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What type of drugs are considered tetracyclines

Doxycycline
Minocycline
Tetracycline

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What are the ribosomal subunits of protein synthesis that antibiotics can effect

30S
50S
tRNA

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Which antibiotics effect 50s protein synthesis

Erythromycin
Chloramphenicol
Clindamycin

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Which antibiotics effect 30s protein synthesis

tetracycline
gentamycin
tobramycin
amikacin

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60% of classes of antibiotics target which part of the cell

Ribosomes / ribosomal RNA

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Where on the ribosome do antibiotics bind

at moving parts

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Aminoglycosides target which ribosomal subunit and are considered bactericidal or static

30s
bactericidal

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Tetracyclines target which ribosomal subunit and are considered cidal or static

30s
bacteriostatic

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Which bacteriostatic antibiotics target the 50s ribosomal subunit

Chloramphenicol
Clindamycin
Macrolides

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which antibiotics are both bactericidal AND bacteriostatic and target the 50s ribosomal subunit

Linezolid
Streptogramins

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What is the main target for aminoglycosides

Pseudomonas

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What kind of interaction do aminoglycosides have when paired with B-lactams and vancomycin

synergistic

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Do aminoglycosides have CNS penetration or GI absorption

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What are the major side effects of aminoglycosides

Ototoxicity (Permanent)
vestibular toxicity (permanent)
renal toxicity (Reversible)

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What drugs do you not combine with aminoglycosides

Loop diuretics

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What is a complete contraindication for using aminoglycosides

M. Gravis

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What type of drug is gentamicin and how is it administered

Aminoglycosides
IM / IV

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What is gentamicin used for

Serious gram neg infections
-pseudomonas
-Enterobacter
-proteus

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If a patient who has CF contracts pseudomonas or enterobacter… what would be the first line of treatment

gentamicin

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When is Amikacin used

For gentamicin resistant bacteria

Would you administer a patient neomycin via IV

No, oral only because of toxicity

What is neomycin generally given for

Bowel surgery prophylaxis

What is the most widely used tetracycline

Doxycycline

Which type of tetracycline is best for someone with a CNS infection and why

Minocycline because its more hydrophobic

If a patient has chlamydia, rickettsia, or mycoplasma, what is the drug of choice to treat

Tetracycline

What is the number 1 Lyme treatment in the country

Doxycycline

What do you recommend to your patient who you are prescribing tetracycline to avoid GI distress

Take with food DO NOT take with dairy or antacids

Which form of tetracycline is safe for renal impaired patients

Doxycycline

What are the adverse effects of tetracycline

Photosensitivity Superinfections Calcified tissue growth inhibitor in kids Causes yellowing of teeth in kids

What is a new class of antibiotics derived from minocycline

Glycylcycines

When are tigecyclines used (glycylcycines)

As a last resort for MRSA, VRE and enterobacteria

What is the mechanism of action for chloramphenicol

Binds 50s subunit which blocks aminoacyl binding to acceptor site which inhibits peptidyl transferase and thus translation

What is unique about chloramphenicol

crosses the blood brain barrier

Where is chloramphenicol generally used

Mostly outside the US for Rocky Mountain spotted fever

What is the major adverse effect of chloramphenicol

grey baby syndrome (incomplete hepatic development)

What is erythromycin useful for

an alternative to penicillin for gram positive infections

How do clarithromycin and erythromycin differ

Clarithromycin has better activity against H. influenza, chlamydia, legionella, moraxella and helicobacter pylori

What is a generic name for azithromycin

Z pack

What is azithromycin typically used for

respiratory tract infections Strep pharyngitis in PCN allergic patients

What is the drug of choice for Chlamydial STI

Azithromycin

Why is Erythromycin not administered via IV

It is associated with high incidence of thrombophlebitis

Why is azithromycin not given with food

food inhibits absorption

What is unique of azithromycin as a macrolide

Has the longest half life (68 hours)

Which patients would you not prescribe a macrolide

patients with hepatic dysfunction

What drug to drug interaction do you have to be aware of with macrolides

They cause CYP inhibition, so drugs like Digoxin will not be metabolized by the liver correctly and increase the levels in the body

What is the mechanism of action for clindamycin

Inhibits peptidyl transferase by binding to the 50s ribosomal subunit

How can clindamycin be administered

IV or PO

Is clindamycin narrow or broad spectrum

Narrow spectrum for gram + cocci

What is the primary use of clindamycin

Anaerobic bacterial infections MRSA

If someone comes in with an abscess, what would you treat them with and why

Clindamycin because it is able to penetrate an abscess

What are major causes of C.Diff or pseudomonas colitis

Doxycycline Clindamycin

What is the MOA for Linezolid

Binds to the 50s ribosomal subunit to inhibit protein synthesis

Is Linezolid bactericidal or bacteriostatic

Mostly bacteriostatic

What is linezolid bactericidal against

Streptococci and C. perfringens

What is the most common use for Linezolid

MRSA and VRE but is NOT the first line agent

What are the adverse effects of Linezolid

Serotonin syndrome when used in combo with anti-depressants Dose dependent Thrombocytopenia

What are the main categories of antimetabolites / DNA gyrase inhibitors

Fluoroquinolones Nitroimidazole Rifamycins Nitrofurantoin

What are the drugs that are involved with folate synthesis inhibitors

TMP-SMX Co-trimoxazole

Which antibiotics are dihydrofolate reductase inhibitors

Trimethoprim

What is the MOA for fluoroquinalones

They inhibit type 2 topoisomerase (inhibit DNA duplication)

What antibiotics make up fluoroquinalones

Ciprofloxacin Levofloxacin Ofloxacin Moxifloxacin

What is Moxifloxacin

4th gen fluoroquinolone that is safe for those with renal disease

What is second generation fluoroquinolone and what is it useful against

Ciprofloxacin Psuedamonas aeruginosa* *Think staph coverage

What is third generation fluoroquinolone and what is it useful against

Levofloxacin Strep pneumoniae *Think for respiratory infections

What is 4th generation fluoroquinalones

Moxifloxacin -> not for pseudomonas aeruginosa

If a patient comes in after taking antibiotics with tendinopathy or an achilles tendon rupture, what antibiotic were they most likely on

Cipro or other fluoroquinalones

What other adverse effects happen with fluoroquinalones

QT prolongation articular cartilage erosion during development (avoid in children and pregnancy)

Patient presents with bacterial sinusitis caused by S. pneumoniae, H.influenza, or M.catarrhalis, what is the first line agent for treatment

Amoxicillin or amoxicillin+calvulanate

Patient presents with bacterial sinusitis caused by S. pneumoniae, H.influenza, or M.catarrhalis, what is the first line agent for treatment if they are allergic to penicillin

Doxycycline

What is a last resort alternative for penicillin allergic patients with bacterial sinusitis

Respiratory fluoroquinolone (levo or moxifloxacin)

A patient with severe sinusitis presents with bacterial bronchitis (most likely cause by pseudomonas). What are you going to treat them with first

IV antipsuedamonal such as cefepime

What are the most common cause of a UTI

E.Coli staph K. pneumoniae

A patient presents with a UTI, what are you going to treat them with

Nitrofurantoin Amoxicillin Cephalosporin Trimethoprim/sulfamethoxazole (if not pregnant)

What is the brand name of Nitrofurantoin

Macrobid

When is Nitrofurantoin used

UTIs

What is the most common species targeted by metronidazole

Bacteroides

A patient presents with Helicobacter Pylori infection, what might you give them as a treatment

Metronidazole

What is the most common side effect of metronidazole

GI upset

What are you going to advise your patient that is taking metronidazole

Avoid alcohol

What is the MOA for sulfonamides

They inhibit folate metabolism

What is the MOA for Trimethoprim

Inhibit dihydrofolate reductase

Which antibiotics make up Bactrim and why

Sulfamethoxazole and trimethoprim They are bacteriostatic alone but when combined turn bactericidal

What is the dosing ratio of sulfamethoxazole trimethoprim

5:1

What are the common side effects of Bactrim

Rash (common) SJS (rare) Neonatal kernicterus

What is neonatal kernicterus

Bilirubin encephalopathy caused by sulfa

What is Bactrim most useful against

UTI Biliary tree infections PJP Toxoplasmosis Salmonella

What is the MOA of Rifampin

Inhibit RNA polymerase Bactericidal

When is rifampin used

Mycobacterium tuberculosis (cannot use alone)

Why do you have to be careful when giving rifampin

There is a large capacity for drug-drug interactions

What is an adverse effect of rifampin

Orange-red tears, saliva, urine & sweat

What is the MOA of Isoniazid

Inhibits the synthesis of mycolic acids (Essential component of mycobacterial cell wall)

What combo of drugs treats most strains of TB

Isoniazid and Rifampin

What are the phases of treating TB

Intensive phase: 4 drug combo (2 months) The last 7 months: Isoniazid and rifampin

What is ethambutol MOA

Inhibits mycobacterial arabinosyl transferase

How is ethambutol given and why

With other anti-TB drugs to prevent resistance