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Pharm 2 Part 3: Chemotherapy and Antibiotics and Antifungals > Pharm: L27: Macrolides > Flashcards

Pharm: L27: Macrolides Flashcards

1
Q

Inhibitors of Protein Synthesis

  1. What 7 Groups?
  2. All of these are 50 S INHIBITORS EXCEPT for what 2?
  3. ALL ARE BACTERIOSTATIC EXCEPT FOR WHICH GROUP?
A
  1. Macrolides
  2. Ketolides
  3. Clindamycin
  4. Streptogramins
  5. Oxazolidinones
  6. Aminoglycosides
  7. Broad Spectrum Antibiotics
  8. AMINOGLYCOSIDES and TETRACYCLINES (broad spectrum): They’re 30S inhibitors
  9. Except for AMINOGLYCOSIDES
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2
Q

Macrolides (1)

  1. What are the 3 Macrolides? (ACE)
  2. Big thing to know about a patient when giving them the BACTERIOSTATIC DRUGS?
A
  1. Azithromycin
  2. Clarithromycin
  3. ERYTHROMYCIN
  4. THEY HAVE TO HAVE A COMPETENT IMMUNE SYSTEM!
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3
Q

Macrolides (2)

  1. Routes of Administration
    a. Azithromycin

b. Clarithromycin
c. ERYTHROMYCIN

A
  1. a. Oral, IV
    b. ORAL ONLY
    c. ORAL, IV
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4
Q

Macrolides (3):

  1. ERYTHROMYCIN
    a. Differences: Clarithromycin
    b. Differences: Azithromycin
  2. What do these DRUGS do?
    a. Bind to what exactly?

b. Bacteriostatic/cidal?
c. How do we normally take them?
d. How does the body get rid of them?

A
  1. a. like Erythromycin
    b. Better PHK
  2. Inhibit PROTEIN SYNTHESIS
    a. Binds reversibly to 50 S ribosomal Subunits
    b. Bacteriostatic; -cidal activity depends on concentration and organism being treated
    c. Orally
    d. Biliary Excretion: Fecal Elimination
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5
Q

Macrolides (4)

  1. Antibacterial Spectrum
    a. Similar to what?
    b. Which organism type is MOST SUSCEPTIBLE?

c. Majority of what Organisms are RESISTANT to ERYTHROMYCIN?
d. What is an Alternative Therapy for H. Pylori?

A
  1. a. to PEN G (good alternative)
    b. G + MOST SUSCEPTIBLE
    c. Majority of G- Organisms

d. Clarithromycin + Omeprazole (+ Ampicillin)

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6
Q

Macrolides (5)

  1. Resistance: 2 ways resistance is built up against these 3 drugs?
A
  1. EFFLUX PUMPS and METHYLATION of Drug BINDING SITE (Ribosome)
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7
Q

Macrolides (6): Toxicity

  1. Major Issues?
  2. Which 1 of these has the MOST ADVERSE GI EFFECTS?
    a. The LEAST?
  3. What can cause Ototoxicity?
  4. Other issue?
A
  1. GI DISTURBANCES and DIARRHEA
  2. ERYTHROMYCIN
    a. Clarithromycin
  3. IV Erythromycin (seldom used though)
  4. HEPATIC CHANGES
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8
Q

Macrolides (7): Drug Interactions

  1. Erythromycin is a POTENT INHIBITOR of WHAT?
    a. This can inhibit what?
  2. What about Clarithromycin?
  3. and Azithromycin?
A
  1. of CYP3A4
    a. can inhibit hepatic metabolism of other drugs that require CYP3A4, increasing their serum concentrations and potentially causing toxicity.
  2. Similar to Erythromycin
  3. More favorable
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9
Q

Macrolides (8): Drug Interactions 2

  1. SERIOUS PROLONGATION of what?
    a. When does this happen?
  2. Carithro?
  3. Azithro?
A
  1. SERIOUS QT PROLONGATION and cardiac arrhythmias
    a. when erythromycin was coadministered with (also due to CYP3A4 inhibtion): CISAPRIDE or PIMOZIDE; SPARFLOXACIN or GREPAFLOXACIN
  2. Similar
  3. MUCH FAVORABLE
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10
Q

Macrolides (9): Drug Interactions (Really..just know this)

  1. GI-Diarrhea
    a. Worst drug?
    b. Best drug?
    c. Kind of in the middle?
  2. Drug Interaction
    a. Worst Drug?
    b. Flip Flopper?
A
  1. a. Erythromycin
    b. Clarithromycin
    c. Azithromycin
  2. a. Erythromycin and Clarithromycin
    b. Azithromycin (kind of flip flops) depending on drug interaction
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11
Q

Macrolides

  1. ERYTHROMYCIN is the DOC for what?
A
  1. Urogenital infections due to CHLAMYDIA during PREGNANCY!!
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12
Q

Ketolides (DWAI on KETOLIDES..just know the drug name and what it does)

  1. What drug is in it?
    a. What does it do?
A
  1. TELITHROMYCIN

a. Blocks Bacterial Protein SYNTHESIS

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13
Q

Ketolides (2): (Telithromycin):

  1. Spectrum
    a. What SPECTRUM IS IT?
    b. Good against what?
    c. Also has activity against what 2 type of bacteria?
    d. What does it AFFECT?
  2. Pharm
    a. Route of administration?
    b. How effective is it compared to Clarithromycin and Amoxicillin?
    c. How is it metabolized?
    d. Inhibitor of what?
    e. Half Life?
A
  1. a. BROAD SPECTRUM
    b. Good against Repiratory pathogens
    c. Good against Intracellular and Atypical Bacteria
  2. a. ORAL
    b. As effective as Clarithromycin and HIGH DOSE Amoxicillin for some infections
    c. By CYP3A4
    d. of CYP3A4( Reversible inhibitor: Slow inhibitor so it can still be metabolized)
    e. 9-10 hrs (just means you just need less frequent dosing…don’t really need to know the hours)
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14
Q

Ketolides (3): Telithromycin

  1. Main cause?
  2. CI in what?
  3. Last resort. Why?
A
  1. DIARRHEA!
  2. Pts w/Myasthenia Gravis
  3. HEPATOTOXICITY (children have died from using it…not first choice…use a MACROLIDE)
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15
Q

Clindamycin

  1. Route of Administration?
  2. Binds to what?
  3. Active against what?
  4. Bacteriostatic/Cidal?
  5. How does the body get rid of it?
A
  1. ORAL, PARENTERAL, Topical
  2. 50 S Ribosomal Subunits and Inhibits Protein Synthesis
  3. a Wide range of AEROBIC G+ COCCI and several ANAEROBIC G- and G+ Organisms
  4. Both. Depends on concentration at site of action and specific susceptibility of the organism
  5. Liver metabolizes it and minimally excreted by the Kidneys
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16
Q

Clindamycin (2): Therapeutic Use

  1. MANY species of Streptococci (except for Enterococci) and staphylcocci are extremely susceptible (MRSA)
  2. Good against Toxic Shock Syndrome. Use with what drug?
  3. What else?
A
  1. Vancomycin
  2. OSTEOMYELITIS (obtains high concentration in bones) *Big thing to know.
    * Can also be used to treat Toxoplasma Encephalitis
17
Q

Clindamycin (Toxicity) (3)

  1. WELL KNOWN CAUSE of what?
  2. Avoid while doing what?
A
  1. PSEUDOMEMBRANOUS COLITIS! (Overgrowth of Clostridium Difficile)
  2. while nursing. it can cross the placenta easily and can be distribute into breast milk
18
Q

Streptogramins (don’t really need to know the group)

  1. 2 Drugs we talked about?
  2. What does each one do?
  3. How should they be administered?
    a. Bactericidal against what types of bacteria?
A
  1. Dalfopristin and Quinupristin
  2. Dalfopristin: binds to 50S ribosomal Particle and Inhibits EARLY PHASE of Protein Synthesis

Quinupristin: binds to 50S Subunit and inhibits the LATE PHASE of protein synthesis

  1. TOGETHER (IV Infusion): Act SYNERGISTICALLY against susceptible Bacteria
    a. G+, AEROBES; COMBO is BACTERICIDAL
19
Q

Streptogramins (Dalfopristin and Quinupristin)

  1. Used against what?
  2. Pharm?
A
  1. VANCOMYCIN-RESISTANT Enterococcus Faecium Bacteremia
  2. MSSA and MRSA (complicated skin and skin-structure infections due to S. Aureus)
  3. PENICILLIN RESISTANT S. Pneumoniae, MDR-Streptococci
  4. SYNERCID (Dalfopristin and Quinuspristin (Synercid)…not sure if it means both… is administered by IV infusion
20
Q

Streptogramins (Dalfopristin and Quinupristin)

  1. Adverse Reactions
  2. CIs?
A
  1. Hepatotoxicity; GI; Inhibit P450 drug metabolizing system (CYP3A4, and have MANY METABOLIC INTERACTIONS (warfarin, diazepam, etc))
  2. Breast-feeding, children, hepatic disease, pregnancy, and streptogramin hypersensitivity
21
Q

Oxazolidinones (dont really need to know class name…just drug)

  1. What’s the drug?
  2. Main activity is AGAINST what?
  3. MOA?
A
  1. LINEZOLID
  2. AEROBIC G+ ORGANISMS!
  3. Inhibits Protein Synthesis; binds to 50S. BACTERIOSTATIC, Except for Streptococci it’s BACTERIOCIDAL
    * Prevents formation of a Functional 70S Initiation Complex!
22
Q

Oxazolidinones (LINEZOLID)

  1. Use for what kind of infections?
  2. Pharm
    a. How is it Taken?
    b. Bioavailability?
    c. How does the body get rid of it?
A
  1. G+ INFECTIONS (Bacterial Pneumonia, skin and skin structure infections, VRE infections and MRSA)
  2. a. IV or Oral
    b. 100% (rarely seen)

c. metabolized via Oxidation but oxidative metabolism of Linezolid is non-enzymatic and Doesn’t involve hepatic microsomal oxidative system

23
Q

Oxazolidinones (LINEZOLID): Adverse Reactions

What are they?

A
  1. Diarrhea
  2. REVERSIBLE, Non-SELECTIVE INHIBITOR of MAO (HUGE ISSUE….SSRIs…etc are a problem) (can lead to Serotonin Toxicity) (Only Antibiotic that does this!)
  3. Superinfection
24
Q

Oxazolidinones (LINEZOLID):

  1. CIs? (2)
  2. Drug Interactions?
A
  1. Hypersensitivity and Pheochromocytoma
  2. B-Blockers, General Anesthetics, Local Anesthetics (Epi), Sympathomimetics, MAO INHIBITORS!

Heterocyclic antidepressants, tricyclic antidepressants, SSRIs

Pharm 2 Part 3: Chemotherapy and Antibiotics and Antifungals (7 decks)

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