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Pharm Exam V > Antibiotics IV - Miscellaneous > Flashcards

Antibiotics IV - Miscellaneous Flashcards

1
Q

Daptomycin:

MOA?

Use?

A

Daptomycin:

MOA: lipopeptide that inserts into the membrane of G+ bacteria, disrupts potential, and inhibits RNA/DNA synthesis. Bactericidal

Use: Reserved for serious or MDR G+: VSE (vancomycin suceptible Enterococcus faecalis), MRSA skin infection, and drug resistant Strep. Right sided endocarditis. NOT for pneumonia (surfactant inactivates daptomycin)

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2
Q

Daptomycin:

Adverse effects?

Administration and resistance?

A

Daptomycin:

AE: injection site reactions, caution with aminoglycosides ( increases nephrotoxicity) or statins (myopathy), possible rhabdomyolysis (monitor creatine kinase)

IV only

Resistance: rare but increasing

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3
Q

Nitrofurantoin:

MOA?

Use?

A

Nitrofurantoin:

MOA: reductive metabolism in bacteria produces free radicals. Bactericidal

Use: Uncomplicated acute lower UTI (can also be prophylactic), tissue levels are too low to treat pyelonephritis (ascending UTI) or abscess. Advantage: no change in natural flora

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4
Q

Nitrofurantoin:

Adverse effects?

Interactions?

A

Nitrofurantoin

AE (rare): Nausea (take with food), Hepatotox (acute, chronic, or irreversible), Peripheral neuropathy (serious damage with long term use, thuse avoid in patients with already established PN: like diabetics), Pulmonary fibrosis (more common with long term use)

Interactions: Hemolytic drugs ( increased risk of hemolysis), Neurotoxic drugs (increased risk of neurotox), Probenecid, sulfinpyrazone: block renal excretion of drug and defeats purpose

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5
Q

Metronidazole:

MOA?

Uses?

A

Metronidazole:

MOA: diffuses into anaerobic bacteria and is reduced to active form (free radicals), disrupts DNA/proteins. Bactericidal

Uses: Prophylaxis in colorectal surgery, serious infection with Bacteroides, Clostridium, and peptostreptococcus, Intra-ab/liver, skin/skin structure, gynecologic, bone/join, CNS, lower RT, and endocardial infections. Also: trichomonas, amebiasis (dysentery and liver abscess), giardiasis, and vaginal infections

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6
Q

Metronidazole:

Adverse effects? (serious and common)

Interactions?

A

Metronidazole:

Serious AE: seizures, encephalopathy, optic neuropathy, peripheral neuropathy, and asceptic meningitis

Common AE: vaginitis, fungal infections, nausea, and metallic taste

Interactions: potentiate anticoagulants and lithium; Barbiturates cause failure of metronidazole; disulfram psychosis; ethanol - disulfram like reaction

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7
Q

Mupirocen:

MOA?

Use?

A

Mupirocen:

MOA: binds isoleucyl-tRNA synthetase –> inhibits isoleucine incorporation and protein synthesis

Use: Topical reserved for skin infections caused by drug resistant G+ bacteria (especially impetigo) and nasal for MRSA

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8
Q

Mupirocen:

Adverse effects?

Resistance? (high and low)

Contraindications?

A

Mupirocen:

AE: minor - HA or rhinitis w/ nasal application

High resistance: plasmid with mupA gene (creates a new isoleucyl RNA synthetase)

Low resistance: native iles base change. Reserve for very resistant

Contraindications: nasal in neonates because absorption may be excessive

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9
Q

Polymyxin B and E:

MOA?

Use?

Adverse effects?

A

Polymyxin B and E:

MOA: polypeptide with long hydrophobic tail that disrupts cellular membranes. Bactericidal

Use: MDR G- especially Acinetobacter and pseudomonas. B topical for eye and ear. E for ear and also available in Oral/IV form. LAST RESORT

AE: highly neurotoxic and NEPHROTOXIC in oral/IV form

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10
Q

Drugs for UTI now covered?

A

UTI drugs:

a. Cephalosporins - esp 1st/2nd generation
b. Penicillins - esp aminopenicillins
c. nitrofurantoin
d. quinolones
e. sulfonamides
f. trimethoprim

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11
Q

Mycobacterium Tuberculosis:

Latent drugs?

Active drugs?

For MDR-TB?

A

Mycobacterium Tuberculosis:

Latent: isoniazid, rifampin, and rifapentine

Active: isoniazid, rifampin, and pyrazinamide (less important: rifampentine and ethambutol)

MDR-TB: Bedaquiline

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12
Q

Preferred initial treatment?

Preferred continuation treatment?

A

Initial: INH/RIF/PZA/EMB daily

Continuation: INH/RIF daily

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13
Q

Isoniazid:

MOA?

Use?

Metabolism

A

Isoniazid:

MOA: inhibits mycolic acid (fatty acid) synthesis, a unique component of mycobacterial cell walls (good selectivity) Bacteriocidal for growing. Bacteriostatic for resting

Use: alone for prophylaxis of TB or in combo for active TB

Metabolism: liver - dont give with active liver disease

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14
Q

Isoniazid:

Adverse effects?

Interactions?

Resistance?

A

Isoniazid:

AE: hepatotox (routinely check LFTs (liver function tests)), peripheral neuritis (can off-set w/ Vit. B6), rash, hemolysis (pts w/ deficient G6PD), convulsions (in those prone to seizures), and SLE

Interactions: can inhibit or induce CYP450 enzymes

Resistance: multiple loci give rise to resistance. Use combo b/c some are naturally resistant to one drug or another

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15
Q
A
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16
Q

Pyrazinamide:

MOA?

Use?

A

Pyrazinamide:

MOA: analog of nicotinamide. MOA not completely known - prodrug inhibits FA synthetase and translation; disrupts cell membrane potential. Bacteriostatic or bacteriocidal

Use: combo for active TB

17
Q

Pyrazinamide:

Adverse effects (serious and common)?

Contraindications?

A

Pyrazinamide:

Serious AE: hepatotoxicity and porphyria

Common AE: F/N/V, anorexia, myalgia, and photosensitivity

Contraindications: severe hepatic damage, acute gout, and pregnancy

18
Q

Rifampin:

MOA?

Use?

A

Rifampin:

MOA: inhibits DNA-dependent RNA polymerase (blocks transcription) - Binds bacterial form with increased affinity than eukaryotic form. Bactericidal

Use: combo for TB/leprosy, increases activity of isoniazid, and prophylaxis of meningococcal and H. influenzae meningitis

19
Q

Rifampin:

Interactions?

Adverse effects?

Resistance?

A

Rifampin:

Interactions: induces CYP450 –> increases metabolism of drugs processed by these enzymes

AE: minor hepatotoxicity (usually in patients with prior liver problems) Reddish tears/sweat/urine

Resistance: mutated drug target - develops quickly (avoid monotherapy)

20
Q

Rifapentine:

MOA?

Use?

Special considerations?

A

Rifapentine:

MOA: like rifampin - inhibits DNA dependent RNA polymerase; Bacteriocidal

Uses: TB in combination

Special considerations: Reddish-brown discoloration of body fluids

21
Q

Rifapentine:

Adverse effects?

Interactions?

Contraindicated?

A

Rifapentine:

AE: HA/N/V, rash, anorexia, neutropenia, hepatitis, and arthralgia

Interactions: induces CYP450 hepatic enzymes

Contraindicated: pregnancy

22
Q

Ethambutol:

MOA?

Use?

Adverse effects?

A

Ethambutol:

MOA: inhibits synthesis of metabolizer –> impairment of cellular metabolism: disrupts formation of cell wall. Bacteriostatic

Use: TB in combo, and other mycobacterial infections in combo

AE: SERIOUS: optic neuritis/blindness (decreased acuity and inability to distinguish red/green)

23
Q

Ethambutol:

Interactions?

Special considerations?

Contraindication?

Resistance?

A

Ethambutol:

Interactions: antacides impare absorption of EMB (ethambutol)

Special: decrease dose in renal impairment

Contraindication: pregnancy

Resistance: natural and acquired; NO cross resistance to other anti-mycobacterials

24
Q

Bedaquiline:

MOA?

Use?

Black box warning?

A

Bedaquiline:

MOA: diarylquinidone. Inhibits mycobacterial ATP synthase essential for energy generation

Use: ONLY when effective treatment for active MDR-TB cannot be provided. Use with >3 other drugs to which TB is suceptible (if unknown use >4). Use only with DOTs therapy; NOT for extrapulmonary TB

Black box: Arrhythmias with long QT interval by blocking hERG channel

25
Q

Bedaquiline:

Serious adverse effects?

Common adverse effects?

A

Bedaquiline:

Serious AE: increased mortality (unknown mechanism), prolongation of QT interval, and hepatic dysfunction

Common AE: HA/N, arthralgia, chest pain, and hemoptysis

26
Q

Bedaquiline:

Interactions?

Resistance?

Special consideration?

A

Bedaquiline:

Interactions: other drugs that affect CYP3A4, hepatotoxic drugs, and drugs that prolong QT

Resistance: high risk; may emerge during therapy

Special: orphan drug (uhh not sure what this means? maybe that its the only one of its kind?)

27
Q

Mycobacterium Leprae: Leprosy:

  1. Obligate ____ bacteria.
  2. Transmission?
  3. Immune role?
  4. Drug for tuberculoid leprosy?
A

Mycobacterium Leprae: Leprosy:

  1. Obligae intracellular bacteria
  2. Low transmission
  3. 95% of us are naturally immune and immune response is responsible for the damage
  4. Tuberculoid leprosy: Dapsone
28
Q

Dapsone:

MOA?

Use?

A

Dapsone:

MOA: antifolate, similar to sulfonamides (PABA analog: reversibly inhibits BHPS: Bacteriostatic)

Use: daily for leprosy (1 year), along with rifampin (combination decreases resistance); also for Pneumocystitis pneumonia

29
Q

Name 7 resistant bacteria and what they cause.

A

Resistant bacteria

a. E. coli/Klebsiella: life threatening UTI/intestinal infection; MDR, extended spectrum beta-lactamases
b. Gonorrhea: Ceftriaxone + azithromycin or doxycyline
c. Staph aureus: MRSA (methacillin resistance)
d. Acinetobacter baumannii - hospital acquired
e. Enterococcus faecium: blood stream infections, meningitis, GI infections, Vancomycin resistant
f. Pseudomonas Aeruginosa: severe pneumonia and UTI (esp in cancer/AIDs pts) MDR

30
Q

Causes of resistance that are NOT our fault?

Causes of resistance that ARE our fault?

A

Not our fault: short generation time favors resistance and mutations of selection

Our fault:

a. Antibiotics taken for granted: prescribed when not warranted/Abundant in animal feed as “growth promoters”
b. Poverty/apathy
c. Noncompliance

31
Q

4 antibiotic resistance mechanisms and examples.

A

Abx resistance mechanisms:

a. Destruction of the antibiotics: B-lactamases and acetylases
b. Altered targets: mutated PBPs (penicillin BPs) in Strep pneumoniae or MRSA; cell wall precursors altered in VRE; methylation of rRNA target/ribosomal protection (macrolides)
c. Altered uptake/export of antibiotics: eg. tetracyclines
d. Over production of pathway components: Increased PABA synthesis in sulfonamide resistant bacteria

32
Q

Given drug - name resistant organism treated:

  1. Bedaquiline?
  2. Ceftaroline?
  3. Daptomycin?
  4. Linezolid?
A

Given drug - name resistant organism treated:

  1. Bedaquiline: MDR-TB
  2. Ceftaroline: MRSA
  3. Daptomycin: MSSA and MRSA
  4. Linezolid: G+: MRSA, VRSA, VRE, and PCN resistant strep pneumoniae
33
Q

Given drug - name resistant organism treated:

  1. Metronidazole?
  2. Moxifloxacin?
  3. Mupirocen?
  4. Polymyxin B and E?
A

Given drug - name resistant organism treated:

  1. Metronidazole: anaerobes: B. fragilis, C. difficile, and Heliobacter
  2. Moxifloxacin: PCN resistant strep pneumoniae
  3. Mupirocen: Strep pyogenes and MRSA
  4. Polymyxin B and E: MDR pseudomonas aeruginosa and acinetobacter
34
Q

Given drug - name resistant organism treated:

  1. Streptogramins?
  2. Tigecycline?
  3. Vancomycin?
A

Given drug - name resistant organism treated:

  1. Streptogramins: VRE, vancomycin resistant strep pyogenes, PCN resistant strep pneumoniae
  2. Tigecycline: MRSA
  3. Vancomycin: metranidazole resistant C. difficle; MRSA, MRSE, and PCN resistant strep pneumoniae

Pharm Exam V (6 decks)

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