Test Two: Penicillin Alternatives Flashcards

0
Q

1st gen cephalosporins

A

Cephalexin: Good for gram+ aerobes and MSSA. Less active for gram- and no enterococci activity. Good for soft tissue infxn and surgical prophy

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1
Q

What is the mechanism of action of cephalosporins?

A

Inhibit cell wall peptidoglycan synthesis by blocking transpeptidase and carboxypeptidase

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2
Q

2nd gen cephalosporins

A

Cefamandole: mainly gram- with less staph activity and some anaerobic effect

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3
Q

3rd gen cephalosporins

A

Cefoperazone: Mostly Gm –ve, penicillin resistant streptococcus pneumoniae, with a subset effective against pseudomonas. Not used much in dentistry

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4
Q

4th gen cephalosporins

A

Cefepime: Wider antibacterial spectrum (pseudomonas, penicillin resistant Streptococcus pneumoniae, MRSA, enterococcus, and hyper β-lactamase producing organism). Administered IV

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5
Q

What cephalosporin penetrates the CSF for meningitis?

A

Cephotaxime

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6
Q

How do 1st gen cephs respond to beta lactamase?

A

Very sensitive to hydrolysis

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7
Q

Dosing for 1st gen ceph?

A

500mg qid. T1/2 is 1 hr

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8
Q

2nd gen ceph kinetics

A

Lower peak plasma level than 1st. T1/2 1-1.5 hrs. 200-400 mg bid. Not widely used

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9
Q

What are some adverse rxns for cephalosporins?

A
  • Hypersensitivity (cross allergy with penicillin(~20%)
  • Maculopapular rashes
  • Transient increase in liver function.
  • Inhibit hemostasis (hypoprothrombinemia)
  • Alcohol intolerance
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10
Q

Carbapenems (imipenem and miropenem)

A

Broad spectrum, beta lactamase resistant, used as alt for MRSA and strep pneumoniae, has cross allergenicity

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11
Q

Monobactams (aztreonam)

A

Aerobic gram-, only injected, sensitive to beta lactamase, no cross allergenicity

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12
Q

Examples of macrolides and mechanism of action

A

Erythromycin, clarithromycin, azithromycin, bind to 50s ribosomal subunit to block translation, hardly any allergies

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13
Q

Erythromycin spectrum and dosage

A

Gram+ aerobes and facultatives, 250-500 mg q6h as enteric coated tablets bc of poor acid resistance, excreted in urine, does not reach brain or CSF

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14
Q

Erythromycin adverse rxns

A

Epigastric pain, ventricular arrhythmia, hepatotoxicity (hepatic microsomal enzyme inhibitor-helps prolong action of other drugs)

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15
Q

Clarithromycin diff from erythromycin

A

Similar spectrum but mainly gram+ anaerobes, rapid absorption, less GI problems, dosing is 250-500 bid, liver and kidney excretion

16
Q

Azithromycin

A

Rapid absorption, more active against strep/staph but mainly gram- anaerobes, stays in tissue for slow release (take 250 qd), excreted by liver

17
Q

When should macrolides be used?

A

1- Best alternative for B-lactam –allergic patient for acute orofacial infections
2- treat acquired bacterial pneumonia
3- chronic sinusitis
4- Asthma complications

18
Q

What are contraindications for macrolides?

A

Patient with cholestatic hepatitis and cardiac arrhythmia

19
Q

Clindamycin spectrum and mechanism of action

A

Gram+ and gram- anaerobes, binds to 50s subunit

20
Q

Clindamycin kinetics

A
  • Completely absorbed after oral administration
  • Widely distributed, penetrate well into bones
  • Metabolized in the liver and its metabolites have also antimicrobial activity
  • Excreted in urine and feces
21
Q

Clindamyin dosage and uses

A

150-300 q6h, Mainly used for bone infection, female genital
tract, pelvic and abdomenal infection.
- For acute orofacial infections for oral microbial resistance to the β-lactam antibiotics.

22
Q

Side effect of clindamycin

A

Some develop diarrhea and can get pseudomembranous colitis

23
Q

Vancomycin spectrum and mechanism of action

A

Effective against gram+ like MRSA, gram- bacilli are resistant, binds to terminal amino acids to block carboxypeptidase

24
Q

Vancomycin dosage and administration

A

Poorly absorbed oral, given iv, t1/2 is 6hr, 500 q6h

25
Q

Vancomycin side effects

A

Can have hypersensitivity like penicillin, can also cause nephrotoxicity esp in combo with other drugs

26
Q

Metronidazole uses

A

1-Protozoal infections (Giardiasis, Trichomoniasis, amebiasis)
2-Anerobia bacterial causing orofacial infection (periodontitis, acute necrotizing ulcerative gingivitis)

27
Q

Metronidazole kinetics

A

completely absorbed from GIT- oral intake attains peak level in 1-2 hours, widely distributed with excellent CNS penetration ( half
life= 8 hours)

28
Q

Side effect of metronidazole with alcohol

A

Disulfiram like action-blocks alcohol dehydrogenase which causes a buildup of acetaldehyde–> nausea, vomiting, flushing, tachycardia

29
Q

Fluoroquinolone mechanism of action

A

Inhibits bacterial gyrase and topoisomerase to prevent supercooling of DNA which stops replication

30
Q

Uses and dosage for fluoroquinolones

A

or UTIs, respiratory infections, GIT, bone, prophylaxis, 250-750 bid (very long 1/2 life, 10-12hrs, good for fewer dosages needed)

31
Q

Most commonly prescribed fluoroquinolones

A

Ciprofloxacin 250-500 bid, ofloxacin (topical), levofloxacin 250-500-750 qd (all 2nd generation bc there are generic forms)

32
Q

Side effects with fluoroquinolones

A

most imp is arrythmia–can disturb ECG, be careful when taking with anti arrhythmic drugs, theophylline or NSAIDs (CNS toxicity)