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Pharm 2 > Test 5: Antibiotics Specific Drugs > Flashcards

Test 5: Antibiotics Specific Drugs Flashcards

1
Q

Which antibiotics are the Beta Lactam Compounds?

A

-Penicillins
-Carbapenems (Imipenem, Meropenem)
-Cephalosporins (1st-4th gen)

All contain Beta Lactam ring. Risk of cross-sensitivity.

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2
Q

What is the MOA of Beta Lactam Compounds?

A

Inhibit bacterial growth!! (Bactericidal)
-Interfere with the transpeptidation (creation of peptidoglycans) of bacterial cell wall synthesis.
-Peptidoglycans are the cross-linked mesh that provides rigid structure and protection to bacteria.
-B-Lactam antibiotics bind to PBPs (Penicillin Binding Proteins) and inhibit bacterial growth.

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3
Q

What breaks down the Beta Lactam antibiotics?

A

Beta Lactamase.
-Resides on the cytoplasmic membrane
-Breaks down B-Lactam antibiotics as they attempt to bind to PBPs (penicillin binding proteins)

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4
Q

What are cellular differences between Gram-Negative and Gram-Positive bacteria?

A

Gram Negative:
-Has an outer membrane that contains Porins (proteins with binding sites that allow hydrophillic access to the inside of the cell)
-Stains red/pink

Gram Positive:
-No outer membrane
-Retains crystal violet dye
-Easier to kill
-Multiple layers of Peptidoglycan

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5
Q

What are the 4 Mechanisms of resistance to Beta-Lactam antibiotics?

A

1) Inactivation of ABX by β-lactamases
-Most common
2) Modification of target PBP’s
-Ex: MRSA
3) Impaired penetration of ABX to the target PBP
-Particularly in gram-negative. Can have down regulation of Porins. Hydrophillic drugs are less effective.
4) Efflux
-Bacteria pumps antibiotic right back out before it had time to work

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6
Q

What is the drug of choice in individuals with a history of penicillin allergy other than immediate hypersensitivity? (Blue Box!)

A

Cephalosporin
-Can use it as long as they don’t have true anaphylactic reactions
-Cross sensitivity is 0.2 -10% occurrence.

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7
Q

What are the Cephalosporins?

A

More stable to many bacterial β-Lactamases:
-Broader spectrum of activity

Classified into 4 major groups (generations) depending on antimicrobial activity

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8
Q

What are the effects of the 1st generation Cephalosporins?

A

Very effective on gram positive bacteria.
Gram Positive Cocci:
-Pneumonococci
-Steptrococci
-Staphylococci

Ex: Cefazolin (Ancef)
-Only agent still in use
-Drug of choice for surgical prophylaxis
-Does not penetrate CNS
-Not useful in meningitis

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9
Q

What are the effects of the 2nd generation Cephalosporins?

A

-Ex: Cefuroxime (Zinacef)
-Active against organisms inhibited by 1st Generation ABX.
-Extended gram negative coverage

Improved activity against:
-Haemophilus influenzae
-Pneumococcus

-Oral & IV
-Treatment against commonly acquired pneumonia
-Crosses the Blood Brain Barrier (Not as effective as Ceftriaxone or Cefotaxime)

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10
Q

What is the difference between the 1st and 2nd generation Cephalosporins?

A

First-generation cephalosporins are active predominantly against Gram-positive bacteria, and successive generations have increased activity against Gram-negative bacteria (albeit often with reduced activity against Gram-positive organisms).

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11
Q

What is Cefuroxime (Zinacef) used for?

A

1.5 g - used often in urology for cysto cases

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12
Q

What is the only Monobactam used in the US?

A

Aztreonam (Azactam)
-Same MOA as B-Lactams
-Bactericidal against gram negative
-Renal cleared
-No toxicity
-No cross allogenicity with PCN. Used if hypersensitivity to PCN

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13
Q

What are the kinetics associated with Cefazolin?

A

-IV
-Renal clearance
-Half-Life 1.5 hours
-Poor penetration into CNS
-Bactericidal to mostly gram positive and a little gram negative

Toxicities:
-Rash
-Drug fever

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14
Q

What is Ceftriaxone (Rocephin)?

A

-3rd generation cephalosporin.
-Same MOA as B-Lactams
-More coverage in the CNS

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15
Q

What are the uses of Penicillins?

A

Penicillins treat steptococcal infections, meningococcal infections, & neurosyphilis

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16
Q

What are the S/Sx of Neuromuscular Hypersensitivity?

A

-Agitation
-Hallucinations
-Asterixis: tremor of the hand when the wrist is extended, sometimes said to resemble a bird flapping its wings.
-Encephalopathy
-Confusion
-Seizures

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17
Q

What is the usual dose of Vancomycin?

A

30-60mg/kg/day in patients with normal renal function
-2-3 divided doses

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18
Q

What is the MOA of Vancomycin?

A

Glycopeptide class.

Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan.
-Bactericidal. Slower killing than B-Lactam group.
-Only kills cells that are actively dividing.

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19
Q

What are the effects of Vancomycin?

A

Bactericidal activity against susceptible bacteria; slower kill than β-lactam ABX

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20
Q

What are the clinical applications for Vancomycin?

A

Infections causes by gram (+) bacteria:
-Endocarditis
-Sepsis
-Meningitis
-C. Diff colitis
-MRSA

21
Q

What are the kinetics of Vancomycin?

A

-Oral & IV
-Renal clearance
-Directly proportional to creatinine clearance
-Decrease dose in pts with renal insufficiency
-Half-Life 6 hours

22
Q

What is Red Man’s Syndrome?

A

Histamine reaction associated with Vancomycin.
-Benadryl
-Administer infusion slowly

23
Q

What are adverse reactions associated with Vancomycin?

A

-Red Man syndrome
-Irritating to tissues = phlebitis at site of injection (use central line if you have it or rotate sites of injection)
-Chills & fever
-Ototoxicity & nephrotoxicity

24
Q

What is Vancomycin + Gentamycin used for?

A

Treatment for enterococcal endocarditis.
-Treatment for patients with serious penicillin allergy

25
Q

What is the drug of choice for dental procedures in patients with valvular heart disease (who have PCN allergies)? (Blue Box!)

A

Clindamycin.
Drug of choice for prophylaxis of endocarditis in patients with valvular heart disease who undergo certain dental procedures and have significant penicillin allergies.

26
Q

What is the dose of Clindamycin?

A

600 mg q8 hours
-No change in dose for renal patients!

27
Q

What is the MOA of Clindamycin?

A

-Lincosamides Class
-Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
-Gram (+)
-Does not penetrate the CNS

28
Q

What are the effects of Clindamycin?

A

-Bacteriostatic (!) against susceptible bacteria (Gram positive)

29
Q

What are the clinical applications for Clindamycin?

A

-Skin & soft tissue infections - MRSA

Anaerobic infections:
-Streptococci
-Staphylococci
-Pneumococci

Lung abscesses
Infections of Female genital tract

Resistant to Clinda:
-Enterococci
-Gram (-)

30
Q

What are the Kinetics of Clindamycin?

A

PO & IV:
-Max 30mg/min
-Infuse over 15-60 min
-Hypotension

Hepatic clearance (inactive and active metabolites)
Half Life 2.5 hrs
90% Protein bound

31
Q

What are the toxicities associated with Clindamycin?

A

-GI upset
-C. Diff colitis
-Rashes
-Decreased Liver Fxn
-Neutropenia

32
Q

What is the dose of Gentamicin?

A

5-6mg/kg/day IV in 3 equal doses
-Smaller dose. More potent drug.

33
Q

What is the MOA of Gentamicin?

A

-Aminoglycoside class
-Prevents bacterial protein synthesis by binding to the 30S ribosomal subunit
-Results in a defective bacterial cell membrane
-Gram (+) & (-)

34
Q

What are the effects of Gentamicin?

A

-Bactericidal activity against susceptible bacteria
-Synergistic effects when combined with β-lactams or Vanco!!
-Concentration dependent killing with significant post-antibiotic effect (staves off bacterial events event after course of treatment is done)

35
Q

What are the clinical applications for Gentamicin?

A

-Sepsis caused by aerobic gram (-) bacteria
-Synergistic activity in endocarditis caused by streptococci, staphylococci, & enterococci
-Can give Intrathecally for meningitis but not as effective as 3rd gen cephalosporins

36
Q

What are the kinetics of Gentamicin?

A

-IV
-Active metabolites
-Renal Clearance
-Half-Life 2.5 hrs

37
Q

What are the toxicities associated with Gentamicin?

A

-Nephrotoxicity (usually reversible and mild)
-Ototoxicity (Irreversible vestibular dysfunction (vertigo) and potential loss of hearing. Due to neural injury.)
-Neuromuscular blockade
-*Hypersensitivity reactions are uncommon

38
Q

What is the MOA of Ciprofloxacin?

A

-Fluoroquinolones class
-Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV (has 2 sites of action)
-Gyrase is required for normal transcription and replication
-Topoisomerase is responsible for the separation of chromosomal DNA into the daughter cells during cell division
-Gram (+) & Gram (-)

39
Q

What are the effects of Ciprofloxacin?

A

Bactericidal activity against susceptible bacteria

40
Q

What are the clinical applications for Ciprofloxacin?

A

-UTIs
-Gastroenteritis
-Osteomyelitis
-Anthrax

41
Q

What are the kinetics of Ciprofloxacin?

A

PO & IV (administer over 60 min)
Mixed clearance (hepatic & renal)
Half-life 4 hrs

42
Q

What is the toxicity associated with Ciprofloxacin?

A

-Tendonitis (joint and tendon inflammation, commonly in the ankles)!
-GI upset
-Neurotoxicity

43
Q

What is the dose of Metronidazole?

A

500 mg TID

44
Q

What is the MOA of Metronidazole?

A

-Nitroimidazoles class
-Disruption of electron transport chain

Selectively absorbed and nonenzymatically reduced
-Toxic byproducts that accumulate in anaerobic cells
-Taken into bacterial DNA forming unstable molecules
-Leads to cell death (little effect on human or aerobic cells. Only selective to anaerobic bacteria)

45
Q

What are the effects of Metronidazole?

A

-Bactericidal activity against susceptible anaerobic bacteria and protozoa
-Little effect on human cells or aerobic cells

46
Q

What are the Clinical Applications for Metronidazole?

A

Technically an anti-fungal. Given due to planned or unplanned disruption of the bowel.
-Used in GYN procedures to prevent opportunistic infections
-Prevents peritonitis due to fecal matter

-Anaerobic infections
-Vaginitis
-C. Diff Colitis
-Brain abscess

47
Q

What can occur with prolonged use of Metronidazole?

A

N/D, stomatitis, & peripheral neuropathy with prolonged use

48
Q

What are the kinetics of Metronidazole?

A

-PO & IV
-Hepatic clearance
-Half-life 8 hrs
-Disulfuram like reaction when given with alcohol (N/V, GI upset)

49
Q

What toxicities are associated with Metronidazole?

A

-GI upset
-Metallic taste
-Neuropathy
-Seizures

Pharm 2 (40 decks)

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