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Spring Pharm > antimicrobials > Flashcards

antimicrobials Flashcards

1
Q

Penicillin G

MOA:

PK:

Allergy:

Anaphylaxis

A

first generation beta-lactamase sensitive penicillin

MOA: beta lactam, bacteriacidal

PK: 90% renal tubular excretion.

Allergy in 10% of pop.

anaphylaxis is 0.004 to 0.04%,

mortality in 10%

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2
Q

Amoxicillin

Class:

MOA:

A

2nd generation beta-lactamase sensitive PCN

MOA: beta-lactam bactericidal

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3
Q

Ampicillin

MOA:

Pk:

A

2nd generation beta-lactamase sensitive PCN

MOA: beta-lactam, bactericidal

Pk: 50% excreted unchanged by the kidney 6 hours after dose

In the anesthesia cart!

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4
Q

Carbenicillin

class:

SE:

A

3rd generation beta-lactamase sensitive PCN

Unique! r/t lots of SE

  1. High sodium load (30-40 mg) -> caution in CHF
  2. Hypokalemia
  3. Metabolic Alkalosis
  4. Prolonged bleeding time despite normal platelet count also needs renal dose.
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5
Q

carbenicillin is avoided in CHF r/t

A

high sodium load, 30-40 mg

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6
Q

beta-lactamase resistant PCNs are affective against

A

staph aureus

but otherwise are narrow spectrum agents

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7
Q

Nafcillin

class:

Pk:

Excretion:

A

beta-lactamase resistant PCN!

  • Good for staph aureus, otherwise narrow spectrum

penetrates the CNS 80%

secreted in BILE!

GOOD FOR RENAL!

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8
Q

PCN for patients renal dysfunction:

A

Nafcillin

beta-lactamse resistant PCN

80% secreted in bile

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9
Q

Dicloxacillin

class:

A

beta-lactamase resistant PCN

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10
Q

Oxacillin

class:

A

beta-lactamase resistant PCN

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11
Q

Unasyn [ampicillin/sulbactam]

A

beta-lactamase sensitive / beta-lactamase resistant PCN

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12
Q

amoxicillin/clavulanic acid [augmentin]

A

beta-lactamase sensitive / beta-lactamase resistant PCN

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13
Q

ticarcillin/clavulanic acid [timentin]

A

beta-lactamase sensitive / beta-lactamase resistant PCN

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14
Q

pipercillin/tazobactam [zosyn]

A

beta-lactamase sensitive / beta-lactamase resistant PCN

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15
Q

Cephalosporin MOA:

A

Cephalosporins also have a beta-lactam ring,

so function by binding to pencillin binding proteins,

inhibiting transpeptidase, and

activating autolysins.

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16
Q

Cephalosporins are usually excreted

A

via renal route

**exception = ceftriaxone

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17
Q

Bleeding Concerns with Cephalosporins:

A

cefoperazone, cefotetan, ceftriaxone

These inhibit the conversion of vitamin K to active form, inhibits factors 2, 4, 10 and prothrombin.

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18
Q

Cefuroxime

class:

A

2nd generation cephalosporin

DOES cross placenta

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19
Q

Cefoxitin

class

A

2nd genration cephalosporin

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20
Q

Cefemetazole

class

SE:

A

2nd generation cephalosporin

Anta-abuse agent

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21
Q

Cefotetan

Class:

SE:

Interacts:

A

2nd generation cephalosporin

r/f bleeding

  • r/t inhibits conversion of vitamin K to active form
  • Antabuse drug!!!
  • Interacts with anti-plt / anti-coag drugs
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22
Q

Ceftazidime

Class:

A

3rd generation cephalosporin

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23
Q

Cefotaxime

Class:

A

3rd generation cephalosporin

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24
Q

Ceftriaxone

Class:

Pk:

SE:

Interacts:

A

3rd generation cephalosporin

  • Has some renal excretion but significant liver metabolism Longest e1/2 time of cephalosporins
  • R/F bleeding r/t inhibits conversion of vitamin K to active form
  • Interacts with anti-platelet drugs / anti-coags
  • FORMS PRECIPITATES WITH CALCIUM - fatal, neonates
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25
Q

Cefepime

Class:

Pk:

Coverage:

A

generation 4 cephalosporin.

  • broadest spectrum activity against gram +, gram -,
  • crosses BBB,
  • activity against anaerobes.
  • $$expensive
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26
Q

Ceftaroline

Class:

A

Either 5th or 3rd generation cephalosporin.

MRSA coverage

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27
Q

Aztreonam

MOA:

Pk:

Excreted by:

SE:

A

class: monobactam

MOA: has a beta-lactam ring

  • but only binds to GRAM NEGATIVE bacteria
  • Very resistant to beta-lactimase

Pk:

  • Penetrates CSF

Excreted

  • unchanged by kidney !!

Biggest SE

  • GI superinfection
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28
Q

Erythromycin

Clarithromycin

Azithromycin

are:

A

macrolides

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29
Q

macrolides

MOA:

metabolism:

excreted:

A

MOA: bind to 50S subunit and therefore are bacteriostatic, can be bactericidal in large concentration

Metabolized by CYP450 - CYP3A4

Excreted in BILE

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30
Q

Macrolides are very good against:

A

ATYPICAL pathogens:

Community Aquired Pneumonia

Legionella Pneumophila

Pertussis

Acute Diptheria

Chlamydial Infections

Bacterial Endocaridits

Limited activity against anaerobes

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31
Q

biggest concern with macrolides

A

r/f for QT prolongation, dysrythymias

especially when prescribed with CYP3A4 inhibitors

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32
Q

Clindamycin

Class:

MOA:

Used for:

Metabolized by:

Excreted by:

A

Clindamycin:

Class: Linomycin

MOA: Binds to 50S sub-unit, so also bacteriostatic

Most Commonly Used: for female GU surgery

Metabolized By: liver

Excreted: mostly in bile

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33
Q

SE of Clindamycin

A
  1. pseudomembranous colitis
  2. 6% C. Diff
  3. Blood Dyscrasia

4. Muscle weakness ->

  • Prolonged pre and post junctional effects NMJ
  • Not antagonized by anticholinesterase or calicum

anti-cholinesterase = acteylcholinesterase inhibitor

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34
Q

Profound NMB with clindamycin

A

is NOT reversed with calcium or neostigmine

neostigmine = acetylcholinesterase inhibitor/anticholinesterase

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35
Q

Decrease dose in clindamycin with

A

severe LIVER disease

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36
Q

Vancomycin

class:

MOA:

PharmacoK:

excretion:

A

vancomycin

class: glycopeptide

MOA: Depletes cell of precursors for cell wall

  • slow bacteriacidal

PharmacoK:

  • poorly absorbed via GI route,
  • slow CSF penetration unless active infalmmation.

Excretion: 90% excreted unchanged kidneys

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37
Q

Vancomycin is a good choice for

A

MRSA coverage!

Good choice for PCN allergy

serious staph infections

surgery with prosthetic devices

CSF/shunt related infections

bacterial endocarditis

Severe C. Diff

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38
Q

Amikacin

Gentamycin

Neomycin

class:

A

aminoglycosides

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39
Q

Aminoglycosides

MOA

Excretion

A

Aminoglycosides:

MOA: bind to 30S subunit and block initiation of protein synthesis - BACTERICIDAL

excretion: 100% renal

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40
Q

Skeletal Muscle Weakness with aminoglycosides

A

Aminoglycoside inhibit the pre-junctional release of acetylcholine and decrease post-synaptic sensitvity to the neurotansmitter

Potentiaton of NDNMB

  • paralysis is usually reversible with calcium gluconate or neostigmine (acetylcholinesterase inhibitor)
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41
Q

amikacin + PCN

A

is C/I because amikacin can antagonize the effects of PCN

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42
Q

Zyvvox

MOA

A

Zyvvox

MOA: Inhibits bacterial protein synthesis by inhibiting formation of functional ribosome unit 23.

BACTERIOSTATIC

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43
Q

Zyvvox Coverage:

A

Zyvvox

Gram positive pathogens

Not active against gram negative

Active against resistant bacteria such as MRSA and VRE

Expensive $$

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44
Q

Zyvox is contraindicated

A

Zyvvox is contraindicated for

  1. PKU patients
    * Formualted with phenylalanine
  2. SSRIs
    * Zyvvox is a weak MAO-I, increase r/f serotonin syndrome
  3. Meperidine
    * Zyvvox is a weak MAO-I, increase r/f serotonin syndrome
  4. Ephedrine
    * zyvvox is a weak MAO-I, increase r/f HTN crisis
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45
Q

Zyvvox acts as a weak …

A

Zyvvox acts as a weak MAO-I and should be avoided with: SSRIs, meperidine, ephedrine.

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46
Q

cephalosporin adverse effects

A

Allergy in 10%

  • (cross sensitivity 1% to PCN)

Bleeding!

  • Inhibits conversion of vitamin K to active form, inhibits factors 2,4,10 and prothrombin
  • Cefotetan, Ceftriaxone, Cefperazone

Thrombophlebitis at IV site

Hemolytic Anemia

R/F Superinfection (C. Diff)

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47
Q

routes of administration for cephalosporins

A

1st and 2nd = PO/oral and IV 3rd, 4th = generally administered IV

48
Q

cephalosporins that cross placenta:

A

cefazolin

49
Q

cephalosporins that cross BBB

A

cefuroxime, 3rd gen (ceftazidime, cefotaxmie, ceftriaxone) 4th generation: cefepime

50
Q

cephalosporin of choice in renal failure

A

ceftriaxone

51
Q

gram + activity in cephalosporins

A

basically of them

52
Q

gram - activity in cephalosporins

A

generation 3 and 4

53
Q

activity against anaerobes in cephalosporins

A

generation 3 and 4

54
Q

beta-lactamase susceptibility in cephalosporins

A

decreases as you get to broader generations.

55
Q

monobactams

A

aztreonam

56
Q

aztreonam is a good in PCN/Cephalosporin allergy

A

because it does not have either side ring but DOES have a beta-lactam ring. BUT! only works on gram negative

57
Q

Beta-Lactamase Resistance PCNs

A

Nafcillin * best

Oxacillin

Dicloxacillin

58
Q

Beta-Lactam Sensistive/Beta-Lactam Resistant Combinations

A

Ampicllin/Sulbactam “Unasyn”

Amoxicllin/Clavulanic Acid “Augmentin”

Ticarcillin/Clavulanic Acid “Timentin”

Pipercillin/Tazobactam “Pipercillin”

59
Q

Aztreonam with PCN allergy

A

Safe!

Has a beta-lactam ring, but does not have iether side ring found in PCN or cephalosporins so good for allergy with either.

But only works on gram-negative bacteria.

60
Q

Macrolide SE:

A

QT prolongation

Severe N/V with IV infusion

May slow gastric emptying, increase r/f aspiration

Cholestatic Hepatitis

IV assocaited with tinnitus

Thrombophlebitis

61
Q

CYP3A4 inhibitors

A

Verapamil

Diltiazem

Protease Inhibitors

Azole Antifungals

will prolong actions of macrolides, increase r/f QT prolongation dramatically

62
Q

Macrolide drugs:

A

Erythromycin

Azithromycin

Clarithromycin

63
Q

Azithromycin is notable because of its

A

class: macrolide

E1/2T = 68 hours.

64
Q

Vancomycin

Dose:

Administration:

A

Vancomycin:

Dose: 10 - 15 mg/kg over 60 minutes

12 hours of therapeutic plasma concentration

IV administration over 60 minutes

65
Q

Vancomycin SE:

A

Thrombophlebitis

Nephrotoxicity (“Rare”)

Otoxicity (>30mcg/mL)

Hypersensitivity

Severe Hypotension / Red Man Syndrome (rapid adminstration)

Immune Mediated Thrombocytopenia and Bleeding (Rare)

66
Q

Nephrotoxicity with Vanco:

A

Usually occurs as the result of combined effect.

Vancomycin + aminoglycoside in compormised pt (DMII, decreased Cr Clearance)

Or

Vancomycin + other nephrotoxic drug.

67
Q

Vancomycin + Aminoglycoside

A

Synergistic effect based on two MOA.

​Vanco: slowly deprives bacterial cells of precursors for cell walls

Aminoglycosides: Bind to 30S ribosome subunit and block the intiation of protein synthesis in bacterial cells

Synergism but increased risk for nephro/ototoxicity

68
Q

Aminoglycosides SE

A

Aminoglycosides SE

Crosses the placenta -> cause ototoxicity in fetus

Ototoxicity -

  • especially with diuretics, mannitol, vancomyci

​Nephrotoxicity

  • esp with amphotericin B, cyclosporine, etracrynic acid, vancomyin, NSAIDs

Skeletal Muscle Weakness

  • Inhibit the prejunctional release of Acetylcholine and decrease post-synaptic sensitivity to the neurotransmitter
69
Q

Gentamicin

A

Aminoglycoside.

Broader spectrum: does pleural, ascitic, synovial infections

Toxic Level = >9mcg/mL

Levels should be monitored.

70
Q

Amikacin

A

Aminoglycoside

Very little abx resistance yet.

Do not use with PCN (may antagonize effects)

71
Q

Neomycin

A

Aminoglycosides

Topical treatment for skin, eye, mucous membrane infections

Allergy Risk: 6-8%

Adjunct therapy to hepatic coma (decreases ammonia concentrations)

Adminsitered to decrease bacteria in intestine before GI surgery

Most nephrotoxic

72
Q

Zyvvox SE:

A
  1. Thrombocytopenia
  2. GI affects (diarrhea/nausea)
  3. Rare: optic / peripheral neuropathy
73
Q

Fluoroquinolone Agents:

A

Flouroquinolones:

Ciprofloxacin

Levofloxacin

Moxifloxacin

74
Q

Flouroquinolones:

MOA:

Excretion:

A

Flouroquinolones:

MOA: Inhibits DNA gyrase and topoisomerase, prevents bacterial replication.

Excretion: Renal excretion!

75
Q

Fluoroquinolones SE:

A

Fluoroquinolones SE:

1. QT prolongation

  1. Nasuea

3. C. Diff superinfection

  1. CNS disturbances
  2. Opportunistic Candida
  3. Rashes
  4. Phototoxicity (severe sunburn)

8. Muscle Wakness in Myasthenia Gravis pts

9. Tendinitis and Achilles Tendon rUPTURE

  • due to extracellular cartilage matrix weakning
  • high risk >65 y/o
  • avoid IV drug in <18 y/o
76
Q

Flouroquinolones Drug Interactions

A

Fluoroquinolones Drug Interactions:

CYP450 interactions: increase levels of theophylline, warfarin, tinidazole

77
Q

Fluoroquinolones are contraindicated with

A

Myasthenia Gravis patients

Cause increased muscle weakness in these patients.

78
Q

Fluroquinolnes wiht the highest risk of adverse SE

A

Moxifloxacin

79
Q

Sulfonamides

MOA

Pharmacokinetics:

A

Sulfonamides

MOA: Prevent normal bacterual use of para-aminobenzoic acid [PABA] by bacteria to synthesize folic acid.

  • Bacteriostatic

Pharmacokinetics: Portion of drug is acetylated by liver and other is renally excreted

80
Q

Sulfonamides: Clincal Uses

A

Sulfonamides: Clincal Uses

  1. UTI
  2. Inflammatory Bowel Disease
  3. Burns
  4. PCP prophylaxis with HIV+
81
Q

Sulfonamides SE

A

Sulfonamides SE

Skin Rash -> Anaphylaxis

Steven-Johnson’s Syndrome (more common c PCP/HIV+)

Photosensitivity

Allergic Nephritis

Drug Fever

Hepatotoxicity

Acute Hemolytic Anemia

Thrombocytopenia

Increase effect of PO anti-coagulant

82
Q

Metronidazole

MOA:

Pharmacokinetics:

A

Metronidazole

MOA:? -> Bacteriacidal

Pharmacokinetics:

  • Well absorbed orally and widely distributed in tissue inlcuding CNS
83
Q

Metronidazole SE:

A

Metronidazole SE:

Dry Mouth

Metallic Taste

Nausea

Avoid Alcohol: Antabuse Drug

Rare: Neuropathy and pancreatitis

84
Q

Metronidazole is used for:

A

Metronidazole is used for:

Anaerobic gram negative bacilli and clostridium

Reccomended for pre-op prophylaxis for colorectal surgery

CNS infections

Abdominal and pelvic sepsis

Psuedomembraneous Colitis (C. Diff)

Endocarditis

85
Q

Antimycobacterial Agents

A

Antimycobacterial Agents

  1. Isoniazid
  2. Rifampin
  3. Ethambutol
  4. Pyrazinamide
86
Q

Isoniazid

class:

MOA:
Note:

A

Isoniazid:

class: Mycobacterial agent

MOA: Bacteriostatic agent, becomes bacteriacidal if cells are dividing.

Note: NAT2 fast vs slow acetylators.

Anesthesi: check LFTs

87
Q

Antimycobacterial Agents are used for

A

1st line treatment against TB

Used in combinatino (3 or 4 agents) for 2 months

Followed by a minimum of 4 months on therapy with 2 agents.

88
Q

Rifampin

class:

MOA:

SE:

A

Rifampin

Class: Mycobacterial Agents

MOA: bacteriacidal

SE: Hepato-renotoxicity, thrombocyopenia

89
Q

Ethambutol

Class

SE

A

Ethambutol

Class: Mycobaterial Agents

SE: Optic neuritis

  • prone with low BP -> r/f optnic neuritis higher
90
Q

Pyrazinamide

Class:

SE:

A

pyrazinamide

Class: mycobaterial agent

SE: Heptoxicity

91
Q

Risk for hepatoxicty with mycobaterial agents increases

A

with acetaminophen or ETOH

92
Q

Amphotericin B

Class:

MOA:

Pharmacokinetics:

A

Amphotericin B:

Class: Anti-Fungals

MOA: Binds to ergosterol in fungal membrane to form pores, altered membrane permeability leakage of cellular contents.

Pharmacokinetics:

  • Slow renal excretion, 80% of patients tx with drug have renal impairment - usually reversible.
  • Poor PO absorption, given IV
93
Q

Amphotericin B

Clincal Uses:

A

Amphotericin B

Clincal Uses: Yeast and fungi

94
Q

Amphotericin B

SE:

A

Amphotericin B:

“ampho-terrible”

SE:

Fevers, chills, dyspnea, hypotension

Impaired hepatic function

Hypokalemia

Allergic Rxns

Seizure

Anemia

Thrombocytopenia

Nephrotoxic

95
Q

Acyclovir:

Class:

Uses:

SE:

A

Acyclovir

Class: Anti-viral Drug

Uses: Tx Herpes

SE:

  • Thrombophlebitis
  • HA with IV infusion
  • May cause renal damage if infused rapidly
96
Q

Interferon B

Class:

MOA:

Uses:

A

Interferon B:

Class: Anti-viral, recombinant DNA

MOA: Bind to receptors on host cell membranes and induce the production of enzymes that inhibit viral replication – degradation of viral mRNA, enhance tumorcidal activites of macrophages

Uses: Hep B, Hep C, MS pts.

97
Q

Interferon B

SE

A

Interferon B:

SE:

  • Flu like symptoms
  • Hematological toxicity
  • Decreased mental concentration
  • Development of autoimmune conditions
  • Depression
  • Irritability
  • Rashes
  • Alopecia
  • Changes in CV, thyroid, hepatic function
98
Q

HIV Fusion/Entry Inhibitors:

Class:

MOA:

Interferes with:

A

HIV Fusion/Entry Inhibitors:

Class: Anti-Retroviral

MOA: Blocks the fusion/entry of virus into cells, blocks CCR5/CXCR4 proteins.

Intereferes with: metabolism/clearance of midazolam.

99
Q

Zidovudine:

Class:

MOA:

SE:

A

Zidovudine:

Class: Nucleoside Reverse Transcriptase Inhibitors - antiretrovirals

MOA: Blocks the actions of reverse transcriptase

SE:

  • Nausea
  • Diarrhea
  • Myalgia
  • Increase LFTs
  • Pancreatitis
  • Peripheral Neuropathy
  • Renal Toxicity
  • Marrow Suppresion
  • Anemia
  • Lactic Acidosis
  • Inhibition of CYP450
100
Q

Zidovudine

+ corticosteroids

+ succinylcholine

A

Zidovudine:

+ Corticosteroids = Severe myopathy, including respiratory muscle dysfunction

+ Succinylcholine = myalgia x 2.

101
Q

NRTIs

Interact with:
Alter Metabolism/Clearance of:

A

NRTIs

Interact with:

  • Anticonvulsants: phenytoin
  • Antifungals: ketoconazole, dapsone
  • Alcohol
  • H2 Blocker: Cimetidine

Alter Metabolism/Clearance of:

  • Opiates: Methadone
102
Q

Delavirdine

Class:

CYP450:

A

Delavirdine

Class: NNRTI, anti-retroviral

CYP450: Inhibits - increases concentrations of sedatives, antiarrthymics, warfarin, Ca-Channel Blockers

103
Q

Nevirapine:

Class:

CYP450:

A

Nevirapine:

Class: NNRTIs - antiretroviral

CYP450: induces! opposite of other drugs in class.

104
Q

NNRTIs

Interact with:

Prolong half life/effects of:

A

NNRTIs

Interact with:

  • Anti-coagulant: warfarin
  • Anticonvulsants: carbamezapine, phenytoin, phenobarbital
  • Anti-TB drug: Rifampin
  • Herbal: St. John’s Wort

Prolong half life/effects of:

  • Sedatives: diazepam, midazolam, triazolam
  • Opiates: fentanyl, meperidine, methadone
105
Q

Protease Inhibitors

MOA:

A

Protease Inhibitors:

MOA: Impair polypeptide chains of new viral DNA from ever forming. (HIV)

106
Q

Ritonavir

Class:

SE:

A

Ritonavir:

Class: Protease-Inhibitors, anti-retroviral

SE:

  • Hyperlipidemia
  • Glucose Intolerance
  • Abnormal Fat distribution
  • Altered LFTs
  • Aging of the CV system
  • Inhibit CYP450
107
Q
A
108
Q

Ritonavir and life-threatening interactions:

A

Ritonavir and life-threatening interactions:

Meperidine

Amiodarone

Diazepam

109
Q

Protease Inhibitors:

Interact With:

Porlong Half-Life/Effect Of:

A

Protease Inhibitors:

Interact With:

  • Anti-coagualant: warfarin
  • Anticvonulsants: Carbamezapine, phenytoin, phenobarbital
  • Antidepressants: Sertraline
  • Calcium Channel Blockers:
  • Anti-TB: Rifampin
  • Herbal: St. John’s Wort
  • Immunosuppressant: Cyclosporine

Porlong Half-Life/Effect Of:

  • Antidysrhytmics: amiodarone, digoxin, quindine
  • Sedatives: diazepam, midazolam, triazolam
  • Opiates: fentanyl, meperidine, methadone
  • Local Anesthetic: Lidocaine
110
Q

Safe ABX for prengnacy:

A

Safe ABX for pregnancy

(no known SE)

PCNs

Cephalosporins

Erythromycin

111
Q

Caution ABX in pregnancy:

A

Caution ABX in pregnancy:

Aminoglycosides (ototoxicity)

Clindamycin (colitis risk in mom)

112
Q

Contraindicated in Pregnancy:

A

Contraindicated in Pregnancy:

Metronidazole

Tetracylines (teeth - until age 8)

Fluoroquinolones

Trimethorphin (folic acid pathway)

113
Q

HIV tx during pregnancy

A

HIV tx during pregnancy

1st Trimester:

  • Does not need to take HAART if asymptomatic.

2nd Trimester:

  • women with HIV should recieve at least AZT, appropirate HAART additions.

3rd Trimester / Labor and Delivery:

  • HAART c AZT even for asymptomatic mothers.
  • During L/D: IV AZT for mom and
  • PO AZT for baby q 6 hours for 6 weeks.
114
Q

Disulfuram Rxns with Cephalosporins

A

+ ETOH:

Cephazolin

Cefmetazole

Cefotetan

Cefoperzone

115
Q

Monobactam Coverage

A

Gram Negative Only

Very beta-lactamse resistant

Does Cross BBB

116
Q

Fluoroquinolones:

Uses

A

Fluoroquinolones:

Uses

  1. complicated GI/GU infections
  2. TB
  3. URI
  4. Anthrax
    * Enteric Gram Negative Bacilli and Mycobacterium*
117
Q

macrolids increase the serum concentrati on:

A

theophylline

warfarin

cyclosporine

methylprednisone

digoxin

Spring Pharm (11 decks)

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