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OU Module ID Fall 2018 > Antibacterials Drug Info Exam 2 > Flashcards

Antibacterials Drug Info Exam 2 Flashcards

1
Q

Penicillin G PK features

A
  • Poor oral absorption
  • Unstable in acid environments
  • Only given by injection, usually continuous IV
  • Ordered in units
  • Half-life is about 30 minutes due to rapid renal elimination. Dosage reduction if impaired renal function
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2
Q

Penicillin V PK features

A
  • Acid-stable, oral use, should be taken on an empty stomach several times a day
  • Half-life is about 30 minutes due to rapid renal elimination. Dosage reduction if impaired renal function
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3
Q

Which PCN(s) has the best oral absorption?

A
  • oxacillin
  • nafcillin
  • dicloxacillin
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4
Q

Ampicillin route of administration

A
  • oral and injected
  • injection preferred
  • take on empty stomach if taking oral
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5
Q

amoxicillin route of administration

A

oral only

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6
Q

piperacillin route of administration

A

injected only

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7
Q

Penicillin G route of administration

A

parenteral

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8
Q

Penicillin V route of administration

A

oral, empty stomach

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9
Q

Hypersensitivity Reactions of Penicillins

A
  • Immediate (anaphylactic)
  • Accelerated
  • Delayed (most common; skin rashes)
  • Assume 100% cross-allergic reactions among the penicillins
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10
Q

Theory for Hypersensitivity Reactions of Penicillins

A

when the β-lactam ring is opened and combines with a human protein

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11
Q

General PK of Cephalosporins

A
  • incompletely absorbed after oral dose
  • short half-life
  • renal elimination
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12
Q

Hypersensitivity Reactions of Cephalosporins

A

Possible cross-allergic reaction with other β-Lactams

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13
Q

ADEs of PCN’s

A
  • CNS Excitation / seizures at high conc.
  • lower doses in case of renal impairment
  • Diarrhea
  • nausea
  • superinfections
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14
Q

ADEs of Cephalosporins

A
  • CNS excitation and seizures with high levels
  • Renal toxicity
  • Bleeding (Kill bacteria that synthetize Vit.K, potential problem with all extended and broad spectrum antibiotics, drug-drug interaction with warfarin that inhibit Vit.K synthesis)
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15
Q

Cefadroxil route of administration

A
  • best absorbed after oral administration (has amoxicillin side chain)
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16
Q

Which First Generation Cephalosporins has the longest half life?

A

Cefazolin

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17
Q

Cefoxitin route of administration

A

parenteral

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18
Q

cefuroxime route of administration

A

oral prodrug and parenteral

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19
Q

cefaclor route of administration

A

oral

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20
Q

cefprozil route of administration

A

oral

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21
Q

Third Generation Cephalosporins route of administration

A
  • Poor oral absorption, some pro-drug formulations can improve oral bioavailability
  • Some injectable third generation Cephalosporins can cross the BBB
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22
Q

Cefotaxime route of administration

A

parenteral

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23
Q

Ceftriaxone route of administration

A

parenteral

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24
Q

Ceftazidime route of administration

A

parenteral

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25
Q

Cefotaxime PK

A

short half-life

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26
Q

Ceftriaxone PK

A

long halflife

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27
Q

Cefepime route of administration

A

parenteral

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28
Q

Ceftaroline route of administration

A

parenteral

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29
Q

Carbapenems PK

A
  • Short half-life, quickly excreted in urine

* Poor oral absorption

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30
Q

Imipenem route of administration

A

parenteral

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31
Q

Imipenem PK

A
  • rapidly degraded by the renal enzyme dehydropeptidase

- metabolites can cause kidney damage

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32
Q

meropenem, doripenem, ertapenem PK

A
  • Chemically modified, resistants to dehydropeptidase

- Not available for oral use.

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33
Q

ADEs with Carbapenems

A
  • Possible cross-allergic reactions

* CNS excitation, seizures more of a concern with Carbapenems

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34
Q

Aztreonam route of administration

A

parenteral

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35
Q

Monobactams (Aztreonam) PK

A
  • Short half-life, quickly excreted in urine
  • Poor oral absorption
  • Because of unusual ring structure, no cross-allergic reactions with other β-lactams
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36
Q

Food with β-lactams

A

Oral absorption is reduced by food (except for amoxicillin)

37
Q

Glycopeptides / lipoglycopeptides history

A
  • Not widely used at first because of renal toxicity and hearing loss
  • Big polar molecule
  • Used as last resort
38
Q

Vancomycin PK

A
  • not absorbed reliably from GI tract
  • Renal clearance (glomerular filtration)
  • half-life 4-6 h
39
Q

Vancomycin route of administration

A
  • intravenously

- oral available too

40
Q

ADE of Glycopeptides

A
  • Nephrotoxicity
  • Ototoxicity with high circulating levels
  • Infusion-related effects: chills, fever rash, flushing; due to histamine release from mast cells; infuse slowly to avoid
41
Q

Lipoglycopeptides PK

A
  • Lower MIC values
  • Less adverse effects
  • Longer half-lives
42
Q

Telavancin route of administration

A
  • Administered by injection once a day

- half-life: 9h

43
Q

Oritavancin route of administration

A
  • Administered by injection once a week

- half-life: 195h

44
Q

Dalbavancin route of administration

A
  • Administered by injection once a week

- half-life: 346h

45
Q

Lipopeptides uses

A
  • Last resort antibiotic

- MRSA and VRSA

46
Q

Lipopeptides route of administration

A
  • injected IV once daily
47
Q

Lipopeptides PK

A
  • half-life 8-9h

- Renal elimination

48
Q

Lipopeptides ADE

A
  • Some apparent muscular toxicity

- drug-drug interaction with statins

49
Q

Oxazolidionones uses

A

Last resort drugs

50
Q

Linezolid PK

A

broken down in the liver by non-enzymatic oxidation, eliminated in urine, short half-life, administered twice daily

51
Q

Tedizolid PK

A

sulfated in the liver and excreted mainly in bile, longer half-life, administered once daily

52
Q

Oxazolidionones ADE

A
  • Bone marrow suppression resulting in low platelet count
  • Peripheral neuropathy (tingling sensation, numbness, burning)
  • Weak monoamine oxidase inhibitor, interaction with other drugs like serotonine reuptake inhibitors used for depression
53
Q

Streptrogramins route of administration

A

Must be given intravenously

54
Q

Streptrogramins PK

A
  • Rapidly metabolized in liver
  • Short half-lives, administered 3-4 times daily
  • Excreted in the bile
  • No dosage adjustments required in case of poor renal function
  • Dosage adjustment in case of hepatic impairment
55
Q

Streptrogramins ADE

A
  • Discomfort at injection site
  • Some joint and muscle pain
  • Potential for drug interactions involving CYP3A4 (these rx are inhibitors)
56
Q

Lincosamide uses

A
  • Penicillin substitute for G+ cocci, useful for some MRSA infections
  • Anaerobic infections
  • Infections of bone and joint
57
Q

Clindamycin PK

A
  • given at 6-8 h intervals
  • Excellent penetration into bone, abscesses, macrophages but not CNS
  • Metabolized in liver but to a small extent
  • Few drug-drug interactions
  • Parent drug and active metabolites mainly excreted into bile
58
Q

Lincosamide ADE

A
  • Rash, Nausea, Diarrhea (usually mild, self-limiting)
  • Increased risk for Clostridium difficile colitis (Gram + anaerobe, NOT sensitive to Clindamycin)
  • Weak neuromuscular blocking activities, drug-drug interaction with other neuromuscular blocking drugs that are used during surgery
59
Q

Erythromycin route of administration

A
  • injection

- poor oral absorption, very unstable in acidic conditions, given orally only as enteric-coated tablets

60
Q

Erythromycin PK

A
  • Pro-drug formulations for better absorption and stability.
  • Short half-life ~1.4 h
  • metabolized in the liver by CYP3A4
61
Q

Clarithromycin PK

A
  • stable in acidic conditions
  • half-life ~3.7h
  • metabolized in the liver by CYP3A4
62
Q

Azithromycin route of administration

A
  • etter oral absorption on an empty stomach

- stable in acidic conditions

63
Q

Azithromycin PK

A
  • long half-life ~68h
64
Q

Macrolides ADE

A

GI intolerance

65
Q

Azithromycin ADE

A

Increased risk for Clostrodium difficile colitis

66
Q

Telithromycin ADE

A
  • hepatotoxicity
  • prolonged QT interval
  • visual disturbances
  • loss of conciousness
67
Q

Sulfamethoxazole plus trimethoprim route of administration

A

oral and parenteral

68
Q

Sulfamethoxazole plus trimethoprim route of administration

A

oral and parenteral

69
Q

Sulfamethoxazole plus trimethoprim PK

A
  • Hydrophobic, well absorbed orally
  • Bound to plasma proteins in the blood, potential for drugdrug interaction
  • Sulfonamides metabolized by acetylation, some glucuronidation and CYP oxidation, potential for drug-drug interaction
  • Mostly renal excretion by glomerular filtration and/or tubular secretion, potential for drug-drug interaction
70
Q

Sulfamethoxazole plus trimethoprim ADE

A
  • Hypersensitivity or allergic reactions at high doses
  • Crystalluria at high doses
  • Aplastic anemia at high doses
  • Do not use in late 3rd trimester of pregnancy or in neonates!
71
Q

Ansamycins PK

A
  • Well absorbed after oral administration, take on an empty stomach
  • Deacetylated in liver, active metabolites
  • Not substrates of CYP450 enzymes
  • Enterohepatic circulation
  • Half-life 1.5 – 5 hours, take once a day
  • About 30% renal elimination, 70% feces
  • Tuberculosis treatment can take several months or longer
72
Q

Ansamycins ADE

A
  • Some hepatotoxicity
  • Gastrointestinal intolerance
  • Colors urine and other body fluids red or orange, not harmful
73
Q

Rifampin PK

A

Rifampin is a powerful inducer of CYP3A4

74
Q

Rifabutin PK

A
  • Longer half-life
  • Less induction of CYP3A4
  • Is effective against some rifampin-resistant strains
75
Q

Rifaximin uses

A
  • Orally administered to treat traveller’s diarrhea caused by E. coli
  • Does not need to be taken on an empty stomach
  • Can be used for C.diff
76
Q

ozenoxacin uses

A

treatment of impetigo

77
Q

Fluoro/quinolones PK

A
  • Good oral absorption, best oral drugs for P. aeruginosa!
  • Third generation are better absorbed and have longer half-lives
  • Chelate metal ions in food and antacids, decreases absorption
  • Excreted in urine, lower dosage when renal insufficiency. Moxifloxacin is excreted in the bile.
  • Good antibacterial activity in bowel in spite of good oral absorption (enterohepatic circulation)
  • Excellent penetration in tissues (bone, prostate, etc), but not in CNS, delafloxacin has the best intracellular penetration
78
Q

Fluoro/quinolones ADE

A
  • Serious adverse effects in tendons, muscles, joints, nerves. Not recommended during pregnancy or in children.
  • CNS excitation and seizures
  • Peripheral neuropathy (pain, burning sensations, numbness)
  • Diarrhea, due to broad antibacterial spectrum and superinfection with C. difficile
  • FLUOROQUINOLONES with most serious toxicity have been withdrawn from the market
79
Q

Tetracycline PK

A

poor oral absorption further decreased by food and dairy products because it forms insoluble, non-absorbed chelates with metal ions from food. Not metabolized, eliminated by urine, short half-life 6-8 h.

80
Q

Doxycycline PK

A

excellent oral absorption. Partly metabolized, excreted by the bile, long half-life 18-20 h

81
Q

Minocycline PK

A

excellent oral absorption. Partly metabolized, excreted by the bile, long half-life 18-20 h and fully metabolized by the liver

82
Q

Tigecycline, omadacycline and eravacycline PK

A

Tigecycline, omadacycline and eravacycline are given intravenously, omadacycline can also be given orally, eliminated by feces and urine, longest half-life 36 h

83
Q

Tetracycline ADE

A
  • Usually uncommon, mostly diarrhea, super-infections of nonsusceptible organisms (Candida, C. difficile) due to broad antibacterial spectrum
  • Teeth discoloration, chelate calcium, discoloration when exposed to light, not used during pregnancy or in children younger than 8
  • Hypersensitivity to sunlight
  • Tigecycline is associated with slightly increased risk of death relative to other antibiotics, only used when no other alternative.
84
Q

Aminoglycosides PK

A
  • Poor oral absorption, administered by injection, or used orally for GI infections
  • Very hydrophilic drugs, dosage adjusted to the lean body mass not total body mass
  • Excreted in urine (UTI), renal function must be checked during long-term therapy
  • Half-life is short but they can be administered only once a day because these drugs remain active long after plasma level decrease below MIC level (post-antibiotic effect), due to the irreversible binding.
85
Q

Aminoglycosides ADE

A
  • Renal toxicity can occur during long-term treatment
  • Neuromuscular junction blockade can occur with high doses. Stop treatment before surgery (when using other neuromuscular blockers)
  • Ototoxicity, vestibular function, loss of balance may be permanent
  • Toxicity is not increased when administered only once a day at a higher dose
86
Q

Polypeptide PK

A
  • No oral absorption, IV injection, aerosol (for Cystic Fibrosis)
  • Short half-life
  • Excreted in urine
87
Q

Polypeptide ADE

A
  • Was abandoned at first because of its kidney toxicity and neurotoxicity
  • Used as last resort drug since the emergence of multidrug resistant G
  • Used only for serious cases of resistant infections and for Cystic Fibrosis
88
Q

Nitromidazoles PK

A
  • Food does not affect oral absorption
  • Administer every 6-8 h (metronidazole) or once (secnidazole)
  • Excreted in urine
  • Mild adverse effects
89
Q

Nitromidazoles route of administration

A

Oral, IV, and topical administration

OU Module ID Fall 2018 (18 decks)

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