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Pharmacology > Exam 8 > Flashcards

Exam 8 Flashcards

1
Q

Fxn of Penicillins

A

B lactam abx: inhibit transpeptidase and formation of PG cell wall

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2
Q

acute otitis media species

A
  1. s. pneumo
  2. hib
  3. moraxella catarrhalis
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3
Q

side chains added to what part of penicillin?

A

6 aminopenicillanic acid

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4
Q

other fxns of penicillin binding proteins

A

cell shape and septum formation during division of cell

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5
Q

penicillins activate what in bacteria

A

autolysins (murein hydrolases)

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6
Q

penicillins used often in combo with:

A

aminoglycoside (gentamycin)

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7
Q

Penicillin G’s downfall

A

cant pass through porin channels

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8
Q

P. aeruginosa resistance mechanisms

A

lack of porins, active efflux

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9
Q

P. aeruginosa, E. coli, N gonorrhoeae

A

active efflux of PCNs

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10
Q

PCN not affected by food

A

Amoxicillin

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11
Q

Highly protein bound penicillins

A

Nafcillin, Oxacillin, Dicloxacillin

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12
Q

PCN poor penetration

A

CNS, eye, prostate

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13
Q

What blocks tubular secretion of PCN

A

Probenecid

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14
Q

major antigenic determinant for PCN

A

Benzypenicilloyl

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15
Q

Oral administration PCN

A

least sensitizing

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16
Q

topical administration PCN

A

most sensitizing

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17
Q

Most common reaction to PCN

A

Type I HSN rxn

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18
Q

Methicillin

A

most common cause of acute interstitial nephritis

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19
Q

Ampicillin and Amoxicillin

A

cause skin rashes that are not allergic

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20
Q

Large doses of PCH=excess Na and K=…

A

cardiac and renal toxicity

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21
Q

PCN intrathecally into CSF

A

Seizures

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22
Q

Natural PCNS

A

PCN G, PCN V Potassium, PCN G Procaine, PCN G Benzathine

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23
Q

Penicillinase Resistant Penicillins (anti-Staph PCNS)

A

Methicillin, Nafcillin, Oxacillin

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24
Q

Extended Spectrum PCNS

A

Ampicillin, Amoxicillin. Greater GN activity

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25
Q

Antipseudomonal PCNS

A

Ticarcillin+Clavulanate Potassium, Piperacillin+Tazobactam

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26
Q

B lactamase inhibitors

A

clavulanic acid, tazobactam

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27
Q

PCN G

A

NATURAL PCN

  1. pH of gastric juice destroys, food interferes with absorption
  2. Parenteral use
  3. Probenicid increases plasma and CNS levels of CSF
  4. ACTIVE AGAINST MANY GP AND GN COCCI, spirochetes
  5. INACTIVE AGAINST GN BACILLI
  6. USE FOR NON RESISTANT STAPH and STREP
  7. C. PERFRINGENS AND TETANI
  8. SYPHILIS
  9. ACTINOMYCES ISRALEII
  10. NOT EFFECTIVE AGAINST ENTEROCOCCAL
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28
Q

N. Gonorrhoea

A

3rd Gen Cephalosporin

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29
Q

Anthrax

A

Cipro is good initial drug

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30
Q

PCN V Potassium

A

NATURAL PCN

  1. MORE STABLE THAN PCN G IN ACID (can be absorbed in GIT
  2. LESS ACTIVE THAN PCN G
  3. only use for minor infections
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31
Q

PCN G Procaine, PCN G Benzathine

A

NATURAL PCN

  1. Slow release from injected area
  2. injections into gluteus maximus/thigh
  3. avoid nerves–permanent neuro damage
  4. Resistance to Strep pneumo pneumonia and gonorrhea
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32
Q

PCN G Procaine

A

NATURAL PCN
Last several days
1. S. PYOGENES (GABHS)

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33
Q

PCN G Benzathine

A 
NATURAL PCN
26 days
1. Strep pharyngitis
2. RF prophylaxis (GAS)
3. Syphilis
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34
Q

Nafcillin

A

Penicillinase resistant penicillins-anti staph penicillin

  1. IV administration is preferred (acid inactivation)
  2. SERIOUS STAPH INFECTIONS
  3. doses don’t need to be adjusted in renal failure
  4. bulkier side chain-resistant to destruction by b lactamase
  5. MOST RESISTANT TO BREAKDOWN
  6. drug of choice for PCNase + S. aureus
  7. PENETRATES CNS AND CAN BE USED FOR STAPH MENINGITIS
  8. Not used for GN aerobes
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35
Q

Oxacillin

A

Penicillinase resistant penicillins-anti staph penicillin

  1. IV administration is preferred (acid inactivation)
  2. SERIOUS STAPH INFECTIONS
  3. doses don’t need to be adjusted in renal failure
  4. bulkier side chain-resistant to destruction by b lactamase
  5. drug of choice for PCNase + S. aureus
  6. not used for GN aerobes
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36
Q

MRSA

A

VANCOMYCIN

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37
Q

Ampicilin

A

EXTENDED SPECTRUM PCNS

  1. can be given IV
  2. need to be adjusted for renal failure
  3. susceptible to b lactamase
  4. SE: DIARRHEA, RASH, decreased effectiveness with OCPS
  5. Better than PCN G for GN bacteria
  6. EXTENDED SPECTRUM: HELPSS ME
    - H. flu
    - E. coli
    - L. monocyt
    - P. mirab
    - Salmonella
    - S. pyogenes/S. pneumo
    - M. catarrhalis
    - E. faecalis
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38
Q

Amoxicillin

A

EXTENDED SPECTRUM PCNS

  1. can use lower dose b/c better absorbed in GI
  2. need to be adjusted for renal failure
  3. susceptible to b lactamase
  4. SE: DIARRHEA, RASH, decreased effectiveness with OCPS
  5. Better than PCN G for GN bacteria
  6. EXTENDED SPECTRUM: HELPSS ME
    - H. flu
    - E. coli
    - L. monocyt
    - P. mirab
    - Salmonella
    - S. pyogenes/S. pneumo
    - M. catarrhalis
    - E. faecalis
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39
Q

Ticarcillin + Clavulanate Potassium

A

ANTIPSEUDOMONAL PCN

  1. semisynthetic
  2. adjust for renal fxn
  3. TX GN aerobic bacilli and mixed anaerobic infections
  4. Excess Na problematic for CHF or renal failure
  5. can prolong bleeding time
  6. CAN USE WITH AMINOGLYCOSIDE (DONT MIX)
  7. must monitor for resistance
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40
Q

Tiementin

A

mixed aerobic-anaerobic infections-intrabdominal with B. fragilis (preferred being metronidazole)

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41
Q

Piperacillin + Tazobacam

A

ANTIPSEUDOMONAL PCN

  1. if CREATININE clearance is <40: dosage must be adjusted
  2. tx of GN aerobic bacilli/ mixed aerobic/anaerobic infxns
  3. MORE USEFUL FOR PTS WITH CHF OR RENAL FAILURE
  4. less prolonged bleeding time
  5. tx CAP (H. flu, P aeru)
  6. Septiciemia by GN bacteria, UTI, PID, Intraabdominal infxn, skin infections (s. aureus)
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42
Q

HAP

A
  1. Empiric: aminoglycoside
  2. P. aeruginosa: Piperacillin plus fluoroquinolone
  3. Higher dose required
43
Q

Aztreonam

A

MONOBACTAM

  1. monocyclic B lactam ring
  2. resistant to enzymatic inactivation by B lactamases
  3. MUST BE IV
  4. adjust for renal impiarment
  5. Less HSN RXNS
  6. ONLY ACTIVE AGAINST GNR (similar to aminoglycosides)
  7. many tx including empiric tx for febrile neutropenic pt
  8. E. coli, K. pneumo, multi-drug resistant p. aeruginosa, s. marcescens, H. flu, Enterobacter
44
Q

Imipenem + Cilastatin

A

CARBAPENEM

  1. B lactam ring. B lactam ab.
  2. Imipenem Not absorbed orally
  3. Broken down by dehydropeptdiases in renal tubule-Cilastin inhibits this enzyme. increases Imipenem concentration
  4. Disrupt cell wall synthesis
  5. Metallo B lactamases will inactivate carbapenems. otherwise resistant to b lactamases
  6. SE: induce B lactamase production. May cause resistance to other drugs. Nausea, vomiting. Allergic rxns to PCN, Seizures
  7. Activity against GP and GN aerobes, and B fragilis (anaerobe)
  8. Should be reserved for serious nosocomial infection (resistant microbes or mixed infections)
  9. DONT USE FOR SURGICAL PROPHYLAXIS, MRSA, C. DIFF, E. FAECIUM
45
Q

Clavulanic Acid

A

B lactamase inhibitor
1. weak antibacterial activity
2. inactivates b-lactamase
3. most active against AMBER class A B lactamases (plasmid)
4. only included with PCNS
NOT GOOD WITH CLASS C B-LACTAMASES (chromosomal and inducible b lactamases of GNB)

46
Q

Tazobactam

A

B lactamase inhibitor
1. weak antibacterial activity
2. inactivates b-lactamase
3. most active against AMBER class A B lactamases (plasmid)
4. only included with PCNS
NOT GOOD WITH CLASS C B-LACTAMASES (chromosomal and inducible b lactamases of GNB)

47
Q

Amoxicillin + Clavulanic Acid

A

AUGMENTIN

  1. Oral
  2. penetrates peritoneal and pleural fluids
  3. high levels of drug in urine
  4. doesnt penetrate CNS
  5. must adjust for renal impairment
  6. Clavulanic Acid: “suicide inhibitor of b lactamase”
  7. Severe respiratory infections: double dose of Amox
  8. DRUG OF CHOICE FOR ACUTE OM, SINUSITIS, HUMAN/ANIMAL BITES, ALTERNATIVE FOR STREP PHARYNGITIS
  9. UTI
  10. CA NOT ACTIVE AGAINST ENTEROBACTER, PSEUDOMONAS, SERRATIA
48
Q

P. aeruginosa

A

Aminoglycoside

49
Q

Cephalosporins

A
  1. Derivative of 7 amino cephalosporanic acid
  2. Interfere with bacterial cell wall synthesis
  3. Bactericidal
  4. Antacid decrease absorption, H2 antagonists can decrease oral absorption
  5. 1st/2nd gen: not for CNS
  6. 3rd/4th: use for meningitis
  7. Avoid alcohol. inhibit aldehyde dehydrogenase–accumulation of acetaldehyde (usually methylthiotetrazole group)–dont use for 24-72hrs
  8. kill of VitK bacteria-coagulation issues
  9. seizures with renal impairment
50
Q

Cefdoxime, cefuroxime,

A

decreased oral absorption with H2 antagonists

51
Q

Cefdinir, Cefpodoxime, Cefaclor ER

A

Antacids decrease oral absorption

52
Q

Longest half life of cephalosporins

A

Ceftriaxone

53
Q

cephalosporin highly protein bound

A

cefonicid

54
Q

cephalosporin and serum sickness

A

Cefaclor

55
Q

Coagulation abnormalities, Cephalosporins

A

Cefazolin, cefmetazole, cefamandole, cefotetan, cefoperazone (dt methyltriotetrazole group)

56
Q

cephalosporin plus aminoglycoside or loop diuretic

A

renal tubular necrosis

57
Q

inactivation by b lactamase, cephalosporins

A

1st gen and 2nd gen cefaclor

58
Q

1st gen cephalosporins

A

Cefazolin, cephalexin

59
Q

2nd gen cephalosporins

A

cefaclor, cefoxitin, cefuroxime, cefprozil

60
Q

3rd gen cephalosporins

A

ceftriaxone, cefixime, cefotaxime, ceftazidime

61
Q

4th gen cephalosporin

A

cefepime

62
Q

5th gen cephalosporin

A

ceftaroline

63
Q

Cefazolin

A

1st gen cephalosporin
1. alcohol interolerance, bleeding disorders (vit K)
2. GOOD FOR GP BACTERIA (not Enterococci, MRSA)
3. GOOD FOR ORAL CAVITY ANAEROBES (NOT B. Fragilis)
4. GN enterics: PECK (proteus, E coli, Kleb)
5. DRUG OF CHOICE FOR SURGICAL PROPHYLAXIS
DONT USE FOR SYSTEMIC REACTIONS

64
Q

Cephalexin

A

1st gen cephalosporin
1. alcohol interolerance, bleeding disorders (vit K)
2. GOOD FOR GP BACTERIA (not Enterococci, MRSA)
3. GOOD FOR ORAL CAVITY ANAEROBES (NOT B. Fragilis)
4. GN enterics: PECK (proteus, E coli, Kleb)
DONT USE FOR SYSTEMIC REACTIONS

65
Q

Cefaclor

A

2nd gen cephalosporin

  1. Antacids decrease oral absorption with ER tablets
  2. LESS GP ACTIVITY THAN 1st
  3. MORE GN ACTIVITY
  4. Good against Sinusitis and OM
  5. Not effective against P. aeruginosa, enterobacter
66
Q

Cefoxitin

A 
ACTIVITY AGAINST B. FRAGILIS
NOT GOOD AGAINST SINUSITIS AND OM
2nd gen cephalosporin
2. LESS GP ACTIVITY THAN 1st
3. MORE GN ACTIVITY
5. Not effective against  P. aeruginosa, enterobacter
67
Q

cefuroxime axetil

A

COVERAGE AGAINST S. PNEUMO, H FLUE, K PNEUMO
GOOD FOR CAP
H2 antagonists decrease oral absorption.
HYDROLYZED INVIVO by esterases to active drug
2nd gen cephalosporin
2. LESS GP ACTIVITY THAN 1st
3. MORE GN ACTIVITY
4. Good against Sinusitis and OM
5. Not effective against P. aeruginosa, enterobacter

68
Q

cefprozil

A

2nd gen cephalosporin

  1. LESS GP ACTIVITY THAN 1st
  2. MORE GN ACTIVITY
  3. Good against Sinusitis and OM
  4. Not effective against P. aeruginosa, enterobacter
69
Q

Ceftriaxone

A 
3rd Generation cepahlosporin
LONGEST HALF LIFE
BILE EXCRETION-dont need to adjust for renal failure
MORE GN ACTIVITY THAN 2nd
RESISTANT TO B lactamases
LESS GP
CANT USE FOR L. Monocytogenes Meningitis
FIRST LINE FOR GONORRHEA
CAN PENETRATE CNS and TX GNR
LYME DISEASE
EMPIRICAL TX of SEPSIS
70
Q

Cefixime

A 
FIRST LINE FOR GONORRHEA
3rd Generation cepahlosporin
MORE GN ACTIVITY THAN 2nd
RESISTANT TO B lactamases
LESS GP
CANT USE FOR L. Monocytogenes Meningitis
EMPIRICAL TX of SEPSIS
71
Q

Cefotaxime

A 
CAN PENETRATE CNS AND TX GNR
3rd Generation cepahlosporin
MORE GN ACTIVITY THAN 2nd
RESISTANT TO B lactamases
LESS GP
CANT USE FOR L. Monocytogenes Meningitis
EMPIRICAL TX of SEPSIS
72
Q

Ceftazidime

A 
EFFECTIVE AGAINST P AERUGINOSA
CAN PENETRATE CNS AND TX GNR (use in combo with Aminoglycoside)
3rd Generation cepahlosporin
MORE GN ACTIVITY THAN 2nd
RESISTANT TO B lactamases
LESS GP
CANT USE FOR L. Monocytogenes Meningitis
EMPIRICAL TX of SEPSIS
73
Q

Cefepime

A

4th generation cephalosporin
1. extended spectrum
resistant to plasmid and chromosomal B lactamases
2. GOOD FOR P. aeruginosa and enterobacteriaceae
ENTEROBACTER INFECTIONS LIKE UTI
can penetrate CSF

74
Q

Ceftaroline fosamil

A

5th generation cephalosporin

  1. increase PBP binding
  2. activity against enterococci
  3. CAP
  4. Acute skin infections including MRSA
75
Q

Highly PCN resistant strep meningitis

A

VANCO

76
Q

Chloramphenicol

A
  1. chloramphenicol palmitate bd to active drug in duodenum
  2. IV use
  3. USE IN MENINGITIS
  4. BD in liver to glucorinide conjugate
  5. adjust for hepatic failure
  6. Binds 50s ribosomal subunit of 70s ribosome. prevents binding of aa tRNA. NO INTERACTION WTH PEPTIDYLTRANSFERASE
  7. SE: can inhibit mitochondrial protein synth in mammals
  8. CIDAL FOR H. flu, N men, S pneumo
  9. GOOD FOR GP GN and anaerobes
  10. MRSA and Pseudomonas are resistant
  11. CAN TREAT ROCKY MOUNTAIN SPOTTED FEVER, Q FEVER, TYPHUS
  12. Alternative tx for meningitis when allergy to PCN
  13. empiric tx for brain abscess
  14. Resistance dt production of acetyltransferase.
  15. SE: bone marrow suppresion, aplastic anemia (def. RBC production)
    GREY BABY SYNDROME: babies dont have enough glucoronl transferase. vomiting tachypnea, abdominal distantion, cyanosis
    PHENOBARBITAL AND RIFAMPIN DECREASE LEVELS
    INDUCES CYP450
77
Q

Tetracycline

A

PREFERRED FOR RICKETSIAL IFX
SHORT ACTING Tetra
found in breast milk and placenta
taking standing up with water. RISK OF ESOPHAGUS ULCERATION
antacids decrease absorption. no dairy
IV can cause thromboembolism
topical: used for blepharitis, conjunctivitis
NO CSF
bacteriostatic. INHIBIT PROTEIN SYNTH BY BINDING 30S. aa cant be added to peptide chain.
NOT DRUG OF CHOICE FOR GP
WILL TREAT GN aerobes. NOT PSEUdOMONAs OR ENTEROBAC
RICKETSIA, MYCOPLASMA, CHLAMYDIA, LYME
duodenal ulcers
RESISTANCE: Tet(AE) efflux pump of GN bacteria. DOXY AN DMINO NOT SUBSTRATES
-resistance encouraged by giving to animals for growth
SE: GI, superinfection, Dental discooration, flourescence, deformity (dont give during pregnancy), renal damage (FANCONI SYNDROME)–>ingestion of outdated drug, increased sens. to sun

78
Q

Doxycicline

A

LONG ACTING tetra
PREFERRED PARENTERAL
DOES NOT ACCUMULATE WITH RENAL FAILURE
DOC for LYME DISEASE
taking standing up with water. RISK OF ESOPHAGUS ULCERATION
antacids decrease absorption. no dairy
IV can cause thromboembolism
topical: used for blepharitis, conjunctivitis
NO CSF
bacteriostatic. INHIBIT PROTEIN SYNTH BY BINDING 30S. aa cant be added to peptide chain.
NOT DRUG OF CHOICE FOR GP
WILL TREAT GN aerobes. NOT PSEUdOMONAs OR ENTEROBAC
RICKETSIA, MYCOPLASMA, CHLAMYDIA, LYME
duodenal ulcers
RESISTANCE: Tet(AE) efflux pump of GN bacteria. DOXY AN DMINO NOT SUBSTRATES
-resistance encouraged by giving to animals for growth
SE: GI, superinfection, Dental discooration, flourescence, deformity (dont give during pregnancy), renal damage (FANCONI SYNDROME)–>ingestion of outdated drug, increased sens. to sun

79
Q

Minocycline

A

LONG ACTING tetra
LIPID SOLUBLE. secreted in tears and saliva. eliminate meningococcal carrier state
IMPORTANT FOR PERIODONTITIS. DECREASE POCKET DEPTH
taking standing up with water. RISK OF ESOPHAGUS ULCERATION
antacids decrease absorption. no dairy
IV can cause thromboembolism
topical: used for blepharitis, conjunctivitis
NO CSF
bacteriostatic. INHIBIT PROTEIN SYNTH BY BINDING 30S. aa cant be added to peptide chain.
NOT DRUG OF CHOICE FOR GP
WILL TREAT GN aerobes. NOT PSEUdOMONAs OR ENTEROBAC
RICKETSIA, MYCOPLASMA, CHLAMYDIA, LYME
duodenal ulcers
RESISTANCE: Tet(AE) efflux pump of GN bacteria. DOXY AN DMINO NOT SUBSTRATES
-resistance encouraged by giving to animals for growth
SE: GI, superinfection, Dental discooration, flourescence, deformity (dont give during pregnancy), renal damage (FANCONI SYNDROME)–>ingestion of outdated drug, increased sens. to sun

80
Q

Tigecycline

A

Tetracycline
1. derivative of monocycline
2. IV
3. eliminated non renally
4. inhibit protein synth by binding 30s ribosomal. prevent protein growth.
5. cant be pumped by Tet(Ae) or Tet(K) or Tet(M)
EFFLUX PUMPS FROM PROTEUS AND PSEUDO PREVENT IT
WORKS AGAINST MRSA< ACINETOBACTER, B lactamase GN
-skin infections, abdominal infxn

81
Q

Erythromycine base film coated

A

MACROLIDE
1. poor oral absorption
2. food decreases absorption
3. esters increase absorption (stearate, estolate, ethysuccinate)
4. IV if necessary
5. not in brain or CSF
6. crosses placenta
Bacteriostatic. reversible binding to 50s ribosomal subunit. inhibit movement of polypep chain and transpeptidation
7. CHLORAMPHENICOL AND MACROLIDES ANTAGONISTIC DT BINDING
8. H flu and Enterbac are resistant
GP and GN good
B fragilis is resistant
Mycoplasma, chlamydia, spirochetes good
CLINCAL USE: mycoplasma DOC, legionella pnemonia, COP, nonstrep hpahryngitis (cornebac), chlamydia. DOC in preg for UG infxn
9. PCN resistant S pneumo resistant to ery
Tx Campy infections
Methylase main cause of resistance
SE: can be used to increase gastric emptying, liver tox (cholestatic hepatitis), QT prolongation ,v tach, arrythmia
INHIBITS CYP450 (increase theophylline, anticoags, antihistamines)

82
Q

Erythromycine estolate

A

MACROLIDE
1. poor oral absorption
2. food decreases absorption
3. esters increase absorption (stearate, estolate, ethysuccinate)
4. IV if necessary
5. not in brain or CSF
6. crosses placenta
Bacteriostatic. reversible binding to 50s ribosomal subunit. inhibit movement of polypep chain and transpeptidation
7. CHLORAMPHENICOL AND MACROLIDES ANTAGONISTIC DT BINDING
8. H flu and Enterbac are resistant
GP and GN good
B fragilis is resistant
Mycoplasma, chlamydia, spirochetes good
CLINCAL USE: mycoplasma DOC, legionella pnemonia, COP, nonstrep hpahryngitis (cornebac), chlamydia. DOC in preg for UG infxn
9. PCN resistant S pneumo resistant to ery
Tx Campy infections
Methylase main cause of resistance
SE: can be used to increase gastric emptying, liver tox (cholestatic hepatitis), QT prolongation ,v tach, arrythmia
INHIBITS CYP450 (increase theophylline, anticoags, antihistamines)

83
Q

Erythromycine sterate

A

MACROLIDE
1. poor oral absorption
2. food decreases absorption
3. esters increase absorption (stearate, estolate, ethysuccinate)
4. IV if necessary
5. not in brain or CSF
6. crosses placenta
Bacteriostatic. reversible binding to 50s ribosomal subunit. inhibit movement of polypep chain and transpeptidation
7. CHLORAMPHENICOL AND MACROLIDES ANTAGONISTIC DT BINDING
8. H flu and Enterbac are resistant
GP and GN good
B fragilis is resistant
Mycoplasma, chlamydia, spirochetes good
CLINCAL USE: mycoplasma DOC, legionella pnemonia, COP, nonstrep hpahryngitis (cornebac), chlamydia. DOC in preg for UG infxn
9. PCN resistant S pneumo resistant to ery
Tx Campy infections
Methylase main cause of resistance
SE: can be used to increase gastric emptying, liver tox (cholestatic hepatitis), QT prolongation ,v tach, arrythmia
INHIBITS CYP450 (increase theophylline, anticoags, antihistamines)

84
Q

Erythromycin ethysuccinate

A

MACROLIDE
1. poor oral absorption
2. food decreases absorption
3. esters increase absorption (stearate, estolate, ethysuccinate)
4. IV if necessary
5. not in brain or CSF
6. crosses placenta
Bacteriostatic. reversible binding to 50s ribosomal subunit. inhibit movement of polypep chain and transpeptidation
7. CHLORAMPHENICOL AND MACROLIDES ANTAGONISTIC DT BINDING
8. H flu and Enterbac are resistant
GP and GN good
B fragilis is resistant
Mycoplasma, chlamydia, spirochetes good
CLINCAL USE: mycoplasma DOC, legionella pnemonia, COP, nonstrep hpahryngitis (cornebac), chlamydia. DOC in preg for UG infxn
9. PCN resistant S pneumo resistant to ery
Tx Campy infections
Methylase main cause of resistance
SE: can be used to increase gastric emptying, liver tox (cholestatic hepatitis), QT prolongation ,v tach, arrythmia
INHIBITS CYP450 (increase theophylline, anticoags, antihistamines)

85
Q

Erthyromycin lactobionate

A

MACROLIDE
1. poor oral absorption
2. food decreases absorption
3. esters increase absorption (stearate, estolate, ethysuccinate)
4. IV if necessary
5. not in brain or CSF
6. crosses placenta
Bacteriostatic. reversible binding to 50s ribosomal subunit. inhibit movement of polypep chain and transpeptidation
7. CHLORAMPHENICOL AND MACROLIDES ANTAGONISTIC DT BINDING
8. H flu and Enterbac are resistant
GP and GN good
B fragilis is resistant
Mycoplasma, chlamydia, spirochetes good
CLINCAL USE: mycoplasma DOC, legionella pnemonia, COP, nonstrep hpahryngitis (cornebac), chlamydia. DOC in preg for UG infxn
9. PCN resistant S pneumo resistant to ery
Tx Campy infections
Methylase main cause of resistance
SE: can be used to increase gastric emptying, liver tox (cholestatic hepatitis), QT prolongation ,v tach, arrythmia
INHIBITS CYP450 (increase theophylline, anticoags, antihistamines)

86
Q

Clarithromycin

A 
MACROLIDE
More acid stable than ery
better oral absorption
penetrates macrophages and PMNS
active metabolite in liver: 14 hydroxyclariothromycin
adjust doses for renal clearance
binds 50s ribosomal subunit
USES: pharyngitis (s. pyogenes (PCN is DOC), acute maxillary sinusitis, CAP dt mycoplasma, s pneumo, skindi infections. TX and PX of MAC
LESS GI UPSET THAN ERY
inhibits CYP
87
Q

Azithromycin

A

Macrolide
more acid stable. better orally than ery
penetrates all but cns
dont use to treat sepsis
slowly release, long duration of action (3d 1/2)
binds 50s ribosomal subunit
SINGLE DOSE TO TX GENITAL AND CHLAMYDIAL INFXN (as effective as 7d doxy)
MORE EFFECTIVE AGAINST H FLU
LESS ACTIVE AGAINST STAPH/STREP
doesNT inactivate CYP450. no drug interactions

88
Q

Telithromycin

A

Macrolide
oral
TX RESPIRATORY INFXN
MACROLIDE RESISTANT BACTERIA MAY BE SUSCEPTIBLE
binds to 50s ribosomal subunit but differently. can avoid methylase.
inhibits CYP3A4. increase statins. LIVER TOX

89
Q

First safe drug for infectious diseases

A

sulfonamides

90
Q

Sulfa and TMX

A

inhibit DNA synthesis by inhibiting folic acid pathway (need for purine bases)

separate: static
together: cidal

91
Q

Sulfasalazine

A

Sulfonamide
1. remains in bowel. use in UC and IBD
2. bd to 5 aminosalycilic acid. topical anti inflammatory and immune modulating
3. INHIBITS BACTERIAL DIHYDROPTEROATE SYNTHAse (converts PABA to dihydropteroic acid…precursor of folic acid)
4. ENTEROCOCCUS FAECALIS IS RESSITANT. AUXOTROPHIC FOR FOLIC ACID
–
SE: Crystaluria at acid pH
pts should increase fluids.
hemolytic anemia
bone marrow suppression-blood dyscrasia
anemia
HSN (more common in HIV). SJS
HyperK (blocks Na import in distal nephron)
malnourished pts: folate decrease
KERNICTERUS-BABIES: BILIRUBIN CROSSES BBB.
SULFA dipslaces drugs that bind albumin. increase serum? (warfarin, phenytoin, sulfonylurea hypglycemics)

92
Q

Sulfacetamide, Mafenide, Silver sulfadiazine

A

Sulfonamide
Topical agents for burns, opthalmological ointments for conjunctivitis and trachoma. Silver sulf is statndard for prevention of burn infection (negligable absorption is less toxicity)
3. INHIBITS BACTERIAL DIHYDROPTEROATE SYNTHAse (converts PABA to dihydropteroic acid…precursor of folic acid)
4. ENTEROCOCCUS FAECALIS IS RESSITANT. AUXOTROPHIC FOR FOLIC ACID
–
SE: Crystaluria at acid pH
pts should increase fluids.
hemolytic anemia
bone marrow suppression-blood dyscrasia
anemia
HSN (more common in HIV). SJS
HyperK (blocks Na import in distal nephron)
malnourished pts: folate decrease
KERNICTERUS-BABIES: BILIRUBIN CROSSES BBB.
SULFA dipslaces drugs that bind albumin. increase serum? (warfarin, phenytoin, sulfonylurea hypglycemics)

93
Q

Sufadoxine

A

Sulfonamide
ROLE IN MALARIA PROPHYLAXIS
3. INHIBITS BACTERIAL DIHYDROPTEROATE SYNTHAse (converts PABA to dihydropteroic acid…precursor of folic acid)
4. ENTEROCOCCUS FAECALIS IS RESSITANT. AUXOTROPHIC FOR FOLIC ACID
–
SE: Crystaluria at acid pH
pts should increase fluids.
hemolytic anemia
bone marrow suppression-blood dyscrasia
anemia
HSN (more common in HIV). SJS
HyperK (blocks Na import in distal nephron)
malnourished pts: folate decrease
KERNICTERUS-BABIES: BILIRUBIN CROSSES BBB.
SULFA dipslaces drugs that bind albumin. increase serum? (warfarin, phenytoin, sulfonylurea hypglycemics)

94
Q

Trimethoprim

A

inhibis dihydrofolate reductase (converts dihydrofolic acid to tetrhydrofolic acid)
1. more sensitive to bacteria than humans
MORE POTENT THAN SULFONAMIDES
1:5 ratio of trimeth: sulf (1:20 ratio in serum)
2. kidney excretion
3. Trimeth distributes more widely than sulfa
4. penetrates CSF
USES: UTI Prostatitis (in combo)
UT pathogens, RT pathogens, GI pathogens (E. coli, salmonella, vibrio)
5. L monocytogenes, yersinia, nocardia, toxoplasma, pneumocystis
6. high metabolites of bacteria=resistance
7. resistant to TMX-sulf: P aeruginosa, b fragilis, treponema, campy, rickets
E faecalis is auxotrophic!!
–
SE: Crystaluria at acid pH
pts should increase fluids.
hemolytic anemia
bone marrow suppression-blood dyscrasia
anemia
HSN (more common in HIV). SJS
HyperK (blocks Na import in distal nephron)
malnourished pts: folate decrease
KERNICTERUS-BABIES: BILIRUBIN CROSSES BBB.
SULFA dipslaces drugs that bind albumin. increase serum? (warfarin, phenytoin, sulfonylurea hypoglycemics)

95
Q

Aminoglycosides

A
  1. more active at alkaline pH
  2. forms complexes with b lactams. dont mix
  3. poor oral absorption
  4. polar. does not enter cells or CNS or eye
  5. can be intrathecal for meningitis (3rd gen ceph preferred)
  6. NEPHROTOXICITY AND OTOTOX
  7. uses O2 dependent active transport (not effective against anaerobes)
  8. cleared from kidney in direct proportion to creatinine
  9. irreversibly binds to 30s ribosomal subunit. cidal.
  10. block ribosome movement. mutant proteins. still works after MIC
  11. must determine trough concentration 30 min prior to next dose >2 is toxicity
  12. resistance: bacterial enzymes phosphorylate drug
  13. best against GN bacteria. NOT ANAEROBES
  14. endocarditis, severe systemic infxn
96
Q

Aminoglycoside ototoxicity

A

Streptomycin is worst
(SK, AG, TN)
worse if with loop diuretic
accumulate endolypm and perilymph in inner ear. destruction of vestbular and cochlear hair cells

97
Q

Auditory toxicity aminoglycoside

A

amikacin, kanaycine, netilmicin, neomycin

98
Q

vestibular toxicity aminoglycoside

A

gentamycin, streptomycine, tobramycin

99
Q

nephrotoxicity aminoglycosides

A

gent, tobra, neomyin

100
Q

treat neuromuscular block of aminoglycoside

A

IV ca slat, AChesterase inhibitor, mechanically ventilate

NEOMYCIN AND NETILMICIN

101
Q

aminoglycosides most resistant to inactivating enzymes

A

amikacin and netilmicin

102
Q

Gentamycin and tobramycin

A

good against S. aureus and S epdiermidis

103
Q

enterococci adn viridians group strep:

A

tx with gent/strep plus PCN G or AMP

104
Q

Bacterial endocarditis

A

PCN plus aminoglycoside

Pharmacology (6 decks)

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