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Pharm 5 > Antibacterial Agents > Flashcards

Antibacterial Agents Flashcards

1
Q

What are the B-lactams?

Are they -cidal or -static?

What is their mechanism?

A

Penecillins

Cephalosporins

Carbapenems

Aztreonam

-cidal

Bind to PBP and inhibit transpeptidation

So, inhibit an enzyme

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2
Q

SE of penicillins

A
  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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3
Q

Penicillin G

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Narrow spectrum: G+

Natural penicillin

Route: IV or IM–hydrolyzed w/ stomach acid

Given w/ procaine to slow release

Destroyed by B lactamase

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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4
Q

Penicillin V

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Narrow spectrum: G+

Route: Oral

Natural penicillin

Absorption unpredictable

Destroyed by B lactamase

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
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5
Q

B lactamase resistant penicillins

Name and spectrum

A

Nafcillin

Oxacillin

Cloxacillin**

Dicloxacillin**

Methicillin

“Nafcillin and -oxacillin”s

NAFcillin=Not AFfected by penicillinase

  • Oxacillin’s=Ox is resistant to penicillinase*
  • Methicillin too but not in use anymore*

Narrow spectrum

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6
Q

Nafcillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons

NAFcillin=Not AFfected by penicillinase

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7
Q

“-oxacillin”s

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons

OXacillin=OX is strong animal, resistant to penicillinase

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8
Q

Methicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

Do not use anymore-too toxic

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9
Q

Broad or extended spectrum penicillins

A

Amoxicillin

Ampicillin

Ticarcillin

Piperacillin

Mezlocillin

Carbenicillin

TAMPAC

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10
Q

Amoxicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Route: Oral

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • B lactam ring may inh. GABAergic neurons
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11
Q

Ampicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Rash in pts who have mononucleosis +other viral inf.
  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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12
Q

Ticarcillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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13
Q

Piperacillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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14
Q

Mezlocillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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15
Q

Carbenicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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16
Q

Sulbactam

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

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17
Q

Clavulanic acid

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

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18
Q

Augmentin

A

Amoxicillin+clavulanic acid

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19
Q

Timentin

A

Ticarcillin and clavulanic acid

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20
Q

Unasyn

A

Ampicillin and sulbactam

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21
Q

What’s the difference b/w each generation of cephalosporins?

A

Succeeding generation has:

  • more G- activity (broader spectrum)
  • More res. to B lactamase
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22
Q

Cephalosporins

A

cef or ceph

SE:

  • Allergic cross activity w/ penicillin sensitive pts
  • Possibility of superinfection
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23
Q

Carbapenems

A

Tx: Antibacterial–mixed infections

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad

Route: IV

SE:

  • Can enter CNS→Seizures
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24
Q

Imipenem

A

Tx: Antibacterial–mixed infections

Class: Carbapenem

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad-Better against G+

Route: IV

SE:

  • Can enter CNS→Seizures
  • Metabolized in kidney to nephrotoxic product
    • Given w/ cilastatin which inh. enzyme that produces toxic product
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25
Q

Meropenem

A

Tx: Antibacterial–mixed infections

Class: Carbapenem

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad-Better against G-

Route: IV

SE:

  • Can enter CNS→Seizures
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26
Q

Cilastatin

A

Given w/ impenem

Prevents nephrotoxic product by inh. enzyme

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27
Q

Aztreonam

A

Antibacterial

Class: Monobactam

Route: IV or IM

Not affected by lactamases

Spectrum: Aerobic G- organisms

Not cross reactive w/ allergic pts

SE:

  • Seizures
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28
Q

Vancomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Binds to dialanine residue on CW and prevents cross linking

Use: Severe infection in which B lactams can’t be used

Primary alt. to penicillins for staph infections.

Spectrum: G+

Route: IV–unless target in gut (pseudomembranous colitis)

SE:

  • Nephrotoxicity
  • Ototoxicity
  • If given rapidly via IV→histamine release→Redman or red neck syndrome
    • Flushing
    • Rash
    • Itching

Resistance:

  • Target changed
  • Dialanine changed to lactic acid

Dr. Van Ron

Dialanine Residue. Vancomycin. Redman. Ototox. Nephrotox

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29
Q

“-vancin”s

A

Televancin

Dalbavancin

Antibacterial

Class: Non B lactam CW inhibitors

Lipoglycopeptide

Mech: Binds to dialanine residue on CW and prevents cross linking + disrupt bacterial CM

SE:

  • Nephrotoxicity
  • Fetal damage
  • Metallic taste
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30
Q

Bacitracin

A

Antibacterial

Class: Non B lactam CW inhibitors

Polypeptide

Mech: Inh. recycling of bactoprenol carrier

Spectrum: G+

Route: Topically–very toxic

SE:

  • Nephrotoxicity–if not given topically
31
Q

Fosfomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Blocks synth of NAM

Spectrum: Aerobic G-

Use: Uncomplicated UTI

SE:

  • Diarrhea–killing bacteria in gut
32
Q

Cycloserine

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Inh. incorporation of alanine into NAM

Enzyme inhibitor

Used against mycobacterium TB

SE:

  • CNS
    • Sedation
    • Tremor
    • Psychosis
  • Cyclo- gives you psycho-*
  • Go to war in NAM, when you come back you have PTSd*
  • Psychosis*
  • Tremors*
  • Sedation*
33
Q

Erythromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth

-static

Mech: Reversibly binds to 50s subunit and inh. translocation of mRNA

Inh binding of tRNA to P site

Spectrum: G+

SE:

  • GI upset, nausea, and heartburn
    • Increase in GI activity b/c activates motilin
  • Inh P450
  • Liver damage
  • Arrythmias

macROlides like erythROmycin inh. transLOcation

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Ototoxicity

34
Q

Clarithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Oral stability

vs. Helicobacter Pylori
* macROlides like erythROmycin inh. transLOcation*

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Oral stability/Ototoxicity

35
Q

Azithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Longer T1/2 (3 days)

macROlides like erythROmycin inh. transLOcation

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Ototoxicity

36
Q

Telithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Same sites as erythromycin (50s) but induces less resistance b/c not readily transported out of bacterial cell

SE:

  • GI upset, nausea, and heartburn
  • Increase in GI activity b/c activates motilin
  • Inh P450
  • Liver damage-_SEVERE liver toxicity_
  • Arrythmias
  • Block cholinergic receptor
    • Worsen myasthenia gravis
    • Inh long ciliary ganglion→Decrease visual accomodation

macROlides like erythROmycin inh. transLOcation

Motility/ Myasthenia gravis worsens

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Ocular inh./Ototoxicity

37
Q

Streptomycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

Spectrum: Aerobic G-

Must be absorbed by active transport

SE:

  • Ototoxicity
    • Hearing and balance affected
    • hearing loss may be permanent
  • Nephrotoxic
    • Most common cause of drug induced renal failure
    • Used very widely
  • High doses
    • Neuromuscular blockade
      • Decrease in ACh+ ACh receptors on mm
    • Fetal damage
      • Preg cat. D

​​​

  • Strippers fornicate*
  • Strep. FORNICAT*

Fetal damage

Ototox.

Renal tox

Negative (G-)

Irr. bind 30s

Cidal

*ACh block *

tRNA can’t bind to mRNA

  • *
38
Q

Aminoglycoside antibacterial agents

Names and mech

A

Streptomycin

Gentamycin

Tobramycin

Neomycin

Amikacin

Kanamycin

Netilmicin

_Kan_ye’s Cobra _A_rose _Gent_ly as _N_aughty _Nat_alie Stripped

_Kan_amycin _Tobra_mycin _A_mikacin _Gent_amycin _N_eomycin _Netil_mycin _Strept_omycin

Mech: Irr bind to 30s subunit

Can inh. or alter tRNA binding along mRNA including initiation site

Irr. mRNA misreading=bactericidal

39
Q

Gentamycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

**Use: **Ointment for eye

40
Q

Tobramycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

41
Q

Neomycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

Route: Topical or oral

**SE: **Very nephrotoxic–so only topically or orally

42
Q

Amikacin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

43
Q

Kanamycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

44
Q

Netilmicin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

DROPPED in the US

45
Q

Tetracycline

A

Tx:

  • Rickettsia
  • Spirochetes (lyme disease)
  • Helicobacter
  • Legionella

Mech: Reversibly bind to 30s.

Inhibits the binding of tRNA to the A site

-static

SE

  • Deposited in Ca storage sites-bones/teeth-esp fetus or child
    • Binds to cations, esp Ca, also Fe and Al.
    • Preg risk D
  • Renal and hepatic toxicity
  • Degrades to toxins–don’t use after expiration date
46
Q

Other cyclines vs tetracycline

A

Less likely to bind Ca+

47
Q

Chloramphenicol

A

Antibacterial agent

Mech: inh. peptidyl transferase

SE:

  • Inh. P450
  • Can cause aplastic anemia
    • Hemolytic anemia too (said this in the review)
  • Gray baby syndrome
    • Metabolized by a phase II enzyme that is not active in newborns.
    • Can’t metabolize it→baby turns blue and circulatory system inhibited
48
Q

Clindamycin

A

Antibacterial agent–lincosamide

Mech: like erythromycin-inh. translocation

SE: Severe superinf. w/ C. dificile

Targets:

  • Severe anaerobic infections (penetrating gut wound)
  • Dental prophylaxis in pts w/ heart valve problems
49
Q

Lincomycin

A

Antibacterial agent–lincosamide

Mech: like erythromycin-inh. translocation

SE: Severe superinf. w/ C. dificile

Targets:

  • Severe anaerobic infections (penetrating gut wound)
  • Dental prophylaxis in pts w/ heart valve problems
50
Q

-pristin

A

Quinupristin (A+P site)

Dalfopristin (P site)

Mech: Inh. A and P sites

Always used together–synergistic

SE: Muscle pain

Spectrum: G+

51
Q

-zolid

A

Linezolid

Tedizolid

Mech: Inh. binding of fmet (start codon) tRNA to P site

Prevents initiation of protein synth.

SE

  • Anemia
  • Pseudomembranous colitis
    • Will happen w/ any powerful AB b/c of C. dificile
52
Q

Daptomycin

A

Antibacterial agent–lipopeptide

Mech: Forms pores in bacterial CM

Targets: Aerobic G+ (staph, strep)

Skin and soft tissue inf. or severe blood inf w/ S. aureus

SE:

  • Muscle pain and weakness
    • careful w/ statins
  • Eosinophilic pneumonia
53
Q

Fidaxomycin

A

Antibacterial agent

Mech: Inh. C. dificile RNA pol

Orally–Not systemically absorbed

Target: C. dificile

54
Q

-floxacin

A

Antibacterial agent

Mech:

  • Inh topoisomerase II (DNA gyrase)
  • Inh topoisomerase IV

No effect on mammalian topoisomerase

SE:

  • May damage developing cartilage
    • Not for children or pregnant women
  • Tendonitis–achilles tendon rupture
  • Phototoxicity (drug in skin responds to sunlight)
  • May worsen myasthenia gravis
    • Peripheral neuropathy (said it in review along w/ retinal detachment)

Spectrum: Broad–G+,G-, Acid fast

55
Q

Sulfisoxazole

A

PABA*→folic acid→DHFA**→THFA

*→=Dihydropterate synthetase

**→DHFR

Mech: Reversible inh. dihydropterate synthetase

For UTIs

SE:

  • Allergic whole body rash (Stevens Johnson syndrome)
  • Hemolytic anemia in G6PDH deficient pts
  • Megaloblastic anemia

Sulfa drugs have sulf or sul

56
Q

Trimethoprim

A

Antibacterial agent

Mech: Inh. DHFR (like methotrexate)

Specific for bact. enzyme

*Used in conj. w/ sulfamethoxazole *

SE:

  • Megaloblastic anemia
    • Can be avoided w/ leucovorin

Targets:

  • G- bacteria
  • UTIs
    • Concentrates in acidic prostate and vaginal tissue
57
Q

Metronidazole

A

Mech: Prodrug-converted to a free radical active molecule by obligate anaerobic bacteria

Route: IV for severe anaerobic bacterial inf.

Use: Protozoal inf:

  • Trichoma (STD)
  • Giardia (from water)

SE:

  • Seizures
  • Peripheral neuropathy
58
Q

Nitrofurantoin

A

Mech: Reduced by bacteria to a highly reactive molecule

Concentrates in urine

Use: UTI

SE:

  • Cough
  • Chest pain
  • Brown urine
59
Q

Polymixin B

A

Antibacterial agent

Mech: Binds to negatively charged sites on LPS of G- bact

→to memb. permeability

Route: Topical

SE: (all reversible)

  • Nephrotoxic
  • Neurotoxic
  • Neuromuscular blockade
  • Ataxia
  • Perioral paresthesia
  • Poly mixes in her PANNNN*
  • Polymixin B. Perioral paresthesia. Ataxia. Neurotoxic. Nephrotoxic. Neuromuscular blockade. binds to Negatively charged sites on LPS*
60
Q

Gramicidin

A

Antibacterial agent

Mixture of 3 diff peptide AB

Mech: forms pores in bacterial CM

Route: topical

NEVER give IV–toxic

Spectrum: G+

61
Q

Retapamulin

A

Antibacterial agent

Mech: inh. peptidyl transferase

Route: Topical

Use: skin staph or strep inf.

62
Q

Mupirocin

A

Mech: Binds to bacterial isoleucyl tRNA synthetase

Route: Topical

Use: Staph inf.

63
Q

Neosporin

A

Neomycin+ polymixin +gramcidin

64
Q

Polysporin

A

polymixin+ bacitracin

65
Q

Polytrim

A

Trimethoprim+ polymixin

66
Q

Terak

A

oxytetracycline+ polymixin

67
Q

Isoniazid

A

Antimycobacterial agent

Mech: Produces inh. of multiply mycobacterial enzymes

Inh CW synth

Prodrug

Cidal, but static for dormant cells

Used alone for prophylaxis–in combo for active tx

Metabolized by acetylation–slow acetylators affected

SE:

  • Increase excretion of vit B6→pyroxidase deficiency→niacin deficiency
  • Pellegra
  • Peripheral neuropathy
  • Optic neuritis
  • Hepatotoxicity

Isoniazid is IHOPPIN

Inh. mycobacterial enz.

  • Hepatotox.
  • O**ptic neuritis.

*Peripheral neuropathy + Pellegra. *

Prodrug + Prophylaxis

Increase excretion of vit B6→→

Niacin def.

68
Q

Rifampin

A

Antimycobacterial agent

Antibacterial agent

Mech: Inh DNA dep. RNA polymerase

-cidal

SE:

  • Hepatic toxicity
  • Red color in all body fluids
  • Induces P450–very strong
    • Can metabolize BC!

Rifampin=red

Will metabolize BC (induce P450) so the sperm will LIVEr

69
Q

Pyrazinamide

A

Antimycobacterial agent

Mech: Inh FA synth

Prodrug converted in macrophase where TB lives

SE:

  • Gout
  • Hepatitis
70
Q

Ethambutol

A

Antimycobacterial agent

Mech: Inh arabinosyl transferase

Necessary for CW synth

SE:

  • Optic neuritis
  • Impaired red/green discrimination
  • Decreased vision
71
Q

Bedaquiline

A

Antimycobacterial agent

Mech: inh. mycobacterial ATP synthetase

Always used w/ 3 other anti-TB drugs

SE:

  • Arrythmias
  • Increase incidence of death

*You’re in your bed MASTurbating your erection (arrection) *

_Bed_aquiline. Mycobacterial Atp SyntheTase. Arrythmia.

72
Q

Dapsone

A

Antimycobacterial agent

Related to sulfonamides

Mech: Reversible inh. dihydropterate synthetase

Use: For mycobacterium leprae (leprosy

73
Q

Antimycoplasma agents

A

NO CELL WALL!

So use non CW inhibitors:

Erythromycin

Tetracycline

74
Q
A

Pharm 5 (4 decks)

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