Pharm antibiotics Part 1 Flashcards

1
Q

Antibiotics that taget the cell wall and membrane?

A
  1. Beta Lactams
    * Pen, Ceph, Carb, Mono
  2. Glycopeptides
    * Vancomycin
  3. Cyclic lipopeptide
    * Daptomycin
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2
Q

types of beta lactams

A
  1. Penicillins
  2. Cephalosporins
  3. Carbapenems
  4. Monobactams
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3
Q

Fxn of beta lactam ab

A

ALL HAVE BETA LACTAM RING

Fxn: inhibit bacterial cell wall synth

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4
Q

Penicillin fxn

A

inhibit cell wall synthesis
structural analogs of PBP binding site- PBP enzyme that facilitates cross linking and stability

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5
Q

Penicillin subgroups

A
  1. Natural penicillins (Narrow spectrum)
  2. Aminopenicillins (broad)
  3. Penicillinase resistant penicillins
  4. Anti-pseudomonal penicillins (broad)
  5. Penicillin/Beta lactamase inhibitors
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6
Q

Categorizes of penicillins

A
  1. Narrow spectrum penicillins
    Natural penicillins= PENICILLIN V AND PENICILLIN G
  2. Broad spectrum penicillins
    Amino penicillins-> AMOXICILLIN AND AMPICILLIN
    Amino w/beta lactamase inhib-> AMOXICILLIN/CLAVULANATE, AMPICILLIN/SULBACTAM
    Antipseudomonal penicillin-> PIPERCILLIN/TAZOBACTAM
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7
Q

Natural Penicillins

ALL NARROW SPEC

A

1.PENICILLIN V-> greatest non bLactamase producing Gram positive ONLY SOME GRAM - FOR NEISSERIA
low systemic levels
2. PENICILLIN G->greatest non bLactamase producing Gram positive ONLY SOME
* Procaine penicillin G-> rapid acting
* Benzathine Penicillin G->long acting RHEUMATIC FEVER PROPHYLAXIS
* Combined repository (CR)-> combo of both

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8
Q

Rheumatic Fever prophylaxis + duration

A

Prophylaxis: Benzathine Penicillin G once a month-> for 5 years or till 21-> life long if valvular disease

Duration:
RF with Carditis + Residual heart disease= 10 yrs or 40 yo (which ever is longer)
RF with carditis NO residual= 10 yrs or 21 yo
RF w/out carditis= 5 yrs or until 21 yo

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9
Q

Treponema pallidum info and tx

A

TP= SYPHILIS (primary, secondary, tertiary)
Testing: Rapid plasma regain (RPR), Flouro trep ab absorp (FTA)
TX: NO KNOWN PCN RESISTANCE= Benzathine PCN for each

has neurosymptoms= Aquaeous Crystalline Penicillin G

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10
Q

Neisseria Meningitidis

Meningococcus

A

MOA: Gram Negative with endotoxin liberated from cell wall
TX:* High dose Penicillin G*
Empirically: if unsure use Ceftriaxone
Secondary contacts: rifampin or Ceftriaxone if prego
Vacc: Menactra and Bexero
Presentations: sudden fever, headache, stiff neck, N/V, sens to light
Children: inactivity, irritability, vomiting, poor reflexes

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11
Q

Penicillinase resistant penicillins

Anti-staphylococcal Penicillins

A

1.Oxacillin - for serious staph- endocarditis
2.Nafcillin- for serious staph- endocarditis
3.Dicloxacillin- skin and soft tissue infections- mild/mod
* Penicillinase producing staphylococci and streptococci

NOT MRSA

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12
Q

MRSA

NOT bETA LACTIMASE ISSUE

A

MUTATION W/ PENICILLIN BINDING PROTEIN
Tx: Vancomycin, Daptomycin

Methicillin Resistant Staphylococcus Aureus- specific to Staph

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13
Q

E
S
K
A
P
E

BUGS CAN BE HARD TO TREAT

A

E- Enteroccoccus faecium or E. coli idk
S- Staphylococcus aureus
K-Klebsiella pneumoniae
A- Acinetobacter baumannii
P-Pseudomonas aeruginosa
E-Enterobacter supp.

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14
Q

Impetigo

A

Cause: Staphylococcus Aureus or Streptococcus pyogenes
Tx depends on number of lesions: TRY TO COVER FOR BOTH BUGS
* Dicloxacillin
* Cephalexin
* narrow spec pen or ceph

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15
Q

Amino penicillins

A
  1. Amoxicillin- better oral than amp-> AOM, Lower resp tract inf-> PREFERRED FOR PNEUMOCOCCI
  2. Ampicillin-> h. pylori-> group B step sepsis in Neonates
    Overall: effective againts GRAM + AND GRAM - BUT NOT PENICILLINASE RESISTANT
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16
Q

Aminopenicillin/Beta lactamase inhib

A
  1. Amoxicillin/Clavulanate-> COVER GRAM NEG -> ACUTE BACTERIAL SINUSITIS
  2. Ampicillin/Sulbactam-> PROPHYLAXIS FOR POST OPP INF IN APPENDICITIS
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17
Q

Streptococcus Pneumoniae

Pneumococcus

A

Gram + diplocci
diseases involved:
* Pneumonia-> Amox
* AOM-> Amox
* Acute bacterial sinusitis-> Augmentin
* Meningitis-> Penicillin G

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18
Q

Antipseudomonal Penicillin

4th gen-> Ureidopenicillin

A

Piperacillin/Tazobactam
* piper only combined with tazo
* GRAM + COVERAGE WITH PIPER
* GRAM NEG-> pseudomonas, E. Coli, Klebsiella
Indications: PNA- pulm nodular amyloidosis, appendicitis or peritonitis, skin infections

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19
Q

Range from narrow to broad

A
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20
Q

General points with penicillin: MOA

drug resistance

PAPI

A

4 basic mech
1. Beta lactamase- MC- penicillinase
2. Alteration of PBPs- methicillin resistance- altered pbps
3. Impaired penetration-> Gram Neg only due to impermeable outer mem of cell wall- beta lactamase can enter Gram Neg via porins
4. Active pumping- efflux pump in gram neg

DRUG RESISTANCE

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21
Q

Beta lactamases

100s of them

A
  • Produced by: staphylococcus aureus, H. flu, Escherichia coli
  • Extended spectrum B lactamases: AmpC B-lactamase PRODUCED BY PSEUDOMONAS AERUGINOSA AND ENTERO-> HYDROLYZES CEPHALO AND PENICILL
  • Carbapenems->mostly res to penicillinases and cephlasporinases-> can hydrolyze metallo-beta lactamases and carbapenemases

typically prefer penicillins to ceph

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22
Q

Pharmacokinetics for Penicillins

A
  1. Oral Pen (not amox) = 1-2 hours after eating-> amox doesnt matter
  2. Serum conc rapidly equilibrate to most tissues EXCEPT EYE, PROSTATE, CNS
  3. Rapidly exreted by kidneys-> tubular secretions
    * Nafcillin = exc hepatic
    * Oxacillin, cloxacillin dicloxacillin- renal/hepatic
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22
Q

Pharmacokinetics for Penicillins

A
  1. Oral Pen (not amox) = 1-2 hours after eating-> amox doesnt matter
  2. Serum conc rapidly equilibrate to most tissues EXCEPT EYE, PROSTATE, CNS
  3. Rapidly exreted by kidneys-> tubular secretions
    * Nafcillin = exc hepatic
    * Oxacillin, cloxacillin dicloxacillin- renal/hepatic
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23
Q

AE Penicillins

A
  • very safe
  • non specific maculopapular rashes
  • GI upset in large doses= N/V, Diarr
  • Seizures in renal failure= high dose
  • TYPE 1 HYPERSENS IS MOST SERIOUS
  • Specific:
  • Nafcillin= NEUTROPENIA
  • Oxacillin, Nafcillin- hepatitis
  • Clavulanate- GI symp elderly, hepatitis, cholestasis
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24
Q

Parenteral Penicillins AE

aqueous

A

Hemolytic anemia
leukopenia
thrombocytopenia/neutropenia
neuropathy
nephropathy
Toxic epidermal necrolysis (TEN)

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25
Q

True Type 1 Hypersensitivity reactions= IgE mediated

A

Pruritis, Urticaria, Angioedema
N/V, flushing, wheezing, hypotension, anaphylaxis

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26
Q

Streptococcus species

Gram + Cocci

A
  1. Streptococcus Pyogenes (Group A strep)
  2. Streptococcus Agalactiae (Group B strep)
  3. Streptococcus Pneumoniae (Pneumococcus)
  4. Viridans Streptococci- Strep mitis, Strep anginous, strep salivarus
27
Q

Group A strep

A
  1. Erysipelas
  2. Cellulitis
  3. Necrotizing Fasciitis
  4. Streptococcal PHaryngitis
  5. Impetigo
  6. Rheumatic Fever
28
Q

Group A strep coccis and Tx

A

TX: Penicillin G or VK- for most strep infections

Erysipelas- tx depends on s&s of toxicity
* none= oral Penicillin or Amoxicillin
* yes= parental use= Ceftriaxone or Parenteral Aqueous crystalline Penicillin G

Necrotizing fasciitis= Penicillin 4 plus clindamycin

29
Q

Group B strep sepsis in neonates

A

Group B strep= GI and genital tracts
Maternal colonization in prego= PRIMARY RISK FACTOR for GBS in neonates
Confirmed during screening: PENICILLIN G 4 IS GIVEN INTRAPARTUM
* ampicillin is alternative or cefazolin if allergic

Diag INFANT= PENICILLIN G IS DRUG OF CHOICE

30
Q

Cephalosporins overall

A
  1. 4 generations based on structures and spectra
  2. MORes same as Penicillins
  3. Broader spectrum of coverage vs penicillins
31
Q

1-4 gen Cephalosporin

A
  1. Cefalexin, Cefazolin
  2. Cefoxitin, Cefuroxine, Cefotetan
  3. Ceftazidime, Ceftriaxon
  4. Cefipime
32
Q

Ceph 1st gen

Cefazolin, Cephalexin

A

Spectrum: GRAM += Staph and Strep
* activity against: E. Coli-, K pneumoniae, Proteus mirabilis

FDA APPROVED FOR SKIN, SOFT TISSUE, UTIS, RESP TRACT, STREP PHARYNGITIS

Cephalexin-> oral for skin, soft tissue, UTI
Cephazolin-> IV and IM= ANTI STAPH SURGICAL PROPHYLAXIS

33
Q

Ceph 2nd gen

Cefoxitin, Cefuroxime, Cefotetan

A

GREATER GRAM - COVERAGE
Cephuroxime- alt for AOM
Cefuroxine and Cefotetan- Anti-Anaerobic activity + pelvic inflam disease, prophylaxis for post opp appendicitis

34
Q

Ceph 3rd gen

Cefizime, Ceftriaxone, Cefdinir

A

EVEN GREATER GRAM - CROSS BBB
Spectrum: CEFTAZIDIME ONLY AGENT FOR PSEUDOMONAS AERUGINOSA
some improved staph coverage
Ceftriaxone= MANY INDICATIONS, use for meningitis for empiric coverage
excreted by kidney, require dose adjustment

35
Q

Ceftrixone uses

A

1.UTI
2.Uncomplicated Gonorrhea
3.Pelvic Inflammatory disease
4.Meningitis for empiric coverage CROSSES BBB

36
Q

Ceph 4th gen

Cefepime

A

hydrolyzed by extended spectrum Beta lactamases
Spectrum: Pseudomonas Aeruginosa, enterobacter,
PENETRATES well into CSF
Indications: Very sick people
Febrile neutropenia- empiric therapy
mod to severe pneumonia
complicated intraabdominal infections
Bacteremia

37
Q

Cephalosporin/BLactamase inhibitor combo

A
  1. Ceftazidime/Avibactam
  2. Ceftolozane/Tazobactam
    Inhibits other beta lactamases
38
Q

Cephalosporin 5th gen

A

Ceftaroline

39
Q

Ceph AE

A

Allergic reactions: common with penicillin, aminopenicillins, 1 and 2nd ceph
hypersens: anaphylaxis, fever, rashes, nephritis, granulocytopenia
Local irritation
renal toxicity/interstitial nephritis rarely
Seizures in renal insufficiency

40
Q

Ceph general info

A

Broader spectrum ceph= greater risk of C. diff diarr
All ceph= renal elim= no dosage adj but MONITOR FOR CKD-> except ceftriaxone= Biliary tract

Meningitis tx that reach csf levels high enough: Ceftriaxone, cefotaxime, ceftazidime, cefepime

41
Q

Ceph general info

A

Broader spectrum ceph= greater risk of C. diff diarr
All ceph= renal elim= no dosage adj but MONITOR FOR CKD-> except ceftriaxone= Biliary tract

Meningitis tx that reach csf levels high enough: Ceftriaxone, cefotaxime, ceftazidime, cefepime

42
Q

Carbapenems

A
  1. Imipenem
  2. Meropenem
  3. Ertapenem
43
Q

Carbapenem basics

A

all parenteral agents
REN ADJUSTING IF RENAL DISEASE
MOA: enter Gram - through porins and bind PBPs
MOR: produce Beta lactamases, efflux pumps, mutations of porins or pbps

44
Q

Carbapenems: Spectrum of activity

A

1.Broad spectrum of Activity
2. Gram - organisms-> H flu, N. Gonorrhea, including those that produce extended spectrum beta lactamases
3. Gram + organisms
4. NO ACTIVITY AGAINST MRSA

45
Q

Imipenem

Carbapenems

A

Beta lactamase resistant
GOOD AGAINST GRAM NEG RODS
inactivated in pct by dehydropeptidase 1 soooo ADD Cilastatin to inhibit
* cause seizures in those with renal failure in high amounts
* GOOD TISSUE PERF INCLUDING CSF

AE: GI, rash, site reactions

46
Q

Meropenem and Ertapenem

dont spend alot of time on

A

Meropenem= no need for Cilastatin, for bacterial meningitis, greater act against neg but less pos than imipenem
Ertapenem= not fo pseudomonas, long half life

47
Q

Antibiotics that target the cell wall and cell membrane

A

1.Beta lactams
2.Glycopeptides-> Vancomycin
3.Daptomycin

48
Q

Glycopeptide->Vancomycin

A

MOA: inhibits cell wall biosynth-> blocks glycopeptide polymerization
MOR: produce D-ala-D-lactate dipsipeptide which thwarts vanc
Excretion: RENAL CLEARANCE = MARKED DOSE ADJ FOR RENAL FAILURE
SE: rash, thrombocytopenia, bullous dermatitis, nephro/ototoxic rare, RED MAN SYNDROME- flushing caused by rapid infusion due to release of histamine

49
Q

Vancomycin indications

A

NO GRAM - COVERAGE
Positive: for sensitive staph aureus, enterococcus, bacteremia and endocarditis caused by MRSA
+ aminoglycosides for serious inf
CLOSTRIDIOIDES DIFFICILE INFECTION

50
Q

Daptomycin

targets cell wall and cell membrane

A

MOA: binds to cell mem via calcium dependent insertion of the lipid tail-> potassium efflux= cell death
Spectrum: GRAM + : MRSA, MSSA, VISA, VRSA
Indications: serious bacterial skin infections by +, bacteremia or endocarditis caused by S. AUREUS STRAINS AND MRSA

51
Q

Daptomycin AE

A
  1. Eosinophilic pneumonia: 2-4 wks after therapy start
  2. DRESS syndrome: angioedema, drug rash w/ eosinophilia, systemic symptoms
  3. Myopathy/Rhabdomyolysis: Creatinine Phosphokinase CPK should be monitored WEEKLY during therapy
52
Q

Empiric tx for common skin and soft tissue infections (SSTI)

A

Purulent (abscess, furuncle, carbuncle, cellulitis with purulence)-> staph aureus is common-> 1. drain 2.Cephalexin or Clindamycin if mrsa 3. extensive= cefazolin low mrsa concern or Vancomycin/daptomycin if mrsa

Non purulent (cellulitis, erysipelas)-> Beta hemolytic strep-> 1.Cephalexin, amox, clindamycins or IV cefazolin or vancomycin

53
Q

Antimetabolites

A
  1. Sulfonamides
  2. Trimethoprim
  3. Trimethoprim-sulfamethoxazole (TMP-SMX)
54
Q

Sulfonamides

A

Topical: Silver Sulfadiazine-> burn tx
Oral: Sulfamethoxazole or Sulfadiazine and Pyrimethamine (acute toxoplasmosis)

General: GRAM POS AND NEG
MOA: inhibits Dihydropteroate Synthase-> INTERRUPTING FOLATE

55
Q

Sulfonamides AE

A

Hematologic effects: Megaloblastic anemia or hemolytic/aplastic anemia
photosens
stevens johnson syndrom
DO NOT GIVE TO NEONATES UNDER 3 MONTHS OR MOMS AT END OF PREGO-> increase unconjugated bilirubin and increase kernicterus in fetus (brain damage)
CANT GIVE TO SULFA ALLERGY OR PORPHYRIA

56
Q

Trimethoprim

A

MOA: interrupt human folate metabolism-> prevent tetrahydrofolic formation
MOR: point mutations in DHFR structural gene

57
Q

Trimethoprim-sulfamethoxazole

bactrim

RUGS

A

Indications:
r- Respiratory tract infections
u-uti
g-GI infections
s-Skin infections- MRSA

Contraindications:
sulfa allergy
AVOID IN PREGO DUE TO EFFECT ON FOLIC ACID METAB

AE: STEVENS JOHNSON SYND, HYPERKALEMIA-> BLOCK OF THE COLLECTING TUBULE SODIUM CHANNEL, HIV + HIGHER CHANCE OF RXN

58
Q

Erythema Multiforme, Stevens Johnson Syndrome, Toxic Epidermal Necrolysis

A
  1. Erythema multiforme-> target lesions, oral lesions, hands forearms
  2. Stevens Johnson Syndrome- kids, uri like prodrome, MOST DUE TO DRUG REACTIONS, MORE THAN 2 MUCOSAL SITES, admit to burn center
  3. Toxic epidermal necrolysis- elderly, HIV increased risk, mucous mem, BURN CENTER
59
Q

Stevens Johnson Syndrome

test question

A

1.Rare
2.RF: Drugs, mycoplasma, CMV
3.start: fever, flu like symp
4.Then: blistering->skin, mucous mem, urogenital tract
5.Difficulty: breathing, swallow, urinating
6.LIFE THREATENING
7.BARRIER LOSS CAUSES FLUID LOSS AND INCREASE SUSCEP TO INFECTION/SEPSIS

60
Q

Antimetabolite indications

A

1.Sulfonamides- topical for sepsis, ORAL= ACUTE TOXOPLASMOSIS
2.Trimethoprim- conjunctivitis
3.Bactrim (TMP/SMX)- UTI, skin infections

61
Q

Antimetabolite indications

A

1.Sulfonamides- topical for sepsis, ORAL= ACUTE TOXOPLASMOSIS
2.Trimethoprim- conjunctivitis
3.Bactrim (TMP/SMX)- UTI, skin infections

62
Q

Fluoroquinolones names

A
  1. Ciprofloxacin
  2. Levofloxacin
  3. Ofloxacin
  4. Moxifloxacin
  5. Gatifloxacin
63
Q

Fluoroquinolones general

A

MOA: directly inhibit bacteria DNA
MOR: site mutations, plasmid= target mimics, Resistance increases the duration of therapy
Route: oral
Excretion: Renal clearance, adjust for GFR
Spectrum coverage: Gram -, Gram +, intracellular and poorly staining organisms-> pseudomonas coverage

64
Q

Fluoroquinolones indications

A

Ciprofloxacin-> Gram - with Pseudomonas: conjunctivitis, anthrax, otitis externa
Levofloxacin-> COMMUNITY ACQUIRED PNEUMONIA, better gram +
Ofloxacin-> conjunctivitis
Moxifloxacin->comm acquired pnemonia, better gram + coverage

65
Q

Ciprofloxacin

A

GOOD FOR PREGO AND POST EXPOSURE ANTHRAX
CHILDREN WITH COMPLICATED UTIs

cipro plus levofloxacin= approved for children for post exposure to inhalation of anthrax or the plague

66
Q

TX for acute bacterial conjunctivitis

COTE

A

Empiric approach:
1. Erythromycin
2. Trimethoprim drops
3. Ofloxacin opthalmic drops
4. Ciprofloxacin drops