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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
Parenteral Penicillins AE | aqueous
Hemolytic anemia leukopenia thrombocytopenia/neutropenia neuropathy nephropathy Toxic epidermal necrolysis (TEN)
25
True Type 1 Hypersensitivity reactions= IgE mediated
**Pruritis, Urticaria, Angioedema** N/V, flushing, wheezing, hypotension, anaphylaxis
26
Streptococcus species | Gram + Cocci
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
Group A strep
1. Erysipelas 2. Cellulitis 3. Necrotizing Fasciitis 4. Streptococcal PHaryngitis 5. Impetigo 6. Rheumatic Fever
28
Group A strep coccis and Tx
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
Group B strep sepsis in neonates
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
Cephalosporins overall
1. 4 generations based on structures and spectra 2. MORes same as Penicillins 3. Broader spectrum of coverage vs penicillins
31
1-4 gen Cephalosporin
1. Cefalexin, Cefazolin 2. Cefoxitin, Cefuroxine, Cefotetan 3. Ceftazidime, Ceftriaxon 4. Cefipime
32
Ceph 1st gen | Cefazolin, Cephalexin
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
Ceph 2nd gen | Cefoxitin, Cefuroxime, Cefotetan
GREATER GRAM - COVERAGE Cephuroxime- alt for AOM Cefuroxine and Cefotetan- Anti-Anaerobic activity + pelvic inflam disease, prophylaxis for post opp appendicitis
34
Ceph 3rd gen | Cefizime, Ceftriaxone, Cefdinir
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
Ceftrixone uses
1.UTI 2.Uncomplicated Gonorrhea 3.Pelvic Inflammatory disease 4.Meningitis for empiric coverage CROSSES BBB
36
Ceph 4th gen | Cefepime
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
Cephalosporin/BLactamase inhibitor combo
1. Ceftazidime/Avibactam 2. Ceftolozane/Tazobactam Inhibits other beta lactamases
38
Cephalosporin 5th gen
Ceftaroline
39
Ceph AE
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
Ceph general info
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
Ceph general info
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
Carbapenems
1. Imipenem 2. Meropenem 3. Ertapenem
43
Carbapenem basics
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
Carbapenems: Spectrum of activity
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
Imipenem | Carbapenems
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
Meropenem and Ertapenem | dont spend alot of time on
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
Antibiotics that target the cell wall and cell membrane
1.Beta lactams 2.Glycopeptides-> Vancomycin 3.Daptomycin
48
Glycopeptide->Vancomycin
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
Vancomycin indications
NO GRAM - COVERAGE Positive: for sensitive staph aureus, enterococcus, bacteremia and endocarditis caused by MRSA + aminoglycosides for serious inf CLOSTRIDIOIDES DIFFICILE INFECTION
50
Daptomycin | targets cell wall and cell membrane
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
Daptomycin AE
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
Empiric tx for common skin and soft tissue infections (SSTI)
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
Antimetabolites
1. Sulfonamides 2. Trimethoprim 3. Trimethoprim-sulfamethoxazole (TMP-SMX)
54
Sulfonamides
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
Sulfonamides AE
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
Trimethoprim
MOA: interrupt human folate metabolism-> prevent tetrahydrofolic formation MOR: point mutations in DHFR structural gene
57
Trimethoprim-sulfamethoxazole | bactrim ## Footnote RUGS
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
Erythema Multiforme, Stevens Johnson Syndrome, Toxic Epidermal Necrolysis
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
Stevens Johnson Syndrome | test question
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
Antimetabolite indications
1.Sulfonamides- topical for sepsis, ORAL= ACUTE TOXOPLASMOSIS 2.Trimethoprim- conjunctivitis 3.Bactrim (TMP/SMX)- UTI, skin infections
61
Antimetabolite indications
1.Sulfonamides- topical for sepsis, ORAL= ACUTE TOXOPLASMOSIS 2.Trimethoprim- conjunctivitis 3.Bactrim (TMP/SMX)- UTI, skin infections
62
Fluoroquinolones names
1. Ciprofloxacin 2. Levofloxacin 3. Ofloxacin 4. Moxifloxacin 5. Gatifloxacin
63
Fluoroquinolones general
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
Fluoroquinolones indications
Ciprofloxacin-> Gram - with Pseudomonas: conjunctivitis, anthrax, otitis externa Levofloxacin-> COMMUNITY ACQUIRED PNEUMONIA, better gram + Ofloxacin-> conjunctivitis Moxifloxacin->comm acquired pnemonia, better gram + coverage
65
Ciprofloxacin
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
TX for acute bacterial conjunctivitis | COTE
Empiric approach: 1. Erythromycin 2. Trimethoprim drops 3. Ofloxacin opthalmic drops 4. Ciprofloxacin drops

Pharm (9 decks)

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