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Pharmacology FINAL (2nd sem) > C: 8-13 > Flashcards

C: 8-13 Flashcards

1
Q

bacterial cell wall synthesis inhibitors

A
  • penicillins
  • cephalosporin
  • Vancomycin
  • Fosfomycin
  • Bacitracin
  • Carbapenams
  • Aztreonam
  • Daptomycin - distrupts cell membrane.
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2
Q

All penicillin are derivatives of ——— and contain a ——–

A

All penicillin are derivatives of —–6-aminopenicillanic acid—- and contain a —-beta lactam ring—-

beta lactam ring is essential for antibacterial activity

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3
Q

penicillin pharmacokinetics

bioavailability, excretion, plasma half life

A
  • subtypes have different resistance to gastric acid & oral bioavalability
  • penicillin are POLAR;
  • NOT metabolized extensively (unchanged in urine)
  • Exceptions: Ampi (excreted mainly in the bile)
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4
Q

forms of Penicillin G

A
  • Procaine
  • Benzathine
    • administered I.M
    • for syphilis
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5
Q

Penicillins cross BBB when?

A

meninges inflammed

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6
Q

penicillin Parenteral formulations available for injection?

A

Ampi

Pipera

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7
Q

beta lactam antibiotics have what effect on bacteria?

A

bactericidal

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8
Q

mechanism of action of penicillin

A

They act to inhibit cell wall synthesis:

(1) binding of the drug to PBPs on cytoplasmic memb.
(2) inhibition of the transpeptidation reaction (cross-link the peptidoglycan)
(3) activation of autolytic enzymes → lesions in the bacterial cell wall.

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9
Q

resistance mechanism against penicillins

A
  • formation of Beta-lactamases (eg penicillinases):

* solution: beta-lactamase inhibtiors (tazobactam, clauvulanate)

  • structural change in PBP
  • changes in porin structures in the (outer cell membrane)
    impedes access of penicillin to PBP
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10
Q

Types of penicillin and names

A
  • Narrow spectrum (penicillinase-susceptible agents)
    • Penicillin G:
      • streptococcal
      • syphilis
    • Penicillin V:
      • oral for oropharngeal infections
  • Very narrow spectrum (penicillinase-resistant)
    • Oxacillin
      • staphylo
  • wider spectrum (penicillinase susceptible)
    • Ampi
    • Amoxi
    • pipera
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11
Q

clinical use for Very narrow spectrum penicillinase resistance drugs

A
  • Oxacillin

known/suspected staphylococci infections

***NOT active against MRSA, MRSE***

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12
Q

clinical use for wider spectrum penicillinase susceptible drugs

A
  • Ampicillin & amoxicillin
    • Streptococcal
    • Enterococci
    • E-coli
    • Hemophilis influenza
  • used in combo with clauvulanic acid
  • synergistic effects with aminoglycosides
  • piperacillin:
    • gram negative rods: (PEK)
      • Pseudomonas,
      • Enterobacter
      • Klebsiella (some species)
    • synergistic effects with aminoglycosides
    • often used in combo with tazobactam & clauvulanic
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13
Q

Toxicity of penicillin

A
  • Allergy: (hypersensitivty reactions)
    • urticaria, pruritis, fever, joint swelling,
    • hemolytic anemia, nephritis, anaphylaxis
  • Ampicillin frequently causes maculopapular rash ( which doesnt appear as allergic rxn)

GI symptoms:
Nausea, diarrhea

due to Direct irritation OR overgrowth of gram + organisms or yeast

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14
Q

cephalosporins are derivative of ——- and contain a ——-

A
  • 7-amino.cephalo.sporanic acid
  • contain a beta lactam ring
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15
Q

cephalosporin pharmacokinetics

A
  • most are administered parenterally
  • major elimination mechanism in renal excretion via active tubular secretion.
  • Exception_:_ ceftriaxone excreted mainly in bile
  • Most 1st and 2nd G DONT enter CSF even when meninges inflammed
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16
Q

Mechanism of action cephalosporin

A
  • inhibit cell wall transpeptidation
  • binds PBPs-→ inhibit cell wall synthesis

Cephalosporins are bactericidal against susceptible organisms.

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17
Q

mechanism of resistance against cephalosporin

A
  • production of other betalactamases that can inactivate cephalosporins.
  • decreases in membrane permeability and from changes in PBPs.
  • MRSA are also resistant to cephalosporins.
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18
Q

clinical uses of 1st generation cephalosporin

A
  • Cefazolin (parenteral)
  • CephaLexin (oraL)
  • They are active against gram-positive cocci:
    • staphylo
    • streptoco
    • E.coli and K.pneumoniae
  • infections caused by these organisms and surgical prophylaxis
  • renal elimination
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19
Q

clinical use for 2nd gen cephalosporin

A
  • *cef.uroxim & cef.oxitin:**
  • *(the ones with OXI)**
  • less activity against gram + but have an extended gram - coverage
  • Ex:
    • cefoxitin: anaerobe Bacteroides fragilis
    • cefuroxime: H.influenza or M catarrhalis
  • short half lives
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20
Q

clinical use for 3rd gen cephalosporin

A

cef.tazi.dime → pseudomonas

cefo.taxime → PRSP

Ceftriaxone (parenteral) → PRSP, gonorrhea

cefixime (oral) → gonorrhea

  • pneumonia, meningitis, gonorrhea

increased activity against gram-negative organisms resistant to other beta lactam drugs

  • ability to penetrate the blood-brain barrier (except cefixime).
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21
Q

clinical use for 4th generation cephalosporin

A
  • *cefepime**
  • *Ceftaroline**

Ceftolozane +tazobactam

Broad activity

Beta-lactamase-stable

  • cefepime: more resistant to beta-lactamases (by gram - )
  • combines G + activity of 1stGs with the wider G - spectrum of 3rdGs
  • Ceftaroline: (MRS)
  • ceftolozane + tazobactam : MRSA
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22
Q

Cephalosporin toxicity

A
  • allergy:
    skin rash + anaphylactic shock
  • penicillin allergic pts can be treated with cephalosporin.
    • However in pts with history of anaphylaxis to penicillin SHOULDNT be treated with cephalo
  • Pain at I.M injection site
  • Phlebitis after I.V
  • increase nephrotoxicity of aminoglycosides when adminitered together
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23
Q

Monobactam

A
  • Az.Treo.nam
  • beta lactam drug
    • resistant to beta-lactamases produced by certain gram - rods
    • NO activity against gram + nor ANarobes
    • mechanism:
      → Bind to and inhibit cell wall transpeptidatio
      → Inhibitor of cell wall synthesis by binding specific PBP
    • Synergistic with aminoglycosides
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24
Q

Aztreonam is administered

eliminated?

A

I.V

eliminated via renal tubular secretion

  • half life is prolonged in renal failure
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25
Q

Aztreonam Adverse effects

A
  • GI upset
  • headache
  • skin rash ( although no cross-alergenicity with penicillins)
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26
Q

Chloramphenicol
Polymixins
Antifolate

A
  • Chloramphenicol
  • is a big long word. Big like 50S “bacteriostatic”-
    • Inhibit Peptydil transferase
    • Grey baby ( If you spill chlorine on a baby it will turn gray) + dose-related anemia
    • For meningitis
  • Antifolate: (anti-metabolite of PABA)
    • Sulfametoxazole inhib Dihydropteroate synthase. Sulga drug, G6PD, nephro (bacteriostatic)
    • Trimethoprin inhib Dihydro folate reductase. Bone marrow supp.
    • Proguanil : bioactivated to cycloguanil.
      • selective inhibitors of protozoan dihydrofolate reductases.
  • Colistin (polymixin E)
    • ​cationic detergent ; distrupts cell membranes
    • bactericidal

sulfametoxazole +trimethoprim = synergistic inhibition of folic acid synthesis (bactericial)

27
Q

Colistin

A

Cationic
Disturb the membrane
Inactivates endotoxins

Give topical due to severe toxicity

28
Q

Aminoglycosides

A

GANT? yeS! קניתי (I bought)

Genta.mycin
Tobra.mycin
Netil.mycin
Strpto.mycin
Neo.mycin
Kana.mycin
Amikacin

For aerobic G-
(E.coli , h.flu, M catarrhalis, shigiella)

* Commonly given with B-lactam
* Ototoxicity, Nephro., teratogenic

29
Q

Neomycin
Kanamycin

A
  • Suppress intestinal flora before bowel surgery
  • Neomycin topical
30
Q

Imipenem/Meropenem
Which genereation?

31
Q

Give imipenem with

A

Cilastatin to inhibit formation of nephrotoxic metabolite

(because its rapidly inactivated by renal-dihydropeptidases 1)

32
Q

Imipenem/Meropenem
When to give

A

Hospital aquired
Pneumonia
Sepsis

  • broad spectrum
    • some PRSP (NOT MRSA)
    • Gram - rods
    • pseudomonas
33
Q

Imipenem/Meropenem
Special SE

A
  • confusion and Seizures due to inhibition of GABA-R
  • partial cross-reactivity with penicillin
34
Q

Give Tzobactam with

A

Pipera.cillin

35
Q

Give Meropeneme with

A

Vabor.bactam

36
Q

Community aquired pneumonia Tx.

A

Clarithromycin
Azithro

37
Q

ICU pneumonia Tx.

A

B lactam IV + Macrolides/Fluoro-

38
Q

B lactam AB resistant to B lactamase

A

Carbapenems

BUT! bacteria can have Carbapenemase (MBL)

39
Q

Chloramphenicol MOA

A

S50
Inhibits Peptydil transferase

40
Q

Chloramphenicol indication

A

Empiric for meningitis

41
Q

Chloramphenicol SE

A

Grey baby syndrome
Bone marrow
Aplastic anemia

42
Q

Polymixin

A

Colistin
Cell wall
Inactivate endotoxins
Topical
Neuro and nephro-toxic

43
Q

Antifolate drugs

A

Sulfamethoxazole- inhibit DH pteroate Synthase
Trimethoprim- inhibit DHF Reductase

Proguanil- inhibit folate synthesis

44
Q

Sulfamethoxazole
Trimethoprim

Indications

A

Gram - (e.coli)

gram + ( MRSA, strep, staph)

PJP -Pneumocystis

45
Q

Sulfamethoxazole MOA

A

inhibits dihydropteroate synthase

Compete with PABA

46
Q

Sulfamethoxazole
Trimethoprim

SE

A
  • Sulfamethoxazole- Sulfa,
    • bone marrow,
    • G6PD,
    • nephro,
    • teratogenic ,
    • SJS

Trimethoprim- Bone marrow

47
Q

Glycyl.cycline

A

Tigecycline

48
Q

Tigecycline
indication

administration

elimination

SE

A

organisms resistant to standard tetracyclin (MRSA , VRE)

IV!

excreted in bile

Enamel, bone growth
Hepatotoxiciy
Nephrotoxic
Photosensitivity
Vestibular toxicity

49
Q

DoxyCycline indications

A

CAP (Community aq pneumonia)

Chlamydia
Gonorrhea

50
Q

Doxycycline elimination

51
Q

Aminglycosides

A

GANTS is in the army
Gentamycin
Amikacin(אני קצין)
Netilmycin
Tobramycin (cobra sign)

**Streptomycin

Neomycin
Kanamycin**

inhibit protein synthesis via 30s

52
Q

Gentamycin
Amikacin(אני קצין)
Netilmycin
Tobramycin(cobra sign)

indication

administration

A

Aerobic G-

parenteral

53
Q

Which AB are time dependant?

A

Penicillin
Cephalosporins

independent of c oncentration once the MIC has been reached.

54
Q

Which AB are concentration dependant?

A

Aminglycosides

55
Q

What does concentration dependant mean?

A

As the plasma level increases above the MIC > antibacterial effect increases

(aminoglycosides kill an increasing proportion of bacteria and at an increasingly rapid

rate)

56
Q

Streptomycin

indication, administration

A

TB (2nd line)
Tuleramia
Plague

I.M/ I.V

57
Q

Neomycin
Kanamycin

A

Suppress intestinal flora before bowel surgery
Neomycin for topical/oral

58
Q

Aminglycosides SE

A

Ototoxicity (irreversible) - in newborns after fetal exposure
Nephrotoxic (reversible)

Neuromascular blockade (at high dose)

Teratogenic

59
Q

How to remember Aminglycosides are teratogenic?

A

צבא זה לא משחק ילדים

חיילים צריכים הרבה אמינו אסידס

This army is not a children’s game

Soldiers need a lot of amino acids

60
Q

Carbapenams

A
  • Imipenem-cilastin
  • Meropenem + Vabor bactam

Binds and inhibit cell wall trans-peptidation

Chemically diff than penicillin but have same beta lactam ring.

61
Q

carbapenams activity spectrum and clinical uses

A
  • Broad spectrum
    • PRSP
    • gram negative rods
    • pseudomonas

DOESNT work against MRSA

62
Q

carbapenams Pharmacokinetics and interaction

A
  • Parenteral
  • Cilastin
    • inhibits renal metabolism of imipenem (inactivated by renal dehydropeptidase 1)
    • inhibits formation of nephrotoxic metabolite
    • other carbapenams are not significantly degraded by kidney
  • Renal elimination
  • useful in infections caused by organisms resistant to other antibiotics
63
Q

Carbapenams toxicity

A
  • Partial cross-reactivity with penicillins
  • CNS effects including : seizure and confusion

Pharmacology FINAL (2nd sem) (37 decks)

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