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Pharmacology > Penicillins > Flashcards

Penicillins Flashcards

1
Q

Beta-lactam antibiotics

A
  1. Penicillins
  2. Cephalosporins
  3. Lactamase-inhibitors
  4. Monobactams
  5. Carbapenems
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2
Q

What do Penicillin work on

A

binds to PBP (penicillin binding protein) in Transpeptidase and Carboxypeptidase which are responisble for the cell wall cross-linking of transpeptide bonds (N-acetyl-muramic acid + N-acetyl-glucoseamine chain) .
effects only dividing cells! (= cell wall synthesis) -> bacteriolysis

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3
Q

Penicillin mode of action

A

Bactericidal
time dependant (3-5 days)
+ post-antibiotic effect

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4
Q

Resistancy

A

Types:

i. Beta-Lactamase production:
1. Staphyloccoci sp - Gram + are the most sensitive as they usually don’t produce B-lactamse- except for Staph
2. Pseudomonas aureginosa - Gram - are more resistant produce B-lactamase, especially P.aureginosa)
3. Mycobacteria, Brucella , Chlamydia- Acid fast bacteria are the most resistant.
4. Mycoplasma (no cell wall)
ii. PBP gene mutation (e.g MRSA+MRSP-methicillin resistant Staphylococcus aureus+ Staph. pseudointermedius)

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5
Q

Penicillin main indications

A

Gram positive bacteria:
Bacillus, Clostridium, streptococcus, Erysipelothrix, Cornybacterium, Arcanobacterium pyogenes , Actinomyces, Listeria .

*NOT in mycobacterium, Staphyloccocus, enterococcus.

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6
Q

Penicillin spectrum classes

A
  1. Narrow spectrum penicillins: G+ , destroyed by beta-lactamase.
  2. Penicillinase stable penicillins: G+ , not destroyed by beta-lactamse
  3. Broad spectrum penicillins (aminopenicillins): both G+ and G- ,amoxicillin . NOT pseudomonas
  4. Penicillins acting against Pseudomonas spp.
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7
Q

Narrow spectrum penicillins - drug names

A

IM,SC

  1. Benzylpenicillin–Na, K: water soluble, 2-4h
  2. Benzylpenicillin–procaine: slow, 24h
  3. Benzylpenicillin – benzathine: very slow 72-96h
  4. Phenoxymethyl-penicillin: PO
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8
Q

Narrow spectrum penicillins - Bacteria

A
  1. Most of the Gram+ bacteria
  2. Gram – fastidious organisms : pasturella, histophilus, haemophilus and mannhemia
  3. Leptospira, Borrelia spp.
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9
Q

Narrow spectrum penicillins - pharmacokinetics

A

Hydrophilic drug,cannot enter the cell (not against IC bacteria), cannot cross BBB, excretion via kidneys unchanged (good for UTI)
short HL
no liver toxicity
*PO: phenoxymethyl-penicillin

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10
Q

Narrow spectrum penicillins - Side effects

A

almost non-toxic , allergies , dysbacteriosis in monogastric herbivores (Eq, rabbit , herbivore rodents)- stop if diarrhea
*Procaine-penicillin - local anesthetic, most toxic, ataxia, termour, piglets are sensitive

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11
Q

Narrow spectrum penicillins - indications

A

drug of choice in:

i. Swine erysipelas
ii. Anthrax
iii. Tetanus
iv. Clostridium perforinges
v. Streptococcosis (eq: strangle, SA: skin, laryngitis , Ru: mastitis , su: septicaemia)
vi. (mastitis,metritis)

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12
Q

Penicillinase stable penicillins - bacteria

A
  • Only G+ (bacillus,clostridium , sterptoccocus, erysipelothrix, cornybacterium, aracnobaterium pyogenes, actinomyces,listeria)
  • staphyloccocus is resistant.
  • does not effect mycobacterium and enterococcus
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13
Q

Penicillinase stable penicillins - drug names

A
  1. Oxacillin (0Cl)
  2. Cloxacillin (1 Cl)
  3. Dicloxacillin (2Cl)
  4. Flucloxacillin (Cl- and Chlorine, best distribution)
  5. Methicillin - not used (acid sensitive - destroyed by stomach)
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14
Q

Penicillinase stable penicillins -Indications

A

i. Mastitis (bo) - Intramammary infusion (staph+strep mostly)
ii. (Dermatitis (ca) - non reliable oral dist.)

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15
Q

Broad spectrum penicillins - Bacteria

A
  1. All G+ except for mycobacterium
  2. G- :
    i. Fastidius: Pasturella,Haemophillus, actinobacillus, Manheimia
    ii. Enterobacteriaceae: E. coli , salmonella, klebsiella
    iii. Anaerobic bacteria: Proteus ,baceriodes , fusobacterium (oral cavity, bite wounds)
    iv. Leptospira and Borrelia
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16
Q

Broad spectrum penicillins - Drugs + Pharmcokinetics

A
  1. Ampicillin: weak-moderate PO, reduces feed, IV (-Na,-Trihydrate)
    * combination: SULBACTAM
  2. Amoxicillin: good-excellent PO, does not reduce feed, IV (-Na, -Trihydrate)
    * combination: CLAVULANIC ACID
  3. Bacampicillin
  4. Pivampicillin
17
Q

Broad spectrum penicillins- Amoxicillin indications

A
  1. UTI: Amoxicillin is the 1st choice (E.coli)
  2. GI - only in Clostridium perfringes
  3. Dermatitis (Staph), in combination with Calvulanic acid
  4. Lyme disease (borrelia)
  5. Bite wounds + oral infections: anaerobic G- , + calvulanic acid
  6. Osteomyelitis - staph , + calvulanic acid
18
Q

Penicillins acting against Pseudomonas spp

A
  • Best and most expensive
  • used in life threatening anaerobic infections (intestinal perforation->peritonitis)
  1. Piperacillin (+ Tazobactam): IV,IM
  2. Ticarcillin (+CA): PO
  3. (Carbenicillin)
19
Q

Beta-lactones inhibitors: Salbactam (+ampicillin), Tazobactam (+piperacillin) and Calvulanic acid (+amoxicillin)

A

suicide inhibitors to be destroyed by B-lactamase instead of the antibiotic.
*works also against G+ Staphylococcus

20
Q

Monobactams

A

Excellent activity against UTI

  1. Azotreonam - parenteral
  2. Tigemonam (PO)
21
Q

Carbapenems

A

Last resort antibiotics!! IV,IM, highly active against all important known pathogenic bacteria!!

  1. Imipenem (+Cilastatin): metabolized by dihydropeptidase in the kidneys
  2. Meropenem

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