Antimicrobial Flashcards

1
Q

Group 1: parenteral penicillin

A

􏰀 Benzyl penicillin

􏰀 Procaine penicillin (long acting)

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2
Q

Group 2: Oral penicillin similar

A

Penicillin

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3
Q

Group 3: Anti-staphylococcal penicillin

A

Cloxacillin

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4
Q

Group 4: Extended-spectrum penicillin

A

􏰀 Active against Enterobacteriacea except Pseudomonas
􏰀 Ampicillin
􏰀 Amoxicillin

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5
Q

Group 5: penicillin active against Pseudomonas aeruginosa

A

Piperacillin

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6
Q

Group 6: β-lactamase-resistant penicillin

A

􏰀 Active only against Gram-negative

􏰀 Temocillin

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7
Q

Penicillin …… Toxicity and Side effects

A

􏰀 Hypersensitivity reaction Mild like skin rash or fatal
􏰀 Anaphylactic reaction ( rare, rapid reaction within minutes, nausea, vomiting , dyspnea and coma, fatal)
􏰀 Purities and urticarial reaction (develop within 1-3days )
􏰀 Skin eruptions usually maculopapular rashes (commonest)
􏰀 Hemolytic anemia and thrombocytopenia
􏰀 Neurotoxicity with high doses (rare)

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8
Q

Cephalosporin

A

􏰀 Have a 6-membered dihydrothiazine ring fused to a β- lactam ring
􏰀 They are derivative of 7- aminocephalosporanic acid (7-ACA)
􏰀 The additional carbon affect the pharmacokinetic and antibacterial activity

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9
Q

Cephalosporin

A

􏰀 The principal target is like penicillin (Transpeptidase)

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10
Q

Cephalosporin

A

􏰀 Have advantages over penicillin in that they are:
􏰀 More stable to enzymes ( Staphylococcus penicillinases)
􏰀 Broader spectrum
􏰀 Less prone to cause hypersensitivity
􏰀 Oral and parenteral preparations
*** Less active against Enterococci

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11
Q

Classification of Cephalosporin

A

1 2 3 4

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12
Q

First generation

A

First generation
􏰀 Cephalexin
􏰀 Cephazolin
􏰀 Wide range of Gram-positive and negative except (Pseudomonas and Haemophilus)

active against Streptococcus, Staphylococcus, Enterobacteriac

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13
Q

Second generation

A

􏰀 Cefuroxime
􏰀 Cefoxitin
􏰀 Wide range of Gram-positive and negative including Haemophilus and
anaerobes
􏰀 Cefuroxime: like cephalexin plus active against Haemophilus and S. pneumoniae

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14
Q

Third generation

A

􏰀 Cefotaxime

􏰀 Ceftriaxone

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15
Q

Third generation

A

􏰀 Ceftazidime (antipseudomonal)

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16
Q

3rd generation

A

Wide range but more anti-Gram-negative than second generation

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17
Q

Cefotaxime

A

active against Enterobactericae, Haemophilus and S. pneumoniae and not active against Pseudomonas spp

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18
Q

4th generation

A

Narrow

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19
Q

4th generation

A

􏰀 Cephepime
􏰀 Anti-Gram-negative
􏰀 cephepime: active against Enterobacteriacae and Pseudomonas

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20
Q

Cephalosporin … Toxicity and

Side Effects

A

􏰀 Local pain and thrombophlebitis at site of injection
􏰀 Hypersensitivity reaction in 0.5-10% of patients (10% cross
reaction with penicillin allergy)
􏰀 Hepatotoxicity Elevates liver enzymes
􏰀 Gastrointestinal disturbance
􏰀 Thrombocytopenia
􏰀 Pseudomembranous colitis

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21
Q

β- lactam

A

Monobactams

22
Q

Monobactams

A

Monocyclic β- lactam antibiotics,

23
Q

Monobactams

A

Aztreonam

24
Q

Aztreonam

A

􏰀 Narrow spectrum (anti-Gram-negative aerobic bacilli)
􏰀 Bactericidal
􏰀 Stable to bacterial enzymes

25
Q

Carbapenem

A

β- lactam

26
Q

Carbapenem

A

Isolated from Streptomyces’s

27
Q

Carbapenem

A

Potent activity against a broad range of Gram-positive and

negative bacteria

28
Q

Carbapenem

A

Resistant to lysis by β-lactamases

29
Q

Carbapenem

A

2 important antibiotics
􏰀 Imipenem
􏰀 Meropenem

30
Q

Carbapenem : Imipenem

A

􏰀 Not stable, it need to be combined with cilastatin to be more stable 􏰀Safe
􏰀 Broad spectrum
􏰀 Seizures and transient changes in liver enzymes are main side effects

31
Q

Carbapenem : Meropenem

A

􏰀 Stable and broad spectrum

􏰀 Side effects .. Similar to imipenem

32
Q

Glycopeptides

A

Vancomycin & Teicoplanin

33
Q

Glycopeptides

A

􏰀 Mode of action
􏰀 Act on cell wall synthesis at a stage prior to B-lactams
􏰀 Not act on PBP & not inactivated by B-lactamases enzymes
*Very big molecule and can’t take it orally *Used mainly for severe cases.

34
Q

Glycopeptides

A

Spectrum and Toxicity
􏰀 Activity is restricted to Gram-positive bacteria only
􏰀 Poorly absorbed from GI
􏰀 IM injections are painful
􏰀Nephrotoxic Reversible
􏰀Ototoxic Irreversible
􏰀 Reversible neutropenia and thrombocytopenia
􏰀 Teicoplanin is less nephrotoxic
􏰀 The level of vancomycin should be monitored in the blood

35
Q

Glycopeptides

A

􏰀 Clinical use
􏰀 MRSA Methicillin resistant staphylococcus aureus
􏰀 Patient allergic to penicillin or cephalosporin with Staphylococcus or Streptococcal infections

36
Q

Inhibition of nucleic acid

synthesis:

A

Inhibit DNA synthesis directly or indirectly

37
Q

Inhibit DNA synthesis directly or indirectly

A

􏰀 Sulphonamides & Trimethoprim indirectly inhibit DNA synthesis

38
Q

Inhibition of NA synthesis

A

􏰀 Quinolones directly inhibit DNA-gyrase

39
Q

Inhibition of NA synthesis

A

Nitrofurantoin bindtobacterialribosomeandinhibitproteinsynthesis

40
Q

Inhibition of NA synthesis

A

Rifampicin inhibit DNA dependent RNA polymerase

41
Q

Nitrofurantoin

A

For uti only!

42
Q

Nitrofurantoin

A

Mode of action is complex

43
Q

Nitrofurantoin

A

􏰀 Act on bacterial mRNA, ribosomal proteins
􏰀 Well absorbed orally
􏰀 Used for UTI

44
Q

Nitrofurantoin

A

Side effects:
􏰀 Nausea and vomiting
􏰀 Peripheral neuropathy
􏰀 Hemolysis in patients with G6PD deficiency

45
Q

Quinolones

A

Form a large group of synthetic compounds

􏰀 Have dual ring structure

46
Q

Quinolones

A

Act by inhibiting DNA gyrase (topoisomerase) this will inhibit DNA replication

47
Q

Quinolones

A

The 4-quinolones like naladixic acid
􏰀 Fluoroquinolones (new like Ciprofloxacin)
􏰀 More potent
􏰀 Broader spectrum (UTI, Osteomyelitis, STD, Pneumonia)
􏰀 Better absorption and distribution (oral & parenteral)

48
Q

Quinolones …. Toxicity

A
Side effects:
􏰀 GI ( nausea, vomiting & diarrhea)
􏰀 Pseudomembranous colitis
􏰀 Skin rash
􏰀 CNS (benign intracranial hypertension) and psychosis 
􏰀 Thrombocytopenia
49
Q

Metronidazole

A

A 5-nitroimidazole

50
Q

Metronidazole

A

Exert its effect by reduction of the nitro group to amine under
low redox potential
(anaerobic atmosphere)

51
Q

Metronidazole

A

Active against obligate anaerobes & helicobacter and
􏰀 Protozoa (T. vaginalis, Giardia, E. histlolytica)
􏰀 Rapidly and completely absorbed form GI

52
Q

Metronidazole

A
Side effect:
􏰀 CNS, confusion and seizures
􏰀 Peripheral neuropathy
􏰀 GI (nausea, vomiting & diarrhea) 􏰀 Neutropenia (reversible)
􏰀 Metallic taste
􏰀 Rash and pruritis