Antimicrobial Flashcards

(52 cards)

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

22
Q

Monobactams

A

Monocyclic β- lactam antibiotics,

23
Q

Monobactams

24
Q

Aztreonam

A

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

25
Carbapenem
β- lactam
26
Carbapenem
Isolated from Streptomyces's
27
Carbapenem
Potent activity against a broad range of Gram-positive and | negative bacteria
28
Carbapenem
Resistant to lysis by β-lactamases
29
Carbapenem
2 important antibiotics 􏰀 Imipenem 􏰀 Meropenem
30
Carbapenem : Imipenem
􏰀 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
Carbapenem : Meropenem
􏰀 Stable and broad spectrum | 􏰀 Side effects .. Similar to imipenem
32
Glycopeptides
Vancomycin & Teicoplanin
33
Glycopeptides
􏰀 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
Glycopeptides
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
Glycopeptides
􏰀 Clinical use 􏰀 MRSA Methicillin resistant staphylococcus aureus 􏰀 Patient allergic to penicillin or cephalosporin with Staphylococcus or Streptococcal infections
36
Inhibition of nucleic acid | synthesis:
Inhibit DNA synthesis directly or indirectly
37
Inhibit DNA synthesis directly or indirectly
􏰀 Sulphonamides & Trimethoprim indirectly inhibit DNA synthesis
38
Inhibition of NA synthesis
􏰀 Quinolones directly inhibit DNA-gyrase
39
Inhibition of NA synthesis
Nitrofurantoin bindtobacterialribosomeandinhibitproteinsynthesis
40
Inhibition of NA synthesis
Rifampicin inhibit DNA dependent RNA polymerase
41
Nitrofurantoin
For uti only!
42
Nitrofurantoin
Mode of action is complex
43
Nitrofurantoin
􏰀 Act on bacterial mRNA, ribosomal proteins 􏰀 Well absorbed orally 􏰀 Used for UTI
44
Nitrofurantoin
Side effects: 􏰀 Nausea and vomiting 􏰀 Peripheral neuropathy 􏰀 Hemolysis in patients with G6PD deficiency
45
Quinolones
Form a large group of synthetic compounds | 􏰀 Have dual ring structure
46
Quinolones
Act by inhibiting DNA gyrase (topoisomerase) this will inhibit DNA replication
47
Quinolones
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
Quinolones .... Toxicity
``` Side effects: 􏰀 GI ( nausea, vomiting & diarrhea) 􏰀 Pseudomembranous colitis 􏰀 Skin rash 􏰀 CNS (benign intracranial hypertension) and psychosis 􏰀 Thrombocytopenia ```
49
Metronidazole
A 5-nitroimidazole
50
Metronidazole
Exert its effect by reduction of the nitro group to amine under low redox potential (anaerobic atmosphere)
51
Metronidazole
Active against obligate anaerobes & helicobacter and 􏰀 Protozoa (T. vaginalis, Giardia, E. histlolytica) 􏰀 Rapidly and completely absorbed form GI
52
Metronidazole
``` Side effect: 􏰀 CNS, confusion and seizures 􏰀 Peripheral neuropathy 􏰀 GI (nausea, vomiting & diarrhea) 􏰀 Neutropenia (reversible) 􏰀 Metallic taste 􏰀 Rash and pruritis ```