Protein Synthesis Inhibitors II

Question 1

Fusidic acid

1. Type of antibiotic
2. MOA
3. Admin + Adjunct
   4.Indications

Answer 1

1. Steriod antibiotic
2. Similar to macrolides(50s) -inhibts translocation
3. Taken with food(orally) and topically-acute skin infections(5days) and conjunctive
4. Severe staphylococcal infections

Question 2

Min days for topical admin for fusidic acid

Answer 2

5 days

Question 3

Fusidic acid S/E and extra info-4?

Answer 3

1. Hepatotoxicity (Reversible)
2. Kernicterus
3. GIT effects(take with meals)
4. IM-Local tissue necrosis

Question 4

Fusidic acid DI?

Answer 4

1. Hydrocortisone (Decreased antibiotic activity of fuisdic acid)
2. Statins (Increased risk of rhabdomyolysis)

Question 5

Fusidic acid CI?

Answer 5

Hepatic dysfunction & pregnancy

Question 6

Mupirocin 3 MOA?

Answer 6

Inhibits:

1. Protein synthesis
2. DNA & RNA synthesis
3. Cell wall synthesis

Question 7

Mupirocin

1. Bacteria MOA
2. Admin
3. Type of bacteria

Answer 7

1. Bactericidal
2. Topical only(no systemic absorption)
3. Gram +ve bacteria

Question 8

Mupirocin preparations?

Answer 8

Preparations contain polyethylene glycol=may lead to toxicity

Question 9

Mupirocin and Methicillin bacteria?

Answer 9

Methicillin-resistant staph aureus

Question 10

Mupirocin S/E?

Answer 10

-Burning
-Mild stinging
-Itching at site of application

Question 11

Mupirocin caution?

Answer 11

Porphyria

Question 12

Ketolides CYP450?

Answer 12

CYP450 Inhibitors

Question 13

Ketolides MOA?

Answer 13

-Similiar effects as macrolides-Inhibit 50s

-Also inhibits the formation of new ribosomes

-Binds to two sites on the bacterial ribosome with higher affinity than macrolides

Question 14

Ketolides derivative?

Answer 14

Semi-synthetic derivatives of Erthromycin A-Telithromycin

Question 15

Ketolides dosage frequency and max days of admin?

Answer 15

Once daily dosage(5 days)

Question 16

Ketolides S/E-4?

Answer 16

1. Respiratory failure (Myasthenia gravis patients)
2. Hepatotoxicity
3. Visual disturbances
4. Loss of consciousness

Question 17

Oxazolidinones type of antibiotic?

Answer 17

Linezolid-reversible non-selective MOA

Question 18

Oxazolidinones resolution rank in antibiotic therapy?

Answer 18

Last resort where every other therapy has failed-Should be reserved for only that purpose

Question 19

Oxazolidinones MOA(2)?

Answer 19

1. Prevents formation of ribosome complex
2. Binds to 235 ribosmal RNA of the 50s ribosomal subunit

Question 20

Oxazolidinones admin & bioavailability ?

Answer 20

IV/Oral(100% bioavailability)

Question 21

Oxazolidinones resistance?

Answer 21

-Mutation of linezolid binding site on 235 ribosomal RNA

Question 22

Oxazolidinones S/E?

Answer 22

1. Moniliasis/Fungal infection
2. Metallic taste
3. Peripheral neuropathy & neurotoxicity
4. Haemolytic toxicty

Question 23

Oxazolidinones DI?

Answer 23

SNS agonist or adrenergic drugs can cause serotonin syndrome

Question 24

Streptogramins & CYP450?

Answer 24

CYP450 Inhibitor

Question 25

Streptogramins composition/ratio?

Answer 25

Quinupristin-Dalfopristin (Fixed 30/70 combination)

Question 26

Streptogramins derivative?

Answer 26

Semi-synthetic derivatives of pristinamycin

Question 27

Streptogramins classes?

Answer 27

Macrolide/ Lincosamide/ Streptogramin class

Question 28

Streptogramins MOA-4?

Answer 28

1. Two components are structurally unrelated 2. Bind to distinict sites on the 50S ribsomal subunit 3.Interfere with peptidyl transferase enzyme action 4.They cooperate to inhibit protein synthesis

Question 29

Streptogramins admin?

Answer 29

IV administration

Question 30

Streptogramins S/E?

Answer 30

1. Arthralgia 2. Myalgia 3. Conj Hyperbilirubinaemia 4. Asthenia Inflammation 5. Oedema, Thrombophlebitis-Via Peripheral Vein 6

Question 31

Streptogramins resistance-2?

Answer 31

1. Quinupristin -A ribosomal methylase that prevents bindIng -Lactonases produced that inactiavte the drug 2. Dalfopristin - Acetyltransferases produced that inactivate the drug -Increased efflux

Question 32

Streptogramins resistance-2?

Answer 32

1. Quinupristin -A ribosomal methylase that prevents bindIng -Lactonases produced that inactiavte the drug 2. Dalfopristin - Acetyltransferases produced that inactivate the drug -Increased efflux

Question 33

Lipopeptides type of drug & bacteria

Answer 33

Daptomycin(IV) Bactericidal

Question 34

Lipopeptides MOA?

Answer 34

1. Inhibition of protein, DNA & RNA synthesis 2. Disrupts bacterial cell membrane function 3. Binds to the membrane and cause rapid depolarisation 4. Cause a loss of membrane potential

Question 35

Lipopeptides S/E-7?

Answer 35

1. Myopathy & Rhabdomyolsis (with statins) 2. Acute renal failure 3. Dyspnea 4. Electrolyte disturbances 5. CVS & CNS effects 6.Haematological effects 7. Hepatic effects 8. Musculoskeletal effects

Question 36

Disruption of bacterial plasma membrane?

Answer 36

Polymyxin B & E(colistin)- positive charged peptides

Question 37

Disruption of bacterial plasma MOA?

Answer 37

1. Attach to phospholipids in bacterial plasma membrane-disrupt 2. Change membrane permeability

Question 38

Disruption of bacterial plasma membrane S/E?

Answer 38

1. Nephrotoxic 2. Neurotoxic

Question 39

Polymyxin E(Colistin) Admin

Answer 39

-IV -Unlicenced

Question 40

Polymyxin E(Colistin) I?

Answer 40

-Severe resistant gram -ve infections (Carbapenems resistant) -Last line treatment for multi-drug resistant infections

Question 41

Polymyxin E(Colistin) S/E?

Answer 41

Nephrotoxicity (Reversible)