Protein Synthesis Inhibitors II Flashcards
Fusidic acid
- Type of antibiotic
- MOA
- Admin + Adjunct
4.Indications
- Steriod antibiotic
- Similar to macrolides(50s) -inhibts translocation
- Taken with food(orally) and topically-acute skin infections(5days) and conjunctive
- Severe staphylococcal infections
Min days for topical admin for fusidic acid
5 days
Fusidic acid S/E and extra info-4?
- Hepatotoxicity (Reversible)
- Kernicterus
- GIT effects(take with meals)
- IM-Local tissue necrosis
Fusidic acid DI?
- Hydrocortisone (Decreased antibiotic activity of fuisdic acid)
- Statins (Increased risk of rhabdomyolysis)
Fusidic acid CI?
Hepatic dysfunction & pregnancy
Mupirocin 3 MOA?
Inhibits:
- Protein synthesis
- DNA & RNA synthesis
- Cell wall synthesis
Mupirocin
- Bacteria MOA
- Admin
- Type of bacteria
- Bactericidal
- Topical only(no systemic absorption)
- Gram +ve bacteria
Mupirocin preparations?
Preparations contain polyethylene glycol=may lead to toxicity
Mupirocin and Methicillin bacteria?
Methicillin-resistant staph aureus
Mupirocin S/E?
-Burning
-Mild stinging
-Itching at site of application
Mupirocin caution?
Porphyria
Ketolides CYP450?
CYP450 Inhibitors
Ketolides MOA?
-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
Ketolides derivative?
Semi-synthetic derivatives of Erthromycin A-Telithromycin
Ketolides dosage frequency and max days of admin?
Once daily dosage(5 days)
Ketolides S/E-4?
- Respiratory failure (Myasthenia gravis patients)
- Hepatotoxicity
- Visual disturbances
- Loss of consciousness
Oxazolidinones type of antibiotic?
Linezolid-reversible non-selective MOA
Oxazolidinones resolution rank in antibiotic therapy?
Last resort where every other therapy has failed-Should be reserved for only that purpose
Oxazolidinones MOA(2)?
- Prevents formation of ribosome complex
- Binds to 235 ribosmal RNA of the 50s ribosomal subunit
Oxazolidinones admin & bioavailability ?
IV/Oral(100% bioavailability)
Oxazolidinones resistance?
-Mutation of linezolid binding site on 235 ribosomal RNA
Oxazolidinones S/E?
- Moniliasis/Fungal infection
- Metallic taste
- Peripheral neuropathy & neurotoxicity
- Haemolytic toxicty
Oxazolidinones DI?
SNS agonist or adrenergic drugs can cause serotonin syndrome
Streptogramins & CYP450?
CYP450 Inhibitor
Streptogramins composition/ratio?
Quinupristin-Dalfopristin
(Fixed 30/70 combination)
Streptogramins derivative?
Semi-synthetic derivatives of pristinamycin
Streptogramins classes?
Macrolide/ Lincosamide/ Streptogramin class
Streptogramins MOA-4?
- Two components are structurally unrelated
- Bind to distinict sites on the 50S ribsomal subunit
3.Interfere with peptidyl transferase enzyme action
4.They cooperate to inhibit protein synthesis
Streptogramins admin?
IV administration
Streptogramins S/E?
- Arthralgia
- Myalgia
- Conj Hyperbilirubinaemia
- Asthenia
Inflammation - Oedema, Thrombophlebitis-Via Peripheral Vein
6
Streptogramins resistance-2?
- Quinupristin
-A ribosomal methylase that prevents bindIng
-Lactonases produced that inactiavte the drug - Dalfopristin
- Acetyltransferases
produced that
inactivate the drug
-Increased efflux
Streptogramins resistance-2?
- Quinupristin
-A ribosomal methylase that prevents bindIng
-Lactonases produced that inactiavte the drug - Dalfopristin
- Acetyltransferases
produced that
inactivate the drug
-Increased efflux
Lipopeptides type of drug & bacteria
Daptomycin(IV)
Bactericidal
Lipopeptides MOA?
- Inhibition of protein, DNA & RNA synthesis
- Disrupts bacterial cell membrane function
- Binds to the membrane and cause rapid depolarisation
- Cause a loss of membrane potential
Lipopeptides S/E-7?
- Myopathy & Rhabdomyolsis (with statins)
- Acute renal failure
- Dyspnea
- Electrolyte disturbances
- CVS & CNS effects
6.Haematological effects
- Hepatic effects
- Musculoskeletal effects
Disruption of bacterial plasma membrane?
Polymyxin B & E(colistin)- positive charged peptides
Disruption of bacterial plasma MOA?
- Attach to phospholipids in bacterial plasma membrane-disrupt
- Change membrane permeability
Disruption of bacterial plasma membrane S/E?
- Nephrotoxic
- Neurotoxic
Polymyxin E(Colistin) Admin
-IV
-Unlicenced
Polymyxin E(Colistin) I?
-Severe resistant gram -ve infections (Carbapenems resistant)
-Last line treatment for multi-drug resistant infections
Polymyxin E(Colistin) S/E?
Nephrotoxicity
(Reversible)