Page 108 - MNU-PM502- Pharmaeutical Microbiology Theoritical Book
P. 108

Pharm D- Clinical Pharmacy Program        Third Level          Pharmaceutical Microbiology& Antimicrobials (PM 502)


                                                Cell membrane inhibitors



                   Glycopeptides: Daptomycin

                   Spectrum:
                       •  active against Gram-positive including highly resistant strains such as
                          MRSA
                       •   NOT active against Gram-negative pathogen                          G+ve bacteria

                    ➢  Used in the treatment of systemic and life-threatening infections (S. aureus
                       bacteremia, S. aureus endocarditis)

                   ➢  Has poor activity in the lungs and should not be used to treat
                       pneumonia.

                   Polymyxins: Colistin

                   Colistin is known as polymyxin E

                       •  a cationic cyclic decapeptide with a fatty acid side chain



                   Mechanism: Altering membrane permeability

                       •  The positive charge allows colistin to
                          bind  to  the  negatively  charged

                          lipopolysaccharide  molecules  in  the
                          bacterial  outer  membrane,  displacing
                             +2
                                           +2
                          Ca   and  Mg   ions  that  normally
                          stabilize these lipids.

                       •  The  fatty  acid  tail  facilitates  further
                          insertion  of  colistin  into  the  outer

                          membrane  leading  to  increased
                          permeability and, eventually, lysis of
                          the bacterium







                                                               95
   103   104   105   106   107   108   109   110   111   112   113