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Clinical pharmacy PharmD program                     Third level                          Phytochemistry-1 (PG-504)





              2. Amikacin



              Amikacin is made semi-synthetically from kanamycin.


              •  Hydroxyaminobutyl  (HABA)  moiety  strongly  enhanced  the  potency  and

                spectrum,

              •  So amikacin is used competitively with gentamicin for the treatment of sensitive

                strains  of  mycobacterium  tuberculosis  and  severe  Pseudomonas  aeruginosa

                infections resistant to other drugs.

                 •  No oral form available as amikacin is not absorbed orally.

                 •  In people with kidney  failure, dosage  must be reduced according to the


                     creatinine clearance.
              II.  Having  carbohydrate  as  small  part  of  the  molecule  but  is  essential:


                      Macrolide antibiotics: (e.g: Erythromycins)


                 •  According to the ring size of the aglycone, the macrolide antibiotics are

                     classified as either 12-, 14-, or 16-membered ring macrolides.

                 •  10 – 16 ring members are very strongly antibacterial

                 •  16 – 40 ring members show very little activity against bacteria, often none

                     at all, but they are highly effective against fungi, yeasts, etc.

                 •  The very large macrolides are highly effective against fungi and viruses.

                 Till now, more than 90 macrolides have been discovered. The change in the


                 antibiotic activity spectrum is due to:


                 o  Changes in the ring size

                 o  The substituents

                 o  The degree of unsaturation.

                 14-Membered Ring Macrolides: Erythromycins


              Erythromycins A, B, C and D are produced by Streptomyces erythreus.

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