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8/6/2012




                                    By- Jitendra Bhangale
                                  Assistant Professor & Head,
                                 Department of Pharmacology,
                              Smt N. M. Padalia Pharmacy College,
                                          Ahmedabad
                                                                                     1
                             © 2010 Delmar, Cengage Learning




                               By Jitendra Bhangale
Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad2
                            © 2010 Smt N. M. Padalia




                                                                                                1
8/6/2012




        It was originally obtained from the soil actinomycetes.


                                By Jitendra Bhangale
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad3
                             © 2010 Smt N. M. Padalia




Oxytetracycline                is   a     natural    product        elaborated      by
        Streptomyces rimosus.
Tetracycline              is        a      semisynthetic          derivative         of
        chlortetracycline.
Demeclocycline is the product of a mutant strain of Strep.
        aureofaciens
Methacycline,             doxycycline,         and     minocycline          all    are
        semisynthetic derivatives.
The     Tetracyclines               are    close     congeners       of    polycyclic
        naphthacenecarboxamide.
Many     others    like        Chlortetracycline,   Methacycline,     Rolitetracycline,
        Lymecycline are no longer commercially available
                                By Jitendra Bhangale
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad4
                             © 2010 Smt N. M. Padalia




                                                                                                 2
8/6/2012




                                              The peptidyl tRNA at the
                                              donor site donates the growing
                                              peptide chain to the aminoacyl
                                              tRNA at the acceptor site in a
                                              reaction catalyzed by peptidyl
                                              transferase.

                                              The tRNA, discharged of its
                                              peptide, is released from the
                                              donor site to make way for
                                              translocation of the newly
                                              formed peptidyl tRNA.

                                              The acceptor site is then free
                                              to be occupied by the next
                                              "charged" aminoacyl tRNA.

                                 By Jitendra Bhangale
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad5
                              © 2010 Smt N. M. Padalia




The tetracyclines are primarily
bacteriostatic;      inhibit    protein
synthesis by binding to 30S
ribosomes         in       susceptible
organism.

Inhibit     aminoaceyl            tRNA
attachment to A site

As a result the peptide chain
fails to grow.

                                 By Jitendra Bhangale
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad6
                              © 2010 Smt N. M. Padalia




                                                                                                  3
8/6/2012




It is a broad spectrum antibiotic that active against many gram-
positive and gram-negative bacteria


    Cocci                                      Gram-negative bacilli
                                                     H. ducreyi,
        N. gonorrhoea                                Calymmatobacterium
        N. Meningitidis                              Granulomatis
    Gram-positive bacilli                           V. cholerae,
        Clostridia                                   Yersinia pestis,
                                                     Y. enterocolitica
        Listeria,                                    Campylobacter,
        Corynebacterta,                              Helicobacter pylori,
        Propionibacterium acnes                      Brucella,
        B. Anthracis                                 F. tularensis

                                 By Jitendra Bhangale
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad7
                              © 2010 Smt N. M. Padalia




Spirochetes, including T. pallidum and Borreha are ouite
         sensitive.

All rickettsiae (typhus, etc.) and chlamydiae are highly sensitive.

Mycoplasma and Actinomyces are moderately sensitive.

Entamoeba histolytica and Plasmodia are inhibited at high
         concentrations.

Resistance microorganisms

Notable      bacilli    that     are    not     inhibited      are    Pseudomonas
         aeruginosa, Proteus, Klebsiella, Salmonella typhi and many
         Bact. fragilis.
                                 By Jitendra Bhangale
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad8
                              © 2010 Smt N. M. Padalia




                                                                                                  4
8/6/2012




Absorption:-
         Absorption after oral administration is approximately
         30% for chlortetracycline;
         60–70% for tetracycline, oxytetracycline, demeclocycline,
                   and methacycline;
         95–100% for doxycycline and minocycline.
Absorption occurs mainly in the upper small intestine and is
         impaired by food (except doxycycline and minocycline); by
         divalent cations (Ca2+, Mg2+, Fe2+) or Al3+; by dairy
         products and antacids, which contain multivalent cations;
         and by alkaline pH.
                                 By Jitendra Bhangale
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad9
                              © 2010 Smt N. M. Padalia




Distribution:- Tetracyclines are widely distributed in the body.
Excretion:- Most tetracyclines are primarily excreted in urine by
         glomerular filtration.
Tetracyclines are classified as
1. Short-acting (chlortetracycline, tetracycline, oxytetracycline)
                            serum half-lives of 6–8 hours
2. Intermediate-acting (demeclocycline and methacycline)
                            serum half-lives of 12 hours
3. Long-acting (doxycycline and minocycline)
                            serum half-lives 16–18 hours

                                 By Jitendra Bhangale
                                                                                       10
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                  5
8/6/2012




Hypersensitivity reactions (drug fever, skin rashes)
Gastrointestinal effects:- Nausea, vomiting, and                   diarrhoea
Bony Structures and Teeth
Liver Toxicity
Kidney Toxicity
Local Tissue Toxicity
Photosensitization
         Systemic      tetracycline    administration,     especially                  of
         demeclocycline, can induce sensitivity to sunlight                            or
         ultraviolet light, particularly in fair-skinned persons.
Vestibular Reactions:- Dizziness, vertigo, nausea, and vomiting
        have been particularly noted with doxycycline at doses above
        100 mg.
                                By Jitendra Bhangale
                                                                                      11
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                 By Jitendra Bhangale
                                                                                       12
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                  6
8/6/2012




It was originally obtained from the Streptomyces venezuelae 1947.


                               By Jitendra Bhangale
                                                                                     13
Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                            © 2010 Smt N. M. Padalia




                                            The peptidyl tRNA at the
                                            donor site donates the growing
                                            peptide chain to the aminoacyl
                                            tRNA at the acceptor site in a
                                            reaction catalyzed by peptidyl
                                            transferase.

                                            The tRNA, discharged of its
                                            peptide, is released from the
                                            donor site to make way for
                                            translocation of the newly
                                            formed peptidyl tRNA.

                                            The acceptor site is then free
                                            to be occupied by the next
                                            "charged" aminoacyl tRNA.

                               By Jitendra Bhangale
                                                                                     14
Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                            © 2010 Smt N. M. Padalia




                                                                                                7
8/6/2012




Chloramphenicol binds to the
50S ribosomal subunit at the
peptidyltransferase site and
inhibits the transpeptidation
reaction.

Chloramphenicol binds to the
50S ribosomal subunit near the
site of action of clindamycin
and the macrolide antibiotics.

These agents interfere with
the binding of chloramphenicol
and thus may interfere with
each other's actions if given
concurrently.

                                 By Jitendra Bhangale
                                                                                       15
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




It is a broad spectrum antibiotic that active against many gram-
positive and gram-negative bacteria




    H. influenzae,                                  Salmonella typhi
    Neisseria meningitidis,
                                                     Escherichia coli
    S. pneumoniae
                                                     Klebsiella pneumoniae
    Enterobacteriaceae
                                                     Proteus mirabilis
    V. cholerae


                                 By Jitendra Bhangale
                                                                                       16
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                  8
8/6/2012




Resistance mechanism

Resistance to chloramphenicol usually is caused by a plasmid-

        encoded acetyltransferase that inactivates the drug.

Acetylated derivatives of chloramphenicol fail to bind to bacterial

        ribosomes.




                                By Jitendra Bhangale
                                                                                      17
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




Absorption:-

        Chloramphenicol             is     absorbed          rapidly     from      the

                  gastrointestinal tract.

        Chloramphenicol succinate in plasma are achieved after

                  intravenous and intramuscular administration.

        Chloramphenicol             palmitate       is   a     prodrug      that     is

                  hydrolyzed        in     the     intestine       to    yield      free

                  chloramphenicol.

                                By Jitendra Bhangale
                                                                                      18
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                                                                                 9
8/6/2012




Distribution:- Chloramphenicol is widely distributed in the

                           body.

Excretion:- Chloramphenicol is primarily excreted in urine by

                  glomerular filtration.




                                By Jitendra Bhangale
                                                                                      19
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




             Typhoid Fever


             Bacterial Meningitis


             Anaerobic Infections


             Rickettsial Diseases


             Brucellosis



                                By Jitendra Bhangale
                                                                                      20
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                                                                                10
8/6/2012




Hypersensitivity reactions (drug fever, skin rashes)

Bone marrow depression

Vestibular Reactions:- Dizziness, vertigo, nausea, and vomiting

Gray baby syndrome: - The baby stopped feeding, vomited,
        became hypotonic and hypothermic, abdomen distended,
        respiration became irregular; an ashen gray cyanosis
        developed in many, followed by cardiovascular collapse and
        death.

Blood lactic acid was raised

                                By Jitendra Bhangale
                                                                                      21
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                By Jitendra Bhangale
                                                                                      22
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                                                                                11
8/6/2012




                                               Macrolide antibiotics contain a
                                               many-membered lactone ring
                                               (14-membered              rings        for
                                               erythromycin & clarithromycin
                                               and a 15-membered ring for
                                               azithromycin)
                                               to which are attached one or
                                               more deoxy sugars.



                                By Jitendra Bhangale
                                                                                      23
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




Narrow spectrum

        Erythromycin (Streptomyces erythreus)

Broad spectrum

        Clarithromycin,

        Roxithromycin

        Azithromycin             are      semisynthetic           derivatives         of

        erythromycin


                                By Jitendra Bhangale
                                                                                      24
 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                             © 2010 Smt N. M. Padalia




                                                                                                 12
8/6/2012




                                              The peptidyl tRNA at the
                                              donor site donates the growing
                                              peptide chain to the aminoacyl
                                              tRNA at the acceptor site in a
                                              reaction catalyzed by peptidyl
                                              transferase.

                                              The tRNA, discharged of its
                                              peptide, is released from the
                                              donor site to make way for
                                              translocation of the newly
                                              formed peptidyl tRNA.

                                              The acceptor site is then free
                                              to be occupied by the next
                                              "charged" aminoacyl tRNA.

                                 By Jitendra Bhangale
                                                                                       25
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




Macrolide       antibiotics     are
bacteriostatic agents that inhibit
protein   synthesis    by    binding
reversibly to the 50S ribosomal
subunits of sensitive organisms.
Erythromycin appears to inhibit
the translocation step wherein the
nascent peptide chain temporarily
residing at the A site of the
transferase reaction fails to move to
the P, or donor, site.
Alternatively, macrolides may
bind and cause a conformational
change that terminates protein
synthesis by indirectly interfering
with      transpeptidation     and
translocation.
                                 By Jitendra Bhangale
                                                                                       26
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                 13
8/6/2012




It is a broad spectrum antibiotic that active against many gram-
positive and gram-negative bacteria


Gram-positive organisms                        Listeria
Pneumococci
Streptococci                                   Mycobacterium kansasii
Staphylococci
Corynebacteria                                 Mycobacterium scrofulaceum
Mycoplasma
Legionella                                     Bordetella pertussis
Chlamydia trachomatis
C psittaci                                     Bartonella henselae
C pneumoniae
Helicobacter                                   B quintana
                                 By Jitendra Bhangale
                                                                                       27
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




Absorption:-

Erythromycin base is destroyed by stomach acid and must be

         administered with enteric coating.

Food interferes with absorption. Stearates and esters are fairly

         acid-resistant and somewhat better absorbed.

Distribution:- Erythromycin are widely distributed in the body.

Excretion:- Erythromycin are primarily excreted in urine.


                                 By Jitendra Bhangale
                                                                                       28
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                 14
8/6/2012




Hypersensitivity reactions (drug fever, skin rashes)


Gastrointestinal effects:- Nausea, vomiting, and                   diarrhoea


Hepatitis with cholestatic jaundice




                                 By Jitendra Bhangale
                                                                                       29
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




Mycoplasma             pneumoniae
                                               Staphylococcal Infections
         Infections
                                               Campylobacter Infections
Legionnaires' Disease
                                               Helicobacter pylori Infection
Chlamydial Infections
                                               Tetanus
Diphtheria
                                               Syphilis
Pertussis
                                               Mycobacterial Infections
Streptococcal Infections


                                 By Jitendra Bhangale
                                                                                       30
  Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                              © 2010 Smt N. M. Padalia




                                                                                                 15
8/6/2012




                               By Jitendra Bhangale
                                                                                     31
Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
                            © 2010 Smt N. M. Padalia




                                                                                               16

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Protein synthesis inhibitors

  • 1. 8/6/2012 By- Jitendra Bhangale Assistant Professor & Head, Department of Pharmacology, Smt N. M. Padalia Pharmacy College, Ahmedabad 1 © 2010 Delmar, Cengage Learning By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad2 © 2010 Smt N. M. Padalia 1
  • 2. 8/6/2012 It was originally obtained from the soil actinomycetes. By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad3 © 2010 Smt N. M. Padalia Oxytetracycline is a natural product elaborated by Streptomyces rimosus. Tetracycline is a semisynthetic derivative of chlortetracycline. Demeclocycline is the product of a mutant strain of Strep. aureofaciens Methacycline, doxycycline, and minocycline all are semisynthetic derivatives. The Tetracyclines are close congeners of polycyclic naphthacenecarboxamide. Many others like Chlortetracycline, Methacycline, Rolitetracycline, Lymecycline are no longer commercially available By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad4 © 2010 Smt N. M. Padalia 2
  • 3. 8/6/2012 The peptidyl tRNA at the donor site donates the growing peptide chain to the aminoacyl tRNA at the acceptor site in a reaction catalyzed by peptidyl transferase. The tRNA, discharged of its peptide, is released from the donor site to make way for translocation of the newly formed peptidyl tRNA. The acceptor site is then free to be occupied by the next "charged" aminoacyl tRNA. By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad5 © 2010 Smt N. M. Padalia The tetracyclines are primarily bacteriostatic; inhibit protein synthesis by binding to 30S ribosomes in susceptible organism. Inhibit aminoaceyl tRNA attachment to A site As a result the peptide chain fails to grow. By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad6 © 2010 Smt N. M. Padalia 3
  • 4. 8/6/2012 It is a broad spectrum antibiotic that active against many gram- positive and gram-negative bacteria Cocci Gram-negative bacilli H. ducreyi, N. gonorrhoea Calymmatobacterium N. Meningitidis Granulomatis Gram-positive bacilli V. cholerae, Clostridia Yersinia pestis, Y. enterocolitica Listeria, Campylobacter, Corynebacterta, Helicobacter pylori, Propionibacterium acnes Brucella, B. Anthracis F. tularensis By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad7 © 2010 Smt N. M. Padalia Spirochetes, including T. pallidum and Borreha are ouite sensitive. All rickettsiae (typhus, etc.) and chlamydiae are highly sensitive. Mycoplasma and Actinomyces are moderately sensitive. Entamoeba histolytica and Plasmodia are inhibited at high concentrations. Resistance microorganisms Notable bacilli that are not inhibited are Pseudomonas aeruginosa, Proteus, Klebsiella, Salmonella typhi and many Bact. fragilis. By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad8 © 2010 Smt N. M. Padalia 4
  • 5. 8/6/2012 Absorption:- Absorption after oral administration is approximately 30% for chlortetracycline; 60–70% for tetracycline, oxytetracycline, demeclocycline, and methacycline; 95–100% for doxycycline and minocycline. Absorption occurs mainly in the upper small intestine and is impaired by food (except doxycycline and minocycline); by divalent cations (Ca2+, Mg2+, Fe2+) or Al3+; by dairy products and antacids, which contain multivalent cations; and by alkaline pH. By Jitendra Bhangale Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad9 © 2010 Smt N. M. Padalia Distribution:- Tetracyclines are widely distributed in the body. Excretion:- Most tetracyclines are primarily excreted in urine by glomerular filtration. Tetracyclines are classified as 1. Short-acting (chlortetracycline, tetracycline, oxytetracycline) serum half-lives of 6–8 hours 2. Intermediate-acting (demeclocycline and methacycline) serum half-lives of 12 hours 3. Long-acting (doxycycline and minocycline) serum half-lives 16–18 hours By Jitendra Bhangale 10 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 5
  • 6. 8/6/2012 Hypersensitivity reactions (drug fever, skin rashes) Gastrointestinal effects:- Nausea, vomiting, and diarrhoea Bony Structures and Teeth Liver Toxicity Kidney Toxicity Local Tissue Toxicity Photosensitization Systemic tetracycline administration, especially of demeclocycline, can induce sensitivity to sunlight or ultraviolet light, particularly in fair-skinned persons. Vestibular Reactions:- Dizziness, vertigo, nausea, and vomiting have been particularly noted with doxycycline at doses above 100 mg. By Jitendra Bhangale 11 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia By Jitendra Bhangale 12 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 6
  • 7. 8/6/2012 It was originally obtained from the Streptomyces venezuelae 1947. By Jitendra Bhangale 13 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia The peptidyl tRNA at the donor site donates the growing peptide chain to the aminoacyl tRNA at the acceptor site in a reaction catalyzed by peptidyl transferase. The tRNA, discharged of its peptide, is released from the donor site to make way for translocation of the newly formed peptidyl tRNA. The acceptor site is then free to be occupied by the next "charged" aminoacyl tRNA. By Jitendra Bhangale 14 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 7
  • 8. 8/6/2012 Chloramphenicol binds to the 50S ribosomal subunit at the peptidyltransferase site and inhibits the transpeptidation reaction. Chloramphenicol binds to the 50S ribosomal subunit near the site of action of clindamycin and the macrolide antibiotics. These agents interfere with the binding of chloramphenicol and thus may interfere with each other's actions if given concurrently. By Jitendra Bhangale 15 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia It is a broad spectrum antibiotic that active against many gram- positive and gram-negative bacteria H. influenzae, Salmonella typhi Neisseria meningitidis, Escherichia coli S. pneumoniae Klebsiella pneumoniae Enterobacteriaceae Proteus mirabilis V. cholerae By Jitendra Bhangale 16 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 8
  • 9. 8/6/2012 Resistance mechanism Resistance to chloramphenicol usually is caused by a plasmid- encoded acetyltransferase that inactivates the drug. Acetylated derivatives of chloramphenicol fail to bind to bacterial ribosomes. By Jitendra Bhangale 17 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Absorption:- Chloramphenicol is absorbed rapidly from the gastrointestinal tract. Chloramphenicol succinate in plasma are achieved after intravenous and intramuscular administration. Chloramphenicol palmitate is a prodrug that is hydrolyzed in the intestine to yield free chloramphenicol. By Jitendra Bhangale 18 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 9
  • 10. 8/6/2012 Distribution:- Chloramphenicol is widely distributed in the body. Excretion:- Chloramphenicol is primarily excreted in urine by glomerular filtration. By Jitendra Bhangale 19 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Typhoid Fever Bacterial Meningitis Anaerobic Infections Rickettsial Diseases Brucellosis By Jitendra Bhangale 20 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 10
  • 11. 8/6/2012 Hypersensitivity reactions (drug fever, skin rashes) Bone marrow depression Vestibular Reactions:- Dizziness, vertigo, nausea, and vomiting Gray baby syndrome: - The baby stopped feeding, vomited, became hypotonic and hypothermic, abdomen distended, respiration became irregular; an ashen gray cyanosis developed in many, followed by cardiovascular collapse and death. Blood lactic acid was raised By Jitendra Bhangale 21 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia By Jitendra Bhangale 22 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 11
  • 12. 8/6/2012 Macrolide antibiotics contain a many-membered lactone ring (14-membered rings for erythromycin & clarithromycin and a 15-membered ring for azithromycin) to which are attached one or more deoxy sugars. By Jitendra Bhangale 23 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Narrow spectrum Erythromycin (Streptomyces erythreus) Broad spectrum Clarithromycin, Roxithromycin Azithromycin are semisynthetic derivatives of erythromycin By Jitendra Bhangale 24 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 12
  • 13. 8/6/2012 The peptidyl tRNA at the donor site donates the growing peptide chain to the aminoacyl tRNA at the acceptor site in a reaction catalyzed by peptidyl transferase. The tRNA, discharged of its peptide, is released from the donor site to make way for translocation of the newly formed peptidyl tRNA. The acceptor site is then free to be occupied by the next "charged" aminoacyl tRNA. By Jitendra Bhangale 25 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Macrolide antibiotics are bacteriostatic agents that inhibit protein synthesis by binding reversibly to the 50S ribosomal subunits of sensitive organisms. Erythromycin appears to inhibit the translocation step wherein the nascent peptide chain temporarily residing at the A site of the transferase reaction fails to move to the P, or donor, site. Alternatively, macrolides may bind and cause a conformational change that terminates protein synthesis by indirectly interfering with transpeptidation and translocation. By Jitendra Bhangale 26 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 13
  • 14. 8/6/2012 It is a broad spectrum antibiotic that active against many gram- positive and gram-negative bacteria Gram-positive organisms Listeria Pneumococci Streptococci Mycobacterium kansasii Staphylococci Corynebacteria Mycobacterium scrofulaceum Mycoplasma Legionella Bordetella pertussis Chlamydia trachomatis C psittaci Bartonella henselae C pneumoniae Helicobacter B quintana By Jitendra Bhangale 27 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Absorption:- Erythromycin base is destroyed by stomach acid and must be administered with enteric coating. Food interferes with absorption. Stearates and esters are fairly acid-resistant and somewhat better absorbed. Distribution:- Erythromycin are widely distributed in the body. Excretion:- Erythromycin are primarily excreted in urine. By Jitendra Bhangale 28 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 14
  • 15. 8/6/2012 Hypersensitivity reactions (drug fever, skin rashes) Gastrointestinal effects:- Nausea, vomiting, and diarrhoea Hepatitis with cholestatic jaundice By Jitendra Bhangale 29 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia Mycoplasma pneumoniae Staphylococcal Infections Infections Campylobacter Infections Legionnaires' Disease Helicobacter pylori Infection Chlamydial Infections Tetanus Diphtheria Syphilis Pertussis Mycobacterial Infections Streptococcal Infections By Jitendra Bhangale 30 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 15
  • 16. 8/6/2012 By Jitendra Bhangale 31 Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad © 2010 Smt N. M. Padalia 16