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    Antimicrobial Chemotherapy I

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    nighat khan
    Antibiotics are chemical agents that kill or inhibit the growth of microorganisms. They work in several ways such as inhibiting cell wall synthesis, damaging cell membranes, or preventing protein synthesis. Some antibiotics are bacteriostatic and inhibit cell replication while others are bactericidal and cause cell death. Antibiotics are classified based on their structure and mechanisms of action. Examples of important classes include penicillins, cephalosporins, carbapenems, aminoglycosides, sulphonamides, and tetracyclines. Antimalarial drugs also work by inhibiting essential metabolic pathways in plasmodium parasites.

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    Antimicrobial Chemotherapy I

    Uploaded by

    nighat khan
    31 views30 pages
    Antibiotics are chemical agents that kill or inhibit the growth of microorganisms. They work in several ways such as inhibiting cell wall synthesis, damaging cell membranes, or preventing protein synthesis. Some antibiotics are bacteriostatic and inhibit cell replication while others are bactericidal and cause cell death. Antibiotics are classified based on their structure and mechanisms of action. Examples of important classes include penicillins, cephalosporins, carbapenems, aminoglycosides, sulphonamides, and tetracyclines. Antimalarial drugs also work by inhibiting essential metabolic pathways in plasmodium parasites.

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    ANTIMICROBIAL CHEMOTHERAPY I

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    Antibiotics are chemical agents that kill or inhibit the growth of microorganisms. They work in several ways such as inhibiting cell wall synthesis, damaging cell membranes, or preventing protein synthesis. Some antibiotics are bacteriostatic and inhibit cell replication while others are bactericidal and cause cell death. Antibiotics are classified based on their structure and mechanisms of action. Examples of important classes include penicillins, cephalosporins, carbapenems, aminoglycosides, sulphonamides, and tetracyclines. Antimalarial drugs also work by inhibiting essential metabolic pathways in plasmodium parasites.

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    Download as pptx, pdf, or txt
    31 views30 pages

    Antimicrobial Chemotherapy I

    Uploaded by

    nighat khan
    Antibiotics are chemical agents that kill or inhibit the growth of microorganisms. They work in several ways such as inhibiting cell wall synthesis, damaging cell membranes, or preventing protein synthesis. Some antibiotics are bacteriostatic and inhibit cell replication while others are bactericidal and cause cell death. Antibiotics are classified based on their structure and mechanisms of action. Examples of important classes include penicillins, cephalosporins, carbapenems, aminoglycosides, sulphonamides, and tetracyclines. Antimalarial drugs also work by inhibiting essential metabolic pathways in plasmodium parasites.

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    of 30

    A L I

    B I Y
    O
    R RA P
    C
    I E
    T IM T H
    N
    A EM O
    CH
    D
    M
    ,
    O
    R
    O
    B
    G
    E
    D
    A
    Z
    A
    O
    B
    DEFINITION OF TERMS
    • Antibiosis: The killing action of one living organism by
    another organism.
    • Antibiotic: Was initially used to describe any organism
    that was able to kill other microorganisms.
    •Today it is used to describe any chemical agent that could
    kill microorganisms. Most antibiotics are now synthesized
    or modified from other antobiotics.
    THE WAY ANTIBIOTICS ACT
    1. Inhibition of cell wall synthesis e.g. penicillin, bacitracin, vancomycin and the
    cephalosporins.
    2. Damage cell membrane permeability e.g colistin, nystatin, chlorhexidine,
    savlon, polymyxins, and amphotericin.
    3. Prevent proper translation of the genetic code and inhibit formation of
    proteins (inhibitions of protein synthesis) act on messenger RNA: ofloxacin,
    ciprofloxacin (Quinolones), erythromycin and chloramphenicol.
    The aminoglycosides such as gentamicin, streptomycin, clindamycin,
    oleandomycin, kanamyun, neomycin and clindeparomycin, also belongs to
    this group.
    4. Inhibit essential metabolites (antimetabolities) e.g. sulphonamides, sulphones,
    PAS (Para aminosalicylic acid) trimethoprim, pyrimethamine and prognanil.
    USE OF ANTIBIOTICS

    a. Prophylactic - e.g Flagyl in abdominal surgery, bacitracin on skin


    after surgery, neomycin and penicillin to prevent endocarditis in
    rheumatic fever patients and people going for tooth extraction.
    b. Therapeutic: For treating infections.
    BACTERIOSTATIC DRUGS

    - Inhibit cell replication.


    - If withdrawn, cell will begin to grow
    again.
    Examples: Sulphonamides
    Chloramphenicol
    Erythromycin
    BACTERICIDAL DRUGS

    - Cause cell death and lysis. If withdrawn, cells


    cannot grow.
    Examples: Penicillin
    Streptomycin
     
    BACTERIOSTATIC AND BACTERICIDAL
    EFFECTS OF ANTIBIOTICS
    CLASSIFICATION OF ANTIBIOTICS
    1. Antimetabolites
    - Sulphonamides: Sulphadimidine, Sulphathiazole, etc
    - pyrimethamine
    - Sulphones
    - trimethoprim
    - PAS- para-amino salicylic acid
    - Proguanil
    2. Inhibitors of cell wall synthesis
    -The penicillins and the cephalosporins act at same points (carboxypeptidase, transpeptidase)
    - Vancomycin
    - Ristocetin
    - bacitracin
    - cycloserine
    - Cephalosporins, Carbapenems
    CLASSIFICATION OF ANTIBIOTICS (CTD)
     3. Antibiotics that act on cell membrane
    - Colicins
    - Amphotericin
    - Gramicidin
    - Tyrocidin
    - Chlorhexidine
    - Savlon
    - Salicylanamide
    - The polymyxins
    - The Colistins
    - Nystatin
    CLASSIFICATION OF ANTIBIOTICS (CTD)
    4. Antibiotics affecting Ribosome function
    Chloramphenicol
    Erythromycin
    Oleandomycin
    Carbomycin
    Lincomycin
    Clindamycin
    5. Aminoglycosides- Streptomycin
    - Neomycin
    - Kanamycin
    - Paromomycin
    - Gentamicin
    6. The tetracyclines: Tetracycline, Oxytetracycline, Doxycycline, etc.
    PENICILLINS
    Note that it has only one side chain (R) and a 5-member nucleus
    and a thiazolidine ring
    Mechanism of action
    Inhibits cell wall synthesis leading to osmotic lysis and death. This
    is bactericidal action
    CEPHALOSPORINS
    CORE STRUCTURE OF THE CEPHALOSPORINS
     These differ from the penicillins in which the nucleus is a five-member ring with
    only one side chain (R1).  
    - A group of compounds isolated from fungi. They have the same mechanism of
    action as the penicillins.
    - Also has similar structure with the characteristic β-lactam ring
    FEATURES OF CEPHALOSPORINS

    First generation: cephalothin, cephapirin, cephradine,


    cefazolin
    Second generation: cefamandole, cefuroxime,
    cefoxitin, cefonicid, cefotetan
    Third generation: ceftotaxime, ceftrizoxime,
    ceftriaxone, maxalactam, cefoperazone ceftrazidime.
    CARBAPEMENS
    New highly effective antibiotic agents used for the treatment of severe
    or high-risk bacterial infections.
    It has three side chains,while cephalosporins have two side chains.

    Used for the treatment of serious multidrug resistant Gm-ve and Gm-
    +ve infections
    EXAMPLES
    Imipenem
    Meropenem
    Ertapenem
    Doripenem
    Panipenem/Betamipron
    Biapenem
    Tebipenem
    They differ as to the route of administration, number of daily
    doses required and whether or not they require combination
    therapy with other drugs
    SULPHONAMIDES
     
    - Structural analogs of para-amino-benzoic acid (PABA)
    -To be a true sulphonamide, the structure must be similar to that of PABA, and its
    action must be inhibited by the latter.
    -They block folic acid synthesis. Folic acid is used in the body for the synthesis of:
    a. Amino acids
    Methionine
    Thymine
    hydroxymethyl cytosine
    IUPAC name
    b. Purines
    DNA 4-Aminobenzoic acid

    RNA
    STRUCTURE OF SULPHONAMIDES
    Sulphonamides

    NH2 R1 varies among the sulphonamides.

    R1

    SO2 N

    Sulphonamides R1

    1. Sulphadiazine (most active)


    N Benzene
    group

    2. Sulphathiazole N

    Imidazole
    grp
    N

    \
    3 Sulphopyridine Benzene group

    N
    MODE OF ACTION OF SULPHONAMIDES

    - Arrest cell growth


    - This is done by inhibition of folic acid synthesis
    - Folic acid is required for growth by both mammalian
    and bacterial cells
    - Mammalian cells cannot synthesise it , as it is absorded
    as cofactor
    OTHER SULPHONAMIDES

    PARA AMINO SALICYLIC ACID (PAS) & DAPSONE: used for


    treating Myco. leprae

    TRIMETHOPRIM & CHLORGUANIDE: Are anti-malaria agents


    TETRACYCLINES
    General formula

    Vibramyan (doxycycline) is a long-acting tetracycline


    SIDE CHAINS OF THE TETRACYCLINES
    The tetracylines R1 R2 R3
    Tetracycline H CH3 H
    Chlortetracyline cl CH3 H Aureomycin
    Oxytetracyline H CH3 OH Terromycin
    dimethylchlortetracyline cl H H
    MODE OF ACTION

    A Tetracycline binds A site of the bacterial


    ribosomes
    And so blocks binding of aa + RNA to the
    mRNA – ribosme complex
    Inhibits binding , to the acceptor site ,
    thus terminates protein synthesis by the
    bacteria
    ANTIBIOTICS THAT AFFECT MEMBRANE
    PERMEABILITY
    Colicins A, E, K, Ia, Ib, Q
    Polyene antibiotics: amphotecicin B, nystatin ( treatment
    of fungal infections)
    The polymyxins: polimyxin B, Colistin (Polimyxin E )-
    Treatment of urinary tract and fungal infections
    Monocyclic polypeptides: Gramicidin, Tyrothricin,
    Chlorhexidine Savlon & Salicylanamide – Some of
    them are antiseptics
    CHLORAMPHENICOL

    - Only active on 70s ribosomes - Binds to the 50s


    ribosome
    - Inhibits transpeptidase enzyme function and prevents
    peptide bond formation
    AMINOGLYCOSIDES
    - Structure
    - Polycatinonic compounds composed of aminosugars connected
    by glycosidic linkages
    MODE OF ACTION

    THEY ARE ALL BACRTERICIDAL and Include:


    Streptomycin
    Gentamicin
    Neomycin
    Kanamycin
    Spectinomycin
    They are all very active against Gram negative bacteria
    They cause misreading of the genetic code at the ribosomal site of
    protein synthesis by bacteria
    CHEMOTHERAPY OF MALARIA I

    1.Chloroquine (CQ)
    • This was one time a very effective 4-amino-quinoline
    both for malaria treatment and prophylaxis.
    • It was first used in the 1940s with few side effects when
    taken in the dose prescribed and it was relatively cheap.
    • Presently it is not useful as antimalarial in most country
    of the world because of its toxicity and the parasites are
    now resistant
    • May have some use in the treatment of COVID-19
    CHEMOTHERAPY OF MALARIA II
    2. Proguanil: It has a biguanide chain attached at one end to a chlorophenyl
    ring and is very close in structure to pyrimethamine.
    It is a folate antagonist that destroys the malarial parasite by binding to the
    enzyme dihydrofolate reductase
    3. Malarone: Malarone is a combination of proguanil and atovaquone.
    When combined with proguanil, there is a synergistic effect and the
    combination is at the present time a very effective antimalarial drug.
    4. Maloprim: This is a combination of dapsone and pyrimethamine. Resistance
    to this drug is now widespread and its use is no longer recommended.
    5. Lapdab: This is combination of dapsone and chlorproguanil. Its use has
    been reduced due to the serious complications of severe haemolysis and
    anaemia requiring transfusion.
    CHEMOTHERAPY OF MALARIA III
    6. Fansidar : This is a combination drug containing sulphadoxine and
    pyrimethamine in ratio 20:1 in each tablet. It acts by interfering with folate
    metabolism. Resistance to Fansidar is now widespread and clinical confidence
    now dropping.
    7. Mefloquine (Lariam): First introduced in 1971, this quinoline methanol
    derivative is related structurally to quinine. It was effective against malaria
    resistant to other forms of treatment when first introduced and because of its
    long half life was a good prophylactic, but widespread resistance has now
    developed.
    8. Halofantrin (Halfan): This belongs to a class of compound called the
    phenanthrene-methanols. It has been associated with neuropsychiatric
    disturbances and arrythmias. It is contraindicated during pregnancy and is
    not advised in women who are breastfeeding.
    CHEMOTHERAPY OF MALARIA IV

    9. Coartem: This is a combination of Lumefantrin and


    Artemether. It has proven very effective. However
    anecdotal experiences are showing early parasitaemic
    recrudescence
    10. Artemisinins: This is derived from a Chinese herbal
    remedy and covers a group of products. The two most
    widely used are artesunate and artemether
    CHEMOTHERAPY OF MALARIA V
    Classification of combination therapies
    a. Artemisinin based combinations
    o Artesunate+ amodiaquine
    o Artesunate + mefloquine for areas with low transmission
    o Co-artemether (Artemether 20mg + Lumefantrine 120mg/tablets
    o Sulphamedoxine-pyrimethamine (SP) + Artemether or Artesunate
    b. SP based combinations
    o SP + CQ as separate tablets
    o SP + Amodiaquine as separate tablets
    o SP + Quinine
    o SP + Mefloquine

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