Faculty of pharmacy and pharmaceutical

sciences

University of Karachi

NAME: MASOOMA BUTOOL

ROLL NO: BP-1750094
FINAL PROF.(MOR.)
COURSE NO: PHL-410

SUBMITTED TO: MAM AFROZ

ANTIBACTERIAL DRUGS:
Effective antibacterial drugs can either inhibit the growth of (bacteriostatic) or kill (bactericidal)
bacteria. Antibacterial effects result from the inhibition of cell wall synthesis, inhibition of
intrabacterial protein synthesis, alteration in nucleic acid metabolism, or intrabacterial enzyme
inhibition. Drugs of choice for most infections are not based on a bacteriostatic or bactericidal
effect of an agent, but rather are chosen based on whether the drug reaches the site of
infection in adequate quantities, the spectrum of the agent, its safety, and cost.
Antibiotics are generally classified according to their molecular structure and their antimicrobial
mechanisms. Ideally, these mechanisms of action either interrupt synthesis of structural
components or alter specific metabolic functions that are unique to microbial cells. Such
specificity cannot always be accomplished, but if it is, human cells can be spared cytotoxic
effects.

MECHANISMS OF ACTION OF ANTIBACTERIAL DRUGS:

Antibacterial drugs are divided into four different categories according to their function i.e.

 Cell wall active agents

 Protein synthesis inhibitors
 Nucleic acid inhibitors
 Antimetabolites.
These four categories consist of several derivatives by the modifications done in their structure,
due which they act as either bacteriostatic or bacteriocidal by doing different types of mode of
action.

CELL WALL ACTIVE AGENTS:

Mechanism of action:
β-Lactam (penicillins, cephalosporins) and glycopeptide antibiotics (vancomycin, telavancin,
teicoplanin) bind to receptors in the bacterial cell wall. The target receptors for penicillins and
cephalosporins are called penicillin-binding proteins. Autolytic enzymes within the cell wall bind
to penicillin-binding proteins; once activated, the enzymes damage the peptidoglycan
component of the cell wall, creating weakening and eventual cell lysis. Glycopeptide antibiotics
bind to a terminal dipeptide (alanine-alanine) in the cell wall peptidoglycan and prevent the
necessary cross-linking for a competent cell wall structure. At usual doses, β-lactam and
glycopeptide antibiotics are bactericidal. Resistance arises due to mutations in the penicillin-
binding proteins, leading to reduced β-lactam binding (e.g., by oxacillin-resistant
Staphylococcus aureus or penicillin-resistant Streptococcus pneumoniae) or changes to the
terminal dipeptide (e.g., by vancomycin-resistant Enterococcus faecium) that reduce the level
of binding.
Spectrum of activity:
They treat staphylococci, streptococci bacterial infections commonly used for dental abscess,
ear infections, gonorrhea, pneumonia, respiratory tract infection, urinary tract infection, strep
throat, sinus infection, meningitis, gonorrhea. Vncomycin treats clostridium difficle

Adverse effects:
 Common adverse effect of penecellin are Nausea, Vomitting, Apigastric distress,
Diarrhea, and black hairy tongue, Adema, Anaphylaxis.
 Common adverse effect of cephalosporines are stumach upset, Diarrhea, yeast
infection, Dizziness.
 Vncomycin cause bitter taste rash on face and upper body low blood pressure, Chills,
Drug fever, High level of white blood cell.

INHIBITORS OF PROTEIN SYNTHESIS:

Mechanism of action:
Enzymes and cellular structures are primarily made of proteins. Protein synthesis is an essential
process necessary for the multiplication and survival of all bacterial cells. Several types of
antibacterial agents target bacterial protein synthesis by binding to either the 30S or 50S
subunits of the intracellular ribosomes. This activity then results in the disruption of the normal
cellular metabolism of the bacteria, and consequently leads to the death of the organism or the
inhibition of its growth and multiplication. Examples: Aminoglycosides, macrolides,
lincosamides, streptogramins, chloramphenicol, tetracyclines.

Spectrum of activity:
 Tetra-cyclins used to treat infections like Pneumoni, Respiratory tract infection,
Infections of skin, eye, lymphatic, Intestinal and Urinary system.
 Aminoglycosides are used in the treatment of severe infection of abdominal and urinary
tract, as well as andocarditis, also used for prophyl excess.
 Macrolides used to treat infection cause by gram positive bacteria for example
Streptococcus pheunomiae and limited gram neg bacteria e.g: Haemophilus influnzae.

Adverse Effects:
 Tetra-cycline causes Nausea, Vomiiting, Diarrhea, Loss of appetide, Mouth source, Black
hairy tougue, Sore throat, Dizziness, Headache, Rectal discomfort.
 Major adverse effect of Aminoglycoside are Ototoxicity, Nephro toxicity, Neuro
muscular blockade.
  Typical adverse effect related to macrolytes are Nausea, Vomitting, Diarrhea and Ringing
or Buzzingin the ear (Tinnitus). Serious side effect includes alargic reaction and
cholestatis hepatitis.

INHIBITORS OF NUCLEIC ACID SYNTHESIS:

Mechanism of action:
DNA and RNA are keys to the replication of all living forms, including bacteria. Some antibiotics
work by binding to components involved in the process of DNA or RNA synthesis, which causes
interference of the normal cellular processes which will ultimately compromise bacterial
multiplication and survival. Examples: quinolones, metronidazole, and rifampicin.

Spectrum of activity:
 Quinolones used extensively for treatment of a broad range of clinical infections include
Genitaryurinary, Gastrointestinal and Resoiratory tracts as well as infections of bone
joints and skin.
 Metronidozole use to treat Skin infections, Rosacea and Mouth infection foe e.g: Dental
abbscesses, also used to treat Bacterial vaginosis.
 Refampicin is used to treat several infections Tuberculosis, Leprosy and Legionnaires
disease.

Adverse Effects:
 Quinolones causes adverse effect includes Gastrointestinal reactions such as Dyspepsia,
CNS reactions such as Dizziness, Insomnia, Headache, Tendonitis, Depression, Fatigue.
 Metonidazole causes Dizziness, Headache, Stumach upset, Loss of appetide,
Constipation, Burning and Stinging, Skin redness and Irretation.
 Refampicin cause Upset stamach, Heart burn, Neusea, Menstual changes and headache.

ANTIMETABOLITES:
Mechanism of action:
Other antibiotics act on selected cellular processes essential for the survival of the bacterial
pathogens. For example, both sulfonamides and trimethoprim disrupt the folic acid pathway,
which is a necessary step for bacteria to produce precursors important for DNA synthesis.
Sulfonamides target and bind to dihydropteroate synthase, trimethophrim inhibit dihydrofolate
reductase both of these enzymes are essential for the production of folic acid, a vitamin
synthesized by bacteria, but not humans.

Spectrum of activity:
  Sulfonamides used to treat urinary teact infection Bromchitus, Eye infection, Bacterial
meningitis, Pneumoniae, Travellars diarrhea.
 Trimethoprim used to treat Urinary tract infection such as Systitis, also used to treat
chest infection and Acne.

Adverse Effect:
 Sulfonamides cause Liver damage, Low WBC count(leucopenia), Trombocytopenia and
Anemia also cause damage to kidney.
 Trimethoprim cause Iching, Stumach upset, Loss of appetide, Changes in taste and
Headache.