Antibiotic
A drug used to treat bacterial infections. Antibiotics have no
effect on viral infections. Originally, an antibiotic was a
substance produced by one microorganism that selectively
inhibits the growth of another. Synthetic antibiotics, usually
chemically related to natural antibiotics, have since been
produced that accomplish comparable tasks.
In 1926, Alexander Fleming discovered penicillin, a substance
produced by fungi that appeared able to inhibit bacterial growth. In
1939, Edward Chain and Howard Florey further studied penicillin and
later carried out trials of penicillin on humans (with what were
deemed fatal bacterial infections). Fleming, Florey and Chain shared
the Nobel Prize in 1945 for their work which ushered in the era of
antibiotics.
Another antibiotic, for example, is tetracycline, a broad-spectrum
agent effective against a wide variety of bacteria
including Hemophilus influenzae, Streptococcus pneumoniae,
Mycoplasma pneumoniae, Chlamydia psittaci, Chlamydia
trachomatis, Neisseria gonorrhoea, and many others. The first drug of
the tetracycline family, chlortetracycline, was introduced in 1948.
GENERAL MECHANISMS OF ACTION OF ANTI
MICROBIAL AGENTS:
1.Other interfere with biosynthesis of bacterial cell wall.
2. Some inhibits protein synthesis
PENICILLINS
STRUCTURE:
A beta-lactam drug, with beta-lactam ring.(beta
lactam antibiotics)
THE ACTION OF PENICILLINS:
CEPHALOSPORINS
1. First Generation
cephalosporins largely
effective against the same
gram-positive organisms
affected by penicillin.
-cefadroxil
-cefazolin
-cephalexin
-cephalotin
-cephapirin
-cephadrine
2. Seond Generation
Cephalosporinseffective against
those strain as well
as Haemophilus
influenza,
Enterobacter
aerogenes and
bacteria, to include
Serratia
marcescens.
-Cefnidir
-Cefixime
-Cefoperazone
-Cefotaxime
-Cefpodoxime
-Ceftazidime
-Ceftibuten
-Moxalactam
4. Fourth Generation
Cephalosporinsdeveloped to fight
against the resistant
gram-negative
bacteria. The first
drug is cefepime.
-Cefepime
AMINOGLYCOSIDES
The following are aminoglycosides:
1.
Gentamycin
2.
Tobramycin
3.
Amikacin
4.
Netilmicin
5.
Kanamycin
MECHANISM OF ACTION:
Bactericidal
Inhibit protein synthesis in susceptible strains of gramnegative bacteria, leading to loss of functional integrity
of the bacterial cell membrane, which causes cell
death.
THERAPEUTIC USE OF AMINOGLYCOSIDES
Used to treat serious infections caused by gramnegative bacteria
CONTRAINDICATIONS AND PRECAUTIONS
Contraindicated in known allergies to
aminoglycosides, in patients with renal failure,
hepatic disease, pre-existing hearing loss, myasthenia
gravis, Parkinsons, pregnancy and lactation.
DRUG TO DRUG INTERACTIONS
Diuretics- increased incidence of
ototoxicity, nephrotoxicity and
neurotoxicity.
ADVERSE EFFECTS
CNS-irreversible deafness vestibular paralysis
confusion depression disorientation,numbness,
tingling and weakness related to drug effects.
Kidney- renal toxicity, which may progress to
renal failure caused by the direct toxicity of
aminoglycosides.
Hema- bonemarrow depression resulting from
direct drug effect may lead to immune
suppression and superinfection.
GI system- nausea,vomiting, diarrhea,weight
loss of bacterial flora and toxicity to mucus
membrane and liver as the drugs are
metabolized.
Skin effects- photosensitivity, purpura, rash,
urticaria and exfloliative dermatitis.
Cardiac- palpitations, hypotension or
hypertension.
MACROLIDES
The macrolides are
Azithromycin
Clarithromycin
Dirithromycin
Erythromycin
MECHANISM OF ACTION:
Bactericidal and sometimes bacteriostatic
Exert effect by binding to the bacterial cell
ribosomes and changing or altering protein
production/ function
Lead to impared cell metabolism and division
PHARMACOKINETICS
Erythromycin is destroyed by gastric juice,
slats are added to stabilize the drug. Food
does not interfere with the absorption of the
macrolides.
THERAPEUTIC USE:
Indicated for the treatment of : Streptococcal
infection, Mycoplasma infection, Listeria
LINCOSAMIDES
Similar to the Macrolides but are more toxic
Bactericidal and bacteriostatic depending on
the dose
Examples: Clindamycin and Lincomycin
MECHANISM OF ACTION
penetrate the cell membrane and bind to the
ribosome in the bacterial cytoplasm to prevent the
protein production.
SIDE EFFECTS AND ADVERSE REACTIONS
GIT-GI irritatin , nausea, vomiting and stomatitis.
Allergic reactions.
DRUG INTERACTIONS
Lyncomycin and clindamycin are incompatible with
aminophyline, phenytoin, barbiturates and
ampicillin.
TETRACYCLINE
FLUOROQUINOLONES
SULFONAMIDES
called sulfa drugs that inhibit folic acid
synthesis
folic acid is necessary for the synthesis
of purine and pyrimidine precursors of DNA
and RNA. Humans cannot produce folic acid
and must obtain it from diet. While bacteria
need to manufacture their own folic acid
inside their cell structure.
1. Sulfazalazine
2. Sulfamethoxazole
3. Sulfadiazine
4. Sulfixoxazole
ADVERSE EFFECTS
GI system nausea, vomiting,diarrhea,abdominal
pain, anorexia, stomatitis,and hepatic injury, which
are all related to the direct irritation of the GIT and
death of normal flora.
Renal system- crystalluria, hematuria and
proteinuria which can progress to a nephritic
syndrome.
CNS- headache, dizziness, vertigo, ataxia,
convulsions and depression related to drug effects
on the nerves.
Hema- bone marrow depression related to the drug
effects on the cells of the bone marrow that turn
over rapidly.
Prescribed for:
Isoniazid
Tuberculosis
Ethambutol
Tuberculosis
Penicillin V & G
Acintobactor
Vancomycin
MRSA
Bacterial Endocarditis
Metroidazole
Penciclovir
Herpes
Augmentin
Prescribed for:
Erythromycin
Strep throat
Clindamycin
If allergic to penicillin
Rifampin
Tuberculosis
Tetracycline
Acne
Chloramphenizol
Salmonella
Nitrofurantoin
E-coli
Penicillin VK
Ear infection
Ciprofloxacin
bacteremia
Bacitracin
streptomycin
neomycin
Mechanism of
Action
Inhibit protein
synthesis by
binding to a
portion of the
bacterial
ribosome.
Most of them are
bacteriocidal
(cause bacterial
cell death).
Inhibits cell wall
production by
blocking a step in
the process
(recycling of the
membrane lipid
carrier) which is
Beta-lactam antibiotics
penicillins
cephalosporins
carbapenems
monobactams
Cephalosporins
Chloramphenicol
Glycopeptides
vancomycin
needed to add on
new cell wall
subunits.
Group of
antiobiotics which
contain a specific
chemical structure
(a beta-lactam
ring)
Similar to
penicillins in their
mode of action,
but they treat a
broader range of
bacterial
infections.
The have
structural
similarities to
penicillins and
many people with
allergies to
penicillins also
have allergic
reactions to
cephalosporins.
Inhibits protein
synthesis by
binding to a
subunit of
bacterial
ribosomes (50S).
Interferes with cell
wall development
by blocking the
Macrolides
erythromycin
Lincosamides
clindamycin
Penicillins
Quinolones
Rifampin
attachment of
new cell wall
subunits
(muramyl
pentapeptides).
Inhibit protein
synthesis by
binding to a
subunit of the
bacterial
ribosome (50S).
Inhibit protein
synthesis by
binding to a
subunit of the
bacterial
ribosome (50S).
Inhibit formation
of the bacterial
cell wall by
blocking crosslinking of the cell
wall structure.
The cell wall is a
needed protective
casing for the
bacterial cell wall.
Block DNA
synthesis by
inhibiting one of
the enzymes
(DNA gyrase)
needed in this
process.
Inhibits RNA
Tetracyclines
Trimethoprim andSulfonamides
synthesis by
inhibiting one of
the enzymes
(DNA-dependent
RNA polymerase)
needed in this
process. RNA is
needed to make
proteins.
Inhibit protein
synthesis by
binding to the
subunit of the
bacterial
ribosome (30S
subunit).
Blocks cell
metabolism by
inhibiting
enzymes which
are needed in the
biosynthesis of
folic acid which is
a necessary cell
compound.
SOURCES:
http://www.medicinenet.com/script/main/art.asp?articlekey=8121
http://scienceaid.co.uk/biology/micro/antibiotics.html
http://pharmacologydeh-28classof2011.wikispaces.com/AntiInfective+Agents