ARTICLES
Antibiotics Classification And Side Effects
What are Antibiotics?
The word "antibiotics" comes from the Greek anti
("against") and bios ("life"). Antibiotics
are drugs that either destroy bacteria or prevent their reproduction.
Antibiotics that kill bacteria are called "bactericidal" and
the ones that stop the growth of bacteria are called "bacteriostatic".
Since penicillin's introduction during the 1940s, scientists
developed numerous other antibiotics. Today, over 100 different
antibiotics are available. About 90% of antibiotics are made
from living organisms such as bacteria, others are produced
synthetically, either in whole or in part.
Antibiotics classification
Although there are several classification schemes for antibiotics,
based on bacterial spectrum (broad, narrow) or route of administration
(injectable, oral, topical), or type of activity (bactericidal,
bacteriostatic), the most useful is based on chemical structure.
Antibiotics within a structural class will generally have
similar patterns of effectiveness, toxicity, and allergic
potential.
Most commonly used types of antibiotics are: Penicillins,
Fluoroquinolones, Cephalosporins, Macrolides, and Tetracyclines.
While each class is composed of multiple drugs, each drug
is unique in some way.
Penicillins
The penicillins are the oldest class of antibiotics. Penicillins
have a common chemical structure which they share with the
cephalopsorins. Penicillins are generally bactericidal, inhibiting
formation of the cell wall.
There are four types of penicillins:
The natural pencillins are based on the original penicillin-G
structure. Penicillin-G types are effective against gram-positive
strains of streptococci, staphylococci, and some gram-negative
bacteria such as meningococcus.
Penicillinase-resistant
penicillins are active even in the presence of the bacterial
enzyme that inactivates most
natural penicillins.
Extended spectrum penicillins which
are effective against a wider range of bacteria.
Aminopenicillins such as ampicillin
and amoxicillin have an extended spectrum of action compared
with the natural
penicillins.
Penicillins side effects Penicillins are among the least toxic drugs known. The most
common side effect of penicillin is diarrhea. Nausea, vomiting,
and upset stomach are also common. In rare cases penicillins
can cause immediate and delayed allergic reactions - specifically,
skin rashes, fever, and anaphylactic shock. Penicillins are
classed as category B during pregnancy.
Cephalosporins
Cephalosporins have a mechanism of action identical to that
of the penicillins. However, the basic chemical structure
of the penicillins and cephalosporins differs in other respects,
resulting in some difference in the spectrum of antibacterial
activity. Like the penicillins, cephalosporins interfere
with synthesis of the bacterial cell wall and so are bactericidal.
Cephalosporins are among the most diverse classes of antibiotics,
they are grouped into "generations" by their antimicrobial
properties. Each generation has a broader spectrum of activity
than the one before.
The first generation cephalosporins include: cephalothin,
cefazolin, cephapirin, cephradine, cephalexin, cefadroxil.
Their spectrums of activity are quite similar. They possess
generally excellent coverage against most gram-positive pathogens
and variable to poor coverage against most gram negative
pathogens.
The second generation cephalosporins include: cefaclor,
cefamandole, cefonicid, ceforanide, cefuroxime. In addition
to the gram-positive spectrum of the first generation cephalosporins,
these agents have expanded gram-negative spectrum. Cefoxitin
and cefotetan also have good activity against Bacteroides
fragilis.
The third generation cephalosporins have much expanded gram-negative
activity. However, some members of this group have decreased
activity against gram-positive organisms. The third generation
cephalosporins include: cefcapene, cefdaloxime, cefditoren,
cefetamet, cefixime, cefmenoxime, cefodizime, cefoperazone,
cefotaxime, cefpimizole, cefpodoxime, ceftibuten, ceftriaxone.
They have the advantage of convenient dosing schedules, but
they are expensive.
The fourth generation cephalosporins are extended-spectrum
agents with similar activity against gram-positive organisms
as first-generation cephalosporins. They also have a greater
resistance to beta-lactamases (bacterial enzymes that may
destroy antibiotic before it can do its work) than the third
generation cephalosporins. Many fourth generation cephalosporins
can cross blood brain barrier and are effective in meningitis.
The fourth generation cephalosporins include: cefclidine,
cefepime, cefluprenam, cefozopran, cefpirome, cefquinome.
Cephalosporin side effects
Cephalosporins generally cause few side effects. Common
side effects associated these drugs include: diarrhoea, nausea,
mild stomach cramps or upset. Approximately 5?10% of patients
with allergic hypersensitivity to penicillins will also have
cross-reactivity with cephalosporins. Thus, cephalosporin
antibiotics are contraindicated in people with a history
of allergic reactions (urticaria, anaphylaxis, interstitial
nephritis, etc) to penicillins or cephalosporins. Cephalosporin
antibiotics are classed as pregnancy category B.
Fluoroquinolones
Fluoroquinolones are the newest class of antibiotics. Their
generic name often contains the root "floxacin".
They are synthetic antibiotics that belong to the family
of antibiotics called quinolones. The older quinolones are
not well absorbed and are used to treat mostly urinary tract
infections. The newer fluoroquinolones are broad-spectrum
bacteriocidal drugs that are chemically unrelated to the
penicillins or the cephaloprosins. Because of their excellent
absorption fluoroquinolones can be administered not only
by intravenous but orally as well.
Commonly used fluoroquinolones include ciprofloxacin, levofloxacin,
lomefloxacin, norfloxacin, sparfloxacin, clinafloxacin, gatifloxacin,
ofloxacin, trovafloxacin.
Fluoroquinolones side effects
Fluoroquinolones are well tolerated and relatively safe.
The most common side effects include nausea, vomiting, diarrhea,
abdominal pain. Other more serious but less common side effects
are central nervous system effects (headache, confusion and
dizziness), phototoxicity (more common with lomefloxacin
and sparfloxacin). All drugs in this class have been associated
with convulsions. Fluoroquinolones are classed as pregnancy
category C.
Tetracyclines
Tetracyclines got their name because they share a chemical
structure that has four rings. They are derived from a species
of Streptomyces bacteria. Tetracycline antibiotics are broad-spectrum
bacteriostatic agents, that inhibit bacterial protein synthesis.
Tetracyclines may be effective against a wide variety of
microorganisms, including rickettsia and amebic parasites.
Tetracyclines are used in the treatment of infections of
the respiratory tract, sinuses, middle ear, urinary tract,
skin, intestines. Tetracyclines also are used to treat Gonorrhoea.
Their most common current use is in the treatment of moderately
severe acne and rosacea.
The most commonly prescribed tetracycline antibiotics are:
tetracycline, doxycycline, minocycline, oxytetracycline.
Tetracycline side effects
Drugs in the tetracycline class become toxic over time.
Expired drugs can cause a dangerous syndrome resulting in
damage to the kidneys.
Common side effects associated with tetracyclines include
cramps or burning of the stomach, diarrhea, sore mouth or
tongue. Tetracyclines can cause skin photosensitivity, which
increases the risk of sunburn under exposure to UV light.
This may be of particular importance for those intending
to take on holidays long-term doxycyline as a malaria prophylaxis.
Rarely, tetracyclines may cause allergic reactions. Very
rarely severe headache and vision problems may be signs of
dangerous secondary intracranial hypertension.
Tetracycline antibiotics should not be used in children
under the age of 8, and specifically during periods of tooth
development. Tetracyclines are classed as pregnancy category
D. Use during pregnancy may cause alterations in bone development.
Macrolides
The macrolide antibiotics are derived from Streptomyces
bacteria, and got their name because they all have a macrocyclic
lactone chemical structure. The macrolides are bacteriostatic,
binding with bacterial ribosomes to inhibit protein synthesis.
Erythromycin, the prototype of this class, has a spectrum
and use similar to penicillin. Macrolide antibiotics are
used to treat respiratory tract infections (such as pharyngitis,
sinusitis, and bronchitis), genital, gastrointestinal tract,
and skin infections.
The most commonly prescribed macrolide antibiotics are:
erythromycin, clarithromycin, azithromycin, roxithromycin,
troleandomycin.
Macrolides side effects
Side effects associated with macrolides include nausea,
vomiting, and diarrhea; infrequently, there may be temporary
auditory impairment. Azithromycin has been rarely associated
with allergic reactions, including angioedema, anaphylaxis,
and dermatologic reactions. Oral erythromycin may be highly
irritating to the stomach and when given by injection may
cause severe phlebitis. Macrolide antibiotics should be used
with caution in patients with liver dysfunction. Pregnancy
category B: Azithromycin, erythromycin. Pregnancy category
C: Clarithromycin, dirithromycin, troleandomycin.
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