There can be variation in the licensing of
different medicines containing the same drug.
Tablet
CAUTIONARY AND ADVISORY LABELS 4, 9, 21, 25
▶Fasigyn (Pfizer Ltd)
Tinidazole 500 mg Fasigyn 500mg tablets | 16 tablet P £11.04
DT = £11.04
ANTIBACTERIALS › PENICILLINS
Penicillins
Benzylpenicillin and phenoxymethylpenicillin
Benzylpenicillin sodium p. 577 (Penicillin G) remains an
important and useful antibiotic but is inactivated by
bacterial beta-lactamases. It is effective for many
streptococcal (including pneumococcal), gonococcal, and
meningococcal infections and also for anthrax, diphtheria,
gas-gangrene, and leptospirosis. Pneumococci,
meningococci, and gonococci which have decreased
sensitivity to penicillin have been isolated; benzylpenicillin
sodium is no longer the drug of first choice for pneumococcal
meningitis. Although benzylpenicillin sodium is effective in
the treatment of tetanus, metronidazole p. 572 is preferred.
Benzylpenicillin is inactivated by gastric acid and absorption
from the gastro-intestinal tract is low; therefore it must be
given by injection.
Benzathine benzylpenicillin p. 577 is used for the
treatment of early syphilis and late latent syphilis; it is given
by intramuscular injection.
Phenoxymethylpenicillin p. 578 (Penicillin V) has a similar
antibacterial spectrum to benzylpenicillin sodium, but is less
active. It is gastric acid-stable, so is suitable for oral
administration. It should not be used for serious infections
because absorption can be unpredictable and plasma
concentrations variable. It is indicated principally for
respiratory-tract infections in children, for streptococcal
tonsillitis, and for continuing treatment after one or more
injections of benzylpenicillin sodium when clinical response
has begun. It should not be used for meningococcal or
gonococcal infections. Phenoxymethylpenicillin is used for
prophylaxis against streptococcal infections following
rheumatic fever and against pneumococcal infections
following splenectomy or in sickle-cell disease.
Penicillinase-resistant penicillins
Most staphylococci are now resistant to benzylpenicillin
because they produce penicillinases. Flucloxacillin p. 586,
however, is not inactivated by these enzymes and is thus
effective in infections caused by penicillin-resistant
staphylococci, which is the sole indication for its use.
Flucloxacillin is acid-stable and can, therefore, be given by
mouth as well as by injection. Flucloxacillin is well absorbed
from the gut.
Temocillin p. 587 is active against Gram-negative bacteria
and is stable against a wide range of beta-lactamases. It
should be reserved for the treatment of infections caused by
beta-lactamase-producing strains of Gram-negative
bacteria, including those resistant to third-generation
cephalosporins. Temocillin is not active against
Pseudomonas aeruginosa or Acinetobacter spp.
Broad-spectrum penicillins
Ampicillin p. 581 is active against certain Gram-positive and
Gram-negative organisms but is inactivated by penicillinases
including those produced by Staphylococcus aureus and by
common Gram-negative bacilli such as Escherichia coli.
Almost all staphylococci, approx. 60% of E. coli strains and
approx. 20% of Haemophilus influenzae strains are now
resistant. The likelihood of resistance should therefore be
considered before using ampicillin for the ‘blind’ treatment
of infections; in particular, it should not be used for hospital
patients without checking sensitivity.
Ampicillin is well excreted in the bile and urine. It is
principally indicated for the treatment of exacerbations of
chronic bronchitis and middle ear infections, both of which
may be due to Streptococcus pneumoniae and H. influenzae,
and for urinary-tract infections.
Ampicillin can be given by mouth but less than half the
dose is absorbed, and absorption is further decreased by the
presence of food in the gut.
Maculopapular rashes commonly occur with ampicillin
(and amoxicillin p. 579) but are not usually related to true
penicillin allergy. They almost always occur in patients with
glandular fever; broad-spectrum penicillins should not
therefore be used for ‘blind’ treatment of a sore throat. The
risk of rash is also increased in patients with acute or chronic
lymphocytic leukaemia or in cytomegalovirus infection.
Amoxicillin is a derivative of ampicillin and has a similar
antibacterial spectrum. It is better absorbed than ampicillin
when given by mouth, producing higher plasma and tissue
concentrations; unlike ampicillin, absorption is not affected
by the presence of food in the stomach. Amoxicillin is also
used for the treatment of Lyme disease.
Co-amoxiclav p. 582 consists of amoxicillin with the
betalactamase inhibitor clavulanic acid. Clavulanic acid itself
has no significant antibacterial activity but, by inactivating
beta-lactamases, it makes the combination active against
beta-lactamase-producing bacteria that are resistant to
amoxicillin. These include resistant strains of Staph. aureus,
E. coli, and H. influenzae, as well as many Bacteroides and
Klebsiella spp. Co-amoxiclav should be reserved for
infections likely, or known, to be caused by amoxicillin-
resistant beta-lactamase-producing strains.
A combination of ampicillin with flucloxacillin (as co-
fluampicil p. 582 is available to treat infections involving
either streptococci or staphylococci.
Antipseudomonal penicillins
Piperacillin, a ureidopenicillin, is only available in
combination with the beta-lactamase inhibitor tazobactam.
Ticarcillin, a carboxypenicillin, is only available in
combination with the beta-lactamase inhibitor clavulanic
acid. Both preparations have a broad spectrum of activity
against a range of Gram-positive and Gram-negative
bacteria, and anaerobes. Piperacillin with tazobactam p. 576
has activity against a wider range of Gram-negative
organisms than ticarcillin with clavulanic acid p. 576 and it is
more active against Pseudomonas aeruginosa. These
antibacterials are not active against MRSA. They are used in
the treatment of septicaemia, hospital-acquired pneumonia,
and complicated infections involving the urinary tract, skin
Infection
and soft tissues, or intra-abdomen. For severe pseudomonas
infections these antipseudomonal penicillins can be given
with an aminoglycoside (e.g. gentamicin p. 545) since they
have a synergistic effect.
Mecillinams
Pivmecillinam hydrochloride p. 585 has significant activity
against many Gram-negative bacteria including Escherichia
coli, klebsiella, enterobacter, and salmonellae. It is not active
against Pseudomonas aeruginosa or enterococci.
Pivmecillinam hydrochloride is hydrolysed to mecillinam,
which is the active drug.
Penicillins
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