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General
- Trimethoprim is a bacteriostatic
antibiotic mainly used in the prophylaxis and treatment of urinary
tract infections.
- Trimethoprim was commonly used in
combination with sulfamethoxazole, a sulfonamide antibiotic, which
inhibits an earlier step in the folate synthesis pathway (see
diagram above). This combination, also known as co-trimoxazole,
TMP-sulfa, or TMP-SMX, results in an in vitro synergistic
antibacterial effect by inhibiting successive steps in folate
synthesis.
- Trimethoprim, combined with a
sulfonamide (sulfadiazine or sulfamethoxazole), is an antibiotic
used to treat respiratory, urinary tract, skin, and gastrointestinal
infections, and infections with coccidia.
- Trimethoprim, an antibacterial
drug, is a bacterial dihydrofolate reductase inhibitor used as a
prophylactic or to treat various bacterial infections particularly
urinary tract infections such as Proteus mirabilis
Application
-
Trimethoprim-sulfamethoxazole(TMP-SMX), a drug regarded to be the
most efficient for the chemoprophylaxis of Pneumocystis carinii
pneumoniaPCP) in patients with HIV infection (5, 10, 18), stands out
because of its wide use.
- Trimethoprim is often used in
combination with sulfamethoxazole to treat a wide variety of aerobic
gram-positive and gram-negative infections
- Trimethoprim,
2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine(TMP), widely used
in conjunction with sulfamethoxazole(SMX), is an effective
antimicrobial agent used, for example, in the treatment of urinary
tract infections and as a powerful bacteriostatic agent, because the
antimicrobial activity is greater than that when the sulfa-drug is
used alone.
- Antibiotics were extracted by
solid-phase extraction (SPE) on a polystyrene–divinylbenzene(SDB)
Empore extraction disk.
Process
- Certain benzylpyrimidines, such
as trimethoprim 1 are potent and selective inhibitors of bacterial
dihydrofolate reductase, the enzyme responsible for the
NADPH-dependent reduction of 7,8-dihydrofolate to
5,6,7,8,-tetrahydrofolate.
- The manufacture of Trimethoprim
involves three distinct stages;starting from Gallic Acid which is
converted into 3, 4, 5 Trimethoxy benzaldehyde and which in turn is
converted into Trimethoprim.
- Manufacture of 3, 4, 5 Trimethoxy
benzaldehyde commences with methoxylation of Gallic Acid with
Dimethyl sulphate to obtain the intermediate product 3, 4, 5
Trimethoxy benzoic acid.
Technology
- The assays are suitable for
pharmacokinetic studies and have been applied to determination of
trimethoprim concentrations in serum and urine during therapy with
Co-trimoxazole, a sulfonamide/ trimethoprim preparation.
- The I... case! competitive
protein binding assay technique can be used toy plasma trimethoprim
concentrations with sensitivity to 0.02mg oftrimethoprim per liter.
- Cotrimoxazole, a combination of
sulfamethoxazole(SMZ) and trimethoprim (TMP), is widely used for the
treatment of not only urinary tract infections, but also infections
of the respiratory tract, septicemia, and gonorrhea.
- The presence of pathogenic Vibrio
cholerae is complicated by the presence in water of a large number
of mostly nonpathogenic V. cholerae strains.
Market
- The anti-infectives market is
forecast to expand at a CAGR of 4.8% over the period 2005-11, driven
largely by gains in the anti-bacterial and anti-viral classes.
- With sales growth of 200.0% in
2005, Tamiflu, an established product was the strongest performing
brand in Roche’s anti-infectives portfolio, with sales of $637.7m,
on the back of increased demands for the product as a treatment for
avian influenza.
- The highest growth rate in the
global anti-bacterials drug class was reported by the beta-lactams
class of drugs which registered a growth rate of 12.8% representing
sales of $1,512m in 2005, an up of $171mfrom year previous sales
reported at $1,341m...
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