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Sulfamethoxazole is primarily renally excreted via glomerular filtration and tubular secretion. [8] About 20% of the sulfamethoxazole in urine is the unchanged drug, about 15–20% is the N-glucuronide conjugate, and about 50–70 % is the acetylated metabolite. [11] Sulfamethoxazole is also excreted in human milk. [8]
Tetrahydrofolate synthesis pathway. The synergy between trimethoprim and sulfamethoxazole was first described in the late 1960s. [25] [26] [27] Trimethoprim and sulfamethoxazole have a greater effect when given together than when given separately, because they inhibit successive steps in the folate synthesis pathway. They are given in a one-to ...
DHPS catalyses the conversion of PABA (para-aminobenzoate) to dihydropteroate, a key step in folate synthesis. [2] Folate is necessary for the cell to synthesize nucleic acids (nucleic acids are essential building blocks of DNA and RNA ), and in its absence cells will be unable to divide.
Sulfamethoxazole is an antibacterial sulfonamide. Sulfonamide is a functional group (a part of a molecule) that is the basis of several groups of drugs, which are called sulphonamides, sulfa drugs or sulpha drugs. The original antibacterial sulfonamides are synthetic antimicrobial agents that contain the sulfonamide group.
Folate deficiency hinders DNA synthesis and cell division, affecting hematopoietic cells and neoplasms the most because of their greater frequency of cell division. RNA transcription and subsequent protein synthesis are less affected by folate deficiency, as the mRNA can be recycled and used again (as opposed to DNA synthesis, where a new ...
β-Lactam antibiotics are indicated for the prevention and treatment of bacterial infections caused by susceptible organisms. At first, β-lactam antibiotics were mainly active only against gram-positive bacteria, yet the recent development of broad-spectrum β-lactam antibiotics active against various gram-negative organisms has increased their usefulness.
Sulfamethoxazole inhibits dihydropteroate synthase, an enzyme involved further upstream in the same pathway. [24] Trimethoprim and sulfamethoxazole are commonly used in combination due to possible synergistic effects, and reduced development of resistance. [24] This benefit has been questioned. [26] Tetrahydrofolate synthesis pathway
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