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Trimethoprim
Overview
What is Trimethoprim?
Trimethoprim is a synthetic antibacterial available as 100 mg tablets for oral administration.
Trimethoprim is 2,4-Diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine. It is a white to cream colored, odorless, bitter compound. The structural formula is represented below:
Trimethoprim Tablets USP, 100 mg contain the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, magnesium stearate, sodium lauryl sulfate, sodium starch glycolate and stearic acid.
What does Trimethoprim look like?
What are the available doses of Trimethoprim?
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What should I talk to my health care provider before I take Trimethoprim?
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How should I use Trimethoprim?
For the treatment of initial episodes of uncomplicated urinary tract infections due to susceptible strains of the following organisms: species and coagulase-negative species, including
Cultures and susceptibility tests should be performed to determine the susceptibility of the bacteria to trimethoprim. Therapy may be initiated prior to obtaining the results of these tests.
The usual oral adult dosage is 100 mg of trimethoprim every 12 hours or 200 mg trimethoprim (two 100 mg tablets) every 24 hours, each for 10 days. The use of trimethoprim in patients with a creatinine clearance of less than 15 mL/min is not recommended. For patients with a creatinine clearance of 15 to 30 mL/min, the dose should be 50 mg every 12 hours.
What interacts with Trimethoprim?
Trimethoprim tablets are contraindicated in individuals hypersensitive to trimethoprim and in those with documented megaloblastic anemia due to folate deficiency.
What are the warnings of Trimethoprim?
6. Cataracts–Subcapsular bilateral cataracts occurred in 10%, and unilateral in 6.3%, of male rats treated with gemfibrozil at 10 times the human dose.
Serious hypersensitivity reactions have been reported rarely in patients on trimethoprim therapy. Trimethoprim has been reported rarely to interfere with hematopoiesis, especially when administered in large doses and/or for prolonged periods.
The presence of clinical signs such as sore throat, fever, pallor or purpura may be early indications of serious blood disorders (see). Complete blood counts should be obtained if any of these signs are noted in a patient receiving trimethoprim and the drug discontinued if a significant reduction in the count of any formed blood element is found.
What are the precautions of Trimethoprim?
General
Trimethoprim should be given with caution to patients with possible folate deficiency. Folates may be administered concomitantly without interfering with the antibacterial action of trimethoprim. Trimethoprim should also be given with caution to patients with impaired renal or hepatic function (see and).
Drug Interactions
Trimethoprim may inhibit the hepatic metabolism of phenytoin. Trimethoprim, given at a common clinical dosage, increased the phenytoin half-life by 51% and decreased the phenytoin metabolic clearance rate by 30%. When administering these drugs concurrently, one should be alert for possible excessive phenytoin effect.
Drug/Laboratory Test Interactions
Trimethoprim can interfere with a serum methotrexate assay as determined by the Competitive Binding Protein Technique (CBPA) when a bacterial dihydrofolate reductase is used as the binding protein. No interference occurs, however, if methotrexate is measured by a radioimmunoassay (RIA).
The presence of trimethoprim may also interfere with the Jaffé alkaline picrate reaction assay for creatinine resulting in over estimations of about 10% in the range of normal values.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenesis
Long-term studies in animals to evaluate carcinogenic potential have not been conducted with trimethoprim.
Mutagenesis
Trimethoprim was demonstrated to be non-mutagenic in the Ames assay. In studies at two laboratories, no chromosomal damage was detected in cultured Chinese hamster ovary cells at concentrations approximately 500 times human plasma levels; at concentrations approximately 1000 times human plasma levels in these same cells, a low level of chromosomal damage was induced at one of the laboratories. No chromosomal abnormalities were observed in cultured human leukocytes at concentrations of trimethoprim up to 20 times human steady-state plasma levels. No chromosomal effects were detected in peripheral lymphocytes of human subjects receiving 320 mg of trimethoprim in combination with up to 1600 mg of sulfamethoxazole per day for as long as 112 weeks.
Impairment of Fertility
No adverse effects on fertility or general reproductive performance were observed in rats given trimethoprim in oral dosages as high as 70 mg/kg/day for males and 14 mg/kg/day for females.
Pregnancy
Pregnancy Category C. Trimethoprim has been shown to be teratogenic in the rat when given in doses 40 times the human dose. In some rabbit studies, the overall increase in fetal loss (dead and resorbed and malformed conceptuses) was associated with doses six times the human therapeutic dose.
While there are no large, well-controlled studies on the use of trimethoprim in pregnant women, Brumfitt and Pursell, in a retrospective study, reported the outcome of 186 pregnancies during which the mother received either placebo or trimethoprim in combination with sulfamethoxazole. The incidence of congenital abnormalities was 4.5% (3 of 66) in those who received placebo and 3.3% (4 of 120) in those receiving trimethoprim and sulfamethoxazole. There were no abnormalities in the 10 children whose mothers received the drug during the first trimester. In a separate survey, Brumfitt and Pursell also found no congenital abnormalities in 35 children whose mothers had received trimethoprim and sulfamethoxazole at the time of conception or shortly thereafter.
Because trimethoprim may interfere with folic acid metabolism, trimethoprim should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
The oral administration of trimethoprim to rats at a dose of 70 mg/kg/day commencing with the last third of gestation and continuing through parturition and lactation caused no deleterious effects on gestation or pup growth and survival.
Nursing Mothers
Trimethoprim is excreted in human milk. Because trimethoprim may interfere with folic acid metabolism, caution should be exercised when trimethoprim is administered to a nursing woman.
Pediatric Use
Safety and effectiveness in pediatric patients below the age of 2 months have not been established. The effectiveness of trimethoprim as a single agent has not been established in pediatric patients under 12 years of age.
What are the side effects of Trimethoprim?
The adverse effects encountered most often with trimethoprim were rash and pruritus.
Dermatologic
Rash, pruritus, and phototoxic skin eruptions. At the recommended dosage regimens of 100 mg b.i.d. or 200 mg q.d. each for 10 days, the incidence of rash is 2.9% to 6.7%. In clinical studies which employed high doses of trimethoprim, an elevated incidence of rash was noted. These rashes were maculopapular, morbilliform, pruritic, and generally mild to moderate, appearing 7 to 14 days after the initiation of therapy.
Hypersensitivity
Rare reports of exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell Syndrome), and anaphylaxis have been received.
Gastrointestinal
Epigastric distress, nausea, vomiting, and glossitis. Elevation of serum transaminase and bilirubin has been noted, but the significance of this finding is unknown. Cholestatic jaundice has been rarely reported.
Hematologic
Thrombocytopenia, leukopenia, neutropenia, megaloblastic anemia, and methemoglobinemia.
Metabolic
Hyperkalemia, hyponatremia.
Neurologic
Aseptic meningitis has been rarely reported.
Miscellaneous
Fever, and increases in BUN and serum creatinine levels.
What should I look out for while using Trimethoprim?
Trimethoprim tablets are contraindicated in individuals hypersensitive to trimethoprim and in those with documented megaloblastic anemia due to folate deficiency.
Serious hypersensitivity reactions have been reported rarely in patients on trimethoprim therapy. Trimethoprim has been reported rarely to interfere with hematopoiesis, especially when administered in large doses and/or for prolonged periods.
The presence of clinical signs such as sore throat, fever, pallor or purpura may be early indications of serious blood disorders (see). Complete blood counts should be obtained if any of these signs are noted in a patient receiving trimethoprim and the drug discontinued if a significant reduction in the count of any formed blood element is found.
What might happen if I take too much Trimethoprim?
How should I store and handle Trimethoprim?
Store unreconstituted vials at 25° C (77° F); excursions permitted to 15°-30° C (59°-86° F) (See USP Controlled Room Temperature).Trimethoprim Tablets USP, 100 mg are scored, oval-shaped, white tablets imprinted “DAN DAN” and “5571” supplied in bottles of 100.Dispense in a tight, light-resistant container with child-resistant closure.Store at controlled room temperature 15°-30°C (59°-86°F) in a dry place.Trimethoprim Tablets USP, 100 mg are scored, oval-shaped, white tablets imprinted “DAN DAN” and “5571” supplied in bottles of 100.Dispense in a tight, light-resistant container with child-resistant closure.Store at controlled room temperature 15°-30°C (59°-86°F) in a dry place.Trimethoprim Tablets USP, 100 mg are scored, oval-shaped, white tablets imprinted “DAN DAN” and “5571” supplied in bottles of 100.Dispense in a tight, light-resistant container with child-resistant closure.Store at controlled room temperature 15°-30°C (59°-86°F) in a dry place.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Trimethoprim is rapidly absorbed following oral administration. It exists in the blood as unbound, protein-bound and metabolized forms. Ten to twenty percent of trimethoprim is metabolized, primarily in the liver; the remainder is excreted unchanged in the urine. The principal metabolites of trimethoprim are the 1- and 3-oxides and the 3'- and 4'-hydroxy derivatives. The free form is considered to be the therapeutically active form. Approximately 44% of trimethoprim is bound to plasma proteins.
Mean peak plasma concentrations of approximately 1.0 mcg/mL occur 1 to 4 hours after oral administration of a single 100 mg dose. A single 200 mg dose will result in serum levels approximately twice as high. The half-life of trimethoprim ranges from 8 to 10 hours. However, patients with severely impaired renal function exhibit an increase in the half-life of trimethoprim, which requires either dosage regimen adjustment or not using the drug in such patients (see). During a 13-week study of trimethoprim administered at a daily dosage of 200 mg (50 mg q.i.d.), the mean minimum steady-state concentration of the drug was 1.1 mcg/mL. Steady-state concentrations were achieved within 2 to 3 days of chronic administration, and were maintained throughout the experimental period.
Excretion of trimethoprim is primarily by the kidneys through glomerular filtration and tubular secretion. Urine concentrations of trimethoprim are considerably higher than are the concentrations in the blood. After a single oral dose of 100 mg, urine concentrations of trimethoprim ranged from 30 to 160 mcg/mL during the 0- to 4-hour period and declined to approximately 18 to 91 mcg/mL during the 8- to 24-hour period. A 200 mg single oral dose will result in trimethoprim urine levels approximately twice as high. After oral administration, 50% to 60% of trimethoprim is excreted in the urine within 24 hours, approximately 80% of this being unmetabolized trimethoprim.
Since normal vaginal and fecal flora are the source of most pathogens causing urinary tract infections, it is relevant to consider the distribution of trimethoprim into these sites. Concentrations of trimethoprim in vaginal secretions are consistently greater than those found simultaneously in the serum, being typically 1.6 times the concentrations of simultaneously obtained serum samples. Sufficient trimethoprim is excreted in the feces to markedly reduce or eliminate trimethoprim-susceptible organisms from the fecal flora.
Trimethoprim also passes the placental barrier and is excreted in human milk.
Microbiology
Trimethoprim blocks the production of tetrahydrofolic acid from dihydrofolic acid by binding to and reversibly inhibiting the required enzyme, dihydrofolate reductase. This binding is much stronger for the bacterial enzyme than for the corresponding mammalian enzyme. Thus, trimethoprim selectively interferes with bacterial biosynthesis of nucleic acids and proteins.
In vitro
Pseudomonas aeruginosa.
The dominant non-fecal organisms, spp. and spp., are not susceptible to trimethoprim concentrations obtained with the recommended dosage.
Susceptibility Tests:
Dilution Techniques:
A report of “Susceptible” indicates that the pathogen is likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where high dosage of drug can be used. This category also provides a buffer zone which prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the pathogen is not likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable; other therapy should be selected.
Standardized susceptibility test procedures require the use of laboratory control microorganisms to control the technical aspects of the laboratory procedures. Standard trimethoprim powder should provide the following MIC values:
Diffusion Techniques:
Reports from the laboratory providing results of the standard single-disk susceptibility test with a 5 mcg trimethoprim disk should be interpreted according to the following criteria:
Interpretation should be as stated above for results using dilution techniques. Interpretation involves correlation of the diameter obtained in the disk test with the MIC for trimethoprim.
As with standardized dilution techniques, diffusion methods require the use of laboratory control microorganisms that are used to control the technical aspects of the laboratory procedures. For the diffusion technique, the 5 mcg trimethoprim disk should provide the following zone diameters in these laboratory test quality control strains.
Non-Clinical Toxicology
Trimethoprim tablets are contraindicated in individuals hypersensitive to trimethoprim and in those with documented megaloblastic anemia due to folate deficiency.Serious hypersensitivity reactions have been reported rarely in patients on trimethoprim therapy. Trimethoprim has been reported rarely to interfere with hematopoiesis, especially when administered in large doses and/or for prolonged periods.
The presence of clinical signs such as sore throat, fever, pallor or purpura may be early indications of serious blood disorders (see). Complete blood counts should be obtained if any of these signs are noted in a patient receiving trimethoprim and the drug discontinued if a significant reduction in the count of any formed blood element is found.
(A) The risk of myopathy and rhabdomyolysis is increased with combined gemfibrozil and HMG-CoA reductase inhibitor therapy (see). Myopathy or rhabdomyolysis with or without acute renal failure have been reported as early as three weeks after initiation of combined therapy or after several months (refs. 8, 9, 10, 11). (See) There is no assurance that periodic monitoring of creatine kinase will prevent the occurrence of severe myopathy and kidney damage.
(B) CAUTION SHOULD BE EXERCISED WHEN ANTICOAGULANTS ARE GIVEN IN CONJUNCTION WITH GEMFIBROZIL. THE DOSAGE OF THE ANTICOAGULANT SHOULD BE REDUCED TO MAINTAIN THE PROTHROMBIN TIME AT THE DESIRED LEVEL TO PREVENT BLEEDING COMPLICATIONS. FREQUENT PROTHROMBIN DETERMINATIONS ARE ADVISABLE UNTIL IT HAS BEEN DEFINITELY DETERMINED THAT THE PROTHROMBIN LEVEL HAS STABILIZED.
(C) data from a study that evaluated the co-administration of gemfibrozil with repaglinide in healthy subjects resulted in a significant increase in repaglinide blood levels. Patients taking repaglinide should not start taking gemfibrozil; patients taking gemfibrozil should not start taking repaglinide. Concomitant use may result in enhanced and prolonged blood glucose-lowering effects of repaglinide. Caution should be used in patients already on repaglinide and gemfibrozil – blood glucose levels should be monitored and repaglinide dose adjustment may be needed. Rare post marketing events of serious hypoglycemia have been reported in patients taking repaglinide and gemfibrozil together. In this same study, gemfibrozil and itraconazole had a synergistic metabolic inhibitory effect on repaglinide. Therefore, patients taking repaglinide and gemfibrozil should not take itraconazole.
Trimethoprim should be given with caution to patients with possible folate deficiency. Folates may be administered concomitantly without interfering with the antibacterial action of trimethoprim. Trimethoprim should also be given with caution to patients with impaired renal or hepatic function (see and).
The adverse effects encountered most often with trimethoprim were rash and pruritus.
Dermatologic
Rash, pruritus, and phototoxic skin eruptions. At the recommended dosage regimens of 100 mg b.i.d. or 200 mg q.d. each for 10 days, the incidence of rash is 2.9% to 6.7%. In clinical studies which employed high doses of trimethoprim, an elevated incidence of rash was noted. These rashes were maculopapular, morbilliform, pruritic, and generally mild to moderate, appearing 7 to 14 days after the initiation of therapy.
Hypersensitivity
Rare reports of exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell Syndrome), and anaphylaxis have been received.
Gastrointestinal
Epigastric distress, nausea, vomiting, and glossitis. Elevation of serum transaminase and bilirubin has been noted, but the significance of this finding is unknown. Cholestatic jaundice has been rarely reported.
Hematologic
Thrombocytopenia, leukopenia, neutropenia, megaloblastic anemia, and methemoglobinemia.
Metabolic
Hyperkalemia, hyponatremia.
Neurologic
Aseptic meningitis has been rarely reported.
Miscellaneous
Fever, and increases in BUN and serum creatinine levels.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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