Overview
Trimethoprim is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), a critical enzyme that catalyzes the formation of tetrahydrofolic acid (THF) - in doing so, it prevents the synthesis of bacterial DNA and ultimately continued bacterial survival. Trimethoprim is often used in combination with sulfamethoxazole due to their complementary and synergistic mechanisms but may be used as a monotherapy in the treatment and/or prophylaxis of urinary tract infections. It is structurally and chemically related to pyrimethamine, another antifolate antimicrobial used in the treatment of plasmodial infections.
Background
Trimethoprim is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), a critical enzyme that catalyzes the formation of tetrahydrofolic acid (THF) - in doing so, it prevents the synthesis of bacterial DNA and ultimately continued bacterial survival. Trimethoprim is often used in combination with sulfamethoxazole due to their complementary and synergistic mechanisms but may be used as a monotherapy in the treatment and/or prophylaxis of urinary tract infections. It is structurally and chemically related to pyrimethamine, another antifolate antimicrobial used in the treatment of plasmodial infections.
Indication
As a monotherapy, trimethoprim is indicated for the treatment of acute episodes of uncomplicated urinary tract infections caused by susceptible bacteria, including E. coli., K. pneumoniae, Enterobacter spp., P. mirabilis, and coagulase-negative Staphylococcus species. In various formulations in combination with sulfamethoxazole, trimethoprim is indicated for the following infections caused by bacteria with documented susceptibility: urinary tract infections, acute otitis media in pediatric patients (when clinically indicated), acute exacerbations of chronic bronchitis in adults, enteritis caused by susceptible Shigella, prophylaxis and treatment of Pneumocystis jiroveci pneumonia, and travelers' diarrhea caused by enterotoxigenic E. coli. Trimethoprim is available as an ophthalmic solution in combination with polymyxin B for the treatment of acute bacterial conjunctivitis, blepharitis, and blepharoconjunctivitis caused by susceptible bacteria.
Associated Conditions
- Acute Exacerbation of Chronic Bronchitis (AECB) caused by susceptible bacteria
- Acute Otitis Media caused by susceptible bacteria
- Bacterial Conjunctivitis caused by susceptible bacteria
- Blepharoconjunctivitis caused by susceptible bacteria
- Brucellosis
- Dysentery, Bacillary
- Nocardiosis
- Pneumocystis Jirovecii Pneumonia
- Urinary Tract Infection caused by susceptible bacteria
- Bacterial blepharitis caused by susceptible bacteria
- Susceptible Cholera
- Susceptible Enteritis infectious caused by Shigella flexneri
- Susceptible Enteritis infectious caused by Shigella sonnei
- Susceptible Travelers' Diarrhea caused by Enterotoxigenic E. Coli (ETEC) Infection
- Uncomplicated Urinary Tract Infection caused by susceptible bacteria
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/05/21 | Phase 4 | Recruiting | |||
2024/11/29 | Phase 4 | Recruiting | |||
2024/08/02 | Phase 2 | Not yet recruiting | |||
2022/06/14 | Phase 1 | Terminated | |||
2022/03/07 | Not Applicable | Recruiting | Leiden University Medical Center | ||
2020/03/13 | Not Applicable | Completed | |||
2019/04/18 | Phase 1 | Active, not recruiting | |||
2018/11/19 | Phase 4 | Completed | |||
2018/04/05 | Phase 2 | Active, not recruiting | |||
2017/08/01 | Phase 4 | Completed | Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| A-S Medication Solutions | 50090-5679 | ORAL | 160 mg in 1 1 | 6/29/2021 | |
| Aurobindo Pharma Limited | 65862-496 | ORAL | 40 mg in 5 mL | 3/12/2024 | |
| A-S Medication Solutions | 50090-2198 | ORAL | 160 mg in 1 1 | 6/3/2021 | |
| NuCare Pharmaceuticals,Inc. | 68071-4431 | ORAL | 160 mg in 1 1 | 2/16/2021 | |
| New Horizon Rx Group, LLC | 58517-140 | ORAL | 160 mg in 1 1 | 12/30/2013 | |
| Department of State Health Services, Pharmacy Branch | 55695-008 | ORAL | 160 mg in 1 1 | 3/11/2016 | |
| Mayne Pharma | 51862-486 | ORAL | 100 mg in 1 1 | 2/16/2021 | |
| AvKARE | 42291-758 | ORAL | 80 mg in 1 1 | 1/10/2024 | |
| A-S Medication Solutions | 50090-6901 | ORAL | 160 mg in 1 1 | 12/27/2022 | |
| Redpharm Drug | 67296-1904 | ORAL | 160 mg in 1 1 | 11/27/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| APO-SULFATRIM PEDIATRIC TABLET | SIN00508P | TABLET | 20 mg | 4/28/1988 | |
| MORTIN TABLET | SIN10251P | TABLET | 80 mg | 10/10/1998 | |
| MORTIN-DS TABLET | SIN10250P | TABLET | 160 mg | 10/10/1998 | |
| APO-SULFATRIM TABLET | SIN00435P | TABLET | 80 mg | 4/27/1988 | |
| SUPRIM B.P. 480 TABLET | SIN02308P | TABLET | 80.00 mg | 8/30/1988 | |
| B.S. SUSPENSION | SIN00526P | SUSPENSION | 40 mg/5 ml | 4/28/1988 | |
| CO-TRIMEXAZOLE SUSPENSION | SIN00583P | SUSPENSION | 40 mg/5 ml | 4/29/1988 | |
| SUPRIM SUSPENSION | SIN01417P | SUSPENSION | 40 mg/5 ml | 5/20/1988 | |
| B.S. TABLET | SIN00960P | TABLET | 80 mg | 5/10/1988 | |
| DBL SULFAMETHOXAZOLE 400MG AND TRIMETHOPRIM 80MG CONCENTRATE INJECTION BP | SIN02183P | INJECTION | 16mg/mL | 6/30/1988 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Trimethoprim Injection | 国药准字H11022418 | 化学药品 | 注射剂(小容量注射剂) | 11/27/2020 | |
| Trimethoprim Injection | 国药准字H14024020 | 化学药品 | 注射剂 | 9/9/2020 | |
| Trimethoprim Injection | 国药准字H13023829 | 化学药品 | 注射剂 | 9/3/2020 | |
| Trimethoprim Injection | 国药准字H45021201 | 化学药品 | 注射剂 | 9/30/2020 | |
| Trimethoprim Injection | 国药准字H20066385 | 化学药品 | 注射剂 | 8/19/2020 | |
| Trimethoprim Injection | 国药准字H41024817 | 化学药品 | 注射剂 | 3/5/2024 | |
| Trimethoprim Injection | 国药准字H13023860 | 化学药品 | 注射剂 | 10/27/2020 | |
| Trimethoprim Injection | 国药准字H31022556 | 化学药品 | 注射剂 | 8/21/2020 | |
| Trimethoprim Tablets | 国药准字H42020551 | 化学药品 | 片剂 | 9/4/2020 | |
| Trimethoprim Tablets | 国药准字H61020720 | 化学药品 | 片剂 | 6/5/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| RESPRIM trimethoprim/sulfamethoxazole 80 mg/400 mg tablet blister pack | 17681 | Medicine | A | 9/20/1991 | |
| Septrin Sugar-free Paediatric Suspension | 11000 | Medicine | A | 8/2/1991 | |
| BACTRIM DS tablet blister pack | 162563 | Medicine | A | 7/8/2009 | |
| SEPTRIN FORTE trimethoprim/sulfamethoxazole 160/800 mg tablet blister pack | 10998 | Medicine | A | 8/2/1991 | |
| SEPTRIN trimethoprim/sulfamethoxazole 80/400 tablet blister pack | 15336 | Medicine | A | 9/5/1991 | |
| TRIMETHOPRIM-WGR trimethoprim 300 mg tablet bottle | 431671 | Medicine | A | 5/31/2024 | |
| RESPRIM FORTE trimethoprim/sulfamethoxazole 160 mg/800 mg tablet blister pack | 17682 | Medicine | A | 9/20/1991 | |
| SEPTRIN trimethorim/sulfazmethoxazole 80/400 mg tablet bottle | 11001 | Medicine | A | 8/2/1991 | |
| DBL SULFAMETHOXAZOLE 400 mg and TRIMETHOPRIM 80 mg/5 mL concentrated injection ampoule | 16293 | Medicine | A | 10/8/1991 | |
| BACTRIM 400/80 sulfamethoxazole 400 mg/5 mL and trimethoprim 80 mg/5mL concentrate for solution for infusion ampoulee | 367590 | Medicine | A | 8/31/2022 |