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Trimethoprim-sulfamethoxazole Combination of Trimethoprim Dihydrofolate reductase inhibitor (16.7%) Sulfamethoxazole Sulfonamide antibiotic (83.3%) Identifiers CAS number 8064-90-2 ATC code J01EE01 PubChem CID 358641 ChemSpider 318412 Therapeutic considerations Pregnancy cat. C(AU) C(US) Legal status ℞-only (US) Routes Oral  Y(what is this?)  (verify) Trimethoprim-sulfamethoxazole or Co-trimoxazole (abbreviated SXT, TMP-SMX, TMP-SMZ or TMP-sulfa) is a sulfonamide antibiotic combination of trimethoprim and sulfamethoxazole, in the ratio of 1 to 5, used in the treatment of a variety of bacterial infections. The name co-trimoxazole is the British Approved Name, and has been marketed worldwide under many trade names including Septra (GSK), Bactrim (Roche), and various generic preparations. Sources differ as to whether co-trimoxazole usually is bactericidal or bacteriostatic. Contents 1 Synergistic action 2 Clinical indications 2.1 HIV 2.2 Bacterial 2.3 Protozoan 2.4 Fungal 3 Safety 4 Trade names 5 References 6 Footnotes // Synergistic action The synergy between trimethoprim and sulphamethoxazole was first described in a series of in vitro and in vivo experiments published in the late 1960s.[1][2][3] Trimethoprim and sulfamethoxazole have a greater effect when given together than when given separately; the reason is because they inhibit successive steps in the folate synthesis pathway (see diagram below). It is unclear whether this synergy occurs at doses used in humans,[4] because, at the concentrations seen in blood and tissues, the ratio of trimethoprim to sulphamethoxazole is 1:20,[5] which is less than the 1:5 ratio needed in vitro for synergy to occur. Tetrahydrofolate synthesis pathway Sulfamethoxazole acts as a false-substrate inhibitor of dihydropteroate synthetase. Sulfonamides such as sulfamethoxazole are analogues of p-aminobenzoic acid (PABA) and, thus, are competitive inhibitors of the enzyme, inhibiting the production of dihydropteroic acid. Trimethoprim acts by interfering with the action of bacterial dihydrofolate reductase, inhibiting synthesis of tetrahydrofolic acid. Folic acid is an essential precursor in the de novo synthesis of the DNA nucleosides thymidine and uridine. Bacteria are unable to take up folic acid from the environment (i.e., the infection host) and, thus, are dependent on their own de novo synthesis - inhibition of the enzyme starves the bacteria of two bases necessary for DNA replication and transcription. Clinical indications Co-trimoxazole was claimed to be more effective than either of its components individually in treating bacterial infections, although this was later disputed.[6] Along with its associated greater incidence of adverse effects including allergic responses (see below), its widespread use has been restricted in many countries to very specific circumstances where its improved efficacy is demonstrated.[7] It may be effective in a variety of upper and lower respiratory tract infections, renal and urinary tract infections, gastrointestinal tract infections, skin and wound infections, septicaemias and other infections caused by sensitive organisms. The global problem of advancing antimicrobial resistance has led to a renewed interest in the use of co-trimoxazole in various settings more recently.[8] Specific indications for its use include: HIV Being an antibiotic, co-trimoxazole does not have any activity against HIV itself, but it is often prescribed to immunocompromised patients as Pneumocystis jiroveci pneumonia prophylaxis. Bacterial infections caused by Listeria monocytogenes, Nocardia spp., Stenotrophomonas maltophilia (Zanthomonas maltophilia) Staphylococcus saprophyticus infections presenting as urinary tract infection or cystitis melioidosis shigellosis Whipple's disease traveller's diarrhea Protozoan Isosporiasis[9] prophylaxis of cerebral toxoplasmosis in HIV patients Cyclospora cayetanensis Fungal treatment and prophylaxis of pneumonia caused by Pneumocystis jirovecii (formerly identified as P. carinii and commonly seen in immunocompromised patients including those suffering from cancer or HIV/AIDS) This article needs additional citations for verification. Please help improve this article by adding reliable references. Unsourced material may be challenged and removed. (September 2008) Safety There has been some concern about its use, however, since it has been associated with both frequent mild allergic reactions and serious adverse effects including Stevens-Johnson syndrome, myelosuppression, mydriasis, agranulocytosis, as well as severe liver damage (cholestatic hepatosis, hepatitis, liver necrosis, fulminant liver failure).[citation needed] Due to displacement of bilirubin from albumin, there is an increased risk of kernicterus in the newborn during the last 6 weeks of pregnancy. Also renal impairment up to acute renal failure and anuria have been reported. These side-effects are seen especially in the elderly and may be fatal. (Joint Formulary Committee, 2004). Both Folic acid and Folinic acid were found equally effective in reducing the adverse effects of TMP-SMX, so unless new evidence is found for Folinic acid that shows it is more effective than the cheaper Folic acid, Folic acid will continue to be the preferred treatment method. In some countries, co-trimoxazole has been withdrawn due to these toxic effects.[citation needed] Thus the current British Committee on Safety of Medicines (CSM) guidelines recommend limiting its use to:[citation needed] Pneumocystis pneumonia Toxoplasmosis and nocardiosis acute exacerbations of chronic bronchitis and infections of the urinary tract where there is good rationale for use acute otitis media in children where there is good rationale Trade names Co-trimoxazole is manufactured and sold by many different companies. Some of the brand names are listed here, but this list is not complete. Bactrim, Bactrimel (Roche) Cotrim Septrin, Septra (GlaxoSmithKline and formerly Burroughs Wellcome) Sulfatrim Biseptol References Rossi S, editor. Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook; 2004. ISBN 0-9578521-4-2. British National Formulary, 51st edition (April 20, 2006). London: British Medical Association and Royal Pharmaceutical Society of Great Britain; 2006. ISBN 0-85369-668-3 briandeer.com Newspaper campaign over adverse events; 1994- Footnotes ^ Bushby SRM, Hitchings GH (1968). "Trimethoprim, a sulphonamide potentiator". Brit J Pharmacol 33 (1): 72. PMID 5301731.  ^ Böhni E (1969). "Vergleichende bakteriologische untersuchungen mit der Kombination Trimethoprim/Sulfamethoxazole in vitro und in vivo". Chemotherapy 14 (Suppl): 1. doi:10.1159/000220651. PMID 4908562.  ^ Böhni E (1969). "Chemotherapeutic activity of the combination of trimethoprim and sulfamethoxazole in infections of mice". Postgrad Med J 45 (Suppl): 18. PMID 4902845.  ^ Brumfitt W, Hamilton-Miller JM (February 1994). "Limitations of and indications for the use of co-trimoxazole". J Chemother 6 (1): 3–11. PMID 8071675.  ^ Kremers P, Duvivier J, Heusghem C (1974). "Pharmacokinetic studies of co-trimoxazole in man after single and repeated doses". J Clin Pharmacol 14: 112–117.  ^ Brumfitt W, Hamilton-Miller JM (December 1993). "Reassessment of the rationale for the combinations of sulphonamides with diaminopyrimidines". J Chemother 5 (6): 465–9. PMID 8195839.  ^ "Co-trimoxazole use restricted". Drug Ther Bull 33 (12): 92–3. December 1995. doi:10.1136/dtb.1995.331292. PMID 8777892.  ^ Falagas ME, Grammatikos AP, Michalopoulos A (October 2008). "Potential of old-generation antibiotics to address current need for new antibiotics". Expert Rev Anti Infect Ther 6 (5): 593–600. doi:10.1586/14787210.6.5.593. PMID 18847400.  ^ Lagrange-Xélot M, Porcher R, Sarfati C, et al (February 2008). "Isosporiasis in patients with HIV infection in the highly active antiretroviral therapy era in France". HIV Med. 9 (2): 126–30. doi:10.1111/j.1468-1293.2007.00530.x. PMID 18257775. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=1464-2662&date=2008&volume=9&issue=2&spage=126.  v • d • e Antibacterials: nucleic acid inhibitors (J01E, J01M) Antifolates (inhibits purine metabolism, thereby inhibiting DNA and RNA synthesis) DR inhibitor 2,4-Diaminopyrimidine (Trimethoprim#, Brodimoprim, Tetroxoprim, Iclaprim†) Sulfonamides (DS inhibitor) Short- acting Sulfaisodimidine · Sulfamethizole · Sulfadimidine · Sulfapyridine · Sulfafurazole · Sulfanilamide (Prontosil) · Sulfathiazole · Sulfathiourea Intermediate- acting Sulfamethoxazole · Sulfadiazine# · Sulfamoxole Long- acting Sulfadimethoxine · Sulfalene · Sulfametomidine · Sulfametoxydiazine · Sulfamethoxypyridazine · Sulfaperin · Sulfamerazine · Sulfaphenazole · Sulfamazone Other/ungrouped sulfanilamide (Sulfacetamide, Sulfametrole) Combinations Sulfamethoxazole and trimethoprim# Topoisomerase inhibitors/ quinolones/ (inhibits DNA replication) 1st g. Cinoxacin‡ · Flumequine · Nalidixic acid · Oxolinic acid · Pipemidic acid · Piromidic acid · Rosoxacin Fluoro- quinolones 2nd g. Ciprofloxacin#  · Enoxacin‡ · Fleroxacin‡ · Lomefloxacin · Nadifloxacin · Ofloxacin · Norfloxacin · Pefloxacin · Rufloxacin 3rd g. Balofloxacin · Grepafloxacin‡ · Levofloxacin · Pazufloxacin · Sparfloxacin‡ · Temafloxacin‡ · Tosufloxacin 4th g. Besifloxacin · Clinafloxacin† · Garenoxacin · Gemifloxacin · Moxifloxacin · Gatifloxacin‡ · Sitafloxacin · Trovafloxacin‡/Alatrofloxacin‡ · Prulifloxacin Vet. Danofloxacin · Difloxacin · Enrofloxacin · Ibafloxacin · Marbofloxacin · Orbifloxacin · Pradofloxacin · Sarafloxacin Related (DG) Aminocoumarins: Novobiocin Anaerobic DNA inhibitors Nitro- imidazole derivatives Metronidazole#  · Tinidazole · Ornidazole Nitrofuran derivatives Nitrofurantoin#  · Furazolidone‡  · Nifurtoinol RNA synthesis Rifamycins/ RNA polymerase Rifampicin · Rifabutin · Rifapentine · Rifaximin #WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III M: BAC bact (clas) gr+f/gr+a(t)/gr-p(c)/gr-o drug(J1p, w, n, m, vacc) v • d • e Antiparasitics – antiprotozoal agents – Chromalveolate antiparasitics (P01) Alveo- late Apicom- plexa Conoidasida/ (Coccidiostats) Cryptosporidiosis thiazole (Nitazoxanide) Isosporiasis Co-trimoxazole# Toxoplasmosis Pyrimethamine • Sulfadiazine Aconoidasida Malaria Individual agents Hemozoin inhibitors Aminoquinolines (4-): Amodiaquine# • Chloroquine# (8-): Primaquine# • Pamaquine 4-methanolquinolines Mefloquine#• Quinine# • Quinidine Other Lumefantrine (combined with artemether as Coartem) Halofantrine Antifolates DHFR inhibitors (antifols) 2,4-Diaminopyrimidines (Pyrimethamine) biguanides (Proguanil# • Chlorproguanil) Sulfonamides Sulfadoxine • Sulfalene Combination Fansidar# (pyrimethamine-sulfadoxine) Sesquiterpene lactones Artemether# • Artesunate#• Dihydroartemisinin • Arteether/Artemotil • Artemisinin Other Atovaquone (always combined with proguanil as Malarone) Tetracycline • Doxycycline# Clindamycin Combi- nations Fixed-dose (coformulated) ACTs Coartem# • ASAQ (Coarsucam) • ASMQ • Duo-Cotecxin (Artekin) • Pyramax Combination therapies (not co-formulated) Quinine/tetracycline • Quinine/clindamycin • Artequin • Ariplus • Co-Arinate • CDA Babesiosis Clindamycin Cilio- phora Balantidiasis: Tetracycline Hetero- kont Blastocystosis: Metronidazole #WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III M: PRO ambz, excv, chrm (strc) ambz, excv, chrm ambz, excv, chrm