Names and pronunciation
(sul-fa-meth-ox′a-zole-trye- meth′oh-prim) Bactrim, Bactrim DS, Septra, Septra DS, SMZ/TMP, Sulfatrim, Sulfatrim Pediatric , Novo-Trimel , Nu-Cotrimox , Septra Pediatric
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Drug reference
(sul-fa-meth-ox′a-zole-trye- meth′oh-prim) Bactrim, Bactrim DS, Septra, Septra DS, SMZ/TMP, Sulfatrim, Sulfatrim Pediatric , Novo-Trimel , Nu-Cotrimox , Septra Pediatric
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Func. class.: Antiinfective
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Chem. class.: Sulfonamide— miscellaneous
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ACTION: Sulfamethoxazole (SMZ) interferes with the bacterial biosynthesis of proteins by competitive antagonism of PABA when adequate levels are main- tained; trimethoprim (TMP) blocks the synthesis of tetrahydrofolic acid; the combination blocks 2 consecutive steps in the bacterial synthesis of essential nucleic acids and protein
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USES: UTI, otitis media, acute and chronic prostatitis, shigellosis, chancroid, traveler’s diarrhea, Enterobacter sp., Escherichia coli, Haemophilus influenzae (beta-lactamase negative), Haemophilus influenzae (beta-lacta- mase positive), Klebsiella sp., Morgan- ella morganii, Pneumocystis carinii, Pneumocystis jiroveci, Proteus mirabi- lis, Proteus sp., Proteus vulgaris, Shi- gella flexneri, Shigella sonnei, Strepto- coccus pneumoniae; may also be effective for Acinetobacter baumannii, Actinomadura madurae, Actinomad- ura pelletieri, Bordetella pertussis, Bur- kholderia pseudomallei, Cyclospora cayetanensis, Haemophilus ducreyi, Isospora belli, Klebsiella granulomatis, Legionella micdadei, Legionella pneu- mophila, Listeria monocytogenes, Moraxella catarrhalis, Neisseria gonor- rhoeae, Nocardia asteroides, Nocardia brasiliensis, Nocardia otitidiscaviarum, Pediculus capitis, Plasmodium falci- parum, Providencia sp., Salmonella sp., Serratia sp., Shigella sp., Staphylococ- cus aureus (MRSA), Staphylococcus aureus (MSSA), Staphylococcus epider- midis, Stenotrophomonas maltophilia, Streptococcus pyogenes (group A beta- hemolytic streptococci), Streptomyces somaliensis, Toxoplasma gondii, Vibrio cholerae, viridans streptococci, Yersinia enterocolitica
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CONTRAINDICATIONS: Breast- feeding, infants <2 mo; hypersensitivity to trimethoprim or sulfonamides; preg- nancy at term, megaloblastic anemia, CCr <15 mL/min Precautions: Pregnancy, geriatric patients, infants, renal disease, G6PD deficiency, impaired hepatic/renal func- tion, possible folate deficiency, severe allergy, bronchial asthma, UV expo- sure, porphyria, hyperkalemia, hypothy- roidism
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SIDE EFFECTS CNS: Headache, insomnia, hallucinations, depression, vertigo, fatigue, anxiety, sei- zures, drug fever, chills, aseptic meningitis CV: Allergic myocarditis EENT: Tinnitus GI: Nausea, vomiting, abdominal pain, stomatitis, hepatitis, glossitis, pancreati- tis, diarrhea, enterocolitis, anorexia, CDAD GU: Renal failure, toxic nephrosis; in- creased BUN, creatinine; crystalluria HEMA: Leukopenia, neutropenia, throm- bocytopenia, agranulocytosis, hemolytic anemia, hypoprothrombinemia, Henoch- Schönlein purpura, methemoglobinemia, eosinophilia INTEG: Rash, dermatitis, urticaria, Stevens- Johnson syndrome, erythema, photosensi- tivity, pain, inflammation at inj site, toxic epidermal necrolysis, erythema multiforme RESP: Cough, SOB SYST: Anaphylaxis, SLE S
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INTERACTIONS Increase: thrombocytopenia—thiazide diuretics Increase: potassium levels—potassium- sparing diuretics, potassium supplements Increase: hypoglycemic response—sul- fonylurea agents Increase: anticoagulant effects—oral anticoagulants Increase: levels of dofetilide Increase: crystalluria—methenamine Increase: bone marrow depressant effects—methotrexate Decrease: hepatic clearance of phenyt- oin, CYP2C9, CYP3A4 inducers Decrease: response—cycloSPORINE Drug/Lab Test Increase: creatinine, bilirubin Decrease: HB, platelets
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DOSAGE AND ROUTES Based on TMP content Most infections • Adult/child >2 mo: PO/IV 6-12 mg TMP/kg/day divided q12hr UTI • Adult: PO 160 mg TMP q12hr × 10-14 days • Child: PO 8 mg/kg TMP/day in 2 di- vided doses q12hr (treatment): 2 mg/kg/ day (prophylaxis) Otitis media • Child: PO 8 mg/kg TMP/day in 2 di- vided doses q12hr × 10 days Chronic bronchitis • Adult: PO 160 mg TMP q12hr × 10-14 days Serious infections/Pneumocystis jiroveci pneumonitis • Adult/child: PO 15-20 mg/kg TMP daily in 4 divided doses q6hr × 14-21 days; IV 15-20 mg/kg/day (based on TMP) in 3-4 divided doses for ≤14 days Renal dose • Adult: PO CCr >30 mL/min, usual dose; CCr 15-30 mL/min, give 50% of usual dose; CCr <15 mL/min, not recommended
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Available forms: Tabs 20 mg TMP/100 SMX , 80 mg trimethoprim/400 mg sulfamethoxazole, 160 mg trimeth oprim/800 mg sulfamethoxazole; susp 40 mg-200 mg/5 mL, 160 mg-800 mg/20 mL; IV 16 mg/80 mg/mL
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Administer: PO route • Medication after C&S; repeat C&S after full course of medication • With resuscitative equipment, EPI- NEPHrine available; severe allergic reac- tions may occur • Without regard to meals • With full glass of water to maintain adequate hydration; increase fluids to 2 L/day to decrease crystallization in kid- neys • Store in tight, light-resistant container at room temperature Intermittent IV INFUSION route • After diluting 5 mL of product/125 mL D5W, run over 1-1½ hr, if using Septra ADD-Vantage vials dilute each 10-mL vial in ADD-Vantage diluent containers con- taining 250 mL of D5W, infuse over 60-90 min, change site q48-72hr Y-site compatibilities: Acyclovir, aldes- leukin, allopurinol, amifostine, amphotericin B cholesteryl, atracurium, aztreonam, cefepime, cyclophospha- mide, diltiaZEM, DOXOrubicin liposome, enalaprilat, esmolol, filgrastim, fludara- bine, gallium, granisetron, HYDROmor- phone, labetalol, LORazepam, magne- sium sulfate, melphalan, meperidine, morphine, pancuronium, perphenazine, piperacillin/tazobactam, remifentanil, sargramostim, tacrolimus, teniposide, thiotepa, vecuronium, zidovudine
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Assess: • I&O ratio; note color, character, pH of urine if product administered for UTI • Renal studies: BUN, creatinine, urinal- ysis with long-term therapy • Type of infection; obtain C&S before starting therapy • Blood dyscrasias, skin rash, fever, sore throat, bruising, bleeding, fatigue, joint pain • Allergic reaction: rash, dermatitis, ur- ticaria, pruritus, dyspnea, bronchospasm; product should be discontinued at 1st sign of rash; AIDS patients more suscep- tible, identify if patient has a sulfa allergy Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may be harmful to fetus, do not breastfeed
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Evaluate: • Therapeutic response: absence of pain, fever; C&S negative
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take each oral dose with full glass of water to prevent crystalluria; to drink 8-10 glasses of water/day; to take prod- uct on an empty stomach 1 hr before meals, 2 hr after meals, not to treat diar- rhea with OTC product, to notify health care professional if diarrhea lasts more than 2 days • To complete full course of treatment to prevent superinfection • To avoid sunlight; to use sunscreen to prevent burns • To avoid OTC medications (aspirin, vit C) unless directed by prescriber • To notify prescriber if skin rash, sore throat, fever, mouth sores, unusual bruis- ing, bleeding occur; to notify prescriber of CNS effects: anxiety, depression, hal- lucinations, seizures
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PHARMACOKINETICS PO: Rapidly absorbed; peak 1-4 hr; half-life 8-13 hr; excreted in urine (metabolites and unchanged), breast milk; crosses placenta; 68% bound to plasma proteins; TMP achieves high levels in prostatic tissue and fluid
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• Adult/child >2 mo: PO/IV 6-12 mg TMP/kg/day divided q12hr UTI
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• Adult: PO 160 mg TMP q12hr × 10-14 days
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• Adult: PO 160 mg TMP q12hr × 10-14 days Serious infections/Pneumocystis jiroveci pneumonitis
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• Adult/child: PO 15-20 mg/kg TMP daily in 4 divided doses q6hr × 14-21 days; IV 15-20 mg/kg/day (based on TMP) in 3-4 divided doses for ≤14 days Renal dose
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• Adult: PO CCr >30 mL/min, usual dose; CCr 15-30 mL/min, give 50% of usual dose; CCr <15 mL/min, not recommended
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