Antibiotic (trimethoprim and sulfonamide combination
in a 1:5 ratio)
Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, Nocardia asteroides, Mycobacterium fortuitum, Escherichia coli, Shigella dysenteriae, Salmonella enterica, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Proteus mirabilis, Stenotrophomonas maltophilia, Haemophilus influenzae, Pasteurella multocida, Bordetella pertussis, Brucella melitensis, Neisseria gonorrhoeae, Neisseria meningitidis
Sulfamethoxazole inhibits the synthesis of
dihydrofolic acid. Trimethoprim inhibits thymidine and DNA synthesis. These two
agents act synergistically in inhibiting folic acid synthesis.
Exhibits time-dependent bactericidal activity
Cmax: 1-2mcg/mL (TMP); 25-60mcg/mL (SMX); Half-life: 10-12 hours (TMP and SMX); Volume of distribution: 100-120 L (TMP); 12-18 L (SMX); Table 7
GI – nausea, vomiting
Hematologic – pancytopenia, agranulocytosis, anemia,
thrombocytopenia
Skin – toxic erythema, erythema nodosum, fixed local eruption, erythema multiforme, Lyell’s syndrome, exfoliative dermatitis, urticaria, necrotizing vasculitis, photodermatitis
Renal – transient blood urea and creatinine
elevations, crystalluria, acute interstitial nephritis
CNS – headache, confusion, depression, aseptic
meningitis
Electrolytes – Hyperkalemia (increased risk with
higher doses, in patients with renal insufficiency, and/or receiving potassium
sparing diuretics, ACE inhibitors, or ARBs)
Increased risk of adverse effects in the elderly
Dosage: The 1:5 ratio (TMP:SMX) remains constant in
all dosage forms
Oral: Tablets Single strength (SS: 80/mg/400mg
TMP/SMX)
Double strength (DS: 160mg/800mg TMP/SMX)
Liquid (suspension) 40mg / 200mg TMP/SMX per 5ml
Parenteral: Vial 5ml: Single strength (80mg/400mg
TMP/SMX)
10ml: Double strength (160mg/800mg TMP/SMX)
30ml: Six times strength (480mg/2400mg TMP/SMX)
Acute exacerbation of chronic bronchitis: 1 DS TMP/SMX PO q12h×14days
Pneumocystis jirovecii pneumonia:
2 DS TMP/SMX PO/IV q6h×14-21days
Pneumocystis jirovecii
prophylaxis: 1DS TMP/SMX PO daily
Pulmonary nocardiosis: 160 mg/800mg TMP/SMX IV q6h or
2 DS TMP/SMX PO q12h
Traveler’s diarrhea: 1DS TMP/SMX PO q12h×5days
Uncomplicated cystitis in women: 1DS TMP/SMX PO
q12h×3 days
Urinary tract infection (other):1 DS TMP/SMX PO
q12h×10-14days
Stenotrophomonas infections: 2 DS TMP/SMX IV q12h
Staphylococcus aureus cellulitis: 1-2 DS TMP/SMX PO
q12h×10-14days
Urinary Tract Infections (10 days duration) or Middle Ear Infections (5 days duration)
The recommended dosage for children 2
months of age or older, given every 12 hours, is determined by weight.
10kg (22 pounds), 1 teaspoonful (5 ml)
20kg (44 pounds), 2 teaspoonfuls (10 ml) or 1 SS tablet
30kg (66 pounds), 3 teaspoonfuls (15 ml) or 1.5SS tablet
40kg (88 pounds), 4 teaspoonfuls (20 ml) or 2 SS or 1 DS tablet
Pneumocystis jirovecii Pneumonia
The recommended doses, taken every 6 hours for 14 to 21 days, are determined by weight. Liquid (suspension) formulation 40mg/200mg TMP/SMX per 5ml
8.2kg (18 pounds), 1 teaspoonful (5
ml)
16kg (35 pounds), 2 teaspoonfuls (10 ml) or 1 SS tablet
24.1kg (53 pounds), 3 teaspoonfuls (15 ml) or 1.5 SStablet
32.3kg (70 pounds), 4 teaspoonfuls (20 ml) or 2 SS or 1 DS tablet
Pneumocystis jirovecii Pneumonia prophylaxis
The dose is determined by body surface area. The dose
is given twice a day, on 3 consecutive days per week. The total dose should not
exceed TMP/SMX = 320mg /1600mg. The safety of repeated use of
TMP/SMX in children under 2 years of age has not been established.
Renal failure: CrCl < 30 mL/min: half of
the usual daily dose should be administered
CrCl < 15 mL/min: TMP serum levels may be monitored
Hemodialysis: Metabolites of TMP and SMX may
accumulate. Half of the maintenance dose is recommended to be administered after
hemodialysis
Hepatic failure: No dosage adjustment
necessary.
Contraindications/Warnings/Precautions
Contraindications: Pregnant patients at term, nursing
mothers, megaloblastic anemia due to folate deficiency
Precautions: should not be used to treat necrotizing group A beta-hemolytic strep infections, patients with possible folate deficiency, severe allergies, asthma, or glucose-6-phosphate dehydrogenase deficiency, elderly patients. Persons with AIDS; have a higher risk for leucopenia and rash.
Other diaminopyrimidines-pyrimethamine, azathioprine,
or methotrexate are potentiated by TMP, resulting in severe leukopenia.
Sulfonamides displace warfarin from binding albumin,
thus increasing its serum level. SMX inhibits the clearance of phenytoin,
prolonging its half-life.
Category C: Risk unknown. Human studies inadequate.
Therapeutic: Monitor signs and symptoms of
infection. Monitor white blood cell count, culture and sensitivity report.
Toxic: Monitor renal function tests, serum potassium.
Brand names/Manufacturer:
Bactrim/Roche; Septra /Aspen Pharmacare; Sulfatrim/Alpharma;
Co-trimoxazole/Sandoz; available as generic