BACTRIM
GENERAL: take with food/liquids, stay well hydrated
1/2-life: 10h (SMX), 11h (TMP)
Peak Effect: 2-3h (SMX); 4h (TMP)
Excretion: 25% urinary unchanged (SMX); 40% to 75% urinary unchanged (TMP)
INDICATION: Proteus, E. coli, Klebsiella, Enterobacter, Morganella
MONITORING: Renal function tests if renal impairment. Renal function tests and CBC monitoring if on long term therapy.
MECHANISM: Inhibit formation of folate (tetrahydrofolic acid). SMX is similar to para-aminobenzoic acid (PABA) and competes to bind dihydropteroate synthetase which form dihydrofolic acid, an intermediate in folate synthesis.TMP inhibits bacterial dihydrofolate reeducates to inhibit late synthesis.
MEDICATION INTERACTIONS:
CONTRAINDICATIONS:
Sulfa allergy
Severe hepatic insufficiency or parenchymal damage
Severe renal insufficiency (CrCl less than 15 mL/min) when renal function status cannot be monitored
Drug-induced immune thrombocytopenia
Megaloblastic anemia secondary to folate deficiency and other blood dyscrasias or severe hematological disorders
Premature infants
Pregnancy or breastfeeding
In combination with dofetilide
Treatment of streptococcal pharyngitis
Infants less than 4 months of age (kernicterus)
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency of glucose-galactose malabsorption
Acute porphyria
WARNINGS/PRECAUTIONS:
May induce photosensitivity
Steven's Johnson
Teratogenic
Use with caution if thyroid dysfunction
Reported association w/ C. diff
Long term use may cause bone marrow depression
Hemolysis possible in dose related manner in glucose-6-phosphate dehydrogenase deficient patients
Trimethoprim induced reported hyperkalmeia
Hyponatremia can occur w/ TMP-SMX
Folate deficiency
Hypoglycemia
SIDE EFFECTS
VERY COMMON >10% : Hyperkalemia, headache
COMMON 1-10%: Rash, urticarial, diarrhea, nausea, vomiting, anorexia, thrush, acute kidney injury
RARE <0.1%: Thrombophlebitis, jaundice, rhabdomyolysis (mainly in AIDS patients)
VERY RARE <.01%: Polyarteritis nodosa, syncope, photosensitivity, Steven's Johnson Syndrome, constipation, glossitis, stomatitis, pseudomembranous colitis, pancreatitis, abdominal pain, bone marrow suppression, hepatitis, elevated LFT's, anaphylaxis, hypoglycemia, hyponatremia, metabolic acidosis, sseptic meningitis, convulsions, peripheral neuritis, ataxia, vertigo, dizziness, tremor, lethargy, paresthesia, convulsions, peripheral neuritis, tinnitus, uveitis, depression, hallucination, confusional state, agitation, anxiety, abnormal behavior, insomnia, nightmares, renal tubular acidosis, hematuria, renal failure, cough, dyspnea, lung infiltration, shortness of breath, wheezing, epistaxis
DOSAGE
ADULT: Double Strength (DS) is 800mg/160mg SMX-TMP
UTI -PO SMX-TMP DS q12h x10-14d
PYELONEPHRITIS: SMX-TMP DS po q12h x10-14d
UTI PROPHYLAXIS: SMX-TMP DS po q24h or 3x weekly at bedtime or postcoitally
PROSTATITIS: SMX-TMP DS po q12h x10-14d (acute) or x1-3mo (chronic)
PEDIATRIC:
UTI: 2 months or older:4 mg/kg po q12h x10-14d
RENAL DOSING:
CrCl < 15 mL/min - Contraindicated
CrCl 15 to 30 mL/min - 50% dose reduction
CrCl > 30 mL/min - No dose reduction
HEPATIC DOSING
Severe hepatic impairment - Contraindication
Mild to moderate hepatic impairment - Caution
DIALYSIS
Peritoneal dialysis not effective and HD somewhat effective in eliminating trimethoprim (TMP) and sulfamethoxazole (SMX). Give after HD because of this.
INTERESTING STUDIES
AKI from Bactrim - A retrospective study of 178,238 patients 65 yrs and over with a cumulative 422,514 UTI episodes treated with antibiotics showed trimethoprim has odds ratio of 1.72 for association with AKI in the 14 days after therapy compared w/ amoxicillin and OR of 2.27 for hyperkalemia. This suggests for 1000 UTI's treated with trimethoprim would result in 1-2 additional cases of hyperkalemia and 2 admissions with AKI, compared to amoxicillin. If patients were taking ARB/ACE and spironolactone, there were 18 additional cases of hyperkalemia and 11 admissions w/ AKI. There was no association with increase risk of death. (1)
GENERAL: take with food/liquids, stay well hydrated
1/2-life: 10h (SMX), 11h (TMP)
Peak Effect: 2-3h (SMX); 4h (TMP)
Excretion: 25% urinary unchanged (SMX); 40% to 75% urinary unchanged (TMP)
INDICATION: Proteus, E. coli, Klebsiella, Enterobacter, Morganella
MONITORING: Renal function tests if renal impairment. Renal function tests and CBC monitoring if on long term therapy.
MECHANISM: Inhibit formation of folate (tetrahydrofolic acid). SMX is similar to para-aminobenzoic acid (PABA) and competes to bind dihydropteroate synthetase which form dihydrofolic acid, an intermediate in folate synthesis.TMP inhibits bacterial dihydrofolate reeducates to inhibit late synthesis.
MEDICATION INTERACTIONS:
CONTRAINDICATIONS:
Sulfa allergy
Severe hepatic insufficiency or parenchymal damage
Severe renal insufficiency (CrCl less than 15 mL/min) when renal function status cannot be monitored
Drug-induced immune thrombocytopenia
Megaloblastic anemia secondary to folate deficiency and other blood dyscrasias or severe hematological disorders
Premature infants
Pregnancy or breastfeeding
In combination with dofetilide
Treatment of streptococcal pharyngitis
Infants less than 4 months of age (kernicterus)
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency of glucose-galactose malabsorption
Acute porphyria
WARNINGS/PRECAUTIONS:
May induce photosensitivity
Steven's Johnson
Teratogenic
Use with caution if thyroid dysfunction
Reported association w/ C. diff
Long term use may cause bone marrow depression
Hemolysis possible in dose related manner in glucose-6-phosphate dehydrogenase deficient patients
Trimethoprim induced reported hyperkalmeia
Hyponatremia can occur w/ TMP-SMX
Folate deficiency
Hypoglycemia
SIDE EFFECTS
VERY COMMON >10% : Hyperkalemia, headache
COMMON 1-10%: Rash, urticarial, diarrhea, nausea, vomiting, anorexia, thrush, acute kidney injury
RARE <0.1%: Thrombophlebitis, jaundice, rhabdomyolysis (mainly in AIDS patients)
VERY RARE <.01%: Polyarteritis nodosa, syncope, photosensitivity, Steven's Johnson Syndrome, constipation, glossitis, stomatitis, pseudomembranous colitis, pancreatitis, abdominal pain, bone marrow suppression, hepatitis, elevated LFT's, anaphylaxis, hypoglycemia, hyponatremia, metabolic acidosis, sseptic meningitis, convulsions, peripheral neuritis, ataxia, vertigo, dizziness, tremor, lethargy, paresthesia, convulsions, peripheral neuritis, tinnitus, uveitis, depression, hallucination, confusional state, agitation, anxiety, abnormal behavior, insomnia, nightmares, renal tubular acidosis, hematuria, renal failure, cough, dyspnea, lung infiltration, shortness of breath, wheezing, epistaxis
DOSAGE
ADULT: Double Strength (DS) is 800mg/160mg SMX-TMP
UTI -PO SMX-TMP DS q12h x10-14d
PYELONEPHRITIS: SMX-TMP DS po q12h x10-14d
UTI PROPHYLAXIS: SMX-TMP DS po q24h or 3x weekly at bedtime or postcoitally
PROSTATITIS: SMX-TMP DS po q12h x10-14d (acute) or x1-3mo (chronic)
PEDIATRIC:
UTI: 2 months or older:4 mg/kg po q12h x10-14d
RENAL DOSING:
CrCl < 15 mL/min - Contraindicated
CrCl 15 to 30 mL/min - 50% dose reduction
CrCl > 30 mL/min - No dose reduction
HEPATIC DOSING
Severe hepatic impairment - Contraindication
Mild to moderate hepatic impairment - Caution
DIALYSIS
Peritoneal dialysis not effective and HD somewhat effective in eliminating trimethoprim (TMP) and sulfamethoxazole (SMX). Give after HD because of this.
INTERESTING STUDIES
AKI from Bactrim - A retrospective study of 178,238 patients 65 yrs and over with a cumulative 422,514 UTI episodes treated with antibiotics showed trimethoprim has odds ratio of 1.72 for association with AKI in the 14 days after therapy compared w/ amoxicillin and OR of 2.27 for hyperkalemia. This suggests for 1000 UTI's treated with trimethoprim would result in 1-2 additional cases of hyperkalemia and 2 admissions with AKI, compared to amoxicillin. If patients were taking ARB/ACE and spironolactone, there were 18 additional cases of hyperkalemia and 11 admissions w/ AKI. There was no association with increase risk of death. (1)
KEFLEX
GENERAL
Food does not affect absorption significantly
Half-life: 0.5 to 2 hours
Excretion:
-Urine: Approximately 80% to 90% excreted as parent drug within 6 to 8 hoursFirst-generation cephalosporin
Report any loose stool/diarrhea w/in 2mo of taking keflex
Category B pregnancy
INDICATIONS:
G+ bacteria skin infection
UTI from E.coli, Proteus, Klebsiella, MSSA, also Streptococci Grp A,B,C,G, Strep Viridans, S. pneumoniae, H. influenzae
MONITORING: Prothrombin time if at high risk, renal function if CKD
MECHANISM
Bactericidal via bacterial cell wall synthesis inhibition by binding to penicillin binding proteins
CONTRAINDICATIONS:
History of major allergy to penicillins (AU)
Patients with porphyria (UK-some oral suspensions)
WARNINGS/PRECAUTIONS:
C. diff reported with nearly all ABX
Reports of drug induced acute intravascular hemolysis
Can cause positive direct Coomb's test
May prolong prothrombin time
May cause allergic reaction (rash, Steven's Johnson's syndrome)
Possible cross reactivity with penicillin allergies
May induce acute porphyria crisis
Possibly lowers seizure threshold, especially if reduced renal function
OK for breastfeeding, but does pass into breast milk and are reports of diarrhea and thrush in infants breastfeeding
SIDE EFFECTS
The most commonly reported side effects included diarrhea, dyspepsia, gastritis, nausea, and vomiting.
Other reported side effects include anal pruritis, some bone marrow suppression, rash, Steven's Johnson syndrome, hepatitis, elevated LFT's, genital pruritus, genital candidiasis, vulvovaginitis/vaginitis and vaginal discharges, seizure, dizziness, headache, agitation, confusion, hallucinations, arthralgia, arthritis, joint disorder, interstitial nephritis, renal dysfunction, toxic nephropathy, increased blood urea nitrogen, increased creatinine, hemorrhage,
DOSE
ADULT
Max dose: 4 g per day
SKIN/SOFT TISSUE INFECTION - 500mg po q6h x7-14d
CYSTITIS - 250mg po q6h or 500mg po q12h 3-7d
PROSTATITIS - 250mg po q6h or 500mg q12h x7-14d
PYELONEPHRITIS - 250mg po q6h or 500mg q12h x7-14d
PEDIATRICS
SKIN or SOFT TISSUE, CYSTITIS, PROSTATITIS, PYELONEPHRITIS - 12.5mg to 25mg/kg po q12h
CYSTITIS TREATMENT - 15mg/kg/dose q8h x7-14d
UTI PROPHYLAXIS - 10mg/kg daily
RENAL DOSING
CrCl 30-59ml/min - max dose 1g po qd
CrCl 15-29ml/min - max dose 250mg po q8-12h
CrCl 5-14ml/min - max dose 250mg po qd
CrCl 1-4ml/min - max dose 250mg po q48-60h
DIALYSIS
unknown*
GENERAL
Food does not affect absorption significantly
Half-life: 0.5 to 2 hours
Excretion:
-Urine: Approximately 80% to 90% excreted as parent drug within 6 to 8 hoursFirst-generation cephalosporin
Report any loose stool/diarrhea w/in 2mo of taking keflex
Category B pregnancy
INDICATIONS:
G+ bacteria skin infection
UTI from E.coli, Proteus, Klebsiella, MSSA, also Streptococci Grp A,B,C,G, Strep Viridans, S. pneumoniae, H. influenzae
MONITORING: Prothrombin time if at high risk, renal function if CKD
MECHANISM
Bactericidal via bacterial cell wall synthesis inhibition by binding to penicillin binding proteins
CONTRAINDICATIONS:
History of major allergy to penicillins (AU)
Patients with porphyria (UK-some oral suspensions)
WARNINGS/PRECAUTIONS:
C. diff reported with nearly all ABX
Reports of drug induced acute intravascular hemolysis
Can cause positive direct Coomb's test
May prolong prothrombin time
May cause allergic reaction (rash, Steven's Johnson's syndrome)
Possible cross reactivity with penicillin allergies
May induce acute porphyria crisis
Possibly lowers seizure threshold, especially if reduced renal function
OK for breastfeeding, but does pass into breast milk and are reports of diarrhea and thrush in infants breastfeeding
SIDE EFFECTS
The most commonly reported side effects included diarrhea, dyspepsia, gastritis, nausea, and vomiting.
Other reported side effects include anal pruritis, some bone marrow suppression, rash, Steven's Johnson syndrome, hepatitis, elevated LFT's, genital pruritus, genital candidiasis, vulvovaginitis/vaginitis and vaginal discharges, seizure, dizziness, headache, agitation, confusion, hallucinations, arthralgia, arthritis, joint disorder, interstitial nephritis, renal dysfunction, toxic nephropathy, increased blood urea nitrogen, increased creatinine, hemorrhage,
DOSE
ADULT
Max dose: 4 g per day
SKIN/SOFT TISSUE INFECTION - 500mg po q6h x7-14d
CYSTITIS - 250mg po q6h or 500mg po q12h 3-7d
PROSTATITIS - 250mg po q6h or 500mg q12h x7-14d
PYELONEPHRITIS - 250mg po q6h or 500mg q12h x7-14d
PEDIATRICS
SKIN or SOFT TISSUE, CYSTITIS, PROSTATITIS, PYELONEPHRITIS - 12.5mg to 25mg/kg po q12h
CYSTITIS TREATMENT - 15mg/kg/dose q8h x7-14d
UTI PROPHYLAXIS - 10mg/kg daily
RENAL DOSING
CrCl 30-59ml/min - max dose 1g po qd
CrCl 15-29ml/min - max dose 250mg po q8-12h
CrCl 5-14ml/min - max dose 250mg po qd
CrCl 1-4ml/min - max dose 250mg po q48-60h
DIALYSIS
unknown*
- Tulane University School of Medicine. http://tmedweb.tulane.edu/pharmwiki/doku.php/cephalosporins
MACROBID
GENERAL
Half-life: 0.7 to 1.7 hours
Excretion: 40% to 45% urinary
Take with food
May cause dizziness or drowsiness
Do not use antacids with magnesium trisilicate while on macrobid
May turn urine brown
If loose stools or diarrhea develops, discontinue and notify prescribing physician
Category B for pregnancy
MECHANISM: Inactivates ribosomal proteins
INDICATION: Lower urinary tract infections from: S aureus, group D Streptococci, Viridans group streptococci, S agalactiae, Citrobacter, Klebsiella, and coagulase negative staphylococci.
CONTRAINDICATIONS:
Pregnant** at end of term due to hemolytic anemia from glutathione system immaturity
Breastfeeding <3mo or any age w/ G6PD deficiency
<3 mo in age due to hemolytic anemia from glutathione system immaturity
Anuria, oliguria, or significant renal dysfunction CrCl < than 60 mL/min (some sources as low as 45ml/min)
G6PD) deficiency
Acute porphyria
MONITORING
Long term: periodic LFT's, renal function tests, pulmonary function
DRUG INTERACTIONS:
Reduced absorption with antacids containing magnesium trisilicate.
Uricosuric drugs (e.g., probenecid, sulfinpyrazone) inhibit renal tubular secretion resulting in increased toxicity with decreased urine macrobid levels
WARNINGS/PRECAUTIONS:
Meets BEERS CRITERIA for elderly adults
C. diff reports (as nearly all ABX)
Brown discoloration of the urine.
Hemolytic Anemia: hemolysis in G6PD deficiency found in ~10 percent of Blacks and a small percentage of ethnic groups of Mediterranean and Near-Eastern origin.
Hepatitis, cholestatic jaundice
Peripheral neuropathy (including optic neuritis), possibly severe or irreversible w/ increased risk if: CrCl <60mL/min, anemia, diabetes, electrolyte imbalance, vitamin B deficiency, and/or debilitating disease.
Pulmonary fibrosis
Reduced sperm count and testicular histology abnormality association
SIDE EFFECTS
COMMON (1-10%): Nausea, emesis, anorexia, flatulence, headache,
UNCOMMON (<1%): Abdominal pain, diarrhea, dyspepsia, constipation, dizziness, drowsiness, blurry vision, fevers, chills, mailase, acute pulmonary hypersensitivity reaction
RARE (<0.1%): Exfoliative dermatitis, erythema multiforme (including Stevens-Johnson syndrome), parotitis, pseudomembranous colitis, cyanosis secondary to methemoglobinemia, aplastic anemia, hepatitis, vertigo, pseudotumor cerebri, optic neuritis, intraretinal crystals causing retinopathy, bulging fontanels, acute interstitial nephritis, cyanosis
VERY RARE (<0.01%):
UNKNOWN PREVALENCE: ST changes, alopecia, dark urine, hemolytic anemia, bone marrow suppression, neuropathy, diplopia, nystagmus, arthralgia, myalgia, confusion, depression, psychotic reaction.
ADULT
CYSTITIS: Regular release: 50 to 100 mg po q6h x3-7d; Dual release: 100 mg po BID x7d
UTI PROPHYLAXIS: Regular release: 50 to 100 mg po qhs
PEDIATRIC
CYSTITIS: Regular release >3mo 5 to 7 mg/kg/day (up to 400 mg/day) po q6h x3-7d; Dual release >12yr: 100mg po bid x3-7d
UTI PROPHYLAXIS: >3mo 1 mg/kg/day (up to 100 mg/day) po qd or bid
RENAL DOSING: Do not give if CrCl <60ml/min. No special dosing necessary if >60ml/min.
DIALYSIS: Is dializable
HEPATIC DOSING: May need reduced dosing if hepatic dysfunction
GENERAL
Half-life: 0.7 to 1.7 hours
Excretion: 40% to 45% urinary
Take with food
May cause dizziness or drowsiness
Do not use antacids with magnesium trisilicate while on macrobid
May turn urine brown
If loose stools or diarrhea develops, discontinue and notify prescribing physician
Category B for pregnancy
MECHANISM: Inactivates ribosomal proteins
INDICATION: Lower urinary tract infections from: S aureus, group D Streptococci, Viridans group streptococci, S agalactiae, Citrobacter, Klebsiella, and coagulase negative staphylococci.
CONTRAINDICATIONS:
Pregnant** at end of term due to hemolytic anemia from glutathione system immaturity
Breastfeeding <3mo or any age w/ G6PD deficiency
<3 mo in age due to hemolytic anemia from glutathione system immaturity
Anuria, oliguria, or significant renal dysfunction CrCl < than 60 mL/min (some sources as low as 45ml/min)
G6PD) deficiency
Acute porphyria
MONITORING
Long term: periodic LFT's, renal function tests, pulmonary function
DRUG INTERACTIONS:
Reduced absorption with antacids containing magnesium trisilicate.
Uricosuric drugs (e.g., probenecid, sulfinpyrazone) inhibit renal tubular secretion resulting in increased toxicity with decreased urine macrobid levels
WARNINGS/PRECAUTIONS:
Meets BEERS CRITERIA for elderly adults
C. diff reports (as nearly all ABX)
Brown discoloration of the urine.
Hemolytic Anemia: hemolysis in G6PD deficiency found in ~10 percent of Blacks and a small percentage of ethnic groups of Mediterranean and Near-Eastern origin.
Hepatitis, cholestatic jaundice
Peripheral neuropathy (including optic neuritis), possibly severe or irreversible w/ increased risk if: CrCl <60mL/min, anemia, diabetes, electrolyte imbalance, vitamin B deficiency, and/or debilitating disease.
Pulmonary fibrosis
Reduced sperm count and testicular histology abnormality association
SIDE EFFECTS
COMMON (1-10%): Nausea, emesis, anorexia, flatulence, headache,
UNCOMMON (<1%): Abdominal pain, diarrhea, dyspepsia, constipation, dizziness, drowsiness, blurry vision, fevers, chills, mailase, acute pulmonary hypersensitivity reaction
RARE (<0.1%): Exfoliative dermatitis, erythema multiforme (including Stevens-Johnson syndrome), parotitis, pseudomembranous colitis, cyanosis secondary to methemoglobinemia, aplastic anemia, hepatitis, vertigo, pseudotumor cerebri, optic neuritis, intraretinal crystals causing retinopathy, bulging fontanels, acute interstitial nephritis, cyanosis
VERY RARE (<0.01%):
UNKNOWN PREVALENCE: ST changes, alopecia, dark urine, hemolytic anemia, bone marrow suppression, neuropathy, diplopia, nystagmus, arthralgia, myalgia, confusion, depression, psychotic reaction.
ADULT
CYSTITIS: Regular release: 50 to 100 mg po q6h x3-7d; Dual release: 100 mg po BID x7d
UTI PROPHYLAXIS: Regular release: 50 to 100 mg po qhs
PEDIATRIC
CYSTITIS: Regular release >3mo 5 to 7 mg/kg/day (up to 400 mg/day) po q6h x3-7d; Dual release >12yr: 100mg po bid x3-7d
UTI PROPHYLAXIS: >3mo 1 mg/kg/day (up to 100 mg/day) po qd or bid
RENAL DOSING: Do not give if CrCl <60ml/min. No special dosing necessary if >60ml/min.
DIALYSIS: Is dializable
HEPATIC DOSING: May need reduced dosing if hepatic dysfunction