|
Pronunciation |
|
(trye
METH oh
prim) |
|
|
U.S. Brand
Names |
|
Proloprim®;
Trimpex® |
|
|
Generic
Available |
|
Yes |
|
|
Synonyms |
|
TMP |
|
|
Pharmacological Index |
|
Antibiotic, Miscellaneous |
|
|
Use |
|
Treatment of urinary tract infections due to susceptible strains of E.
coli, P. mirabilis, K. pneumoniae, Enterobacter sp
and coagulase-negative Staphylococcus including S.
saprophyticus; acute otitis media in children; acute exacerbations of
chronic bronchitis in adults; in combination with other agents for treatment of
toxoplasmosis, Pneumocystis carinii; treatment of superficial ocular
infections involving the conjunctiva and cornea |
|
|
Pregnancy Risk
Factor |
|
C |
|
|
Contraindications |
|
Hypersensitivity to trimethoprim or any component, megaloblastic anemia due
to folate deficiency |
|
|
Warnings/Precautions |
|
Use with caution in patients with impaired renal or hepatic function or with
possible folate deficiency |
|
|
Adverse
Reactions |
|
1% to 10%:
Dermatologic: Rash (3% to 7%), pruritus
Hematologic: Megaloblastic anemia (with chronic high doses)
<1%: Fever, exfoliative dermatitis, nausea, vomiting, epigastric distress,
thrombocytopenia, neutropenia, leukopenia, hyperkalemia, cholestatic jaundice,
increased LFTs, elevated BUN/serum creatinine |
|
|
Overdosage/Toxicology |
|
Symptoms of acute toxicity includes: nausea, vomiting, confusion, dizziness;
chronic overdose results in bone marrow suppression
Treatment of acute overdose is supportive following GI decontamination;
treatment of chronic overdose is use of oral leucovorin 5-15 mg/day
|
|
|
Drug
Interactions |
|
Increased effect/toxicity/levels of phenytoin; increased myelosuppression
with methotrexate; may increase levels of digoxin |
|
|
Stability |
|
Protect the 200 mg tablet from light |
|
|
Mechanism of
Action |
|
Inhibits folic acid reduction to tetrahydrofolate, and thereby inhibits
microbial growth |
|
|
Pharmacodynamics/Kinetics |
|
Absorption: Oral: Readily and extensive
Protein binding: 42% to 46%
Metabolism: Partially in the liver
Half-life: 8-14 hours, prolonged with renal impairment
Time to peak serum concentration: Within 1-4 hours
Elimination: Significantly in urine (60% to 80% as unchanged drug)
|
|
|
Usual Dosage |
|
Oral:
Adults: 100 mg every 12 hours or 200 mg every 24 hours; in the treatment of
Pneumocystis carinii pneumonia; dose may be as high as 15-20 mg/kg/day
in 3-4 divided doses
Dosing interval in renal impairment: Clcr 15-30 mL/minute:
Administer 50 mg every 12 hours
Hemodialysis: Moderately dialyzable (20% to 50%) |
|
|
Dietary
Considerations |
|
May cause folic acid deficiency, supplements may be
needed. |
|
|
Reference Range |
|
Therapeutic: Peak: 5-15 mg/L; Trough: 2-8 mg/L |
|
|
Mental Health: Effects
on Mental Status |
|
None reported |
|
|
Mental Health:
Effects on Psychiatric
Treatment |
|
May cause neutropenia; use caution with clozapine and
carbamazepine |
|
|
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
No information available to require special precautions |
|
|
Dental Health:
Effects on Dental Treatment |
|
No effects or complications reported |
|
|
Patient
Information |
|
Take per recommended schedule. Complete full course of therapy; do not skip
doses. Do not chew or crush tablets; swallow whole with milk or food. Maintain
adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid
intake). You may experience nausea, vomiting, or GI upset (small frequent meals,
frequent mouth care, sucking lozenges, or chewing gum may help). Report skin
rash, redness, or irritation; feelings of acute fatigue or weakness; unusual
bleeding or bruising; or other persistent adverse effects. Pregnancy
precautions: Inform prescriber if you are or intend to be
pregnant. |
|
|
Nursing
Implications |
|
Monitor for signs of bone marrow suppression such as fever, sore throat, or
bleeding; tablets can be crushed |
|
|
Dosage Forms |
|
Solution, oral: 50 mg (base)/5 mL
Tablet: 100 mg, 200 mg |
|
|
References |
|
Hoppu K, Koskimies O, and Vilska J,
"Trimethoprim in the Treatment of Acute Urinary Tract Infections in Children,"
Int J Clin Pharmacol Ther Toxicol, 1988, 26(2):65-8.
Hoppu K,
"Age Differences in Trimethoprim Pharmacokinetics: Need for Revised Dosing in Children?"
Clin Pharmacol Ther, 1987, 41(3):336-43.
Varoquaux O, Lajoie D, Gobert C, et al,
"Pharmacokinetics of the Trimethoprim-Sulfamethoxazole Combination in the Elderly,"
Br J Clin Pharmacol, 1985, 20:575-81. |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|