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acetohydroxamic acid (Lithostat)
Tradename: Lithostat.
Indications:
- treatment of bacterial infections due to susceptible bacteria
- adjunctive therapy in chronic urea-splitting urinary tract infection (UTI), such as that caused by Proteus spp.
- treatment of struvite renal calculi [2]
Dosage: 250 mg PO TID-QID, max dose 1.5 g
Dosage adjustment in renal failure:
serum creatinine max daily dose
< 1.4 mg/dL 1.5 g
1.4-1.8 mg/dL 1.0 g
> 2.0 mg/dL 0.5 g
Pharmacokinetics:
1) well absorbed orally
2) 35-70% eliminated unchanged in the urine
Adverse effects:
1) headache
2) depression
3) anxiety
4) nausea
5) anorexia
6) lethargy
7) reticulocytosis
8) phlebitis in the legs
9) deep venous thrombosis (DVT)
10) rash
11) hemolysis
Drug interactions:
1) heavy metals: chelates all heavy metals including iron, leading to diminished absorption
2) alcohol: combination increases incidence of rash
Mechanism of action:
1) reversibly inhibits bacterial urease
2) reduction of ammonia production in the urine
3) reduction of pH which enhances activity of antimicrobial agents
Related
Proteus
urease
General
enzyme inhibitor
hydroxamic acid
metabolic agent (metabolic modifier)
Properties
INHIBITS: urease
MISC-INFO: elimination route KIDNEY
1/2life 5-10 HOURS
Database Correlations
PUBCHEM cid=1990
References
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998 - not on National VA formulary
- Deprecated Reference