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acetohydroxamic acid (Lithostat)

 

Classes: Antimicrobials, Adjunct

Dosing and uses of Lithostat (acetohydroxamic acid)

 

Adult dosage forms and strengths

tablet

  • 250mg

 

Chronic Urinary Tract Infection

Indicated for chronic UTS caused by urea-splitting organisms

Initial: 12 mg/kg/day PO divided q6 -8hr on empty stomach

Maintenance: 250 mg PO q6-8hr; not to exceed 1.5 g/day

 

Renal Impairment

SCr 1.8-2.5 mg/dL [159-221 micromoles/L]: Dose q12hr; not to exceed 1 g/day

SCr >2.5 mg/dL [>221 micromoles/L]: Not recommended

 

Pediatric dosage forms and strengths

tablet

  • 250mg

 

Chronic Urinary Tract Infection

Indicated for chronic UTS caused by urea-splitting organisms

Initial: 10 mg/kg/day PO divided q6-8hr on empty stomach; titrate to patient response

 

Geriatric dosage forms and strengths

 

Chronic Urinary Tract Infection

Indicated for chronic UTS caused by urea-splitting organisms

Initial: 12 mg/kg/day PO divided q6-8hr on empty stomach

Maintenance: 250 mg PO q6-8hr; not to exceed 1.5 g/day

 

Lithostat (acetohydroxamic acid) adverse (side) effects

>10%

Mild headache; first 48 hours (30%)

Anorexia (20-25%)

Malaise (20-25%)

Nausea (20-25%)

Vomiting (20-25%)

Anxiety (20%)

Confused (20%)

Depression (20%)

Involuntary quivering (20%)

Hemolytic anemia (15%)

 

<1%

Alopecia

Blood clot

Macular rash

Phlebitis

 

Warnings

Contraindications

Hypersensitivity

Pts. amenable to definitive surgery & antimicrobial agents, infection by non-urease producing organisms, urinary infections controlled by culture-specific antimicrobials, severe renal impairment (CrCl <20 mL/min &/or serum creatinine>2.5 mg/dL [221 umol/L]), inadequate contraception (females), pregnancy

 

Cautions

Always use with appropriate antimicrobial treatment

Potential teratogen

 

Pregnancy and lactation

Pregnancy category: X

Lactation: excretion in breast milk unknown/not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Lithostat (acetohydroxamic acid)

Mechanism of action

Inhibits bacterial urease, decreasing ammonia production

Does not acidify urine or have direct antibacterial effect

 

Pharmacokinetics

Absorption: Well-absorbed

Peak Plasma Time: 15 min -1 hr

Excretion: Urine (55% of oral dose unchanged)