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Enzyme Inhibitor

How it worksAcetohydroxamic acid works by blocking a specific enzyme called bacterial urease. This stops bacteria from turning urea into ammonia, which helps lower the amount of ammonia and alkalinity in the urine.

Brand names:LITHOSTAT

Used for
As an extra treatment for people with chronic urinary infections caused by bacteria that split urea.
Conditions
Chronic urea-splitting urinary infection
Class
Enzyme InhibitorUrease InhibitorUrinaryHematologic

How to take

FormsOral tablet
RoutesOral

The usual dose is one 250 mg tablet taken 3 to 4 times a day. It is best taken when the stomach is empty. The total daily dose is based on body weight (10-15 mg/kg/day), but should not exceed 1.5 grams per day.

People with kidney issues may need a lower dose. People with advanced kidney disease (creatinine levels above 2.5 mg/dl) should not use this medication. Children should start with a dose of 10 mg/kg/day.

Key warnings

  • ·Acetohydroxamic acid can cause a type of anemia called Coombs negative hemolytic anemia.
  • ·Blood tests (CBC and reticulocyte count) are recommended after two weeks of use and every three months during treatment.
  • ·This drug should not be used as a replacement for surgery or antibiotic treatments.
  • ·It should not be used in women who are pregnant or who do not have a reliable method of birth control.

Do not use if

  • ·Patients who can be cured with surgery or specific antibiotics.
  • ·Patients with urinary infections not caused by urea-splitting organisms.
  • ·Patients with poor kidney function (creatinine above 2.5 mg/dl or clearance below 20 ml/min).
  • ·Pregnant women or women not using reliable birth control.
  • ·Patients with infections caused by organisms that do not produce urea.

Side effects

Common

Mild headachesNauseaVomitingLoss of appetiteFeeling unwell (malaise)Nervousness or tremors

Serious

  • ·Hemolytic anemia (a type of red blood cell disorder)
  • ·Changes in blood counts (reticulocyte count)
  • ·Skin rash if taken with alcohol

Seek help if

  • ·Severe nausea, vomiting, or malaise
  • ·Signs of anemia
  • ·Skin rash

Interactions

  • ·Taking this drug with alcohol may cause a rash.
  • ·This drug can bind to iron, which might prevent both the iron and the drug from being absorbed properly. If you need iron supplements, your doctor may recommend an injection instead.
  • ·Use with caution when taking insulin, antibiotics, or progesterone-type medications.
FoodAcetohydroxamic acid can bind to iron in the gut, which may reduce the absorption of both the iron and the medication.
AlcoholTaking acetohydroxamic acid with alcoholic beverages may result in a skin rash.

Special populations

PregnancyAcetohydroxamic acid should not be used during pregnancy as it may cause harm to the developing fetus.

BreastfeedingIt is not known if this drug passes into human milk. Because of the risk of serious reactions in nursing infants, you should consider stopping breastfeeding or stopping the drug.

PediatricChildren with long-term urea-splitting urinary infections may benefit from this drug, but they must be closely monitored by a doctor.

Talk to your doctor

Monitor

  • ·Reticulocyte count
  • ·Complete blood count (CBC)
  • ·Kidney function (serum creatinine)
  • ·Symptoms of anemia (nausea, vomiting, malaise)

Questions to ask

  • ·Is my kidney function healthy enough for Acetohydroxamic acid?
  • ·How often should I have my blood counts checked?
  • ·Should I take a different form of iron while on this medication?
  • ·Is my urinary infection caused by a urea-splitting organism?

Pharmacokinetics

OnsetPeak blood levels occur 0.25 to 1 hour after dosing
Half-lifeIncreases with higher doses in rodents
BioavailabilityWell absorbed from the gastrointestinal tract
Protein bindingNo known binding to any tissue
MetabolismIn rodents, 25% is excreted as acetamide or acetate
Excretion55% is excreted unchanged in urine; 7% is excreted by the lungs as CO2; less than 1% in feces

Practical

OverdoseAn overdose may cause nausea, vomiting, anxiety, tremors, and a serious reaction where red blood cells are destroyed (hemolysis), which may require hospital treatment.

Ingredients

Inactive

CelluloseMicrocrystalline silicon dioxideMagnesium stearatePeppermint oil

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.