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Methenamine and Methenamine Salts

Pronouncation: (meh-THEN-uh-meen and meh-THEN-uh-meen salts)
Class: Anti-infective agent Methenamine Hippurate

Trade Names:
Hiprex
- Tablets 1 g

Trade Names:
Urex
- Tablets 1 g

Methenamine Mandelate

Trade Names:
Mandameth
- Tablets 0.5 mg
- Tablets, enteric-coated 1 g

Trade Names:
Mandelamine
- Tablets 0.5 g
- Tablets 1 g

Pharmacology

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In acidic urine, methenamine is hydrolyzed to ammonia and formaldehyde, which is bactericidal to certain bacteria in urine. Acid salts (methenamine mandelate and hippurate) have some nonspecific bacteriostatic activity and help to maintain low urine pH.

Pharmacokinetics

Absorption

Methenamine absorption is rapid (30% to 60% hydrolyzed by gastric acid if not enteric-coated). T max of urinary formaldehyde concentrations are 0.5 to 1.5 h for methenamine, 2 h for methenamine hippurate, and 3 to 8 h for methenamine mandalate.

Distribution

Methenamine is freely distributed to body tissues and fluids. Vd is approximately 0.56 L/kg.

Metabolism

Methenamine is metabolized in the liver (approximately 10 to 25%) and through hydrolysis in acidic urine (pH at least 5.5) to ammonia and formaldehyde.

Elimination

Methenamine is eliminated renally via glomerular filtration and tubular secretion. The t ½ is 3 to 6 h.

Indications and Usage

Suppression or elimination of bacteriuria associated with pyelonephritis, cystitis and other chronic UTIs; treatment of infected residual urine, sometimes accompanying neurologic disease or diabetes.

Contraindications

Renal insufficiency; severe dehydration; severe hepatic insufficiency with hyperammonemia; acute UTIs involving renal parenchyma.

Dosage and Administration

Methenamine Hippurate
Adults and Children (older than 12ߙyr of age)

PO 1 g twice daily.

Children (6 to 12 yr of age)

PO 500 mg to 1 g twice daily.

Methenamine Mandelate
Adults

PO 1 g 4 times daily after meals and at bedtime.

Children (6 to 12 yr)

PO 500 mg 4 times daily.

Children (younger than 6 yr)

PO 250ߙmg for q 30 lb body weight 4 times daily (18.4 mg/kg 4 times daily).

Storage/Stability

Store at room temperature (59° to 86°F) in tightly closed container. Protect from excessive heat.



Drug Interactions

Sulfonamides

May increase chance of crystalluria.

Urine alkalizers (acetazolamide, sodium bicarbonate, carbonate)

Prevents hydrolysis of methenamine to formaldehyde with possible decrease in antimicrobial action.

Laboratory Test Interactions

Methenamine may interfere with laboratory urine determinations of 17-hydroxycorticosteroids, catecholamines and vanillylmandelic acid (false increases) and 5-hydroxyindoleacetic acid (false decrease). Taken during pregnancy, can interfere with laboratory tests for urine estriol (false decrease) when acid hydrolysis procedure is used; use enzymatic hydrolysis procedure.

Adverse Reactions

CNS

Headache.

Dermatologic

Pruritus; urticaria; erythematous eruptions; rash.

GI

Nausea; vomiting; cramps; diarrhea; stomatitis; anorexia.

Genitourinary

Bladder irritation; dysuria; proteinuria; hematuria; frequency; urgency; crystalluria.

Hematologic

Serum transaminase elevation.

Respiratory

Dyspnea.

Miscellaneous

Generalized edema.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Special Risk Patients

Use with caution to avoid inducing lipoid pneumonia in debilitated patients and patients with swallowing difficulty.

Tartrazine Sensitivity

Some products contain tartrazine, which may cause rash or bronchial asthma in susceptible patients.

Acid urine

If acidification of urine cannot be obtained or is contraindicated, drug is not recommended.

Gout

May cause precipitation of urate crystals in urine.

Lipoid pneumonia

Methenamine mandelate oral suspension is vegetable oil-based; aspiration could result in lipoid pneumonitis.

Patient Information

  • Explain significance of adequate hydration.
  • Tell patient to report the following symptoms to health care provider: painful urination, skin rash, headache, swelling or severe stomach upset.
  • Instruct patient to avoid use of milk products and antacids while taking drug to help keep urine acidic and allow drug to work better. Instruct patient to take vitamin C and drink cranberry or prune juice to acidify urine.
  • Caution patient not to self-medicate with OTC medications containing sodium bicarbonate or sodium carbonate.
  • Teach patient how to read dipstick tests for urine pH and specific gravity and to report to health care provider if required values are not attained.



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