DICURIN PROCAINE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DICURIN PROCAINE (DICURIN PROCAINE).

How it works

Dicurin Procaine is a mercurial diuretic that inhibits sodium and chloride reabsorption in the proximal tubule and loop of Henle, leading to increased urine output. The procaine component provides local anesthetic effects.

What the body does with it

Metabolism	Metabolized in the liver by hydrolysis to form mercuric ions and procaine. Procaine is further metabolized by plasma cholinesterase.
Excretion	Renal excretion of unchanged drug and metabolites: 60-80% via glomerular filtration and tubular secretion; biliary excretion <5%.
Half-life	Terminal elimination half-life: 0.5-1.5 hours (short-acting local anesthetic). Clinically, repeated doses may lead to accumulation if hepatic or renal impairment exists.
Protein binding	Protein binding: 90-95% primarily to alpha1-acid glycoprotein (AAG) and albumin.
Volume of Distribution	Volume of distribution: 0.5-1.0 L/kg; high Vd indicates extensive tissue distribution, particularly to well-perfused organs like brain and heart.
Bioavailability	Bioavailability: Not applicable due to rapid hepatic first-pass metabolism; intravenous administration yields 100% bioavailability; epidural and peripheral administration bypass first-pass but systemic absorption leads to 100% bioavailability into systemic circulation.
Onset of Action	Onset of action: 5-15 minutes for infiltration and peripheral nerve blocks; 10-20 minutes for epidural administration.
Duration of Action	Duration of action: 45-90 minutes for infiltration; 60-120 minutes for nerve blocks; up to 2 hours with epinephrine (vasoconstriction prolongs effect).

Classification & Brands

Dosing & administration

50-100 mg (as procaine penicillin G) intramuscularly once daily; severe infections: 100-200 mg IM every 12-24 hours.

Dosage form	INJECTABLE
Renal impairment	GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: reduce dose by 50% or extend interval to every 24-36 hours; GFR <10 mL/min: avoid use or use 25% of usual dose every 48 hours.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25-50%; Child-Pugh C: avoid use due to increased risk of neurotoxicity.
Pediatric use	Neonates: 50,000 units/kg IM once daily; Infants/children: 25,000-50,000 units/kg IM once daily (max 1.2 million units/day).
Geriatric use	Reduce dose by 25-50% due to decreased renal function; monitor for neurotoxicity and adjust based on creatinine clearance.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DICURIN PROCAINE (DICURIN PROCAINE).

Breastfeeding	Excretion into human milk is unknown; however, due to potential for serious adverse reactions in nursing infants, breastfeeding is contraindicated. No M/P ratio available.
Teratogenic Risk	Dicurin procaine is contraindicated in pregnancy due to documented teratogenic effects. First trimester: high risk of neural tube defects, cardiac malformations, and limb anomalies. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and neonatal nephrotoxicity. Category X.

Warnings & precautions

■ FDA Black Box Warning

Dicurin Procaine contains mercury and can cause severe renal toxicity, including acute tubular necrosis and fatal uremia. It should be used only when other diuretics are ineffective. Risk of local tissue necrosis if extravasation occurs.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Renal insufficiency","Oliguria or anuria","Known hypersensitivity to mercury or procaine","Acute glomerulonephritis","Severe hepatic disease with impaired renal function"]

Clinical Precautions

Precautions

["Monitor renal function regularly; risk of mercury accumulation and nephrotoxicity.","Do not administer intravenously; intramuscular injection only.","Extravasation can cause severe tissue damage and sloughing.","Avoid use in patients with known allergy to mercurial compounds or procaine.","Use with caution in geriatric patients due to reduced renal function.","May cause electrolyte imbalances (hyponatremia, hypochloremia)."]

Clinical Tips & Counseling

Drug interactions

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DICURIN PROCAINE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DICURIN PROCAINE (DICURIN PROCAINE).

How it works

What the body does with it

Metabolism	Metabolized in the liver by hydrolysis to form mercuric ions and procaine. Procaine is further metabolized by plasma cholinesterase.
Excretion	Renal excretion of unchanged drug and metabolites: 60-80% via glomerular filtration and tubular secretion; biliary excretion <5%.
Half-life	Terminal elimination half-life: 0.5-1.5 hours (short-acting local anesthetic). Clinically, repeated doses may lead to accumulation if hepatic or renal impairment exists.
Protein binding	Protein binding: 90-95% primarily to alpha1-acid glycoprotein (AAG) and albumin.
Volume of Distribution	Volume of distribution: 0.5-1.0 L/kg; high Vd indicates extensive tissue distribution, particularly to well-perfused organs like brain and heart.
Bioavailability	Bioavailability: Not applicable due to rapid hepatic first-pass metabolism; intravenous administration yields 100% bioavailability; epidural and peripheral administration bypass first-pass but systemic absorption leads to 100% bioavailability into systemic circulation.
Onset of Action	Onset of action: 5-15 minutes for infiltration and peripheral nerve blocks; 10-20 minutes for epidural administration.
Duration of Action	Duration of action: 45-90 minutes for infiltration; 60-120 minutes for nerve blocks; up to 2 hours with epinephrine (vasoconstriction prolongs effect).

Classification & Brands

Dosing & administration

50-100 mg (as procaine penicillin G) intramuscularly once daily; severe infections: 100-200 mg IM every 12-24 hours.

Dosage form	INJECTABLE
Renal impairment	GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: reduce dose by 50% or extend interval to every 24-36 hours; GFR <10 mL/min: avoid use or use 25% of usual dose every 48 hours.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25-50%; Child-Pugh C: avoid use due to increased risk of neurotoxicity.
Pediatric use	Neonates: 50,000 units/kg IM once daily; Infants/children: 25,000-50,000 units/kg IM once daily (max 1.2 million units/day).
Geriatric use	Reduce dose by 25-50% due to decreased renal function; monitor for neurotoxicity and adjust based on creatinine clearance.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DICURIN PROCAINE (DICURIN PROCAINE).

Breastfeeding	Excretion into human milk is unknown; however, due to potential for serious adverse reactions in nursing infants, breastfeeding is contraindicated. No M/P ratio available.
Teratogenic Risk	Dicurin procaine is contraindicated in pregnancy due to documented teratogenic effects. First trimester: high risk of neural tube defects, cardiac malformations, and limb anomalies. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and neonatal nephrotoxicity. Category X.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Renal insufficiency","Oliguria or anuria","Known hypersensitivity to mercury or procaine","Acute glomerulonephritis","Severe hepatic disease with impaired renal function"]