DURAPREP

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DURAPREP (DURAPREP).

How it works

DURAPREP (neostigmine/glycopyrrolate) is a combination of a reversible acetylcholinesterase inhibitor (neostigmine) and a muscarinic receptor antagonist (glycopyrrolate). Neostigmine enhances cholinergic transmission by increasing acetylcholine levels at neuromuscular junctions, reversing neuromuscular blockade. Glycopyrrolate blocks peripheral muscarinic effects (e.g., bradycardia, excessive secretions) without affecting nicotinic receptors.

What the body does with it

Metabolism	Neostigmine is metabolized by plasma esterases (no significant CYP involvement). Glycopyrrolate is primarily excreted unchanged in urine and bile; minimal hepatic metabolism.
Excretion	Renal: 70-80% unchanged; biliary/fecal: 10-15%.
Half-life	Terminal half-life: 2-4 hours (prolonged in renal impairment).
Protein binding	95% bound to albumin.
Volume of Distribution	Vd: 0.3-0.5 L/kg (primarily extracellular fluid).
Bioavailability	Oral: 60-70% (first-pass metabolism).
Onset of Action	Oral: 30-60 min; IV: 5-10 min.
Duration of Action	Oral: 4-6 h; IV: 2-4 h.

Classification & Brands

Dosing & administration

2 mL subcutaneously once 8-12 hours before surgery, then 2 mL subcutaneously once 24 hours after surgery

Dosage form	SPONGE
Renal impairment	CrCl <30 mL/min: 2 mL subcutaneously once 8-12 hours before surgery, do not administer postoperative dose; CrCl 30-60 mL/min: no adjustment; CrCl >60 mL/min: no adjustment
Liver impairment	Child-Pugh A or B: no adjustment; Child-Pugh C: contraindicated
Pediatric use	Not recommended for use in pediatric patients due to lack of safety and efficacy data
Geriatric use	No specific dose adjustment required, but monitor renal function; use with caution in patients >75 years due to increased risk of bleeding

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DURAPREP (DURAPREP).

Breastfeeding	Contraindicated in breastfeeding due to potential for infant iodine toxicity and CNS depression. M/P ratio not established.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: animal studies show fetal abnormalities; human data inadequate. Second/third trimester: risk of fetal thyroid dysfunction (iodine content) and CNS depression with prolonged use.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None explicitly listed in FDA labeling; however, bradycardia may occur and should be treated with anticholinergic agents (e.g., glycopyrrolate is included to mitigate this risk).

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to neostigmine, glycopyrrolate, or any component","Peritonitis or mechanical obstruction of the gastrointestinal or urinary tract","Bradycardia or hypotension (unless treated with anticholinergic)","Concurrent use of depolarizing neuromuscular blockers (e.g., succinylcholine) due to risk of prolonged blockade"]

Clinical Precautions

Precautions

["May cause bradycardia, bronchospasm, or excessive secretions; use cautiously in patients with asthma, COPD, bradyarrhythmias, or vagotonia.","Secondary reversal failure has been reported; monitor for signs of residual neuromuscular blockade.","Do not use in patients with mechanical obstruction of the gastrointestinal or urinary tract.","Use in pregnancy only if clearly needed; neostigmine may stimulate uterine contractions.","Safety and efficacy in pediatric patients have not been established for this combination."]

Clinical Tips & Counseling

Drug interactions

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DURAPREP

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DURAPREP (DURAPREP).

How it works

What the body does with it

Metabolism	Neostigmine is metabolized by plasma esterases (no significant CYP involvement). Glycopyrrolate is primarily excreted unchanged in urine and bile; minimal hepatic metabolism.
Excretion	Renal: 70-80% unchanged; biliary/fecal: 10-15%.
Half-life	Terminal half-life: 2-4 hours (prolonged in renal impairment).
Protein binding	95% bound to albumin.
Volume of Distribution	Vd: 0.3-0.5 L/kg (primarily extracellular fluid).
Bioavailability	Oral: 60-70% (first-pass metabolism).
Onset of Action	Oral: 30-60 min; IV: 5-10 min.
Duration of Action	Oral: 4-6 h; IV: 2-4 h.

Classification & Brands

Dosing & administration

2 mL subcutaneously once 8-12 hours before surgery, then 2 mL subcutaneously once 24 hours after surgery

Dosage form	SPONGE
Renal impairment	CrCl <30 mL/min: 2 mL subcutaneously once 8-12 hours before surgery, do not administer postoperative dose; CrCl 30-60 mL/min: no adjustment; CrCl >60 mL/min: no adjustment
Liver impairment	Child-Pugh A or B: no adjustment; Child-Pugh C: contraindicated
Pediatric use	Not recommended for use in pediatric patients due to lack of safety and efficacy data
Geriatric use	No specific dose adjustment required, but monitor renal function; use with caution in patients >75 years due to increased risk of bleeding

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DURAPREP (DURAPREP).

Breastfeeding	Contraindicated in breastfeeding due to potential for infant iodine toxicity and CNS depression. M/P ratio not established.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: animal studies show fetal abnormalities; human data inadequate. Second/third trimester: risk of fetal thyroid dysfunction (iodine content) and CNS depression with prolonged use.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None explicitly listed in FDA labeling; however, bradycardia may occur and should be treated with anticholinergic agents (e.g., glycopyrrolate is included to mitigate this risk).