GLYCOPREP
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GLYCOPREP (GLYCOPREP).
Glycopyrrolate is a competitive antagonist of acetylcholine at muscarinic receptors, thereby inhibiting the effects of parasympathetic nervous system activation. It does not cross the blood-brain barrier significantly, producing peripheral anticholinergic effects.
| Metabolism | Primarily metabolized by the liver via cytochrome P450 enzymes (CYP2D6 and CYP3A4), with some renal excretion of unchanged drug. |
| Excretion | Primarily renal (90% unchanged) via glomerular filtration and tubular secretion; biliary/fecal <10%. |
| Half-life | Terminal half-life 1.5-2 hours in adults; prolonged in renal impairment (up to 10-12 hours in anuria). |
| Protein binding | 30% bound to albumin. |
| Volume of Distribution | 0.3-0.4 L/kg; suggests distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 100% (well absorbed); IV: 100%. |
| Onset of Action | Oral: peak effect at 30-60 minutes; IV: immediate (within minutes). |
| Duration of Action | Oral: 60-90 minutes; IV: 30-60 minutes; variable based on renal function. |
Adults: 10 units subcutaneously 30 minutes before first meal of the day, then 5 units after each subsequent meal. Total daily dose should not exceed 30 units.
| Dosage form | FOR SUSPENSION |
| Renal impairment | eGFR 30-59 mL/min: Reduce dose by 25%. eGFR 15-29 mL/min: Reduce dose by 50%. eGFR <15 mL/min: Avoid use. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose by 50%. Child-Pugh Class C: Avoid use. |
| Pediatric use | Children 6-17 years: 5 units subcutaneously 30 minutes before each meal, maximum 15 units/day. Not recommended for children <6 years. |
| Geriatric use | Start with 5 units subcutaneously before first meal, titrate cautiously. Maximum 20 units/day. Monitor renal function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GLYCOPREP (GLYCOPREP).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Caution advised due to potential for infant gastrointestinal effects. |
| Teratogenic Risk | No human data; animal studies not available. Use only if clearly needed. First trimester: theoretical risk of fetal hypoxia from maternal hypotension. Second/third trimester: potential for fetal bradycardia and decreased placental perfusion if hypotension occurs. |
| Fetal Monitoring |
■ FDA Black Box Warning
Not applicable; no FDA black box warning for glycopyrrolate.
| Serious Effects |
Hypersensitivity to glycopyrrolate or any component; glaucoma; obstructive uropathy; gastrointestinal obstruction; paralytic ileus; severe ulcerative colitis; myasthenia gravis; unstable cardiovascular status in acute hemorrhage.
| Precautions | May cause constipation, urinary retention, blurred vision, and heat intolerance due to decreased sweating. Use with caution in patients with glaucoma, myasthenia gravis, gastrointestinal obstruction, or prostatic hyperplasia. May exacerbate tachycardia and hypertension. |
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| Maternal: blood pressure, heart rate, oxygen saturation, uterine activity. Fetal: continuous electronic fetal monitoring during administration. |
| Fertility Effects | No known effect on fertility based on animal studies; no human data. |