glycopyrrolate 1 mg/5mL Solution
Other active recalls for Glycopyrrolate (different manufacturers) — 4 · tap to view
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Anticholinergic class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Glycopyrrolate is used in combination with other medications to treat ulcers in adults and children 12 years of age and older. Glycopyrrolate (Cuvposa) is used to reduce saliva and drooling in children between 3 and16 years of age that have certain medical conditions that cause drooling. Glycopyrrolate is in a class of medications called anticholinergics. It decreases stomach acid and saliva production by blocking the activity of a certain natural substance in the body.
Read the full MedlinePlus article ↗Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Glycopyrrolate — tap one for details:
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII 2968PHW8QP
A weak organic acid derived from citrus fruits or made through fermentation. It works as a buffer to control pH, a preservative to extend shelf life, and a flavoring agent in medications.
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UNII PDC6A3C0OX
Glycerin is a clear, thick liquid derived from plant oils or fats. It acts as a humectant to retain moisture, a sweetener, and a solvent in medications.
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UNII A2I8C7HI9T
Methylparaben is a preservative derived from benzoic acid that prevents growth of bacteria, fungi, and mold in medicines. It extends the product's shelf life and maintains safety during storage.
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UNII 6DC9Q167V3
Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
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UNII Z8IX2SC1OH
Propylparaben is a chemical preservative used to prevent bacterial and fungal growth in medicines and personal care products. It helps extend shelf life and maintain product safety during storage.
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UNII SB8ZUX40TY
Saccharin sodium is an artificial sweetener made from saccharin salt. It's added to medicines to improve taste, especially in liquid formulations for children or bitter drugs.
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UNII 8KW3E207O2
A liquid sweetener made from sorbitol, a sugar alcohol derived from glucose. It sweetens the medicine and also acts as a humectant to help retain moisture and improve texture in liquid formulations.
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UNII B22547B95K
A salt derived from citric acid that helps maintain the proper acid-base balance in the medicine. It's used as a buffer to keep the product stable and at the right pH level.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
9 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.5483 | $259.35 / 473 ml |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Glycopyrrolate 1 mg/5mL 31722-0016-47 | Camber | 1 bottle | $0.203 | AA | Availability likely | — |
| Glycopyrrolate 1 mg/5mL 49884-0042-33 | Par | 16 ml | $0.203 | AA | Availability likely | — |
| Glycopyrrolate Oral Solution 1 mg/5mL 51672-5316-09 | Sun | 1 bottle | $0.203 | AA | Availability likely | — |
| Glycopyrrolate 1 mg/5mL 59651-0435-47 | Aurobindo | 1 bottle | $0.203 | AA | Availability likely | — |
| glycopyrrolate 1 mg/5mL 71656-0061-16 | Saptalis | 1 bottle | $0.203 | AA | Availability likely | — |
| Glycopyrrolate 1 mg/5mL 72205-0070-72 | Novadoz | 1 bottle | $0.203 | AA | Availability likely | — |
| Glycopyrrolate 1 mg/5mL 72603-0240-01 | NorthStar | 1 bottle | $0.203 | AA | Availability likely | — |
| Cuvposa 1 mg/5mL 00259-0501-16 | Merz | 1 bottle | $1.008 | AA | Availability likely | — |
| Glycopyrrolate 1 mg/5mL 17856-1016-01 | Atlantic | 120 syringes | — | AA | FDA listed | — |
| Glycopyrrolate 1 mg/5mL 62135-0961-47 | Chartwell | 473 ml | — | AA | FDA listed | — |
| Glycopyrrolate 1 mg/5mL 63629-9592-01 | Bryant | 473 ml | — | AA | FDA listed | — |
| Glycopyrrolate 1 mg/5mL 68094-0073-58 | Precision | 1 syringe | — | AA | FDA listed | — |
| glycopyrrolate 1 mg/5mLthis 69452-0406-88 | Bionpharma | 1 bottle | — | AA | FDA listed | — |
| Glycopyrrolate Oral Solution 1 mg/5mL 70010-0106-44 | Granules | 473 ml | — | AA | FDA listed | — |
| Glycopyrrolate Oral Solution 1 mg/5mL 82983-0428-47 | AJENAT | 1 bottle | — | AA | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 69452-0406-88 You're viewing this | 1 BOTTLE in 1 CARTON (69452-406-88) / 473 mL in 1 BOTTLE | 2026-05-11 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Glycopyrrolate oral solution is indicated to reduce chronic severe drooling in patients aged 3 years to 16 years with neurologic conditions associated with problem drooling (e.g., cerebral palsy). Glycopyrrolate oral solution is an anticholinergic indicated to reduce chronic severe drooling in patients aged 3 years to 16 years with neurologic conditions associated with problem drooling (e.g., cerebral palsy). ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Glycopyrrolate oral solution must be measured and administered with an accurate measuring device [see Patient Counseling Information (17) ]. Initiate dosing at 0.02 mg/kg orally three times daily and titrate in increments of 0.02 mg/kg every 5 days to 7 days based on therapeutic response and adverse reactions. The maximum recommended dosage is 0.1 mg/kg three times daily not to exceed 1.5 mg to 3 mg per dose based upon weight.
For greater detail, see Table 1. During the four-week titration period, dosing can be increased with the recommended dose titration schedule while ensuring that the anticholinergic adverse events are tolerable. Prior to each increase in dose, review the tolerability of the current dose level with the patient's caregiver.
Glycopyrrolate oral solution should be dosed at least one hour before or two hours after meals. The presence of high fat food reduces the oral bioavailability of glycopyrrolate oral solution if taken shortly after a meal [see Clinical Pharmacology (12.3) ]. Table 1: Recommended Dose Titration Schedule (each dose to be given three times daily) Weight Dose Level 1 Dose Level 2 Dose Level 3 Dose Level 4 Dose Level 5 kg lbs (~0.02 mg/kg) (~0.04 mg/kg) (~0.06 mg/kg) (~0.08 mg/kg) (~0.1 mg/kg) 13 to 17 27 to 38 0.3 mg 1.5 mL 0.6 mg 3 mL 0.9 mg 4.5 mL 1.2 mg 6 mL 1.5 mg 7.5 mL 18 to 22 39 to 49 0.4 mg 2 mL 0.8 mg 4 mL 1.2 mg 6 mL 1.6 mg 8 mL 2 mg 10 mL 23 to 27 50 to 60 0.5 mg 2.5 mL 1 mg 5 mL 1.5 mg 7.5 mL 2 mg 10 mL 2.5 mg 12.5 mL 28 to 32 61 to 71 0.6 mg 3 mL 1.2 mg 6 mL 1.8 mg 9 mL 2.4 mg 12 mL 3 mg 15 mL 33 to 37 72 to 82 0.7 mg 3.5 mL 1.4 mg 7 mL 2.1 mg 10.5 mL 2.8 mg 14 mL 3 mg 15 mL 38 to 42 83 to 93 0.8 mg 4 mL 1.6 mg 8 mL 2.4 mg 12 mL 3 mg 15 mL 3 mg 15 mL 43 to 47 94 to 104 0.9 mg 4.5 mL 1.8 mg 9 mL 2.7 mg 13.5 mL 3 mg 15 mL 3 mg 15 mL ≥ 48 ≥ 105 1 mg 5 mL 2 mg 10 mL 3 mg 15 mL 3 mg 15 mL 3 mg 15 mL Initiate dosing at 0.02 mg/kg three times daily and titrate in increments of 0.02 mg/kg every 5 days to 7 days, based on therapeutic response and adverse reactions.
( 2 ) Maximum recommended dose is 0.1 mg/kg three times daily, not to exceed 1.5 mg to 3 mg per dose based upon weight. ( 2 ) Administer at least one hour before or two hours after meals. ( 2 )
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Glycopyrrolate oral solution is available as a 1 mg/5 mL clear, colourless liquid for oral administration in 16 ounce bottles. 1 mg/5 mL, oral solution in 16 ounce bottles. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Glycopyrrolate oral solution is contraindicated in: Patients with medical conditions that preclude anticholinergic therapy (e.g., glaucoma, paralytic ileus, unstable cardiovascular status in acute hemorrhage, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, myasthenia gravis). Patients taking solid oral dosage forms of potassium chloride. The passage of potassium chloride tablets through the gastrointestinal (GI) tract may be arrested or delayed with coadministration of glycopyrrolate oral solution.
Medical conditions that preclude anticholinergic therapy. ( 4 ) Concomitant use of solid oral dosage forms of potassium chloride. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Constipation or intestinal pseudo-obstruction: May present as abdominal distention, pain, nausea, or vomiting. Assess patients for constipation, particularly within 4 days to 5 days of initial dosing or after a dose increase. ( 5.1 ) Incomplete mechanical intestinal obstruction: May present as diarrhea.
If obstruction is suspected, discontinue glycopyrrolate oral solution and evaluate. ( 5.2 ) High ambient temperature: To reduce the risk of heat prostration, avoid high temperatures. ( 5.3 )
5.1Constipation or Intestinal Pseudo-obstruction Constipation is a common dose-limiting adverse reaction which sometimes leads to glycopyrrolate discontinuation [see Adverse Reactions (6.1) ]. Assess patients for constipation, particularly within 4 days to 5 days of initial dosing or after a dose increase. Intestinal pseudo-obstruction has been reported and may present as abdominal distention, pain, nausea or vomiting.
5.2Incomplete Mechanical Intestinal Obstruction Diarrhea may be an early symptom of incomplete mechanical intestinal obstruction, especially in patients with ileostomy or colostomy. If incomplete mechanical intestinal obstruction is suspected, discontinue treatment with glycopyrrolate oral solution and evaluate for intestinal obstruction.
5.3High Ambient Temperatures In the presence of high ambient temperature, heat prostration (fever and heat stroke due to decreased sweating) can occur with the use of anticholinergic drugs such as glycopyrrolate oral solution. Advise patients/caregivers to avoid exposure of the patient to hot or very warm environmental temperatures.
5.4Operating Machinery or an Automobile Glycopyrrolate oral solution may produce drowsiness or blurred vision. As appropriate for a given age, warn the patient not to engage in activities requiring mental alertness such as operating a motor vehicle or other machinery, or performing hazardous work while taking glycopyrrolate oral solution.
5.5Anticholinergic Drug Effects Use glycopyrrolate oral solution with caution in patients with conditions that are exacerbated by anticholinergic drug effects including: Autonomic neuropathy Renal disease Ulcerative colitis – Large doses may suppress intestinal motility to the point of producing a paralytic ileus and for this reason may precipitate or aggravate “toxic megacolon”, a serious complication of the disease Hyperthyroidism Coronary heart disease, congestive heart failure, cardiac tachyarrhythmias, tachycardia, and hypertension Hiatal hernia associated with reflux esophagitis, since anticholinergic drugs may aggravate this condition
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in the labeling: Constipation or intestinal pseudo-obstruction [see Warnings and Precautions (5.1) ] Incomplete mechanical intestinal obstruction [see Warnings and Precautions (5.2) ] The most common adverse reactions reported with glycopyrrolate oral solution are dry mouth, vomiting, constipation, flushing, and nasal congestion. The most common adverse reactions (incidence ≥ 30%) are dry mouth, vomiting, constipation, flushing, and nasal congestion.
( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Bionpharma Inc. at 1-888-235-BION or 1-888-235-2466 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data described below reflect exposure to glycopyrrolate oral solution in 151 subjects, including 20 subjects who participated in an 8-week placebo-controlled study (Study 1) and 137 subjects who participated in a 24-week open-label study (six subjects who received glycopyrrolate oral solution in the placebo-controlled study and 131 new subjects).
Table 2 presents adverse reactions reported by ≥ 15% of glycopyrrolate oral solution-treated subjects from the placebo-controlled clinical trial. Table 2: Adverse Reactions Occurring in ≥ 15% of Glycopyrrolate Oral Solution-Treated Subjects and at a Greater Frequency than Placebo in Study 1 Glycopyrrolate Oral Solution (N = 20) n (%) Placebo (N = 18) n (%) Dry Mouth 8 (40%) 2 (11%) Vomiting 8 (40%) 2 (11%) Constipation 7 (35%) 4 (22%) Flushing 6 (30%) 3 (17%) Nasal Congestion 6 (30%) 2 (11%) Headache 3 (15%) 1 (6%) Sinusitis 3 (15%) 1 (6%) Upper Respiratory Tract Infection 3 (15%) 0 Urinary Retention 3 (15%) 0 The following adverse reactions occurred at a rate of < 2% of patients receiving glycopyrrolate oral solution in the open-label study.
Gastrointestinal: Abdominal distention, abdominal pain, stomach discomfort, chapped lips, flatulence, retching, dry tongue General Disorders: Irritability, pain Infections: Pneumonia, sinusitis, tracheostomy infection, upper respiratory tract infection, urinary tract infection Investigations: Heart rate increase Metabolism and Nutrition: Dehydration Nervous System: Headache, convulsion, dysgeusia, nystagmus Psychiatric: Agitation, restlessness, abnormal behavior, aggression, crying, impulse control disorder, moaning, mood altered Respiratory: Increased viscosity of bronchial secretion, nasal congestion, nasal dryness Skin: Dry skin, pruritus, rash Vascular: Pallor
6.2Post marketing Experience The following adverse reactions have been identified during post approval use of other formulations of glycopyrrolate for other indications. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Additional adverse reactions identified during post approval use of glycopyrrolate tablets include: loss of taste and suppression of lactation.
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Digoxin tablets: Use with glycopyrrolate can increase digoxin serum levels. Monitor patients and consider use of alternative dosage forms of digoxin. ( 7 ) Amantadine: Effects of glycopyrrolate may be increased with concomitant administration of amantadine.
Consider decreasing the dose of glycopyrrolate during concomitant use. ( 7 ) Atenolol or metformin: Glycopyrrolate may increase serum levels of atenolol or metformin. Consider dose reduction when used with glycopyrrolate.
( 7 ) Haloperidol or levodopa: Glycopyrrolate may decrease serum levels of haloperidol or levodopa. Consider a dose increase when used with glycopyrrolate. ( 7 ) Drugs Affected by Reduced GI Transit Time Glycopyrrolate reduces GI transit time, which may result in altered release of certain drugs when formulated in delayed- or controlled-release dosage forms.
The passage of potassium chloride tablets through the GI tract may be arrested or delayed with coadministration of glycopyrrolate. Solid dosage forms of potassium chloride are contraindicated [see Contraindications (4) ]. Digoxin administered as slow dissolution oral tablets may have increased serum levels and enhanced action when administered with glycopyrrolate.
Monitor patients receiving slow dissolution digoxin for increased action if glycopyrrolate is coadministered regularly. Consider the use of other oral dosage forms of digoxin (e.g., elixir or capsules). Amantadine The anticholinergic effects of glycopyrrolate may be increased with concomitant administration of amantadine.
Consider decreasing the dose of glycopyrrolate during coadministration of amantadine. Drugs Whose Plasma Levels May be Increased by Glycopyrrolate Coadministration of glycopyrrolate may result in increased levels of certain drugs. Atenolol’s bioavailability may be increased with coadministration of glycopyrrolate.
A reduction in the atenolol dose may be needed. Metformin plasma levels may be elevated with coadministration of glycopyrrolate, increasing metformin’s pharmacologic and toxic effects. Monitor clinical response to metformin with concomitant glycopyrrolate administration; consider a dose reduction of metformin if warranted.
Drugs Whose Plasma Levels May be Decreased by Glycopyrrolate Coadministration of glycopyrrolate may result in decreased levels of certain drugs. Haloperidol’s serum level may be decreased when coadministered with glycopyrrolate, resulting in worsening of schizophrenic symptoms, and development of tardive dyskinesia. Closely monitor patients if coadministration cannot be avoided.
Levodopa’s therapeutic effect may be reduced with glycopyrrolate administration. Consider increasing the dose of levodopa.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Pediatric use: The safety and effectiveness of glycopyrrolate has not been established in patients less than 3 years of age. ( 8.4 ) Renal impairment: Use glycopyrrolate oral solution with caution in patients with renal impairment. ( 8.6 )
8.1Pregnancy Risk Summary There are no available data in pregnant women for glycopyrrolate oral solution to inform decisions concerning any drug-associated risks. In pregnant rats, daily oral administration of glycopyrrolate during organogenesis at dose exposures 2.5 times to 113 times the exposure at the maximum recommended human dose (MRHD) did not result in an increased incidence of gross external or visceral defects [see Data]. When glycopyrrolate was administered intravenously to pregnant rabbits during organogenesis at dose exposures equivalent to up to approximately 7.8 times the exposure at the MRHD, no adverse effects on embryo-fetal development were seen.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Animal Data Glycopyrrolate was orally administered to pregnant rats at dosages of 50 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day during the period of organogenesis.
These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 2.5 times, 23 times, and 113 times, respectively, the estimated systemic exposure in humans at the MRHD (9 mg per day, administered in three divided doses). Glycopyrrolate had no effect on maternal survival, but significantly reduced mean maternal body weight gain over the period of dosing at all dosages evaluated. Mean fetal weight was significantly reduced in the 200 mg/kg/day and 400 mg/kg/day dose groups.
There were two litters with all resorbed fetuses in the 400 mg/kg/day dose group. There were no effects of treatment on the incidence of gross external or visceral defects. Minor treatment-related skeletal effects included reduced ossification of various bones in the 200 mg/kg/day and 400 mg/kg/day dose groups; these skeletal effects were likely secondary to maternal toxicity.
Glycopyrrolate was intravenously administered to pregnant rabbits at dosages of 0.1 mg/kg/day, 0.5 mg/kg/day, and 1 mg/kg/day during the period of organogenesis. These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 0.8 times, 4.6 times, and 7.8 times, respectively, the estimated systemic exposure in humans at the MRHD. Glycopyrrolate did not affect maternal survival under the conditions of this study.
Mean maternal body weight gain and mean food consumption over the period of dosing were lower than the corresponding control value in the 0.5 mg/kg/day and 1 mg/kg/day treatment groups. There were no effects of treatment on fetal parameters, including fetal survival, mean fetal weight, and the incidence of external, visceral, or skeletal defects. Female rats that were pregnant or nursing were orally dosed with glycopyrrolate daily at dosages of 0 mg/kg/day, 50 mg/kg/day, 200 mg/kg/day, or 400 mg/kg/day, beginning on day 7 of gestation, and continuing until day 20 of lactation.
These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 2.5 times, 23 times, and 113 times, respectively, the estimated systemic exposure in humans at the MRHD (9 mg per day, administered in three divided doses). Mean body weight of pups in all treatment groups was reduced compared to the control group during the period of nursing, but eventually recovered to be comparable to the control group, post-weaning. No other notable delivery or litter parameters were affected by treatment in any group, including no effects on mean duration of gestation or mean numbers of live pups per litter.
No treatment-related effects on survival or adverse clinical signs were…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary There are no available data in pregnant women for glycopyrrolate oral solution to inform decisions concerning any drug-associated risks. In pregnant rats, daily oral administration of glycopyrrolate during organogenesis at dose exposures 2.5 times to 113 times the exposure at the maximum recommended human dose (MRHD) did not result in an increased incidence of gross external or visceral defects [see Data]. When glycopyrrolate was administered intravenously to pregnant rabbits during organogenesis at dose exposures equivalent to up to approximately 7.8 times the exposure at the MRHD, no adverse effects on embryo-fetal development were seen.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Animal Data Glycopyrrolate was orally administered to pregnant rats at dosages of 50 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day during the period of organogenesis.
These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 2.5 times, 23 times, and 113 times, respectively, the estimated systemic exposure in humans at the MRHD (9 mg per day, administered in three divided doses). Glycopyrrolate had no effect on maternal survival, but significantly reduced mean maternal body weight gain over the period of dosing at all dosages evaluated. Mean fetal weight was significantly reduced in the 200 mg/kg/day and 400 mg/kg/day dose groups.
There were two litters with all resorbed fetuses in the 400 mg/kg/day dose group. There were no effects of treatment on the incidence of gross external or visceral defects. Minor treatment-related skeletal effects included reduced ossification of various bones in the 200 mg/kg/day and 400 mg/kg/day dose groups; these skeletal effects were likely secondary to maternal toxicity.
Glycopyrrolate was intravenously administered to pregnant rabbits at dosages of 0.1 mg/kg/day, 0.5 mg/kg/day, and 1 mg/kg/day during the period of organogenesis. These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 0.8 times, 4.6 times, and 7.8 times, respectively, the estimated systemic exposure in humans at the MRHD. Glycopyrrolate did not affect maternal survival under the conditions of this study.
Mean maternal body weight gain and mean food consumption over the period of dosing were lower than the corresponding control value in the 0.5 mg/kg/day and 1 mg/kg/day treatment groups. There were no effects of treatment on fetal parameters, including fetal survival, mean fetal weight, and the incidence of external, visceral, or skeletal defects. Female rats that were pregnant or nursing were orally dosed with glycopyrrolate daily at dosages of 0 mg/kg/day, 50 mg/kg/day, 200 mg/kg/day, or 400 mg/kg/day, beginning on day 7 of gestation, and continuing until day 20 of lactation.
These dosages resulted in systemic exposures (estimated AUC 0-inf values) approximately 2.5 times, 23 times, and 113 times, respectively, the estimated systemic exposure in humans at the MRHD (9 mg per day, administered in three divided doses). Mean body weight of pups in all treatment groups was reduced compared to the control group during the period of nursing, but eventually recovered to be comparable to the control group, post-weaning. No other notable delivery or litter parameters were affected by treatment in any group, including no effects on mean duration of gestation or mean numbers of live pups per litter.
No treatment-related effects on survival or adverse clinical signs were observed in pups. There were no effects of maternal treatment on behavior, learning, memory, or reproductive function of pups.
🧒 Pediatric Use ▾
8.4Pediatric Use Glycopyrrolate oral solution was evaluated for chronic severe drooling in patients aged 3 years to 16 years with neurologic conditions associated with problem drooling. Glycopyrrolate oral solution has not been studied in subjects under the age of 3 years.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of glycopyrrolate oral solution did not include subjects aged 65 and over.
🆘 Overdosage ▾
10 OVERDOSAGE Because glycopyrrolate is a quaternary amine which does not easily cross the blood-brain barrier, symptoms of glycopyrrolate overdosage are generally more peripheral in nature rather than central compared to other anticholinergic agents. In case of accidental overdose, therapy may include: Maintain an open airway, providing ventilation as necessary. Managing any acute conditions such as hyperthermia, coma and or seizures as applicable, and managing any jerky myoclonic movements or choreoathetosis which may lead to rhabdomyolysis in some cases of anticholinergic overdosage.
Administering a quaternary ammonium anticholinesterase such as neostigmine to help alleviate-peripheral anticholinergic effects such as anticholinergic induced ileus. Administering activated charcoal orally as appropriate.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Glycopyrrolate is a competitive inhibitor of acetylcholine receptors that are located on certain peripheral tissues, including salivary glands. Glycopyrrolate indirectly reduces the rate of salivation by preventing the stimulation of these receptors.
12.2Pharmacodynamics Glycopyrrolate inhibits the action of acetylcholine on salivary glands thereby reducing the extent of salivation.
12.3Pharmacokinetics Absorption In a parallel study of children (n = 6 per group) aged 7 years to 14 years undergoing intraocular surgery, subjects received either intravenous (IV) or oral glycopyrrolate as a premedication. The mean absolute bioavailability of oral glycopyrrolate tablets was low (approximately 3%) and highly variable among subjects (range 1.3% to 13.3%). A similar pattern of low and variable relative bioavailability is seen in adults.
Analysis of population pharmacokinetic data from normal adults and children with cerebral palsy associated chronic moderate to severe drooling failed to demonstrate linear pharmacokinetics across the dose range. In the same analysis, population estimates of the apparent oral clearance (scaled by weight in children and adults) ranged from
5.28 L/hr/kg to
38.95 L/hr/kg for healthy adults and
8.07 L/hr/kg to
25.65L/hr/kg for patients with cerebral palsy, a reflection of the low and highly variable oral bioavailability of glycopyrrolate. Absorption of glycopyrrolate oral solution (fasting) was compared to that of a marketed glycopyrrolate oral tablet. The C max after oral solution administration was 23% lower compared to tablet administration and AUC 0-inf was 28% lower after oral solution administration.
Mean C max after oral solution administration in the fasting state was 0.318 ng/mL, and mean AUC 0-24 was 1.74 ng·hr/mL. Mean time to maximum plasma concentration for glycopyrrolate was 3.1 hours, and mean plasma half-life was 3 hours. In healthy adults, a high fat meal was shown to significantly affect the absorption of glycopyrrolate oral solution (10 mL, 1 mg/5 mL).
The mean C max under fed high fat meal conditions was approximately 74% lower than the C max observed under fasting conditions. Similarly, mean AUC 0-T was reduced by about 78% by the high fat meal compared with the fasting AUC 0-T . A high fat meal markedly reduces the oral bioavailability of glycopyrrolate oral solution.
Therefore, glycopyrrolate oral solution should be dosed at least one hour before or two hours after meals. Pharmacokinetic results (mean ± SD) are described in Table 3. Table 3: Pharmacokinetic Parameters (mean±SD) for Glycopyrrolate Oral Solution, Fasting and Fed, in Healthy Adults C max (ng/mL) T max (hrs) AUC 0-T (ng∙hr/mL) AUC 0-Inf (ng∙hr/mL) T 1/2 (hrs) Fasting (n = 37) 0.318 ± 0.190 3.10 ± 1.08 1.74 ± 1.07 1.81 ± 1.09 3.0 ±
1.2Fed (n = 36) 0.084 ± 0.081 2.60 ± 1.12 0.38 ± 0.14 0.46 ± 0.13 n = 35 3.2 ±
1.1Distribution After IV administration, glycopyrrolate has a mean volume of distribution in children aged 1 year to 14 years of approximately
1.3 L/kg to
1.8 L/kg, with a range from
0.7 L/kg to
3.9L/kg. In adults aged 60 years to 75 years, the volume of distribution was lower (0.42 L/kg +/-
0.22L/kg). Metabolism In adult patients who underwent surgery for cholelithiasis and were given a single IV dose of tritiated glycopyrrolate, approximately 85% of total radioactivity was excreted in urine and < 5% was present in T-tube drainage of bile. In both urine and bile, > 80% of the radioactivity corresponded to unchanged drug.
These data suggest a small proportion of IV glycopyrrolate is excreted as one or more metabolites. Elimination Approximately 65% to 80% of an IV glycopyrrolate dose was eliminated unchanged in urine in adults. In two studies, after IV administration to pediatric patients ages 1 year to 14 years, mean clearance values ranged from
1.01 L/kg/hr to
1.41 L/kg/hr (range
0.32 L/kg/hr to
2.22L/kg/hr). In adults, IV clearance values were
0.54 L/kg/hr…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Glycopyrrolate is a competitive inhibitor of acetylcholine receptors that are located on certain peripheral tissues, including salivary glands. Glycopyrrolate indirectly reduces the rate of salivation by preventing the stimulation of these receptors.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING NDC 69452-406-88; 1 mg/5mL clear, colourless liquid; 16 oz. bottle. Store at room temperature 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature].
📦 Storage and Handling ▾
Store at room temperature 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature].
📋 Description ▾
11 DESCRIPTION Glycopyrrolate is an anticholinergic drug available as an oral solution containing 1 mg glycopyrrolate per 5 mL. The chemical name for glycopyrrolate is Pyrrolidinium, 3-[(SR)-(cyclopentylhydroxyphenylacetyl) oxy]-1,1-dimethyl-, [RS-] bromide; (RS)-[3-(SR)-Hydroxy-1,1-dimethylpyrrolidinium bromide] α- cyclopentylmandelate. The chemical structure is: The molecular formula for glycopyrrolate is C 19 H 28 BrNO 3 and the molecular weight is 398.34.
The inactive ingredients in glycopyrrolate oral solution are: citric acid monohydrate, glycerin, methylparaben, propylene glycol, propylparaben, saccharin sodium, sodium citrate dihydrate, sorbitol solution, and purified water. Glycopyrrolate meets USP organic impurities procedure 2. structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA-approved patient labeling (Patient Information) Advise patients/caregivers to measure glycopyrrolate oral solution with an accurate measuring device. A household teaspoon is not an accurate measuring device. Patients/caregivers should use a dosing cup available in pharmacies to accurately measure the correct milliliter dose.
An oral syringe, also available in pharmacies, should be used to dispense glycopyrrolate oral solution into the child’s mouth from the cup. A pharmacist can recommend an appropriate measuring device and can provide instructions for measuring the correct dose. Administering glycopyrrolate oral solution with a high fat meal substantially reduces the amount of glycopyrrolate absorbed.
Administer glycopyrrolate oral solution at least one hour before or two hours after meals. Glycopyrrolate oral solution is started at a low dose and gradually titrated over a period of weeks based on therapeutic response and adverse reactions. Patients/caregivers should not increase the dose without the physician’s permission.
Common adverse reactions from glycopyrrolate oral solution include overly dry mouth, constipation, vomiting, flushing of the skin or face, and urinary retention. Side effects can sometimes be difficult to detect in some patients with neurologic problems who cannot adequately communicate how they feel. If side effects become troublesome after increasing a dose, decrease the dose to the prior one and contact your physician.
Constipation is the most common side effect of glycopyrrolate, and if constipation occurs, stop administering glycopyrrolate to the patient and call their healthcare practitioner. Inability of the patient to urinate, dry diapers or undergarments, irritability or crying may be signs of urinary retention, and if urinary retention occurs, patients/caregivers should stop administering glycopyrrolate and call their healthcare practitioner. If the patient develops a skin rash, hives or an allergic reaction, parents/caregivers should stop administering glycopyrrolate and call their healthcare practitioner as this could be a sign of hypersensitivity to this product.
Drugs like glycopyrrolate can reduce sweating, and if the patient is in a hot environment and flushing of the skin occurs this may be due to overheating. Avoid exposure of the patient to hot or very warm environmental temperatures to avoid overheating and the possibility of heat exhaustion or heat stroke.