Brand name: Zunveyl
Drug class: Parasympathomimetic (Cholinergic) Agents

Medically reviewed by Drugs.com on Feb 10, 2025. Written by ASHP.

Introduction

Prodrug of galantamine, a reversible acetylcholinesterase inhibitor.

Uses for Benzgalantamine Gluconate

Alzheimer's Disease

Treatment of mild to moderate dementia of the Alzheimer’s type in adults.

Efficacy is based on 3 bioavailability studies comparing galantamine (active drug) to benzgalantamine in addition to efficacy results from previous studies conducted with galantamine.

Cholinesterase inhibitors remain a cornerstone of treatment due to the lack of curative options, and guidelines emphasize individualized treatment plans and ongoing evaluation of benefits and risks.

Benzgalantamine Gluconate Dosage and Administration

General

Patient Monitoring

• Monitor patient's weight during therapy.

• Monitor for GI bleeding, especially in patients at increased risk for developing ulcers (e.g., patients with a history of ulcers or receiving NSAIAs).

• Monitor for respiratory adverse events.

• Monitor for seizures as cholinesterase inhibitors may induce seizure activity.

Administration

Administer orally twice daily with or without food.

Ensure adequate intake of fluid during treatment.

Do not take with alcohol.

Swallow tablets whole and do not cut, crush, or chew.

Dosage

Dosage of benzgalantamine gluconate is expressed in terms of benzgalantamine.

Adults

Alzheimer's Disease

Oral

Initially, 5 mg twice daily (10 mg/day); may increase to 10 mg twice daily (20 mg/day) after at least 4 weeks, based on response and tolerability. May further increase dosage to a maximum of 15 mg twice daily (30 mg/day) after a minimum of 4 weeks at 10 mg twice daily.

If therapy is interrupted for more than 3 days, restart at the lowest dosage and escalate to current dosage.

Special Populations

Hepatic Impairment

Mild hepatic impairment (Child-Pugh score 5-6): no adjustment needed.

Moderate hepatic impairment (Child-Pugh score 7-9): do not exceed 10 mg twice daily (20 mg/day).

Severe hepatic impairment (Child-Pugh score 10-15): use not recommended.

Renal Impairment

Creatinine clearance of 9–59 mL/minute: do not exceed 10 mg twice daily (20 mg/day).

Creatinine clearance <9 mL/minute: do not use.

Geriatric Patients

No specific dosage recommendations.

Cautions for Benzgalantamine Gluconate

Contraindications

• Known hypersensitivity to benzgalantamine, galantamine, or any inactive ingredients in benzgalantamine.

Warnings/Precautions

Serious Skin Reactions

Rashes, including serious reactions like Stevens-Johnson syndrome and acute generalized exanthematous pustulosis, have been reported; discontinue immediately if a rash occurs, avoid restarting, and consider alternative therapy.

Anesthesia

May enhance the neuromuscular blocking effects of succinylcholine and similar agents.

Cardiovascular Conditions

Cholinesterase inhibitors may cause bradycardia and heart block due to vagotonic effects, with cases reported in all patients regardless of underlying cardiac conduction abnormalities.

GI Conditions

May increase gastric acid secretion, requiring monitoring for bleeding in high-risk patients, such as those with a history of ulcers or those using NSAIAs. May cause weight loss.

Genitourinary Conditions

May cause bladder obstruction, although not seen in trials.

Neurological Conditions

May cause seizures; monitor Alzheimer’s patients closely.

Pulmonary Conditions

Use cautiously in patients with severe asthma or obstructive pulmonary disease; closely monitor respiratory function.

Specific Populations

Pregnancy

Based on animal data may cause fetal harm.

Lactation

Data on benzgalantamine in human milk, its effects on infants, or milk production are lacking; breastfeeding benefits should be weighed against maternal need and potential risks.

Pediatric Use

Safety and effectiveness not established.

Geriatric Use

Galantamine has been studied in 6,519 patients with mild to moderate Alzheimer's dementia, primarily 65–84 years of age, with insufficient younger adults to evaluate age-based response differences.

Hepatic Impairment

Dosage adjustment required in patients with moderate hepatic impairment; not recommended in patients with severe hepatic impairment.

Renal Impairment

Dosage adjustment required for patients with Cl_cr 9–59 mL/minute; not recommended in patients with Cl_cr <9 mL/minute.

Common Adverse Effects

Most common adverse reactions with galantamine (≥5%): nausea, vomiting, diarrhea, dizziness, headache, decreased appetite.

Drug Interactions

Metabolized by CYP isoenzymes 2D6 and 3A4; may interact with inducers or inhibitors of these enzymes.

Does not inhibit CYP isoenzymes 1A2, 2A6, 3A4, 4A, 2C, 2D6, or 2E1.

Specific Drugs

Benzgalantamine Gluconate Pharmacokinetics

Benzgalantamine, a prodrug of galantamine, has systemic exposure <1%; therefore, pharmacokinetics reflect that of galantamine.

Absorption

Bioavailability

Rapidly converted to the active moiety galantamine, with only about 1% of the prodrug detectable in the bloodstream.

Food

Delayed peak concentration to 6 hours.

Plasma Concentration

Time to peak concentration: 2.5-3 hours.

Special Populations

Concentrations 30-40% higher in patients with Alzheimer's disease than in healthy young subjects.

Distribution

Plasma Protein Binding

18%

Elimination

Metabolism

Primary enzymes responsible for metabolism: CYP2D6 and CYP3A4.

Elimination Route

Metabolized by hepatic CYP enzymes, glucuronidation, and renal (20% excreted as unchanged drug within 24 hours).

Half-life

7 hours

Special Populations

Clearance approximately 20% lower in women than men.

Race did not affect clearance.

Moderate hepatic impairment (Child Pugh 7-9) decreased clearance by about 25%.

Renal impairment increased AUC by 37% with moderate and 67% with severe impairment.

No clinically significant differences in pharmacokinetics observed based on CYP2D6 metabolizer status.

Stability

Storage

Oral

Tablets

Store at 20-25°C; excursions permitted between 15-30°C.

Actions

• Prodrug of galantamine; a phenanthrene alkaloid.

• Exact mechanism unclear, but likely related to increasing acetylcholine levels by reversibly inhibiting cholinesterase; however, effectiveness may decline as cholinergic neurons diminish with disease progression.

Advice to Patients

• Advise patients and caregivers to discontinue benzgalantamine and seek immediate medical attention at the first appearance of skin rash.

• Instruct patients or caregivers about the recommended dosage and administration of benzgalantamine delayed-release tablets, which should be administered twice daily with or without food.

• Instruct patients to swallow benzgalantamine whole and not to split, crush, or chew the tablets.

• Advise patients and caregivers to ensure adequate fluid intake during treatment and that benzgalantamine should not be taken with alcohol.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.

• Advise patients to inform their clinician if they are or plan to become pregnant or plan to breast-feed.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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