Pharmacokinetics of Neostigmine and Glycopyrrolate

NCT04027972 | Completed Early Phase 1 DMC FDA Drug FDA Device

• 1 other identifier: KOR-18-16
• Study Type: interventional
• Target: 13
• Locations: 1 country
• Sites: 1

Brief Summary

A group of 6 able-bodied healthy volunteers will receive Neostigmine (NEO) and Glycopyrrolate (GLY) intravenously and via 2 methods of Iontophoresis (ION): one-patch and two-patch administration, with subsequent blood draws over 1 hour in order to measure the pharmacokinetic behavior of the drugs in-vivo.

Conditions

Spinal Cord Injuries; Constipation; Fecal Incontinence; Neurogenic Bowel

Keywords

Neostigmine; Glycopyrrolate; Transdermal; Intravenous; Pharmacokinetic; Constipation; Bowel Control; Mass Spectroscopy; Stool Incontinence

Outcome Measures

Primary Outcomes (1)

• Serum concentrations of Neostigmine and Glycopyrrolate within 1 hour post-administration

  Measurement of serum concentration of Neostigmine and of Glycopyrrolate to determine pharmacokinetic profiles

  Within Two Hours

Secondary Outcomes (1)

• Presence or absence of headache, dry mouth, muscle twitching and abdominal cramps.

  Within 1 hour of administration

Study Arms (1)

Primary

EXPERIMENTAL

6 Subjects will receive all 4 types of medication administration in random sequence

Drug: Combination of Neostigmine and Glycopyrrolate; Device: I-Box by Dynatronics

Interventions

Combination of Neostigmine and Glycopyrrolate DRUG

Intravenous or transdermal

Primary

I-Box by Dynatronics DEVICE

Electric field conducting drugs through the skin without compromising its integrity

Also known as: Iontophoresis

Primary

Eligibility Criteria

• Age: 18 Years - 70 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male or Female
• Age 18-70 years

You may not qualify if:

• Previous adverse reaction or hypersensitivity to electrical stimulation,
• Known sensitivity to neostigmine or glycopyrrolate,
• History of mechanical obstruction of the GI or urinary tract,
• Myocardial infarction within 6 months of trial,
• Malignant and/or Uncontrollable Hypertension Defined by a blood pressure reading of 160/100 mmHg or higher with or without taking 3 or more different classes of anti-hypertensive medications,
• Organ damage (heart \& kidney) and/or TIA-CVA as a result of hypertension,
• Known past history of coronary artery disease or bradyarrhythmia,
• Symptomatic orthostatic hypotension
• Deep brain stimulation
• Pregnancy (women who are sexually active and of childbearing potential must utilize a method of contraception and agree to maintain a contraceptive method until completion of the study),
• Lactating, nursing females
• Inability to provide informed consent signaled by MoCA cognitive test score of 20 or less,
• History of ingrown hair folliculitis,
• Concurrent illness and fever,
• Concurrent participation in a research study,

Sponsors & Collaborators

• James J. Peters Veterans Affairs Medical Center: lead

Study Sites (1)

James J Peters VA Medical Center

The Bronx, New York, 10468, United States

Location

Related Publications (4)

• Korsten MA, Lyons BL, Radulovic M, Cummings TM, Sikka G, Singh K, Hobson JC, Sabiev A, Spungen AM, Bauman WA. Delivery of neostigmine and glycopyrrolate by iontophoresis: a nonrandomized study in individuals with spinal cord injury. Spinal Cord. 2018 Mar;56(3):212-217. doi: 10.1038/s41393-017-0018-2. Epub 2017 Nov 8.

  PMID: 29116244 BACKGROUND

• Korsten MA, Rosman AS, Ng A, Cavusoglu E, Spungen AM, Radulovic M, Wecht J, Bauman WA. Infusion of neostigmine-glycopyrrolate for bowel evacuation in persons with spinal cord injury. Am J Gastroenterol. 2005 Jul;100(7):1560-5. doi: 10.1111/j.1572-0241.2005.41587.x.

  PMID: 15984982 BACKGROUND

• Chang JY, Locke GR 3rd, McNally MA, Halder SL, Schleck CD, Zinsmeister AR, Talley NJ. Impact of functional gastrointestinal disorders on survival in the community. Am J Gastroenterol. 2010 Apr;105(4):822-32. doi: 10.1038/ajg.2010.40. Epub 2010 Feb 16.

  PMID: 20160713 BACKGROUND

• Sabiev A, Korsten MA, Bauman WA (2021) A Comparison among Three Skin Preparations for the Transdermal Delivery of Vitamin B12 by Iontophoresis: A Novel Approach to Determine Systemic Absorption. J Pharm Drug Deliv Res 10:3.

  BACKGROUND

MeSH Terms

Conditions

Spinal Cord Injuries; Constipation; Fecal Incontinence; Neurogenic Bowel; Encopresis

Interventions

Glycopyrrolate; Iontophoresis

Condition Hierarchy (Ancestors)

Spinal Cord Diseases; Central Nervous System Diseases; Nervous System Diseases; Trauma, Nervous System; Wounds and Injuries; Signs and Symptoms, Digestive; Signs and Symptoms; Pathological Conditions, Signs and Symptoms; Rectal Diseases; Intestinal Diseases; Gastrointestinal Diseases; Digestive System Diseases; Colonic Diseases, Functional; Colonic Diseases; Behavioral Symptoms; Behavior; Elimination Disorders; Mental Disorders

Intervention Hierarchy (Ancestors)

Quaternary Ammonium Compounds; Amines; Organic Chemicals; Onium Compounds; Pyrrolidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Drug Administration Routes; Drug Therapy; Therapeutics; Electrophoresis; Electrochemical Techniques; Investigative Techniques

Study Officials

• Christopher P Cardozo, MD

  James J. Peters Veterans Affairs Medical Center

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: early phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: FED
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Principal Investigator

Model Details: Same group receives all 2 treatments but in a randomized order after the IV phase.

Study Record Dates

• First Submitted: July 19, 2019
• First Posted: July 22, 2019
• Study Start: March 9, 2020
• Primary Completion: December 20, 2022
• Study Completion: December 20, 2022
• Last Updated: September 17, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)