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Pyridostigmine

Generic Name
Pyridostigmine
Brand Names
Mestinon, Regonol
Drug Type
Small Molecule
Chemical Formula
C9H13N2O2
CAS Number
155-97-5
Unique Ingredient Identifier
19QM69HH21

Overview

Myasthenia gravis is an autoimmune disease involving dysfunction at the neuromuscular junction, most commonly due to autoantibodies directed against the acetylcholine receptor (AChR), which results in muscle tone loss, muscle weakness, and fatigue. Acetylcholinesterase inhibitors have been the symptomatic treatment of choice in myasthenia gravis since the 1930s with the early use of physostigmine and neostigmine. By inhibiting the breakdown of acetylcholine in the neuromuscular junction, they increase signalling and relieve symptoms. Pyridostigmine is the current drug of choice, with superior pharmacokinetics and reduced side effects compared to neostigmine. In addition to treating myasthenia gravis, pyridostigmine is used to reverse neuromuscular blocks, relieve symptoms in congenital myasthenic syndromes, and protect against certain nerve agents, notably during the Gulf War. Pyridostigmine was granted initial FDA approval on April 6, 1955, as an oral tablet. Possible dose forms have been expanded to include extended-release tablets, syrups, and injections, marketed under various brand and generic names.

Background

Myasthenia gravis is an autoimmune disease involving dysfunction at the neuromuscular junction, most commonly due to autoantibodies directed against the acetylcholine receptor (AChR), which results in muscle tone loss, muscle weakness, and fatigue. Acetylcholinesterase inhibitors have been the symptomatic treatment of choice in myasthenia gravis since the 1930s with the early use of physostigmine and neostigmine. By inhibiting the breakdown of acetylcholine in the neuromuscular junction, they increase signalling and relieve symptoms. Pyridostigmine is the current drug of choice, with superior pharmacokinetics and reduced side effects compared to neostigmine. In addition to treating myasthenia gravis, pyridostigmine is used to reverse neuromuscular blocks, relieve symptoms in congenital myasthenic syndromes, and protect against certain nerve agents, notably during the Gulf War. Pyridostigmine was granted initial FDA approval on April 6, 1955, as an oral tablet. Possible dose forms have been expanded to include extended-release tablets, syrups, and injections, marketed under various brand and generic names.

Indication

Pyridostigmine is indicated for the treatment of myasthenia gravis. When administered intravenously, it is indicated for the reversal or antagonism of the neuromuscular blocking effects of nondepolarizing muscle relaxants. Pyridostigmine has also been used as a prophylactic agent against irreversible organophosphorus acetylcholinesterase inhibitors, primarily in a military capacity.

Associated Conditions

  • Congenital Myasthenia (CM)
  • Constipation
  • Myasthenia Gravis
  • Neuromuscular Blockade
  • Post-Poliomyelitis Syndrome
  • Orthostatic syncope
  • Soman nerve gas poisoning

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/04/08
Phase 2
Withdrawn
2025/03/25
Phase 4
Completed
2024/04/16
Phase 2
Recruiting
2023/09/13
Phase 4
Recruiting
2023/08/01
Phase 4
Completed
2023/06/26
Phase 3
Recruiting
Leiden University Medical Center
2022/11/03
Phase 2
Recruiting
2022/04/19
Phase 2
Recruiting
Stefan Holubar MD MS FACS, FASCRS
2021/11/08
Phase 4
UNKNOWN
2020/04/20
Phase 1
ENROLLING_BY_INVITATION

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Amneal Pharmaceuticals of New York LLC
0115-2134
ORAL
30 mg in 1 1
12/31/2023
Major Pharmaceuticals
0904-6622
ORAL
60 mg in 1 1
5/4/2017
American Health Packaging
68084-494
ORAL
60 mg in 1 1
2/23/2024
Athem LLC
73152-028
ORAL
60 mg in 5 mL
3/23/2023
Method Pharmaceuticals, LLC
58657-810
ORAL
30 mg in 1 1
12/9/2023
NuCare Pharmaceuticals,Inc.
68071-5032
ORAL
180 mg in 1 1
2/19/2021
Amneal Pharmaceuticals of New York LLC
0115-1404
ORAL
180 mg in 1 1
1/31/2019
Rising Pharma Holdings, Inc.
16571-833
ORAL
60 mg in 5 mL
9/7/2022
VistaPharm, LLC
66689-406
ORAL
60 mg in 5 mL
9/1/2023
Acella Pharmaceuticals, LLC
42192-626
ORAL
60 mg in 5 mL
10/9/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
MESTINON TABLET 60 mg
SIN02898P
TABLET, SUGAR COATED
60 mg
5/22/1989

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Pyridostigmine Bromide Tablets
国药准字H20143421
化学药品
片剂
7/4/2024
Pyridostigmine Bromide Tablets
国药准字H31020867
化学药品
片剂
8/21/2024
Pyridostigmine Bromide Tablets
国药准字H31022744
化学药品
片剂
12/23/2019

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.
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