Mestinon

Name: Mestinon

What is pyridostigmine-oral, and how does it work (mechanism of action)?

Pyridostigmine (Mestinon) is an oral cholinesterase inhibitor. Acetylcholine is one of many neurotransmitters in our bodies. Neurotransmitters are chemicals that help our cells communicate with each other. Depending on the organ that it acts upon, acetylcholine produces different effects. One important function of acetylcholine is to produce muscle contractions and movement. In people with myasthenia gravis or people treated with neuromuscular blocking medicines there is a decrease in the levels of acetylcholine. In such cases pyridostigmine may be used to increase acetylcholine levels and improve muscle contraction or movement. Pyridostigmine increases the concentration of acetylcholine at nerve junctions by inhibiting cholinesterase, the enzyme that destroys acetylcholine.

In comparison to neostigmine (Bloxiverz, Prostigmin), another cholinesterase inhibitor, pyridostigmine has a longer duration of action. Pyridostigmine was approved by the FDA for the treatment of myasthenia gravis in 1955.

What else should I know about pyridostigmine-oral?

What preparations of pyridostigmine-oral are available?

Oral: 60 mg tablets, 60 mg/5 ml syrup, 180 mg timespan (slow release) tablets.

How should I keep pyridostigmine-oral stored?

Pyridostigmine tablets and syrup should be stored at room temperature between 59 F to 86 F (15 C to 30 C). Pyridostigmine should be protected from light.

What Is Pyridostigmine?

Pyridostigmine affects chemicals in the body that are involved in the communication between nerve impulses and muscle movement.

Pyridostigmine is used to treat the symptoms of myasthenia gravis. It is also used in military personnel who have been exposed to nerve gas.

Pyridostigmine may also be used for purposes not listed in this medication guide.

You should not use pyridostigmine if you you have a bladder or bowel obstruction.

You should not use pyridostigmine if you are allergic to it, or if you have a bladder or bowel obstruction.

To make sure you can safely take pyridostigmine, tell your doctor if you have any of these other conditions:

  • asthma; or
  • kidney disease.

FDA pregnancy category C. It is not known whether pyridostigmine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

It is not known whether pyridostigmine passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Pyridostigmine is not approved for use by anyone younger than 18 years old.

Pyridostigmine Dosage

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Take this medicine with food or milk if it upsets your stomach.

Do not crush, chew, or break an extended-release tablet. Swallow it whole.

Measure liquid medicine with the dosing syringe provided, or with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.

The amount and timing of this medicine is extremely important to the success of your treatment. Carefully follow your doctor's instructions about how much medicine to take and when to take it.

Your doctor may occasionally change your dose to make sure you get the best results. You may be asked to keep a daily record of when you took each dose and how long the effects lasted. This will help your doctor determine if your dose needs to be adjusted.

If you need surgery, tell the surgeon ahead of time that you are using pyridostigmine. You may need to stop using the medicine for a short time.

Store at room temperature away from moisture and heat.

Keep the tablets in their original container, along with the canister of moisture-absorbing preservative that comes with this medicine.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include nausea, vomiting, diarrhea, stomach cramps, sweating, blurred vision, drooling, and weak or shallow breathing.

Worsening muscle weakness, or no change in your myasthenia gravis symptoms, may also be signs of overdose.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Warnings

Although failure of patients to show clinical improvement may reflect underdosage, it can also be indicative of overdosage. As is true of all cholinergic drugs, overdosage of Mestinon (pyridostigmine) may result in cholinergic crisis, a state characterized by increasing muscle weakness which, through involvement of the muscles of respiration, may lead to death. Myasthenic crisis due to an increase in the severity of the disease is also accompanied by extreme muscle weakness, and thus may be difficult to distinguish from cholinergic crisis on a symptomatic basis. Such differentiation is extremely important, since increases in doses of Mestinon (pyridostigmine) or other drugs of this class in the presence of cholinergic crisis or of a refractory or "insensitive" state could have grave consequences. Osserman and Genkins1indicate that the differential diagnosis of the two types of crisis may require the use of Tensilon® (edrophonium chloride) as well as clinical judgment. The treatment of the two conditions obviously differs radically. Whereas the presence of myasthenic crisis suggests the need for more intensive anticholinesterase therapy, the diagnosis of cholinergic crisis, according to Osserman and Genkins,1 calls for the prompt withdrawal of all drugs of this type. The immediate use of atropine in cholinergic crisis is also recommended.

Atropine may also be used to abolish or obtund gastrointestinal side effects or other muscarinic reactions; but such use, by masking signs of overdosage, can lead to inadvertent induction of cholinergic crisis.

For detailed information on the management of patients with myasthenia gravis, the physician is referred to one of the excellent reviews such as those by Osserman and Genkins,2 Grob3 or Schwab.4,5

Usage in Pregnancy: The safety of Mestinon (pyridostigmine) during pregnancy or lactation in humans has not been established. Therefore, use of Mestinon (pyridostigmine) in women who may become pregnant requires weighing the drug's potential benefits against its possible hazards to mother and child.

What is the most important information i should know about pyridostigmine (mestinon, mestinon timespan)?

You should not use pyridostigmine if you are allergic to it, or if you have a bladder or bowel obstruction.

Before taking pyridostigmine, tell your doctor if you have asthma, kidney disease, an ulcer or other serious stomach disorder, high blood pressure, heart disease, overactive thyroid, or a history of seizures.

The amount and timing of this medicine is extremely important to the success of your treatment. Carefully follow your doctor's instructions about how much medicine to take and when to take it.

This medication may cause blurred vision or impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Your doctor may occasionally change your dose to make sure you get the best results. You may be asked to keep a daily record of when you took each dose and how long the effects lasted. This will help your doctor determine if your dose needs to be adjusted.

If you need surgery, tell the surgeon ahead of time that you are using pyridostigmine. You may need to stop using the medicine for a short time.

Mestinon (pyridostigmine) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using pyridostigmine and call your doctor at once if you have any of these serious side effects:

  • extreme muscle weakness;

  • loss of movement in any part of your body;

  • weak or shallow breathing;

  • slurred speech, vision problems; or

  • worsening or no improvement in your symptoms of myasthenia gravis.

Common side effects may include:

  • stomach pain, nausea, vomiting, diarrhea;

  • muscle cramps, twitching;

  • sweating, increased salivation;

  • cough with mucus;

  • rash; or

  • blurred vision.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Precaution

Pyridostigmine is mainly excreted unchanged by the kidney.6,7,8 Therefore, lower doses may be required in patients with renal disease, and treatment should be based on titration of drug dosage to effect.6,7

Pediatric Use:

Safety and effectiveness in pediatric patients have not been established.

PRINCIPAL DISPLAY PANEL - 180 mg Bottle Label

NDC 0187-3013-30
Rx OnlyPull here

Mestinon®
(pyridostigmine bromide)
TIMESPAN®

180 mg

Each tablet
contains180 mg
pyridostigmine
bromide
n a specially
constructed tablet for
sustained release

30
Tablets

VALEANT

Mestinon 
pyridostigmine bromide syrup
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0187-3012
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
pyridostigmine bromide (pyridostigmine) pyridostigmine bromide 60 mg  in 5 mL
Inactive Ingredients
Ingredient Name Strength
alcohol  
glycerin  
LACTIC ACID, UNSPECIFIED FORM  
sodium benzoate  
sorbitol  
sucrose  
FD&C Red No. 40  
FD&C Blue No. 1  
water  
Product Characteristics
Color      Score     
Shape Size
Flavor RASPBERRY Imprint Code
Contains     
Packaging
# Item Code Package Description
1 NDC:0187-3012-20 473 mL in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA015193 01/25/1965
Mestinon 
pyridostigmine bromide tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0187-3010
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
pyridostigmine bromide (pyridostigmine) pyridostigmine bromide 60 mg
Inactive Ingredients
Ingredient Name Strength
LACTOSE, UNSPECIFIED FORM  
silicon dioxide  
stearic acid  
Product Characteristics
Color WHITE Score 4 pieces
Shape ROUND Size 10mm
Flavor Imprint Code Mestinon;V;60
Contains     
Packaging
# Item Code Package Description
1 NDC:0187-3010-30 100 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA009829 04/06/1955
Mestinon 
pyridostigmine bromide tablet, extended release
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0187-3013
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
pyridostigmine bromide (pyridostigmine) pyridostigmine bromide 180 mg
Inactive Ingredients
Ingredient Name Strength
carnauba wax  
magnesium stearate  
silicon dioxide  
tribasic calcium phosphate  
Product Characteristics
Color YELLOW (light straw) Score no score
Shape OVAL (capsule-shaped) Size 19mm
Flavor Imprint Code MES;V;180
Contains     
Packaging
# Item Code Package Description
1 NDC:0187-3013-30 30 TABLET, EXTENDED RELEASE in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA011665 01/12/1959
Labeler - Valeant Pharmaceuticals North America LLC (042230623)
Establishment
Name Address ID/FEI Operations
Valeant Pharmaceuticals International 245141858 MANUFACTURE(0187-3012, 0187-3010, 0187-3013), LABEL(0187-3012, 0187-3010, 0187-3013), PACK(0187-3012, 0187-3010, 0187-3013)
Revised: 06/2017   Valeant Pharmaceuticals North America LLC

Pyridostigmine Identification

Substance Name

Pyridostigmine

CAS Registry Number

101-26-8

Drug Class

Cholinesterase Inhibitors

Parasympathomimetics

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