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Drug overview for MESTINON (pyridostigmine bromide):
Generic name: pyridostigmine bromide (pir-ID-oh-STIG-meen)
Drug class: Antimyasthenic Agents
Therapeutic class: Locomotor System
Pyridostigmine is a reversible anticholinesterase agent.
No enhanced Uses information available for this drug.
Generic name: pyridostigmine bromide (pir-ID-oh-STIG-meen)
Drug class: Antimyasthenic Agents
Therapeutic class: Locomotor System
Pyridostigmine is a reversible anticholinesterase agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
MESTINON 60 MG/5 ML SOLUTION
MESTINON 180 MG TIMESPAN
The following indications for MESTINON (pyridostigmine bromide) have been approved by the FDA:
Indications:
Myasthenia gravis
Prevention of nerve agent poisoning
Professional Synonyms:
Erb-Goldflam disease
Goldflam's disease
Goldflam-Erb disease
Prophylaxis of nerve gas poisoning
Indications:
Myasthenia gravis
Prevention of nerve agent poisoning
Professional Synonyms:
Erb-Goldflam disease
Goldflam's disease
Goldflam-Erb disease
Prophylaxis of nerve gas poisoning
The following dosing information is available for MESTINON (pyridostigmine bromide):
In the initial treatment of myasthenia gravis in adults, oral pyridostigmine bromide should be started at a low dosage (usually 60 mg 3 times daily as conventional tablets or oral solution), and increased gradually at intervals of 48 hours or more to provide maximum relief of symptoms. The usual oral adult daily maintenance dosage of pyridostigmine bromide in myasthenia gravis ranges from 60 mg to 1.5 g, with an average of 600 mg.
Pyridostigmine bromide extended-release tablets (Mestinon(R) Timespan(R)) are designed to slowly release the drug for a prolonged duration of action. The immediate effect of a 180-mg extended-release tablet is similar to that of a 60-mg conventional tablet, but the duration of effect is about 2.5 times longer.
Although the manufacturer states that adults may receive 180-540 mg of pyridostigmine bromide as extended-release tablets once or twice daily (with at least 6 hours between doses), this dosage form is generally used only at bedtime in patients who awaken at night or in the early morning with impairing weakness.
Changes in oral dosage may take several days to show results. When a further increase in dosage produces no corresponding increase in muscle strength, dosage should be reduced to the previous level, so that the patient receives the smallest dosage necessary to produce maximum strength.
In adults with myasthenia gravis requiring parenteral therapy, approximately 1/30 of the usual oral dose of pyridostigmine bromide has been given by IM or very slow IV injection. However, the currently available parenteral preparation (Regonol(R)) is not FDA-labeled for the treatment of myasthenia gravis.
Neonatal myasthenia gravis+ has been treated with an oral pyridostigmine bromide dosage of 5 mg every 4-6 hours (given as an immediate-release formulation) or, if parenteral therapy is necessary, an IV or IM dosage of 0.05-0.15 mg/kg (maximum single dose of 10 mg) every 4-6 hours.
In children+ with myasthenia gravis, some clinicians have suggested an oral dosage of 7 mg/kg daily (given as an immediate-release formulation and divided into 5 or 6 doses) or, if parenteral therapy is necessary, an IV or IM dosage of 0.05-0.15 mg/kg (maximum single dose of 10 mg) every 4-6 hours.
Since pyridostigmine is excreted predominantly by the kidneys, the manufacturer of Mestinon(R) states that lower dosages of pyridostigmine bromide may be required in patients with renal disease. In such patients, the dosage should be titrated carefully to produce the desired effect.
Pyridostigmine bromide extended-release tablets (Mestinon(R) Timespan(R)) are designed to slowly release the drug for a prolonged duration of action. The immediate effect of a 180-mg extended-release tablet is similar to that of a 60-mg conventional tablet, but the duration of effect is about 2.5 times longer.
Although the manufacturer states that adults may receive 180-540 mg of pyridostigmine bromide as extended-release tablets once or twice daily (with at least 6 hours between doses), this dosage form is generally used only at bedtime in patients who awaken at night or in the early morning with impairing weakness.
Changes in oral dosage may take several days to show results. When a further increase in dosage produces no corresponding increase in muscle strength, dosage should be reduced to the previous level, so that the patient receives the smallest dosage necessary to produce maximum strength.
In adults with myasthenia gravis requiring parenteral therapy, approximately 1/30 of the usual oral dose of pyridostigmine bromide has been given by IM or very slow IV injection. However, the currently available parenteral preparation (Regonol(R)) is not FDA-labeled for the treatment of myasthenia gravis.
Neonatal myasthenia gravis+ has been treated with an oral pyridostigmine bromide dosage of 5 mg every 4-6 hours (given as an immediate-release formulation) or, if parenteral therapy is necessary, an IV or IM dosage of 0.05-0.15 mg/kg (maximum single dose of 10 mg) every 4-6 hours.
In children+ with myasthenia gravis, some clinicians have suggested an oral dosage of 7 mg/kg daily (given as an immediate-release formulation and divided into 5 or 6 doses) or, if parenteral therapy is necessary, an IV or IM dosage of 0.05-0.15 mg/kg (maximum single dose of 10 mg) every 4-6 hours.
Since pyridostigmine is excreted predominantly by the kidneys, the manufacturer of Mestinon(R) states that lower dosages of pyridostigmine bromide may be required in patients with renal disease. In such patients, the dosage should be titrated carefully to produce the desired effect.
Pyridostigmine bromide is administered orally (as conventional tablets, extended-release tablets, or oral solution) or by IV injection. The drug also has been administered by IM injection, but the manufacturer of the currently available injectable preparation states that the injection is for IV use only. When used as a neuromuscular reversal agent, pyridostigmine should be administered only by trained clinicians experienced in the use of such agents.
Patients must be well ventilated and have a patent airway prior to administration of pyridostigmine and until complete recovery of normal respiration. Continuous monitoring of neuromuscular function is recommended to ensure adequate reversal from the neuromuscular block. To exclude with certainty the possibility of residual paralysis, an objective (quantitative) method of monitoring such as peripheral nerve stimulation should be used in conjunction with other clinical assessments (e.g., observation of skeletal muscle tone, respiratory measurements).
Adequate recovery of neuromuscular function generally is defined as a train-of-four (TOF) ratio of 0.9 in addition to the patient's ability to maintain satisfactory ventilation and a patent airway. When pyridostigmine is administered as conventional dosage forms for the symptomatic treatment of myasthenia gravis, the dosage should be adjusted so that larger doses are taken at times of greatest fatigue (e.g., 30-45 minutes before meals to assist patients who have difficulty eating). Pyridostigmine oral solution is especially useful for children and patients who have difficulty swallowing, and the solution may be administered through a nasogastric tube, if necessary.
Patients must be well ventilated and have a patent airway prior to administration of pyridostigmine and until complete recovery of normal respiration. Continuous monitoring of neuromuscular function is recommended to ensure adequate reversal from the neuromuscular block. To exclude with certainty the possibility of residual paralysis, an objective (quantitative) method of monitoring such as peripheral nerve stimulation should be used in conjunction with other clinical assessments (e.g., observation of skeletal muscle tone, respiratory measurements).
Adequate recovery of neuromuscular function generally is defined as a train-of-four (TOF) ratio of 0.9 in addition to the patient's ability to maintain satisfactory ventilation and a patent airway. When pyridostigmine is administered as conventional dosage forms for the symptomatic treatment of myasthenia gravis, the dosage should be adjusted so that larger doses are taken at times of greatest fatigue (e.g., 30-45 minutes before meals to assist patients who have difficulty eating). Pyridostigmine oral solution is especially useful for children and patients who have difficulty swallowing, and the solution may be administered through a nasogastric tube, if necessary.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| MESTINON 60 MG TABLET | Maintenance | Adults take 1 tablet (60 mg) by oral route 4 times per day |
| MESTINON 60 MG/5 ML SOLUTION | Maintenance | Adults take 2.5 milliliters (30 mg) by oral route every 8 hours |
| MESTINON 180 MG TIMESPAN | Maintenance | Adults take 1 tablet (180 mg) by oral route once daily |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| PYRIDOSTIGMINE ER 180 MG TAB | Maintenance | Adults take 1 tablet (180 mg) by oral route once daily |
| PYRIDOSTIGMINE BR 60 MG TABLET | Maintenance | Adults take 1 tablet (60 mg) by oral route 4 times per day |
| PYRIDOSTIGMINE 60 MG/5 ML SOLN | Maintenance | Adults take 2.5 milliliters (30 mg) by oral route every 8 hours |
| PYRIDOSTIGMINE 60 MG/5 ML CUP | Maintenance | Adults take 2.5 milliliters (30 mg) by oral route every 8 hours |
The following drug interaction information is available for MESTINON (pyridostigmine bromide):
There are 0 contraindications.
There are 1 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Selected Anticholinesterase/Corticosteroids SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: The mechanism of this interaction is unknown. CLINICAL EFFECTS: Concurrent use of these agents may contribute to increased muscle weakness and decreased response to anticholinesterases shortly after onset of corticosteroid therapy in the treatment of myasthenia gravis. Deterioration in muscle strength, including severe muscular depression, has been documented in patients with myasthenia gravis while receiving corticosteroids and anticholinesterases. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: If possible, hold anticholinesterase agents at least 24 hours before initiating corticosteroid therapy. If concurrent use is necessary, close observation of the patient is indicated and life support systems should be available. DISCUSSION: Decreased effectiveness of anticholinesterases during the period of corticosteroid-induced increased weakness probably reflects a temporary increase in the severity of the disease process itself rather than a specific, direct interaction between the two drugs. Despite the initial adverse effect, glucocorticoid (or ACTH) therapy subsequently produces improvement, beyond pre-therapy muscle strength, in most myasthenia gravis patients. In an uncontrolled study involving nine patients receiving therapeutic doses of pyridostigmine, the concurrent administration of methylprednisolone resulted in a decrease in muscle strength in 71% of treatment courses. During 57% of treatment courses, severe muscle weakness occurred, necessitating mechanical ventilation. Improvement in muscle strength and response to pyridostigmine above baseline levels occurred after methylprednisolone was discontinued. Other clinical observations have indicated that the concomitant use of these agents can affect muscle strength, although each agent alone has been used successfully in treating myasthenia gravis. |
AGAMREE, ALDOSTERONE, ALKINDI SPRINKLE, ANUCORT-HC, ANUSOL-HC, BECLOMETHASONE DIPROPIONATE, BETA 1, BETALOAN SUIK, BETAMETHASONE ACETATE MICRO, BETAMETHASONE ACETATE-SOD PHOS, BETAMETHASONE DIPROPIONATE, BETAMETHASONE SOD PHOS-ACETATE, BETAMETHASONE SOD PHOS-WATER, BETAMETHASONE SODIUM PHOSPHATE, BETAMETHASONE VALERATE, BSP 0820, BUDESONIDE, BUDESONIDE DR, BUDESONIDE EC, BUDESONIDE ER, BUDESONIDE MICRONIZED, BUPIVACAINE-DEXAMETH-EPINEPHRN, CELESTONE, CLOBETASOL PROPIONATE MICRO, CORTEF, CORTENEMA, CORTIFOAM, CORTISONE ACETATE, DEFLAZACORT, DEPO-MEDROL, DESONIDE MICRONIZED, DESOXIMETASONE, DESOXYCORTICOSTERONE ACETATE, DEXABLISS, DEXAMETHASONE, DEXAMETHASONE ACETATE, DEXAMETHASONE ACETATE MICRO, DEXAMETHASONE INTENSOL, DEXAMETHASONE ISONICOTINATE, DEXAMETHASONE MICRONIZED, DEXAMETHASONE SOD PHOS-WATER, DEXAMETHASONE SODIUM PHOSPHATE, DEXAMETHASONE-0.9% NACL, DMT SUIK, DOUBLEDEX, EMFLAZA, EOHILIA, FLUDROCORTISONE ACETATE, FLUNISOLIDE, FLUOCINOLONE ACETONIDE, FLUOCINOLONE ACETONIDE MICRO, FLUOCINONIDE MICRONIZED, FLUTICASONE PROPIONATE, FLUTICASONE PROPIONATE MICRO, HEMADY, HEMMOREX-HC, HEXATRIONE, HYDROCORTISONE, HYDROCORTISONE ACETATE, HYDROCORTISONE SOD SUCCINATE, HYDROCORTISONE-PRAMOXINE, JAYTHARI, KENALOG-10, KENALOG-40, KENALOG-80, KHINDIVI, LIDOCIDEX-I, MAS CARE-PAK, MEDROL, MEDROLOAN II SUIK, MEDROLOAN SUIK, METHYLPREDNISOLONE, METHYLPREDNISOLONE AC MICRO, METHYLPREDNISOLONE ACETATE, METHYLPREDNISOLONE SODIUM SUCC, MILLIPRED, MILLIPRED DP, MOMETASONE FUROATE, ORAPRED ODT, ORTIKOS, P-PACK PREDNISONE, PEDIAPRED, PREDNISOLONE, PREDNISOLONE ACETATE MICRONIZE, PREDNISOLONE MICRONIZED, PREDNISOLONE SODIUM PHOS ODT, PREDNISOLONE SODIUM PHOSPHATE, PREDNISONE, PREDNISONE INTENSOL, PREDNISONE MICRONIZED, PRO-C-DURE 5, PRO-C-DURE 6, PROCTOCORT, RAYOS, SOLU-CORTEF, SOLU-MEDROL, TAPERDEX, TARPEYO, TRIAMCINOLONE, TRIAMCINOLONE ACETONIDE, TRIAMCINOLONE DIACETATE, TRIAMCINOLONE DIACETATE MICRO, TRILOAN II SUIK, TRILOAN SUIK, UCERIS, VERIPRED 20, ZCORT, ZILRETTA |
There are 3 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Cholinergics/Quinidine SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: The anticholinergic properties of quinidine may oppose cholinergic drug effects. CLINICAL EFFECTS: Quinidine may antagonize the effects of cholinergic drugs in the treatment of myasthenia gravis. Cardiac slowing secondary to cholinergic drugs would tend to be prevented by quinidine. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: If both drugs are administered, observe the myasthenic patient for signs and symptoms of the disease. DISCUSSION: Caution is warranted in co-administration of these drugs due to their opposing pharmacologic properties. |
NUEDEXTA, QUINIDINE GLUCONATE, QUINIDINE SULFATE |
| Anticholinesterases/Succinylcholine SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Anticholinesterases inhibit plasma cholinesterases, delaying succinylcholine hydrolysis and prolonging its duration of action. CLINICAL EFFECTS: May see an increase in the neuromuscular blocking effects of succinylcholine, producing profound sedation, respiratory depression, coma, and/or death. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Avoid concurrent administration of anticholinesterases and succinylcholine in patients with depolarizing type (phase I) neuromuscular blockade. In addition, use with caution in the presence of a nondepolarizing type (phase II) blockade. If concurrent use is necessary, monitor patients for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. DISCUSSION: Concomitant administration of anticholinesterases and succinylcholine has been associated with prolonged respiratory depression and apnea. |
ANECTINE, QUELICIN, SUCCINYLCHOLINE CHLORIDE, SUCCINYLCHOLINE CHLORIDE-NACL |
| Anticholinesterases/Beta-Blockers SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Anticholinesterases inhibit plasma cholinesterases and increase cholinergic activity. Use of anticholinesterases may have vagotonic effects on heart rate (e.g. bradycardia). Concurrent use of anticholinesterases and beta-blockers may have additive effects on bradycardia.(1) CLINICAL EFFECTS: Concurrent use of anticholinesterases and beta-blockers may have additive effects on bradycardia.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Concurrent use of anticholinesterases and beta-blockers is not recommended. Additive effects may be increased with cardioselective beta-blockers (e.g. atenolol). Monitor patients closely if concurrent use is warranted.(1) DISCUSSION: Concurrent use of anticholinesterases and beta-blockers may have additive effects on cardiac conduction and increase the risk of bradycardia.(1) A case report of a 65 year old African American female had a witnessed a presyncopal episode followed by a true syncopal episode with concurrent use of rivastigmine and atenolol. On day 2 of the hospital stay, the patient developed bradycardia with a heart rate in the 40s and sinus pauses greater than 2 seconds. Atenolol was discontinued yet bradycardia persisted. Following discontinuation of rivastigmine, sinus pauses resolved and heart rate returned to normal.(2) A population-based cohort study in Ontario, Canada reviewed the relationship between cholinesterase inhibitor use and syncope-related outcomes over a two year period. Hospital visits for syncope were more frequent in patients receiving cholinesterase inhibitors than controls (31.5 vs 18.6 events per 1000 person-years; adjusted hazard ratio (HR) 1.76; 95% confidence interval (CI) 1.57-1.98). Other syncope-related events were also more common in patients receiving cholinesterase inhibitors than controls: hospital visits for bradycardia (6.9 vs 4.4 events per 1000 person-years; HR 1.69; 95% CI 1.32-2.15); permanent pacemaker insertion (4.7 vs 3.3 events per 1000 person-years; HR 1.49; 95% CI 1.12-2.00); and hip fracture (22.4 vs 19.8 events per 1000 person-years; HR 1.18; 95% CI 1.04-1.34).(3) A population based case-time-control study of 1,009 patients hospitalized for bradycardia within 9 months of using a cholinesterase inhibitor were reviewed for outcomes. Of these patients, 11% required pacemaker insertion during hospitalization and 4% died prior to discharge. With adjustment for temporal changes in drug utilization, hospitalization for bradycardia was associated with recent initiation of a cholinesterase inhibitor drug (adjusted odds ratio (OR) 2.13; 95% CI 1.29-3.51). Risk was similar in patients with pre-existing cardiac disease (adjusted OR 2.25; 95% CI 1.18-4.28) and those receiving negative chronotropic drugs (adjusted OR 2.34; 95% CI 1.16-4.71).(4) |
ACEBUTOLOL HCL, ATENOLOL, ATENOLOL-CHLORTHALIDONE, BETAPACE, BETAPACE AF, BETAXOLOL HCL, BISOPROLOL FUMARATE, BISOPROLOL-HYDROCHLOROTHIAZIDE, BREVIBLOC, BYSTOLIC, CARVEDILOL, CARVEDILOL ER, COREG, COREG CR, ESMOLOL HCL, ESMOLOL HCL-SODIUM CHLORIDE, ESMOLOL HCL-WATER, HEMANGEOL, INDERAL LA, INDERAL XL, INNOPRAN XL, KAPSPARGO SPRINKLE, LABETALOL HCL, LABETALOL HCL-WATER, LOPRESSOR, METOPROLOL SUCCINATE, METOPROLOL TARTRATE, METOPROLOL-HYDROCHLOROTHIAZIDE, NADOLOL, NEBIVOLOL HCL, PINDOLOL, PROPRANOLOL HCL, PROPRANOLOL HCL ER, PROPRANOLOL-HYDROCHLOROTHIAZID, RAPIBLYK, SOTALOL, SOTALOL AF, SOTALOL HCL, SOTYLIZE, TENORETIC 100, TENORETIC 50, TENORMIN, TIMOLOL MALEATE, TOPROL XL |
The following contraindication information is available for MESTINON (pyridostigmine bromide):
Drug contraindication overview.
No enhanced Contraindications information available for this drug.
No enhanced Contraindications information available for this drug.
There are 2 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Gastrointestinal obstruction |
| Urinary tract obstructive uropathy |
There are 0 severe contraindications.
There are 4 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Asthma |
| Bradycardia |
| Chronic obstructive pulmonary disease |
| Kidney disease with reduction in glomerular filtration rate (GFr) |
The following adverse reaction information is available for MESTINON (pyridostigmine bromide):
Adverse reaction overview.
No enhanced Common Adverse Effects information available for this drug.
No enhanced Common Adverse Effects information available for this drug.
There are 3 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. | None. |
| Rare/Very Rare |
|---|
|
Bradycardia Cardiac arrhythmia Hypotension |
There are 35 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abdominal pain with cramps Diarrhea Hyperhidrosis Nausea Sialorrhea Vomiting |
Abdominal distension Acute cognitive impairment Alopecia Dizziness Dry skin Dysmenorrhea Dyspnea Epistaxis Eye tearing Flatulence Hypertonia Hypoesthesia Increased bronchial secretions Increased urinary frequency Miosis Myalgia Neck pain Ocular pain Rhinorrhea Tingling sensation of hands or feet Toxic amblyopia Urinary urgency |
| Rare/Very Rare |
|---|
|
Cramps General weakness Headache disorder Malaise Muscle fasciculation Skin rash Vertigo |
The following precautions are available for MESTINON (pyridostigmine bromide):
No enhanced Pediatric Use information available for this drug.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Few data are available regarding the effects of cholinesterase inhibitors, including pyridostigmine, on the fetus because of the rarity of maternal conditions requiring the use of these drugs during pregnancy. Transient muscular weakness has occurred in 10-20% of neonates whose mothers received anticholinesterase drugs for the treatment of myasthenia gravis, although similar symptoms have also been reported in infants whose mothers were not treated with these drugs. Some experts state that oral pyridostigmine is the first-line treatment of choice for pregnant women with myasthenia gravis.
However, anticholinesterase drugs may cause uterine irritability and induce premature labor when given IV to pregnant women near term. Use of pyridostigmine in pregnant women requires that the possible benefits be weighed against the potential risks.
However, anticholinesterase drugs may cause uterine irritability and induce premature labor when given IV to pregnant women near term. Use of pyridostigmine in pregnant women requires that the possible benefits be weighed against the potential risks.
Since it is not known whether pyridostigmine is distributed into milk, the drug should be used with caution in nursing women.
No enhanced Geriatric Use information available for this drug.
The following prioritized warning is available for MESTINON (pyridostigmine bromide):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for MESTINON (pyridostigmine bromide)'s list of indications:
| Myasthenia gravis | |
| G70.0 | Myasthenia gravis |
| G70.00 | Myasthenia gravis without (acute) exacerbation |
| G70.01 | Myasthenia gravis with (acute) exacerbation |
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