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Drug overview for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
Generic name: NEOSTIGMINE METHYLSULFATE
Drug class: Antimyasthenic Agents
Therapeutic class: Locomotor System
Neostigmine methylsulfate is an anticholinesterase agent.
No enhanced Uses information available for this drug.
Generic name: NEOSTIGMINE METHYLSULFATE
Drug class: Antimyasthenic Agents
Therapeutic class: Locomotor System
Neostigmine methylsulfate is an anticholinesterase agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
NEOSTIGMINE 10 MG/10 ML VIAL
NEOSTIGMINE 5 MG/10 ML VIAL
The following indications for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate) have been approved by the FDA:
Indications:
Reversal of neuromuscular blockade
Professional Synonyms:
Reversal of muscle blockade
Indications:
Reversal of neuromuscular blockade
Professional Synonyms:
Reversal of muscle blockade
The following dosing information is available for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
No enhanced Dosing information available for this drug.
Neostigmine methylsulfate is administered by slow IV injection (over a period of at least 1 minute). The drug also has been administered by IM or subcutaneous injection+, but the manufacturer of the currently available injectable preparation labeled for reversal of neuromuscular blocking agents states that the injection is for IV use only. Neostigmine methylsulfate injection should be stored at controlled room temperature (20-25degreesC) but may be exposed to temperatures ranging from 15-30degreesC; the injection should be stored in the original carton until time of use and protected from light.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
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, PYQUVI, 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 NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
Drug contraindication overview.
*Known hypersensitivity to neostigmine. *Mechanical obstruction of the intestinal or urinary tract. *Peritonitis.
*Known hypersensitivity to neostigmine. *Mechanical obstruction of the intestinal or urinary tract. *Peritonitis.
There are 4 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Colonic necrosis |
| Gastrointestinal obstruction |
| Peritonitis |
| Urinary tract obstructive uropathy |
There are 3 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Cardiac arrhythmia |
| Coronary artery disease |
| Sinus bradycardia |
There are 0 moderate contraindications.
The following adverse reaction information is available for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
Adverse reaction overview.
The most common adverse effects of neostigmine include bradycardia, nausea, and vomiting. Adverse effects of neostigmine methylsulfate generally are due to exaggerated pharmacologic effects of the drug, particularly at muscarinic-cholinergic receptors.
The most common adverse effects of neostigmine include bradycardia, nausea, and vomiting. Adverse effects of neostigmine methylsulfate generally are due to exaggerated pharmacologic effects of the drug, particularly at muscarinic-cholinergic receptors.
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 NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
Neostigmine may be used in pediatric patients of all ages to reverse the effects of nondepolarizing neuromuscular blocking agents after surgery. The available data indicate that efficacy and pharmacokinetics of neostigmine are similar across all pediatric age groups and also similar to those in adults when the same dosing guidelines are applied. Based on limited data, neostigmine dosing requirements for reversal of neuromuscular blockade may be lower in infants and neonates than in older pediatric patients and adults; however, pediatric patients have a greater risk of incomplete reversal of neuromuscular blockade because of their decreased respiratory reserve.
Therefore, the risks of administering higher doses of neostigmine (up to maximum recommended dosage) should not outweigh the risks associated with incomplete reversal in this age group. Because pediatric patients, particularly neonates and infants, may be more sensitive to changes in heart rate, the effects of anticholinergic agents should be observed prior to administration of neostigmine to lessen the probability of bradycardia and hypotension.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Therefore, the risks of administering higher doses of neostigmine (up to maximum recommended dosage) should not outweigh the risks associated with incomplete reversal in this age group. Because pediatric patients, particularly neonates and infants, may be more sensitive to changes in heart rate, the effects of anticholinergic agents should be observed prior to administration of neostigmine to lessen the probability of bradycardia and hypotension.
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
It is not known whether neostigmine can cause fetal harm when administered to pregnant women or affect reproductive capacity; the drug should be used during pregnancy only when clearly indicated as no adequate or well-controlled studies of the drug have been conducted in pregnant women. Administration of anticholinesterase drugs such as neostigmine to pregnant women near term may cause uterine irritability and induce premature labor. There are limited data from animal reproduction studies; in such studies, no teratogenic or other adverse effects were identified; however, drug exposure was well below the predicted exposures in humans.
It is not known whether neostigmine is distributed into human milk. Caution should be exercised when the drug is used in nursing women.
Because geriatric patients may have decreased renal function, neostigmine should be used with caution and increased monitoring in this age group. The duration of action of neostigmine is prolonged in geriatric patients; however, such patients also experience slower spontaneous recovery from neuromuscular blocking agents. Geriatric patients should be monitored for longer periods of time to ensure that additional doses of neostigmine are not necessary to adequately reverse neuromuscular blockade.
The following prioritized warning is available for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for NEOSTIGMINE METHYLSULFATE (neostigmine methylsulfate)'s list of indications:
| Reversal of neuromuscular blockade | |
| T48.1x1A | Poisoning by skeletal muscle relaxants [neuromuscular blocking agents], accidental (unintentional), initial encounter |
| T48.1x2A | Poisoning by skeletal muscle relaxants [neuromuscular blocking agents], intentional self-harm, initial encounter |
| T48.1x3A | Poisoning by skeletal muscle relaxants [neuromuscular blocking agents], assault, initial encounter |
| T48.1x4A | Poisoning by skeletal muscle relaxants [neuromuscular blocking agents], undetermined, initial encounter |
| T48.1x5A | Adverse effect of skeletal muscle relaxants [neuromuscular blocking agents], initial encounter |
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