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neostigmine (Rx)Brand and Other Names:Prostigmin, Bloxiverz

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution (methylsulfate salt; Bloxiverz)

  • 0.5mg/mL
  • 1mg/mL

tablet (bromide salt; Prostigmin)

  • 15mg
more...

Myasthenia Gravis

Acute: 0.5-2.5 mg IV/IM/SC qDay 

Maintenance: 15-375 mg/day PO divided q6-8hr

Use injectable with 0.6-1.2 mg atropine IV to counteract muscarinic effects

Myasthenia Gravis Diagnosis

0.022 mg/kg IM x1 

Discontinue all anticholinesterase agents for >8 hr

Give atropine 0.011 mg/kg IV (if IM give 30 minutes before) with neostigmine 0.022 mg/kg IM

If cholinergic response, stop test and give 0.4-0.6 mg atropine IV

If inconclusive, retest another day with neostigmine 0.031 mg/kg IM preceded by 0.016 mg/kg atropine

Nondepolarizing Neuromuscular Blockade, Reversal

0.03-0.07 mg/kg IV will generally achieve a TOF twitch ratio of 90% within 10-20 minutes of administration

Not to exceed 0.07 mg/kg or a cumulative total of 5 mg, whichever dose is less Inject by slow IV over at least 1 minute

Dose selection should be based on the extent of spontaneous recovery that has occurred at the time of administration, the half-life of the NMBA being reversed, and whether there is a need to rapidly reverse the NMBA

Administer an IV anticholinergic (eg, atropine, glycopyrrolate) prior to, or concomitantly with neostigmine for NMB reversal; if bradycardia present, give anticholinergic before neostigmine

0.03 mg/kg

  • Use for reversal of NMBAs with shorter half-lives (eg, rocuronium), OR
  • When the first twitch response to the TOF stimulus is substantially >10% of baseline or when a second twitch is present

0.07 mg/kg

  • Use for NMBAs with longer half-lives (eg, vecuronium, pancuronium), OR
  • When the first twitch response is relatively weak (ie, not substantially >10% of baseline), OR
  • There is need for more rapid recovery

Post-Op Distention or Urinary Retention

Prevention: 0.25mg IM after surgery. Repeat q4-6hr for 2-3 days

Treatment: 0.5-1 mg IM and up to q3hr PRN (for 5 doses for retention)

Colonic Pseudo-obstruction (Orphan)

Orphan designation for treatment of acute colonic pseudo-obstruction

Orphan sponsor

  • Luitpold Pharmaceuticals, Inc.; One Luitpold Drive, P. O. Box 9001; Shirley, NY 11967

Administration

IV TOF monitoring for NMB reversal

  • Peripheral nerve stimulation devices capable of delivering a train-of-four (TOF) stimulus are essential to effectively and safely adjust IV dose
  • There must be a twitch response to the first stimulus in the TOF of at least 10% of its baseline level (ie, the response before NMBA administration, prior to neostigmine)

Dosage Forms & Strengths

injectable solution (methylsulfate salt; Bloxiverz)

  • 0.5mg/mL
  • 1mg/mL

tablet (bromide salt; Prostigmin)

  • 15mg
more...

Myasthenia Gravis Diagnosis

Use with atropine

0.025-0.04 mg/kg IM x1 

Myasthenia Gravis Treatment

Use with atropine

0.01-0.04 mg/kg IV/IM/SC q2-3hr PRN 

2 mg/kg/day divided q4hr PO; no more than 375mg/day

Nondepolarizing Neuromuscular Blockade, Reversal

Adult guidelines should be followed when administered to pediatric patients, including neonates; pediatric patients require doses similar to those for adults

0.03-0.07 mg/kg IV will generally achieve a TOF twitch ratio of 90% within 10-20 minutes of administration

Not to exceed 0.07 mg/kg or a cumulative total of 5 mg, whichever dose is less Inject by slow IV over at least 1 minute

Dose selection should be based on the extent of spontaneous recovery that has occurred at the time of administration, the half-life of the NMBA being reversed, and whether there is a need to rapidly reverse the NMBA

Administer an IV anticholinergic (eg, atropine, glycopyrrolate) prior to, or concomitantly with neostigmine for NMB reversal; if bradycardia present, give anticholinergic before neostigmine

0.03 mg/kg

  • Use for reversal of NMBAs with shorter half-lives (eg, rocuronium), OR
  • When the first twitch response to the TOF stimulus is substantially >10% of baseline or when a second twitch is present

0.07 mg/kg

  • Use for NMBAs with longer half-lives (eg, vecuronium, pancuronium), OR
  • When the first twitch response is relatively weak (ie, not substantially >10% of baseline), OR
  • There is need for more rapid recovery

Administration

IV TOF monitoring for NMB reversal

  • Peripheral nerve stimulation devices capable of delivering a train-of-four (TOF) stimulus are essential to effectively and safely adjust IV dose
  • There must be a twitch response to the first stimulus in the TOF of at least 10% of its baseline level (ie, the response before NMBA administration, prior to neostigmine)
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Interactions

Interaction Checker

neostigmine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Allergic: Allergic reactions and anaphylaxis

            Neurologic: Dizziness, convulsions, loss of consciousness, drowsiness, headache, dysarthria, miosis and visual changes

            Cardiovascular: Cardiac arrhythmias (including bradycardia, tachycardia, A-V block and nodal rhythm) and nonspecific EKG changes have been reported, as well as cardiac arrest, syncope and hypotension (predominantly with parenteral dosage form)

            Respiratory: Increased oral, pharyngeal and bronchial secretions, and dyspnea; respiratory depression, respiratory arrest and bronchospasm have been reported following the use of the injectable form

            Dermatologic: Rash and urticaria

            Gastrointestinal: Nausea, emesis, flatulence, and increased peristalsis and salivation

            Genitourinary: Urinary frequency

            Musculoskeletal: Muscle cramps and spasms, arthralgia

            Miscellaneous: Diaphoresis, flushing and weakness

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            Warnings

            Contraindications

            Hypersensitivity, previous history of reaction to bromides

            Peritonitis or mechanical GI or urinary tract obstruction

            Cautions

            Caution in epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias, peptic ulcer

            Neonates; because of self-limiting nature of myasthenia gravis, reduce daily dosage gradually released until drug can be withdrawn

            Avoid large doses in situations where there might be an increased absorption rate from the intestinal tract; caution when coadministered with anticholinergic drugs because of decreased GI motility

            Differentiate between myasthenic crisis and cholinergic crisis caused by overdosage of neostigmine; both conditions result in extreme muscle weakness but require radically different treatment

            Anticholinesterase insensitivity can develop

            If excess cholinergic symptoms develop, discontinue therapy

            Atropine and epinephrine must be available to treat a hypersensitivity reaction

            Not recomended for use in patients with vagotonia

            May prolong the phase 1 block of depolarizing muscle relaxants

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            Pregnancy & Lactation

            Pregnancy: There are no adequate or well-controlled studies in pregnant women; not known whether neostigmine can cause fetal harm or affect reproductive capacity; should administer only if clearly needed

            Lactation: Unknown if distributed in human breast milk; use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Competitive inhibitor of cholinesterase resulting in decreased hydrolysis of acetylcholine by cholinesterase; by reducing the breakdown of acetylcholine, neostigmine increases acetylcholine in the synaptic cleft which competes for the same binding site as nondepolarizing neuromuscular blocking agents, and reverses the neuromuscular blockade

            Absorption

            Bioavailability: 1-2% (PO); general PO:IV equivalence ~15 mg neostigmine bromide PO is equivalent to 0.5 mg neostigmine methylsulfate parenteral

            Onset: 1-20 min (IV); 20-30 min (IM)

            Duration: 2.5-4 hr (IM); 1-2 hr (IV)

            Peak plasma time: 30 min (IM); 1-2 hr (PO)

            Distribution

            Protein bound: 15-25% to albumin (PO)

            Metabolism

            Liver microsomal enzymes and hydrolysis by cholinesterase enzymes

            Elimination

            Half-Life: 47-60 min (IV); 51-90 min (IM); 42-60 min (PO)

            Excretion: 50% urine

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            Administration

            IV Incompatibilities: none specified

            IV Administration: slow IV injection

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            Images

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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