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pyridostigmine (Rx)Brand and Other Names:Mestinon, Regonol

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

inj solution

  • 5mg/mL

tablet, controlled release

  • 180mg

tablet

  • 60mg

syrup

  • 60mg/5mL (240mL)
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Myasthenia Gravis

Tablets/syrup: 600 mg/day spaced to provide maximum relief

Sustained release: 180-540 mg PO qDay or q12hr; not to exceed 1.5 g/day

Reversal of Nondepolarizing Muscle Relaxants

0.1-0.25 mg/kg/dose 

10-20 mg generally effective; full recovery may occur as early as <15 min but may require >30 min

To minimize side effects 0.6-1.2 mg IV atropine sulfate recommended immediately prior to pyridostigmine

Pretreatment for Soman Nerve Gas Exposure

30 mg PO q8hr beginning several hours prior to exposre

Discontinue at first sign of nerve agent exposure then begin atropine and pralidoxime

Dosage Forms & Strengths

inj solution

  • 5mg/mL

tablet, controlled release

  • 180mg

tablet

  • 60mg

syrup

  • 60mg/5mL (240mL)
more...

Myasthenia Gravis

Children

  • 7 mg/kg/day PO divided q4hr
  • 0.05-0.15 mg/kg IV/IM q4-6hr; not to exceed 10 mg/dose 

Neonates

  • 5 mg PO q4-6hr
  • 0.05-0.15 mg/kg IV/IM q4-6hr; not to exceed 10 mg/dose 

Reversal of Nondepolarizing Muscle Relaxants

0.1-0.25 mg/kg/dose IV

Dosing range: 0.1-0.25 mg/kg/dose; full recovery may occur as early as <15 min but may require >30 min

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Interactions

Interaction Checker

pyridostigmine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Fewer GI effects than neostigmine

            Frequency Not Defined

            Cholinergic effects (N/V, increases peristalsis, increases salivation, urinary frequency

            Weakness

            Hypotension

            ECG changes

            Loss of consciousness

            Convulsions

            Drowsiness

            Thrombophlebitis

            Urticaria

            Arrhythmia

            Laryngospasm

            Bradycardia

            Cardiac standstill (rare)

            Cholinergic crisis (rare)

            Transient rash in bromide-sensitive patients

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            Warnings

            Black Box Warning

            Therapy must be administered by trained personnel

            Contraindications

            Hypersensitivity

            Mechanical intestinal or urinary obstruction

            Cautions

            Caution in epilepsy, asthma, COPD, recent MI, hypertension, vagotonia, hyperthyroidism, dysrhythmia

            Keep atropine and epinephrine immediately available to treat hypersensitivity reactions resulting from therapy

            Injection unstable in alkaline solutions

            If symptoms of excess cholinergic activity occur discontinue therapy

            Anticholinesterase sensitivity may develop for brief or prolonged periods

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Compatible

            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

            Anticholinesterase agent which inhibits metabolism of acetylcholine by acetylcholinesterase thereby enhancing its cholinergic effects fascilitating impulses across myoneural junction

            Pharmacokinetics

            Half-Life: 1-2 hr (IV)

            Onset: 15-30 min (PO/IM); 2-5 min (IV)

            Duration: 6-8 hr (PO); 2-3 hr (IV)

            Bioavailability: 10-20%

            Distribution: ~19 L

            Metabolism: Liver microsomal enzymes

            Metabolites: 3-hydroxy-N-methylpyridinium

            Total Body Clearance: 8.5-9.7 mL/min/kg

            Excretion: Urine (80-90%)

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            Administration

            IV Compatibilities

            Syringe: glycopyrrolate

            Y-site: heparin, hydrocortisone Na-succinate, KCl, vit B/C

            Other Information

            IV Administration: very slow 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.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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