neostigmine

CLINICAL USE

Myasthenia gravis Antagonist to non-depolarising neuromuscular blockade

DOSE IN NORMAL RENAL FUNCTION

Myasthenia gravis: neostigmine bromide 15–30 mg at suitable intervals throughout day – total daily dose 75–300 mg; Neostigmine metilsulfate, IM, SC, 1–2.5 mg – usual total daily dose 5–20 mgAntagonist to non-depolarising neuromuscular blockade: 50–70 mcg/kg over 1 minute; maximum dose 5 mg

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :223.3 (303.2 as bromide); (334.4 as metilsulphate)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :15–25

%Excreted unchanged in urine &nbsp &nbsp : 50

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.5–1

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :0.8–1.5/3

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : 50–100% of normal dose

10 to 20 &nbsp &nbsp : 50–100% of normal dose

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : 50–100% of normal dose

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAminoglycosides, clindamycin and polymyxins antagonise effects of neostigmine

ADMINISTRATION

Reconstition

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Route

Neostigmine bromide: Oral Neostigmine metilsulfate: SC, IM, IV

Rate of Administration

IV: Very slowly

Comments

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OTHER INFORMATION

Neostigmine 0.5 mg IV = 1–1.5 mg IM/SC =15 mg orallyWhen used for reversal of non- depolarising neuromuscular blockade, atropine (0.6–1.2 mg IV) or glycopyrronium should be given before or with neostigmine in order to prevent bradycardia, excessive salivation and other muscarinic actions of neostigmineThe physicochemical nature of neostigmine may tend to encourage its removal by various renal replacement therapies.

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