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Pronunciation |
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(fye
zoe STIG
meen) |
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U.S. Brand
Names |
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Antilirium® |
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Generic
Available |
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Yes: Ophthalmic |
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Synonyms |
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Eserine Salicylate; Physostigmine Salicylate; Physostigmine
Sulfate |
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Pharmacological Index |
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Acetylcholinesterase Inhibitor; Ophthalmic Agent,
Antiglaucoma |
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Use |
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Reverse toxic CNS effects caused by anticholinergic drugs; used as miotic in
treatment of glaucoma |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to physostigmine or any component; GI or GU obstruction;
physostigmine therapy of drug intoxications should be used with extreme caution
in patients with asthma, gangrene, severe cardiovascular disease, or mechanical
obstruction of the GI tract or urogenital tract. In these patients,
physostigmine should be used only to treat life-threatening
conditions. |
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Warnings/Precautions |
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Use with caution in patients with epilepsy, asthma, diabetes, gangrene,
cardiovascular disease, bradycardia. Discontinue if excessive salivation or
emesis, frequent urination or diarrhea occur. Reduce dosage if excessive
sweating or nausea occurs. Administer I.V. slowly or at a controlled rate not
faster than 1 mg/minute. Due to the possibility of hypersensitivity or
overdose/cholinergic crisis, atropine should be readily available; ointment may
delay corneal healing, may cause loss of dark adaptation; not intended as a
first-line agent for anticholinergic toxicity or Parkinson's
disease. |
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Adverse
Reactions |
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Ophthalmic:
>10%:
Ocular: Lacrimation, marked miosis, blurred vision, eye pain
Miscellaneous: Diaphoresis
1% to 10%:
Central nervous system: Headache, browache
Dermatologic: Burning, redness
Systemic:
>10%:
Gastrointestinal: Nausea, salivation, diarrhea, stomach pains
Ocular: Lacrimation
Miscellaneous: Diaphoresis
1% to 10%:
Cardiovascular: Palpitations, bradycardia
Central nervous system: Restlessness, nervousness, hallucinations, seizures
Genitourinary: Frequent urge to urinate
Neuromuscular & skeletal: Muscle twitching
Ocular: Miosis
Respiratory: Dyspnea, bronchospasm, respiratory paralysis, pulmonary edema
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Overdosage/Toxicology |
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Symptoms of overdose include muscle weakness, blurred vision, excessive
sweating, tearing and salivation, nausea, vomiting, bronchospasm, seizures
If physostigmine is used in excess or in the absence of an anticholinergic
overdose, patients may manifest signs of cholinergic toxicity. At this point a
cholinergic agent (eg, atropine 0.015-0.05 mg/kg) may be necessary.
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Drug
Interactions |
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Increased toxicity: Bethanechol, methacholine, succinylcholine may increase
neuromuscular blockade with systemic administration |
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Stability |
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Do not use solution if cloudy or dark brown |
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Mechanism of
Action |
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Inhibits destruction of acetylcholine by acetylcholinesterase which
facilitates transmission of impulses across myoneural junction and prolongs the
central and peripheral effects of acetylcholine |
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Pharmacodynamics/Kinetics |
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Onset of action: Ophthalmic instillation: Within 2 minutes; Parenteral:
Within 5 minutes
Duration: Ophthalmic: 12-48 hours; Parenteral: 0.5-5 hours
Absorption: I.M., ophthalmic, S.C.: Readily absorbed
Distribution: Crosses the blood-brain barrier readily and reverses both
central and peripheral anticholinergic effects
Duration: Ophthalmic: 12-48 hours; Parenteral: 0.5-5 hours
Metabolism: In the liver
Half-life: 15-40 minutes
Elimination: Via hydrolysis by cholinesterases |
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Usual Dosage |
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Children: Anticholinergic drug overdose: Reserve for life-threatening
situations only: I.V.: 0.01-0.03 mg/kg/dose, (maximum: 0.5 mg/minute); may
repeat after 5-10 minutes to a maximum total dose of 2 mg or until response
occurs or adverse cholinergic effects occur
Adults: Anticholinergic drug overdose:
I.M., I.V., S.C.: 0.5-2 mg to start, repeat every 20 minutes until response
occurs or adverse effect occurs
Repeat 1-4 mg every 30-60 minutes as life-threatening signs (arrhythmias,
seizures, deep coma) recur; maximum I.V. rate: 1 mg/minute
Ophthalmic:
Ointment: Instill a small quantity to lower fornix up to 3 times/day
Solution: Instill 1-2 drops into eye(s) up to 4 times/day
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Administration |
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Infuse slowly I.V. at a maximum rate of 0.5 mg/minute in children or 1
mg/minute in adults |
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Test
Interactions |
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aminotransferase [ALT
(SGPT)/AST (SGOT)] (S),
amylase
(S) |
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Mental Health: Effects
on Mental Status |
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May cause restlessness, nervousness, or hallucinations |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Systemic: Maintain adequate hydration (2-3 L/day of fluids unless instructed
to restrict fluid intake). May cause dizziness, drowsiness, or hypotension (rise
slowly from sitting or lying position and use caution when driving or climbing
stairs); vomiting or loss of appetite (frequent small meals, frequent mouth
care, chewing gum, or sucking lozenges may help); or diarrhea (boiled milk,
yogurt, or buttermilk may help). Report persistent abdominal discomfort;
significantly increased salivation, sweating, tearing, or urination; flushed
skin; chest pain or palpitations; acute headache; unresolved diarrhea; excessive
fatigue, insomnia, dizziness, or depression; increased muscle, joint, or body
pain; vision changes or blurred vision; or shortness of breath or wheezing.
Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend
to be pregnant. Consult prescriber if breast-feeding. |
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Nursing
Implications |
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Too rapid administration (I.V. rate not to exceed 1 mg/minute) can cause
bradycardia, hypersalivation leading to respiratory difficulties and seizures
Monitor heart rate, respiratory rate |
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Dosage Forms |
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Injection, as salicylate: 1 mg/mL (2 mL)
Ointment, ophthalmic, as sulfate: 0.25% (3.5 g, 3.7 g) |
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References |
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Brier RH, "Physostigmine Dose for Tricyclic Drug Overdose," Ann Intern
Med, 1978, 89(4):579.
Caine ED, "Anticholinergic Toxicity," N Engl J Med, 1979,
300(22):1278.
Dysken MW and Janowsky DS,
"Dose-Related Physostigmine-Induced Ventricular Arrhythmia: Case Report," J
Clin Psychiatry, 1985, 46(10):446-7.
Jenike MA, Albert MS, Heller H, et al,
"Oral Physostigmine Treatment for Patients With Presenile and Senile Dementia of the Alzheimer's Type: A Double-Blind Placebo-Controlled Trial,"
J Clin Psychiatry, 1990, 51(1):3-7.
Pentel P and Peterson CD,
"Asystole Complicating Physostigmine Treatment of Tricyclic Antidepressant Overdose,"
Ann Emerg Med, 1980, 9(11):588-90.
Tomassoni AJ and Prybys K,
"Isolated Central Effects of Atropine Eye Drops Reversed by Physostigmine,"
Clin Toxicol, 1995, 33(5):505.
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