Yes: Ophthalmic

Acetylcholinesterase Inhibitor; Ophthalmic Agent, Antiglaucoma

Reverse toxic CNS effects caused by anticholinergic drugs; used as miotic in treatment of glaucoma

C

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.

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.

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

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.

Increased toxicity: Bethanechol, methacholine, succinylcholine may increase neuromuscular blockade with systemic administration

Do not use solution if cloudy or dark brown

Inhibits destruction of acetylcholine by acetylcholinesterase which facilitates transmission of impulses across myoneural junction and prolongs the central and peripheral effects of acetylcholine

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

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

Infuse slowly I.V. at a maximum rate of 0.5 mg/minute in children or 1 mg/minute in adults

aminotransferase [ALT (SGPT)/AST (SGOT)] (S), amylase (S)

May cause restlessness, nervousness, or hallucinations

None reported

No information available to require special precautions

No effects or complications reported

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.

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

Injection, as salicylate: 1 mg/mL (2 mL)

Ointment, ophthalmic, as sulfate: 0.25% (3.5 g, 3.7 g)

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.