physostigmine [IM/IV]

Adult Dosing

Post-anesthesia Care

Anticholinergic toxicity

2 mg IM/IV; rate of IV administration should be 1 mg/minute
Repeat dose, if life-threatening symptoms such as arrhythmia, convulsions or coma occur

Note:

Provide appropriate supportive measures in all cases of poisoning
Keep appropriate antidote, such as atropine sulfate, readily available to manage a possible cholinergic crisis

Pediatric Dosing

Anticholinergic toxicity

0.02 mg/kg IM/IV; rate of IV administration should be 0.5 mg/minute
If toxic effects persist or there is no sign of cholinergic effects, repeat dose at intervals of 5-10 minutes until therapeutic effect is achieved or a maximum of 2 mg dose is attained

Note:

Provide appropriate supportive measures in all cases of poisoning
Keep appropriate antidote, such as atropine sulfate, readily available to manage a possible cholinergic crisis

[Outline]

Indications ⬆ ⬇

To reverse the neurological effects of drugs capable of causing anticholinergic syndrome with clinical or toxic doses

Contraindications ⬆ ⬇

Hypersensitivity to any of the ingredients of the product
Hypersensitivity to sulfites
Asthma
Gangrene
Diabetes mellitus
Cardiovascular disease
Arrhythmias
Angle-closure glaucoma
Intestinal obstruction
Urogenital tract obstruction
Vagotonic state
Concomitant use of choline esters
Co-administration of depolarizing neuromuscular blockers (decamethonium, succinylcholine)
Concomitant use of atropine (for post-anesthesia)
Neonates

Black Box Warnings ⬆ ⬇

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Hepatic Dose Adjustment

Warnings/Precautions ⬆ ⬇

The product contains sodium bisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening asthmatic episodes in susceptible individuals, particularly in asthmatic people
Discontinue therapy if excessive symptoms of salivation, emesis, urination and defecation occur. Consider dose reduction in case of excessive nausea or sweating
For IV use, ensure administration at a slow, controlled rate (1 mg/minute). Rapid administration may result in bradycardia, hypersalivation leading to respiratory difficulties and convulsions
A cholinergic crisis may occur as a result of overdosage of physostigmine injection
Atropine sulfate, an antagonist and antidote for physostigmine, should be readily available to manage any possible hypersensitivity reactions

Cautions: Use cautiously in

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:C

Breastfeeding: Safety unknown. Manufacturer advises considering risk-benefit analysis before administering to nursing women.

Adverse Reactions ⬆ ⬇

CV: Bradycardia, severe hypotension, palpitations, AV block, arrhythmias, cardiac arrest
CNS: Convulsions, dizziness, restlessness, hallucinations, CNS stimulation, syncope, paralysis, headache
GI: Nausea, vomiting, hypersalivation, abdominal bloating/cramps, diarrhea, flatulence
GU: Urinary frequency or urgency
EENT: Increased lacrimation, miosis, blurred vision, rhinorrhea
RESP: Bronchospasm, respiratory depression, respiratory arrest, respiratory paralysis, increased pulmonary secretions, pulmonary edema, dyspnea
MUSC: Muscle twitching, muscle weakness, fasciculations
MISC: Anaphylaxis, cholinergic crisis, diaphoresis

Clinical Pharmacology ⬆ ⬇

Cholinesterase inhibitors; inhibits the destructive action of acetylcholinesterase, which increases the concentration of acetylcholine at the sites of cholinergic transmission, thereby prolonging the effect of acetylcholine at cholinergic synapses
Readily absorbed from IM sites
Quickly hydrolyzed by tissue/plasma cholinesterases
Excreted in urine minimally
Half-life: 15-40 min

Brands and Availability ⬆ ⬇