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physostigmine (Antilirium, Isopto Eserine)
Tradenames: Antilirium, Isopto Eserine.
Indications:
1) reversal of toxic CNS effects caused by anticholinergic agents*
2) ointment used as a miotic agent in treatment of glaucoma
* bicarbonate is 1st line for tricyclic antidepressant overdose [4]
Contraindications:
- tricyclic antidepressant overdose (may precipitate asystole) [4]
Dosage:
1) 0.5-2 mg IM or IV (slowly, < 1 mg/min)
2) repeat in 10-30 minutes if desired response not obtained
3) ophthalmic ointment QHS
Injection: (as salicylate): 1 mg/mL (2 mL).
Ointment: (as sulfate) 0.025% (3.5 g)
Pharmacokinetics:
1) readily absorbed from GI tract, mucus membranes & subcutaneous tissue
2) freely crosses blood-brain barrier after IM or IV administration
3) onset of action is 3-8 minutes
4) duration of action is 30 minutes to 5 hours
5) inactivated via hydrolysis by cholinesterase
6) elimination 1/2life is 15-40 minutes
Adverse effects:
1) ophthalmic agent
a) common (> 10%)
- lacrimation, sweating, excessive miosis, blurred vision, eye pain
b) less common (1-10%)
- burning, headache, browache, redness
2) systemic agent
a) common (> 10%)
- nausea, sweating, lacrimation, salivation, diarrhea, epigastric pain
b) less common (1-10%)
- frequent urge to urinate, restlessness, miosis, nervousness, palpitations, bradycardia, hallucinations, seizures, muscle twitching, dyspnea, bronchospasm, respiratory tract paralysis, pulmonary edema
c) other [1]
- nausea/vomiting
- epigastric pain
- dyspnea
- CNS stimulation
- irregular pulse
- weakness
- seizures [3] (rare)
Mechanism of action:
1) reversible inhibitor of cholinesterase
2) produces generalized cholinergic responses:
a) miosis
b) increased tone of intestinal musculature
c) bronchial constriction
d) increased secretion of salivary & sweat glands
Interactions
drug interactions
drug adverse effects of cholinesterase inhibitors
General
alkaloid
carbamate
cholinesterase inhibitor
Properties
MISC-INFO: elimination route PLASMA
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Medications Can Cause Seizures
Prescriber's Letter 10(3):16 2003
Detail-Document#: 190320
(subscription needed) http://www.prescribersletter.com
- Medical Knowledge Self Assessment Program (MKSAP) 17,
American College of Physicians, Philadelphia 2015