Physostigmine

Physostigmine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

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Overview

Physostigmine is a central nervous system agent, cholinesterase inhibitor and anti glaucoma that is FDA approved for the treatment of clinical or toxic dosages of drugs capable of producing the anticholinergic syndrome. Common adverse reactions include diaphoresis, abnormal defecation (diarrhea), excessive salivation and nausea and vomiting.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Past Anesthesia Care

• Dosage: 0.5 to 1.0 mg intramuscularly or intravenously. IV administration should be at allow controlled rate of no more than 1 mg per minute. Dosage may be repeated at intervals of 10 to 30 minutes if desired patient response is not obtained.

Clinical or Toxic Dosages of Drugs Capable of Producing the Anticholinergic Syndrome

• Case report of a 68-year-old male patient admitted to the ICU for treatment of a severe thioridazine intoxication.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Physostigmine in adult patients.

Non–Guideline-Supported Use

Reversal of Postoperative Reactions to Scopolamine

• Dosage: 1.0-1.2 milligrams IV. Unique dose.

Reversal of Postoperative Reactions to Scopolamine in Post-Partum

• Clinical trial of 5 postpartum patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Clinical or Toxic Dosages of Drugs Capable of Producing the Anticholinergic Syndrome

• Case report of a 27 month-old patient with amitriptyline overdose.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Physostigmine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Physostigmine in pediatric patients.

Contraindications

• Physostigmine Salicylate Injection should not be used in the presence of asthma, gangrene, diabetes, cardiovascular disease, mechanical obstruction of the intestine or urogenital tract or any vagotonic state, and in patients receiving choline esters and depolarizing neuromuscular blocking agents (decamethonium, succinylcholine).
• For post-anesthesia, the concomitant use of atropine with physostigmine salicylate is not recommended, since the atropine antagonizes the action of physostigmine.

Warnings

• Contains sodium bisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people.
• If excessive symptoms of salivation, emesis, urination and defecation occur, the use of Physostigmine Salicylate Injection should be terminated. If excessive sweating or nausea occur, the dosage should be reduced.
• Intravenous administration should be at a slow, controlled rate, no more than 1 mg per minute. Rapid administration can cause bradycardia, hypersalivation leading to a respiratory difficulties and possible convulsions. An overdosage of Physostigmine Salicylate Injection can cause a cholinergic crisis.

Adverse Reactions

Clinical Trials Experience

Cardiovascular Effects

• Asystole
• Bradyarrhythmia
  • Case Report of Alzheimer patients being treated with Physostigmine
  • Case Report of a patient treated with physostigmine for post-operative anesthesia with Scopolamine.
• Cardiac dysrhythmia
• Hypertension
  • Case report of a 72 year-old patient treated with 0.5 mg q2h for Alzheimer's disease.
• Increased cardiac output
• Increased pulmonary arterial wedge pressure
• Tachycardia
  • Dosage: 2mg may cause tachycardia

Endocrine/Metabolic Effects

• Increased leves of growth hormone
  • Dosage: 12.5 mg/kg.

Gastrointestinal Effects

• Abnormal defecation: diarrhea
• Excessive salivation
• Hyperperistalsis
• Nausea and vomiting

Immunological Effects

• Hypersensitivity reactions

Musculoeskeletal Effects

• Muscle fasciculation
• Muscle weakness

Neurological Effects

• Seizures
• Dosage: May appear if doses surpass1 mg/min in adults or 0.5 mg/min in children.

Psychiatric Depression

• Depression

Renal Effects

• Polyuria
• Urinary incontinence

Respiratory Effects

• Bronchospasm
• Excessive bronchial secretion

Postmarketing Experience

There is limited information regarding Physostigmine Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Physostigmine Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• Safe use in pregnancy and lactation has not been established; therefore, use in pregnant women, nursing mothers or women who may become pregnant requires that possible benefits be weighed against possible hazards to mother and child.

Pregnancy Category (AUS): C

• Safe use in pregnancy and lactation has not been established; therefore, use in pregnant women, nursing mothers or women who may become pregnant requires that possible benefits be weighed against possible hazards to mother and child.

Labor and Delivery

There is no FDA guidance on use of Physostigmine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Physostigmine in women who are nursing.

Pediatric Use

• Recommended dosage is 0.02 mg/kg; intramuscularly or by slow intravenous injection, no more than 0.5 mg per minute. If the toxic effects persist, and there is no sign of cholinergic effects, the dosage may be repeated at 5 to 10 minute intervals until a therapeutic effect is obtained or a maximum of 2 mg dosage is attained.

Geriatic Use

There is no FDA guidance on the use of Physostigmine in geriatric settings.

Gender

There is no FDA guidance on the use of Physostigmine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Physostigmine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Physostigmine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Physostigmine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Physostigmine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Physostigmine in patients who are immunocompromised.

Administration and Monitoring

Administration

• IV administration should be at allow controlled rate of no more than 1 mg per minute. Dosage may be repeated at intervals of 10 to 30 minutes if desired patient response is not obtained.

Monitoring

There is limited information regarding Physostigmine Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Physostigmine and IV administrations.

Overdosage

Can cause a cholinergic crisis. Appropriate antidote is atropine sulfate.

Pharmacology

Physostigmine
Systematic (IUPAC) name
(3aR,8aS)-1,3a,8-Trimethyl-1H,2H,3H,3aH,8H,8aH-pyrrolo[2,3-b]indol-5-yl N-methylcarbamate
Identifiers
CAS number	57-47-6
ATC code	S01EB05 V03AB19 (WHO)
PubChem	5983
DrugBank	DB00981
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	275.346 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	?
Metabolism	Major metabolite: Eseroline
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	[[Prescription drug|Template:Unicode-only]](US)
Routes	intravenous, intramuscular, ophthalmic

Mechanism of Action

Physostigmine Salicylate Injection is a reversible anticholinesterase which effectively increases the concentration of acetylcholine at the sites of cholinergic transmission. The action of acetylcholine is normally very transient because of its hydrolysis by the enzyme, acetylcholinesterase. Physostigmine Salicylate Injection inhibits the destructive action of acetylcholinesterase and thereby prolongs and exaggerates the effect of the acetylcholine.

Structure

There is limited information regarding Physostigmine Structure in the drug label.

Pharmacodynamics

There is limited information regarding Physostigmine Pharmacodynamics in the drug label.

Pharmacokinetics

• Physostigmine Salicylate Injection contains a tertiary amine and easily penetrates the blood brain barrier, while an anticholinesterase, such as neostigmine, which has a quaternary ammonium ion is not capable of crossing the barrier. Physostigmine Salicylate Injection can reverse both central and peripheral anticholinergia. The anticholinergic syndrome has both central and peripheral signs and symptoms. Central toxic effects include anxiety, delirium, disorientation, hallucinations, hyperactivity and seizures. Severe poisoning may produce coma, medullary paralysis and death. Peripheral toxicity is characterized by tachycardia, hyperpyrexia, mydriasis, vasodilation, urinary retention, diminution of gastrointestinal motility, decrease of secretion in salivary and sweat glands, and loss of secretions in the pharynx, bronchi, and nasal passages.
• Dramatic reversal of the effects of anticholinergic symptoms can be expected in minutes after the intravenous administration of Physostigmine Salicylate Injection, if the diagnosis is correct and the patient has not suffered anoxia or other insult. The duration of action of Physostigmine Salicylate Injection is relatively short, approximately 45 to 60 minutes.

Nonclinical Toxicology

There is limited information regarding Physostigmine Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Physostigmine Clinical Studies in the drug label.

How Supplied

• 2 mL Ampules packed 10 per box, 1 mg per mL.

Storage

• Store at 20° to 25°C (68° to 77°F)

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Physostigmine Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Physostigmine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Antilirium
• Isopto Eserine

Look-Alike Drug Names

There is limited information regarding Physostigmine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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