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Pediatric Emergency Care Jun 1998
Review
Topics: Adolescent; Antidepressive Agents, Tricyclic; Antidotes; Child, Preschool; Cholinergic Antagonists; Contraindications; Fatal Outcome; Female; Heart Arrest; Humans; Physostigmine; Poisoning
PubMed: 9655671
DOI: 10.1097/00006565-199806000-00015 -
The Journal of Emergency Medicine 1985
Topics: Humans; Physostigmine
PubMed: 3837049
DOI: 10.1016/0736-4679(85)90008-3 -
Archives of General Psychiatry Jan 1978Seven men and one woman with primary affective disorder, mania, were given a slow intravenous infusion of physostigmine salicylate. In six patients, mood and thought... (Clinical Trial)
Clinical Trial
Seven men and one woman with primary affective disorder, mania, were given a slow intravenous infusion of physostigmine salicylate. In six patients, mood and thought content changed from mania toward depression as evaluated by either a visual analog mood scale or the Pettersen scale. Two other patients, who were the only predominantly irritable manics in the study, demonstrated little change in their hostility, although one became somewhat depressed. These findings are consistent with earlier reports of suppression of manic symptoms after physostigmine infusion in some but not all patients with mania. The pharmacologic mechanism of physostigmine reversal of manic symptoms may be the direct result of increased cholinergic activity or a result of the effect of increased cholinergic activity on other brain neurotransmitters.
Topics: Affect; Bipolar Disorder; Clinical Trials as Topic; Drug Evaluation; Female; Humans; Infusions, Parenteral; Male; Nausea; Physostigmine; Psychiatric Status Rating Scales; Vomiting
PubMed: 339869
DOI: 10.1001/archpsyc.1978.01770250121012 -
Journal of the Academy of... 2021Second-generation antipsychotic agents are commonly used by clinicians for the treatment of various psychiatric and medical conditions. Despite their presumed safety, an... (Review)
Review
BACKGROUND
Second-generation antipsychotic agents are commonly used by clinicians for the treatment of various psychiatric and medical conditions. Despite their presumed safety, an overdose with olanzapine may lead to the development of anticholinergic toxicity. The anticholinergic toxidrome is characterized by both central and peripheral physical findings. Central anticholinergic syndrome, a term used to describe the symptoms that arise from reduced cholinergic activity in the central nervous system, is characterized primarily by signs and symptoms consistent with hyperactive delirium. Signs of peripheral anticholinergia include mydriasis and blurred vision, tremors, ataxia, fever/hyperthermia, flushed and dry skin, dry oral mucosa, decreased bowel sounds, constipation, and urinary retention, among other symptoms. In extreme cases, central anticholinergic syndrome can be associated with seizures, coma, respiratory failure, and cardiovascular collapse.
OBJECTIVE
To provide scientific evidence regarding the efficacy and safety of physostigmine use in cases of anticholinergic toxicity.
METHODS
We conducted a comprehensive review of the published literature on the symptoms, diagnosis, and treatment of anticholinergic toxicity.
RESULTS
Currently the recommended treatment for olanzapine overdose, as is the case of most severe anticholinergic toxicity cases, involves supportive care, along with cardiac, neurological, and respiratory status monitoring. In addition, we detail the symptoms characteristic of anticholinergic toxicity, using the case of a patient experiencing central anticholinergic syndrome after an overdose with olanzapine.
CONCLUSION
Physostigmine, a tertiary acetylcholinesterase inhibitor, can be used to assist in the both the diagnosis and management of severe anticholinergic toxicity associated with an olanzapine overdose, which might be applicable to the antimuscarinic toxidrome associated with the ingestion of agents with significant anticholinergic activity.
Topics: Acetylcholinesterase; Anticholinergic Syndrome; Cholinergic Antagonists; Humans; Olanzapine; Physostigmine
PubMed: 34102130
DOI: 10.1016/j.jaclp.2020.12.013 -
International Journal of Clinical... Aug 1989Physostigmine (Phy) is one of the oldest drug isolated from Calabar beans and successfully used for the treatment of glaucoma in 1864. Since then, it has been widely... (Review)
Review
Physostigmine (Phy) is one of the oldest drug isolated from Calabar beans and successfully used for the treatment of glaucoma in 1864. Since then, it has been widely employed for various therapeutic purposes. Recently, it has gained prominence because of its clinical trials in the treatment of Alzheimer's disease. Phy is also considered to be a potent prophylactic antidote for organophosphate poisoning. It is a reversible cholinesterase (ChE) inhibitor and has a short duration of action. It crosses the blood-brain barrier readily. Hence, it is a centrally acting carbamate. For the last 50 years, numerous authors have shown that pretreatment with Phy would rapidly improve the incapacitating effects of organophosphate intoxication in various animal species. Phy carbamylates to a portion of ChE enzyme and thus protects the enzyme from binding with organophosphate, which are irreversible ChE inhibitors. Organophosphates are metabolized very quickly in the body or bind to non-specific binding sites. The carbamylated ChE enzyme decarbamylates to free the enzyme for normal functioning. The rates of decarbamylation of butyrylcholinesterase (BuChE) in plasma and ChE in brain and muscle are different and are related to the half-life of Phy in these tissues. In addition to ChE inhibition, Phy has got a direct action on acetylcholine (ACh) receptor ionophore complex by interacting with the ACh-gated cation channels. Physostigmine has a half-life of 16, 23 and 30 min in rat, dog and man, respectively. The bioavailability of Phy is very low (about 2%) and it is extensively metabolized in the liver. Less than 4% of Phy is excreted unchanged in the urine and a portion is also eliminated in the bile. Physostigmine has a narrow margin of safety, and a slight increase in dose causes cholinergic symptoms, which can be counteracted by cholinolytic therapy. This review article deals with various aspects of physostigmine such as historical, therapeutic uses, mechanisms of action, methods for the determination, disposition and pharmacokinetics, toxicity and finally as an antidote against organophosphate intoxication.
Topics: Animals; Humans; Organophosphate Poisoning; Physostigmine
PubMed: 2676871
DOI: No ID Found -
The Journal of Emergency Medicine Aug 2003Ingestion of cyclic antidepressant medications or prolongation of the electrocardiographic QRS interval are commonly considered as contraindications to the use of... (Review)
Review
Ingestion of cyclic antidepressant medications or prolongation of the electrocardiographic QRS interval are commonly considered as contraindications to the use of physostigmine as an antidote for antimuscarinic toxicity. This dictum seems to stem from a few well-publicized cases in which administration of physostigmine was temporally associated with the development of asystole. Before the report of these cases, physostigmine was more frequently used and had been considered a first-line antidote for both the neurologic and cardiac toxic effects of cyclic antidepressant overdose. This apparent inconsistency, and a resurgence of interest in physostigmine as an antidote, begs the question of the appropriateness of this drug's contraindication in all cyclic antidepressant ingestions. Review of the published clinical and experimental evidence provides little support for the clinical utility of using electrocardiographic criteria or the ingestion of cyclic antidepressants as contraindications to the use of physostigmine.
Topics: Animal Experimentation; Antidepressive Agents; Antidotes; Cholinesterase Inhibitors; Contraindications; Drug Interactions; Humans; Physostigmine
PubMed: 12902007
DOI: 10.1016/s0736-4679(03)00169-0 -
Tidsskrift For Den Norske Laegeforening... Apr 1992Physostigmine was originally isolated from the Calabar Bean, which was used for ordeal by poison in West Africa. The main alkaloid was isolated in 1864. It acts through... (Review)
Review
Physostigmine was originally isolated from the Calabar Bean, which was used for ordeal by poison in West Africa. The main alkaloid was isolated in 1864. It acts through inhibition of acetylcholinesterase, and has been of major importance in elucidating the kinetics and configuration of the enzyme. Physostigmine has been important for our understanding of neurohumoral chemical transmission, and in mapping the cholinergic nerves. It was the first antagonist to curare, and has been widely used for various therapeutic purposes. Today it has been largely replaced by more efficient and safe drugs. It is still used as an antidote to poisoning from various psychopharmacological drugs, and to treat postoperative somnolence and respiratory depression. It is considered a potent antidote to organophosphorous poisoning and is used experimentally to treat Alzheimer's disease.
Topics: Antidotes; History, 19th Century; History, 20th Century; Physostigmine; Plants, Toxic
PubMed: 1579914
DOI: No ID Found -
Journal of the American Geriatrics... Jan 1989Sixteen patients with early Alzheimer's disease (AD) completed a 3-month outpatient double-blind parallel trial of oral physostigmine versus placebo. Ten subjects... (Clinical Trial)
Clinical Trial Comparative Study Review
Sixteen patients with early Alzheimer's disease (AD) completed a 3-month outpatient double-blind parallel trial of oral physostigmine versus placebo. Ten subjects received drug; six received placebo. After a dose-titration phase, each patient was placed on his or her best dose of drug or placebo. Subjects were evaluated with both memory and nonmemory tasks. Seven of the ten drug-treated patients, but none of the six placebo-treated patients, demonstrated improvement on a selective reminding task, a test of verbal memory. Family members reported improvement in six of ten drug-treated patients and none of six placebo-treated individuals. There was a trend toward greater improvement with increasing drug dose. There was no improvement on the nonmemory tests administered. The data indicate that oral physostigmine improves memory but not other areas of cognition.
Topics: Activities of Daily Living; Administration, Oral; Aged; Alzheimer Disease; Double-Blind Method; Humans; Memory; Physostigmine; Psychological Tests
PubMed: 2642499
DOI: 10.1111/j.1532-5415.1989.tb01567.x -
Anaesthesiologie Und Reanimation 1989Physostigmine is widely used for treatment of the central anticholinergic syndrome during recovery from anaesthesia. The drug is also very useful in treatment of... (Review)
Review
Physostigmine is widely used for treatment of the central anticholinergic syndrome during recovery from anaesthesia. The drug is also very useful in treatment of intoxicated patients, in differential-diagnostic procedures of coma of unknown origin, and in restoration of vigilance after prolonged sedation for mechanical ventilation. Besides the specific central cholinergic action of physostigmine, several new pharmacological actions have now been established. Analgesic action is dependent on the interaction with the 5-HT (serotoninergic) system and is independent of narcotic or cholinergic agonists. The antianalgetic stress hormone, ACTH, also does not interfere with this action. Physostigmine does not interfere with the anaesthetic state when given during general anaesthesia. It attenuates several withdrawal states, especially alcohol delirium, opiate and nitrous oxide withdrawal syndromes. The drug may offer a protective mechanism against hypoxic damage of the brain and may also be beneficial in amnestic syndromes and sleep disorders. Physostigmine produces central and peripheral cardiovascular stimulation. It has been shown that physostigmine can be useful in prevention and treatment of postanaesthetic behavioural disturbances following anaesthesia with propofol. Number of indications for use of physostigmine has increased considerably.
Topics: Animals; Humans; Physostigmine
PubMed: 2675888
DOI: No ID Found -
JACEP Jun 1976Physostigmine salicylate, a cholinesterase inhibitor, has been shown to reverse the effects of certain drugs with anticholinergic properties. The paper provides a brief...
Physostigmine salicylate, a cholinesterase inhibitor, has been shown to reverse the effects of certain drugs with anticholinergic properties. The paper provides a brief historical account of physostigmine, reviews the cholinergic drugs and their effects and suggests a management protocol based on physiologic criteria. Twenty-six overdose cases, recently treated with physostigmine, are summarized. The controversy regarding the etiology of seizures following physostigmine administration is discussed.
Topics: Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Humans; Physostigmine; Poisoning; Substance-Related Disorders
PubMed: 933411
DOI: 10.1016/s0361-1124(76)80253-5