Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A 72-year-old man was exposed to the sarin gas attack in a Tokyo subway on March 20 th, 1995. After exposure, he noticed eye discomfort, chest tightness, headache and weakness of the lower limbs and oropharyngeal muscles. Despite these symptoms, he visited a hot spring on the same day with his family. On March 25 th, his muscle weakness progressed, and a low grade fever appeared. His muscle weakness disappeared 8 days after exposure to sarin, but respiratory failure rapidly developed, necessitating artificial ventilation within four day after hospitalization on March 28th. Chemotherapy with erythromycin, imipenem/cilastatin, and steroid pulse therapy was begu. PCR and culture of sputum collected by bronchofiberscopy were positive for Legionella pneumophila, serogroup I. His respiratory state improved, but subsequent infection with Pseudomonous aeruginosa. Enterobacter cloacae, and Candida tropicalis/glabrata caused his death 71 days after admission. Oropharyngeal muscle weakness caused by sarin-mediated cholinesterase inhibition was strongly suspected as the cause of hot spring water aspiration. Transbronchial lung biopsy revealed organizing pneumonia with fibrosis. Bronchoscopic findings included redness, edema and fragility of all visible areas of the airway, which was thought to be due to bronchitis caused by Legionellosis.
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PMID:[Legionella pneumonia caused by aspiration of hot spring water after sarin exposure]. 965 77

Non-selective acetylcholinesterase (AChE) inhibitors are known hypotensive agents. The purpose of the present investigation was carried out to ascertain whether rivastigmine, a selective carbamate-type inhibitor of AChE, which inhibits selectively an isoform of this enzyme found almost exclusively in the central nervous system, is able to depress the intraocular pressure (IOP) in normotensive rabbits. IOP was monitored with a TonoPen XL in conscious adult rabbits before and hourly up to 8 hr after administration of the drug. Baseline measurements without treatment and after one single topical application of rivastigmine [1% (n=8); 2% (n=4); and 5% (n=6)] to the right eye and of the vehicle alone to the left one were performed. Rivastigmine reduced the IOP of treated eyes significantly (p<0.05) in a dose-independent manner. Maximal effects of 23.2% (5% rivastigmine), 19.6% (2% rivastigmine) and 15.2% (1% rivastigmine) were achieved 1, 3 and 5 hr after application of the drug. A non-significant reduction of IOP in the contralateral eye was also observed. Rabbits evidenced no signs of discomfort after administration of rivastigmine. No conjunctival discharge or other signs of drug related local toxicity were found. Rivastigmine, a selective antagonist of AChE, lowers IOP significantly and may thus be of potential use in glaucoma therapy.
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PMID:Topical rivastigmine, a selective acetylcholinesterase inhibitor, lowers intraocular pressure in rabbits. 1067 28

The human sweating response is subject to the influence of diverse classes of drugs. Some act centrally at the hypothalamus or at spinal thermoregulatory centres, while others act at sympathetic ganglia or at the eccrine-neuroeffector junction. Pharmacological disturbances of sweating have broad clinical implications. Drugs that induce hyperhidrosis, or sweating in excess of that needed to maintain thermoregulation, can cause patient discomfort and embarrassment, and include cholinesterase inhibitors, selective serotonin reuptake inhibitors, opioids and tricyclic antidepressants. Drugs that induce hypohidrosis, or deficient sweating, can increase the risk of heat exhaustion or heat stroke and include antimuscarinic anticholinergic agents, carbonic anhydrase inhibitors and tricyclic antidepressants. As acetylcholine is the principal neuroeccrine mediator, anhidrosis is one of the clinical hallmarks by which acute anticholinergic toxicity may be recognized. The symptom of dry mouth often accompanies the less apparent symptom of hypohidrosis because the muscarinic M(3) acetylcholine receptor type predominates at both sweat and salivary glands. Management options include dose reduction, drug substitution or discontinuation. When compelling medical indications require continuation of a drug causing hyperhidrosis, the addition of a pharmacological agent to suppress sweating can help to reduce symptoms. When hypohidrotic drugs must be continued, deficient sweating can be managed by avoiding situations of heat stress and cooling the skin with externally applied water. The availability of clinical tests for the assessment of sudomotor dysfunction in neurological disease has enhanced recognition of the complex effects of drugs on sweating. Advances in the understanding of drug-induced anhidrosis have also enlarged the therapeutic repertoire of effective treatments for hyperhidrosis.
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PMID:Drug-induced hyperhidrosis and hypohidrosis: incidence, prevention and management. 1821 88

Cholinesterase inhibitors have beneficial effects on the cognitive, functional, and behavioural symptoms of Alzheimers disease (AD). Up to date, they represent almost the only drugs approved by the U.S. Food and Drug Administration agency for AD treatment. The group involves donepezil, rivastigmine and galantamine. Apart from the above mentioned cholinesterase inhibitors, memantine is used for AD treatment as well acting as Nmethyl-D-aspartate (NMDA) non-competitive antagonist. Tacrine (9-amino-1,2,3,4-tetrahydroacridine) was the first cholinesterase inhibitor approved for symptomatic AD treatment. However, its several side effects (hepatotoxicity and gastrointestinal discomfort) limited tacrine further use. Recently, novel tacrine analogues are extensively investigated in endeavour to find less toxic compounds with the "multi-target directed ligand" profile affecting more AD pathological mechanisms. The following study summarizes the knowledge of up to date published tacrine analogues, their structural aspects and biological properties. According to structural aspects, tacrine derivatives are divided into three groups, where they are discussed.
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PMID:[Tacrine and its derivatives in the therapy of Alzheimers disease]. 2325 54