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Home: Drug Development: Drugs in Clinical Trials
Drugs In Clinical Trials

Important Notice: The Forum does not endorse any medical product or therapy. ALL medications and supplements should be taken ONLY under the supervision of a physician, due to the possibility of side-effects, drug interactions, etc.

Name: Physostigmine Salicylate
Other Names: Synapton
Development Status: investigational in U.S.
FDA Phase: Discontinued
Primary Medical Role: Treatment for mild-to-moderate dementia.
Role in Alzheimer's Disease: Improvment of short-term memory.
Pharmacological Role: Sustained-release version of physostigmine, which is an acetylcholinesterase inhibitor.
Side Effects: Nausea (45% vs. 5 % placebo); Vomiting (40% vs. 3%); Diarrhea (12% vs. 1%); Anorexia (11% vs. 2%); Dizziness (11% vs. 4%); Headache (9% vs. 5%); stomach pain (8.7% vs. 0.5%); sweating (8.7% vs. 0.5%); and flatulence (5% vs. 0%).
Evidence pro its efficacy: In a big, double-blinded, placebo-controlled, multicenter study, this sustained-release form of physostigmine seemed to help improve cognitive test scores slightly.
Evidence con its efficacy: It has high side effects (nausea, vomiting, diarrhea, anorexia, dyspepsia, and abdominal pain for patients), and its effectiveness is limited due to high drop out rate.
Dosage: Up to 15 mg, twice a day.
Companies: Forest Laboratories, Inc.

References

Beach TG, Kuo YM, Schwab C, Walker DG, Roher AE. Reduction of cortical amyloid beta levels in guinea pig brain after systemic administration of physostigmine. Neurosci Lett. 2001 Sep 7;310(1):21-4. Abstract

Petrie EC, Peskind ER, Dobie DJ, Veith RC, Raskind MA. Plasma catecholamine and cardiovascular responses to physostigmine in Alzheimer's disease and aging. Psychoneuroendocrinology. 2001 Feb;26(2):147-64. Abstract

Coelho F, Birks J. Physostigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2001;(2):CD001499. Abstract

Thal LJ, Ferguson JM, Mintzer J, Raskin A, Targum SD. A 24- week randomized trial of controlled-release physostigmine in patients with Alzheimer's disease. Neurology. 1999 Apr 12;52(6):1146-52. Abstract

Blin J, Ivanoiu A, De Volder A, Michel C, Bol A, Verellen C, Seron X, Duprez T, Laterre EC. Physostigmine results in an increased decrement in brain glucose consumption in Alzheimer's disease. Psychopharmacology (Berl). 1998 Apr;136(3):256-63. Abstract

Perola E, Cellai L, Lamba D, Filocamo L, Brufani M. Long chain analogs of physostigmine as potential drugs for Alzheimer's disease: new insights into the mechanism of action in the inhibition of acetylcholinesterase. Biochim Biophys Acta. 1997 Nov 14;1343(1):41-50. Abstract

Thal LJ, Schwartz G, Sano M, Weiner M, Knopman D, Harrell L, Bodenheimer S, Rossor M, Philpot M, Schor J, Goldberg A. A multicenter double-blind study of controlled-release physostigmine for the treatment of symptoms secondary to Alzheimer's disease. Physostigmine Study Group. Neurology. 1996 Dec;47(6):1389-95. Abstract


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