Tacrine: A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Alzheimer’s Disease

Drugs & Aging

Volumn 4, Issue 6, 1994, Pages 510-540

  Wagstaff, Antona J ^a   McTavish, Donna ^a  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLINERGIC RECEPTOR; NEUROTRANSMITTER; TACRINE;

ALZHEIMER DISEASE; ANIMAL; BIOAVAILABILITY; BRAIN; CLINICAL TRIAL; COGNITION; DRUG EFFECT; ENZYMOLOGY; HALF LIFE TIME; HUMAN; INTESTINE ABSORPTION; ION CHANNEL; LIVER; METABOLISM; REVIEW; TISSUE DISTRIBUTION;

ALZHEIMER DISEASE; ANIMAL; BIOLOGICAL AVAILABILITY; BRAIN; CLINICAL TRIALS; COGNITION; HALF-LIFE; HUMAN; INTESTINAL ABSORPTION; ION CHANNELS; LIVER; NEUROTRANSMITTERS; RECEPTORS, CHOLINERGIC; TACRINE; TISSUE DISTRIBUTION;

EID: 0028448282     PISSN: 1170229X     EISSN: 11791969     Source Type: Journal    
DOI: 10.2165/00002512-199404060-00006     Document Type: Article

References (203)

1. Chronic treatments with cholinoceptor drugs influence spatial learning in rats
2. Putative mechanisms of action of tacrine in Alzheimer’s disease
3. Tetrahydroaminoacridine inhibits human and rat brain monoamine oxidase
4. Multiple effects of tetrahydroaminoacridine on the cholinergic system: biochemical and behavioural aspects
5. Pharmacokinetics of tetrahydroaminoacridine: relations to clinical and biochemical effects in Alzheimer patients
6. Tetrahydroaminoacridine in Alzheimer’s dementia: clinical and biochemical results of a double-blind crossover trial
7. The relationship of cerebrospinal fluid monoamine metabolites with clinical response to tetrahydroaminoacridine in patients with Alzheimer’s disease
8. Psychometric discrimination of tetrahydroaminoacridine responders in Alzheimer patients
9. Discrimination of tetrahydroaminoacridine responders by a single dose pharmaco-EEG in patients with Alzheimer’s disease
10. Discrimination of Alzheimer patients responding to cholinesterase inhibitor therapy
11. Somatostatin and cognitive functions in Alzheimer’s disease — the relationship of cerebrospinal fluid somatostatin increase with clinical response to tetrahydroaminoacridine
12. Long-term treatment with tacrine (THA) in Alzheimer’s disease — evaluation of neuropsychological data
13. Hepatotoxicity of tetrahydroacridine. Correspondence
14. Heterogeneity of adverse hepatic reactions to tetrahydroaminoacridine
15. Studies on new, centrally active and reversible acetylcholinesterase inhibitors
16. Functional and pharmacokinetic studies of tetrahydroaminoacridine in patients with amyotrophic lateral sclerosis
17. Systemic administration of lithium chloride and tacrine increases nitric oxide synthase activity in the hippocampus of rats
18. Measurements of tacrine and monoamines in brain by in vivo microdialysis argue against release of monoamines by tacrine at therapeutic doses
19. Tetrahydroaminoacridine, 3,4 diaminopyridine and physostigmine: direct comparison of effects on memory in aged primates
20. Effects of velnacrine, tacrine and physostigmine on tetanic twitch responses at the rat neuromuscular junction
21. The cholinergic system and the excitatory amino acids in Alzheimer’s disease
22. Neurotransmitter-related enzymes and indices of hypoxia in senile dementia and other abiotrophies
23. Tacrine in relation to amino acid transmitters in Alzheimer’s disease
24. Effects of tacrine, velnacrine (HP029), suronacrine (HP128), and 3,4-diaminopyridine on skeletal neuromuscular transmission in vitro
25. Effect of amiridine and tacrine, drugs effective in Alzheimer’s disease, on monoamine oxidase A and B activity
26. Interaction of tacrine and velnacrine with neocortical synaptosomal membranes: relevance to Alzheimer’s disease
27. Tetrahydroaminoacridine but not 4-aminopyridine inhibits high-affinity choline uptake in striatal and hippocampal synaptosomes
28. 42K efflux from rat brain synaptosome by minaprine and tetrahydroaminoacridine
29. Tetrahydroaminoacridine in Alzheimer’s disease: a review of its safety and its effectiveness
30. Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial
31. Effects of four non-cholinergic cognitive enhancers in comparison with tacrine and galanthamine on scopolamine-induced amnesia in rats
32. SPECT brain imaging in Alzheimer’s disease during treatment with oral tetrahydroaminoacridine and lecithin
33. Alzheimer’s disease: a disorder of cortical cholinergic innervation
34. Inhibition of rat brain histamine-N-methyl-transferase by 9-amino-1,2,3,4-tetrahydroacridine (THA)
35. Physostigmine inhibition of 3′,5′-cyclic AMP phosphodiesterase from cat sciatic nerve
36. Steady-state pharmacokinetic s of tacrine in patients with Alzheimer’s disease
37. Tetrahydroaminoacridine selectively attenuates NMDA receptor-mediated neurotoxicity
38. Selective loss of central cholinergic neurons in Alzheimer’s disease
39. A double-blind, placebo-controlled multicenter study of tacrine for Alzheimer’s disease
40. Reversibility of the inhibition of acetylcholinesterase by tacrine
41. Tacrine slows the rate of ageing of sarin-inhibited acetylcholinesterase
42. Memory facilitation by histamine
43. Inhibitory effect of 1,2,3,4-tetrahydro-9-aminoacridine on the depolarization-induced release of GABA from cerebral cortex
44. Comparison of DuP 996, with physostigmine, THA and 3,4-DAP on hypoxia-induced amnesia in rats
45. f) in the rabbit sinoatrial node and in canine Purkinje fibres by 9-amino-1,2,3,4-tetrahydroacridine
46. Tetrahydroaminoacridine facilitates passive avoidance learning in rats with nucleus basalis magnocellularis lesions
47. Investigation of the mechanism of the effect of tacrine (tetrahydroaminoacridine) on the metabolism of acetylcholine and choline in brain cortical prisms
48. Positive and negative effects of tacrine (tetrahydroaminoacridine) and methoxytacrine on the metabolism of acetylcholine in brain cortical prisms incubated under “resting” conditions
49. + current
50. Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer’s disease
51. Effects of tetrahydro-9-aminoacridine on cortical and hippocampal neurons in the rat: an in vivo and in vitro study
52. Tacrine in Alzheimer’s disease
53. Tacrine in Alzheimer’s disease. Correspondence
54. Parallel group analysis of the effects of tacrine versus placebo in Alzheimer’s disease
55. Tacrine in Alzheimer’s disease. Time course of changes in cognitive function and practice effects
56. Investigation of the central and peripheral cholinomimetic effects and plasma cholinesterase inhibition of tacrine. Abstract no. PIII-18
57. Mechanisms of the tetrahydroaminoacridine effect on action potential and ion currents in myelinated axons
58. Effects of THA on ionic currents in myelinated axons of Xenopus laevis
59. Prevalence of Alzheimer’s disease in a community population of older persons. Higher than previously reported
60. A controlled trial of tacrine in Alzheimer’s disease
61. Tacrine in Alzheimer’s Disease. Correspondence
62. Treatment of Alzheimer’s disease with short- and long-term oral THA and lecithin: a double-blind study
63. Effect of acute arecoline, tacrine, and arecoline + tacrine post-training administration on retention in late middle-aged mice
64. Effect of acute arecoline, tacrine and arecoline + tacrine post-training administration on retention in old mice
65. Multiple in vitro interactions with and differential in vivo regulation of muscarinic receptor subtypes by tetrahydroaminoacridine
66. Serum concentrations of tacrine hydrochloride predict its adverse effects in Alzheimer’s disease
67. Clinical experience with and side-effects of tacrine hydrochloride in Alzheimer’s disease: a pilot study
68. Pharmacokinetics of tacrine hydrochloride in Alzheimer’s disease
69. Tacrine, a drug with therapeutic potential for dementia: post-mortem biochemical evidence
70. Open trial of tacrine therapy in 70 HIV-infected patients
71. Tacrine: a pharmacological review
72. + channel by tacrine: interactions with muscarinic and adenosine receptors
73. Therapeutic trials using tacrine and other cholinesterase inhibitors
74. + channel blockers
75. Tetrahydroaminoacridine-lecithin combination treatment in patients with intermediate-stage Alzheimer’s disease. Results of a Canadian double-blind, crossover, multicenter study
76. Tacrine in Alzheimer’s disease. Correspondence
77. Comparison of 4-aminopyridine and tetrahydroaminoacridine on basal forebrain neurons
78. The effect of acute nicotine infusion on the local cerebral glucose utilization of the awake rat
79. Physostigmine, tacrine and metrifonate: the effect of multiple doses on acetylcholine metabolism in rat brain
80. 9-Amino-1,2,3,4-tetrahydroacridine (THA) blocks agonist-induced potassium conductance in rat hippocampal neurones
81. Acute hepatitis after tetrahydroaminoacridine administration for Alzheimer’s disease
82. Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4-tetrahydroacridine, tacrine
83. Pharmacokinetics and effects of 9-amino-1,2,3,4-tetrahydroacridine in the immediate postoperative period in neurosurgical patients
84. Effects of tacrine, aminopyridines, and physostigmine on acetylcholinesterase, acetylcholine release, and potassium currents
85. THA and Alzheimer’s disease
86. Diagnostic and pharmacological approaches in Alzheimer’s disease
87. Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer’s type. Correspondence
88. Tetrahydroaminoacridine block of N-methyl-D-aspartate-activated cation channels in cultured hippocampal neurons
89. Low dose tetrahydroaminoacridine (THA) improves cognitive function but does not affect brain acetylcholine in rats
90. The prevalence of dementia in Europe: a collaborative study of 1980–1990 findings
91. The cholinergic pharmacology of tetrahydroaminoacridine in vivo and in vitro
92. Utility of an elevated plus-maze for the evaluation of memory in mice: effects of nootropics, scopolamine and electroconvulsive shock
93. The effects of tacrine and zacopride on the performance of adult rats in the working memory task
94. Tacrine in Alzheimer’s disease. Correspondence
95. Characterisation of dopamine and serotonin uptake inhibitory effects of tetrahydroaminoacridine in rat brain
96. Histamine-induced arousal in the conscious and pentobarbital-pretreated rat
97. ++ efflux from rat pancreatic islets
98. Modest facilitation of memory in dementia with combined lecithin and anticholinesterase treatment
99. Muscarinic subtype selectivity of tetrahydroaminoacridine: possible relationship to its capricious efficacy
100. Muscarinic receptor function and acetylcholinesterase activity after chronic administration of tacrine to mice at therapeutic drug concentrations
101. A 30-week randomized controlled trial of high-dose tacrine in patients with Alzheimer’s disease
102. Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer’s type. Correspondence
103. Inhibitory effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on the potassium current of rabbit sinoatrial node
104. Changes of high-affinity choline uptake in the hippocampus of old rats after long-term administration of two nootropic drugs (tacrine and Ginkgo biloba extract)
105. Clinical pharmacology of tetrahydroaminoacridine: a possible therapeutic agent for Alzheimer’s disease
106. Interaction of tacrine with muscarinic receptors
107. Tetrahydroaminoacridine improves the spatial acquisition deficit produced by nucleus basalis lesions in rats
108. Tacrine in Alzheimer’s disease. Correspondence
109. Tacrine and lecithin in Alzheimer’s disease. Correspondence
110. Evidence for histaminergic arousal mechanisms in the hypothalamus of cat
111. The effect of tacrine on acetylcholine overflow in the heart
112. A double-blind, placebo controlled trial of high-dose lecithin in Alzheimer’s disease
113. Effect of nicotine and tacrine on acetylcholine release from rat cerebral cortical slices
114. Effects of nicotine on local cerebral glucose utilization in the rat
115. An investigation into the formation of stable, protein-reactive and cytotoxic metabolites from tacrine in vitro. Studies with human and rat liver microsomes
116. What effect do ageing and disease have on the in vitro plasma protein binding of tacrine hydrochloride (THA)?
117. Efficacy of tacrine and lecithin in mild to moderate Alzheimer’s disease: double blind trial
118. Pharmacological significance of acetylcholinesterase inhibition by tetrahydroaminoacridine
119. Changes in the regional brain histamine and histidine levels in postmortem brains of Alzheimer patients
120. Quantitative whole-body autoradiographic determination of tacrine tissue distribution in rats following intravenous or oral dose
121. Shifting patterns of cortical cholinesterases in Alzheimer’s disease: implications for treatment, diagnosis, and pathogenesis
122. Anatomy of cholinesterase inhibition in Alzheimer’s disease: effect of physostigmine and tetrahydroaminoacridine on plaques and tangles
123. Cholinesterases within neurofibrillary tangles related to age and Alzheimer’s disease
124. Oral tetrahydroaminoacridine treatment of Alzheimer’s disease evaluated clinically and by regional cerebral blood flow and EEG
125. Learning deficits in aged rats pretreated chronically with barbital and tested late in abstinence: alleviation by tetrahydroaminoacridine
126. Effect of tetrahydroaminoacridine on cognition, function and behaviour in Alzheimer’s disease
127. Potential therapeutic strategies for senile cognitive disorders
128. Reversal by tetrahydroaminoacridine of scopolamine-induced memory and performance deficits in rats
129. Evaluation of HP 029 (velnacrine maleate) in Alzheimer’s disease
130. The effect of tacrine (THA) on cycloheximide- and basal forebrain lesion-induced memory deficit in rats
131. Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes
132. Do tetrahydroaminoacridine (THA) and physostigmine restore acetylcholine release in Alzheimer brains via nicotinic receptors?
133. Tetrahydroaminoacridine induces opposite changes in muscarinic and nicotinic receptors in rat brain
134. 9-Amino-1,2,3,4-tetrahydroacridine is a potent inhibitor of histamine N-methyltransferase
135. Clinical studies in Alzheimer patients with positron emission tomography
136. Effect of long-term treatment with tacrine (THA) in Alzheimer’s disease as visualized by PET
137. Neuroreceptor changes in Alzheimer disease
138. Tacrine restores cholinergic nicotinic receptors and glucose metabolism in Alzheimer patients as visualized by positron emission tomography
139. 3H]acetylcholine binding sites in the frontal cortex of Alzheimer brains
140. Metrifonate and tacrine: a comparative study on their effect on acetylcholine dynamics in mouse brain
141. Effects of tetrahydroaminoacridine on liver function in patients with Alzheimer’s disease
142. 9-Amino-1,2,3,4-tetrahydroacridine (THA) is a potent blocker of cardiac potassium channels
143. Influence of tetrahydro-9-aminoacridine on excitatory amino acid release
144. Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA), a potential drug for treatment of Alzheimer’s disease, on the physical state of human erythrocyte membranes
145. Structure-activity investigation of the alteration of the physical state of the skeletal network of proteins in human erythrocyte membranes induced by 9-amino-1,2,3,4-tetrahydroacridine
146. Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitro
147. Delayed matching-to-sample performance during a double-blind trial of tacrine (THA) and lecithin in patients with Alzheimer’s disease
148. Tetrahydroaminoacridine increases acetylcholine synthesis and glucose oxidation by mouse brain slices in vitro
149. THA does not affect sleep or EEG spectral power in Alzheimer’s disease
150. Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer’s type. Correspondence
151. Comparison of brain to plasma metabolic distributions of tacrine and 1-hydroxytacrine in rat. Abstract no. 274.11
152. Tetrahydroaminoacridine and physostigmine have opposing effects on probability of transmitter release at the frog neuromuscular junction
153. THA increases action potential duration of central histamine neurons in vitro
154. Tetrahydroaminoacridine inhibits high voltage spindle activity in aged rats after acute and chronic treatment
155. Tetrahydroaminoacridine alleviates medial septal lesion-induced and age-related spatial reference but not working memory deficits
156. The effects of THA on scopolamine and nucleus basalis lesioninduced EEG slowing
157. Combination of atipamezole and tetrahydroaminoacridine/pilocarpine treatment suppresses high voltage spindle activity in aged rats
158. Tetrahydroaminoacridine improves passive avoidance retention defects induced by aging and medial septal lesion but not by fimbria-fornix lesion
159. Effects of atipamezole and tetrahydroaminoacridine on nucleus basalis lesion-induced EEG changes
160. The mechanism of tetrahydroaminoacridine-evoked release of endogenous 5-hydroxytryptamine and dopamine from rat brain tissue prisms
161. Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neurons
162. Direct comparison of cognitive facilitation by physostigmine and tetrahydroaminoacridine in two primate models
163. Further analysis of the cognitive effects of tetrahydroaminoacridine (THA) in Alzheimer’s disease: assessment of attentional and mnemonic function using CANTAB
164. Tetrahydroaminoacridine blocks potassium channels and inhibits sodium inactivation in Myxicola
165. Do blood pressure and age predict response to tacrine (THA) in Alzheimer’s disease? A preliminary report
166. Pharmacokinetics of tacrine in healthy subjects. Abstract no. PP 1477
167. Relative bioavailability of tacrine capsules in healthy subjects. Abstract no. PP 1292
168. Interactions between scopolamine and muscarinic cholinergic agonists or cholinesterase inhibitors on spatial alternation performance in rats
169. Cholinesterase inhibitor therapy for Alzheimer dementia: what do animal models tell us?
170. Glucose metabolism and acetylcholine synthesis in relation to neuronal activity in Alzheimer’s disease
171. Comparative effects of alpha-2 receptor agents and THA on the performance of adult and aged rats in the delayed non-matching to position task
172. Tacrine effects on rat brain acetylcholinesterase activity in vitro. Abstract no. 121
173. Tacrine for treating Alzheimer’s disease
174. Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer’s type. Correspondence
175. Oral tetrahydroaminoacridine in long-term treatment of senile dementia, Alzheimer type
176. Three-dimensional structure of acetylcholinesterase and of its complexes with anticholinesterase drugs
177. 2 cholinoceptors in guinea pig brain
178. Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer’s type. Correspondence
179. 11C]methyl-tetrahydroaminoacridine (methyl-tacrine) in baboon brain
180. Distribution of tacrine across the blood-brain barrier in awake, freely moving rats using in vivo microdialysis sampling
181. Tetrahydroaminoacridine (tacrine) stimulates neurosecretion at mammalian motor endplates
182. In vitro effects of various cholinesterase inhibitors on acetyl- and butyrylcholinesterase of healthy volunteers
183. Comparison of the Chromatographic characteristics of metabolites of tacrine hydrochloride in human serum and urine with those of in vitro metabolic products from hepatic microsomes
184. Negative effects of tacrine (tetrahydroaminoacridine) and methoxytacrine on the metabolism of acetylcholine in brain slices incubated under conditions stimulating neurotransmitter release
185. Effects of cholinergic drugs on learning impairment in ventral globus pallidus-lesioned rats
186. Prevention by choline of the depletion of membrane phosphatidylcholine by a cholinesterase inhibitor. Correspondence
187. Modulation of EEG rhythmicity and spike activity in the rat hippocampus by systemically administered tetrahydroaminoacridine, scopolamine and atipamezole
188. Differential effects of physostigmine and 1,2,3,4-tetrahydro-9-aminoacridine on the β-adrenoceptor transductor system
189. Alternatives in the treatment of memory loss in patients with Alzheimer’s disease
190. Hepatotoxic effects of tacrine administration in patients with Alzheimer’s disease
191. Tetrahydroaminoacridine and lecithin in the treatment of Alzheimer’s disease. Effect on cognition, functioning in daily life, behavioural disturbances and burden experienced by the carers
192. Tacrine in Alzheimer’s disease. Correspondence
193. Tacrine and lecithin in Alzheimer’s disease. Correspondence
194. Long-term use of tacrine. Correspondence
195. An evaluation of the efficacy and safety of tetrahydroaminoacridine (THA) without lecithin in the treatment of Alzheimer’s disease
196. Tacrine — recommendation for approval
197. A psychopharmacological perspective of cognitive functions. II Specific pharmacologic agents
198. Protease inhibitors and indoleamines selectively inhibit cholinesterases in the histopathologic structures of Alzheimer disease
199. 3H]-N-(1-[2-thienyl]cyclohexyl)-3,4-piperidine. Abstract no. 431.5