Detail

Tacrine

Description

Name: Tacrine
Type: small molecule
Groups: withdrawn
Indication: For the palliative treatment of mild to moderate dementia of the Alzheimer's type.
Accession Number: DB00382 ( APRD00690)
Description: A centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. Tacrine has been discontinued for the United States market.
Structure:
Prescription Products: Not Available
Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients

Categories
  • Nootropic Agents
  • Cholinesterase Inhibitors
  • Parasympathomimetics
  • Acetylcholinesterase Inhibitors
  • Acetylcholinesterase Inhibitors (Central)

Pharmacology

Indication: For the palliative treatment of mild to moderate dementia of the Alzheimer's type.
Pharmacodynamics: Not Available
Mechanism of action: The mechanism of tacrine is not fully known, but it is suggested that the drug is an anticholinesterase agent which reversibly binds with and inactivates cholinesterases. This inhibits the hydrolysis of acetylcholine released from functioning cholinergic neurons, thus leading to an accumulation of acetylcholine at cholinergic synapses. The result is a prolonged effect of acetylcholine.
Absorption: Tacrine is rapidly absorbed. Absolute bioavailability of tacrine is approximately 17%.
Volume of distribution:
  • 349 ± 193 L

Protein binding: 55%
Metabolism: Not Available
Route of elimination: Not Available
Half life: 2 to 4 hours
Clearance: Not Available
Toxicity: Overdosage with cholinesterase inhibitors can cause a cholinergic crisis characterized by severe nausea/vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. The estimated median lethal dose of tacrine following a single oral dose in rats is 40 mg/kg, or approximately 12 times the maximum recommended human dose of 160 mg/day.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Shionogi pharma inc

Packagers:
Dosage forms
FormRouteStrength

Prices
Unit descriptionCostUnit
Cognex 10 mg capsule$3.03capsule
Cognex 20 mg capsule$3.03capsule
Cognex 40 mg capsule$3.03capsule

Patents
CountryPatent NumberApprovedExpires (estimated)

Interactions

Drug Interactions
DrugInteraction
AcebutololTacrine may increase the bradycardic activities of Acebutolol.
AclidiniumThe therapeutic efficacy of Aclidinium can be decreased when used in combination with Tacrine.
AmitriptylineThe therapeutic efficacy of Amitriptyline can be decreased when used in combination with Tacrine.
AmoxapineThe therapeutic efficacy of Amoxapine can be decreased when used in combination with Tacrine.
AripiprazoleTacrine may increase the central neurotoxic activities of Aripiprazole.
AsenapineTacrine may increase the central neurotoxic activities of Asenapine.
AtenololTacrine may increase the bradycardic activities of Atenolol.
Atracurium besylateTacrine may decrease the neuromuscular blocking activities of Atracurium besylate.
AtropineThe therapeutic efficacy of Atropine can be decreased when used in combination with Tacrine.
AzelastineThe therapeutic efficacy of Azelastine can be decreased when used in combination with Tacrine.
BendroflumethiazideTacrine may increase the bradycardic activities of Bendroflumethiazide.
BenzatropineThe therapeutic efficacy of Benzatropine can be decreased when used in combination with Tacrine.
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Tacrine.
BetaxololTacrine may increase the bradycardic activities of Betaxolol.
BethanecholThe risk or severity of adverse effects can be increased when Tacrine is combined with Bethanechol.
BisoprololTacrine may increase the bradycardic activities of Bisoprolol.
BrexpiprazoleTacrine may increase the central neurotoxic activities of Brexpiprazole.
BrompheniramineThe therapeutic efficacy of Brompheniramine can be decreased when used in combination with Tacrine.
CarbacholThe risk or severity of adverse effects can be increased when Tacrine is combined with Carbachol.
CarbinoxamineThe therapeutic efficacy of Carbinoxamine can be decreased when used in combination with Tacrine.
CarteololTacrine may increase the bradycardic activities of Carteolol.
CarvedilolTacrine may increase the bradycardic activities of Carvedilol.
CetirizineThe therapeutic efficacy of Cetirizine can be decreased when used in combination with Tacrine.
CevimelineThe risk or severity of adverse effects can be increased when Tacrine is combined with Cevimeline.
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Tacrine.
ChlorphenamineThe therapeutic efficacy of Chlorphenamine can be decreased when used in combination with Tacrine.
ChlorpromazineThe therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Tacrine.
Cisatracurium besylateTacrine may decrease the neuromuscular blocking activities of Cisatracurium besylate.
ClemastineThe therapeutic efficacy of Clemastine can be decreased when used in combination with Tacrine.
ClidiniumThe therapeutic efficacy of Clidinium can be decreased when used in combination with Tacrine.
ClofedanolThe therapeutic efficacy of Clofedanol can be decreased when used in combination with Tacrine.
ClomipramineThe therapeutic efficacy of Clomipramine can be decreased when used in combination with Tacrine.
ClozapineThe therapeutic efficacy of Clozapine can be decreased when used in combination with Tacrine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Tacrine.
CorticotropinThe risk or severity of adverse effects can be increased when Corticotropin is combined with Tacrine.
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Tacrine.
CyclizineThe therapeutic efficacy of Cyclizine can be decreased when used in combination with Tacrine.
CyclobenzaprineThe therapeutic efficacy of Cyclobenzaprine can be decreased when used in combination with Tacrine.
CyclopentolateThe therapeutic efficacy of Cyclopentolate can be decreased when used in combination with Tacrine.
CyproheptadineThe therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Tacrine.
DarifenacinThe therapeutic efficacy of Darifenacin can be decreased when used in combination with Tacrine.
DesipramineThe therapeutic efficacy of Desipramine can be decreased when used in combination with Tacrine.
DesloratadineThe therapeutic efficacy of Desloratadine can be decreased when used in combination with Tacrine.
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Tacrine.
DexbrompheniramineThe therapeutic efficacy of Dexbrompheniramine can be decreased when used in combination with Tacrine.
Dexchlorpheniramine maleateThe therapeutic efficacy of Dexchlorpheniramine maleate can be decreased when used in combination with Tacrine.
DicyclomineThe therapeutic efficacy of Dicyclomine can be decreased when used in combination with Tacrine.
DifenoxinThe therapeutic efficacy of Difenoxin can be decreased when used in combination with Tacrine.
DimenhydrinateThe therapeutic efficacy of Dimenhydrinate can be decreased when used in combination with Tacrine.
DiphenhydramineThe therapeutic efficacy of Diphenhydramine can be decreased when used in combination with Tacrine.
DiphenoxylateThe therapeutic efficacy of Diphenoxylate can be decreased when used in combination with Tacrine.
DipyridamoleThe therapeutic efficacy of Tacrine can be decreased when used in combination with Dipyridamole.
DisopyramideThe therapeutic efficacy of Disopyramide can be decreased when used in combination with Tacrine.
DoxepinThe therapeutic efficacy of Doxepin can be decreased when used in combination with Tacrine.
DoxylamineThe therapeutic efficacy of Doxylamine can be decreased when used in combination with Tacrine.
DroperidolThe therapeutic efficacy of Droperidol can be decreased when used in combination with Tacrine.
EsmololTacrine may increase the bradycardic activities of Esmolol.
FenoterolThe therapeutic efficacy of Fenoterol can be decreased when used in combination with Tacrine.
FesoterodineThe therapeutic efficacy of Fesoterodine can be decreased when used in combination with Tacrine.
FexofenadineThe therapeutic efficacy of Fexofenadine can be decreased when used in combination with Tacrine.
FlavoxateThe therapeutic efficacy of Flavoxate can be decreased when used in combination with Tacrine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Tacrine.
FlupentixolThe therapeutic efficacy of Flupentixol can be decreased when used in combination with Tacrine.
FluphenazineThe therapeutic efficacy of Fluphenazine can be decreased when used in combination with Tacrine.
Fluticasone PropionateThe therapeutic efficacy of Fluticasone Propionate can be decreased when used in combination with Tacrine.
GlycopyrrolateThe therapeutic efficacy of Glycopyrrolate can be decreased when used in combination with Tacrine.
GuanidineThe risk or severity of adverse effects can be increased when Tacrine is combined with Guanidine.
HaloperidolThe therapeutic efficacy of Haloperidol can be decreased when used in combination with Tacrine.
HomatropineThe therapeutic efficacy of Homatropine can be decreased when used in combination with Tacrine.
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Tacrine.
HydroxyzineThe therapeutic efficacy of Hydroxyzine can be decreased when used in combination with Tacrine.
HyoscyamineThe therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Tacrine.
IloperidoneTacrine may increase the central neurotoxic activities of Iloperidone.
ImipramineThe therapeutic efficacy of Imipramine can be decreased when used in combination with Tacrine.
Ipratropium bromideThe therapeutic efficacy of Ipratropium bromide can be decreased when used in combination with Tacrine.
IsocarboxazidThe therapeutic efficacy of Isocarboxazid can be decreased when used in combination with Tacrine.
LabetalolTacrine may increase the bradycardic activities of Labetalol.
LevocabastineThe therapeutic efficacy of Levocabastine can be decreased when used in combination with Tacrine.
LevocetirizineThe therapeutic efficacy of Levocetirizine can be decreased when used in combination with Tacrine.
LoratadineThe therapeutic efficacy of Loratadine can be decreased when used in combination with Tacrine.
LoxapineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Tacrine.
LurasidoneTacrine may increase the central neurotoxic activities of Lurasidone.
MaprotilineThe therapeutic efficacy of Maprotiline can be decreased when used in combination with Tacrine.
MeclizineThe therapeutic efficacy of Meclizine can be decreased when used in combination with Tacrine.
MepenzolateThe therapeutic efficacy of Mepenzolate can be decreased when used in combination with Tacrine.
MethacholineThe risk or severity of adverse effects can be increased when Tacrine is combined with Methacholine.
MethotrimeprazineThe therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Tacrine.
MethscopolamineThe therapeutic efficacy of Methscopolamine can be decreased when used in combination with Tacrine.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Tacrine.
MetoprololTacrine may increase the bradycardic activities of Metoprolol.
MoclobemideThe therapeutic efficacy of Moclobemide can be decreased when used in combination with Tacrine.
NadololTacrine may increase the bradycardic activities of Nadolol.
NebivololTacrine may increase the bradycardic activities of Nebivolol.
NortriptylineThe therapeutic efficacy of Nortriptyline can be decreased when used in combination with Tacrine.
OlanzapineThe therapeutic efficacy of Olanzapine can be decreased when used in combination with Tacrine.
OlopatadineThe therapeutic efficacy of Olopatadine can be decreased when used in combination with Tacrine.
OrphenadrineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Tacrine.
OxybutyninThe therapeutic efficacy of Oxybutynin can be decreased when used in combination with Tacrine.
PaliperidoneTacrine may increase the central neurotoxic activities of Paliperidone.
PancuroniumTacrine may decrease the neuromuscular blocking activities of Pancuronium.
PenbutololTacrine may increase the bradycardic activities of Penbutolol.
PerphenazineThe therapeutic efficacy of Perphenazine can be decreased when used in combination with Tacrine.
PhenelzineThe therapeutic efficacy of Phenelzine can be decreased when used in combination with Tacrine.
PilocarpineThe risk or severity of adverse effects can be increased when Tacrine is combined with Pilocarpine.
PimozideThe therapeutic efficacy of Pimozide can be decreased when used in combination with Tacrine.
PindololTacrine may increase the bradycardic activities of Pindolol.
PizotifenThe therapeutic efficacy of Pizotifen can be decreased when used in combination with Tacrine.
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Tacrine.
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Tacrine.
ProchlorperazineThe therapeutic efficacy of Prochlorperazine can be decreased when used in combination with Tacrine.
ProcyclidineThe therapeutic efficacy of Procyclidine can be decreased when used in combination with Tacrine.
PromazineThe therapeutic efficacy of Promazine can be decreased when used in combination with Tacrine.
PromethazineThe therapeutic efficacy of Promethazine can be decreased when used in combination with Tacrine.
PropanthelineThe therapeutic efficacy of Propantheline can be decreased when used in combination with Tacrine.
PropranololTacrine may increase the bradycardic activities of Propranolol.
ProtriptylineThe therapeutic efficacy of Protriptyline can be decreased when used in combination with Tacrine.
QuetiapineThe therapeutic efficacy of Quetiapine can be decreased when used in combination with Tacrine.
Repository corticotropinThe risk or severity of adverse effects can be increased when Repository corticotropin is combined with Tacrine.
RisperidoneThe therapeutic efficacy of Risperidone can be decreased when used in combination with Tacrine.
RocuroniumTacrine may decrease the neuromuscular blocking activities of Rocuronium.
ScopolamineThe therapeutic efficacy of Scopolamine can be decreased when used in combination with Tacrine.
Scopolamine butylbromideThe therapeutic efficacy of Scopolamine butylbromide can be decreased when used in combination with Tacrine.
SolifenacinThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Tacrine.
SotalolTacrine may increase the bradycardic activities of Sotalol.
SuccinylcholineThe serum concentration of Succinylcholine can be increased when it is combined with Tacrine.
ThioridazineThe therapeutic efficacy of Thioridazine can be decreased when used in combination with Tacrine.
ThiothixeneThe therapeutic efficacy of Thiothixene can be decreased when used in combination with Tacrine.
TimololTacrine may increase the bradycardic activities of Timolol.
TiotropiumThe therapeutic efficacy of Tiotropium can be decreased when used in combination with Tacrine.
TolterodineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Tacrine.
TranylcypromineThe therapeutic efficacy of Tranylcypromine can be decreased when used in combination with Tacrine.
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Tacrine.
TrifluoperazineThe therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Tacrine.
TrihexyphenidylThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Tacrine.
TrimethobenzamideThe therapeutic efficacy of Trimethobenzamide can be decreased when used in combination with Tacrine.
TrimipramineThe therapeutic efficacy of Trimipramine can be decreased when used in combination with Tacrine.
TriprolidineThe therapeutic efficacy of Triprolidine can be decreased when used in combination with Tacrine.
TrospiumThe therapeutic efficacy of Trospium can be decreased when used in combination with Tacrine.
UmeclidiniumThe therapeutic efficacy of Umeclidinium can be decreased when used in combination with Tacrine.
VecuroniumTacrine may decrease the neuromuscular blocking activities of Vecuronium.
ZiprasidoneTacrine may increase the central neurotoxic activities of Ziprasidone.
ZuclopenthixolThe therapeutic efficacy of Zuclopenthixol can be decreased when used in combination with Tacrine.

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Aminopyridines and derivatives
  • Aminoquinolines and derivatives
  • Azacyclic compounds
  • Benzenoids
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • Primary aromatic amines

substituent:
  • Acridine
  • Amine
  • Aminopyridine
  • Aminoquinoline
  • Aromatic heteropolycyclic compound
  • Azacycle
  • Benzenoid
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Primary amine
  • Primary aromatic amine
  • Pyridine

References

Synthesis Reference: S. Shirley Yang, Wayne Boisvert, Nouman A. Muhammad, Jay Weiss, "Controlled release tacrine drug delivery systems and methods for preparing same." U.S. Patent US5576022, issued February, 1993.
General Reference: # Qizilbash N, Whitehead A, Higgins J, Wilcock G, Schneider L, Farlow M: Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration. JAMA. 1998 Nov 25;280(20):1777-82. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9842955 # Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20480924
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic2/tacrine.htm
Drugs.comhttp://www.drugs.com/cdi/tacrine.html

ATC Codes:
  • Array

AHFS Codes:
  • Not Available

MSDS: Download
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