anti-alzheimers drug

10,106 views 31 slides Oct 20, 2022
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About This Presentation

Alzheimer's disease is a progressive neurologic disorder that causes the brain to shrink (atrophy) and brain cells to die. Alzheimer's disease is the most common cause of dementia — a continuous decline in thinking, behavioral and social skills that affects a person's ability to functi...


Slide Content

Vijay salvekar
Dept. of Pharmacology
GRY Institute of Pharmacy

Alzheimer's is the most common form ofdementia.
It is a neurodegenerative disease that occurs in thebrain.
Alzheimer’sdiseasecausesadeteriorationinthebrainby
destroyingthenervecells.Oncethenervecellsbeginto
deteriorateitcausesareductionofresponsestoother
nervecells.

The first person to describe thisdisease

The first Alzheimer Patient inHistory
AugusteDeter

Generally,itisdiagnosedinpeopleover65yearsofage,
althoughtheless-prevalentearlyonsetofAlzheimer’scan
occurmuchearlier.
In 2006, there were 26.6 million sufferersworldwide.
Alzheimer’s is predicted to affect 1 in 85 people globally
by2050.



Alzheimer’s affects thebrain.
Alzheimer'scausesneuronstodiewhichcausesthebrain
toshrink.Thisleadstoalossoffunctioningcapabilitiesin
almostallpartsofbrain,notjusttheonesthataffect
memory.
Thisleadstotheformationofclumpsandtangleswithin
thebrainandeventuallyleadstodeath.
WhenyouhaveAlzheimer’sthecerebralcortexshrinks
massively.Thecerebralcortexistheoutersurfaceofthe
brainanditisresponsibleforallintellectualfunctioning.
Thespacesinthefoldsofthebrain(thesulci)aregrossly
enlarged.
YoucannotcatchorspreadAlzheimer’s



Short term memory loss –forgetting recent events, names
andplaces
Difficulty performing familiartasks
Disorientation especiallyawayfromyournormal
surroundings
Increasing problems with planning and managing
Trouble withlanguage
Rapid, unpredictable mood swings
Lack ofmotivation
Changes in sleep and confusion about the time ofday
Reduced judgement e.g. being unaware ofdanger





MemantineisthefirstinanovelclassofAlzheimer's
diseasemedicationsactingontheglutamatergicsystem
byblockingNMDAreceptors.ItwasfirstsynthesizedbyEli
LillyandCompanyin1968.Memantineismarketedunder
, Namenda byForest,the brands Axura and Akatinol by
Ebixa and and Memox byUnipharm.
Pharmacokinetic data
Bioavailability ~100%
Metabolism Hepatic(<10%)
Biological half-life 60–100 hours
ExcretionRenal




Memantineisaclinicallyusefuldruginmanyneurological
disorders,includingAlzheimer'sdisease.Theprincipal
mechanismofactionofmemantineisbelievedtobethe
blockadeofcurrentflowthroughchannelsofN-methyl-d-
aspartate(NMDA)receptors—aglutamatereceptor
subfamilybroadlyinvolvedinbrainfunction.Surprisingly,
otherdrugsthatblockNMDAreceptorchannels,suchas
ketamine,exhibitseriousdeleteriouseffects.Theunusual
therapeuticutilityofmemantineprobablyresultsfrom
inhibitorymechanismssharedwithketamine,combined
withactionsspecifictomemantine.Thesepotentially
importantdifferencesbetweenmemantineandketamine
includeeffectsongatingofblockedchannelsandbinding
ofmemantinetotwositesonNMDAreceptors






Wernicke-Korsakoff syndrome.
Huntingtondisease.
Bipolardisorder.
Treatmentofopioid-resistantcancerpain.
Clinicaltrialsofmemantineinneuropathicpainhavenot
beenpromisingsofar,anditsroutineuseinneuropathic
painisnotcurrentlyrecommended
Memantinehasbeenusedforthetreatmentofvascular
dementia,butcurrentlythereisinsufficientevidenceto
recommenduseinpurevascular.

Namenda (memantine hydrochloride) is contraindicated in
patients with known hypersensitivity to memantine
hydrochloride or to any excipients used in the
formulation.

Aricept
Donepezil
Used to delay or slow the symptoms ofAD
•Loses its effect over time
•Used for mild, moderate and severeAD
•Does not prevent or cureAD
Celexa
Citalopram Used to reduce depression andanxiety
•May take 4 to 6 weeks towork
•Sometimes used to help people get tosleep
Depakote
SodiumValproate
Used to treat severeaggression
•Also used to treat depression andanxiety
Exelon
Rivastigmine
Used to delay or slow the symptoms ofAD
•Loses its effect overtime
•Used for mild to moderateAD
•Can get in pill form or as a skinpatch
•Does not prevent or cureAD


Used to reduce depression andanxiety
•May take 4 to 6 weeks towork
•Sometimes used to help people get tosleep
Depakote®(DEP-uh-cote)
Sodium valproate (so-DEE-umVAL-pro-ate)
Used to treat severeaggression
•Also used to treat depression andanxiety
Exelon® (EKS-uh-lawn) Rivastigmine
(riv-uh-STIG-meen)
Used to delay or slow the symptoms ofAD
•Loses its effect overtime
•Used for mild to moderateAD
•Can get in pill form or as a skinpatch
•Does not prevent or cureAD



Namenda
Memantine
Used to delay or slow the symptoms ofAD
•Loses its effect overtime
•Used for moderate to severeAD
•Sometimes given with Aricept®,Exelon®
•Does not prevent or cureAD
Used to prevent or slow the symptoms ofAD
•Loses its effect overtime
•Used for mild to moderateAD
•Can get in pill form or as a skinpatch
•Does not prevent or cureAD
Used to reduce depression andanxiety
•May take 4 to 6 weeks towork
•Sometimes used to help people get tosleep
Used to treat severeaggression
•Also used to treat depression andanxiety
Razadyne
Galantamine
Zoloft
Sertraline
Trileptal
Oxcarbazepine

Tegretol
Carbamazepine
Remeron
Mirtazepine
Used to treat severeaggression
•Also used to treat depression andanxiety
Used to reduce depression andanxiety
•May take 4 to 6 weeks towork
•Sometimes used to help people get tosleep

Levodopa wasdevelopedinthelate1960sandwasthefirst
medicationproveneffectiveintreatingachronic
neurodegenerative disease likePD.
Levodopainpillformisabsorbedinthebloodfromthesmall
intestineandtravelsthroughthebloodtothebrain,whereitis
convertedintodopamine.
Levodopaisalmostalwaysgivenincombinationwithanother
medicationcalledCarbidopa.Carbidopaisalsoalevodopa
enhancer.

Nausea
Vomiting







Loss of appetite
Lightheadedness
Lowered blood pressure
Confusion
Dyskinesia
Uncommon SideEffects


Sleepiness,suddenonsetsleep
Impulsecontroldisorders(compulsivebehaviors)suchas
excessivegambling,shopping,internetuseorincreased
sexualbehavior

Tacrine improves the function of nerve cells in the brain.
It works by preventing the breakdown of a chemicalcalled
acetylcholine.Peoplewithdementiausuallyhavelower
levelsofthischemical,whichisimportantforthe
processesofmemory,thinking,andreasoning.
Tacrine is used to treat mild to moderate dementia caused
by Alzheimer'sdisease.
Tacrine may also be used for purposes other than those
listed in this medicationguide.

Themechanismoftacrineisnotfullyknown,butitis
suggestedthatthedrugisananticholinesteraseagent
whichreversiblybindswithandinactivates
acetylcholinereleased
cholinesterases.Thisinhibitsthehydrolysisof
fromfunctioningcholinergic
neurons,thusleadingtoanaccumulationofacetylcholine
atcholinergicsynapses.Theresultisaprolongedeffectof
acetylcholine.

confusion,hallucinations;
extreme or sudden changes in behavior;
seizure(convulsions);





painorburningwhenyouurinate;or
nausea,stomachpain,lowfever,lossofappetite,dark
urine,clay-coloredstools,jaundice(yellowingoftheskin
oreyes).
Lessserioussideeffectsoftacrineinclude:
mild nausea, vomiting, diarrhea, upset stomach;
weight loss;
urinating more than usual;
agitation, depressedmood;
fever or chills, runny nose,cough;





Galantamineimprovesthefunctionofnervecellsinthe
brain.Itworksbypreventingthebreakdownofachemical
calledacetylcholine.Peoplewithdementiausuallyhave
lowerlevelsofthischemical,whichisimportantforthe
processesofmemory,thinking,andreasoning.
Galantamine is used to treat mild to moderate dementia
caused byAlzheimer'sdisease.
Galantamine may also be used for purposes not listed in
this medicationguide.

Galantamineisaphenanthrenealkaloidandareversible,
competitiveacetylcholinesteraseinhibitor.Itisnot
structurallyrelatedtootheracetylcholinesterase
inhibitors.Galantamine'sproposedmechanismofaction
involvesthereversibleinhibitionofacetylcholinesterase,
whichpreventsthehydrolysisofacetycholine,leadingto
anincreasedconcentrationofacetylcholineatcholinergic
synapses.
nicotinic
Galantaminealsobindsallostericallywith
acetylcholinereceptorsandmaypossibly
potentiate the action of agonists (such as acetylcholine) at
thesereceptors.

chest pain, slow heart rate;
feeling like you might passout;
blood in your urine or stool;
painful or difficulturination;






urinating less than usual or not atall;
weakness, confusion, decreased sweating, extreme thirst,
hot dry skin;or
Less serious side effects mayinclude:





feeling tired, dizzy, or drowsy;
headache, blurred vision, runny nose;
depression, sleep problems(insomnia);
nausea, vomiting, stomach pain, loss of appetite;
weight loss;or