Cogitive Enhancers - Lichtblau Flashcards
What are the potential uses of cognitive enhancers?
- Attention Deficit (Hyperactivity) Disorder
- ADD
- ADHD
- Alzheimer disease
- “Smart drug” (nootropics)
What are the key characteristics of ADHD?
- Charachterized by co-existence of:
- attentional problems (inattentive)
- hyperactivity
- impulsivity
- each behavior occurring infrequently alone
- Symptoms onset before age 7
How should ADHD be diagnosed?
- Complete developmental, mental, nutritional, physical, and psychosocial examination
- Parent & teacher questionnaires
- Psychological evaluation of the child AND family
- IQ testing
- psychological testing
What drugs (classes) are used to treat ADHD?
- Psychostimulants
- Methylphenidate
- Amphetamines
- Atomoxetine (Straterra)
What is the neurochemical action of psychostimulants?
- Enhances DA release and blocks reuptake
- Enhances NE release
What are some specific examples of psychostimulant amphetamines used to treat ADHD?
- Dexedrine = immediate release
- Dexedrine Spansules/Adderall XR = sustained release
What are some specific examples of psychostimulant methylphenidates used to treat ADHD?
- Ritalin = immediate release
- Concerta/Metadate CD = sustained release
Why are CNS stimulants effective in treating ADHD?
These drugs stimulate activation of inhibitory areas that allow the patient to focus (inhibit excitatory stimuli).
-increase underactive inhibitory centers
What areas of the brain are activated by psychostimulants at low (therapeutic) doses?
Areas of the prefrontal and limbic cortex involved with focusing and maintaining attention and prioritizing behaviors.
What areas of the brain are activated by psychostimulants at higher (euphoric/toxic) doses?
Areas of the brain involved in motor activity and arousal
What is the MOA of Atomoxetine (Strattera)?
- Highly selective NE reuptake inhibitor
- Elevates DA levels in the prefrontal cortex
- NOT nucleus accumbens/striatum
- Increase ACh release from post-synaptic neurons in the frontal cortex
- only when alpha1-NE & D1-DA receptors on post-synaptic membrane are simultaneously activated by NE/DA
What is different about ADHD treatment with Atomoxetine (Strattera) compared to psychostimulants?
- No abuse potential
- Not a DEA Schedule II controlled substance
- Only drug approved by the FDA to treat adult ADHD
What are the microscopic changes in patients with Alzheimer Disease?
- Neurofibrillary tangles within the neuron cell body
- surround neurons’ microtubules
- interfere with cell’s ability to eliminate waste from the cell body –> axon terminal
- Beta-amyloid polypetides along axon dentrite are overproduced
- accumulate in synapse and interfere with normal cholinergic neurotransmission
What are the macroscopic changes in patients with Alzheimer Disease?
Brain looks like swiss cheese
- large ventricles
- shrunken cortex
What is the basic mechanism for all drugs used to treat mild to moderate Alzheimer Disease?
Elevate ACh levels by inhibiting acetylcholinesterase
What AD drug inhibits both AChE & BuChE, is administered twice daily, and causes gastrointestinal problems/muscle weakness?
Rivastigmine (Exelon)
What AD drug has a short half-life so it needs to be given multiple times per day, has poor compliance because of this, may cause liver damage, also has many drug interactions (esp. NSAIDs), and is the second-line therapy for AD?
Tacrine (Cognex)
What AD drug inhibits AChE only, stimulates nicotinic cholinergic neurons to release more stored ACh, should be taken cautiously due to drug interference with elimination from the body, and increases the risk of stomach ulcers so NSAID us is with great caution?
Galantamine (Razadyne)
What AD drug is useful in patients with moderate to severe AD, is an antagonist at the NMDA subtype of glutamate receptor, found to help patients in the later stages of the disease maintain additional independence, and has adverse side effects that include dizziness, headache, constipation, and confusion?
Memantine (Namenda)
What AD drug may have a modest benefit for patients with AD, but has serious side effects like bleeding, seizures, and coma?
Ginko Biloba
What four drugs are sometimes taken for AD, but have insufficient evidence that they improve cognition or function?
- Vitamin E
- Selegiline (Eldepryl)
- Estrogen
- NSAIDs
What are Nootropics?
“Mind Bend/Turn”
Also Known As:
- Smart drugs
- Memory enhancers
- Cognitive enhancers
- Intelligence enhancers
What are some examples of Nootropics?
- Supplements
- Piracetam (Nootropil, Nootropyl, Nooracetam)
- Aniracetam (Memotropil, Memodrin, Ampamet, Draganon, Referan)
- Oxiracetam
- Choline
- Ampakines
- Nootropic Vitamins
What are Eugeroics?
“Wakefulness Enhancers”
What are two examples of Eugeroics? MOA?
- Modafinil (Provigil)
- Armodafinil (Nuvigil)
Increase release of NE & DA
Elevate hypothalamic histamine levels
