Pharmacology for Cognitive Issues Flashcards
How do most drugs impact the CNS?
They cross the BBB and act by altering neurotransmission
Can have stimulant properties like excitement, euphoria, decreased fatigue, increased motor activity
Can have inhibitory properties like depression, sedation, fatigue and decreased motor activity
What does endogenous mean?
Having an internal cause or origin; growing or originating from within an (animal)*
What does exogenous mean?
Relating to or developing from external factors; growing or originating from outside an organism*
-mimetic
marked by simulation of another bodily process or disease; also used as a word termination indicating simulation of a function, process, etc., designated by the root to which it is affixed; “mimics”
-lytic
word termination denoting lysis of the substance indicated by the stem to which it is affixed
What do agonists and antagonists drugs do to the nervous system?
Drugs that stimulate a nervous system are called agonists
Drugs that inhibit a nervous system are called antagonists
What are “adrenergics” or “pressors”?
Any drugs that are agonists on the sympathetic nervous system sympathomimetics
Mydriasis, increased heart rate and blood pressure, bronchodilation
What are “beta blockers” or “alpha blockers”?
Any drugs that are antagonists on the sympathetic nervous system sympatholytics
Miosis, decreased heart rate and blood pressure, bronchoconstriction (in patients with bronchospastic disease)
What are “cholinergic agents”?
Any drugs that are agonists on the parasympathetic nervous system
parasympathomimetics
Miosis, decreased heart rate and blood pressure, bronchoconstriction (in patients with bronchospastic disease)
Increased tear production
What are “anticholinergic agents”
Any drugs that are antagonists on the parasympathetic nervous system
parasympatholytics
Mydriasis, increased heart rate and blood pressure, bronchodilation
Decreased tear production (dry eyes)
What are some drugs used for ADD or ADHD (all stimulants)
Methylphenidate: Ritalin, Methylin, Metadate, Concerta, Daytrana
Dexmethylphenidate: Focalin
Amphetamines: Adderall , Dexedrine, Dextrostat, Vyvanse
What are endogenous chemicals, what do they control and how are they impacted?
Control involuntary functions: heart rate, blood pressure, respiration, perspiration, digestion
Can be influenced by thought and emotion
Adjusts in response to stressful situations (trauma, fear, hypoglycemia, cold, exercise, emergency)
How are the four descriptors of drugs intertwined or how do they cross over?
Sympathomimetic = Parasympatholytics
Sympatholytic = Parasympathomimetic
How do ADD and ADHD medications work?
These drugs are psychomotor stimulants: they increase motor activity in patients with ADD or ADHD; if abused, they cause excitement and euphoria
Blockade of the reuptake of monoamines (norepinephrine, serotonin, dopamine)
Sympathomimetic
What are some Dopamine agonists?
Bromocriptine (Parlodel), pergolide (Permax)
Pramipexole (Mirapex), ropinirole (ReQuip)
What are Dopamine agonists used for and what do they do?
Uses: Parkinson’s disease; restless leg syndrome
These drugs increase dopamine in the CNS (not as effective as dopaminergics)
What are some side effects for stimulants?
What would happen if you’re scared:
Insomnia
Weight loss (due to decreased appetite)
Anxiety
Agitation
Cardiac arrhythmias
Tachycardia
Increased respiration
Dyspnea
Seizures
Tremors
Vertigo
Hypertension
Confusion
Nausea
Diarrhea
Addiction potential
Where does dopamine work in the brain?
Mesocortical: cognition, memory, attention, emotional behavior and learning
Nigrostriatial: movement and sensory stimulus
Mesolimbic: pleasure and reward, seeking behavior, addition, emotion and perception
What are some adverse effects specifically PTs should care about or be aware of for stimulants?
Postural hypotension
Dyskinesias: Ataxia, Facial & Extremity tics
Hallucination
Insomnia
What are some adverse effects for dopamine agonists?
Hallucination
Insomnia
Malaise
Nightmares
Dizziness
Dyskinesia
Confusion
What are some common Anticholinergics?
Benztropine (Cogentin) trihexyphenidyl (Artane) biperiden ( Akineton ), diphenhydramine (Benadryl)
What are Anticholinergics used for and how do they work?
Uses: used in Parkinson’s disease, and allergic reactions
These drugs inhibit central cholinergic activity
Parasympatholytics
What are some adverse effects for Anticholinergics?
Confusion
Agitation
Tachycardia
Palpitations
Dry mouth
Urinary retention
Constipation
Blurred vision
What are some common Alzheimer’s disease medications?
Acetylcholinesterase inhibitors: cholinergics donepezil (Aricept), rivastigmine (Exelon), galantamine (Razadyne)
What are Acetylcholinesterase inhibitors used for and how do they work?
In early, mild/moderate Alzheimer’s disease to improve cognitive function, and to slow the progression of AD
These drugs enhance cholinergic function by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase
Parasympathomimetic
What are some common tri cyclic antidepressants (TCA) and what are the used for?
amitriptyline (Elavil), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Sinequan), imipramine (Tofranil), nortriptyline, (Pamelor, Aventyl), protriptyline (Vivactil), trimipramine (Surmontil)
Uses: depression, sleep, pain (nerve pain)
How do tri cyclic antidepressants work?
TCAs block the reuptake of NE and/or 5-HT into noradrenergic or serotonergic nerve terminals, respectively
(have an impact on norepinephrine and serotonin)
Also block “dirty receptors”: muscarinic cholinergic receptors, α1 adrenergic receptors, and histamine H1 receptors what causes many of their side effects
What are some common SSRIs (Selective Serotonin Reuptake Inhibitors)? and what are they’re uses?
Citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac), paroxetine (Paxil), sertraline (Zoloft)
Uses: depression, PTSD, PMDD, eating disorders
Why are SSRIs so popular?
SSRIs have the highest affinity for the 5-HT transporter
What are some “atypical” compounds of SSRIs?
SNRIs (serotonin norepinephrine reuptake inhibitors): duloxetine (Cymbalta) Cymbalta), venlafaxine (Effexor), desvenlafaxine (Pristiq)
NDRI (norepinephrine dopamine reuptake inhibitors): bupropion (Wellbutrin, SR, and XL)
SARIs (serotonin antagonist and reuptake inhibitors): nefazodone (Serzone), trazodone (Desyrel) also used for sleep
NaSSA (noradrenergic and specific serotonergic antidepressant)
SRI/5 HT1A (partial agonist serotonin reuptake inhibitor/serotonin 1A partial agonist)
What three transmitters impact cognition, emotions and mood?
Noradrenaline, Serotonin and Dopamine
How do SSRIs work?
Selective for serotonin and increase the amount of serotonin available
With no real impact on dopamine nor acetylcholine, nor norepinephrine
What are some uses for “atypical” compounds of SSRIs and what do they do?
Uses: depression, anxiety syndromes, smoking cessation, sleep, peripheral neuropathy, pain syndromes, hot flashes
These drugs result in a relative increase in both norepinephrine and serotonin
What are some adverse effects of SSRIs?
Sedation
Weight gain
Postural hypotension
Sexual dysfunction
Dizziness
Anxiety
Confusion
What are some common (Anxiolytic) Benzodiazepines (BZDPs) and what are they used for?
Alprazolam (Xanax) Xanax), chlordiazepoxide (Librium), clonazepam (Klonopin) Klonopin), diazepam (Valium) Valium), clorazepate (Tranxene), lorazepam (Ativan) Ativan), oxazepam
Flurazepam (Dalmane), temazepam (Restoril), triazolam (Halcion; marketed for sleep
LAM and PAM
Uses: sleep, muscle relaxers, amnesia, anxiety syndromes, seizure syndromes, alcohol withdrawal
How do BZDPs work? and how long do they last?
Benzodiazepines bind to receptors to inhibit neurotransmitter release
Inhibits GABA throughout the CNS
Compounding inhibitory effect
**The duration of action of the BZDPs varies considerably, and the formation of active metabolites plays a major role in their effects
What are some adverse effects of anxiolytics/BZDPs?
Drowsiness
Psychomotor impairment
Ataxia
Disorientation/confusion
Depression
Aggression
Irritability
Behavioral disinhibition
Anterograde amnesia
What are some common sedatives/soporific agents and what are they used for?
Zolpidem (Ambien), zaleplon (Sonata), eszopiclone (Lunesta)
“Z hypnotics”
Uses: to induce sleep
How do sedatives/soporific agents work?
Acts on only one subset of benzodiazepine receptor family, BZ1
No anticonvulsant or muscle relaxant properties; no withdrawal effects; little/no tolerance (like BZDPs)
What are some adverse effects forsedatives/soporific agents
Nightmares
Sleep eating
Sleep walking
Agitation
Dizziness
Daytime drowsiness
What are some common antihistamines that are used for vertigo or balance disorders?
Diphenhydramine (Benadryl), hydroxyzine (Atarax, Visteril), chlorpheniramine (Chlor Trimeton), promethazine (Phenergan), doxylamine (in NyQuil), Meclizine (Antivert), brompheniramine (Dimetane), dimenhydrinate (Dramamine)
When are antihistamines used (in regards to vestibular issues)?
Used in Type 1 hypersensitivity reactions (rhinitis, urticaria, conjunctivitis, anaphylaxis); prophylaxis for motion sickness and vestibular diseases
How does an antihistamine work for vertigo or balance disorders?
These agents prevent motion sickness and reduce the severity of its symptoms, even if taken after the onset of symptoms
They may suppress vestibular responses through an effect on the CNS, although their mechanism remains unknown
All the antihistamines used for the control of vertigo have anticholinergic activity, and antihistamines that do not cross the BBB are not used to control vertigo
What are some adverse reactions to antihistamines for vertigo or balance disorders?
Sedation
Confusion
Dry eyes
Dry mouth
Ataxia
What are some common Opioid agonists (“narcotics”) that are used for pain management?
Morphine (MS Contin, Avinza, Kadian, MSIR)
Oxycodone (Oxycontin, Percocet)
Hydromorphone (Dilaudid)
Fentanyl (Duragesic, Actiq)
Codeine (Tylenol #3)
Hydrocodone and acetaminophen (Vicodin, Norco, Lortab)
Meperidine (Demerol)
Methadone (Dolobid)
How does opioids work?
These drugs relieve pain and induce euphoria by binding to the opioid receptors (mu, delta, kappa) in the brain
They mimic the actions of endogenous opioid compounds: enkephalins, dynorphins, endorphins
What are some adverse effects for opioids?
Sedation
Constipation
Confusion
Dizziness
Nausea/vomiting
Respiratory depression
Dysphoria
Euphoria
Hallucinations
Itching
What are some common muscle relaxers and what are they used for?
Baclofen (Lioresal), carisoprodol (Soma) Soma), chlorzoxazone (Parafon Forte DSC, Remular S), cyclobenzaprine (Flexeril) Flexeril), diazepam (Valium), metaxalone (Skelaxin) Skelaxin), methocarbamol (Robaxin), orphenadrine (Norflex), tizanidine (Zanaflex)
Tramadol (Ultram)
Uses: for muscle spasms and hyper reflexia
What are some adverse effects of muscle relaxers?
Mental depression
Drowsiness
Dizziness/lightheadedness
May impair mental and physical abilities
Driving and operating machinery not recommended
Trembling
Muscle weakness
Hypotension
Blurred vision
Drug interactions alcohol
