pharm 4th j cns

What is acetylcholine involved in?

Learning, memory, muscle movement

-Myasthenia gravis, Alzheimer's (loss), Parkinson's (increase)

What is Serotonin (Inhibitory) & Norepinephrine (Excitatory) involved in?

Involved in mood, depression, pain regulation

-Antidepressants, CNS stimulants

What is Dopamine (Excitatory) involved in?

involved in movement, arousal & mood states, thought processes

-Schizophrenia (overactive), Parkinson's (loss)

What is GABA (Inhibitory) involved in?

Main inhibitory neurotransmitter

-Anxiety disorders, Huntington's Chorea (loss of neurons using GABA)

What is Glutamate (Excitatory) involved in?

Main excitatory neurotransmitter

-High concentrations → neuronal cell death

Epinephrine

fight or flight response

Histamine (Neuromodulator) affects what?

Alertness, cardiac stimulation, peripheral allergic response, gastric secretions

What is an anxiety disorder?

An uncomfortable state with psychologic and physical components

What is insomnia?

Difficulty with: falling asleep, staying asleep, waking early

-Poor: sleep quantity or quality

What is an anxiolytic?

"Sedative" - Produce calm & relaxation, reduces excitement

-benzodiazepines

What is hypnotic analgesia?

produce sleep

Benzodiazepines are used for what?

insomnia and anxiety
-inducing anesthesia, etc.

Benzos are generally \_____________________

very well tolerated

Benzodiazepines potentiate \____________

GABA
-are not that harmful bc they use the GABA we have in the body

Side effects of benzodiazepines

-CNS depression
-weak respiratory depression
-IV use could cause hypotension and cardiac arrest

What pregnancy category are benzodiazepines?

pregnancy D or X

What do we use flumazenil (Romazicon) do in relation to benzodiazepines?

antidote for Benzodiazepines but only affects sedation not the respiratory depression

What do we need to be constantly assessing in patients taking benzodiazepines?

respiratory depression

What do benzodiazepines end in?

end in -am (-epam, -olam)
-lorazepam [Ativan]
-alprazolam [Xanax]

When should we take benzodiazepines?

take with food for GI upset

What are the preferred agents for insomnia, not indicated for anxiety?

Benzodiazepine-like Drugs

Benzodiazepine-like drugs have a \______ potential for tolerance, dependence, and abuse

low

What are the Z drugs (benzodiazepine-like drugs)?

-Zolpidem (Ambien)
-Zaleplon (Sonata)
-Eszopiclone (Lunesta)

What is Ramelteon (Rozerem)?

melotonin agonist

What is ramelteon used for?

sleep onset insomnia

What are barbiturates used for?

CNS depressants used to
-relieve anxiety
-induce sleep
-anti-seizure
-induce anesthesia

Barbituates can cause \______________ and \________________

tolerance and dependance

Barbiturates are POWERFUL \___________ \______________

respiratory depressants

What is the relationship between barbiturates and GABA?

they potentiate and mimic GABA
-dangerous levels of natural and unnatural GABA production (respiratory depression)

Adverse effects of barbiturates

-respiratory depression
-suicide (only give 2 doses)
-abuse

Phenobarbital (barbiturate) is used for what?

seizures

What drugs can we use to treat generalized anxiety disorder?

-antidepressants
-buspirone
-benzodiazepines

Benzodiazepines are primarily now used for \________ \____________

anxiety attacks
-not good for long-term anxiety management

If a patient comes in with generalized anxiety disorder what would they be prescribed?

buspirone (BuSpar)

If a patient comes in with generalized anxiety disorder and depression what should they be prescribed?

anti-depressants
-the side effects help control anxiety

Buspirone (Buspar) is good because it doesn't have \_________ \__________

CNS depression

Depression symptoms must be present for how long in order to be diagnosed?

Symptoms must be present most of the day, nearly every day, for at least 2 weeks

What tool do we use to diagnose depression?

PHQ-9

Treatment for depression

antidepressants

If your patient expresses that they are suicidal what question should you ask?

do they have a plan?

How long does it take for antidepressants to kick in?

about 1-2 months

antidepressants have a \________ \____ warning

black box warning
-suicidal ideation

What are the most commonly prescribed antidepressants?

Selective Serotonin Reuptake Inhibitors (SSRIs)
-fluoxetine [Prozac]

Side effects of SSRIs

-serotonin syndrome
-sexual dysfunction, weight gain, n/v
-withdrawal syndrome (do not stop abruptly)

Symptoms of serotonin syndrome

-Hyperreflexia (clonus/tremors)
-diaphoresis/fever
-Diarrhea
-tachycardia
-agitation

How do we treat serotonin syndrome?

discontinue SSRIs

Examples of SSRIs

-fluoxetine [Prozac]
-citalopram [Celexa]
-escitalopram [Lexapro]
-sertraline [Zoloft]
-paroxetine [Paxil]

Examples of Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs)

-venlafaxine
-duloxetine [Cymbalta]

What are tricyclic antidepressants used for?

-Depression
-bipolar disorder
-fibromyalgia

Adverse effects of Tricyclic antidepressants (TCA)

-sedation
-orthostatic hypotension
-anticholinergic effects
-cardiac toxicity!!!

If cardiac toxicity occurs with TCA what must we have on hand to treat the dysrhythmias?

sodium bicarbonate

If a patient attempts to overdose on tricyclic antidepressants (or really any drug) how do we get it out of their system?

gastric lavage

What is the suffix of tricyclic antidepressants?

-tyline or -ipramine
amitriptyline

Monoamine Oxidase Inhibitors (MAOI) are used for what?

depression

Monoamine Oxidase Inhibitors (MAOI) inactivate tyramine and if the patient eats a diet rich in dietary tyramine that could cause what?

hypertensive crisis

What can we use to treat a hypertensive crisis?

sodium nitroprusside

Adverse effects of MAOI's

-hypertensive crisis with dietary tyramine
-orthostatic hypotension
-CNS stimulation

Examples of MAOIs

Isocarboxazid (Marplan)

When a patient is on an MAOI they should avoid \_______ medications

ALL

What is Bupropion used for?

depression and smoking cessation

When do we start to see the effects of bupropion?

1-3 weeks (faster)

bupropion has the \________ adverse effects of other antidepressants

opposite AEs of other antidepressants making it a great drug to give along with them to counteract the AEs

How would we usually used bupropion?

in conjunction with other antidepressants to counteract side effects
-doesn't work as well

What do we use trazodone for?

sedation
-use for pts with depression induced insomnia

What can we use to treat bipolar disorder?

-mood stabilizers
-antipsychotics
-antidepressants

What is the most common drug regimen for bipolar disorder?

Mood stabilizer + antidepressant

What is the most common mood stabilizer?

Lithium

Lithium has a \__________ therapeutic range

narrow
-we must commonly check levels

When a pt is on lithium we need to asses their \________ levels

sodium

If the pt sodium levels fluctuate the body will bind to lithium which could cause \__________ toxicity

Lithium toxicity

symptoms of lithium toxicity

-GI upset
-tremors
-polyuria
-renal toxicity
-goiter/hypothyroid
-teratogenesis

Types of drugs for mania

-divalproex sodium (valproate)
-carbamazepine
-Iamotrigine

types of antipsychotic drugs

-risperidone
-aripriprazole

Adverse effects of Antipsychotics

-Extrapyramidal syndrome (EPS)
-Neuroleptic Malignant Syndrome (NMS)

Extrapyramidal Symptoms (EPS)

Muscle tone disorders

Early - acute dystonia, parkinsonism, akathisia
Late* - tardive dyskinesia (TD)

How do we treat Extrapyramidal symptoms (EPS)?

diphenhydramine (anticholinergics)

What is neuroleptic malignant syndrome?

-fever
-muscle rigidity
-altered mental status
-cardiovascular instability

Supportive measures for NMS

-cooling blanket
-antipyretics/hydration
-benzodiazepines
-dantrolene
-bromocriptine

What is the most common high-potency antipsychotic?

haloperidol

What is the most common low-potency antipsychotic?

chlorpromazine

Second-Generation (Atypical) Antipsychotics adverse effects

can cause dyslipidemia/ cause a higher risk for diabetes \= cardiovascular issues

What is the difference between 1st ten and 2nd ten antipsychotics?

1st gen \= EPS and NMS
2nd gen\= metabolic effects

Clozapine is used to treat

schizophrenia

Clozapine adverse effects

-weight gain
-hyperglycemia
-orthostatic hypotension
-sedation

\_____________ is the most effective for treating the core illness of schizophrenia

clozapine

Parkinson's disease is caused by a lack of \__________ which caused \_______________ to take more effect

a lack of dopamine causes acetylcholine to take more effect

What are the 2 main categories for Parkinson's Pharmacotherapy:

-dopaminergic agents
-anticholinergic

Do anti-Parkinson drugs cure the disease?

no, they help to alleviate symptoms but do not cure the disease

What is the most common dopaminergic agents?

Levodopa

adverse effect of levodopa

-n/v

wearing-off effect
and
on-off syndrome

What is the wearing off effect?

symptom control is really good until after a few years symptoms of PD return or worsen before the next dose of meds is due
-expected over time

What is the "on-off" effect of levodopa?

Fluctuations in clinical response, drug doesn't function adequately only some of the time

If we give a pt levodopa and it doesn't work what do we question?

if they even have Parkinson's

Levodopa is almost always combined with \_____________

carbidopa
-enhances the effect

When do we need to take Levodopa/carbidopa?

In the morning to combat the n/v

What other drugs can we use to treat the symptoms of Parkinson's?

-Dopamine agonists
-Ergot derivatives
-Nonergot derivatives
-COMT Inhibitors
-MAO-B Inhibitors
-Amantadine
-Centrally acting anticholinergics

What drugs are used for Alzheimer's disease?

Cholinesterase Inhibitors

Do Cholinesterase Inhibitors cure Alzheimer's?

May delay or slow disease - will not stop AD

What are the 3 types of cholinesterase Inhibitors?

-Donepezil
-Galantamine
-rivastigmine

"Ron Gets Dumb"
ron has alzheimer's

What is Memantine (Namenda) used for?

moderate to severe AD
-NMDA receptor antagonists

"Mema needs memantine bc she has Alzheimer's"