CNS review Flashcards
3 1st generation AEDs that are enzyme inducers
Phenytoin, Phenobarbital and Carbamazepine
MOA of oxcarbazepine
Stabilizes inactivated Na channels
The major inhibitory transmitter in the brain
GABA
Treatment options for status epilepticcus `
IV benzodiazepine, phenytoin or phenobarbital
The major excitatory neurotransmitter in the brain
Glutamate
What is special about the metabolism of phenytoin
saturable metabolism
What is special about the metabolism of carbamazepine
autoinduction
Type of receptor that GABA-A receptor is
inotropic Cl channel
Major toxicities of phenytoin
nystagmus, ataxia, gingival hyperplasia, osteomalacia
Amount of oxcarbazepine that can induce OC metabolism
> 1200 mg/day
Toxicities of oxcarbazepine
dizziness, diplopia, ataxia, hyponatremia
toxicity with lacosamide
diplopia, HA, dizziness, nausea
The most studied AED in pregnancy
Lamotrigine
MOA of carbamazepine
Stabilizes inactivated Na Channels
AED that was recently moved to pregnancy category D due to risk of low birth weights
topiramate
Amount of topiramate that induces OC metabolism
> 200 mg/day
Toxicities with lamotrigine
sedation, diplopia, ataxia, nausea, rash
Toxicities associated with topiramate
difficulty concentrating, kidney stones, weight loss
MOA of zonisamide
Stabilizes inactivated Na channels and acts on Ca channels
Toxicities associated with zonisamide
somnolence, dizziness, kidney stones, weight lossq
MOA of rufinamide
Stabilizes inactivated Na channels
MOA of phenobarbital
GABA-A agonist
Toxicities with phenobarbital
sedation, paradoxical hyperactivity, osteomalacia
Seizure that involves brief episodes of staring, unable to respond
absence/ patit mal
Black box warning for vigabatrin
irreversible visual field loss
MOA of vigabatrin
Irreversible inhibitor of GABA transaminase
SSRI that has potential for QTc prolongation
Citalipram
MOA of ethosuximide
Inhibits T-type Ca channels
Drug of choice for absence seizures
ethosuximide
MOA of tiagabine
decreases GABA reuptake into neurons and glial cells
MOA of valproic acid
Inhibits T-type Ca channels, weak effect of Na channels and increases GABA activity
1st generation AED that is an enzyme inhibitor
valproic acid
Type of receptor that GABA-B is
metaboltropic
Toxicities associated with gabapentin
fatigue, ataxia, dizziness
Major toxicities of carbamazepine
diplopia, dizziness, leukopenia, osteomalacia
MOA of pregabalin
Binds to alpha2-delta site of Ca channels
Toxicities associated with pregabalin
dizziness, ataxia, weight gain
MOA of levetiracitam
Binds to synaptic vesicle protein (SV2A)
Toxicities associated with ezogabine
dizziness, fatigue, diplopia, ataxia, urinary retention
What is notable about gabapentins metabolism
saturable absorption
QIDS score that indicates very severe depression
> 20
MOA of ezogabine
potassium channel stabilizer
MOA of phenytoin
Stabilizes inactivated Na channels
MOA of perampanel
noncompetitive AMPA receptor antagonist
Black box warning with parampanel
suicidality and homocidality
MOA of topiramate
Stabilizes inactivated Na channels, GABA agonist and glutamate antagoinist
SSRI that is pregnancy category D
Paroxetine
Black box warning with ezogabine
bluish discoloration of the skin and ocular toxicity
QIDS score that indicates severe depression
16-20
Issue with felbamate that limits its use
hepatotoxicity
Seizure in 1 hemisphere in which consciousness is not impaired
Simple partial seizure
MOA of ketamine
NMDA antagonist
QIDS score that indicates mild depression
6-10
SSRI that has the highest rate of diarrhea
Sertraline
Location where norepinephrine is synthesized
locus ceruleus
Presynaptic NE autoreceptor that is important in feedback inhibition
Alpha2
The hormonal influence on seizures in women who are menstrating
Catamenial influence
Seizure in 1 hemisphere in which consciousness and memory are impaired
Complex partial seizure
Precursor for NE
Tyrosine
Precursor for serotonin
tryptophan
Length of an untreated major depressive episode
> 6 months
Length of a typical treated major depressive episode
4-5 months
toxicities associated with valproic acid
weight gain, hair loss, tremor, thrombocytopenia
QIDS16 score that indicates remission
A diminished interest in activities
anhedonia
2nd line antidepressant pharmacotherapy options
TCAs, trazadone, nefazadone
QIDS score that indicates normal
0-5
QIDS score that indicates moderate depression
11-15
QIDS16 score that indicates a response
6-8
Return of symptoms meeting full criteria within 6-12 months of full and sustained remission from the index episode
Relapse
1st line options for antidepressant pharmacotherapy
SSRIs, SNRIs, buproprion, mirtazepine
Occurrence of a new episode following 6-12 months of full and sustained remission from the index episode
Reoccurance
3rd line antidepressant pharmacotherapy options
MAOIs
MOA of lacosamide
Stabilized inactivated Na channels
MOA of lamotrigine
Stabilizes inactivated Na channels and decreases glutamate release
SSRI with highest rate of sexual dysfunction
Paroxetine
Toxicities associated with levetiracitam
somnolence, dizziness, behavioral changes
5 most common residual symptoms of depression
insomnia, fatigue, pain, difficulty concentrating, lack of interest
MOA of Gabapentin
Binds to alpha2-delta site of Ca channels, decreasing neurotransmitter release
4 most common triggers of seizures
lack of sleep, stress, acute infections, missed medications
MOA of vilazodone
SSRI and partial 5HT1A receptor agonist
MOA of trazadone
weak SSRI and 5HT2A and 5HR2C antagonist
Black box warning for nefazodone
rare hepatic failure
Non-selective serotonin antagonist that is used to treat serotonin syndrome
Cyproheptidine
MOA of buproprion
Inhibits DA and NE reuptake
MOA of mirtazapine
alpha2-adrenergic antagonist, 5HT2A and 5HT3 antagonist and H1 antagonist
5 tertiary amine TCAs
amitriptyline, trimipramine, imipramine, clomipramine, doxepin
3 secondary amine TCAs
desipramine, nortriptyline, protriptyline
5 patient populations to use caution when using TCAs
- underlying CV disease (QT prolongation)
- seizures
- glaucoma
- urinary retention
- elderly
3 major groups of SEs with TCAs (tertiary > secondary amines)
- anticholinergic SEs
- orthostatic hypotension
- sedation
Antagonist of what receptor leads to orthostatic hypotension
alpha adrenergic receptor
3 non-selective MAO-A and MAO-B irreversible inhibitors
phenelzine,, tranylcypromine, isocarboxazid
A selective MAO-A irreversible inhibitor
Selegiline
Dietary restriction associated with MAO-Is
tyramine containing foods
Drug used to treat hypertensive crisis created by food or drug interactions with MAO-Is
phentolamine
4 major groups of SEs associated with MAO-Is
- orthostatic hypotension
- CNS stimulation (anxiety, insomnia)
- weight gain
- sexual dysfunction
Wash out period needed when switching from MAO-I to another antidepressant or vice versa
2 weeks
Length of time to see effect in GAD
2-4 weeks until effect, 4-6 weeks until max effect
Wash out period needed when switching between fluoxitine and another antidepressant
5 weeks
A transcription factor, whose levels are increased by antidepressants that leads to an increase in the neuronal growth factor BDNF
CREB
Area of the brain that processes threatening or taumatic stimuli
Hippocamous
1st line pharmacologic treatments in anxiety disorder
SSRIs and SNRIs
MOA of buspirone
5HT1A receptor partial agonist
Difference in dose of SRIs between treatment of depression and anxiety
use 1/2 the starting dose in anxiety
GABA-A receptor subunits that are required for BZD binding
alpha and beta
GABA-A receptor subunits that are required for GABA binding
alpha and gamma
3 preferred BZDs in liver disease
Lorazepam, oxazaepam and temazepam
Length of time of excessive anxiety/worry to qualify as generalized anxiety disorder
> 6 months
GAD-7 Score that qualifies as mild GAD
5-9
GAD-7 score that qualifies as moderate GAD
10-14
Transtheoretical model for change phase that a patient is i when they are ready to quit within the next 30 days
Preparation
Transtheoretical model for change phase that a patient is i when they are ready to quit within the next 30 days
Preparation
GAD-7 score that qualifies as severe GAD
> 15
Minimum length of treatment for GAD
12 months
Length of time of persistent worry about another panic attack to qualift as panic disorder
1 month
SSRI that is 2nd line for panic disorder
citalipram
Treatments that are NOT effective for panic disorder
propanolol, buspirone, antihistamines, antipsychotis
Time it takes to see max effect during treatment of manic disorder
6-12 weeks
Length of treatment for panic disorder
12-24 months
Length of fear of social situation to qualify as social anxiety disorder
> 6 months
Treatment options for performance only SAD
propranolol, atenolol
Treatments that are not effective for general SAD
TCAs, buspirone monotherapy, atenolol
Length of medication trial in SAD
8-12 weeks
Length of treatment for SAD
usually long-term
Therapies that are not effective in PTSD
buspirone, buproprion, desimpramine
Time until treatment effect is seen in PTSD
8-12 weeks
Length of therapy in PTSD
Minimum 12 months after response
1st line options for OCD
SSRIs, clmipramine
Length of delay in treatment effect in OCD
10-12 weeks
Length of treatment for OCD
1-2 years, usually lifelong
3 best options for treating anxiety in pregnancy
citalopram, fluoxetine, sertraline
BZD to use if absolutely necessary in pregnancy
clonazepam and lorezapam
Timing of bright light therapy for advanced sleep phase sleeping disorder
PM
Timing of bright light therapy for advanced sleep phase sleeping disorder
PM
Transthoretical model for change that a patient is in when they are thinking about quitting in the next 6 months
Contemplation
BZD antagonist that can reverse effects in overdose
flumazenil
SSRI that has been shown to be safetly used post-MI
Sertraline
GABA receptor subtype that Z-hypnotics preferentially bind to that creates sedative effects but no anxiolytic effects
Alpha-1
Area of the hypothalamus that controls circadian rhythm
suprahiasmatic nucleus
Where melatonin is synthesized
pineal gland
AA precursor of melatonin
tryptophan
MOA of ramelteon
M1 and M2 melatonin receptor agonist
Timing of melatonin therapy in advanced sleep phase disorder
dawn
Transtheoretical model of change stage that a patient is in when they are not yet ready to quit
Pre-contemplation
Location of the hypothalamus where histamine is produced
tuberomemmillary nucleus
Transthoretical model for change that a patient is in when they are thinking about quitting in the next 6 months
Contemplation
Inhibitory dopamine receptors
Type2 (D2, D3 and D4)
Hoehn and Yahr Parkinson’s stage when motor dysfunction is bilateral with postural abnormalities
Stage IV
BZD antagonist that can reverse effects in overdose
flumazenil
TCA that is FDA approved for insomnia characterized by sleep maintenance issues
doxepin (silenor)
MOA of suvorexant
Orexin receptor (OX1 and OX2) antagonist
Transtheoretical model for change that patients are in when they are 6 or more months after their quit date and are now considered a former user
Maintenance
Peptide neurotransmitters implicated in wakefulness that are lost in patients with narcolepsy
Orexins A and B
FDA approved medications for sleep onset
BZDs
Z-hypnotics
Remelteon
Max trial of antidepressants that should be tried with no response
9 weeks
FDA approved medications for sleep maintenance
BZDs
Z-hypnotics
Silenor
3 sleep medications/classes that should not be taken with high fat meals due to decreased absorption
z-hypnotics
ramelteon
silenor
The best established pathway for reinforcement
dopaminergic projection from the ventral tagmental are (VTA) to the nucleus accumbens
Preferred class of sleep drugs in the elderly
Z-hypnotics
MOA of tolcapone
COMT inhibitor in the periphery and CNS
Transtheoretical model of change phase that patients are in when they are actively trying to quit and are still within 6 months of their quit date
Action
GABA receptor subtype that Z-hypnotics preferentially bind to that creates sedative effects but no anxiolytic effects
Alpha-1
5 A’s for clinicians when dealing with substance abuse
Ask Advise Assess Assist Arrange
1st line therapy for alcohol withdraw
BZDs
4 vitamins given to patients with alcohol withdraw
Thiamine (B1)
Folic Acid
Phosphate
Magnesium
The only 2 treatments that were found to be effective for alcohol dependance
Acamprosate
Naltrexone
MOA of disulfiram in treatment of alcohol dependance
increases acetyl aldehyde, creating a terrible rxn when patients drink
Hoehn and Yahr Parkinson’s stage when motor dysfunction is bilateral but there are no postural abnormalities
Stage II
Initial symptoms that anticholinergics help to treat in Parkinson’s disease
tremor and rigidity
Hoehn and Yahr Parkinson’s stage when the disease is fully developed and the patient is bed or chair bound
Stage V
Treatment for the physical symptoms of cocaine intoxicatoin
phentoamine
Ferritin level that worents ferrous sulfate supplementation in RLS
1st line sleep therapy in children
Non-drug therapy
MAO of pramiprexole
D2 and D3 agonist
Area of the brain in which DA is too high, creating the positive symptoms in schizophrenia
mesolimbic pathway
MOA of naltrexone
opioid receptor antagonist
Timing of bright light therapy in delayed sleep phase type sleep disorder
30-60 min in the AM
MOA of phentolamine
alpha-1 blocker
1st line treatment for Parkinson’s disease for a patient
Amantadine and MAO-B-Is
MOA of naloxone
mu-receptor antagonist
Hoehn and Yahr Parkinson’s stage when motor dysfunction is unilateral
Stage I
MOA of carbidopa
peripheral dopa decarboxylase inhibitor
Location in the brain where dopamine is synthesized
substantia nigra
MOA of entacapone
COMT inhibitor in the periphery
High potency FGAs
Trifluoperazine, Fluphenazine, Haloperidol
2 anticholinergic medications that can be used to treat Parkinson’s disease
trihexyphenidyl
benztropine
2 MAO-B inhibitors used to treat Parkinson’s disease
Selegilline
Rasagiline
MAO of bromocriptine
D2 agonist and mild D3 antagonist
MAO of Ropinerole
D2 and D3 agonist
2 DA agonist used to treat Parkinson’s Disease that may cause peripheral edema
amantadine
pramiprexole
MOA of apomorphine
D2 and D3 agonist and D4 antagonist
1st line treatment for Parkinson’s disease for a patient
Dopamine agonist
MOA of all SGAs and FGAs
D2 receptor antagonists
1st line treatment for Parkinson’s disease in a patient that has some cognitive impairment
Carbidopa/levodopa
Inability to sit still
choreiform
1st line treatment for Parkinson’s disease for a patient
Anticholinergics or MAO-B-I
2 antipsychotics that have been studied in Parkinson’s disease
Clozapine and quetiapine
MOA of caffeine
Adenosine A1 and A2 receptor antagonist
Low potency FGAs
Chlorpromazine, Thioridazine
MOA of guanfacine and clonidine
alpha-2 adrenergic agonists
Area of the hypothalamus that controls circadian rhythm
suprahiasmatic nucleus
Area of the brain in which DA is too low, creating the negative symptoms in schizophrenia
Mesocortical pathway
Schizophrenia + bipolar disorder
Schizoaffective disorder
2 TCAs that are preferred in the treatment of ADHD with depression
Imipramine and desipramine
Medium potency FGAs
Loxapine, Perphenazine, Thiothixene
Low potency SGAs
Clozapine, Quetiapine
High potency SGAs
Risperidone, Paliperidone
Receptor that SGAs block that gives them additional efficacy on negative symptoms
5HT2A
SGA that has the highest risk of akathisia (inner restlessness)
Aripiprazole
Antagonism of what receptor by antipsychotics causes anticholinergic SEs
M1
Antagonism of this receptor leads to sedation created by antipsychotics
H1
Antagonism of this receptor leads to hypotension created by antipsychotics
alpha-1
Antipsychotics that have the highest risk of DIMD
high potency, slow dissociation (FGAs)
Antipsychotics that have the highest risk of anticholinergic SEs and sedation
low potency
Antipsychotics that have the highest risk of hypotension
low potency and Iloperidone
Antipsychotics with the highest risk of hyperprolactinemia
FGAs, risperidone and paliperidone
Antagonism of this receptor leads to weight gain associated with antipsychotics
H1
Antagonism of these 3 receptors is associated with lipid and glucose changes associated with antipsychotics
H1, M3, 5HT2C
SGAs that have the highest risk of metabolic issues
clozapine and olanzapine
SGAs that have the lowest risk of metabolic issues
ziprasidone, lurasidone, aripiprazole
Antipsychotics that have the highest risk of neuroleptic malignant syndrome
high potency
3 antipsychotics that are the most important not to abruptly discontinue
clozapine, quetiapine, iloperidone
Antipsychotic that has the highest risk of QT prolongation
Thioridizone
Antipsychotic that has the highest risk of seizures
clozapine
Antipsychotic that has the lowest seizure risk
quetiapine
Special dietary restriction with asenapine
no food or drink within 10-15 min
Dietary restriction with ziprasidone
must take with > 500 cal
Dietary restriction with lurasidone
must take with >300 cal
Antipsychotic medications that are both anti-manic and anti-depressive
quetiapine
lorasidone
olanzepine + fluoxitine
Order of increasing risk of mood switching for antidepressants used in bipolar disorder
bupropriod
AEDs used to treat bipolar disorder that are mainly anti-manic with slight anti-depressive effects
valproic acid
carbamazepine
oxcarbazepine
AED that is used in bipolar disorder that has mainly antidepressive effects
Lamotrigine
Treatment that tends to be the most effective for classic euphoric mania
Lithium
Treatment that tends to be the most effective for dysphoric mania
AEDs
What qualifies a HA as chronic
Occurs more days in a month than not
Best acute treatment for a cluster HA
100% O2 inhalation
Best treatment for an ice-pick HA (stabbing pain for a short period of time)
Indomethacin
Drug of choice for prophylactic treatment of tension type HAs
amitriptylline
MOA of triptans
5HT1B/1D receptor agonists
5 medications that are FDA approved for prophylaxis of migraines
valproic acid topiramate propranolol timolol anabotulinum toxin A
SGA that is a D2 receptor partial agonist
Aripiprazole
Classification when schizophrenia symptoms have lasted less than 6 months
Schizophreniform disorder
Antipsychotic that has superior efficacy in treating positive symptoms
Clozapine
Issue with tolcapone that limits its use
Increases risk of hepatic failure
Where melatonin is synthesized
pineal gland
AA precursor of melatonin
tryptophan
Excitatory dopamine receptors
Type 1 (D1 and D5)
Hoehn and Yahr Parkinson’s stage when movement dysfunction is bilateral and there are mild postural abnormalities
Stage III
MOA of ramelteon
M1 and M2 melatonin receptor agonist
Timing of melatonin therapy in delayed sleep phase sleep disorder
At dusk, about 5 hours before bedtime
Timing of melatonin therapy in advanced sleep phase disorder
dawn
Transtheoretical model of change stage that a patient is in when they are not yet ready to quit
Pre-contemplation
Location of the hypothalamus where histamine is produced
tuberomemmillary nucleus
TCA that is FDA approved for insomnia characterized by sleep maintenance issues
doxepin (silenor)
MOA of rotigotine transdermal patch
D1, D2 and D3 agonist
MOA of suvorexant
Orexin receptor (OX1 and OX2) antagonist
Transtheoretical model for change that patients are in when they are 6 or more months after their quit date and are now considered a former user
Maintenance
FDA approved medications for sleep maintenance
BZDs
Z-hypnotics
Silenor
Preferred class of sleep drugs in the elderly
Z-hypnotics
Peptide neurotransmitters implicated in wakefulness that are lost in patients with narcolepsy
Orexins A and B
3 sleep medications/classes that should not be taken with high fat meals due to decreased absorption
z-hypnotics
ramelteon
silenor
Transtheoretical model of change phase that patients are in when they are actively trying to quit and are still within 6 months of their quit date
Action
5 A’s for clinicians when dealing with substance abuse
Ask Advise Assess Assist Arrange
1st line sleep therapy in children
Non-drug therapy
The best established pathway for reinforcement
dopaminergic projection from the ventral tagmental are (VTA) to the nucleus accumbens
Timing of bright light therapy in delayed sleep phase type sleep disorder
30-60 min in the AM
Timing of melatonin therapy in delayed sleep phase sleep disorder
At dusk, about 5 hours before bedtime
FDA approved medications for sleep onset
BZDs
Z-hypnotics
Remelteon
Effect mediated by the mu opioid receptor
analgesia, sedation, inhibition of respiration and slowed GI transit
Effects mediated by the kappa opioid receptor
analgesia, dysphoria, slowed GI transit
G alpha receptor type for opioid receptors
Gi
MOA of morphine
mu-opioid receptor agonist
Inactive metabolite of morphine that has neuroexcitatory properties
morphine-3-glucuronide
Active metabolite of morphine that is more potent than the parent
Morphine-6-glucuronide
MOA of methadone
Mu and delta opioid receptor agonist, NMDA receptor antagonist, SNRI
MOA of fentanyl
mu-opioid receptor agonist
MOA of oxycodone
mu-opioid receptor agonist and kappa agonist
MOA of hydrocodone
mu-opioid receptor agonist
MOA of codeine
mu-opioid receptor agonist
MOA of tramadol
5HT/NE reuptake inhibitor and metabolite is a weak mu-opioid agonist
MOA of pentazocaine
partial mu-agonist and k-agonist
MOA of butorphanol
partial mu-agonist and kappa-agonist
MOA of nalbuphine
mu antagonist and kappa agonist
MOA of buphenorphine
partial mu agonist and possible k antagonist
The primary agent use for opioid overdose
naloxone
Effects mediated by the delta opioid receptor
analgesia
MOA of methylnaltrexone
peripherally acting mu-opioid receptor antagonist
FDA approved indication for methylnaltrexone
refractory opioid-induced constipation in patients with advanced illness receiving palliative care
2 effects of opioids that patients do not gain tolerance to
GI effects and pupillary constriction
MOA of aspirin
irreversible inhibition of COX via acetylation
Intrathercal spinal infusion of cone snail venom that is reserved for severe neuropathic pain and blocks presynaptic N-type Ca channels
Zoconitide
MOA of epinephrine that makes it useful when combined with local anesthetics
vasoconstrictor
Main MOA of local anesthetics
Block Na channel function
Alkaloid derived from plants of Solanaceae that activates TRPVI receptor of C fiber sensory neurons and then desensitizes it, depleting Substance P
Capsaicin
Normal processing of a stimulus
nociceptive
nociceptive pain due to damage to bone, muscle, ligament or skin
somatic
nociceptive pain due to damage to solid or hollow organs (liver, heart, spleen, kidney, GI tract)
Visceral
Abnormal processing on pain stimuli
neuropathic
Only FDA indication of lidocaine patches
Post herpetic neuralgia
The drug of choice for trigeminal neuralgia
Carbamazepine
MOA of ketamine, used for neuropathic pain
NMDA receptor antagonist
Opioid that is the most effective in neuropathic pain
methadone
4 1st line agents for neuropathic pain
TCAs
Gabapentin/pregabalin
lidocaine patch
SNRIs
NSAID that has the lowest CV risk
naproxen
Most common therapy given to patients experiencing opioid-inducted constipation
Senna + docusate
Opioid with the worst nausea SE
Codeine
2 Opioids that it is most common to have a true allergy to
codeine + morphine
2 drugs that are the most common options to switch to if a patient has a true allergy to morphine
fentanyl or methadone
Dose of naloxone that should be given to a patient with a respiratory rate of
0.04 mg (diluted) IVP over 15 sec q1-3min
Dose of naloxone that should be given to a patient in respiratory arrest
0.4-2 mg
Opioid that should specifically be avoided in renal disease
Morphine
4 pain medications that can contribute to serotonin toxicity
fentanyl, methadone, meperidine, tramadol
MOA of tapntadol
weak mu agonist and NE reuptake inhibitor
Active metabolite of hydrocodone
hydromorphone
MOA of meperidone
strong mu agonist and NMDA agonist
Neurotoxic metabolite of hydromorphone
H3G
Non-active, non–toxic CYP3A4 metabolite of oxycodone
noroxycodone
Active CYP2D6 metabolite of oxycodone
oxymorphone
Cut off for non-opioid naive patients
> 60mg/day MEQ for past 7 days
