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Psych Drugs Flashcards

1
Q

Typical antipsychotics

A

Dopamine-2 receptor antagonists

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2
Q

Atypical antipsychotics

A

Serotonin-dopamine antagonists

D2 partial agonists

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3
Q

Indications of typicals

A 
Psychotic disorders
Mood disorders
Dementia
Psychosis secondary to medical conditions, medications, and drugs of abuse
Personality disorder
Obsessive-compulsive disorder
Autism
Tourette’s disorder
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4
Q

dopamine-mediated effects: nigrostriatal pathway

A

EPS (Parkinsonism, Akathisia, Dystonic reactions, Tardive dyskinesia, NMS)

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5
Q

dopamine-mediated effects: mesolimbic pathway

A

dysphoria

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6
Q

dopamine-mediated effects: mesocortical pathway

A

worsening negative and cognitive symptoms

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7
Q

dopamine-mediated effects: tuberoinfundibular pathway

A

Hyperprolactinemia, and resultant galactorrhea, amenorrhea, sexual dysfunction

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8
Q

acute EPS

A

Dystonia – usually within hours
Akathisia – usually within days
Parkinsonism – usually within days to weeks

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9
Q

chronic/late set EPS

A

Tardive Dyskinesia usually after 3 months

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10
Q

treatment of dystonia (EPS)

A

Anticholinergics – injectable if needed

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11
Q

treatment of akathisia

A

beta blockers, anticholinergics

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12
Q

treatment of parkinsonism

A

anticholinergics, amantadine

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13
Q

Dopamine does what to ACh

A

suppresses

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14
Q

Dopamine blockade ___ ACh

A

increases

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15
Q

EPS caused by

A

decreased dopamine and increased ACh

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16
Q

improvement of EPS by

A

anticholinergics

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17
Q

mechanism of tardive dyskinesia

A

blockade of receptors in nigrostriatal dopamine pathway causes up-regulation, increased ACh

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18
Q

increased risk of TD w/

A

age > 50
dose
total exposure
mood disorder

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19
Q

anticholinergic side effects (M1)

A

constipation, blurred vision, dry mouth, drowsiness

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20
Q

antihistaminergic side effects (H1)

A

weight gain, drowsiness

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21
Q

anti-alpha adrenergic side effects

A

dizziness, decreased BP, drowsiness

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22
Q

neuroleptic malignant syndrome

A

life-threatening condition of
hyperpyrexia, autonomic instability, muscle rigidity, and delirium
Death occurs secondary to arrhythmia, rhabdomyolysis or respiratory failure
Discontinue the antipsychotic, aggressive hydration
Mortality rate of 20-30%

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23
Q

how to increase compliance

A

depot preparations

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24
Q

why was clozapine originally withdrawn

A

agranulocytosis

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25
benefits of clozapine
Much lower incidence of extrapyramidal symptoms and tardive dyskinesia Improves negative and cognitive symptoms
26
indications of clozapine
Treatment resistant schizophrenia Schizophrenia with tardive dyskinesia Schizophrenia or schizoaffective disorder with recurrent suicidal behavior
27
agranulocytosis
Life-threatening drop in white blood count Contraindicated with pre-existing blood disorder Estimated at 1-2%, about 0.38% with monitoring Requires continuous monitoring
28
adverse effects of atypicals
Sedation Anticholinergic side effects, including dry mouth, constipation, blurry vision, urinary retention, confusion, ECG changes Myocarditis Orthostatic hypotension Weight gain, which can be substantial Hypersalivation Seizures, especially with high doses or fast titrations Metabolic problems, including diabetes and hyperlipidemias
29
benefits of atypicals
Cause fewer EPS, little-to-no TD Improve positive symptoms Improve negative and cognitive symptoms
30
blocking 5HT2A receptor
disinhibits DA release and reduces D2 blockade
31
indications of atypical anatipsychotics
``` Psychotic disorders Mood disorders ? Dementia Psychosis secondary to medical conditions, medications, and drugs of abuse Personality disorder Obsessive-compulsive disorder Autism Tourette’s disorder **Mania ```
32
atypical agents
- pine - zine - done (risperidone)
33
aripiprazole
D2 partial agonist
34
metabolic side effects of atypicals
``` weight gain hyperlipidemia hyperglycemia diabetes ketoacidosis ```
35
metabolic syndrome (Syndrome X)
central obesity high PB high triglycerides low HDL-cholesterol insulin resistance
36
CATIE trial
atypicals vs. perphenazine. found to be equally effective olanzapine more efficacious but worst for weight gain
37
mania symptoms
Inflated self-esteem or grandiosity Decreased need for sleep More talkative than usual or pressure to keep talking Flight of ideas or subjective experience that thoughts are racing Attention is easily drawn to unimportant or irrelevant items Increase in goal-directed activity (either socially, at work or school, or sexually) or psychomotor agitation Excessive involvement in pleasurable activities that have a high potential for painful consequences (e.g., engaging in unrestrained buying sprees, sexual indiscretions, or foolish business investments)
38
depression symptoms
Depressed mood most of the day, nearly every day, Markedly diminished interest or pleasure in all, or almost all, activities most of the day Significant weight loss when not dieting or weight gain or decrease or increase in appetite Insomnia or hypersomnia Psychomotor agitation or retardation Fatigue or loss of energy Feelings of worthlessness or excessive or inappropriate guilt Diminished ability to think or concentrate, or indecisiveness Recurrent thoughts of death, recurrent suicidal ideation without a specific plan, or a suicide attempt or a specific plan for committing suicide
39
Definition of Mood stabilizer
efficacy in at least one of the three phases of bipolar disorder (acute mania, acute depression, or prophylaxis), AND it should not cause affective switch to the opposite mood state nor should it worsen the acute episode.
40
Indications for mood stabilizers
``` Bipolar Disorder: Mania/Hypomania, Depression, Prophylaxis, Cyclothymia Depression Augmentation Schizoaffective Disorders Borderline Personality Disorder Intermittent Explosive Disorder Post-Traumatic Stress Disorder Neuropathic Pain Alcohol Detoxification Refractory Schizophrenia ```
41
Lithium formulations
Li2CO3 LiCl LiCitrate
42
Lithium mechanism
Thought to involve modulation of second messenger systems, particularly in phosphatidyl inositol system Alteration of G proteins, signal tranduction Alteration downstream enzymes Regulation of gene expression
43
Lithium first-line indications
Classic euphoric mania Pure bipolar depression Bipolar maintenance
44
Lithium second-line indications
Mixed mania | Rapid cycling
45
Lithium adverse effects
``` GI abdominal cramps, nausea, vomiting, diarrhea Neurologic cognitive dulling, decreased creativity tremor decreased memory and concentration Metabolic weight gain increased thirst and urination Dermatologic Psoriasis, acne Benign leukocytosis ```
46
Lithium: medically serious side effects
``` Hypothyroidism Renal polyuria and polydipsia (nephrogenic diabetes insipidus Nephrotoxicity (long-term) Cardiac arrhythmias Teratogenicity: Ebstein’s anomaly Overdose ```
47
Lithium therapeutic levels
0.8-1.2 mEq/L
48
Lithium Toxicity
1.5 + mEq/L
49
lithium management issues
requires blood monitoring | significant drug-drug interactions
50
lithium interactions
NSAIDs Thiazide diuretics ACE Inhibitors Calcium channel blockers
51
valproic acid proposed mechanism
Proposed: Inhibition of Na+/Ca++ channels, thereby boosting GABA inhibition and decreasing glutamatergic excitation
52
valproic acid first-line indications
Mixed (dysphoric) mania | Rapid cycling
53
valproic acid second-line indications
Pure depressive states | Classic euphoric mania
54
valproic acid adverse effects
``` Dyspepsia and diarrhea Sedation Dizziness Increased appetite and weight gain Tremor Edema Neurotoxicity (cognitive blunting, ataxia) Hair loss ```
55
valproic acid serious adverse effects
``` Thrombocytopenia Hepatotoxicity Pancreatitis Polycystic Ovarian Syndrome? Teratogenicity: Neural tube defects Overdose ```
56
carbamazepine mechanism
Proposed: Effects at Na+/K+ channels, enhancement of GABA inhibition
57
carbamazepine indications
bipolar disorder: mixed mania, rapid cycling
58
carbamazepine indications
``` Nausea, anorexia, vomiting Sedation Dizziness Cognitive dulling Electrolyte abnormalities Anticholinergic effects ```
59
carbamazepine =
tegretol
60
carbamazepine medically serious side effects
Hematologic (thrombocytopenia, agranulocytosis, aplastic anemia) Hepatotoxicity Allergic reactions, rash Teratogenicity: Neural tube defects, craniofacial abnormalities Overdose
61
oxcarbazepine description
Metabolite of carbamazepine Fewer drug-drug interactions, toxicities as compared to carbamazepine Does not require therapeutic blood monitoring
62
Lamotrigine =
lamictal
63
lamotrigine mechanism
Inhibits Na+, glutamate
64
lamotrigine indication
maintenance (FDA), depression
65
lamotrigine adverse effects
Nausea, vomiting, diarrhea Sedation, lightheadness, tremor Cognitive blunting Weight gain less of an issue than with the others
66
lamotrigine serious adverse effects
Rash, common, 8-10%, usually benign but can progress to.. Stevens-Johnson Syndrome, 0.08%, potentially life threatening rash that can lead affect multiple organs
67
Stevens-Johnson rash management
Rapid increases in dose correlated with rash Careful titration Hold drug, at sign of serious rash Watch for drug interactions
68
gabapentin =
neurontin
69
gabapentin description
Mechanism: Unclear; GABA analogue, decreases glutamate Not effective as monotherapy Has anxiolytic, analgesic properties Well tolerated
70
topiramate =
topamax
71
topiramate description
Mechanism: Unclear; Inhibits Na+ and Ca++ channels, inhibits glutamate and enhances GABA Not effective as monotherapy Has weight loss effects Significant sedation, cognitive dulling
72
other bipolar agents
``` Atypical Antipsychotics Typical Antipsychotics Omega 3 Fatty Acids? Calcium Channel Blockers? Benzodiazepines ```
73
TCA actions
antagonism at 5HT and NE presynaptic reuptake pumps
74
why are TCA's dirty?
also block muscarinic, alpha-adrenergic, and histamine receptors
75
how long do TCA's take to work?
3-4 weeks
76
are TCA's lethal in overdose?
yes
77
amitriptyline (elavil)
TCA- for pain, headache, insomnia
78
clomipramine (anafranil)
highly serotonergic TCA | indicated for OCD
79
nortriptyline (Pamelor)
``` demethylated imipramine (secondary amine) least orthostasis of TCA's ```
80
indications for TCA's
``` major depressive disorder bipolar depression dysthymia panic disorder generalized anxiety disorder OCD pain disorder ```
81
contraindications for TCA's
cardiac conduction delays | arrhythmias
82
adverse effects of TCA's
``` anticholinergic sedation weight gain orthostatic hypotension sexual dysfunction mania (bipolar) seizures ``` serious: cardiotoxicity neurotoxicity
83
MAOI mechanism
irreversible monoamine oxidase inhibitors | disables monoamine degradation
84
which MAO blockage is necessary for antidepressant effect?
MAO A
85
do MAOIs block any other receptors?
alpha 1 adrenergic receptors | histamine receptors
86
serious adverse effects of MAOIs
tyramine-induced hypertensive crisis
87
SSRI's mechanism
selective antagonism at 5HT reuptake pumps
88
when do SSRI's take effect?
3-4 weeks of administration
89
SSRI major plus
well tolerated, widely indicated
90
SSRI contraindications
co-administration w/ MAOI's
91
serotonin syndrome
associated w/ hyperthermia, myoclonus, autonomic instability, rigidity, coma, death need MAOI washout of 2 weeks prior to SSRI treatment
92
serotonergic side effects- 5HT3
GI system: diarrhea, nausea, vomiting
93
serotonergic side effects- 5HT2C
CNS: anxiety and mental agitation
94
serotonergic side effects- 5HT2A
CNS: akathisia, insomnia, myoclonus, sexual dysfunction
95
serotonin discontinuation syndrome
headache, dizziness, irritability, fatigue | upon abrupt discontinuation
96
SNRI mechanism
selective antagonism at NE and 5HT presynaptic reuptake pumps
97
curvilinear dose response of SNRI
additional dopamine reuptake inhibition at higher dosages
98
SNRI contraindications
co-administration w/ MAOIs
99
SNRI indications
major depressive disorder generalized anxiety disorder panic disorder generalized social phobia
100
NaSSAs mechanism
dual mechanism of action antagonism at central alpha-2 autoreceptors (disinhibition of NE and 5HT release) stimulation of alpha-1 somatodendritic receptors on serotonin neurons, boosting 5HT release
101
NaSSA agent
mirtazapine (Remeron)
102
indications of NaSSA
major depressive disorder
103
serious NaSSA adverse effect
agranulocytosis and other blood dyscrasias
104
SARIs mechanism
selective antagonism at 5HT presynaptic reuptake pumps w/ simultaneous 5HT2A blockade
105
SARI indications
major depressive disorder | dysthymia
106
trazodone (type, adverse effect)
SARI | priapism (rare)
107
nefazodone (type, adverse effect)
SARI | liver toxicity
108
bupropion (wellbutrin, zyban)- type
noradrenergic and dopaminergic reuptake inhibitor
109
bupropion indications
``` major depressive disorder dysthymia bipolar depression ADHD smoking cessation ```
110
bupropion contraindications
co-administration w/ MAOI's anorexia nervosa bulimia nervosa seizure disorder
111
bupropion adverse effects
``` activation insomnia nausea tremor seizures at higher doses ```
112
benzodiazepines action
increased frequency of GABA receptor open- hyper polarizes cell by Cl influx
113
why are benzo's used in detoxification in sedative and alcohol addiction?
they are cross tolerant with alcohol and barbiturates
114
which benzo's don't undergo Phase II glucuronidation
lorazepam oxazepam temazepam
115
alprazolam (Xanax)
perhaps greater addictive potential, but very effective for panic
116
lorazepam (ativan)
available in PO, IM, and IV forms | widely used
117
clonezepam (kloponin)
long half life, most potent
118
diazepam (valium)
fast onset but w/ active metabolite
119
chlordiazepoxide (librium)
used for alcohol detox
120
how to counteract benzo overdose
flumazenil
121
nonbenzodiazepine anxiolytics
various forms and mechanisms, generally non-addictive
122
buspirone
5HT1A agonist, effective in anxiety no sedationor addictive potential of benzos
123
benzo withdrawal toxicity
potentially lethal anxiety, insomnia, restlessness, agitation, irritability, muscle tension
124
nonbenzodiazepine hypnotics
indicated for insomnia
125
ramelteon (rozerem)
agonist at melatonin receptors, thought to normalize circadian rhythms

Neuro (15 decks)

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