Benzos, anxiolytics, and mood stabilizers Flashcards
1
Q
What two properties do benzodiazepines have?
A
anxiolytic and hypnotic
2
Q
What do anxiolytics do?
A
reduces anxiety with little effect on motor function and moderates excitement
3
Q
What do hypnotics do?
A
produces drowsiness and promotes the onset and maintenance of sleep
4
Q
What are the two major subtypes of GABA?
A
GABAa and GABAb
5
Q
How many subunits form a chloride channel and GABAa receptor?
A
5
6
Q
What receptors can benzodiazepines bind to?
A
alpha 1, 2, 3, 4, and 5
7
Q
Which alpha receptor controls sleep
A
1
8
Q
Which alpha receptors are responsible for anxiolytic, muscle relaxation?
A
2 and 3
9
Q
Which alpha receptor affects cognition?
A
5
10
Q
What is the MOA of benzodiazepines?
A
increase the frequency of Cl channel opening through allosteric modulation, allowing influx of chloride ions
11
Q
What are the adverse effects of benzodiazepines?
A
- dose-dependent CNS depression
- drowsiness, impaired judgment
- anterograde amnesia
- lethargy
- respiratory depression
12
Q
What are the most common side effects of typical use of benzos?
A
- sedation
- drowsiness
- memory difficulties
- fatigue
- muscle weakness
13
Q
What are the most common symptoms of benzo overdose?
A
- over-sedation
- confusion
- dysarthria
- diplopia
- ataxia
- lethargy
- dizziness
- difficulty breathing
14
Q
What are the contraindications for benzodiazepines?
A
- hypersensitivity
- acute narrow angle glaucoma
- sleep apnea
- respiratory insufficiency
- concomitant CNS depressants
- Hx of drug dependence
- abrupt withdrawal
- falls and mental alertness
15
Q
What are the withdrawal symptoms for benzos?
A
- anxiety
- agitation
- insomnia
- restlessness
- muscle tension
- irritability
16
Q
What is considered short term use of a benzo?
A
4-8 weeks
17
Q
How long should a patient taper off of short term benzo use?
A
1-2 months
18
Q
How long should a patient taper off of long term benzo use?
A
2-6 months
19
Q
How long should a patient taper off of extended benzo use?
A
2-3 months (10-25% q4wks)
20
Q
What is considered long term benzo use?
A
greater than 1 year
21
Q
Which benzo has a rapid onset and distribution half life?
A
diazepam
22
Q
Which benzo is highly lipophilic and crosses the BBB readily?
A
diazepam
23
Q
What benzo is the only pregnancy category X?
A
temazepam
24
Q
What is the MOA of buspirone?
A
5HT1A partial agonist and 5HT2 agonist, moderate dopamine antagonist
25
What is the onset of buspirone?
greater than 2 weeks (not a good prn drug)
26
What are the uses for buspirone?
GAD and off-label MDD (adjunct therapy)
27
What is the MOA of hydroxyzine?
histamine receptor antagonist
28
What are the approved uses of hydroxyzine?
pruritus and anxiety withdrawal symptoms in alcoholics
29
What are the off-label uses of hydroxyzine?
insomnia and anxiety
30
What is the onset of hydroxyzine?
15-20 minutes
31
What is one of the favorable factors of hydroxyzine?
no abuse liability
32
What are the adverse effects of hydroxyzine?
anticholinergic effects: sedation, dry mouth, and tremor
33
What is the black box warning on the mood stabilizers?
increased suicidality
34
Which mood stabilizer does not have the black box warning?
lithium
35
What is the MOA of lithium?
1) It's thought to alter cation transport across nerve and muscle cell membranes
2) influences reuptake of serotonin and/or norepinephrine
3) effect on second messenger systems
36
What is the CrCl cutoff of lithium?
< 50 mL/min
37
Since lithium is a NTI drug, when are drug levels taken?
8-12 hours post dose (trough)
38
What is the goal lithium level for acute depression?
0.6-1.0
39
What is the goal lithium level for maintenance/prophylaxis?
0.7-1.0
40
What is the goal lithium level for acute mania?
1.0-1.5
41
What is the drug level cut off for lithium toxicity?
> 1.5 with symptoms
42
What is more important in the management of lithium toxicity?
treating symptoms rather than drug levels
43
What should you do if a patient does not have symptoms of toxicity?
redraw level to make sure it was a trough
44
What are the mild symptoms of lithium toxicity (1.5-2.0)?
1. N/V
2. loose stools
3. lethargy
4. drowsiness
5. coarse hand tremor
6. muscular weakness
45
What are the moderate symptoms of lithium toxicity (2.1-2.5)?
1. severe N/V
2. diarrhea
3. confusion
4. dysarthria
5. nystagmus
6. ataxia
7. myoclonic twitches
46
What are the severe symptoms of lithium toxicity (> 2.5)?
1. severe N/V
2. diarrhea
3. impaired consciousness
4. increased deep tendon reflex
5. seizures
6. syncope
7. coma
47
What are the baseline labs needed before initiation of lithium?
1. BUN
2. SCr
3. TFT
4. ECG if > 40 yo
5. CBC
6. HCG (females)
48
What are the common side effects of lithium?
thirst, increased urination, tremor, weight gain
49
What are the dose related, transient, GI side effects of lithium?
N/V, anorexia, diarrhea, and abdominal pain
50
What are the common neuro/cognitive side effects of lithium?
lethargy, fatigue, weakness, and cognitive slowing
51
What are the other side effects of lithium?
hypothyroidism, arrhythmias, acne, psoriasis, increased WBCs, and weight gain
52
What drugs can increase lithium levels?
NSAID, ACE/ARB, CCBs, and thiazides
53
What drugs can decrease lithium levels?
loop diuretics and caffeine
54
What are the symptoms of lithium toxicity?
coarse tremor, ataxia, confusion, and visual changes
55
What are the severe symptoms of lithium toxicity?
seizures, delirium, coma, and death
56
What is the MOA of valproate?
It is a voltage-sensitive sodium channel antagonist
57
No matter the formulation of valproic acid, what does it circulate in the body as?
valproate sodium
58
When do you draw a valproate trough level?
1 hour prior to the next dose
59
What drug specifically makes it difficult to achieve therapeutic VPA levels?
carbamazepine
60
What are the monitoring parameters for VPA?
CBC w/ diff, LFTs, BUN/SCr, TDM, weight, electrolytes, ammonia, prothrombin time, bone marrow suppression, and HCG if suspicion of pregnancy
61
What are the common side effects of VPA?
N/V, anorexia, heartburn, thrombocytopenia, LFT increases, liver impairment, sedation, dizziness, headache, tremor, ataxia, weakness, hair loss, and weight gain
62
What is the MOA of carbamazepine and oxcarbazepine?
inhibits voltage-sensitive sodium channels
63
Why do carbamazepine and oxcarbazepine have so many drug interactions?
both agents are inducers of CYP3A4
64
What other enzymes does carbamazepine induce?
1A2, 2C9, 2C19, 2C8, and PGP
65
What unique metabolism characteristic does carbamazepine have that isn't seen with oxcarbazepine?
It auto-induces its own metabolism
66
What are the NTI drugs?
carbamazepine, oxcarbazepine, and lithium
67
What are the renal adjustments for carbamazepine?
avoid if CrCl is less than 60 mL/min
68
What are the renal adjustments for oxcarbazepine?
start with 300mg QD instead of BID if CrCl is less than 30 mL/min
69
What monitoring is crucial in the 1st 3 months with carbamazepine and oxcarbazepine?
Chem 7
70
What monitoring is needed for carbamazepine and oxcarbazepine?
CBC w/ diff (not for oxcarbazepine), ECG, LFT, TFT, BUN/SCr, TDM, weight, electrolytes, rash development, and HCG if suspicion of pregnancy
71
What allele requires testing due to serious skin reactions?
HLA-B*1502
72
What are the side effects of carbamazepine and oxcarbazepine?
GI upsets, aplastic anemia, LFT elevations, hyponatremia, and reduced efficacy of contraceptives
73
What are the main differences between oxcarbazepine and carbamazepine?
less sedating, less bone marrow toxicity, fewer CYP3A4 interactions, and no auto-induction
74
What is the MOA of lamotrigine?
inhibits voltage-sensitive sodium channels
75
What is the interaction between lamotrigine and oral contraceptives?
estrogen contraceptives can reduce lamotrigine levels
76
What is the dosing regimen of lamotrigine for bipolar disorder?
titrated slowly to avoid skin rash (SJS). 25 mg daily x 2 weeks, then 50 mg daily x 2 weeks, the 100 mg daily x 1 week, then 200 mg/day
77
What should you do to the dose of lamotrigine in the presence of valproic acid or any other substance that induces glucuronidation?
double the dosing schedule
78
What is the most severe side effect of lamotrigine that is seen in about 10% of patients?
Stevens Johnson syndrome
79
What is the MOA of topiramate?
It interferes with both calcium and sodium channels, enhances GABA, and reduces glutamate function
80
What is topiramate used for?
adjunct in bipolar (not studied enough for monotherapy as a mood stabilizer)
81
What are the side effects of topiramate?
Dizziness, ataxia, somnolence, psychomotor slowing, memory difficulties, fatigue, decreased concentration, and confusion
82
What is the MOA of pregabalin and gabapentin?
alpha-2-delta ligands that binds to the alpha-2-delta subunit of voltage sensitive calcium channels
83
What can pregabalin be used for in psych?
anxiety
84
What are the side effects of pregabalin?
dizziness and cognitive impairment
85
What is gabapentin used for in psych?
off-label for anxiety
86
What are the side effects of gabapentin?
dizziness, drowsiness, ataxia, fatigue, and edema
87
What is the biggest therapeutic consideration for gabapentin?
renal dose adjustments
88
What is the MOA of levetiracetam?
inhibition of N-type calcium channels, potassium channel blockade, GABAergic actions
89
What are the major side effects of levetiracetam?
behavioral symptoms, somnolence, headache, and hostility
