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Essentials 1.3 Drugs > Week 3 > Flashcards

Week 3 Flashcards

Sedatives, hypnotics, anxiolytics, mood stabilizers, and antidepressants (127 cards)

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1
Q

Which barbiturates increase duration of GABA-gated chloride channel opening?

A

Phenobarbital and pentoarbital

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2
Q

What is the clinical use for Phenobarbital and Pentoarbital?

A

Anxiety and anesthesia

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3
Q

What are common side effects of Phenobarbital and Pentoarbital?

A

Depression of CNS activity: sedation/hypnosis, dizziness, ataxia, paradoxical hyperactivity (kids), headache, unsteadiness, nausea, blood dyscrasias, rash, mood change.

More likely to cause dependence than benzodiazepines.

Overdose can be lethal.

Can have drug-drug interaction between CYP inducer

Additive CNS depression with ethanol and other CNS depressants

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4
Q

What benzodiazepines (BZD) enhance GABA’ effects without directly activating GABA by increasing the frequency of Cl-channel opening?

A

Midazolam, Alprazolam, Lorazepam, Clonazepam

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5
Q

What is the clinical uses of benzodiazepines (BZD) like Midazolam, Alprazolam, Lorazepam, and Clonazepam?

A

Anxiety, Insomnia, Sedation.

Chlordiazepoxide: Alcohol withdrawal.

Diazepam and Lorazepam=epilepsy/seizure. REM Sleep Disorder.

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6
Q

What are the side effects of Midazolam, Alprazolam, Lorazepam, and Clonazepam?

A

CNS Depression: low doses=drowsiness, impaired judgment, diminished motor skills, poor driving ability, decreased concentration, cognitive deficits, impaired memory, dose-related anterograde amnesia.

High doses: toxicity may present as lethargy, exhaustion, or equivalent to ethanol intoxication.

Rebound insomnia after discontinuation.

Tolerance as a hypnotic develops in 2-4 weeks; higher doses are often needed over time.

Dependence can develop (seizures may occur in withdrawal); always taper patients off of benzodiazepines.

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7
Q

Which drug is benzodiazepine antagonist that is given by IV and has a short duration of action (20-30min)?

A

Flumazenil

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8
Q

What is the clinical use of Flumazenil?

A

Reverses sedative actions of benzodiazepines, used in overdose (can precipitate withdrawal)

Unpredictable antagonism of respiratory depression

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9
Q

Which drugs are benzodiazepines partial agonists that bind to the BZD receptor on alpha-1 subunit of GABA receptor which decreases latency to persistent sleep?

A

Zolpidem, Zaleplon, Eszopiclone

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10
Q

What is the clinical use of Zolpidem, Zaleplon, Eszopiclone?

A

Insomnia

Lower doses for elderly and females (zolpidem)

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11
Q

Which antiepileptic blocks sodium channels to reduce post-tetanic potentiation (the increase in neurotransmitter release which results from a stream of high frequency action potentials–key to the spread of many seizures).

A

Phenytoin

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12
Q

What is the clinical use of Phenytoin?

A

Focal and generalized seizures, prophylaxis after neurosurgical procedures, status epilepticus that do not respond to benzodiazepines.

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13
Q

What are the common side effects of Phenytoin?

A

Gum hyperplasia, coarsening facial features, hirsutism
(Most important to remember)

Can exacerbate absence seizures and myoclonus.

Cerebellar degeneration->ataxia, nystagmus, drowsiness, lethargy, rash, headaches, N/V, bone marrow hypoplasia, vitamin K and folate deficiency, and osteoporosis.

Metabolized by CYP-450 in the liver. Strong inducer of hepatic enzymes; alters the metabolism of other drugs.

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14
Q

Which antiepileptic is a phenytoin prodrug that is administered parenteral?

A

Fosphenytoin sodium

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15
Q

What is the clinical use of Fosphenytoin Sodium?

A

status epilepticus loading dose for phenytoin

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16
Q

What are the side effects of Fosphenytoin Sodium?

A

Better tolerated than parenteereal phenytoin, fewer CV side effects, including less hypotension.

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17
Q

Which antiepileptic blocks sodium channels and induces its own metabolism without dose increase (metabolized in the liver)?

A

Carbamazepine

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18
Q

What is the clinical use of Carbamazepine?

A

Focal epilepsies, generalized tonic-clonic seizures.

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19
Q

What are the side effects of Carbamazepine?

A

Hyponatremia, leukopenia, rare aplastic anemia, hepatitis, Stevens-Johnson (rare)

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20
Q

What barbiturate acts on GABA-A binding site to prolong the duration of Calcium channel opening?

A

Phenobarbital

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21
Q

What is Phenobarbital clinically used for?

A

Focal-onset, generalized seizures, and neonatal seizures.

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22
Q

What are side effects of phenobarbital?

A

Sedation, Dupuytren’s contractures, rebound seizures with rapid tapering.

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23
Q

Which antiepileptic enhances GABA function and is used in primary generalized epilepsies?

A

Valproic Acid

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24
Q

What is Valproic Acid used clinically?

A

Primary generalized epilepsies: juvenile myoclonic epilepsy, absence epilepsy, photosensitive epilepsy, Lennox-Gastaut Syndrome.

2nd line treatment in epileptic spasms, can be used in high doses to treat focal epilepsy.

Parenteral form (depacon) can treat status epilepticus

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25
What are the side effects of Valproic Acid?
Risk of Stevens-Johnson Syndrome recurrence. Tremor, weight gain, alopecia, thrombocytopenia, PCOS. Rare: hepatitis, pancreatitis, risk of teratogenesis and neural tube defects.
26
Which antiepileptic drug blocks T-type Calcium channels to treat typical absence epilepsy only?
Ethosuximide
27
What are the side effects of Ethosuximide?
Dyspepsia, nausea, loss of appetite, tiredness.
28
Which antiepileptic drug enhances glutamic acid decarboxylase (GAD) to increase levels of GABA?
Gabapentin
29
What is the clinical use of Gabapentin?
Focal seizures with or without secondary generalization.
30
What are some important pharmacokinetics of Gabapentin that may be important to address with patients?
Excreted unchanged by the kidneys; adjust dose in renal disease.
31
Which antiepileptic drug is a sodium channel blockage that inhibits release of glutamate?
Lamotrigine
32
What is Lamotrigine clinically used for?
Broad spectrum: adjunctive treatment of focal-onset seizures with or without secondary generealization, crossover to monotherapy, Lennox-Gastaut syndrome, atypical absence, tonic/atonic seizures, and myoclonic seizures. Preferred for elderly and pregnant patients.
33
What are the side effects of Lamotrigine?
Stevens-Johnson Syndrome. Tremor, insomnia, headaches, ataxia, somnolence. Levels increase significantly with coadministration of valproate.
34
Which antiepileptic drugs binds synaptic vesicle protein 2A-SV2A?
Levetiracetam
35
What is the clinical use of Levetiracetam?
Broad spectrum: adjunctive treatment of primary generalized tonic-clonic seizures in adults and children (6 y/o+) with idiopathic generealized epilepsy, adjunctive tx of focal onset seizures in adults and kids (4 y/o+), and adjunctive treatment of myoclonic seizures in adults and kids (12 y/o+). Off-label use includes prophylaxis in patients after TBI and in status epilepticus.
36
What are side effects of Levetiracetam?
Behavioral changes (avoid in pts with psychiatric conditions), somnolence, asthenia, headache, dizziness, flu-like symptoms. Safe for elderly and pregnant pts. No effect on metabolism of other drugs. Dose-adjust in pts with renal disease and after hemodialysis.
37
Which antiepileptic drugs is an analogue of carbamazepine that is usually better tolerated?
Oxcarbazepine
38
What is the clinical use of Oxcarbazepine?
Monotherapy or adjunct therapy in focal epilepsies in adults and as monotherapy in tx of focal epilepsies in children 4y+, adjunctive in kids 2y+.
39
What are the side effects of Oxcarbazepine?
May exacerbate myoclonic seizures and absence seizures. Hyponatremia in elderly. Dizziness, fatigue, headache. Interacts with oral contraceptives, reducing its efficacy.
40
Which antiepileptic drug inhibits sodium conductance and (weakly) inhibits carbonic anhydrase, blocks the AMPA glutamate receptor, and enhances GABA?
Topiramate
41
What is the clinical use of Topiramate?
Broad spectrum: Tx of focal-onset seizures, tx of primary generalized epilepsy as an add-on, tx of Lennox-Gastaut syndrome.
42
What are the side effects of Topiramate?
Word finding difficulties, weight loss (decreased appetite), paresthesias in fingers and mouth, kidney stones, anhidrosis, acute myopia in close-angle glaucoma, ataxia, and tiredness. Dose adjustments in pts with renal failure. Enzyme inducers (like phenytoin) decrease levels of topiramate by 50%. Topiramate reduces the levels of oral contraceptives, decreasing their effectiveness.
43
Which antiepileptic drugs is a sodium channel blockade (major) and also works on T-type calcium channels and weakly inhibits carbonic anhydrase?
Zonisamide
44
What is the clinical use of Zonisamide?
Broad spectrum: tx of focal epilsepsy with or without secondary generalization. Tx of myoclonus and absence seizures.
45
What are the side effects of Zonisamide?
Anorexia, headache, mental slowing, confusion, ataxia, dizziness, kidney stones, oligohidrosis, paresthesias (due to carbonic anhydrase inhibition) Similar structure to sulfonamides-contraindicated in pts with sulfonamide abx allergies. Long half life allows one-per-day dosing. Half-life decreased by enzyme inducers and valproate.
46
Which antiepileptic drug irreversibly binds GABA-T which increases GABA concentrations in the brain?
Vigabatrin
47
What are the clinical uses of Vigabatrin?
Epileptic spasms in tuberous sclerosis, refractory focal-onset epilepsies
48
What are the side effects of Vigabatrin?
May exacerbate myoclonic seizures and absence seizures, may cause status epilepticus in pts with absence seizures or primary generalized epilepsy. Other side effects: visual field defects (nasal constriction and concentric constriction with preserved central vision) which may be irreversible, fatigue, dizziness, headache, tremor, and double vision.
49
What antiepileptic drug enhances the slow inactivation of voltage-gated sodium channels?
Lacosamide
50
What is the clinical use of Lacosamide?
Adjunt tx and monotherapy tx of focal onset epilepsies. Off label use: status epilepticus in the ICU. IV use available
51
What are the side effects of Lacosamide
cardiac conduction abnormalities
52
Which benzodiazepine/antiepileptic drug binds GABA-A receptors?
Clobazam
53
What is the clinical use of Clobazam?
Adjunct tx of Lennox-Gastaut syndrome, tx of primary or focal seizures with secondary generalized seizures, and in catamenial epilepsy.
54
What are the side effects of Clobazam?
Sedation, dizziness, ataxia, weakness.
55
Which antiepileptic drug is a phytocannabinoid that treats Draven Syndrome?
Cannabidiol (CBD oil)
56
Which mood stabilizers involve the inositol pathway to increase 5-HT synthesis and decrease NE release?
Lithium, Lithium Carbonate, Lithium Carbonate slow release, and Lithium Citrate
57
What is the clinical use of Lithium, Lithium Carbonate, Lithium Carbonate slow release, and Lithium Citrate?
Acute and maintenance of bipolar PO (Lithium carbonate) Liquid (lithium Citrate) Off label: Augmentation of MDD
58
What are the side effects of Lithium, Lithium Carbonate, Lithium Carbonate slow release, and Lithium Citrate?
Tremor, polydipsia, polyuria, acne, metallic taste, rash Renal Excretion Can induce Serotonin Syndrome Lithium levels increase with: NSAIDS, ACE-inhibitors, HCTZ, Dehyration Hypothyroidism Renal injury Ebstein Anomaly in pregnancy Black Box Warning: Lithium toxicity: tremor, ataxia, confusion, GI
59
What are contraindications for Lithium, Lithium Carbonate, Lithium Carbonate slow release, and Lithium Citrate?
renal failure, dehydration, hyponatremia
60
What do you monitor when patients are on Lithium, Lithium Carbonate, Lithium Carbonate slow release, or Lithium Citrate?
Narrow TI: Acute: 0.8-1.2 mEq/L Maintenance: 0.5-0.7 mEq/L Thyroid function (TSH, fT4) Kidney function (BUN/Cr)
61
Which mood stabilizers have multiple MOAs including voltage-gated sodium channel inhibition and effects on GABA?
Valproic Acid, Divalproex sodium, and Sodium Valproate
62
What is the clinical use of Valproic Acid, Divalproex sodium, and Sodium Valproate?
Acute and maintenance of bipolar Epilepsy Migraine prophylaxis Impulsivity Agitation in Traumatic Brain injury Can be taking PO, IV, or Sprinkles
63
What are the side effects of Valproic Acid, Divalproex sodium, and Sodium Valproate?
Sedation Weight gain CYP inhibitor Strongly bound to plasma albumin Can cause PCOS Black Box Warnings: hepatotoxicity, pancreatitis, teratogenicity Generally don’t prescribe to women of reproductive age
64
What are the contraindications of Valproic Acid, Divalproex sodium, and Sodium Valproate?
hepatic impairment, urea cycle and mitochondrial disorders, pregnancy
65
What would you monitor for a patient on Valproic Acid, Divalproex sodium, or Sodium Valproate
Levels (mania): 50-125 mcg/mL Liver function (LFTs)
66
Which mood stabilizer has multiple MOAs including voltage-gated calcium channel inhibition and 5-HT release?
Carbamazepine
67
What is the clinical use of Carbamazepine?
Maintenance bipolar Epilepsy Trigeminal Neuralgia PO or liquid
68
What are the side effects of Carbamazepine?
Sedation, dizziness, constipation, dry mouth Powerful CYP3A4 inducer – induces its own metabolism CBZ decreases levels of many CYP3A4 substrates such as OCPs Black Box Warnings: Bone marrow suppression, Stevens-Johnson syndrome (SJS), Toxic Epidermal Necrolysis (TEN)
69
What are the contraindications of Carbamazepine?
hepatic impairment, urea cycle and mitochondrial disorders, pregnancy
70
What would you monitor for a patient on Carbamazepine?
Blood count (CBC) Liver function (LFTs)
71
Which mood stabilizer has multiple MOAs including voltage-gated calcium channel inhibition and 5-HT release?
Lamotrigine
72
What is the clinical use of Lamotrigine?
Maintenance bipolar Epilepsy PO
73
What are the side effects of Lamotrigine?
Dizziness, headache, GI, rash Inactivated by hepatic glucuronidation Black Box Warning: Stevens-Johnson Syndrome with rapid dose changes
74
What is the MOA of 2nd-generation (atypical ) antipsychotics?
* DA- and 5-HT antagonism
75
What is the clinical use of 2nd-generation (atypical) antipsychotics?
Acute and maintenance bipolar, psychotic disorders
76
What are the side effects of 2nd-generation (atypical) antipsychotics?
Metabolic Weight Gain EPS
77
What is the acute treatment of manic episodes?
Antipsychotics (quickest-acting) Lithium or valproate (take days-weeks)
78
What medications should be considered for maintenance and/or prevention of manic episodes?
lithium, valproate, carbamazepine, lamotrigine (often, several agents needed)
79
Why must you use caution when using antidepressants as mood stabilizers?
They can precipitate mania
80
What medication should you consider for pregnant patients who are having manic episodes?
When prescribing in pregnancy, lamotrigine is considered lowest risk. Must consider and balance risk of teratogenicity with risks associated with manic episode.
81
What is the MOA of SSRIs?
nhibit presynaptic reuptake of 5-HT
82
What do SSRIs commonly treat?
Depressive and Anxiety disorders
83
What are some side effects of SSRIs?
Serotonergic: GI (nausea, diarrhea), sleep disturbance, sexual dysfunction, easy bruising Most also have some mild anticholinergic effects (dry mouth) Toxicity: Serotonin Syndrome
84
Which SSRI is the most activating, has a long half life, and is FDA-approved for depression in teens?
Fluoxetine (PO)
85
Which SSRI tends to have more GI side effects and is usually taking PO or as a liquid?
Sertaline
86
Which SSRI can cause QT prolongation at doses >40 mg which means patients should have regular EKGs to monitor doses above 40 mg?
Citalopram
87
Which SSRI is a S-isomer of citalopram, is taking PO, and is FDA approved for depression in teens?
Escitalopram
88
Which SSRI has a short half life leading to higher risk of discontinuation syndrome and is considered the most sedating SSRI?
Paroxetine (PO)
89
Which SSRI inhibits several CYP enzymes leading to a lot of drug-drug interaction and can also be used to treat OCD?
Fluvoxamine (PO)
90
Which SSRI is taken PO and can cause hyponatremia?
Vortioxetine
91
Which SSRI is a SSRI+5HT1A partial agonism that is taking PO?
Vilazodone
92
What is the MOA of SNRIs?
Inhibit presynaptic reuptake of 5-HT and NE
93
What is the clinical use of SNRIs?
Depressive and Anxiety disorders, Chronic pain syndromes
94
What are the side effects of SNRIs?
Serotonergic Side Effects: GI (nausea, diarrhea), sleep disturbance, sexual dysfunction Noradrenergic Side Effects (higher doses): HTN, jitteriness Most also have some mild anticholinergic effects (dry mouth) Toxicity: Serotonin Syndrome
95
Which SNRI has a short half life and can either be taking twice a day or using an extended release form to allow for daily dosing?
Venlafaxine (PO)
96
Which SNRI is FDA approved for diabetic neuropathic pain and GAD in children (7-17) but should be avoided in chronic liver disease/cirrhosis?
Duloxetine (PO)
97
Which SNRI is FDA-approved for MDD only?
Desvenlafaxine (PO)
98
Which SNRI has a long half life and is FDA-approved for MDD only?
Levomilnacipran (PO)
99
Which antidepressant is a Norepinephrine and Dopamine Reuptake Inhibitor?
Bupropion (PO)
100
What is Bupropion clinically used for
Depression Also FDA-approved for smoking cessation Off-label use for ADHD
101
What are common side effects of Bupropion?
Jitteriness Fewer sexual SE Short half-life requiring either BID dosing or extended release for daily dosing.
102
Which antidepressant is a 5-HT, H-1, and Alpha-1 receptor antagonist?
Trazodone (PO)
103
What is the clinical use of Trazodone?
Depression Used for insomnia due to excessive sedation
104
What are the side effects of Trazodone?
Sedation Priapism (rare)
105
Which tetracyclic antidepressant is an alpha-2 and 5-HT antagonist?
Mirtazepine (PO)
106
What is the clinical use of Mirtazepine?
Depression Lower doses are more sedating
107
What are the side effects of Mirtazepine?
Fewer sexual SE Appetite stimulation
108
In general, what is the MOA of tricyclic antidepressants (TCA)?
Affect multiple receptors: – 5-HT and NE reuptake inhibition – Alpha-1 and alpha-2, muscarinic, and histamine antagonism
109
What is the clinical use of tricyclic antidepressants?
Depression Many also used for neuropathic/chronic pain
110
What are common side effects of tricyclic antidepressants?
Anticholinergic: dry mouth, constipation, blurred vision, urinary retention Antihistamine: sedation Alpha-1 antagonism: orthostatic hypotension Deliriogenic Toxicity: 3Cs – Cardiac arrhythmia, prolonged QT – Convulsions – Coma – Potentially fatal in OD
111
Name 5 tricyclic antidepressants (TCAs).
Amitriptyline (PO) Desipramine (PO) Doxepin (PO) Imipramine (PO) Nortiptyline (PO)
112
Which tricyclic antidepressant (TCA) can also treat insomnia leading to a more sedating effect (side effect)?
Doxepin
113
Which tricyclic antidepressant (TCA) can also treat nocturnal enuresis (bed wetting) and neuropathic pain?
Imipramine
114
Which tricyclic antidepressant (TCA) can also treat chronic pain?
Nortriptyline
115
What is the MOA of monoamine oxidase inhibitors (MOAIs)?
Inhibit NT degradation in synaptic cleft by MAO-A and/or MAO-B
116
What is the clinical use of monoamine oxidase inhibitors (MOAIs)?
Depression Usually reserved for treatment-resistant depression
117
What are the side effects of monoamine oxidase inhibitors (MOAIs)?
Multiple side effects: o Serotonergic o Noradrenergic o Alpha-1 blockade o Antihistaminergic Need 14-day washout period before starting other antidepressants to avoid serotonin syndrome Toxicity: Hypertensive Crisis o Other antidepressants o Decongestants o Tyramine-containing foods
118
Name 4 monoamine oxidase inhibitors (MOAIs)?
Isocarboxazid (PO) Phenelzine (PO) Selegiline (PO) Tranylcypromine (PO)
119
Which monoamine oxidase inhibitor (MOAIs) is also FDA-approved for panic disorder and social anxiety disorder?
Phenelzine
120
Which monoamine oxidase inhibitor (MOAI) is also FDA-approved for Parkinson disease and inhibits NT degradation in the synaptic cleft by MOA-B ONLY?
Selegiline
121
How long does it take for antidepressants to reach peak efficacy?
Antidepressants take 4-6 weeks to reach peak efficacy (some effect may be seen in 1-2 weeks)
122
Why is it important to taper antidepressants?
All antidepressants should be tapered to discontinuation to minimize risk of Serotonergic Discontinuation Syndrome
123
What is important to consider when considering antidepressants that have a short half-life?
Antidepressants with shorter half-life confer higher risk of discontinuation syndrome
124
What side effects do most antidepressants have?
anticholinergic side effects (dry mouth)
125
When should you refer to psychiatry when trying to find an antidepressant for your patient?
Referral to psychiatry after trial of 2 antidepressant medications of adequate duration and dose
126
What is important to consider when prescribing antidepressants for children and adolescents?
Only a few antidepressants are FDA-approved in children and adolescents; most are used off-label
127
What is the FDA Black Box Warning for antidepressants?
Antidepressants increase the risk of suicidal thinking and behavior (suicidality) in children and adolescents with MDD and other psychiatric disorders. Anyone considering the use of an antidepressant in a child or adolescent for any clinical use must balance the risk of increased suicidality with the clinical need. Patients who are started on therapy should be observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised to closely observe the patient and to communicate with the prescriber.

Essentials 1.3 Drugs (9 decks)

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