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424 Pharmacology > CNS: Psychopharm and Cannabis > Flashcards

CNS: Psychopharm and Cannabis Flashcards

1
Q

What is a common consideration across antidepressants/anxiolytics?

A

Do not discontinue abruptly

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2
Q

What is the black box warning for all antidepressants?

A

increases risk of SI in children, adolescents and young adults

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3
Q

Common contraindication across TCAs, SSRIs, SNRIs, bupropion, methylphenidate, amphetamines

A

Contraindicated if MAOI use within 2 weeks

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4
Q

What nutrient do MAOIs interact with that make it difficult to prescribe? What can that cause?

A

Tyramine - can cause hypertensive crisis

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5
Q

What is usually prescribed for panic dx?

A

alprazolam, clonazepam, fluoxetine, paroxetine, sertraline, Buspar (not monotherapy)

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6
Q

What is usually prescribed for GAD (generalized anxiety)?

A

alprazolam, duloxetine, escitalopram, paroxetine, venlafaxine

off-label: citalopram, desvenlafaxine, fluoxetine, fluvoxamine, mirtazapine, pregabalin, sertraline

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7
Q

What are the first-line agents for PTSD?

A

VA guidelines: sertraline, paroxetine

Canadian guidelines: paroxetine, venlafaxine, fluoxetine, sertraline

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8
Q

What are some medications to be aware of that affect the CYP450 system and thus interact with several antidepressants/anxiolytics?

A
  • azole antifungals
  • macrolide antibiotics
  • HIV protease inhibitors
  • calcium channel blockers
  • SSRIs
  • nefazodone
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9
Q

What is neuroleptic malignant syndrome?

A

rare but potentially fatal - extreme muscle rigidity, high fevers, coma, death

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10
Q

Tricyclic antidepressants

Amitriptyline, nortriptyline, imipramine, doxepin, trimipramine maleate, amoxapine, desipramine, protriptyline hydrochloride, clomipramine

Indication & MOA

A

Indications: depression, anxiety with sleep disturbance (doxepin, elavil), enuresis in children 6+ (imipramine), OCD (clomipramine), eating disorders

Doxepin: insomnia

MOA: Acts on serotonin, norepinephrine, histamine and acetylcholine

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11
Q

Tricyclic antidepressants

Amitriptyline, nortriptyline, imipramine, doxepin, trimipramine maleate, amoxapine, desipramine, protriptyline hydrochloride, clomipramine

Prescribing considerations

A
  • Long half-life of 6-8 hours
  • Metabolized by the CYP450 system
  • Highly cardiotoxic; can cause life-threatening arrythmias
  • narrow TI OD can be fatal OD dose isn’t that high - avoid in those with SI
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12
Q

Tricyclic antidepressants

Amitriptyline, nortriptyline, imipramine, doxepin, trimipramine maleate, amoxapine, desipramine, protriptyline hydrochloride, clomipramine

Avoid, caution

A
  • Avoid: angle closure glaucoma, suicidal patients, cardiovascular disorders, glaucoma
  • Caution: metabolic syndrome, seizure disorder, elderly (anticholinergic fx, hip fractures)
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13
Q

Tricyclic antidepressants

Amitriptyline, nortriptyline, imipramine, doxepin, trimipramine maleate, amoxapine, desipramine, protriptyline hydrochloride, clomipramine

Adverse fx (5)

A
  • Paradoxical diaphoresis
  • Anticholinergic fx
  • Orthostatic hypotension
  • Sedation
  • drowsiness
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14
Q

SSRIs

Fluoxetine, olanzapine-fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram

Indications & MOA

A

indications: depression, anxiety, panic disorders, OCD, body dysmorphic disorder, bulimia, PDD, PTSD, vasomotor symptoms in menopause

MOA: Selective inhibitory fx on presynaptic serotonin reuptake and weak fx on NE and dopamine reuptake

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15
Q

SSRIs

Fluoxetine, olanzapine-fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram

Considerations (specific to fluoxetine, paroxtine, sertraline, citalopram, escitalopram)

A
  • Long half-life: 26 hours
  • Takes a few weeks to take effect
  • Extensive first-pass metabolism
  • Metabolized by the CYP450 system
  • Fluoxetine: least likely to cause weight gain, increases energy can be activating (may feel like worsening anxiety), long half-life; start low and titrate slow
  • Paroxetine: interacts with a lot of other medications, nasty withdrawal, stimulates appetite, significant weight gain, excessively sedating
  • Sertraline: increases energy
  • Citalopram: BBW for QT prolongation - max dose 40mg daily, 20mg daily if over 60
  • Escitalopram: tends to be weight neutral and neither sedating nor activating
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16
Q

SSRIs

Fluoxetine, olanzapine-fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram

BBW, pregnancy/lactation, peds, contraindications

A
  • BBW for citalopram: QT prolongation
  • Pregnancy/lactation: Eval risk vs. benefit, newborn can have withdrawal symptoms; lactation: sertraline and escitalopram have the lowest relative infant dose
  • Peds: Fluoxetine is first line
  • CI: hypersensitivity to SSRIs, renal or hepatic insufficiency
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17
Q

SSRIs

Fluoxetine, olanzapine-fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram

adverse fx

A
  • CNS: agitation, insomnia, serotonin syndrome, blurred vision, headache, drowsiness, tremor
  • GI: nausea, vomiting, diarrhea, GI bleed, hyponatremia, weight changes, dry mouth, constipation
  • Other: Sexual dysfunction, rash/itching
  • CV: QT prolongation (citalopram)
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18
Q

What is serotonin syndrome?

A
  • ADR that occurs with more than one serotonergic agent taken at the same time
  • Sx = altered mental status or agitation, GI distress, neuromuscular changes (clonus, tremors, hyperreflexia), VS changes, sweating, hyperthermia
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19
Q

SNRIs

Venlafaxine, duloxetine, milnacipran, desvenlafaxine

Indications, MOA

A
  • MDD, GAD, neuropathy, fibromyalgia (Milnacipran), social anxiety, binge eating disorder, OCD, postmenopausal disorder, PTSD, panic disorder
  • MOA: Inhibit reuptake of norepinephrine and serotonin
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20
Q

SNRIs

Venlafaxine, duloxetine, milnacipran, desvenlafaxine

Prescribing considerations

A
  • Long half-life 8-17 hours
  • Metabolized by CYP450
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21
Q

SNRIs

Venlafaxine, duloxetine, milnacipran, desvenlafaxine

Avoid, pregnancy

A
  • Avoid: uncontrolled HTN, renal & hepatic impairment
  • Pregnancy: venlafaxine & desvenlafaxine - consider tapering in 3rd trimester
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22
Q

SNRIs

Venlafaxine, duloxetine, milnacipran, desvenlafaxine

Interactions & Monitoring

A
  • Interactions
    • Antibiotics
    • OTC medications that stimulate or cause insomnia or drowsiness
  • Monitoring
    • Serum transaminase levels
    • SI
    • Activation of hypomanic or manic symptoms
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23
Q

SNRIs

Venlafaxine, duloxetine, milnacipran, desvenlafaxine

Adverse fx

A
  • CNS: Headache, somnolence, dizziness, Insomnia, Fatigue, sedation
  • GI: Dry mouth, Constipation, nausea
  • CV: Orthostatic hypotension
  • GU: Erectile dysfunction, Ejaculation failure
  • Other: sweating
24
Q

Bupropion (Wellbutrin)

Indications & MOA

A
  • indications: good with co-morbid mood dx; ADHD, MDD, smoking cessation
  • MOA: inhibits reuptake of norepinephrine and dopamine
25
Q

Bupropion

Contraindication & adverse fx

A
  • CI: bupropion in seizure disorders or when tapering/withdrawing from other CNS depressants; avoid in anxiety
  • ADR: insomnia
26
Q

Mirtazapine/trazodone

Indications, MOA, ADRs

A
  • Indications: Mirtazapine is an antagonist of 5HT2, 5HT3 and histamine receptors
  • ADR: drowsiness at higher levels
27
Q

Typical Antipsychotics

Phenothiazines: Chlorpromazine (Thorazine)

Non-phenothiazine: haloperidol (Haldol)

MOA, CI, BBW

A

Block dopamine receptors in the basal ganglia, hypothalamus, limbic system, medulla

CI: glaucoma, bone-marrow depression, severe liver or CVD

BBW: increased mortality in older adult patients

28
Q

Typical Antipsychotics

Phenothiazines: Chlorpromazine (Thorazine)

Non-phenothiazine: haloperidol (Haldol)

Monitoring & ADRs

A
  • Monitoring: Abnormal involuntary movement scale (AIMS)
  • ADRs
    • STANCE
      • Sedation/sunlight sensitivity/skin effects/sexual side fx
      • Tardive dyskinesia
      • Anticholinergic effects and agranulocytosis
      • Neuroleptic malignant syndrome
      • Cardiac arrythmias
      • Extrapyramidal symptoms/akathisia endocrine effects - increased prolactin
    • Weight gain
29
Q

Atypical antipsychotics

Ariprazole (Abilify),clozapine (Clozaril), olanzapine (Zyprexa), quetiapine (Seroquel), risperidone (Risperdal), ziprasidone (Geodon)

Indications & MOA

A
  • psychotic mania, nonpsychotic mania
  • Block serotonin and dopamine receptors
30
Q

Atypical antipsychotics

Ariprazole (Abilify),clozapine (Clozaril), olanzapine (Zyprexa), quetiapine (Seroquel), risperidone (Risperdal), ziprasidone (Geodon)

Considerations, CI, ADRs

A
  • Considerations: -pines are more sedating than the -dones, related to their antihistamine actions
  • CI: hepatic or renal disease
  • ADRs
    • Seizures
    • Weight gain
    • Diabetes
    • Hyperprolactinemia
    • Dizziness
    • Orthostatic hypotension
    • Clozapine: fatal agranulocytosis
31
Q

Benzodiazepines

Lorazepam (Ativan), Flurazepam (dalmane), Temazepam (restoril), Triazolam (Halcion)

Indications

A
  • anxiety, panic disorders, alcohol withdrawal, seizures, insomnia, muscle spasms, pre-anesthesia sedation, IBS, restless leg syndrome, chemo N/V
  • Flurazepam, temazepam, triazolam for insomnia
  • MOA: increase the action of GABA, which decreases the effect of neuronal excitation
32
Q

Benzodiazepines

Lorazepam (Ativan), Flurazepam (dalmane), Temazepam (restoril), Triazolam (Halcion)

Considerations, caution, CI, peds

A
  • rapidly and widely distributed throughout the body following oral intake; peak 30min-8 hours
  • Caution: elderly - BEERS
  • CI: pregnancy, renal & hepatic impairment, hypersensitivity to benzodiazepines, acute narrow-angle glaucoma
  • Peds: 6+
33
Q

With which medications should you educate your patient to avoid driving while taking?

What are the treatment durations of these medications?

A
  • Flurazepam, temazepam, triazolam: Should not be used more than 3x a week for less than 3 months
  • Zolpidem not to be used longer than 8 weeks; females take half-dose
  • Zaleplon should not be used longer than 5 weeks
34
Q

Benzodiazepines

Lorazepam (Ativan), Flurazepam (dalmane), Temazepam (restoril), Triazolam (Halcion)

Interactions, Monitoring, ADRs

A
  • Interactions
    • digoxin, TCAs: benzo increases level
    • barbiturates, nefazodone, fluoxetine, fluvoxamine, MAOIs, sertraline, antihistamines: increased CNS depression
    • Clozapine: increased sedation, salivation, hypotension, delirium, respiratory arrest
  • Monitoring if long term use: LFTs, CBC, TCA and digoxin levels
  • ADRs
    • CNS depression
    • Sedation
    • Physical dependence
35
Q

Buspirone (BuSpar)

MOA, considerations

A
  • partial agonist for serotonin 5-HT1a receptors in the brain
  • May take up to 6 weeks to see fx
  • No physical dependence/withdrawal/abuse potential
  • Less sedating and limited psychomotor impairment
  • Lack of interaction with alcohol
36
Q

Buspirone (BuSpar)

Interactions, ADRs

A
  • Interactions
    • MAOIS, SSRIs may cause serotonin syndrome
    • Atypical antipsychotics
  • ADRs
    • Dizziness
    • Drowsiness
    • nausea
37
Q

Benzodiazepine receptor agonist

Zolpidem (ambien), zaleplon (sonata), eszopiclone (Lunesta)

Indication, MOA, CI, Interactions, monitoring, ADRs

A
  • Indication: Insomnia
  • MOA: agonists on the benzodiazepine site of the GABAa receptor
  • CI: pregnancy, elderly, children, long-term use
  • Interactions: Avoid with alcohol, other CNS depressants
  • Monitoring: LFTs
  • ADRs: CNS depression, sedation, abnormal behaviors
38
Q

Lithium (Lithobid, eskalith)

Indications, considerations

A
  • Indications: Mood stabilizer: manic episodes, maintenance treatment of manic depressive patients with hx of mania; off-label maintenance for bipolar depression and adjunct for MDD, dementia
  • Considerations
    • Not metabolized by the liver, excreted by kidneys
    • Long half-life: 15-36 hours
    • Maintain adequate salt intake
39
Q

Lithium (Lithobid, eskalith)

CI, Monitoring

A
  • CI: pregnancy
  • Monitoring
    • Narrow TI - monitor every 10-14 days after initiating then every 2-3 months after
    • TSH, kidney function, EKG
40
Q

Lithium (Lithobid, eskalith)

ADRs

A
  • Toxicity
  • ECG changes
  • LMNOP: Lithium can cause movement issues (tremors); nephrotoxicity; hypothyroidism; pregnancy problems
41
Q

Valproic acid

Indications, MOA, consideration, CI, monitoring

A
  • Indications - Mood stabilizer: acute mania and mixed episodes; off-label: maintenance tx of bipolar disorder, bipolar depression, psychosis, schizophrenia
  • MOA: Block GABA
  • Considerations: Metabolized by the CYP450 system
  • CI: pregnancy
  • Monitoring
    • Plasma levels every 3 months
    • Platelets, LFTs, coagulation studes
42
Q

Lamotrigine, gabapentin, topiramate

Indications, monitoring, ADRs

A
  • Indications: Mood stabilizer: maintenance of bipolar I; off-label: bipolar depression, bipolar mania, neuropathic/chronic pain, MDD
  • Monitoring: ophthalmological checks required, baseline kidney/liver function tests
  • ADRs
    • Somnolence
    • Dizziness
    • Weight changes
    • Topiramate has 1% chance of renal calculi
43
Q

Carbamazepine (Tegretol)

Indications, considerations, monitoring

A
  • Indications: off-label - bipolar depression, bipolar maintenance, psychoses, schizophrenia adjunct
  • Considerations: Ancestry across broad areas of asia should consider screening for HLA-B1502 allele - can increase risk of Stevens-Johnson syndrome
  • Monitoring: CBCs, LFTs, kidney function, TSH
44
Q

Stimulants

Methylphenidate, dexamphetamine, amphetamine

Indications, MOA

A
  • First line ADHD, narcolepsy
  • increase neurotransmission of dopamine and norepinephrine
45
Q

Stimulants

Methylphenidate, dexamphetamine, amphetamine

Considerations

A
  • Methylphenidate: food slows absorption and onset of action
  • Amphetamines - Vyvanse is the least likely to cause addiction
46
Q

Stimulants

Methylphenidate, dexamphetamine, amphetamine

General CI & caution, then specific to methylphenidate vs. other amphetamines

A
  • CI: CVD, HTN, pregnancy
  • Caution: glaucoma, other mental health conditions, personal/family hx of Tourette’s or tics, seizure dx, Anxious/agitated/tense patient
  • Methylphenidate: circulation issues in fingers or toes
  • Amphetamines: hyperthyroidism, history of drug misuse, hx of issues with stimulants, liver or kidney issues, thyroid issues
47
Q

Stimulants

Methylphenidate, dexamphetamine, amphetamine

ADRs

A
  • Insomnia
  • Weight loss
  • Palpitations
  • HA
  • HTN
48
Q

Non-stimulants

Atomoxetine, guanfacine, clonidine

Indications, MOA, considerations

A
  • Indications: 2nd line ADHD
    • Guanfacine, clonidine: best if hyperactivity and impulsivity poorly controlled
  • MOA: inhibits presynaptic norepinephrine transport
  • Consideration: Potential for patients with hx of substance abuse, tics or severe adverse fx to stimulants
49
Q

Cannabis

Indications, MOA

A
  • Indications
    • THC: analgesia, anti-inflammatory fx, antiemetic
    • CBD: analgesic, anti-inflammatory and anti-seizure
  • CB1: cannabinoid receptors in the CNS modulate cognition, memory, motor function and analgesia
  • CB2: cannabinoid receptors found in tissues related to immune fxn such as WBC, bone marrow, tonsils, thymus and spleen
50
Q

Cannabis

Types

A
  • Sativa: uplifting, energetic, anti-depressive fx, preferred for daytime use
  • Indica: relaxing, calming, sedating, preferred for nighttime use
  • CBD/THC: can be used day or night - CBD mitigates the psychoactive component of THC
51
Q

Cannabis

ADRs

A
  • Xerostomia, nausea, vomiting with excessive use, drowsiness, somnolence, vertigo/dizziness
  • Cannabinoid hyperemesis syndrome may occur with people who smoke excess of marijuana daily and long term - once stopped this should go away but can return if use resumes
52
Q

Clonidine

MOA & Indications

A
  • MOA: centrally acting alpha-2 agonist
  • Indications: approved for HTN and ADHD; off-label for PTSD, social anxiety, Tourette’s, substance withdrawal, menopausal flushing, severe pain not relieved by opiates alone
53
Q

Propranolol (Inderal)

Indications & MOA

A
  • Indication: off-label: PTSD, GAD, violence/aggressive behavior
  • MOA:
    • Helps to prevent the development of PTSD: blocks beta-1 adrenergic receptors and may prevent fear conditioning and reconsolidation of fear
    • Violence/aggression: presumed to be related to central actions at beta adrenergic and serotonin receptors
54
Q

Pediatric considerations for the following:

Lithium, olanzapine, risperidone, ariprazole, ziprasidone, asenapine

A
  • Lithium: approved for acute mania/mixed mania and bipolar maintenance 7+
  • Olanzapine: approved 13+ for schizophrenia and acute mania; 10+ in combo with fluoxetine for bipolar depression
  • Risperidone: approved 13+ for schizophrenia; 10+ acute mania/mixed mania; 5-16 for autism-related irritability
  • Ariprazole: approved 13+ schizophrenia; 10+ acute mania/mixed mania; 6-17 autism related irritability; 6-18 Tourette’s
  • Ziprasidone: clinical trials have demonstrated efficacy for behavioral disturbances in children and adolescents
  • Asenapine: approved 10-17
55
Q

Pregnancy considerations for the following:

Lithium, valproates, carbamazepine, lamotrigine

A
  • Lithium: associated with increased neonatal readmissions, first-trimester exposure has major risk for malformation in infant
  • Valproate: avoid as it can cause fetal abnormalities
  • Carbamazepine: avoid as it can cause fetal carbamazepine syndrome
  • Lamotrigine: potential option for maintenance therapy

424 Pharmacology (12 decks)

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