Chapter 18: Psychopharmacology Flashcards

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1
Q

TCA side effects

A

= HAM
anti-Histamine (sedation, weight gain)
anti-Adrenergic (hypotension)
anti-Muscarinic (dry mouth, blurred vision, urinary retention, constipation)

TCAs and low-potency anti-psychotics

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2
Q

Serotonin syndrome

A

confusion, flushing, diaphoresis, tremor, yoclonic jerks, hyperthermia, hypertonicity, rhabdomyolysis, renal failure, and death
- occurs when there is too much serotonin, classically when SSRIs and MAOs are combined

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3
Q

Hypertensive crisis

A

caused by a buildup of stored catecholamines; caused by the combination of MAOIs with tyramine-rich foods (e.g. red wine, cheese, chicken liver, cured meats) or with sympathomimetics

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4
Q

Extrapyramidal side effects (EPS)

A

Parkinsonism- masklike face, cogwheel rigidity, badyinesia, pill-rolling tremor,

akathisia- restlessness, need to move, and agitation;

dystonia- sustained, painful contraction of muscles of neck, tongue, eyes, diaphragm

  • Occur with high-potency, typical (first generation) antipsychotics
  • Reversible
  • Occur within hours to days of starting medications or increasing doses
  • in rare cases can be life threatening (e.g., dystonia of the diaphragm causing asphyxiation)
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5
Q

Hyperprolactiemia

A

Occurs with high-potency, typical (first generation) antipsychotics and risperidone

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6
Q

Tardive Dyskinesia (TD)

A

Choreoathetoid muscle movments, usualy of the mouth and tongue (can affect extremities, as well)

  • occurs after years of antipsychotic use (more likely with high-potency, first-generation antipsychotics)
  • usually is irreversible
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7
Q

Neuroleptic malignant syndrome

A

Mental status changes, fever, tachycardia, hypertension, tremor, elevated creatine phosphokinase (CPK), “lead pipe” rigidity

  • can be caused by any antipsychotic after a short or long time (increased with high-potency, typical antipsychotics)
  • a medical emergency with up to 20% mortality rate
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8
Q

Important CYP 450 inducers include

A
Tobacco
Carbamazepine
Barbotirates
St Kpjm
s wprt
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9
Q

Important CYP 450 inhibitors include

A
Fluvoxamine
Fluoxetine
Paroxetine
Duloxetine
Sertraline
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10
Q

Keeping the “kinesias” straight

A

Tardive dyskinesia - grimacing and tongue protrusion
Acute dystonia- twisting and abnormal postures
Akathisia- inability to sit still
Bradykinesia- slow body movement

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11
Q

First-line treatment for extrapyramidal symptos

A

benztropine (Cogentin)

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12
Q

Common side effect of anticholinergic meds

A

constipation

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13
Q

dementia and anticholinergics

A

They make it worse

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14
Q

Antidepressants

A

Major categories: SSRIs, heterocyclics (including TCAs), MAOIs, Miscellaneous

  • 60-70% of pts with major depression will respond to an antidepressant med
  • Most require a trial of 3-4 weeks, sometimes 6-8 weeks to see improvement
  • many have withdrawal phenomenon (dizziness, headaches, nausea, insomnia, malaise); may need to taper
  • SSRIs and related are most frequently prescribed (safety, tolerability), but go off: pt symptoms, previous treatments, side-effects, comorbid conditions, risk of suicide via overdose, cost
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15
Q

SSRIs

A

inhibit presynaptic serotnin pumpts–> increased availability of serotonin in synaptic clefts –> brain plasticity (may explain delay of onset)

  • sometimes different SSRIs –> different response
  • most dosed daily. Fluoxetine has weekly form
  • no correlation between plasma levels and efficacy/ side effects
  • Most commonly prescribed. Advantages: low side effects, no food restrictions, much safer in overdose

Examples: Fluoxetine (prozac), Sertraline (Zoloft), Paroxetine (Paxil), Fluvoxamine (luvox), Citalopram (celexa), escitalopram (Lexapro)

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16
Q

Fluoxetine

A

(prozac)
Longest half-life, with active metabolites; no need to taper
safe in pregnancy, ok for kids
side effects: insomnia, anxiety, sexual dysfunction
can elevate levels of antipsychotics leading to increased side effects

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17
Q

serotonin syndrome and OTC

A

increased serotonin can be caused by OTC cold remedies (dextromethorphan, e.g.)

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18
Q

treating sex side effects of SSRIs

A

reduce the dose (if clinically appropriate), change to non-SSRI antidepressant, augment with bupropion, or, in men, add sildenafil/ etc.

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19
Q

Sertraline

A

(zoloft)

  • GI disturbances
  • few drug interactions
  • other side effects: insomnia, anxiety, sex dysfunction
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20
Q

Paroxetine

A

(paxil)
Highly protein bound –> several drug interactions
S/E: anticholinergic (sedation, constipation, weight gain), sex dysfunction
short half-life –> withdrawal phenomena if not taken consistently

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21
Q

Citalopram

A

(celexa)
fewest drug-drug interactions
dose dependent QTc prolongation

22
Q

Escitalopram

A

Lexapro
- levo-enantiomer of citalopram; similar efficacy, possibly fewer side effects
dose dependent QTc prolongation

23
Q

Side Effects of SSRIs

A

significantly fewer than TCAs and MAOIs due to serotonin selectivity (do not act on histamine, adrenergic, or muscarinic receptors)
much safer in overdose. Mose s/e occur because of high number of serotonin receptors throughout the body, including GI tract
Many s/e resolve within a few days to weeks:
- GI disturbance (nausea, diarrhea; give with food)
- Insomnia; vivid dreams, resolves over time
- headache
- anorexia, weight loss

Other s/e:

  • sex dysfunction: decreased libido, anorgasmia, delayed ejaculation. Weeks to months, typically do not resolve
  • restlessness: an akathisia-like state
  • SEROTONIN SYNDOME- 2 meds , both of which increasee serotnonin–> too much in the brain. E.g.: triptans (for headaches), with SSRIs.
  • hyponatremia: rare
  • seizures: .2%
24
Q

Serotonin syndrome symptoms

A

fever, diaphoresis, tachycardia, HTN, delirium, neuromuscular excitability (hyperreflexia and “electric jolt” limb movements)

25
Q

SNRIs

A

Venlafaxine- for depression, anxiety disorders like GAD, neuropathic pain. Low drug interaction potential

  • extended-release (XR form) allows once-daily
  • Side effects similar to SSRIs, with the exception of increased BP in higher doses; do not use in pts with untreated or labile BP
  • new form: desvenlafaixine (Pritiq)- active metabolite, expensive, no known benefit over venlafaxine

Duloxetine (Cymbalta)- often used for depression, neuropathic pain, fibromyalgia

  • similar side effects to SSRIs, more dry mouth and constipation (NE effects)
  • hepatotoxicity more likely in pts with liver disease or heavy alcohol use
  • expensive
26
Q

Norepinephrine-Dopamine Reuptake inhiitors

A

Bupropion (Wellbutrin)

  • relative lack of sex side effects compared to SSRIs
  • some efficacy in adult ADHD
  • effective for smoking cessation
  • side effects: increased anxiety, risk of seizures and psychosis at high doses
  • contraindicated in pts with seizure or active eating disorders, and in those currently on an MAOI
27
Q

Serotonin receptor antagonists and agonists

A

Trazodone (Dsyrel) and Nefazodone (Serzone)

  • useful for major depression, major depression with anxiety, and INSOMNIA (2ndary to sedative effects)
  • not sexual side effects of SSRIs and do not affect rapid eye movement sleep
  • side effects: nausea, dizziness, orthostatic hypotension, cardiac arrhythmias, SEDATION, PRIAPISM (esp trazoBONE)
  • because of orthostatic hypotension in higher doses, trazodone not frequently used solely as an antidepressant. Commonly used to treat insomnia, often when initiating an SSRI (until insomnia improves as depression resolves)
  • Nefazodone carries BLACK BOX WARNING- rare but serious liver failure.
28
Q

alpha-2 adrenergic receptor antagonists

A

Mirtazapine (Remeron)
useful in treatment of major depression, esp. in patients who have significant weight loss and/or insomnia
- side effects include sedation, weight gain, dizziness, tremor, dry mouth, constipation, and rarely agranulocytosis
- fewer sex side effects compared to SSRIs and few drug interactions

29
Q

SSRIs and warfarin

A

can increase levels of warfarin–> monitor carefully when starting and stopping!

30
Q

Bupropion and seizure

A

lowers the seizure threshold. Caution in patients with epilepsy and eating disorders

31
Q

Remeron special use

A

treating major depression in the elderly- helps with sleep and appetite

32
Q

Heterocyclic antidepressants

A

= TCAs
inhibit the reuptake of NE and serotonin, increased availability of monoamines in the synapse
- long half-lives; most dosed once daily
- rarely first-line agents- higher side effects, titration of dosing, LETHALITY OF OVERDOSE

33
Q

Tricyclic antidepressants: Tertiary amines

A

highly anticholinergic, antihistaminergic (more sedating)/ antiadrenergic with greater lethality in overdose.

Amitryptiline- chornic pain, migraines, insomnia
Imipramine- intrauscular form as well. Useful in enureisis, panic disorder
Clomipramine- most serotonin-specific, thereful useful in OCD
Doxepin- chronic pain, sleep aid in low doses

34
Q

Tricyclic antidepressants: Secondary amines

A

metabolites of tertiary amines (less anticholinergic/ antihistaminic/ antiadrenergic)
Nortriptyline - least likely to cause orthostatic hypotension. good for chronic pain
Desipriamine- more activating/ less sedating. Least anticholinergic

35
Q

Treatment for TCA overdose

A

IV sodium bicarbonate

36
Q

Tetracyclic antidepressants

A

Amoxapine- metabolite of antipsychoic loxapine. May cause EPS and siilar side-effect profile to typical antipsychotics

37
Q

how much TCA is lethal in OD?

A

one week supply; 1-2 g

38
Q

Major complications of TCAs mnemonic

A

3-Cs: Cardiotoxicity, Convulsions, Coma

39
Q

MAOIs vs TCAs

A

MAOIs more effective in depression with atypical fetures (hypersomnia, increased appetite, heavy feeling in extremities, and increased sensitivity to interpersonal rejection)

40
Q

Side effects of TCAs

A

hihgly protein bound and lipid soluble; can interact with other meds that have high protein binding
mostly due to lack of specificity and interaction with other receptors

Antihistaminic: sedation and weight gain
Antiadrenergic: Cardivascular (orthostatic hypotension, dizziness, reflex tachycardia, arrhythmias - block cardiac sodium channel, electrocardiographic (ECG) changes- widening QRS, QT, PR intervals. Avoid in patients with preexisting conduction abnormalities or recent MI.
Antimuscarinic effects- (anticholinergic)- dry mouth, constipation, urinary retention, blurred vision, tachycardia, exacerbation of narrow angle glaucoma
Serotonin effects: Erectile/ ejaculatory dysfunction in males, anorgasmia in females

Lethal in OD- carefully assess suicide risk when prescribing

41
Q

Symptoms of TCA overdose

A

agitation, tremors, ataxia, arrhythmias, delirium, hypoventilation from CNS depression, myoclonus, hyperreflexia, seizures, coma.

42
Q

Monoamine Oxidase Inhibitors- action

A

prevent inactivation of biogenic amines such as NE, serotonin, dopamine, and tyramine. (intermediate in the conversion of tyrosine to NE)
By IRREVERSIBLY inhibiting the MAO-A and -B enzymes, increases number of neurotransmitters available in synapses.

not first-line because of increased safety and tolerability of newer stuff (SSRIs, SNRIs). Used for REFRACTORY DEPRESSION and refractory anxiety disorders.

Phenelzine, Tranylcypromine, Isocarboxazid

43
Q

MAO-A

A

preferentially deactivates serotonin and NE

44
Q

MAO-B

A

preferentially deactivates phenethylamine

both MAO-A and B act on dopamine and tyramine

45
Q

Side effects of MAOIs

A

Serotonin syndrome when combined with SSRIs and others that increase serotonin levels

Hypertensive crisis with tyramine-rich foods

othostatic hypotension (most common)
drowsiness
weight gain
sex dysfunction
dry mouth
sleep dysfunction
Pts with pyridoxine deficiency can have numbness or paresthesias, so they should supplement with B6
Liver toxicity, seizures, and edema (rare)

START LOW AND GO SLOW

46
Q

Serotonin syndrome symptoms

A

initially lethargy, restlessness, confusion, flushing, diaphoresis, tremor, myoclonic jerks.
My progress to hyperthermia, hypertonicity, rhabdomyolysis, renal failure, convulsions, coma, and death
Wait at least 2 weeks before switching from SSRI to MAOI, and at least 5-6 weeks with fluoxetine

47
Q

Hypertensive crisis

A

risk when MAOIs are taken with tyramine-rich foods or sympathomimetics

  • red wine, cheese, chicken liver, fava beans, cured meats)–> buildup of stored catecholamines
  • increased BP, headache, sweating, nausea and vomiting, photophobia, autonomic instability, chest pain, arrhythmias, and death.
48
Q

Selegeline

A

MAOI used to treat depression that does not require following the dietary restrictions when used in low dosages. However, decongestants, opiats (meperidine, fentanyl, tramadol) and serotonergic drugs must still be avoided.

49
Q

First steps when suspecting serotonin syndrome

A

discontinue the meds.
Provide supportive care and benzos
cyproheptadine (serotonin antagonist) can also be used.

50
Q

Antidepressant use in other disorders

A

OCD- SSRIs (high doses), TCAs (clomipramine)
Panic disorder: SSRIs, TCAs, MAOIs
Eating disorders: SSRIs (in high doses), TCAs
Persistent depressive disorder (dysthymia): SSRIs, SNRIs
Social anxiety disorder (social phobia): SSRIs, SNRIs, MAOIs
GAD: SSRIs, SNRIs, TCAs
Post traumatic stress disorder: SSRIs
IBS: SSRIs, TCAs
Eneuresis: TCAs (imipramine)
Neuropathic pain: TCAs (amotripyline, nortriptyline), SNRIs
Chronic pain: SNRIs, TCAs
Fibromyalgia: SNRIs
Migraine headaches: TCAs (amitriptyline)
Smoking cessation: Bupropion
Premenstrual dysphoric disorder: SSRIs
Insomnia: Mirtazapine, trazodone, TCAs (doxepin)