A/26. Non benzodiazepine anxiolytics and non-benzodiazepine hypnotics. Pharmacotherapy of anxiety disorders. Flashcards

1
Q

Drugs need to know in this topic

A

zolpidem

zaleplon

melatonin

ramelteon

buspirone

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2
Q

Zaleplon
Zolpidem

A

GABA-A agonist

Oral

*CNS depressant effects can be antagonized by flumazenil
**Do not produce the anxiolytic, muscle relaxant,
or anticonvulsant effects associated with BZ’s

  1. Sleep disorders (sleep-onset insomnia → zaleplon, zolpidem;

sleep-maintenance insomnia → eszopiclone)

  • *Side effects:**
    1. CNS depression, additive with other CNS depressants
    2. Dependence liability (to lesser extent than BZ’s)
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3
Q

Buspirone

A

5-HT1A partial agonist

Oral

The onset of clinical effect takes 1-2 weeks

  1. Generalized anxiety disorders
    Side effects:
  2. GI distress
  3. Tachycardia
  4. Paraesthesia
    *Minimal abuse liability

(inhibitory receptor)

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4
Q

Melatonin

A

Regulation of sleep-wake cycle

Oral

  1. Sleep disorders
  2. Available as over-the-counter drug
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5
Q

Ramelteon

A

Activates MT1, MT2 receptors in the suprachiasmatic nucleus

Oral

  1. Sleep disorders (effective for sleep-onset insomnia)
    Side effects:
  2. Dizziness, fatigue
  3. Endocrine alterations (testosterone ↓, prolactin ↑)
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6
Q

Selective serotonin reuptake inhibitors (SSRI’s)

A
  1. Selective inhibition of 5-HT reuptake; allosterically inhibit the transporter, binding at a site other than that of serotonin
  2. Minimal inhibitory effects on NE transporter, cholinergic, and adrenergic receptors
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7
Q

Drug’s name of SSRI’s

A

Fluoxetine

(ES)Citalopram

Sertraline

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8
Q

Fluoxetine

(ES)Citalopram

Sertraline

A

Oral

Inhibitors of cytochrome P450 enzymes (fluoxetine most potent)

  1. Major depressive disorders
  2. Anxiety disorders (GAD – generalized anxiety disorder)
  3. Obsessive compulsive disorder (OCD)
  4. Post-traumatic stress disorder (PTSD)
  5. Premenopausal dysphoric disorder (PMDD)
  6. Panic disorders
  7. Bulimia
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9
Q

Adverse effects

A

1.Anxiety, agitation*
2.Sleep disorders
3.Bruxism
4.Sexual dysfunction** (mediated by 5-HT2A receptors) – libido↓, anorgasmia, erectile dysfunction
5.Weight gain
6.SIADH
7.Withdrawal syndrome → flu-like symptoms, dizziness, anxiety, tremor, palpitations
*Benzodiazepines (alprazolam) may be given as adjunct therapy in the first few weeks of SSRI treatment, to control anxiety and agitation symptoms
**Potential off-label use of SSRI’s in the management of premature ejaculation

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10
Q

Drug interactions

A
  1. Inhibition of P450 enzymes → increased levels of TCA’s, benzodiazepines, warfarin
  2. Serotonin syndrome (with MAO inhibitors, TCA’s, meperidine) → muscle rigidity, myoclonus, hyperthermia, CV instability, ANS instability, seizures
    *Citalopram is the agent least frequently associated with drug-drug interactions
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