Psych Meds Flashcards

Question

Nefazodone | Trazadone

Answer 1

Serotonin antagonist reuptake inhibtors - Nefazodone= too many contraindications - Trazadone= sedative, not therapeutic for depression at lower doses (Priapism!)

Answer 2

Tricyclic antidepressants - Closely resemble phenothiazines - More efficacious than SSRIs, but more side effects MOA: - Affect multiple receptors (NE, 5-HT= serotonin) - Blocks active reuptake of NE, Serotonin--> higher levels in synaptic celft--> longer contact with post-synaptic sites * * GOLD STANDARD efficacy - Used for treatment-resistant depression (due to side effect burden) Uses: * Depression * Enuresis in childhood (e.g., Imipramine) * Chronic pain, neuralgias, migraine, diabetic neuropathy (e.g., Amitriptyline, Imipramine and Desipramine) AEs: - * Sedation - * Anticholinergic (constipation dry mouth, urinary hesitancy, blurry vision, impaired memory) - * Orthostatic hypotension/ falls - * ECG changes (e.g. QRS, PR and QT prolongation) - * Weight gain - * Headache, tremor & seizures - *Obstructive jaundice - *Sexual side effects (impotence) - *Class 1a anti-arrhythmic (avoid in BBB, post MI arrhythmias) - *More likely than SSRI to precipitate mania (MAKE SURE IT'S UNIPOLAR DEPRESSION) Can be fatal in overdose (1 week supply) - Medical emergency: Cardiac monitoring, gastric lavage, lidocaine, phenytoin, bicarb need STAT administration Drug interactions: - Metabolism affected by race, sex (slower in AA, Asians, higher in women) * * Nortriptyline is only TCA that doesn't require drug monitoring

Answer 3

MAO-inhibitors - MAO-A enzyme deaminates NA/5-HT/Tyramine - MAO-B deaminates DA/histamine/tyramine MOA: - Inhibits intraneuronal MAO type A isoenzyme--> higher levels of NE, serotonin release Uses: - Superior to TCA for bipolar and atypical depression, dysthymia - Phobic anxiety states - Migraine - neurodermatitis AEs (Phenelzine): - Hydrazine derivative - More weight gain - More orthostatic hypotension - More hepatotoxicity potential - More anxielytic - Slower onset of action - Sexual dysfunction AEs (Tranylcypromine): - Non-hydrazine - Related to amphetamine structure (cyclopropyl ring) - Faster onset of action, some abuse potential - Sexual dysfunction Drug interactions: - Tyramine containing food (aged food, chianti wine, fava beans)--> dangerous rise in BP--> stroke - Amphetamines, demerol, sympathomimetics--> HTN crisis - Must be discontinued 2 weeks prior to surgery (interaction with anesthetics) - MAOI/ SSRI combination--> serotonin syndrome (need 2 week washout)

Answer 4

Cell bodies in Locus Coeruleus. Project to: - Caudate - amygdala - Thalamus - Hypothalammus - Limbic cortex

Answer 5

Cell bodies in Raphe nuclei. Project to: - Limbic system (hippocampus, hypothalamus, amygdala) - Cortex

Answer 6

SSRI Prodrug with v. long half-life (2.5 days) - 4-5 week steady state

Answer 7

``` SSRI Short half-life than Fluoxetine - Time to achieve steady state= 1 week - Short wash-out period Fewer drug interactions than Fluoxetine ```

Answer 8

SSRI Some anticholinergic action= more sedating - Early relief of anxiety and insomnia - Can cause constipation - Short half-life, severe discontinuation syndrome if stopped abruptly= akasthesia, restlessness, GI upset, dizziness, tingling, dysesthesias, nausea

Answer 9

reduce daytime anxiety, decrease excessive excitement, promote calm state.

Answer 10

produce drowsiness and promote onset and maintenance of sleep.

Answer 11

MOA: bind to specifc site on GABA(A) receptor - Enhance GABA effect without directly activating GABA receptor or opening Chloride channel - GABA needs to be present for benzos to work - alpha-1 subunit appears to mediate both sedation and memory effects of benzodiazepines. AEs: - Potential for Abuse including Intoxication - can be associated with behavioral disinhibition * * Withdrawal--> Seizures, death - short term use (< 6 weeks) of long-acting benzos unlikely to have withdraw - Year or longer use= careful monitoring - Discontinuation needs slow taper (50%, then 10% per week) Side effects: - Daytime drowsiness - Dangerous in combination with other sedatives esp. ETOH--> drowsiness, disinhibition, respiratory depression. - Dizziness and ataxia (< 2%) - Avoid in COPD, sleep apnea patients - Avoid in pts with cognitive defects (amnesia, memory impairment) OVERDOSE: lethal to effective dose: 200:1 Drug interactions: - Decreased absorption: antacids - Increased CNS depression: antihistamines, barbiturates, TCAs, EtOH - CYP450 competition--> increased BZD levels (cimetidine, erythromycin, estrogens, fluoxetine, isoniazid, fluvoxamine, cisapride, grapefruit juice) * * Lorazepam, oxazepam, temazepam can be used in liver disease patients

Answer 12

MOA: increase duration of channel openings - May directly activate Cl-channel opening - Can also directly depress excitatory neurotransmitters - More powerful CNS suppression, low margin of safety * * Potential for drug interactions, abuse, use in suicide attempts make them obsolete as routine meds for insomnia

Answer 13

Alprazolam, Triazolam, Lorazepam, Oxazepam

Answer 14

Flurazepam, Clorazepate, Prazepam

Answer 15

Barbituate-like effect at GABA receptor - Prodrug - Lethal dose (3x therapeutic dose) - Liver injury - Only used in pediatrics, limited use

Answer 16

Antagonists of CNS H-1 receptors- need to penetrate BBB to produce sedation - Diphenhydramine used at 25-50 mg - Anticholinergic and serotonergic properties - Frequently used, effects on sleep not well-documented ``` Side effects: = Cognitive impairment - Confusion - Sedation - Delirium, urinary retention ```

Answer 17

``` Estazolam Flurazepam (t1/2= 100 hours, not ideal) Quazepam Temazepam Triazolam ```

Answer 18

Benozodiazepine receptor agonists: 1. Zolpidem (Ambien®): t ½ - 2.5 hrs - Liver metabolizm - XR tablets-- longer action, longer onset 2. Zaleplon (Sonata®): t ½ - 1 hr - useful for middle of the night insomnia, less likely to cause next-day impairment 3. Eszopiclone (Lunesta): t ½ - 6 hrs - Act on Alpha subunit of GABA-A type receptor - Better specificity to produce hypnotic effect * AEs: - daytime sedation, psychomotor/cognitive impairment - Rebound insomnia - Respiratory depression - Abuse ``` Melatonin receptor agonists: 1. Ramelteon= melatonin receptor agonist AEs: - HA, somnolence, fatigue, dizziness - Prolactin elevation in females, testosterone elevation in older males - No abuse ```

Answer 19

DA Agonists used for Restless Legs syndrome Side effects: - Nausea, orthostatic hypotension (gradual dose increase) - Insomnia (Benso) - Fatigue (reduce dose, switch to L-dopa) - Hallucinations (discontinue) - Tolerance (Rx holiday) - Augmentation (daytime dose, discontinue if severe)

Answer 20

1. Modafinil 2. Methylphenidate (ritalin) 3. Dextroampetamine/Methamphetamine 4. Pemoline (NOT used any more- hepatotoxic)

Answer 21

1. Tricyclic antidepressants 2. SSRIs 3. Misc: Venlafaxine, gamma hydroybutyrate