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SSRI half lives
- Most are 24 hours.
- Fluoxetine is 2-4 days (it's metabolite norfluoxetine is 7-10 days. this means it takes over a month to reach steady-state plasma concentrations, the others take 5 days)
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SSRIs are bound to...
Plasma proteins (except fluoxetine). Have much less effect on muscarinic, histaminic, and adrenergic receptors, compared to TCAs so they are better tolerated.
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How long does it take for SSRIs to start treating depression?
2-4 weeks. Should be continued 6-8 weeks before pt is considered refractory
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Adverse drug reactions of SSRIs
GI, decreased appetite, insomnia (most common with fluoxetine), headaches, sexual dysfunction, serotonine syndrome (if used with MAOIs)
In general the lesser effects go away after consistent use
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CYP450 Inducers
Smoking, Carbamazepine, Barbiturates, St. Johns wort
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CYP450 Inhibitors
Fuoxetine, Paroxetime, Duloxetime, Sertraline
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Features of Fluoxetine
- longest half life, so no need to taper
- safe in pregnancy
- can elevate levels of neuroleptics
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Features of Sertraline
- high risk for GI disturbances
- very few drug interactions
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Features of Paroxetine
- highly protein bound, so several drug interactions
- anticholinergic effects: sedation, constipation, weight gain
- short half life causes withdrawal if not take consistantly
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Features of Fluvoxamine
- treats OCD
- lots of drug interactions
- CYP inhibitor
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Features of Citalopram
fewest drug-drug interactions
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If taken with cough medicine, SSRIs cause
serotonin syndrome
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Features of serotonin syndrome
- fever
- tachycardia
- hypertension
- delerium
- hyperreflexia
- "electric jolt" limb movements
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Features of Venlafaxine
- used for depression and GAD
- low drug interaction potential
- elevates BP (don't use for pts with htn)
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Features of Duloxetine
- used for pts with depression and neuropathic pain
- side effects include dry mouth and constipation
- liver effects, don't give to alcoholics
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Features of Trazodone
- useful for refractory MDD, insomnia
- no sexual side effects, doesn't effect REM sleep
- side effects: nausea, dizziness, orthostatic hypotension, arrhythmias, sedation, and priapism
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Features of Mirtazapine
- used for refractory MDD, especially in pts who need to gain weight
- good for elderly, helps with sleep and appetite
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Features of Amitriptyline
- TCA (sedating)
- Useful in chronic pain, migraines, and insomnia
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Features of Imipramine
- TCA
- used in enuresis and panic disorder
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Features of Clomipramine
- TCA
- most serotonin specific
- used for OCD
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Features of Nortriptyline
- TCA
- least likely to cause orthostatic hypotension
- used for chronic pain
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Treatment for TCA overdose
IV sodium bicarbonate
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MAOIs prevent the breakdown of...
norepi, serotinin, dopamine, and tyramine
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MAO-A preferentially deactivates...
serotonin
also dopamine and tyramine
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MAO-B preferentially deactivates
norepi/epi
also dopamine and tyramine
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Commen MAOIs
- Phenelzine
- Tranylcypromine
- Isocarboxazid
- Selegeline
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To aid in treating serotonin syndrome
calciam channel blockers (nifedipine). Monitor carefully if use chlorpromazine or phentolamine
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Antidepressants that treat... OCD
- SSRIs (high doses)
- TCAs (clomipramine)
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Antidepressants that treat... Panic disorders
- SSRIs
- TCAs (imipramine)
- MAOIs
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Antidepressants that treat... Eating disorders
- SSRIs (high dose)
- TCAs
- MAOIs
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Antidepressants that treat... social phobia
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Antidepressants that treat... GAD
- SSRIs
- SNRIs (venlafaxine)
- TCAs
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Antidepressants that treat... IBS
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Antidepressants that treat... PTSD
SSRIs
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Antidepressants that treat... Enuresis
TCAs (imipramine)
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Antidepressants that treat... Neuropathic pain
- TCAs (amitriptyline and nortriptyline)
- Duloxetine
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Antidepressants that treat... chronic pain
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Antidepressants that treat... Fibromyalgia
SSRIs
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Antidepressants that treat... Migrane headaches
- TCAs (amitriptyline)
- SSRIs
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Antidepressants that treat... PMDD
SSRIs
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Antidepressants that treat... depressive phase of bipolar
SSRIs
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Antidepressants that treat... insomnia
- Mirtazapine
- TCAs (amitriptyline)
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Atypical vs Typical antidepressant MOIs
- typical block dopamine receptors (D2)
- atypical block D2 and serotonin (2A) receptors
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When presribing Lithium, check
lithium levels, creatinine, and thyroid levels
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Low potency typical antipsychotics
- higher incidence of anticholinergic and antimuscarinic side effects
- QTc prolongation
- Chlorpromazine - orthostaic hypotension, blue skin discoloration, pohosensitivity, can treat nausea, vomitting, and irretractable hiccups
- Thioridazine - retinitis pigmentosa
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High potency typical antipsychotics
- less sedation, orthostatic hypotension, and anticholinergic effects, greater risk for EPS and tardive dyskinesia
- Haloperidol
- Fluphenazine
- Pimozide - cardiac side effects
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Positive symptoms of schizophrenia treated via
mesolimbic pathway: nucleus accumbens, fornix, amygdala, hippocampus
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Negative symptoms of schizophrenia via...
mesocortical pathway
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Symptoms of Neuroleptic Malignant Syndrome
- FALTERED:
- Fever
- Autonomic instability
- Leukicytosis
- Tremor
- Elevated CPK
- Rigidity (lead pipe)
- Excessive sweating
- Delerium
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Onset of neuroleptic side effects
- hours to days - acute dystonia
- days to months - EPS/akathisia
- months to years - tardive dyskinesia
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Clozapine
- great in refractory schizo, only antipsychotic shown to decrease risk of suicide
- tachycardia, hypersalivation
- more anticholinergic side effects than atypicals or high potency typical
- can develop myocarditis
- agranulocytosis - must stop if absolute neutrophil count drops below 1500
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Risperidone
- can increase prolactin
- orthostatic hypotension and reflex tachycardia
-
Quetiapine
sedation and orthostatic hypotension
-
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Aripiprazole
- Unique mechanism of partial D2 agonism
- less potential for weight gain
- more activating and less sedating
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Common side effects of atypical antipsychotics
- metabolic syndrome
- weight gain
- hyperlipidemia
- hyperglycemia
- liver function
- QTc prolongation
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Lithium
- metabolized by kidney
- Prior to initiating, do ECG, basic chemistry, thyroid function tests, CBC, pregnancy test
- onset of action 5-7 days
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Factors that affect lithium levels
- NSAIDS (decrease)
- Aspirin
- Dehydration (increase)
- Salt deprivation (increase)
- Sweating - salt loss (increase)
- Impaired renal function (increase)
- Diuretics, esp thiazides
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Carbamazepine
- anticonvulsant
- tx mixed episodes and rapid-cycline bipolar disorder (less for depressed phase)
- tx trigeminal neuralgia
- acts by blocking Na channels and inhibiting action potentials
- Onset of action 5-7 days
- Must do CBC and LFTs before treatment, monitor regularly - leukocytosis esp dangerous if given with other meds that lower WBC (clozapine)
- Side effects - GI, sedation, ataxia, Steven-Johnson syndrome, leukopenia, hyponatremia, aplastic anemia, agranulocytosis, elevation of liver enzymes causing hepatitis, TERATOGENIC (neural tube defects)
- Autoinduction of CYP450
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Valproic Acid
- tx mixed and rapid-cycling bipolar
- Must montor LFTs and CBC
- Levels checked after 3-5 days (normal 50-150)
- Side effects: GI, weight gain, sedation, alopecia, pancreatitis, hepatotoxicity, increased ammonia, thrombocytopenia, teratogenic (neural tube)
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Lamotrigine (Lamictol)
- tx bipolar depression (not mania)
- works on Na channels that modulate glutamate and aspartate
- May cause Stevens-Johnson syndrome by 4-6 weeks
Note: Valproate will increase lamotrigine levels, and lamotrigine with decrease valproate levels
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Oxcarbazepine
mood stabalizer like carbamasepine, but less risk of rash and hepatotoxicity
-
Gabapentin
often used adjunctively to help with anxiety and sleep
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Topiramate
- tx impulse control disorder and anxiety
- weight loss, hypochloremic non-anion gap metabolic acidosis, kidney stones, cognitive slowing
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Benzos not metabolized by liver
- LOT:
- Lorazepam
- Oxazepam
- Temazepam
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Diazepam
- Valium
- Rapid onset, long acting
- used for detox
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Clonazepam
- tx anxiety, panic attacks
- long acting
- avoid with renal dysfunction
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Alprazolam
- Xanax
- tx anxiety, panic attacks
- shot onset of action causes euphoria, high abuse potential
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Lorazepam
- Ativan
- tx panic attacks, detox, agitation
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Triazolam
- short acting
- tx insomnia, medical and surgical settings
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Tx benzo overdose with...
flumazenil (must be done slowly so withdrawal isn't too quick)
-
Midazolam
- Versed
- used in medical and surgical settings
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Zolpidem/zaleplon.eszopiclone
- non-benzo hypnotics
- selective receptor binding to bendo receptor 1, which is responsible for sedation
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Ramelteon
- non-benzzo hypnotic
- selective melatonin MT1 and MT2 agonist
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Buspirone
- partial agonist of 5HT-1A receptor
- takes 1-2 weeks for effect
- tx anxiety when combined with SSRI, useful in alcoholics bc doesn't potentiate CNS depression of alcohol
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Propanolol
tx autonomic effects of panic attacks or performanch anxiety, or to tx akathisia from typical antipsychotics
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Meds that may cause psychosis
- sympathomimetics
- analgesics
- antibiotics (isoniazid)
- anticholinergis
- anticonvulsants
- antihistamines
- corticosteroids
- anti-parkinsonian meds
- esp: isoniazid, cimetidine, steroids
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Meds that may cause agitation/confusion/delerium
- antipsychotics
- antidepressants
- antiarrhythmics
- antineoplastics
- corticosteroids
- cardiac glycosides
- esp: procainamide, quinidine, albuterol
- NSAIDs
- antiasthmatics
- antibiotics
- antihypertensives
- antiparkinsonian mends
- thyroid hormones
- esp: albuterol, quinidine, procainamide, steroids
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Meds that may cause depression
- antihypertensives
- antiparkinsonian agents
- corticosteroids
- Ca channel blockers
- NSAIDs
- antibiotics
- peptic ulcer drugs
- esp: tetracycline, nifedipine, verapamil, cimetidine
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Meds that may cause anxiety
- sympathomimetics
- antiasthmatics
- antiparkosonian meds
- hypoglycemic
- NSAIDs
- thyroid hormones
- esp: albuterol, steroids
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EPS
- Parkonsonian - masklike face, cog-wheel rigidity, pill-rolling tremor
- akathisia - restlessness and agitation
- dystonia - sustained contraction of muscles of neck, tongue, eyes, diaphragm
- Occur with high potency typical antipsychotics
- tx: benztropine
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Major complications of TCAs
- Cardiotoxicity
- Convulsions
- Coma
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