Antidepressant Pharm Flashcards
Name the SSRIs
Fluoxetine (Prozac), Sertraline (Zoloft), Paroxetine (Paxil), Citalopram (Celexa), Fluvoxamine (Luvox), Escitalopram (Lexapro)
SSRIs that are isomers and have similar SE/metabolism profiles
citalopram and escitalopram
Block the presynaptic serotonin reuptake pump. Increases the time that serotonin is available in the synapse. Increases postsynaptic receptor occupancy
SSRIs
SSRI that has an active metabolite
fluoxetine (Prozac)
General elimination half life range for SSRIs
20-30 hours. Except fluoxetine (Prozac)- 4-16 days
Which SSRIs inhibit liver enzymes less than other SSRIs? (ie good when you’re worried about drug-drug interactions)
Citalopram and escitalopram
What happens when another drug is introduced that also works at same enzyme sites as first drug?
Stays in system longer, more chance of toxicty, overdose, greater side effects
Why are SSRIs contraindicated if taking MAOis within 2 weeks?
risk of serotonin syndrome
Top three side effects of SSRIs
sexual dysfunction, drowsiness, weight gain
Sx include: dysphoria, dizziness, GI distress, fatigue, chills, myalgias. More common with fluvoxamine and paroxetine
serotonin withdrawal syndrome
How long should someone be on SSRI for depression?
at least 1 yr after resolution of symptoms otherwise there may be recurrence
Risk associated with citalopram
QT prolongation at doses over 40mg or at 20mg for >60yr/hepatic impairment/cimetidine
Advantages of fluoxetine (Prozac)
capsule for weekly dosing and least problems with weight gain
SSRIs CI with Tamoxifen
fluoxetine (Prozac), paroxetine (Paxil),
SSRI with significant withdrawal symptoms
Paroxetine (Paxil)
SSRI more likely to cause diarrhea than others
Sertaline (Zoloft)
Name the SNRIs
Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Desvenlafaxine (Pristiq)
use for treatment of depression if intolerable side effects or poor response to first line SSRI therapy
SNRIs
inhibit the reuptake of norepinephrine and serotonin. leads to increased stimulation of the post-synaptic receptors
SNRIs
Food decreases the rate of absorption but not the degree of absorption (ie less side effects)
SNRIs
Most common side effects of SNRIs
nausea, dizziness, diaphoresis
SNRI that most commonly causes nausea. Monitor for elevation of blood pressure
Desvenlafaxine (Pristiq)
SNRI that is CI in uncontrolled angle closure glaucoma, severe renal or liver impairment. Indicated for diabetic neuropathy and fibromyalgia
Duloxetine (Cymbalta)
SNRI with increased risk of upper GI bleed, slow taper off of it to avoid withdrawal symptoms, can cause QT prolongation
Venlafaxine (Effexor)
Usually avoided in clinical practice for the treatment of depression due to anticholinergic side effects
TCAs
Highly sedating so are often used for insomnia and for those with night time neuropathic pain or fibromyalgia
TCAs
Inhibit reuptake of serotonin and norepinephrine. Also block muscarinic, histamine and alpha-adrenergic receptors
TCAs
Group of medications whose cardiac SE include: Heart block, ventricular arrhythmias, sudden death
TCAs
what patients do you need to screen for cardiac conduction system disease with an EKG before initiation of TCAs?
patients >40yrs
Lower the seizure threshold, Increase in bone fractures, dangerous in overdose due to their broad spectrum
TCAs
Block histamine receptors causing sedation, increased appetite, confusion, delirium
TCAs
Block acetylcholine receptors causing blurred vision, constipation, dry mouth, urinary retention
TCAs
Name the MAOi
Phenelzine (Nardil). Tranylcypromine (Parnate)
Medication group most likely to cause serotonin syndrome. Need to avoid tyramine containing foods
MAOi
Serotonin antagonist and reuptake inhibitors. Good for sleep at low doses. If tolerated – functions as an antidepressant at higher doses
Trazodone (Desyrel)
Uses include: Major Depressive disorder, ADHD, Smoking cessation
Bupropion (Wellbutrin)
Structurally related to amphetamine. Can cause anxiety. Lowers the seizure threshold. Avoid in bulemia
Bupropion
No withdrawal syndrome upon discontinuation or sexual dsyfxn.
Bupropion
Mildly stimulating so good for patients with fatigue, hypersomnia, or poor concentration
Bupropion
Blocks adrenergic receptors leading to an increased release of norepinephrine and serotonin. Blocks serotonergic receptors and increases serotonin mediated neurotransmission
Mirtazapine (Remeron)
Used off-label for insomnia. Used off-label for appetite stimulant. Good for patients with nausea
Mirtazapine
classically associated with the simultaneous administration of two serotonergic agents. Majority present within 24 hrs.
serotonin syndrome
Sx include: hyperthermia, agitation, tremor, clonus, dilated pupils, diaphoresis, DTR hyperreflexia, flushed skin
serotonin syndrome
What does HARM stand for with serotonin syndrome?
hyperthermia, autonomic instability, rigidity, myoclonus
Tx for serotonin syndrome
DC serotonin agents, sedate using benzos, O2, Fluids, avoid acetaminophen.
At what temp of serotonin syndrome do you need to intubate and sedate immediately?
> 41.1C (105.98F)
If benzos don’t work, what is the antidotes for serotonin syndrome?
cyproheptadine
