CNS Part 3 Flashcards
(24 cards)
What are the Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs)?
Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Desvenlafaxine (Pristiq)
What is the mechanism of actions of SNRIs?
treat depression by initially blocking presynaptic serotonin and NE transporter proteins. This inhibits reuptake of these neurotransmitters and leads to increased stimulation of post-synaptic receptors.
Which serotonins are believed to be responsible for chronic pain?
NE and serotonin
What other uses are there for taking SNRIs is there?
SNRIs have become a useful drug class in persons who are unable to take or cannot tolerate adverse effects of opioids, anti-inflammatories, or anticonvulsants for chronic pain relief.
How do you remember to dose Venlafaxine?
A convenient way to remember how to dose this drug (and other SNRIs) is that at a low dose, the drug acts like an SSRI; at a medium dose, it blocks NE; and at a high dose the dopamine pump is activated to block dopamine reuptake
What is the mechanism of action of venlafaxine?
dual serotonin and NE inhibitor, similar to the tricyclic antidepressants, that also weakly blocks dopamine reuptake thus increasing available serotonin, NE and dopamine at the synapses
What are the indications of venlafaxine?
Major depression
Generalized anxiety disorder
Social anxiety disorder
Panic disorder
Migraine headache prophylaxis (off-label)
What is the adverse effects of venlafaxine?
CNS-Headache, nervousness, somnolence, insomnia
GI- Nausea, weight loss/anorexia
Sweating
Sexual dysfunction
Diastolic hypertension
Hyponatremia (in elderly)
Neonatal withdrawal syndrome
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What is the mechanism of action of duloxetine?
duloxetine is a serotonin and norepinephrine reuptake inhibitor; it also weakly inhibits dopamine reuptake
What are the indications of duloxetine?
Major Depression
Generalized Anxiety Disorder
Diabetic peripheral neuropathy pain
Fibromyalgia
Chronic musculoskeletal pain (osteoarthritis, lower back pain)
What are the PK effects of duloxetine?
Although food reduces the rate of absorption of duloxetine, food intake does not affect drug distribution and may alleviate nausea commonly associated with this drug. This drug is highly protein bound, and its half-life is 12 hours.
What are the adverse effects of duloxetine?
Nausea
Headache, somnolence, or insomnia
Dry mouth
Sweating
Blurred vision
What are the atypical antidepressants?
Bupropion
Nefazodone
Trazodone
Mirtazapine
Maprotiline
What is the actions of Bupropion?
, it exerts its effect by blocking NE and serotonin transport and also seems to be more selective for blocking dopamine transport that other agents
What are the indications of Bupropion?
Acts as stimulant and suppresses appetite
Indicated for major depression, seasonal affective disorder, tobacco dependence, obesity, low libido
When do the effects of Bupropion take effect?
1-3 weeks
When taking bupropion for smoking cessation, when should therapy start?
therapy should start at least 1 week before targeted quit date and efficacy of maintenance therapy has been demonstrated for up to 6 months.
What are the adverse effects of bupropion?
Can cause seizures
Dry mouth
Nausea
Insomnia
Dizziness
Anxiety/agitation
Tremor
What is the mechanism of action of MAO-Is?
inhibitors act by irreversibly blocking the action of the enzyme monoamine oxidase subtypes A and B. These enzyme subtypes are involved in the metabolism of the monoamine serotonin and catecholamine neurotransmitters such as epinephrine, norepinephrine, and dopamine.
What are the monoamine oxidase inhibitors (MAO-I)?
Phenelzine
Tranycypromine
Isocarbozazide
Selegiline
What are the therapeutic uses of MAO-Is?
Depression
Second-line uses
- Bulimia nervosa
- Obsessive-compulsive disorders
- Panic attacks
Why should MAO-Is not be given with other antidepressants?
The risk of hypertensive crisis or serotonin syndrome
What are the adverse effects of MAO-Is?
CNS: delirium, dizziness, fatigue, fever, HA
Orthostatic hypotension
Serotonin syndrome
Hypertensive crisis from dietary tyramine
Anticholinergic effects: blurred vision, urinary retention, dry mouth, constipation
Weight gain
Which antidepressant is most likely associated with risk of seizure?
Bupropion
