Antidepressants Flashcards
Fluoxetine differs from the other members of the class (SSRIs) in 3 respects.
GO!
- it has a much longer half-life (50 hours).
- the metabolite of the S-enantiomer, S-norfluoxetine, is as potent as the parent compound. The half-life of the metabolite is quite long, averaging 10 days.
- can be used to treat bulimia and bipolar and (along with Sertraline) Premenstrual dysphoric disorder
list Monoamine oxidase inhibitors (MAOIs)-mitochondrial enzyme
“PI-TS”
which one is selective for MAO-B?
hydrazine derivatives
phenelzine and isocarboxazid
non-hydrazines
tranylcypromine and selegiline.
selegiline = selective for MAO-B
what class of antidepressants is MIRTAZAPINE
NORADRENERGIC & SPECIFIC SEROTONERGIC ANTIDEPRESSANTS (NASSA)
list the SELECTIVE SEROTONIN-REUPTAKE INHIBITORS (SSRIs)
CITALOPRAM
ESCITALOPRAM (S-enantiomer of citalopram)
FLUOXETINE (prototype) (-)CYP2D6
PAROXETINE (-)CYP2D6 (also undergo fecal excretion, in addition to renal like the rest)
FLUVOXAMINE-just inhibits all the CYPs
SERTRALINE (also undergo fecal excretion in addition ro renal like the rest)
The combination of a MAO inhibitor with which drugs can result in a life-threatening serotonin syndrome.
SSRIs
SNRIs
TCAs
St. Johns worts
Meperidine & Dextromethorphan (opioid analgesic)
agonists at opioid receptors (μ = β-endorphin, δ = enkephalin, κ = dynorphin)
An irreversible MAO inhibitor with a serotonergic agent is the most toxic reported combination,
side note: OTC cold preparations that contain pseudoephedrine and phenylpropanolamine are contraindicated in patients taking MAO inhibitors.
which SSRI is the only one to undergo significant first-pass metabolism?
sertraline
which
α1 selective (-osin ending) &
Nonselective a-blockers
are helpful in the management of tyramine-induced hypertension.
Phentolamine or prazosin are helpful in the management of tyramine-induced hypertension.
which drug because of its long half-life, should be discontinued 4-5 weeks (instead of the usual 2 weeks) before a MAO inhibitor is started
Fluoxetine (SSRI)-selective for SERT
which SNRI is being described
is a potent inhibitor of 5HT uptake and, at higher doses, an inhibitor of norepinephrine uptake.
It also inhibits reuptake of dopamine very weakly.
At lower therapeutic doses it behaves like an SSRI. (Free from α1, cholinergic, and H1 receptor blocking properties)
Venlafaxine (short half life)
on the other hand, Duloxetine (longer half life) inhibits serotonin and norepinephrine reuptake at all doses.
which 3 SSRI’s have have low potential for interactions.
Citalopram,
Escitalopram
Sertraline
• Sexual effects in TCAs are common, particularly with highly serotonergic agents such as…
(1)
clomipramine.
DRUG INTERACTIONS with Lithium:
how do the following drugs interact with lithium
Diuretics
ACE inhibitors and ARBs
NSAIDs
Renal clearance of lithium is reduced by diuretics, and doses may need to be reduced.
By altering renal perfusion, NSAIDs can facilitate renal proximal tubular resorption of lithium and thereby increase lithium serum concentrations
ACE inhibitors and ARBs also can cause lithium retention.
5HT2 ANTAGONIST/REUPTAKE INHIBITORS (SARIs), list them (2) and which one is discontinued probs due to its hepatoxicity
- TRAZODONE
TRAZZZZZODONE bc Extremely sedating. Excellent hypnotic. The most common use of trazodone in current practice is as an unlabeled hypnotic.
- NEFAZODONE (discontinuted)
which SSRI is an inhibitor of CYP1A2, CYP2C19 and CYP3A4 and therefore it also has high potential for drug interactions.
Fluvoxamine
which MAO inhibitor is being described
- selective for MAO-B
- approved for treatment of early Parkinson’s disease.
- also antidepressant effects, particularly at high doses that also inhibit MAO-A.
- its the first antidepressant available in a transdermal delivery system.
- better tolerated and safer. It is unlikely to lead to tyramine-induced hypertensive crisis.
The MAO-B inhibitor selegiline
which antidepressant is approved for treatment of bulimia.
Fluoxetine (SSRI)
what 2 anti-epileptic drugs ALTERNATIVES TO LITHIUM
valproate and carbamazepine
Liver function and CBC should be monitored in patients taking valproic acid.
CBC should be monitored in patients taking carbamazepine.
list the SEROTONIN & NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs)
VENLAFAXINE
DULOXETINE
These agents may be effective in treating depression in patients in whom SSRIs are ineffective.
which SNRI was the first antidepressant to be given FDA approval for the treatment of pain associated with diabetic neuropathy and fibromyalgia.
duloxetine
what class of Antidepressants is usually considered first line for the treatment of premature ejaculation?
SSRIs
DISCONTINUATION SYNDROME is most likely to occur with a short half-life drug, such as________
It is less likely to occur with _____________ , due to its long half-life
paroxetine
fluoxetine
__(antidepressant________was approved in 1997 as a treatment for smoking cessation and appears to be as effective as nicotine patches in smoking cessation.
Bupropion
what occurs during a Bupropion overdose?
OVERDOSE
Bupropion is associated with seizures in overdose.
Contraindicated in patients with seizure disorder,
out of the SSRI’s, which are the 2 oddballs with respect to metabolism?
Excretion of the SSRIs is primarily through the kidneys, except for:
paroxetine and sertraline, which also undergo fecal excretion (35 and 50 %).
which 3 ATYPICAL ANTIPSYCHOTICS can be used AS ADJUNCTS FOR MAJOR DEPRESSION
Quetiapine
Aripiprazole
Olanzapine
have been approved for adjunctive treatment of major depressive disorder.
list the 2 SSRIs which are potent inhibitors of CYP2D6 and therefore have high potential for drug interactions.
Fluoxetine and paroxetine
CYP2D6 is responsible for the elimination of
TCAs
neuroleptic drugs
some antiarrhythmic
β-blockers.
• TCAs block:
(4)
- α-adrenergic receptors
- Muscarinic receptors
- Histamine receptors
- Cardiac fast sodium channels
blurred vision, xerostomia, urinary retention, constipation and aggravation of narrow-angle glaucoma are AE of TCA due to their blockade at what site
Blockade of muscarinic receptors
PREMENSTRUAL DYSPHORIC DISORDER, which 2 antidepressants can be used
both are SSRI’s
Fluoxetine and sertraline (SSRI’s)
are SSRIs effective for chronic pain?
Nerp
List the TCA’s
AMITRIPTYLINE
NORTRIPTYLINE
DESIPRAMINE
IMIPRAMINE
CLOMIPRAMINE
________ assists in decreasing the craving and attenuating the withdrawal symptoms for nicotine in tobacco users. (used for smoking cessation)
and is not associated to sexual dysfunction problems which occur with SSRIs because it lacks the serotonergic component.
name that Class/Specific Drug
NOREPINEPHRINE & DOPAMINE REUPTAKE INHIBITORS (NDRIs)
Bupropion
(only one in this category)
whats the most common cause of death in patients with TCA intoxication?
Blockade of cardiac fast sodium channels may cause arrhythmias:
during overdose of TCAs, which can induce lethal arrhythmias________ is useful in reversing conduction block.
Sodium bicarbonate
Normally degraded by monoamine oxidase (MAO). Levels in patients taking MAO inhibitors who ingest tyramine-rich foods (eg, cheese, wine).
explain this mechanism
*which MAO inhibitor is least likely to cause tyramine induced hypertensive crisis
Excess tyramine enters presynaptic vesicles and displaces other neurotransmitters (eg, NE) active presynaptic neurotransmitters diffusion
of neurotransmitters into synaptic cleft sympathetic stimulation. Classically results in a hypertensive crisis.
selegiline transdermal patch
the SNRI Duloxetine, in addition to being used for Depression refractory to SSRI’s is also used to treat
- diabetic neuropathy
- fibromyalgia
