Antidepressants

Question 1

Fluoxetine differs from the other members of the class (SSRIs) in 3 respects.

GO!

Answer 1

1. it has a much longer half-life (50 hours).
2. 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.
3. can be used to treat bulimia and bipolar and (along with Sertraline) Premenstrual dysphoric disorder

Question 2

list Monoamine oxidase inhibitors (MAOIs)-mitochondrial enzyme

“PI-TS”

which one is selective for MAO-B?

Answer 2

hydrazine derivatives

phenelzine and isocarboxazid

non-hydrazines

tranylcypromine and selegiline.

selegiline = selective for MAO-B

Question 3

what class of antidepressants is MIRTAZAPINE

Answer 3

NORADRENERGIC & SPECIFIC SEROTONERGIC ANTIDEPRESSANTS (NASSA)

Question 4

list the SELECTIVE SEROTONIN-REUPTAKE INHIBITORS (SSRIs)

Answer 4

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)

Question 5

The combination of a MAO inhibitor with which drugs can result in a life-threatening serotonin syndrome.

Answer 5

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.

Question 6

which SSRI is the only one to undergo significant first-pass metabolism?

Answer 6

sertraline

Question 7

which

α1 selective (-osin ending) &

Nonselective a-blockers

are helpful in the management of tyramine-induced hypertension.

Answer 7

Phentolamine or prazosin are helpful in the management of tyramine-induced hypertension.

Question 8

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

Answer 8

Fluoxetine (SSRI)-selective for SERT

Question 9

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)

Answer 9

Venlafaxine (short half life)

on the other hand, Duloxetine (longer half life) inhibits serotonin and norepinephrine reuptake at all doses.

Question 10

which 3 SSRI’s have have low potential for interactions.

Answer 10

Citalopram,

Escitalopram

Sertraline

Question 11

• Sexual effects in TCAs are common, particularly with highly serotonergic agents such as…

(1)

Answer 11

clomipramine.

Question 12

DRUG INTERACTIONS with Lithium:

how do the following drugs interact with lithium

Diuretics

ACE inhibitors and ARBs

NSAIDs

Answer 12

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.

Question 13

5HT2 ANTAGONIST/REUPTAKE INHIBITORS (SARIs), list them (2) and which one is discontinued probs due to its hepatoxicity

Answer 13

1. TRAZODONE

TRAZZZZZODONE bc Extremely sedating. Excellent hypnotic. The most common use of trazodone in current practice is as an unlabeled hypnotic.

2. NEFAZODONE (discontinuted)

Question 15

which SSRI is an inhibitor of CYP1A2, CYP2C19 and CYP3A4 and therefore it also has high potential for drug interactions.

Answer 15

Fluvoxamine

Question 16

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.

Answer 16

The MAO-B inhibitor selegiline

Question 17

which antidepressant is approved for treatment of bulimia.

Answer 17

Fluoxetine (SSRI)

Question 18

what 2 anti-epileptic drugs ALTERNATIVES TO LITHIUM

Answer 18

valproate and carbamazepine

Liver function and CBC should be monitored in patients taking valproic acid.

CBC should be monitored in patients taking carbamazepine.

Question 19

list the SEROTONIN & NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs)

Answer 19

VENLAFAXINE

DULOXETINE

These agents may be effective in treating depression in patients in whom SSRIs are ineffective.

Question 20

which SNRI was the first antidepressant to be given FDA approval for the treatment of pain associated with diabetic neuropathy and fibromyalgia.

Answer 20

duloxetine

Question 21

what class of Antidepressants is usually considered first line for the treatment of premature ejaculation?

Answer 21

SSRIs

Question 22

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

Answer 22

paroxetine

fluoxetine

Question 23

__(antidepressant________was approved in 1997 as a treatment for smoking cessation and appears to be as effective as nicotine patches in smoking cessation.

Answer 23

Bupropion

Question 24

what occurs during a Bupropion overdose?

Answer 24

OVERDOSE

Bupropion is associated with seizures in overdose.

Contraindicated in patients with seizure disorder,

Question 25

out of the SSRI’s, which are the 2 oddballs with respect to metabolism?

Answer 25

Excretion of the SSRIs is primarily through the kidneys, except for:

paroxetine and sertraline, which also undergo fecal excretion (35 and 50 %).

Question 26

which 3 ATYPICAL ANTIPSYCHOTICS can be used AS ADJUNCTS FOR MAJOR DEPRESSION

Answer 26

Quetiapine

Aripiprazole

Olanzapine

have been approved for adjunctive treatment of major depressive disorder.

Question 27

list the 2 SSRIs which are potent inhibitors of CYP2D6 and therefore have high potential for drug interactions.

Answer 27

Fluoxetine and paroxetine

CYP2D6 is responsible for the elimination of

TCAs

neuroleptic drugs

some antiarrhythmic

β-blockers.

Question 28

• TCAs block:

(4)

Answer 28

• α-adrenergic receptors
• Muscarinic receptors
• Histamine receptors
• Cardiac fast sodium channels

Question 29

blurred vision, xerostomia, urinary retention, constipation and aggravation of narrow-angle glaucoma are AE of TCA due to their blockade at what site

Answer 29

Blockade of muscarinic receptors

Question 30

PREMENSTRUAL DYSPHORIC DISORDER, which 2 antidepressants can be used

both are SSRI’s

Answer 30

Fluoxetine and sertraline (SSRI’s)

Question 31

are SSRIs effective for chronic pain?

Answer 31

Nerp

Question 32

List the TCA’s

Answer 32

AMITRIPTYLINE

NORTRIPTYLINE

DESIPRAMINE

IMIPRAMINE

CLOMIPRAMINE

Question 33

________ 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

Answer 33

NOREPINEPHRINE & DOPAMINE REUPTAKE INHIBITORS (NDRIs)

Bupropion

(only one in this category)

Question 34

whats the most common cause of death in patients with TCA intoxication?

Answer 34

Blockade of cardiac fast sodium channels may cause arrhythmias:

Question 35

during overdose of TCAs, which can induce lethal arrhythmias________ is useful in reversing conduction block.

Answer 35

Sodium bicarbonate

Question 36

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

Answer 36

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 ​

Question 37

the SNRI Duloxetine, in addition to being used for Depression refractory to SSRI’s is also used to treat

Answer 37

1. diabetic neuropathy
2. fibromyalgia