Tag: Selective Serotonin Reuptake Inhibitors (SSRI)

Selective Serotonin Reuptake Inhibitors (SSRI)

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI)

Q. 1 Inhibitors of serotonin (5-HT) uptake, such as paroxetine, can cause clinically significant drug interactions with which of the following?
 A Diazepam
 B Digoxin
 C Halothane
 D Tranylcypromine
 
Q. 1 Inhibitors of serotonin (5-HT) uptake, such as paroxetine, can cause clinically significant drug interactions with which of the following?
 A Diazepam
 B Digoxin
 C Halothane
 D Tranylcypromine
 
Ans. D

Explanation:

Fatalities have been reported when fluxetine and MAO  inhibitors  (MAOI’s)  such  as tranylcypromine have been given simultaneously. The MAOIs should be stopped at least 2weeks before the administration of fluoxetine or paroxetine. Note that a similar severe interaction can occur between tricyclic antidepressants and MAOIs; the same warning against “overlapping” the two classes of drugs, and allowing one to “Clear” the system completely before starting the other, applies.


Q. 2 Not a selective serotonin reuptake inhibitor:
 A Flouxetine
 B Fluvoxamine
 C Buspirone
 D Citalopram
Q. 2 Not a selective serotonin reuptake inhibitor:
 A Flouxetine
 B Fluvoxamine
 C Buspirone
 D Citalopram
Ans. C

Explanation:

Buspirone


Q. 3

Fluoxetine is a potent reuptake blocker of this substance?

 A

Morphine

 B

Serotonin

 C

Norepinephrine

 D

Cholecystokinin

Q. 3

Fluoxetine is a potent reuptake blocker of this substance?

 A

Morphine

 B

Serotonin

 C

Norepinephrine

 D

Cholecystokinin

Ans. B

Explanation:

Serotonin 

Quiz In Between


Q. 4

The pharmacokinetics of Paroxetine include its ability to be easily absorbed after oral administration in healthy volunteers even after food is ingested.  Which of the following is TRUE?

 A

Main portion of the medication resides in system circulation

 B

Little of the medication is absorbed into the tissues

 C

Less than 1% of the drug is in systemic circulation owing to extensive distribution in body tissues.

 D

Less than 25% is eliminated by the kidneys

Q. 4

The pharmacokinetics of Paroxetine include its ability to be easily absorbed after oral administration in healthy volunteers even after food is ingested.  Which of the following is TRUE?

 A

Main portion of the medication resides in system circulation

 B

Little of the medication is absorbed into the tissues

 C

Less than 1% of the drug is in systemic circulation owing to extensive distribution in body tissues.

 D

Less than 25% is eliminated by the kidneys

Ans. C

Explanation:

The major portion of paroxetine is distributed into the tissues and less than 1% if in systemic circulation while 64% if eliminated by the kidneys and 36% in the feces. The primary effect is believed to be on brain neurons because of its qualities as a selective serotonin reuptake inhibitor (SSRI).
 
Ref: Pollock B.G., Semla T.P., Forsyth C.E. (2009). Chapter 63. Psychoactive Drug Therapy. In J.B. Halter, J.G. Ouslander, M.E. Tinetti, S. Studenski, K.P. High, S. Asthana (Eds), Hazzard’s Geriatric Medicine and Gerontology, 6e.

Q. 5

Mode of action of fluoxetine is

 A

GABA inhibition

 B

Adrenergic neuron blocking action

 C

Inhibition of axonal uptake of 5HT

 D

Adrenergic stimulation

Q. 5

Mode of action of fluoxetine is

 A

GABA inhibition

 B

Adrenergic neuron blocking action

 C

Inhibition of axonal uptake of 5HT

 D

Adrenergic stimulation

Ans. C

Explanation:

C i.e. Inhibition of axonal uptake of 5 HT


Q. 6

Side effect of SSRI

 A

Nausea

 B

Diarrhea

 C

Weight gain

 D

All

Q. 6

Side effect of SSRI

 A

Nausea

 B

Diarrhea

 C

Weight gain

 D

All

Ans. D

Explanation:

A i.e. Nausea; B i.e. Diarrhea; C i.e. Weight gain

Quiz In Between


Q. 7

The common side effect with fluoxetine therapy is:

 A

Seizure

 B

Anxiety

 C

Hypotension

 D

All

Q. 7

The common side effect with fluoxetine therapy is:

 A

Seizure

 B

Anxiety

 C

Hypotension

 D

All

Ans. B

Explanation:

B i.e. Anxiety 


Q. 8

Side effects of fluoxetine are A/E

 A

Weight gain

 B

Sweating

 C

Urinary retention

 D

Diarrhoea

Q. 8

Side effects of fluoxetine are A/E

 A

Weight gain

 B

Sweating

 C

Urinary retention

 D

Diarrhoea

Ans. C

Explanation:

C i.e. Urinary retention

SSRIs (ex. Fluoxetine) are almost devoid of sedation, hypotension, cardiac arrhythmia, seizure precipitation & anticholinergic side effectsQ, such as dry mouth, bad taste, urinary retention, constipation & epigastric distressQ when compared to tricyclic antidepressants.

–    Least sedative antidepressants are – Venlafaxine (atypical), Tianeptine & Citalopram (SSRI) > other SSRIs fluoxetine, fluvoxemine, paroxetine, sertraline)Q.

At that time (1993), Selective serotonin reuptake inhibitors fluoxetine, fluvoxamine, paroxetine, Sertraline & Citolapram were the latest antidepressant. Now Venlafaxine, Nifazodone, Reboxetine, Mirtazapine, Tianeptine are novel antidepressants.

–  Fluoxetine is a longest acting SSRI (Selective serotonin reuptake inhibitor). It is devoid of anticholinergic, arrythmogenic, sedative (abuse liability) & Hypotensive side effectsQ. It has new constellation of mild S/E viz – Nervousness, Anxiety, Insomnia, Anorexia, Nausea, DiarrheaQ & Headache, Weight lossQ. Fluoxetine, by inhibiting drug metabolism can elevate drug levels of TCA & Haloperidol to dangerous level.

–  Gastrointestinal S/E of SSRI’s are anorexia, nausea, vomiting, diarrheoa. Anorexia is most common in fluoxetine & weight loss begin as soon as drug is taken & peak at 20 weeks, after which weight often returns to baseline. Although most patient loose weight but some person gain weight while taken fluoxetine. (Kaplan & Sadock’s – Synopsis of Psychiatry 9/e P. 1099)

–  Buprenorphine & Dextroprophoxyphene are opioids & have abuse liability.

–  Increased psychomotor activity like anxiety, akathesia, agitation and insomnia is seen in one quarter of persons initiating treatment with SSRIs specifically fluoxetine.

Tianeptine is an antidepressant which increase rather than inhibit 5-HT (Serotonin) uptakeQ.

Treatment of choice for OCD – Behaviour therapyQ. Drug of choice for OCD is fluoxetineQ > ClomipramineQ


Q. 9

Features of serotonin syndrome associated with SSRI & MAOIs are :

 A

Tremors

 B

Agitation

 C

Cardiovascular collapse

 D

All

Q. 9

Features of serotonin syndrome associated with SSRI & MAOIs are :

 A

Tremors

 B

Agitation

 C

Cardiovascular collapse

 D

All

Ans. D

Explanation:

A, B, C i.e. Tremors, Agitation, Cardiovascular collapse

Quiz In Between


Q. 10

A middle aged man presented with pain in back, lack of interest in recreational activities, low mood, lethargy, decreased sleep and appetite for two months. There was no history suggestive of delusions of hallucinations. He did not suffer from any chronic medical illness. There was no family history of psychiatric illness.

Routine investigations including haemogram, renal function tests, liver function tests electrocadiogram did not reveal any abnormality. This patient should be treated with :

 A

Haloperidol

 B

Sertraline.

 C

Alprazolam.

 D

Olanzapine

Q. 10

A middle aged man presented with pain in back, lack of interest in recreational activities, low mood, lethargy, decreased sleep and appetite for two months. There was no history suggestive of delusions of hallucinations. He did not suffer from any chronic medical illness. There was no family history of psychiatric illness.

Routine investigations including haemogram, renal function tests, liver function tests electrocadiogram did not reveal any abnormality. This patient should be treated with :

 A

Haloperidol

 B

Sertraline.

 C

Alprazolam.

 D

Olanzapine

Ans. B

Explanation:

B i.e. Sertraline

The patients in questions are suffering from major depression and only antidepressant given in option is sertraline. Alprazolam is anxiolytic; haloperidol and olanzapine are antipsychotics.


Q. 11

SSRI is first line treatment for :

 A

OCD

 B

Panic disorder

 C

Social phobia

 D

All

Q. 11

SSRI is first line treatment for :

 A

OCD

 B

Panic disorder

 C

Social phobia

 D

All

Ans. D

Explanation:

Ans:D.)All

Selective serotonin reuptake inhibitors (SSRIs) are US-FDA approved drugs of first choice (line) for major Depression, Obscessive – compulsive disorder (OCD), Premenstrual dysphoric disorder, Post traumatic stress disorder (PTSD), Panic disorder, Eating disorder (bulimia nervosa), and Social phobia (social anxiety disorder)Q. Mn-SSRI for “DOPES” is 1st choice.

SSRIs are also used in generalized anxiety disorder, treatment of premature ejaculation (paroxetiene is most useful), body dysmorphic disorders, compulsive buying, & kleptomania.

Psychotherapy (group, supportive) remains the treatment of choice for adjustment disordersQ. And medications are used only to treat specific symptoms for brief periods. Patients with severe anxiety bordering on panic can benefit from anxiolytics (diazepam); those in withdrawn or inhibited states may benefit from short course of psychostimulant drugs; those with signs of decompensation or impending psychosis may be helped by antipsychotic drugs; whereas, SSRIs are useful in treating symptoms of traumatic grief. There is recent trend of increased antidepressant use, however, to augment psychotherupy in adjustment disorder rather than serving as the primary modality. All SSRIs (except fluvoxamine) are US-FDA approved for treatment of major depression. Fluvoxemine is only used for treatment of OCD in US (b/o commercial reasons not d/t therapeutic profile as it is used for major depression in other countries). In US, citalopram is used only in major depression; escitalopram in major depression & GAD; paroxetine is only not used in bulimia nervosa; and setraline is not used in bulimia & GAD. Fluoxetine is not used in GAD, PTSD and social anxiety but is approved for treatment of bipolar depression (with olanzapine).


Q. 12

Which of the following is not a SSRI?

 A

Esclitalopram

 B

Sertraline

 C

Paroxetine

 D

Amitriptyline

Q. 12

Which of the following is not a SSRI?

 A

Esclitalopram

 B

Sertraline

 C

Paroxetine

 D

Amitriptyline

Ans. D

Explanation:

Ans. is ‘d’ i.e., Amitriptyline

SSRIs are

o Fluextine               o Fluvoxamine        o Citalopram

o Sertaline               o Paroxetine           o Escitalopram

Quiz In Between


Q. 13

The common side effect with Fluoxetine therapy is

 A

Seizure

 B

Anxiety

 C

Hypotension

 D

Loose stools

Q. 13

The common side effect with Fluoxetine therapy is

 A

Seizure

 B

Anxiety

 C

Hypotension

 D

Loose stools

Ans. D

Explanation:

Ans. is ‘d’ i.e., Loose stools

o Amongst the given options, option d i.e. is the best answer (read below).

o Most common side effects on long term treatment is sexual dysfunction. However, you should keep in mind sexual dysfunction is the most common side effect on long term use. Otherwise, mused and GI disturbances are the most common side effects.

“Transient nausea is the most frequent complainst with the SSRIs”.    — Katzung

“The prominant side effects with SSRIs are gastrointestinal”.   —KDT

“Gastrointestinal side effects are very common. The most frequent GI complaints are nausea, diarrhea, anorexia, flatulence, dyspepsia”.  — Kaplan & Saddocks

  • So, remember following facts :-

(i)     The most common side effect of SSRIs is transient nausea.

(ii)   If nausea is not given in options, then any other GI symptom (diarrhea, vomiting, anorexia) is the best answer.

(iii)  The most common side effect of SSRIs on long term use is sexual dysfunction.


Q. 14

The drug of choice in obessive compulsive disorder is which one of the following-

 A

Sertraline

 B

Amoxapine

 C

Hydroxyzine

 D

Alprazolam

Q. 14

The drug of choice in obessive compulsive disorder is which one of the following-

 A

Sertraline

 B

Amoxapine

 C

Hydroxyzine

 D

Alprazolam

Ans. A

Explanation:

Ans. is ‘a’ i.e., Sertraline


Q. 15

SSRIs are drug of choice for all of the following conditions except –

 A

Panic attack

 B

Social phobia

 C

Post traumatic stress disorder

 D

Generalized anxiety disorder

Q. 15

SSRIs are drug of choice for all of the following conditions except –

 A

Panic attack

 B

Social phobia

 C

Post traumatic stress disorder

 D

Generalized anxiety disorder

Ans. D

Explanation:

Ans. is ‘d’ i.e., Generalized anxiety disorder

o For generalized anxiety disorder Benzodiazipines are preferred.

Quiz In Between


Q. 16

Drug of choice for obsessive-compulsive disorder is:

March, 2005, September 2009

 A

Sertraline

 B

Alprazolam

 C

Chlorpromazine

 D

Fluoxetine

Q. 16

Drug of choice for obsessive-compulsive disorder is:

March, 2005, September 2009

 A

Sertraline

 B

Alprazolam

 C

Chlorpromazine

 D

Fluoxetine

Ans. D

Explanation:

Ans. D: Fluoxetine

The two medications proven to be most effective in the treatment of OCD are tricyclic antidepressants (TCAs) and selective serotonin reuptake inhibitors (SSRIs).

Serotonin is a chemical in the brain called a neurotransmitter that may be imbalanced in people with OCD.

While both drugs are very effective, SSRIs have generally become the preferred medication for anxiety disorders including OCD.

SSRIs have less side effects than other forms of antidepressants, less withdrawal symptoms, less danger in the event of an overdose and overall are considered safer that other types of drugs (TCAs and SSRIs are both very safe drugs, however). Common SSRIs include fluoxetine, fluvoxamine, sertraline, paroxetine, citalopram, and escitalopram.


Q. 17

Which of the following SSRI is a prodrug?

 A

Fluoxetine

 B

Paroxetine

 C

Citalopram

 D

Fluvoxamine

Q. 17

Which of the following SSRI is a prodrug?

 A

Fluoxetine

 B

Paroxetine

 C

Citalopram

 D

Fluvoxamine

Ans. A

Explanation:

Ans. is ‘a’ i.e., Fluoxetine

Selective serotonin reuptake inhibitors (SSRI)

  • 5-HT (serotonine) is the major player in depressive illness and serotonergic pathways are closely related to mood disorders especially depression.
  • Thus, drugs affecting the 5-HT levels in the neural synapse and serotonergic pathways are effective in the treatment of depression.
  • Therefore, the SSRIs have been shown to alleviate depression and are the most commonly used drugs in the therapy of depression.
  • These drugs act by inhibiting reuptake of 5-HT.
  • These drugs are now 1st choice for depression.
  • Advantages over TCAs.

1.Little or no sedation, no weight gain.

2.No interference with psychomotor or cognitive function.

3.No anticholinergic side effects.

4.No postural hypotension (no action of a-adrenergic receptors).

5.No propensity to cause seizures or arrythmias.


Q. 18

Remission with SSRI or TCA patient again havingrelapse. There may be deficiency of ‑

 A

Pyridoxine

 B

Cobalamine

 C

Ascorbate

 D

Retinol

Q. 18

Remission with SSRI or TCA patient again havingrelapse. There may be deficiency of ‑

 A

Pyridoxine

 B

Cobalamine

 C

Ascorbate

 D

Retinol

Ans. B

Explanation:

Ans. is `b’ i.e., Cobalamine 

  • Subjects with vitamin B 12deficiency and depression may present with history of past episodes with spontaneous
  • remission or response to treatment with antidepressants and later recognition or development Budeficiency”
  • Studies have found that some people with depression may have low levels of folic acid, vitamin B12 or vitamin D.

Quiz In Between



Selective Serotonin Reuptake Inhibitors (SSRI)

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI)


SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI)

MOA:

  • Inhibits 5-HT only (not NA).
  • Lack anticholinergic and α-blocking properties.

Drugs: Paroxetine, Sertraline, Citalopram,  Fluoxetine, Fluvoxamine & Escitalopram

Uses:

  • DOC for depression, phobias, OCD, PTSD, bulimia, premenstrual tension syndrome, sustained treatment of generalized anxiety disorders & panic attacks.

Advantages over TCAs:

  • No anticholinergic adverse effects.
  • No sedation or weight gain.
  • No propensity to cause seizures or arrhythmias.

1. Depression:

  • Mild to moderate – Fluoxetine.

2. Panic disorder:

  • Sustained treatment – Sertraline.

3. Neurotic disorders:

  • Obsessive compulsive disorder – Fluoxetine.
  • Post-traumatic stress disorder – Sertraline/paroxetine.
  • Bulimia – Fluoxetine.
  • Phobia – Sertraline.
  • Impulse-control disorders – Fluoxetine.

4. GAD (generalized anxiety disorders):

  • Paroxetine & venlafaxine – Indicated for chronic GAD treatment.

5. Severe premenstrual tension syndrome (PMS):

  • Fluoxetine & sertraline.
  • Effective as continuous treatment for 2 weeks out of a month in luteal phase.
  • Associated with rapid increases in pregnenolone levels.

General adverse effects:

  • Most common adverse effects:
    • Nausea –> Anxiety –> Diarrhea
    • Due to 5-HT 3 receptor stimulation in CNS & periphery.
  • Abnormal bleeding – 
    • Due to disturbance in platelet serotonin levels.
  • Insomnia, anxiety, irritability, akathisia & decreased libido
    • Due to excessive stimulation of brain 5-HT2 receptors.
  • Sexual side effects including erectile dysfunction, anorgasmia, ejaculation inhibition & ejaculatory delay (Mainly paroxetine) –
    • Due to excessive activity at spinal 5-HT2 receptors.
  • Serotonin syndrome (Coadministration of SSRIs & MAO-inhibitors).

Individual drugs:

1. Fluoxetine:

  • Prototype SSRI.
  • Prodrug
  • Longest-acting & metabolized to nor-fluoxetine retaining anti-depressant activity.
  • Hence, anti-depressant drug of SSRI.

2. Fluvoxamine:

  • Shortest-acting SSRI.

3. Escitalopram:

  • Most specific SSRI.

4. Paroxetine:

  • Most teratogenic among SSRIs.
  • Increased risk of congenital cardiac malformations.
  • More prominent sexual side effects (erectile dysfunction, anorgasmia, ejaculation inhibition & ejaculatory delay).

6. Sertraline & citalopram:

  • Safest SSRIs for combination with warfarin.

Discontinuation syndrome of SSRI’s:

  • Withdrawal symptoms include dizziness, headache, nervousness, nausea & insomnia.
  • Paroxetine (More intense) – Due to relatively short-acting nature.
  • Fluoxetine – Safer in this regard due to very long-acting metabolite. 

Exam Important

  • (SSRI) Selective Serotonin Reuptake Inhibitors inhibits 5-HT only (not NA).
  • SSRI lack anticholinergic and α-blocking properties.
  • Paroxetine, Sertraline, Citalopram,  Fluoxetine, Fluvoxamine, Escitalopram, Duloxetine are all SSRI’s.
  • SSRI are DOC for depression, phobias, OCD, PTSD, bulimia, premenstrual tension syndrome, sustained treatment of generalized anxiety disorders & panic attacks.
  • Fluoxetine is DOC for mild to moderate depression, obsessive compulsive disorder, impulse-control disorders, bulimia & also for severe premenstrual tension syndrome (PMS).
  • Sertraline is DOC for sustained treatment of panic disorder, post-traumatic stress disorder, phobia & severe PMS.
  • Paroxetine & venlafaxine are indicated for chronic GAD treatment.
  • Most common adverse effects include Nausea –> Anxiety –> Diarrhea (in order), which occur mainly due to 5-HT 3 receptor stimulation in CNS & periphery.
  • Abnormal bleeding is reported with SSRI due to disturbance in platelet serotonin levels.
  • Insomnia, anxiety, irritability, akathisia & decreased libido are seen with SSRI, due to excessive stimulation of brain 5-HT2 receptors.
  • Sexual side effects including erectile dysfunction, anorgasmia, ejaculation inhibition & ejaculatory delay (Mainly paroxetine) are seen with SSRI, due to excessive activity at spinal 5-HT2 receptors.
  • On coadministration of SSRIs & MAO-inhibitors, serotonin syndrome occurs.
  • Fluoxetine is a prototype SSRI, longest-acting prodrug & metabolized to nor-fluoxetine retaining anti-depressant activity, hence anti-depressant drug of SSRI.
  • Fluvoxamine is shortest-acting SSRI.
  • Escitalopram is the most specific SSRI.
  • Paroxetine is most teratogenic among SSRIs with increased risk of congenital cardiac malformations & more prominent sexual side effects (erectile dysfunction, anorgasmia, ejaculation inhibition & ejaculatory delay).
  • Sertraline & citalopram are safest SSRIs for combination with warfarin.
  • Discontinuation syndrome of SSRI’s produces withdrawal symptoms including dizziness, headache, nervousness, nausea & insomnia.
  • More intensive discontinuation syndrome is seen with Paroxetine, due to their relatively short-acting nature.
  • Fluoxetine is safer without discontinuation syndrome, due to their very long-acting metabolite. 
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