Antideppressant Drugs Sheet to My Own Flash Cards
What is the primary function of monoamine oxidase (MAO) in the neuron?
a) Synthesizing neurotransmitters
b) Breaking down excess neurotransmitter molecules
c) Regulating membrane potential
d) Facilitating neuronal communication
b) Breaking down excess neurotransmitter molecules
Which of the following neurotransmitters are affected by monoamine oxidase inhibitors (MAOIs)?
a) Acetylcholine
b) Glutamate
c) Norepinephrine, dopamine, and serotonin
d) Gamma-aminobutyric acid (GABA)
c) Norepinephrine, dopamine, and serotonin
Where is monoamine oxidase (MAO) primarily found in the body?
a) Kidneys
b) Heart
c) Nerves, gut, and liver
d) Lungs
c) Nerves, gut, and liver
What is the therapeutic effect of monoamine oxidase inhibitors (MAOIs) in the treatment of depression?
a) Decreasing neurotransmitter levels
b) Inhibiting neurotransmitter synthesis
c) Increasing neurotransmitter levels
d) Stabilizing neurotransmitter release
c) Increasing neurotransmitter levels
Location of MAOA ?
1 - Placenta,
2 Gut mucosa,
3 Liver & Brain
Location of MAOB ?
1 Platelets,
2 Liver & Brain
Substrates of MAOA?
1 NA & 5-HT.
MAOB substrate ?
Dopamine.
MAOIB
Selegiline
MAOIA
Clorgyline & Moclobemide
Three MAO inhibitors are currently available ?
- Phenelzine
- tranylcypromine
- selegiline,
What is the primary reason for the limited widespread use of MAO inhibitors?
a) High cost of medication
b) Narrow therapeutic window
c) Severe side effects
d) Limited availability in pharmacies
c) Severe side effects
Which of the following foods contains tyramine, a substance that can cause adverse reactions in individuals taking MAO inhibitors?
a) Fresh fruits and vegetables
b) Whole grains
c) Aged cheeses , chicken liver and meats
d) Dairy products
c) Aged cheeses , chicken liver and meats
How does tyramine contribute to adverse reactions in individuals receiving MAO inhibitors?
a) By inhibiting the action of MAO in the gut
b) By promoting the release of large amounts of stored catecolamines from nerve terminals
c) By decreasing blood pressure
d) By enhancing the metabolism of medication
b) By promoting the release of large amounts of stored catecolamines from nerve terminals
What symptoms can tyramine-induced release of catecholamines cause in individuals taking MAO inhibitors?
a) Drowsiness and lethargy
b) Muscle weakness and fatigue
c) Headache, stiff neck, tachycardia, and hypertension
d) Decreased heart rate and respiratory depression
c) Headache, stiff neck, tachycardia, and hypertension
Which of the following is a potential consequence of consuming tyramine-rich foods while on MAO inhibitors?
a) Decreased blood pressure
b) Increased insulin sensitivity
c) Risk of serotonin syndrome
d) Hypertensive crisis and stroke
d) Hypertensive crisis and stroke
Tyramine, found in foods like aged cheeses and meats, is typically inactivated by which enzyme in the gut?
a) Lipase
b) Amylase
c) Monoamine oxidase (MAO)
d) Protease
c) Monoamine oxidase (MAO)
What happens when individuals receiving an MAO inhibitor consume foods containing tyramine?
a) Tyramine is metabolized more efficiently
b) Tyramine levels in the body decrease
c) Tyramine cannot be degraded in the gut
d) Tyramine is converted into a harmless substance
c) Tyramine cannot be degraded in the gut
Which of the following foods is likely to contain tyramine?
a) Fresh fruits and vegetables
b) Whole grains
c) Aged cheeses
d) Skim milk
c) Aged cheeses
What is the consequence of tyramine not being degraded in the gut due to MAO inhibition?
a) Increased risk of gastrointestinal bleeding
b) Enhanced absorption of tyramine
c) Release of large amounts of catecholamines from nerve terminals
d) Improved digestion of protein-rich foods
c) Release of large amounts of catecholamines from nerve terminals
What is the mechanism by which MAO-A inhibitors contribute to the “cheese effect”?
a) They increase the production of tyramine in the gut
b) They enhance the breakdown of tyramine in the body
c) They inhibit the breakdown of tyramine, leading to high tyramine levels
d) They deactivate tyramine receptors in the brain
c) They inhibit the breakdown of tyramine, leading to high tyramine levels
What is the consequence of high tyramine levels in individuals taking MAOIs?
a) Increased blood pressure
b) Decreased heart rate
c) Lowered cholesterol levels
d) Improved cognitive function
a) Increased blood pressure
How can the risk of hypertensive crisis due to the “cheese effect” be mitigated?
a) By increasing the dosage of MAOIs
b) By avoiding foods rich in tyramine
c) By combining MAOIs with SSRIs
d) By reducing physical activity
b) By avoiding foods rich in tyramine
Which adverse reaction is a potential consequence of combining MAOIs with certain drugs like pain medications and SSRIs?
a) Hypotension
b) Serotonin syndrome
c) Hyperglycemia
d) Insomnia
b) Serotonin syndrome
What has caused MAOIs to be positioned as second or third-line treatments despite their superior efficacy?
a) Limited availability in pharmacies
b) High cost of medication
c) Severe side effects
d) Short duration of action
c) Severe side effects
What is the primary reason for the cautious use of MAOIs in clinical practice?
a) They have minimal side effects
b) They are the first-line treatment for most psychiatric disorders
c) They interact with many common foods and medications
d) They have a short half-life
) They interact with many common foods and medications
Which of the following behaviors is characteristic of mania?
a) Sluggishness and lethargy
b) Slow thought and speech patterns
c) Rapid thought and speech patterns
d) Excessive sleepiness
c) Rapid thought and speech patterns
Which of the following best describes the self-confidence of individuals during a manic episode?
a) Extreme self-doubt and insecurity
b) Moderate self-assurance
c) Overwhelming self-confidence
d) Lack of self-awareness
c) Overwhelming self-confidence
Classification Of Anti- Depressants ?
“4”
1 - Selective serotonin re-uptake inhibitors (SSRI)
2- Tricyclic anti-depressants (TCA):
3- Atypical anti-depressants (second & third generation)
4-Monoamine oxidase inhibitors
(MAOI)
TRICYCLIC ANTIDEPRESSANTS
“10”
*Amitriptyline من ضمن الخيارات ف الفاينال
Protriptyline
#Nortriptyline
من ضمن الخيارات ف الفاينال Maprotiline
*Clomipramine
*Desipramine
*Imipramine
Trimipramine
Doxepin
Amoxapine
Which of the following conditions are SNRIs commonly used to treat?
a) Hypertension
b) Diabetes
c) Depression
d) Osteoporosis
c) Depression
Besides depression, SNRIs are also used to treat:
a) Schizophrenia
b) Bipolar disorder
c) chronic pain esp.nerve pain & Anxiety disorders
d) Parkinson’s disease
c) chronic pain esp.nerve pain & Anxiety disorders
SNRIs are particularly effective in treating which type of pain?
a) Muscular pain
b) Headaches
c) Nerve pain
d) Bone pain
c) Nerve pain
Which neurotransmitters are primarily targeted by SNRIs?
a) Dopamine and serotonin
b) Serotonin and norepinephrine
c) Norepinephrine and dopamine
d) Acetylcholine and GABA
b) Serotonin and norepinephrine
Which neurotransmitters do both duloxetine and venlafaxine primarily affect?
a) Serotonin and dopamine
b) Serotonin and norepinephrine
c) Dopamine and norepinephrine
d) GABA and acetylcholine
b) Serotonin and norepinephrine
Two of the most common SNRIs are……. and venlafaxine
duloxetine
SELECTIVE SEROTONIN RE-UPTAKE
INHIBITORS (SSRIs)
1 Citalopram
2 Escitalopram
3 Fluoxetine “the prototype”
4 Fluvoxamine
5 Paroxetine
6 Sertraline
G.R
more vigilance is required when changing from Fluxitine medicine to another SSRI drug ?
. A four to seven day wash-out period is recommended to allow concentrations of fluoxetine and its active metabolite to decrease.
G.R
Discontinuation symptoms are unlikely with fluoxetine SSRI ?
b.c Fluoxetine has a longer half-life than other SSRIs.
Google
Which medication is known for reducing total sleep time and increasing sleep latency?
a) Sertraline
b) Paroxetine
c) Fluoxetine
d) Escitalopram
a) Sertraline “SSRI”
Which SSRI is described as the most sedating and is commonly used to aid sleep in anxious patients?
a) Sertraline
b) Paroxetine
c) Fluoxetine
d) Escitalopram
b) Paroxetine
What is the safest antidepressant drug for MI pts ?
Sertraline “SSRI“ is the recommended first-choice antidepressant
What is one of the chronic effects associated with long-term use of SSRIs?
a) Up-regulation of presynaptic inhibitory receptors
b) Down-regulation of presynaptic inhibitory receptors
c) Decreased release of neurotransmitters
d) Increased sensitivity to serotonin
b) Down-regulation of presynaptic inhibitory receptors
How does down-regulation of presynaptic inhibitory receptors affect neurotransmitter release?
a) It decreases neurotransmitter release
b) It increases neurotransmitter release
c) It has no effect on neurotransmitter release
d) It stabilizes neurotransmitter release
b) It increases neurotransmitter release
Which neurotransmitter is primarily affected by the chronic use of SSRIs?
a) Dopamine
b) Serotonin
c) GABA
d) Acetylcholine
b) Serotonin
What are the therapeutic implications of down-regulation of presynaptic inhibitory receptors by SSRIs?
a) Reduced effectiveness over time
b) Increased effectiveness over time
c) Immediate relief of symptoms
d) No change in effectiveness
b) Increased effectiveness over time
Therapeutic Uses of SSRIs?
1 Psychic depression
2 panic disorders
3 Obsessive compulsive disorders (better
than the TCA clomipramine).
4 Eating disorders e.g. Bulimia nervosa.
Pharmacokinetics of SSRIs
Oral bioavailability 70%
Convert to active metabolites
fluoxetine differs from the other members of
the class in two respects.
First, it has a much longer half-life (50 hours)
and is available as a sustained-release
preparation allowing once-weekly dosing.
Second, 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
Chronic effects of SSRI drugs
- Down-regulation of presynaptic
inhibitory receptors leads to increased
release of neurotransmitter - Increased neuro-transmitter synaptic cleft
- Enhanced postsynaptic receptor activity leading
to a therapeutic response.
تجميعة من رسمة
F.E
All of the following regarding fluoxetine are correct Except:
A. Inhibit neuronal reuptake of both 5-HT & NA.
B. Long half-life (50 hour).
C. Their effect appears after 2-3 weeks.
D. All of the above.
A. Inhibit neuronal reuptake of both 5-HT & NA.
SSRI side effects
Nausea
Anxiety
Drowrsiness
Insomnia
Sexual dysfunction
Drug interactions
من الرسمة ⤴️
في السلايد اللي بعد الرسمة كاتب c و d على طول
c- Increases aggression, violence & suicide.
d- Fluoxetine + MAOI → Serotonin
syndrome. May be FATAL..
Discontinuation syndrome •
headache, malaise and flu-like symptoms, •
agitation and irritability, nervousness, and
changes in sleep pattern
Mechanism of Action of TCA
- Inhibit Neuronal Uptake of Noradrenaline & Serotonin •
→ ⬆️ NA, serotonin Inter-Synaptically.
The antidepressant effect appears after 2-3 WEEKS and •
lasts for 2-3 WEEKS after stop of TCA.
2- SEDATION: Especially at beginning of treatment & in •
Normal individuals.
Amitriptyline > Imipramine > Desipramine.
3- Lower Seizure Threshold. •
4- Anti-Cholinergic (Anti-Muscarinic =
Atropine-Like).
5- Anti-Histaminic (H1-Block) & H2-Block.
6- Anti-Serotonin.
7- Alpha blocking effect
Therapeutic Uses of TCA
1- Psychic depression (Main Use).
2- Panic & Phobic states. •
4- Obsessive compulsive disorders •
(Clomipramine or Better SSRI as Fluoxetine). •
Imp **5- Chronic pain •dr.J / neuropathic pain ( tigeminal neuralgia , peripheral neuropathy ) NSRI are also used for this use .
6- Nocturnal enuresis in children (Imipramine). •
But ADH is better alternative
Tricyclic Antidepressants are particularly effective in the treatment of:
A. Acute stress disorder
B. Bipolar depression
C. Nocturnal enuresis in children
D. Seasonal affective disorder
C. Nocturnal enuresis in children
Among the following, which is a specific therapeutic use of Imipramine, a Tricyclic Antidepressant?
A. Treatment of fibromyalgia
B. Management of diabetic neuropathy
C. Relief of chronic pain
D. Resolution of nocturnal enuresis in children
D. Resolution of nocturnal enuresis in children
Which of the following conditions is typically managed with Clomipramine rather than other TCAs?
A. Major depressive disorder
B. Generalized anxiety disorder
C. Obsessive-compulsive disorder
D. Panic disorder
C. Obsessive-compulsive disorder
Or better SSRI as fluoxetine
G.R Physical and psychological dependence •
has been rarely reported with TCA ttt , however, this
necessitates slow withdrawal ?
to minimize
discontinuation syndromes and cholinergic
rebound effects.
TCA side effects
Dry mouth
Constipation
Urinary retention.
Blurred vision
Tachycardia
Arrhythmias
Atropine like actin ⤴️بإختصار
Nausea
Drowsiness
كلهم من الرسمة ⤴️
Acute Toxicity:
Common & FATAL.
Manifestations: Excitement, Seizures,
Arrhythmia & Atropine Like
نقدروا انزيدوا عليهم الكلام اللي مكتوب ف البداية مع ال ميكانيزم
lower seizures threshold
And sedation in normal individuals
بإختصار من رسمة تانية مجمعة كل الكلام
• Sedation
• Orthostatic Hypotension
• ⬇️ Sexual Ability/Desire
• Dry Mouth
• Urinary Retention
• Tachycardia
Acute Toxicity which TCA
Common & FATAL.
a- Manifestations: Excitement, Seizures,
Arrhythmia & Atropine Like action
- b- Treatment:
- Stomach wash + Charcoal.
+ Diazepam → Treats excitement & Seizures.
+ Phenytoin → Treats Seizures & Ventricular arrhythmias.
+ Physostigmine treats → Atropine-like effects
Advantages of Fluoxetine (SSRI) over TCA:
a- Less Adverse Effects →
*NO Atropine like effects(Allowed in Glaucoma patients)
*NO CVS side effects,
*NO weight gain.
b- Low acute toxicity → NO Cardiotoxicity or Hepatotoxicity
c- Little interactions & NO Interaction with food.
Atypical Antidepressants
Dr.J “ heterocyclic “
mixed group of agents that have actions at several different sites.
•
They are not any more efficacious than the TCA or SSRls, but their
side effect profiles are different.” No sexual dysfunction “
Atypical Antidepressants
Bupropion
mirtazapine
nefazodone
trazodone
Atypical Antidepressants
Bupropion
mirtazapine
nefazodone
trazodone
What distinguishes Bupropion from other antidepressants?
A. It primarily affects serotonin reuptake
B. It has a long half-life, allowing for once-daily dosing
C. It acts as a dopamine and norepinephrine reuptake inhibitor
D. It is associated with high incidences of sexual dysfunction
C. It acts as a dopamine and norepinephrine reuptake inhibitor
Bupropion is particularly beneficial for:
A. Enhancing sleep quality in patients with insomnia
B. Reducing cravings and withdrawal symptoms in tobacco users
C. Managing symptoms of social anxiety disorder
D. Treating symptoms of obsessive-compulsive disorder
B. Reducing cravings and withdrawal symptoms in tobacco users
Which side effect is commonly associated with Bupropion use?
A. Weight gain
B. Bradycardia
C. Hypotension
D. Tremor and nervousness
D. Tremor and nervousness
Side effects
dry mouth, sweating, nervousness, tremor, a very low incidence of
sexual dysfunction, and an increased risk for seizures at high doses
•
At higher doses, Bupropion carries an increased risk for:
A. Hallucinations
B. Gastrointestinal bleeding
C. Seizures
D. Allergic reactions
C. Seizures
The pharmacokinetic profile of Bupropion necessitates:
A. Intravenous administration
B. More than one Daily dosing due to its short half-life
C. Use only in elderly patients
D. Adjustment of renal function before administration
B. More than one Daily dosing due to its short half-life
Mirtazapine
is an atypical antidepressant that enhances serotonin and norepinephrine neurotransmission by blocking presynaptic alpha-2 adrenergic receptors. This blockade leads to increased release of both serotonin (5-HT) and norepinephrine (NE).
كلام مرتب وسمح من chat gpt
أهم معلومة عليه في الإمتحان does not cause sexual dysfunction
One of the pharmacological actions of Mirtazapine is:
A. Antimuscarinic activity
B. Dopamine reuptake inhibition
C. H1 histamine receptor blockade
D. Potentiation of serotonin receptor agonism
C. H1 histamine receptor blockade
Explanation:
Mirtazapine has significant H1 histamine receptor blocking properties, which contribute to its sedating effects.
Mirtazapine is less likely to cause which common side effect compared to other antidepressants?
A. Dry mouth
B. Sexual dysfunction
C. Weight gain
D. Insomnia
B. Sexual dysfunction
Which receptor does Mirtazapine block, leading to its sedative effects?
A. Muscarinic receptors
B. Alpha-1 adrenergic receptors
C. H1 histamine receptors
D. Dopamine D2 receptors
C. H1 histamine receptors
mirtazapineكلام الشيت
enhance 5HT&NA secreation. by blocking alpha2 receptors من الرسمة
Sedating H1 blocking action •
No antimuscarinic action •يعني no atropine like action
الزيادات المهمة
No sexual dysfunction
Which antidepressant medication blocks 5HT2A receptors and is associated with chronic downregulation of 5HT1A presynaptic receptors, along with a significant risk of hepatotoxicity?
A) Fluoxetine
B) Trazodone
C) Nefazodone
D) B and C
D) B and C
A patient is prescribed a medication that primarily acts by blocking 5HT2A receptors and is known for its potential to cause liver damage. Which antidepressant is most likely prescribed?
A) Venlafaxine
B) Trazodone & Nefazodone
C) Amitriptyline
B) Trazodone & Nefazodone
Mood Stabilizing Drugs
(Antimanic Drugs)
Lithium •
Carbamazepine •
Valproic acide •
Pharmacokinetics •
Absorbed orally •
Eliminated by kidney •
Low therapeutic index •
Mood stabilizing drugs uses
uses
Mainly in prophylaxisis and treatment of •
manic depressive disorder
Mood stabilizing drugs side effects
S.E
1. Anorexia, vomiting, diarrhea •
2. Nephrogenic diabetes insipidus •
3. Goiter •
3. Epileptic seizures •
4. Teratogenecity •
5. Arrhthemia •
6. Leukocytosis •
Toxicity with mood stabilizing drugs treated with?
Toxicity treated by: •
Osmotic diuretics •
Na bicarbonate •
Dialysis in severe poisoning •
A 55-year-old teacher began to experience
changes in mood. He was losing interest in his
work and lacked the desire to play his daily
tennis match. He was preoccupied with feelings
of guilt, worthlessness, and hopelessness. In
addition to the psychiatric symptoms, the patient
complained of muscle aches throughout his
body. Physical and laboratory tests were
unremarkable. After 6 weeks of therapy with
fluoxetine, the patient’s symptoms resolved.
However, the patient complains of sexual
dysfunction. Which of the following drugs might
be useful in this patient
A. Fluvoxamine
.B. Sertraline
.C. Citalopram
.D. Mirtazapine
.E. Lithium
D. Mirtazapine
تجميعه لل antidepressants تكلم عليها د جمال ف المحاضرة
Depression with anxiety ➡️ SSRI
Depression with sexual impairment ➡️ Mertizapine
Depression with pain ➡️ TCA / NSRI / MAOI
Depression with insomnia ➡️ sedative SSRI / TCA
Depression with hypersomnia ➡️ activating SSRI
*NSRI ( NE and serotonin reuptake inhibitor)
- Activating SSRI ( fluxetine flavuoxamine citalopram )
*Sedating SSRI ( Escitalopram paroxetine sertaline )
