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Questions and Answers
What is the primary mechanism of action for Agomelatine in treating depression?
What is the primary mechanism of action for Agomelatine in treating depression?
Which of the following drugs primarily acts as a serotonin reuptake inhibitor?
Which of the following drugs primarily acts as a serotonin reuptake inhibitor?
What type of drug interaction might occur with Lithium in patients with renal impairment?
What type of drug interaction might occur with Lithium in patients with renal impairment?
Which class of drugs primarily acts as a selective serotonin reuptake inhibitor?
Which class of drugs primarily acts as a selective serotonin reuptake inhibitor?
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Which mechanism is primarily responsible for the anxiolytic effects of Benzodiazepines?
Which mechanism is primarily responsible for the anxiolytic effects of Benzodiazepines?
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What is a common side effect of tricyclic antidepressants (TCA)?
What is a common side effect of tricyclic antidepressants (TCA)?
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Which of the following effects is associated with the use of Valproate?
Which of the following effects is associated with the use of Valproate?
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What cardiovascular effect may be observed with the use of atypical antipsychotics like Olanzapine?
What cardiovascular effect may be observed with the use of atypical antipsychotics like Olanzapine?
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Which mechanism is primarily responsible for the antidepressant effects of sertraline?
Which mechanism is primarily responsible for the antidepressant effects of sertraline?
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Which drug class is most likely to lead to orthostatic hypotension due to its mechanism of action?
Which drug class is most likely to lead to orthostatic hypotension due to its mechanism of action?
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For which condition is Lamotrigine primarily used?
For which condition is Lamotrigine primarily used?
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What is the mechanism of action for bupropion?
What is the mechanism of action for bupropion?
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What side effect is commonly associated with the use of Carbamazepine for mood disorders?
What side effect is commonly associated with the use of Carbamazepine for mood disorders?
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Which adverse effect is associated with the use of venlafaxine?
Which adverse effect is associated with the use of venlafaxine?
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What is the primary action of Risperidone among atypical antipsychotics?
What is the primary action of Risperidone among atypical antipsychotics?
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What cardiovascular effect can be triggered by the use of MAOIs?
What cardiovascular effect can be triggered by the use of MAOIs?
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What unique property does Mirtazapine possess that influences its clinical effect?
What unique property does Mirtazapine possess that influences its clinical effect?
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Which neurotransmitter's reuptake is primarily inhibited by duloxetine?
Which neurotransmitter's reuptake is primarily inhibited by duloxetine?
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What side effects may occur with prolonged use of Lithium?
What side effects may occur with prolonged use of Lithium?
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Which neurotransmitter's reuptake is inhibited by both Mirtazapine and Trazodone?
Which neurotransmitter's reuptake is inhibited by both Mirtazapine and Trazodone?
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What is a critical dosing consideration when prescribing clomipramine?
What is a critical dosing consideration when prescribing clomipramine?
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Which of the following drugs may lead to metabolic syndrome due to its side effects?
Which of the following drugs may lead to metabolic syndrome due to its side effects?
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Which drug may induce a short-term hepatic toxicity risk?
Which drug may induce a short-term hepatic toxicity risk?
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What is the main pharmacological effect of atomoxetine on neurotransmitter levels?
What is the main pharmacological effect of atomoxetine on neurotransmitter levels?
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What is a common misuse misconception regarding the use of Benzodiazepines?
What is a common misuse misconception regarding the use of Benzodiazepines?
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What potential drug interaction should be closely monitored with buprenorphine?
What potential drug interaction should be closely monitored with buprenorphine?
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Which drug is least likely to cause sexual dysfunction as a side effect?
Which drug is least likely to cause sexual dysfunction as a side effect?
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Which drug is primarily used for its vasodilatory effects at small doses?
Which drug is primarily used for its vasodilatory effects at small doses?
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What cardiovascular effect is NOT expected from high doses of catecholamines?
What cardiovascular effect is NOT expected from high doses of catecholamines?
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Which beta receptor is responsible for smooth muscle relaxation in the context of anaphylaxis treatment?
Which beta receptor is responsible for smooth muscle relaxation in the context of anaphylaxis treatment?
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What is a common clinical indication for administering high doses of norepinephrine?
What is a common clinical indication for administering high doses of norepinephrine?
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Which of the following effects is primarily associated with alpha agonists?
Which of the following effects is primarily associated with alpha agonists?
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What mechanism allows epinephrine to increase both heart rate and blood pressure?
What mechanism allows epinephrine to increase both heart rate and blood pressure?
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Which statement is true regarding beta-agonists in cardiogenic effects?
Which statement is true regarding beta-agonists in cardiogenic effects?
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Epinephrine at low doses primarily has what effect on blood pressure?
Epinephrine at low doses primarily has what effect on blood pressure?
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Which drug class is most beneficial in managing acute anaphylaxis?
Which drug class is most beneficial in managing acute anaphylaxis?
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Which combination of receptor actions would most likely lead to improved coronary perfusion during cardiogenic shock?
Which combination of receptor actions would most likely lead to improved coronary perfusion during cardiogenic shock?
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How does norepinephrine primarily act on blood vessels?
How does norepinephrine primarily act on blood vessels?
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High doses of dopamine can lead to what adverse effect?
High doses of dopamine can lead to what adverse effect?
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Which of the following mechanisms does NOT contribute to the metabolic effects of catecholamines?
Which of the following mechanisms does NOT contribute to the metabolic effects of catecholamines?
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Which drug interaction should be considered when using beta-agonists?
Which drug interaction should be considered when using beta-agonists?
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Which effect is specific to α-agonists in terms of their hemodynamic impact?
Which effect is specific to α-agonists in terms of their hemodynamic impact?
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Study Notes
Antidepressants
- St. John's Wort is an herbal supplement with antidepressant and anxiolytic properties
- St. John's Wort acts on:
- Serotonin (5HT)
- Dopamine
- Norepinephrine (NA)
- GABA
- Glutamate
- Reuptake
- Mirtazapine is an antidepressant with an antihistamine action
- Mirtazapine acts on:
- α2 receptors
- 5HT2C receptors
- H1 receptors
- Trazodone is an antidepressant and sedative
- Trazodone acts on:
- 5HT2A receptors
- 5HT2C receptors
- It doesn't bind to the 5HT reuptake channels
Antidepressants Used for Specific Purposes
- Agomelatine is a melatonin agonist with antidepressant properties.
- Agomelatine acts on MT1 and MT2 receptors
- Agomelatine treats severe depression and circadian disturbance
- Agomelatine has a short half-life and can cause hepatotoxicity
Mood Stabilizers for Bipolar Disorder
- Lithium salts are mood stabilizers used for bipolar disorder and Alzheimer's disease
- Lithium salts modulate:
- NA
- 5HT
- Release
- Lithium salts cause:
- Gastrointestinal discomfort
- Nausea
- Vomiting
- Diarrhea
- Anorexia
- Weight gain
- Polyuria (antidiuretic)
- Tremors in hands
- Thyroid and/or kidney disorders
- Fetal malformations
- Carbamazepine is a mood stabilizer used for bipolar disorder, epilepsy, and trigeminal neuralgia
- Carbamazepine is an enzyme inducer
- Carbamazepine has few adverse drug reactions
- Carbamazepine causes:
- Teratogenicity (spina bifida)
- Valproate is a mood stabilizer used for epilepsy and manic psychoses
- Valproate is an acute attack preventer, it prevents recurrence
- Valproate can cause teratogenicity (spina bifida)
- Lamotrigine is a mood stabilizer used for epilepsy
- Lamotrigine is a proven anti-recurrence treatment
Atypical Antipsychotics
- Olanzapine is an atypical antipsychotic used for schizophrenia and mania + bipolar disorder
- Olanzapine acts as a D2 + 5HT2A receptor antagonist
- Risperidone is an atypical antipsychotic used for schizophrenia
- Risperidone acts as a D2 + 5HT2A receptor antagonist
- Quetiapine is an atypical antipsychotic used for schizophrenia (2nd generation) and mania + bipolar disorder
- Aripiprazole is an atypical antipsychotic used for schizophrenia and mania
- Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) used for depression
Other Mood Stabilizers
- Haloperidol is used for prophylaxis of mania, depression, and disorders
Anxiolytics
- Benzodiazepines (BZD) are anxiolytics used orally (lipid soluble)
- Benzodiazepines act as GABA A receptor selective agonists
- They have a longer duration of action (>24h) compared to Diazepam (60h)
- Benzodiazepines at higher doses cause CNS depression
- Benzodiazepines at higher doses cause an increased risk of developing antidepressant activity
- Benzodiazepines bind to adipose tissue
Antidepressant Medications
-
Tricyclic Antidepressants (TCAs)
- Mechanism of Action: Inhibit reuptake of dopamine, serotonin, and norepinephrine.
- Therapeutic Uses: Depression, anxiety, enuresis (bedwetting), neuropathic pain, and oncologic conditions.
- Pharmacokinetic Properties: Lipid soluble, orally administered.
-
Pharmacodynamic Properties:
- Cardiovascular Effects: Orthostatic hypotension, palpitations, tachycardia.
- Anticholinergic Effects: Dry mouth, constipation, blurred vision.
- Other Effects: Crosses the Blood-Brain Barrier (BBB), increases catecholamine effects, including sedation, analgesia, and antihistamine properties.
-
Adverse Drug Reactions (ADRs)
- Common: Headaches, nausea, insomnia, weight gain, tremors, anxiety, and sexual dysfunction
-
Less Common:
- Cardiac: Heart block, arrhythmia, heart failure.
- Seizure: Coma.
- Hematologic: Leukopenia, agranulocytosis, and aplastic anemia
- Liver: Hepatitis, jaundice
- Other: Skin rashes, photosensitivity, urinary retention, and increased risk of falls.
-
Drug Interactions:
- Monoamine oxidase inhibitors (MAOIs): hypertensive crisis
- Alcohol: exacerbates sedation and hypotension
- Warfarin: Increased anticoagulant effect, may lead to bleeding.
- Overdose: Atropine-like effects, cardiovascular effects, coma.
-
Selective Serotonin Reuptake Inhibitors (SSRIs)
- Mechanism of Action: Selectively inhibit the reuptake of serotonin.
- Therapeutic Uses: Depression, anxiety disorders (e.g., panic disorder, obsessive-compulsive disorder, and generalized anxiety disorder), bulimia nervosa, and premenstrual dysphoric disorder
- Pharmacokinetic Properties: Orally administered, achieve peak concentration in 15-25 hours.
-
Pharmacodynamic Properties:
- Cardiovascular Effects: May prolong the QT interval, increase risk of bleeding, and worsen existing arrhythmias.
- Other Effects: May cause serotonin syndrome, with symptoms including agitation, restlessness, confusion, hallucinations, hyperthermia, seizures, and cardiovascular instability.
-
Adverse Drug Reactions (ADRs)
- Common: Nausea, anorexia, insomnia, anxiety, sexual dysfunction, and headache
-
Less Common:
- Serotonin syndrome
- Hematologic: Bleeding, thrombocytopenia
- Central Nervous System (CNS): Seizures, tremors, akathisia, dystonia
- Gastrointestinal (GI): Gastrointestinal upset, diarrhea, vomiting.
- Skin: Pruritis, rash, urticaria
-
Drug Interactions:
- MAOIs: serotonin syndrome
- St. John's Wort: Increased risk of serotonin syndrome
- Warfarin: increased anticoagulant effect, potential for bleeding.
- Overdose: Significant risk - CNS, cardiovascular, and respiratory complications.
-
Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)
- Mechanism of Action: Inhibits the reuptake of serotonin and norepinephrine.
- Therapeutic Uses: Depression, anxiety disorders, generalized anxiety disorder, neuropathic pain, fibromyalgia, and premenstrual dysphoric disorder.
- Pharmacokinetic Properties: Orally administered, reach steady state in 1-4 weeks.
-
Pharmacodynamic Properties:
- Cardiovascular Effects: Hypertension, may worsen pre-existing hypertension.
- CNS Effects: Insomnia, headache, dizziness, and tremor.
- Other Effects: Potential for serotonin syndrome.
-
Adverse Drug Reactions (ADRs)
- Common: Nausea, headache, constipation, drowsiness, insomnia, dry mouth, and sweating
- Serious: Cardiovascular complications, hepatic injury, suicidal thoughts and behaviors, and serotonin syndrome.
-
Drug Interactions:
- MAOIs: Serotonin syndrome
- Triptans: Serotonin syndrome
- St. John's Wort: Serotonin syndrome
- Warfarin: Increased bleeding risk
- Overdose: CNS depression, cardiovascular effects, seizures, and serotonin syndrome
-
Monoamine Oxidase Inhibitors (MAOIs)
- Mechanism of Action: Inhibit the enzyme monoamine oxidase, which breaks down neurotransmitters like serotonin, norepinephrine, and dopamine.
- Therapeutic Uses: Depression, Parkinson's disease, and anxiety disorders.
- Pharmacokinetic Properties: Available in oral and transdermal formulations, achieve peak concentration in 1-2 hours.
-
Pharmacodynamic Properties:
- Cardiovascular Effects: Orthostatic hypotension, tachycardia, and palpitations.
- CNS Effects: Insomnia, agitation, restlessness, and tremor.
- Other Effects: May cause tyramine reactions, leading to hypertensive crisis.
-
Adverse Drug Reactions (ADRs)
- Common: Dizziness, headache, sleep problems, dry mouth, constipation, and orthostatic hypotension.
-
Less Common:
- Tyramine reactions:
- Liver failure (rare)
- Serotonin syndrome
- Thrombocytopenia
- Pulmonary hypertension (rare)
- Seizures
- Weight gain
-
Drug Interactions:
- Other antidepressants: Increased risk of serotonin syndrome
- Tyramine-containing foods: Hypertensive crisis
- Common over-the-counter drugs: Increased risk of adverse effects
- Overdose: Hypertensive crisis, coma, and death.
-
Bupropion
- Mechanism of Action: Inhibits the reuptake of dopamine and norepinephrine.
- Therapeutic Uses: Depression, smoking cessation.
- Pharmacokinetic Properties: Oral administration, reaches peak plasma levels in 1-2 hours.
-
Pharmacodynamic Properties:
- CNS Effects: Stimulant effects, may worsen anxiety and insomnia, and increase risk of seizures.
-
Adverse Drug Reactions (ADRs):
- Common: Nausea, headache, dry mouth, constipation, insomnia, and anxiety.
- Serious: Seizures, agitation, psychosis, and neuroleptic malignant syndrome.
-
Drug Interactions:
- MAOIs: Increased risk of hypertensive crisis
- Alcohol: Increased risk of CNS depression
- Other CNS depressants: Increased risk of sedation and respiratory depression
- Overdose: Seizures, coma, and death.
-
Reboxetine
- Mechanism of Action: Norepinephrine reuptake inhibitor.
- Therapeutic Uses: Attention Deficit Hyperactivity Disorder (ADHD), major depressive disorder, and smoking cessation.
- Pharmacokinetic Properties: Oral administration, reaches peak blood levels in 1-2 hours.
- Pharmacodynamic Properties: May cause increased heart rate and blood pressure.
-
Adverse Drug Reactions (ADRs):
- Common: Nausea, headache, insomnia, difficulty concentrating, and anxiety.
- Serious: Seizures, agranulocytosis, and suicidal thoughts and behaviors.
-
Drug Interactions:
- MAOIs: Increased risk of hypertensive crisis
- Other antidepressants: Increased risk of serotonin syndrome
- Overdose: Seizures, coma, and death.
-
Atomoxetine
- Mechanism of Action: Norepinephrine reuptake inhibitor.
- Therapeutic Uses: Attention Deficit Hyperactivity Disorder (ADHD)
- Pharmacokinetic Properties: Oral administration, reaches peak blood levels in 1-2 hours.
- Pharmacodynamic Properties: Modulates neurochemical activity in brain regions involved in attention, focus, and impulse control.
-
Adverse Drug Reactions (ADRs):
- Common: Nausea, decreased appetite, abdominal pain, drowsiness, insomnia, headache, dizziness, and dry mouth.
- Less Common: Emotional lability, suicidal ideation, agitation, restlessness, and anxiety.
- Serious: Seizures, liver problems, and growth suppression.
-
Drug Interactions:
- MAOIs: Increased risk of hypertensive crisis
- Other CNS stimulants: May lead to excessive CNS stimulation.
- CYP3A4 inhibitors: Increased risk of atomoxetine accumulation and potential adverse effects.
- Overdose: Seizures, coma, and death.
Other Agents
-
St. John's Wort
- Mechanism of Action: Unknown, but thought to increase serotonin, dopamine, and norepinephrine levels.
- Therapeutic Uses: Mild to moderate depression.
- Pharmacokinetic Properties: Orally administered in herbal supplement form.
- Pharmacodynamic Properties: May interact with other medications and may increase serotonin levels to unsafe levels.
-
Adverse Drug Reactions (ADRs):
- Common: Gastrointestinal upset, fatigue, anxiety, and headaches
- Less Common: Photosensitivity, skin rashes, and serotonin syndrome
-
Drug Interactions:
- MAOIs, SSRIs, SNRIs: Increased risk of serotonin syndrome.
- CYP3A4 inhibitors: Increased risk of St. John's Wort accumulation.
- Immunosuppressants (e.g., cyclosporine): Reduced efficacy of immunosuppressants.
- Oral contraceptives: Reduced effectiveness of oral contraceptives.
- Overdose: Potential for serotonin syndrome and liver toxicity.
Adrenaline
- Administered intravenously, subcutaneously, intramuscularly and by inhalation
- α-adrenergic effects (high doses): vasoconstriction, increased heart rate and blood pressure, and decreased contractility
- β1-adrenergic effects (low doses): cardiac effects, increased heart rate and contractions, and increased contractility
- β2-adrenergic effects: bronchodilation and smooth muscle relaxation
- Other effects:
- Increased heart rate and blood pressure
- Increased force of contraction
- Bronchodilation
- Nasal decongestion
- Anaesthesia and anaphylaxis
- Angioedema
- Uterine contraction
- Gastrointestinal relaxation
- Hyperglycaemia
- Lipolysis
Noradrenaline
- Administered intravenously and intramuscularly
- α-adrenergic effects: vasoconstriction
- β-adrenergic effects: increased heart rate and contractility force.
- Other effects:
- Increased heart rate
- Increased force of contraction
- Increased blood pressure
- Increased rate of contraction
- Arrhythmias - tachycardia
- Hypertension, Necrosis and bleeding
- Decreased gastrointestinal motility
- Bronchodilation
- Topical nasal decongestion
Dopamine
- Administered intravenously
- Small doses: vasodilation (D1 receptor action)
- Other effects:
- Increased heart rate
- Increased force of contraction
- Increased blood pressure
- Decreased gastrointestinal motility
- Increased renal blood flow
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