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Which benzodiazepine is classified as having a short half-life?
What is a primary characteristic of SSRIs compared to benzodiazepines?
Which of the following is a common symptom of insomnia?
What is the primary purpose of hypnotic benzodiazepines?
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Which drug class includes agents structurally unrelated to benzodiazepines?
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Which side effect is commonly associated with the use of hypnotic benzodiazepines?
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What duration characterizes intermediate half-life benzodiazepines?
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Which of the following drugs is NOT a non-benzodiazepine hypnotic?
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Which of the following is a potential adverse drug reaction when using hypnotic benzodiazepines?
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What is the primary mechanism of action of non-benzodiazepine hypnotics?
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What is a primary pharmacological effect of benzodiazepines?
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Which of the following is a common side effect of high doses of benzodiazepines?
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Which of the following is true regarding benzodiazepines' pharmacokinetics?
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What is the recommended approach for discontinuing benzodiazepine treatment?
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Which drug interaction significantly increases the effects of benzodiazepines?
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Which of the following statements regarding benzodiazepines' treatment duration is true?
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Which of the following pharmacokinetic properties is associated with benzodiazepines?
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Which condition could worsen drug interactions involving benzodiazepines?
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What effect do benzodiazepines have on neuronal excitability?
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What is the primary neurotransmitter associated with the GABAergic system?
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Which class of drugs is primarily classified as anxiolytics, muscle relaxants, and anticonvulsants?
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What is the key difference in the mechanism of action between benzodiazepines and selective serotonin reuptake inhibitors (SSRIs)?
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Which of the following is NOT classified as a hypnotic drug?
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How do benzodiazepines primarily exert their anxiolytic effects?
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Which neurotransmitter imbalance is associated with anxiety and hyperactivity of the adrenergic system?
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What is a significant treatment consideration when using benzodiazepines for anxiety disorders?
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In the context of treating insomnia, which type of drug is often preferred over traditional benzodiazepines?
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Which of the following statements is true regarding the serotonergic system's role in anxiety?
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What is the primary role of the GABA-A receptor in the treatment of anxiety?
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Study Notes
Benzodiazepines
- Classified by half-life:
- Short half-life (less than 6 hours): Midazolam, Triazolam
- Intermediate half-life (6-24 hours): Alprazolam, Lorazepam, Oxazepam, Temazepam
- Long half-life (more than 24 hours): Diazepam, Clonazepam, Flurazepam, Nitrazepam
Selective Serotonin Reuptake Inhibitors (SSRIs)
- Antidepressants effective for anxiety.
- Medium to long-term efficacy (3-4 weeks)
- Lack addictive potential
- Generally do not cause sedation.
- Examples: Fluoxetine, Paroxetine, Citalopram, Sertraline
Insomnia
- Characterized by:
- Prolonged latency to onset (difficulty falling asleep)
- Decreased sleep duration
- Numerous nocturnal awakenings
- Early morning awakening with difficulty falling back asleep
Hypnotic Drugs - Treatment of Insomnia
- Benzodiazepine hypnotics:
- Lorazepam, Lormetazepam
- Short action (10-20 hours), quickly removed from the body.
- Decrease sleep onset latency, reduce nighttime awakenings, and increase total sleep time.
- Adverse Drug Reactions (ADRs): daytime sleepiness, dizziness, headache, motor and cognitive impairment, memory loss, tolerance, dependence.
- Non-benzodiazepine hypnotics:
- Zolpidem, Zopiclone
- Structurally unrelated to benzodiazepines.
- Agonists of the GABA-A receptor.
- Other hypnotics:
- Melatonin
Anxiety
- Common disorder linked to work and social environment
- Normal feeling in certain situations, becomes pathological when adaptive capacity is exceeded.
- Symptoms:
- Cognitive: fear, irritability, overwhelm, insomnia
- Motor: tremor, muscle tension
- Vegetative: palpitations, sweating, nausea, dry mouth
- Behavioral: avoidance or flight from certain situations.
- Caused by excessive CNS activation:
- Alteration in adrenergic and serotonergic systems
- Attenuation of the GABAergic neurotransmitter system
GABAergic System
- GABA (gamma-aminobutyric acid) is the main inhibitory neurotransmitter in the brain.
- Acts as a natural "calmer".
Serotonergic System
- Serotonin contributes to well-being and happiness.
Adrenergic System
- Noradrenaline regulates mood, attention, and vigilance.
- Hyperactivity in this system is linked to anxiety.
Glutamatergic System
- Glutamate is the main excitatory neurotransmitter in the brain.
- Imbalance in glutamatergic activity is linked to anxiety.
Anxiolytic Drugs
- Psychotropic drugs that relieve or suppress anxiety symptoms without causing sleepiness or sedation.
- Benzodiazepines: Also anticonvulsants, muscle relaxants, and sleep inducers.
- Serotonin Reuptake Inhibitors (SSRIs):
Benzodiazepines - Mechanism of Action
- GABA is the main inhibitory neurotransmitter in the CNS.
- GABA-A receptor is the most abundant inhibitory receptor in the CNS, coupled to a selective ion channel for chloride ions.
- Benzodiazepines potentiate the effect of GABA on its receptors, allowing greater chloride influx into neurons.
- This hyperpolarizes the neuron (makes it less excitable) and produces a state of neuronal inhibition.
Benzodiazepines - Pharmacokinetics
- Very liposoluble:
- Good oral bioavailability (C max after approximately 1 hour).
- High plasma protein binding.
- Good tissue distribution (including adipose tissue).
- Crosses the blood-brain barrier and placenta.
- Administered orally, intravenously.
- Children: Rectally and intravenously for febrile convulsions.
- Hepatic metabolism: Some give rise to active metabolites (e.g., diazepam) leading to a long half-life (t1/2 = 60 hours).
- Enterohepatic circulation (e.g., diazepam).
- Easily metabolized in patients with hepatic alterations or the elderly, resulting in an intermediate half-life (e.g., lorazepam).
- Excretion in urine as glucuronides.
Benzodiazepines - ADRs
- Wide therapeutic margin, generally safe and well-tolerated.
- At high doses: drowsiness, confusion, amnesia, incoordination, impaired ability to drive, dependence, and tolerance (treatments exceeding 6 months).
Benzodiazepines- Drug Interactions
- Increased effects when combined with:
- Other CNS depressants
- Alcohol
- Antihistamines (affecting metabolism/elimination)
- Hormonal contraceptives (affecting elimination)
- Omeprazole (affecting metabolism).
Benzodiazepine - Pharmacological Effects
- Anxiolytic: Reduces anxiety and aggressiveness.
- Hypnosedative: Induces sleep and sedation.
- Myorelaxant: Reduces muscle tone.
- Anticonvulsant.
Benzodiazepine - Treatment Considerations
- Use the lowest effective dose.
- Never stop treatment abruptly; gradually reduce dosage over several weeks.
- Treatment duration should be as short as possible, not exceeding 8-12 weeks (including the phase-out phase).
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Description
This quiz covers key concepts related to benzodiazepines, selective serotonin reuptake inhibitors (SSRIs), and their applications in treating insomnia and anxiety. Identify the classifications, characteristics, and examples of these medications. Test your knowledge on their pharmacological effects and therapeutic uses.
