Benzodiazepines Quiz

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Questions and Answers

Which of the following benzodiazepines is classified as a short-acting agent?

  • Alprazolam
  • Diazepam
  • Triazolam (correct)
  • Lorazepam

What is a common usage of long-acting benzodiazepines?

  • Patients with sleep-onset insomnia
  • Patients with transient insomnia
  • Elderly patients
  • Patients with significant daytime anxiety (correct)

Which of the following is NOT an adverse effect of benzodiazepines?

  • Increased reaction time
  • Hypotension (correct)
  • Anterograde amnesia
  • Mental impairment

What symptom is commonly associated with withdrawal from benzodiazepines?

<p>Dysphoria (B)</p> Signup and view all the answers

Which benzodiazepine is recommended for elderly patients or those with liver disease due to its fast elimination?

<p>Lorazepam (A)</p> Signup and view all the answers

What is a significant risk factor in benzodiazepine overdosage?

<p>Concomitant intake of ethanol (D)</p> Signup and view all the answers

Which options describe an appropriate duration for benzodiazepine treatment?

<p>Less than 12 weeks (A)</p> Signup and view all the answers

Z compounds are preferred over benzodiazepines for managing insomnia because they have:

<p>Lower risk of dependence (C)</p> Signup and view all the answers

What therapeutic use of benzodiazepines is primarily aimed at reducing anxiety?

<p>Anxiolytic (C)</p> Signup and view all the answers

Which neurotransmitter do benzodiazepines enhance the effects of?

<p>GABA (D)</p> Signup and view all the answers

What is a primary pharmacokinetic characteristic of benzodiazepines?

<p>Cross the blood-brain barrier quickly (B)</p> Signup and view all the answers

Which is NOT a therapeutic use of benzodiazepines?

<p>Creating awareness (B)</p> Signup and view all the answers

In which situation are benzodiazepines used as an anticonvulsant?

<p>Status epilepticus (D)</p> Signup and view all the answers

What happens to the neuron when benzodiazepines enhance GABA's effects?

<p>Chloride ions enter the neuron (A)</p> Signup and view all the answers

What route of administration is considered appropriate for immediate anxiety relief using benzodiazepines in a dental setting?

<p>Intramuscular (C)</p> Signup and view all the answers

What effect do benzodiazepines have on neuronal excitability?

<p>Reduce excitability leading to calming effects (C)</p> Signup and view all the answers

What is a significant safety advantage of serotonin-norepinephrine reuptake inhibitors (SNRI) compared to tricyclic antidepressants (TCA)?

<p>Less cardiac adverse effects (B)</p> Signup and view all the answers

Which side effect is associated with tricyclic antidepressants (TCA)?

<p>Tachycardia (A)</p> Signup and view all the answers

Which medication class is not associated with cardiovascular effects?

<p>Selective serotonin reuptake inhibitors (SSRI) (A)</p> Signup and view all the answers

Which symptom is classified as a negative symptom of schizophrenia?

<p>Apathy (C)</p> Signup and view all the answers

Which of the following medications is an example of a serotonin-norepinephrine reuptake inhibitor (SNRI)?

<p>Duloxetine (D)</p> Signup and view all the answers

What is a potential consequence of overdosage with tricyclic antidepressants (TCA)?

<p>Death (A)</p> Signup and view all the answers

What common side effect is reported for selective serotonin reuptake inhibitors (SSRI)?

<p>Insomnia (A)</p> Signup and view all the answers

What is an example of a positive symptom of schizophrenia?

<p>Hallucinations (A)</p> Signup and view all the answers

Which class of antidepressants primarily enhances the neurotransmission of serotonin and norepinephrine?

<p>Serotonin-norepinephrine reuptake inhibitors (SNRIs) (C)</p> Signup and view all the answers

What is the term for the delay in therapeutic response to antidepressants?

<p>Therapeutic lag (C)</p> Signup and view all the answers

Which symptom is commonly associated with depressive episodes?

<p>Diminished interest in normal activities (D)</p> Signup and view all the answers

What typically follows after the initial remission of depression when treated with antidepressants?

<p>Maintenance treatment phase (D)</p> Signup and view all the answers

Which neurotransmitter is NOT directly involved in the mechanism of action for most antidepressants?

<p>Glutamate (D)</p> Signup and view all the answers

What is a common side effect of first-generation antihistamines, which is utilized in insomnia treatment?

<p>Sedation (C)</p> Signup and view all the answers

What percentage of the population is estimated to experience depression at some point in their lives?

<p>10-15% (D)</p> Signup and view all the answers

Which antidepressant classification is often considered a 2nd-line treatment?

<p>Monoamine oxidase inhibitors (MAOI) (B)</p> Signup and view all the answers

What is the primary neurotransmitter associated with the adverse effects of typical antipsychotics?

<p>Dopamine (C)</p> Signup and view all the answers

Which of the following is a characteristic adverse effect associated with typical antipsychotics?

<p>Tardive dyskinesias (D)</p> Signup and view all the answers

What type of antipsychotics primarily blocks serotonin receptors?

<p>Atypical antipsychotics (B)</p> Signup and view all the answers

Which of the following conditions is considered a rare but serious side effect of antipsychotic treatment?

<p>Neuroleptic malignant syndrome (A)</p> Signup and view all the answers

Which symptom is NOT effectively treated by typical antipsychotics?

<p>Negative symptoms (D)</p> Signup and view all the answers

What is a common metabolic side effect associated with antipsychotic treatment?

<p>Weight gain (C)</p> Signup and view all the answers

Which of the following describes the effect of Haloperidol specifically?

<p>It is a potent antipsychotic used in mental health crises. (D)</p> Signup and view all the answers

What neurological condition may result soon after administration of a typical antipsychotic?

<p>Akathisia (C)</p> Signup and view all the answers

Which atypical antipsychotic is known to potentially cause agranulocytosis?

<p>Clozapine (D)</p> Signup and view all the answers

Which of the following symptoms is characteristic of mania?

<p>Elevated mood (C)</p> Signup and view all the answers

What is the primary therapeutic use of lithium carbonate?

<p>Acute mania treatment and bipolar disorder prevention (D)</p> Signup and view all the answers

Which of the following antipsychotic agents is least likely to cause motor side effects?

<p>Clozapine (D)</p> Signup and view all the answers

What is a known major interaction effect of lithium carbonate?

<p>Increased lithium levels when combined with NSAIDs (B)</p> Signup and view all the answers

What is a common CNS effect associated with lithium therapy?

<p>Fine postural hand tremor (C)</p> Signup and view all the answers

Which of the following is NOT a condition commonly treated with atypical antipsychotics?

<p>Diabetes insipidus (B)</p> Signup and view all the answers

Chronic use of lithium can lead to which renal complication?

<p>Nephropathy (A)</p> Signup and view all the answers

Flashcards

What are benzodiazepines used for?

Benzodiazepines are a class of drugs that reduce anxiety (anxiolytic), promote sleep (hypnotic), help with seizures (anticonvulsant), and relax muscles (muscle relaxant). They also enhance the effects of general anesthesia.

How do benzodiazepines work?

Benzodiazepines work by boosting the effects of GABA, the brain's main inhibitory neurotransmitter, by binding to GABA receptors and increasing chloride ion (Cl-) influx into neurons.

How do benzodiazepines reach the brain?

Benzodiazepines are easily absorbed into the brain because they are fat-soluble (lipophilic). They can be taken orally, under the tongue (sublingual), rectally, or injected.

Where and how are benzodiazepines metabolized?

Benzodiazepines are broken down primarily by enzymes called CYPs in the liver.

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What is the overall effect of benzodiazepines on neurons?

Benzodiazepines reduce the excitability of neurons, leading to calming effects like reduced anxiety, sedation, and muscle relaxation.

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How do benzodiazepines interact with GABA receptors?

Benzodiazepines bind to GABA receptors allosterically. This means they bind to a site different from GABA itself, but their binding enhances GABA's activity.

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How does chloride ion influx affect neuron activity?

The influx of chloride ions (Cl-) through GABA receptors hyperpolarizes the neuron, making it less likely to fire and transmit signals.

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Why might intramuscular administration be chosen for a benzodiazepine?

The intramuscular route is often preferred in situations requiring rapid action, like managing anxiety in a dental setting.

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Half-life of a drug

The time it takes for the concentration of a drug in the body to reduce by half.

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Short-acting benzodiazepines

Benzodiazepines with a short half-life (2-4 hours) are suitable for sleep-onset insomnia, especially in the elderly.

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Long-acting benzodiazepines

Benzodiazepines with a long half-life (over 24 hours) are preferred for patients with daytime anxiety or those receiving treatment for anxiety/depression.

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Benzodiazepines and driving

Benzodiazepines can cause drowsiness, dizziness, impaired coordination, and mental confusion, making them potentially dangerous when driving.

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Flumazenil

Antidote for benzodiazepine overdose, acting as a benzodiazepine receptor antagonist.

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Benzodiazepine withdrawal symptoms

Prolonged benzodiazepine use can lead to dependence, and abrupt discontinuation can cause withdrawal symptoms like insomnia, anxiety, irritability, and tremors.

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Benzodiazepines and GABA

Benzodiazepines enhance the effects of GABA, an inhibitory neurotransmitter, reducing anxiety and promoting sleep.

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Z-drugs as hypnotics

Zolpidem, zaleplon, and eszopiclone are non-benzodiazepine hypnotics that work on GABA receptors. They offer a lower risk of dependence and have shorter half-lives.

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What is depression?

A common mental health condition affecting approximately 10-15% of the population, characterized by persistent sadness, loss of interest, sleep disturbances, and other symptoms, potentially leading to suicidal ideation in severe cases.

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What is therapeutic lag?

The delay before an antidepressant medication produces noticeable therapeutic effects, typically taking 3-4 weeks for initial improvements.

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What are SNRI antidepressants?

A type of antidepressant medication that primarily inhibits the reuptake of serotonin and norepinephrine, impacting their levels in the brain.

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What are SSRI antidepressants?

A type of antidepressant medication that selectively inhibits the reuptake of serotonin, affecting its concentration in the brain.

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What are MAOI antidepressants?

Antidepressant medications inhibiting monoamine oxidase (MAO), an enzyme responsible for breaking down neurotransmitters like serotonin and norepinephrine.

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What are atypical antidepressants?

A type of antidepressant medication that targets different mechanisms compared to other classes, often used as an alternative treatment option.

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What are tricyclic antidepressants (TCAs)?

Antidepressant medications that typically have a broader impact on neurotransmitters, including serotonin, norepinephrine, and others.

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What is maintenance treatment?

The continued use of antidepressant medications even after achieving remission, aiming to prevent a return of depressive symptoms.

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What are SNRIs?

These drugs block the reuptake of both serotonin and norepinephrine, increasing their levels in the synapse.

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How does Amitriptyline work?

Amitriptyline is a tricyclic antidepressant (TCA) that has poor selectivity for serotonin and norepinephrine reuptake transporters, meaning it can also affect other receptors.

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What are the common side effects of TCAs?

TCAs have anticholinergic effects like blurred vision, dry mouth, constipation, and difficulty urinating. They also cause sedation, orthostatic hypotension, and weight gain.

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What are the advantages of newer SNRIs like Venlafaxine and Duloxetine?

Venlafaxine and duloxetine are newer SNRIs with a safer profile compared to TCAs. They have fewer cardiac adverse effects, less sedation, and a wider therapeutic window.

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What are the common side effects of SNRIs?

SNRIs can cause side effects such as nausea, insomnia, nervousness, headaches, and sexual dysfunction. They can also have mild anticholinergic effects like dry mouth and constipation.

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Why are SSRIs considered safer than TCAs and newer SNRIs?

SSRIs like fluoxetine, paroxetine, sertraline, and citalopram have a better safety margin compared to TCAs and newer SNRIs. They are much safer in overdose, have fewer anticholinergic effects, and do not cause sedation.

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What are the common side effects of SSRIs?

SSRIs are generally well-tolerated and have a minimal impact on cognitive functions. Minor side effects include agitation in the first few doses, decreased libido, nausea, and some dullness of intellectual abilities.

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Why are SSRIs often the preferred choice for treating depression?

SSRIs are often preferred due to their safety profile and good tolerability, making them a suitable choice for long-term treatment. They can also be effective in managing anxiety disorders, OCD, and bulimia.

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What is psychosis?

Psychosis involves a loss of reality contact, often with hallucinations and delusions.

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Which neurotransmitters play a key role in psychosis?

Dopamine and serotonin are neurotransmitters implicated in psychosis.

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How do antipsychotics work?

Antipsychotics aim to manage the symptoms of psychosis, but they don't cure the underlying cause.

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What are typical antipsychotics?

Typical antipsychotics are older drugs that mainly block dopamine receptors.

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What are atypical antipsychotics?

Atypical antipsychotics are newer drugs that block both dopamine and serotonin receptors.

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What are extrapyramidal effects?

Extrapyramidal effects are movement disorders caused by antipsychotics, particularly typical ones.

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What is tardive dyskinesia?

Tardive dyskinesia is a long-term, usually irreversible, movement disorder caused by antipsychotics.

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What are some common side effects of antipsychotics?

Antipsychotics can cause weight gain, hormonal imbalances, and other metabolic changes.

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What are atypical antipsychotics and what conditions do they treat?

Atypical antipsychotics are a group of medications used to treat various mental health conditions, including schizophrenia, bipolar disorder, acute mania, and major depression. Unlike typical antipsychotics, they tend to improve both positive and negative symptoms of schizophrenia. Atypical antipsychotics have a lower risk of producing side effects like motor problems and hyperprolactinemia compared to typical antipsychotics, however, clozapine can cause agranulocytosis and seizures.

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What is mania?

Mania is a period of elevated, expansive, or irritable mood with increased energy and decreased need for sleep. It is characterized by a sense of euphoria and a heightened sense of self-importance.

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What is bipolar disorder and its two main types?

Bipolar disorder is a mental health condition characterized by alternating periods of mania or hypomania and depression. Bipolar I disorder is marked by episodes of full-blown mania, while Bipolar II disorder involves periods of hypomania alternating with major depression.

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What is lithium carbonate and what is it used for?

Lithium carbonate is a mood stabilizer primarily prescribed for the treatment of acute mania and preventing recurrences of bipolar disorder. Also, it can be used to address depression in patients unresponsive to other antidepressants.

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What is the importance of monitoring lithium levels and what factors can affect them?

Lithium carbonate has a low therapeutic index, meaning the difference between a therapeutic dose and a toxic dose is narrow, demanding careful monitoring of blood levels. NSAIDs and diuretics can increase lithium levels in the blood, potentially leading to toxicity.

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What are some potential side effects of lithium carbonate?

Lithium carbonate can cause a range of side effects, including CNS effects such as tremor, incoordination, and slurred speech. It also has impacts on the thyroid, causing hypothyroidism, and the kidneys, possibly leading to kidney problems in the long term.

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What treatment options are available for mania besides lithium carbonate?

Antiepileptics, atypical antipsychotic agents, and antidepressants are alternative or additional treatments for mania, often used alongside lithium or when lithium is not effective.

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What are some important drug interactions of antipsychotics?

Antipsychotics potentiate the effects of CNS depressants, including alcohol, hypnotics, anxiolytics, and opioids, increasing the risk of sedation and other adverse effects. Antipsychotics also block the actions of levodopa and dopamine agonists, used for Parkinson's disease, which can exacerbate Parkinson's symptoms.

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Study Notes

Psychopharmacological Agents

  • Psychopharmacological agents are drugs used to treat mental illnesses.
  • This includes various categories of conditions, including anxiety, depression, psychosis, mania, and neuropathic pain.

Benzodiazepines

  • Benzodiazepines are anxiolytic and hypnotic agents.
  • They have therapeutic uses as anxiolytics (reducing anxiety), sedatives/hypnotics (treating insomnia), anticonvulsants (treating seizures), preanesthetics (reducing the dose of general anesthetic), and centrally acting muscle relaxants.
  • Examples of benzodiazepines include Diazepam, Alprazolam, Clorazepate, Lorazepam, Halazepam, Clonazepam, Triazolam, and Prazepam.
  • Benzodiazepines act allosterically on GABA receptors to increase the effects of GABA enhancing its inhibitory effects.
  • The entrance of chloride ions into the neuron hyperpolarizes the membrane, and inhibits transmission.
  • They are lipophilic and cross the blood-brain barrier quickly.
  • They are absorbed orally, but also sublingually, rectally, and parenterally.
  • They have a large volume of distribution and are extensively metabolized by hepatic cytochrome P450 enzymes.
  • Benzodiazepines are classified based on their half-life (short, intermediate, and long-acting).
  • Short-acting benzodiazepines are used for sleep-onset insomnia and in the elderly. Intermediate and long-acting benzodiazepines may be used for daytime anxiety, depressive/anxiety disorders.
  • Adverse effects include sleepiness, light-headedness, increased reaction time, motor incoordination, impairment of mental and motor function, and confusion. Anterograde amnesia, irritability, and aggression (especially in the elderly) can also occur. At high doses, respiratory depression is a concern, especially in children and the elderly.
  • Drug warnings and precautions include pregnancy and breastfeeding concerns, allergic reactions, respiratory depression, geriatric considerations, liver disease, pediatric considerations, alcohol interaction, and driving safety.
  • Overdosage can be a serious concern, with ethanol being a common contributing factor to deaths. In overdose, loss of consciousness is common. The antidote is Flumazenil (IV), a benzodiazepine receptor antagonist.
  • Withdrawal symptoms are possible. Long-term use can lead to dependence. Tapering the dosage is crucial when discontinuing treatment to avoid a rebound effect.

Classification of Benzodiazepines

  • Short-acting agents (t1/2 2-4 hours): Triazolam, Midazolam
  • Intermediate-acting agents (t1/2 6-24 hours): Alprazolam (Trankimacin®), Lorazepam
  • Long-acting agents (t1/2 > 24 hours): Diazepam (Valium®), Flurazepam

Other Hypnotics

  • "Z-compounds" (e.g., Zolpidem, Zaleplon) are GABA receptor enhancers.
  • They are preferred to benzodiazepines for hypnotics because they have a lower risk of dependence, shorter half-lives, and less impact on sleep architecture.
  • Antihistamines (first generation) have sedation as a side effect, used to treat insomnia.
  • Melatonin restores the circadian rhythm.

Drug Therapy of Depression

  • Depression affects 10-15% of the population.
  • Depressive episodes are characterized by decreased interest in activities, significant weight changes, insomnia/hypersomnia, feelings of guilt or worthlessness and suicidal ideation.
  • Therapeutic lag (time) for initial response is 3-4 weeks for antidepressants. Side effects may appear on initial doses.
  • Maintenance treatment is often given to prevent relapses.
  • Combination therapy (multiple drugs) may be needed for some patients.
  • Psychotherapy is also commonly used.

Neurotransmitters Involved in Depression

  • Dopamine is related to motivation, reward.
  • Norepinephrine is linked with mood, cognition, energy, interests, anxiety, and depression.
  • Serotonin is connected to mood, cognition, appetite, and impulse control.

Classification of Antidepressant Drugs

  • They enhance neurotransmission of serotonin (5HT) and norepinephrine (NE).
  • Types include:
    • Serotonin-norepinephrine reuptake inhibitors (SNRIs)
    • Tricyclic antidepressants (TCAs)
    • Selective serotonin reuptake inhibitors (SSRIs)
    • Monoamine oxidase inhibitors (MAOIs)

Pharmacotherapy of Psychosis and Mania

  • Psychosis is a mental illness characterized by a distorted or non-existent sense of reality.
  • Schizophrenia has a prevalence of roughly 1%.
  • Schizophrenia has positive and negative symptoms including hallucinations, delusions, disorganized/agitated behavior (positive symptoms), and apathy/reduced talking (negative symptoms).
  • Psychosis is primarily related to dopamine and serotonin overactivity.
  • Treatment takes time (days) to be fully effective.
  • Antipsychotics, specifically typical (first-generation) and atypical (second-generation), manage symptoms by targeting different dopamine receptors (D2, D1 D4 and 5-HT). Atypical drugs typically have less side effects and lower risk of extrapyramidal movements.
  • Possible adverse effects include: neurologic motor dysfunction (e.g., acute dystonia, akathisia, parkinsonism, neuroleptic malignant syndrome), sedation, and autonomic system problems.
  • Potential metabolic problems include weight gain and hyperprolactinemia.

Neuropathic Pain

  • Neuropathic pain results from damage to nerves (peripheral, spinal nerve roots, and dorsal root ganglia).
  • Causes include nerve damage from diseases, amputation, multiple sclerosis, strokes, post-traumatic conditions, and certain infections/diseases (like postherpetic neuralgia).
  • Idiopathic (unknown cause) neuropathic pain is also possible.
  • Symptoms include sensory abnormalities (dysesthesia, hyperesthesia, allodynia, hyperpathia), burning sensation, and persistent/deep aching pain.
  • Drugs include tricyclic antidepressants (using lower doses than for depression), anticonvulsants, and tramadol.

Management of Anxiety and Insomnia

  • Anxiety management should ideally be focused on short-term treatments with rapid elimination.
  • This may include rapid-effect benzodiazepines (e.g., lorazepam).
  • Insomnia management should incorporate sleep hygiene and temporary use of hypnotics for transient insomnia (<3 weeks).
  • Long-term insomnia requires a full medical evaluation.

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