Pharmacology quiz 3
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Questions and Answers

What is the increased risk associated with all categories of antidepressants for certain age groups?

  • Increased risk of suicidal thoughts and behavior (correct)
  • Increased anxiety levels
  • Decreased effectiveness in treatment
  • Increased risk of weight gain

Which of the following SSRIs is approved solely for treating OCD in the USA?

  • Fluvoxamine (correct)
  • Escitalopram
  • Citalopram
  • Sertraline

What is the approximate time frame for the maximum benefit of SSRIs?

  • 1-2 weeks
  • Up to 12 weeks (correct)
  • 6-8 weeks
  • 24 weeks

Which herb is known to interact with SSRIs and increase the risk of serotonin syndrome?

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

Which of the following is a common side effect of SNRIs?

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

What are common side effects of mirtazapine?

<p>Sedation and increased appetite (B)</p> Signup and view all the answers

What is the mechanism of action for Desvenlafaxine, an SNRI?

<p>Inhibit serotonin and norepinephrine reuptake (B)</p> Signup and view all the answers

Which of the following medications is a tricyclic antidepressant?

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

What should be closely monitored during the first 2-3 weeks after starting an SSRI?

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

For what conditions are tricyclic antidepressants indicated?

<p>Depression and migraine prevention (A)</p> Signup and view all the answers

Which medication class is contraindicated for patients who have received monoamine oxidase inhibitors (MAOIs) in the previous two weeks?

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

What is a recommended starting dose of amitriptyline for neuropathic pain?

<p>5-10 mg/day (D)</p> Signup and view all the answers

Which medication is best for sleep onset insomnia?

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

What is a common side effect of medications used to help patients sleep?

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

How should anxiolytics be dosed in elderly patients?

<p>Max 2 mg (D)</p> Signup and view all the answers

What is the mechanism of action of zolpidem?

<p>Binds to GABAa receptors (D)</p> Signup and view all the answers

What is the primary goal of anti-Parkinson's medication treatment?

<p>To restore dopamine levels in the basal ganglia (D)</p> Signup and view all the answers

What is the role of carbidopa in Parkinson's treatment?

<p>It inhibits the metabolism of levodopa outside the CNS (B)</p> Signup and view all the answers

Which medication is a Monoamine oxidase type B inhibitor?

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

What are common side effects associated with tolcapone?

<p>Hepatic necrosis and orthostatic hypotension (D)</p> Signup and view all the answers

What is the effect of donepezil in Alzheimer's disease?

<p>It improves cholinergic transmission (C)</p> Signup and view all the answers

What side effect is associated with memantine?

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

Which of the following melatonin receptor agonists is associated with abnormal dreams?

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

Which of the following statements regarding treatment goals in Alzheimer's disease is true?

<p>The aim is to prevent excitotoxic actions from NMDA receptors (A)</p> Signup and view all the answers

What is a common cause of neuropathic pain?

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

What is the primary action of gabapentin in treating neuropathic pain?

<p>It binds to calcium channels. (D)</p> Signup and view all the answers

Which medication is considered first-line therapy for trigeminal neuralgia?

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

What is a common side effect of gabapentin/pregabalin?

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

How long should a trial of gabapentin for neuropathic pain typically last?

<p>2 months or more (B)</p> Signup and view all the answers

What is the mechanism of action of capsaicin cream?

<p>Depletes substance P. (A)</p> Signup and view all the answers

When using ketamine in patients on chronic opioids, how should baseline opioids be adjusted?

<p>Reduce by 25%-50% (A)</p> Signup and view all the answers

What is an adverse effect of tricyclic antidepressants (TCAs)?

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

What serious side effect is associated with long-term opioid use?

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

Which benefit is a key advantage of medicated patches?

<p>Medication is delivered directly to the pain area (D)</p> Signup and view all the answers

What is a potential adverse drug effect (ADE) of 5-alpha reductase inhibitors?

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

How do GnRH analogs affect the reproductive system?

<p>They temporarily disrupt testicular/ovarian function (C)</p> Signup and view all the answers

Which medication is known for preventing osteoporosis in postmenopausal women?

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

Which form of estrogen is best when taken orally due to first-pass metabolism?

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

What is the primary function of mifepristone in pregnancy termination?

<p>It interferes with progesterone (C)</p> Signup and view all the answers

Which contraceptive method is safe for use while breastfeeding?

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

Which type of pain are opioids primarily used to treat?

<p>Chronic pain conditions (D)</p> Signup and view all the answers

What is the mechanism of action of NSAIDs?

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

How does naloxone work to treat opioid overdose?

<p>Displaces opioid agonists at the μ-opioid receptor (A)</p> Signup and view all the answers

What characterizes nociceptive pain?

<p>It results from injury or damage to tissues. (B)</p> Signup and view all the answers

Which of the following statements about NSAIDs is correct?

<p>They produce a dose-sparing effect when combined with opioids. (D)</p> Signup and view all the answers

What is one key function of endogenous opioids released by the body?

<p>Provide natural pain relief (C)</p> Signup and view all the answers

Which of these conditions is NOT typically associated with opioid use?

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

Which receptor is predominantly targeted by opioids for analgesia?

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

What is the primary reason for monitoring ethosuximide in patients with psychological disturbances?

<p>To adjust doses based on plasma levels (A)</p> Signup and view all the answers

Which antiepileptic is known to interfere with the effectiveness of oral contraceptives?

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

Among the following antiepileptics, which is considered the safest during pregnancy?

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

What are common side effects associated with phenytoin therapy?

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

What is the primary mechanism of action of COX-1 inhibitors that leads to gastrointestinal (GI) bleeding?

<p>Decreased production of mucosal protection (A)</p> Signup and view all the answers

Which of the following statements regarding COX-2 inhibitors is true?

<p>COX-2 activity is regulated by glucocorticoids (B)</p> Signup and view all the answers

Which of the following is an indication for using tricyclic antidepressants?

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

What is the optimal starting dose of amitriptyline for neuropathic pain?

<p>5-10 mg/day (C)</p> Signup and view all the answers

Which of these medications is best suited for patients with sleep maintenance insomnia?

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

What is a potential side effect of medications used to help patients sleep?

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

How should the dose of eszopiclone be adjusted in elderly patients?

<p>Decrease the dose to a maximum of 2 mg (B)</p> Signup and view all the answers

What is typically observed when using shorter-acting medications for sleep onset insomnia?

<p>Lower risk of dependency (D)</p> Signup and view all the answers

What type of pain are opioids particularly effective in treating?

<p>Moderate to severe pain (B)</p> Signup and view all the answers

Which of the following statements accurately describes the mechanism of action of NSAIDs?

<p>They inhibit cyclooxygenase to prevent the formation of prostaglandins. (C)</p> Signup and view all the answers

Naloxone primarily functions as what type of medication?

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

What is the primary action of opioids when they bind to their receptors in the body?

<p>They inhibit the release of neurotransmitters involved in pain transmission. (B)</p> Signup and view all the answers

Which pain condition is characterized by intense spikes of pain that occur despite ongoing pain management?

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

What role do NSAIDs play when used in conjunction with opioids?

<p>They enhance the effects of opioids without reducing their dosage. (B)</p> Signup and view all the answers

Which of the following conditions is NOT typically associated with the use of opioids?

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

PGE₂ sensitizes nerve endings in the context of pain. Which medication type inhibits its production?

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

What is the primary goal of anti-Parkinson's medications?

<p>To restore dopamine balance in the basal ganglia (D)</p> Signup and view all the answers

Which medication is primarily responsible for inhibiting the metabolism of levodopa outside the CNS?

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

What side effect is more specifically associated with tolcapone?

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

Which of the following is a focus of treatment with donepezil in patients with Alzheimer's disease?

<p>Improving cholinergic transmission (A)</p> Signup and view all the answers

What is the major side effect associated with memantine?

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

Which of the following compounds is a Monoamine oxidase type B inhibitor?

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

What is a common side effect of melatonin receptor agonists like ramelteon and tasimelteon?

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

Which condition does not improve with donepezil treatment in Alzheimer's patients?

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

What is the primary risk associated with all categories of antidepressants for young adults under 24 years of age?

<p>Increased risk of suicidal thoughts and behavior (B)</p> Signup and view all the answers

Which side effect is not commonly associated with SNRIs?

<p>Severe allergic reactions (D)</p> Signup and view all the answers

What is the typical onset time for SSRIs to begin showing effects?

<p>2 weeks to 12 weeks for maximum benefit (B)</p> Signup and view all the answers

What should be carefully monitored for the first 2-3 weeks after initiating SSRI treatment?

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

Which of the following herbs is known to increase the risk of serotonin syndrome when taken with SSRIs?

<p>Garcinia cambogia (B), Gingko Biloba (C)</p> Signup and view all the answers

For which of the following conditions are SNRIs indicated?

<p>Chronic Pain Conditions (C), Generalized Anxiety Disorder (D)</p> Signup and view all the answers

What is a major contraindication for SNRIs?

<p>Patients who received MAOIs in the previous two weeks (B)</p> Signup and view all the answers

What unique mechanism of action do SNRIs possess that aids in pain relief?

<p>Inhibition of both serotonin and norepinephrine reuptake (B)</p> Signup and view all the answers

What is the primary mechanism of action of gabapentin in epilepsy management?

<p>Enhances inhibition of gabaergic impulses (D)</p> Signup and view all the answers

Which side effect is commonly associated with levetiracetam?

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

Which condition is NOT a contraindication for the use of phenytoin?

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

What monitoring parameter is crucial for patients on carbamazepine?

<p>Regular blood counts (C)</p> Signup and view all the answers

Which of the following is a key concern when prescribing antiepileptics to women who are pregnant?

<p>Risk of major congenital malformations (D)</p> Signup and view all the answers

What is the mechanism of action of lamotrigine in seizure management?

<p>Blocks sodium channels and enhances GABA (C)</p> Signup and view all the answers

What serious condition can arise from the use of valproic acid?

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

Which of the following side effects is NOT associated with topiramate?

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

What is the maximum duration for which adolescents and young adults should be monitored for suicidal ideation after starting antidepressant treatment?

<p>2-3 weeks (A)</p> Signup and view all the answers

Which of the following conditions can SSRIs be off-label used to treat?

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

What is a significant interaction concern when combining herbs with SSRIs?

<p>Serotonin syndrome risk (D)</p> Signup and view all the answers

Which SNRI medication requires dosage adjustment for hepatic and renal impairment?

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

What is the half-life range of SSRIs?

<p>16-36 hours (A)</p> Signup and view all the answers

Which common side effect is associated with higher dosages of SNRIs?

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

Which of the following SSRIs was the first approved in the USA for depression treatment?

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

What organ system primarily contributes to the glucuronidation excretion of Desvenlafaxine?

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

Which of the following conditions is a known cause of neuropathic pain?

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

What is a key mechanism of action for carbamazepine in treating trigeminal neuralgia?

<p>Prevents repeated discharge in neurons (A)</p> Signup and view all the answers

Which adverse effect is commonly associated with the use of gabapentin or pregabalin?

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

What is the recommended duration for a trial of gabapentin when treating chronic neuropathic pain?

<p>2 months (C)</p> Signup and view all the answers

Which of the following is a common side effect of tricyclic antidepressants (TCAs)?

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

What action does capsaicin cream have on substance P in neuropathic pain management?

<p>Depletes substance P from neurons (C)</p> Signup and view all the answers

When adjusting opioids for a patient also being treated with ketamine, how should the baseline opioids be modified?

<p>Reduce by 25% to 50% (B)</p> Signup and view all the answers

Which medication is specifically indicated for painful diabetic neuropathy?

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

What psychological issues can ethosuximide trigger, especially in younger patients?

<p>Profound intellectual and affective issues (C)</p> Signup and view all the answers

Which antiepileptic medications are recognized as safer during pregnancy?

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

What is the primary action of COX-1 in the body related to gastrointestinal health?

<p>Regulation of gastric cytoprotection (D)</p> Signup and view all the answers

Which antiepileptics are known to reduce the effectiveness of oral contraceptives?

<p>Carbamazepine, phenytoin, and topiramate (A)</p> Signup and view all the answers

Which of the following describes nociceptive pain?

<p>Pain due to inflammation or musculoskeletal conditions (C)</p> Signup and view all the answers

What is a common side effect of phenytoin?

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

What occurs when COX-1 is inhibited, particularly concerning gastrointestinal function?

<p>Decreased mucosal protection (B)</p> Signup and view all the answers

Which condition is primarily treated with COX-2 inhibitors?

<p>Chronic inflammation and pain (D)</p> Signup and view all the answers

Which type of pain are opioids primarily indicated for?

<p>Moderate to severe pain, including post-surgical and cancer-related pain (D)</p> Signup and view all the answers

What is the primary mechanism of action of NSAIDs?

<p>Inhibition of cyclooxygenase, reducing prostaglandin formation (B)</p> Signup and view all the answers

What is the role of naloxone in the treatment of opioid overdose?

<p>Blocks mu-opioid receptors, reversing opioid effects (C)</p> Signup and view all the answers

Which of the following conditions is least likely to be treated effectively with opioid analgesics?

<p>Mild headache pain (A)</p> Signup and view all the answers

What is the impact of combining NSAIDs with opioids?

<p>Dose-sparing effect in pain management (B)</p> Signup and view all the answers

Which receptor type is primarily targeted by opioids for their analgesic effects?

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

Which of the following best describes the role of endogenous opioids in the body?

<p>They are natural pain-relievers released in response to pain. (A)</p> Signup and view all the answers

What physiological effect occurs when opioids bind to mu receptors?

<p>Inhibition of neurotransmitter release involved in pain signal transmission (C)</p> Signup and view all the answers

What is the primary action of levodopa in the treatment of Parkinson's disease?

<p>It is converted to dopamine in the CNS. (B)</p> Signup and view all the answers

Which side effect is specifically associated with tolcapone?

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

Which of the following medications is considered a Monoamine oxidase type B inhibitor?

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

What potential serious side effect can result from long-term opioid use?

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

Which benefit of medicated patches distinguishes them from oral medications?

<p>Localized relief without systemic side effects (D)</p> Signup and view all the answers

What is the main goal of treatment with donepezil in Alzheimer's disease?

<p>To improve cholinergic transmission and prevent excitotoxicity. (D)</p> Signup and view all the answers

What is a common adverse drug effect associated with 5-alpha reductase inhibitors like finasteride?

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

What potential adverse effect might occur with the use of melatonin receptor agonists?

<p>Increased liver function tests (C)</p> Signup and view all the answers

What is the primary mechanism of action of GnRH analogs?

<p>Disrupt hormone release from the pituitary gland (B)</p> Signup and view all the answers

What common side effect might be observed with memantine treatment?

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

Which statement about raloxifene's role in osteoporosis prevention is accurate?

<p>It is indicated for postmenopausal women only. (D)</p> Signup and view all the answers

What is the expected benefit of using carbidopa in conjunction with levodopa?

<p>Prevents levodopa metabolism outside the CNS. (B)</p> Signup and view all the answers

Which statement about the goals of Parkinson's disease treatment is accurate?

<p>Dopamine/acetylcholine balance is essential for treatment success. (D)</p> Signup and view all the answers

What property differentiates estradiol from other forms of estrogen when taken orally?

<p>Significant first-pass metabolism (B)</p> Signup and view all the answers

What role does mifepristone (RU486) play in pregnancy management?

<p>Terminates pregnancy by acting on estrogen receptors (A)</p> Signup and view all the answers

Which contraceptive method is most recommended for breastfeeding women?

<p>Intrauterine Devices (IUDs) (D)</p> Signup and view all the answers

Flashcards

Antidepressant Warning

All antidepressants carry an increased risk of suicidal thoughts and behaviors, especially in children, adolescents, and young adults (under 24) during the first couple months of treatment.

SSRI Medications

Selective Serotonin Reuptake Inhibitors (SSRIs) are a class of antidepressants that increase serotonin levels in the brain.

SSRI Onset of Action

SSRIs typically take a few weeks (2+) to show improvement, possibly up to 12 weeks for the full benefit.

SSRI Interactions

Certain herbs, such as St. John's Wort, Ginkgo Biloba, and others, can interact with SSRIs, increasing the risk of serotonin syndrome.

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SNRI Mechanism

Serotonin and Norepinephrine Reuptake Inhibitors (SNRIs) block the reuptake of both serotonin and norepinephrine in the brain.

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SNRI Indications

SNRIs are used to treat depression, anxiety, and other conditions, sometimes including pain.

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SNRI Side Effects

Common SNRI side effects include nausea, constipation, dry mouth, and possible sexual side effects; higher dosages might cause hypertension or palpitations.

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Desvenlafaxine MOA

Desvenlafaxine, an SNRI, blocks the reuptake of serotonin and norepinephrine; dosage affects the block's strength, and adjustments are required depending on kidney and liver health.

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Mirtazapine side effects

Mirtazapine, an atypical antidepressant, can cause sedation, increased appetite, and weight gain.

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Tricyclic antidepressants (TCAs)

A class of antidepressants including Imipramine, Trimipramine, Nortriptyline, Doxepin, Desipramine, Amitriptyline, Clomipramine, and Protriptyline Amoxapine.

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TCA use for neuropathic pain

TCAs, particularly amitriptyline, are used to treat neuropathic pain. Doses are often lowered.

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Anxiolytic choice for sleep onset insomnia

For sleep onset problems, pick short-acting medications like zaleplon, zolpidem, triazolam, ramelteon, temazepam, or eszopiclone in the initial trial.

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Anxiolytic choice for sleep maintenance insomnia

For sustained sleep, choose longer-acting medications like zolpidem extended release, eszopiclone, temazepam, lorazepam or low-dose doxepin, suvorexant.

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Zolpidem Mechanism

Zolpidem works by binding to GABAa receptors, showing selectivity for α₁ subunit.

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Anxiolytic dosing in the elderly

Reduce anxiolytic dosages for older adults and those with liver issues; max dose can also lower for these groups.

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Side effects of sleep medications

Sleep medications can cause drowsiness, confusion, ataxia, cognitive impairment, sleepwalking/driving, memory loss, dizziness, headaches, dry mouth, peripheral edema, somnolence, and suicidal ideation.

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Melatonin receptor agonists side effects

Adverse drug events (ADE) associated with melatonin receptor agonists may include headache (HA), elevated liver function tests (LFT), and abnormal dreams.

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Parkinson's treatment goal

Restoring dopamine in the basal ganglia and counteracting the excitatory effects of cholinergic neurons to balance dopamine and acetylcholine levels in the brain.

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Carbidopa's role

Carbidopa inhibits levodopa's breakdown outside the central nervous system (CNS).

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Monoamine oxidase type B (MAO-B) inhibitors

Selegiline, rasagiline, and safinamide are MAO-B inhibitors used with levodopa to enhance its effects.

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Tolcapone side effects

Tolcapone can cause diarrhea, low blood pressure, nausea, loss of appetite, uncontrolled movements, hallucinations, sleep disturbances, and, rarely, liver damage.

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Donepezil's goal in Alzheimer's

Donepezil, an acetylcholinesterase inhibitor, aims to improve cholinergic transmission and reduce harmful effects of overstimulated brain receptors (NMDA-glutamate).

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Memantine side effects

Memantine, an NMDA receptor blocker, can cause confusion, agitation, and restlessness, sometimes resembling Alzheimer's symptoms.

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Parkinson's treatment limitations

No drug currently stops or reverses Parkinson's disease progression.

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Neuropathic Pain Causes

Damage or pathology in the nervous system (central or peripheral) can cause neuropathic pain.

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Gabapentin/Pregabalin for Neuropathic Pain

Anticonvulsants used to treat neuropathic pain, affecting calcium channels.

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Gabapentin Trial Length

Chronic neuropathic pain treatment with gabapentin/pregabalin may require 2 months or more.

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Trigeminal Neuralgia Treatment

Carbamazepine is the first-line treatment for trigeminal neuralgia, reducing neuron firing.

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Capsaicin Cream Mechanism

Repeated application depletes substance P, reducing nerve pain signals.

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Ketamine Dosing in Opioid Patients

Lower-than-anesthesia doses are used, with opioid dose adjustments needed to reduce side effects.

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Topical Lidocaine Use

Lidocaine is used for localized neuropathic pain as an adjunct or sole therapy.

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Neuropathic pain

Pain caused by damage to the nervous system

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Nociceptive Pain Treatment

Relieving nociceptive pain primarily involves using non-narcotic and opioid analgesics, alongside non-pharmacologic therapies, to address the pain source.

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When are Opioids Useful?

Opioids are effective for moderate to severe pain, including post-surgical pain, cancer pain, severe trauma, chronic pain, and breakthrough pain.

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Naloxone's Action

Naloxone is an opioid antagonist that displaces opioids from their receptor sites, primarily the mu-opioid receptor, reversing opioid overdose effects.

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Opioids' Pain Relief Mechanism

Opioids bind to mu, delta, and kappa receptors, mainly the mu receptors, activating signaling pathways that reduce pain perception.

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Opioid Risks

Long-term opioid use can lead to tolerance, dependence, and serious side effects like respiratory depression and overdose.

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Medicated Patches: Advantages

Medicated patches offer targeted relief, controlled release, convenience, reduced side effects, and a non-invasive option.

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5-alpha Reductase Inhibitors: Side Effects

Medications like finasteride and dutasteride, used for BPH, can cause decreased libido, impotence, gynecomastia, and orthostatic hypotension.

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GnRH Analogs: Mechanism

GnRH analogs act as reversible chemical 'castration', temporarily disrupting the function of testes/ovaries by inhibiting pituitary hormone release.

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Raloxifene: Osteoporosis Prevention

Raloxifene is a selective estrogen receptor modulator used to prevent osteoporosis in postmenopausal women.

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Oral Estrogen: Best Choice

Estradiol is preferred for oral estrogen therapy due to its lower first-pass metabolism.

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Mifepristone: Pregnancy Termination

Mifepristone (RU486) is used to terminate pregnancy by interfering with progesterone, which is necessary to maintain pregnancy.

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Safe Contraception During Breastfeeding

IUDs, both hormonal and non-hormonal, are safe and effective contraception during breastfeeding. Avoid estrogen-containing contraceptives in the first few weeks postpartum.

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SSRI Warning

All antidepressants, especially SSRIs, carry a risk of increased suicidal thoughts and behaviors, particularly in young people (under 24) during the first few months of treatment.

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SSRI Medication Examples

Common SSRIs include citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline.

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SSRI Herb Interactions

Certain herbs, such as St. John's Wort, Ginkgo Biloba, and L-tryptophan, can interact with SSRIs, increasing the risk of serotonin syndrome.

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Mirtazapine's Action

Mirtazapine increases serotonin and norepinephrine levels in the brain, leading to antidepressant effects.

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TCA Uses

TCAs are used to treat depression, panic disorder, prevent migraines, and manage chronic pain syndromes.

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Lowering TCA Dose

When using TCAs for neuropathic pain, especially amitriptyline, the dose is often lowered to minimize side effects.

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Sleep Onset Insomnia

Difficulty falling asleep.

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Sleep Maintenance Insomnia

Difficulty staying asleep throughout the night.

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Zolpidem's Action

Zolpidem promotes sleep by binding to GABAa receptors, specifically targeting the α₁ subunit.

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Melatonin Agonists: Side Effects

Melatonin receptor agonists like ramelteon and tasimelteon can cause headache, increased liver function tests (LFTs), and abnormal dreams.

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MAO-B Inhibitors: What are they?

Selegiline, rasagiline, and safinamide are examples of MAO-B inhibitors used in Parkinson's treatment, slowing down the breakdown of dopamine.

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Donepezil: Alzheimer's Treatment Goal

Donepezil, an acetylcholinesterase inhibitor, aims to improve communication in the brain by increasing acetylcholine levels, potentially slowing down Alzheimer's progression.

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Gabapentin MOA in Epilepsy

Gabapentin works by enhancing the inhibitory effects of GABA, a neurotransmitter that helps to suppress seizures. It does this by attaching to the alpha2delta subunit of voltage-gated calcium channels, which reduces the release of excitatory neurotransmitters.

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Levetiracetam Side Effects

Levetiracetam can cause a range of side effects, including central nervous system depression, suicidal ideation, blood disorders, skin reactions (like Steven-Johnson syndrome), nausea, weight changes, and rarely, liver failure.

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Phenytoin Contraindications

Phenytoin should not be used in individuals who are pregnant, have liver problems, have a slow heart rate (sinus bradycardia), are hypersensitive to the drug, or have significant drug interactions.

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Carbamazepine Monitoring

Carbamazepine can suppress bone marrow function, leading to low blood cell counts. Regular blood tests are essential to monitor for leukopenia, thrombocytopenia, and agranulocytosis.

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Valproic Acid in Pregnancy

Valproic acid should be avoided during pregnancy unless absolutely necessary because it can cause major birth defects and decrease IQ in the baby.

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Lamotrigine MOA

Lamotrigine is a broad-spectrum antiepileptic that works by blocking sodium channels, preventing rapid neuron firing that triggers seizures. Additionally, it enhances GABAergic neurotransmission and inhibits glutamate release, further reducing seizures.

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Valproic Acid Contraindications

Valproic acid is contraindicated in individuals with liver disease, urea cycle disorders, certain genetic mitochondrial disorders, allergies to valproic acid, and during pregnancy.

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Ethosuximide Monitoring

Therapeutic drug monitoring helps adjust ethosuximide doses based on individual plasma concentrations. This is important due to significant variations in patient responses and possible psychological side effects.

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Ethosuximide and Pregnancy

Ethosuximide may have implications for pregnancy. Monitoring pregnancy status regularly is essential for women of childbearing age.

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Antiepileptics and Contraceptives

Certain antiepileptics like carbamazepine, phenytoin, and topiramate can interfere with oral contraceptives by inducing the cytochrome P450 enzyme system, which reduces the levels of contraceptive hormones.

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Safest Antiepileptics During Pregnancy

Lamotrigine and levetiracetam are considered the safest antiepileptic medications during pregnancy due to a lower risk of major congenital malformations compared to other antiepileptics.

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Common Side Effects of Phenytoin

Phenytoin is known for side effects like drowsiness, slurred speech, abnormal eye movements, balance problems, nausea, dizziness, tremors, gingival hyperplasia, and skin rashes.

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COX-1's Role in Gastrointestinal Protection

COX-1 is a "housekeeping" enzyme crucial for various cellular functions, including gastric cytoprotection, which helps prevent ulcers by increasing mucosal protection.

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Primary Indications for COX-2 Inhibitors

COX-2 inhibitors are primarily used to reduce inflammation. COX-2 is a regulated enzyme expressed in specific tissues and is upregulated during inflammatory states.

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What is Nociceptive Pain?

Nociceptive pain is often caused by musculoskeletal conditions, inflammation, or mechanical/compressive problems. It's related to tissue damage and signals sent to the brain.

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NSAIDs MOA

NSAIDs inhibit cyclooxygenase, preventing the production of inflammatory prostaglandins, thereby reducing pain and inflammation.

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Opioids MOA for Pain

Opioids bind to opioid receptors in the brain, mainly the mu receptor, and decrease pain sensation by influencing pain signaling pathways.

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Mechanism of Action of Naloxone

Naloxone is an opioid antagonist that displaces opioids from their receptor sites, mainly the mu-opioid receptor, reversing opioid overdose effects.

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Opioids are useful in the treatment of which type of pain

Opioids are effective for moderate to severe pain, including pain from surgeries, cancer, serious injuries, chronic conditions, and sudden pain spikes.

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Common SNRI Side Effects

Common side effects of SNRI medications include nausea, constipation, dry mouth, and potential sexual side effects. Higher dosages might cause hypertension or palpitations.

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MAO-B Inhibitors

Selegiline, rasagiline, and safinamide are examples of MAO-B inhibitors used in Parkinson's. They slow down the breakdown of dopamine, enhancing its effects.

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Treatment Limitations for Parkinson's

No current medication can stop or reverse Parkinson's disease progression.

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What causes neuropathic pain?

Neuropathic pain results from damage to or problems with the nervous system, either in the central nervous system (brain and spinal cord) or the peripheral nervous system (nerves outside the brain and spinal cord).

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Diabetes and neuropathic pain

Diabetes can damage nerves, leading to neuropathic pain, often in the feet and hands.

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Trigeminal Neuralgia

Trigeminal neuralgia is a painful condition affecting the trigeminal nerve, causing sharp, stabbing pain in the face.

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Gabapentin's Role in Neuropathic Pain

Gabapentin is an anticonvulsant drug commonly used to treat neuropathic pain. It works by affecting calcium channels in nerves.

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Carbamazepine for Trigeminal Neuralgia

Carbamazepine is often the first choice for treating trigeminal neuralgia. It helps reduce the frequency of nerve firing, reducing pain.

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Ketamine for Opioid-Tolerant Patients

Ketamine can be used for chronic pain in patients who have developed tolerance to opioids. Doses are adjusted to avoid side effects.

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Ethosuximide Side Effects

Ethosuximide can sometimes cause mental health problems, especially in younger people. It can affect their thinking and mood.

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Antiepileptics and Birth Control

Some antiepileptic medications can interfere with how birth control pills work, making them less effective. This is because these medications increase the activity of certain enzymes in the liver that break down the hormones in birth control.

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Safest Antiepileptics in Pregnancy

Lamotrigine and levetiracetam are generally considered the safest antiepileptic medications for pregnant women. They seem to have a lower risk of causing birth defects.

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Phenytoin: Common Side Effects?

Phenytoin can cause a variety of side effects, including drowsiness, slurred speech, balance problems, and gum overgrowth.

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COX-1 and Stomach Protection

COX-1 is an enzyme that helps protect the stomach lining from ulcers. When COX-1 is blocked, the stomach lining can become more vulnerable.

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COX-2 and Inflammation

COX-2 is an enzyme that is involved in inflammation. It is turned on when there is inflammation, such as in a joint with arthritis.

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Nociceptive Pain: What is it?

Nociceptive pain is a type of pain that is caused by damage to tissues, such as muscles, bones, or organs. It is a normal response to injury.

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Opioid Risk Discussion

When prescribing opioids, healthcare providers should discuss potential risks with patients, including tolerance, dependence, respiratory depression, and overdose.

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Medicated Patches: Benefits

Medicated patches offer targeted pain relief, controlled release, convenience, reduced side effects, and a non-invasive option.

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Safe Contraception While Breastfeeding

Intrauterine Devices (IUDs), both hormonal and non-hormonal, are safe and effective contraception during breastfeeding. Avoid estrogen-containing contraceptives in the first few weeks postpartum.

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Estradiol: Oral Estrogen Therapy

Estradiol is preferred for oral estrogen therapy due to its lower first-pass metabolism.

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Nociceptive Pain

Pain that arises from tissue damage or inflammation, often caused by musculoskeletal conditions or physical injuries.

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What's the main pharmacologic approach for Nociceptive pain?

The main pharmacologic approach is to use non-narcotic and opioid analgesics, like NSAIDs and opioids, along with non-pharmacologic methods to address the pain's source.

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What is Neuropathic Pain?

Neuropathic pain arises from damage to the nervous system itself. It's often characterized as burning, tingling, or shooting pain.

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What's the main difference between Nociceptive and Neuropathic pain?

Nociceptive pain is caused by tissue damage and inflammation, while neuropathic pain arises from nerve damage. They have different underlying causes and may require different treatment approaches!

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Study Notes

FDA Warning on Antidepressants

  • All antidepressants carry an increased risk of suicidal thoughts and behavior, especially in children, adolescents, and young adults (up to 24 years old) during the first two months of treatment.
  • Depression and other psychiatric illnesses are risk factors.

SSRI Medications

  • Citalopram
  • Escitalopram
  • Fluoxetine (First FDA-approved for depression, inhibits CYP450)
  • Fluvoxamine (Only FDA-approved for OCD in the USA)
  • Paroxetine (Inhibits CYP450)
  • Sertraline
  • Closely monitor patients for the first 2-3 weeks after starting any SSRI for suicidal thoughts.

Herbs that Interact with SSRIs

  • Ginkgo Biloba
  • St. John's Wort
  • Garcinia cambogia (HCA)
  • L-tryptophan (or 5-HTP)
  • SAMe (S-adenosyl-methionine) supplements.

Onset and Mechanism of Action of SSRIs

  • Onset of action is typically two weeks, and up to 12 weeks for maximum benefit.
  • Half-life (T½) is 16-36 hours.
  • SSRIs block the reuptake of serotonin, increasing its concentration in the synaptic cleft. This prevents serotonin from being reabsorbed by the presynaptic nerve, increasing serotonin availability at postsynaptic receptors.

Indications for SSRIs

  • Depression
  • Anxiety
  • Panic disorder
  • OCD
  • Bulimia (off-label)
  • Anorexia (off-label)
  • Fluvoxamine is not indicated for depression.

Other Medications

  • SNRIs (Serotonin-Norepinephrine Reuptake Inhibitors):
    • Desvenlafaxine
    • Duloxetine
    • Levomilnacipran
    • Milnacipran
    • Venlafaxine
    • Block reuptake of serotonin and norepinephrine.
  • MOA of Desvenlafaxine
    • Blocks reuptake of serotonin and norepinephrine.
    • Degree of block is dose-dependent.
    • Dosage adjustment may be needed for hepatic or renal impairment.
  • Side Effects of Venlafaxine and Duloxetine:
    • Common: CNS effects, nausea, constipation, dry mouth, sexual dysfunction (higher dosages).
    • Higher Dosages: hypertension.
  • Side Effects of Milnacipran: Similar to Venlafaxine (such as palpitation), ADE Levomilnacipran similar to others, urinary hesitation.

Tricyclic Antidepressants (TCAs) and Other Medications

  • Imipramine
  • Trimipramine
  • Nortriptyline
  • Doxepin
  • Desipramine
  • Amitriptyline
  • Clomipramine
  • Protriptyline
  • Amoxapine
  • Dosage for Neuropathic Pain: Amitriptyline and duloxetine are commonly used at low doses to control neuropathic pain
  • Anxiolytics for Sleep Patterns:
    • Zaleplon, zolpidem, triazolam, and ramelteon, temazepam, Eszopiclone (short-acting)
    • Zolpidem extended release, eszopiclone, temazepam, lorazepam, eszopiclone, low-dose doxepin, and suvorexant (longer-acting)
    • Longer-acting medications can increase the risk of morning drowsiness
  • Side Effects of Mirtazapine:
    • Sedation, increased appetite, weight gain.
  • Gabapentin/Pregabalin: used for neuropathic pain and binds to calcium channels
    • Chronic use may need a trial of 2 months or more.

Ketamine

  • Used for chronic opioid pain, but at a lower dosage than for anesthesia.
  • Use with caution in patients with epilepsy or schizophrenia
  • Requires concomitant reduction in baseline opioid dose by 25% to 50%.

Lidocaine (Topical)

  • Used to treat localized neuropathic pain.
  • Blocks nerve impulse conduction.

Gabapentin

  • Mechanism involves increased GABAergic impulses.
  • Used for managing epilepsy.

Antiepileptic Drugs

  • Levetiracetam - Side effects include CNS depression, suicidal ideation, blood dyscrasias, Steven-Johnson Syndrome, nausea, and weight gain/loss.
  • Phenytoin - Contraindicated with pregnancy, liver problems, sinus bradycardia, and hypersensitivity.
  • Carbamazepine - Monitor patients for bone marrow complications like leukopenia, thrombocytopenia, and agranulocytosis (agranulocytosis can cause death if not caught)
  • Valproic Acid - Can interact with other antiepileptics (e.g., carbamazepine and lamotrigine)
  • Lamotrigine - Risk of adverse effects is increased with valproic acid.
  • Topiramate- Side effects include numbness, tingling, weight loss/decreased appetite, nausea, diarrhea, blurred vision, mental slowing, anxiety, and metallic taste.
  • Contraindications to valproic acid include liver disease, urea cycle disorders, and genetic mitochondrial disorders (especially in children under 2).

Other Indications and Contraindications

  • COX-1 Inhibitors: Gastric cytoprotection.
  • Opioids: Used for moderate to severe pain (post-surgical, cancer-related, trauma, chronic pain)
  • NSAIDs: Used for mild to moderate pain (strains, sprains).
  • Monoamine Oxidase Inhibitors (MAOIs) are contraindicated with SSRIs/SNRIs.
  • Ethosuximide Therapeutic drug monitoring is necessary.
  • Pregnancy Risks: Some anti-epileptic drugs (AEDs) have pregnancy risks, eg., valproic acid.
  • Anti-epileptics interference with Hormones: Certain AEDs induce the enzymes that break down other medications or interfere with hormone levels, requiring dose adjustments.
  • Hormonal Contraceptives: AEDs might reduce the effectiveness of oral contraceptives, requiring adjustments if necessary.

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Description

This quiz covers key information about antidepressants, particularly SSRI medications, their associated risks such as increased suicidal thoughts, and interactions with herbal supplements. Additionally, it discusses the onset and mechanism of action of these medications.

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