Pharmacology 3 hard version
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Questions and Answers

Which condition is NOT commonly associated with neuropathic pain?

  • Phantom limb pain
  • Diabetes mellitus
  • Trigeminal neuralgia
  • Acute pancreatitis (correct)

What is a primary mechanism of action for gabapentin?

  • Binds to NMDA receptors
  • Inhibits serotonin reuptake
  • Enhances GABA activity
  • Binds to calcium channels (correct)

What is a common adverse effect associated with the use of TCAs for neuropathic pain?

  • Increased heart rate
  • Acute renal failure
  • Elevated liver enzymes
  • Dry mouth (correct)

Which statement about capsicum cream is accurate?

<p>It depletes substance P from afferent neurons (A)</p> Signup and view all the answers

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

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

What should be done to the baseline opioid dosage when starting ketamine in an opioid-tolerant patient?

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

What is a key side effect of pregabalin compared to gabapentin?

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

Which of the following is NOT a characteristic of lidocaine usage for localized neuropathic pain?

<p>Only effective for chronic pain (D)</p> Signup and view all the answers

Which type of pain are opioids primarily indicated for?

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

What is the primary mechanism of action of NSAIDs?

<p>They inhibit cyclooxygenase enzyme. (D)</p> Signup and view all the answers

What role does naloxone play in opioid overdose situations?

<p>Competes with opioid agonists at receptors. (B)</p> Signup and view all the answers

Which statement correctly describes the mechanism of action of opioids?

<p>Opioids activate pathways that inhibit neurotransmitter release. (A)</p> Signup and view all the answers

What effect do NSAIDs have when combined with opioids?

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

What is one of the primary side effects associated with mirtazapine?

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

Which of the following is NOT a type of pain that opioids are effective for treating?

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

How do NSAIDs alleviate inflammation?

<p>By inhibiting the formation of prostaglandins. (C)</p> Signup and view all the answers

Which of the following medications is recognized as a tricyclic antidepressant?

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

Which of the following conditions would NOT be classified as an opioid-responsive pain?

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

For which condition are tricyclic antidepressants NOT indicated?

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

What dosing strategy is recommended for amitriptyline when used for neuropathic pain?

<p>Initiate at low doses to assess tolerance (B)</p> Signup and view all the answers

What is a recommended choice for patients experiencing sleep onset insomnia?

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

Which of these side effects is commonly associated with medications intended for sleep?

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

How should the dosage of eszopiclone be adjusted for elderly patients?

<p>Decrease the dose, with a maximum of 2mg (D)</p> Signup and view all the answers

What is the primary mechanism of action of zolpidem?

<p>Binding to GABAa receptors (B)</p> Signup and view all the answers

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

<p>Restoring dopamine balance and reducing excitatory cholinergic effects (B)</p> Signup and view all the answers

Which of the following are recognized side effects associated with tolcapone?

<p>Diarrhea, orthostatic hypotension, and hepatic necrosis (A)</p> Signup and view all the answers

Which medications are classified as Monoamine oxidase type B inhibitors?

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

What role does carbidopa play in the treatment of Parkinson's disease?

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

What is the primary action of donepezil in Alzheimer's disease management?

<p>It enhances cholinergic transmission in the CNS (D)</p> Signup and view all the answers

What is a significant psychological side effect of ethosuximide in certain populations?

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

What side effects are commonly associated with memantine?

<p>Confusion, agitation, and restlessness (C)</p> Signup and view all the answers

What is one of the potential adverse reactions associated with melatonin receptor agonists?

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

Which antiepileptic drugs are known to reduce the efficacy of oral contraceptives?

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

Which of the following statements about the management of anti-Parkinson's medications is accurate?

<p>The approach must be tailored to symptoms, age, and functional ability. (C)</p> Signup and view all the answers

Which antiepileptic medication is considered safest during pregnancy due to a lower risk of major congenital malformations?

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

Which of the following is NOT a common side effect associated with phenytoin?

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

What is the primary function of COX-1 in gastrointestinal physiology?

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

What is a primary concern with long-term opioid use?

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

Which condition is primarily associated with nociceptive pain?

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

What is a significant advantage of using medicated patches for pain relief?

<p>They allow for consistent pain relief over time (B)</p> Signup and view all the answers

What characterizes COX-2 as compared to COX-1?

<p>Increased during inflammatory states (B)</p> Signup and view all the answers

What adverse effect is NOT associated with 5-alpha reductase inhibitors?

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

Which of the following is NOT a typical side effect of ethosuximide?

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

What is the mechanism of action for GnRH analogs?

<p>Disrupting pituitary gland function (D)</p> Signup and view all the answers

What is the function of Raloxifene in postmenopausal women?

<p>It prevents osteoporosis (B)</p> Signup and view all the answers

Which estrogen has the best bioavailability when taken orally?

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

What is the primary role of Mifepristone (RU486)?

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

Which contraceptive method is considered safe for breastfeeding mothers?

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

Flashcards

Mirtazapine side effects

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

Tricyclic antidepressants (TCAs)

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

TCA indications

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

TCA dosing for neuropathic pain

Lower doses are often used to manage neuropathic pain. Meds like Amitriptyline are started at 5-10mg/day, and adjusted for tolerance and effectiveness.

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Sleep onset insomnia meds

Short-acting sleep medications like zaleplon, zolpidem, triazolam, and ramelteon are good choices for initial treatment.

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Sleep maintenance insomnia meds

Longer-acting sleep meds like zolpidem extended-release, eszopiclone, and temazepam are often preferred for sleep maintenance issues.

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Anxiolytic dosing in elderly/sleep-impaired

Start with lower doses, especially for those with liver issues or age-related considerations. Maximum doses should be considered. Example: eszopiclone maximum of 2mg.

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Mechanism of Zolpidem

Zolpidem binds to GABA receptors, specifically α1 subunit, which contributes to fewer side effects and lower risk of rebound insomnia.

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Ramelteon/Tasimelteon effect on melatonin receptors

Agonists for MT1 & MT2 melatonin receptors.

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Parkinson's treatment goal

Restore dopamine levels in the basal ganglia, balancing them with acetylcholine.

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Levodopa's role in Parkinson's

Converted to dopamine in the brain to compensate for dopamine loss.

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Carbidopa's function

Prevents levodopa breakdown outside the brain, allowing more levodopa to reach the CNS.

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Monoamine oxidase type B (MAO-B) inhibitors

Selegiline, rasagiline, and safinamide; used with levodopa to enhance its effects.

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Tolcapone side effects

Diarrhea, orthostatic hypotension, nausea, anorexia, dyskinesias, hallucinations, sleep disorders, and potentially hepatic necrosis.

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Donepezil's action and goal

Acetylcholinesterase inhibitor; goal is to improve cholinergic transmission and prevent NMDA-glutamate receptor overstimulation in Alzheimer's.

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Memantine's treatment goal

Blocks NMDA receptors to prevent excess calcium levels, but has side effects similar to Alzheimer's symptoms.

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Gabapentin for neuropathic pain

Gabapentin and pregabalin are anticonvulsants used to treat neuropathic pain. They bind to calcium channels, with pregabalin having better absorption. Common side effects include dizziness, drowsiness, fatigue, and peripheral edema.

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Gabapentin trial duration

A trial of gabapentin for chronic neuropathic pain may last 2 months or longer. Pregabalin has a faster onset of action.

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Carbamazepine for trigeminal neuralgia

Carbamazepine is a first-line treatment for trigeminal neuralgia. It prevents repetitive neuronal discharge, reducing pain. It's related to tricyclic antidepressants (TCAs).

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TCAs for neuropathic pain

TCAs have anticholinergic and antihistaminergic effects. Their impact on serotonin and norepinephrine reuptake inhibition helps with neuropathic pain. Lower doses are used compared to depression treatment, and effects can last for 1-3 weeks.

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SNRIs for neuropathic pain

Venlafaxine is used for both acute and chronic neuropathic pain. Duloxetine helps with painful diabetic neuropathy, fibromyalgia, chronic low back pain, and osteoarthritis.

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Capsaicin cream mechanism

Repeated application of capsaicin cream depletes substance P from primary afferent neurons, reducing pain. Watch for burning, stinging, or redness. Patches work faster than cream.

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Ketamine dosing for neuropathic pain

Ketamine reduces NMDA receptor firing. Lower doses are used than for anesthesia, and it's not used in infants under 3 months or those with schizophrenia. Higher doses may be needed with opioid-tolerant patients. Reduce baseline opioids by 25%-50% when combining with ketamine. Watch for agitation, confusion, hallucinations, and vivid imagery.

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Topical lidocaine for neuropathic pain

Lidocaine is used as an adjunctive or sole treatment for localized neuropathic pain.

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Ethosuximide's Impact on Pregnancy

Ethosuximide, a medication used for epilepsy, can potentially affect pregnancy. Regular monitoring of pregnancy status is essential for women of childbearing age taking this medication.

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Antiepileptics Impacting Oral Contraceptives

Some antiepileptic drugs, like carbamazepine, phenytoin, and topiramate, can interfere with oral contraceptives by reducing their effectiveness. This is due to their effect on liver enzymes.

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Safest Antiepileptics for Pregnancy

Lamotrigine and levetiracetam are considered the safest antiepileptic drugs during pregnancy, as they are associated with a lower risk of birth defects compared to other options.

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Phenytoin: Common Side Effects

Phenytoin, an antiepileptic drug, can cause various side effects, including drowsiness, slurred speech, balance problems, nausea, tremors, gum overgrowth, and skin rashes.

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COX-1's Role in GI Bleeding

COX-1, an enzyme found in most tissues, plays a crucial role in protecting the stomach lining against ulcers. Inhibiting COX-1 can increase the risk of gastrointestinal bleeding.

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COX-2's Role in Inflammation

COX-2, an enzyme involved in inflammation, is highly regulated and mainly found in the brain, kidney, and bone. It is increased during inflammation and suppressed by corticosteroids.

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Nociceptive Pain: What is it?

Nociceptive pain is caused by damage to tissues, such as muscles, bones, or nerves. It is often associated with inflammation or mechanical problems.

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Opioid analgesia

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

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NSAIDs MOA

NSAIDs inhibit cyclooxygenase, preventing the conversion of arachidonic acid to prostaglandins which causes inflammation. This leads to anti-inflammatory effects, pain relief, and fever reduction.

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Naloxone MOA

Naloxone is an opioid antagonist that reverses opioid overdose by competitively displacing opioids from the mu-opioid receptor.

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Opioid MOA for pain

Opioids bind to mu, delta, and kappa receptors, mainly mu, reducing pain perception by inhibiting neurotransmitter release and stimulating endorphin release.

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What is Nociceptive Pain?

Nociceptive pain results from stimulation of pain receptors in response to tissue damage or injury.

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How are NSAIDs used for pain?

NSAIDs are used for mild to moderate pain, strain, and sprain. They also have a dose-sparing effect when combined with opioids.

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What is Breakthrough Pain?

Breakthrough pain is a sudden, intense spike of pain that occurs despite ongoing pain management.

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Difference between Nociceptive and Neuropathic Pain

Nociceptive pain arises from tissue damage, while neuropathic pain originates from nerve damage.

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Opioid Risks

Long-term opioid use can lead to tolerance, dependence, respiratory depression, and overdose. These risks are important to discuss with patients.

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Medicated Patches: Targeted Relief

Patches deliver medication directly to the painful area, providing localized relief without affecting the whole body.

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5-alpha Reductase Inhibitors: Side Effects

Drugs like finasteride and dutasteride can cause decreased libido, impotence, breast enlargement (gynecomastia), and low blood pressure when standing up (orthostatic hypotension).

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GnRH Analogs: Mechanism

These drugs act like a temporary chemical castration, disrupting the function of the testes or ovaries.

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Raloxifene (Evista): Osteoporosis

Raloxifene helps prevent osteoporosis, particularly in postmenopausal women.

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Estradiol: Oral Estrogen

Estradiol is the best form of estrogen when taken orally because it undergoes first-pass metabolism.

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Mifepristone (RU486): Pregnancy Termination

Mifepristone blocks progesterone, which is crucial for maintaining pregnancy, thereby leading to pregnancy termination.

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Breastfeeding and Contraception: Safe Options

Intrauterine devices (IUDs), both hormonal and non-hormonal, are safe and effective for breastfeeding mothers. Avoid contraceptives containing estrogen during early postpartum as it can affect milk supply.

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Study Notes

FDA Warning on All Antidepressants

  • Increased risk of suicidal thoughts and behavior 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 approved in the USA for depression; inhibits CYP450.

  • Fluvoxamine - Primarily used for OCD in the USA.

  • Paroxetine - Inhibits CYP450.

  • Sertraline

  • Closely monitor patients for the first 2-3 weeks after starting any of these medications for suicidal ideation.

Herbs that Interact with SSRIs

  • Ginkgo Biloba

  • St. John's Wort

  • Garcinia cambogia (HCA)

  • L-tryptophan (or 5-HTP)

  • SAMe (S-adenosyl-methionine) supplements

  • These can increase the risk of serotonin syndrome.

Onset of Action of SSRIs

  • Onset typically takes 2 weeks, up to 12 weeks for maximum benefit.
  • Half-life (T½) is 16-36 hours.

Mechanism of Action of SSRIs

  • SSRIs block the reuptake of serotonin in the synaptic cleft.
  • This increases the concentration of serotonin in the synapse, making more available to bind to postsynaptic receptors.
  • This prevents the reuptake of serotonin back into the presynaptic nerve.

Indications for SSRI Use (excluding Fluvoxamine)

  • Depression
  • Anxiety
  • Panic disorders
  • OCD
  • Bulimia (off-label use)

Which Medications Are SNRIs?

  • Desvenlafaxine
  • Duloxetine
  • Levominacipran
  • Milnacipran
  • Venlafaxine

MOA of Desvenlafaxine (SNRI)

  • Blocks the reuptake of serotonin and norepinephrine.
  • The degree of blockade is dose-dependent.

Side Effects of SNRIs (Venlafaxine/Duloxetine)

  • Common: CNS effects (nausea,constipation, dry mouth, sexual effects), higher dosage may increase hypertension
  • Adverse effects: similar to those in SSRIs (and/or) palpitation, potential for ADEs similar to other medications.

Side Effects of Mirtazapine

  • Sedation, increased appetite, and weight gain.

Which Medications Are Tricyclic Antidepressants?

  • Imipramine, Trimipramine, Nortriptyline, Doxepin
  • Desipramine, Amitriptyline, Clomipramine, Protriptyline, Amoxapine

Dosing of Tricyclic Antidepressants (for Neuropathic Pain)

  • Amitriptyline and duloxetine are commonly used.
  • Start with low doses (5-10 mg/day) to assess tolerance.

Which Anxiolytic to Choose Based on Sleep Patterns

  • Sleep onset insomnia: Zaleplon, zolpidem, triazolam, ramelteon, temazepam, Eszopiclone
  • Sleep maintenance insomnia: Zolpidem extended release, eszopiclone, temazepam, lorazepam, eszopiclone, low dose doxepin, suvorexant

Side Effects of Medications for Sleep

  • Drowsiness, confusion, ataxia, cognitive impairment, sleepwalking, driving, anterograde amnesia, dizziness, headache, dry mouth, peripheral edema, somnolence, and suicidal ideation.

Mechanism of Action of Zolpidem

  • Binds to GABAa receptors.
  • Relatively selective for the a1 subunit.
  • Fewer withdrawal symptoms, minimal rebound insomnia, and minor tolerance.

ADEs Associated with Melatonin Receptor Agonists

  • Headache (HA)
  • Increased liver function tests (LFT)
  • Abnormal dreams

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Description

This quiz covers FDA warnings regarding the use of antidepressants, focusing specifically on SSRIs and their interaction with various herbs. It also discusses the increased risk of suicidal thoughts in young patients and the mechanisms of action of these medications. Test your knowledge on the critical safety information and pharmacology related to SSRIs!

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