Migraines, Emesis and Sleep Disorder Drugs

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Questions and Answers

What is the capital of France? (example question)

  • Paris (correct)
  • London
  • Berlin
  • Madrid

Flashcards

Which two triptans have a slower onsets but longer duration (half-life) than other triptans?

Naratriptan and especially frovatriptan

Lasmiditan

Selective 5HT1F receptor agonist - works similar to triptans in that it inhibits neurotransmitter and neuropeptide release but does NOT cause vasoconstriction and thus can be used in patients with vascular disease.

Ergotamine and Dihydroergotamine MOA/use

Broad spectrum serotonin agonists (meaning it acts on a variety of serotonin receptors) - MOA similar to triptans but not as frequently used given its more severe side effects

Which two CGRP antagonists can be given to a patient during an acute migraine attack?

Rimegepant and Ubrogepant

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Six Preventative therapies for migraines

  1. Monoclonal antibodies targeting CGRP
  2. Beta blockers
  3. CGRP antagonists (gepants)
  4. Antiepileptic drugs
  5. Antidepressants
  6. Behavioral therapy
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Erenumab

Monoclonal Antibody that targets the CGRP RECEPTOR --> thus by binding to the receptor itself, Erenumab prevents CGPR from doing so and thus exerting its effects

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Fremanezumab, Galcanezumab, Eptinezumab

Monoclonal Antibodies that target CGPR ITSELF --> thus by blocking the CGPR, the CGPR is stopped in its tracks and can't get to its receptor

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Which two gepants were approved to be used as preventative treatments?

Altogepant and Rimegepant

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Nucleus of tractus solitarius

Vomitting center

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Why are 5-HT3 receptor antagonists useful for the treatment of emesis?

5-HT3 receptors are present in the vomiting center and when the body detects a stimulus to induce vomiting, serotonin is released which activates the 5-HT3 receptors. By blocking these receptors, the serotonin will be unable to bind to them and thus the emesis signals will be cut short

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Administering 5-HT3 receptor antagonists with what other drug will help abolish emesis?

Dexamethason

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5-HT3 receptor antagonists

Ondansetron, granisetron, dolasetron, palonosetron

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T or F: 5-HT3 receptor antagonists are useful to treat delayed phase chemotherapy emetic response

FALSE - the delayed emetic response is responsive to antiseptics that block Neurokinin 1 (NK1) Receptors

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Aprepitant, Netupitant and Rolapitant are all examples of...

Neurokinin 1 (NK1) Receptor blockers

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Treatment for insomnia

Shorting acting benzodiazepines - Zolpidem, Zaleplon, and Escoplicone

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MOA of benzodiazepines

While GABA binds to the GABAa receptor, benzodiazepines bind to an allosteric site on the same GABAa receptor and they enhance the effect of allowing more Cl- ions to enter the neuron. This in turn hyper polarizes the neuron, inducing an inhibitory effect - something we want for anxiety or insomnia.

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What is one common treatment for hypersomnia?

Modafinil

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What is thought to cause narcolepsy with cataplexy?

Loss of hypothalamic neurons that produce orexin A and B (hypocretin). Orexins typically act through two GPCR receptors (OX1 and OX2) and they help to mediate the structure of sleep/wake cycles. However, when the neurons that produce them are destroyed, we get a disordered state of sleep such as narcolepsy.

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Suvorexant

Orexin receptor antagonists that block sedative effects and thus promote wakefulness - used to treat insomnia

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T or F: The sedative sodium oxybate (GHB) is used to treat narcolepsy

TRUE: GBH condenses sleep into its discrete period during the night time, thus helping combat the sleep fragmentation that occurs in patients with narcolepsy as a result of orexin producing neurons

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MOA of migraines

5-HT₁B/1D receptor agonists. They cause cranial vasoconstriction and inhibit trigeminal nerve pain pathways,

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