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    Assignment - Headache Disorders

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    Ayessa Salazar
    CGRP inhibitors have demonstrated effectiveness in treating migraine disorders. There are two types - monoclonal antibodies that antagonize the CGRP molecule or receptor, and small molecule CGRP receptor antagonists (gepants) that block the CGRP receptor. Key counseling points for patients include monitoring for side effects, avoiding medication overuse which can cause rebound headaches, and working closely with their doctor to determine if treatment is effective.

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    Assignment - Headache Disorders

    Uploaded by

    Ayessa Salazar
    75 views2 pages
    CGRP inhibitors have demonstrated effectiveness in treating migraine disorders. There are two types - monoclonal antibodies that antagonize the CGRP molecule or receptor, and small molecule CGRP receptor antagonists (gepants) that block the CGRP receptor. Key counseling points for patients include monitoring for side effects, avoiding medication overuse which can cause rebound headaches, and working closely with their doctor to determine if treatment is effective.

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    CGRP inhibitors have demonstrated effectiveness in treating migraine disorders. There are two types - monoclonal antibodies that antagonize the CGRP molecule or receptor, and small molecule CGRP receptor antagonists (gepants) that block the CGRP receptor. Key counseling points for patients include monitoring for side effects, avoiding medication overuse which can cause rebound headaches, and working closely with their doctor to determine if treatment is effective.

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    75 views2 pages

    Assignment - Headache Disorders

    Uploaded by

    Ayessa Salazar
    CGRP inhibitors have demonstrated effectiveness in treating migraine disorders. There are two types - monoclonal antibodies that antagonize the CGRP molecule or receptor, and small molecule CGRP receptor antagonists (gepants) that block the CGRP receptor. Key counseling points for patients include monitoring for side effects, avoiding medication overuse which can cause rebound headaches, and working closely with their doctor to determine if treatment is effective.

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    © All Rights Reserved
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    Assignment – HEADACHE DISORDERS CLINICAL PHARMACY & PHARMACOTHERAPEUTICS 1

    Name: Salazar, Ayessa Nedine F. Date Submitted: September 29, 2020


    Section: PM 301

    I. Research the new class of drugs known as Calcitonin Gene-Related Peptide Receptor
    Inhibitors (CGRPI) and answer the following questions:

    1. In which headache disorders have these agents demonstrated effectiveness?


    Answer:

    Migraine is a complex neurological disease involving many regions of the brain. One
    area of particular interest is the trigeminovascular system, which includes the trigeminal
    ganglia, the branches of the trigeminal nerve, and the cranial blood vessels that they innervate.
    The trigeminovascular system is involved in the regulation of cranial blood flow and
    transmission of pain. CGRP is a key neuropeptide in trigeminovascular activation and is
    implicated in pain signaling and vasodilation. Release of CGRP triggers a cascade of events that
    activate the peripheral nervous system (throbbing pain) and central nervous system (including
    the brain stem, thalamus, and cortex), which are associated with allodynia and other migraine
    sensory symptoms.

    Although there are many migraine therapies available, there are limitations associated
    with their use. Triptans are effective in the majority of patients for treatment of acute migraine,
    with optimal outcomes associated with early administration while pain is still mild. A major
    concern with use of acute medications such as triptans is the development of medication-
    overuse headache, which is caused by overuse of medication to treat acute or symptomatic
    headaches. Several classes of medications, including antidepressants, beta-blockers,
    anticonvulsants, and onabotulinumtoxinA, have been used in migraine prevention. Adherence
    to many of these preventive treatments can be poor, with adverse effects and lack of efficacy
    cited as the most common reasons for discontinuation of treatment.

    The development of Calcitonin Gene-Related Peptide Receptor Inhibitors (CGRPI)


    heralds a new era for preventive treatment of migraine. These are used treat patients with
    frequent, episodic, and/or chronic migraine headaches that act by antagonism of the calcitonin
    gene-related peptide (CGRP) pathway. This is the first category of pharmaceuticals developed
    as targeted therapy for migraine prevention. Within this class, monoclonal antibodies exert
    their effect by antagonism of the CGRP molecule (eptinezumab, galcanezumab, and
    fremanezumab) or the CGRP receptor (erenumab). Prescribing them for people can diminish
    migraine frequency, headache days, and medication usage. These therapies effectively
    attenuate migraines with or without aura, episodic variants, chronic versions, and medication-
    overuse headaches.

    2. Differentiate the 2 types of CGRP inhibitors. Discuss their mechanism of action?


    Answer:

    The second type of CGRP inhibitors are the CGRP receptor antagonists (gepants). These
    are small molecule drugs which block the CGRP receptor and are effective at both relieving
    migraines and preventing them. Unlike monoclonal antibodies, gepants rapidly penetrate the
    brain so work quickly; however, they are metabolized in the liver so there is a higher potential
    for interactions and possibly liver damage. Gepants demonstrate an extremely high affinity for
    CGRP receptors of human and non-human primates, preventing in this way the interaction
    Assignment – HEADACHE DISORDERS CLINICAL PHARMACY & PHARMACOTHERAPEUTICS 1

    between CGRP and its receptor. The structured N-terminal extracellular (ECD) domain of CLR
    serves as a binding site for gepants, thus providing its fast-acting antagonistic action.

    3. What key patient counseling points should be provided to those taking these medications?
    Answer:

    Reference/s (APA format):

    Deen, M., Correnti, E., Kamm, K., et al. (2017). Blocking CGRP in migraine patients – a review of
    pros and cons. The Journal of Headache and Pain, 18(1). doi:10.1186/s10194-017-0807-1

    Russell, F. A., King, R., Smillie, S.-J., Kodji, X., & Brain, S. D. (2014). Calcitonin Gene-Related
    Peptide: Physiology and Pathophysiology. Physiological Reviews, 94(4), 1099–1142.
    doi:10.1152/physrev.00034.2013

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