Gepant
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Gepant
Calcitonin gene-related peptide (CGRP) receptor antagonists, commonly known as gepants, are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR). Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine. Nerve activation triggers the release of CGRP and other neuropeptides, leading to inflammation, pain, and swelling. Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents. Drugs of this class have also been investigated for use in osteoarthritis. Examples Non-peptide small molecules * Ubrogepant is approved for acute treatment of migraines *Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines * Atogepant (AGN-241689) is approved for preventative treatment of migraines * Zavegepant (BHV- 3500) is a nasal spray approved for acute treatment of migraines. * Telcagepant (MK-0974), reached phase III clinical trials; ...
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Atogepant
Atogepant, sold under the brand name Qulipta among others, is a medication used to prevent migraines. It is a gepant, a calcitonin gene-related peptide receptor antagonist administered orally. The most common side effects include nausea, constipation, tiredness, somnolence (sleepiness), decreased appetite, and decreased weight. Atogepant was approved for medical use in the United States in September 2021, and in the European Union in August 2023. Medical Uses Atogepant is indicated for the preventive treatment of episodic migraine in adults. In the European Union, atogepant (Aquipta) is indicated for prophylaxis (prevention) of migraine in adults who have at least four migraine days per month. History Atogepant was developed by the biopharmaceutical company AbbVie. The benefits and side effects of atogepant were evaluated in two clinical trials of 1,562 participants with a history of migraine headaches occurring on 4 to 14 days per month. The two trials to show the ben ...
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Rimegepant
Rimegepant, sold under the brand name Nurtec ODT among others, is a medication used for the acute treatment of migraine with or without aura (migraine), aura in adults and the prophylactic/ preventive treatment of episodic migraine in adults. It is taken Oral administration, by mouth to dissolve on or sublingual medication, under the tongue. It works by blocking CGRP receptors. In the United States, rimegepant was approved for treating acute migraine in February 2020, and its approval was extended to preventing episodic migraine in June 2021. It is produced and marketed by Pfizer. In March 2021, rimegepant was approved for medical use in the United Arab Emirates and in Israel. It was approved for medical use in Canada in December 2023. In the United Kingdom, rimegepant is approved by NICE for the prophylaxis and treatment of acute migraine in adults. Medical uses Rimegepant is indicated for the treatment of acute migraine with or without aura in adults and for the preventati ...
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Ubrogepant
Ubrogepant, sold under the brand name Ubrelvy, is a medication used for the acute (immediate) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not indicated for the preventive treatment of migraine. Ubrogepant is a small-molecule calcitonin gene-related peptide receptor antagonist. It is the first drug in this class approved for the acute treatment of migraine. The most common side effects are nausea, tiredness and dry mouth. Ubrogepant is contraindicated for co-administration with strong CYP3A4 inhibitors. History Ubrogepant, also known as MK-1602, was discovered by scientists at Merck. The effectiveness of ubrogepant for the acute treatment of migraine was demonstrated in two randomized, double-blind, placebo-controlled trials. In these studies, 1,439 adult patients with a history of migraine, with and without aura, received the approved doses of ubrogepant to treat an ongoing migraine. In both studies, the percentages ...
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Zavegepant
Zavegepant, sold under the brand name Zavzpret, is a medication used for the treatment of migraine. Zavegepant is a calcitonin gene-related peptide receptor antagonist. It is sprayed into the nose. It is sold by Pfizer. The most common adverse reactions include taste disorders, nausea, nasal discomfort, and vomiting. Zavegepant was approved for medical use in the United States in March 2023. Medical uses Zavegepant is indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ... for the acute treatment of migraine with or without aura in adults. References Further reading * * * External links * * {{Portal bar , Medicine Antimigraine drugs Calcitonin gene-related peptide receptor antagonists Drugs developed by Pfizer Piperazines Piperidines Indazoles ...
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Telcagepant
Telcagepant (INN; development code MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co. In the acute treatment of migraine, it was found to have equal efficacy to rizatriptan and zolmitriptan. A Phase IIa clinical trial studying telcagepant for the prophylaxis of episodic migraine was stopped on March 26, 2009, after the "identification of two patients with significant elevations in serum transaminases". A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme alanine transaminase (ALT) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication. In July 2011, Merck announced that it had discontinued development of telcagepant. See also * Olcegepant Olcegepant (INN, code name BIBN-4096BS) is a calcitonin gene-rel ...
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Olcegepant
Olcegepant (INN, code name BIBN-4096BS) is a calcitonin gene-related peptide receptor antagonist being studied as a potential treatment for migraine Migraine (, ) is a complex neurological disorder characterized by episodes of moderate-to-severe headache, most often unilateral and generally associated with nausea, and light and sound sensitivity. Other characterizing symptoms may includ ...s. A 2013 meta-analysis found olcegepant and telcagepant were effective and safe compared to placebo. See also * Telcagepant References Amines Antimigraine drugs Carboxamides Organobromides Piperazines Piperidines 4-Pyridyl compounds Quinazolines Calcitonin gene-related peptide receptor antagonists {{nervous-system-drug-stub ...
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Antimigraine Agent
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks. Treatment of acute symptoms Examples of specific antimigraine drug classes include triptans (first line option), ergot alkaloids, ditans and gepants. Migraines can also be treated with unspecific analgesics such as nonsteroidal anti-inflammatory drugs (NSAIDs) or acetaminophen. Opioids are not recommended for treatment of migraines. Triptans The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. Due to their safety, efficacy and selectivity, triptans are considered first line agents for abortion of migraines. These medications are selective 5-HT1B/1D receptor agonists with some activity at 5-HT1F. They produce an antimigraine effect by vasoconstriction of the vessels in the brain, as w ...
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Galcanezumab
Galcanezumab, sold under the brand name Emgality, is a humanized monoclonal antibody used for the prevention of migraine. It is also used for the treatment of cluster headaches. A substance called calcitonin gene-related peptide (CGRP) has been shown to be involved in the development of migraine by widening blood vessels in the brain. Galcanezumab is a monoclonal antibody (a type of protein) designed to attach to and block CGRP, thereby helping blood vessels to return to their normal size. This will stop the symptoms of migraine. Galcanezumab is generally delivered through self-injections. Common side effects include injection site reactions such as pain or redness. Other side effects may include hypersensitivity reactions. Galcanezumab was developed by Eli Lilly. It was approved for medical use in the United States and in the European Union in 2018, becoming the third calcitonin gene-related peptide (CGRP) inhibitor to be approved by the US Food and Drug Administration ...
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Fremanezumab
Fremanezumab, sold under the brand name Ajovy, is a medication used to prevent migraines in adults. It is given by subcutaneous injection (injection under the skin). The most common side effect is pain and redness at the site of injection. Other side effects include allergic reactions. It is in the calcitonin gene-related peptide antagonist class of medications. It was approved for medical use in the United States in 2018, the European Union in 2019, the United Kingdom in 2020, and Argentina by September 2021. Medical uses Fremanezumab was shown to be effective in adults with four or more attacks per month. It comes in Monthly and Quarterly injection dosages. Adverse effects The most common adverse reactions are located at the injection site, which occurred in 43 to 45% of people in studies (as compared to 38% under placebo). Hypersensitivity reactions occurred in fewer than 1% of patients. Interactions Fremanezumab does not interact with other antimigraine drugs ...
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Erenumab
Erenumab, sold under the brand name Aimovig, is a medication which blocks the calcitonin gene-related peptide receptor (CGRPR) for the prevention of migraine. It is administered by subcutaneous injection. Erenumab, which was developed by Amgen and Novartis, was approved in May 2018, and was the first CGRPR antagonist to be approved by the U.S. Food and Drug Administration. In 2020, it was the 234th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses Erenumab is indicated for the prevention of migraine in adults. Side effects Common side effects are constipation, pruritus, muscle spasms, as well as mild and mostly transient reactions at the injection site. Interactions Erenumab was shown not to interact with ethinylestradiol, norgestimate or the migraine drug sumatriptan. It is expected to generally have a low potential for interactions because it is not metabolized by cytochrome P450 enzymes. Pharmacology M ...
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Necrotizing Fasciitis
Necrotizing fasciitis (NF), also known as flesh-eating disease, is an infection that kills the body's soft tissue. It is a serious disease that begins and spreads quickly. Symptoms include red or purple or black skin, swelling, severe pain, fever, and vomiting. The most commonly affected areas are the limb (anatomy), limbs and perineum. Bacterial infection is by far the most common cause of necrotizing fasciitis. Despite being called a "flesh-eating disease", bacteria do not eat human tissue. Rather, they release toxins that cause tissue death. Typically, the infection enters the body through a break in the skin such as a cut or burn. Risk factors include recent trauma or surgery and immunodeficiency, a weakened immune system due to diabetes or cancer, obesity, alcoholism, intravenous drug use, and peripheral artery disease. It does not usually spread between people. The disease is classified into four types, depending on the infecting organisms. Medical imaging is often helpfu ...
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