Clinical data | |
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Trade names | Maxalt, Maxalt-MLT, Rizafilm, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601109 |
License data |
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Pregnancy category |
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Routes of administration | By mouth |
Drug class | Triptan |
ATC code | |
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Legal status | |
Pharmacokinetic data | |
Bioavailability | 45% |
Protein binding | 14% |
Metabolism | By monoamine oxidase |
Elimination half-life | 2–3 hours |
Excretion | 82% urine; 12% feces |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.243.719 |
Chemical and physical data | |
Formula | C15H19N5 |
Molar mass | 269.352 g·mol−1 |
3D model (JSmol) | |
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Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. [1] [3] It is taken by mouth. [1] [3] It can also be applied on the tongue. [2] It is a serotonin (5-HT) 1B/1D receptor agonist (triptan). [1] [2]
Common side effects include chest pain, dizziness, dry mouth, and tingling. [3] Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis. [3] Excessive use may result in medication overuse headaches. [3] Use is not recommended during pregnancy and breastfeeding is not recommended within 24 hours after taking a dose. [4] Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor. [3]
Rizatriptan was patented in 1991 and came into medical use in 1998. [5] [6] It is available as a generic medication. [4] In 2021, it was the 159th most commonly prescribed medication in the United States, with more than 3 million prescriptions. [7] [8]
Rizatriptan is indicated to treat acute migraine attacks with or without aura. [1] [2] It does not prevent future migraine attacks. [9] A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan. [10]
Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions. [11]
Frequent adverse effects (incidence less than 10%) are dizziness, drowsiness, asthenia/fatigue, and nausea. Clinical adverse experiences were typically mild and short-lasting (2–3 hours). [11]
Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. [13] Like the other triptans sumatriptan and zolmitriptan, rizatriptan induces vasoconstriction—possibly by inhibiting the release of calcitonin gene-related peptide from sensory neurons in the trigeminal nerve. [13]
Brand names include Rizalt, Rizalt RPD, Rizact (India), Rizafilm, [2] Maxalt, [1] and Maxalt-MLT. [1] [14] [15] [16]
Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken orally, intranasally, or by subcutaneous injection. Therapeutic effects generally occur within three hours.
Ergotamine, sold under the brand name Ergomar among others, is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is structurally similar to several neurotransmitters, and it acts as a vasoconstrictor. It is used for acute migraines, sometimes with caffeine as the combination ergotamine/caffeine.
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. This drug class was first commercially introduced in the 1990s. While effective at treating individual headaches, they do not provide preventive treatment and are not considered a cure. They are not effective for the treatment of tension–type headache, except in persons who also experience migraines. Triptans do not relieve other kinds of pain.
Zolmitriptan, sold under the brand name Zomig among others, is a triptan used in the acute treatment of migraine attacks with or without aura and cluster headaches. It is a selective serotonin receptor agonist of the 1B and 1D subtypes.
Prochlorperazine, formerly sold under the brand name Compazine among others, is a medication used to treat nausea, migraines, schizophrenia, psychosis and anxiety. It is a less preferred medication for anxiety. It may be taken by mouth, rectally, injection into a vein, or injection into a muscle.
Dihydroergotamine (DHE), sold under the brand names D.H.E. 45 and Migranal among others, is an ergot alkaloid used to treat migraines. It is a derivative of ergotamine. It is administered as a nasal spray or injection and has an efficacy similar to that of sumatriptan. Nausea is a common side effect.
Ergotamine/caffeine, sold under the brand name Cafergot among others, is a fixed-dose combination medication used for the treatment of migraine. It contains ergotamine, as the tartrate, an alpha adrenergic blocking agent; and caffeine, a cranial vasoconstrictor.
Methylergometrine, also known as methylergonovine and sold under the brand name Methergine, is a medication of the ergoline and lysergamide groups which is used as an oxytocic in obstetrics and in the treatment of migraine. It reportedly produces psychedelic effects similar to those of lysergic acid diethylamide (LSD) at high doses.
Methysergide, sold under the brand names Deseril and Sansert, is a monoaminergic medication of the ergoline and lysergamide groups which is used in the prophylaxis and treatment of migraine and cluster headaches. It has been withdrawn from the market in the United States and Canada due to adverse effects. It is taken by mouth.
Almotriptan is a triptan medication discovered and developed by Almirall for the treatment of heavy migraine headache.
Eletriptan, sold under the brand name Relpax and used in the form of eletriptan hydrobromide, is a second-generation triptan medication intended for treatment of migraine headaches. It is used as an abortive medication, blocking a migraine attack which is already in progress. Eletriptan is marketed and manufactured by Pfizer Inc.
Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin, a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors.
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.
Naratriptan (trade names include Amerge) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. It is a selective 5-HT1 receptor subtype agonist.
Sumatriptan/naproxen, sold under the brand name Treximet among others, is a fixed-dose combination medication used to treat migraines. It is taken by mouth. It contains sumatriptan, as the succinate, a serotonin 5-hydroxytryptamine (5-HT) 1b/1d receptor agonist (triptan); and naproxen as the sodium salt, a member of the arylacetic acid group of nonsteroidal anti-inflammatory drugs (NSAIDs).
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They are selective 5-hydroxytryptamine/serotonin1B/1D (5-HT1B/1D) agonists. Migraine is a complex disease which affects about 15% of the population and can be highly disabling. Triptans have advantages over ergotamine and dihydroergotamine, such as selective pharmacology, well established safety record and evidence-based prescribing instructions. Triptans are therefore often preferred treatment in migraine.
Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute treatment of migraine with or without aura in adults. It is not useful for prevention. It is taken by mouth.
Migraine may be treated either prophylactically (preventive) or abortively (rescue) for acute attacks. Migraine is an complex condition; there are various preventive treatments which disrupt different links in the chain of events that occur during a migraine attack. Rescue treatments also target and disrupt different processes occurring during migraine.
Ditans are a class of abortive medication for the treatment of migraines. The first ditan, Eli Lilly's lasmiditan, was approved by the FDA in 2019.
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