Rizatriptanum
Rizatriptanum Uses, Dosage, Side Effects, Food Interaction and all others data.
Rizatriptanum binds with high affinity to human cloned 5-HT1B/1D receptors. Rizatriptanum Benzoate presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system.
Rizatriptanum is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Rizatriptanum also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Rizatriptanum in humans.
Trade Name | Rizatriptanum |
Availability | Prescription only |
Generic | Rizatriptan |
Rizatriptan Other Names | Risatriptan, Rizatriptán, Rizatriptan, Rizatriptanum |
Related Drugs | Ubrelvy, Botox, diclofenac, celecoxib, metoclopramide, sumatriptan, Imitrex, Reglan |
Type | |
Formula | C15H19N5 |
Weight | Average: 269.3449 Monoisotopic: 269.164045633 |
Protein binding | 14% |
Groups | Approved |
Therapeutic Class | 5-HT Agonists |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rizatriptanum Benzoate is used for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years old.
Rizatriptanum is also used to associated treatment for these conditions: Migraine with acute onset aura, Acute Migraine without aura
How Rizatriptanum works
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
Dosage
Rizatriptanum dosage
Dosing Information In Adults: The recommended starting dose of Rizatriptanum Benzoate is either 5 mg or 10 mg for the acute treatment of migraines in adults. The 10-mg dose may provide a greater effect than the 5-mg dose, but may have a greater risk of adverse reactions.
Redosing In Adults: Although the effectiveness of a second dose or subsequent doses has not been established in placebocontrolled trials, if the migraine headache returns, a second dose may be administered 2 hours after the first dose. The maximum daily dose should not exceed 30 mg in any 24-hour period. The safety of treating, on average, more than four headaches in a 30-day period has not been established.
Dosing Information In Pediatric Patients (Age 6 to 17 Years): Dosing in pediatric patients is based on the patient's body weight. The recommended dose of Rizatriptanum Benzoate is 5 mg in patients weighing less than 40 kg, and 10 mg in patients weighing 40 kg or more.
The efficacy and safety of treatment with more than one dose of Rizatriptanum Benzoate within 24 hours in pediatric patients 6 to 17 years of age have not been established.
Dosage Adjustment For Patients On Propranolol: Sections or subsections omitted from the full prescribing information are not listed.
- Adult Patients: In adult patients taking propranolol, only the 5-mg dose of Rizatriptanum Benzoate is recommended, up to a maximum of 3 doses in any 24-hour period (15 mg)
- Pediatric Patients: For pediatric patients weighing 40 kg or more, taking propranolol, only a single 5-mg dose of Rizatriptanum Benzoate is recommended (maximum dose of 5 mg in a 24-hour period). Rizatriptanum Benzoate should not be prescribed to propranolol-treated pediatric patients who weigh less than 40 kg
Administration of Rizatriptanum Benzoate Tablets, administration with liquid is not necessary. Orally disintegrating tablets are packaged in a blister within an outer aluminum pouch and patients should not remove the blister from the outer pouch until just prior to dosing. The blister pack should then be peeled open with dry hands and the orally disintegrating tablet placed on the tongue, where it will dissolve and be swallowed with the saliva.
Side Effects
The following adverse reactions are discussed in more detail in other sections of the labeling:
- Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina
- Arrhythmias
- Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure
- Cerebrovascular Events
- Other Vasospasm Reactions
- Medication Overuse Headache
- Serotonin Syndrome
- Increase in Blood Pressure
Toxicity
Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.
Precaution
Elderly; mild to moderate hepatic or renal impairment; coronary artery disease; pregnancy, lactation. May cause drowsiness. History of seizures. Ensure an interval of at least 24 hr after stopping an ergotamine compound and starting a serotonin (5-HT1) agonist.
Interaction
Propranolol: The dose of Rizatriptanum should be adjusted in propranolol-treated patients, as propranolol has been shown to increase the plasma AUC of rizatriptan by 70%
Ergot-Containing Drugs: Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and Rizatriptanum within 24 hours is contraindicated
Other 5-HT1 Agonists: Because their vasospastic effects may be additive, co-administration of Rizatriptanum and other 5-HT1 agonists within 24 hours of each other is contraindicated
SSRIs /SNRIs And Serotonin Syndrome: Cases of serotonin syndrome have been reported during co-administration of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs)
Monoamine Oxidase Inhibitors: Rizatriptanum is contraindicated in patients taking MAO-A inhibitors and non-selective MAO inhibitors. A specific MAO-A inhibitor increased the systemic exposure of rizatriptan and its metabolite
Food Interaction
- Take with or without food. However, the onset of action may be delayed by approximately 1 hour when taken with food.
Rizatriptanum Cholesterol interaction
[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.
Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).
Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.
In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.
As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.
Periodic cardiovascular evaluations should be performed during intermittent, long-term use.
Rizatriptanum Drug Interaction
Major: duloxetine, ondansetronModerate: acetaminophen / hydrocodoneUnknown: amphetamine / dextroamphetamine, erenumab, diphenhydramine, galcanezumab, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, albuterol, montelukast, topiramate, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, lisdexamfetamine, alprazolam, cetirizine
Rizatriptanum Disease Interaction
Major: CAD risk factors, cardiovascular disease, liver disease, migrainesModerate: PKU, renal dysfunction
Volume of Distribution
- 140 L [male]
- 110 L [female]
Elimination Route
Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.
Half Life
2-3 hours
Elimination Route
Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.
Pregnancy & Breastfeeding use
Pregnancy: Inform patients that Rizatriptanum Benzoate should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus
Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Rizatriptanum Benzoate is administered to a nursing woman. Rizatriptanum is extensively excreted in rat milk, with levels in milk at least 5-fold higher than levels in maternal plasma.
Contraindication
Rizatriptanum Benzoate is contraindicated in patients with:
- Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or other significant underlying cardiovascular disease
- Coronary artery vasospasm including Prinzmetal's angina
- History of stroke or transient ischemic attack (TIA)
- Peripheral vascular disease (PVD)
- Ischemic bowel disease
- Uncontrolled hypertension
- Recent use (i.e., within 24 hours) of another 5-HT1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide)
- Hemiplegic or basilar migraine
- Concurrent administration or recent discontinuation (i.e., within 2 weeks) of a MAO-A inhibitor
- Hypersensitivity to Rizatriptanum Benzoate (angioedema and anaphylaxisseen)
Special Warning
Pediatric Use: Safety and effectiveness in pediatric patients under 6 years of age have not been established. The efficacy and safety of Rizatriptanum in the acute treatment of migraine in patients aged 6 to 17 years was established in an adequate and well-controlled study. The incidence of adverse reactions reported for pediatric patients in the acute clinical trial was similar in patients who received Rizatriptanum to those who received placebo. The adverse reaction pattern in pediatric patients is expected to be similar to that in adults.
Geriatric Use: Clinical studies of Rizatriptanum did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.
Although the pharmacokinetics of rizatriptan were similar in elderly (aged ≥65 years) and in younger adults (n=17), in general, dose selection for an elderly patient should be cautious, starting at the low end of the dosing range. This reflects the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Geriatric patients who have other cardiovascular risk factors (e.g., diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) should have a cardiovascular evaluation prior to receiving Rizatriptanum
Renal Impairment: For mild-moderate impairment, initate with 5 mg. Further dose of 5 mg may be taken after an interval of at least 2 hr. Max: 10 mg/24 hr. Avoid in severe impairment.
Hepatic Impairment: For mild-moderate impairment, initate with 5 mg. Further dose of 5 mg may be taken after an interval of at least 2 hr. Max: 10 mg/24 hr. Avoid in severe impairment.
Acute Overdose
May cause hypertension and CV symptoms. Gastric lavage using activated charcoal may be considered. Monitor ECG and clinical status of the patient.
Storage Condition
Store at 15-30° C.
Innovators Monograph
You find simplified version here Rizatriptanum
Rizatriptanum contains Rizatriptan see full prescribing information from innovator Rizatriptanum Monograph, Rizatriptanum MSDS, Rizatriptanum FDA label
FAQ
What is Rizatriptanum used for?
Rizatriptanum is used to treat acute migraine headaches in adults and children 6 years of age and older. It is not used to prevent migraine headaches and is not used for cluster headaches. Rizatriptanum works in the brain to relieve the pain from migraine headaches.
How does Rizatriptanum work?
Rizatriptanum works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and blocking the release of certain natural substances that cause pain, nausea, and other symptoms of migraine.
How safe is Rizatriptanum?
Rizatriptanum can commonly cause chest,jaw,neck tightness, pain, or pressure that is usually not serious. However, these side effects are like symptoms of a heart attack, which may include chest,jaw,left arm pain, shortness of breath, or unusual sweating.
What are the common side effects of Rizatriptanum?
Common side effects of Rizatriptanum are include:
- drowsiness
- dizziness
- tiredness
- upset stomach
- vomiting
- diarrhea
- muscle pain or cramps
- tremors
- flushing (feeling of warmth)
- dry mouth
Is Rizatriptanum safe during pregnancy?
There is insufficient data to draw conclusions about drug-associated risk for major birth defects and miscarriage; animal studies do not indicate harmful effects at dose levels that exceed therapeutic dose levels with respect to the development of the embryo or fetus, or the course of gestation, parturition and post-natal development.
Is Rizatriptanum safe during breastfeeding?
Infant risk should be minimized by avoiding breastfeeding for 24 hours after administration of this drug.There are no data on the effects of this drug on the breastfed infant or its effects on milk production.
Can I drink alcohol with Rizatriptanum?
Drinking alcoholic beverages can make headaches worse or cause new headaches to occur. People who suffer from severe headaches should probably avoid alcoholic beverages, especially during a headache.
Can I drive after taking Rizatriptanum?
As long as you are feeling dizzy or drowsy, do not drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.
How quickly does Rizatriptanum work?
Take 1 tablet (10 mg) at the start of the migraine attack. Rizatriptanum should work within 30 minutes. If your migraine improves but then comes back, wait at least 2 hours before taking another tablet (10 mg). Do not take more than 3 tablets (30 mg) in 24 hours.
Does Rizatriptanum help with anxiety?
Rizatriptanum is good for treating depression and anxiety, but it can cause more withdrawal symptoms if you stop suddenly compared to other antidepressants.
Does Rizatriptanum make I gain weight?
While it's true that you may notice some weight gain, the benefits of relieving yourself of migraine pain are stronger. Some users may not see any change in weight, and some may even lose weight.
Is Rizatriptanum bad for my heart?
Rizatriptanum should not be used by people with heart or blood vessel disease.
Can Rizatriptanum cause a stroke?
Rizatriptanum may increase your risk of having abnormal heart rhythm, heart attack, angina, or stroke.
Can Rizatriptanum make your headache worse?
Using Rizatriptanum too often can lead to worsened headaches and can cause your migraines to occur more often.
Who should not take Rizatriptanum?
You should not use this medicine if you have uncontrolled high blood pressure, heart problems, a history of heart attack or stroke, or circulation problems that cause a lack of blood supply within the body. Do not take Rizatriptanum within 24 hours before or after using another migraine headache medicine.
Can a diabetic take Rizatriptanum?
Rizatriptanum should not be used by people with heart or blood vessel disease.
What happens if I miss a dose?
Rizatriptanum is used as needed, it does not have a daily dosing schedule. Call your doctor promptly if your symptoms do not improve after using Rizatriptanum.
What happens if I take too much Rizatriptanum?
Using too much Rizatriptanum may increase the chance of side effects. Do not use this medicine for a headache that is not a migraine headache.
Is Rizatriptanum a blood thinner?
Rizatriptanum is a headache medicine that narrows the blood vessels around the brain.
Is Rizatriptanum a painkiller?
Rizatriptanum is not an ordinary pain reliever. It will not relieve any kind of pain other than migraine headaches.