Rizatriptan (Maxalt) - Uses, Dose, Brands

Rizatriptan (Maxalt) is a 5-HT receptor agonist that causes vasoconstriction of the serotonin receptors present in the cranial arteries. It is prescribed for the short-term relief of migraines, aura or not.

Rizatriptan (Maxalt) Dose in Adults:

Note:

In a medical context where ECG monitoring is possible, patients who have coronary artery disease risk factors should be advised to start taking the first medication.

Rizatriptan (Maxalt) Dose in the treatment of Migraine:

  • 5 to 10 mg orally
  • If the patient's symptoms are still present after two hours, the dose may be repeated.
  • 30 mg is the maximum daily dose.
  • Dose adjustment with concomitant propranolol therapy:

    • 5 mg/dose
    • The maximum dose should not exceed 15 mg per day.

Rizatriptan (Maxalt) Dose in Children

Rizatriptan (Maxalt) Dose in the treatment of acute Migraine:

  • Children older than 6 years:

  • Note:
    • Multiple daily doses have not been proven to be safe or effective in youngsters.
      • weight < 40 kgs:

        • one dose of 5 mg
      • Children weighing 40 kgs or more:

        • one dose of 10 mg
  • Dosage adjustment with concomitant propranolol:

    • Children and Adolescents 6 to 17 years:

      • Less than 40 kgs:

        • Avoid using rizatriptan
      • Weight more than 40 kgs:

        • the single dose of 5 mg
        • The maximum dose is 5 mg over the course of a day.
    • Adolescents ≥ 18 years:

      • orally 5 mg
      • After two hours, the dose may be repeated.
      • The daily dose cap is set at 15 mg.

Pregnancy Risk Factor C

  • Pregnant women are being tested for Rizatriptan.
  • Although limited data has not shown any adverse outcomes for fetal health, the manufacturer suggests that you consider other preferred treatment options.

Use while breastfeeding

  • It is unknown if the drug will be excreted into breastmilk.
  • Manufacturer recommends alternative preferred drugs.
  • You should use it with caution when breastfeeding infants.

Dose in renal disease:

  • The manufacturer has not recommended any adjustments in the dose.
  • However, in patients on hemodialysis, the AUC was 44% greater.

Dose in liver disease:

  • The manufacturer has not recommended any adjustments in the dose.
  • In patients with moderate hepatic impairment, plasma concentration may increase by 30%. 

Side Effects of Rizatriptan (Maxalt):

  • Cardiovascular:

    • Chest Pain
    • Flushing
    • Palpitations
    • Flushing
  • Central Nervous System:

    • Dizziness
    • Drowsiness
    • Fatigue
    • Paresthesia
    • Pain
    • Feeling Of Heaviness
    • Headache
    • Euphoria
    • Hypoesthesia
  • Gastrointestinal:

    • Nausea
    • Xerostomia
    • Sore Throat
    • Abdominal Distress
    • Diarrhea
    • Vomiting
  • Neuromuscular & Skeletal:

    • Weakness
    • Jaw Pain
    • Jaw Pressure
    • Jaw Tightness
    • Neck Pain
    • Neck Pressure
    • Neck Tightness
    • Tremor
  • Respiratory:

    • Pharyngeal Edema
    • Pressure On Pharynx
    • Dyspnea

Contraindications to Rizatriptan (Maxalt):

  • Allergy reactions to any component of the drug or the drug itself
  • Ischemic heart disease and other serious cardiovascular diseases
  • Vasospasm of the Coronary Artery
  • History of strokes or TIA (transient ischemic attacks)
  • Peripheral Vascular Disease
  • Bowel Ischemia
  • Hypertension uncontrolled
  • Basilar or hemiplegic headache
  • Within 24 hours of taking another 5-HT antagonist, an ergot-containing or ergot-type medicine, such as methysergide, or after using MAO inhibitors concurrently within 2 weeks or less.
  • Ophthalmoplegic migraine
  • Severe hepatic impairment.

Warnings and precautions

  • Cardiac events

    • The use of 5-HT agonists has been linked to fatal cardiac events include acute coronary artery vasospasm, myocardial damage, ischemia, ventricular tachycardia, and ventricular fibrillation.
    • Patients should be told to seek medical attention if they experience chest pain, heaviness or chest tightness, exertional pain or dyspnea, as well as apprehension.
    • Patients with symptoms should be examined for prinzmetal's Angina.
  • Cerebrovascular events

    • Use of 5-HT agonists has been linked to stroke, cerebral and subarachnoid hemorhage.
    • Triptans should be avoided in patients who have had strokes or transient ischemic attacks.
  • High blood pressure

    • Hypertension and hypertensive crises can develop in patients.Triptans have been linked to hypertension in patients who were previously normotensives.
  • Headaches

    • Patients who take acute migraine medication for more than 10 days per month may experience headaches from medication overuse.
    • Treatment withdrawal might be required in these cases.
  • Vasospasm-related events

    • It can cause ischemic and vasospasm.It is possible for patients to develop peripheral vascular or gastrointestinal ischemia.
  • Visual effects

    • With 5-HT agonists, vision problems can be permanent or transient.
  • Coronary artery disease

    • Patients with coronary heart disease risk factors shouldn't be given the medication without receiving a proper cardiac examination.
    • Patients with a satisfactory evaluation should receive the first dose in a healthcare setting and ECG monitoring.
    • These are coronary heart disease risk factors:
      • Hypertension
      • Hypercholesterolemia
      • Smoker
      • Obesity
      • Diabetes
      • Strong family history in CAD
      • Menopause
      • Males over 40 years old
    • Patients at high risk should be checked for signs and symptoms of angina.
  • Hepatic impairment

    • Drug plasma concentrations rise as clearance is reduced. It shouldn't be used by anyone with severe hepatic impairment.
  • Renal impairment

    • Patients with kidney disease are more likely to be exposed systemically.Take care.

Rizatriptan: Drug Interaction

Risk Factor C (Monitor therapy)

Antiemetics (5HT3 Antagonists)

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Antipsychotic Agents

Serotonin modulators might make antipsychotic drugs more harmful or toxic. Serotonin modulators, in particular, may enhance dopamine blockade, potentially raising the risk for neuroleptic malignant syndrome. Serotonin modulators' serotonergic effects may be strengthened by antipsychotic drugs.Serotonin syndrome might occur from this.

Droxidopa

Droxidopa's hypertensive action may be enhanced by serotonin 5-HT1D receptor antagonists.

Metaxalone

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Methylphenidate

Serotonin modulators' harmful or toxic effects could be exacerbated. In particular, there may be an increased risk of serotonin syndrome or serotonin poisoning.

Metoclopramide

Serotonin modulators may intensify Metoclopramide's harmful or hazardous effects. These could appear as signs of neuroleptic malignant syndrome or serotonin syndrome.

Opioid Agonists

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Serotonin Modulators

The negative or hazardous effects of other serotonin modulators might be increased. Serotonin syndrome may start to develop. Nicergoline and Tedizolid are exceptions.

TraMADol

Serotonin modulators may intensify TraMADol's harmful or hazardous effects. Seizures may become more likely. The serotonergic impact of serotonin modulators may be enhanced by TraMADol. Serotonin syndrome might occur from this.

Risk Factor D (Consider therapy modification)

Propranolol

Rizatriptan serum levels can rise. Treatment: Patients using propranolol should only get 5 mg of the adult dose of rizatriptan.

Risk Factor X (Avoid combination)

Dapoxetine

May enhance the adverse/toxic effect of Serotonin Modulators.

Ergot Derivatives

May enhance serotonin 5-HT1D receptor antagonists' ability to constrict blood vessels. The vasoconstrictive effects of ergot derivatives may be enhanced by serotonin 5-HT1D receptor antagonists. Exceptions: Nicergoline.

Methylene Blue

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Monoamine Oxidase Inhibitors

May slow down the metabolism of substances that block serotonin 5-HT1D receptors. Management: Naratriptan, eletriptan, or frovatriptan may be suitable 5-HT1D agonists to use if MAO inhibitor medication is necessary.

SUMAtriptan

The negative/toxic effects of sumatriptan may be increased by serotonin 5-HT1D receptor antagonists.

Monitor:

  • Patients' reaction to treatment (Monitor Headache severity).
  • Examine the angina clinical signs.
  • Patients at high risk for coronary artery disease should monitor their BP, heart rate and ECG. The first dose is used to monitor the patient. Patients at high risk who require cardiac monitoring include:
    • Patients with hypertension
    • Patients with Dyslipidemia
    • Obese
    • Diabetic patients
    • Smokers
    • Patients with strong family history of coronary heart disease.

How to administer Rizatriptan (Maxalt)?

  • It can be taken without regard for food. MAXALT-MLT tablets can be taken orally. 
  • Patients have the option of placing the tablet on their tongue and letting it dissolve. After that, the saliva will be swooled.

Mechanism of action of Rizatriptan (Maxalt):

  • It acts as a selective serotonin receptor agonist (5-HT-1B, 5-HT-1D), in the cranial arteries. 
  • It reduces migraine symptoms by increasing blood flow and reducing inflammation.

The beginning of actionThe time taken to respond to treatment is 2 hours.

Absorption is Complete

Protein binding: 14%

Metabolism: It is metabolized by the enzyme monoamine oxidase-A forming metabolites. It undergoes significant first-pass metabolism.

Bioavailability: About 45%

Half-life elimination: 2-3 hours

Time to peak:

  • Maxalt: 1 to 1.5 hours;
  • Maxalt-MLT: 1.6 to 2.5 hours

Excretion: Urine (82%, 14% as unchanged drug); feces (12%)

Brand Names of Rizatriptan (International):

  • Maxalt
  • Maxalt-MLT
  • ACT Rizatriptan
  • ACT Rizatriptan ODT
  • APO-Rizatriptan
  • APO-Rizatriptan RPD
  • AuroRizatriptan
  • CCP-Rizatriptan ODT
  • DOM-Rizatriptan RDT
  • JAMP-Rizatriptan
  • JAMP-Rizatriptan IR
  • JAMP-Rizatriptan ODT
  • MAR-Rizatriptan
  • MAR-Rizatriptan ODT
  • Maxalt
  • Maxalt RPD
  • MINTRizatriptan ODT
  • MYLAN-Rizatriptan ODT
  • NAT-Rizatriptan ODT
  • PMS-Rizatriptan RDT
  • RIVARizatriptan ODT
  • SANDOZ Rizatriptan ODT
  • TEVA-Rizatriptan ODT
  • VAN-Rizatriptan ODT
  • VAN-Rizatriptan
  • Amigran
  • maxalt
  • Maxalt
  • Maxalt RPD
  • Maxaltlyo
  • Maxatan
  • Migoff
  • Migrapain
  • Migriz
  • Migson
  • Ouliting
  • Risamigren
  • Rizact
  • Rizagrain
  • Rizalt
  • Rizamelt
  • Rizamig
  • Rizat
  • Rizatan
  • Rizatin
  • Triptaxalat

Rizatriptan Brand Names in Pakistan:

No Brands Available in Pakistan.