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Rizatriptan Use and Side Effect | Mechanism of Action

Rizatriptan Use for Treatment of Migraine Headache

Rizatriptan is used for the treatment of migraine headaches, it can’t cure the disease completely
but it can reduce the symptoms of disease. it also used for the treatment of other migraine
symptoms like vomiting , pain in headache and eye irritation or light-sensitive to the eye. So this
medicine is prescribed by the doctor for instant action, not for long term use.
Rizatriptan tablets
Rizatriptan tablets

Rizatriptan is available in the market as brand name Maxalt manufacturing by Merck & co
for the migraine headache. Strength of the tablets is 5 mg and 10 mg .

Types of condition when you don’t take Rizatriptan

  • If you have the allergic to this medicine then don’t take this .
  • If you have the moderate blood pressure or severe blood pressure then you don’t take
this medicine.
  • If you suffer the heart disease before some days then you don’t take this medicine .
  • If you suffer the liver problem or kidney problem then you must avoid this medicine .
  • If you recently get the cardiac stroke or ischemic heart disease then you must avoid
the medicine.
  • If patient are a blockage in the arteries then don't take this medicine.
  • If you taking monoamine oxidase inhibitor like moclobemide, phenelzine,
tranylcypromine .
  • If you are anti depression medicine like pargyline.
  • If you are taking antibiotic like linezolid.
  • If you are taking ergotamine for the treatment of migraine headache .
  • If you taking any other tryptan group medicine .

Rizatriptan Side Effect

Some common side effects are

Tingling , headache, decreased sensitivity of skin, reduce the brain sharpness, insomnia,
dizziness, sleepiness, and tiredness, irregular heart beat, redness of face , throat discomfort,
nausea, dry mouth, vomiting , diarrhea, indigestion, neck pain, pain in abdomen or chest.

Some uncommon side effect are


  • Change is mouth taste .
  • Blurred vision
  • Tremon
  • Fainting
  • Confusion
  • Nervousness
  • High blood pressure
  • Thirst
  • Hot flushes
  • Wheezing
  • Life threatening allergic reaction

Mechanism of action

When you read about this medicine one question is comes to your mind
how rizatriptan works so i try to clear the doubt this question.
Chemically it is derived from the N,N dimethyltryptamine and comes from tryptamine group.
Rizatriptan is a selective 5-HT receptor agonist. 5 HT receptor subtype named as 5-HT1B
and 5-HT 1D. It has a weak affinity to another subtype 5HT receptor-like 5-HT1A and 5HT5A
and 5HT7 and no affinity towards the receptor 5 HT2, 5HT3 and 5-HT4 receptor .


This medicine is bind with the 5 HT 1B or 1D it show the action like vasoconstriction of
meningeral ,dural,cerebral or pial vessel. In the migraine headache occur because dilation
of vessel when secretion of neurotransmitter from the nerve ending .

It also inhibit the trigeminal nuclei cell (which is the largest nerve nuclei present is the human)
via 5-HT1B and 5-5HT1D receptor agonist in the brain.

Pharmacokinetics  of Rizatriptan

Absorption

This medicine is completely orally absorbed and its bioavailability is about 45% .plasma
peak concentration of the medicine are 1-1.5 hours. Without food its plasma peak
concentration is reaches fast. Food is not affect the bioavailability of the medicine .
oral disintegrating tablets are also available for the better absorption.


Rizatriptan bioavailability is more than sumatriptan so this medicine is more effective against
the migraine disease.

Distribution

This medicine volume of distribution is 140 -110 liter in the male and female .its plasma
protein binding capacity is 14 % .

Metabolism

This medicine is metabolized monoamine oxidase A isoenzyme to formation of indole acetic
acid and other compound like N-oxide and 6-hydroxy group containing compound . which is
inactive against the receptor 5-HT1B/1D . but N-monodesmethyl -rizatriptan having binding
capacity is 14% in the plasma protein .

Excretion

This medicine is excreted through the urine and also faces .complete excretion time is
120 hours in between 120 hours 82% of drug are excreted through the urine and 12% are
excreted through the faces.

Dose of rizatriptan

Always take the medicine as per the doctor prescription if have seen any side effect
immediately consult your doctor .

The normal dose of this medicine is 10 mg but if you suffer any kidney or liver problem
then you reduced the dose up to 5 mg .dose of this medicine is takes for the single migraine
stroke attacks for the next stroke you take another dose . two conjugative dose time gap is
2 hours.

Maxalt is available in the oral lyophilisate form to avoid nausea and vomiting.
don’t take multiple-dose in the single day .if some take multiple doses is taken then immediately
take into medicals for better observation.

Rizatriptan interaction with other medicine

Don’t take this medicine with the monoamine oxidase inhibitor like isocarboxazid , linezolid,
methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline . if
you take rizatriptan with the above medicine then you suffer the serious interaction.consult
with the doctor before take this medicine .
If you take rizatriptan with other medicine which is increase the serotonin level in the body .
selective serotonin reuptake inhibitor like fluoxetine paroxetine .it may produce the harmfull
drug interaction.


This medicine may interact with ergotamine medicine like dihydroergotamine . and it also
interact with the medicine like all triptan group like sumatriptan.

What is the price of rizatriptan tablets

Sun pharmaceutical manufacture named as Rizanet 10 mg oral Disintegrating strips price
53 rupees for one pouch.
Intas pharmaceutical ltd manufacture RIZORA 10 mg tablets price 254 rupees for the 4
tablets .
Sun pharmaceutical ltd also manufacture named as RIZANET 10 mg tablets tablets 53
rupees for 10 tablets
Cipla manufacture named as RIZACT 10 mg tablets price 230 rupees for the 4 tablets .


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