DESCRIPTION
PHARMACOLOGY-
Zolmitriptan 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 Zolmitriptan 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 Zolmitriptan in humans.
MECHANISM OF ACTION-
Zolmitriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
SIDE EFFECTS-
The Zomig ZMT dissolvable pill contains aspartame, and should be avoided by anyone sensitive to that ingredient and by those suffering from phenylketonuria.
Rarely, serious cardiac events, including myocardial infarction, have been associated with zolmitriptan.
minor adverse reactions include: hypesthesia, paresthesia (all types), warm and cold sensations, chest pain, throat and jaw tightness, dry mouth, dyspepsia, dysphagia, nausea, somnolence, vertigo, asthenia, myalgia, myasthenia and sweating.
DRUG DRUG INTERACTIONS-
The serum concentration of Zolmitriptan can be increased when it is combined with Abiraterone.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Acepromazine.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Aceprometazine.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Acetophenazine.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Almotriptan.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Amisulpride.
The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Amitriptyline.
USES-
Zolmitriptan is used to treat migraines. It helps to relieve headache, pain, and other migraine symptoms (including nausea, vomiting, sensitivity to light/sound). Prompt treatment helps you return to your normal routine and may decrease your need for other pain medications. Zolmitriptan belongs to a class of drugs known as triptans. It affects a certain natural substance (serotonin) that causes narrowing of blood vessels in the brain. It may also relieve pain by affecting certain nerves in the brain.
Zolmitriptan does not prevent future migraines or lessen how often you get migraine attacks.
REFERENCE:
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.179
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