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Zolmitriptan of Usage and Synthesis.

Zolmitriptan is a highly effective and specific treatment for acute migraine by activating the 5-HT1 receptor to cause vasoconstriction and inhibit the release of neuropeptides, thereby relieving migraine attacks. The results show that Zolmitriptan can control cerebral peripheral blood flow, and can also act on the pain center of the brain, so as to play a role in the treatment of migraine.

When trigeminal nerve stimulation or migraine attack, cerebral blood flow increased, calcitonin gene-related peptide (CGRP) released, CGRP and vasoactive peptide (VIP) increased in the external jugular vein. Zolmitriptan can penetrate the blood-brain barrier, has dual functions of central and peripheral nerves, selectively constricts intracranial blood vessels, especially cranial arteries, and controls cerebral peripheral blood flow.

It can also inhibit the release of vasoactive substances such as CGRP, neurotransmitters A and P, so that the dural artery blood vessels contraction, reduce sterile inflammation. Studies have shown that Zolmitriptan has an inhibitory effect on HVA Ca2+ ion channels, thereby reducing the release of neurotransmitters (such as CGRP) and playing a role in the treatment of migraine.

Uses of Zolmitriptan.

For the acute treatment of migraine with or without premonitory symptoms.It is suitable for the acute treatment of migraine with or without aura symptoms, and should not be used for basilar artery or hemiplegic migraine. Zolmitriptan is a selective 5-hydroxytryptamine (5-HT) receptor agonist that is indicated for the acute treatment of migraine with or without premensive symptoms.

Drug interaction of Zolmitriptan.

1. There is no evidence that the use of migraine prophylactic drugs (e.g., beta blockers, oral dihydroergosine, benthidine) has any effect on the efficacy of this product. Acute symptomatic treatment, such as the use of acetaminophen, metoclopramide and ergotamine do not affect the pharmacokinetics and tolerance of this product.

2. Selegiline (a monoamine oxidase B inhibitor) and fluoxetine (a selective serotonin reuptake inhibitor) have no effect on the pharmacokinetic parameters of this product. Use of other 5HTID agonists should be avoided within 12 hours of treatment with this product. With Moclobemide, A specific monoamine oxidase A inhibitor, there was a small (26%) increase in area under the curve of Zolmitriptan and a threefold increase in area under the curve of the active metabolite. Therefore, for patients using monoamine oxidase A inhibitors, it is recommended that the maximum dose of this product be 7.5mg within 24 hours.

3. When combined with cimetidine and oral contraceptives, the blood concentration of this product can also be increased.

4. Combined with propranolol can delay the metabolism of this product.

Product method of Bulk Zolmitriptan Powder.

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