Zultra 50mg Tab 20’s

Potential Overview:

Drug Name :Zultra 50 mg Tablet

Generic Name :Zolmitriptan

Pack Size:20 Tablets

Strength:50 mg per tablet

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Mechanism of Action (MOA):

Zolmitriptan is a selective serotonin (5-HT1) receptor agonist (often referred to as a triptan). It specifically acts on the 5-HT1B/1D receptors located on blood vessels and nerve terminals in the brain. Here’s how it works:

1. Constricts blood vessels in the brain: It binds to 5-HT1B receptors, causing vasoconstriction (narrowing of the blood vessels) and reducing the inflammation associated with migraine attacks.
2. Inhibits neurogenic inflammation: By stimulating 5-HT1D receptors, it reduces the release of pro-inflammatory neuropeptides (like substance P and calcitonin gene-related peptide, CGRP), which contribute to migraine pain and other symptoms.
3. Modulates pain pathways: Zolmitriptan reduces the transmission of pain signals through the trigeminal nerve, which is involved in the migraine process.

This combined effect helps to relieve acute migraine attacks and provides symptomatic relief by addressing both the vascular and neurogenic components of migraines.

Indications:

• Acute treatment of migraine attacks: Zolmitriptan is used for the acute treatment of migraine headaches, with or without aura. It is not used for the prevention of migraines.
• Cluster headaches (off-label use): Sometimes used in the acute treatment of cluster headaches, although this is not an FDA-approved indication.

Dosage:

1. Migraine Attack:
   • Initial Dose: 2.5 mg to 5 mg (taken as a single dose).
   • If the migraine is not completely relieved after the first dose, a second dose can be taken after 2 hours. However, do not exceed 10 mg in a 24-hour period.
   • Maintenance Dose: Typically 5 mg per attack.
2. Special Populations:
   • Renal or Hepatic Impairment: Reduce the dose in patients with severe renal or hepatic impairment.
   • Elderly: It is recommended to start at a lower dose (e.g., 2.5 mg) and adjust based on response.

Side Effects:

Common side effects include:

1. Central Nervous System:
   • Dizziness, somnolence (sleepiness), numbness, or a tingling sensation (paresthesia).
   • Fatigue, headache (unrelated to the migraine), lightheadedness.
2. Cardiovascular:
   • Chest discomfort or tightness (rare but serious).
   • Flushing (redness or warmth of the skin).
   • Increased blood pressure.
3. Gastrointestinal:
   • Nausea, dry mouth, or bad taste.
4. Serious Side Effects:
   • Chest pain, which may indicate a potential risk of cardiac ischemia (especially in patients with underlying cardiovascular disease).
   • Severe allergic reactions such as anaphylaxis, though rare.
   • Serotonin syndrome (rare, but serious when combined with other serotonergic drugs).

Precautions:

• Cardiovascular Health: Caution in patients with a history of cardiovascular disease (e.g., heart attack, arrhythmia, angina). Zolmitriptan can cause vasoconstriction, which may worsen underlying heart conditions.
• Renal or Hepatic Impairment: Dosage adjustments may be required in patients with severe renal or hepatic impairment.
• Serotonin Syndrome: Risk increases when zolmitriptan is taken with other drugs that increase serotonergic activity (e.g., SSRIs, SNRIs, MAO inhibitors).
• Pregnancy: Category C (risk cannot be ruled out). Use during pregnancy only if clearly needed.
• Breastfeeding: It is not known if zolmitriptan passes into breast milk; caution should be used when considering its use during breastfeeding.
• Elderly: Lower starting doses are recommended in elderly patients due to the potential for decreased hepatic and renal function.

Contraindications (CI):

1. Hypersensitivity: Contraindicated in patients with a known allergy or hypersensitivity to zolmitriptan or any of its components.
2. Cardiovascular Disease: Contraindicated in patients with a history of coronary artery disease, stroke, or peripheral vascular disease, due to the risk of vasoconstriction and cardiovascular events.
3. Uncontrolled Hypertension: Contraindicated in patients with severe or uncontrolled hypertension.
4. Use with MAO Inhibitors: Do not use with monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping MAOIs.
5. Severe Liver or Renal Impairment: Contraindicated in patients with severe liver or renal impairment.

Pharmacist Related Data

Chemical Formula:

• C16H21N3O2 (Zolmitriptan)

Half-life:

• Zolmitriptan has a half-life of approximately 3 hours.
• Its active metabolite, N-desmethylzolmitriptan, has a half-life of 10 hours.

Metabolism:

• Zolmitriptan is extensively metabolized in the liver primarily by CYP1A2 enzymes into active and inactive metabolites.
• Its major active metabolite, N-desmethylzolmitriptan, also exhibits serotonin 5-HT1B/1D receptor agonist properties, although it is less potent than the parent compound.
• Excreted primarily in urine (around 60% of the dose) and in feces.

Drug Interactions:

1. With Food:
   • The absorption of Zolmitriptan is not significantly affected by food. However, it is recommended to take the medication as soon as a migraine starts for the best results.
2. With Medications:
   • Serotonergic Drugs (e.g., SSRIs, SNRIs): When combined with other serotonergic drugs, there is an increased risk of serotonin syndrome, a rare but serious condition.
   • Monoamine Oxidase Inhibitors (MAOIs): Concomitant use with MAOIs (e.g., phenelzine) may increase the levels of zolmitriptan, leading to an increased risk of serotonin syndrome or hypertension.
   • Other Triptans: Do not combine with other triptans (e.g., sumatriptan, rizatriptan) due to the risk of serotonin syndrome and enhanced vasoconstriction effects.
   • Ergotamine Derivatives: Co-administration of zolmitriptan with ergotamine derivatives (e.g., dihydroergotamine) is contraindicated because of the increased risk of vasoconstriction and vascular complications.
3. With Alcohol:
   • Alcohol does not significantly affect the pharmacokinetics of zolmitriptan, but the sedative effects of alcohol may enhance the drowsiness and dizziness caused by zolmitriptan.
4. Lithium: Zolmitriptan may increase the plasma concentration of lithium, and co-administration should be carefully monitored.

Pharmacodynamics:

• Zolmitriptan is a selective serotonin (5-HT1) receptor agonist, which works by binding to the 5-HT1B and 5-HT1D receptors in the brain. These receptors are involved in the pathophysiology of migraines, specifically in vasoconstriction and inhibition of neurogenic inflammation.

1. Vasoconstriction: Zolmitriptan causes vasoconstriction of dilated cerebral blood vessels, which are thought to contribute to the pain and other symptoms of migraines.
2. Inhibition of neurogenic inflammation: It reduces the release of pro-inflammatory neuropeptides such as CGRP (calcitonin gene-related peptide) from the trigeminal nerve, alleviating the inflammation and pain associated with migraines.
3. Pain relief: Zolmitriptan blocks the pain transmission from the trigeminal nerve to the brain, thus helping to relieve the migraine pain.

Pharmacokinetics:

1. Absorption:
   • Zolmitriptan is well absorbed after oral administration. Its bioavailability is about 40-50% due to first-pass metabolism in the liver.
   • Peak plasma concentrations are reached in about 1-2 hours after ingestion.
2. Distribution:
   • Zolmitriptan is highly protein-bound (approximately 70% to plasma proteins).
   • It is widely distributed throughout the body, with a low volume of distribution of about 16.7 L.
3. Metabolism:
   • Zolmitriptan is metabolized in the liver by CYP1A2 enzymes to its active metabolite, N-desmethylzolmitriptan, which also has similar serotonin agonist activity but is less potent than the parent compound.
4. Excretion:
   • Zolmitriptan and its metabolites are primarily excreted in urine (approximately 60% of the dose) and the remainder in feces.
   • About 30% of the drug is excreted unchanged in the urine, while the rest is excreted as metabolites.