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Initial human experience with MK-462 (rizatriptan): a novel 5-HT1D agonist
D G Sciberras1, W J Polvino, B J Gertz
1Merck Research Laboratories, Rahway, New Jersey, USA.
British Journal of Clinical Pharmacology
|January 1, 1997
Summary
MK-462, a novel 5-HT1D agonist, demonstrated rapid oral absorption and similar pharmacodynamic effects to sumatriptan. Further research is recommended for MK-462 in acute migraine treatment.
Area of Science:
- Pharmacology
- Clinical Pharmacology
- Neuroscience
Background:
- Migraine treatment often involves serotonin receptor agonists.
- Sumatriptan is a widely used oral medication for acute migraine attacks.
- Understanding the pharmacokinetic and pharmacodynamic profiles of novel drug candidates is crucial.
Purpose of the Study:
- To compare the pharmacokinetics and pharmacodynamics of oral MK-462 with oral sumatriptan.
- To evaluate the safety and tolerability of MK-462 in healthy male volunteers.
Main Methods:
- A randomized, double-blind, placebo-controlled, rising single-dose study design.
- Sixteen healthy male volunteers were enrolled in two panels of eight subjects.
- MK-462 and sumatriptan were administered orally, with placebo controls at each dose level.
Main Results:
- MK-462 exhibited significantly faster absorption (median tmax 1.3 h) compared to sumatriptan (median tmax 2.5 h).
- Both drugs caused similar, mild elevations in blood pressure without affecting heart rate.
- Mild increases in serum growth hormone were observed with both agents; drowsiness was the most common side effect of MK-462.
Conclusions:
- Oral MK-462 is rapidly absorbed and possesses a pharmacokinetic profile that warrants further investigation.
- MK-462 demonstrates comparable pharmacodynamic effects to sumatriptan.
- The novel 5-HT1D agonist MK-462 shows potential for the treatment of acute migraine.