Lack of Interaction Between Oral Dihydroergotamine and the Novel Antimigraine Compound Zolmitriptan in Healthy Volunteers

Veronese, L.; Gillotin, Catherine; Marion-Gallois, R.; Weatherley, B.C.; Thebault, J. J.; Guillaume, M.; Peck, Richard

doi:10.2165/00044011-199714030-00009

Cited by 8 publications

(4 citation statements)

References 7 publications

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“…Both ergotamine and zolmitriptan administered alone reduced the toe-arm systolic pressure gradients; maximum changes were -23.0 mmHg (95% CI -28.2, ~ 17.7 mmHg) for zolmitriptan and -7.6 mmHg (95% CI -12.9, -2.4 mmHg) for ergotamine, and the effects of the ergotamine/zolmitriptan combination were additive (6). There were no consistent trends for changes in cardiac output.…”

Section: Pi~nunracon!/narnicsmentioning

confidence: 88%

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

Rolan

1997

Cephalalgia

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Seven randomized studies in healthy volunteers have investigated interactions between zolmitriptan (Zomig, formerly 311C90), a 5HT1B/1D agonist for acute migraine therapy, and selected drugs with which there was a possibility of interaction or a likelihood of concurrent use. Co-administration of oral dihydroergotamine, ergotamine, pizotifen, fluoxetine, paracetamol (acetaminophen)/metoclopramide or selegiline had no clinically significant effects on the pharmacokinetics of zolmitriptan or its metabolites, although small changes were observed in some cases. Co-administration of propranolol resulted in a 56% increase in the area under the plasma concentration-time curve (AUC) of zolmitriptan and a 11% decrease in the AUC of the active metabolite 183C91. However, these pharmacokinetic changes are unlikely to be relevant at lower clinical doses. Moclobemide, a monoamine oxidase A (MAO-A) inhibitor, decreased the clearance of zolmitriptan and, in particular, 183C91. This suggests that MAO-A is involved in the metabolism of 183C91 and it may be prudent to limit the daily zolmitriptan dose in migraine patients maintained on a MAO-A inhibitor. The clinically insignificant blood pressure increases produced by zolmitriptan, and the tolerability profile of this agent, were unaffected by any of the concomitant medications. Clinically significant interactions between zolmitriptan and commonly co-prescribed antimigraine therapies are unlikely.

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Section: Pi~nunracon!/narnicsmentioning

confidence: 88%

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

Rolan

1997

Cephalalgia

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“…56 No clinically signifi cant interactions with other commonly prescribed medications in headache management such as metoclopramide, dihydroergotamine, fl uoxetine, and propranolol, or monoamine oxidase-B inhibitors such as selegiline, have been demonstrated. 56,57 However, it is contraindicated to give zolmitriptan to a patient on MAO-A inhibitor or within 24 hours of use of an ergot or another triptan. 59,60 In addition, it has been demonstrated that cimetidine inhibits the metabolism of zolmitriptan and its active metabolite, increasing the mean Cmax by 16 and 50% and the mean AUC by 48 and 105%, respectively.…”

Section: Drug-drug Interactionsmentioning

confidence: 99%

A Review of the Pharmacokinetics, Pharmacodynamics and Efficacy of Zolmitriptan in the Acute Abortive Treatment of Migraine

Kalanuria

Peterlin

2009

Clinical Medicine. Therapeutics

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Migraine is a common and often disabling neurovascular disorder. Changes in the metabolism and the central processing of serotonin, as well as abnormalities in the modulation of the central and peripheral trigeminal nociceptive pathways, have been shown to play signifi cant roles in migraine pathophysiology. Recent evidence suggests that a low serotonin state facilitates activation of the trigeminal nociceptive pathways. In addition, several pharmacological agents that modulate serotonin are used in the treatment of migraine. Specifi cally there are seven FDA approved, 5-hydroxytryptamine (5-HT) 1B/1D receptor agonists, used for the acute abortive therapy of migraine. Zolmitriptan is one such triptan. Zolmitriptan is available as a tablet, orally disintegrating tablet and as a nasal spray. It is rapidly absorbed and detectable within the plasma, within 2 to 5 minutes for the nasal spray and within 15 minutes for the tablet. Zolmitriptan reaches peak plasma levels in 2-4 hours, with good levels maintained for up to 6 hours. Although the metabolism of zolmitriptan is predominantly hepatic, only 25% of zolmitriptan is bound to plasma proteins. Thus it is unlikely for drug interactions involving the displacement of highly protein-bound drugs. Zolmitriptan is very well tolerated with less than half of participants in clinical trials reporting adverse events, most of which were mild and transient. Although rare, serious cardiovascular events have been reported with all triptans. However, when patients are appropriately selected, zolmitriptan is both, a safe and effective acute migraine abortive agent. In this article, we will fi rst briefl y review the biological role of serotonin and the literature linking serotonin to migraine pathophysiology. This will be followed by a comprehensive review of the pharmacodynamics, pharmacokinetics and effi cacy of zolmitriptan. Finally, the clinical application of the use of zolmitriptan in migraine therapy will be discussed.

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“…The pharmacokinetics of zolmitriptan are not significantly altered by coadministered dihydroergotamine, 67 propranolol, 68 pizotifen, 69 fluoxetine, 70 metoclopramide, or acetaminophen (paracetamol 71 ). In addition, the shift in metabolism away from MAO‐A toward the cytochrome P450 system with zolmitriptan permits its use with the MAO‐A inhibitor moclobemide 72 .…”

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confidence: 99%

Zolmitriptan Intranasal: A Review of the Pharmacokinetics and Clinical Efficacy

Goadsby¹,

Yates²

2006

Headache

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Migraine is a common disabling neurological disorder, associated with headache, nausea, and on occasions vomiting. Zolmitriptan is a widely available serotonin 5HT(1B/1D) receptor agonist with a long track record in clinical studies and in the treatment of acute migraine. A nasal formulation has been developed that has clear evidence for local absorption, resulting in plasma drug concentrations within 2 minutes of dosing, central nervous system penetration 3 minutes later, and a significant efficacy benefit versus placebo 10 to 15 minutes after dosing. Intranasal zolmitriptan offers advantages to migraineurs, particularly those seeking a more rapid onset of effect without wishing to self-inject, or those with gastrointestinal upset. The comparison of pharmacokinetic and clinical data available from different formulations of zolmitriptan contributes both to the understanding of its mode of action and the characteristics required of an acute migraine treatment if it is to meet patient needs.

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Lack of Interaction Between Oral Dihydroergotamine and the Novel Antimigraine Compound Zolmitriptan in Healthy Volunteers

Cited by 8 publications

References 7 publications

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

A Review of the Pharmacokinetics, Pharmacodynamics and Efficacy of Zolmitriptan in the Acute Abortive Treatment of Migraine

Zolmitriptan Intranasal: A Review of the Pharmacokinetics and Clinical Efficacy

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