title: Pharmacokinetics and interactions of headache medications, part I: introduction, pharmacokinetics, metabolism and acute treatments.
abstract: Recent progress in the treatment of primary headaches has made available specific, effective and safe medications for these disorders, which are widely spread among the general population. One of the negative consequences of this undoubtedly positive progress is the risk of drug-drug interactions. This review is the first in a two-part series on pharmacokinetic drug-drug interactions of headache medications. Part I addresses acute treatments. Part II focuses on prophylactic treatments. The overall aim of this series is to increase the awareness of physicians, either primary care providers or specialists, regarding this topic. Pharmacokinetic drug-drug interactions of major severity involving acute medications are a minority among those reported in literature. The main drug combinations to avoid are: i) NSAIDs plus drugs with a narrow therapeutic range (i.e., digoxin, methotrexate, etc.); ii) sumatriptan, rizatriptan or zolmitriptan plus monoamine oxidase inhibitors; iii) substrates and inhibitors of CYP2D6 (i.e., chlorpromazine, metoclopramide, etc.) and -3A4 (i.e., ergot derivatives, eletriptan, etc.), as well as other substrates or inhibitors of the same CYP isoenzymes. The risk of having clinically significant pharmacokinetic drug-drug interactions seems to be limited in patients with low frequency headaches, but could be higher in chronic headache sufferers with medication overuse.
authors.affiliation: University of Modena and Reggio Emilia, Division of Toxicology and Clinical Pharmacology, Headache Centre, University Centre for Adaptive Disorders and Headache, Section Modena II, Largo del Pozzo 71, Modena, Italy.
authors.forename: Emilio
authors.initials: E
authors.lastname: Sternieri
authors.forename: Ciro Pio Rosario
authors.initials: CP
authors.lastname: Coccia
authors.forename: Diego
authors.initials: D
authors.lastname: Pinetti
authors.forename: Anna
authors.initials: A
authors.lastname: Ferrari
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000627:therapeutic use; D004347:Drug Interactions; D020773:Headache Disorders / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D008996:Monoamine Oxidase Inhibitors / Q000009:adverse effects / Q000627:therapeutic use; D010599:Pharmacokinetics; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000378:metabolism / Q000493:pharmacokinetics*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D008996:Monoamine Oxidase Inhibitors; D017366:Serotonin Receptor Agonists