Pharmacokinetics and interactions of headache medications, part II: prophylactic treatments.

Article Details

Citation

Sternieri E, Coccia CP, Pinetti D, Guerzoni S, Ferrari A

Pharmacokinetics and interactions of headache medications, part II: prophylactic treatments.

Expert Opin Drug Metab Toxicol. 2006 Dec;2(6):981-1007. doi: 10.1517/17425255.2.6.981 .

PubMed ID
17125412 [ View in PubMed
]
Abstract

The present part II review highlights pharmacokinetic drug-drug interactions (excluding those of minor severity) of medications used in prophylactic treatment of the main primary headaches (migraine, tension-type and cluster headache). The principles of pharmacokinetics and metabolism, and the interactions of medications for acute treatment are examined in part I. The overall goal of this series of two reviews is to increase the awareness of physicians, primary care providers and specialists regarding pharmacokinetic drug-drug interactions (DDIs) of headache medications. The aim of prophylactic treatment is to reduce the frequency of headache attacks using beta-blockers, calcium-channel blockers, antidepressants, antiepileptics, lithium, serotonin antagonists, corticosteroids and muscle relaxants, which must be taken daily for long periods. During treatment the patient often continues to take symptomatic drugs for the attack, and may need other medications for associated or new-onset illnesses. DDIs can, therefore, occur. As a whole, DDIs of clinical relevance concerning prophylactic drugs are a limited number. Their effects can be prevented by starting the treatment with low dosages, which should be gradually increased depending on response and side effects, while frequently monitoring the patient and plasma levels of other possible coadministered drugs with a narrow therapeutic range. Most headache medications are substrates of CYP2D6 (e.g., beta-blockers, antidepressants) or CYP3A4 (e.g., calcium-channel blockers, selective serotonin re-uptake inhibitors, corticosteroids). The inducers and, especially, the inhibitors of these isoenzymes should be carefully coadministered.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
AcebutololCytochrome P450 2D6ProteinHumans
Unknown
Substrate
Inhibitor
Details
AnisodamineCytochrome P450 2D6ProteinHumans
No
Substrate
Details
ArotinololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
AtenololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BefunololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BevantololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BopindololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BucindololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
BupranololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
CeliprololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
CloranololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
EpanololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
EsatenololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
EsmololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
IndenololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
LandiololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
LevobetaxololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
LevobunololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
MepindololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
MetipranololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
OxprenololCytochrome P450 2D6ProteinHumans
Unknown
Substrate
Inhibitor
Details
PenbutololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
PractololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
SotalolCytochrome P450 2D6ProteinHumans
No
Substrate
Details
TalinololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
TertatololCytochrome P450 2D6ProteinHumans
No
Substrate
Details
Drug Reactions
Reaction
Details