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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/04/01 20:06:59」(JST)

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Almotriptan (trade names Axert (US, Canada), Almogran (Belgium, Denmark, Finland, France, Germany, Italy, Ireland Portugal, Spain, the United Kingdom, the Netherlands, Sweden, Switzerland, South Korea… ), Almotrex (Italy) and Amignul (Spain)) is a triptan drug discovered and developed by Almirall for the treatment of heavy migraine headache. It is available in 12.5 mg in most countries and also 6.25 mg in US and Canada.

Indications

Almotriptan is prescribed to treat the acute headache phase of migraine attacks with or without aura.^[1]
Almotriptan is the only oral triptan approved in the USA for the treatment of migraine in adolescent from 12 to 17 years of age.

Mechanism of action

Almotriptan has a high and specific affinity for serotonin 5-HT_1B/1D receptors. Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels. Even though it affects cranial blood vessels a single dose of almotriptan (12.5 mg) has no clinically significant effect on blood pressure or heart rate in both young and elderly healthy volunteers. However larger doses seem to slightly increase blood pressure but not beyond clinical relevance.^[2]

Pharmacokinetics

Almotriptan has a linear pharmacokinetic up to 200 mg dose. Its half life is 3 hours and nearly 70% bioavailability.
C_max is observed 1.5–4 hours after oral administration and approximately 50% of the drug is excreted unchanged in the urine. Metabolism is mediated through MAO-A and CYP3A4 and CYP2D6 oxidation. Almotriptan clearance is moderately reduced in the elderly but does not require dose adjustment. Sex does not alter the pharmacokinetics of the drug. However, patients with moderate-to-severe renal dysfunction should limit their total daily dose to 12.5 mg. ^[3]

Drug interactions

As mentioned previously almotriptan is metabolized mainly by MAO-A and to lesser extent by CYP3A4 and CYP2D6. Studies of drugs used as preventive against migraine (propranolol and verapamil), anti-depressants (moclobemide and fluoxetine) yielded results that showed significant altering of the pharmacokinetics of almotriptan though they were deemed not clinically relevant.^[2]

Efficacy

The efficacy and tolerability of almotriptan has been studied in numerous randomised, control-led trials totaling more than 4800 adults with either moderate or severe attacks of migraine. Its efficacy is significantly more effective than placebo and alleviates nausea, photophobia and phonophobia linked to migraine attacks. Compared to other triptan drug, 12.5 mg of almotriptan has similar efficacy as 50 mg of sumatriptan and fewer adverse effects.^[2]

Contraindications

(see SmPC) Hypersensitivity to the active substance or to any of the excipients.
As with other 5-HT1B/1D receptor agonists, almotriptan should not be used in patients with a history, symptoms or signs of ischaemic heart disease (myocardial infarction, angina pectoris, documented silent ischaemia, Prinzmetal’s angina) or severe hypertension and uncontrolled mild or moderate hypertension.
Patients with a previous cerebrovascular accident (CVA) or transient ischaemic attack (TIA). Peripheral vascular disease.
Concomitant administration with ergotamine, ergotamine derivatives (including methysergide) and other 5-HT1B/1D agonists is contraindicated.
Patients with severe hepatic impairment.

Side effects

(see SmPC) Almotriptan has proved to have an adverse effects profile similar to placebo when used following the Summary of Product Characteristics instructions (see references).

"For rare adverse events, please refer to the manufacturer´s webpage"

References

Early vs. non-early intervention in acute migraine-'Act when Mild (AwM)'. A double-blind, placebo-controlled trial of almotriptan. Goadsby PJ et al., Cephalalgia. 2008 Apr;28(4):383-91
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials. MD Ferrari et al., (Cephalalgia 2002; 22:633-658)
Almotriptan is effective and well tolerated in migraine patients who respond poorly to oral sumatriptan: A double-blind, randomized trial, Diener HC (Headache. 2005 Jul-Aug;45(7):874-82)
Triptans and CNS side effects: pharmacokinetic and metabolic mechanisms. DW Dodick et al. Cephalalgia. 2004 Jun;24(6):417-24
Triptans and chest symptoms: the role of pulmonary vasoconstriction. DW Dodick (Cephalalgia, 2004,24, 298–304)
Almotriptan improves response rates when treatment is within 1 hour of migraine onset. AJ Dowson et al., (Headache 2004; 44: 318-322)
A long-term open-label study of oral almotriptan 12.5 mg for the treatment of acute migraine. NT. Mathew; for the Oral Almotriptan Study Group (Headache. 2002;42:32-40)
Almotriptan is an effective and well-tolerated treatment for migraine pain: results of a randomized, double-blind, placebo-controlled clinical trial. AJ Dowson et al. (Cephalalgia 2002; 22, 453-461)
Tolerability and efficacy of almotriptan in the long-term treatment of migraine, J. Pascual et al. (Eur Neurol 2001;45:206-213)
Consistent efficacy and tolerability of almotriptan in the acute treatment of multiple migraine attacks: results of a large, randomized, double-blind, placebo-controlled study. J. Pascual et al. Cephalalgia. 2000;20:588-596
Almotriptan in the treatment of migraine attacks in clinical practice: results of the TEA 2000 observational study, Pascual J et al., Neurologia. 2003 Jan-Feb;18(1):7-17.
Early intervention with almotriptan: results of the AEGIS trial (AXERT Early Migraine Intervention Study). Mathew et al., Headache. 2007 Feb;47(2):189-98
Evaluation of efficacy, tolerability, and treatment satisfaction with almotriptan in 3 consecutive migraine attacks. The migraine—satisfaction with treatment: reality with Almogran study. Massiouu H et al., Eur Neurol. 2006;55(4):198-203
Triptans in the treatment of migraine: drug selection by means of the SOJA method Expert Opin Pharmacother. Janknegt J,2007 Oct;8 Suppl 1:S15-30
Patient preference in migraine therapy. A randomized, open-label, crossover clinical trial of acute treatment of migraine with oral almotriptan and rizatriptan Díez FI et al., J Neurol. 2007 Feb;254(2):242-9
Use of the sustained pain-free plus no adverse events endpoint in clinical trials of triptans in acute migraine. Dodick DW et al. CNS Drugs. 2007;21(1):73-82
A pharmacoeconomic evaluation of oral triptans in the treatment of migraine in Italy. Gori S. et al. Minerva Med. 2006 Dec;97(6):467-77
Management costs of chest and CNS-related adverse events associated with the treatment of acute migraine attacks with oral triptans. Slof J et al., Neurologia. 2005 Jul-Aug;20(6):290-8
Efficacy, speed of action and tolerability of almotriptan in the acute treatment of migraine: pooled individual patient data from four randomized, double-blind, placebo-controlled clinical trials. Dahlöf CG et al. Cephalalgia 2006;26:400–408
Characteristics of migraine attacks and responses to almotriptan treatment: a comparison of menstrually related and nonmenstrually related migraines. Diamond ML et al., Headache 2008;48:248–258

External links

R&D page by Almirall Prodesfarma
Axert Official homepage by Ortho-McNeil
Axert prescribing information

References

^ "Almotriptan Facts and Comparisons". Drugs.com. Retrieved 7 October 2012.
^ ^a ^b ^c Keam, SJ; Goa, KL; Figgitt, DP (2002). "Almotriptan: a review of its use in migraine.". Drugs 62 (2): 387–414. doi:10.2165/00003495-200262020-00010. PMID 11817980.
^ McEnroe, JD; Fleishaker, JC (2005). "Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine.". Clinical pharmacokinetics 44 (3): 237–46. doi:10.2165/00003088-200544030-00002. PMID 15762767. |access-date= requires |url= (help)

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 成人における片頭痛の急性期治療 acute treatment of migraine in adults
2. 性行為に伴う一次性頭痛 primary headache associated with sexual activity
3. 小児における片頭痛の急性期治療 acute treatment of migraine in children
4. 患者情報：成人における片頭痛（詳細） migraine headaches in adults beyond the basics
5. 患者情報：成人における頭痛の治療（詳細） headache treatment in adults beyond the basics

English Journal

Comparative efficacy of triptans for the abortive treatment of migraine: A multiple treatment comparison meta-analysis.

Thorlund K, Mills EJ, Wu P, Ramos E, Chatterjee A, Druyts E, Goadsby PJ.Author information Department of Clinical Epidemiology & Biostatistics, McMaster University, Canada.AbstractBACKGROUND: Migraine is the most common neurological condition in developed countries. The abortive treatment of migraine attacks is important both for quality of life and costs associated with illness. Triptans, serotonin 5-HT1B/1D receptor agonists, effectively relieve the pain, disability, and associated symptoms of migraine while improving health-related quality of life. Although a number of direct head-to-head triptan comparisons have been made, data for all possible permutations are not available, and unlikely to ever be so, although in clinical practice such information would be useful.
Cephalalgia : an international journal of headache.Cephalalgia.2013 Dec 19. [Epub ahead of print]
BACKGROUND: Migraine is the most common neurological condition in developed countries. The abortive treatment of migraine attacks is important both for quality of life and costs associated with illness. Triptans, serotonin 5-HT1B/1D receptor agonists, effectively relieve the pain, disability, and as
PMID 24108308

Canadian Headache Society Guideline: acute drug therapy for migraine headache.

Worthington I, Pringsheim T, Gawel MJ, Gladstone J, Cooper P, Dilli E, Aube M, Leroux E, Becker WJ; Canadian Headache Society Acute Migraine Treatment Guideline Development Group.Collaborators (24)Pringsheim T, Davenport WJ, Mackie G, Christie SN, Gawel M, Aube M, Becker WJ, Dilli E, Cooper P, Giammarco R, Purdy RA, Robinson G, Gladstone J, Leroux E, Amoozegar F, Spacey S, Saly V, Shapero G, Magnoux E, Worthington I, O'Callaghan I, South V, Cote J, Montgomery L.
The Canadian journal of neurological sciences. Le journal canadien des sciences neurologiques.Can J Neurol Sci.2013 Sep;40(5 Suppl 3):S1-S80.
OBJECTIVES: The primary objective of this guideline is to assist the practitioner in choosing an appropriate acute medication for an individual with migraine, based on current evidence in the medical literature and expert consensus. It is focused on patients with episodic migraine ( headache on ≤
PMID 23968886

Comparative cost-effectiveness analysis of oral triptan therapy for migraine in four European countries.

Hens M, Villaverde-Hueso A, Alonso V, Abaitua I, Posada de la Paz M.Author information Rare Diseases Research Institute, Instituto de Salud Carlos III, Monforte de Lemos 5 (Pabellon 11), 28029, Madrid, Spain.AbstractAIM: To assess the differences in the cost-effectiveness of oral triptan therapy for migraines among European countries.
The European journal of health economics : HEPAC : health economics in prevention and care.Eur J Health Econ.2013 Jul 10. [Epub ahead of print]
AIM: To assess the differences in the cost-effectiveness of oral triptan therapy for migraines among European countries.METHODS: A cost-effectiveness analysis of triptan therapy for migraine was conducted from a health-care payer perspective in four European countries (France, Italy, Spain and the U
PMID 23839914

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リンク元	「アルモトリプタン」「リンゴ酸アルモトリプタン」
関連記事	「almotriptan」

「アルモトリプタン」

Almotriptan
Systematic (IUPAC) name
	N,N-dimethyl-2- [5-(pyrrolidin-1-ylsulfonylmethyl)- 1H-indol-3-yl]-ethanamine
Clinical data
Trade names	Axert
AHFS/Drugs.com	monograph
MedlinePlus	a603028
Pregnancy; category	US: C (Risk not ruled out); ;
Routes of; administration	Oral
Legal status
Legal status	UK: POM (Prescription only); Prescription only;
Pharmacokinetic data
Bioavailability	70%
Protein binding	35%
Metabolism	Hepatic
Biological half-life	3–4 hours
Identifiers
CAS Number	154323-57-6
ATC code	N02CC05 (WHO)
PubChem	CID 123606
IUPHAR/BPS	7110
DrugBank	DB00918
ChemSpider	110198
UNII	1O4XL5SN61
KEGG	D02824
ChEBI	CHEBI:520985
ChEMBL	CHEMBL1505
Chemical data
Formula	C17H25N3O2S
Molar mass	335.465 g/mol
	SMILES O=S(=O)(N1CCCC1)Cc3cc2c(cnc2cc3)CCN(C)C ;
	InChI InChI=1S/C17H25N3O2S/c1-19(2)10-7-15-12-18-17-6-5-14(11-16(15)17)13-23(21,22)20-8-3-4-9-20/h5-6,11-12,18H,3-4,7-10,13H2,1-2H3 ; Key:WKEMJKQOLOHJLZ-UHFFFAOYSA-N ;
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