Almotriptan

Article Author:
Gursharan Sidhu
Article Editor:
Priti Patel
Updated:
4/12/2020 11:11:38 PM
For CME on this topic:
Almotriptan CME
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Almotriptan

Indications

Almotriptan is the first FDA-approved drug used to treat migraine headaches in adults with or without an aura.[1] The drug is also useful in adolescents with a history of a migraine that, when left untreated, lasts 4 hours or longer. Certain triptan medications such as almotriptan and rizatriptan have also shown to be effective and safe for the management of acute migraines and other benign headaches in the pediatric population (less than 18 years of age).[2] 

Almotriptan has approval for use as monotherapy and in conjunction with migraine-abortive medications such as non-steroidal anti-inflammatory drugs (e.g., aceclofenac).[3] It is usually taken by mouth as a tablet.[4] Almotriptan is a white, coated circular tablet, and requires a prescription from a registered physician in the United States.[5] 

In pregnant women with migraines or headaches, triptan use is less frequent; where drugs like metoclopramide, and acetaminophen are more common choices for migraines due to their effectiveness and safety.[6] Triptans have also found to be quite effective in treating menstrual migraines in premenopausal women. Various studies have shown that among the triptans, rizatriptan has proven to be the most beneficial in treating acute menstrual migraines in females.[7] A randomized, placebo-controlled study showed that rizatriptan provided pain relief between 2 to 24 hours with an efficacy of 63 percent when compared to other classes of triptans.[7] 

Mechanism of Action

Almotriptan is a selective serotonin agonist on the 5-HT1B and 5-HT1D receptors in the cranial arteries. Activation of the 5HT receptors is associated with a reduction in neurogenic inflammation, which researchers hypothesize to be involved in the migraine relief process.

Almotriptan works by narrowing the blood vessels in the brain, thereby reducing the cerebral blood flow, stopping the transmission of pain signals to the brain center.[8] The drug has a relatively short half-life of 3 hours, and research the oral bioavailability was found to be 69.1%.[9] Almotriptan is excreted in the urine and metabolized predominantly by the cytochrome CYP450 system.[9] When compared with earlier generation triptans such as sumatriptan, almotriptan has a higher oral bioavailability and a shorter plasma half-life.[8]

Administration

The recommended oral dose of almotriptan is 12.5 mg for the effective treatment of acute migraine attacks in adults and adolescents.[9] The dose may be repeated after two hours if a headache returns. It is recommended not to administer more than two doses or more than 25 mg/day. Studies have also shown that almotriptan has a synergistic effect when combined with aceclofenac 100 mg in the treatment of an acute migraine attack.[3] 

Food intake has not demonstrated any effect on the absorption of almotriptan; therefore, its dosing can be without regard to food intake.[9] Dosing adjustment recommended in patients with renal insufficiency. Dosing adjustment is necessary when the drug used with cytochrome P450 inducers (e.g., phenytoin, phenobarbital) and with cytochrome P450 inhibitors (e.g., antibiotics, grapefruit juice, ketoconazole, protease inhibitors). 

Adverse Effects

The common adverse effects of almotriptan are drowsiness, dizziness, headache, nausea, vomiting, chest pain, and fatigue.[10] The drug is associated with a similar incidence of nausea/vomiting as compared to other classes of triptans (e.g., sumatriptan). However, it shows a decreased incidence of the other common adverse effects listed above, especially when compared to first-generation triptans.[8][10] 

Almotriptan works on the 5HT1B receptors which are present in the coronary arteries; thus, the administration may result in coronary artery narrowing or spasms, leading to potential coronary artery vasospasm or myocardial infarction.[11] Some rare side effects of almotriptan include pulmonary vasoconstriction, serotonin syndrome, inhibition of trigeminal nerves.[12][13]

Contraindications

Almotriptan is contraindicated in patients with renal dysfunction or insufficiency, as well as in the elderly due to a physiological decrease in renal function and renal clearance with advanced age.[9] 

Minor clearance of almotriptan occurs through the CYPP450 system (specifically, CYP3A4); therefore, the clinician should avoid other drugs metabolized through this pathway because they may decrease almotriptan clearance. These drugs include but are not limited to verapamil, nifedipine, losartan, cyclosporine, and moclobemide.[9] It is then reasonable to assume that patients with a mutation in this specific enzyme should be cautious in dosing the drug.

Contraindications to almotriptan also include patients with underlying cardiovascular disease due to the presence of 5HT1B receptors on the coronary arteries. Almotriptan can potentially attach to such receptors resulting in further narrowing or spasm of the arteries.[11] Patients with hypersensitivity to almotriptan should not use the drug, nor should patients that may have a history of a hemiplegic or basilar migraine or a heart condition. Moreover, this medication is not for use in patients that have cerebrovascular syndromes, peripheral vascular disease, or high blood pressure. Caution is necessary if dosing almotriptan within 24 hours of use of a serotonin agonist or an ergotamine-classified medication due to the vasoconstrictive effects of both drugs.[13] 

Monitoring

Patients taking almotriptan should require monitoring for the presence of side effects and response to therapy. Kidney function should be monitor when taking the drug as renal clearance may affect the drug clearance from the body, causing toxicity. Regular monitoring of the blood pressure should take place at each clinical visit due to the narrowing effect of the 5-HT1B receptors on the blood vessels, and assess the effectiveness of the drug.[13] 

Toxicity

There are no associated toxicities with almotriptan due to the limited data, although studies demonstrate increased preterm birth rates in pregnant women that received triptans for migraine relief.[14]

An analysis of several case reports of patients undergoing dual triptan-SSRI/SNRI therapy or triptan monotherapy suggested that the addition of triptans to SSRI/SNRI therapy does not necessarily increase the risk of patients developing serotonin syndrome. However, providers should remain cautious and vigilant of the symptoms.[15]

Enhancing Healthcare Team Outcomes

Managing the administration of almotriptan in patients with acute migraines requires an interprofessional team of healthcare professionals that include a neurologist, primary care physician, nephrologist in the case of a compromised renal function, psychiatrist, specialty-trained nursing staff, and pharmacist for appropriate dosing and safety precautions, all working collaboratively to ensure optimal patient outcomes. The nursing staff must be ready to inform the prescriber regarding any potential adverse events form the medication, and can also monitor whether almotriptan is providing adequate migraine pain relief. The pharmacist must look into possible drug-drug interactions, and can counsel the patient on proper administration. A robust support system consisting of the patients' family and friends may also be beneficial in successful treatment.

Consistent patient follow-up and adherence to appointment times are essential for proper monitoring of vital signs and management of any adverse effects. Moreover, it is also necessary for assessing drug effectiveness. This type of interprofessional team effort is essential to optimize therapy with almotriptan so the patient can achieve the best outcomes. [Level V]


References

[1] Eiland LS,Hunt MO, The use of triptans for pediatric migraines. Paediatric drugs. 2010 Dec 1;     [PubMed PMID: 21028917]
[2] Acute Treatment Therapies for Pediatric Migraine: A Qualitative Systematic Review., Patniyot IR,Gelfand AA,, Headache, 2016 Jan     [PubMed PMID: 26790849]
[3] Schoenen J,De Klippel N,Giurgea S,Herroelen L,Jacquy J,Louis P,Monseu G,Vandenheede M, Almotriptan and its combination with aceclofenac for migraine attacks: a study of efficacy and the influence of auto-evaluated brush allodynia. Cephalalgia : an international journal of headache. 2008 Oct;     [PubMed PMID: 18644036]
[4] Dowson AJ, Oral almotriptan: practical uses in the acute treatment of migraine. Expert review of neurotherapeutics. 2004 May;     [PubMed PMID: 15853532]
[5] Sharma M,Vadhariya A,Johnson ML,Marcum ZA,Holmes HM, Association between industry payments and prescribing costly medications: an observational study using open payments and medicare part D data. BMC health services research. 2018 Apr 2;     [PubMed PMID: 29609611]
[6] Hamilton KT,Robbins MS, Migraine Treatment in Pregnant Women Presenting to Acute Care: A Retrospective Observational Study. Headache. 2019 Feb;     [PubMed PMID: 30403400]
[7] Maasumi K,Tepper SJ,Kriegler JS, Menstrual Migraine and Treatment Options: Review. Headache. 2017 Feb;     [PubMed PMID: 27910087]
[8] Formulation Approaches of Triptans for Management of Migraine., Kassem AA,, Current drug delivery, 2016     [PubMed PMID: 27109335]
[9] McEnroe JD,Fleishaker JC, Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. Clinical pharmacokinetics. 2005;     [PubMed PMID: 15762767]
[10] Thorlund K,Toor K,Wu P,Chan K,Druyts E,Ramos E,Bhambri R,Donnet A,Stark R,Goadsby PJ, Comparative tolerability of treatments for acute migraine: A network meta-analysis. Cephalalgia : an international journal of headache. 2017 Sep;     [PubMed PMID: 27521843]
[11] Tepper SJ,Millson D, Safety profile of the triptans. Expert opinion on drug safety. 2003 Mar;     [PubMed PMID: 12904112]
[12] Dodick DW, Triptans and chest symptoms: the role of pulmonary vasoconstriction. Cephalalgia : an international journal of headache. 2004 Apr;     [PubMed PMID: 15030540]
[13] Tepper SJ,Rapoport AM,Sheftell FD, Mechanisms of action of the 5-HT1B/1D receptor agonists. Archives of neurology. 2002 Jul;     [PubMed PMID: 12117355]
[14] Soldin OP,Dahlin J,O'Mara DM, Triptans in pregnancy. Therapeutic drug monitoring. 2008 Feb;     [PubMed PMID: 18223456]
[15] Shader RI,Greenblatt DJ, Is There Always a Right or Wrong?: Comments on the FDA Warnings About Triptans and the Serotonin Syndrome. Journal of clinical psychopharmacology. 2018 Dec;     [PubMed PMID: 30303862]