Almotriptan

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Drug Info:

Almotriptan

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Brand names: Axert®

Chemical formula:



Almotriptan Malate Oral tablet

What is this medicine?

ALMOTRIPTAN (al moh TRIP tan) is used to treat migraines with or without aura. An aura is a strange feeling or visual disturbance that warns you of an attack. It is not used to prevent migraines.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•bowel disease or colitis
•diabetes
•family history of heart disease
•fast or irregular heart beat
•heart or blood vessel disease, angina (chest pain), or previous heart attack
•high blood pressure
•high cholesterol
•history of stroke, transient ischemic attacks (TIAs or mini-strokes), or intracranial bleeding
•kidney or liver disease
•overweight
•poor circulation
•postmenopausal or surgical removal of uterus and ovaries
•Raynaud's disease
•seizure disorder
•an unusual or allergic reaction to almotriptan, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. This medicine is taken at the first symptoms of a migraine. It is not for everyday use. If your migraine headache returns after one dose, you can take another dose as directed. You must leave at least 2 hours between doses, and do not take more than 25 mg total in any 24 hour period. If there is no improvement at all after the first dose, do not take a second dose without talking to your doctor or health care professional. Do not take your medicine more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose or an appointment for a dose, take it as soon as possible or reschedule your appointment as soon as possible. If a dose is missed, administer the dose as soon as possible then skip the following day. Do not give on two consecutive days. Return to the regular schedule the following week.

What may interact with this medicine?

Do not take this medicine with any of the following medicines:
•amphetamine or cocaine
•dihydroergotamine, ergotamine, ergoloid mesylates, methysergide, or ergot-type medication - do not take within 24 hours of taking almotriptan
•feverfew
•MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate - do not take almotriptan within 2 weeks of stopping MAOI therapy
•other migraine medicines like eletriptan, naratriptan, rizatriptan, zolmitriptan - do not take within 24 hours of taking almotriptan
•tryptophan

This medicine may also interact with the following medications:
•erythromycin
•lithium
•medicines for fungal infections like ketoconazole and itraconazole
•medicines for mental depression, anxiety or mood problems
•medicines for weight loss such as dexfenfluramine, dextroamphetamine, fenfluramine, or sibutramine
•ritonavir
•St. John's wort

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Only take this medicine for a migraine headache. Take it if you get warning symptoms or at the start of a migraine attack. It is not for regular use to prevent migraine attacks.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. To reduce dizzy or fainting spells, do not sit or stand up quickly, especially if you are an older patient. Alcohol can increase drowsiness, dizziness and flushing. Avoid alcoholic drinks.

Smoking cigarettes may increase the risk of heart-related side effects from using this medicine.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•changes in vision
•chest or throat pain, tightness
•fast, slow, or irregular heart beat
•high or low blood pressure
•pain, tingling, numbness in the hands or feet
•seizures
•severe stomach pain and cramping, bloody diarrhea

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•drowsiness
•feeling warm, flushing, or redness of the face
•muscle pain or cramps
•nausea, vomiting, diarrhea or stomach upset
•weak or tired

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.


A 5-HT1 agonist used for the treatment of headache in acute migraine attacks. It is available as tablets on prescription only.

Side effects:
include dizziness, somnolence, nausea, vomiting, fatigue, headache, palpitations, sensations of tingling, and throat tightness.

Precautions:
people with severely impaired liver function should not take this medicine, and those with severely impaired kidney function should take no more than one tablet in a 24-hour period. Almotriptan should not be taken by people with a history or symptoms of coronary artery disease, hypertension, previous stroke, or peripheral artery disease.

Interactions with other drugs:

Antimigraine drugs: ergotamine and methysergide should not be taken with almotriptan because of a risk of spasm of the blood vessels.

Proprietary preparation:
Almogran.

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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 cat. C (US)
Legal status Prescription only
Routes Oral
Pharmacokinetic data
Bioavailability 70%
Protein binding 35%
Metabolism Hepatic
Half-life 3–4 hours
Identifiers
CAS number 154323-57-6 N
ATC code N02CC05
PubChem CID 123606
DrugBank DB00918
ChemSpider 110198 YesY
UNII 1O4XL5SN61 YesY
KEGG D02824 YesY
ChEBI CHEBI:520985 YesY
ChEMBL CHEMBL1505 YesY
Chemical data
Formula C17H25N3O2S 
Mol. mass 335.465 g/mol
SMILES eMolecules & PubChem
 N (what is this?)  (verify)

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… ) + also 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.

Contents

Indications

Almotriptan is prescribed to treat the acute headache phase of migraine attacks with or without aura.
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 is a selective and potent serotonin 5-HT1B/1D agonist. Almotriptan binds to specific serotonin receptors on meningeal arteries inhibiting the release of vasoactive peptides and causing constriction of the arteries. It has a limited effect on arteries supplying blood to the brain, and little effect on cardiac and pulmonary vessels.

Pharmacokinetics

Almotriptan has no clinically relevant pharmacokinetic drug interactions and is metabolized through different pathways, requiring no dosage adjustment in patients with non-severe renal or hepatic impairment. There are also no clinically relevant differences between men and women or between the young and the elderly.

Efficacy

The efficacy of almotriptan in the acute treatment of migraine attacks was established in clinical trials involving more than 3000 patients who were administered 12.5 mg and it was found to have a fast onset of action and high efficacy to reach pain free status (see references). Almotriptan relieves nausea, vomiting, photophobia (light hypersensitivity) and phonophobia (sound hypersensitivity) associated with migraine attacks pain. In the recent Act When Mild study, it was proven that taking almotriptan at the first sign of a migraine attack, while pain is still mild, provides optimal outcomes to ensure patients’ suffering is minimised. (see references)

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

• 1. 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

• 2. 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)

• 3. 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)

• 4. Triptans and CNS side effects: pharmacokinetic and metabolic mechanisms. DW Dodick et al. Cephalalgia. 2004 Jun;24(6):417-24

• 5. Triptans and chest symptoms: the role of pulmonary vasoconstriction. DW Dodick (Cephalalgia, 2004,24, 298–304)

• 6. Almotriptan improves response rates when treatment is within 1 hour of migraine onset. AJ Dowson et al., (Headache 2004; 44: 318-322)

• 7. 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)

• 8. 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)

• 9. Tolerability and efficacy of almotriptan in the long-term treatment of migraine, J. Pascual et al. (Eur Neurol 2001;45:206-213)

• 10. 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

• 11. 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.

• 12. Early intervention with almotriptan: results of the AEGIS trial (AXERT Early Migraine Intervention Study). Mathew et al., Headache. 2007 Feb;47(2):189-98

• 13. 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

• 14. 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

• 15. 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

• 16. 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

• 17. 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

• 18. 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

• 19. 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

• 20. 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

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