Almotriptan (Axert) - for the acute treatment of migraine

Almotriptan is a selective agonist of serotonin receptors in the brain. It is used in the acute management of migraine with or without aura in adults and adolescents. It should be avoided in patients with ischemic heart disease, uncontrolled hypertension, peripheral arterial disease, and cerebrovascular diseases.

Almotriptan Dose in Adults

Almotriptan dose in adults with migraine:

  • 6.25 to 12.5 mg as a single dose.
  • The dose may be repeated after 2 hours to a maximum of 2 doses per day ( 25 mg per day)
  • Patients receiving potent CYP 3A4 inhibitors may receive a maximum dose of 12.5 mg/day
  • Patients with severe renal and hepatic impairment and in potent CYP 3A4 inhibitors should avoid almotriptan.

Almotriptan Dose in Childrens

Dose in children older than 12 years of age and Adolescents:

  • 6.25 to 12.5 mg as a single dose.
  • The dose may be repeated after 2 hours to a maximum of 2 doses per day ( 25 mg per day)
  • Patients receiving potent CYP 3A4 inhibitors may receive a maximum dose of 12.5 mg/day
  • Patients with severe renal and hepatic impairment and in potent CYP 3A4 inhibitors should avoid almotriptan.

Pregnancy Risk Factor C

  • Although Almotriptan's use during pregnancy is not recommended, there have been animal studies that showed adverse pregnancy outcomes.

Almotriptan use during breastfeeding:

  • It is unknown if almotriptan can be found in breastmilk. It should not be used by nursing women.

Almotriptan Dose in Renal Disease:

Severe renal impairment with a CrCl of 30 mL/minute or less:

  • 6.25 mg in a single dose to a maximum daily dose of 12.5 mg

Almotriptan Dose in Liver Disease:

  • 6.25 mg as a single dose to a maximum of 12.5 mg daily dose. 

Common SIde Effects to almotriptan:

  • Central nervous system:
    • Drowsiness and dizziness
  • Gastrointestinal:
    • Nausea, vomiting, and xerostomia.
  • Neuromuscular & skeletal:
    • Paresthesia

Rare side effcts include:

Anaphylaxis, abdominal pain & cramps, angina, chest pain & myocardial infarction, blurred vision & dry eyes, dyspepsia, fatigue, fever, gastritis, GERD, hypercholesterolemia, hypertension, insomnia, tachycardia, syncope, and cardiac arrhythmias.

Contraindications to almotriptan:

  • Severe allergic reactions to almotriptan and any component of its formulation.
  • Basilar or hemiplegic migraine
  • Example of Ischemic Heart Disease: Angina pectoris, Myocardial Infarction, Coronay artery vasospasm or Prinzmetal’s variant angina
  • Cerebrovascular disorders like stroke and transient ischemic attack
  • Peripheral Vascular Disease (ischemic bowel disease)
  • Hypertension uncontrolled
  • Use within 24 hours after another serotonin-agonist
  • Use within 24 hours after ergotamine derivatives

Warnings and Precautions

  • Headaches
    • Almotriptan can cause headaches to worsen if taken for more than 10 days.
  • Ocular effects
    • ​​​​​​​It can cause temporary and permanent vision impairments.
  • Allergy to sulfonamide
    • ​​​​​​​Almotriptan should not be used by patients who are allergic to sulfa medications.
    • Patients with high risk for cardiovascular disease, such as diabetes, hypertension, dyslipidemias, and a family history of IHD should be evaluated periodically for adverse events
  • Serotonin syndrome
    • ​​​​​​​Concomitant proserotonergic drugs may cause agitation, confusion and hyperreflexia.
    •  You should not use it with other serotonergic drugs.
    • Patients with liver and renal disease should use it with caution.

Almotriptan: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Antiemetics (5HT3 Antagonists) This may increase the serotonergic effects of Serotonin Activators. This could lead to serotonin syndrome.
Antipsychotic Agents Antipsychotic Agents may have a greater adverse/toxic effect if they are regulated with serotonin modulators. Serotonin modulators can increase dopamine blockade and, therefore, may increase the risk of developing neuroleptic malignant syndrome. Serotonin modulators may have a serotonergic effect that is enhanced by antipsychotic agents. This could lead to serotonin syndrome.
Droxidopa Droxidopa's hypertensive effects may be enhanced by Serotonin 5-HT1D Receptor Aggonists.
Metaxalone This may increase the serotonergic effects of Serotonin Activators. This could lead to serotonin syndrome.
Methylphenidate Can increase the toxic/adverse effects of Serotonin modulators. In particular, there may be an increase in the risk of serotonin syndrome and serotonin toxicities.
Metoclopramide The adverse/toxic effects of Metoclopramide may be exacerbated by Serotonin Modulators. This could manifest as serotonin syndrome, neuroleptic malignant syndrome, or other symptoms.
Opioid Agonists This may increase the serotonergic effects of Serotonin Activators. This could lead to serotonin syndrome.
Serotonin Modulators This may increase the toxic/adverse effects of other Serotonin Activators. Serotonin syndrome can develop. Exceptions: Nicergoline; Tedizolid.
TraMADol The adverse/toxic effects of TraMADol may be exacerbated by Serotonin Modulators. Seizures may increase. TraMADol could increase the serotonergic effects of Serotonin Activators. This could lead to serotonin syndrome.

Risk Factor D (Consider therapy modifications)

 
Strong CYP3A4 inhibitors May increase the serum concentration of Almotriptan. Use strong CYP3A4 inhibitors to limit almotriptan's initial adult dose to 6.25mg and to 12.5mg/24-hour for maximum dose. Patients with impaired renal or hepatic function should not be given concurrently.

Risk Factor X (Avoid Combination)

 
Dapoxetine Can increase the toxic/adverse effects of Serotonin Activators.
Ergot Derivatives May increase the vasoconstricting effects of Serotonin 5-HT1D receptor Agonists. The vasoconstricting effects of Ergot Derivatives could be enhanced by Serotonin 5-HT1D receptor Agonists. Nicergoline is an exception.
Methylene Blue This may increase the serotonergic effects of Serotonin Activators. This could lead to serotonin syndrome.
Monoamine Oxidase Inhibitors May reduce the metabolism of Serotonin 5-HT1D Receptor Aggonists. Management: Freovatriptan, Eletriptan and Naratriptan are suitable 5-HT1D agonists to use if MAO inhibitor therapy must be used.
SUMAtriptan The adverse/toxic effects of SUMAtriptan may be exacerbated by 5-HT1D Receptor Aggonists.

Monitoring Parameters:

  •  Monitor the patient for symptoms of ischemic heart disease and periodically with ECG and stress testing.
  • Baseline ECG, Liver and renal function tests should be performed routinely in all patients started on almotriptan therapy.
  • The first dose, in high risk patients (for IHD), should be given at a place where medical facility is available.

How to Administer Almotriptan?

 Almotriptan may be administered without regard to meals. 

Mechanism of action Almotriptan:

  • It reduces inflammation and causes vasoconstriction, relieving migraine symptoms.
  • It is well absorbed and is 35% protein bound. 
  • Metabolism to inactive metabolites is via MAO type A oxidative deamination and CYP3A4 and 2D6.
  • Bioavailability is around 70%
  • Half-life elimination is 3 to 5 hours.
  • Time to peak plasma concentration is 1 to 3 hours
  • Excretion is via Urine
  • AlmotriptanIt is a selective agonist for serotonin receptors of 5-HT1B and 1-Dtype in the cerebral arteries.

International Brands of Almotriptan:

  • Almogran
  • Almoptan
  • Almozen
  • Altrip
  • Magriban
  • Seratova
  • Triptagrain
  • APO-Almotriptan
  • Axert
  • MYLAN-Almotriptan
  • SANDOZ Almotriptan
  • TEVA-Almotriptan

Almotriptan Brands in Pakistan:

 No Brands available in Pakistan

How to treat moderate to severe acne? Read

Comments

Maurice Baldor
[email protected]

It's really a nice and helpful piece of information. I am glad that you shared this helpful information with us. Please stay us up to date like this. Thanks for sharing.|