- March 15, 2022
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Brand Name :
Axert
Synonyms :
almotriptan
Class :
Serotonin 5 HT-receptor agonists
Dosing forms and strengths
Tablet
(6.25 mg)
(12.5 mg)
Dosage forms and strengths
Tablet
(6.25 mg)
(12.5 mg)
Refer adult Dosing
may enhance the serum concentration of CYP3A4 inhibitors
may have an increasingly adverse effect when combined with serotonin 5-HT1D receptor agonists
may enhance the serum concentration of CYP3A4 Inhibitors
may have an increasingly adverse effects when combined with almotriptan
may have an increased effect of CNS depression when combined with Almotriptan
may enhance the risk of hypertension when combined with almotriptan
may increase the risk of CNS depression when combined
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
may enhance the serotonergic effect of monoamine oxidase inhibitors
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may increase the risk or severity of adverse effects when combined
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased vasoconstricting effect when combined with ergot derivatives
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increased serotonergic effect when combined with monoamine oxidase inhibitors
may have an increasingly adverse effect when combined with sumatriptan
serotonin 5-HT1D receptor agonists increase the serotonergic effect of MAO inhibitors
May have an increased serotonergic effect when combined with Serotonergic Agents
may have an increased serotonergic effect when combined with serotonergic agents
It may enhance serotonin levels when combined with tramadol
The effectiveness of guanoxan's antihypertensive properties could be diminished by the presence of almotriptan
Combining levobetaxolol and almotriptan can diminish levobetaxolol’s metabolism
The potential for increased CNS depression risk or seriousness occurs when almotriptan is used together with pinazepam
It may enhance the risk of bleeding when combined with nimesulide
The potential for CNS depression may enhanced when almotriptan is used together with fencamfamin
Combining tegafur with almotriptan can reduce tegafur’s metabolism
When almotriptan is used together with medazepam, the risk or seriousness of CNS depression is enhanced
almotriptan may intensify paraldehyde's CNS depressant effects
when both drugs are combined, there may be an increased risk or severity of adverse effects
may enhance the serotonergic effect of serotonergic agents
may increase the risk or severity of hypertension when combined
may enhance the risk or severity of hypertension when combined
may enhance the risk or severity of hypertension when combined
may have an increased hypertensive effect when combined with droxidopa
may increase the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists
It may diminish the metabolism when combined with nilvadipine
almotriptan serum concentration may also be increased by CYP3A4 inhibitors (strong)
almotriptan serum concentration may also be increased by CYP3A4 inhibitors (strong)
almotriptan serum concentration may also be increased by CYP3A4 inhibitors (strong)
almotriptan serum concentration may also be increased by CYP3A4 inhibitors (strong)
almotriptan serum concentration may also be increased by CYP3A4 inhibitors (strong)
Actions and Spectrum:
Serotonin receptor agonism: almotriptan acts as an agonist (activator) of serotonin receptors, specifically the 5-HT1B and 5-HT1D receptors found in the blood vessels and nerves in the brain
Vasoconstriction: almotriptan causes vasoconstriction, or narrowing of blood vessels, which can help to reduce the excessive dilation of blood vessels that occurs during a migraine attack. The spectrum of almotriptan is specific to the treatment of acute migraine attacks.
It is not intended for the prevention of migraines or for the treatment of other types of headaches. almotriptan is typically used in adults and is available in different formulations, including oral tablets and orally disintegrating, for convenient administration.
Frequency defined
Adults
1-10%
Dry mouth (1-2%)
Headache (1-2%)
Somnolence (1-5%)
Dizziness (3-4%)
Nausea (1-3%)
Nausea (1-2%)
Paresthesia (1-2%)
Paresthesia (1%)
Somnolence (>1%)
<1%
Back pain, myalgia, neck pain, rigid neck, Increased CPK
Bronchitis, chest pain, dyspnea, pharyngitis, rhinitis, sinusitis
Conjunctivitis, tinnitis, vertigo
Black Box Warning:
WARNING: SERIOUS CARDIOVASCULAR AND CEREBROVASCULAR EVENTS
almotriptan is contraindicated in patients with a history of ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal’s angina.
Cardiovascular events, including myocardial infarction and stroke, have been reported using almotriptan. almotriptan should not be used in patients with risk factors for cardiovascular disease, including smoking, obesity, diabetes, high cholesterol levels, family history of cardiovascular disease, or patients who are postmenopausal or male over 40 years of age.
Serotonin syndrome, a potentially life-threatening condition, has been reported with the use of almotriptan, particularly when used concomitantly with serotonergic drugs, such as (SSRIs), (SNRIs), (MAOIs).
Contraindication/Caution:
Hypersensitivity: almotriptan is contraindicated in individuals who have a known hypersensitivity or allergy to almotriptan or any of its components.
Ischemic heart disease: almotriptan should not be used in patients with a history of ischemic heart disease, including angina (chest pain), myocardial infarction (heart attack), or other significant cardiovascular disease, as it may increase the risk of cardiovascular events.
Uncontrolled hypertension: almotriptan is contraindicated in patients with uncontrolled hypertension (high blood pressure) as it can potentially exacerbate high blood pressure and increase the risk of cardiovascular events.
Severe hepatic impairment: almotriptan should not be used in individuals with severe hepatic impairment (liver dysfunction) as it may affect the metabolism and elimination of the drug, leading to increased levels of almotriptan in the blood and potential adverse effects.
Concurrent use of MAO inhibitors: almotriptan is contraindicated in these patients.
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
<b>Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
almotriptan is administered orally and is rapidly absorbed from the gastrointestinal tract.
It undergoes extensive metabolism in the liver, primarily via the enzyme CYP3A4, and is excreted in the urine and feces.
The half-life of almotriptan is approximately 3-4 hours, and it is eliminated from the body relatively quickly.
Pharmacodynamics:
almotriptan is a selective serotonin 5-HT1B/1D receptor agonist, which means it binds to specific serotonin receptors in the brain.
It has high affinity for 5-HT1B receptors located on blood vessels, including those in the meninges, and inhibits the release of pro-inflammatory neuropeptides.
MOA: The mechanism of action of almotriptan involves its selective binding to certain serotonin receptors in the brain, leading to several effects that help alleviate migraine symptoms.
Pharmacokinetics:
Absorption: almotriptan is rapidly and well absorbed after oral administration. It is highly lipophilic, meaning it has a strong affinity for fat, and can penetrate cell membranes easily.
Distribution : almotriptan has a moderate volume of distribution, indicating that it is moderately distributed throughout the body. It binds extensively to plasma proteins (about 35%) and has a relatively long plasma elimination half-life of approximately 3-4 hours.
Metabolism: almotriptan is primarily metabolized in the liver by the enzyme CYP3A4, which converts it to its active metabolite, 1-hydroxyalmotriptan. This metabolite also has affinity for serotonin receptors and contributes to the therapeutic effect of almotriptan.
Elimination and Excretion:
almotriptan and its metabolites are mainly eliminated through renal excretion, with approximately 60% of the dose excreted in urine and about 40% excreted in feces.
Administration:
The healthcare provider will provide the patient with specific instructions on how to take almotriptan. This may include information on the timing of the dose in relation to the onset of a migraine attack, as well as any additional dosing instructions, such as taking a second dose if the headache recurs after an initial dose.
Patient information leaflet
Generic Name: almotriptan
Why do we use almotriptan ?
almotriptan works by binding to serotonin receptors in the brain, which helps to reduce the swelling of blood vessels and block pain signals, ultimately relieving the symptoms of a migraine attack. It is available in different forms, including tablets, orally disintegrating tablets, and as a nasal spray, allowing for different routes of administration depending on the preference and convenience of the patient.
almotriptan, like other triptans, is typically used when other non-prescription pain relievers, such as acetaminophen or ibuprofen, are not effective in relieving migraine symptoms. It is important to note that almotriptan is not suitable for everyone, and it should be used only as prescribed by a healthcare professional.
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