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Almogran

Almogran - General Information

Almogran is a triptan drug for the treatment of migraine headaches. Almogran is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stopping the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Almogran does not prevent migraine attacks.

 

Pharmacology of Almogran

Almogran is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almogran is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almogran is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almogran also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almogran in humans.

 

Almogran for patients

 

Almogran Interactions

Ergot-Containing Drugs

These drugs have been reported to cause prolonged vasospastic reactions. Because there is a theoretical basis that these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and AXERT within 24 hours of each other should be avoided.

Monoamine Oxidase Inhibitors

Coadministration of moclobemide resulted in a 27% decrease in almotriptan clearance and an increase in Cmax of approximately 6%. No dose adjustment is necessary.

Other 5-HT1B/1D Agonists

Concomitant use of other 5-HT1B/1D agonists within 24 hours of treatment with AXERT® is contraindicated.

Propanolol

The pharmacokinetics of almotriptan were not affected by coadministration of propranolol.

Selective Serotonin Reuptake Inhibitors (SSRIs)

SSRIs (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline) have been rarely reported to cause weakness, hyperreflexia, and incoordination when coadministered with 5-HT1 agonists.

If concomitant treatment with AXERT and an SSRI is clinically warranted, appropriate observation of the patient is advised.

Verapamil

Coadministration of almotriptan and verapamil resulted in a 24% increase in plasma concentrations of almotriptan. No dose adjustment is necessary.

Ketoconazole and Other Potent CYP3A4 Inhibitors

Coadministration of almotriptan and the potent CYP3A4 inhibitor ketoconazole (400 mg q.d. for 3 days) resulted in an approximately 60% increase in the area under the plasma concentration-time curve and maximal plasma concentrations of almotriptan. Although the interaction between almotriptan and other potent CYP3A4 inhibitors (e.g., itraconazole, ritonavir, and erythromycin) has not been studied, increased exposures to almotriptan may be expected when almotriptan is used concomitantly with these medications.

Drug/Laboratory Test Interactions

AXERT is not known to interfere with commonly employed clinical laboratory tests.

 

Almogran Contraindications

AXERT (almotriptan malate) Tablets should not be given to patients with ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or to patients who have symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm, including Prinzmetal's variant angina, or other significant underlying cardiovascular disease.

Because AXERT may increase blood pressure, it should not be given to patients with uncontrolled hypertension.

AXERT® should not be administered within 24 hours of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide.

AXERT should not be given to patients with hemiplegic or basilar migraine.

AXERT is contraindicated in patients who are hypersensitive to almotriptan or any of its ingredients.

 

Additional information about Almogran

Almogran Indication: For the treatment of acute migraine headache in adults
Mechanism Of Action: Almogran binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction.
Drug Interactions: Citalopram Increased risk of CNS adverse effects
Dihydroergotamine Possible severe and prolonged vasoconstriction
Escitalopram Increased risk of CNS adverse effects
Fluoxetine Increased risk of CNS adverse effects
Fluvoxamine Increased risk of CNS adverse effects
Ergotamine Possible severe and prolonged vasoconstriction
Isocarboxazid MOA inhibitor increases the effects and toxicity of 5-HT agonist
Ergonovine Possible severe and prolonged vasoconstriction
Itraconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Ketoconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Ergonovine Possible severe and prolonged vasoconstriction
Methylergonovine Possible severe and prolonged vasoconstriction
Methysergide Possible severe and prolonged vasoconstriction
Nefazodone Increased risk of CNS adverse effects
Paroxetine Increased risk of CNS adverse effects
Phenelzine MAO inhibitor increases the effects and toxicity of 5-HT agonist
Sertraline Increased risk of CNS adverse effects
Sibutramine Increased risk of CNS adverse effects
Tranylcypromine MAO inhibitor increases the effects and toxicity of 5-HT agonist
Venlafaxine Increased risk of CNS adverse effects
Dihydroergotoxine Possible severe and prolonged vasoconstriction
Ergonovine Possible severe and prolonged vasoconstriction
Food Interactions: Take without regard to meals.
The absorption is unaffected by food.
Generic Name: Almotriptan
Synonyms: Not Available
Drug Category: Anti-migraine Agents; Anti-inflammatory Agents; Vasoconstrictor Agents; Selective Serotonin Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Almotriptan: Axert; Almogran;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: 35%
Biotransformation: Not Available
Half Life: 3-4 hours
Dosage Forms of Almogran: Tablet Oral
Chemical IUPAC Name: N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine
Chemical Formula: C17H25N3O2S
Almotriptan on Wikipedia: http://en.wikipedia.org/wiki/Almotriptan
Organisms Affected: Humans and other mammals