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Almotriptan; Uses, Dosage, Side Effects, Interactions

Almotriptan is a sulfonamide triptan with extracerebral, intracranial vasoconstrictor activity. Almotriptan selectively binds to and activates serotonin 5-HT 1B and 1D receptors in the central nervous system (CNS), thereby causing extracerebral, intracranial blood vessel constriction. This may lead to pain relief from vascular headaches. Almotriptan may also relieve vascular headaches by preventing the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during a migraine, by reducing extravasation of plasma proteins, and by decreasing the release of other mediators of inflammation from the trigeminal nerve.

Almotriptan is a triptan drug for the treatment of migraine headaches. Almotriptan 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 a migraine. Almotriptan does not prevent migraine attacks.

Mechanism of action of Almotriptan

Almotriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction. Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of a migraine or for use in the management of a hemiplegic or a basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT_1D family) having only a weak affinity for 5-HT_1A, 5-HT_5A, 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 a migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan 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 Almotriptan in humans.

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Indications of Almotriptan

Migraines

Contra-Indications of Almotriptan

A migraine Headache with Temporary Paralysis of One Side
Severe uncontrolled high blood pressure
Transient ischaemic attack(TIA), peripheral vascular disease, severe hepatic impairment, concomitant administration of ergotamine, ergotamine derivatives
Heart attack
Myocardial infarction, angina pectoris, documented silent ischemia, Prinzmetal’s angina
Type of angina where Chest Pain Occurs at Rest
Coronary artery disease
Disease of Inadequate Blood Flow to the Heart Muscle, abnormal heart rhythm
Occasional Numbness or Tingling of Fingers and Toes
Peripheral vascular disease
Insufficiency of the vascular system of the intestine
Severe renal impairment
Family History of inadequate blood flow to the heart muscle
Increased cardiovascular event risk
Allergies to triptans-5-HT1 Antimigraine Agents

Do not take almotriptan within 24 hours before or after using another migraine headache medicine

Dosage of Almotriptan

Strengths: 6.25 mg; 12.5 mg, 25 mg

A migraine

Initial dose: 6.25 mg or 12.5 mg orally as a single dose
Repeat dose: If a headache is relieved, but returns, may repeat with 1 dose orally provided there is a minimum interval of 2 hours between doses.
Maximum daily dose: 25 mg

A pediatric Migraine

Adolescents (12 to 17 years)

Initial dose: 6.25 mg or 12.5 mg orally as a single dose
Repeat dose: If a headache is relieved, but returns, may repeat 1 dose orally provided there is a minimum interval of 2 hours between doses.
Maximum daily dose: 25 mg

Side Effects of Almotriptan

The most common

Nausea/vomiting
sleepiness
feeling of pain or tightness in your jaw, neck, or throat;
chest pain or heavy feeling, pain spreading to the arm or shoulder, sweating, general ill feeling;
sudden numbness or weakness,
Confusion, problems with vision, speech, or balance;
a headache
dry mouth
dizziness
Constipation
Weight gain/loss

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More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities

Drug Interactions of Almotriptan

Almotriptan may interact with the following drug, supplements, & may change the efficacy of the drug

amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
azathioprine
barbiturates (e.g., butalbital, pentobarbital phenobarbital)
antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, quetiapine, risperidone)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
ergotamine-containing or ergot-type medications (e.g., dihydroergotamine, methysergide)
macrolide antibiotics (e.g., clarithromycin, erythromycin)
metoclopramide
other 5-hydroxytryptamine receptor agonists (e.g., eletriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan)
peginterferon alfa-2b
protease inhibitors (e.g., indinavir, lopinavir, ritonavir)
selective norepinephrine reuptake inhibitors (SNRIs; e.g., venlafaxine)
selective serotonin receptor agonists (SSRIs; e.g., fluoxetine, fluvoxamine, paroxetine, sertraline)
trimethoprim
valproic acid
warfarin

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Pregnancy Category of Almotriptan

FDA Pregnancy Category C

Pregnancy

This medication should not be taken during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if almotriptan passes into breast milk. If you are breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children less than 12 years of age. Its use by people in this age group is not recommended.