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-HT1B and 5-HT1D 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-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 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.
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
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
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.
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