Mechanism of action of Eletriptan
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has ma oddest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in a migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of a migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
Indications of Eletriptan
Contra-Indications of Eletriptan
- 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 Eletriptan
Strengths: 20 mg; 40 mg
Migraine
Use only after a clear diagnosis of a migraine has been established
- Initial dose: 20 mg or 40 mg orally, once
- Provided there has been some response to the first dose, a second dose may be administered at least 2 hours later if migraine returns or symptoms recur.
- Maximum dose: 80 mg in a 24-hour period
Side Effects of Eletriptan
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
- 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 Eletriptan
Eletriptan may interact with the following drug, suppliments, & may change the efficacy of the drug
- amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
- atypical anti-psychotics (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)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- cyclobenzaprine
- cyclosporine
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- metoclopramide
- other 5-hydroxytryptamine receptor agonists (e.g., eletriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan)
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, rasagiline, selegiline, tranylcypromine)
- 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)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- trimethoprim
- valproic acid
Pregnancy Category of Eletriptan
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 a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.T he 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.
Reference
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