Frovatriptan; Uses, Dosage, Side Effects, Interactions

Frovatriptan is a triptan drug Serotonin-1b and Serotonin-1d Receptor Agonist for the treatment of migraine headaches, in particular, those associated with menstruation. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. It is available as 2. 5 mg tablets.

Frovatriptan is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular, those associated with menstruation. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. It is available as 2. 5 mg tablets.

Mechanism of Action of Frovatriptan

Frovatriptan succinate is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. Frovatriptan is structurally distinct from but pharmacologically related to, other selective 5-HT1B/1D receptor agonists (e.g., almotriptan, naratriptan, rizatriptan, sumatriptan). Because the mechanisms involved in the pathogenesis of a migraine are not clearly understood, the precise mechanism of action of 5-HT1 receptor agonists in the management of a migraine has yet to be established. However, current data suggest that 5-HT1 receptor agonists, including frovatriptan, may ameliorate a migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and/or reduced transmission in the trigeminal pain pathway.

Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in a migraine. Research has shown that a migraine can be caused by the swelling of blood vessels around the brain. Frovatriptan eases the pain associated with a migraine by narrowing these blood vessels. Frovatriptan has one of the highest affinities for the 5-HT_1B of the second-generation triptan agonists. Frovatriptan is a second generation triptan 5-HT receptor agonist that binds with high affinity for 5-HT_1B and 5-HT_1Dreceptors. It is structurally distinct from but pharmacologically related to other selective 5-HT_1B/1D receptor agonists. Frovatriptan has no significant effects on GABA_A mediated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in a migraine. Research has shown that a migraine can be caused by the swelling of blood vessels around the brain. Frovatriptan eases the pain associated with a migraine by narrowing these blood vessels. Frovatriptan has one of the highest affinities for the 5-HT_1B of the second-generation triptan agonists.

Indications of Frovatriptan

• Menstrual migraines
• A migraine with aura
• Migraine without aura
• For the acute treatment of a migraine with or without aura.

Contra-Indications of Frovatriptan

Frovatriptan should not be given to patients with

• Ischemic heart disease
• Cerebrovascular syndrome
• Peripheral vascular disease
• Uncontrolled hypertension
• Hemiplegic or basilar migraine
• 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, angina
• Type of angina where Chest Pain Occurs at Rest
• Coronary artery disease

Dosage of Frovatriptan

Strengths: 2.5 mg, 5 mg, 7.5 mg

 Migraine

Use only after a clear diagnosis of a migraine has been established

• Initial dose: 2.5 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: 7.5 mg in a 24-hour period.

Side Effects of Frovatriptan

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;
• 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
• hallucinations
• a headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities

Drug Interactions of Frovatriptan

Frovatriptan 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 Frovatriptan

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 frovastriptan passes into breast milk. If you are a 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.

References

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