Relpax


eletriptan hydrobromide

Relpax

Pharmacologic class: 5-hydroxytryptamine-1 (5-HT1) receptor agonist

Therapeutic class: Antimigraine agent

Pregnancy risk category C

Action

Binds with serotonin 5-HT1B receptors on intracranial blood vessels and serotonin 5-HT1D receptors on sensory nerve endings, constricting cranial arteries and thereby relieving migraine

Availability

Tablets: 20 mg, 40 mg

Indications and dosages

➣ Migraine with or without aura

Adults: Initially, 20 to 40 mg P.O.; may repeat in 2 hours if headache returns after initial improvement. Maximum recommended single dosage is 40 mg.

Contraindications

• Hypersensitivity to drug

• Basilar and hemiplegic migraine

• Severe hepatic disease

• Ischemic heart disease

• Peripheral vascular disease

• Cerebrovascular syndromes

• Uncontrolled hypertension

• Ischemic bowel disease

• Within 24 hours of another serotonin agonist or ergot-type drug

Precautions

Use cautiously in:

• hepatic or renal impairment, diabetes mellitus, hypercholesterolemia, cardiac disorders

• pregnant or breastfeeding patients

• children.

Administration

• Give first dose as soon as migraine symptoms arise.

See Be aware that first dose should be given under close supervision to patients with coronary artery disease.

• If headache improves but then recurs, give second dose at least 2 hours after first.

• Be aware that drug's safety in treating an average of more than three headaches within a 30-day period has not been established.

Adverse reactions

CNS: dizziness, insomnia, drowsiness, headache, fatigue, anxiety, paresthesia, asthenia,cerebrovascular ischemia

CV: chest pain, palpitations, hypertension,cardiovascular ischemia

GI: nausea, vomiting, diarrhea, dry mouth

Musculoskeletal: muscle weakness

Respiratory: chest tightness or pressure

Skin: flushing

Other: hot or cold sensation

Interactions

Drug-drug. Antihistamines, ergotamine, ergot derivatives: increased vasospastic effects

CYP450-3A4 inhibitors (such as clarithromycin, ketoconazole, propranolol): increased eletriptan blood level

MAO inhibitors: increased eletriptan effects

Patient monitoring

• Monitor vital signs and assess for chest pain, tightness, or pressure.

Patient teaching

• Instruct patient to take first dose as soon as migraine symptoms occur. If headache improves but then recurs, advise him to take second dose at least 2 hours after first.

• Caution patient to avoid driving and other hazardous activities until drug no longer affects concentration and alertness.

• Tell patient to report chest pain, pressure, or tightness.

• Inform patient that drug won't prevent migraines and isn't effective against other headache types.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.

eletriptan

(e-le-trip-tan) eletriptan,

Relpax

(trade name)

Classification

Therapeutic: vascular headache suppressants
Pharmacologic: five ht1 agonists
Pregnancy Category: C

Indications

Acute treatment of migraine headache.

Action

Acts as an agonist at specific 5-hydroxy-tryptamine receptor sites in intracranial blood vessels and sensory trigeminal nerves.

Therapeutic effects

Cranial vessel vasoconstriction with resultant decrease in migraine headache.

Pharmacokinetics

Absorption: 50% absorbed after oral administration.Distribution: Enters breast milk.Metabolism and Excretion: Mostly metabolized by the liver via the CYP3A4 enzyme system.Half-life: 4 hr.

Time/action profile (decreased migraine pain)

ROUTEONSETPEAKDURATION
POwithin 2 hr2 hrup to 24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Hemiplegic or basilar migraine;Ischemic heart disease or Prinzmetal's angina;Uncontrolled hypertensionWolff-Parkinson-White syndrome or other arrhythmias involving conduction pathwaysStroke or transient ischemic attack;Peripheral vascular disease;Ischemic bowel diseaseSevere hepatic impairment;Should not be used within 24 hr of other 5-HT1 agonists or ergot-type compounds (dihydroergotamine);Should not be used within 72 hr of potent CYP3A4 inhibitors including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, and nelfinavir.Use Cautiously in: Obstetric: Use only if potential benefits justify potential risk to fetus; Lactation: Doses up to 80 mg daily not expected to cause adverse effects in breast-fed infants >2 mo (NIH); Pediatric: Safety not established; Geriatric: ↑ risk of ↑ BP.Exercise Extreme Caution in: Cardiovascular risk factors (hypertension, hypercholesterolemia, cigarette smoking, obesity, diabetes, strong family history, menopausal women or men >40 yr); use only if cardiovascular status has been evaluated and determined to be safe and 1st dose is administered under supervision.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • drowsiness
  • weakness

Cardiovascular

  • mi (life-threatening)
  • ventricular fibrillation (life-threatening)
  • ventricular tachycardia (life-threatening)
  • angina
  • chest tightness/pressure
  • coronary vasospasm
  • ECG changes
  • transient hypertension

Gastrointestinal

  • abdominal pain
  • dry mouth
  • dysphagia
  • nausea

Neurologic

  • paresthesia

Miscellaneous

  • anaphylaxis (life-threatening)

Interactions

Drug-Drug interaction

Blood levels and risk of adverse reactions are ↑ by potent CYP3A4 inhibitors (including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, and nelfinavir ); use within 72 hr is contraindicated.Concurrent use (within 24 hr of each other) with ergot-containing drugs (dihydroergotamine ) may result in prolonged vasospastic reactions and should be avoided.↑ serotonin levels and serotonin syndrome may occur when used concurrently with SSRI and SNRI antidepressants.

Route/Dosage

Oral (Adults) 20 or 40 mg; may be repeated in 2 hr if initial response is inadequate (not to exceed 80 mg/24 hr or treatment of 3 headaches/mo).

Availability

Tablets: 20 mg, 40 mg

Nursing implications

Nursing assessment

  • Assess pain location, intensity, character, duration and associated symptoms (photophonia, phonophobia, nausea, vomiting) during migraine attack.

Potential Nursing Diagnoses

Acute pain (Indications)

Implementation

  • Oral: Administer at the first sign of a headache. If after the initial dose, headache improves but then returns, dose may be repeated at least 2 hr after initial dose. If initial dose is ineffective, second dose is unlikely to be effective.

Patient/Family Teaching

  • Instruct patient that eletriptan should only be used during a migraine attack. Eletriptan is used for treatment of a migraine attack, not for prevention. Advise patient to read the Patient Summary of Information before starting therapy and with each Rx refill in case of changes.
  • Instruct patient to take eletriptan at the first sign of a migraine, but may be administered at any time during attack. Allow at least 2 hr between doses and do not use more than 80 mg/day or 3 attacks/mo.
  • Caution patient not to take eletriptan within 24 hr of other vascular headache suppressants.
  • Advise patient that lying down in a darkened room after eletriptan administration may further help relieve headache.
  • Advise patient to notify health care professional if she plans or suspects pregnancy, or if breast feeding.
  • Advise patient to notify health care professional before next dose of eletriptan if pain or tightness in the chest occurs. If chest pain is severe or does not subside, notify health care professional immediately. If feelings of tingling, heat, flushing, heaviness, pressure, drowsiness, dizziness, tiredness, or sickness develop, discuss with health care provider at next visit.
  • May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise patient to avoid alcohol, which aggravates headaches, during therapy.
  • Advise patient that overuse (use more than 10 days/month) may lead to exacerbation of headache (migraine-like daily headaches, or as a marked increase in frequency of migraine attacks). May require gradual withdrawal of rizatriptan and treatment of symptoms (transient worsening of headache).
  • Instruct patient to notify health care professional if signs of serotonin syndrome (mental status changes: agitation, hallucinations, coma; autonomic instability: tachycardia, labile BP, hyperthermia; neuromuscular aberrations: hyperreflexia, incoordination; and/or gastrointestinal symptoms: nausea, vomiting, diarrhea) occur.
  • Advise patient to notify health care professional if pregnancy is planned or suspected, or if breast feeding.

Evaluation/Desired Outcomes

  • Relief of migraine attack.

Relpax

(rĕl′păks′) A trademark for the drug eletriptan hydrobromide.

Relpax

A brand name for ELETRIPAN.