Axert


almotriptan malate

Axert

Pharmacologic class: Serotonin (5-hydroxytryptamine [5-HT]) receptor agonist

Therapeutic class: Vascular headache suppressant, antimigraine drug

Pregnancy risk category C

Action

Promotes vascular constriction and relieves migraine by stimulating specific 5-HT receptors in intracranial blood vessels and sensory trigeminal nerves

Availability

Tablets: 6.25 mg, 12.5 mg

Indications and dosages

Acute migraine

Adults: Single dose of 6.25 to 12.5 mg P.O. at first sign or symptom of migraine; may be repeated after 2 hours. Don't exceed two doses in a 24-hour period.

Dosage adjustment

• Severe renal or hepatic impairment

Contraindications

• Hypersensitivity to drug

• Ischemic heart disease, history of myocardial infarction (MI), documented silent ischemia, symptoms or findings consistent with ischemic heart disease, cerebrovascular accident, uncontrolled hypertension, coronary artery vasospasm

• Ischemic bowel disease

• Basilar or hemiplegic migraine

• MAO inhibitor use in past 14 days

• Use of other 5-HT agonists or ergotamine-containing or ergot-type drugs within past 24 hours

Precautions

Use cautiously in:

• impaired renal or hepatic function

• cardiovascular risk factors

• pregnant or breastfeeding patients

• children younger than age 18 (use not recommended).

Administration

• Give with or without food.

• Wait at least 2 hours after initial dose before giving repeat dose.

• Don't exceed two doses in 24 hours.

See Don't give within 14 days of MAO inhibitors or within 24 hours of other 5-HT agonists or ergotamine-containing or ergot-type drugs.

Adverse reactions

CNS: headache, anxiety, dizziness, fatigue, malaise, weakness, cold or hot sensations, sedation, numbness, burning or tingling sensations

CV: blood pressure changes, palpitations, tachycardia, coronary artery vasospasm, MI, ventricular fibrillation, ventricular tachycardia

EENT: vision changes; nasal, throat, and mouth discomfort

GI: nausea, abdominal distress, dysphagia, dry mouth

Musculoskeletal: weakness, stiff neck, muscle pain

Respiratory: chest tightness or pressure

Skin: sweating, flushing

Interactions

Drug-drug. CYP2D6 inhibitors (erythromycin, itraconazole, ritonavir): increased almotriptan effect

Ergot derivatives, other 5-HT agonists: prolonged vasoactive action

Ketoconazole and other CYP3A inhibitors: increased almotriptan blood level, leading to toxicity

MAO inhibitors: decreased almotriptan absorption

Selective serotonin reuptake inhibitors: weakness, hyperreflexia, poor coordination

Patient monitoring

• Assess patient's cardiovascular status, noting chest tightness or pressure.

• Monitor vital signs.

Patient teaching

See Tell patient to immediately report chest tightness or pressure.

• Inform patient that he may take drug with or without food.

• If second dose is needed, tell patient to take it at least 2 hours after first.

• Caution patient not to take more than two doses in 24 hours.

• Instruct patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

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

almotriptan

(al-moe-trip-tan) almotriptan,

Axert

(trade name)

Classification

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

Indications

Acute treatment of migraine headache (for adolescents, migraines should be ≥4 hr in duration).

Action

Acts as an agonist at specific 5-HT1 receptor sites in intracranial blood vessels and sensory trigeminal nerves.

Therapeutic effects

Cranial vessel vasoconstriction with associated decrease in release of neuropetides and resultant decrease in migraine headache.

Pharmacokinetics

Absorption: Well absorbed following oral administration (70%).Distribution: Unknown.Metabolism and Excretion: 40% excreted unchanged in urine; 27% metabolized by monoamine oxidase-A (MAO-A); 12% metabolized by cytochrome P450 hepatic enzymes (3A4 and 2D6); 13% excreted in feces as unchanged and metabolized drug.Half-life: 3–4 hr.

Time/action profile (Blood levels)

ROUTEONSETPEAKDURATION
POunknown1–3 hrunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Ischemic cardiovascular, cerebrovascular, or peripheral vascular syndromes (including ischemic bowel disease);History of significant cardiovascular disease;Uncontrolled hypertension;Should not be used within 24 hr of other 5-HT1 agonists or ergot-type compounds (dihydroergotamine);Basilar or hemiplegic migraine;Concurrent MAO-A inhibitor therapy or within 2 wk of discontinuing MAO-A inhibitor therapy.Use Cautiously 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 first dose is administered under supervision;Impaired hepatic or renal function;Hypersensitivity to sulfonamides (cross-sensitivity may occur); Obstetric / Lactation: Safety not established; Pediatric: Children <12 yr (safety not established).

Adverse Reactions/Side Effects

Central nervous system

  • drowsiness
  • headache

Cardiovascular

  • coronary artery vasospasm (life-threatening)
  • mi (life-threatening)
  • ventricular arrhythmias (life-threatening)
  • myocardial ischemia

Gastrointestinal

  • dry mouth
  • nausea

Neurologic

  • paresthesia

Interactions

Drug-Drug interaction

Concurrent use with MAO-A inhibitors ↑ blood levels and the risk of adverse reactions (concurrent use or use within 2 wk or MAO inhibitor is contraindicated).Concurrent use with other 5-HT1 agonists or ergot-type compounds (dihydroergotamine ) may result in additive vasoactive properties (avoid use within 24 hr of each other).↑ serotonin levels and serotonin syndrome may occur when used concurrently with SSRI and SNRI antidepressants.Blood levels and effects may be ↑ by ketoconazole, itraconazole, ritonavir, and erythromycin (inhibitors of CYP3A4 enzymes).

Route/Dosage

Oral (Adults and Children ≥12 yr) 6.25–12.5 mg initially, may repeat in 2 hr; not to exceed 2 doses per 24-hr period.

Hepatic/Renal Impairment

Oral (Adults) 6.25 mg initially, may repeat in 2 hr; not to exceed 2 doses per 24-hr period.

Availability

Tablets: 6.25 mg, 12.5 mg

Nursing implications

Nursing assessment

  • Assess pain location, character, intensity, and duration and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
  • Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs).

Potential Nursing Diagnoses

Acute pain (Indications)

Implementation

  • Do not confuse Axert with Antivert.
  • Oral: Tablets should be swallowed whole with liquid.

Patient/Family Teaching

  • Inform patient that almotriptan should only be used during a migraine attack. It is meant to be used for relief of migraine attacks but not to prevent or reduce the number of attacks.
  • Instruct patient to administer almotriptan as soon as symptoms of a migraine attack appear, but it may be administered any time during an attack. If migraine symptoms return, a second dose may be used. Allow at least 2 hr between doses, and do not use more than 2 doses in any 24-hr period.
  • If first dose does not relieve headache, additional almotriptan doses are not likely to be effective; notify health care professional.
  • Caution patient not to take almotriptan within 24 hr of another vascular headache suppressant.
  • Advise patient that lying down in a darkened room following almotriptan administration may further help relieve headache.
  • Advise patient to notify health care professional prior to next dose of almotriptan if pain or tightness in the chest occurs during use. If 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 professional at next visit.
  • May cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to avoid alcohol, which aggravates headaches, during almotriptan use.
  • Advise 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 notify health care professional immediately if signs or symptoms of serotonin syndrome occur.
  • Caution patient not to use almotriptan if she is pregnant, suspects she is pregnant, plans to become pregnant, or is breast feeding. Adequate contraception should be used during therapy.

Evaluation/Desired Outcomes

  • Relief of migraine attack.

Axert

A selective serotonin 5-HT1B/1D receptor agonist, which is used for acute management of severe migraine in adults.
 
Adverse effects
Nausea, somnolence, headache, paraesthesia, dry mouth.