sumatriptan intranasal (Imitrex Intranasal, Onzetra Xsail)

Dosing and uses of Imitrex Intranasal, Onzetra Xsail (sumatriptan intranasal)

• Adult
• Pediatric

 

Adult dosage forms and strengths

intranasal spray (Imitrex Intranasal)

• 5 mg/actuation
• 20 mg/actuation

intranasal powder (Onzetra Xsail)

• 11mg/capsule in disposable nosepiece

 

Migraine Headache

Indicated for acute treatment of migraine headache with or without aura

Imitrex IntranasaL

• Individualized dose of 5 mg, 10 mg, or 20 mg intranasally once
• Administer 5 mg or 20 mg dose into 1 nostril; 10 mg dose achieved by administering 5 mg in each nostril
• If headache returns, may repeat dose once after 2 hr; not to exceed 40 mg/day

Onzetra Xsail intranasal powder

• 22 mg (2 nosepieces) administered using the Xsail breath-powered delivery device (see Administration)
• A second 22-mg dose may be administered if the migraine has not resolved by 2 hr after taking the first dose, or returns after a transient improvement
• Not to exceed 2 doses in 24 hr (ie, 44 mg/4 nosepieces) or 1 dose of Onzetra Xsail and 1 dose of another sumatriptan product, separated by at least 2 hr

 

Dosing Considerations

Safety not established for treating >4 headaches/30 days

 

Pediatric dosage forms and strengths

<18 years: Safety and efficacy not established

 

Imitrex Intranasal, Onzetra Xsail (sumatriptan intranasal) adverse (side) effects

>10%

Bad/unusual taste (13.5-24.5%)

Gastrointestinal: nausea/vomiting (11-13.5%)

 

1-10%

Disorder/discomfort of nasal cavity/sinuses (2.5-3.8%)

Throat discomfort (0.8-2.4%)

Dizziness/vertigo (1-1.7%)

Burning sensation (0.4-1.4%)

 

Frequency not defined

Atypical Sensations: Tingling, numbness, pressure sensation, cold sensation, feeling of tightness

Cardiovascular: Flushing, hypertension, palpations, tachycardia, arrhythmia, edema

Chest tightness/discomfort, chest pressure/heaviness

Disturbance of hearing, ear infections

Eye irritation and visual disturbances

Gastrointestinal: Abdominal discomfort, diarrhea, dysphagia, GERD, dry mouth, thirst

Musculoskeletal: Neck pain/stiffness, backache, weakness, joint symptoms, arthritis, myalgia, muscle cramps

Neurological: Drowsiness/sedation, anxiety, sleep disturbances, tremors, syncope, chills, depression, agitation, confusion

Respiratory: Dyspnea, lower respiratory infection

Skin: Rash/skin eruption, pruritus, erythema

Urogenital: Dysuria, dysmenorrhea

 

Postmarketing Reports

Blood: Hemolytic anemia, pancytopenia, thrombocytopenia

Cardiovascular: Atrial fibrillation, cardiomyopathy, colonic ischemia, Prinzmetal variant angina, pulmonary embolism, shock, thrombophlebitis

Ear, nose, throat: Deafness

Eye: Ischemic optic neuropathy, retinal artery occlusion, retinal vein thrombosis, loss of vision

Gastrointestinal: Ischemic colitis, dry mouth

Hepatic: Elevated LFTs

Neurological: CNS vasculitis, cerebrovascular accident, dysphasia, serotonin syndrome, subarachnoid hemorrhage

Psychiatric: Panic disorder

Respiratory: bronchospasm in patients with or without a history of asthma

Skin: exacerbation of sunburn, hypersensitivity reactions (erythema, pruritus, rash), photosensitivity

Urogenital: acute renal failure

Nonspecific: Angioneurotic edema, cyanosis, death, temporal arteritis

 

Warnings

Contraindications

Current/history of: ischemic cardiac, cerebrovascular, or peripheral vascular syndromes (angina, MI, stroke, TIA, ischemic bowel disease)

Uncontrolled hypertension

Coadministration of MAO-A inhibitors or use within 2 weeks after discontinuing MAO-A inhibitors

Use within 24 hr of any ergotamine-containing or ergot-type medication (eg, dihydroergotamine or methysergide)

Use within 24 hr of other 5-HT1 agonists

Hypersensitivity

Severe hepatic impairment

Not indicated for basilar or hemiplegic migraine

 

Cautions

Clear diagnosis of migraine headache has been established

Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache)

Serious cardiac and cerebrovascular events, including cerebral hemorrhage, subarachnoid hemorrhage, stroke, acute MI, arrhythmias, and death reported within a few hours after administration

Chest discomfort and jaw or neck tightness reported infrequently following intranasal administration (relatively common following SC injection)

Not for use with unrecognized CAD as predicted by risk factors (eg, hypertension, hypercholesterolemia, smoking, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, male aged >40 yr)

Serotonin syndrome may occur, particularly when coadministered with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine) Increased blood pressure, including hypertensive crisis reported (rare)

Local irritation of nose and throat reported

 

Pregnancy and lactation

Pregnancy category: C

Reproductive toxicity studies for sumatriptan by intranasal route have not been conducted; embryolethality and blood vessel abnormalities observed with PO or IV doses in pregnant rabbits during organogenesis

Lactation: Excreted in human breast milk in very low levels (NLM Toxnet); minimize infant to potential exposure by avoiding breastfeeding for 8-12 hr after administration

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Imitrex Intranasal, Onzetra Xsail (sumatriptan intranasal)

Mechanism of action

Selective 5-HT1 receptor agonist in cranial arteries; elicits vasoconstrictive and anti-inflammatory effects; associated with antidromic neuronal transmission and relief of migraine headache

 

Absorption

Bioavailability: 80-100%

Onset: 30 min

Peak Plasma Concentration: 5-16 ng/mL (dose dependent)

 

Distribution

Protein Bound: 14-21%

 

Metabolism

Metabolized by MAO-A

Metabolites: indole acetic acid analogue of sumatriptan

 

Elimination

Half-life: 2 hr

Total body clearance: 1,200 mL/min

Excretion: urine (3% unchanged, 42% as major metabolite)

 

Administration

Intranasal Administration

Imitrex IntranasaL

• Administer 5 mg or 20 mg metered-spray dose into 1 nostril
• 10 mg dose achieved by administering 5 mg in each nostril

Onzetra XsaiL

• Remove the clear device cap from the reusable delivery device, then remove a disposable nosepiece from its foil pouch and click the nosepiece into the device body
• Fully press and promptly release the white piercing button on the device body to pierce the capsule inside the nosepiece; the white piercing button should only be pressed once and released prior to administration to each nostril
• Insert the nosepiece is then inserted into the nostril so that it makes a tight seal; keeping the nosepiece in the nose, rotate the device to place the mouthpiece into the mouth
• The patient blows forcefully through the mouthpiece to deliver the sumatriptan powder into the nasal cavity
• Vibration (eg, a rattling noise) may occur, and indicates that the patient is blowing forcefully, as directed
• Once the medication in the first nosepiece has been administered, remove and discard the nosepiece
• The same process must then be repeated using a second 11 mg nosepiece into the other nostril to administer the remainder of the total recommended 22 mg dose

 

Storage

Imitrex IntranasaL

• Store between 36-86°F (2-30°C)
• Protect from light

Onzetra XsaiL

• Store at room temperature between 20-25°C (68-77°F), with excursions permitted between 15-30°C (59-86°F)
• Do not store in the refrigerator or freezer
• Use nosepiece immediately after removing from foil pouch