Dosing and uses of Zecuity (sumatriptan transdermal)
transdermal patch (iontophoretic transdermal system)
6.5mg/4hr
Migraine Headache
NOTE (June 2016): Transdermal patch sales and distribution temporarily suspended to investigate the cause of burns and scars associated with the patch
Indicated for acute treatment of migraine with or without aura
Apply one 6.5 mg transdermal patch to dry, intact, non-irritated skin of upper arm or thigh at onset of migraine (see Administration section for instruction on how to activate iontophoretic system within the patch)
May apply a second patch if inadequate migraine relief after 2 hr; not to exceed 2 patches in 24 hr
Patch should not be applied to a previous application site until that site remains erythema free for at least 3 days
Do not cut the patch
Safety of using more than 4 patches in 1 month has not been established
Also see Administration
Pediatric dosage forms and strengths
Safety and efficacy not established
Zecuity (sumatriptan transdermal) adverse (side) effects
>10%
Application site pain (4-26%)
1-10%
Application site paresthesia (9%)
Application site pruritus (8%)
Application site warmth (6%)
Application site discomfort (6%)
Skin discoloration (3-5%)
Contact dermatitis (4%)
Application site irritation (4%)
Vesicles (3%)
Bruising (2%)
<1%
Skin erosion (0.4%)
Frequency not defined
Myocardial ischemia
Arrhythmias
Pain/tightness/pressure of chest, throat, neck and/or jaw
Cerebral hemorrhage, subarachnoid hemorrhage, and stroke
Noncoronary vasospastic reactions (eg, peripheral vascular ischemia, GI vascular ischemia and infarction)
Medication overuse headache
Serotonin syndrome Increased blood pressure
Anaphylaxis
Seizures
Warnings
Contraindications
Ischemic coronary artery disease (CAD) or coronary artery vasospasm; includes angina pectoris, MI, documented silent ischemia, Prinzmetal’s angina
Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders
History of stroke, TIA, hemiplegic or basilar migraine (higher stroke risk)
Peripheral vascular disease
Ischemic bowel disease
Uncontrolled hypertension
Use within 24 hr of ergotamine-containing medication, ergot-type medication, or another 5-HT1 agonist
Coadministration of an MAO-A inhibitor or use of MAO-A inhibitor within 2 weeks
Hypersensitivity
Severe hepatic impairment
Allergic contact dermatitis
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)
Risk of injury during MRI; patch must be removed before MRI procedure
Allergic contact dermatitis reported; discontinue patch if suspected
Cardiovascular evaluation should be performed in triptan-naïve patients who have multiple cardiovascular risk factors (increased age, diabetes, hypertension, smoking, obesity, family history)
Arrhythmias reported, including ventricular tachycardia and ventricular fibrillation
Tightness, pain, pressure, and heaviness in the chest, throat, neck and jaw reported
Cerebral hemorrhage, subarachnoid hemorrhage, and stroke reported
Noncoronary vasospasm reactions reported, including peripheral vascular ischemia, gastrointestinal vascular ischemia and infarct, splenic infarction, and Raynaud’s syndrome
Significant partial vision loss, and transient and permanent blindness reported; causal relationship not clearly established since visual disorders may be part of migraines
Serotonin syndrome may occur, particularly when coadministered with SSRIs, SNRIs, TCAs, and MAOIs; symptoms include mental status changes, autonomic instability, neuromuscular aberrations, and gastrointestinal symptoms
Increased blood pressure, including hypertensive crisis reported (rare)
Anaphylactic/anaphylactoid reactions reported
Seizures reported; use with caution in patients with history of epilepsy or conditions associated with a lowered seizure threshold
Should not be applied in areas near or over electrically-active implantable or body-worn medical devices (eg, cardiac pacemaker, insulin pump, deep brain stimulator)
Advise patients not to bathe, shower, or swim while wearing sumatriptan patch
Pregnancy and lactation
Pregnancy category: C
Reproductive toxicity studies for sumatriptan by transdermal route have not been conducted; embryolethality and blood vessel abnormalities observed with PO or IV doses in pregnant rabbits during organogenesis
Lactation: Excreted in 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 Zecuity (sumatriptan transdermal)
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; agonist effects specifically at the 5-HT 1B/1D receptors on intracranial blood vessels and trigeminal nerves result in cranial vessel constrictions and inhibition of pro-inflammatory neuropeptide release (substance P and calcitonin gene-related peptide)
Other pharmacodynamic actions include increased blood pressure and increased peripheral resistance
Absorption
Peak plasma time: 1.1 hr
Peak plasma concentration: 22 ng/mL
AUC: 110 hr•ng/mL
Cmax and AUC of transdermal application ~37% and 45% the values measured following sumatriptan 100 mg PO
Distribution
Protein bound: 14-21%
Vd: 2.4 L/kg
Metabolism
Metabolized by monamine oxidase (predominantly MAO-A)
Metabolites (inactive): Indole acetic acid (IAA) or the IAA glucuronide
Elimination
Half-life: 3.1 hr
Excretion: 11% urine (unchanged); 69% urine (IAA metabolite)
Administration
Transdermal Administration
Disposable, single use transdermal system designed to deliver sumatriptan through the skin using iontophoresis (noninvasive method of delivering a drug through the skin using a low electrical current); patch powered by 2 coin cell lithium batteries
Apply patch to dry, intact, nonirritated skin of upper arm or thigh; may secure with medical tape if needed
Within 15 minutes of applying the patch, push the application button to activate the iontophoretic transdermal system (red light will turn on)
When dosing is completed at 4 hr, the system stops operating (red light turns off) and the patch may be removed; system cannot be reactivated If the light turns off before 4 hr, dosing has stopped and the patch may be removed
Fold the adhesive sides together for disposal; patch contains lithium-manganese dioxide batteries and should be disposed in accordance with state and local regulations
