Suzetrigine Formulation and Administration
Suzetrigine tablets must not be cut, divided, crushed, chewed, or dissolved—the FDA-approved labeling explicitly states "do not divide, crush, chew or dissolve the tablet" and the medication must be swallowed whole with a full glass of water. 1
Formulation Characteristics
- Suzetrigine is formulated as an oral tablet designed for once-daily administration 1
- The medication is rapidly absorbed following oral administration with peak plasma concentrations (Tmax) occurring approximately 3 hours after dosing under fasting conditions 2
- The effective half-life is 23.6 hours, which supports the once-daily dosing schedule 2
Critical Administration Requirements
The tablet integrity must be maintained for proper drug delivery—any alteration of the tablet form (cutting, crushing, chewing, or dissolving) is contraindicated per FDA labeling. 1
- Adults and children 12 years and older should take 1 tablet daily with a full glass of water 1
- No more than 1 tablet should be taken in any 24-hour period 1
- Children under 12 years of age should not receive suzetrigine without consulting a physician 1
Special Population Considerations
- Patients with liver or kidney disease must consult a physician before taking suzetrigine, as the medication is primarily eliminated via hepatic metabolism 1, 2
- The FDA labeling specifically requires medical consultation for consumers with hepatic or renal impairment before initiating therapy 1
Seizure Disorder Context
For patients with seizure disorders, suzetrigine offers a theoretical safety advantage because it does not cross the blood-brain barrier and acts exclusively on peripheral nociceptors, avoiding central nervous system effects. 2
- Suzetrigine selectively blocks voltage-gated sodium channel Nav1.8 located only in peripheral pain-sensing neurons, with no expression in the brain 2, 3
- The medication exhibits greater than 31,000-fold selectivity for Nav1.8 compared to other sodium channel subtypes, minimizing off-target neurological effects 2
- Unlike medications that lower seizure threshold (such as bupropion or certain antidepressants), suzetrigine's peripheral-only mechanism avoids CNS-mediated seizure risk 2
Clinical Efficacy and Safety Profile
- Phase 3 trials demonstrated suzetrigine was generally safe and well-tolerated across 256 participants with various acute pain conditions, with most adverse events being mild (27.7%) or moderate (8.2%) in severity 4
- The most common side effects in clinical trials were headache and constipation, with no CNS side effects such as dependence, addiction, sedation, or respiratory depression 2, 5
- One case report documented patient-reported paresthesia following suzetrigine administration, representing a potential emerging side effect as the medication enters wider clinical use 5