General

Pronunciation:
soo-se-tri-jeen

Trade Name(s)

• Journavx

Ther. Class.

nonopioid analgesics

Pharm. Class.

sodium channel blockers

Indications

Moderate to severe acute pain.

Action

Acts as a selective blocker of the Na_v  1.8 voltage-gated sodium channel, which then inhibits transmission of pain signals from peripheral sensory neurons to the spinal cord and brain.

Therapeutic Effect(s):

Reduction in pain.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: 99%.

Metabolism and Excretion: Primarily metabolized by the liver via the CYP3A isoenzyme to an active metabolite (M6–SUZ). 50% excreted in feces (primarily as metabolites), 44% excreted in urine (primarily as metabolites).

Half-life: Suzetrigine: 24 hr;  M6–SUZ: 33 hr.

TIME/ACTION PROFILE (plasma concentrations)

Contraindication/Precautions

Contraindicated in:

• Concurrent use of strong CYP3A inhibitors.
• End-stage renal disease
• Severe hepatic impairment.

Use Cautiously in:

• Moderate hepatic impairment (↓ dose)
• Rep:  Women of reproductive potential
• OB:  Safety not established in pregnancy;
• Lactation:  Safety not established in breastfeeding;
• Pedi:   Safety and effectiveness not established in children.

Adverse Reactions/Side Effects

Derm: pruritus, rash

GI: nausea, vomiting

GU: renal impairment

MS: ↑ CK, muscle spasms

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

•  Strong CYP3A inhibitors, including  itraconazole, may significantly ↑ levels and risk of toxicity; concurrent use contraindicated.
•  Moderate CYP3A inhibitors, including  fluconazole, may ↑ levels and risk of toxicity; ↓ suzetrigine dose.
• May ↓ levels and effectiveness of  CYP3A substrates, including  midazolam.
•  Strong CYP3A inducers, including  rifampin, and  moderate CYP3A inducers, including  efavirenz, may ↓ levels and effectiveness; avoid concurrent use.
• May ↓ levels and effectiveness of  hormonal contraceptives  containing progestins OTHER than levonorgestrel or norethindrone.

Drug-Natural Products:

 St. John's wort may ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

Grapefruit juice may ↑ levels and risk of toxicity; avoid concurrent use.

Route/Dosage

PO (Adults): 100 mg initially, then 50 mg every 12 hr starting 12 hr after initial dose. Do not exceed treatment duration of 14 days. Concurrent use of moderate CYP3A inhibitors: 100 mg initially, then starting 12 hr after initial dose, give 50 mg every 12 hr for 3 doses, then 12 hr later, give 50 mg once daily. Do not exceed treatment duration of 14 days.

Hepatic Impairment 
PO (Adults): 100 mg initially, then starting 12 hr after initial dose, give 50 mg every 12 hr for 3 doses, then 12 hr later, give 50 mg once daily. Do not exceed treatment duration of 14 days.

Availability

Tablets: 50 mg

Assessment

• Assess pain level and location before and during therapy.
• Assess for pruritus, rash, and muscle spasms.

Lab Test Considerations:

• May ↑ CK.
• May ↓ eGFR.
• Monitor liver function tests periodically during therapy.

Implementation

• Use for the shortest duration consistent with patient treatment goals; use >14 days has not been evaluated.
• PO  DNC: Swallow tablets whole. Do not chew or crush. 
• Administer starting dose, 100 mg, on an empty stomach >1 hr before or 2 hr after food. Clear liquids may be consumed (water, apple juice, vegetable broth, tea, black coffee) during this time. Subsequent doses can be administered with or without food.

Patient/Family Teaching

• Explain purpose and side effects of medication to patient. Advise patient to read  Patient Information  before starting therapy. If a dose is missed, take the missed dose as soon as possible and then take the next scheduled dose at the recommended time. If >2 doses are missed, take 100 mg and then take the next scheduled dose at the recommended time.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
• Advise patient to avoid foods or drinks containing grapefruit during therapy.
• Rep:  Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise patient taking concurrent hormonal contraceptives containing progestins other than levonorgestrel and norethindrone to use additional nonhormonal contraceptives (condoms) or alternative contraceptives (a combined oral contraceptive containing ethinyl estradiol as the estrogen and levonorgestrel or norethindrone as the progestin or an intrauterine system) during treatment and for 28 days after final dose.

Evaluation/Desired Outcomes

Reduction in pain.