suzetrigine

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.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: pruritus, rash

GI: nausea, vomiting

GU: renal impairment

MS: ↑CK, muscle spasms

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 wortmay ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

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

Availability ⬆ ⬇

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.

US Brand Names ⬆ ⬇

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 effects:

Reduction in pain.

Classifications ⬆ ⬇

Therapeutic Classification: nonopioid analgesics

Pharmacologic Classification:

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: 99%.

Metabolism/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)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3 hr	12 hr

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.

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Indications ⬇

Contraind./Precautions ⬆ ⬇