ruxolitinib (topical)

Absorption: Systemic absorption occurs following topical administration and is dependent on dose and surface area of application.

Distribution: Unknown.

Protein Binding: 97%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme, with minor contribution from CYP2C9. Primarily excreted in the urine (74%), with 22% excreted in the feces. Less than 1% excreted as unchanged drug.

Half-Life: 116 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
Topical	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Active, serious infection
;
Risk factor for thrombosis;
Lactation: Lactation.

Use Cautiously in:

Chronic or recurrent infection
;
History of a serious infection or opportunistic infection
;
Exposure to tuberculosis (TB)
;
Resided or traveled in areas of endemic TB or endemic mycoses
;
>50 yr old with ≥1 cardiovascular risk factor (may ↑ risk of all-cause mortality, cardiovascular death, MI, stroke, and thrombosis)
;
Immunocompromised;
Known malignancy (other than a successfully treated nonmelanoma skin cancer or cervical cancer)
;
OB: Other agents preferred for the topical treatment of atopic dermatitis and vitiligo in pregnancy;
Pedi: Children <12 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: ARTERIAL THROMBOSIS, CARDIOVASCULAR DEATH, DEEP VEIN THROMBOSIS

Derm: acne, erythema, folliculitis, NONMELANOMA SKIN CANCER, pruritus, urticaria

EENT: nasopharyngitis, rhinorrhea, tonsillitis

GI: diarrhea

Hemat: anemia, eosinophilia, neutropenia, thrombocytopenia

Metab: hyperlipidemia

Neuro: headache

Resp: PULMONARY EMBOLISM

Misc: fever, INFECTION(INCLUDING REACTIVATION TB AND OTHER OPPORTUNISTIC INFECTIONS DUE TO BACTERIAL, FUNGAL, VIRAL, AND MYCOBACTERIAL PATHOGENS), MALIGNANCY

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including ketoconazole, may ↑ levels and risk of toxicity; avoid concurrent use.

Route/Dosage ⬆ ⬇

Atopic Dermatitis

(Adults and Children ≥12 yr): Apply a thin layer twice daily to affected area(s) of up to 20% body surface area. Discontinue once signs/symptoms resolve. Reassess therapy if signs/symptoms have not resolved within 8 wk. Do not use more than one 60-g tube per wk or one 100-g tube per 2 wk.

Nonsegmental Vitiligo

(Adults and Children ≥12 yr): Apply a thin layer twice daily to affected area(s) of up to 10% body surface area. Reassess need for continued therapy if no meaningful improvement with repigmentation by 24 wk. Do not use more than one 60-g tube per wk or one 100-g tube per 2 wk.

Availability ⬆ ⬇

Assessment ⬆ ⬇

Assess area of skin affected before applying and periodically during therapy.
Monitor signs and symptoms of infection during and after therapy. If serious or opportunistic infection or sepsis occurs, hold ruxolitinib; may resume when infection is controlled.
Evaluate patients for latent and active TB infection before administration. Monitor for signs and symptoms of TB during therapy.
Monitor for signs and symptoms of viral reactivation during therapy. If herpes zoster occurs during therapy, consider holding ruxolitinib until episode resolved.
Assess for hepatitis B and C before starting therapy. Avoid therapy in patients with active hepatitis B or C.
Perform periodic skin examination in ↑ risk patients of skin cancer.

Lab Test Considerations:

Monitor CBC periodically during therapy. May cause thrombocytopenia, anemia, and neutropenia. If clinically significant cytopenias occur, discontinue ruxolitinib.
- May ↑ total cholesterol, LDL-C, and triglycerides.

Implementation ⬆ ⬇

Topical Atopic dermatitis: Apply a thin layer of ruxolitinib twice daily to affected areas of up to 20% body surface area. Stop using when signs/symptoms of atopic dermatitis (itch, rash, redness) resolve. If dermatitis does not improve within 8 wk, re-examine affected area.
Nonsegmental Vitiligo: Apply a thin layer of ruxolitinib twice daily to affected areas of up to 10% body surface area; may require >24 wk. If no meaningful repigmentation occurs by 24 wk, re-evaluate affected area.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient to wash hands after applying, unless hands are being treated. Do not use in eyes, mouth, or vagina.
Advise patient to notify health care provider if signs and symptoms of infections (fever; sweating; chills; muscle aches; cough or shortness of breath; blood in phlegm; weight loss; warm, red, or painful skin or sores on the body; diarrhea or stomach pain; burning on urination or urinating more often than usual; feeling very tired) occur.
Advise patient to notify health care provider promptly if signs/symptoms of heart attack or stroke (pain or pressure in chest, throat, neck, jaw, stomach, arms, or back; shortness of breath; sweatiness; nausea; vomiting; dizziness; weakness in one part of body; slurred speech), blood clots (swelling, pain, or tenderness in one or both legs; sudden, unexplained chest or upper back pain; difficulty breathing; unusual bleeding, bruising, fever, or tiredness) occur.
Inform patient that ruxolitinib may ↑ risk of cancer (lymphoma, lung cancer). Advise patient to have periodic skin examinations and to tell health care provider if they have ever had any type of cancer.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications during therapy.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected and to avoid breastfeeding during therapy and for 4 wk after last dose. Encourage patients who are exposed to ruxolitinib during pregnancy to enroll in registry that monitors outcomes in pregnancy by calling 1-855-463-3463.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇