sirolimus (topical)

Contraindicated in:

Hypersensitivity;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Rep: Women of reproductive potential;
Pedi: Children <6 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: acne, dry skin, pruritus, dermatitis

EENT: eye irritation, ocular hyperemia

GU: amenorrhea, infertility (men), menorrhagia, ovarian cysts

Local: application site irritation

Metab: hypercholesterolemia, hypertriglyceridemia

Neuro: PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML)

Resp: interstitial lung disease (ILD)

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), INFECTION , MALIGNANCY

Interactions ⬆ ⬇

Drug-drug:

CYP3A4 inhibitors may ↑ levels and risk of toxicity.
May ↑ levels and risk of toxicity of CYP3A4 substrates and CYP3A4 inhibitors.
Concurrent use with ACE inhibitors may ↑ risk of angioedema.
Vaccines may be less effective if given concurrently with sirolimus; avoid use of live-virus vaccines.

Availability ⬆ ⬇

Topical gel: 0.2%

Route/Dosage ⬆ ⬇

(Adults and Children ≥12 yr): Apply twice daily (in the AM and at bedtime) to affected facial area(s) (max daily dose = 800 mg [2.5 cm]). If symptoms do not improve within 12 wk, re-evaluate need for continuing therapy.
(Children 6–11 yr): Apply twice daily (in the AM and at bedtime) to affected facial area(s) (max daily dose = 600 mg [2 cm]). If symptoms do not improve within 12 wk, re-evaluate need for continuing therapy.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits mammalian target of rapamycin activation. Mechanism in treatment of angiofibroma associated with tuberous sclerosis unknown.

Therapeutic effects:

Reduction in size and redness of facial angiofibroma.

Classifications ⬆ ⬇

Therapeutic Classification: Immunosuppressant agents

Pharmacokinetics ⬆ ⬇

Absorption: Minimally absorbed into systemic circulation.

Distribution: Not distributed to tissues.

Metabolism/Excretion: Unknown.

Half-Life: Unknown.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
Topical	unknown	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to wash hands thoroughly after application and to not cover the skin being treated with a bandage or wrap.
Advise patient to discontinue sirolimus and notify health care professional immediately for symptoms of hypersensitivity (rash, exfoliative dermatitis, angioedema), difficulty breathing, or serious infection.
Advise patient to minimize or avoid exposure to natural or artificial sunlight with protective clothing.
Inform patient to avoid live vaccines during therapy.
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.
Rep: May cause fetal harm. Women of reproductive potential should use effective contraception during and for 12 wk after last dose, and avoid breastfeeding. Notify health care professional if pregnancy is planned or suspected or if breastfeeding. May cause female and male infertility.

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Indications ⬇

Contraind./Precautions ⬆ ⬇