aprocitentan

Contraindicated in:

Hypersensitivity;
New York Heart Association class III–IV HF;
Unstable cardiac disease;
NT-pro-BNP ≥500 pg/mL;
Severe anemia;
End-stage renal disease or hemodialysis;
Moderate to severe hepatic impairment or AST/ALT >3 times upper limit of normal;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Chronic kidney disease (↑ risk of edema);
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be at ↑ risk of edema.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema

GI: ↑liver enzymes

GU: ↓fertility (men)

Hemat: anemia

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Tablets: 12.5 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 12.5 mg once daily

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as an endothelin receptor antagonist, inhibiting the binding of endothelin-1 to endothelin A and B receptors.

Therapeutic effects:

Reduction in BP.

Classifications ⬆ ⬇

Therapeutic Classification: antihypertensives

Pharmacologic Classification: endothelin receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption unknown.

Distribution: Well distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized by the liver via UGT1A1 and UGT2B7. 52% excreted in urine (<1% as unchanged drug); 25% excreted in feces (7% as unchanged drug).

Half-Life: 41 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4–5 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy. Advise to take as directed. If a dose is missed, skip the missed dose and take the next dose at the regular time. Do not take two doses on the same day.
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 with symptoms of hepatotoxicity (nausea, vomiting, right upper quadrant pain, fatigue, anorexia, jaundice, dark urine, fever, itching) to immediately stop treatment and notify health care professional.
Educate patient on signs of fluid retention and to weigh themselves daily. Advise patient to contact health care professional if ↑ weight or swelling of the ankles or legs.
Educate patient on how to properly measure BP, symptoms of hypotension (dizziness, fainting) and hypertension (headache, visual disturbances).
Rep: May cause fetal harm. Advise women who can become pregnant to avoid pregnancy and use acceptable contraception before starting treatment, monthly during treatment, and for 1 mo after last dose. Acceptable forms of contraception include an IUD, contraceptive implant, tubal sterilization, a combination of a hormone method plus a barrier method, or two barrier methods. When a hormone method is chosen, a barrier method must also be used. If the patient's partner has had a vasectomy, a hormone or barrier method must also be used. Health care providers should counsel patients on use of emergency contraception. May impair fertility in men. Health care providers should enroll any patient exposed to aprocitentan during pregnancy in the Pregnancy Safety Study by calling 1-866-429-8964.

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Indications ⬇

Contraind./Precautions ⬆ ⬇