ambrisentan

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation;
Idiopathic pulmonary fibrosis;
Moderate or severe hepatic impairment;
Significant anemia.

Use Cautiously in:

Mild hepatic impairment;
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema(more common when used with tadalafil)

GU: ↓sperm count

Hemat: ↓hemoglobin

Neuro: headache

Resp: PULMONARY VENO-OCCLUSIVE DISEASE

Interactions ⬆ ⬇

Drug-drug:

Cyclosporine may ↑ levels and risk of toxicity; do not exceed ambrisentan dose of 5 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 10 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily, may ↑ to 10 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Antagonizes endogenous endothelin, resulting in vasodilation.

Therapeutic effects:

Improved exercise capacity and delayed clinical worsening; reduced hospitalizations (when used with tadalafil).

Classifications ⬆ ⬇

Therapeutic Classification: antihypertensives

Pharmacologic Classification: endothelin receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption following oral administration unknown.

Distribution: Unknown.

Protein Binding: 99%.

Metabolism/Excretion: Highly metabolized.

Half-Life: 15 hr (effective half-life 9 hr).

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take ambrisentan as directed, at the same time each day. Review medication guide and patient education brochures with every patient. Explain Ambrisentan REMS to patient. Take missed dose as soon as remembered that day. Take next dose at regular time; do not take two doses at the same time to make up for missed dose.
Advise patient to notify health care professional promptly if symptoms of fluid retention (swelling of hands, legs, ankles, feet or all over the body) or hepatotoxicity (anorexia, nausea, vomiting, fever, malaise, fatigue, right upper quadrant abdominal discomfort, jaundice, dark urine or itching) occur.
Rep: May cause fetal harm if taken during pregnancy. Inform patients a pregnancy test is required prior to beginning therapy and acceptable methods of contraception (one highly effective form of contraception: intrauterine devices [IUD], contraceptive implants, or tubal sterilization or a combination of methods: [hormone method with a barrier method or two barrier methods]) must be used throughout therapy and for 1 mo following discontinuation. If a partner’s vasectomy is method of contraception chosen, a hormone or barrier method must be used along with this method. Educate women with reproductive potential on the use of emergency contraception in the case of unprotected sex or contraceptive failure. Advise patient to avoid breastfeeding during therapy. Advise patient to notify health care professional if pregnancy is suspected.
Rep: Inform patients that ambrisentan may cause low sperm count.
Advise patient of the importance of regular liver and hemoglobin testing.

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Indications ⬇

Contraind./Precautions ⬆ ⬇