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Drug overview for AMBRISENTAN (ambrisentan):
Generic name: AMBRISENTAN (AM-bri-SEN-tan)
Drug class: PAH Agents- Endothelin Receptor Antagonists
Therapeutic class: Cardiovascular Therapy Agents
Ambrisentan, a selective propionic-acid endothelin-1 (ET-1) type A receptor antagonist, is a vasodilator.
No enhanced Uses information available for this drug.
Generic name: AMBRISENTAN (AM-bri-SEN-tan)
Drug class: PAH Agents- Endothelin Receptor Antagonists
Therapeutic class: Cardiovascular Therapy Agents
Ambrisentan, a selective propionic-acid endothelin-1 (ET-1) type A receptor antagonist, is a vasodilator.
No enhanced Uses information available for this drug.
DRUG IMAGES
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The following indications for AMBRISENTAN (ambrisentan) have been approved by the FDA:
Indications:
Pulmonary arterial hypertension
Professional Synonyms:
Hypertensive pulmonary arterial disease
Pulmonary hypertensive arterial disease
Indications:
Pulmonary arterial hypertension
Professional Synonyms:
Hypertensive pulmonary arterial disease
Pulmonary hypertensive arterial disease
The following dosing information is available for AMBRISENTAN (ambrisentan):
No enhanced Dosing information available for this drug.
No enhanced Administration information available for this drug.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| AMBRISENTAN 5 MG TABLET | Maintenance | Adults take 1 tablet (5 mg) by oral route once daily |
| AMBRISENTAN 10 MG TABLET | Maintenance | Adults take 1 tablet (10 mg) by oral route once daily |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| AMBRISENTAN 5 MG TABLET | Maintenance | Adults take 1 tablet (5 mg) by oral route once daily |
| AMBRISENTAN 10 MG TABLET | Maintenance | Adults take 1 tablet (10 mg) by oral route once daily |
The following drug interaction information is available for AMBRISENTAN (ambrisentan):
There are 2 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Ambrisentan (Greater Than 5 mg)/Cyclosporine SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Cyclosporine may inhibit the metabolism/transport of ambrisentan by CYP3A4, OATP, and P-gp.(1,2) CLINICAL EFFECTS: Concurrent use of cyclosporine may result in elevated levels of and toxicity from ambrisentan.(1,2) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients maintained on cyclosporine should receive a maximum daily dose of 5 mg of ambrisentan.(1,2) DISCUSSION: In an open-label, parallel-treatment study, 28 healthy subjects had ambrisentan (5 mg daily) added to steady-state cyclosporine (100-150 mg BID) and 24 subjects had cyclosporine (100-150 mg BID) added to steady-state ambrisentan (5 mg daily). All drug levels were evaluated at steady-state. Ambrisentan maximum concentration (Cmax) and area-under-curve (AUC) increased 1.5-fold and 2-fold, respectively, in the presence of cyclosporine. There were no significant effects on cyclosporine levels. The addition of ambrisentan to cyclosporine was less tolerable than the addition of cyclosporine to ambrisentan therapy.(1,2) |
CYCLOSPORINE, CYCLOSPORINE MODIFIED, GENGRAF, NEORAL, SANDIMMUNE |
| Sparsentan/Angiotensin II Receptor Blockers; Endothelin Receptor Antagonists; Aliskiren SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Sparsentan is an antagonist of the endothelin type A receptor and the angiotensin II type 1 receptor which are thought to contribute to the pathogenesis of IgA nephropathy.(1) Coadministration with angiotensin II receptor blockers (ARBs), endothelin receptor antagonists (ERAs), or aliskiren may result in additive inhibition of angiotensin. CLINICAL EFFECTS: Concurrent use of sparsentan with ARBs, ERAs, or aliskiren may result in hypotension, syncope, hyperkalemia, and changes in renal function (including renal failure).(1) PREDISPOSING FACTORS: Patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, or volume depletion may be at risk of developing acute kidney injury on sparsentan.(1) Patients with advanced kidney disease or taking concomitant potassium-increasing drugs (e.g., potassium supplements, potassium-sparing diuretics), or using potassium-containing salt substitutes are at increased risk for developing hyperkalemia.(1) PATIENT MANAGEMENT: Do not coadminister sparsentan with ARBs, ERAs, or aliskiren. Prior to initiating treatment with sparsentan, discontinue use of ARBs, ERAs, and aliskiren.(1) DISCUSSION: The US manufacturer of sparsentan states that concomitant use of sparsentan with ARBs, ERAs, or aliskiren is contraindicated.(1) |
FILSPARI |
There are 0 severe interactions.
There are 1 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Ambrisentan (Less than or Equal To 5 mg)/Cyclosporine SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Cyclosporine may inhibit the metabolism/transport of ambrisentan by CYP3A4, OATP, and P-gp.(1,2) CLINICAL EFFECTS: Concurrent use of cyclosporine may result in elevated levels of and toxicity from ambrisentan.(1,2) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients maintained on cyclosporine should receive a maximum daily dose of 5 mg of ambrisentan.(1,2) DISCUSSION: In an open-label, parallel-treatment study, 28 healthy subjects had ambrisentan (5 mg daily) added to steady-state cyclosporine (100-150 mg BID) and 24 subjects had cyclosporine (100-150 mg BID) added to steady-state ambrisentan (5 mg daily). All drug levels were evaluated at steady-state. Ambrisentan maximum concentration (Cmax) and area-under-curve (AUC) increased 1.5-fold and 2-fold, respectively, in the presence of cyclosporine. There were no significant effects on cyclosporine levels. The addition of ambrisentan to cyclosporine was less tolerable than the addition of cyclosporine to ambrisentan therapy.(1,2) |
CYCLOSPORINE, CYCLOSPORINE MODIFIED, GENGRAF, NEORAL, SANDIMMUNE |
The following contraindication information is available for AMBRISENTAN (ambrisentan):
Drug contraindication overview.
*Pregnancy. *Idiopathic pulmonary fibrosis, with or without pulmonary hypertension (WHO group 3).
*Pregnancy. *Idiopathic pulmonary fibrosis, with or without pulmonary hypertension (WHO group 3).
There are 3 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Lactation |
| Pregnancy |
| Pulmonary fibrosis |
There are 0 severe contraindications.
There are 4 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Anemia |
| Chronic heart failure |
| Disease of liver |
| Edema |
The following adverse reaction information is available for AMBRISENTAN (ambrisentan):
Adverse reaction overview.
The most common adverse effects (>3%) of ambrisentan in clinical studies were peripheral edema, nasal congestion, sinusitis, and flushing. When used in combination with tadalafil, the most common adverse effects (>5% compared to either monotherapy) were peripheral edema, headache, nasal congestion, cough, anemia, dyspepsia, and bronchitis.
The most common adverse effects (>3%) of ambrisentan in clinical studies were peripheral edema, nasal congestion, sinusitis, and flushing. When used in combination with tadalafil, the most common adverse effects (>5% compared to either monotherapy) were peripheral edema, headache, nasal congestion, cough, anemia, dyspepsia, and bronchitis.
There are 8 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Anemia Peripheral edema |
None. |
| Rare/Very Rare |
|---|
|
Abnormal hepatic function tests Angioedema Body fluid retention Heart failure Hyperbilirubinemia Pulmonary edema |
There are 10 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Flushing Nasal congestion Oligospermia Sinusitis |
None. |
| Rare/Very Rare |
|---|
|
Dizziness Fatigue General weakness Nausea Skin rash Vomiting |
The following precautions are available for AMBRISENTAN (ambrisentan):
Safety and efficacy of ambrisentan have not been established in children and adolescents younger than 18 years of age. Juvenile animal data revealed a reduction in brain weight, but no morphologic or neurobehavioral changes following drug exposures 1.8 to 7 times the human pediatric exposures at 10 mg (based on AUC).
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Ambrisentan may cause fetal harm. Exclude pregnancy prior to starting ambrisentan and perform monthly pregnancy tests during treatment and for 1 month after stopping treatment. (See Females and Males of Reproductive Potential under Cautions.)
It is not known whether ambrisentan is distributed into human milk. Because many drugs are distributed into human milk and because of the potential for serious adverse reactions to ambrisentan in nursing infants, a decision should be made to discontinue nursing or the drug.
A higher incidence of peripheral edema has been observed in geriatric patients 65 years of age or older relative to younger adults. Clinical trials of ambrisentan included 21% of patients >=65 years of age and 5% of patients >=75 years of age. Improvement in walk distance was less in elderly compared to younger patients, although the prescribing information states to interpret this information, which comes from subgroup analysis, with caution.
The following prioritized warning is available for AMBRISENTAN (ambrisentan):
WARNING: This medication must not be used during pregnancy. It may harm an unborn baby. It is important to prevent pregnancy while taking this medication and for 1 month after treatment.
Female patients must use reliable birth control before starting treatment, during treatment, and for 1 month after the last dose. Ask your doctor which forms of birth control to use while taking this medication. Female patients must take a pregnancy test before starting treatment. If you become pregnant or think you may be pregnant, tell your doctor right away.
WARNING: This medication must not be used during pregnancy. It may harm an unborn baby. It is important to prevent pregnancy while taking this medication and for 1 month after treatment.
Female patients must use reliable birth control before starting treatment, during treatment, and for 1 month after the last dose. Ask your doctor which forms of birth control to use while taking this medication. Female patients must take a pregnancy test before starting treatment. If you become pregnant or think you may be pregnant, tell your doctor right away.
The following icd codes are available for AMBRISENTAN (ambrisentan)'s list of indications:
| Pulmonary arterial hypertension | |
| I27.0 | Primary pulmonary hypertension |
| I27.21 | Secondary pulmonary arterial hypertension |
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