Ambrisentan Brand Name– LETAIRIS
What is Ambrisentan
Ambrisentan is an oral cardiovascular agent that belongs to a class of compounds known as endothelin-receptor antagonists and is indicated as monotherapy or in combination with tadalafil for the treatment of pulmonary arterial hypertension (PAH) (WHO Group I).
Unlike bosentan, which is a competitive antagonist for both type A and B endothelin-1 (ET-1) receptors, ambrisentan is a highly selective and potent endothelin-A receptor antagonist.
Endothelin-A receptor selectivity is believed to offer advantages by blocking the deleterious vasoconstrictive effects of endothelin-A on pulmonary vasculature while maintaining the vasodilator and ET-1 clearance functions of endothelin-B. In two randomized, double-blind, 12-week, placebo-controlled phase 3 studies (ARIES-1 and ARIES-2), treatment with ambrisentan resulted in a significant improvement in 6-minute walking distances (6MWD) and a significant delay in time to clinical worsening.
Ambrisentan is contraindicated in pregnancy and, due to the teratogenic potential, all prescribers, pharmacies, and female patients must enroll in the Ambrisentan REMs program.
Pregnancy testing is required in women of reproductive potential before initiating treatment and routinely during therapy.
Indications
- pulmonary hypertension
For improvement in exercise ability and delay in clinical worsening in patients with WHO Group I pulmonary hypertension (PAH)
Side Effects
- anemia
- angioedema
- anorexia
- asthenia
- cough
- dizziness
- dyspepsia
- elevated hepatic enzymes
- fatigue
- fever
- fluid retention
- flushing
- headache
- hyperbilirubinemia
- hypotension
- jaundice
- malaise
- nasal congestion
- nausea
- oligospermia
- peripheral edema
- rash
- sinusitis
- teratogenesis
- testicular atrophy
- vomiting
Monitoring Parameters
- hemoglobin/hematocrit
- LFTs
- pregnancy testing
Contraindications
- anemia
- breast-feeding
- contraception requirements
- geriatric
- hepatic disease
- hepatitis
- infertility
- peripheral edema
- pregnancy
- pregnancy testing
- pulmonary edema
- pulmonary fibrosis
- reproductive risk
- veno-occlusive disease (VOD)
Interactions
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
- Acetaminophen; Dextromethorphan; Phenylephrine
- Acetaminophen; Dichloralphenazone; Isometheptene
- Acetaminophen; Guaifenesin; Phenylephrine
- Alfuzosin
- Amiloride
- Amiloride; Hydrochlorothiazide, HCTZ
- Amphetamine
- Amphetamine; Dextroamphetamine
- Amphetamine; Dextroamphetamine Salts
- Articaine; Epinephrine
- Asenapine
- Benzphetamine
- Bosentan
- Brompheniramine; Carbetapentane; Phenylephrine
- Carbetapentane; Chlorpheniramine; Phenylephrine
- Carbetapentane; Diphenhydramine; Phenylephrine
- Carbetapentane; Guaifenesin; Phenylephrine
- Carbetapentane; Phenylephrine
- Carbetapentane; Phenylephrine; Pyrilamine
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Phenylephrine
- Cariprazine
- Chlophedianol; Guaifenesin; Phenylephrine
- Chlorpheniramine; Dextromethorphan; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Phenylephrine
- Co-Enzyme Q10, Ubiquinone
- Codeine; Phenylephrine; Promethazine
- Cyclosporine
- Dexmethylphenidate
- Dextroamphetamine
- Dextromethorphan; Diphenhydramine; Phenylephrine
- Dextromethorphan; Guaifenesin; Phenylephrine
- Diazoxide
- Diethylpropion
- Diphenhydramine; Hydrocodone; Phenylephrine
- Diphenhydramine; Phenylephrine
- Dobutamine
- Dopamine
- Duloxetine
- Dutasteride; Tamsulosin
- Enflurane
- Ephedrine
- Epinephrine
- Eplerenone
- Epoprostenol
- Etomidate
- Fospropofol
- General anesthetics
- Guaifenesin; Phenylephrine
- Halothane
- Hydrochlorothiazide, HCTZ; Spironolactone
- Hydrochlorothiazide, HCTZ; Triamterene
- Hydrocodone; Phenylephrine
- Iloperidone
- Iloprost
- Isocarboxazid
- Isoflurane
- Isoproterenol
- Ketamine
- Lisdexamfetamine
- Lurasidone
- Mepivacaine
- Mepivacaine; Levonordefrin
- Methamphetamine
- Methylphenidate
- Midodrine
- Minoxidil
- Monoamine oxidase inhibitors
- Nitroprusside
- Norepinephrine
- Oxymetazoline
- Pentoxifylline
- Phendimetrazine
- Phenelzine
- Phenoxybenzamine
- Phentermine
- Phentermine; Topiramate
- Phentolamine
- Phenylephrine
- Phenylephrine; Promethazine
- Potassium-sparing diuretics
- Prazosin
- Prilocaine; Epinephrine
- Propofol
- Rasagiline
- Ritodrine
- Selegiline
- Sevoflurane
- Sildenafil
- Silodosin
- Sotalol
- Spironolactone
- Tamsulosin
- Testosterone
- Tizanidine
- Tranylcypromine
- Triamterene
