Ambrisentan

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

  1. anemia
  2. angioedema
  3. anorexia
  4. asthenia
  5. cough
  6. dizziness
  7. dyspepsia
  8. elevated hepatic enzymes
  9. fatigue
  10. fever
  11. fluid retention
  12. flushing
  13. headache
  14. hyperbilirubinemia
  15. hypotension
  16. jaundice
  17. malaise
  18. nasal congestion
  19. nausea
  20. oligospermia
  21. peripheral edema
  22. rash
  23. sinusitis
  24. teratogenesis
  25. testicular atrophy
  26. 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
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