Opsumit vs Tracleer For PAH – Differences & Side Effects

Opsumit

It is the brand name of a medication called macitentan, that belongs to the class of medications known as endothelin receptor antagonists.

Mechanism of Action

This medication lowers blood pressure in the lungs, helping the heart pump blood more efficiently.

Uses

It is used to treat pulmonary arterial hypertension, a rare, progressive disorder that is characterized by high blood pressure in the arteries of the lungs for no apparent reason.

In many cases of PAH, the cause is unknown. However, some causes include:

  • connective tissue/autoimmune disorders;
  • HIV infection;
  • drugs.

Pulmonary hypertension symptoms may include:

  • heart palpitations;
  • shortness of breath, initially while exercising and eventually while at rest;
  • bluish color of your lips and skin;
  • swelling in your ankles, legs and eventually in your abdomen;
  • chest pressure or pain;
  • dizziness or fainting spells;
  • fatigue.

Dosage

The usual recommended dose is 10 mg orally once per day.

Side Effects and Precautions

Common side effects may include:

  • headaches;
  • a sore throat;
  • sinus pain;
  • a stuffy nose.

Rare side effects may include:

  • jaundice (yellowing of the skin or eyes);
  • burning when you urinate;
  • fast or uneven heart rate;
  • rapid weight gain;
  • chest pain;
  • a cough with foamy mucus;
  • nausea;
  • gasping for breath;
  • severe shortness of breath;
  • pale skin;
  • clay-colored stools;
  • dark urine;
  • loss of appetite;
  • tired feeling;
  • upper stomach pain.

Contraindications

Before taking this medication, tell your healthcare provider if you have:

  • anemia (low red blood cells);
  • heart disease;
  • liver disease.

Alcoholalcohol

Avoid drinking alcoholic beverages while taking this endothelin receptor antagonist since alcohol use can substantially increase the risk of severe side effects.

Drug Interactionsdrugs pills

It may negatively interact with other medications, especially:

  • gabapentin;
  • Adcirca (tadalafil);
  • levothyroxine;
  • Adempas;
  • metformin;
  • victoza;
  • Aspir 81 (aspirin);
  • Revatio (sildenafil);
  • atorvastatin;
  • spironolactone;
  • digoxin;
  • Xanax (alprazolam);
  • furosemide;
  • Synthroid (levothyroxine);
  • Lasix (furosemide);
  • sildenafil;
  • losartan;
  • potassium chloride;
  • omeprazole;
  • lantus;
  • metolazone.

Pregnancy & Breastfeeding

This endothelin receptor antagonist can harm a developing fetus or cause birth defects. Do not use it if you are pregnant or think you may become pregnant.

It is not known exactly whether this endothelin receptor antagonist passes into human breast milk or if it could negatively affect a breastfed infant. You should not breast-feed while using this endothelin receptor antagonist.

Tracleer

It is the brand name of a drug called bosentan, that belongs to a group of drugs known as endothelin receptor antagonists.

Mechanism of Action

It helps blood vessels to relax, lowering blood pressure and allowing the heart to pump blood more efficiently.

Uses

This prescription medication is used to treat high blood pressure in the vessels of the lungs, known medically as pulmonary arterial hypertension.

Dosage

The usual recommended dose is 62.5 mg twice per day.

Side Effects and Precautions

Common side effects may include:

  • a sore throat;
  • headaches;
  • sneezing;
  • flushing (warmth or tingly feeling);
  • sinus pain;
  • stuffy nose;
  • fainting;
  • joint pain;
  • low blood pressure.

Rare side effects may include:

  • jaundice (yellowing of the skin or eyes);
  • swelling in your legs or ankles;
  • fast or uneven heart rate;
  • trouble concentrating;
  • chest pain;
  • a feeling like you might pass out;
  • a cough with foamy mucus;
  • gasping for breath;
  • severe shortness of breath;
  • clay-colored stools;
  • pale skin;
  • dark urine;
  • loss of appetite;
  • upper stomach pain.

Contraindications

Before taking this endothelin receptor antagonist, tell your healthcare provider:

  • if you have had a heart or kidney transplant;
  • if you have liver disease;
  • if you have an autoimmune disorder like psoriasis or rheumatoid arthritis;
  • if you have diabetes;
  • if you experience fluid retention.

Alcohol

Avoid drinking alcoholic beverages while taking this endothelin receptor antagonist since alcohol use can substantially increase the risk of severe side effects.

Drug Interactions

It may negatively interact with other medications, especially:

  • drugs to treat high cholesterol, such as – Lipitor, Crestor, Pravachol, Zocor;
  • hormonal forms of birth control, such as – injections, birth control pills, or implants;
  • HIV/AIDS medication that contains ritonavir;
  • antifungal medications, such as – itraconazole, fluconazole, ketoconazole, or voriconazole;
  • dotarem;
  • warfarin (Coumadin, Jantoven);
  • tacrolimus;
  • rifampin.

Pregnancy & Breastfeeding

It is not known exactly whether this endothelin receptor antagonist passes into human breast milk or if it could negatively affect a breastfed infant. You should not breast-feed while using this endothelin receptor antagonist.

This drug can harm a developing fetus or cause birth defects. Do not use it if you are pregnant or think you may become pregnant.

Bottom Line – Opsumit vs Tracleer

Opsumit (active ingredient – macitentan) is a medication that is used to treat pulmonary arterial hypertension. It works by improving your ability to exercise and prevents your condition from getting worse.

Tracleer (active ingredient – bosentan) is a medication that is used to treat pulmonary arterial hypertension (PAH). It works by lowering blood pressure in your lungs, helping your heart pump blood more efficiently.

According to a 2017 study, no measurable difference in clinical benefit was observed between these two endothelin receptor antagonists for treating pulmonary arterial hypertension.

Regarding their price, the average retail price for 30 tablets of Opsumit 10mg is $9,200, while the average retail price for 60 tablets of Tracleer 125mg is $12,100.

References

http://www.internationaljournalofcardiology.com/article/S0167-5273(16)34582-
http://www.nejm.org/doi/full/10.1056/NEJMoa1213917
http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines

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