What is Opsumit Macitentan? How to use, Side Effects, Dosage

What is Opsumit Macitentan? How to use, Side Effects, Dosage

What is Opsumit?

Opsumit (Macitentan) is used to treat high blood pressure in the lungs (pulmonary arterial hypertension). This condition is thought to be caused by increased levels of a certain natural substance (endothelin-1). This medication blocks the effects of endothelin-1, which helps decrease the blood pressure in the lungs, slow the worsening of symptoms from the disease, and improve your ability to exercise.

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How to use Opsumit?

Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start taking macitentan and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth with or without food as directed by your doctor, usually once daily. Swallow the tablet whole. Do not split, crush, or chew the tablet.

Use Opsumit (Macitentan) regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.

Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

Dosage of Opsumit

Pulmonary Arterial Hypertension

Indicated for the treatment of pulmonary arterial hypertension (WHO Group I) to delay disease progression

10 mg PO qDay

Dosage Modifications

Renal impairment

Severe (CrCl 15-29 mL/min): No dosage modification needed

Systemic Exposure to macitentan and its active metabolite were increased by 30% and 60% respectively (this increase ise not considered clinically relevant)

Hepatic impairment

Mild, moderate, or severe (Child-Pugh Class A, B, and C): No dosage modification needed

System exposure decreased by 21%, 34%, and 6% and exposure to the active metabolite was decreased by 20%, 25%, and 25% in subjects with mild, moderate, or severe hepatic impairment respectively (this decrease is not considered clinically relevant)

Orphan Designations

Fixed dose combination of macitentan and tadalafil for treatment of pulmonary arterial hypertension

Fontan-palliated patients

Chronic thromboembolic pulmonary hypertension (CTEPH)

Side Effects of Opsumit

Runny nose, sore throat, cough, headache, chills, or body aches may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: signs of low red bloodcell count (such as unusual tiredness, rapid breathing, pale skin, shortness of breath, fast heartbeat), unusual weight gain, new or worsening swelling of the hands/ankles/feet.

Macitentan may rarely cause serious liver disease. Tell your doctor right away if you have any symptoms of liver disease, including: dark urine, persistent nausea/vomiting/loss of appetite, stomach/abdominal pain, yellowing eyes/skin.

Macitentan may decrease sperm production, an effect that may lower male fertility. Consult your doctor for more details.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Opsumit Drug Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Other medications can affect the removal of macitentan from your body, which may affect how macitentan works. Examples include azole antifungals (such as ketoconazole), cobicistat, macrolide antibiotics (such as clarithromycin), HIV protease inhibitors (such as ritonavir), rifamycins (such as rifampin), among others.

Opsumit Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip themissed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Opsumit MacitentanPlease if you have any questions about Opsumit (Macitentan), you can ask us by commenting below this text, we'll answer you as soon as possible.

Opsumit Overdose

Macitentan has been administered as a single dose of up to 600 mg to healthy subjects. Adverse reactions of headache, nausea, and vomiting were observed. In the event of an overdose, standard supportive measures must be taken, as required.Due to the high degree of protein binding of macitentan, dialysis is unlikely to be effective.

Warnings of Opsumit

The benefit/risk balance of macitentan has not been established in patients with WHO class I functional status of pulmonary arterial hypertension.

Liver function:

Elevations of liver aminotransferases (AST, ALT) have been associated with PAH and with endothelin receptor antagonists (ERAs). Opsumit is not to be initiated in patients with severe hepatic impairment or elevated aminotransferases (> 3 × ULN) (see sections 4.2 and 4.3), and is not recommended in patients with moderate hepatic impairment. Liver enzyme tests should be obtained prior to initiation of Opsumit.

Patients should be monitored for signs of hepatic injury and monthly monitoring of ALT and AST is recommended. If sustained, unexplained, clinically relevant aminotransferase elevations occur, or if elevations are accompanied by an increase in bilirubin > 2 × ULN, or by clinical symptoms of liver injury (e.g., jaundice), Opsumit treatment should be discontinued.

Reinitiation of Opsumit may be considered following the return of hepatic enzyme levels to within the normal range in patients who have not experienced clinical symptoms of liver injury. The advice of a hepatologist is recommended.4

Haemoglobin concentration:

Decrease in haemoglobin concentrations has been associated with endothelin receptor antagonists (ERAs) including macitentan (see section 4.8). In placebo-controlled studies, macitentan-related decreases in haemoglobin concentration were not progressive, stabilised after the first 4–12 weeks of treatment and remained stable during chronic treatment. Cases of anaemia requiring blood cell transfusion have been reported with macitentan and other ERAs. Initiation of Opsumit is not recommended in patients with severe anaemia. It is recommended that haemoglobin concentrations be measured prior to initiation of treatment and tests repeated during treatment as clinically indicated.

Pulmonary veno-occlusive disease:

Cases of pulmonary oedema have been reported with vasodilators (mainly prostacyclins) when used in patients with pulmonary veno-occlusive disease. Consequently, if signs of pulmonary oedema occur when macitentan is administered in patients with PAH, the possibility of pulmonary veno-occlusive disease should be considered.

Use Opsumit in women of childbearing potential:

Opsumit treatment should only be initiated in women of childbearing potential when the absence of pregnancy has been verified, appropriate advice on contraception provided, and reliable contraception is practised (see sections 4.3 and 4.6). Women should not become pregnant for 1 month after discontinuation of Opsumit. Monthly pregnancy tests during treatment with Opsumit are recommended to allow the early detection of pregnancy.

Concomitant use with strong CYP3A4 inducers:

In the presence of strong CYP3A4 inducers reduced efficacy of macitentan could occur. The combination of macitentan with strong CYP3A4 inducers (e.g., rifampicin, St. John’s wort, carbamazepine, and phenytoin) should be avoided.

Concomitant use with strong CYP3A4 inhibitors:

Caution should be exercised when macitentan is administered concomitantly with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, voriconazole, clarithromycin, telithromycin, nefazodone, ritonavir, and saquinavir).

Renal impairment:

Patients with renal impairment may run a higher risk of experiencing hypotension and anaemia during treatment with macitentan. Therefore,monitoring of blood pressure and haemoglobin should be considered. There is no clinical experience with the use of macitentan in PAH patients with severe renal impairment. Caution is recommended in this population. There is no experience with the use of macitentan in patients undergoing dialysis, therefore Opsumit is not recommended in this population (

Elderly:

There is limited clinical experience with macitentan in patients over the age of 75 years, therefore Opsumit should be used with caution in this population.

Excipients:

Opsumit contains lactose. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.5

Opsumit contains soya bean lecithin. If a patient is hypersensitive to soya, Opsumit must not be used.

Storage of Opsumit

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed.

Opsumit MacitentanPlease if you have any questions about Opsumit (Macitentan), you can ask us by commenting below this text, we'll answer you as soon as possible.

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