Macitentanum

Macitentanum Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Macitentanum is a brand name. Its generic name is Macitentan.

Macitentanum Introduction

Macitentanum (Opsumit) is an orally administered, selective endothelin receptor antagonist (ERA) developed and marketed by Actelion on behalf of the Japanese pharmaceutical company Takeda. It is used in the treatment of pulmonary arterial hypertension (PAH). Macitentanum is a dual inhibitor of endothelin-1 (ET-1) and endothelin-2 (ET-2) receptors, acting on the ETAR to decrease the production and action of ET-1, and on the ETBR to reduce the effect of ET-2. The drug has also been investigated for its potential use in other diseases in which the endothelin system is believed to be involved in pathogenesis, such as congestive heart failure, atherosclerosis, and pre-eclampsia.

Macitentanum Uses

Macitentanum is indicated for the treatment of pulmonary arterial hypertension (PAH). This includes individuals with WHO Functional Class II-IV symptoms of PAH. Additionally, Macitentanum (Opsumit) has been investigated for its potential use in other diseases in which the endothelin system is believed to be involved in pathogenesis, such as congestive heart failure, atherosclerosis, and pre-eclampsia.

Macitentanum Mechanism of Action

Macitentanum functions as a dual inhibitor of the endothelin-1 (ET-1) and endothelin-2 (ET-2) receptors, acting on the ETAR to decrease the production and action of ET-1, and on the ETBR to reduce the effect of ET-2. The drug also reduces the expression of pro-fibrotic genes, leading to an attenuation of fibrosis in pulmonary arterial endothelium. Macitentanume also increases the interactions between pulmonary arterial endothelial cells and smooth muscle cells, leading to an important contribution to the maintenance of the wall of the pulmonary arterial vessels.

How Long does it Take for Macitentanum to Work?

The onset of action varies depending on individual patient characteristics. Generally, Macitentanum is expected to start working within 1-4 weeks; however, some patients may notice an effect as early as 1 week.

Macitentanum Absorption

Macitentanum is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations achieved after 1-2 hours, with a bioavailability of approximately 100%. The drug is highly bound to plasma proteins (approximately 98%).

Macitentanum Route of Elimination

The primary route of elimination of Macitentanum is through metabolism via CYP2C9 and, to a lesser extent, CYP2C8 and CYP2C19. After metabolism, the drug is mainly eliminated via renal excretion in bile acids and feces.

Macitentanum Dosage

The recommended dose of Macitentanum is 10 mg once daily. It can be taken with or without food. Unless there is an intolerance or contraindication, Macitentanum should be taken at the same time each day.

Macitentanum Administration

Macitentanum is administered orally, through tablets. It should be taken with a full glass of water. Patients should not chew, divide, or crush the tablets.

Macitentanum Side Effects

The most commonly reported side effects of Macitentanum include headache, diarrhea, nasopharyngitis, back pain, and an increase in liver enzymes. Other rarer but more serious side effects may include anemia, serious skin reactions, and liver damage.

Macitentanum Toxicity

There is a potential for serious toxicity if Macitentanum is taken in overdose. Symptoms of toxicity include headache, dizziness, nausea, vomiting, diarrhea, abdominal pain, and hypotension. Treatment of overdose includes symptomatic and supportive care as needed.

Macitentanum Precaution

Patients should be monitored closely for liver function, blood pressure, and symptoms of toxicity. Macitentanum should not be used in combination with other endothelin receptor antagonists or in patients with known hypersensitivity to the drug.

Macitentanum Interaction

Macitentanum may interact with strong CYP2C8 and CYP2C9 inducers or inhibitors, as well as drugs that are known to prolong the QT interval. Macitentanum should be used with caution in patients taking other drugs that may have similar effects.

Macitentanum Disease Interactions

Macitentanum is contraindicated in patients with severe hepatic impairment. Use with caution in patients with mild-to-moderate hepatic impairment and in those with a history of hepatic impairment. Use should be avoided in patients with moderate-to-severe renal impairment.

Macitentanum Drug Interactions

Macitentanum Food Interactions

Macitentanum should not be taken with food that is high in fat as this may decrease the absorption of Macitentanum. Grapefruit juice should be avoided as this may increase the amount of Macitentanum that is absorbed in the body.

Macitentanum Pregnancy Use

Macitentanum is not recommended for use in pregnant women. There is no data on the use of Macitentanum in pregnant animals. Animal studies have shown reproductive toxicity.

Macitentanum Lactation Use

Neither Macitentanum nor any of its metabolites have been detected in human milk. However, a clinical decision should be made about whether to discontinue breastfeeding based on the importance of the drug to the mother.

Macitentanum Acute Overdose

In the event of an acute overdose of Macitentanum, the patient should be monitored for signs and symptoms of toxicity and supportive care should be given as needed.

Macitentanum Contraindication

Macitentanum is contraindicated in patients with severe hepatic impairment and in those with known hypersensitivity to the drug. It should also be used with caution in patients with mild-to-moderate hepatic impairment and in those taking other drugs that may have similar effects.

Macitentanum Use Direction

Macitentanum Storage Condition

Macitentanum should be stored at room temperature away from light and moisture. Do not store it in the bathroom. Keep the container tightly closed when not in use.

Macitentanum Volume of Distribution

The volume of distribution of Macitentanum is 4.6 L/kg.

Macitentanum Half-Life

The half-life of Macitentanum is approximately 7.2 hours.

Macitentanum Clearance

The clearance of Macitentanum is 1.3 L/h/kg.

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