Emend

Aprepitant (Aprepitant) instructions

Common name: Aprepitant

Trade name: Emend

Full names: Aprepitant, Aprepitant capsules, Yimei, Apr epitant, Emend

Indications:

Aprepitant capsules are administered in combination with other antiemetic drugs and are suitable for the prevention of acute and delayed nausea and vomiting during initial and repeated treatment with highly emetogenic anti-tumor chemotherapy.

Dosage:

EMEND is administered as a three-day intervention and includes a course of treatment with a corticosteroid and a 5-HT3 antagonist.

The recommended dose of EMEND is 125 mg taken orally one hour before chemotherapy on the first day, and 80 mg once daily in the morning on the second and third days.

Adverse reactions:

The most common drug-related adverse reactions include: hiccups (4.6%), weakness/tiredness (2.9%), increased liver index ALT (2.8%), constipation (2.2%), headache (2.2%) and anorexia ( 2.0%).

Other adverse reactions include: redness, upper respiratory tract infection, tachycardia, weakness, pelvic pain, bone pain, pelvic pain, rash, hypokalemia, anxiety, etc. Bradycardia, disorientation, perforated duodenal ulcer, and Stevens-Johnson syndrome have also been reported.

Contraindications:

Contraindicated for use by those allergic to any ingredients in this product.

This product should not be used simultaneously with pimozide, terfenadine, astemizole, and cisapride. Aprepitant can produce a dose-dependent inhibition of cytochrome P450 isoenzyme 3A4 (CYP3A4), which increases the plasma concentration of these drugs, which may cause serious or life-threatening adverse reactions.

Notes:

Corrections must be made when treating patients with EMEND and drugs that are primarily metabolized by the CYP3A4 enzyme; some chemotherapy drugs are metabolized by the CYP3A4 enzyme. The inhibitory effect of Aprepitant on CYP3A4 will lead to increased blood concentrations of these concomitant drugs.

When EMEND is used together with warfarin, it will lead to shortening of the prothrombin time (prothrombin time), as measured by the International Normalized Ratio (International Normalized Ratio, INR) expressed. For patients receiving warfarin treatment for a long time, the prothrombin tim should be strictly monitored after each three-day course of EMEND treatment. INR) to connect and maintain the desired warfarin dose.

Long-term use of EMEND may reduce the effectiveness of oral contraceptives. Although the effects of a three-day regimen of EMEND on oral contraceptives have not been studied, an alternative or complementary method of contraception should be used during use of EMEND.

During pregnancy, EMEND should be used only when the potential benefits outweigh the possible risks to the mother and woman.

EMEND may induce adverse reactions in infants who drink breast milk, so the nature of this drug to the mother must be considered and a choice should be made between stopping breastfeeding or discontinuing medication.

Storage:

General medicines should be placed in a dry place at 15 to 25 degrees Celsius, and refrigerated medicines should be placed in a refrigerator at 2 to 8 degrees Celsius (do not freeze); if they deteriorate or expire, they should not be eaten again.

Mechanism of action:

Aprepitant has a unique mode of action. It is a selective and high-affinity antagonist to the receptor of human substance P Neurokinin1 (NK1).

Preclinical studies have shown that aprepitant can penetrate into the brain and bind to the NK1 receptor in the brain. Preclinical studies have shown that aprepitant has a long-lasting effect on the central system and can inhibit and enhance the acute and delayed vomiting caused by cisplatin. The antiemetic 5-HT3-receptor antagonist ondansetron and the leather steroid dexamethasone inhibit the vomiting caused by cisplatin.

Safety and efficacy:

With in-depth research on substance P and NK1 receptors, aprepitant, the first NK1 receptor blocker approved for clinical use in 2003, provides a powerful weapon for the prevention and treatment of CINV. Aprepitant has a brand-new pharmacological mechanism of action, is selective and has high affinity for NK1 receptors, and can maintain long-term central activity. It has significantly improved the CR rate of acute and delayed CINV, and has especially made new breakthroughs in the control of delayed CINV. The results of multiple studies have confirmed that the antiemetic regimen of aprepitant combined with the 5-HT3 receptor antagonist + dexamethasone regimen is more effective in preventing acute or delayed vomiting caused by chemotherapy regimens with moderate or high emetogenic risks, without significantly increasing toxic effects.

Two randomized controlled clinical studies in 2003 compared standard antiemetic regimen (ondansetron + dexamethasone) ± aprepitant to patients receiving highly emetogenic chemotherapy drugs (HEC, cisplatin ≥70 mg/m2) to prevent CINV in patients. The results showed that the combined aprepitant group had significantly better CR (68% vs. 48%, P<0.001) and no vomiting rate (72% vs. 50%, P<0.01) for acute and delayed CINV caused by HEC than the standard antiemetic group. In 2011, Chinese scholars conducted a high-dose cisplatin (≥70 mg/m2) study also obtained similar results. The CR (69% vs. 57%, P=0.007) and vomiting-free rate (71% vs. 57%, P=0.003) of CINV of aprepitant + standard antiemetic regimen (granisetron + dexamethasone) were significantly higher than those of the standard antiemetic group (Figure 1). In women with breast cancer treated with AC regimen, aprepitant combined with standard antiemetic regimen also showed better CR (P=0.015) and vomiting-free rate (P<0.001) in preventing CINV.

Based on clinical research results, in the 2011 MASCC updated CINV prevention guidelines, aprepitant was recommended as one of various antiemetic regimens.