Aprecap (Aprepitant) 1x125mg 2 x80mg 3 Capsules/Pack

Aprecap general information

What is Aprecap used for?

Aprecap capsules are used to prevent nausea and vomiting associated with cancer chemotherapy and are used as combination therapy with other mediations for both highly and moderately emetogenic (vomiting inducing) chemotherapy.  Chemotherapy is the use of cytotoxic drugs to kill cancer cells, which grow more rapidly than most normal cells, and nausea and vomiting are common side effects of chemotherapy.  Drugs used for chemotherapy stimulate the vomiting reflex that is triggered in the brain.  Aprecap capsules block the vomiting reflex and prevent nausea and vomiting induced by these drugs.

How does Aprecap work?

Aprecap capsules contain aprepitant, a selective high-affinity antagonist of the substance P neurokinin 1 (NK₁) receptor.  Substance P belongs to a group of neurokinins (NKs), which are small neurotransmitters, or chemical messengers that transmit signals to and from the neurones (brain cells), and it has an important role triggering emesis (vomiting).  The vomiting reflex is triggered by stimulation of vomiting centre in the brain, which is a complex area of neuronal networks, by one of several afferent nerve pathways (nerve signals carried to the brain).  This can activate vomiting via one of several neurotransmitter receptors.  The chemoreceptor trigger zone (CTZ) is one of these afferent nerve pathways and is located in the area postrema of the brain, which is not protected by the blood-brain barrier and therefore, is readily accessible to circulating toxins and drugs.  The vomiting centre contains high concentrations of substance P and its receptor neurokinin 1 (NK₁), in addition to other receptors for neurotransmitters like serotonin (5HT) and dopamine.  Substance P is released by nerve cells in response to stressful stimuli such as toxins and the biological effects of substance P, including emesis, are triggered by the binding of substance P to its NK1 receptor.  Aprepitant in Aprecap capsules competitively binds to NK1 receptors, which blocks the binding of substance P to its receptor and this prevents signal transduction that induces the vomiting reflex.  Chemotherapy can also cause the release of serotonin (5HT) from the cells of the small intestine, which stimulates 5HT3 receptors that are found on the vagal nerves in the intestines, sending signals to the vomiting centre in the brain, and this is another afferent pathway that induces the vomiting reflex.  Standard therapy for preventing nausea and vomiting following chemotherapy includes a serotonin receptor antagonist, as well as an anti-inflammatory corticosteroid.  Aprepitant in Aprecap capsules combined with standard therapy augments the antiemetic effects to improve protection against emetogenic chemotherapy^{1, 2}.  

What does Aprecap contain?

Aprecap capsules contain the active ingredient aprepitant, an NK1 receptor antagonist used to prevent nausea and vomiting induced by chemotherapy.  Each pack contains three capsules for a 3-day dosing regimen: 1 x 125mg and 2 x 80mg. 

Aprecap for preventing chemotherapy induced nausea and vomiting

Aprecap capsules contain aprepitant, an NK1 receptor antagonist used to prevent nausea and vomiting induced by cancer chemotherapy, which is the use of cytotoxic drugs to kill cancer cells.  These emetogenic (vomiting inducing) chemotherapy drugs induce the vomiting reflex by stimulation of the vomiting centre in the brain, which is a complex area of neuronal networks.  This works via the chemoreceptor trigger zone (CTZ), which is located in the area postrema of the brain and is readily accessible to circulating toxins and drugs, as this part of the brain is not protected by the blood-brain barrier.  Substance P is a neurotransmitter belonging to a group of neurokinins (NKs) (small neurotransmitters that transmit signals to and from brain cells), and has an important role in triggering emesis (vomiting).  Substance P is released by nerve cells in response to stressful stimuli such as toxins and when Substance P binds to its NK1 receptor in the vomiting centre of the brain, this triggers emesis (vomiting).  Aprepitant in Aprecap capsules competitively binds to NK1 receptors, which blocks the binding of substance P to its receptor and this prevents signal transduction that induces the vomiting reflex, preventing chemotherapy induced nausea and vomiting. 

What are the side effects of Aprecap?

The most commonly reported side effects when taking Aprecap include, constipation, dyspepsia (heartburn), decreased appetite, hiccups, headache, asthenia (weakness), fatigue.

When should Aprecap not be used?

You should not use Aprecap capsules if you:

• are allergic to aprepitant or any ingredients in Aprecap
• are pregnant or are breastfeeding
• have liver disease
• are taking medicines that interact with Aprecap, including the anticoagulant warfarin, the antipsychotic pimozide, the antihistamines terfenadine and astemizole, cisapride for reflux, hormonal contraceptives, the sedative midazolam, tolbutamide for diabetes, the antifungal ketoconazole, the antibiotic rifampicin, the antidepressant paroxetine, diltiazem for high blood pressure St John's Wort,

What medications interact with Aprecap?

Several medications interact with Aprecap capsules and should either not be taken while you are taking Aprecap or only after discussion and instruction from your doctor:

• Drugs that cause a serious reaction with Aprecap: the antipsychotic pimozide, the antihistamines terfenadine and astemizole, cisapride for reflux,
• Drugs that affect Aprecap: the antifungal ketoconazole, the antibiotic rifampicin, the antidepressant paroxetine, diltiazem for high blood pressure, St John's Wort
• Drugs that are affected by Aprecap:  the anticoagulant warfarin, hormonal contraceptives, the sedative midazolam, tolbutamide for diabetes, the antidepressant paroxetine, diltiazem for high blood pressure

How should Aprecap be taken?

You should take your Aprecap capsules swallowed whole, with a glass of water, with or without food, as part of a 3-day regimen that includes a corticosteroid and a 5-HT3 antagonist.  You should take your first capsule (125mg) on day 1, one hour before starting chemotherapy.  You should take your next two capsules (80mg) once daily on days 2 and 3 in the morning.  You should take your Aprecap capsules in addition to other antiemetic medications as recommended by your doctor.

Missed dose of Aprecap

If you miss a dose of Aprecap capsules contact your doctor for instructions. 

How should Aprecap be stored?

You should store your Aprecap capsules below 25°C in a cool dry place. 

References

1. Warr DG.  Chemotherapy- and cancer-related nausea and vomiting.  Curr Oncol 2008 Jan; 15(Suppl 1): S4–S9.
2. Miya T, Kobayashi K, Hino M, Ando M, Takeuchi S, Seike M, Kubota K, Gemma A, East Japan Chesters Group. Efficacy of triple antiemetic therapy (palonosetron, dexamethasone, aprepitant) for chemotherapy-induced nausea and vomiting in patients receiving carboplatin-based, moderately emetogenic chemotherapy.  Springerplus 2016 Dec 7;5(1):2080.