Everything about Aprepitant powder

 

  1.What is Aprepitant
  2.What is Aprepitant powder
  3. How does Aprepitant powder works
  4.Where Aprepitant powder usage for ?
  5. How should Aprepitant powder be used
  6.Aprepitant powder Dosage?
  7. Other Comments for Aprepitant powder
  8.What special precautions should I follow?
  9. Aprepitant powder other uses

 


 

Aprepitant powder video

 

 


I.Aprepitant powder basic Characters:

 

Name: Aprepitant powder
CAS: 170729-80-3
Molecular Formula: C23H21F7N4O3
Molecular Weight: 534.4266624
Melt Point: 244-246°C
Storage Temp: -20°C Freezer
Color: White powder

 


 

1.What is Aprepitant powder?aasraw

 

Aprepitant powder (brand name: Emend) is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by blocking the neurokinin 1 (NK1) receptor. It’s used for prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for prevention of postoperative nausea and vomiting. Aprepitant powder may also be useful in the treatment of cyclic vomiting syndrome and late-stage chemotherapy induced vomiting.

 


 

2.What is Aprepitant powder?aasraw

 

Name:    Aprepitant powder
CAS:    170729-80-3
Molecular Formula:    C23H21F7N4O3
Molecular Weight:    534.4266624
Melt Point:    244-246°C
Storage Temp:    -20°C Freezer
Color:    White powder

 

Raw Aprepitant powder (170729-80-3) hplc≥98% | AASraw powder

Aprepitant raw powder is made up of a morpholine core with two substituents attached to adjacent ring carbons. These substitute groups are trifluoromethylated phenyl ethanol and fluorophenyl group. Aprepitant powder also has a third substituent (triazolinone), which is joined to the morpholine ring nitrogen. It has three chiral centres very close together, which combine to produce an amino acetal arrangement. Its empirical formula is C23H21F7N4O3.

Aprepitant raw powder is an off-white crystalline solid that has a molecular weight of around 534.53. It has a very limited solubility in water. It does have a reasonably high solubility in non-polar molecules such as oils. This would, therefore, suggest that Aprepitant powder as a whole, despite having components that are polar, is a non-polar substance.

 


 

3.How does Aprepitant powder works?aasraw

 

Aprepitant powder is classified as an NK1 antagonist because it blocks signals given off by NK1 receptors. This, therefore, decreases the likelihood of vomiting in patients.

NK1 is a G protein-coupled receptor located in the central and peripheral nervous system. This receptor has a dominant ligand known as Substance P (SP). SP is a neuropeptide, composed of 11 amino acids, which sends impulses and messages from the brain. It is found in high concentrations in the vomiting center of the brain, and, when activated, it results in a vomiting reflex. In addition to this it also plays a key part in the transmission of pain impulses from the peripheral receptors to the central nervous system.

Aprepitant powder has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brain’s neurons. Positron emission tomography (PET) studies, have demonstrated that Aprepitant raw powder can cross the blood brain barrier and bind to NK1 receptors in the human brain. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.

Aprepitant powder is taken orally in the form of a capsule. Before clinical testing, a new class of therapeutic agent has to be characterized in terms of preclinical metabolism and excretion studies. Average bioavailability is found to be around 60-65%. Aprepitant powder is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19. Seven metabolites of Aprepitant raw powder, which are only weakly active, have been identified in human plasma. As a moderate inhibitor of CYP3A4, Aprepitant powder can increase plasma concentrations of co-administered medicinal products that are metabolized through CYP3A4. Specific interaction has been demonstrated with oxycodone, where Aprepitant raw powder both increased the efficacy and worsened the side effects of oxycodone; however it is unclear whether this is due to CPY3A4 inhibition or through its NK-1 antagonist action. Following IV administration of a 14C-labeled prodrug of Aprepitant powder (L-758298), which is converted rapidly and completely to Aprepitant raw powder, approximately 57% of the total radioactivity is excreted in the urine and 45% in feces. No unchanged substance is excreted in urine.

One of the main features of Aprepitant powder, and a major advantage it has over other chemotherapy-induced side-effect treatments, is its ability to selectively antagonize NK1 receptors, while having very low affinity to other common receptors such as serotonin, dopamine, and corticosteroid. It is estimated that Aprepitant raw powder is at least 3,000 times more selective to NK1 receptors compared to these other enzyme transporter, The normal dosing of Aprepitant powder given as 125 mg in the first day after chemotherapy and followed by 80 mg the following 2 days.

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4.Where Aprepitant powder usage for?aasraw

 

Aprepitant powder is used to help prevent nausea and vomiting that can sometimes follow chemotherapy treatment. For patients receiving chemotherapy, nausea and vomiting may occur within the 24 hours immediately following treatment (acute), or several days later (delayed). Given in combination with other medications, Aprepitant raw powder may prevent both acute and delayed nausea and vomiting. Aprepitant powder is not used to treat nausea and vomiting once they have already begun.

Aprepitant raw powder is used with other medications in adults and children 6 months of age and older to prevent nausea and vomiting that may occur within 24 hours after receiving cancer chemotherapy treatment. It is also used with other medications in adults and children 6 months of age and older to prevent delayed nausea and vomiting that may occur several days after receiving certain chemotherapy medications. Aprepitant powder is also used alone in adults to prevent nausea and vomiting caused by surgery. Aprepitant powder is not used to treat nausea and vomiting that you already have. Aprepitant raw powder is in a class of medications called antiemetics. It works by blocking the action of neurokinin, a natural substance in the brain that causes nausea and vomiting.

 


 

5.How should Aprepitant powder be used?aasraw

 

Aprepitant powder comes as a capsule and as an oral suspension (liquid) to take by mouth. To prevent nausea and vomiting caused by cancer chemotherapy, Aprepitant raw powder is usually taken once daily, with or without food, during the first few days of your cancer chemotherapy treatment. You will probably take Aprepitant powder 1 hour before your chemotherapy on days 1, 2, and 3 of your treatment. If you do not receive chemotherapy on days 2 and 3, then you will take Aprepitant raw powder on those days in the morning. To prevent nausea and vomiting caused by surgery, Aprepitant powder is usually taken as one dose within 3 hours before the start of surgery. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take Aprepitant raw powder exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Aprepitant powder capsules come in two different strengths. Your doctor may prescribe both of the strengths for you to take at different times. You should be careful to take the right strength at the right time as directed by your doctor.

Swallow the capsules whole; do not split, chew, or crush them.

The oral suspension will be prepared by your healthcare provider and given to you in an oral dispenser. Store the oral dispenser in the refrigerator until it is time for your dose; however, it can be stored at room temperature for up to 3 hours before use. When ready to use, remove the cap from the dispenser before placing it in your mouth to slowly release the medication.

Aprepitant raw powder only works to prevent nausea and vomiting. Call your doctor if you already have these symptoms and do not begin to take Aprepitant powder.

When used to prevent nausea and vomiting caused by cancer chemotherapy, Aprepitant raw powder is usually used only during the first 3 days of the chemotherapy treatment cycles. Do not continue taking Aprepitant powder longer than instructed by your doctor.

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6.Aprepitant powder Dosageaasraw

 

Usual Adult Dose for Nausea/Vomiting – Chemotherapy Induced

MODERATELY TO HIGHLY EMETOGENIC CANCER CHEMOTHERAPY (HEC/MEC):
Oral Capsules:
-Day 1: 125 mg orally once 1 hour before chemotherapy
-Days 2 and 3: 80 mg orally once a day, 1 hour before chemotherapy OR in the morning (if chemotherapy is not given on Days 2 and 3)
-Duration of therapy: 3 days/cycle

Oral Suspension:

-Day 1: 3 mg/kg orally once 1 hour before chemotherapy
—Maximum dose: 125 mg/dose
-Days 2 to 3: 2 mg/kg orally once a day, 1 hour before chemotherapy OR in the morning (if chemotherapy is not given on Days 2 and 3)
—Maximum dose: 80 mg/dose
-Duration of therapy: 3 days/cycle

Comments:

-The recommended dosage of dexamethasone is 12 mg orally on Day 1 administered 30 minutes prior to chemotherapy and 8 mg orally in the mornings on Days 2 through 4 (HEC) or Days 2 through 3 (MEC).
-The 5-HT3 antagonist is administered on Day 1 only. Consult the package insert for the 5-HT3 antagonist dosing prior to initiation of treatment.
-This drug may be taken with or without food.

Uses:
-In combination with other antiemetic agents for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of HEC including high-dose cisplatin
-In combination with other antiemetic agents for the prevention of nausea and vomiting associated with initial and repeat courses of MEC

Usual Adult Dose for Nausea/Vomiting – Postoperative

40 mg orally once within 3 hours prior to induction of anesthesia

Use: Prevention of nausea and vomiting

Usual Pediatric Dose for Nausea/Vomiting – Chemotherapy Induced

12 years and older:
MEC/HEC:

Oral Capsules:-Day 1: 125 mg orally once 1 hour before chemotherapy
-Days 2 and 3: 80 mg orally once a day, 1 hour before chemotherapy OR in the morning (if chemotherapy is not given on Days 2 and 3)
-Duration of therapy: 3 days/cycle

Oral Suspension:

-Day 1: 3 mg/kg orally once 1 hour before chemotherapy
—Maximum dose: 125 mg/dose
-Days 2 to 3: 2 mg/kg orally once a day, 1 hour before chemotherapy OR in the morning (if chemotherapy is not given on Days 2 and 3)
—Maximum dose: 80 mg/dose
-Duration of therapy: 3 days/cycle

Comments:

-If a corticosteroid (e.g., dexamethasone) is coadministered, patients should be given 50% of the recommended pediatric dose on Days 1 to 4. Consult the package insert for the corticosteroid dosing prior to initiation of treatment.
-The 5-HT3 antagonist is administered on Day 1 only. Consult the package insert for the 5-HT3 antagonist dosing prior to initiation of treatment.
-This drug may be taken with or without food.

Uses

-In combination with other antiemetic agents for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of HEC including high-dose cisplatin
-In combination with other antiemetic agents for the prevention of nausea and vomiting associated with initial and repeat courses of MEC


 

7.Other Comments for Aprepitant powderaasraw

 

Administration advice:
-Take with or without food.
-Oral suspension: Oral syringes should be placed along the inner cheek, and should be dispensed slowly.
-Oral capsules: Swallow whole.
-For prevention of CINV, take first dose 1 hour prior to chemotherapy.
-For prevention of PONV, receive medication within 3 hours prior to induction of anesthesia.

 

Storage requirements:

-Oral suspension: Refrigerate; use within 72 hours of preparation, and discard any remaining suspension after 72 hours.

 

General:

-Limitations of use: Use has not been studied for the treatment of established nausea and vomiting.
-Patient profiles may change during chronic continuous administration; chronic use is not recommended.

 

Monitoring:

-Hematologic: INR in patients on chronic warfarin therapy
-Hypersensitivity: Hypersensitivity reactions at any time during treatment

 

Patient advice:

-Patients should be advised to report all concurrent prescription and nonprescription medications or herbal products they are taking.
-Instruct patients to immediately report any signs/symptoms of Stevens-Johnson syndrome, toxic epidermal necrolysis, or hypersensitivity reactions.
-Patients should be advised to speak to healthcare provider if pregnant, intend to become pregnant, or are breastfeeding; patients using hormonal contraception to prevent pregnancy will need to speak with their health care provider about using a non-hormonal back-up method of birth control for up to 2 months after completing therapy.

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8.What special precautions should I follow?aasraw

 

Before taking Aprepitant powder

    • tell your doctor and pharmacist if you are allergic to Aprepitant powder, any other medications, or any of the ingredients in Aprepitant raw powder capsules or oral suspension. Ask your pharmacist for a list of the ingredients.
    • do not take Aprepitant powder if you are taking pimozide (Orap). Your doctor will probably tell you not to take Aprepitant raw powder if you are taking this medication.
    • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: anticoagulants (‘blood thinners’) such as warfarin (Coumadin, Jantoven); antifungals such as itraconazole (Onmel, Sporanox) and ketoconazole ; benzodiazepines such as alprazolam (Xanax), diazepam (Valium), midazolam , and triazolam (Halcion); cancer chemotherapy medications such as ifosfamide (Ifex), irinotecan (Camptosar), vinblastine, and vincristine (Marqibo Kit); carbamazepine (Equetro, Tegretol, Teril); clarithromycin (Biaxin, in Prevpac); diltiazem (Cardizem, Cartia, Tiazac); HIV protease inhibitors such as nelfinavir (Viracept) and ritonavir (Norvir); hormonal contraceptives (birth control pills, patches, rings, and injections); nefazodone; oral steroids such as dexamethasone and methylprednisolone (Medrol); phenytoin (Dilantin, Phenytek); rifampin (Rifadin, Rimactane, in Rifamate, in Rifater); and troleandomycin (TAO; no longer available in U.S.). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with Aprepitant powder, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
    • tell your doctor if you have or have ever had liver disease.

  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you are taking birth control medications during treatment with Aprepitant raw powder you should also use an additional method of birth control to avoid pregnancy during treatment with Aprepitant powder and for one month after your final dose. Talk to your doctor about birth control methods while you are taking Aprepitant raw powder and after treatment. If you become pregnant while taking Aprepitant powder, call your doctor.

 


 

9.Aprepitant powder other usesaasraw

 

Major depression

Encouraged by positive results in their early controlled studies of Aprepitant powder (300 mg/d with enforced food intake) and L-759,274(another NK1 receptor antagonist), as well as those of CP-122,721 (Pfizer) in patients with major depressive disorder, Merck & Co. conducted Phase III clinical trials on Aprepitant powder in which patients received 80 mg or 160 mg/d (a new formulation, prescribed without enforced food intake) as a treatment for major depressive disorder. Despite achieving 90-95% receptor occupancy of Aprepitant raw powder in certain brain regions, negative clinical results were observed in three actively controlled studies. The company has since abandoned plans to market Aprepitant powder 160 mg as an antidepressant. Subsequently, large clinically positive double blind controlled studies with two additional NK1 receptor antagonists, casopitant, and orvepitant (both GlaxoSmithKine compounds) have been published in peer reviewed medical journals. This work now replicates the early findings of Merck and Co with Aprepitant raw powder and L-759,274, and of Pfizer with CP-122,721. Arguably, the weight of preclinical data and positive clinical evidence provides evidence that NK1 receptor antagonism, including that of Aprepitant powder, is a distinct antidepressant mechanism. Across all these studies, efficacy appeared to be dose-related. Only mild, transient, and tolerable side effects, not those typically observed with either the SSRI, SNRI, or NRI classes of antidepressants, have been observed.

Beyond suggestions that PET receptor occupancy must not be used routinely to cap dosing for new medical indications for this class, or that > 99% human receptor occupancy might be required for consistent psycho-pharmacological or other therapeutic effects, critical scientific dissection and debate of the above data might be needed to enable Aprepitant raw powder, and the class of NK1 antagonists as a whole, to fulfill preclinically predicted utilities beyond CINV (i.e., for other psychiatric disorders, addictions, neuropathic pain, migraine, osteoarthritis, overactive bladder, inflammatory bowel disease, and other disorders with suspected inflammatory or immunological components (see anti-cancer below.) However, most data remain proprietary and thus reviews on the expanded clinical potential for drugs like Aprepitant powder range from optimistic to crepe-hanging.

 


 

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1 Response Comment

  • Viagracheap06/11/2018 at 5:45 pm

    Thanks Pooja- I’m loving it so far!!!

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