Maropitant Citrate: The Ultimate Guide
Maropitant citrate is a pivotal active pharmaceutical ingredient (API) widely used in veterinary medicine, particularly in the treatment and prevention of nausea and vomiting in dogs and cats.
As an API importer, medicine manufacturer, or compounding pharmacy, understanding the intricacies of maropitant citrate is essential to producing high-quality veterinary formulations and meeting your clients’ needs.
What Is Maropitant?
Maropitant citrate API is the citrate salt of maropitant and a white to off-white crystalline powder used as a veterinary antiemetic agent.
Please note that there are three crystal forms for maropitant citrate: forms A, B, and C.
Form C has better solubility in water and methanol and higher stability.
Its solubility in water at room temperature for form A is 0.238 g/l, andfor formC itc is 0.445 g/l.
When we raise the temperature to 37 Degrees Celsius, its solubility will not increase much. Still, if we change the solvent from water to methanol, solubility will increase by 10 times or more.
Nevertheless, the water solubility of maropitant citrate salt is much better than that of maropitant base.
Maropitant citrate is used for vomiting in cats and dogs under the Cerenia brand.
Maropitant injections are for acute vomiting, while tablets or capsules are for common types of vomiting.
Maropitant is a neurokinin-1 (NK1) receptor antagonist.
It works by blocking the action of substance P, a neurotransmitter in the vomiting reflex.
By inhibiting substance P, maropitant effectively prevents vomiting and reduces nausea in cats and dogs.
What is Maropitant Citrate Used for in Dogs?
Maropitant citrate is primarily used in veterinary medicine to treat and prevent nausea and vomiting caused by various conditions, including:
- Motion Sickness in Dogs: Maropitant is highly effective at preventing vomiting during car rides or travel. It is often prescribed before long trips or for dogs prone to motion sickness.
- Chemotherapy-Induced Vomiting: Dogs undergoing chemotherapy often experience nausea and vomiting as a side effect. Maropitant helps alleviate these symptoms, improving the quality of life for these patients.
- Postoperative Nausea and Vomiting: After surgery, dogs may experience nausea and vomiting due to anesthesia or pain. Maropitant can be administered to prevent and treat these symptoms.
- Gastrointestinal Disorders: Conditions such as gastritis, pancreatitis, or intestinal obstruction can cause a dog to vomit. Maropitant helps manage these symptoms while the underlying condition is being treated.
How Does Maropitant Citrate Work? (Mechanism of action)
1. Neurokinin-1 (NK1) Receptor Antagonism
Maropitant citrate primarily functions as a selective neurokinin-1 (NK1) receptor antagonist, a critical component in the vomiting reflex pathway.
- NK1 Receptor Localization: These receptors are densely expressed in the vomiting center of the medulla oblongata and the chemoreceptor trigger zone (CTZ) in the brainstem
- P blockade: By binding to NK1 receptors, maropitant inhibits the binding of substance P, a neuropeptide that triggers vomiting by activating vagal afferent pathways and gastrointestinal motility
2. Central and Peripheral Effects
- Central Antiemetic Action:
- Suppresses vomiting signals originating from the brainstem, including motion sickness and chemotherapy-induced nausea
- Reduces the minimum alveolar concentration (MAC) of inhalant anesthetics like sevoflurane by 16%, suggesting analgesic properties via inhibition of visceral pain pathways
- Peripheral Antiemetic Action:
- Stabilizes the gastrointestinal tract by reducing intestinal contraction pressure and delaying gastric emptying, though it does not alter intestinal transit time
Is Maropitant Citrate the Same as Cerenia?
No, it isn’t.
But you can say Cerenia is maropitant citrate because Cerenia contains maropitant citrate, and there is no doubt about it.
Maropitant citrate is not the only ingredient, but it is the active ingredient in Cerenia, which contains excipients.
Cerenia is the best-known and most widely used formulation of maropitant citrate in the veterinary field.
While Cerenia is the brand name of the relevant maropitant citrate formulation, maropitant citrate is the generic name of the active compound.
However, when someone refers to maropitant citrate, it doesn’t necessarily mean it is Cerenia; it could be a non-branded compounded formulation by a pharmacist.
Is Maropitant Safe for Dogs?
Maropitant is generally considered safe and well-tolerated in dogs when used as directed.
However, like any medication, it may cause side effects in some animals.
Extensive clinical trials and post-market monitoring support the safety profile of maropitant, but it’s essential to consider the following:
- Dosage: The recommended maropitant dose varies with the dog’s weight and formulation (injectable or oral). Always follow the veterinarian’s instructions carefully.
- Pregnancy and Lactation: While maropitant is considered safe for use in lactating dogs, its safety in pregnant dogs has not been fully established. Consult a veterinarian before administering maropitant to pregnant animals.
- Age Restrictions: Maropitant is approved for use in dogs 16 weeks or older. For younger dogs, consult a veterinarian for alternative treatments.
How Long Does Maropitant Last in Dogs?
Maropitant citrate is formulated to provide long-lasting relief from nausea and vomiting.
The duration of action depends on the formulation:
- Injectable Maropitant: The injectable form of maropitant typically provides 24 hours of anti-emetic protection. This makes it ideal for acute and preventive use, such as before travel or chemotherapy.
- Oral Maropitant: The oral tablets (Cerenia Caplets) typically last 24 hours, making them convenient for daily administration.
Creating extended-release formulations of maropitant may be feasible for compounding pharmacies, but this requires careful scientific evaluation to ensure safety and efficacy.
What Are the Side Effects of Maropitant?
While maropitant is well-tolerated by most dogs, some animals may experience mild side effects, including:
- Pain or Swelling at the Injection Site: This is the most common side effect of the injectable form but is usually temporary.
- Lethargy: Some dogs may appear drowsy or less active after taking maropitant.
- Diarrhea or Decreased Appetite: These gastrointestinal symptoms may occur in some animals but are usually mild and short-lived.
Severe side effects are rare but may include hypersensitivity reactions or vomiting shortly after administration.
If your dog exhibits severe side effects, seek veterinary attention immediately.
Can Humans Take Maropitant?
No, we can’t.
Maropitant citrate is not for human use.
It is specifically formulated for veterinary use and has not been tested or approved for human consumption.
Humans have their meds to manage nausea and vomiting, primarily caused by chemotherapy, such as ondansetron hydrochloride, granisetron hydrochloride, or metoclopramide, which are designed for human physiology.
Is Maropitant Used in Humans?
No, it isn’t.
Maropitant citrate is not used in humans; the concept of NK1 receptor antagonism has been applied in human medicine.
Drugs like aprepitant and fosaprepitant are NK1 receptor antagonists that prevent chemotherapy-induced nausea and vomiting in humans.
These medications work similarly to maropitant but are specifically designed for humans.
How Much Does Maropitant API Cost?
For 99% type pure maropitant powder, the costs of the citrate salt and the free base are about the same.
Please clarify which one you need before placing your order.
#1. If you are looking for reference substances or working standards with very high purity requirements, over 99.9% type.
The price of this type of pure powder from reagent companies is around 9500 USD/25mg and 400 USD/5 mg.
#2. If you need pure maropitant powder for research, please check reagent companies for larger packages, such as 1g or 5g.
The cost from reagent companies is about 1000 USD/1G
#3. If you are a pharmacist trying to compound tablets or capsules for dogs and cats, you may check our cost for your reference below:
For 100 Grams, our price is around 5000 USD, and for 1 kg, our price is about 25000 USD.
How To Ship and Store Maropitant API?
China Safety Authorities have tested maropitant citrate and considered it a safe chemical suitable for air, sea, rail, and truck shipping.
It is not a dangerous product, not poisonous, flammable, explosive, or oxidizing either.
As for the shipping temperatures and conditions, let’s first review the stability testing data.
Stability tests have shown that it is photochemically stable as well. When exposed to accelerated (40ºC/75% RH), intermediate (30ºC/60% RH), and long-term (25ºC/60% RH) VICH storage conditions, no solid-state degradation is observed.
Based on the data above, it is okay to ship it at room temperature; seal it in a foil bag. (Protected from light and moisture)
We recommend storing it at -20 Degrees Celsius for long-term storage, but maropitant citrate is stable at room temperature for 24 months.
Addressing the Pain Points for API Importers, Medicine Manufacturers, and Compounding Pharmacies
As an API importer, medicine manufacturer, or compounding pharmacy, you may face several challenges when working with maropitant citrate. Let’s address these pain points and provide solutions:
Quality and Compliance: Ensure that the maropitant citrate you source meets pharmacopeial standards and regulatory requirements. Work with reputable suppliers who provide Certificates of Analysis (CoA) and comply with Good Manufacturing Practices (GMP).
Formulation Challenges: Maropitant’s crystalline structure can pose formulation challenges. Collaborate with formulation experts to develop stable and effective veterinary products in injectable, oral, or compounded forms.
Market Trends: Stay informed about market demand for maropitant-based products. While Cerenia dominates the market, there is growing interest in generic and compounded formulations, particularly among compounding pharmacies.
Supply Chain Reliability: Ensure a consistent supply of maropitant citrate to meet production needs—partner with API manufacturers that offer competitive pricing and dependable delivery.
Conclusion
Maropitant citrate is a cornerstone of veterinary medicine, offering safe and effective relief from nausea and vomiting in dogs and cats.
For API importers, medicine manufacturers, and compounding pharmacies, maropitant citrate presents a lucrative opportunity to produce high-quality veterinary products.
By understanding its uses, benefits, and potential challenges, you can position your business to meet the growing demand for veterinary antiemetics.
Whether sourcing maropitant citrate for bulk production or creating customized formulations, staying informed about its scientific properties and regulatory requirements is key to success.
Partner with trusted suppliers, invest in quality control, and leverage market trends to create innovative veterinary products that meet your clients’ needs.
For more information about maropitant citrate and its applications, contact our team today and learn how we can support your veterinary pharmaceutical endeavors.
Disclaimer:
This content is for informational purposes only and is intended for business-to-business communication within the pharmaceutical industry. It is not intended as medical advice. The manufacture, import, and use of API must comply with all applicable laws and regulations in the relevant country or region.
This blog post is informational only and does not constitute medical advice.
Always consult a healthcare professional before starting any new medication or treatment.
