Injectable Solution is indicated for the prevention and treatment of acute vomiting in dogs and cats, CERENIA analog!
Composition
1 ml of the drug contains:
maropitant citrate — 10 mg
Description
The solution is colorless or light yellow, transparent.
Pharmacological properties
Maropitant is a selective antagonist of the neurokinin 1 (NK1) receptor. Inhibits the binding of substance P (P-neuropeptide of the tachykinin family in the CNS). It is found in significant concentrations in the nuclei of the vomiting center and is considered a key neurotransmitter involved in the act of vomiting. By inhibiting the binding of substance P in the center of vomiting, maropitant is effective against nervous and humoral (central and peripheral) causes of vomiting.
The effectiveness of maropitant, which neutralizes the effect of agents that affect the central and peripheral centers of vomiting, was demonstrated by experimental studies on dogs with the use of apomorphine, cisplatin and syrup of ipecac and cats with the use of xylazine.
The composition of the drug includes sulfobutyl ether of ß-cyclodextrin, which binds to cooled maropitant. When heated, the ability of ether to bind to maropitant quickly disappears.
With a single subcutaneous injection of 1 mg of maropitant per 1 kg of body weight to dogs, its maximum concentration (Cmax) in blood plasma reaches 92 ng/ml 0.75 hours after administration (Tmax). The elimination half-life (t1/2) is 8.84 hours.
With a single intravenous administration of 1 mg of maropitant per 1 kg of body weight to dogs, its initial concentration in the blood plasma is 363 ng/ml, the volume of distribution in the steady state (Vss) is 9.3 l/kg, and the systemic clearance is 1.5 l/h/kg. The elimination half-life (t1/2) after intravenous administration is approximately 5.8 hours.
The therapeutic level of maropitant in the blood plasma of dogs is reached 1 hour after administration. Bioavailability after subcutaneous administration to dogs is 90.7%. Maropitant demonstrates linear kinetics when administered subcutaneously in the dose range of 0.5-2 mg per 1 kg of body weight.
After subcutaneous administration of 1 mg of maropitant per 1 kg of body weight once a day to dogs for 5 days, the accumulation is 146%. Maropitant is metabolized by cytochrome P450 (CYP) in the liver. CYP2D15 and CYP3A12 have been identified as canine isoforms involved in the biotransformation of maropitant in the liver.
Renal clearance is a secondary route of elimination. Less than 1% of the subcutaneous dose is found in the urine as maropitant or its main metabolite. Binding to plasma proteins in dogs is more than 99%.
The pharmacokinetic profile of maropitant when administered subcutaneously to cats at a dose of 1 mg per 1 kg of body weight is characterized by a maximum concentration (Cmax) in the blood plasma of about 165 ng/ml on average 19 minutes after administration (Tmax). The elimination half-life (t1/2) is 16.8 hours. After a single intravenous administration at a dose of 1 mg per 1 kg of body weight, the initial concentration of maropitant in plasma is 1040 ng/ml, the volume of distribution in the steady state (Vss) is 2.3 L/kg, and the systemic clearance is 0.51 L /hour/kg. The elimination half-life (t1/2) after intravenous administration is approximately 4.9 hours. Pharmacokinetics of maropitant in the body of cats depends on age: clearance in kittens is higher than in adult cats.
The concentration of maropitant in the blood plasma of cats reaches a therapeutic level 1 hour after administration.
Bioavailability after subcutaneous administration to cats is 91.3%. Maropitant exhibits linear kinetics when administered subcutaneously in doses of 0.25–3 mg per 1 kg of body weight.
After subcutaneous administration of 1 mg of maropitant per 1 kg of body weight once a day for 5 consecutive days, the accumulation is 250%. It is metabolized by cytochrome P450 (CYP) in the liver. CYP1A and CYP3A enzymes have been identified as feline isoforms involved in the biotransformation of maropitant in the liver.
After subcutaneous administration at a dose of 1 mg per 1 kg of body weight, maropitant is found unchanged in urine (10.4%) and feces (9.3%). Binding to blood plasma proteins in cats is 99.1%.
Indication
Prevention and treatment of dogs and cats with vomiting and nausea of various genesis.
Contraindication
Do not prescribe to animals with increased sensitivity to the active substances of the drug, with reduced body weight, exhausted, sick and productive animals.
Method of application and dosage
The drug is used intravenously (injected within 1-2 minutes!) or subcutaneously, once a day, the course is up to 5 days. Before subcutaneous administration, the product is cooled to reduce the likelihood of painful reactions.
Dogs — 0.1 ml (1 mg of maropitant citrate) per 1 kg of body weight: 2-4 months old — subcutaneously, 4 months old — subcutaneously or intravenously, 4 months old and older to prevent vomiting after emetogenic or chemotherapeutic agents — intravenously or subcutaneously, 45-60 minutes before using the drug that causes vomiting.
Cats older than 4 months — 0.1 ml (1 mg of maropitant citrate) per 1 kg of body weight, intravenously or subcutaneously.
Before using the drug, the cause of vomiting and nausea should be established. If vomiting persists despite treatment, the case should be re-evaluated.
Reservation
When used in recommended doses, side effects usually do not occur.
With subcutaneous administration, pain may appear at the injection site. It passes within a few minutes. Occasionally, anaphylactic-type reactions may occur (allergic edema, urticaria, erythema, collapse, shortness of breath, pallor of the mucous membranes). Allergic reactions usually pass within 48 hours after stopping the use of the drug and appropriate treatment.
The safety of maropitant has not been studied in dogs less than 8 weeks of age and cats less than 16 weeks of age, nor in pregnant or lactating dogs and cats. The drug can be used in such animals only under the supervision of a veterinarian and after assessing the benefit/risk ratio for the animal’s health.
Maropitant is metabolized in the liver, so it should be used with caution in animals with liver disease. During long-term treatment, it is necessary to carefully monitor liver function and detect side effects as soon as possible.
Caution should be used in animals with or prone to heart disease, as maropitant has an affinity for Ca and K ion channels.
Use in parallel with other veterinary and auxiliary measures – diet control, fluid replacement therapy, elimination of the main causes of vomiting.
Do not use simultaneously with Ca-channel antagonists, as maropitant has an affinity for Ca-ion channels.
Maropitant is highly bound to plasma proteins and may compete with other highly protein bound agents (nonsteroidal anti-inflammatory drugs (NSAIDs), cardiac, anticonvulsant, and behavior modification drugs).
Maropitant is well tolerated by dogs and young cats. They were administered daily up to 5 mg per 1 kg of body weight (5 times more than the recommended dose) for 15 consecutive days (3 times longer than the recommended course). There are no data on overdose in adult cats.
Intravenous administration should be carried out once and do not mix the drug with other means.
To prevent vomiting after other medicinal products, the drug is administered more than 1 hour before their use. Since the drug works for about 24 hours, it is administered, for example, at night, and in the morning a chemotherapeutic agent is used.
Personnel who work with the drug must follow the basic hygiene and safety rules adopted when working with veterinary drugs.
If the product gets on the skin, mucous membranes or in the eyes, they must be washed with a large amount of running water.
Storage conditions
In a dry, dark place inaccessible to children at temperatures from +5 to +25 °C.
After opening the bottle, store the drug in the refrigerator and use it within 28 days.
Shelf life
2 years.