This triggers the gag reflex and its accompanying feeling of nausea. Tropisetron selectively blocks the excitation of the presynaptic 5-HT 3 receptors on peripheral testosterone enanthate vs cypionate neurons involved in causing this reflex, and may also provide additional direct action on 5-HT 3 receptors located in CNS and mediate the effect on the vagus nerve area postrema. It is believed that these effects are the basis of the mechanism of antiemetic action tropisetron.
- The duration of Navobana is 24 hours, it can be used 1 time per day.
- When using Navobana extrapyramidal side effects were observed.
Bioavailability depends on the dose: after dosing at a dose of 5 mg, it reaches about 60% and increases (up to 100%) after administration at a dose of 45 mg. The values of bioavailability and terminal half-life in children are similar to the corresponding figures observed in healthy volunteers. Metabolism tropisetron hydroxylation is carried out by a 5, 6 or 7 positions of the indole ring, followed by reaction with the formation of glucuronide conjugation or sulfate and elimination in urine or bile (ratio of metabolites in the urine and where to buy testosterone enanthate feces of 5: 1). Tropisetron Active metabolites in 5-HT s receptors is significantly reduced, and they do not participate in the implementation of the pharmacological action of the drug. The metabolism of tropisetron is connected with the genetically determined sparteine polymorphism metabolism / debrizohina. It is known that about 8% of those Caucasians have a low metabolic rate sparteine / debrizohina.
In repeated Navobana appointments at doses exceeding 10 mg 2 times a day, liver enzyme system saturation can occur, tropisetron involved in metabolism, which may lead to a dose-dependent increase in the plasma concentration of tropisetron. However, even in those with low metabolic tropisetron Navobana use of such doses did not increase above tropisetron concentration values tolerable plasma.Therefore, when applying Navobana at the recommended dose of 5 mg 1 time a day for 6 days cumulation tropisetron is not considered to be clinically significant.
Individuals with high metabolic half-life tropisetron (beta phase) is about 8 hours; patients with low metabolic tropisetron, this rate may be extended to 45 hours.
Tropisetron total clearance of about 1 l / min and the renal clearance is about 10% of this value. Patients with low metabolic tropisetron total clearance is reduced to 0.1-0.2 l / min and the renal clearance value is not changed. Reducing extrarenal clearance is responsible for approximately 4-5-fold lengthening half-life and a 5-7-fold increase in the values of the area under “concentration-time” curve (AUC). The value C max and volume of distribution in these patients do not differ from those in patients with high levels of metabolic tropisetron. Patients with low metabolic tropisetron proportion of unchanged tropisetron, is output in the urine is higher than that of patients with high metabolic tropisetron.
- Prevention of nausea and vomiting arising from cancer chemotherapy
- Elimination of nausea and vomiting that occur in the postoperative period
- Prevention of nausea and vomiting that occur after intra-abdominal gynecological surgery in order to achieve optimal value ratio “benefit / risk” should use the drug in a limited contingent of patients, namely – in with a history of an indication of the development of postoperative nausea and vomiting.
- Hypersensitivity to tropisetron, other 5-HT antagonists s receptors or any other components of the drug.
Precautions should be taken when applying Navobana in patients with cardiac arrhythmias and conduction, as well as in patients who are being treated with antiarrhythmic agents or beta-blockers, as the existing experience and Navobana simultaneous application of narcosis in such cases is limited.
Pregnancy and lactation
Since research applications Navobana in pregnant women have not been conducted, it should not be used during pregnancy.
It is not known whether tropisetron into breast milk in humans is excreted, so patients taking Navoban should not breast-feed.
Dosing and Administration
The solution for intravenous injection is administered as an infusion (after pre-dissolving) or intravenously slowly (at least 1 min). The solution, if necessary, can be taken by mouth, pre-diluted contents of the vial of orange juice or cola (accept the prepared solution immediately after dilution).
The capsules are taken orally in the morning an hour before a meal with water.
Prevention testosterone enanthate vs cypionate of nausea and vomiting arising from cancer chemotherapy
Recommended Navobana dose for children older than 2 years of age is 0.2 mg / kg; the maximum daily dose – 5 mg. On the first day, a short time before applying antineoplastic chemotherapy drug is administered intravenously. From the 2nd to the 6th day of the drug is prescribed orally at a dose rate of 0.2 mg / kg; the maximum daily dose – 5 mg.
Adults are encouraged to nominate Navoban as 6-day courses of 5 mg per day. On the first day of drug administered in / in for a short time prior to application of anticancer chemotherapy. From the 2nd to the 6th day of the drug is prescribed inside.
If the application of tropisetron is not achieved satisfactory antiemetic action to achieve clinical effect can be further appoint dexamethasone.
Elimination and prevention of nausea and vomiting that occur in the postoperative period
Navoban recommended for use on / in a dose of 2 mg. For the prevention of nausea and vomiting arising postoperative Navoban be applied shortly before anesthesia.
Use in elderly patients
No dose adjustment Navobana in elderly patients is not required.
Instructions for use of the solution for solution for infusion tropisetron diluted with 5% dextrose solution, 10% mannitol solution, Ringer’s solution, 0.9% solution of sodium chloride, potassium chloride solution or 0.3% at 1 mg / 20 ml.
The solution contained in vials, containers compatible with the conventional type of infusion (made of glass, PVC) and infusion systems.
The diluted solution is physically and chemically stable for at least 24 hours. From the point of view of possible microbial contamination, preferably diluted use solutions immediately after preparation. Unused right solution can be stored in the refrigerator at a temperature of + 2-8 ° C for up to 24 hours.
When using testosterone enanthate vs cypionate at recommended doses adverse effects are transient in nature. In applying the drug of 2 mg most frequently reported development of headache. When using the drug at a dose of 5 mg were also observed constipation and, less frequently, dizziness, fatigue, disorders of the gastrointestinal (GI) tract, such as abdominal pain and diarrhea.
Just as the use of other 5-HT antagonists s receptors, is rarely observed hypersensitivity reactions of type 1, is characterized by one or more of the following symptoms: feeling a rush of blood to the face and / or generalized urticaria testosterone enanthate vs testosterone cypionate, feeling of heaviness in the chest, shortness of breath , acute bronchospasm developing expressed reduction of blood pressure (BP).
It was reported about rare cases of collapse, fainting or cardiac arrest, but the causal relationship of these events using Navobana has not been established. Some of them could be due to concomitant therapy or the underlying disease.
In case of repeated use of very high doses were observed Navobana visual hallucinations; in patients with prior hypertension – increased blood pressure.
Displaying symptomatic treatment under the constant control of the vital functions of the organism and the patient’s condition.
The interaction with other drugs and other interactions simultaneous use Navobana rifampicin or with other drugs inducing liver enzyme system (e.g., phenobarbital), leads to a decrease in plasma concentrations of tropisetron. Therefore, in patients with a high level of metabolism is necessary to increase doses of tropisetron Navobana (in patients with a low level of metabolism of tropisetron is not required).
Effects of inhibitors of cytochrome P450 enzyme system, such as cimetidine. troiisetrona on plasma levels are insignificant: change the dosing regimen Navobana ® in such cases is not required.
Interaction studies with means not conducted for anesthesia.
QTc prolongation was observed in some patients who was administered in combination with drugs causing prolongation of the interval. At the same time, in those studies where only one used at therapeutic doses, QTc interval prolongation was observed. However, care should be taken while the application and drugs that cause QTc prolongation.
Before the drug in capsule form together with a small increase food tropisetron bioavailability (approximately 60% to 80%), which had no clinical significance.
In applying in patients with uncontrolled hypertension in a daily dose greater than 10 mg, may further increase the blood pressure (BP).
In patients with low levels of sparteine / debrizohina metabolic half-life period is extended tropisetron (4-5 times. Compared with those with high levels of sparteine / debrizohina metabolism). However, under / in a Navobana ® at doses as high as 40 mg. 2 times a day for 7 days to healthy volunteers, relating to categories of persons with low sparteine metabolism / debrizohina serious adverse events were noted.These observations indicate that during the 6-day course of treatment of patients, classified as those with low-sparteine metabolism / debrizohina. necessary to reduce the usual daily dose, 5 mg of component. occurs.
In patients with acute hepatitis or fatty liver changes in the pharmacokinetics of tropisetron is not marked. In contrast, in patients with liver cirrhosis or impaired renal function, plasma concentrations of tropisetron may exceed (maximum 50% pa) indicators that are identified in healthy volunteers, tnosyaschihsya of a group of persons with a high level of metabolism sparteine / debrizohina. However, when using testosterone enanthate vs cypionate in these patients as the recommended 6-day course of 5 mg / day, the drug dosing regimen correction is required.
Otmecheno that children older than 2 years tolerability was good. Data on the impact of on the ability to drive a car is not available. However, some side effects of the drug, such as dizziness and fatigue can adversely affect driving ability and the performance of potentially hazardous activities that require high concentration and speed of psychomotor reactions. how much to inject for weight loss
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