Relenza powder for inhalation dosed vials
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Active ingredients
Zanamivir
Release form
Powder
Composition
Active ingredient: Zanamivir. Excipients: lactose monohydrate. Concentration of active ingredient (mg): 5 mg
Pharmacological effect
Zanamivir is a strong and highly selective inhibitor of neuroaminidase (the surface enzyme of the influenza virus). Viral neuroaminidase provides the release of viral particles from an infected cell and can accelerate the penetration of the virus through the mucous barrier to the surface of epithelial cells, thereby ensuring the infection of other cells of the respiratory tract. The inhibitory activity of zanamivir is shown both in vitro and in vivo and includes all 9 subtypes of neuraminidase influenza viruses, including those circulating and virulent for various species. Half of the inhibitory concentration (1С50) for virus strains A and B is from 0. 09 to 95. 2 nM. Influenza virus replication is restricted to the surface epithelium of the respiratory tract. Zanamivir acts in the extracellular space, reducing the reproduction of both types of influenza virus (A and B) and preventing the release of viral cell particles from the cells of the surface epithelium of the respiratory tract. The effectiveness of zanamivir inhalation use was confirmed in controlled clinical trials. The use of zanamavir as a treatment for acute infections caused by the influenza virus led to a decrease in the release of the virus (compared to placebo). Development of resistance to zanamivir is not registered.
Pharmacokinetics
Absorption: low and at about 10% to 20% of the administered dose is absorbed in the mean after the inhalation inhalation. After a single dose of 10 mg, the maximum plasma concentration of Ctah was 97 ng / ml at 1. 25 hours. Low absorption results in low systemic concentrations and insignificant area under the concentration-time curve. A low degree of absorption is maintained during repeated inhalations. Distribution: After oral inhalation, zanamivir is deposited in the airways in high concentrations, ensuring the drug is delivered to the “entrance gate” of the infection. After inhalation, 10 mg of zanamivir in the epithelial layer of the respiratory tract concentrations exceeded the average half of the inhibitory concentration for neuroamididase 340 times 12 hours after inhalation and 52 times after 24 hours, ensuring rapid inhibition of the viral enzyme. The main sites of sedimentation are the oropharynx and lungs (average 77.6% and 13.2%, respectively).Metabolism and excretion: not metabolized, excreted by the kidneys unchanged. The plasma elimination half-life after oral inhalation varies from 2.6 to 5.05 hours. Total clearance is from 2.5 to 10.9 l / h.
Indications
Treatment and prevention of infections caused by influenza A and B viruses in children over 5 years old and adults.
Contraindications
Hypersensitivity to the drug. Precautions should be prescribed the drug for diseases of the respiratory tract, accompanied by bronchospasm (including in history).
Precautionary measures
Before you begin taking this drug, tell your doctor about medicines already used, nutritional supplements (such as vitamins, natural supplements, etc.), allergic reactions, existing diseases, and current health status (such as pregnancy, impending surgery, etc.). Side effects of the drug may be more pronounced in a certain state of your body. Take the drug as directed by your doctor or follow the instructions for use supplied with the drug. The dosage of the drug depends on your condition. Notify your doctor if your condition has not changed or worsened. Important points to discuss with your doctor are listed below. Pregnant, planning a pregnancy or breastfeeding, Do not drive or work with appliances
Use during pregnancy and lactation
The efficacy and safety of zanamivir during pregnancy and lactation has not been studied. Experimental studies on animals have shown that zanamivir penetrates through the placenta and into breast milk, however, there is no teratogenic effect or a decrease in fertility or clinical manifestations of any abnormalities in the peri- and postnatal periods. There is no information about penetration through the placental barrier or into breast milk. However, zanamivir should not be used during pregnancy and during breastfeeding, especially in the first trimester, only if the expected benefit of the use for the mother exceeds the possible risk to the fetus.
Dosage and administration
Intended only for inhalation administration to the respiratory tract using the supplied discharger inhaler.Other inhalation drugs, such as high-speed bronchodilators, should be taken before the start of inhalation with Relenza. In the treatment of influenza A and B, adults and children over 5 years old are recommended to prescribe 2 inhalations (2 × 5 mg) 2 times a day for 5 days. Daily dose - 20 mg. Dosage adjustment is not required for elderly patients and patients with impaired renal and hepatic function. For optimal effect, treatment should be started as early as possible. In order to prevent influenza A and B, adults and children over 5 years old are recommended to take 2 inhalations (2 × 5 mg) 1 per day for 10 days. Daily dose - 10 mg. The course of prevention can be extended to 1 month, if the risk of the disease persists for more than 10 days. Dosage adjustment is not required for elderly patients and patients with impaired renal and hepatic function. Rules for the use of Diskhaler. The device Diskhaler is used for inhalations of a rotadisk (release form of Relenza). The disc holder consists of the following parts: a housing with a lid and a plastic needle to pierce a rotadisk cell, a case for the mouthpiece, a sliding tray with a mouthpiece and a rotating wheel, on which Rotadisk is placed. Rotadisk consists of 4 blisters, each of which contains a specific dose of the drug. Rotadisk can be stored in the Dischaler for inhalation device, however, the blister should be pierced just before the inhalation of the drug. Failure to comply with this recommendation may disrupt the operation of the Diskhaler and, accordingly, reduce the effectiveness of the drug. Important: do not pierce the rotadisk before it is placed in the Diskhaler. Download rotadiska in Diskhaler. 1. Remove the cover from the mouthpiece, make sure that the mouthpiece is clean inside and out. 2. Carefully pull out the drawer until the plastic clips exit, grasping the corners of the tray. Pull the tray all the way out so that the notches on the side of the clamps are visible. 3. Pull out the tray completely, squeezing the notches on the side of the clamps with your thumb and index finger. 4. Place the rotadisk on the wheel cells down and insert the tray back into the Diskhaler. Conduct inhalation. 1. Raise the Disc Cover up to the stop to pierce the top and bottom foils of the Rotadisc. Close the lid. Important: Do not lift the lid until the drawer is fully installed. 2After a full exhalation, place the mouthpiece between the teeth, tightly clasp the mouthpiece with your lips, without closing the air holes on either side of the mouthpiece. Take a slow deep breath (always through the mouth, not through the nose). Remove the mouthpiece from the mouth. Hold your breath as much as possible. Exhale slowly. Do not exhale into the inhaler. 3. Carefully pull out the pull-out tray once until it stops, without pressing the clips, and push it in. In this case, the rotadisk will turn one cell and is ready for the next inhalation. Important: piercing the cell should be only immediately before inhalation. For repeated inhalations repeat p. 1 and p. 2. Replacing the empty rotadisk. Each rotadisk contains 4 cells. After four inhalations, the empty rotadisk should be replaced with a new one (p. 2-4). Important: Children should use an inhalation device under adult supervision.
Side effects
In controlled clinical trials, the incidence of adverse events is similar in the zanamivir group and the placebo group. Spontaneous messages contained information about undesirable reactions to the use of zanamivir and were classified as follows: very often (≥110), often (≥1100, less than 110) sometimes (≥11000, less than 1100), rarely (≥1000, less than 11000), very rarely (less than 110 000), including individual cases. Allergic reactions: very rarely - allergic reactions, including swelling of the face and larynx. On the part of the respiratory system: very rarely - bronchospasm, difficulty breathing. Dermatological reactions: very rarely - rash, urticaria, severe skin reactions, including erythema polymorphic, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Overdose
Accidental overdose is unlikely due to the nature of the release form itself, route of administration, and low bioavailability after oral administration of zanamivir. With inhalation use of 64 mg per day (more than 3 times the recommended daily dose) no side effects have been registered. Also, they are not registered with parenteral administration for 5 days, 1,200 mg per day.
Interaction with other drugs
Zanamivir does not bind to proteins, nor is it metabolized and does not undergo changes in the liver. Clinically significant drug interaction is unlikely.
special instructions
Elderly: bioavailability after administration of a therapeutic dose of 20 mg is 10-20%, as a result, the concentrations in the systemic circulation are insignificant. Correction of the dosage regimen is not required, since any age-related changes, usually leading to changes in the pharmacokinetic profiles of various drugs, in this case do not affect the pharmacokinetics of zanamivir. Children: Zanamivir pharmacokinetics were evaluated in a controlled pediatric study in 24 patients aged 3 months to 12 years using a nebulizer (10 mg) and a powder inhaler (10 mg). The pharmacokinetic parameters in children did not differ from those in adults. Patients with impaired renal function: when applying therapeutic doses of 20 mg, bioavailability is low and amounts to 10-20%, therefore, systemic concentrations of zanamivir are insignificant. Given the wide range of drug safety, a possible increase in systemic concentrations in patients with severe renal failure remains clinically insignificant and does not require correction of the dosage regimen. Patients with impaired liver function: since zanamivir is not metabolized, no dosage regimen needs to be adjusted. The clinical efficacy and safety of zanamivir used in doses used in the treatment of influenza in healthy people at risk (usually in contact with the diseased) alleviates the symptoms and shortens the duration of the disease. A combined analysis of the results of 3 studies showed that the median time to alleviate the symptoms of the disease is reduced to 1.5 days in patients in the zanamivir group compared with patients in the placebo group (p less than 0. 001). The number of complications decreased in the zanamivir group 171/769 (22%) compared with placebo 208/711 (29%) and the relative risk was: 0. 77; (95% CI: 0. 65 to 0. 92; p = 0. 004). The use of antibiotics for treating complications after a postponed flu also decreased from 136/711 (19%) in the placebo group to 110/769 (14%) in the zanamivir group (relative risk: 0. 76; 95% CI: 0. 60 to 0. 95; p = 0. 021). Optimal efficacy of zanamivir was shown in the case of initiation of treatment as soon as possible after the onset of the first symptoms of the disease. It has been shown that zanamivir is also effective as a means of preventing influenza in children over 5 years old and in adults.The percentage of effective protection is 67-79% compared with placebo and 56-61% compared with active control.