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Relenza - instructions for use, price, reviews, analogues

Zanamivir is a strong and highly selective inhibitor of neuraminidase (the surface enzyme of the influenza virus). Viral neuraminidase 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. Zanamivir inhibitory activity is shown as in vitro so and in vivo and includes all 9 subtypes of neuraminidase influenza viruses, incl. circulating and virulent for various species. For virus strains A and B, 50% inhibitory concentration (IC50) ranges 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), preventing the release of viral 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 zanamivir as a treatment for acute infections caused by the influenza virus led to a decrease in the release of the virus (compared with placebo). The development of resistance to zanamivir is not registered.

Pharmacokinetics

Suction. Absolute bioavailability is low and averages 2% after oral administration. After oral inhalation, approximately 10 to 20% of the administered dose is absorbed. After a single dose of 10 mg Cmax plasma level was 97 ng / ml after 1.25 hours. Low absorption results in low systemic concentrations and insignificant AUC. A low degree of absorption is maintained during repeated inhalations.

Distribution. After oral inhalation, zanamivir is deposited in the airways in high concentrations, ensuring delivery of the drug 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 neuraminidase 340 times 12 hours after inhalation and 52 times after 24 hours, providing rapid inhibition of the viral enzyme. The main sites of sedimentation are the oral part of the pharynx and lungs (77.6 and 13.2% on average, respectively).

Metabolism and excretion. Not metabolized, excreted by the kidneys unchanged. T1/2 from blood plasma after oral inhalation varies from 2.6 to 5.05 hours. Total clearance is from 2.5 to 10.9 l / h.

Special patient populations

Elderly Bioavailability after administration of a therapeutic dose of 20 mg is 10–20%, resulting in insignificant concentrations in the systemic circulation. Correction of the dosing 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. The pharmacokinetics of zanamivir was evaluated in a controlled pediatric study in 24 patients aged from 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. With the use of therapeutic doses of 20 mg, bioavailability is low at 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, the dosage regimen does not need to be adjusted.

Clinical efficacy and safety. Zanamivir, used in doses used in the treatment of influenza in healthy, at risk groups (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 ®

treatment of infections caused by influenza viruses type A and B in children over 5 years old and adults,

prevention of infections caused by influenza A and B viruses in children over 5 years of age and adults.

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 in humans.

However, zanamivir should not be used during pregnancy and during breastfeeding, especially in the first trimester, use is possible only if the expected benefit of using for the mother exceeds the possible risk to the fetus.

Side effects

In controlled clinical trials, the incidence of adverse events is similar in the zanamivir group and the placebo group. Spontaneous reports contained information about undesirable reactions to the use of zanamivir and were classified as follows: very often (≥1 / 10), often (≥1 / 100, ® should be used only after these drugs.

Adults and children from 5 years: The recommended dose of zanamivir is 2 inhalations (2 × 5 mg), 2 times a day for 5 days. The total daily dose is 20 mg. To achieve an optimal effect, treatment should be initiated when the first symptoms of the disease appear.

Elderly patients: correction of the mode of dispensing is not required.

Patients with impaired renal function: correction of the mode of dispensing is not required.

Patients with impaired liver function: correction of the mode of dispensing is not required.

Adults and children from 5 years: The recommended dose of zanamivir is 2 inhalations (2 × 5 mg) once a day for 10 days. The total daily dose is 10 mg. The duration of use can be increased to 1 month, if the risk of infection persists for more than 10 days (for example, longer contact with the diseased is assumed).

Elderly patients: correction of the mode of dispensing is not required.

Patients with impaired renal function: correction of the mode of dispensing is not required.

Patients with impaired liver function: correction of the mode of dispensing is not required.

Instructions for use Diskhalera with rotadiskami

The device Diskhaler is used for inhalation of rotadisk (the release form of Relenza ®).

Diskhaler consists of the following parts:

- a housing with a lid and a plastic needle to pierce a rotadisk cell,

- case for mouthpiece,

- a sliding tray with a mouthpiece and a rotating wheel on which the rotadisk is placed.

Rotadisk consists of 4 blisters, each of which contains a specific dose of the drug.

Rotadisk may 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 rotadisk in Diskhaler

1. Remove the case 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 by 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.

5. Raise the Disc Cover up to the stop to pierce the top and bottom foil of the rotadisk. Close the lid.

Important! Do not lift the lid until the drawer is fully installed.

6. After 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.

7. 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! Puncture the cell should only immediately before inhalation!

For repeated inhalations repeat points 5 and 6.

Replacing an empty rotadisk

Each rotadisk contains 4 cells. After 4 inhalations, replace the empty rotadisk with a new one (points 2-4).

Important! Children should use an inhalation device under adult supervision.

Overdose

Accidental overdose is unlikely due to the nature of the release form, 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 use for 5 days at a dose of 1200 mg / day.

special instructions

Very rare individual reports on the development of bronchospasm and / or impaired respiratory function after the use of zanamivir, including without previous illness in history. If one of the above phenomena develops, one should stop taking zanamivir and consult a doctor. Patients with respiratory diseases should have short-range bronchodilators for zanamivir treatment as an ambulance.

Infection caused by the influenza virus may be associated with various neurological and behavioral disorders. Reports received during the post-marketing period included convulsive seizures, delirium, hallucinations, and deviant behavior in patients infected with the influenza virus and taking neuraminidase inhibitors, including zanamivir (mainly in children in Japan). These phenomena were observed mainly in the early stages of the disease, often had a sudden onset and a rapid onset of outcome. The causal relationship between zanamivir intake and the above adverse events has not been proven. If any neuropsychiatric symptoms occur, it is necessary to assess the risk-benefit ratio of further treatment with zanamivir for each individual patient.

Influence on ability to drive a car and other mechanisms: not noted.

Release form and composition

The dosage form of release of Relenza is a metered-dose powder for inhalation: from almost white to white [in a carton bundle one vial containing 20 doses (5 rotadisks of 4 cells each), complete with a Discaller].

Ingredients 1 dose powder:

  • active ingredient: zanamivir (micronized) - 5 mg,
  • auxiliary component: lactose monohydrate - up to 25 mg.

pharmachologic effect

It is an antiviral drug, a highly selective neuraminidase inhibitor, which is a surface enzyme of the influenza virus. Viral neuraminidase is able to release cells and accelerates the passage of the virus through the mucous barrier to the surface of epithelial cells, causing other cells of the respiratory tract to become infected.

When treating the mucous membrane of the respiratory tract zanamivirvirus, falling on it, remains on the surface and can not get into the epithelium cells. If the nasopharynx and respiratory tract cells that are already infected with the virus are processed, the spread of the infection throughout the body stops. The drug does not enter the cell space, affecting the extracellular environment.

The drug is also effective for the prevention of influenza in adults and children over 5 years. Compared to placebo, the percentage of efficacy ranges from 67 to 79 percent, compared to active control, from 56 to 61 percent.

Contraindications

Should not be taken for allergic reactions to zanamivirin the anamnesis. Also contraindications are:

  • lactation,
  • pregnancy in the first trimester
  • age up to 5 years
  • an increased bronchial reaction to inhalants,
  • diseases that are accompanied bronchospasm,
  • lactose intolerance.

Instructions for use Relenza (method and dosage)

The instructions for use of Relenza indicate that the drug is used with a special inhaler called Diskhaler, supplied. For patients of all ages, the same dosage is applied - 20 milligrams per day. To maximize the effectiveness of treatment, it is necessary to begin inhalation at the slightest detection of symptoms.

The use of the drug is divided into two doses, in each of which is administered 10 milligrams of zanamivir in the form of inhalation (two inhalations of 5 milligrams). Duration of use is five days.

In order to prevent the drug can be used for ten days, two inhalations (10 milligrams of the active substance) once a day. If the risk of infection persists, prophylactic use can be extended to one month.

To place the rotadisk in Diskhaler:

  • check the integrity of the rotadisk,
  • remove the case from the mouthpiece and make sure the mouthpiece is clean,
  • pull the tray up to the stop by the corners so that the plastic clips come out (it is necessary that the serifs are visible),
  • squeeze the clamps and fully extend the tray,
  • rotadisk place on the wheel cell down,
  • Insert the tray into place.

For inhalation, you must:

  • raise the lid of the diskhaler up to the stop to puncture the upper and lower foil of the rotadisk, then close the lid,
  • make a full exhalation and place the mouthpiece between the teeth, while not closing the air holes on both sides of the mouthpiece, tightly clasp his lips. Slowly take a deep breath through your mouth and remove the mouthpiece from the mouth, as far as possible to hold your breath and slowly exhale. Exhalation in the inhaler is prohibited,
  • once gently push the drawer out until it stops, do not press the clips, and slide it in to rotate the rotadisk one cell, after which it will be ready for subsequent inhalation. It is worth considering that it is possible to pierce the cell only immediately before the inhalation.

Each rotadisk has four cells. After four inhalations, an empty rotadisk should be replaced with a new one.

Indications for use

What does Relenza help? According to the instructions, the drug is prescribed in the following cases:

  • treatment of infections caused by influenza viruses type A and B in children over 5 years old and adults,
  • prevention of infections caused by influenza A and B viruses in children over 5 years of age and adults.

Instructions for use Relenza dosage

Used with a special inhaler Diskhaler, which comes bundled with the drug.

According to the instructions for use, for all age groups, the dosage of Relenza is the same - 20 mg / day. Inhalation is carried out when detecting the first symptoms of influenza - this significantly increases the effectiveness of treatment.

Divide the use of the drug into 2 doses, each of which provides for the introduction in the form of inhalation of 10 mg of zanamivir (two inhalations of 5 mg). Duration of use - 5 days.

For prophylaxis use Relenzu 10 days, making 2 inhalations (10 mg zanamivir) once a day. If necessary, prophylaxis is extended up to a month if the risk of infection persists.

Instructions for the inhaler

To place the rotadisk in Diskhaler:

  • check the integrity of the rotadisk,
  • remove the case from the mouthpiece and make sure the mouthpiece is clean,
  • pull the tray up to the stop by the corners so that the plastic clips come out (it is necessary that the serifs are visible),
  • squeeze the clamps and fully extend the tray,
  • rotadisk place on the wheel cell down,
  • Insert the tray into place.

For inhalation, you must:

  • Raise the top and bottom foil of the rotadisk, then close the lid,
  • Make a full exhalation and place the mouthpiece between the teeth, while not closing the air holes on both sides of the mouthpiece, tightly clasp it with your lips. Slowly take a deep breath through your mouth and remove the mouthpiece from the mouth, as far as possible to hold your breath and slowly exhale. Exhalation in the inhaler is prohibited,
  • Once carefully, pull out the drawer until it stops, do not press the clips, and slide it in to rotate the rotadisk one cell, after which it will be ready for subsequent inhalation. It is worth considering that it is possible to pierce the cell only immediately before the inhalation.

Each rotadisk has four cells. After four inhalations, an empty rotadisk should be replaced with a new one.

Children should use an inhalation device under adult supervision.

Additionally

The effectiveness of inhalation Relenza directly depends on the time of the start of the use of the drug (the earlier, the more effective).

При заболеваниях бронхов обязательно иметь быстродействующие бронходилататоры в роли препаратов скорой помощи.

Side effects

The instruction warns of the possibility of the development of the following side effects when prescribing Relenza:

  • On the part of the immune system: very rarely - allergic reactions, including swelling of the face and larynx.
  • On the part of the respiratory tract: very rarely - bronchospasm, difficulty breathing.
  • On the part of the skin and its appendages: very rarely - a rash, urticaria, severe skin reactions, including erythema polymorphic, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Contraindications

It is contraindicated to appoint Relenza in the following cases:

  • lactation,
  • first trimester pregnancy
  • age up to 5 years
  • an increased bronchial reaction to inhalants,
  • diseases that are accompanied by bronchospasm,
  • lactose intolerance.

Overdose

Due to the nature of the dosage form, the route of administration and the low bioavailability of the active substance, accidental overdose is unlikely.

Under the conditions of clinical studies, adverse reactions with intravenous administration in a daily dose of 1200 mg for 5 days were not registered.

Hemodialysis can be considered as a treatment option, since zanamivir has a low molecular weight, low bond with plasma proteins and low Vd.

Analogs Relenza, price in pharmacies

If necessary, Relenza can be replaced by an analogue for therapeutic action - these are drugs:

Choosing analogues it is important to understand that the instructions for use of Relenza, the price and reviews of drugs of similar action do not apply. It is important to consult a doctor and not to make an independent replacement of the drug.

The price in pharmacies in Russia: Relenza powder for inhalation of 5 mg / dose No. 5 bottles with an inhaler - from 900 to 1121 rubles, according to 802 pharmacies.

Store at temperatures up to 30 ° C. Keep out of the reach of children. Shelf life - 7 years. Conditions of sale from pharmacies - prescription.

What is the drug Relenza

The drug is available in powder form 5 mg. One dose contains:

  • active ingredient - zanamivir
  • excipient - milk sugar

White powder is very light in color. The active substance is capable of removing the virus from the diseased cell to prevent its further spread and reproduction. Relenza helps in the treatment of 9 viral neuraminidase subtypes.

In addition to the instructions and the drug itself, the device for inhalation of dischaler is also in the carton.

Producing company

Manufacturing country - France. Glaxo Wellcome Production.

The drug is intended for the treatment of colds, infectious diseases caused by influenza viruses A and B in adults and children under 5 years of age. In the same age group, Relenza is used for prevention.

Principle of operation

The action of Relenza is aimed at releasing influenza virus cells from the diseased to the surface with its further destruction.

With the inhalation method of use, the active substance zanamivir is most active. A significant relief in the patient's well-being comes within 1.5 days. Most of all his work comes when dealing with a virus that is in the body for no more than 2 days. When applied at the initial stage, the threshold for protection against further infection is 79%.

When administered orally, Relezna has a low absorption percentage (up to 2%). When reused for inhalation, it does not change. As a result, the concentration of the active components in the blood plasma does not increase.

The drug is excreted by the kidneys and does not participate in the metabolic processes of the human body. Dose adjustment in the elderly is not required.

How to apply

Relenza powder is used exclusively for inhalation. In the treatment of influenza type A or B, 2 procedures are performed using 2x5 mg each. The maximum daily dosage is 20 mg. For children older than 5 years old and adult portions of the drug are taken the same. When problems with the work of the kidneys or liver dose does not require adjustment.

For the prevention of influenza infection, the daily use of Relenza is halved, that is, 1 inhalation per day from 2x5 mg of the drug. The maximum dosage per day is 1 mg. The duration of such a course is up to 10 days.

Information about the impact of Relenza on the pregnant woman's body is not, therefore, women in the position it is not prescribed. In particular, this is especially true of the first trimester. It does not apply to lactating breast milk. If there is an urgent need for its use, then reception is carried out with the utmost care and recording the changes in well-being. There is a risk of normal fetal development.

How to use Relenzoo, see in our video:

Use of the device for inhalation

The disc drive into the package includes several parts:

  1. A housing with a lid and a needle there that is used to pierce the cell with the powder.
  2. Sliding tray with a wheel that rotates manually.
  3. Case with mouthpiece.

The powder is distributed at a specific dosage by rotodisk, which can be stored in the attached device for inhalation. Puncture is carried out immediately before using the powder for inhalation. Violation of technology implementation can significantly affect the effectiveness of Relenza.

On the photo device dischaler

How to do the procedure

Having studied the structure of the diskhaler, it is important to understand the scheme of its application. Proceed as follows to properly use antiviral agent:

  1. Make sure the mouthpiece is used.
  2. Pull the tray out until plastic clips with side notches appear.
  3. Place powder on the wheel with the cells looking down without making any punctures.
  4. Lift the device cover to the limit. It closes, puncturing the cell with the powder on both sides.
  5. Do not lift the lid until the tray is fully installed.
  6. While exhaling, hold the mouthpiece with your mouth while not blocking the holes in it.
  7. Breathe in through your mouth through the diskhaler and hold your breath for as long as possible.
  8. Exhale by removing the inhaler.

In the photo step by step instructions on the use of the inhaler

Interaction

Data on the interaction with other drugs have not been established.

One of the drawbacks of Relenza is its high cost. Otherwise, the drug has proven itself very well: it quickly relieves symptoms and makes you feel better.

Reviews of treatment with Relenza:

The price of Relenza's medicine varies from 1100-1200 rubles per pack. Its formation depends on the pharmacy chain where the product is purchased, and on the region of sale.

Dosage Form

Relenza drug is available in powder form for inhalation. It is packaged in a vial containing 5 rotadisks, in which there are 4 cells (doses) each. Included with the bottle is "Relenza-Diskhaler." The cardboard pack contains 1 bottle (totally 20 doses), diskhaler and instructions for use.

Pharmacological group

Powder for inhalation Relenza refers to antiviral agents. The main active component of the drug zanamivir selectively inhibits the activity of the enzyme neuraminidase of influenza virus pathogens type A and B. This leads to disruption of the process of release of new viral particles from infected cells. The binding of the virus to the cellular receptors of the respiratory mucosa epithelial cells worsens.

The therapeutic effect develops after inhalation (inhalation) of the active ingredient of Relenza powder. It has been confirmed in clinical studies. Addiction to the drug has not been established.

After inhalation of Relenza powder, the therapeutic concentration in the airways is reached for a short period of time. Zanamivir is poorly absorbed from the mucous membrane of the respiratory tract into the systemic circulation. In the body, it is not metabolized and is excreted unchanged.

for adults

For adults, the drug is used for medical reasons, which include:

  • Treatment of influenza caused by types of virus A and B.
  • Conducting prevention of influenza A and B during periods of epidemiological increase in the incidence.

Powder for inhalation Relenza can be used for children over the age of 5 years. For the treatment and prophylaxis of influenza, type A and B are prescribed in appropriate therapeutic dosages recommended for adults.

for pregnant women and during lactation

Reliable data on the safety of the drug Relenza for pregnant and lactating women today is not. It is allowed to use the drug for pregnant women in the II and III trimester of pregnancy, but only after a doctor's prescription, if the intended benefit to the mother outweighs the potential risks to the fetus or infant.

Uses and doses

Relenza powder is designed to perform inhalation with the aid of the Dischaler apparatus included in the package, which is included in the package. In a plastic sliding tray on a special wheel cells placed rotadisk. After the tray with the rotadisk has been pushed back, the lid of the Dischaler opens, which leads to the puncturing of the cell. The lid is then closed, the mouthpiece is clamped in the teeth, tightly covered with the lips and a slow deep breath is taken by the mouth (no breath can be taken through the nose, as powder will not get into the airways). After 4 inhalations (the rotadisk contains 4 cells, 1 dose each), the empty rotadisk is replaced with a new one.

Storage conditions

The drug should be stored in its original packaging at air temperature not higher than + 30 ° C. Shelf life is 5 years.

Today there are no structural analogues for Relenza powder on the pharmacological market. The following therapeutic substitutes have similar therapeutic effects:

  • Amizon - the drug is available in the form of tablets or syrup for children, the main active ingredient is the isonicotinic acid derivative. It has an inhibitory effect on influenza viruses, and also stimulates the activity of the immune system. The drug is used for the treatment and prevention of influenza, as well as other acute respiratory viral diseases in adults and children. Prophylactic medication is indicated in the period of increasing incidence of catarrhal and respiratory diseases.
  • Tamiflu is a medicament that is made in an oral capsule dosage form and powder for suspension. The active ingredient oseltamivir has a selective inhibitory effect on the neuraminidase enzyme. The activity of the drug is equally pronounced in relation to influenza viruses type A and B. It is used for the treatment and prevention of influenza.
  • Arbidol is a drug that has the ability to stimulate antiviral immunity, including protective mechanisms against influenza pathogens. The drug is made in tablets and capsules, it can be used for adults and children from the age of 2 years. The drug is used to treat the prevention of influenza caused by various types of pathogens, as well as other acute respiratory viral infections (ARVI).

The cost of Relenza is an average of 942 rubles. Prices range from 797 to 1400 rubles.

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