Fentanyl. Instructions for use in capsules, patch. Price, reviews, analogues

To prevent development of or alleviate pain using various categories of drugs. Fentanyl is included in the group of narcotic drugs. The most convenient form of release - ampoules. A detailed study of the instructions for use will help prevent the development of unwanted side effects of the therapy.

release Form

The drug is commercially available in two dosage forms: ampules and transdermal therapeutic systems (abbreviated - TTC or films for applications on the skin).

Fentanyl (instructions for use in ampoules have in each package) produced in the dose of 50 .mu.g / ml. It is used for intravenous or intramuscular administration. Manufacturer implements means in glass ampoules of 1 ml or 2 packed in separate boxes 5 pcs.

Fentanyl Transdermal therapeutic systems are available in the form of sachets packed 5 pcs. The dosage of the active ingredient corresponds to its rate of release. Thus, the manufacturer offers patches with a release rate: 12.5 micrograms, 25 micrograms, 50 micrograms, 75 micrograms and 100 micrograms (one hour).

the drug

Fentanyl contains only one active ingredient - fentanyl. It connects to the opiate receptors in various areas of the nervous system. This leads to the block of nociceptive information. This property allows the use of a drug for the treatment of acute or chronic pain.

Fentanyl is an injectable medicament transparent, 1 ml of which contains 50 mcg of the drug. The solvent is a liquid for injection.

Transdermal systems have an adhesive layer on the skin for fixation (polyacrylates), a substrate and protected by a polyethylene layer (siliconized polyethylene terephthalate) from the environment. The dosage of analgesic in the composition of the patch varies from a minimum of 2.1 mg to a maximum of 16.8 mg.

pharmacological properties

Fentanyl, instructions for use (in ampoules) which contains detailed information about features biotransformation binds to mu-receptors of certain parts of the nervous system, including the tissue end. The chemical compound gives a conducting thalamic pain impulses, hypothalamic, cerebral amygdaloid nucleus.

Fentanyl causes a change in the patient's mental state, namely:

• changing emotional painful experiences;
• It causes a feeling of euphoria;
• It can have a hypnotic effect.

Repeated administration of the agent may cause physical dependence and reduce receptor sensitivity (tolerance growth).

Effect on formation of the stem, located in the brain, is the depression of the respiratory and activate the vomiting center, as well as stimulation of the nuclei of the vagus nerve (vagus). In response to the application of the patient decreases blood pressure, slows the heart rate.

Activation of the vagus nerve has the following clinical manifestations:

• increases the tone of the intestinal sphincters and the urinary tract;
• reduced peristaltic contractions of the intestine;
• renal blood flow becomes less active.

Pharmacokinetics

The effect of the drug occurs after entering the bloodstream. The fastest pain relief occurs by intravenous injection. Relief there for 4 min, the greatest effect is noticeable for 7 minutes by means of entering the bloodstream.

About 80% of the substance binds to albumin (transport protein) of blood. This means that the effect will be faster and more massive in the appointment of Fentanyl malnourished patients with low serum albumin.

The half-life is:

• 30 min after intravenous injection;
• about 2 hours at intramuscular injection.

Fentanyl biotransformation as liver and kidney, the intestine. Up to 78% of the material comes from the urine in an inactivated form. The drug is also found in breast milk.

Fentanyl transdermal system is working for 3 days. This information is noted in the instructions for use. This is the fundamental difference from the drug injections. The release agent occurs gradually with the same speed.

Its plasma concentration gradually increases during the first days and maintained within the same values. Data from clinical studies show a slight increase in speed with repeated use. Thus, when the applique adhered fourth means half-life of about 17 hours.

After removal of the transdermal concentration of active compound in the body media gradually decreases.

Indications

Fentanyl is a drug used in both hospital and outpatient management for individuals with acute or chronic pathologies.

Agent recommended in the following cases:

• for sedation before surgery;
• for induction of anesthesia;
• for the purpose of pain relief after surgery;
• for the treatment of severe pain in patients with cancer pathology or somatic chronic diseases.

Instructions for use

Fentanyl (instructions for use in ampoules contained in each package of the drug) used for anesthesia during the operation, as an analgesic in other conditions.

In adult patients the following dosage and administration of the plan recommended:

1. When required neyroleptanalgezii 2 ml injection of fentanyl and 0.5 ml fenotiazidnogo neuroleptic droperidol. Are administered intravenously 15 min before surgery.
2. Dosages for anesthesia in surgical practice vary depending on the duration and volume of operation:

• to achieve general anesthesia - up to 0.6 mg / in;
• of 0.05-1.5 mg for maintenance after 25-30 minutes from the start of the operation; administration is repeated every 30 minutes;
• for analgesia after intervention Fentanyl administered intramuscularly at 0.1 mg.

If such a background therapy in a patient in postoperative pain occurs, and it needs to facilitate state means in the same dosage administered at intervals of 1.5 hours; if necessary repeating the introduction.

Fentanyl is also prescribed for persons with acute myocardial infarction with Q-tooth or without new-onset angina within neyroleptanalgezii. The reading - the inability to stop pain nonsteroidal analgesics.

To achieve a rapid effect, the drug is administered intravenously and slowly at a dose of 1 ml. Fentanyl is diluted with 20 ml 0.86% sodium chloride. Depending on the initial blood-pressure syringe gain from 1 to 4 ml of droperidol.

The patient is evaluated after 5-8 min of infusion. With insufficient analgesia fentanyl repeated after 20 min, after evaluating the patient's condition. The drug is resolved at a frequency of 14 respiratory cycles per minute. Upon reaching the effect of patient transferred to non-steroidal analgesics.

Transdermal fentanyl is indicated for the deliverance of man from chronic pain. Patch drug applied to the clean and dry skin as possible devoid expressed hairline.

The repeated use of space applications need to be alternated. Dosage selection is carried out only in the hospital, taking into account a number of factors. Since persons without receiving those funds history selection start from 25 micrograms.

Calculating dosages to patients with resistance to this group is carried out by means of special tables which are different dosages previous preparations. If the patient suffers from a strong expression of pain. the dosage of 300 ug / hr is achieved by a combination of injection and transfer applications or for intravenous or intramuscular route of administration.

Pregnancy and lactation

According to FDA classification, Fentanyl belongs to category C. This means that in conducting animal studies during pregnancy revealed adverse effects on the fetus.

Similar studies in human populations have not been conducted. If necessary, medication can be assigned to women during childbearing, if the potential benefit of treatment is greater than the potential harm to the fetus.

Proved active substance from entering into breast milk. Fentanyl appointment requires the child transfer to artificial milk substitutes. Formally on the drug pregnancy and lactation instructions - contraindications to treatment.

children

Fentanyl is approved for use in pediatric practice. Dosage is calculated according to age and weight of the child. The table below shows recommendations on the appointment of the injection mold.

Age of the child	Scheme for small interventions	Protocol for persons in need of long-term pain relief
2-3 years	w / w or w / o to 3 mg / kg administered repeatedly after 30 minutes if necessary	From 1 ug / kg bolus - the initial dosage. Then, at the child lead supporting dosage - to 3 mg / kg per hour.
From 3 to 12 years	w / w or w / o of 1-2 mg / kg, repeated application is not earlier than 30 min	From 1 ug / kg bolus before surgery. During the operation of administered 2 mg / kg per hour.

Children from 12 years of age receive a drug in the same dosage as adults. The drug is not recommended for patients under the age of 2 years, the dosage is not installed.

Appointment of a transdermal system for the relief of chronic pain is possible with the age of two. It should be noted that this category of patients on background applications such Fentanyl likely undesirable effects, such as:

• itching;
• nausea and vomiting;
• headache;
• constipation or diarrhea.

Use in the elderly

Study of the pharmacokinetics of fentanyl in elderly patients indicates a decline in the rate of excretion of his kidneys. As a result, the half-life means increases, and also increases the sensitivity of receptors to it. Concomitant liver damage exacerbates the situation.

Use of the drug for these patients requires a careful selection of the dosage of fentanyl. Thus, the drug in applications begin to pick up from 12.5 g / h.

Contraindications

Fentanyl (instructions for use in vials or in the form of a TTS contains a full list of contraindications) are not recommended in the following cases:

• patients with hypersensitivity to the facility;
• persons with asthma;
• Patients with depression of the respiratory center in the medulla oblongata;
• patients with head injuries any gravity;
• persons suffering from drug addiction;
• obstetric anesthesia during operations;
• during pregnancy or breastfeeding.

Side effects

In response to the introduction of the drug may develop a number of undesirable effects.

These include:

• respiratory depression, hypoventilation condition;
• respiratory arrest;
• spasm of the bronchial tubes;
• paradoxical activation of the central nervous system;
• state of confusion, psychotic symptoms;
• convulsions;
• headaches and dizziness;
• increased intracranial pressure;
• blurred vision (blurred, double vision);
• transient appearance of muscular rigidity;
• decrease in heart rate;
• cardiac arrest;
• drop in blood pressure;
• nausea and vomiting;
• constipation, urinary retention;
• respiratory or allergic skin reactions;
• biliary colic (in patients with similar symptoms in the anamnesis).

When applications transdermal system may cause local skin reactions - itching, redness, rashes of various kinds. These symptoms disappear within a day after the removal of the patch from the skin.

Overdose

Overdose develops in case of hypersensitivity to the drug or the violation of his removal.

Manifestations include:

• general weakness;
• severe drowsiness;
• dizziness;
• pale skin;
• clammy sweat on the skin;
• pupillary constriction (miosis);
• drop in blood pressure, heart rate slowing;
• expressed bradypnea;
• the absence of spontaneous breathing.

With the development of the symptoms the patient is administered an overdose of the drug-receptor antagonist (naloxone) as well as funds to support the basic functions of the body:

• atropine for bradycardia development;
• muscle relaxants, translation ventilated in violation of spontaneous breathing;
• infusion liquid at sharp pressure drop to replenish blood volume.

special instructions

Given the pronounced systemic effect of the drug and a high probability of adverse effects, should be approached with caution to his appointment.

There are a number of recommendations and guidance on selection and continuation of therapy:

• Fentanyl is approved for use in hospitals under the supervision of staff. It is necessary to carefully monitor the possible adverse effects.
• Appointment neyroleptanalgezii possible only in a hospital with the possibility of rapid transfer of the patient on a ventilator.
• Use of the drug in any form of release - the indication to stop breastfeeding.
• Fentanyl affect the results of a study on the lipase and amylase. A blood test taken for 2-4 hours prior to the receiving means after 1 day after injection.
• In patients with low weight on the background of a continuous infusion or by repeated use may more prolonged effect of the drug.
• Spasm of the sphincter of Oddi during therapy prevents qualitative visualization of hepatic biliary tract, if necessary, radionuclide studies. This fact is taken into account to correct diagnostic procedure time.
• Fentanyl patch is not recommended for the relief of pain in the postoperative period because of the complexity and the impossibility of selecting the dosage adequate control of breathing function in a patient.
• Use of the drug in women of reproductive age needs careful protection to prevent pregnancy.
• The drug is in the form of a TTS should not be prescribed to the elderly, children under 2 years of age, patients with gross brain damage, impaired consciousness, respiratory depression when, kidney and liver failure.

  

• Persons receiving Fentanyl should be excluded from activities requiring attention and quick switching speed reactions, in hazardous or dangerous conditions (road management, work with mechanisms for adjustment work, depth).
• Patients using patches with the drug should not be heated space applications (including heaters, exploring baths or saunas, sun exposure).

Compatible with alcohol

Fentanyl has a depressant effect on the nervous system. Concomitant use of alcohol is forbidden, as the risk grows hypoventilation, development of bradycardia, drop in blood pressure.

drug interactions

When using the drug on a background of surgical intervention or therapy appointment, should have information about what other means the patient takes, and that may be imposed in the near future time. This will allow to calculate all the possible drug interactions of fentanyl.

• The simultaneous use of fenotiazidnymi antipsychotics, tricyclic antidepressants, opioids, tranquillizers, hypnotics and sedatives, undesirable frequency increases effects. The patient may suffer from the respiratory disorders, drop in blood pressure, inhibition of consciousness.
• Nitrous oxide enhances overall muscle rigidity.
• The use of benzodiazepine tranquilizers in the background neyroleptanalgezii leads to a longer way out of this state.
• drugs of beta-blockers (used to control hypertension) during therapy with Fentanyl increase the likelihood of severe bradycardia.
• Antagonists means Naltrexone, Naloxone reduce its analgesic effect and eliminate the inhibitory effect on the medulla oblongata. It helps to remove the inhibitory effect of the drug on the respiratory center.
• Antidepressants, monoamine oxidase inhibitors groups increase the risk of severe complications.
• Use of the drug in patients receiving insulin, requires the correction of its dosage downwards.

Where can I buy

The drug is available in the network of pharmacies on prescription only established form, which can be obtained with a doctor on a residence, an oncologist at the decision of the medical commission. Not in time otovarennye recipes need to return the expert who wrote them. Unused funds must be disposed of in the prescribed manner.

The estimated cost of the drug package is:

• Fentanyl solution for injection - 2 ml ampoule, № 5 - 80 rubles;
• Fentanyl transdermal therapeutic system - from 1500 to 3300 rubles per pack of 5 sachets, depending on the dosage of the substance.

Storage conditions

The drug should be stored no longer than 4 years from date of manufacture at temperatures up to 23 degrees, in the dark and protected from children and incapacitated persons place.

analogs

Information on potential analogues of the drug may be useful for patients. These tables contain information about medications that can help with the pain syndrome of different severity.

drug Name	The mechanism of action and composition	How to apply	Efficiency and price 1 package
Paracetamol	Tablets for oral administration. The active substance - paracetamol. Blocking COX-1, COX-2, providing a central analgesic action, decreasing body temperature	The drug is prescribed for relief of pain associated with trauma, menstruation, headaches. The drug is recommended for controlling fever in infectious diseases. Approved for infants, elderly patients. pregnant women.	The drug is effective against pain syndrome weak or moderate severity The cost of packaging 10 tablets of 500 mg of the preparation is from 14 rubles.
Thermo ketonal	Plaster with a warming effect. Active ingredient: ketoprofen - inhibitor of COX-1, COX-2.	Patch is indicated for the relief of pain in the muscles, it is used in uncomfortable sensation in the back, shoulders. Used only for adult patients. Should not be prescribed to women during pregnancy and lactation.	The drug is effective in reducing low-grade pain, it helps to relax the muscles of the back or shoulders. 10 sachets cost about 800 rubles.
Panoksen	Tablets containing a combination of two non-steroidal antiinflammatory and analgesic agents - paracetamol and sodium diclofenac	It recommended for the treatment of pain associated with various acute and chronic diseases in patients older than 18 years. The drug is banned for the treatment of specific categories of people - pregnant and lactating women, patients with severe heart, liver or kidney problems.	The drug has proven effective against pain of average severity. The cost of the package of 20 tablets is about 138 rubles.

Drug Fentanyl in ampoules administered during surgery in children and adults. It is contraindicated for obstetric interventions and is not recommended for the appointment of persons with brain lesions. Instructions for use of the drug warns about the possible development of addiction on the background of long-term administration.

Author: Irina Sizov

Registration of the article: Mila Friedan

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