Index of drugs

Chronic severe pain requiring the use of opioid drugs.

1 transdermal patch with an area of ​​3.75, 7.5, 15, 22.5 or 30 cm² contains 2.063 mg, 4.125 mg, 8.25 mg, 12.375 mg or 16.5 mg of fentanyl, corresponding to a release rate of fentanyl 12.5 μg / h, 25 μg / h, 50 μg / h, 75 μg / h or 100 μg / h.

A strong analgesic from the group of pure opioid receptor agonists. The main therapeutic activity is analgesia and sedation. The maximum effective analgesic concentration (MAC) is 0.3-1.5 ng / ml (in patients not previously treated with opioids). Side effects are more frequent after exceeding the 2 ng / ml concentration of fentanyl in the serum. With increasing tolerance to the drug (high individual variability) increases its MAC and concentrations at which side effects are intensifying. The preparation ensures that the first fentanyl system increases gradually until the skin reaches the equilibrium level between 12 and 24 hours after applying the first transdermal patch. The fentanyl concentration in the blood continues to be kept relatively constant for 72 h and depends on the surface of the applied transdermal patch. The concentration of fentanyl in the blood reaches steady state during the second 72-hour period of application and stays at this level during subsequent applications (if transdermal patches of the same size are used). Fentanyl is approximately 84% bound to plasma proteins. It is metabolised mainly in the liver with the participation of cytochrome P450 CYP3A4. The main metabolite - norfentanyl is inactive. Approximately 75% of the dose is excreted in the urine in the majority as metabolites, less than 10% excreted unchanged. About 9% of the dose is excreted in faeces, mainly in the form of metabolites. After removing the transdermal patch, the concentration of fentanyl in the blood decreases gradually reaching 50% of the baseline value after 13-22 h in adults or after 22-25 h in children. Elderly or weakened patients may have an extended half-life of the drug. In patients with renal or hepatic impairment, the clearance of fentanyl may change due to changes in the composition of plasma proteins, which leads to increased blood levels of the drug.

Hypersensitivity to fentanyl or any of the excipients used in the transdermal patch. acute pain (including postoperative). Severe functional disorders o.u.n. Concomitant use of MAO inhibitors or use within 14 days of discontinuation of MAO inhibitors. Do not use during delivery. Do not use in children under 2 years and in children who have not received opioid medicines before.

The drug should be used as part of the integral pain treatment in a patient adequately evaluated in terms of medical, social, and psychological. Caution should be exercised (monitoring the patient's condition or reducing the dose) in patients with: existing respiratory depression, lung diseases (eg with chronic obstructive pulmonary disease), increased intracranial pressure, consciousness disorders, coma, bradyarrhythmias, hypovolaemia, hypotension, disorders hepatic or renal function, high fever (accelerates absorption), myasthenia gravis, debilitated or elderly patients and those with a history of drug or alcohol addiction. The concentration of fentanyl in the blood decreases gradually after the removal of the transdermal patch, so patients who experience severe side effects (especially depression of the respiratory center) should be monitored for the Next 24 hours after removing the transdermal patch.

The safety of fentanyl in transdermal patches during pregnancy has not been established - the drug can only be used during pregnancy if it is absolutely necessary. Do not use during labor. Prolonged use in pregnancy may cause withdrawal symptoms in the newborn.The drug is excreted in breast milk and may cause sedation and respiratory depression in the breast-fed child - do not breast-feed while using the medicine and within 72 hours after removing the transdermal patch.

Very common: drowsiness, pain and dizziness, nausea, vomiting, constipation, sweating, pruritus. Common: confusion, depression, hallucinations, sedation, nervousness, loss of appetite, dry mouth, indigestion, skin reactions at the site of the transdermal patch. Uncommon: euphoria, amnesia, insomnia, agitation, tremor, paresthesia, speech disorders, tachycardia, bradycardia, hypertension, hypotension, dyspnoea, hypoventilation, diarrhea, rash, erythema, urinary retention. Rarely: arrhythmias, vasodilation, hiccups, swelling, feeling cold. Very rare: delusions, excitement, weakness, anxiety, sexual dysfunction, withdrawal symptoms, ataxia, convulsions (including clonic seizures and grand mal), amblyopia, respiratory depression, apnea, hemoptysis, pharyngitis, painful flatulence, intestinal obstruction , pain in the bladder, oliguria, anaphylaxis. In children and adolescents, the profile of side effects is similar to that seen in adults. The most common side effects in children are: fever, vomiting, nausea. During long-term use may develop tolerance to the drug and psychological and physical dependence. After the change of previously used opioids to fentanyl in the form of a transdermal patch or after abrupt discontinuation of treatment, withdrawal symptoms may occur (nausea, vomiting, diarrhea, anxiety, chills).

Individually based on the assessment of the general condition of the patient, diagnosis, current use of opioids, and the occurrence of tolerance to opioids.
The initial dose in adult patients who have not received strong opioids before should not exceed 25 μg / h. In opioid-treated patients (whether orally or parenterally), in the case of switching to a transdermally administered fentanyl drug, the daily dose used should be assessed (eg for morphine used orally, taking the dose of intramuscular to oral = 1: 3-1: 4), and then calculate the daily requirement for fentanyl by taking oral daily doses of morphine (MF in mg / day) and the corresponding dosage of Fentanyl-ratiopharm (F in μg / h): MF 0-44 = F 12.5; MF 45-134 = 25; MF 135-224 = F 50; MF 225-314 = F 75; MF 315-404 = F 100; MF 405-494 = F 125; MF 495-584 = F 150; MF 585-674 = F 175; MF 675-764 = F200; MF 765-854 = F 225; MF 855-944 = F 250; MF 945-1034 = F 275; MF 1035-1124 = F 300. For children over 2 years: MF 30-44 = F 12.5; MF 45-134 = 25. The conversion of doses of the preparation larger than 25 μg / h is the same for adults as well as for children. Data from clinical trials on children receiving morphine orally at doses> 90 mg / day are limited. Other conversion methods used in clinical practice may be used. Evaluation of the effect of the preparation can be made only after 24 h. During the first 12 hours after the change to Fentanyl-ratiopharm, the patient should continue to receive the previous painkiller at the current dose within the next 12 h - depending on the need. The transdermal patch should be changed every 72 hours. The dose should be increased individually until the analgesic effect is effective. If, at the end of the initial period of application of the transdermal patch, analgesia is insufficient, the dose can be increased after 3 days until the desired effect is achieved. Typically, the dose should be increased each time by 12-25 μg / h, taking into account the patient's need for additional analgesics. If a patient requires over 100 μg / h of fentanyl, several transdermal patches can be used simultaneously. Patients may require a short-acting analgesic to control the so-called "breakthrough pain". If the dose of the preparation exceeds 300 μg / h, additional or alternative methods of pain treatment should be considered.
The transdermal patch should be carefully attached to clean (purified water without the use of washing agents), dry, hairless (if need be cut, not shaved), unchanged (without irritation and radiation changes) flat skin of the torso or upper arms. The transdermal patch should be worn for 72 hours. Next, after removing the used one, stick it on another place (in the same place, the medicine can be applied after a 7-day break).Transdermal patches should not be divided.