Index of drugs

Treatment of breakthrough pain in adults who are on opioid maintenance therapy for chronic cancer pain. Breakthrough pain is a transient intensity of pain that appears on the background of otherwise controlled chronic pain. Patients receiving opioid maintenance are patients who take at least: 60 mg morphine oral / day, 25 μg fentanyl percutaneous / h, 30 mg oxycodone / day, 8 mg hydromorphone per oral / day or the corresponding dose of another opioid for one week or more.

1.8 ml of the solution contains 0.9 mg of fentanyl (as citrate), providing 10 doses of 50 μg of fentanyl. 2.9 ml of the solution contains 2.9 mg of fentanyl (as citrate), providing 20 doses of 100 μg of fentanyl. 5 ml of solution contains 10 mg of fentanyl (as citrate), provides delivery of 40 doses of 200 μg of fentanyl.

A strong analgesic from the group of pure opioid receptor agonists. Fentanyl is rapidly absorbed through the nasal mucosa, reaching C_max during 12-15 min; bioavailability is around 89%. About 80% of fentanyl is bound by plasma proteins. Fentanyl is metabolised primarily in the liver via CYP3A4; the main metabolite - norfentanyl, is inactive. About 75% of fentanyl is excreted in the urine, mainly in the form of inactive metabolites; about 9% of the dose is excreted in the faeces, mainly in the form of metabolites. T_0,5 is about 3-4 hours.

Hypersensitivity to the active substance or to any of the excipients. Use in patients who do not receive opioid maintenance because of the increased risk of respiratory depression. Treatment of acute pain other than breakthrough pain. Severe respiratory depression or severe obstructive pulmonary disease. Previous face radiotherapy. Repeated cases of nosebleeds.

After administration of fentanyl, clinically significant respiratory depression may occur, so patients should be monitored for their effects. In patients with long-term opioid pain, tolerance to respiratory depression develops, therefore the risk of respiratory depression in these patients is reduced. The concomitant use of CNS-inhibitory preparations may increase the risk of respiratory depression. In patients with COPD, fentanyl may cause more serious side effects. In these patients, opioids can reduce respiratory drive and increase respiratory resistance. Use with caution in patients with moderate or severe renal or hepatic impairment, signs of increased intracranial pressure, impaired consciousness, coma, brain tumor or head injury. In patients with previous or previously diagnosed bradyarrhythmias, fentanyl should be used with extreme caution (risk of bradycardia). Opioids can cause hypotension, especially in patients with hypovolaemia - use caution in patients with hypotonia and / or hypovolaemia. Potentially life-threatening serotonin syndrome can occur during simultaneous use with serotonergic drugs and with drugs that disturb the metabolism of serotonin. Serotonin syndrome may occur at the recommended doses. If a serotonin syndrome is suspected, treatment with the preparation should be discontinued. If the patient is experiencing recurrent nosebleeds or nasal discomfort while taking the product, a different route of administration for the treatment of breakthrough pain should be considered. The total range of exposure to fentanyl in people with frequent colds, previously untreated nasal vasoconstrictor drugs, is comparable to healthy people. Multiple opioids, such as fentanyl, may develop tolerance and physical and / or psychological dependence. The occurrence of discontinuation symptoms may be accelerated by the administration of opioid antagonists (e.g., naloxone) or a mixture of an analgesic agonist / antagonist (e.g.pentazocine, butorphanol, buprenorphine, nalbuphine). Caution should be exercised when treating elderly patients and those who are debilitated or weakened.

Do not use during pregnancy unless clearly necessary. Long-term treatment may result in withdrawal symptoms in an infant. Fentanyl should not be used during labor (including cesarean section) as it passes through the placenta and may cause fetal respiratory depression. When giving the preparation, easy access to the antidote appropriate for the child should be provided. Fentanyl passes into breast milk and may cause sedation and respiratory depression in the breast-fed infant. Fentanyl should not be used in breast-feeding women and breastfeeding should not be restarted for at least 5 days after the last administration of fentanyl.

Common: drowsiness, pain and dizziness, sudden redness (especially of the face), hot flushes, throat irritation, nausea, vomiting, excessive sweating. Uncommon: addiction, insomnia, sedation, muscle clonic convulsions, paresthesias, sensory disturbances, dysgeusia, kinetosis, hypotension, respiratory depression, epistaxis, nasal ulceration, watery nasal discharge, constipation, inflammation or dry mucous membrane oral, skin pain, pruritus, fever. Frequency unknown: hallucinations, convulsions, perforation of the nasal septum, diarrhea, fatigue, apathy, peripheral edema, withdrawal syndrome (nausea, vomiting, diarrhea, anxiety, chills, muscle tremors, excessive sweating), falls. The most serious side effects observed were: respiratory depression, cardiovascular depression, hypotension and shock, so all patients should be closely monitored for these symptoms.

Intranasally. Treatment should be started and used under the supervision of a doctor who has experience in opioid therapy in patients with cancer. One should remember about the possibility of abuse of fentanyl. Dosage of the drug should be determined individually for each patient, so that the administered dose provides adequate pain control, with tolerated levels of side effects. Patients should be closely monitored during dosing. Increasing the dose requires contact with the attending physician. In clinical studies, the dose of nasally administered fentanyl used to treat breakthrough pain was independent of the daily opioid maintenance dose.Dose setting. It can be started in patients who are expected to have chronic chronic pain controlled by long-term opioid therapy and who have no more than 4 episodes of breakthrough pain per day. The patient should wait at least 4 hours before the Next application in the next breakthrough pain bump, both during dose setting and maintenance treatment.The method of setting the dose. The initial dose should be 50 μg once to one nostril, if necessary, the dosage can be increased using the available doses (50 μg, 100 μg and 200 μg). If satisfactory pain relief is achieved after 10 min after 1 dose, the dose should be considered. If the effect is unsatisfactory, repeat the same dose (repeated use of the same dose may take place at the earliest after 10 minutes); the next higher dose should be considered at the next administration. Each stage of dose setting should be assessed in several attacks of transient pain.Maintenance treatment. Use the dose of the preparation determined in accordance with the above description. If pain relief is insufficient, repeated use of the same dose may occur at the earliest after 10 min.Dose adjustment. Typically, the maintenance dose of the formulation should be increased if the patient requires more than one dose of medication over several consecutive breakthrough pain episodes. The maximum daily dose: treatment for up to 4 episodes of breakthrough pain, in each no more than 2 doses, with an interval of at least 10 minutes. If the patient consistently has more than 4 episodes of breakthrough pain per day, it may be necessary to change the dosage of the primary opioid treatment. If the side effects are not tolerated or persist, the dose should be reduced or the treatment replaced with another pain medication.Discontinuation of treatment. The preparation should be discontinued immediately if the patient does not have breakthrough pain episodes. When all opioid therapies are required, the patient must remain under strict medical supervision, as to avoid severe withdrawal symptoms, a gradual reduction in the opioid dose is required.Special groups of patients. In clinical trials, elderly patients were less effective than patients under 65 years of age; Special care should be taken when setting the dose. Caution should be exercised when treating debilitated or debilitated patients and patients with moderate to severe hepatic or renal impairment. The safety and efficacy of the preparation in children below 18 years have not been established.Way of giving. The patient should sit or stand while holding the device in an upright position.