Index of drugs

The use of the preparation is indicated for the management of breakthrough pain (BTP) in adults who receive maintenance opioid therapy in chronic cancer pain. Breakthrough pain is a transient intensity of pain that occurs on the background of otherwise controlled chronic pain. Patients receiving opioid maintenance therapy are patients who are treated orally with at least 60 mg morphine per day, at least 25 μg / h transdermal fentanyl, at least 30 mg oxycodone per day, orally with at least 8 mg hydromorphone per day or an equivalent dose of another opioid for one week or longer.

1.55 ml of solution contains 1.55 mg of fentanyl (as citrate), which allows for 8 full sprays of 100 μg. 1.55 ml of the solution contains 6.2 mg of fentanyl (as citrate), which allows administration of 8 full sprays of 400 μg of fentanyl. The preparation contains propyl parahydroxybenzoate.

Opioid analgesic with affinity for opioid μ receptors. His main activities are the elimination of pain and calmness. Secondary pharmacological effects of fentanyl are: respiratory depression, bradycardia, hypothermia, constipation, miosis, physical dependence and euphoria. After a single intranasal dose, fentanyl is rapidly absorbed with the median T_max in the range of 15-21 min. Fentanyl is a highly lipophilic substance and is well distributed outside the blood system. The results of animal studies indicate that after absorption, fentanyl is rapidly distributed to the brain, heart, lungs, kidneys and spleen, and then subject to slower redistribution to muscle and adipose tissue. 80-85% of fentanyl is bound to plasma proteins. Fentanyl is metabolised in the liver via CYP3A4 to norfentanyl (inactive). It is eliminated in over 90% by biotransformation to N-dealkylated and hydroxylated inactive metabolites. Less than 7% of the administered dose of fentanyl is excreted unchanged in the urine. Approx. 1% of the dose is eliminated unchanged with faeces. Metabolites are mainly excreted in the urine, whereas excretion in the faeces plays a smaller role.

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. Severe respiratory depression or severe obstructive pulmonary disease. Treatment of acute pain, other than breakthrough pain.

Patients and their carers should be advised that the preparation contains the active ingredient in an amount that can be fatal to the child. It is important to stabilize the long-term treatment with opioids used to treat the patient before starting treatment. There is a clinically significant risk of respiratory depression due to the use of fentanyl. Patients with pain treated with opioids develop tolerance to respiratory depression, therefore the risk of respiratory depression in these patients is reduced. Simultaneous use of inhibitory preparations on o.u.n. may increase the risk of respiratory depression. In patients with chronic obstructive pulmonary disease, fentanyl may cause more serious side effects. In these patients, opioids can reduce respiratory drive and increase respiratory resistance. The preparation should be used with particular caution in patients who may be particularly sensitive to the central CO-retention effect₂such as people with increased intracranial pressure or with consciousness disorders. Opioids may obscure the clinical picture in patients with head injuries and should only be used if necessary for clinical reasons. Fentanyl can cause bradycardia. Patients with pre-existing or previously diagnosed bradyarrhythmias should be used with extreme caution. The preparation should be used with caution in patients with renal or hepatic impairment. Special care should be taken in patients with hypovolaemia and hypotension.When multiple opioids such as fentanyl are given, tolerance may develop. However, cases of iatrogenic dependence as a result of the use of opioids in treatment are rare. 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. Caution should be exercised when co-administered with agents that affect serotoninergic neurotransmitter systems. Potentially life-threatening serotonin syndrome may occur when used concomitantly with serotonergic drugs, such as selective serotonin reuptake inhibitors (SSRIs), serotonin and noradrenaline reuptake inhibitors (SNRIs), and drugs that interfere with serotonin metabolism (including MAO inhibitors). This can occur at the recommended doses. If a serotonin syndrome is suspected, treatment with the preparation should be discontinued. Caution should be exercised when using the preparation in elderly patients. The safety and efficacy of the preparation in children under 18 have not yet been established. The preparation contains propyl para-hydroxybenzoate, which in some patients may cause allergic reactions (probably delayed) and in exceptional cases, bronchospasm (in the case of incorrect administration of the preparation).

It should not be used during pregnancy unless clearly necessary. As a result of long-term treatment, fentanyl may cause 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 should be provided easy access toantidote suitable for a child. Fentanyl passes into breast milk and may cause sedation and respiratory depression in the breast-fed baby. Fentanyl should not be used during breastfeeding; you should not breastfeed within 48 hours of the last administration of fentanyl.

Common: confusion, taste disturbances, dizziness, drowsiness, headache, nosebleeds, watery runny nose, discomfort in the nose, vomiting, nausea, constipation, pruritus. Uncommon: pneumonia, nasopharyngitis, pharyngitis, rhinitis, neutropenia, hypersensitivity, dehydration, hyperglycemia, decreased appetite, increased appetite, drug abuse, delirium, hallucinations, confusion, depression, attention deficit hyperactivity disorder attention deficit, anxiety, euphoric mood, nervousness, loss of consciousness, reduced level of consciousness, convulsions, lack of taste, lack of smell, memory disorders, angina, speech disorders, sedation, apathy, tremor, diarrheal headache, cyanosis, cardiac insufficiency vascular edema, lymphedema, hypotonia, hot flushes, upper airway obstruction, throat-laryngeal pain, nasal pain, nasal mucosal disorders, cough, dyspnea, sneezing, upper respiratory tract congestion, nasal congestion, hypnotesis of the nasal cavity, irritation throat, flowing secretion on the back of the throat, dry nose, intestinal perforation, peritonitis, hypoaesthesia, impaired mouth, diarrhea, retching, abdominal pain, language disorders, mouth ulcer, indigestion, dry mouth, excessive sweating, urticaria, joint pain, muscle tremor, anuria, dysuria, proteinuria, difficulty urinating, vaginal haemorrhage, chest pain of non-cardiac origin, asthenia, chills, facial swelling, peripheral edema, gait disturbances, fever, fatigue, malaise, thirst, decreased platelet count, weight gain, falls, intentional abnormal use of medication, abnormal treatment. Not known: blush, respiratory depression.

Intranasally. Adults. Treatment should be started and used under the supervision of a physician experienced in conducting opioid therapy in patients with cancer. The dose of the preparation should be determined individually to obtain an "effective" dose, which will provide for two consecutive episodes of pain that pierces adequate pain control with minimal side effects, without excessive (or unacceptable) side effects.The effectiveness of the administered dose should be assessed after 30 min. Until an effective dose is achieved, patients should be carefully observed. 1 dose can be 1 spray (100 μg or 400 μg) or 2 spray (200 μg or 800 μg) at the same dose (100 μg or 400 μg). Patients should not take more than 4 doses per day. The starting dose for the treatment of breakthrough pain episodes is always 100 μg (1 spray), even if the patient has previously been used to treat breakthrough pain with other fentanyl containing medicines. Patients should wait at least 4 hours before using the product again to treat breakthrough pain. Patients in whom the initial dose (100 μg) is ineffective may apply during the Next episode of breakthrough pain 2 pulses of 100 μg (one for each nostril). If this dose is ineffective, the patient may take one dose of 400 μg (1 spray of 400 μg / dose) for the next episode of pain. If the dose used turns out to be ineffective, the patient should be instructed to increase the dose to 2 sprays of 400 micrograms (one for each nostril). From the start of treatment, patients should be carefully monitored and the dose should be determined until the effective dose is confirmed and confirmed during two consecutive breakthrough pain episodes. When determining the dose in patients switching from preparations containing immediate-release fentanyl, it is very important to reconstitute the dose with the new formulation and not to administer the same dose (in μg). When the effective dose is determined during its setting, patients should continue to take this dose up to a maximum of 4 doses per day. In principle, the maintenance dose should only be increased if the dose used does not provide adequate control of breakthrough pain over the next few episodes. If the patient has more than 4 episodes of breakthrough pain within 24 h, it may be necessary to assess the dose of opioids used to control basic pain. If the side effects are unacceptable or of a chronic nature, the dose should be reduced or the preparation replaced with another painkiller. Stop using the medicine immediately if the patient does not have breakthrough pain episodes. When all opioid therapies are required, the patient must remain under close medical supervision, as to avoid severe withdrawal symptoms, a gradual reduction in the opioid dose is required. Use caution when adjusting the dose in patients with moderate or severe hepatic or renal impairment.
The preparation is intended for nasal administration only. Drops of the sprayed product form a gel in the nose - patients should avoid blowing out the nose immediately after administration.