Index of drugs

Treatment of breakthrough pain in adult patients using opioid therapy in chronic cancer pain. Breakthrough pain is a temporary worsening of controlled chronic primary pain.

1 tabl sublingual contains 100 μg, 200 μg, 300 μg, 400 μg, 600 μg, 800 μg of fentanyl (as citrate).

Opioid analgesic with strong affinity for the μ-opioid receptor. The onset of action is rapid and the analgesic effect is short. Fentanyl causes dose-dependent respiratory depression. The risk is higher in patients who have not previously taken opioids than in patients using long-term opioid therapy. Long-term treatment with opioids leads most often to the development of tolerance to their side effects. Fentanyl is a highly lipophilic drug very quickly absorbed through the oral mucosa (bioavailability is about 70%), reaching C_max after 22.5-240 min after administration. The absorption from further parts of the digestive tract is slower. After oral administration, the liver and intestines are clearly affected by the first pass. About 80-85% is bound to plasma proteins. It is mainly metabolised by CYP3A4 to pharmacologically inactive metabolites. It is excreted mainly in urine (approximately 75% of the dose), mainly in the form of metabolites, with less than 10% of the drug excreted unchanged. About 9% of the dose is excreted in the faeces, mainly in the form of metabolites. The total plasma clearance of fentanyl is approximately 0.5 l / h / kg. T_0,5 in the elimination phase it is about 7h (3-12.5 h), and the final T_0,5 is about 20 hours (11.5-25 hours).

Hypersensitivity to fentanyl or other ingredients. Respiratory depression and obstructive pulmonary diseases. It is not recommended for patients who have not previously received opioids due to the increased risk of life-threatening respiratory depression.

The preparation is not recommended for use in children and adolescents under 18 years of age due to lack of data on safety and efficacy. Use with particular caution (especially when choosing a dose) in patients with chronic obstructive pulmonary disease or other conditions predisposing them to respiratory depression (eg myasthenia gravis); with bradyarrhythmia; in old age, debilitated or weakened; with impaired liver or kidney function; with hypovolaemia and hypotonia; prone to intracranial hypercapnia. In patients with head injuries, the clinical course can be masked by the use of opioids; in this case, opioids can only be used if absolutely necessary. The product has not been studied in patients with oral cavity or oral mucositis - there is an increased risk of side effects of fentanyl in these patients and therefore caution is advised when choosing a dose.

Fentanyl can be used during pregnancy only when it is absolutely necessary. Long-term treatment during pregnancy may cause withdrawal symptoms in infants. It should not be used during labor (including cesarean section) as it crosses the placenta barrier and can dump respiratory depression in the fetus or newborn child. Fentanyl is excreted in human milk and may cause sedation or respiratory depression in a breast-fed child. The drug can be used during lactation, only in cases when the benefit for the mother is greater than the potential risk to the child.

The most serious adverse reactions characteristic of opioids are respiratory depression (which may lead to respiratory arrest), hypotension and shock. The side effects are listed below for both Lunaldin and other fentanyl-containing medicines. Very common: dizziness, drowsiness, headache, nausea, fatigue, excessive sweating.Common: vasovagal reaction, hypoaesthesia, paresthesia, hyperaesthesia, abnormal vision, respiratory depression, rhinitis, pharyngitis, vomiting, abdominal pain, diarrhea, constipation, discomfort in the stomach, dyspeptic symptoms, dry mouth, rash, pruritus, orthostatic hypotension, headache, flushing, asthenia, irritation of the drug application site, depression, anorexia, concentration disorders, euphoria, myoclonus, insomnia, taste disorders, gastrointestinal obstruction, dysphagia, oral ulcers / oral mucositis , language disorders, accidental injuries, vasodilatation, hallucinations, confusion, tension, nervousness, unusual thoughts, unusual dreams. Uncommon: bradycardia, tachycardia, hypertension, walking disorder / coordination, dizziness, amnesia, speech disorder, tremor, hypoventilation, asthma, shortness of breath, enlarged abdomen, flatulence, thirst, urinary retention, changes in frequency of urination , bad mood, agitation, loss of self-esteem, emotional instability. Rarely: hiccups. Very rare: arrhythmia, apnea, hemoptysis, urinary incontinence, oliguria.
Long-term use of the drug may cause the development of tolerance to the drug and the occurrence of physical and mental dependence. Abrupt discontinuation of treatment may lead to withdrawal symptoms.

It should only be given to those patients who have experienced tolerance to opioid therapy for the relief of chronic cancer pain, that is, those who take at least 60 mg of morphine orally, 25 μg fentanyl administered percutaneously every 1 hour or the equivalent dose of another opioid for at least one one week. Change of other preparations containing fentanyl to Lunaldin can not take place in a 1: 1 ratio due to different absorption profiles. If another fentanyl-containing medicine is changed to Lunaldin, a new titration is required.Titration of the dose. The aim of the dose titration is to determine the optimal maintenance dose for the treatment of breakthrough pain episodes, which dose should provide adequate pain relief at an acceptable level of adverse reactions. The optimal dose of the drug will be determined by titration upwards for each patient individually. It is possible to use several doses during the titration phase. The initial dose of the preparation should be 100 μg, however, if necessary, it can be titrated up. Patients should be kept under strict control until the optimal dose is reached. If, after a dose of 100 μg, the pain relief is not achieved within 15-30 minutes of the administration of a single sublingual tablet, a supplementary (second) dose of 100 μg can be given. If the pain relief is not achieved within 15-30 minutes of the first dose, increase the dose to the Next higher available strength when the next breakthrough pain episode occurs. The dose should be increased gradually until the desired pain relief is achieved. The strength of the booster dose (second) sublingual tablet should be increased from 100 to 200 μg for doses of 400 μg and above. In the event of a single episode of breakthrough pain occurring during the titration phase of the drug, do not give more than 2 tablets. sublingual. When pain relief is achieved after a higher dose, but side effects can not be tolerated, an intermediate dose (using 100 μg sublingual tablets, as needed) can be used. Doses greater than 800 μg have not been evaluated in clinical trials.Maintenance therapy. Once the appropriate dose, which can be more than one tablet, has already been determined, patients should receive it continuously and limit themselves to taking up to four doses per day.Repeated titration. If the response (pain relief or side effects) to the titrated dose changes significantly, adjust the dose so that the most appropriate dose is maintained. If more than four episodes of breakthrough pain occur over a period of more than four consecutive days during the day, the dose of long-acting opioids should be adjusted again for chronic pain.If long-acting opioids or their doses have been altered, Lunaldin doses should be re-evaluated and titrated so as to provide the patient with the optimal dose.Discontinuation of treatment. For patients who no longer require opioid therapy, the dose should be carefully adjusted before the opioid titration down to minimize the possible withdrawal symptoms. In patients who are still under opioid therapy for chronic pain relief, but no longer require the use of anti-puncture agents, the usual treatment with the product may be discontinued immediately.
Sublingual tablets should be inserted deeply into the tongue. They should not be swallowed. Allow them to dissolve completely under the tongue without chewing or sucking them. Do not eat liquids and food until the tablet is completely dissolved. Patients with dry mouth are advised to wet the oral mucosa prior to taking the preparation.