Durogesic - Instructions For Using The Patch, Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Durogesic

Durogesic: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Durogesic

ATX code: N02AB03

Active ingredient: fentanyl (fentanyl)

Producer: Janssen Pharmaceutica NV (Belgium)

Description and photo update: 2019-26-08

Durogesic is a drug with an analgesic effect.

Release form and composition

Durogesic is produced in the form of a transdermal therapeutic system (TTS): a rectangular plaster with rounded corners, translucent, hermetically sealed, contains a transparent gel; the presence of crystalline particles and air bubbles is allowed in the gel; inscriptions on the outer shell: 0.025 mg / h - pink, 0.05 mg / h - light green, 0.075 mg / h - blue, 0.1 mg / h - gray (1 pc. in bags of combined material, 5 bags in a cardboard box).

1 system includes:

• Active ingredient: fentanyl - 2.5 mg, 5 mg, 7.5 mg or 10 mg;
• Auxiliary components: hydroxyethyl cellulose, ethyl alcohol, purified water.

The composition of the functional layers of the patch:

• Outer protective shell: copolymer of ethylene vinyl acetate and polyester;
• Reservoir: ethanol (0.1 ml / 10 cm ²) and fentanyl (2.5 mg / 10 cm ²) in the form of an aqueous gel based on hydroxyethyl cellulose;
• Releasing membrane: ethylene vinyl acetate (controls the rate of release of the active substance);
• Silicone adhesive coated with a protective release film: polyester and fluorocarbon diacrylate.

Pharmacological properties

Pharmacodynamics

Durogesic is a topical opioid analgesic. Fentanyl belongs to synthetic analgesics and interacts mainly with μ-opioid receptors. The drug is included in the list II of narcotic drugs, psychotropic drugs and their precursors, approved by the Decree of the Government of the Russian Federation No. 681 of June 30, 1998. It activates the activity of the antinociceptive system and increases the pain threshold. Fentanyl prevents the transmission of excitation along nonspecific and specific pain pathways to the amygdala complex and the nuclei of the hypothalamus and thalamus.

Durogesic has a predominantly analgesic and sedative effect. Fentanyl inhibits the work of the respiratory center, stimulates the vomiting center and the centers located in the vagus nerve. It increases the tone of the smooth muscles of the sphincters (including the sphincter of Oddi, bladder, urethra) and biliary tract, improves water absorption in the gastrointestinal tract, and suppresses intestinal peristalsis. The drug provides a decrease in renal blood flow and does not have a clinically significant effect on blood pressure, and also increases the level of lipase and amylase in the blood.

Fentanyl is characterized by a pronounced hypnotic effect. He also provokes a state of euphoria.

Drug dependence and tolerance to the analgesic effect of Durogesic develop at different rates, which are determined by significant individual variations.

Pharmacokinetics

The minimum analgesic concentration of fentanyl, at which the therapeutic effect is manifested, in patients who have not previously been prescribed opioid analgesics, varies from 0.3 to 1.5 ng / ml. The use of a transdermal therapeutic system promotes a continuous systemic release of fentanyl for 72 hours after application. The release of the active substance Durogesic is carried out at a relatively constant rate, determined by the properties of the copolymer membrane and the diffusion of fentanyl through the skin. After using Durogesic, the content of fentanyl in blood plasma gradually increases during the first 12-24 hours and remains relatively stable over the remaining period of time. The concentration of a substance in blood plasma is directly proportional to the size of the TTS.

Repeated applications lead to the achievement of an equilibrium concentration of fentanyl in the blood plasma, which can be maintained by the following applications of TTS of a similar size. The content of fractions of the active component of Durogesic in plasma, which remain unbound with blood plasma proteins, averages 13–21%. Fentanyl is determined in breast milk.

After removal of TTS, the level of fentanyl in the blood plasma gradually decreases, the half-life is on average 17 hours (the range of variation is 13-22 hours). The absorption of the active substance from the skin continues for a certain period of time (this effect is observed to a greater extent after the 4th application), which causes the slow elimination of the drug from the blood plasma.

Fentanyl is metabolized primarily in the liver through its participation in hydroxylation and N-dealkylation processes, as well as in the adrenal glands, kidneys and intestines.

Approximately 75% of the ingested dose of fentanyl is excreted in the urine, mainly in the form of metabolites that do not have pharmacological activity. In this case, less than 10% of the active substance is excreted unchanged. Approximately 9% of the drug is excreted in the faeces, mainly as metabolites.

In debilitated or malnourished patients, as well as in elderly patients, the clearance of fentanyl may decrease, which leads to an increase in the half-life. Since fentanyl is metabolized in the liver with the formation of inactive metabolites, liver diseases often delay drug elimination from the body. In patients with cirrhosis of the liver, with a single application of Durogesic, no significant change in pharmacokinetic parameters was observed, however, there was a tendency to an increase in the level of fentanyl in the blood plasma.

Information obtained from intravenous administration of fentanyl to patients with renal insufficiency allows us to make an assumption about a possible change in the volume of distribution of fentanyl during hemodialysis, which may contribute to a change in the concentration of the active component in blood plasma.

The results of studies that examined the pharmacokinetic parameters of Durogesic in elderly patients confirm the absence of significant differences from the pharmacokinetic parameters in young patients, although the content of fentanyl in the serum of elderly patients was slightly higher.

The pharmacokinetic model of the drug suggests that serum fentanyl concentrations may increase by about one third when body temperature rises to 40 ° C.

Indications for use

According to the instructions, Durogesic is prescribed for chronic pain syndrome of moderate to severe severity, including:

• Pain associated with cancer;
• Pain syndromes of non-oncological etiology requiring anesthesia with narcotic analgesics: neuropathic pain (with shingles (Herpes zoster), syringomyelia, diabetic polyneuropathy, multiple sclerosis, nerve injuries), phantom pain associated with limb amputation.

Contraindications

Absolute:

• Depression of the respiratory center;
• Irritated, irradiated, or damaged skin;
• Acute and / or postoperative pain requiring a short period of therapy;
• Age under 18;
• Pregnancy and lactation;
• Hypersensitivity to drug components.

Relative (Durogesic should be used with caution):

• Chronic lung disease;
• Increased intracranial pressure, incl. with brain tumors;
• Bradyarrhythmias;
• Arterial hypotension;
• Hepatic and renal failure;
• Acute surgical diseases of the abdominal organs (before the diagnosis is established);
• History of hepatic colic;
• Caesarean section and other obstetric operations (before fetal extraction);
• Simultaneous use with insulin, glucocorticosteroids and antihypertensive drugs;
• Elderly age.

Instructions for the use of Durogesic: method and dosage

Durogesic is used topically. TTS should be applied to a completely dry, flat surface of the skin of the upper arms or trunk. It is recommended to choose a place with the smallest hairline for application. The hair at the application site must be cut (do not shave off). If, before using Durogesic, the application site needs to be washed, this should be done with clean water without using soap, lotions, oils or other agents, as they can lead to skin irritation or a change in its properties.

You need to stick the plaster Durogesic immediately after removing it from the sealed bag. Press the TTS at the application site firmly with your palm for 30 seconds. Make sure the patch fits snugly against the skin, especially around the edges.

Durogesic is designed for 72 hours of continuous use. The new system can be applied to another area of the skin after removing the previously applied patch. On one and the same area of skin, TTS can be glued only with a break of several days.

The dose of the drug is selected individually, depending on the patient's condition (it must be re-evaluated after each TTS application).

When using Durogesic for the first time, the size of the system (dose) is selected based on the previous use of opioid analgesics, the patient's condition and the degree of tolerance. In patients who have not previously taken opioids, the lowest dose is prescribed as the initial dose - 0.025 mg / h. The same dose is used for patients who previously received Promedol.

When switching from parenteral or oral forms of opioids to Durogesic in patients with opioid tolerance, the dose is calculated individually.

The initial assessment of the maximum analgesic effect of the drug should not be carried out earlier than 24 hours after application, due to a gradual increase in serum fentanyl concentration.

For a successful transition from one drug to another, the previous analgesic treatment must be canceled gradually after the application of the initial dose of Durogesic.

If adequate pain relief is not achieved after application of the initial dose, the dose can be increased after 3 days. Further, it is possible to increase the dose every 3 days. At a time, the dose is usually increased by 0.025 mg / h, however, it is necessary to take into account the patient's condition and the need for additional anesthesia (a daily oral dose of morphine 90 mg approximately corresponds to a dose of Durogesic 0.025 mg / h). To achieve a dose greater than 0.1 mg / h, it is possible to use several TTS simultaneously. Occasionally, when "bursting" pain occurs, patients may require additional doses of short-acting analgesics. Some patients, when using a dose of Durogesic above 0.3 mg / h, may need additional or alternative methods of administration of opioid analgesics.

Side effects

• Nervous system: headache, depression, drowsiness, anxiety, confusion, hallucinations, anorexia; rarely - agitation, euphoria, tremors, insomnia, amnesia, paresthesia;
• Digestive system: vomiting, nausea, constipation, biliary colic (in patients with a history of indications), dyspepsia, dry mouth; rarely diarrhea;
• Respiratory system: hypoventilation, respiratory depression and bronchospasm (in case of overdose); in rare cases - shortness of breath;
• Local reactions: sometimes - skin rash, itching and erythema at the site of application (as a rule, they disappear on their own within 24 hours after removal of the TTS);
• Others: tachycardia, short-term muscle stiffness (including chest muscles), bradycardia, hypertension, decreased blood pressure, urinary retention, increased sweating, itching, tolerance, as well as physical and mental dependence; very rarely - sexual dysfunction, asthenia, "withdrawal syndrome".

When switching to Durogesic from previously taken narcotic analgesics or in cases of sudden cessation of treatment, symptoms that are characteristic of opioid withdrawal are possible (manifested in the form of nausea, vomiting, diarrhea, anxiety, chills). A gradual dose reduction helps to reduce the severity of these symptoms.

Overdose

Symptoms of an overdose of Durogesic include bradycardia, decreased blood pressure, apnea, bradypnea, depression of the respiratory center, muscle rigidity. In this case, the TTS is immediately removed and verbal and physical stimulation is carried out (the patient must be called by name, patted on the cheeks). If necessary, carry out auxiliary and artificial ventilation. A specific antidote is also introduced - naloxone. When fentanyl is ingested in high doses, respiratory depression may be longer than the time period during which this opioid receptor antagonist acts, therefore, in some cases, re-administration of naloxone is required.

Supportive and symptomatic therapy should be prescribed, including mechanical ventilation (artificial ventilation of the lungs), the introduction of muscle relaxants, the replenishment of the circulating blood volume with a decrease in blood pressure, the introduction of atropine for bradycardia. Termination of the analgesic effect can provoke a sharp painful attack and lead to the release of catecholamines into the blood.

special instructions

Durogesic is prescribed with caution in the presence of the following diseases / conditions:

• Chronic lung diseases: against the background of chronic obstructive and other lung diseases, Durogesic can lead to the development of a number of severe side effects (in the form of a decrease in the excitability of the respiratory center and an increase in breathing resistance);
• Increased intracranial pressure: patients who are especially sensitive to an increase in CO2 content, Durogesic should be prescribed with caution. The risk group includes patients with increased intracranial pressure, impaired consciousness and patients in a coma. The drug is prescribed with caution for brain tumors;
• Cardiovascular diseases: due to the likelihood of developing bradycardia, caution requires the use of TTS in patients with bradyarrhythmias and arterial hypotension;
• Liver diseases: it is necessary to carefully monitor the condition of patients with liver pathologies, since such diseases can lead to a delay in the excretion of the active substance; if symptoms of fentanyl overdose appear, a dose reduction is required;
• History of hepatic colic: Durogesic can increase the tone of the smooth muscles of the biliary tract and gastrointestinal tract, therefore, such patients need careful monitoring;
• Kidney disease: in case of renal failure, careful monitoring of the condition of patients is necessary; when symptoms of an overdose of an active substance appear, the dose of the drug should be reduced;
• Elderly age: due to the risk of a decrease in the clearance of fentanyl and an extension of its half-life, as well as the likelihood of hypersensitivity to the action of the drug, the condition of elderly patients requires careful monitoring; if symptoms of an overdose with an active substance appear, the dose of Durogesic should be reduced;
• Respiratory depression: Some patients, due to the likelihood of developing significant respiratory depression, need careful examination in order to detect such effects. After removal of the TTS, respiratory depression may continue;
• Drug dependence: In cases of repeated use of opioids, tolerance and mental and physical dependence can develop. Iatrogenic dependence during Durogesic therapy is rare;
• Fever / External Heat: As the body temperature rises to 40 ° C, the concentration of fentanyl increases, so patients with fever need to be closely monitored for side effects associated with opioids. If necessary, the dose of Durogesic is adjusted. Patients are advised to avoid direct exposure to external heat sources at the site of the TTS application (heating lamps, intense sunbathing, heating pads, saunas, hot water baths, etc.).

The condition of patients who have experienced the development of severe side effects should be carefully monitored, since the concentration of fentanyl in plasma decreases gradually.

Durogesic patches should not be divided into parts, cut or damaged in any way, as this can lead to uncontrolled release of fentanyl.

If it is necessary to stop therapy, the replacement of Durogesic with other opioids should be carried out gradually, starting with low doses. To prevent the development of "withdrawal syndrome", opioid analgesia should be withdrawn gradually.

Influence on the ability to drive vehicles and complex mechanisms

Since Durogesic can affect the physical and / or mental functions necessary when performing potentially hazardous work (including driving or working with equipment), it is recommended to refrain from participating in them during the period of therapy.

Application during pregnancy and lactation

Information on the use of Durogesic in pregnant women is considered insufficient. It should not be prescribed during pregnancy, except in cases of urgent need.

The use of the drug during labor is contraindicated because fentanyl crosses the placental barrier and can lead to depression of the respiratory center in the newborn.

Fentanyl is found in breast milk and is sedative and can cause breathing problems in babies. In this regard, it is not recommended to use it during lactation.

Pediatric use

For children and adolescents under the age of 18, Durogesic is not prescribed.

With impaired renal function

Patients with renal insufficiency should take the drug with caution.

For violations of liver function

Patients with hepatic impairment should take the drug with caution.

Use in the elderly

Elderly patients should be careful when using Durogesic.

Drug interactions

With the simultaneous use of Durogesic with some drugs, the following effects may occur:

• Other drugs that have a depressing effect on the central nervous system, including opioids, hypnotics and sedatives, phenothiazines, general anesthetics, central muscle relaxants, tranquilizers, sedative antihistamines, alcoholic beverages: increased risk of developing and increasing hypoventilation, lowering arterial pressure, excessive sedation (joint therapy requires special monitoring of the patient's condition);
• Potential inhibitors of cytochrome P ₄₅₀ CYP3A4 (ritonavir): an increase in the concentration of fentanyl in plasma, which increases the likelihood of increasing or prolonging the therapeutic effect and the occurrence of side effects (the combination is not recommended);
• Nitrous oxide: increased muscle rigidity;
• Buprenorphine: reducing the effect of Durogesic;
• Monoamine oxidase inhibitors: increased risk of severe complications.

When used together with insulin, glucocorticosteroids and antihypertensive drugs, it is necessary to reduce the dose of fentanyl.

Analogs

Analogs of Durogezik are: Lunaldin, Fendivia, Dolforin, Fentadol Reservoir, Fentadol Matrix, Dolforin, Durogesic Matrix.

Terms and conditions of storage

Keep out of reach of children at a temperature of 15-25 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Durogesic

Basically, the network provides positive reviews about Durogesic. Patients report ease of use and effective and long-term (the effect of the drug lasts up to 3 days) relief of pain attacks, which significantly improves the quality of life. This method of pain relief is psychologically more acceptable for many patients in comparison with the injection of anesthetic drugs.

Patients who have previously taken oral morphine note that Durogesic is better tolerated. It also allows you to get rid of constipation, which is often a side reaction of taking morphine-containing drugs. However, the drug also has side effects, among which nausea and vomiting are most often mentioned, in isolated cases of constipation. Nausea usually goes away on its own within 5-7 days, but sometimes patients had to take antiemetics in small doses. Mental dependence does not develop when using the drug. Sometimes after the application of Durogesic, local allergic reactions are observed in the form of hyperemia, which disappears on its own or after taking antihistamines.

The price of Durogesic in pharmacies

The price of Durogesic at the moment remains unknown, since the drug is not available for sale.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!