Фентанила цитрат
Фентанила цитрат Uses, Dosage, Side Effects, Food Interaction and all others data.
Фентанила цитрат is an opioid analgesic. Фентанила цитрат interacts predominately with the opioid mu-receptor but also binds to kappa and delta-type opioid receptors. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, Фентанила цитрат exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Фентанила цитрат may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Фентанила цитрат depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Фентанила цитрат produces strong analgesia through its activation of opioid receptors. It has a duration of action of several hours and a wider therapeutic index as patients develop tolerance to opioids. Фентанила цитрат is associated with a risk of addiction and abuse and should not be mixed with alcohol or benzodiazepines.
Trade Name | Фентанила цитрат |
Availability | Prescription only |
Generic | Fentanyl |
Fentanyl Other Names | Fentanil, Fentanila, Fentanilo, Fentanyl, Fentanyl CII, Fentanylum, Phentanyl |
Related Drugs | Buprenex, Subutex, aspirin, acetaminophen, tramadol, trazodone, duloxetine, hydroxyzine, naproxen, Tylenol |
Type | |
Formula | C22H28N2O |
Weight | Average: 336.4705 Monoisotopic: 336.220163528 |
Protein binding | Fentanyl is 80-85% bound to plasma proteins. In one study, a 0.1µg/L solution of fentanyl was 77.9±1.1% bound to human serum albumin and 12.0±5.4% bound to α-1 acid glycoprotein. A 0.1µg/L solution of norfentanyl, the primary metabolite of fentanyl, was 7.62±1.2% bound to human serum albumin and 7.24±1.9% bound to α-1 acid glycoprotein. |
Groups | Approved, Illicit, Investigational, Vet approved |
Therapeutic Class | Opioid analgesics |
Manufacturer | |
Available Country | Russia |
Last Updated: | September 19, 2023 at 7:00 am |
![Фентанила цитрат Фентанила цитрат](https://www.medicinesfaq.com/media/png/fentanila-citrat.png)
Uses
Фентанила цитрат is used for the management of breakthrough pain in patients with cancer who are already receiving and who are tolerant to opioid therapy for their underlying persistent cancer pain. Patients considered opioid tolerant are those who are taking at least 60 mg of oral morphine/day, at least 25 mcg of transdermal Фентанила цитрат/hour, at least 30 mg of oxycodone daily, at least 8 mg of oral hydromorphone daily or an equianalgesic dose of another opioid for a week or longer.
Фентанила цитрат is also used to associated treatment for these conditions: Cancer Related Pain (Breakthrough Pain), Severe, Chronic Pain, Anesthetic premedication therapy, Anesthetics Agent, General Anesthesia, Induction of anesthesia therapy, Maintenance of anesthesia therapy, Regional Anesthesia, Preanesthetic medication therapy
How Фентанила цитрат works
Фентанила цитрат binds to opioid receptors, especially the mu opioid receptor, which are coupled to G-proteins. Activation of opioid receptors causes GTP to be exchanged for GDP on the G-proteins which in turn down regulates adenylate cyclase, reducing concentrations of cAMP. Reduced cAMP decreases cAMP dependant influx of calcium ions into the cell. The exchange of GTP for GDP results in hyperpolarization of the cell and inhibition of nerve activity.
Dosage
Фентанила цитрат dosage
Oral-
- Starting Dose:The initial dose of Фентанила цитрат should be 100 mcg.
- Re-dosing patients within a single episode: Dosing may be repeated once during a single episode of breakthrough pain if pain is not adequately relieved by one Фентанила цитрат dose. Re-dosing may occur 30 minutes after the start of administration of Фентанила цитрат and the same dosage strength should be used.
- Increasing the dose: Titration should be initiated using multiples of the 100 mcg Фентанила цитрат tablet. Patients require to titrate above 100 mcg can be instructed to use two 100 mcg tablets (one on each side of the mouth in the buccal cavity). If this dose is not successful in controlling the breakthrough pain episode, the patient may be instructed to place two 100 mcg tablets on each side of the mouth in the buccal cavity (total of four 100 mcg tablets). Titrate above 400 mcg by 200 mcg increments bearing in mind using more than 4 tablets simultaneously has not been studied and it is important to minimize the number of strengths available to patients at any time to prevent confusion and possible overdose. To reduce the risk of overdose during titration, patients should have only one strength of Фентанила цитрат tablet available at any one time.
- Dosage Adjustment:Generally, the dose of Фентанила цитрат should be increased when patients require more than one dose per breakthrough pain episode for several consecutive episodes.
Injection-
- Фентанила цитрат injection can be administered intravenously either as a bolus or by infusion & by intramuscular route also. The dose of fentanyl should be individualized according to age, body weight, physical status, underlying pathological condition, use of other drugs and type of surgery and anesthesia.
- Doses in excess of 200mcg are for use in anesthesia only. As a premedicant, 1-2 ml fentanyl may be given intramuscularly 45 minutes before induction of anesthesia. After IV administration in unpremedicated adult patients, 2ml fentanyl may be expected to provide sufficient analgesia for 10-20 minutes in surgical procedures involving low pain intensity. 10 ml fentanyl injected as a bolus gives analgesia lasting about one hour. The analgesia produced is sufficient for surgery involving moderately painful procedures. Giving a dose of 50mcglkg fentanyl will provide intense analgesia for some four to six hours, for intensely stimulating surgery.
- Фентанила цитрат may also be given as an infusion. In ventilated patients, a loading dose of fentanyl may be given as a fast infusion of approximately 1 mcg/kg/min for the first 10 minutes followed by an infusion of approximately 0.1 mcg/kg/min. Alternatively the loading dose of fentanyl may be given as a bolus. Infusion rates should be titrated to individual patient response; lower infusion rates may be adequate. Unless it is planned to ventilate post operatively, the infusion should be terminated at about 40 minutes before the end of surgery.
- Lower infusion rates, e.g. 0.05-0.08 mcg/kg/min. are necessary if spontaneous ventilation .is to be maintained. Higher infusion rates (up to 3 mcg/kg/min) have been used in cardiac surgery. Фентанила цитрат is chemically incompatible with the induction agents thiopentone & methohexitone because of wide differences in pH
- Use in elderly and debilitated patients: It is wise to reduce the dosage in the elderly and debilitated patients. The effect of the initial dose should be taken into account in determining supplemental doses.
Transdermal-
Intractable chronic pain:
- Adult:Patches deliver fentanyl in doses that range from: 12-100 mcg/hr. Doses should be individually titrated based on previous use of opioids. Opioid-naive patients: Initially, ≤25 mcg/hr; it is recommended to initially titrate w/ low doses of short-acting opioids before starting fentanyl patches. Patients receiving a strong opioid analgesic: Initial dose should be based on the previous 24-hr opioid requirements. During transfer to fentanyl patches, previous opioid treatment should be phased out gradually. If patient requires doses >100 mcg/hr, >1 patch may be used; consider alternative or additional therapy if doses >300 mcg/hr are required. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days.
- Elderly:Dose reduction may be needed.
Tablet Administration: Patients should remove the tablet from the blister strip and immediately place the entire tablet in the buccal cavity (above a rear molar, between the upper cheek and gum). Patients should not attempt to split the tablet. The tablet should not be chewed or swallowed, as this will result in lower plasma concentrations than when taken as directed. The tablet should be left between the cheek and gum until it has disintegrated, which usually takes approximately 14-25 minutes. After 30 minutes, if remnants from the tablet remain, they may be swallowed with a glass of water.
Side Effects
As with other narcotic analgesics, the most common serious adverse reactions reported to occur with Фентанила цитрат are respiratory depression, apnoea, muscular rigidity, myoclonic movements, and bradycardia. Respiratory depression is more likely to occur with intravenous administration if a dose is given too rapidly and it rarely occurs with intramuscular administration.
Toxicity
Фентанила цитрат has an intravenous LD50 of 2.91mg/kg in rats, an oral LD50 of 18mg/kg in rats and 368mg/kg in mice. The LD50 in humans is not known.
Symptoms of overdose include respiratory depression, somnolence, stupor, coma, skeletal muscle flaccidity, cold and clammy skin, pupillary constriction, pulmonary edema, bradycardia, hypotension, airway obstruction, atypical snoring, and death. In case of overdose, patients should receive naloxone or nalmefene to reverse the action of the opioids as well as supportive measures to maintain the airway or advanced life support in the case of cardiac arrest.
Precaution
Opioid analgesics impair the mental and/or physical ability required for the performance of potentially dangerous tasks (e.g. driving a car or operating machinery). Patients taking Фентанила цитрат should be warned of these dangers and should be counseled accordingly. The use of concomitant CNS active drugs requires special patient care and observation.
Chronic pulmonary disease: Фентанила цитрат should be titrated with caution in patients with chronic obstructive pulmonary disease or pre-existing medical conditions predisposing them to respiratory depression.
Head injuries and increased intracranial pressure: Opioids may obscure the clinical course of a patient with a head injury and should be used only if clinically warranted.
Cardiac disease: Intravenous Фентанила цитрат may produce bradycardia. Therefore, Фентанила цитрат should be used with caution in patients with bradyarrhythmias.
Hepatic or renal disease: Фентанила цитрат should be used with caution because of the hepatic metabolism and renal excretion of Фентанила цитрат.
Interaction
Co-administration of different antifungals, macrolide antibiotics, CNS depressant drugs like ketoconazole, itraconazole, troleandomycin, clarithromycin, nelfinavir, and nefazadone may enhance or prolong the effects of Фентанила цитрат. The concomitant use of amprenavir, aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, and verapamil with Фентанила цитрат may also result in an increase in Фентанила цитрат plasma concentrations, which could increase or prolong adverse drug effects and may cause potentially fatal respiratory depression.
Food Interaction
- Avoid alcohol.
[Major] GENERALLY AVOID: Alcohol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics including fentanyl.
Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.
In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.
GENERALLY AVOID: Consumption of grapefruit juice during treatment with oral transmucosal formulations of fentanyl may result in increased plasma concentrations of fentanyl, which is primarily metabolized by CYP450 3A4 isoenzyme in the liver and intestine.
Certain compounds present in grapefruit are known to inhibit CYP450 3A4 and may increase the bioavailability of swallowed fentanyl (reportedly up to 75% of a dose) and The clinical significance is unknown. In 12 healthy volunteers, consumption of 250 mL regular-strength grapefruit juice the night before and 100 mL double-strength grapefruit juice one hour before administration of oral transmucosal fentanyl citrate (600 or 800 mcg lozenge) did not significantly affect fentanyl pharmacokinetics, overall extent of fentanyl-induced miosis (miosis AUC), or subjective self-assessment of various clinical effects compared to control. However, pharmacokinetic alterations associated with interactions involving grapefruit juice are often subject to a high degree of interpatient variability. The possibility of significant interaction in some patients should be considered. Any history of alcohol or illicit drug use should be considered when prescribing fentanyl, and therapy initiated at a lower dosage if necessary. Patients should be closely monitored for signs and symptoms of sedation, respiratory depression, and hypotension. Due to a high degree of interpatient variability with respect to grapefruit juice interactions, patients treated with fentanyl should preferably avoid the consumption of grapefruit and grapefruit juice. In addition, patients receiving transdermal formulations of fentanyl should be cautioned that drug interactions and drug effects may be observed for a prolonged period beyond removal of the patch, as significant amounts of fentanyl are absorbed from the skin for 17 hours or more after the patch is removed.
MANAGEMENT: Patients should not consume alcoholic beverages or use drug products that contain alcohol during treatment with fentanyl.
Фентанила цитрат Drug Interaction
Major: zolpidem, zolpidem, lorazepam, lorazepam, duloxetine, duloxetine, hydromorphone, hydromorphone, pregabalin, pregabalin, acetaminophen / hydrocodone, acetaminophen / hydrocodone, alprazolam, alprazolam, ondansetron, ondansetronModerate: furosemide, furosemideUnknown: cholecalciferol, cholecalciferol
Фентанила цитрат Disease Interaction
Major: impaired GI motility, infectious diarrhea, liver disease, prematurity, acute alcohol intoxication, drug dependence, gastrointestinal obstruction, hypotension, intracranial pressure, respiratory depressionModerate: fever, adrenal insufficiency, biliary spasm, hypothyroidism, renal dysfunction, seizure disorders, urinary retention, arrhythmias
Volume of Distribution
The intravenous volume of distribution is 4L/kg (3-8L/kg). The oral volume of distribution is 25.4L/kg. In hepatically impaired patients, the intravenous volume of distribution ranges from 0.8-8L/kg.
Фентанила цитрат crosses the blood brain barrier and the placenta.
Elimination Route
Фентанила цитрат sublingual tablets are 54% bioavailable, transmucosal lozenges are 50% bioavailable, buccal tablets are 65% bioavailable, sublingual spray is 76% bioavailable, and nasal spray is 20% more bioavailable than transmucosal (or approximately 64% bioavailable).
Фентанила цитрат transmucosal lozenges reach a Cmax of 0.4±0.1ng/mL for a 200µg dose and 2.5±0.6ng/mL for a 1600µg dose with a Tmax of 20-40 minutes. The AUC was 172±96ng*min/mL for a 200µg dose and 1508±1360ng*min/mL for a 1600µg dose.
Фентанила цитрат sublingual spray reached a Cmax of 0.20±0.06ng/mL for a 100µg dose and 1.61±0.60ng/mL for an 800µg dose with a Tmax of 0.69-1.25 hours, decreasing as the dose increased. The AUC was 1.25±0.67ng*h/mL for a 100µg dose and 10.38±3.70ng*h/mL for a 800µg dose.
Фентанила цитрат transdermal systems reached a Cmax of 0.24±0.20ng/mL with a Tmax of 3.6±1.3h for a 25µg/h dose. The AUC was 0.42±0.35ng/mL*h.
Фентанила цитрат nasal spray reaches a Cmax of 815±301pg/mL with a Tmax of less than 1 hour for a 200µg/100µL dose. The AUC was 3772pg*h/mL.
Half Life
The half life of fentanyl is 7 hours. The half life of fentanyl sublingual spray is 5-12 hours.
Clearance
Total plasma clearance of fentanyl is 0.5L/hr/kg (0.3-0.7L/hr/kg) or 42L/hr. Following an intravenous dose, surgical patients displayed a clearance of 27-75L/h, hepatically impaired patients displayed a clearance of 3-80L/h, and renally impaired patients displayed a clearance of 30-78L/h.
Elimination Route
Within 72 hours, 75% of a dose of fentanyl is excreted in the urine with Label,15,19
Pregnancy & Breastfeeding use
Pregnancy category C. There are no adequate and well-controlled studies in pregnant women. Фентанила цитрат should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Фентанила цитрат is excreted in human milk; therefore Фентанила цитрат should not be used in nursing women because of the possibility of sedation and/or respiratory depression in their infants.
Contraindication
Фентанила цитрат is contraindicated in the management of acute or postoperative pain. Фентанила цитрат Citrate must not be used in opioid non-tolerant patients. Фентанила цитрат is contraindicated in patients with known intolerance or hypersensitivity to any of its components or the drug Фентанила цитрат.
Acute Overdose
In insufficient overdosage, Фентанила цитрат would produce narcosis, marked skeletal muscle rigidity. Cardio-respiratory depression and cyanosis may also occur. In the presence of hypoventilation or apnoea, oxygen should be administered and respiration should be assisted. A specific narcotic antagonist, such as naloxane, should be available for use as indicated to manage respiratory depression.
Storage Condition
Store between 20-25°C. Protect from light.
Innovators Monograph
You find simplified version here Фентанила цитрат
Фентанила цитрат contains Fentanyl see full prescribing information from innovator Фентанила цитрат Monograph, Фентанила цитрат MSDS, Фентанила цитрат FDA label
FAQ
What is Фентанила цитрат used for?
Фентанила цитрат used to treat patients with severe pain or to manage pain after surgery. Фентанила цитрат is also used as a recreational drug, sometimes mixed with heroin, cocaine, or methamphetamine, and its potentially deadly overdose effects can be neutralized by naloxone.
How safe is Фентанила цитрат?
Фентанила цитрат has a risk for abuse and addiction, which can lead to overdose and death. Фентанила цитрат may also cause severe, possibly fatal, breathing problems. Do not use transdermal patches unless you have been regularly using moderate to large amounts of opioid pain medication. Otherwise, it may cause overdose (even death).
How does Фентанила цитрат work?
Фентанила цитрат works by binding to the body's opioid receptors, which are found in areas of the brain that control pain and emotions. Its effects include extreme happiness, drowsiness, nausea, confusion, constipation, sedation, tolerance, addiction, respiratory depression and arrest, unconsciousness, coma, and death.
What are the common side effects of Фентанила цитрат?
Common side effcets of Фентанила цитрат are include:
- drowsiness
- stomach pain
- gas
- heartburn
- weight loss
- difficulty urinating
- changes in vision
- anxiety
- depression
- unusual thinking
- unusual dreams
- difficulty falling asleep or staying asleep
- dry mouth
- sudden reddening of the face, neck, or upper chest
- uncontrollable shaking of a part of the body
- back pain
- chest pain
- pain, sores, or irritation in the mouth in the area where you placed the medication
- swelling of the hands, arms, feet, ankles, or lower legs
Is Фентанила цитрат safe during pregnancy?
Use of this Фентанила цитрат is not recommended unless the benefit outweighs the risk to the developing fetus.
Is Фентанила цитрат safe during breastfeeding?
Фентанила цитрат are usually small and are not expected to cause any adverse effects in breastfed infants.
Can I drink alcohol with Фентанила цитрат?
While using a Фентанила цитрат patch, you should avoid drinking alcohol. Alcohol and Фентанила цитрат will still interact with your system, regardless of the delivery method of the Фентанила цитрат. The same risks of mixing Фентанила цитрат and alcohol apply in the case of using a patch.
Can I drive after taking Фентанила цитрат?
You should not plan on driving or doing anything that requires you to be awake and alert right after you are treated with this medication.
How many time can I take Фентанила цитрат daily?
Do not use Фентанила цитрат more than four times a day.
How many time can I take Фентанила цитрат daily?
Yes. It does not have any side effects like acidity / gastritis if taken on empty stomach.
How long should Фентанила цитрат be administered?
Onset of action after IV administration of Фентанила цитрат is 3-5 minutes; duration of action is 30-60 minutes. Women should be observed closely for signs of adverse reaction and possible respiratory distress.
How long does Фентанила цитрат stay in my system?
Фентанила цитрат will usually show up on a urine test between 24-72 hours after last use. Hair tests can detect the drug for up to 3 months, and blood tests can detect it between 5 and 48 hours after use depending on the dose.
Who should not take Фентанила цитрат?
You should not use Фентанила цитрат unless you recently used opioid medicine and your body is tolerant to it (ask your doctor if you're not sure). Do not put a fentanyl skin patch on any person who does not have a personal prescription for this medicine. You should not use Фентанила цитрат if you are allergic to it, or if you have: severe asthma or other breathing problems; or a stomach or bowel obstruction (including paralytic ileus).
What happens if I miss a dose?
If you are using the skin patches on a schedule, apply the missed patch as soon as you remember. Continue wearing the patch for up to 72 hours and then apply a new one if needed for pain. Do not wear extra patches to make up a missed dose.
What happens if I overdose?
Seek emergency medical attention. A Фентанила цитрат overdose can be fatal, especially in a child or other person using the medicine without a prescription. Overdose symptoms may include slow breathing and heart rate, severe drowsiness, muscle weakness, cold and clammy skin, pinpoint pupils, and fainting.
Is Фентанила цитрат hard on the heart?
When someone uses an opioid like fentanyl chronically, it can lead to a condition called long Q-T syndrome, where the electrical conduction of the heart is slowed and the heart's natural rhythm is disrupted. This can even happen with short-term opioid use.
Can Фентанила цитрат affect my kidneys?
Direct and indirect effects of anesthesia and surgical stress can affect kidney function.
Can Фентанила цитрат affects my liver?
Although Фентанила цитрат has many serious side effects and has been implicated in deaths from overdose and inadvertent use, it has not been linked to cases of clinically apparent liver injury.
Will Фентанила цитрат affect my fertility?
Фентанила цитрат generally has been shown to lower fertility in men.