What Is Fentanyl?

Fentanyl, suitable for all kinds of pain and analgesia after surgery and gynecology, etc .; also used to prevent or reduce delirium after surgery; can also be used in combination with anesthesia as an anesthetic aid; and with fluoride Piperidol is formulated as a "sedative analgesic" for use in large-area dressing changes and minor analgesia.

On April 1, 2019, the Ministry of Public Security, the National Health and Health Commission, and the State Drug Administration jointly issued an announcement announcing that fentanyls would be included in the "Non-medicine anesthetics and psychotropic substances" from May 1, 2019. Supplementary Catalogue of Controlled Varieties. ^[1]

Drug Name: Fentanyl
Drug type: Essential medicines

English name: Fentanyl
English alias: Fentanest; Fentanil; Sublimaze

Fentanyl chemical name

N- [l- (2-phenethyl) -4-piperidinyl] -N-phenylpropionamide

Fentanyl molecular structure

Fentanyl Formula

C22H28N20

Fentanyl molecular weight

336

Physical and chemical properties of fentanyl

Its citrate is commonly used as a white crystalline powder with a bitter taste and an acidic reaction in aqueous solution. Easily soluble in hot isopropanol, soluble in methanol, slightly soluble in water or chloroform. It has a melting point of 150 to 153 ° C and decomposes at the same time when melting.

Fentanyl Pharmacology

It is an opioid receptor agonist. It is a potent narcotic analgesic with a pharmacological effect similar to morphine. Animal experiments show that its analgesic effect is about 80 times that of morphine. The analgesic effect is rapid, but the duration is short. It takes effect 1 minute after intravenous injection, reaches a peak in 4 minutes, and maintains the effect for 30 minutes. The effect is about 7 minutes after intramuscular injection, and it is maintained for about 1 to 2 hours. This product is weaker in respiratory depression than morphine and has less adverse reactions than morphine.

Fentanyl indications

It is suitable for various pains and analgesia after surgery and gynecological surgery. It is also used to prevent or reduce delirium after surgery. It can also be used in combination with anesthesia as an anesthetic aid; compatible with droperidol It can be used as an analgesic agent for large-area dressing change and minor analgesia.

Fentanyl usage and dosage

Due to different dosage forms and specifications, please read the drug instructions carefully or follow the doctor's advice.

Fentanyl adverse reactions

(1) Nausea and vomiting may occur in individual cases. After about 1 hour, it will relieve itself and cause blurred vision, itching and euphoria, but it is not obvious. (2) Use with caution in pregnant women and patients with arrhythmia. Bronchial asthma, respiratory depression, patients who are particularly sensitive to this product, and patients with myasthenia gravis are contraindicated.

Fentanyl Contraindications

Patches are contraindicated in patients with acute or postoperative pain who are not effective with non-opioid analgesics. Be used with caution in intracranial tumors, brain trauma, liver and kidney dysfunction, children or patients under the age of 18 who weigh less than 50 kg.

Fentanyl notes

(1) Intravenous injection may cause rigidity of the chest wall muscles. If it appears, muscle relaxants should be used to counteract it. Respiratory depression can also occur when the intravenous injection is too fast, and care should be taken. (2) Be alert for weak addiction. (3) When the patch is combined with other opioids and sedatives, the latter dose should be reduced by 1/3. (4) The patch should be used in small doses, and the specifications above 50µg are only used for patients who have tolerated opioid therapy. (5) This medicine is irritating. Avoid applying on the skin and mucous membrane surface or entering the trachea.

Fentanyl drug interactions

(1) It should not be combined with monoamine oxidase inhibitors (such as phenelzine, pagiline, etc.). (2) Central inhibitors such as barbiturates, tranquilizers, and anesthetics can enhance the effect of fentanyl. If used in combination, the dose of this product should be reduced by 1/4 to 1/3. (3) Combination with ritonavir increases the toxicity of fentanyl. (4) Combination with M choline receptor blockers (especially atropine) makes constipation worse and increases the risk of paralytic intestinal obstruction and urinary retention. (5) Serotonin syndrome occurred in combination with sibutramine. (6) Competing with naltrexone for opioid receptors, causing acute opioid withdrawal symptoms. (7) Respiratory suppression and analgesic effects of naloxone and allyl morphinyl. (8) Severe hypotension may occur in combination with calcium antagonists and -adrenergic receptor blockers.

Fentanyl

Injection: 2ml: 0.1mg

Fentanyl Pharmacopeia Introduction

[Identification] (1) Take about 0.1g of this product, add 5ml of water to dissolve, add 10ml of trinitrophenol test solution, stir, that will precipitate out, filter, filter the residue and wash it a little bit with water. After drying at 105 , according to the law As determined (Appendix VI C), the melting point was 173 ~ 176 ° C. (2) The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 266). (3) Identification of citrate in aqueous solution (Appendix III). [Inspection] Take this product, add mobile phase to dissolve and dilute it to make a solution containing about 0.4mg per 1ml as the test solution; take N-phenyl-1- (2-phenethyl) piperidine An appropriate amount of -4-amine (impurity I) reference substance is added to the mobile phase to dissolve and make a solution containing 0.4mg per lml as the reference solution; the precise amount is to take 1ml of the test solution and 1ml of the reference solution, and set to 200ml. In the bottle, dilute to the mark with the mobile phase, shake well, and use it as a control solution; take another amount of citric acid, add the mobile phase to dissolve and dilute to make a solution containing 0.15mg per 1ml, and use it as a blank solution. Tested according to high performance liquid chromatography (Appendix VD), using octadecylsilane bonded silica as a filler; a solution containing 0.1% anhydrous sodium sulfate and 0.2% ammonium acetate-methanol-acetonitrile (4: 3: 1 ) (Adjust the pH to 6.3 ± 0.1 with glacial acetic acid) as the mobile phase; the detection wavelength is 220 nm; the column temperature is 30 ° C. The order of the peaks is impurity I and fentanyl. The resolution between the two peaks should be greater than 5. The number of theoretical plates calculated based on the fentanyl peak is not less than 3000. Take 50µl of the control solution and inject it into the liquid chromatograph. Adjust the detection sensitivity so that the peak height of the fentanyl chromatographic peak is about 10% of the full scale. Then accurately measure 50l of each of the test solution, control solution and blank solution, and inject them into the liquid chromatograph respectively, and record the chromatogram to twice the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak should not be greater than 0.5 times (0.25%) of the fentanyl peak area of the control solution, except for the chromatographic peaks at the same position as the blank solution. The sum of N and N must not be greater than the area of the fentanyl peak in the control solution (0.5%). Any peak that is less than 0.1 times the area of the fentanyl peak in the control solution chromatogram can be ignored. Loss on drying Take this product and dry it to constant weight at 105 ° C. Lose weight should not exceed 0.5% (Appendix L). The ignition residue shall not exceed 0.2% (Appendix N). Take 1.0g of this product, add 2ml of acetate buffer solution (pH3.5), mix well, and add an appropriate amount of water to dissolve it into 25ml. Check according to the law (Appendix H the first method). Twenty. [Content determination] Take about 0.5g of this product, weigh it accurately, add 15ml of glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, titrate with perchloric acid titration solution (0.1mol / L) until it is green, and The titration results are corrected with a blank test. Each 1ml of perchloric acid titration solution (0.1mol / L) is equivalent to 52.86mg of C22H28N20·C4H807. [Category] Analgesics. [Storage] Keep sealed.

^[2] ^[3] ^[4] ^[5]