What Is Sufentanil?

Mainly acts on opioid receptors. Used as an analgesic. Its lipophilicity is about twice that of fentanyl, it is easier to cross the blood-brain barrier, its plasma protein binding rate is higher than fentanyl, and its distribution volume is smaller than fentanyl. Although its elimination half-life is shorter than fentanyl, but Because it has a stronger affinity for opiate receptors than fentanyl, it not only has greater analgesic intensity, but also lasts longer (about twice as much as fentanyl). Sufentanil undergoes extensive biotransformation in the liver to form N-dehydrocarbyl and O-desmethyl metabolites, which are excreted through the kidneys. Among them, norsufentanil has pharmacological activity, and its potency is about 1/10 of that of sufentanil, which is equivalent to fentanyl, which is one of the reasons for the long duration of sufentanil. ^[1]

Mainly acts on opioid receptors. Used as an analgesic. Its lipophilicity is about twice that of fentanyl, it is easier to cross the blood-brain barrier, its plasma protein binding rate is higher than fentanyl, and its distribution volume is smaller than fentanyl. Although its elimination half-life is shorter than fentanyl, but Because it has a stronger affinity for opiate receptors than fentanyl, it not only has greater analgesic intensity, but also lasts longer (about twice as much as fentanyl). Sufentanil undergoes extensive biotransformation in the liver to form N-dehydrocarbyl and O-desmethyl metabolites, which are excreted through the kidneys. Among them, norsufentanil has pharmacological activity, and its potency is about 1/10 of that of sufentanil, which is equivalent to fentanyl, which is one of the reasons for the long duration of sufentanil. ^[1]

Sufentanil compounds

This product mainly acts on opioid receptors. Its lipophilicity is about twice that of fentanyl, it is easier to cross the blood-brain barrier, its plasma protein binding rate is higher than fentanyl, and its distribution volume is smaller than fentanyl. Although its elimination half-life is shorter than fentanyl, but Because it has a stronger affinity for opiate receptors than fentanyl, it not only has greater analgesic intensity, but also lasts longer (about twice as much as fentanyl). Sufentanil undergoes extensive biotransformation in the liver to form N-dehydrocarbyl and O-desmethyl metabolites, which are excreted through the kidneys. Among them, norsufentanil has pharmacological activity, and its potency is about 1/10 of that of sufentanil, which is equivalent to fentanyl, which is one of the reasons for the long duration of sufentanil.

Sufentanil Basic Information

Chinese name

English name: sufentanil

English alias: Chronogesic; Sufentanilum; UNII-AFE2YW0IIZ; SUFENTANIL; Sulfentanil;

CAS number: 56030-54-7

Molecular formula: C ₂₂ H ₃₀ N ₂ O ₂ S

Molecular weight: 386.55100

Exact mass: 386.20300

PSA: 61.02000

LogP: 4.15270

Sufentanil physical and chemical properties

Density: 1.132g / cm ³

Melting point: 96.6ºC

Boiling point: 493.1ºC at 760mmHg

Flash point: 252ºC

Refractive index: 1.576 ^[2]

Sufentanil related drug label information

Sufentanil Classification Name

Primary classification: Nervous system drugs Second classification: Analgesics Third classification: Strong analgesics

Sufentanil drug English name

Sufentanil

Sufentanil drug alias

Thioperaniline, Sufentanil, Neofentanil, Thifenol, Sufentanyl, Sufenta

Sufentanil drug dosage form

Injection (powder): 50 g, 100 g, 250 g.

Sufentanil pharmacological effects

This product is a benzidine derivative with structure and function similar to fentanyl. Its citrate is used clinically under the trade name Sufenta. 1. This product is a powerful narcotic analgesic. Its analgesic effect is about 5-10 times stronger than fentanyl. When the dose reaches 8 g / kg, deep anesthesia can be produced. Mainly acts on receptors. 2. Compared with fentanyl, this product has a faster onset of effect and faster recovery from anesthesia and ventilation inhibition.

Sufentanil Pharmacokinetics

This product works quickly after injection, but its duration is short. It can quickly redistribute from the brain and other tissues to adipose tissue, and the final elimination of t1 / 2 is about 2.5h. The plasma protein binding rate is 92.5%, which is mainly metabolized in the liver and small intestine. 80% of the amount was excreted within 24 hours.

Sufentanil indication

1. Used as an analgesic during general anesthesia. 2. When auxiliary ventilation is needed, this product is used as the main anesthetic.

Sufentanil contraindications

Those who are allergic to this product are prohibited.

Sufentanil notes

Patients with respiratory diseases and liver and kidney dysfunction should be used with caution and should not be used in the delivery process.

Sufentanil adverse reactions

1. Similar to fentanyl, it can cause respiratory depression, sphincter spasm, and skeletal muscle rigidity. 2. Occasionally nausea, vomiting, bronchospasm, tachycardia, arrhythmia, itching, and erythema. 3. Long-term application can be addictive.

Sufentanil dosage

1. Anesthesia-assisted analgesia: those with anesthesia for about 2 hours, 1 2g / kg; those with anesthesia for about 2-8h, 2 8g / kg 2. Anesthesia induction or maintenance anesthesia: 10-30 g / kg, given in divided doses. An initial dose of 2 to 5 g / kg usually causes loss of consciousness.

Sufentanil Drug Interactions

See also: Fentanyl

Sufentanil drug evaluation

Clinically, it is not commonly used as an analgesic for severe pain. Used as the main drug for intravenous compound anesthesia, or analgesics to assist anesthesia. ^[3]

Sufentanil citrate

This product is N- [4- (methoxymethyl) -l- [2- (2-thienyl) ethyl] -4-piperidinyl] propionanilide citrate. 0% Based on dry product calculation, including C22H 3 () N 2 0 2 SC 6 H 80 7

Sufentanil Traits

This product is white or off-white crystalline powder.

This product is easily soluble in methanol, soluble in ethanol or water, and slightly soluble in acetone or chloroform. Melting point The melting point of this product is 137 ~ 143 ° C (general rule 0612). It melts and decomposes at the same time.

Sufentanil identification

(1) Take about 5mg of this product, add an appropriate amount of water to dissolve, add 1 to 2 drops of phosphotungstic acid test solution, and a white precipitate will precipitate.

(2) The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 1320).

(3) Identification of citrate in aqueous solution of this product (General Rule 0301).

Sufentanil check

5 The acidity of this product 0.2 g, add 20ml of water to dissolve, determined according to law (general rule 0631), p H value should be 3. 5 ~ 4.5. The clarity and color of the solution shall be 0.1 g, and 10 ml of water shall be added to dissolve the solution. The solution shall be clear and colorless; if it is turbid, compare it with No. 1 turbidity standard solution (General Rule 0902, the first method), and it shall not be more concentrated; Compared with yellow standard colorimetric liquid No. 1 (General Rule 0901, the first method), the color must not be deeper. Take cyanide 1. Og of this product, check according to law (General Rule 0806 second method), including

Cyanide must not exceed five parts per million.

Relevant substances: Take this product, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 7.5 mg per lml, as the test solution; take 1ml precisely, place in a 100ml volumetric flask, and use the mobile phase. Dilute to the mark as the control solution; take another

An appropriate amount of citric acid was added to dissolve and dilute the mobile phase to make a solution containing about 2.5 mg per 1 ml, as a blank solution. Measured according to high performance liquid chromatography (General Rule 0512), using octadecylsilane bonded silica as filler (Thermo ODS-2 HYPER-SIL C18, 4.6 mm x 2 50 mm, 5 ^ m or equivalent) Chromatographic column); Methanol-0. 13mol / L ammonium acetate solution-acetonitrile (45:31:24), adjust the pH value with glacial acetic acid or ammonia to 1.1 as the mobile phase; detection wavelength is 228nm; the column temperature is

40 ° C. Take about 10 mg of sufentanil citrate, add 10 ml of dilute hydrochloric acid to dissolve, heat and reflux for 4 hours on a water bath, adjust to neutrality with a dilute sodium hydroxide test solution, evaporate to dryness in the water bath, let cool, add 10 ml Dissolve the residue in methanol, filter, and take 1 ml of the filtrate, place it in a 10 ml volumetric flask, and dilute to the mark with mobile phase as the system suitability solution. Measure the solution 10 1 into a liquid chromatograph and record the chromatogram. The resolution of the sulfentanyl peak and the degradation impurity peak (relative retention time is about 0.5) should be greater than 10. Precisely measure 10 ^ x1 of each of the control solution, test solution and blank solution, and inject them into the liquid chromatograph respectively. Record the chromatogram to 4 times the peak retention time of the main component. If there are impurity peaks in the chromatogram of the test solution, except for the chromatographic peaks at the same position as the blank solution, the area of a single impurity peak must not be greater than 0.5 times (0.5%) the area of the main peak of the control solution. Greater than the area of the main peak of the control solution (1.0%).

Residual solvents: ethyl acetate, acetone, isopropanol, and methanol. Take about 1 lg of this product, weigh it accurately, put it in a 10 ml volumetric flask, add appropriate amount of water to dissolve and dilute to the mark, shake well, and use it as the test solution Another ethyl acetate, acetone, isopropanol and

Methanol, precisely weighed, and quantitatively diluted with water to make a solution containing about 0.5 mg of ethyl acetate, 0.5 mg of acetone, 0.5 mg of isopropanol, and 0.3 mg of methanol per lml as a reference solution . Precisely measure 2 ml each of the two solutions, place them in a headspace bottle, and seal. Measured according to the residual solvent measurement method (General Rule 0861, the first method). A capillary column with modified polyethylene glycol (or similar polarity) as the fixed liquid is used as the column; 5 0 C, the detector temperature is 2 5 0 1. The headspace bottle has an equilibration temperature of 70 ° C and an equilibration time of 20 minutes. Take the reference solution headspace sample, the theoretical plate number calculated based on the acetone peak is not less than 1000, the resolution between each peak should meet the requirements. Then take the reference solution and the test solution separately for headspace injection and record the chromatogram. The peak area is calculated according to the external standard method, and the residual amounts should meet the requirements.

Carbon tetrachloride was taken from lg and accurately weighed, placed in a 10 ml measuring bottle, and an appropriate amount of iV, iV-dimethylformamide was added to dissolve and dilute to the mark, as a test solution; take another tetrachloride Carbon amount, accurately weighed, determined with N, N-dimethylformamide

The amount of dilution was made into a solution containing about 0.4 pg per lm l as a reference solution. Accurately measure 2ml each of the reference solution and the test solution, place them in a headspace bottle, and seal. According to the residual solvent determination method (General Rule 0861, the second method), a capillary column with 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polarity) as the fixed liquid is used as the chromatographic column. The column temperature was 40 ° C, maintained for 5 minutes, and heated to 240 ° C at a rate of 5 ° C per minute; the inlet temperature was 150 ° C, and the electron capture detector was used, and the temperature was 400X :. The headspace bottle equilibrium temperature is 70 ° C, and the equilibration time is 20 minutes. D Take the reference solution and the test solution separately and inject them into the headspace to record the chromatogram. The peak area is calculated according to the external standard method, and the residual amount should meet the requirements.

Take this product after losing weight and dry it under reduced pressure at 60 ° C to constant weight. The weight loss should not exceed 0.5% (General Rule 0831).

1% (General Rule 0841).

Take 1.0g of this product, add 23ml of water to dissolve it, add 2ml of acetate buffer solution (pH 3.5), and check according to law (General Rule 0821, the first method). The content of heavy metals must not exceed 20 parts per million.

Determination of Sufentanil

Take 0.5g of this product, accurately weigh, add 30ml of glacial acetic acid to dissolve, add 3 drops of naphthol methanol indicator, titrate with perchloric acid titration solution (0.1 lmol / L) to yellow-green, and titrate the results Calibration with blank test, that is. Each 1 ml of chloric acid titration solution (0.1 mol / L) is equivalent to 57. 87 mg of C 2 2 H 3 0 N 2 O 2 S · Ce Hg O 7.

Sufentanil Categories

Analgesics.

Sufentanil storage

Shaded and sealed.

Sufentanil

Sufentanil citrate injection. ^[4]