What Is Flunitrazepam?

Flunazepam, English name Flunitrazepam, alias flunitrozidine, Rohypnol, Darkene. Light yellow crystalline solid. Slightly soluble in water, easily soluble in ethanol.

Drug Name: Flunitrazepam
Alias: Flunitroazepam
Foreign name: F1unitrazepam

Whether prescription drugs: prescription
Main indications: Sedative hypnotics
Athletes use with caution: Use with caution

Basic information of Flunazepam

Chinese name: Flunazepam

Chinese alias: flunazepam

English name: Flunitrazepam

English alias: 5- (2-fluorophenyl) -1-methyl-7-nitro-3H-1,4-benzodiazepin-2-one; 5- (2-Fluorophenyl) -1-methyl-7-nitro-3H-1 , 4-benzodiazepin-2 (1H) -one Ro 5-4200; Rohypnol; Darkene

CAS number: 1622-62-4

Molecular formula: C ₁₆ H ₁₂ FN ₃ O ₃

Molecular weight: 313.28300

Exact mass: 313.08600

PSA: 78.49000

LogP: 2.57150

Physical and chemical properties

Density: 1.39g / cm ³

Melting point: 166-167ºC

Boiling point: 540.9ºC at 760mmHg

Flash point: 280.9ºC

Refractive index: 1.648

Storage conditions: 2-8ºC

Vapor pressure: 9.13E-12mmHg at 25 ° C ^[1]

Structural formula:

Flunitrazepam

Flunazepam Flunazepam Related Drug Product Information

Pharmacological effects of flunitrazepam

This drug is a benzodiazepine drug, which has hypnotic, forgetful, sedative, anxiolytic, muscle relaxation, and anticonvulsant effects, of which hypnotic and forgetfulness are more significant. Its pharmacological effects are similar to other benzodiazepines, and its sedative and hypnotic effects are stronger than nitrazepam and diazepam.

medicine interactions

1.Central inhibitory drugs such as antidepressants, antihistamines, general anesthetics, other sedative hypnotics, neuroleptics, and opioid analgesics will aggravate the sedative effect of this drug and affect the respiratory system and heart Inhibition of the vascular system. 2. When combined with Danshen, it can increase the central inhibitory effect of this medicine. 3. Angelica sinensis can inhibit the metabolism of benzodiazepines. When combined with this drug, it can cause excessive central inhibition, and can also cause excessive muscle relaxation. 4. Kfargan combined with this medicine can enhance the central inhibitory effect of this medicine. The two should be avoided. 5. Several components in Scutellaria baicalensis can compete with benzodiazepines to bind to GABA-A receptor binding sites and enhance central inhibition. 6. Valproic acid can slow down the metabolism of this drug. Patients taking valproic acid should use this drug with caution. 7. Cimetidine can inhibit the metabolism of the drug by the liver and prolong the half-life of the drug. 8. Some experiments have shown that intravenous injection of heparin sodium can reduce the binding rate of this drug to plasma proteins. 9. Theophylline can reduce the sedative effect of this medicine. 10. Excessive sedation and psychomotor damage may occur when this medicine is combined with alcohol. 11. Caffeine can reduce the sedative and anxiolytic effects of this medicine. 12. Food can reduce the speed and extent of absorption of this medicine.

Pharmacokinetics

Intramuscular injection and sublingual administration are well absorbed, and oral absorption is about 80% to 90%, while rectal suppositories are absorbed only 50%. Food reduces the speed and extent of absorption. Sedation occurs 20 to 30 minutes after oral or intramuscular injection. The maximum effect is achieved in 1 to 2 hours. The sedative effect of oral administration lasts 8 hours. Intravenous administration is effective for 1 to 3 minutes (loss of consciousness) when anesthesia is induced. The blood drug concentration reached a peak 1 to 2 hours after oral administration, and significant sedative and anxiolytic effects appeared when the plasma concentration was 7 to 8 ng / ml. The peak time for intramuscular injection is 30 to 45 minutes, while the peak time for intranasal administration is 41 to 185 minutes (increased with increasing dose). The protein has a protein binding rate of 78% to 80%, can be distributed in tissues and cerebrospinal fluid, and can penetrate the placenta. Its distribution volume is 3.3 ~ 5.5L / kg. Metabolized mainly in the liver. The total clearance rate was 94 ml per minute, and the clearance rate for children 3 to 10 years old was 8 to 12 ml / kg per minute. Can be secreted into milk, but the concentration is lower than the maternal plasma concentration. Most are excreted in the form of metabolites through urine, and about 10% are excreted in feces. The elimination half-life of the parent compound is 16-35h. The elimination half-life of newborns and infants decreases significantly with age, and the elimination half-life of children is 12 h. Because the drug is quickly distributed to the tissue, the sedative effect is not related to the elimination half-life.

Dosage form and specifications

Tablet: 1mg, 2mg; 2. Injection (powder): 2mg.

Flunitrazepam indications

For sedation and various insomnia before surgery. Can also be used as an intravenous anesthetic (single or induced anesthesia).

Fenazepam contraindications

1. People who are allergic to this medicine and nitrazepam. 2. Pregnant and lactating women. 3. Patients with acute angle closure glaucoma. 4. Patients with myasthenia gravis

Precautions for flunitrazepam

1. Use with caution: (1) aged and debilitated; (2) infants and young children; (3) patients with organic damage to the brain; (4) patients with heart, liver, and kidney disease. 2. Do not drive, engage in high-altitude operations, or operate machines after taking medication.

Flunazepam adverse reactions

The adverse reactions of this drug are similar to other benzodiazepines, and are mild at normal doses. Gastrointestinal reactions such as thirst, appetite, diarrhea, abdominal pain, constipation, and allergic reactions such as rash and flushing may occur; sometimes reactions such as excitement, confusion, dizziness, and headache; Most patients have mild respiratory depression and reports of cardiac arrest. Occasionally dependence at high doses, abnormal clinical test values of liver and kidney function (such as SGOT, SGPT, LPH, BUN increase, etc.). There have been cases of overuse that have caused loss of consciousness. Animal overdose tests have proven that this drug is teratogenic.

Flunazepam usage and dosage

1. Oral administration: Hypnosis: The commonly used amount is 0.5 1mg, which can be increased to 2mg before bedtime. Intravenous injection, induced anesthesia: slow intravenous injection, the usual amount is 1 ~ 2mg or calculated by weight (0.015 ~ 0.030mg / kg). 3. Intramuscular injection: pre-operative administration: commonly used amount is 1-2mg or calculated by weight (0.015-0.030mg / kg).

Efficacy Evaluation of Flunazepam

This product is worse than diazepam when used for induction of anesthesia, but it is not as good as thiopental. Patients can have long sleepiness after surgery, so it is not suitable for routine induction, especially for shorter surgery ^[2] .