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Home > Encyclopedia > Flurazepam hydrochloride

Flurazepam hydrochloride

Flurazepam hydrochloride structure

Flurazepam hydrochloride 

structure
  • CAS No:

    1172-18-5

  • Formula:

    C21H23ClFN3O.2ClH

  • Chemical Name:

    Flurazepam hydrochloride

  • Synonyms:

    2H-1,4-Benzodiazepin-2-one,7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-,hydrochloride (1:2);2H-1,4-Benzodiazepin-2-one,7-chloro-1-[2-(diethylamino)ethyl]-5-(o-fluorophenyl)-1,3-dihydro-,dihydrochloride;2H-1,4-Benzodiazepin-2-one,7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-,dihydrochloride;Ro 5-6901;7-Chloro-1-[2-(diethylamino)ethyl]-5-(o-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one dihydrochloride;Dalmane;Flurazepam hydrochloride;7-Chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one dihydrochloride;ID 480;Flurazepam dihydrochloride;Dalmadorm;Dalmate;Lunipax;Insumin;Dormodor;Benozil;Felson;Somlan;NSC 78559

  • Categories:

    Active Pharmaceutical Ingredients  >  Nervous System Drugs

Description

PHYSICAL DESCRIPTION: Odorless off-white to yellow crystalline powder. (NTP, 1992)


Flurazepam dihydrochloride is an odorless off-white to yellow crystalline powder. (NTP, 1992)


Flurazepam dihydrochloride is an odorless off-white to yellow crystalline powder. (NTP, 1992)|Flurazepam hydrochloride is a benzodiazepine.|Dalmane is a DEA Schedule IV controlled substance. Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|Flurazepam is an orally available benzodiazepine used for therapy of insomnia. As with most benzodiazepines, flurazepam therapy has not been associated with serum aminotransferase or alkaline phosphatase elevations; clinically apparent liver injury from flurazepam has been reported, but is very rare.|Flurazepam Hydrochloride is the hydrochloride salt form of flurazepam, a member of the benzodiazepines and a long-acting depressor of the central nervous system (CNS) with sedative and hypnotic effects. Flurazepam binds to a specific site on the benzodiazepine-gamma-aminobutyric acid (GABA)-A-chloride ionophore receptor complex located on the neuronal membrane. Binding causes an allosteric modification of the receptor thereby enhancing the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events, which leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability. By modulating binding of the GABA inhibitory neurotransmitter to GABA-A receptors in the ascending reticular activating system, flurazepam blocks arousal of the cortical and limbic system, thereby exerting its sedative and hypnotic effect.|A benzodiazepine derivative used mainly as a hypnotic.

Flurazepam hydrochloride Basic Attributes

460.8

459.10500

214-630-0

756RDM536M

2767

3249

DTXSID3025334

C29060

Characteristics

35.91000

5.10950

light yellow solid

190-220 °C

551.4ºC at 760mmHg

287.2ºC

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: <6 mg/mL

2-8°C

Water soluble.

Amides and Imides

Safety Information

III

6.1(b)

3249

3

22-33-39/23/24/25-23/24/25-11

1/2-22-36-36/37/39-45-36/37-16-7

DF0875000

Xn,T,F

P260-P301 + P312 + P330

H302-H373

Flash point data for this chemical are not available. It is probably combustible. (NTP, 1992)

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P260, P264, P270, P301+P312, P314, P330, and P501|Aggregated GHS information provided by 41 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Fires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)

Excerpt from ERG Guide 151 [Substances - Toxic (Non-combustible)]: As an immediate precautionary measure, isolate spill or leak area in all directions for at least 50 meters (150 feet) for liquids and at least 25 meters (75 feet) for solids. SPILL: Increase, in the downwind direction, as necessary, the isolation distance shown above. FIRE: If tank, rail car or tank truck is involved in a fire, ISOLATE for 800 meters (1/2 mile) in all directions; also, consider initial evacuation for 800 meters (1/2 mile) in all directions. (ERG, 2016)

SMALL SPILLS AND LEAKAGE: If you spill this chemical, you should dampen the solid spill material with water, then transfer the dampened material to a suitable container. Use absorbent paper dampened with water to pick up any remaining material. Seal your contaminated clothing and the absorbent paper in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned. STORAGE PRECAUTIONS: You should protect this material from exposure to light, and store it under ambient temperatures. This compound is a Schedule IV DEA Controlled Substance and is to be stored according to State and Federal Regulations. Refer to Code of Federal Regulations Title 21 Part 1300 to End. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

Toxicity

Flurazepam, as with other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury is rare. Only a few case reports of acute liver injury from flurazepam have been published and mostly before 1980. The latency to onset of acute liver injury has varied from a 2 to 6 months and the pattern of liver enzyme elevations was cholestatic. The injury is usually mild to moderate in severity and self-limited. Fever and rash have not been described nor has autoantibody formation.

Drug Information

Flurazepam is an orally available benzodiazepine used for therapy of insomnia. As with most benzodiazepines, flurazepam therapy has not been associated with serum aminotransferase or alkaline phosphatase elevations; clinically apparent liver injury from flurazepam has been reported, but is very rare.

Sedatives and Hypnotics

Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)|Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here. (See all compounds classified as Anti-Anxiety Agents.)|Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here. (See all compounds classified as GABA Modulators.)

SYMPTOMS: Symptoms of exposure to this compound may include dizziness, drowsiness, light-headedness, staggering, ataxia, severe sedation, lethargy, headache, disorientation, coma, heartburn, upset stomach, nausea, vomiting, diarrhea, constipation, gastrointestinal pain, nervousness, talkativeness, apprehension, irritability, weakness, palpitations, chest pains, body and joint pains and genitourinary complaints. Other symptoms include hypotension, excitement, skin rash, leukopenia, elevated liver enzymes, and jaundice. It has additive effects with alcohol, barbituates, and other central nervous system depressants. ACUTE/CHRONIC HAZARDS: When heated to decomposition, this compound emits toxic fumes of chloride ion, fluoride ion and NOx. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. If symptoms (such as redness or irritation) develop, immediately transport the victim to a hospital. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

Apo Flurazepam

Flurazepam|Dalmane|2767|Schedule IV - Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|No

Flurazepam hydrochloride Use and Manufacturing

Uses

Flurazepam is used as an sedative, hypnotic. This is a controlled substance (depressant).

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:460.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:6
Exact Mass:459.104724
Monoisotopic Mass:459.104724
Topological Polar Surface Area:35.9
Heavy Atom Count:29
Complexity:540
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

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