TEMAZEPAM Property

Melting point:

119-121°C

Boiling point:

211°C (rough estimate)

Density 

1.2682 (rough estimate)

refractive index 

1.5200 (estimate)

Flash point:

11 °C

storage temp. 

2-8°C

solubility 

Practically insoluble in water, freely soluble in methylene chloride, sparingly soluble in ethanol (96 per cent).

pka

pKa 1.6 (Uncertain)

BCS Class

2

CAS DataBase Reference

846-50-4(CAS DataBase Reference)

IARC

3 (Vol. 66) 1996

EPA Substance Registry System

Temazepam (846-50-4)

Safety

Hazard Codes 

Xn,T,F

Risk Statements 

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

Safety Statements 

16-36/37-45-7

RIDADR 

UN 1230 3/PG 2

WGK Germany 

3

RTECS 

DF1225000

HS Code 

2933910000

Toxicity

LD50 oral in rat: 2gm/kg

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

TEMAZEPAM Chemical Properties,Usage,Production

Chemical Properties

Crystalline Solid

Originator

Levanxol,Carlo Erba,Italy,1970

Uses

Pharmacologically active metabolite of Diazepam. Controlled substance (depressant). Sedative, hypnotic

Uses

Pharmacologically active labelled metabolite of Diazepam. Controlled substance (depressant). Sedative, hypnotic

Uses

Temazepam, is pharmacologically active metabolite of Diazepam (D416855). It is Sedative, and hypnotic. Controlled substance (depressant).

Definition

ChEBI: Temazepam is a benzodiazepine.

Manufacturing Process

According to British Patent 1,022,645 3.4 g of 3-acetoxy-7-chloro-1-methyl-5- phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one suspended in 80 ml alcohol was treated with 6 ml of 4 N NaOH. After complete solution had taken place, a solid precipitated; this solid was redissolved by the addition of 80 ml of water. The solution was acidified with acetic acid to give white crystals which were recrystallized from alcohol to yield 7-chloro-3-hydroxy-5-phenyl-1- methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one, MP 119° to 121°C.

brand name

Restoril (Tyco); Temaz (Quantum Pharmics).

Therapeutic Function

Tranquilizer

World Health Organization (WHO)

Temazepam is a widely used benzodiazepine derivative. As with other drugs in this class, cases of misuse and drug dependence are known.

General Description

Temazepam, 7-chloro-1,3-dihydro-3-hydroxy-1-methyl-5-phenyl -2H-1,4-benzodiazepine-2-one(Restoril), also occurs as a minor metabolite of diazepam.It can be visualized as N-methyl oxazepam, and indeed, asmall amount of N-demethylation occurs slowly. However,metabolism proceeds mainly through glucuronidationof the 3-hydroxyl group, thus, it is intermediate acting andmarketed as a hypnotic said to have little or no residualeffect.

Clinical Use

Benzodiazepine:
Insomnia (short-term use)
Pre-med anxiolytic prior to minor procedures

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: metabolism possibly increased by rifampicin.
Antipsychotics: increased sedative effects; risk of serious adverse effects in combination with clozapine.
Antivirals: concentration possibly increased by ritonavir.
Disulfiram: metabolism of temazepam inhibited (increased toxicity).
Sodium oxybate: enhanced effects of sodium oxybate - avoid.

Metabolism

Temazepam is metabolised mainly in the liver. It is excreted mainly in the urine in the form of its inactive glucuronide conjugate together with small amounts of the demethylated derivative, oxazepam, also in conjugated form.