A report on Benzodiazepine

Structural formula of benzodiazepines.
Midazolam 1 & 5 mg/mL injections (Canada)
Temazepam (Normison) 10 mg tablets
Addiction experts in psychiatry, chemistry, pharmacology, forensic science, epidemiology, and the police and legal services engaged in delphic analysis regarding 20 popular recreational drugs. Benzodiazepines were ranked in this graph 7th in dependence, physical harm, and social harm.
Diazepam 2 mg and 5 mg diazepam tablets, which are commonly used in the treatment of benzodiazepine withdrawal.
Chlordiazepoxide 5 mg capsules, which are sometimes used as an alternative to diazepam for benzodiazepine withdrawal. Like diazepam it has a long elimination half-life and long-acting active metabolites.
Schematic diagram of the (α1)2(β2)2(γ2) GABAA receptor complex that depicts the five-protein subunits that form the receptor, the chloride (Cl−) ion channel pore at the center, the two GABA active binding sites at the α1 and β2 interfaces and the benzodiazepine (BZD) allosteric binding site at the α1 and γ2 interface.
Left: The 1,4-benzodiazepine ring system. Right: 5-phenyl-1H-benzo[e] [1,4]diazepin-2(3H)-one forms the skeleton of many of the most common benzodiazepine pharmaceuticals, such as diazepam (7-chloro-1-methyl substituted).
A pharmacophore model of the benzodiazepine binding site on the GABAA receptor. White sticks represent the carbon atoms of the benzodiazepine diazepam, while green represents carbon atoms of the nonbenzodiazepine CGS-9896. Red and blue sticks are oxygen and nitrogen atoms that are present in both structures. The red spheres labeled H1 and H2/A3 are, respectively, hydrogen bond donating and accepting sites in the receptor, while L1, L2, and L3 denote lipophilic binding sites.
The molecular structure of chlordiazepoxide, the first benzodiazepine. It was marketed by Hoffmann–La Roche from 1960 branded as Librium.
Xanax (alprazolam) 2 mg tri-score tablets

Fusion of a benzene ring and a diazepine ring.

- Benzodiazepine
Structural formula of benzodiazepines.

114 related topics with Alpha

Overall

Diazepam tablets (10, 5, and 2 mg)

Diazepam

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Diazepam tablets (10, 5, and 2 mg)
5 mg Valium Roche packaging Australia

Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that acts as an anxiolytic.

Diazepam is sometimes used in the treatment of benzodiazepine withdrawal.

Benzodiazepine withdrawal syndrome

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Diazepam is sometimes used in the treatment of benzodiazepine withdrawal.
Chlordiazepoxide, 5 mg capsules, are sometimes used as an alternative to diazepam for benzodiazepine withdrawal. Like diazepam, it has a long elimination half-life and long-acting active metabolites.

Benzodiazepine withdrawal syndrome—often abbreviated to benzo withdrawal or BZD withdrawal —is the cluster of signs and symptoms that emerge when a person who has been taking benzodiazepines, either medically or recreationally, and has developed a physical dependence, undergoes dosage reduction or discontinuation.

0.5 mg tablets of the Ativan brand of lorazepam

Lorazepam

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0.5 mg tablets of the Ativan brand of lorazepam
1987 advertisement. "In a world where certainties are few...no wonder Ativan is prescribed by so many caring clinicians."

Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication.

Zolpidem tartrate, a common but potent sedative-hypnotic drug. Used for severe insomnia.

Hypnotic

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To induce sleep (or surgical anesthesia ) and to treat insomnia (sleeplessness).

To induce sleep (or surgical anesthesia ) and to treat insomnia (sleeplessness).

Zolpidem tartrate, a common but potent sedative-hypnotic drug. Used for severe insomnia.
Le Vieux Séducteur by .
(A corrupt old man tries to seduce a woman by urging her to take a hypnotic draught in her drink)

Among individuals with sleep disorders, 13.7% are taking or prescribed nonbenzodiazepines, while 10.8% are taking benzodiazepines, as of 2010, in the USA.

Barbituric acid, the parent structure of all barbiturates

Barbiturate

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Drug that acts as a central nervous system depressant.

Drug that acts as a central nervous system depressant.

Barbituric acid, the parent structure of all barbiturates
Addiction experts in psychiatry, chemistry, pharmacology, forensic science, epidemiology, and the police and legal services engaged in delphic analysis regarding 20 popular recreational drugs. Barbiturates were ranked third in physical harm, fourth in social harm, and fifth in dependence.
Generic structure of a barbiturate, including numbering scheme

They have largely been replaced by benzodiazepines and nonbenzodiazepines ("Z-drugs") in routine medical practice, particularly in the treatment of anxiety and insomnia, because of the significantly lower risk of addiction and overdose and the lack of an antidote for barbiturate overdose.

Anxiolytic

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Medication or other intervention that reduces anxiety.

Medication or other intervention that reduces anxiety.

Benzodiazepines are prescribed to quell panic attacks.

A drawing of someone with insomnia from the 14th century

Insomnia

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Sleep disorder in which people have trouble sleeping.

Sleep disorder in which people have trouble sleeping.

A drawing of someone with insomnia from the 14th century
Potential complications of insomnia.
Normison (temazepam) is a benzodiazepine commonly prescribed for insomnia and other sleep disorders.
Disability-adjusted life year for insomnia per 100,000 inhabitants in 2004.
no data
less than 25
25–30.25
30.25–36
36–41.5
41.5–47
47–52.5
52.5–58
58–63.5
63.5–69
69–74.5
74.5–80
more than 80

Like alcohol, benzodiazepines, such as alprazolam, clonazepam, lorazepam, and diazepam, are commonly used to treat insomnia in the short-term (both prescribed and self-medicated), but worsen sleep in the long-term.

Structure of the GABAA receptor (α1β1γ2S: PDB: 6DW1). Top: side view of the GABAA receptor embedded in a cell membrane. Bottom: view of the receptor from the extracellular face of the membrane. The subunits are labeled according to the GABAA nomenclature and the approximate locations of the GABA and benzodiazepine (BZ) binding sites are noted (between the α- and β-subunits and between the α- and γ-subunits respectively).

GABAA receptor

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Ionotropic receptor and ligand-gated ion channel.

Ionotropic receptor and ligand-gated ion channel.

Structure of the GABAA receptor (α1β1γ2S: PDB: 6DW1). Top: side view of the GABAA receptor embedded in a cell membrane. Bottom: view of the receptor from the extracellular face of the membrane. The subunits are labeled according to the GABAA nomenclature and the approximate locations of the GABA and benzodiazepine (BZ) binding sites are noted (between the α- and β-subunits and between the α- and γ-subunits respectively).
Schematic structure of the GABAA receptor. Left: GABAA monomeric subunit embedded in a lipid bilayer (yellow lines connected to blue spheres). The four transmembrane α-helices (1–4) are depicted as cylinders. The disulfide bond in the N-terminal extracellular domain which is characteristic of the family of cys-loop receptors (which includes the GABAA receptor) is depicted as a yellow line. Right: Five subunits symmetrically arranged about the central chloride anion conduction pore. The extracellular loops are not depicted for the sake of clarity.
Schematic diagram of a GABAA receptor protein ((α1)2(β2)2(γ2)) which illustrates the five combined subunits that form the protein, the chloride (Cl−) ion channel pore, the two GABA active binding sites at the α1 and β2 interfaces, and the benzodiazepine (BZD) allosteric binding site
GABAA receptor and where various ligands bind.

These allosteric sites are the targets of various other drugs, including the benzodiazepines, nonbenzodiazepines, neuroactive steroids, barbiturates, alcohol (ethanol), inhaled anaesthetics, kavalactones, and picrotoxin, among others.

Physical dependence

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Physical condition caused by chronic use of a tolerance-forming drug, in which abrupt or gradual drug withdrawal causes unpleasant physical symptoms.

Physical condition caused by chronic use of a tolerance-forming drug, in which abrupt or gradual drug withdrawal causes unpleasant physical symptoms.

Protracted withdrawal syndrome is noted to be most often caused by benzodiazepines.

Alprazolam

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Alprazolam pills in boxes, as sold in France. Both Xanax (original Pfizer alprazolam product) and various generic forms of alprazolam are depicted here.
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Side effects from alprazolam
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Binding at the α1β3γ2 GABAA receptor. Alprazolam with red space-filling carbon atoms. γ2 receptor subunit in mint green. The α1' subunit is hidden.
Alprazolam is metabolized into 4-hydroxyalprazolam (top) and α-hydroxyalprazolam (bottom).

Alprazolam, sold under the brand name Xanax, among others, is a fast-acting tranquilizer of medium duration in the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring.