Diazepam (Valium)

What is Diazepam?

Diazepam, sold under the brand name Valium among others, is a medicine of the benzodiazepine family that acts as an anxiolytic.

The active ingredient diazepam is used to treat physical and psychological states of tension and excitement. Diazepam is also used to prepare for anesthesia. Diazepam belongs to the benzodiazepines.

Application

The active ingredient diazepam is used to treat physical and psychological states of tension and excitement. These include, for example, anxiety disorders (oral use), but also acute anxiety states such as after a heart attack (parenteral use). Diazepam is also used to prepare for anesthesia before diagnostic or surgical procedures.

Diazepam belongs to the group of active ingredients known as benzodiazepines . It has an anti-anxiety, muscle-relaxing, antispasmodic and calming effects. Diazepam increases the effect of the body’s own neurotransmitter gamma-aminobutyric acid (GABA), which regulates the excitability of nerve cells. To do this, diazepam binds agonistically to GABA-A receptors. As a result, more chloride ions flow into the cell. This leads to increased cell membrane tension and a reduced excitability of the cell. Diazepam thus reduces neuronal excitation. On the one hand, this reduces psychological symptoms such as restlessness or anxiety. On the other hand, tense and/or cramped muscles are relaxed.

he effect of diazepam sets in quickly and lasts for 24 to 48 hours. In addition, the breakdown products of the active ingredient can have a sedative effect for up to 80 hours after administration. This makes diazepam one of the long-acting benzodiazepines. Diazepam is broken down primarily in the liver. This produces the metabolites N-desmethyldiazepam ( Nordazepam ), temazepam and oxazepam , which are also pharmacologically active and appear in the urine as glucuronides.

dosage

Oral intake

The dosage is 5 to 10 mg daily. It should preferably be taken in the evening and not on a full stomach, as otherwise the onset of effects may be delayed. At the end of therapy, the dosage should be tapered off.

suppositories

The dosage is 10 mg once daily.

Further dosages, including for other formulations, can be found in the respective product information.

Diazepam (Valium) side effects

The side effects of diazepam are typical for the benzodiazepine group of drugs. The higher the dosage, the greater the likelihood of unwanted effects, all of which are caused by the central depressant effect. The most common side effects of diazepam are impaired cognitive abilities, including impaired reaction time. Dizziness, headaches, an increased risk of falls, gastrointestinal complaints and dry mouth are also side effects of the depressant effect on the central venous system. The more serious unwanted effects of diazepam include breathing problems, a drop in blood pressure, a slowed pulse (up to cardiac arrest) and bladder dysfunction with urinary retention or incontinence.

Diazepam (Valium) interactions

The oxidative degradation of diazepam occurs through the cytochrome P450 isoenzymes CYP2C19 and CYP3A . Drugs that contain active ingredients that are also substrates of the enzymes mentioned can increase and prolong the sedative effect of diazepam when used at the same time. These include:

• cimetidine
• Omeprazole
• disulfiram

Diazepam  Legal status

The regulation of therapeutic goods, defined as drugs and therapeutic devices, varies by jurisdiction. In some countries, such as the United States, they are regulated at the national level by a single agency. In other jurisdictions they are regulated at the state level, or at both state and national levels by various bodies, as in Australia.