What is the mechanism of action for benzodiazepines?
Benzodiazepines work by enhancing a very important neurotransmitter called GABA (gamma-aminobutyric acid) at the GABA A receptor. This results in the sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties for which the drugs are prescribed.
How do benzodiazepines work in the body?
Like other mental health medications, these work by impacting chemical messengers in the brain called neurotransmitters. Benzodiazepines enhance the action of the neurotransmitter gamma-aminobutyric acid (GABA), which slows down the central nervous system.
How does benzodiazepines affect the nervous system?
Benzodiazepines are depressants. This means they can change your mental state by slowing down activity in the central nervous system, reducing feelings of tension, and relaxing muscles. This is why they’re highly effective at treating severe anxiety, panic disorders, insomnia, and seizures.
What are the physiological effects of benzodiazepines?
Common side effects among all BZDs include drowsiness, lethargy, and fatigue. At higher dosages, impaired motor coordination, dizziness, vertigo, slurred speech, blurry vision, mood swings, and euphoria can occur, as well as hostile or erratic behavior in some instances.
How do Benzos work on GABA?
Benzodiazepines facilitate the inhibitory actions of GABA by binding to γ-aminobutyric acid type A receptors (GABAARs), GABA-gated chloride/bicarbonate channels, which are the key mediators of transmission at inhibitory synapses in the brain.
How does GABA antagonist work?
Gamma-aminobutyric acid (GABA) inhibitors, or GABA antagonists, are drugs that inhibit the action of GABA, the primary inhibitory neurotransmitter of the central nervous system. They predominantly work at the GABA receptor. GABA receptors categorize into the GABA-A receptor and GABA-B receptor subtypes.
What are the pharmacokinetics of benzodiazepines?
Benzodiazepines are extensively bound to plasma proteins (80–98%), resulting in a small ‘free fraction’ which can cross the blood-brain barrier. Although benzodiazepines are well absorbed after oral administration, midazolam has the largest first-pass elimination by the liver.
How do benzodiazepines increase GABA?
Benzodiazepines increase the frequency of chloride channel influx which hyperpolarizes the GABA receptor, resulting in increased inhibitory postsynaptic potential. α1–6, β1–3, γ1–3, δ, ε, θ, and π make up the currently defined GABAA subunits in the human brain. Abbreviation: GABA, gamma aminobutyric acid.
How does benzodiazepines affect GABA?
What is the role of GABA in the nervous system?
GABA is the principal inhibitory neurotransmitter in the central nervous system (CNS) (1). GABA inhibitory neurotransmission is essential in normal brain function, in neuronal activity, information processing and plasticity, and network synchronization, and in disease.
How do Benzodiazepines work?
Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA A receptor, resulting in sedative, hypnotic ( sleep-inducing ), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties.
What is benzodiazepine (BZD)?
BENZODIAZEPINE PHARMACOLOGY General/Pharmacodynamics BZDs act as positive allosteric modulators on the gamma amino butyric acid (GABA)-A receptor. The GABA-A receptor is a ligand-gated chloride-selective ion channel. GABA is the most common neurotransmitter in the central nervous system, found in high concentrations in the cortex and limbic system.
What is the pharmacokinetics of benzodiazepines?
Benzodiazepine Pharmacokinetics. Pharmacokinetics (determination of the onset of action and the duration of drug effect) is affected by route of administration, absorption, and volume of distribution. BZDs can be administered via intramuscular, intravenous, oral, sublingual, intranasal, or rectal gel forms.
Which receptors are involved in the mechanism of action of benzodiazepines?
Rudolph U, Crestani F, Benke D, et al. Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. Nature. 1999 Oct 21;401(6755):796–800. Erratum in: Nature. 2000 Apr 6;404(6778):629.