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Benzodiazepine

Medical Uses and Effects of Benzodiazepines: – Benzodiazepines possess psycholeptic, sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant actions. – They are administered orally, intravenously, intramuscularly, […]

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Medical Uses and Effects of Benzodiazepines:
– Benzodiazepines possess psycholeptic, sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant actions.
– They are administered orally, intravenously, intramuscularly, or rectally.
– Generally well-tolerated and effective in the short term for various conditions.
– Mode of action involves enhancing GABA neurotransmitter at receptors.
– Useful for anxiety, panic disorder, insomnia, seizures, muscle spasms, and premedication.
– Categorized into short, intermediate, and long-acting types based on treatment purposes.
– Short-term use is considered safe, but long-term use may lead to cognitive deficits and other adverse effects.
– Risks include tolerance, dependence, withdrawal syndrome, cognitive impairment, and paradoxical effects.

Risks and Guidelines on Benzodiazepine Use:
– Increased risk of suicide, aggression, impulsivity, and negative withdrawal effects.
– Concerns about decreasing effectiveness, physical dependence, and withdrawal syndrome.
– Safety concerns in pregnancy and overdose risks, especially when combined with alcohol or opioids.
– Recommendations for discontinuation in long-term users and those on opioids.
– Efforts to reduce usage to prevent serious adverse health outcomes.
– Varying views on long-term use for panic disorder, with APA guidelines supporting initial benzodiazepine treatment.
– NICE questioning non-placebo-controlled studies and not recommending benzodiazepine use based on placebo-controlled findings.

Specific Medical Uses of Benzodiazepines:
– Common uses include treating panic disorder, generalized anxiety disorder, anxiety, insomnia, seizures, and alcohol withdrawal.
– Indications for alcohol detoxification, managing alcohol withdrawal syndrome, preventing seizures, and treating severe delirium.
– Other uses include sedation in mechanical ventilation, managing breathlessness in advanced diseases, and before surgery to relieve anxiety.
– Used for dental phobia, ophthalmic procedures, muscle spasms, restless legs syndrome, acute agitation, acute psychosis, parasomnia, and obsessive-compulsive disorder.

Special Considerations and Contraindications:
– Contraindications in individuals with myasthenia gravis, sleep apnea, excessive alcohol use, or non-medical opioid use.
– Caution needed in people with personality disorders or intellectual disability.
– Risk of life-threatening interactions with barbiturates.
– Categorized as potentially harmful in pregnancy by the FDA.
– Considered potentially inappropriate for older adults due to increased risks of dependence and adverse effects.

Adverse Effects and Cognitive Impact:
– Common side effects include drowsiness, dizziness, decreased alertness, and lack of coordination.
– Long-term use can lead to cognitive impairment, affective and behavioral problems.
– Cognitive effects include interference with memory formation, anterograde amnesia, and moderate to large adverse effects on cognition.
– Paradoxical reactions like aggression, violence, impulsivity, and irritability can occur.
– Long-term use may worsen anxiety, depression, and sleep disturbances, inhibiting memory consolidation and psychotherapy benefits.

Benzodiazepine (Wikipedia)

Benzodiazepines (BZD, BDZ, BZs), colloquially called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide.

Benzodiazepines
Drug class
Structural formula of benzodiazepines.
Class identifiers
UseAnxiety disorders, seizures, muscle spasms, panic disorder
ATC codeN05BA
Mode of actionGABAA receptor
Legal status
In Wikidata

Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses of many shorter-acting benzodiazepines may also cause anterograde amnesia and dissociation. These properties make benzodiazepines useful in treating anxiety, panic disorder, insomnia, agitation, seizures, muscle spasms, alcohol withdrawal and as a premedication for medical or dental procedures. Benzodiazepines are categorized as short, intermediate, or long-acting. Short- and intermediate-acting benzodiazepines are preferred for the treatment of insomnia; longer-acting benzodiazepines are recommended for the treatment of anxiety.

Benzodiazepines are generally viewed as safe and effective for short-term use—about two to four weeks—although cognitive impairment and paradoxical effects such as aggression or behavioral disinhibition can occur. According to the Department of Health (Victoria), long-term use can cause “impaired thinking or memory loss. anxiety and depression. irritability, paranoia, aggression, etc.” A minority of people have paradoxical reactions after taking benzodiazepines such as worsened agitation or panic. Benzodiazepines are associated with an increased risk of suicide due to aggression, impulsivity, and negative withdrawal effects. Long-term use is controversial because of concerns about decreasing effectiveness, physical dependence, benzodiazepine withdrawal syndrome, and an increased risk of dementia and cancer. The elderly are at an increased risk of both short- and long-term adverse effects, and as a result, all benzodiazepines are listed in the Beers List of inappropriate medications for older adults. There is controversy concerning the safety of benzodiazepines in pregnancy. While they are not major teratogens, uncertainty remains as to whether they cause cleft palate in a small number of babies and whether neurobehavioural effects occur as a result of prenatal exposure; they are known to cause withdrawal symptoms in the newborn.

Taken in overdose, benzodiazepines can cause dangerous deep unconsciousness, but they are less toxic than their predecessors, the barbiturates, and death rarely results when a benzodiazepine is the only drug taken. Combined with other central nervous system (CNS) depressants such as alcohol and opioids, the potential for toxicity and fatal overdose increases significantly. Benzodiazepines are commonly used recreationally and also often taken in combination with other addictive substances, and are controlled in most countries.

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