Benzodiazepines

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Top 100 drugs.
Andrew Street
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Andrew Street
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Give eg's of & indications for benzodiazepines. eg's: diazepam, midazolam, lorazepam, chlordiazepoxide (used for alcohol withdrawal) Indications: • Seizures & status epilepticus • Alcohol withdrawal reactions • Sedation for interventional procedures • Anxiety - short term Rx for severe, disabling, distressing • Insomnia - short term Rx for severe, disabling, distressing
MOA of benzodiazepines. The target of benzodiazepines is the γ-aminobutyric acid type A (GABAA) receptor. The GABAA receptor is a chloride channel that opens in response to binding by GABA, the main inhibitory neurotransmitter in the brain. Opening the channel allows chloride to flow into the cell, making the cell more resistant to depolarisation. Benzodiazepines facilitate and enhance binding of GABA to the GABAA receptor. This has a widespread depressant effect on synaptic transmission. The clinical manifestations of this include reduced anxiety, sleepiness, sedation & anticonvulsive effects. Ethanol (‘alcohol’) also acts on the GABAA receptor, & in chronic excessive use the pt becomes tolerant to its presence. Abrupt cessation then provokes the excitatory state of alcohol withdrawal. This can be treated by introducing a benzodiazepine, which can then be withdrawn in a gradual & more controlled way.
SE's of benzodiazepines. • Drowsiness • Sedation • Coma (high doses or OD) • Airway obstruction & death due to loss of airway reflexes (as opposed to opioid respiratory depression) • Dependence • Withdrawal reactions
CI's, cautions, & important interactions of benzodiazepines. CI's: • None Cautions: • Elderly • Respiratory impairment • Neuromuscular DS (eg myasthenia gravis) • Liver failure Important interactions: The effects of benzodiazepines are additive to those of other sedating drugs, including alcohol & opioids. Most depend on cytochrome P450 enzymes for elimination, so concurrent use with cytochrome P450 inhibitors (e.g. amiodarone, diltiazem, macrolides, fluconazole, protease inhibitors) may ^their effects.
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