Examination Questions: Sedative and Hypnotics, and Antiepilepsy agents 1. What is the actinic name of GABA? a. The amino acerbic derivative, ? -aminobutyrate, additionally alleged 4-aminobutyrate, (GABA) is a acclaimed inhibitor of presynaptic manual in the CNS. 2. Explain: the anatomy of GABAA receptor circuitous and area of Benzodiazepine’s and barbiturate’s bounden sites on GABAA receptors. a. The GABAA receptor circuitous accept chloride channels associated with in the receptor (influx of Cl account hyperpolarization causing CNS depression) b. In this isoform, the two bounden sites for GABA are amid amid adjoining ? and ? 2 subunits, and the bounden abridged for benzodiazepines (the BZ armpit of the GABAA receptor) is amid an ? 1 and the ? 2 subunit. i.? 1 subunits in GABAA receptors arbitrate sedation, amnesia, and ataxic furnishings of benzodiazepine 3. Describe the aberration in the activity of barbiturates at lower and college dosage on GABAA receptors a. BZ access synaptic inhibition of GABA b. They enhance GABAergic furnishings after anon activating GABAA receptor by aperture of chloride channels but by accretion abundance of chloride aperture contest and acceptable chloride ion conductance. . Barbiturates access the continuance of the GABA-gated chloride approach openings d. At aerial concentrations, the barbiturates may additionally be GABA-mimetic, anon activating chloride channels. e. Barbiturates are beneath careful in their accomplishments than benzodiazepines, because they additionally abase the accomplishments of the excitatory neurotransmitter glutamic acerbic via bounden to the AMPA receptor (can account abounding surgical anesthesia and arresting axial biologic furnishings – low allowance of safety). f.
If GABA is not present, benzodiazepines cannot aftermath their furnishings (they can access the abundance but cannot initiate; alone GABA opens the channels). 4. Name GABAA and GABAB receptor agonist a. GABAA is the above inhibitory neurotransmitter in analgesic cord, hypothalamus, hippocampus, substantia nigra, cerebellar case and bookish case b. GABAA absolute ? 1 subunit agonist: zolpidem, zaleplon, and eszopiclone 5. Describe how Clorazepate produces its aftereffect afterward articulate administering a.
Diazepam and the alive metabolite of clorazepate is added rapidly captivated than alternative frequently acclimated benzodiazepines. b. Clorazepate, a prodrug, is adapted to its alive form, desmethyldiazepam (nordiazepam), by acerbic hydrolysis in the stomach. 6. Explain why benzodiazepines cantankerous biological membranes advisedly and administer rapidly in assorted agency systems including academician and placenta. a. Most of hypnotics and sedatives are lipid acrid and appropriately accept accelerated access of axial afraid arrangement effects. b.
All sedative-hypnotics cantankerous the placental barrier during abundance (NOT TO BE USED DURING PREGNANCY). 7. Explain the apparatus of activity of Flumazenil a. Competitive antagonists with aerial affection for the BZ bounden armpit b. It blocks abounding of the accomplishments of benzodiazepines, zolpidem, zaleplon, and eszopiclone c. Flumazenil is accustomed for use in abandoning the axial afraid arrangement biologic furnishings of benzodiazepine balance and to accelerate accretion in analgesic and analytic procedures. 8. Name short-acting benzodiazepines a. Short-acting agents (t1/2
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