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PHARMACOLOGY TUTORING FOR SEDATIVE HYPNOTICS AND ANTIEMETICS By Alaina Darby • Which of the following is not a sedative property? Decrease activity b. Moderate excitement c. Produce drowsiness d. Calms recipient a. • During which of the following sleep stages does one experience light sleep? Stage 1 b. Stage 2 c. Stage 3 d. Stage 4 a. • Which of the following is true of sleep cycles and their stages? The physiological state in REM sleep is indicative of wakefulness b. The first cycle can last from 5-15 minutes c. Cycles decrease in length throughout the night d. A normal night’s sleep usually includes 6 cycles a. Which of the following correctly outlines the pattern of a normal sleep cycle? • Waking, stage 1, 2, 3, 4, 3, 2, 1, REM b. Waking, stage 1, 2, 3, 4, 3, 2, REM c. Waking, stage 1, 2, 3, 4, REM d. Waking, stage 4, 3, 2, 1, REM a. Which of the following describes the manner in which the progressive effects of CNS depressants from drowsiness to fatal depression are produced? • Concentration dependent b. Metabolization dependent c. Response dependent d. Dose dependent a. • Which of the following is not a CNS effect of benzodiazepines? Sedation b. Muscle relaxation c. Neuromuscular blocker d. Anterograde amnesia a. Which of the following does not describe how benzodiazepines exert their effects? • They are specific for certain GABA channel subunits b. They increase frequency of channel opening c. They decrease time spent in all stages but increase the number of stages d. They increase total sleep time a. Respiration becomes a concern of benzodiazepines particularly in all but which of the following? • Impaired renal function b. Children c. Ethanol users d. Impaired hepatic function a. • Which accurately describes the metabolization of benzodiazepines? Mainly occurs through cytochrome P450 in the kidneys b. Glucuronidation produces active metabolites c. It includes a three stage process with each stage being progressively slower d. Triazolam and alprazolam do not undergo hydroxylation at R3 a. Which of the following causes a drug interaction with a mechanism other than the inhibition of CYP3A4? • Erythromycin b. Ketoconazole c. Oral contraceptives d. Ritonavir a. • Which of the following is the closest to an ideal hypnotic? Triazolam b. Alprazolam c. Midazolam d. Estazolam a. • Which of the following is a paradoxical side effect of benzodiazepines? Lassitude b. Paranoia and depression c. Motor incoordination d. Anterograde amnesia a. • Which of the following is true of benzodiazepines? Short-acting benzodiazepines are rapidly metabolized and more likely to cause rebound insomnia b. Short-acting benzodiazepines are slowly metabolized and more likely to cause rebound insomnia c. Long-acting benzodiazepines are rapidly metabolized and more likely to cause rebound insomnia d. Long-acting benzodiazepines are slowly metabolized and more likely to cause rebound insomnia a. • Estrazolam is classified into which of the following categories? Ultra-short acting b. Short-acting c. Intermediate-acting d. Long-acting a. A benzodiazepine has a half-life of 12 hours. Into which of the following categories would it be classified? • Ultra-short acting b. Short-acting c. Intermediate-acting d. Long-acting a. • How do benzodiazepine agonists bind? Nonspecifically on the GABA receptor b. Specifically to the alpha and beta subunits on the GABA receptor c. Specifically to different subunits on the GABA receptor depending on the drug d. Specifically to the alpha1 subunit on the GABA receptor a. • Which of the following is true of benzodiazepine agonists? The dose of zaleplon should be half of what it is in men b. Risk of next day driving is a concern when taking eszopiclone c. All benzodiazepine agonists should only be taken for 7-10 days d. Zolpidem is the most likely of these drugs to produce hangover at therapeutic doses a. • Which of the following is not a concern for benzodiazepine agonists? Use in psychotic patients b. Effects from withdrawal c. Thoughts of suicide d. Use in pregnancy and nursing a. Which of the following is classified as a benzodiazepine antagonist and can be used to reverse sedative effects after a diagnostic procedure? • Chlordiazepoxide b. Flumazenil c. Ramelteon d. Meprobomate a. • Which of the following is not a sleep stage effect of barbiturates? Increased total sleep time b. Decreased sleep latency c. Increased REM and stage 3-4 sleep d. Decreased number of awakenings a. • How do barbiturates produce their action? Increase duration of GABA channel opening and antagonize AMPA receptors b. Increase frequency of GABA channel opening and antagonize AMPA receptors c. Increase duration of GABA channel opening and agonize AMPA receptors d. Increase frequency of GABA channel opening and agonize AMPA receptors a. Which of the following is true of the effects that barbiturates produce throughout the body? • Respiration may be severely depressed at hypnotic doses b. Blood pressure is slightly increased c. Combination with cytochrome P450 enzymes may inhibit steroid metabolism d. The induction of liver enzymes decreases the metabolism of other drugs a. Which of the following is not true of the use of barbiturates for hypnotic purposes? • They are often administered by IV b. Their onset of action may range from 10-60 minutes c. The onset of action is delayed by the presence of food a. d. They distribute to highly-perfused tissues first • Which of the following is not a side effect of barbiturates? Hangover b. Paradoxical excitement c. Increased pain perception d. Nausea and vomiting a. • Which of the following is the primary contraindication for barbiturates? Pregnancy b. Elderly c. Porphyria d. Liver failure a. • Which of the following is not true of ramelteon? It is approved for long term use b. It may cause rebound insomnia c. It is a melatonin receptor agonist d. It may cause missed menstrual period or disinterest in sex a. • Which of the following would be limited to the hospital setting? Paraldehyde b. Chloral hydrate c. Etomidate d. Meprobamate a. • What would not be a characteristic of a perfect hypnotic? Increased duration of sleep b. Absence of rebound insomnia c. Lack of drug interactions a. d. Minimal next day effects Sally is dealing with the death of her father, and has had trouble sleeping for the last week. How would her insomnia be classified and what would be the method of treating it? • Transient insomnia treated with a low dose of hypnotic for 2-3 days b. Short-term insomnia treated with a low dose of hypnotic for 2-3 days c. Long-term insomnia treated with an adjunct hypnotic intermittently for 710 days d. Short-term insomnia treated with an adjunct hypnotic intermittently for 710 days a. • How should insomnia lasting longer than 3 weeks be treated? Benzodiazepine b. Barbiturate c. Nonpharmacological d. Benzodiazepine agonist a. What would not typically be a consideration in the treatment of insomnia in older patients? • Increased body water b. Decreased renal function c. Polyphasic sleep patterns d. Increased body fat a. Which of the following is true of the mechanisms of barbiturates and benzodiazepines in terms of GABA channel opening? a. Barbiturates increase frequency while benzodiazepines increase duration of channel opening b. Barbiturates increase duration while benzodiazepines increase frequency of channel opening c. Barbiturates and benzodiazepines both increase frequency of channel opening d. Barbiturates and benzodiazepines both increase duration of channel opening • Which of the following is true of barbiturates and benzodiazepines in terms of mechanism? • Barbiturates require GABA and benzodiazepines do not b. Benzodiazepines require GABA and barbiturates do not c. Barbiturates and benzodiazepines both require GABA d. Neither barbiturates nor benzodiazepines require GABA a. • How should benzodiazepines be prescribed? Long acting for sleep onset insomnia and short acting for anxiety b. Short acting for sleep onset insomnia and long acting for anxiety c. Long acting for sleep onset insomnia and for anxiety d. Short acting for sleep onset insomnia and for anxiety a. Which of the following types of receptors is not present in the chemoreceptor trigger zone? • 5-HT3 b. D2 c. M1 d. H1 a. • Which of the following has activity at only one type of receptor? Scopolamine b. Ondansetron c. Droperidol d. Chlorpromazine a. • Which of the following does not have any activity at the serotonin receptor? Scopolamine b. Ondansetron c. Droperidol d. Chlorpromazine a. Which of the following is in the class that has been described as the most effective antiemetics to date? • Scopolamine b. Ondansetron c. Droperidol d. Chlorpromazine a. Concomitant administration with dexamethasone significantly increases potency of which of the following? • Scopolamine b. Ondansetron c. Droperidol d. Chlorpromazine a. • Which of the following is true of serotonin antagonists? Not effective when used alone since they only have effects at the serotonin receptor b. Antiemetic effects decline quickly after they are removed from circulation c. Block serotonin receptors in the stomach, small intestines, and CTZ d. Administered on an as needed basis a. Which of the following has an extended half-life due to the production of an active metabolites? • Ondansetron b. Palonosetron c. Granisetron d. Dolasetron a. Which of the following adverse effects is not commonly seen with serotonin antagonists? • Constipation b. GI discomfort c. Diarrhea d. Headache a. Which of the following serotonin antagonists has the highest affinity for the serotonin receptor? • Ondansetron b. Palonosetron c. Granisetron d. Dolasetron a. • Which of the following serotonin antagonists has the longest half-life? Ondansetron b. Palonosetron c. Granisetron d. Dolasetron a. Which of the following serotonin antagonists has affinity for more than one type of serotonin receptor? • Ondansetron b. Palonosetron c. Granisetron d. Dolasetron a. Which of the following is used in combination with antiemetic agents to prevent peritumoral inflammation? • Aprepitant b. Dexamethasone c. Ondansetron d. Chlorpromazine a. Which of the following has central action and is used only as an adjunct therapy? • Aprepitant b. Dexamethasone c. Ondansetron d. Chlorpromazine a. Which of the following classes of antiemetics is most effective for chemotherapy-induced nausea? • Serotonin antagonists b. Neurokinin 1 receptor antagonists c. Butyrophenones d. Phenothiazines a. Which of the following classes of antiemetics would be most valuable for motion sickness? • Serotonin antagonists b. Neurokinin 1 receptor antagonists c. Butyrophenones d. Phenothiazines a. Which of the following is given prophylactically prior to cancer chemotherapy and to prevent postoperative N/V? • Chlorpromazine b. Droperidol c. Metoclopramide d. Dimenhydrinate a. • Which of the following does not describe the effects of meclizine? Decreased stimulation of labyrinthine function b. Exerts anticholinergic effects to decrease vestibular secretions c. Works on vestibular afferents and within the brainstem d. Used to treat vertigo and Menier’s disease a. • Which of the following is not true of scopolamine? May cause extrapyramidal effects b. Used to treat N/V from chemotherapy c. Works through an anticholinergic mechanism d. May cause sedation a. Which of the following is used only when patients fail to respond to other antiemetics? • Metoclopramide b. Droperidol c. Dronabinol d. Lorazepam a. • Which of the following is given one day prior to chemotherapy? Metoclopramide b. Droperidol c. Dronabinol d. Lorazepam a.