Pharm 59 Sedative-Hypnotic drugs – Flashcards
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Why are Diazepam and Flurazepam such long acting drugs
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They are metabolized into active metabolites
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How are most benzodiazepines metabolized
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Most benzodiazepines undergo phase I reactions, mainly by CYP3A4. The metabolites are then conjugated in phase II to form glucuronides that are excreted in the urine
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Which three Benzos and are not metabolized by the P450 system
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Conjugated directly to their glucuronides (still in liver) Their plasma levels are not significantly affected in liver disease. Other benzodiazepines may need dose adjustment in liver disease.
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Are benzos used for short term or long term anxiety
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Short term, due to dependance and minimal effect on PTSD and OCD *SSRIs* have replaced them for long term use
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How do you determine which benzo is used to treat sleep specific sleep disturbances
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Shot acting: used to help initiate sleep Long acting: used for people who keep waking up
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What is an adverse effect of benzodiazepines where they cause the opposite symptoms than expected (e.g. anxiety, hostility, rage, paranoia, and depression)
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*Paradoxical effects*
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What is one of the most serious/common adverse effects of long term benzodiazepine use
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On of the few drugs that cause DEATH due to withdraws
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What drug is used to treat overdose of benzodiazepines
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Fast acting but short duration, frequent administration may be necessary *May precipitate withdrawal in physiologically dependent patients*
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Do Barbiturates act on the same channel as benzodiazepines? How do they effect the GABA channel
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Increase the *DURATION* of the GABA channel
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Why do Barbiturates cause more adverse side effects than benzodiazepines
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dirty drugs that act on several receptors
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How do Barbiturates effect respiratory system and the CYP450 enzymes
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Decreased respiration is the main cause of death
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How does N-phenylbarbital treat hyperbilirubinemia and kernicterus
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induces liver CYP450 to metabolize bilirubin N-phenylbarbital is a metabolite and does not cause CNS depression
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In which RBC disorders are barbiturates contraindication
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porphyria (mostly Acute Intermittent Porphyria)
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On which receptors do the non-benzodiazepine act
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BZ1 subtype of benzodiazepine receptors.
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Zolpidem
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Ambien
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Advantages of Busiprone
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disadvantage; not as effective
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What drug is a melatonin agonist used as a sleep aid
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absorbed better than melatonin supplements
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Which antihistamines are commonly used to help with insomnia?
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Not effective in chronic insomnia
