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Questions and Answers
Quel est le principal effet du médicament hypnotique sur le système nerveux central?
Quel est le principal effet du médicament hypnotique sur le système nerveux central?
Quel terme décrit le type d'insomnie qui se produit plus de 3 fois par semaine pendant plus de 3 mois?
Quel terme décrit le type d'insomnie qui se produit plus de 3 fois par semaine pendant plus de 3 mois?
Quelle substance était historiquement utilisée pour ses propriétés hypnotiques avant que d'autres médicaments ne soient développés?
Quelle substance était historiquement utilisée pour ses propriétés hypnotiques avant que d'autres médicaments ne soient développés?
Quelle caractéristique distingue le sommeil de l'éveil?
Quelle caractéristique distingue le sommeil de l'éveil?
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Quel effet secondaire majeur est associé à l'utilisation d'hypnotiques, notamment ceux issus de l'opium?
Quel effet secondaire majeur est associé à l'utilisation d'hypnotiques, notamment ceux issus de l'opium?
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Quel est le principal avantage des benzodiazépines par rapport aux barbituriques ?
Quel est le principal avantage des benzodiazépines par rapport aux barbituriques ?
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Quel composé a ouvert la voie à la classe des benzodiazépines ?
Quel composé a ouvert la voie à la classe des benzodiazépines ?
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Quel est le mécanisme de préparation des barbituriques ?
Quel est le mécanisme de préparation des barbituriques ?
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Quel type de dérivés des antihistaminiques est encore exploité aujourd'hui ?
Quel type de dérivés des antihistaminiques est encore exploité aujourd'hui ?
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Qu'est-ce qui n'est pas vrai à propos de l'acide barbiturique ?
Qu'est-ce qui n'est pas vrai à propos de l'acide barbiturique ?
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Study Notes
Introduction to Hypnotics
- Hypnotics are substances that induce sedation and sleep in the central nervous system.
- Sleep is characterized by cyclical phases including paradoxical and slow-wave sleep.
- Hypnotics are a diverse group of medications with varying chemical structures, mechanisms of action, and side effects.
Sleep
- Sleep is a natural, recurring state characterized by loss of consciousness, reduced sensory activity, and muscle relaxation.
- It contrasts with wakefulness by a lowered responsiveness to external stimuli.
- It differs from a coma in that it's reversible.
- Insomnia is defined by difficulty falling asleep, or maintaining sleep, or waking up too early, with daytime functional impairment.
Historical Classification of Hypnotics
- Opium-based solutions (Laudanum) were used for centuries as sedatives and hypnotics.
- Bromides and paraldehyde were early hypnotics.
- Chloral hydrate and various alcohol derivatives followed, with barbituates becoming prominent.
- Antihistamines were later discovered to also have sedative properties.
- Benzodiazepines emerged to replace barbituates and other earlier hypnotic agents, due to their greater safety profile.
- More recently, drugs with similar mechanisms of action to benzodiazepines have been developed.
Barbituates
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Barbituates are a class of cyclic ureides derived from malonylurea.
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They are synthesized by condensing urea with malonic acid.
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Substitution on the malonic acid moiety can lead to different durations and intensities of action.
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Barbituates have been widely used, but replaced by benzodiazepines for their higher safety profile.
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Different barbituates have varying durations of action: from short- to long-acting
Benzodiazepines (BZDs)
- BZDs are a class of drugs that act by enhancing the effects of GABA on GABA receptors in the central nervous system..
- These drugs possess a high therapeutic index, less acute toxicity, and fewer side effects compared to the barbituates.
- Benzdiazepinone sub-types: 1-4-benzodiazepinone & 2-3-benzoodiazepinone
- Structures & Nomenclature
- Mechanisms of Action, including their roles in GABAergic transmission.
Newer Hypnotics
- Newer drugs demonstrate structural variations of chemical structure, including cyclopyrrolone or pyrazolopyrimidine sub-types) and imidazopyridine subtypes (like zolpidem).
- These newer hypnotics are often associated with a reduced risk of some adverse effects compared to older drugs like barbiturates.
- Differences in their duration and potency
Antihistamines
- Some antihistamines have sedative properties, often used as sleep aids.
- The sedative effect is due to central histamine inhibition and adrenolytic effects.
- These possess better safety profiles than barbituates, benzodiazepines
- Mechanism of action: antagonism of histamine H1 receptors.
Chloral Hydrate
- Chloral hydrate is a sedative and hypnotic agent.
- Its mechanism of action involves conversion to trichloroethanol by liver enzymes .
- This results in an effect on GABAergic transmission within the central nervous system.
- Important: Chloral hydrate has been linked to increased risk of cancer.
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Description
Ce quiz explore le monde des hypnotiques, des substances qui induisent la sédation et le sommeil. Il traite des phases du sommeil, des classifications historiques et des divers mécanismes d'action de ces médicaments. Testez vos connaissances sur les médicaments hypnotiques et leurs effets.
