Information about Zaleplon
Zaleplon (marketed under the brand names Sonata and Starnoc) is a sedative/hypnotic, mainly used for insomnia. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class.
Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Although not a benzodiazepine, zaleplon can cause similar effects: anterograde amnesia (forgetting the period during the effects) as the most common.
Zaleplon is primarily metabolised by aldehyde oxidase, and its half-life can be affected by substances which inhibit or induce aldehyde oxidase.
A meta-analysis of randomised controlled clinical trials which compared benzodiazepines against Zaleplon or other Z Drugs such as zolpidem, zopiclone has found that there are few clear and consistent differences between Zaleplon and the benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia and daytime alertness.[1]
Zaleplon has a pharmacological profile similar to benzodiazepines, that is characterized by an increase in SWDS with rapid onset of hypnotic action. Zaleplon is a selective full agonist for the benzodiazepine omega1 receptor located on the GABAA receptor ionophore complex in the brain. It selectively enhances the action of GABA similar to but more selectively than benzodiazepines. Zaleplon, although not benzodiazepine-like in chemical structure induces sedative-hypnotic, anticonvulsant and anticonflict effects via by its binding to the central nervous system (CNS) type benzodiazepine receptors. The elimination half life of zaleplon is 1 hour irrespective of dose. Absorption of is rapid. Zaleplon can be classed as an ultra short acting sedative hypnotic drug for the treatment of insomnia characterised by difficulty in falling asleep. Zaleplon increases EEG power density in the delta frequency band and a decrease in the energy of the theta frequency band. In tests on rabbits zaelplon shows drowsy pattern of spontaneous EEG characterized by high-voltage slow waves and desynchronization of hippocampal theta waves and an increase in the energy of the delta frequency band on the spectral analysis of the electroencephalogram.[2]
Zaleplon is habit-forming, meaning addiction may occur. Stopping this medication suddenly after prolonged or frequent use may cause withdrawal effects such as mood changes, anxiety, and restlessness.
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Chemistry
Zaleplon is a white to off-white powder that has very low solubility in water as well as low solubility in alcohol and propylene glycol. It has a partition coefficient in octanol/water is constant (log PC = 1.23) when the pH range is between 1 and 7.Pharmacology
Taken orally, zaleplon reaches full concentration in approximately one hour. It is extensively metabolised, into 5-oxo-zaleplon and 5-oxo-desethylzaleplon (the latter via desethylzaleplon), with less than 1% of it excreted intact in urine.Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Although not a benzodiazepine, zaleplon can cause similar effects: anterograde amnesia (forgetting the period during the effects) as the most common.
Zaleplon is primarily metabolised by aldehyde oxidase, and its half-life can be affected by substances which inhibit or induce aldehyde oxidase.
A meta-analysis of randomised controlled clinical trials which compared benzodiazepines against Zaleplon or other Z Drugs such as zolpidem, zopiclone has found that there are few clear and consistent differences between Zaleplon and the benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia and daytime alertness.[1]
Zaleplon has a pharmacological profile similar to benzodiazepines, that is characterized by an increase in SWDS with rapid onset of hypnotic action. Zaleplon is a selective full agonist for the benzodiazepine omega1 receptor located on the GABAA receptor ionophore complex in the brain. It selectively enhances the action of GABA similar to but more selectively than benzodiazepines. Zaleplon, although not benzodiazepine-like in chemical structure induces sedative-hypnotic, anticonvulsant and anticonflict effects via by its binding to the central nervous system (CNS) type benzodiazepine receptors. The elimination half life of zaleplon is 1 hour irrespective of dose. Absorption of is rapid. Zaleplon can be classed as an ultra short acting sedative hypnotic drug for the treatment of insomnia characterised by difficulty in falling asleep. Zaleplon increases EEG power density in the delta frequency band and a decrease in the energy of the theta frequency band. In tests on rabbits zaelplon shows drowsy pattern of spontaneous EEG characterized by high-voltage slow waves and desynchronization of hippocampal theta waves and an increase in the energy of the delta frequency band on the spectral analysis of the electroencephalogram.[2]
Side-effects
Zaleplon may cause hallucinations, abnormal behavior, severe confusion, day-time drowsiness, dizziness or lightheadedness, unsteadiness and/or falls, double vision or other vision problems, agitation, headache, nausea, vomiting, diarrhea or abdominal pain, depression, muscle weakness, tremor, vivid or abnormal dreams and memory difficulties or amnesia.Zaleplon is habit-forming, meaning addiction may occur. Stopping this medication suddenly after prolonged or frequent use may cause withdrawal effects such as mood changes, anxiety, and restlessness.
Recreational use
Zaleplon (Sonata) has a relatively high potential to be abused. Often this use involves a different delivery method (snorting) to induce effects faster. The side effects of Zaleplon are greatly increased when taken improperly, especially memory loss, including the inability to remember the time during which the user was under the influence of the drug. Zaleplon is a nonbenzodiazepine drug, and research on other nonbenzodiazepine drugs has indicated that their potential for abuse was far lower than that of benzodiazepine drugs, but that nonbenzodiazepines still carried a risk higher than first believed. The study specifically mentions persons with prior substance abuse problems as individuals with a high risk for addiction to nonbenzodiazepine type drugs. [3]References
1. ^ Dündar, Y; Dodd S, Strobl J, Boland A, Dickson R, Walley T. (Jul 2004). "Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis.". Hum Psychopharmacol. 19 (5): 305-22. PMID 15252823.
2. ^ Noguchi H; Kitazumi K, Mori M, Shiba T. (Mar 2004). "Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats." (pdf). J Pharmacol Sci. 94 (3): 246-51. PMID 15037809.
3. ^ [1]
2. ^ Noguchi H; Kitazumi K, Mori M, Shiba T. (Mar 2004). "Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats." (pdf). J Pharmacol Sci. 94 (3): 246-51. PMID 15037809.
3. ^ [1]
A sedative is a substance that depresses the central nervous system (CNS), resulting in calmness, relaxation, reduction of anxiety, sleepiness, and slowed breathing, as well as slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes.
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Hypnotic drugs are a class of drugs that induce sleep (which differentiates them from the sedative category), used in the treatment of insomnia and in surgical anesthesia. Often the treatment of insomnia will not begin with drugs at all.
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MeSH D007319
Insomnia is a sleeping disorder characterized by the inability to fall asleep and/or the inability to remain asleep for a reasonable amount of time.
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Insomnia is a sleeping disorder characterized by the inability to fall asleep and/or the inability to remain asleep for a reasonable amount of time.
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The nonbenzodiazepines are comparatively new drugs whose actions are very similar to those of the benzodiazepines, but are structurally unrelated to the benzodiazepines and are believed to have fewer side effects.
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Hypnotic drugs are a class of drugs that induce sleep (which differentiates them from the sedative category), used in the treatment of insomnia and in surgical anesthesia. Often the treatment of insomnia will not begin with drugs at all.
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The Pyrazolopyrimidines are a class of sedative and anxiolytic drugs related (in terms of their effect) to benzodiazepines.
Most of the drugs from this class marketed to date are intended to induce sleep, and are prescribed for people suffering insomnia, however some newer
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Most of the drugs from this class marketed to date are intended to induce sleep, and are prescribed for people suffering insomnia, however some newer
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Solubility is a physical property referring to the ability for a given substance, the solute, to dissolve in a solvent.[1] It is measured in terms of the maximum amount of solute dissolved in a solvent at equilibrium. The resulting solution is called a saturated solution.
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alcohol is any organic compound in which a hydroxyl group (-OH) is bound to a carbon atom of an alkyl or substituted alkyl group. The general formula for a simple acyclic alcohol is CnH2n+1OH.
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Propylene glycol, known also by the systematic name propane-1,2-diol, is an organic compound (a diol alcohol), usually a tasteless, odorless, and colorless clear oily liquid that is hygroscopic and miscible with water, acetone, and chloroform.
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The GABA receptors are a class of receptors that respond to the neurotransmitter γ-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system.
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Pharmacology is the study of how drugs interact with living organisms to produce a change in function.[1] If substances have medicinal properties, they are considered pharmaceuticals.
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The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
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The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
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Anterograde amnesia
Classifications and external resources
ICD-10 R 41.1
ICD-9 780.93
Anterograde amnesia is a form of amnesia, or memory loss, in which new events are not transferred from short-term memory to long-term memory.
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Classifications and external resources
ICD-10 R 41.1
ICD-9 780.93
Anterograde amnesia is a form of amnesia, or memory loss, in which new events are not transferred from short-term memory to long-term memory.
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Identifiers
Symbol AOX2
Entrez 344454
HUGO 18450
RefSeq NR_001557
Other data
Locus Chr. 2 q33.2 Aldehyde oxidase is an enzyme which generates carboxylic acids from aldehydes.
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Symbol AOX2
Entrez 344454
HUGO 18450
RefSeq NR_001557
Other data
Locus Chr. 2 q33.2 Aldehyde oxidase is an enzyme which generates carboxylic acids from aldehydes.
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In statistics, a meta-analysis combines the results of several studies that address a set of related research hypotheses. The first meta-analysis was performed by Karl Pearson in 1904, in an attempt to overcome the problem of reduced statistical power in studies with small sample
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In health care, a clinical trial is a comparison test of a medication or other medical treatment (such as a medical device), versus a placebo (inactive look-a-like), other medications/devices, or the standard medical treatment for a patient's condition.
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Zolpidem is a prescription short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to benzodiazepine receptors which are located on the gamma-aminobutyric acid receptors.
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Zopiclone (pronunciation perhaps IPA: /ˈzɒpɪkloʊn/) sold as Imovane and Zimovane in Europe, and as the eszopiclone analogue Lunesta
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The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
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The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
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The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
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Electroencephalography is the neurophysiologic measurement of the electrical activity of the brain by recording from electrodes placed on the scalp or, in special cases, subdurally or in the cerebral cortex.
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A hallucination is a perception in the absence of a stimulus that is believed to be genuine, ie. the subject experiences an imaginary stimulus as being real. A pseudohallucination is similar to an hallucination in all respects except that of absolute belief in the authenticity of
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Severe mental confusion of a degree considered pathological usually refers to loss of orientation (ability to place oneself correctly in the world by time, location, and personal identity), and often memory (ability to correctly recall previous events or learn new material).
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dizziness. Common descriptions include words such as lightheaded, floating, whoozy, giddy, confused, helpless or fuzzy. Vertigo, Disequilibrium and Pre-syncope are the terms in use by most doctors. Dizziness is sometimes a symptom of a balance disorder.
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Double vision refers to Diplopia, the perception of two images from a single object.
Double vision may also refer to:
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Double vision may also refer to:
- Double Vision (album), a 1978 album by Foreigner
- Double Vision (film), a 2002 film by Chen Kuo-fu
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Headache
Classifications and external resources
ICD-10 R 51.
ICD-9 784.0
A headache (cephalgia in medical terminology) is a condition of pain in the head; sometimes neck or upper back pain may also be interpreted as a headache.
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Classifications and external resources
ICD-10 R 51.
ICD-9 784.0
A headache (cephalgia in medical terminology) is a condition of pain in the head; sometimes neck or upper back pain may also be interpreted as a headache.
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