メダゼパム。塩酸メダゼパム
WordNet
- a complex consisting of an organic base in association with hydrogen chloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2018/01/31 09:03:03」(JST)
[Wiki en表示]
Medazepam
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| Clinical data |
| Trade names |
Rudotel |
| AHFS/Drugs.com |
International Drug Names |
Routes of
administration |
Oral |
| ATC code |
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| Legal status |
| Legal status |
- CA: Schedule IV
- DE: Prescription only (Anlage III for higher doses)
- US: Schedule IV
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| Pharmacokinetic data |
| Bioavailability |
50–75% (Сmax = 1–2 hours) |
| Protein binding |
>99% |
| Metabolism |
Hepatic |
| Biological half-life |
2 hours, 36–150 hours (terminal) |
| Excretion |
Renal (63–85%), Biliary 15–37% |
| Identifiers |
IUPAC name
- 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepine
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| CAS Number |
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| PubChem CID |
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| DrugBank |
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| ChemSpider |
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| UNII |
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| KEGG |
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| ChEMBL |
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| ECHA InfoCard |
100.018.895 |
| Chemical and physical data |
| Formula |
C16H15ClN2 |
| Molar mass |
270.8 g/mol |
| 3D model (JSmol) |
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SMILES
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ClC1=CC(C(C2=CC=CC=C2)=NCCN3C)=C3C=C1
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InChI
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InChI=1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3 Y
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Key:YLCXGBZIZBEVPZ-UHFFFAOYSA-N Y
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| NY (what is this?) (verify) |
Medazepam is a drug that is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam.[1] Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.[2]
Contents
- 1 Pharmacology
- 2 See also
- 3 References
- 4 External links
Pharmacology
Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor.[3] Benzodiazepines may also act via micromolar benzodiazepine-binding sites as Ca2+ channel blockers and significantly inhibited depolarization-sensitive calcium uptake in experiments with cell components from rat brains. This has been conjectured as a mechanism for high dose effects against seizures in a study.[4] It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effects after administration.[5]
See also
- Benzodiazepine
- Benzodiazepine dependence
- Benzodiazepine withdrawal syndrome
- Long-term effects of benzodiazepines
References
- ^ Encyclopedia of Drugs: Benzodiazepines
- ^ Professor heather Ashton (April 2007). "BENZODIAZEPINE EQUIVALENCY TABLE". Retrieved September 23, 2007.
- ^ Zakusov VV; Ostrovskaya RU; Kozhechkin SN; Markovich VV; Molodavkin GM; Voronina TA. (October 1977). "Further evidence for GABA-ergic mechanisms in the action of benzodiazepines". Archives Internationales de Pharmacodynamie et de Thérapie. 229 (2): 313–26. PMID 23084.
- ^ Taft WC; DeLorenzo RJ (May 1984). "Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations" (PDF). Proc Natl Acad Sci USA (PDF). 81 (10): 3118–22. doi:10.1073/pnas.81.10.3118. PMC 345232 . PMID 6328498.
- ^ Jochemsen R, Breimer DD (1984). "Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles". Curr Med Res Opin. 8 Suppl 4: 60–79. doi:10.1185/03007998409109545. PMID 6144464.
External links
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Anxiolytics (N05B)
|
| 5-HT1AR agonists |
- Buspirone
- Gepirone†
- Tandospirone
|
| GABAAR PAMs |
- Benzodiazepines: Adinazolam
- Alprazolam
- Bromazepam
- Camazepam
- Chlordiazepoxide
- Clobazam
- Clonazepam
- Clorazepate
- Clotiazepam
- Cloxazolam
- Diazepam#
- Ethyl loflazepate
- Etizolam
- Fludiazepam
- Halazepam
- Ketazolam
- Lorazepam#
- Medazepam
- Nordazepam
- Oxazepam
- Pinazepam
- Prazepam; Others: Alpidem‡
- Barbiturates (e.g., phenobarbital)
- Carbamates (e.g., meprobamate)
- Chlormezanone‡
- Ethanol (alcohol)
- Etifoxine
- Imepitoin; Herbs:
- Kava
- Skullcap
- Valerian
|
Gabapentinoids
(α2δ VDCC blockers) |
- Gabapentin
- Gabapentin enacarbil
- Phenibut
- Pregabalin
|
| Antidepressants |
- SSRIs (e.g., escitalopram)
- SNRIs (e.g., duloxetine)
- SARIs (e.g., trazodone)
- TCAs (e.g., clomipramine)
- TeCAs (e.g., mirtazapine)
- MAOIs (e.g., phenelzine); Others: Agomelatine
- Bupropion
- Tianeptine
- Vilazodone
- Vortioxetine
|
Sympatholytics
(Antiadrenergics) |
- Alpha-1 blockers (e.g., prazosin)
- Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine)
- Beta blockers (e.g., propranolol)
|
| Others |
- Benzoctamine
- Cannabidiol
- Cycloserine
- Fabomotizole
- Hydroxyzine
- Kanna
- Lavender
- Lorpiprazole
- Mebicar
- Mepiprazole
- Nicotine
- Opipramol
- Oxaflozane‡
- Phenaglycodol
- Phenibut
- Picamilon
- Selank
- Tiagabine
- Tofisopam
- Validolum
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
GABAA receptor positive modulators
|
| Alcohols |
- Brometone
- Butanol
- Chloralodol
- Chlorobutanol (cloretone)
- Ethanol (alcohol) (alcoholic drink)
- Ethchlorvynol
- Isobutanol
- Isopropanol
- Menthol
- Methanol
- Methylpentynol
- Pentanol
- Petrichloral
- Propanol
- tert-Butanol (2M2P)
- tert-Pentanol (2M2B)
- Tribromoethanol
- Trichloroethanol
- Triclofos
- Trifluoroethanol
|
| Barbiturates |
- (-)-DMBB
- Allobarbital
- Alphenal
- Amobarbital
- Aprobarbital
- Barbexaclone
- Barbital
- Benzobarbital
- Benzylbutylbarbiturate
- Brallobarbital
- Brophebarbital
- Butabarbital/Secbutabarbital
- Butalbital
- Buthalital
- Butobarbital
- Butallylonal
- Carbubarb
- Crotylbarbital
- Cyclobarbital
- Cyclopentobarbital
- Difebarbamate
- Enallylpropymal
- Ethallobarbital
- Eterobarb
- Febarbamate
- Heptabarb
- Heptobarbital
- Hexethal
- Hexobarbital
- Metharbital
- Methitural
- Methohexital
- Methylphenobarbital
- Narcobarbital
- Nealbarbital
- Pentobarbital
- Phenallymal
- Phenobarbital
- Phetharbital
- Primidone
- Probarbital
- Propallylonal
- Propylbarbital
- Proxibarbital
- Reposal
- Secobarbital
- Sigmodal
- Spirobarbital
- Talbutal
- Tetrabamate
- Tetrabarbital
- Thialbarbital
- Thiamylal
- Thiobarbital
- Thiobutabarbital
- Thiopental
- Thiotetrabarbital
- Valofane
- Vinbarbital
- Vinylbital
|
| Benzodiazepines |
|
| Carbamates |
- Carisbamate
- Carisoprodol
- Clocental
- Cyclarbamate
- Difebarbamate
- Emylcamate
- Ethinamate
- Febarbamate
- Felbamate
- Hexapropymate
- Lorbamate
- Mebutamate
- Meprobamate
- Nisobamate
- Pentabamate
- Phenprobamate
- Procymate
- Styramate
- Tetrabamate
- Tybamate
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| Flavonoids |
- 6-Methylapigenin
- Ampelopsin (dihydromyricetin)
- Apigenin
- Baicalein
- Baicalin
- Catechin
- EGC
- EGCG
- Hispidulin
- Linarin
- Luteolin
- Rc-OMe
- Skullcap constituents (e.g., baicalin)
- Wogonin
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| Imidazoles |
- Etomidate
- Metomidate
- Propoxate
|
| Kava constituents |
- 10-Methoxyyangonin
- 11-Methoxyyangonin
- 11-Hydroxyyangonin
- Desmethoxyyangonin
- 11-Methoxy-12-hydroxydehydrokavain
- 7,8-Dihydroyangonin
- Kavain
- 5-Hydroxykavain
- 5,6-Dihydroyangonin
- 7,8-Dihydrokavain
- 5,6,7,8-Tetrahydroyangonin
- 5,6-Dehydromethysticin
- Methysticin
- 7,8-Dihydromethysticin
- Yangonin
|
| Monoureides |
- Acecarbromal
- Apronal (apronalide)
- Bromisoval
- Carbromal
- Capuride
- Ectylurea
|
| Neuroactive steroids |
- Acebrochol
- Allopregnanolone (brexanolone)
- Alfadolone
- Alfaxalone
- 3α-Androstanediol
- Androstenol
- Androsterone
- Certain anabolic-androgenic steroids
- Cholesterol
- DHDOC
- 3α-DHP
- 5α-DHP
- 5β-DHP
- DHT
- Etiocholanolone
- Ganaxolone
- Hydroxydione
- Minaxolone
- ORG-20599
- ORG-21465
- P1-185
- Pregnanolone (eltanolone)
- Progesterone
- Renanolone
- SAGE-105
- SAGE-217
- SAGE-324
- SAGE-516
- SAGE-689
- SAGE-872
- Testosterone
- THDOC
|
| Nonbenzodiazepines |
- β-Carbolines: Abecarnil
- Gedocarnil
- Harmane
- SL-651,498
- ZK-93423
- Cyclopyrrolones: Eszopiclone
- Pagoclone
- Pazinaclone
- Suproclone
- Suriclone
- Zopiclone
- Imidazopyridines: Alpidem
- DS-1
- Necopidem
- Saripidem
- Zolpidem
- Pyrazolopyrimidines: Divaplon
- Fasiplon
- Indiplon
- Lorediplon
- Ocinaplon
- Panadiplon
- Taniplon
- Zaleplon
- Others: Adipiplon
- CGS-8216
- CGS-9896
- CGS-13767
- CGS-20625
- CL-218,872
- CP-615,003
- CTP-354
- ELB-139
- GBLD-345
- Imepitoin
- JM-1232
- L-838,417
- Lirequinil (Ro41-3696)
- NS-2664
- NS-2710
- NS-11394
- Pipequaline
- ROD-188
- RWJ-51204
- SB-205,384
- SX-3228
- TGSC01AA
- TP-003
- TPA-023
- TP-13
- U-89843A
- U-90042
- Viqualine
- Y-23684
|
| Phenols |
- Fospropofol
- Propofol
- Thymol
|
| Piperidinediones |
- Glutethimide
- Methyprylon
- Piperidione
- Pyrithyldione
|
| Pyrazolopyridines |
- Cartazolate
- Etazolate
- ICI-190,622
- Tracazolate
|
| Quinazolinones |
- Afloqualone
- Cloroqualone
- Diproqualone
- Etaqualone
- Mebroqualone
- Mecloqualone
- Methaqualone
- Methylmethaqualone
- Nitromethaqualone
- SL-164
|
| Volatiles/gases |
- Acetone
- Acetophenone
- Acetylglycinamide chloral hydrate
- Aliflurane
- Benzene
- Butane
- Butylene
- Centalun
- Chloral
- Chloral betaine
- Chloral hydrate
- Chloroform
- Cryofluorane
- Desflurane
- Dichloralphenazone
- Dichloromethane
- Diethyl ether
- Enflurane
- Ethyl chloride
- Ethylene
- Fluroxene
- Gasoline
- Halopropane
- Halothane
- Isoflurane
- Kerosine
- Methoxyflurane
- Methoxypropane
- Nitric oxide
- Nitrogen
- Nitrous oxide
- Norflurane
- Paraldehyde
- Propane
- Propylene
- Roflurane
- Sevoflurane
- Synthane
- Teflurane
- Toluene
- Trichloroethane (methyl chloroform)
- Trichloroethylene
- Vinyl ether
|
| Others/unsorted |
- 3-Hydroxybutanal
- α-EMTBL
- AA-29504
- Avermectins (e.g., ivermectin)
- Bromide compounds (e.g., lithium bromide, potassium bromide, sodium bromide)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- DEABL
- Dihydroergolines (e.g., dihydroergocryptine, dihydroergosine, dihydroergotamine, ergoloid (dihydroergotoxine))
- DS2
- Efavirenz
- Etazepine
- Etifoxine
- Fenamates (e.g., flufenamic acid, mefenamic acid, niflumic acid, tolfenamic acid)
- Fluoxetine
- Flupirtine
- Hopantenic acid
- Lanthanum
- Lavender oil
- Lignans (e.g., 4-O-methylhonokiol, honokiol, magnolol, obovatol)
- Loreclezole
- Menthyl isovalerate (validolum)
- Monastrol
- Niacin
- Nicotinamide (niacinamide)
- Org 25,435
- Phenytoin
- Propanidid
- Retigabine (ezogabine)
- Safranal
- Seproxetine
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal), tetronal, trional)
- Terpenoids (e.g., borneol)
- Topiramate
- Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol)
- Unsorted benzodiazepine site positive modulators: α-Pinene
- MRK-409 (MK-0343)
- TCS-1105
- TCS-1205
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|
See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators
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English Journal
Related Links
- Medazepam hydrochloride [USAN] S 804 CCRIS 1916 EINECS 220-782-9
- Medazepam hydrochloride Molecular Formula C 16 H 16 Cl 2 N 2 Average mass 307.218 Da Monoisotopic mass 306.069061 Da ChemSpider ID 16934 More details: Systematic name 7-Chloro-1-methyl-5-phenyl-2,3-dihydro-1 H-1 ...
- A benzodiazepine derivative used in the treatment of anxiety. It has sedative, muscle relaxant, and anticonvulsant properties. One of its metabolites is DIAZEPAM and one of its excretion products is OXAZEPAM.
★リンクテーブル★
[★]
- 英
- medazepam
- ラ
- medazepamum
- 化
- 塩酸メダゼパム medazepam hydrochloride
- 商
- レスミット、パムネース
[★]
塩酸塩、ハイドロクロライド