テラゾシン。塩酸テラゾシン
WordNet
- a complex consisting of an organic base in association with hydrogen chloride
- antihypertensive drug (trade name Hytrin) used to treat high blood pressure (同)Hytrin
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/04/25 09:02:41」(JST)
[Wiki en表示]
Terazosin
|
Systematic (IUPAC) name |
(RS)-6,7-dimethoxy-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine |
Clinical data |
Trade names |
Hytrin |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a693046 |
Legal status |
RX-Only (US) |
Pharmacokinetic data |
Protein binding |
90-94% |
Half-life |
12 hours |
Identifiers |
CAS number |
63590-64-7 Y |
ATC code |
G04CA03 |
PubChem |
CID 5401 |
DrugBank |
DB01162 |
ChemSpider |
5208 Y |
UNII |
8L5014XET7 Y |
KEGG |
D08569 Y |
ChEBI |
CHEBI:9445 Y |
ChEMBL |
CHEMBL611 Y |
Synonyms |
[4-(4-amino-6,7-dimethoxy-quinazolin-2-yl)piperazin-1-yl]-tetrahydrofuran-2-yl-methanone |
Chemical data |
Formula |
C19H25N5O4 |
Mol. mass |
387.433 g/mol |
SMILES
- O=C(N3CCN(c2nc1cc(OC)c(OC)cc1c(n2)N)CC3)C4OCCC4
|
InChI
-
InChI=1S/C19H25N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22) Y
Key:VCKUSRYTPJJLNI-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
Terazosin (marketed as Hytrin or Zayasel) is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It also acts to lower the blood pressure, and is therefore a drug of choice for men with hypertension and prostate enlargement.
It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Most common side effects include dizziness, drowsiness, headache, constipation, loss of appetite, fatigue, nasal congestion or dry eyes, but they generally go away after only a few days of use. Therapy should always be started with a low dose to avoid first dose phenomenon.[1] Sexual side effects are rare, but may include priapism or erectile dysfunction.
References
- ^ Hytrin (Terazosin Hcl) drug warnings and precautions - prescription drugs and medications at RxList
Drugs used in benign prostatic hypertrophy (G04C)
|
|
5α-reductase inhibitors |
|
|
Alpha blockers (α1) |
- Alfuzosin
- Doxazosin
- Silodosin
- Tamsulosin
- Terazosin
|
|
Herbals |
- Pygeum africanum
- Saw palmetto extract
|
|
Other |
|
|
|
|
noco/cong/tumr, sysi/epon
|
|
|
|
|
Adrenergics
|
|
Receptor ligands
|
|
α1
|
- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
* Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
|
|
α2
|
- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
|
|
β
|
|
|
|
|
Reuptake inhibitors
|
|
NET
|
- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
|
|
VMAT
|
- Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
|
|
|
Enzyme inhibitors
|
|
Anabolism
|
PAH
|
|
|
TH
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
AAAD
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
DBH
|
- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
|
|
PNMT
|
- CGS-19281A
- SKF-64139
- SKF-7698
|
|
|
Catabolism
|
MAO
|
- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also D-Deprenyl)
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
|
|
COMT
|
- Entacapone
- Nitecapone
- Tolcapone
|
|
|
|
|
Others
|
|
Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
|
|
Cofactors
|
- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
|
|
Others
|
- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
|
|
|
|
List of adrenergic drugs
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Anti-hypertensive treatment in pheochromocytoma and paraganglioma: current management and therapeutic features.
- Mazza A1, Armigliato M, Marzola MC, Schiavon L, Montemurro D, Vescovo G, Zuin M, Chondrogiannis S, Ravenni R, Opocher G, Colletti PM, Rubello D.Author information 1Department of Internal Medicine, Santa Maria della Misericordia Hospital, Viale Tre Martiri 140, 45100, Rovigo, Italy, mazza.alberto@azisanrovigo.it.AbstractPheochromocytoma (PH) and paraganglioma (PG) are neuroendocrine neoplasms arising from chromaffin cells of the adrenal medulla and the sympathetic ganglia, respectively. Although are unusual cause of hypertension (HT) accounting for at most 0.1-0.2 % of cases, they may lead to severe and potentially lethal hypertensive crisis due to the effects of the released catecholamines. However, both PH and PG may be asymptomatic as ~30 % of subjects are normotensive or have orthostatic hypotension and in these cases the 24 h ambulatory blood pressure (BP) monitoring is an important toll to diagnose and treat HT. HT treatment may be difficult when PH or PG occurs in pregnancy or in the elderly subjects and in these cases a multidisciplinary team is required. When surgical excision is mandatory the perioperative management requires the administration of selective α1-adrenergic blocking agents (i.e., doxazosin, prazosin or terazosin) followed by a β-adrenergic blockade (i.e., propranolol, atenolol). This latter should never be started first because blockade of vasodilatory peripheral β-adrenergic receptors with unopposed α-adrenergic receptor stimulation can lead to a further elevation of BP. Although labetalol is traditionally considered the ideal agent due to its α- and β-adrenergic antagonism, experimental studies do not support its use in this clinical setting. As second regimen, the administration of vasodilators as calcium channel blockers (i.e., nicardipine, nifedipine) may be required to control BP. Oral and sublingual short-acting nifedipine are potentially dangerous in patients with hypertensive emergencies and are not recommend. The latest evidences into the diagnosis and treatment of hypertensive crisis due to PH and PG are reviewed here.
- Endocrine.Endocrine.2014 Apr;45(3):469-78. doi: 10.1007/s12020-013-0007-y. Epub 2013 Jul 2.
- Pheochromocytoma (PH) and paraganglioma (PG) are neuroendocrine neoplasms arising from chromaffin cells of the adrenal medulla and the sympathetic ganglia, respectively. Although are unusual cause of hypertension (HT) accounting for at most 0.1-0.2 % of cases, they may lead to severe and potentiall
- PMID 23817839
- α-Adrenergic Blockers for the Treatment of Lower-Urinary-Tract Symptoms and Dysfunction in Women.
- Boyd K1, Hilas O.Author information 1UAB Medicine, Birmingham, AL, USA.AbstractOBJECTIVE: To evaluate the efficacy and safety of α-adrenergic blockers in the treatment of female lower-urinary-tract symptoms and dysfunction.
- The Annals of pharmacotherapy.Ann Pharmacother.2014 Mar 10. [Epub ahead of print]
- OBJECTIVE: To evaluate the efficacy and safety of α-adrenergic blockers in the treatment of female lower-urinary-tract symptoms and dysfunction.DATA SOURCES: Literature searches were conducted using EMBASE (1974 to January 2014), International Pharmaceutical Abstracts (1970 to January 2014), and ME
- PMID 24615630
- Doxazosin selectively potentiates contraction to serotonin via 5-HT2A receptors in longitudinal muscle strips of the rabbit gastric body.
- Zhao Y1, Cao XB, Ren LM.Author information 1a Department of Pharmacology, Institute of Chinese Integrative Medicine, Hebei Medical University, 361 East Zhong-shan Road, Shijiazhuang 050017, Hebei, P.R. China.AbstractThe aims of this study were to examine the effects of doxazosin on contractile responses to 5-hydroxytryptamine (5-HT), carbachol, and histamine, and to compare them with those of prazosin, alfuzosin, and terazosin, and then characterize a pharmacological profile of the 5-HT-induced contractile response using preparations of isolated longitudinal muscle strips from the rabbit gastric body. The results from these preparations showed that the contraction response to 5-HT, but not to carbachol or histamine, was found to be dose-dependently potentiated by doxazosin and its enantiomers. The specific potentiation effect on 5-HT was not observed in the preparations that were treated with prazosin, terazosin, or alfuzosin. The contractile response to 5-HT and its potentiation by doxazosin were not affected by treatment with phenoxybenzamine. However, 5-HT-induced contraction was competitively antagonized by nefazodone (with pA2 value of 8.64 ± 0.17), and was almost completely inhibited by treatment with indomethacin. In conclusion, doxazosin, but not prazosin, alfuzosin, or terazosin, selectively potentiates 5-HT-induced contraction in the rabbit gastric body strips via an α1-adrenoceptor-independent mechanism, without chiral recognition of its enantiomers. Additionally, the contraction to 5-HT was found to be mediated via 5-HT2A receptors, and was similar to PGs synthesis in the preparations.
- Canadian journal of physiology and pharmacology.Can J Physiol Pharmacol.2014 Mar;92(3):197-204. doi: 10.1139/cjpp-2013-0067. Epub 2013 Dec 18.
- The aims of this study were to examine the effects of doxazosin on contractile responses to 5-hydroxytryptamine (5-HT), carbachol, and histamine, and to compare them with those of prazosin, alfuzosin, and terazosin, and then characterize a pharmacological profile of the 5-HT-induced contractile resp
- PMID 24593784
Japanese Journal
- 前立腺肥大症に伴う排尿障害に対する塩酸テラゾシンの有用性の検討 ―1日1回投与と1日2回投与の多施設共同比較試験―
- 鈴木 英訓,大西 哲郎,池本 庸,大石 幸彦,鈴木 康之,山崎 春城
- 泌尿器科紀要 47(2), 77-81, 2001-02
- … 均尿流量率において,1日1回投与群,1日2回投与群共に有意な改善を認め,かつ2群間では差を認めなかった.副作用はいずれも軽度であった.よって2群間の有用性に差はないものと考え,塩酸テラゾシン1日1回投与法は薬剤コンブライアンスの点から推奨できる有用な治療法と考えたWe compared the efficacy of once a day administration of terazosin hydrochloride with that of twice a day administration for benign prostatic hyperplasia (BPH) …
- NAID 120002142071
- 佐々木 昌一,林 祐太郎,郡 健二郎,寺尾 暎治,池井 和紀,伏見 登,渡瀬 秀樹,堀 武,平尾 憲昭,岩瀬 豊,加藤 文英,最上 徹,戸澤 啓一,多和田 俊保
- 西日本泌尿器科 60(2), 120-123, 1998-02-20
- NAID 10019101592
- 大鳥 聡,出口 敬章,東條 角治
- あたらしい眼科 = Journal of the eye 13(8), 1263-1266, 1996-08-30
- NAID 10018592577
Related Links
- te·ra·zo·sin hydrochloride (t-r z-s n) n. A crystalline compound that blocks adrenergic receptors and is used to treat hypertension. terazosin hydrochloride Hytrin Pharmacologic class: Anti-adrenergic (peripherally acting) Therapeutic ...
- Terazosin hydrochloride definition at Dictionary.com, a free online dictionary with pronunciation, synonyms and translation. Look it up now! Thesaurus Translator Reference Word of the Day Blog Slideshows Apps by Dictionary ...
Related Pictures
★リンクテーブル★
[★]
- 英
- terazosin
- 化
- 塩酸テラゾシン terazosin hydrochloride
- 商
- ハイトラシン、バソメット
[★]
- 英
- terazosin hydrochloride
- 関
- テラゾシン
[★]
塩酸塩、ハイドロクロライド