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antihypertensive drug (trade name Minipress) (同)Minipress

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/24 14:44:13」(JST)

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Prazosin, trade names Minipress, Vasoflex, Pressin and Hypovase, is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder. It is an alpha-adrenergic blocker that is specific for the alpha-1 receptors. These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of norepinephrine. They are also found throughout the central nervous system.^[1] As of 2013, prazosin is off-patent in the US, and the FDA has approved at least one generic manufacturer.

In addition to its alpha-blocking activity, prazosin is an antagonist of the MT₃ receptor (which is not present in humans), with selectivity for this receptor over the MT₁ and MT₂ receptors.^[2]

Medical use

Prazosin is orally active and has a minimal effect on cardiac function due to its alpha-1 receptor selectivity. However, when prazosin is started, heart rate and contractility go up in order to maintain the pre-treatment blood pressures because the body has reached homeostasis at its abnormally high blood pressure. The blood pressure lowering effect becomes apparent when prazosin is taken for longer periods of time. The heart rate and contractility go back down over time and blood pressure decreases.

The antihypertensive characteristics of prazosin make it a second-line choice for the treatment of high blood pressure.^[3]

Prazosin is also useful in treating urinary hesitancy associated with prostatic hyperplasia, blocking alpha-1 receptors, which control constriction of both the prostate and urethra. Although not a first line choice for either hypertension or prostatic hyperplasia, it is a choice for patients who present with both problems concomitantly.^[3]

This medication has shown to be effective in treating severe nightmares in children and people with PTSD symptoms.^[4] Veterans have also been treated successfully at Seattle's VA Puget Sound Health Care System (VAPSHCS) for sleep disturbance related to PTSD. Doses are lower for this purpose than for control of blood pressure.^[4]

Prazosin holds promise as a pharmacologic treatment for alcohol dependence after a 2009 pilot trial^[5] was completed. A larger controlled Phase II "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently underway.^[6]

The drug is usually recommended for severe stings from Indian Red Scorpion Hottentotta tamulus in Indian Subcontinent.^[7]^[8]^[9]

Adverse effects

Side effects of prazosin include orthostatic hypotension, syncope, and nasal congestion. The orthostatic hypotension and syncope are associated with the body's poor ability to control blood pressure without active alpha-adrenergic receptors. Patients on prazosin should be told not to stand up too quickly, since their poor baroreflex may cause them to faint if their blood pressure is not adequately maintained during standing. The nasal congestion is due to dilation of vessels in the nasal mucosa.

One phenomenon associated with prazosin is known as the "first dose response", in which the side effects of the drug, especially orthostatic hypotension and fainting, are especially pronounced in the first dose.

One very rare side effect of prazosin is priapism.^[10]

Another possible side effect is dreaming while awake or hallucinations of wakefulness while falling asleep on the medication (see oneirophrenia).^{[citation needed]}

References

^ Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy 13 (2): 115–139. doi:10.1016/S0891-0618(97)00042-2. PMID 9285356.
^ Yu CX, Zhu CB, Xu SF, Cao XD, Wu GC (March 2000). "Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats". Neuroscience Letters 282 (3): 161–4. doi:10.1016/S0304-3940(00)00883-1. PMID 10717416.
^ ^a ^b Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN 1-59541-101-1.
^ ^a ^b "Drug Helps PTSD Nightmares" (PDF) (Press release). VA Research Currents. April 2007. Retrieved 2014-01-06.
^ Simpson, TL; Saxon, AJ; Meredith, CW; Malte, CA; McBride, B; Ferguson, LC; Gross, CA; Hart, KL; Raskind, M (2009). "A pilot trial of the alpha-1 adrenergic antagonist, prazosin, for alcohol dependence". Alcoholism, clinical and experimental research 33 (2): 255–63. doi:10.1111/j.1530-0277.2008.00807.x. PMID 18945226.
^ Study of the Medication Prazosin for Alcohol Dependence
^ Bawaskar, H.S. & P.H. Bawaskar (2008). "Scorpion sting: A study of clinical manifestations and treatment regimes" (PDF). Current Science 95 (9): 1337–1341. Retrieved 14 April 2010.
^ Bawaskar, H.S. & P.H. Bawaskar (2007). "Utility of scorpion anti-venin vs. prazosin in the management of severe Mesobuthus tamulus (Indian red scorpion) envenoming at rural settings" (PDF). JAPI 55: 14–21. Retrieved 14 April 2010.
^ Pandi, K.; Krishnamurthy, S.; Srinivasaraghavan, R.; Mahadevan, S. (18 February 2014). "Efficacy of scorpion antivenom plus prazosin versus prazosin alone for Mesobuthus tamulus scorpion sting envenomation in children: a randomised controlled trial". Archives of Disease in Childhood 99 (6): 575–580. doi:10.1136/archdischild-2013-305483.
^ Bhalla AK, Hoffbrand BI, Phatak PS, Reuben SR (October 1979). "Prazosin and priapism". Br Med J 2 (6197): 1039. doi:10.1136/bmj.2.6197.1039. PMC 1596841. PMID 519276.

UpToDate Contents

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1. Sleep-wake disorders in patients with traumatic brain injury
2. 心的外傷後ストレス障害の薬物療法 pharmacotherapy for posttraumatic stress disorder
3. 物質使用障害および不安関連障害を併発した成人の治療 treatment of co occurring substance use disorder and anxiety related disorders in adults
4. 降圧剤と脂質 antihypertensive drugs and lipids
5. 初期治療に抵抗性を示したレイノー現象の治療 treatment of the raynaud phenomenon resistant to initial therapy

English Journal

Altered liver α(1)-adrenoceptor density and phospholipase C activity in the human hepatocellular carcinoma.

Kassahun WT, Günl B, Jonas S, Ungemach FR, Abraham G.SourceUniversity of Leipzig, Department of Surgery II, Liebig Straße 20a, Germany.
European journal of pharmacology.Eur J Pharmacol.2011 Nov 16;670(1):92-5. Epub 2011 Sep 2.
The human hepatocellular carcinoma (HCC) is a common cancer with high mortality rate. We examined the density and coupling to phospholipase C (PLC) of the α(1)-adrenoceptors. In HCC liver, the α(1)-adrenoceptor density - as assessed by [³H]-Prazosin binding - was significantly reduced to about 75
PMID 21910987

Norepinephrine reduces ω-Conotoxin-sensitive Ca2+-Currents in Renal Afferent Neurons in Rats.

Ditting T, Linz P, Freisinger W, Heinlein S, Reeh PW, Fiedler C, Siegel K, Scrogin KE, Neuhuber W, Veelken R.Source1Friedrich Alexander University Erlangen-Nuremberg.
American journal of physiology. Renal physiology.Am J Physiol Renal Physiol.2011 Nov 2. [Epub ahead of print]
Sympathetic efferent and peptidergic afferent renal nerves likely influence hypertensive and inflammatory kidney disease. Our recent investigation with confocal microscopy revealed that in the kidney, sympathetic nerve endings are co-localized with afferent nerve fibers. However, it is not known whe
PMID 22049399

Japanese Journal

Restraint Stress Induces Connexin-43 Translocation via α-Adrenoceptors in Rat Heart

UNUMA Kana,SHINTANI ISHIDA Kaori,YAHAGI Naoki,TSUSHIMA Kensuke,SHIMOSAWA Tatsuo,UEYAMA Takashi,YOSHIDA Ken-ichi
Circulation journal : official journal of the Japanese Circulation Society 74(12), 2693-2701, 2010-11-25
… IMO induced translocation of Cx43 to the GJ-enriched membrane fraction, with a peak at 60min. The IMO-induced Cx43 translocation was inhibited by pretreatment with the α1-adrenoceptor blockers, prazosin (1mg/kg, PO) and bunazosin (4mg/kg, PO), but not with either the β1-blocker, metoprolol (10mg/kg, IP), or the β1+2-blocker, propranolol (1mg/kg, PO). …
NAID 10027424654

Determination of metoclopramide in human plasma by LC-ESI-MS and its application to bioequivalance studies

YAN Miao,LI Huan-De,CHEN Ben-Mei,LIU Xiao-Lei,ZHU Yun-Gui
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 878(11), 883-887, 2010-04-01
NAID 10028034141

Related Pictures

★リンクテーブル★

リンク元	「薬理学」「プラゾシン」「α受容体遮断薬」
拡張検索	「prazosin hydrochloride」

「薬理学」

Prazosin
Systematic (IUPAC) name
	2-[4-(2-Furoyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine
Clinical data
Trade names	Minipress
AHFS/Drugs.com	monograph
MedlinePlus	a682245
Legal status	UK: Prescription-only (POM);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	~60%
Protein binding	97%
Biological half-life	2–3 hours
Identifiers
CAS Registry Number	19216-56-9
ATC code	C02CA01
PubChem	CID: 4893
IUPHAR/BPS	503
DrugBank	DB00457
ChemSpider	4724
UNII	XM03YJ541D
KEGG	D08411
ChEBI	CHEBI:8364
ChEMBL	CHEMBL2
Chemical data
Formula	C19H21N5O4
Molecular mass	383.401 g/mol
	SMILES O=C(N3CCN(c2nc1cc(OC)c(OC)cc1c(n2)N)CC3)c4occc4 ;
	InChI InChI=1S/C19H21N5O4/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/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22) ; Key:IENZQIKPVFGBNW-UHFFFAOYSA-N ;
(what is this?) (verify)

　　[★]

英: pharmacology
関: drug entries

定義

生物系と化学物質の選択的な相互作用を研究する学問 (SPC.2)

生物系と薬の相互作用

薬の生物系に対する相互作用：薬理作用 <-化学の視点
生物系の薬に対する相互作用：薬物動態 <-生物の視点

薬品の命名

Ending of the drug name	Category	Example
～afil	Erectile dysfunction	sildenafil
～ane	Inhalatinal general anesthetic	halothane
～azepam	Benzodiaizepine	diazepam
～azine	Phenothiazine (neuroleptic, antiemetic)	chlorpromazine
～azole	Ailtifungal	ketoconazole
～barbital	Barbiturate	phenobarbital
～caine	Local anesthetic	lidocaine
～cillin	Penicillin	methicillin
～cycline	Antibiotic, protein syntlesis inhibitor	tetracycline
～ipramine	TCA	iimipramine
～navir	Protease inhibitor	saquinavir
～olol	β-antagonist	propranolol
～operidol	Butyrophenone ( neuroleptic )	haloperidol
～oxin	Cardiac glycoside ( inotropic agent )	digoxin
～phylline	Methylxanthine	theophylline
～pril	ACE inhibitor	captopril
～terol	β₂ agonist	albuterol
～tidine	H₂ antagonist	cimtidine
～triptyline	TCA	amitriptyline
～tropine	Pituitary hormone	somatotropine
～zosin	a₁ antagonist	prazosin

薬一覧

薬物代謝

薬理動態

神経伝達物質

貧血治療薬

甲状腺関連物質

甲状腺ホルモン製剤

レボチロキシン levothyroxine
リオチニシン liothyronine

抗甲状腺薬

痛風治療薬

痛風発作予防薬

コルヒチン colchicine

尿酸排泄促進薬

尿酸生成抑制薬

アロプリノール allopurinol

「プラゾシン」

　　[★]

英: prazosin
化: 塩酸プラゾシン prazosin hydrochloride
商: ミニプレス Minipress、ダウナット
関: αアドレナリン受容体遮断薬、アドレナリン受容体

GOO. 269.

分類

αアドレナリン受容体遮断薬

選択的α1受容体拮抗薬

薬理作用

末梢動脈の拡張→末梢血管抵抗↓→血圧↓(α₁受容体遮断による) (SPC.249)
動静脈に働き末梢血管抵抗を減少させ、静脈還流量を低下させる (GOO.269)
心臓の前負荷を減らす。心拍出量と心拍数には影響を与えない (GOO.269)
反射性頻脈が少ない。(他の血管拡張薬では心拍数↑。hydralazine) (GOO.269)

→前負荷減少、選択的α1遮断、さらには中枢神経に働いて、交感神経系の出力を抑制しているのかも (GOO.269)

ホスホジエステラーゼ阻害

ミニプレス

プラゾシンは高血圧自然発症ラット、腎性高血圧ラット、DOCA高血圧ラットのいずれにおいても優れた降圧作用が認められている。
プラゾシンの降圧作用はα受容体を遮断することにより末梢血管を拡張させ、その抵抗を減少させることによるが、従来のα遮断薬と異なり、シナプス後α受容体を選択的に遮断し、シナプス前α受容体にはほとんど作用しない。このためシナプス前α受容体を介するノルアドレナリン放出の負のフィードバック機構を抑制せず、過剰のノルアドレナリン放出をおこさないことがin vitroにおけるウサギ肺動脈の試験で認められている。シナプス後α受容体に対するプラゾシンの選択的な作用は本態性高血圧症患者に反射性頻脈をほとんどきたさないこと、レニン活性に及ぼす影響が少ないこと、長期連用による耐性発現がみられないこと10)などの特性に関連するものと考えられている。

適応

抗高血圧薬として(SPC.249)
前立腺肥大症での排尿障害
腎機能低下例にも適応可能
静脈系の拡張作用を持つので、心臓の前負荷・後負荷を軽減し、心不全にも適応可

副作用

first-dose phenomenone (SPC.249)
起立性低血圧 postural hypotension syncope

老人に多い

「α受容体遮断薬」

　　[★]

英: α adrenergic receptor blocker α-adrenergic blocking agent, α-adrenoceptor blocking agent
同: αアドレナリン受容体遮断薬、α遮断薬 α-blocker, α-blockade

非選択的α受容体拮抗薬

選択的α₁受容体拮抗薬

選択的α₂受容体拮抗薬

ヨヒンビン yohimbine

「prazosin hydrochloride」

　　[★] 塩酸プラゾシン、プラゾシン

[pmid9285356-1] Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy 13 (2): 115–139. doi:10.1016/S0891-0618(97)00042-2. PMID 9285356.

[pmid10717416-2] Yu CX, Zhu CB, Xu SF, Cao XD, Wu GC (March 2000). "Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats". Neuroscience Letters 282 (3): 161–4. doi:10.1016/S0304-3940(00)00883-1. PMID 10717416.

[pharmnemonics-3] Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN 1-59541-101-1.

[Drug_helps_PTSD-4] "Drug Helps PTSD Nightmares" (PDF) (Press release). VA Research Currents. April 2007. Retrieved 2014-01-06.

[5] Simpson, TL; Saxon, AJ; Meredith, CW; Malte, CA; McBride, B; Ferguson, LC; Gross, CA; Hart, KL; Raskind, M (2009). "A pilot trial of the alpha-1 adrenergic antagonist, prazosin, for alcohol dependence". Alcoholism, clinical and experimental research 33 (2): 255–63. doi:10.1111/j.1530-0277.2008.00807.x. PMID 18945226.

[6] Study of the Medication Prazosin for Alcohol Dependence

[bawaskar.26bawaskar2008-7] Bawaskar, H.S. & P.H. Bawaskar (2008). "Scorpion sting: A study of clinical manifestations and treatment regimes" (PDF). Current Science 95 (9): 1337–1341. Retrieved 14 April 2010.

[bawaskar.26bawaskar2007-8] Bawaskar, H.S. & P.H. Bawaskar (2007). "Utility of scorpion anti-venin vs. prazosin in the management of severe Mesobuthus tamulus (Indian red scorpion) envenoming at rural settings" (PDF). JAPI 55: 14–21. Retrieved 14 April 2010.

[9] Pandi, K.; Krishnamurthy, S.; Srinivasaraghavan, R.; Mahadevan, S. (18 February 2014). "Efficacy of scorpion antivenom plus prazosin versus prazosin alone for Mesobuthus tamulus scorpion sting envenomation in children: a randomised controlled trial". Archives of Disease in Childhood 99 (6): 575–580. doi:10.1136/archdischild-2013-305483.

[pmid519276-10] Bhalla AK, Hoffbrand BI, Phatak PS, Reuben SR (October 1979). "Prazosin and priapism". Br Med J 2 (6197): 1039. doi:10.1136/bmj.2.6197.1039. PMC 1596841. PMID 519276.

匿名

検索

案内

prazosin