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関: penbutolol

WordNet

convert into a sulfate
a salt or ester of sulphuric acid (同)sulphate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/26 21:25:18」(JST)

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Penbutolol (Levatol, Levatolol, Lobeta, Paginol, Hostabloc, Betapressin) is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker [1]. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors [2]. Penbutolol has also been found to be one of very few compounds that are 5-HT1A antagonists. 5-HT1A receptors are activated by serotonin, which have many different actions in different species. This makes it difficult to create generalizations about serotonin and its effects [1].

Hypertension

Hypertension can result from a multitude of alterations to blood volume, heart or kidney function. Hypertension involving a high heart rate can lead to myocardial ischemia [3]. Penbutolol acts by blocking β adrenergic receptors and blocking the sympathetic nervous system to decrease the heart rate and cardiac output to lower arterial blood pressure. β blockers also decrease renin levels, which ultimately results in less water being reabsorbed by the kidneys and therefore a lower blood volume and blood pressure [3].

β1 Blockade

Penbutolol acts on the β1 adrenergic receptors in both the heart and the kidney. When β1 receptors are activated by a catecholamine, they stimulate a coupled G protein which activates adenylyl to convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP) [1]. The increase in cAMP leads to activation of protein kinase A (PKA), which alters the movement of calcium ions in heart muscle and increases heart rate [4]. Penbutolol blocks this and decreases heart rate, which lowers blood pressure. The ability of penbutolol to act as a partial agonist proves useful in the prevention of bradycardia as a result of decreasing the heart rate excessively [2]. Penbutolol binding β1 adrenergic receptors also alters kidney functions. Under normal physiological conditions, the enzyme renin converts angiotensinogen to angiotensin I, which will then be converted to angiotensin II. Angiotensin II stimulates the release of aldosterone from the adrenal gland, causing a decrease in electrolyte and water retention, ultimately increasing water excretion and decreasing blood volume and pressure [5].

Characteristics

Penbutolol is typically administered orally in doses of 20 mg per day [7]. It is rapidly absorbed from the gastrointestinal tract, has a bioavailability over 90% [6], and has a rapid onset of effect. Penbutolol has a half life of five hours [1], and a low frequency of side effects [7]. These side effects include dizziness, light headedness, and nausea [6]. When penbutolol is being metabolized, it undergoes a series of biotransformations, the main one being hydroxylation. One potential drawback of penbutolol is the inactivation of β2 adrenergic receptor, which makes this a less than ideal hypertensive treatment for people suffering from asthma or insulin dependent diabetes mellitus.

References

Katzung, Bertram G. (1998). Basic and Clinical Pharmacology (7th ed.). London: Appleton & Lange. ISBN 0838505651
Frishman, W. H., Covey, S. (1990). Penbutolol and carteolol: two new beta-adrenergic blockers with partial agonism. Journal of Clinical Pharmacology, 30(5):412-21
Berdeaux, A., Duhaze, P., Giudicelli, J. F. (1982). Pharmacological analysis of beta adrenoceptor blockade-induced coronary blood flow redistribution in dogs using l-penbutolol. The Journal of Pharmacology and Experimental Therapeutics, 221(3):740-747
Dent, M. R., Singal, T., Tappia, P. S., Sethi, R., Dhall, N. S. (2008). Signal transduction in the cardiovascular system in health and disease. Advances in Biochemistry in Health and Disease, 3:27-49
Howland, Richard D., Mycek, Mary J. (2006). Lippincott’s Illustrated Reviews: Pharmacology (3rd ed.). New York: Lippincott Williams & Wilkins. ISBN 0781741181
Vallner, J. J., Jun H. W., Needham, T. E., Stewart, J. T., Brown, W., Frazer, H., Honigberg, I. L. (1977). Plasma level studies of penbutolol after oral dose in man. Journal of Clinical pharmacology, 17(4):231-23
Schoenberger, J. A. (1989). Usefulness of penbutolol for systemic hypertension: Penbutolol

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English Journal

Influence of sonophoresis and chemical penetration enhancers on percutaneous transport of penbutolol sulfate.

Ita KB1, Popova IE2.
Pharmaceutical development and technology.Pharm Dev Technol.2016 Dec;21(8):990-995. Epub 2015 Sep 18.
The effect of ultrasound and chemical penetration enhancers on transcutaneous flux of penbutolol sulfate across split-thickness porcine skin was investigated. Penbutolol sulfate is a potent, noncardioselective beta-blocker, which is used for the management of hypertension. The drug is one of the mos
PMID 26383739

Broad screening and identification of β-agonists in feed and animal body fluid and tissues using ultra-high performance liquid chromatography-quadrupole-orbitrap high resolution mass spectrometry combined with spectra library search.

Li T1, Cao J2, Li Z2, Wang X1, He P3.
Food chemistry.Food Chem.2016 Feb 1;192:188-96. doi: 10.1016/j.foodchem.2015.06.104. Epub 2015 Jun 30.
Broad screening and identification of β-agonists in feed, serum, urine, muscle and liver samples was achieved in a quick and highly sensitive manner using ultra high performance liquid chromatography-quadrupole-orbitrap high resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS) combined with a spect
PMID 26304337

Sulfonated polystyrene magnetic nanobeads coupled with immunochromatographic strip for clenbuterol determination in pork muscle.

Wu K1, Guo L2, Xu W2, Xu H2, Aguilar ZP3, Xu G4, Lai W2, Xiong Y5, Wan Y2.
Talanta.Talanta.2014 Nov;129:431-7. doi: 10.1016/j.talanta.2014.06.007. Epub 2014 Jun 14.
A magnetic solid-phase extraction method (MSPE) was developed to pre-concentrate and cleanup clenbuterol (CLE) from pork muscle. Novel sulfonated polystyrene magnetic nanobeads (spMNBs) were synthesized via a one-pot emulsion copolymerization method by using divinylbenzene, styrene, and sodium styre
PMID 25127616

「ペンブトロール」

Penbutolol
Systematic (IUPAC) name
	(S)-1-(tert-butylamino)-3-(2-cyclopentylphenoxy)propan-2-ol
Clinical data
Trade names	Levatol
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a601091
Identifiers
CAS Registry Number	36507-48-9
ATC code	C07AA23
PubChem	CID: 37464
IUPHAR/BPS	7263
DrugBank	DB01359
ChemSpider	34369
UNII	78W62V43DY
KEGG	D08074
ChEMBL	CHEMBL1290
Chemical data
Formula	C18H29NO2
Molecular mass	291.428 g/mol
	SMILES O[C@@H](CNC(C)(C)C)COc1ccccc1C2CCCC2 ;
	InChI InChI=1S/C18H29NO2/c1-18(2,3)19-12-15(20)13-21-17-11-7-6-10-16(17)14-8-4-5-9-14/h6-7,10-11,14-15,19-20H,4-5,8-9,12-13H2,1-3H3/t15-/m0/s1 ; Key:KQXKVJAGOJTNJS-HNNXBMFYSA-N ;
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　　[★]

英: penbutolol
化: 硫酸ペンブトロール penbutolol sulfate
商: ベータプレシン

β受容体遮断薬
非選択的β遮断薬

「sulfate」

　　[★]

n.

(官能基やイオンを表して)硫酸、(化合物)硫酸塩、硫酸エステル、硫酸化する

関: H2SO4、inorganic sulfate、sulfate ester、sulfated、sulfation、sulfuric acid、sulfuric acid ester、sulphate、sulphuric acid

「sulfated」

　　[★]

adj.

硫酸化の

関: sulfate、sulfation、sulphate

「sulfa」

　　[★]

スルファ、サルファ

リンク元	「ペンブトロール」
関連記事	「sulfate」「sulfated」「sulfa」

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案内

案内

penbutolol sulfate