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an oral beta blocker (trade name Visken) used in treating hypertension (同)Visken

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/17 07:33:16」(JST)

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Pindolol (Visken, Betapindol, Blockin L, Blocklin L, Calvisken, Cardilate, Decreten, Durapindol, Glauco-Visken, Pectobloc, Pinbetol, Prindolol, Pynastin) is a beta blocker.

Pharmacology[edit]

Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity. It possesses ISA (Intrinsic Sympathomimetic Activity). This means that pindolol, particularly in high doses, exerts effects like epinephrine or isoprenaline (increased pulse rate, increased blood pressure, bronchodilation), but these effects are limited. Pindolol also shows membrane stabilizing effects like quinidine, possibly accounting for its antiarrhythmic effects. It also functions as a 5-HT_1A receptor weak partial agonist / antagonist (K_i=33nM^[1]).

Pharmacokinetics[edit]

Pindolol is rapidly and well absorbed from the GI tract. It undergoes some first-pass-metabolization leading to an oral bioavailability of 50 to 95%. Patients with uremia may have a reduced bioavailability. Food does not alter the bioavailability, but may increase the resorption. Following an oral single dose of 20 mg peak plasma concentrations are reached within 1 to 2 hours. The effect of pindolol on pulse rate (lowering) is evident after 3 hours. Despite the rather short halflife of 3 to 4 hours, hemodynamic effects persist for 24 hours after administration. Plasma halflives are increased to 3 - 11.5 hours in patients with renal impairment, to 7 – 15 hours in elderly patients, and from 2.5 to 30 hours in patients with liver cirrhosis. Approximately 2/3 of pindolol are metabolized in the liver giving hydroxylates, which are found in the urine as gluconurides and ethereal sulfates. The remaining 1/3 of pindolol is excreted in urine in unchanged form.

Indications[edit]

Angina pectoris and hypertension. The use of pindolol in the treatment of unstable angina may be less effective compared to beta blockers without ISA.
In some other countries also arrhythmias and prophylaxis of acute stress reactions.

Investigational use[edit]

Augmentation therapy of clinical depression: Pindolol is sometimes added to a standard antidepressant therapy,^[2] if the patient fails to respond to the standard therapy alone. Fluoxetine is the most commonly used standard antidepressant. The results of augmentation therapy are encouraging. It is not known whether pindolol has antidepressive activities as monotherapeutic agent.

Augmentation therapy of premature ejaculation: According to a recent study, pindolol can be effectively added to a standard anti-premature-ejaculation therapy, which usually consists of daily doses of an SSRI antidepressant such as fluoxetine or paroxetine. Augmentation of pindolol results in substantial increase of ejaculatory latency, even in those who previously did not experience in an improvement with the SSRI monotherapy.^[3]

Contraindications[edit]

Dosage[edit]

Usual doses are 5 mg 3 or 4 times daily or 15 to 20 mg in one single dose daily. Slow Release forms (20 mg) may be available to increase patient compliance. The maximum daily dose is 60 mg for hypertension and 40 mg for angina. Treatment should be started with low doses and slowly increased according to the clinical response. The initial and maintenance doses should be reduced in patients with severe liver disease. In some countries pindolol exists as injection concentrate for the emergency treatment of serious arrhythmias. In these cases 0.4 to 1 mg is injected i.v. under strict ECG-monitoring. Further treatment, if necessary, should then be oral.

The recommendation for augmentation in depressive patients is 2.5 mg (or possibly 5 mg) three times daily.

References[edit]

^ "PDSP". Retrieved 12 June 2013.
^ Isaac MT (November 2004). "Review: combining pindolol with an SSRI improves early outcomes in people with depression". Evid Based Ment Health 7 (4): 107. doi:10.1136/ebmh.7.4.107. PMID 15504795.
^ Safarinejad, MR (2008). "Once-daily high-dose pindolol for paroxetine-refractory premature ejaculation: a double-blind, placebo-controlled and randomized study.". Journal of Clinical Psychopharmacology 28 (1): 39–44. doi:10.1097/jcp.0b013e31816073a5. PMID 18204339.
^ http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20%28General%20Monographs-%20V%29/VISKEN.html

UpToDate Contents

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English Journal

Serotonin is involved in the psychostimulant and hypothermic effect of 4-methylamphetamine in rats.

Rubio M1, López-Arnau R1, Pubill D1, Escubedo E2, Camarasa J1.
Neuroscience letters.Neurosci Lett.2015 Mar 17;590:68-73. doi: 10.1016/j.neulet.2015.01.075. Epub 2015 Jan 29.
4-Methylamphetamine (4-MA) has recently emerged as a designer drug of abuse in Europe and it is consumed always with amphetamine. There have been reported some deaths and non-fatal intoxications related to 4-MA. We investigated the changes in locomotor activity and body temperature after 4-MA admini
PMID 25641130

Electroanalytical detection of pindolol: comparison of unmodified and reduced graphene oxide modified screen-printed graphite electrodes.

Cumba LR1, Smith JP, Brownson DA, Iniesta J, Metters JP, do Carmo DR, Banks CE.
The Analyst.Analyst.2015 Mar 7;140(5):1543-50. doi: 10.1039/c4an02005g. Epub 2015 Jan 22.
Recent work has reported the first electroanalytical detection of pindolol using reduced graphene oxide (RGO) modified glassy carbon electrodes [S. Smarzewska and W. Ciesielski, Anal. Methods, 2014, 6, 5038] where it was reported that the use of RGO provided significant improvements in the electroan
PMID 25610919

Is pindolol augmentation effective in depressed patients resistant to selective serotonin reuptake inhibitors? A systematic review and meta-analysis.

Liu Y1, Zhou X, Zhu D, Chen J, Qin B, Zhang Y, Wang X, Yang D, Meng H, Luo Q, Xie P.
Human psychopharmacology.Hum Psychopharmacol.2015 Feb 17. doi: 10.1002/hup.2465. [Epub ahead of print]
OBJECTIVE: This systematic review and meta-analysis was conducted to assess the use of pindolol augmentation in depressed patients resistant to selective serotonin reuptake inhibitor (SSRI) therapy.METHODS: A comprehensive search of PubMed, Cochrane, Embase, Web of Science, and PsychINFO databases f
PMID 25689398

Japanese Journal

抗うつ薬の増強療法 (第1土曜特集うつ病 : 治療・研究の最前線) -- (薬物療法)

寺尾岳
医学のあゆみ 244(5), 373-380, 2013-02-02
NAID 40019561508

ラット扁桃核キンドリングモデルにおけるパロキセチンの効果 : 5-HT_<1A>自己受容体拮抗薬, ピンドロールの併用による促進作用について

平尾直久
金沢大学十全医学会雑誌 = Journal of the J◆U00FB◆zen Medical Society 116(4), 151-162, 2007-12-01
原著 ; 平成19年10月30日受付，平成19年12月10日受理
NAID 10026960295

Determination of pindolol enantiomers in amniotic fluid and breast milk by high-performance liquid chromatography : Applications to pharmacokinetics in pregnant and lactating women

GONCALVES Paulo Vinicius Bernardes,CAVALLI Ricardo Carvalho,DA CUNHA Sergio Pereira,LANCHOTE Vera Lucia
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 852(1), 640-645, 2007-06-01
NAID 10025803223

Related Pictures

★リンクテーブル★

リンク元	「ピンドロール」
拡張検索	「bopindolol malonate」「bopindolol」「iodocyanopindolol」

「ピンドロール」

Pindolol
Systematic (IUPAC) name
	(RS)-1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a684032
Pregnancy cat.	C (AU) B (US)
Legal status	℞ Prescription only
Routes	oral, iv
Pharmacokinetic data
Bioavailability	50% to 95%
Metabolism	Hepatic
Half-life	3–4 hours
Excretion	Renal
Identifiers
CAS number	13523-86-9
ATC code	C07AA03
PubChem	CID 4828
IUPHAR ligand	91
DrugBank	DB00960
ChemSpider	4662
UNII	BJ4HF6IU1D
KEGG	D00513
ChEBI	CHEBI:8214
ChEMBL	CHEMBL500
Chemical data
Formula	C14H20N2O2
Mol. mass	248.321 g/mol
	SMILES CC(C)NCC(O)COc2cccc1nccc12;
	InChI InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3 ; Key:JZQKKSLKJUAGIC-UHFFFAOYSA-N ;
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