Ketanserin in Women With Chronic Hypertension and Underlying Thrombophilia

Banga, F.R.; Bolte, Antoinette C.; Dekker, Gustaaf A.; Geijn, H.P. van

doi:10.1097/01.aog.0000117085.65925.f2

Cited by 3 publications

(1 citation statement)

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“…Ketanserin is an antihypertensive drug used in the management of pre‐eclampsia ( Bolte et al ., 2001 ; Banga et al ., 2004 ; Duley et al ., 2006 ) and in the treatment of chronic ulcers in leprosy patients ( Salazar et al ., 2001 ) and diabetic patients ( Martinez‐de Jesus et al ., 1997 ; Quatresooz et al ., 2006 ). Ketanserin acts pharmacologically as an antagonist of the 5‐HT 2 receptor in blood vessels to counteract the vasoconstrictive response to 5‐HT ( Bolte et al ., 2001 ; Banga et al ., 2004 ; Duley et al ., 2006 ). However, ketanserin was found to have a potentially adverse effect of prolonging the cardiac QT interval of the ECG ( Aldariz et al ., 1986 ; Zehender et al ., 1989 ; Frishman and Grewall, 2000 ).…”

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confidence: 99%

The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

Tang

et al. 2008

British J Pharmacology

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Background and purpose: Ketanserin, a selective 5-HT receptor antagonist, prolongs the QT interval of ECG in patients. The purpose of the present study was to determine whether ketanserin would block human cardiac ether-à-go-go-related gene (hERG) potassium channels. Experimental approach: Whole-cell patch voltage-clamp technique was used to record membrane currents in HEK 293 cells expressing wild type or mutant hERG channel genes. Key results: Ketanserin blocked hERG current (I hERG ) in a concentration-dependent manner (IC 50 ¼ 0.11 mM). The drug showed an open channel blocking property, the block increasing significantly at depolarizing voltages between þ 10 to þ 60 mV. Voltage-dependence for inactivation of hERG channels was negatively shifted by 0.3 mM ketanserin. A 2.8 fold attenuation of inhibition by elevation of external K þ concentration (from 5.0 to 20 mM) was observed, whereas the inactivation-deficient mutants S620T and S631A had the IC 50 s of 0.84±0.2 and 1.7±0.4 mM (7.6 and 15.4 fold attenuation of block). In addition, the hERG mutants in pore helix and S6 also significantly reduced the channel block (2-59 fold) by ketanserin. Conclusions and implications: These results suggest that ketanserin binds to and blocks the open hERG channels in the pore helix and the S6 domain; channel inactivation is also involved in the blockade of hERG channels. Blockade of hERG channels most likely contributes to the prolongation of QT intervals in ECG observed clinically at therapeutic concentrations of ketanserin.

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Section: Introductionmentioning

confidence: 99%

The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

Tang

et al. 2008

British J Pharmacology

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Effects of a Serotonin S₂-Receptor Blocker on Healing of Acute and Chronic Tendon Injuries

Oryan

Silver

Goodship

2009

Journal of Investigative Surgery

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The beneficial effects of serotonin S(2)-receptor blockers on healing skin and muscle ulcers and refractory lesions such as leprosy and diabetic and ischemic ulcers have been reported previously, but their mechanisms of actions are not clear. The present study sought to elucidate the action of an S(2)-receptor blocker, metrenperone, on the healing of collagenase-induced injuries in superficial digital flexor tendons of two groups of rabbits. In one group, oral and topical therapy for 28 days with metrenperone, was started within 48 hr of a single acute injury. The animals were then left untreated for another 60 days, when it was found that most of the morphological, biochemical, and biomechanical characteristics of the healed tendons matched those of their normal uninjured controls. Injured, untreated controls showed poor healing. In the second group of animals, tendon injury was induced by four separate injections of collagenase at weekly intervals. The rabbits were left for another 60 days, before being treated with metrenperone for 26 days. This delayed treatment had no apparent effect on the biomechanical, biochemical, or morphological characteristics of the healing tendons. It appeared that metrenperone had a significant effect on collagen turnover and organization of scar tissue, but only while the inflammatory and fibroplastic processes were active in the early stages of healing. S(2)-receptor blockers may, therefore, be of potential value for modulating repair in acutely injured collagenous tissue.

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Uneventful delivery of two pregnancies in a woman with severe factor XII deficiency: case report and systematic review

Petousis

Karavas

Margioula‐Siarkou

et al. 2018

Case Reports in Perinatal Medicine

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Background Deficiency of factor XII (FXII) is widely considered to have a detrimental effect on pregnancy. Several reports underline the increased risk for antenatal complications with few published case reports of uncomplicated deliveries. The main objective of our article is to perform a systematic review to highlight pregnancies with severe deficiency of FXII that have been delivered uneventfully, along with presenting our relative case of a woman with severe deficiency of FXII. Materials and methods A systematic review was performed in the Pubmed database. Inclusion criteria were considered to be case reports and case series presenting delivery of uncomplicated pregnancies in women with severe FXII deficiency. Medical records of our patient were also reviewed in terms of signs and symptoms, laboratory and imaging examinations and neonatal outcomes. Results There were 62 abstracts derived while 44 were assessed for eligibility. There were finally three case reports of women with FXII deficiency delivering live newborns and one case series of 12 women with a final outcome of 19 deliveries. Regarding our case presentation, the woman with FXII levels <12%, after a neonatal death because of extreme prematurity (24 weeks + 4 days), was set in regular follow-up and treatment with bemiparin natriate, 3.5 mg/kg and acetylsalicylic acid, 100 mg/day. She finally managed to have her second pregnancy delivered at 38 weeks + 3 days, her third pregnancy ended up as a miscarriage and her fourth pregnancy was also delivered at 37 weeks + 4 days. Conclusion Despite the increased risk for antenatal complications, appropriate follow-up of pregnancies with severe FXII pregnancy may finally lead to an uneventful delivery.

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Ketanserin in Women With Chronic Hypertension and Underlying Thrombophilia

Abstract: Clinical trials are warranted to analyze the role of oral ketanserin in preventing preeclampsia and IUGR.

Cited by 3 publications

References 5 publications

The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

Effects of a Serotonin S₂-Receptor Blocker on Healing of Acute and Chronic Tendon Injuries

Uneventful delivery of two pregnancies in a woman with severe factor XII deficiency: case report and systematic review

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Ketanserin in Women With Chronic Hypertension and Underlying Thrombophilia

Abstract: Clinical trials are warranted to analyze the role of oral ketanserin in preventing preeclampsia and IUGR.

Cited by 3 publications

References 5 publications

The 5‐HT2 antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

The 5‐HT2 antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

Effects of a Serotonin S2-Receptor Blocker on Healing of Acute and Chronic Tendon Injuries

Uneventful delivery of two pregnancies in a woman with severe factor XII deficiency: case report and systematic review

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The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

The 5‐HT₂ antagonist ketanserin is an open channel blocker of human cardiac ether‐à‐go‐go‐related gene (hERG) potassium channels

Effects of a Serotonin S₂-Receptor Blocker on Healing of Acute and Chronic Tendon Injuries