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doxazosin (Cardura XL / doxazosin, GITS / Cardura CR)

✓ Approved

Ipsen Pharma · 小分子 · 小分子

什么是 doxazosin？

doxazosin 是一种小分子，由Ipsen Pharma研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Cardura XL, doxazosin, GITS, Cardura CR
公司Ipsen Pharma
药物类别小分子
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Ipsen Pharma

治疗适应症

doxazosin 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersHypertension✓ Approved
Reproductive system and breast disordersBenign prostatic hyperplasia✓ Approved

相关研究文献

PubMedSurgery2026-10-25

Preoperative normetanephrine levels, but not doxazosin dose, predict intraoperative hemodynamic instability in pheochromocytoma surgery.

Liljefors Victor V, Falhammar Henrik H, Stenman Adam A, Bränström Robert R et al.

Preoperative α-adrenergic blockade is routinely recommended before adrenalectomy for pheochromocytoma to reduce intraoperative hemodynamic instability. However, the need, intensity, and duration of preoperative blockade remain uncertain. This single-center, retrospective study included adult patients who underwent adrenalectomy for pheochromocytoma at Karolinska University Hospital between 2014 and 2023. The association between preoperative doxazosin treatment, plasma metanephrine and normetanephrine concentrations, and intraoperative hemodynamic instability was evaluated. Correlation analysis and multivariable linear regression were performed. Thirty-three patients were included (49% female; median age 59 years). Neither preoperative doxazosin dose nor treatment duration was associated with intraoperative systolic blood pressure reduction or intraoperative adenosine requirements. In contrast, higher preoperative metanephrine and normetanephrine concentrations were significantly associated with greater intraoperative vasoactive support requirements and a greater systolic blood pressure reduction after adrenal vein ligation. Tumor size showed a significant positive correlation with normetanephrine concentrations but was not independently associated with intraoperative hemodynamic instability. In multivariate analysis, preoperative normetanephrine concentration remained the only independent predictor of intraoperative reduction in systolic blood pressure after adrenal vein ligation. Preoperative normetanephrine concentration is associated with intraoperative hemodynamic instability in pheochromocytoma surgery, whereas doxazosin dose and treatment duration were not. These findings suggest that biochemical tumor activity may be more clinically relevant than the intensity of preoperative α-blockade when assessing perioperative cardiovascular risk.

PMID 42926151
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PubMedEndocrine journal2026-10-18

Growth hormone-releasing hormone-secreting giant pheochromocytoma causing acromegaly: a case report with a review of the literature.

Kitamura Takuya T, Nanba Kazutaka K, Mishina Mutsuki M, Kanno Toru T et al.

The ectopic secretion of growth hormone (GH) or growth hormone-releasing hormone (GHRH) is responsible for fewer than 1% of acromegaly cases. Furthermore, within this small population, GHRH-secreting pheochromocytomas/paragangliomas (PPGLs) are even rarer. A 57-year-old Japanese woman presented to our hospital for treatment of a large left-sided pheochromocytoma (PCC). A physical examination revealed enlargement of the nose and lips as well as macroglossia, thereby raising the suspicion of acromegaly, which was biochemically confirmed by a 75-g oral glucose tolerance test. Magnetic resonance imaging demonstrated a slightly enlarged pituitary gland but no definitive tumor. A left adrenalectomy was performed after careful dose titration of doxazosin and metyrosine. Postoperative biochemical improvement of GH excess and immunohistochemical analysis of the resected tumor confirmed the diagnosis of GHRH-secreting PCC. Given the possibility that PPGLs produce various ectopic hormones and peptides, thorough physical examinations remain fundamental for the accurate diagnosis and optimal management of patients with these tumors.

PMID 42893849
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PubMedBrazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas2026-10-15

Alpha1-adrenoceptor antagonists block the positive chronotropic effect of 6-nitrodopamine in the isolated rat right atrium.

Alves B L BL, Niederauer A J S AJS, Britto-Júnior J J, Sobanski J F JF et al.

6-Nitrodopamine (6-ND) released from isolated rat atria produces potent positive chronotropic actions. Direct negative chronotropic responses to some selective α1-adrenoceptor (AR) antagonists like prazosin have been reported. Since α1-AR antagonists inhibit 6-ND-induced smooth muscle contractions, we have hypothesized that negative chronotropism induced by α1-AR antagonists reflects 6-ND blockade. This study investigated whether selective α1-AR antagonists affect 6-ND-induced positive chronotropism in isolated rat atria. Alfuzosin at 10 nM did not affect the atrial rate, but at 100 nM, it significantly reduced the atrial rate. This effect was not observed in L-NAME (100 mM)-treated preparations or in atria from rats chronically treated with L-NAME. Alfuzosin (100 nM) significantly reduced the 6-ND-induced positive chronotropism without affecting the chronotropic responses to noradrenaline, adrenaline, or dopamine. Similar results were obtained with doxazosin (1-10 nM), tamsulosin (10-100 nM), and prazosin (1-10 nM). Isoprenaline induced concentration-dependent increases in atrial rate, which were not significantly affected by any of these α1-AR antagonists. The results demonstrated that α1-AR antagonists reduced atrial basal rate only at concentrations affecting the positive chronotropic effect of 6-ND, and this reduction was not observed when NO synthesis was blocked, indicating that the negative chronotropic effect may involve 6-ND receptor blockade.

PMID 42879640
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PubMedEuropean journal of pharmacology2026-10-14

Tyramine modulates synaptic transmission in vertebrate neuromuscular junction by releasing catecholamines and activating alpha-adrenergic receptors.

Nevsky Egor S ES, Fedorov Nikita S NS, Mikshina Polina V PV, Sibgatullina Guzel V GV et al.

Tyramine is a biogenic amine whose role is closely linked to the sympathetic nervous system. Sympathetic axons densely innervate the neuromuscular junction regions of skeletal muscles. We hypothesized that tyramine might be the involvement in modulation of acetylcholine (ACh) release in the neuromuscular junctions. On the mouse Levator Auris Longus muscle it was found that tyramine enhances the loss of fluorescent false monoamine neurotransmitter FNN 511, preloaded into sympathetic varicosities located near the neuromuscular junctions. This indicates tyramine-induced release of endogenous catecholamines. Analysis of the ACh release demonstrated that tyramine decreases spontaneous exocytosis (estimated by the frequency of miniature endplate potentials) and evoked ACh secretion (assessed by the quantal content of the endplate potential). These inhibitory effects of tyramine were completely eliminated by doxazosin, an α1-adrenoreceptor blocker, but not SKF 86466, an α2-adrenoreceptor inhibitor. The negative action of tyramine on neuromuscular transmission was also manifested as a decrease in muscle contraction force during strong nerve activation. At the same time, tyramine did not inhibit the contractile responses to the direct muscle fiber stimulation. Finally, we obtained evidence of endogenous release of tyramine (and its derivative, octopamine) from the isolated neuromuscular preparation. Thus, tyramine can supress ACh release and, hence, contractile response to nerve activation probably by an indirect mechanism likely engaging the enhancement of endogenous catecholamine release and the downstream activation of α1-adrenoreceptors.

PMID 42874907
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PubMedCase reports in urology2026-10-13

Catecholamine-Secreting Retroperitoneal Paraganglioma: A Case Report and Literature Review.

Felício Eduardo E, Gião Nuno N, Bernardo Guilherme G, Barcelos André A et al.

Paragangliomas are rare neuroendocrine tumors arising from autonomic paraganglia. These tumors have metastatic potential, and histopathological findings alone cannot reliably predict their biological behavior. Clinical manifestations range from the classic triad of headache, diaphoresis, and palpitations to incidental findings in asymptomatic patients. A 75-year-old man was incidentally found to have a 5 cm retroperitoneal mass adjacent to the right renal hilum. Biochemical testing confirmed marked catecholamine hypersecretion, and 18F-FDOPA PET/CT demonstrated isolated uptake within the lesion without additional disease. Preoperative preparation included progressive alpha-adrenergic blockade with doxazosin for approximately 1 month, followed by atenolol for heart rate control. An open approach through a right subcostal hemichevron incision was selected because the tumor was located between the right renal artery and vein and lateral to the inferior vena cava. During dissection, an iatrogenic renal artery injury with intraoperative hemorrhage occurred, necessitating en bloc removal of the tumor, right kidney, and right adrenal gland. Histopathological examination confirmed a paraganglioma with a Ki-67 proliferation index below 1%, focal nuclear atypia, no mitotic figures, no tumor necrosis, no vascular invasion, and microscopic margin involvement. Immunohistochemistry was positive for Chromogranin A, synaptophysin, GATA-3, and S100. Germline testing using a 14-gene pheochromocytoma-paraganglioma panel identified no reported pathogenic or likely pathogenic variants. At 6 months, contrast-enhanced thoracoabdominopelvic computed tomography showed no evidence of local recurrence or metastatic disease, and plasma and urinary metanephrines had normalized, consistent with postoperative biochemical remission. The patient remains under joint endocrinology and urology follow-up with lifelong annual clinical and biochemical surveillance. This case highlights the diagnostic and surgical challenges of a functioning perihilar retroperitoneal paraganglioma. Careful endocrine preparation, vascular planning, multidisciplinary management, and lifelong surveillance are essential, particularly when the surgical margin is microscopically involved.

PMID 42865698
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PubMedClinical case reports2026-10-04

Pediatric Pheochromocytoma With Rapid Cyclic Blood Pressure Fluctuations: A Case Report.

Yamazaki Katsuaki K, Maeda Chika C, Morikawa Kaori K, Okamoto Naomi N

Cyclic blood pressure fluctuations in pheochromocytoma are extremely rare, and previously reported cases have been limited to adults. We report a 5-year-old boy with von Hippel-Lindau disease and a left adrenal pheochromocytoma who developed rapid cyclic blood pressure fluctuations immediately after tracheal intubation. Despite preoperative doxazosin (titrated from 0.5 to 3 mg/day over 27 days) and fluid loading, systolic blood pressure oscillated between 50 and 150 mmHg at approximately 7-min intervals after tracheal intubation. The fluctuations were independent of surgical manipulation and refractory to phenylephrine and phentolamine. Plasma norepinephrine was markedly elevated before tumor manipulation. After tumor resection, profound vasoplegic hypotension required high-dose norepinephrine, epinephrine, and vasopressin; hemodynamics gradually stabilized, and all vasoactive agents were discontinued on postoperative Day 3. This case demonstrates that pediatric pheochromocytoma can develop cyclic blood pressure fluctuations similar to those in adults and underscores the importance of individualized preoperative α-blockade and strict postoperative hemodynamic management after tumor resection.

PMID 42829526
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