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Methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2,3-dihydro-1,4-benzodioxin-2-yl)-,methanesulfonate (1:1)(CAS No. 77883-43-3)

Methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2,3-dihydro-1,4-benzodioxin-2-yl)-,methanesulfonate (1:1) C24H29N5O8S (cas 77883-43-3) Molecular Structure

77883-43-3 Structure

Identification and Related Records

【Name】
Methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2,3-dihydro-1,4-benzodioxin-2-yl)-,methanesulfonate (1:1)
【Iupac name】
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(2,3-dihydro-1,
4-benzodioxin-3-yl)methanone; methanesulfonic acid
【CAS Registry number】
77883-43-3
【Synonyms】
Normothen
Supressin
UK 33274-27
doxazolazine mesylate
Piperazine,1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]-,monomethanesulfonate (9CI)
Alfadil
Cardenalin
Cardran
Cardular
Cardura
Cardura (pharmaceutical)
Carduran
Diblocin
Doxazosin mesylate
Doxazosin monomethanesulfonate
【Molecular Formula】
C24H29N5O8S (Products with the same molecular formula)
【Molecular Weight】
547.58076
【Inchi】
InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4)
【InChIKey】
VJECBOKJABCYMF-UHFFFAOYSA-N
【Canonical SMILES】
COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4)N)OC.CS(=O)(=O)O
【MOL File】
77883-43-3.mol

Chemical and Physical Properties

【Appearance】
white to off-white crystalline powder
【Melting Point】
275-277°C
【Boiling Point】
718 °C at 760 mmHg
【Flash Point】
388 °C
【Water】
Slightly soluble
【Solubilities】
Slightly soluble Appearance:white to off-white crystalline powder
Transport Information: PRI
Hazard Symbols:UN NO.
particular:particular
【Color/Form】
white
【Stability】
Protect from light
【Storage temp】
Desiccate at RT
【Computed Properties】
Molecular Weight:547.58076 [g/mol]
Molecular Formula:C24H29N5O8S
H-Bond Donor:2
H-Bond Acceptor:8
Rotatable Bond Count:4
Tautomer Count:3
Exact Mass:547.173684
MonoIsotopic Mass:547.173684
Topological Polar Surface Area:175
Heavy Atom Count:38
Formal Charge:0
Complexity:770
Isotope Atom Count:0
Defined Atom Stereocenter Count:0
Undefined Atom Stereocenter Count:1
Defined Bond Stereocenter Count:0
Undefined Bond Stereocenter Count:0
Covalently-Bonded Unit Count:2

Safety and Handling

【Hazard Codes】
UN NO.
【Risk Statements】
R36/37/38
【Safety Statements 】
26-36/37
【Safety】
Hazard Codes:Xi
Risk Statements:36/37/38
36/37/38:Irritating to eyes, respiratory system and skin
Safety Statements:26-36/37
26:In case of contact with eyes, rinse immediately with plenty of water and seek medical advice
36/37:Wear suitable protective clothing and gloves
WGK Germany:2
Hazardous Substances Data:77883-43-3(Hazardous Substances Data)
【Transport】
PRI
【Formulations/Preparations】
Alfadil; Benur; Cardenalin; Cardular; Cardura; Carduran; Diblocin; Normothen; Supressin; Zoxan.
【Exposure Standards and Regulations】
The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl doxazosin mesylate, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.
【Specification】

White Crystalline Powder
usageEng:A selective a-1-adrenergicblocker related to prazosin
Safety Statements:26-36/37
26:In case of contact with eyes, rinse immediately with plenty of water and seek medical advice
36/37:Wear suitable protective clothing and gloves
【Disposal Methods】
SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Use and Manufacturing

【Use and Manufacturing】
Methods of Manufacturing

Prepn: S.F. Campbell, DE 2847623; idem, US 4188390 (1979, 1980 both to Pfizer). /Doxazosin/
【Usage】

A selective a-1-adrenergicblocker related to prazosin

Biomedical Effects and Toxicity

【Biological Activity】
Selective α 1 -adrenoceptor antagonist (pK i values are 9.0, 8.5 and 8.4 for human α 1B , α 1A and α 1D receptors respectively). Displays antihypertensive activity.
【Pharmacological Action】
- Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
- Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
【Therapeutic Uses】
Doxazosin is indicated for the treatment of both the urinary outflow obstruction and the obstructive and irritative symptoms associated with benign prostatic hyperplasia (BPH). Obstructive symptoms are hesitation, intermittency, dribbling, weak urinary stream, and incomplete emptying of the bladder; while irritative symptoms include nocturia, daytime frequency, urgency, and burning. Doxaxosin may be used in nomotensive or hypertensive patients. In normotensive patients with BPH, doxazosin does not appear to significantly lower blood pressure. In hypertensive patients with BPH, both conditions are effectively treated with doxazosin. The long term effects of doxazosin on the incidence of acute urinary obstruction or other complications of BPH or on the need for surgery have not yet been determined. /Included in US product labeling/ /Salt not specified/
Doxazosin is indicated in the treatment of hypertension. /Included in US product labeling/ /Salt not specified/
Antihypertensive; in treatment of benign prostatic hypertrophy. /Salt not specified/
Evaluation of atherosclerosis is important in the treatment of hypertension. To evaluate the preventive effects of a small amount of alpha-blockade, arterial and endothelial dysfunction were measured by noninvasive tests, i.e., pulse wave velocity, acceleration plethysmography and strain-gauge plethysmography, in patients with essential hypertension. Fifteen patients (65+/-3 years old) with essential hypertension (WHO stage I or II) were analyzed in this study. We performed noninvasive evaluations to measure aortic stiffness and endothelial dysfunction, in addition to measuring blood pressure, cholesterol profile, and levels of cells adhesion molecules and nitric oxide before and 6 and 12 months after the start of doxazosin treatment (1.0 mg/day). Blood pressure and heart rate did not significantly change during treatment. The pulse wave velocity index was significantly reduced both at 6 (7.72+/-0.23 m/s; p<0.05) and 12 (7.34+/-0.26 m/s; p<0.05) months after the start of treatment compared to the pretreatment level that at baseline. There was also a significant improvement in b/a after 12 months (-0.46+/-0.04; p<0.05) and in d/a after 6 months (-0.38+/-0.03; p<0.05) and 12 months (-0.39+/-0.03; p=0.05) compared to the pretreatment values. Moreover, reactive hyperemia evaluated by strain-gauge plethysmography after 6 months (1.34+/-0.11; p<0.05) and 12 months (1.49+/-0.16; p<0.05) was significantly improved compared to that before treatment, and NOx was significantly increased after 12 months (89.7+/-15.7 micromol/l; p<0.005). These data suggest that a low dose of doxazosin may play an important role in improving arterial stiffness and endothelial dysfunction without changing cardiac hemodynamics. /Salt not specified/
The acute and chronic haemodynamic effects of doxazosin were studied in 14 patients (10 males, four females) with essential hypertension, at rest supine and sitting and during 100 W bicycling exercise. Blood pressure (BP) was recorded intra-arterially in the brachial artery, cardiac output (CO) was measured by Cardiogreen and heart rate (HR) by ECG. One hour after injection of doxazosin 0.5-1.0 mg i.v., mean arterial pressure (MAP) was reduced by 8% at rest supine, 12% at rest sitting and 10% at 100 W (all changes statistically significant), associated with a reduction in total peripheral resistance index (TPRI) of 5% at rest supine, 9% at rest sitting (P less than 0.01) and 14% at 100 W (P less than 0.001). HR was slightly increased (5%, NS) and cardiac index (CI) was unchanged during rest and slightly increased during exercise (4%, P less than 0.05). Patients were then given doxazosin capsules (2-16 mg once daily), aiming at a casual BP of less than or equal to 140/90 mmHg without side-effects. Central haemodynamics were restudied after 1 year. After 1 year of doxazosin treatment, MAP was reduced by 13% at rest supine, 16% at rest sitting and 17% at 100 W (all P-values less than 0.001). TPRI was reduced by 19% at rest supine, 20% at rest sitting and 18% at 100 W (all changes statistically significant). CI was increased by 8% at rest supine (P less than 0.05) but was unchanged sitting and at 100 W. It is concluded that doxazosin lowers BP through a reduction in TPRI acutely as well as chronically, without reductions in CO. BP control was maintained over 1 year without side-effects. Thus, doxazosin normalizes central haemodynamics in patients with mild to moderate essential hypertension, both at rest and during exercise /Salt not specified/
Patients with peripheral vascular disease or diabetes mellitus tend to have elevated circulating levels of naturally occurring platelet agonists like serotonin (5 hydroxytryptamine; 5-HT). This bioamine can induce platelet shape change (PSC) an early phase of platelet activation, which is essentially aspirin resistant. In addition, 5-HT exerts other harmful effects (eg stimulating vascular smooth muscle proliferation and inducing vasoconstriction in atheromatous coronary vessels). The aim of this study was to determine whether doxazosin inhibits 5-HT-induced PSC. Doxazosin is a long acting alpha(1)-adrenoceptor antagonist, used in the treatment of essential hypertension and/or benign prostatic hyperplasia (BPH). Platelet rich plasma (PRP) was prepared from healthy volunteers (n = 8; five males and three females with a median age of 32 years, range: 26-57). Agonists (5-HT, 0.06-0.5; ADP, 0.1-0.2 micromol/l or U46619, a TXA(2)analogue, 0.025-0.05 micromol/l) were added to PRP and aliquots were removed at specific time points for median platelet volume (MPV) measurement (using a high-resolution channelyser). The MPV was used as an indicator of PSC. PRP was also incubated with doxazosin (final concentration: 0.33 microM, a concentration similar to therapeutic plasma levels) prior to the addition of each of the above-mentioned agonists. Doxazosin significantly inhibited (P = 0.007 and P = 0.008, at 30 sec and 60 sec, respectively) the 5-HT-induced increase in MPV. Doxazosin did not significantly inhibit ADP- or U46619-induced PSC. The inhibitory effect of doxazosin seems to be specific to platelet 5-HT(2) receptors, since there was no effect on ADP- or U46619-induced PSC. This inhibition of platelet activation may be an additional, clinically relevant, advantage. Future in vivo studies should consider assessing the effect of doxazosin on 5-HT-induced platelet activation. /Salt not specified/
Hypertension is common in patients with type 2 diabetes mellitus (DM), and contributes to the progression of its complications in patients with diabetes. Doxazosin is a selective alpha1-adrenoceptor-blocking anti-hypertensive agent and has a favorable impact upon lipid metabolism. We investigated the effect of doxazosin on the lipid metabolism in hypertensive patients with type 2 diabetes, especially low-density lipoprotein (LDL) particle size that is associated with many elements of the insulin resistance syndrome. Cross-sectional study (n=19) was designed to determine whether doxazosin, administered with an angiotensin II-converting enzyme inhibitor (ACEI) and a Ca antagonist, affects LDL particle size. As a follow-up study (n=6), lipid and glucose metabolism and LDL particle size were followed for 12 weeks before and after the initiation of doxazosin administration (1-4 mg/day). The average size of LDL particle was significantly larger in the patients treated with doxazosin (LDL-migration index (LDL-MI): 0.348+/-0.027) than those in the patient treated without doxazosin (0.378+/-0.035), although LDL cholesterol levels did not differ between the two groups. The plasma glucose and HbA1c levels remained unchanged. Lipid profile showed normolipemia throughout the period of the study. However, LDL particle size was demonstrated to become larger during the following period. Small LDL fraction (LDL3-7) diminished remarkably and large LDL (LDL1-2) increased on the polyacrylamide gel electrophoresis (PAGE) LDL system (LipoPrint). From this pilot study, it was concluded that doxazosin is a useful anti-hypertensive agent for hypertensive type 2 diabetic patients in improving the size of LDL particle. /Salt not specified/
We evaluated the sustained efficacy and safety of doxazosin for long-term treatment (up to 48 months) of normotensive and hypertensive patients with benign prostatic hyperplasia (BPH). MATERIALS AND METHODS: A total of 272 normotensive and 178 mildly to moderately hypertensive men entered a long-term extension study of doxazosin therapy (1 to 8 and 1 to 12 mg. 1 time daily, respectively) for BPH following participation in double-blind, placebo controlled studies. The starting dose of doxazosin was 1 mg. with upward titrations at 2-week intervals to a stable, efficacious and well tolerated dose. At the time of data analysis patients had received between 1 and 48 months of stable dose doxazosin therapy (mean 668 days for normotensive and 807 for hypertensive patients). Mean daily doses were 4 and 6.4 mg. for normotensive and hypertensive men, respectively. RESULTS: At the end point analysis doxazosin treatment resulted in significant increases above baseline in maximum and average urinary flow rates (1.9 and 1.0 ml. per second, respectively). As assessed by the patient, total, obstructive and irritative BPH symptoms also improved significantly with doxazosin treatment. In the 28 patients who completed 45 to 48 months of treatment improvement in symptom bothersomeness (13.2%) was similar to that of the overall group at the end point (14.8%). Sustained blood pressure decreases (approximately 8/11 mm. Hg systolic/diastolic blood pressure) with doxazosin were statistically and clinically significant in hypertensive patients. Blood pressure decreases in normotensive patients were not clinically significant (approximately 4/2 mm. Hg) and few withdrew from study for reasons related directly to decreased blood pressure or hypotension. Changes in heart rate were not significant. Doxazosin was well tolerated with almost 90% of adverse experiences considered mild or moderate in severity. The most common adverse events were dizziness, headache and fatigue in normotensive and hypertensive patients. CONCLUSIONS: In this study long-term doxazosin treatment was significantly effective and well tolerated for treating BPH in normotensive and hypertensive patients. /Salt not specified/
To investigate the effect of doxazosin on orthostatic blood pressure changes with daily activity, the relationship among blood pressure, physical position and physical activities using an ambulatory multibiomedical monitoring system(TM2425) were studied. The subjects were 22 patients with essential hypertension(EHT group), 23 patients with diabetic mellitus(DM group) and 17 healthy volunteers for the control. Patients were administered doxazosin at 2-8 mg/day for 0.5 month to 12 months. Twenty-four-hour blood pressure, posture and activity were monitored. Systolic blood pressure was higher in the standing position than that in the sitting position in the control group, but there were no differences between these values in the EHT group and DM groups. During the awake, sleep, and standing periods, doxazosin significantly decreased blood pressure in the EHT group; however, it significantly decreased only the standing systolic blood pressure in the DM group. Absolute changes in blood pressure after the administration of doxazosin were not significantly different between the standing and sitting periods in each group. These findings suggest that doxazosin decreases the blood pressure of both patients with essential hypertension and patients with diabetic mellitus without an excessive decrease in standing blood pressure. /Salt not specified/
Despite adverse side effects, phenoxybenzamine has been widely used for the preoperative management of patients with pheochromocytoma. Doxazosin, a specific a 1-adrenoceptor antagonist, has a pharmacologic profile more suited to controlling blood pressure in such patients. A sequential study of 35 patients with pheochromocytoma encompassed a definite and prescribed change in preoperative drug management from phenoxybenzamine to doxazosin. Hemodynamic, pharmacologic, and biochemical indicators of a- and b-adrenoceptor blockade were measured before, during, and after anesthesia and surgery in 8 patients pretreated with phenoxybenzamine and 27 patients pretreated with doxazosin. Doxazosin (2-16 mg/day) was as effective as phenoxybenzamine in controlling arterial pressure and heart rate before and during surgery, but doxazosin caused fewer undesirable side effects both before and after surgery. Following phenoxybenzamine therapy substantial a 1-adrenoceptor blockade, detected as a right shift of phenylephrine dose-response curves, persisted for more than 2 days postoperatively, whereas after doxazosin it was undetectable on the first postoperative day. Doxazosin provided safe, efficacious pre- and perioperative control of arterial pressure. In patients with predominantly norepinephrine-secreting tumors, pretreatment 24-hour urinary norepinephrine excretion gave an indication of the daily doxazosin requirement. /Salt not specified/
Doxazosin is a long-acting selective alpha 1-adrenoceptor antagonist which has been shown to be effective and well tolerated in the treatment of hypertension given in once-daily doses as monotherapy for up to 1 year or as an adjunct to thiazide or beta-adrenoceptor blockers. Doxazosin has a pharmacokinetic profile in both young adult and elderly subjects which is compatible with once-daily administration. This has been confirmed by measurement of steady state pharmacokinetics in patients receiving long-term doxazosin therapy. In controlled double-blind studies involving approximately 550 patients on doxazosin 1-16 mg once daily, significant reductions in both standing and supine BP were maintained throughout the 24 h dosing interval. Effectiveness of doxazosin in terms of BP lowering and proportion of responders was similar to that achieved with hydrochlorothiazide 25-100 mg once daily, atenolol 50-100 mg once daily, nadolol 40-160 mg once daily, metoprolol 100-200 mg per day given twice daily, or prazosin 1-20 mg per day given twice daily. Doxazosin was as effective in elderly patients as in the younger age group and was as effective in blacks as in caucasians. Doxazosin was well tolerated. Side-effects were generally mild to moderate in severity. Overall incidence, including postural effects early in treatment, was similar to that seen with the comparative agents. In comparison with placebo, doxazosin favourably increased (P less than 0.05) the HDL/total cholesterol ratio /Salt not specified/
Small dense low density lipoprotein (LDL) and remnant lipoproteins are potent atherogenic lipoproteins, often elevated in the plasma of patients with type 2 diabetes. The alpha1-blocker doxazosin has been reported to favorably affect the plasma lipid profile. We examined whether doxazosin could reduce these atherogenic lipoproteins in hypertensive subjects with and those without type 2 diabetes. Seventeen nondiabetic hypertensive patients and 33 hypertensive patients with type 2 diabetes were studied. Doxazosin (2 to 4 mg) was administered alone or with other previously received antihypertensive drugs for 6 months. Mean LDL size was measured by 2% approximately 16% gradient gel electrophoresis. Remnant-like particle (RLP)-cholesterol was measured with the use of an affinity column containing anti-apoA1 and B100 monoclonal antibodies. Doxazosin effectively decreased blood pressure (BP) without significantly affecting glucose, glycosylated hemoglobin (HbA1c), or C-peptide levels in both nondiabetic and diabetic patients. Doxazosin significantly reduced triglyceride, apo CIII, and apo B, but did not alter total-, LDL- or HDL-cholesterol. Mean LDL particle diameter was significantly increased from 25.6+/-0.6 nm to 25.9+/-0.4 nm (P < .001) by doxazosin treatment, regardless of the presence of diabetes. Consequently, the prevalence of small dense LDL (<25.5 nm) was halved in both groups. The increase in LDL size significantly correlated with decrease in triglyceride level (r=-0.798, P < .0001). Doxazosin significantly reduced RLP-cholesterol in both groups. These results suggest that doxazosin may help to prevent coronary artery disease by reducing atherogenic lipoproteins, including small dense LDL and remnant lipoproteins, in hypertensive patients, regardless of the presence of diabetes. /Salt not specified/
A significant proportion of patients with cardiac syndrome X have impaired coronary vasodilator capacity, which is thought to be caused by an increased sympathetic drive. The alpha1-adrenoceptor blocker, doxazosin, increases the coronary vasodilator reserve in patients with syndrome X. To study whether the augmentation is associated with clinical improvement in patients, we conducted a double-blind, placebo controlled, crossover study with doxazosin 1 to 4 mg once daily for 10 weeks in 16 patients with syndrome X (14 women and 2 men; mean +/- SD age 56+/-5 years). Time to angina, exercise duration, time to 0.1 mV ST-segment depression, and maximal ST-segment depression during bicycle exercise testing were compared after treatment with doxazosin 2 mg or placebo for 5 weeks and again after treatment with doxazosin 4 mg or placebo for 10 weeks. Insulin sensitivity was assessed by the minimal model after 10 weeks of doxazosin or placebo treatment. Twelve patients completed the protocol. Doxazosin 4 mg/day decreased systolic blood pressure at rest (109+/-16 vs 125+/-18 mm Hg, p <0.05) and increased basal heart rate (85+/-9 vs 76+/-11 beats/min, p <0.05), whereas hemodynamics were unaffected during exercise. Time to angina, exercise duration, time to 0.1 mV ST-segment depression, and maximal ST-segment depression were similar during treatment with doxazosin and placebo irrespective of the doxazosin dose. Insulin sensitivity was not different with doxazosin and placebo. In conclusion, alpha1 blockade does not significantly improve exercise duration, angina pectoris, and ST-segment depression despite a favorable vasodilator effect in patients with syndrome X. The absent clinical efficacy of doxazosin may challenge the use of the coronary vasodilator capacity as an appropriate method to subclassify patients with syndrome X. /Salt not specified/
The aim of our study is to verify the effects of doxazosin on sexual function in patients with benign prostatic hyperplasia (BPH). MATERIALS AND METHODS: We enrolled 102 patients with BPH, selected by nine Italian Urology Departments. Patients were evaluated with the International Prostatic Symptom Score (I-PSS) and divided into two groups: those with intact sexual activity and those with erectile dysfunction. According to the International Index of Erectile Function (IIEF), the second cohort was divided into three subgroups on the basis of the degree of erectile dysfunction degree (severe, moderate or mild). All patients underwent 3 months of therapy with doxazosin. The effects of doxazosin on sexual activity and on voiding symptoms were monitored at 1, 2 and 3 months with IIEF and I-PSS scales. RESULTS: Eighty-six of the 102 initial patients (84%) were monitored until follow-up was completed. The follow-up at 1 month showed a significant decrease in the I-PSS (p < 0.0001) from 20.2 +/- 2.01 (base visit) to 13.1 +/- 2.21. The mean IIEF was 19.24 +/- 6.59 at baseline and 1 month later the score reached 21.44 +/- 5.40, thus showing a statistically significant increase (p = 0.0177). This is more evident in the group presenting with severe to moderate erectile dysfunction. I-PSS and IIEF do not significantly change at the 2- and 3-month follow-ups. CONCLUSIONS: The use of doxazosin improved sexual function in patients with BPH. /Salt not specified/
Most alpha-receptor blocking drugs require divided daily administration because of a short plasma half-life. This multicenter study examined the effectiveness and safety of once-daily administration with doxazosin, a quinazoline analog alpha 1-receptor blocking drug with a plasma half-life of 19 hours. Patients with diastolic blood pressure (BP) of 90 to 115 mm Hg entered 4 weeks of single-blind placebo therapy and then were randomized to double-blind treatment with doxazosin (63 patients) or placebo (67 patients). After 10 weeks of titration, standing arterial BP was lowered by 14/11 mm Hg with doxazosin and by 0.5/0.9 mm Hg with placebo (p less than 0.001). Measured hourly for 12 hours after the dose, all standing and supine arterial BP values were significantly lower in the doxazosin group at each hour. Pulse rate increased slightly in both groups int he double-blind phase, but the increase with doxazosin never significantly exceeded that of placebo. Dizziness was the most common complaint with doxazosin, but syncope did not occur. Side effects were mild and transient and did not necessitate withdrawing any participants from the study. Body weight increased by 1.5 kg in the doxazosin group and decreased by 0.2 kg in the placebo group (p less than 0.01). Safe and effective in once-daily administration, doxazosin is suitable for initial therapy in mild and moderate hypertension. /Salt not specified/
The safety and efficacy of the selective alpha 1-adrenoceptor antagonist doxazosin were evaluated in a 10-week open, non-comparative multicentre trial in 4809 hypertensive patients (sitting diastolic blood pressure 95-114 mmHg) in general practice. Multiple coronary risk factor were present in the study population (mean age 58.4 years, 1486 patients > or = 65 years) on entry: mean blood pressure was 173/103 mmHg, 21% were cigarette smokers, and baseline blood cholesterol (mean 6.84 mmol/l) exceeded 6.5 mmol/l in 56% and 5.2 mmol/l in 88% of patients. In all, 4385 patients (91%) completed the study, including 89% of those > or = 65 years. Blood pressure was controlled (diastolic BP < or = 90 mmHg or a reduction > or = 10 mmHg) in 81% of patients with a mean reduction of 21/15 mmHg and a mean final daily dose of 2.9 mg doxazosin. Adverse events were reported in 827 patients (17%), were severe in 72 (1.5%), and led to withdrawal in 269 patients (5.7%). Dizziness and related symptoms (6%; severe 1.1%), headache (3.8%) and fatigue (2.6%) were most frequent; dizziness led to study withdrawal in 1.3% of patients. Fainting or syncope occurred in 13 patients (0.3%). Differences in adverse event frequency between younger (< 65) and older patients were small (dizziness: younger 5.1%, older 8.1%). Troublesome postural hypotension was uncommon as a clinical problem. Modest but statistically significant reductions occurred in blood total (4.09%) and LDL (5.13%) cholesterol. These results are in accord with those of controlled studies, and help confirm the suitability of doxazosin as part of a multiple risk factor approach to the management of hypertension. /Salt not specified/
Doxazosin is a long-acting selective alpha 1-adrenoceptor antagonist structurally related to prazosin. Like prazosin, doxazosin exerts its antihypertensive effect by reducing total peripheral resistance by selective postsynaptic alpha 1-blockade, without reducing cardiac output, and similarly, doxazosin appears to have a negligible effect on heart rate. Doxazosin differs from prazosin in that its long half-life enables once-a-day oral administration. Doxazosin significantly lowers both standing and supine blood pressure and appears to maintain this antihypertensive effect over a 24-hour dosing interval. Doxazosin 1 to 16 mg once daily has been found to be comparable in efficacy to atenolol 50 to 100 mg and prazosin 1 to 20 mg daily. Characteristic of alpha 1-adrenoceptor antagonists, doxazosin also has favourable effects on the plasma lipid profile in that it decreases total cholesterol and triglycerides, and increases high density lipoprotein (HDL) cholesterol as well as the HDL/total cholesterol ratio. Although further long term trials are needed to clarify the role of doxazosin in multidrug regimens in more severe hypertension, it appears to be a suitable drug for consideration as first-line therapy in mild to moderate essential hypertension. /Salt not specified/
Although post exercise proteinuria has long been known, its exact pathophysiology is unclear. Our objective was to determine whether long-term angiotensin converting enzyme (ACE) inhibition by different ACE inhibitors had an influence on post exercise proteinuria. We studied 14 patients who also had mild, chronic proteinuria caused by diabetes mellitus or chronic glomerulonephritis. We compared changes both in chronic (baseline) and post exercise proteinuria, during and after treatment with three different ACE inhibitors, with appropriate washout periods for the three drugs to all 14 patients. Proteinuria (mg/24 hours +/- SD), prior to the treatment was 682 +/- 92. Proteinuria after treatment for 30 days with benazepril was 464.4 +/- 82.6 (p < 0.001), with enalapril: 477.1 +/- 105.5 (p < 0.001), and captopril: 504.7 +/- 100.1 (p < 0.001). Proteinuria three days after discontinuing the treatment with benazepril was 532.4 +/- 113.5, (p < 0.01), with enalapril: 561.3 +/- 128.5, (p < 0.01), and with captopril: 620.8 +/- 101.8, p = n.s. Post exercise proteinuria prior to treatment (mg/min. +/- SD) was: 1.38 +/- 0.32, vs. after a 30-day treatment period with benazepril: 0.81 +/- 0.19 (p < 0.001), enalapril: 0.95 +/- 0.24, (p < 0.001), captopril: 1.09 +/- 0.27 (p < 0.02). Post exercise proteinuria three days after discontinuing the treatment was (blood pressure already back to baseline): in case of benazepril: 1.26 +/- 0.36 (p = n.s.), of enalapril: 1.17 +/- 0.46 (p = n.s.), and of captopril: 1.34 +/- 0.41 (p = n.s.). We conclude that the renin-angiotensin system plays a significant role in the pathogenesis of post exercise proteinuria; the antiproteinuric effect of ACE inhibition in exercise-induced proteinuria seems to be associated chiefly with the hemodynamic changes due to these drugs, whereas in chronic proteinuria the antiproteinuric and antihypertensive effects are, at least partially, dissociated. /Salt not specified/
【Biomedical Effects and Toxicity】
Most doxazosin metabolites are eliminated in the feces. /Salt not specified/
Well absorbed from gastrointestinal tract; bioavailability is about 65%. /Salt not specified/
Elimination: Fecal: Unchanged drug, about 5%; metabolites, 63 to 65%. Renal: 9%. /Salt not specified/

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