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Doxazosin mesylate tablets [English name] DoxazosinMesylate Tablets [Pinyin] Jiahuangsuan Duoshazuoqin Pian [Main ingredients] [1 - (4 - amino -6,7 - dimethoxy -2- quinazoline-yl) - 4 - (1,4 - Benzodioxan -2- support carbonyl)] piperazine mesylate [Characters] product is white or white film [The role of category] prostate medication [toxicology] sandy azole hydrochloride tablets is a long-acting 1-receptor blocker. The product selectivity for 1-adrenergic receptors in the Festival, so that peripheral vasodilation, decreased peripheral vascular resistance and lower blood pressure, had little effect on cardiac output. With other 1-blockers like doxazosin Orthostatic blood pressure and heart rate greater impact. This product is acting on the prostate and bladder neck smooth muscle of the 1-adrenergic receptors, the bladder neck, prostate, prostate capsule smooth muscle relaxation, urethra and bladder to reduce the resistance, thus reducing the urethral obstruction caused by benign prostatic hyperplasia symptoms. This product can be slightly lower total cholesterol (2 ~ 3%), LDL-cholesterol (4%), and HDL-cholesterol increased slightly (4%). However, the clinical significance of these changes is unclear. Carcinogenic, mutagenic and reproductive toxicity in rats and mice were long-term oral (24 months) the maximum tolerated dose of doxazosin (40mg/kg / day and 120mg/kg / day) showed no carcinogenic activity. Mutagenicity studies have not shown this product and its metabolit


es on chromosomes and sub-chromosome structure. Rat studies confirmed that oral administration of the product 20mg/kg / day, can reduce the reproductive ability of male rats; but stop taking this product can be restored after 2 weeks of their reproductive capacity. 5 and the product in the oral 10mg/kg / day seen its influence on male fertility. This product has not yet seen any human male fertility impact report. Pregnant rabbits and rats, respectively, daily oral administration of the goods up to 41mg/kg and 20mg/kg (the human equivalent of taking this 12mg / day and the ACU Cmax 10 times and 4 times), the cubs did not find an impact on the child. In taking this up to 80mg/kg in rabbits, it can reduce fetal survival rate of cubs. Studies have shown that the radioactive materials through the pregnant rat placenta. Perinatal study in rats showed that daily oral administration of the goods 40 or 50mg/kg (the human equivalent of taking this 12mg / day 8 times ACU) may delay the post-natal development of young rats. Lactating rat study found that female rats a single oral dose of [2-14C] labeled 1mg/kg this product, its maximum concentration in milk than in maternal plasma concentrations 20 times higher than [Pharmacokinetics] after oral administration of the product rapid absorption, peak time of 2-3 hours, bioavailability of about 65%, and 98% protein binding, terminal elimination half-life (t1 / 2) for 19 to 22 hours. Delayed drug absorption after eating about 1 hour, but no significant decrease of clinical efficacy. Extensive in the liver metabolism of the product. Although identified several active and inactive metabolites, but its pharmacokinetic properties is not clear. This product is mainly excluded from the stool, 63% of the metabolites, 4.8% for the prototype; renal excretion of 9%. Morning administration of the product area under the curve 11% lower than the evening dose, and time to peak was significantly lower than the night about 2 hours. Hypertension study steady-state plasma concentrations, the daily oral administration of doxazosin 2-16mg, the dose and the efficacy of linear. Pharmacokinetic studies have shown that doxazosin plasma half-life and clearance rate from the age or the impact of impaired renal function, but a single oral dose in patients with cirrhosis of doxazosin 2mg increase of 40% when the above parameters. Currently the drug on hepatic metabolism of doxazosin is not yet much of the information. [Indications] essential hypertension; benign prostatic hyperplasia. [Usage and dosage] 1. Adult usual dose of oral initial dose of 1mg, once daily, 1-2 weeks after the clinical response and tolerability based on adjust the dose; the first agent should adjust the dose before bedtime. Maintenance dose of 1-8mg, day 1, but more than 4mg easy to cause orthostatic hypotension. Foreign research data suggest that the maximum dose of this product to 16mg / day.
2. Pediatric dose has not been determined. [Adverse reactions] 1. More than 10% incidence of adverse reactions: dizziness, headache, malaise and discomfort.
2. 2-10% incidence of adverse reactions: drowsiness, edema, nausea, rhinitis, dyspnea, orthostatic hypotension, palpitations, dizziness, dry mouth, abnormal vision, nervousness, sexual dysfunction, diarrhea, polyuria, chest pain and body pain. Orthostatic hypotension, edema, and dyspnea often dose dependent.
3. 1% incidence of adverse reactions: arrhythmia, hypotension, rash, itching, joint pain / arthritis, muscle weakness, myalgia, paresthesia, dyskinesia, ataxia, excessive tension, muscle spasm , flushing, conjunctivitis, tinnitus, depression, insomnia, constipation, indigestion, flatulence, nose bleeding, urinary incontinence, weakness, and facial swelling.
4. 0.3% incidence of adverse reactions: tachycardia, peripheral peripheral ischemia. [Taboo] 1. Of quinazoline (such as prazosin, terazosin) allergy. 2. After taking this serious hypotension. [Note] 1. To reduce the first dose effect and orthostatic hypotension, treatment should be the first dose of 1mg, demand to increase the dose every 1-2 weeks, after the initial and the first dose of each increment are advised before going to bed taking.
2. The patient at the beginning of treatment and the treatment dose should be increased to avoid sudden changes in posture and action, and pay attention to the possible harm to the body.
3. This product, if additional therapy with other antihypertensive drugs, the product dose should be reduced; If the product has been added to antihypertensive drug treatment should be extra careful.
4. If syncope occurs, patients in the supine position should be set, if necessary, to support treatment. Patients with impaired liver function or are using any drugs that affect liver metabolism, the application doxazosin should be very cautious.
5. Penis treatment of spasticity is the product a very rare adverse reactions, can cause persistent impotence, in the event of requiring immediate treatment.
6. Prostate cancer and benign prostatic hyperplasia many of the symptoms of the same, and both often in combination, it is the beginning of doxazosin in the treatment of benign prostatic hyperplasia, should be ruled out prostate cancer. [Pregnant and lactating women drug] is currently using the product's safety in pregnant women has not been established, the product only be used for pregnant women is necessary. Is not known whether the drug through human milk secretion, breast-feeding women should be careful of this drug. [Pediatric patients] as anti-hypertensive drugs, application of this product in children's safety and effectiveness is not yet clear. [Medication in elderly patients] of the goods hypertension in the elderly may have a significant hypotension, the need to reduce daily maintenance dose. This product is the treatment of benign prostatic hyperplasia, the elderly and non-elderly safety and effectiveness are the same. [Drug interactions] 1. Indomethacin or other non-steroidal anti-inflammatory drugs and the chemicals can be reduced with the use of antihypertensive effect. May be due to inhibition of renal prostaglandin synthesis and (or) cause water and sodium retention.
2. Cimetidine may slightly increase doxazosin plasma concentration and half-life, but their clinical significance is unknown.
3. Other antihypertensive drugs with the goods when the same antihypertensive effect with the increased need to adjust the dose.
4. Estrogen in combination with this product and increased fluid retention as high blood pressure.
5. Sympathomimetic amines combined with the product can boost the role of the former and the latter are reduced hypotensive effect.
6. Outside the body plasma studies have shown that doxazosin digoxin, warfarin, phenytoin, indomethacin had no effect on protein binding. [Drug overdose] more performance for the orthostatic hypotension, dizziness, headache, fatigue, drowsiness, severe cases, shock or death. Light Purchase patient supine, low blood pressure are given rehydration, boost treatment; In severe cases, gastric lavage should be immediately activated carbon, while giving the anti-shock treatment. Doxazosin because of high protein binding, hemodialysis can not be excreted. [Storage] shading, sealed. [Specification] 2mg prosperity depend on our support forum
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