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Doxazosin Mesylate Tablets

Function and Efficacy

Doxazosin tablets are long-acting a1-receptor blockers. This product selectively acts on postganglionic a1-adrenergic receptors, causing peripheral vasodilation, reducing peripheral vascular resistance and lowering blood pressure, with little effect on cardiac output. Like other a1-receptor blockers, doxazosin has a greater effect on standing blood pressure and heart rate. This product acts on the a1-adrenergic receptors of the prostate and bladder neck smooth muscles, relaxing the bladder neck, prostate, and prostate capsule smooth muscles, reducing urethral and bladder resistance, thereby alleviating the symptoms of urethral obstruction caused by prostatic hyperplasia. This product can slightly reduce total cholesterol (2-3%), LDL-cholesterol (4%), and slightly increase HDL-cholesterol (4%). However, the clinical significance of these changes is currently unclear. Carcinogenicity, mutagenicity and reproductive toxicity Rats and mice were given the maximum tolerated dose of doxazosin (40 mg/kg/day and 120 mg/kg/day) for a long time (24 months), and no carcinogenic activity was found. Mutagenicity studies did not show the effects of this product and its metabolites on chromosome and subchromosome structure. Rat studies have confirmed that oral administration of 20 mg/kg/day of this product can reduce the reproductive capacity of male rats; however, their reproductive capacity can be restored within 2 weeks after stopping this product. No effect on male rat fertility was observed when this product was taken orally at 5 and 10 mg/kg/day. There are no reports on the effect of this product on human male fertility. When pregnant rabbits and rats were orally administered this product up to 41 mg/kg and 20 mg/kg per day, respectively (equivalent to 10 times and 4 times the Cmax and ACU of humans taking this product at 12 mg/day), no effect on the fetus was found. When rabbits took this product up to 80 mg/kg, the survival rate of the fetus was reduced. Radioactivity studies have shown that this product can pass through the placenta of pregnant rats. Perinatal studies in rats have shown that daily oral administration of 40 or 50 mg/kg of this product (equivalent to 8 times the ACU of humans taking this product at 12 mg/day) can delay the postnatal development of young rats. A study on lactating rats found that when the mother rats were given a single oral dose of 1 mg/kg of [2-14C]-labeled tamoxifen, the maximum concentration in their milk was 20 times higher than the maternal plasma concentration.

Ingredients

The main ingredients of this product are: doxazosin mesylate. Molecular formula: C23H25N5O5CH4O3S, molecular weight: 547.59.

Name Description Content CAS NO. Manufacturer
Doxazosin mesylateIngredients

Doxazosin tablets are long-acting a1-receptor blockers. This product selectively acts on postganglionic a1-adrenergic receptors, causing peripheral vasodilation, reducing peripheral vascular resistance and lowering blood pressure, with little effect on cardiac output. Like other a1-receptor blockers, doxazosin has a greater effect on standing blood pressure and heart rate. This product acts on the a1-adrenergic receptors of the prostate and bladder neck smooth muscles, relaxing the bladder neck, prostate, and prostate capsule smooth muscles, reducing urethral and bladder resistance, and thus alleviating urethral obstruction symptoms caused by prostate hyperplasia. This product can slightly reduce total cholesterol (2-3%), LDL-cholesterol (4%), and slightly increase HDL-cholesterol (4%). However, the clinical significance of these changes is still unclear.

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77883-43-3 34

Appearance

This product is white or off-white tablets.

Indication

Essential hypertension; benign prostatic hyperplasia.

Usage and Dosage

1. The usual dosage for adults is oral administration, with a starting dose of 1 mg once a day. The dosage is adjusted after 1-2 weeks based on clinical response and tolerance. The first dose and dosage adjustment should be taken before bedtime. The maintenance dose is 1-8 mg once a day, but more than 4 mg can easily cause postural hypotension. Foreign research data suggest that the maximum dosage of this product is 16 mg/day. 2. The dosage for children has not yet been determined.

Adverse Reactions

1 Adverse reactions with an incidence of more than 10%: dizziness, headache, fatigue and discomfort. 2 Adverse reactions with an incidence of 2-10%: drowsiness, edema, nausea, rhinitis, dyspnea, postural hypotension, palpitations, vertigo, dry mouth, visual abnormalities, nervousness, sexual dysfunction, diarrhea, polyuria, chest pain and body pain. Postural hypotension, edema and dyspnea are often dose-dependent. 3 Adverse reactions with an incidence of about 1%: arrhythmia, hypotension, rash, itching, joint pain/arthritis, muscle weakness, myalgia, paresthesia, movement disorders, ataxia, hypertonia, muscle spasm, flushing, conjunctivitis, tinnitus, depression, insomnia, constipation, indigestion, flatulence, epistaxis, urinary incontinence, weakness and facial edema. 4 Adverse reactions with an incidence of about 0.3%: tachycardia and peripheral peripheral ischemia.

Precautions

1. Those who are allergic to quinazolines (such as prazosin, terazosin). 2. Those who develop severe hypotension after taking this product.

Special Population Medication

Precautions for children: As an antihypertensive drug, the safety and effectiveness of this product in children have not yet been determined. Precautions for pregnancy and lactation: The safety of this product for pregnant women has not yet been determined. This product can only be used in pregnant women when it is absolutely necessary. It is not yet known whether this drug can be secreted through human breast milk. Lactating women should use this drug with caution. Precautions for the elderly: This product may cause obvious hypotension reactions in elderly hypertensive patients, and the daily maintenance dose must be reduced. In the treatment of benign prostatic hyperplasia, the safety and effectiveness of this product are consistent in the elderly and non-elderly.

Drug Interactions

1. The use of indomethacin or other non-steroidal anti-inflammatory drugs with this product may weaken the antihypertensive effect. This may be due to the inhibition of renal prostaglandin synthesis and/or the retention of water and sodium. 2. Cimetidine can slightly increase the blood concentration and half-life of doxazosin, but its clinical significance is unknown. 3. When other antihypertensive drugs are used with this product, the antihypertensive effect is enhanced and the dose needs to be adjusted. 4. When estrogen is used in combination with this product, blood pressure increases due to fluid retention. 5. The combination of sympathomimetic amines with this product can weaken both the pressor effect of the former and the antihypertensive effect of the latter. 6. In vitro plasma studies have shown that doxazosin has no effect on the protein binding rate of digoxin, warfarin, phenytoin, and indomethacin.

Storage

Keep away from light and store in sealed container.

Packaging Specification

Calculated as doxazosin 1mg

Validity Period

36 months.

Manufacturer

Topfond Pharmaceutical Co., Ltd.

  • Founded in:

    2013-11-13
  • Address:

    No. 2 Guangming Road, Yicheng District, Zhumadian City
  • Tax NO.:

    91411700083473072R
  • Registered Funds:

    420 million yuan
  • Website:

  • Email:

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