Bisoprolol fumarate tablets
Pharmacology:
Bisoprolol is highly selective? 1- adrenoceptor antagonist has no inherent sympathetic activity and membrane stabilizing activity. Effect of bisoprolol on bronchial and vascular smooth muscle? 1- receptor has high affinity for bronchial and vascular smooth muscle and regulates metabolism. 2- receptors have very low affinity. So bisoprolol usually does not affect respiratory resistance and? Metabolic effects of 2- receptor regulation. Bisoprolol exceeds the therapeutic dose. Is there anything else? Selective action of 1- receptor.
Clinical control studies show that the daily dose of bisoprolol is 65438±000mg, which is equivalent to the daily dose of atenolol, metoprolol or propranolol.
Bisoprolol has no obvious negative inotropic effect.
The maximum effect was achieved after 3-4 hours of oral administration of bisoprolol. Because the half-life is 10- 12 hours, the action of bisoprolol can last for 24 hours. Bisoprolol usually reaches the maximum antihypertensive effect after 2 weeks.
Toxicology:
The study of reproductive toxicity in rats showed that bisoprolol did not affect the reproductive ability and general reproductive behavior of rats.
taboo
Bisoprolol is contraindicated in the following patients:
1. Patients with acute heart failure or decompensated heart failure who need intravenous inotropic drugs.
2. Patients with cardiogenic shock
3. Patients with second or third degree atrioventricular block (without pacemaker)
4. Sick sinus syndrome patients
5. Sinus atrial block
6. Bradycardia, the heart rate is lower than 60 beats/min at the initial stage of treatment.
7. Patients with hypotension (systolic blood pressure lower than 100mmHg)
8. Patients with severe bronchial asthma or severe chronic lung obstruction
9 patients with advanced peripheral arterial occlusive disease and Raynaud's syndrome
10. Patients with untreated pheochromocytoma
1 1. Patients with metabolic acidosis
12. Patients who are known to be allergic to bisoprolol and its derivatives or any component of this product.
Drug Name Irbesartan Hydrochlorothiazide Tablets
English names irbesartan and hydrochlorothiazide
pharmacodynamics
This product is a compound medicine composed of angiotensin Ⅱ receptor antagonist irbesartan and thiazide diuretic hydrochlorothiazide. The hypotensive effect of this compound is synergistic and more effective than any single drug. Irbesartan is a potent and effective oral selective angiotensin II receptor antagonist (subtype AT 1). No matter the source or synthetic pathway of angiotensin ⅱ, it can block all the effects of angiotensin ⅱ mediated by AT 1 receptor. Its selective antagonism to angiotensin Ⅱ receptor (AT 1) leads to the increase of plasma renin and angiotensin Ⅱ levels and the decrease of plasma aldosterone levels. When the recommended dose of irbesartan is given to patients without electrolyte disorder alone, serum potassium will not be significantly affected. Irbesartan does not inhibit angiotensin converting enzyme (ACE kininase II), which can produce angiotensin II and degrade bradykinin into inactive metabolites. The activity of irbesartan does not need metabolic activation. Hydrochlorothiazide is a thiazide diuretic. It can affect the reabsorption mechanism of electrolyte by renal tubules and directly increase the excretion of sodium and chlorine (approximately equal). Hydrochlorothiazide reduces blood volume, increases plasma renin activity and aldosterone secretion, thereby increasing the excretion of potassium and bicarbonate in urine and reducing the level of potassium in serum. Combined use of irbesartan can reverse diuretic-related potassium loss by blocking renin-angiotensin-aldosterone system.
pharmacokinetics
The combined use of irbesartan and hydrochlorothiazide has no effect on the pharmacokinetics of the two drugs.
Irbesartan and hydrochlorothiazide are effective oral drugs, and they can exert their activities without biotransformation. After oral administration, its absolute bioavailability is 60-80% in irbesartan and 50-80% in hydrochlorothiazide. Eating does not affect the bioavailability of this product. The peak plasma concentrations of irbesartan and hydrochlorothiazide were 1.5-2 hours and 1-2.5 hours, respectively. The binding rate of irbesartan plasma protein is about 96%, and it hardly binds to blood cells, with a distribution volume of 53-93 liters. The plasma protein binding rate of hydrochlorothiazide is 68%, and its apparent distribution volume is 0.83- 1. 14l/kg.
Irbesartan is metabolized in the liver by combining with glucuronic acid and oxidation. The main oral metabolite is glucuronic acid bound irbesartan (about 6%). In vitro experiments showed that irbesartan was mainly oxidized and metabolized by cytochrome P450 CYP2C9, and CYP3A4 had little effect. Irbesartan and its metabolites are excreted through biliary tract and kidney. Hydrochlorothiazide is not metabolized, but is quickly excreted by the kidneys. At least 6 1% of the oral dose is discharged in prototype within 24 hours. Hydrochlorothiazide can penetrate the placenta, but not the blood-brain barrier, and can be secreted into milk.
Renal Insufficiency: There was no significant change in the pharmacokinetic parameters of irbesartan in patients with renal insufficiency or receiving hemodialysis. Irbesartan cannot be removed by hemodialysis. Creatinine clearance rate
Liver function damage: For patients with mild to moderate liver cirrhosis, the pharmacokinetic parameters of irbesartan have no obvious change. Pharmacokinetics of patients with severe liver injury has not been studied.
indicate
Can be used for treating essential hypertension.
The fixed-dose compound is used for treating patients whose blood pressure cannot be effectively controlled by using irbesartan or hydrochlorothiazide alone.
dosage
Take orally, on an empty stomach or with meals. The usual initial and maintenance dose is 1 tablet, daily 1 time, which can be increased to 2 tablets per day 1 time according to the condition.
It is suggested that patients can adjust a single component (i.e. irbesartan or hydrochlorothiazide).
It is not recommended to use a daily dose greater than 300mg/irbesartan/25mg hydrochlorothiazide. When necessary, this product can be combined with other antihypertensive drugs.
counteraction
The adverse reactions of patients treated with this product are usually mild and temporary.
According to the comparison of the two prescriptions, I believe you have a certain understanding of the three drugs. How to choose is up to you. In addition, I suggest you pay more attention to your diet.
Finally, I wish you good health. ..