Perindopril tert-butylamine tablets
Function and Efficacy
1. Perindopril is an angiotensin converting enzyme inhibitor (ACEI). Angiotensin converting enzyme can convert angiotensin I into angiotensin II. Angiotensin II has a significant vasoconstrictive effect and can stimulate the adrenal cortex to secrete aldosterone. Perindopril can lead to: 1.1 Decreased aldosterone secretion. 1.2 Increased renin activity due to the lack of aldosterone side feedback. 1.3 Long-term use reduces total peripheral arterial resistance and preferentially acts on muscle and renal blood flow without sodium and fluid retention or reflex tachycardia. 2. Like all ACE inhibitors, perindopril inhibits the degradation of bradykinin, a strong peptide vasodilator, into inactive peptides. Perindopril can lower blood pressure in patients with low or normal renin levels. 3. Perindopril acts with its active ingredient perindoprilat, and other metabolites are inactive. Characteristics of antihypertensive effects Treatment of hypertension 1. Perindopril can be used to treat various degrees of hypertension: mild, moderate, or severe. Lowers systolic and diastolic blood pressure in supine and standing positions. 2. After taking a single dose, the maximum antihypertensive effect occurs 4-6 hours later and lasts for more than 24 hours. 3. After 24 hours, the residual angiotensin converting enzyme inhibition is still high (close to 80%). 4. For effective patients, blood pressure can return to normal after 1 month of treatment, and no drug resistance will be developed. 5. After stopping treatment, it does not cause blood pressure rebound. 6. Perindopril has a vasodilating effect, restores the elasticity of large arteries and reduces left ventricular hypertrophy. 7. When necessary, it can produce a synergistic effect when used in combination with thiazide diuretics. The combination of converting enzyme inhibitors and thiazide diuretics can reduce the risk of hypokalemia caused by taking diuretics alone. Treatment of heart failure 1. Three studies on chronic heart failure showed that compared with other similar drugs, perindopril lowers blood pressure more gently, and rarely causes sudden blood pressure drops. 2. Hemodynamic mechanism of action of heart failure 3. Perindopril reduces cardiac load: 3.1 It may change the metabolism of prostaglandins and dilate veins: reduce preload. 3.2 Reduce total peripheral vascular resistance: Reduce afterload. Studies on patients with heart failure show: 3.3 Reduce left and right ventricular filling pressure 3.4 Reduce total peripheral vascular resistance 3.5 Increase cardiac output and improve cardiac index 3.6 Increase local muscle blood flow and improve exercise endurance
Ingredients
Perindopril tert-butylamine salt
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Perindopril erbumineIngredients |
1. Perindopril is an angiotensin-converting enzyme inhibitor (ACEI) that reduces aldosterone secretion, increases renin activity, and reduces total peripheral arterial resistance in the long term; 2. It inhibits the degradation of bradykinin into inactive peptides; 3. It can lower blood pressure in patients with low or normal renin levels; 4. Its active ingredient, perindoprilat, exerts an antihypertensive effect without producing drug resistance, and there is no blood pressure rebound after drug withdrawal; 5. It has a vasodilatory effect, restores the elasticity of the large arteries and reduces left ventricular hypertrophy; 6. It can be used in combination with thiazide diuretics to synergistically lower blood pressure; 7. It can moderately lower blood pressure, reduce cardiac load, and increase cardiac output and exercise endurance in the treatment of heart failure. More |
107133-36-8 | 35 |
Appearance
This product is a green round tablet with scores on both sides.
Indication
Used for hypertension and congestive heart failure.
Usage and Dosage
Perindopril tablets must be taken before meals because food changes the bioavailability of its active metabolite perindoprilat. Perindopril is taken once a day. Essential hypertension 1. No sodium loss or renal failure (i.e. under normal circumstances): The effective dose is 4 mg/day, taken once in the morning. Depending on the efficacy, the dose can be gradually increased to a maximum dose of 8 mg/day within three to four weeks. If necessary, potassium-excreting diuretics can be used in combination to further lower blood pressure. 2. Hypertensive patients who have been treated with diuretics 2.1 Stop taking diuretics three days before starting treatment. If necessary, diuretics can be added again later. 2.2 Or start treatment with 2 mg and adjust the dose according to the antihypertensive effect. 2.3 It is recommended to monitor blood creatinine and blood potassium levels before treatment and within the first 15 days of treatment. 3. Elderly (see: Precautions) Start treatment with a low dose (2 mg/day, take the medicine in the morning) and increase to 4 mg/day after one month if necessary. If previous examinations show that renal dysfunction is not due to age, the dose can be adjusted according to the patient's renal function if necessary. Creatinine clearance can accurately show the renal function of the elderly. Creatinine clearance is based on serum creatinine and corrected by age, weight and gender, and calculated using Cockroft's formula: *Clcr=(140-age)×weight/0.814×serum creatinine (age is expressed in years, weight is expressed in kilograms, and serum creatinine is expressed in mmol/l. This formula is applicable to adult males, and women are corrected by multiplying by 0.85.) Renovascular hypertension 1. The recommended starting dose is 2 mg/day, and the dose is adjusted according to the patient's blood pressure response. 2. Serum creatinine and potassium should be checked to detect the presence of functional renal insufficiency. (See: Precautions) 3. In case of renal insufficiency, the dose of perindopril should be adjusted according to the degree of renal insufficiency: 4. If the creatinine clearance is ≥60ml/min, no dose adjustment is required. 5. If creatinine clearance is <60 ml/min, refer to the following table: Creatinine clearance (ml/min) Recommended dose 30 < creatinine clearance < 602 mg/day; 15 < creatinine clearance < 302 mg/every other day 6. The usual medical treatment for such patients includes regular monitoring of serum potassium and serum creatinine, such as once every two months in the stable stage of treatment. In this case, the diuretic that can be used in combination is a loop diuretic. Hypertensive patients on hemodialysis (Clcr < 15 ml/min) Perindopril can be cleared by dialysis. The dialysis clearance is 70 ml/min. Give 2 mg of perindopril on the day of dialysis. Congestive heart failure 1. Start treatment with a low dose, especially in the following cases: Initial low blood pressure or normal renal failure hyponatremia, whether or not caused by drugs (diuretics). 2. ACE inhibitors can be used in combination with diuretics, and digitalis glycosides can be added if necessary. 3. It is recommended to start treatment with 2 mg every morning while monitoring blood pressure. If necessary, increase to the conventional therapeutic dose, i.e. 2-4 mg per day, taken once. 4. The selected daily therapeutic dose should make the standing systolic blood pressure not less than 90 mmHg. High-risk heart failure patients (severe heart failure, patients receiving high-dose diuretic treatment) 1. Symptomatic hypotension may occur after medication. The starting dose for such patients should be halved (i.e. 1 mg/day). 2. Blood potassium and blood creatinine should be tested each time the dose is increased, and tests should be performed every 3-6 months according to the cardiac function classification in order to evaluate the safety of treatment.
Adverse Reactions
Clinical side effects 1. Headache, fatigue, dizziness, mood or sleep disorders, cramps 2. Postural or non-postural hypotension (see: Precautions) 3. Rashes in a few cases 4. Stomach pain, anorexia, nausea, abdominal pain, taste disorders 5. Dry cough has been reported to be associated with the use of ACE inhibitors, which is characterized by persistence, but the dry cough disappears after discontinuation of the drug. If the above situation occurs, it should be considered that this symptom may be caused by the drug. 6. Very rare: angioedema (Quigan edema) (see: Warnings) Effects on laboratory indicators 1. Moderate increase in blood urea and blood creatinine, which can be restored after stopping treatment. This increase is more common in patients with hypertension and renal failure with combined renal artery stenosis, diuretic treatment. 2. In patients with glomerular nephropathy, ACE inhibitors can cause proteinuria. 3. Hyperkalemia, usually transient. 4. Anemia has been reported (see: Precautions) in special patients (renal transplantation, hemodialysis) treated with ACE inhibitors.
Precautions
It is contraindicated for people who are allergic to this product, children, pregnant women, and lactating women; the dosage should be carefully adjusted for patients with renovascular hypertension, surgery, anesthesia, or renal insufficiency.
Special Population Medication
Precautions for children: Children are prohibited from taking this drug. Precautions for pregnancy and lactation: Precautions for pregnant and lactating women are prohibited. Precautions for the elderly: Before starting treatment, renal function and blood potassium should be checked (see: Dosage and Administration). The initial dose should be adjusted according to changes in blood pressure, and should be used with caution in cases of water and sodium loss to avoid a sudden drop in blood pressure.
Drug Interactions
Contraindications 1. Potassium-sparing diuretics (amiloride, potassium canrenoate, spironolactone, triamterene, alone or in combination), except for the treatment of heart failure (low-dose ACE inhibitors and low-dose thiazide diuretics), potassium salts. Hyperkalemia (can be fatal, especially in cases of renal failure, the drugs have a synergistic effect on the increase in blood potassium). Except for patients with hypokalemia, do not use potassium supplements or potassium-sparing diuretics with ACE inhibitors. 2. Lithium ACE inhibitors increase blood lithium concentrations and even reach toxic levels (reduce renal excretion of lithium). If ACE inhibitors must be used, blood lithium levels must be closely monitored and the dose adjusted. 3. Estramustine increases the risk of angioedema. 1. Nonsteroidal anti-inflammatory drugs and acetylsalicylic acid (aspirin) ge; 3 g/day In high-risk patients (elderly and/or dehydrated patients), the combination of ACE inhibitors and nonsteroidal anti-inflammatory drugs can cause acute renal failure by reducing glomerular filtration and inhibiting the synthesis of vasodilator prostaglandins, while the hypotensive effect is weakened. Therefore, appropriate fluid replacement should be given at the beginning of treatment, and renal function should be monitored. 2. Antidiabetic preparations (insulin, sulfonylureas) Capture of captopril and enalapril In patients receiving insulin and sulfonylurea hypoglycemic drugs, ACE inhibitors can enhance the effect of lowering blood sugar. However, symptoms of hypoglycemia rarely occur (improving glucose tolerance and reducing the need for insulin). Strengthen self-monitoring of blood sugar. 3. Baclofen increases the antihypertensive effect. Monitor blood pressure and adjust the dose of antihypertensive drugs when necessary. 4. Thiazide diuretics have the risk of causing sudden hypotension and/or acute renal failure when starting ACE inhibitor treatment in cases of water and sodium loss. In patients with hypertension, if the previous diuretic treatment has caused water and sodium loss (especially patients who have recently received diuretic treatment, low-salt diet, and hemodialysis). Recommendations: 1. Stop using diuretics before starting ACE inhibitor treatment, and if necessary, use non-potassium-sparing diuretics again. Or start ACE inhibitor treatment with a low dose and gradually increase the dose. 2. For patients with congestive heart failure who are taking diuretics, if necessary, start ACE inhibitor treatment with a low dose after reducing the dose of non-potassium-sparing diuretics. 2.1 In all cases, renal function (serum creatinine) should be monitored in the first few weeks of ACE inhibitor treatment. 2.2 Potassium-sparing diuretics: They can be used alone (amiloride, potassium canrenoate, spironolactone, triamterene), or in combination with New York Heart Association class III or IV patients with an ejection fraction of 35% who have already used ACEI and loop diuretics. If the prescription principles of combined medication are not followed, the combination of ACE inhibitors and potassium-sparing diuretics may cause hyperkalemia, which may even be fatal. Therefore, hyperkalemia and renal insufficiency should be excluded before medication, and serum potassium and serum creatinine should be closely monitored (measured once a week in the first month after treatment, and once a month thereafter). Possible combinations 2.3 Amifostine enhances the hypotensive effect. 3. Tricyclic antidepressants and neuroleptics increase the risk of antihypertensive effects and orthostatic hypotension (synergistic effect) 4. Cortisone, tecositide (oral) (except corticosteroids used as replacement therapy for Addison's disease) weaken the antihypertensive effect (corticosteroids cause water and sodium retention) 5. Alpha-receptor blockers used in the urinary tract: alfuzosin, prazosin, terazosin, tamsulosin will enhance the antihypertensive effect and increase the risk of orthostatic hypotension.
Storage
Keep away from light, seal and store in a cool place (not exceeding 20℃).
Packaging Specification
8mg
Validity Period
24 months.