What Is Perindopril Erbumine?
Perindopril, clinically used for hypertension and congestive heart failure.
- Drug Name
- Perindopril tablets
- Drug type
- Occupational injury medical insurance
- Hanyu Pinyin
- Pei Duo Pu Li Pian
- Use classification
- Angiotensin I converting enzyme inhibitor
- Perindopril, clinically used for hypertension and congestive heart failure.
Perindopril tablets ingredients
- Chemical name: Perindopril tert-butylamine salt, (2S, 3aS, 7aS) -1 {(S) -N-[(S) -1-ethylethylbutyl] alanyl} octahydro-1H-indole -2-carboxylic acid, tert-butylamine salt (1: 1)
Chemical Structure:
Molecular formula: C 19 H 32 N 2 O 5 · C 4 H 11 N
Molecular weight: 441.6
Perindopril tablets
- 4mg: This product is a white strip-shaped tablet with indentations in the middle.
8mg: This product is a green round tablet with scores on both sides, with printed on one side and printed on the other.
Perindopril tablets indications
- Hypertension and congestive heart failure.
Perindopril tablets specifications
- 4mg; 8mg (based on perindopril tert-butylamine salt C 19 H 32 N 2 O 5 · C 4 H 11 N).
Perindopril tablets dosage
- It is recommended to take it every morning before meals.
The dosage can be individualized according to the patient's specific conditions and blood pressure response.
hypertension:
Yashida can be used alone or in combination with other antihypertensive drugs.
Anhydrous sodium loss or renal failure (ie under normal conditions):
For essential hypertension without complications such as water and sodium loss or renal failure, it is recommended to start treatment with 4mg and take it once a day in the morning. According to the efficacy, it can be gradually increased to a maximum dose of 8 mg / day within three to four weeks.
In patients with excessive activation of the renin-angiotensin-aldosterone system (especially: renal vascular hypertension, loss of sodium and / or volume, cardiac decompensation or severe hypertension), blood pressure may be caused at the end of the starter Excessive decline. For such patients, it is recommended to start with a dose of 2 mg. Initial treatment should be performed under medical observation.
Symptomatic hypotension may occur after initiation of Yashida treatment. This condition is more likely to occur in patients treated with diuretics in combination, because such patients may have reduced volume and / or sodium and should be treated with caution.
If necessary, diuretics should be discontinued 2-3 days before starting Yashida treatment.
For patients with hypertension who cannot stop diuretics, Yashida should start with 2mg and monitor renal function and serum potassium concentration.
The subsequent dose of Yashida should be adjusted based on the blood pressure response. Diuretic therapy can be resumed if needed.
The elderly should start with 2mg and gradually increase to 4mg after one month. If necessary, it can be increased by 8mg according to the renal function (see the table below).
Congestive heart failure:
When used in combination with non-potassium-preserving diuretics and / or digoxin and / or beta-blockers, Yashida is advised to take 2mg as the starting dose in the morning under careful medical observation. If the patient can tolerate it, the dose can be increased to 4 mg once a day after 2 weeks. The dose adjustment should be based on the individual clinical response of the patient.
In patients with severe heart failure and patients considered to be at high risk (patients with impaired renal function and prone to electrolyte disturbances, and treated with diuretics and / or vasodilators), treatment should be started with careful observation. Recommended starting The dose was 1 mg / day.
Patients who are very prone to symptomatic hypotension, such as patients with sodium loss (with or without hyponatremia), patients with reduced blood volume, or patients undergoing potent diuretics, these should be corrected before treatment with Yashida Happening. Patients' blood pressure, renal function, and serum potassium should be closely observed before and during the treatment.
Dose adjustment in the case of kidney damage:
The dosage of patients with impaired renal function should be listed in Table 1 based on creatinine clearance:
Table 1: Dose-adjusted creatinine clearance (ml / min) at renal impairment Maintenance dose creatinine clearance 60 4 mg per day
30 <creatinine clearance <60 2mg per day
15 <creatinine clearance <30 2mg every other day
Patients on hemodialysis *
Creatinine clearance <15 with 2 mg on the day of dialysis
* The dialysis clearance of perindopril is 70 ml / min. For hemodialysis patients, medication should be taken after dialysis.
The most adjusted when the liver is damaged:
Patients with liver damage do not need to adjust the dose.
Perindopril adverse reactions
- During the treatment with perindopril, the following adverse reactions were found, ranked by frequency: very common (> 1/10); common (> 1/1 00, <1/10), uncommon (> 1/1000, <1/100). Rare (> 1/1 0000, <1/1000), extremely rare "1/10000". Unknown (cannot be evaluated from available data).
Hematological and lymphatic disorders:
Reports of decreased hemoglobin, hematocrit, thrombocytopenia, leukopenia / neutropenia, agranulocytosis or pancytopenia are extremely rare. In patients with congenital glucose hexaphosphate dehydrogenase deficiency, reports of hemolytic anemia are extremely rare.
Metabolic disorders and nutritional imbalances:
Unknown: hypoglycemia.
Mental disorders:
Uncommon: mood or sleep disorders.
Nervous system disorders:
Common: headache, dizziness, dizziness, and paresthesia.
Very rare: unconscious.
Visual impairment:
Common: Visual impairment.
Hearing and Lost Disorders:
Common: Tinnitus.
Cardiovascular abnormalities:
Very rare: Arrhythmias, angina pectoris, and myocardial infarction may be secondary to high blood pressure in high-risk patients.
Vascular diseases:
Common: Hypotension and hypotension-related reactions.
Rarely: Strokes in patients at high risk may be secondary to an excessively low blood pressure.
Unknown: vasculitis.
Respiratory, chest and mediastinal disorders:
Common: Cough, difficulty breathing.
Uncommon: bronchospasm.
Very rare: eosinophilic pneumonia, rhinitis.
Gastrointestinal Dysfunction:
Common: nausea, vomiting, abdominal pain, taste disorders, indigestion, diarrhea, constipation.
Uncommon: dry mouth.
Very rare: pancreatitis.
Hepatobiliary Dysfunction:
Very rare: cytolytic or cholestatic hepatitis.
Dysfunction of skin and subcutaneous tissue:
Common: rash, pruritus.
Uncommon: Angioedema of the face, limbs, lips, mucous membranes, tongue, glottis and / or throat, rubella
Very rare: polymorphic erythema.
Muscle, connective tissue and skeletal system dysfunction:
Common: muscle cramps.
Renal and urinary dysfunction:
Uncommon: Renal insufficiency.
Very rare: acute renal failure.
Reproductive system and breast dysfunction:
Uncommon: Impotence.
Systemic disorders:
Common: Weakness.
Uncommon: Sweating.
Laboratory inspection:
Elevated blood urea and plasma creatinine may occur. Hyperkalemia can also occur, but it can recover after stopping the drug. These conditions are more likely to occur in patients with renal insufficiency, severe heart failure, and renal vascular hypertension. Reports of elevated liver enzymes and serum bilirubin are rare.
Perindopril taboo
- Allergic to perindopril, any excipient, or other angiotensin-converting enzyme inhibitor. History of angioedema related to the use of angiotensin-converting enzyme inhibitors. Genetic or idiopathic angioedema. The fourth to ninth month of pregnancy.
Perindopril tablets precautions
- Because the drug contains lactose, it is contraindicated in patients with congenital galactosemia, glucose and galactose malabsorption syndrome, or patients who lack lactase.
Hypotension:
Angiotensin-converting enzyme inhibitors can cause blood pressure to drop. Symptomatic hypotension is rare in patients with simple hypertension and is more likely to occur in patients with reduced volume, such as those treated with diuretics, a salt-limited diet, dialysis, diarrhea or vomiting, or severe renin dependence Patients with hypertension. For congestive heart failure, whether with or without renal insufficiency, symptomatic hypotension has been observed. This condition is more likely to occur in patients with severe heart failure (patients using high-dose diuretics, hyponatremia, or impaired renal function).
In patients at higher risk for symptomatic hypotension, close monitoring should be performed when starting treatment and adjusting doses. This is also true for patients with ischemic heart disease and cerebrovascular disease, where excessive blood pressure drops in these patients can lead to myocardial infarction or cerebrovascular events.
Patients with hypotension should be placed in the supine position. If necessary, saline should be infused intravenously. Transient hypotension is not a contraindication to continued medication, and can be continued after expansion of blood pressure and blood pressure.
In some patients with congestive heart failure with normal or low blood pressure, Yashida will further reduce systemic blood pressure. This response is predictable and usually does not require stopping treatment. If the patient has symptoms of hypotension, reduce the dose or stop using Yashida.
Aortic or mitral stenosis / hypertrophic cardiomyopathy:
As with other angiotensin-converting enzyme inhibitors, patients with mitral stenosis and obstruction of the left ventricular outflow tract, such as aortic stenosis or hypertrophic cardiomyopathy, should be used with caution.
Renal impairment:
In the case of impaired renal function (creatinine clearance <60ml / min), the starting dose of perindopril should be adjusted according to the patient's creatinine clearance and used as the patient's response to treatment. For these patients, potassium and creatinine should be used as part of a routine test.
In patients with congestive heart failure, hypotension after initiation of treatment with angiotensin-converting enzyme inhibitors may lead to further impairment of renal function. There have been reports of acute renal failure in this case, and this acute renal failure is usually reversible.
Some patients with bilateral renal artery stenosis or single renal artery stenosis who have been treated with angiotensin converting enzyme inhibitors can see an increase in blood urea and serum creatinine, which is reversible after stopping treatment. This is more likely to occur in patients with renal insufficiency.
The risk of severe hypotension and renal insufficiency is increased if renal vascular hypertension is present. For these patients, treatment should be started from a small dose under the medical observation of a doctor, and the dose should be carefully adjusted. Because diuretic therapy may be related to the above, these patients should discontinue diuretic and monitor renal function during the first few weeks of treatment with Yashida.
In some patients with hypertension who have no previous significant renal vascular disease, especially when Yashida is used in combination with diuretics, elevated blood urea and serum creatinine can occur, usually mildly, and transiently. This condition is more likely to occur in patients with pre-existing renal impairment. It may be necessary to reduce the dose and / or discontinue diuretics and / or discontinue Yashida.
For hemodialysis patients:
Life-threatening allergic reactions have been reported in patients treated with high-flow membrane dialysis combined with angiotensin-converting enzyme inhibitors. Should consider using different types of dialysis membranes or using different types of antihypertensive drugs.
Kidney transplant:
There is no Yashida experience in recent kidney transplant patients.
Hypersensitivity / Angioedema:
In patients treated with angiotensin-converting enzyme inhibitors including Yashida, reports of angioedema of the face, limbs, lips, mucous membranes, tongue, glottis, and / or laryngeal vessels are rare. It can occur at any time during treatment. Yashida should be discontinued immediately and monitored appropriately until symptoms have completely resolved. For patients whose edema is confined to the face and lips, antihistamines can alleviate symptoms, but usually they can be relieved without treatment.
Patients with a history of angiotensin-converting enzyme inhibitor-free angioedema may have an increased risk of angioedema when receiving angiotensin-converting enzyme inhibitor therapy.
There are very rare reports that taking angiotensin-converting enzyme inhibitors can cause intestinal vascular edema in patients. These patients usually show abdominal pain (with or without nausea and vomiting); usually, these patients do not progress to facial angioedema and the patient has normal Cl esterase levels. Can be confirmed by abdominal CT scan, ultrasound or surgery. Symptoms disappear after angiotensin converting enzyme inhibitor is stopped. For patients using angiotensin-converting enzyme inhibitors, if abdominal pain occurs, intestinal angioedema should be considered in the differential diagnosis.
Allergic reactions during LDL clearance:
Patients treated with angiotensin-converting enzyme inhibitors during the removal of low-density lipoprotein with dextran sulfate can experience life-threatening allergic reactions, which are very rare. These allergic reactions can be avoided by temporarily stopping angiotensin-converting enzyme inhibitor treatment for at least 24 hours before each LDL clearance.
Allergic reactions during desensitization:
Rare reports of life-threatening allergic reactions in patients undergoing desensitization with hymenoptera insect venom have been reported using angiotensin-converting enzyme inhibitors. In these patients, temporarily stopping angiotensin-converting enzyme inhibitor treatment for at least 24 hours can avoid these reactions. These reactions reappear when the angiotensin-converting enzyme inhibitor is not reapplied.
Liver failure:
In rare cases, ACEI is associated with cholestatic jaundice and can progress to sudden liver necrosis and (sometimes) death. The mechanism for this symptom is unknown. Patients receiving ACEI who have jaundice or significant elevated liver enzymes should be discontinued from ACEI and undergo appropriate medical follow-up.
Neutrophil / Granulocytosis / Thrombocytopenia / Anemia:
Patients treated with angiotensin-converting enzyme inhibitors have reported neutropenia / agranulocytosis, thrombocytopenia, and anemia. In patients with normal renal function and no other risk factors, neutropenia rarely occurs. Permopril should be used with caution in patients with: collagen vascular disease, immunosuppressive therapy, allopurinol or procainamide, or both, especially in patients with pre-existing renal impairment .
Some of these patients can develop severe infections, and some infections do not respond to intensive antibiotic treatment. If these patients use perindopril, it is recommended to monitor the white blood cell count regularly and instruct patients to report any signs of infection.
race:
Angiotensin-converting enzyme inhibitors cause angioedema in the black population to be higher than in non-black populations. Like other angiotensin-converting enzyme inhibitors, perindopril's blood pressure lowering effect is worse in black people than in non-black people, probably because the incidence of low renin status is higher in black people with hypertension.
cough:
There are reports of cough caused by taking angiotensin-converting enzyme inhibitors. This cough is characterized by a persistent dry cough that can be relieved after stopping treatment. In the differential diagnosis of cough, the possibility of cough caused by angiotensin-converting enzyme inhibitors should be considered.
Surgery / Anesthesia:
Yashida can block the formation of angiotensin II secondary to renin release in patients undergoing major surgery or anesthesia with drugs that can cause hypotension. Yashida should be discontinued the day before surgery. If hypotension occurs and is thought to be due to this mechanism, it can be corrected by expanding blood volume.
Hyperkalemia:
Elevated serum potassium was found in some patients treated with angiotensin-converting enzyme inhibitors including perindopril. High-risk patients who are prone to hyperkalemia include: renal insufficiency (over 70 years of age), diabetes, patients with dehydration, acute decompensated heart disease, and metabolic acidosis, combined with potassium-sparing diuretics (such as spironolactone , Eplerenone, chlorpheniramine, amiloride), potassium supplements or alternatives containing potassium salts, and other treatments that can cause elevated potassium (eg, heparin). The use of potassium-sparing diuretics, potassium supplements, or potassium-containing alternatives, especially in patients with altered renal function, can cause significant increases in serum potassium. Hyperkalemia can cause severe arrhythmias and is sometimes fatal. If it is considered appropriate for the patient to combine the above mentioned drugs, periodic monitoring of serum potassium is recommended.
Patients with diabetes:
Diabetics treated with oral hypoglycemic drugs or insulin should closely monitor blood glucose control during the first month of treatment with angiotensin converting enzyme inhibitors.
lithium:
Combination of lithium with perindopril is not recommended.
Potassium-preserving diuretics, potassium supplements, or alternatives containing potassium salts:
Perindopril is not recommended for use with potassium-sparing diuretics, potassium supplements, or potassium-containing salt alternatives.
Impact on ability to drive motor vehicles and manipulate machines:
Yashida does not directly affect the ability to drive motor vehicles and manipulate machines, but some patients may experience individual reactions related to decreased blood pressure, especially in the early stages of treatment or in combination with other antihypertensive drugs. As a result, the ability to drive and operate machines may be reduced.
Perindopril tablets for pregnant and lactating women
- Pregnancy:
Perindopril should not be used in the first 3 months of pregnancy. Perindopril is banned from the 4th to 9th month of pregnancy.
Existing epidemiological data cannot conclude that exposure to angiotensin-converting enzyme inhibitors during the first 3 months of pregnancy is teratogenic. However, this risk cannot be ruled out slightly.
For patients planning a pregnancy, unless continuous use of angiotensin-converting enzyme inhibitors is necessary, treatment with other antihypertensive drugs with established safety during pregnancy should be recommended. If pregnancy is confirmed, angiotensin-converting enzyme inhibitors should be discontinued immediately, and other treatments should be switched if necessary.
Exposure to angiotensin-converting enzyme inhibitors from 4 to 9 months of pregnancy is known to cause human fetal toxicity (reduced renal function, oligohydramnios, delayed skull development) and neonatal toxicity (renal failure, hypotension, high blood pressure) Kalemia). If perindopril has been used in 4-6 months of pregnancy, ultrasound examination of renal function and skull is recommended. If angiotensin-converting enzyme inhibitors are used in the mother, they should be closely monitored for hypotension.
Lactation:
Because there is no information on the use of perindopril during breastfeeding, perindopril tablets are not recommended for lactating women. It is also recommended to use known to be more effective during breastfeeding, especially when nursing newborns or premature infants. Good safety for other treatments.
Perindopril tablets for children
- The effectiveness and safety of use by children and adolescents has not been determined. Therefore it is not used for children and adolescents.
Perindopril tablets for the elderly
- The elderly should start with 2mg and gradually increase to 4mg after one month. If necessary, it can be increased to 8mg according to the renal function (see the dosage for details).
Perindopril drug interactions
- Diuretics:
With diuretics, especially in patients with reduced blood volume and / or salt content, an excessive drop in blood pressure may occur when starting treatment with an angiotensin-converting enzyme inhibitor. Perindopril treatment should start with a small dose and gradually increase the dose. Diuretics, blood volume, and salt should be stopped before starting treatment to reduce the possibility of hypotension. Renal function should be monitored during treatment. Potassium-preserving diuretics.
Potassium supplements or alternatives containing potassium salts:
Although serum potassium is usually within the normal range when treated with perindopril, some patients develop hyperkalemia. Potassium-sparing diuretics (such as spironolactone, cyanobendipine, or aminoli), potassium supplements, or potassium-containing alternatives can cause significant increases in blood potassium, so perindopril and these drugs are not recommended Joint use. If there are indications for obvious hypokalemia, care must be taken and serum potassium monitored closely.
lithium:
It has been reported that angiotensin-converting enzyme inhibitors combined with lithium cause reversible increase in serum lithium concentration and frontal poisoning. The combination of thiazide diuretics can increase the risk of lithium poisoning and further increase the lithium toxicity that has been increased by the combination of angiotensin converting enzyme inhibitors. Although combination of perindopril with lithium is not recommended, serum lithium levels must be closely monitored if it proves necessary.
Non-steroidal anti-inflammatory drugs include aspirin 3g / day:
Use of non-steroidal anti-inflammatory drugs (such as acetylsalicylic acid, COX-2 inhibitors and non-selective non-steroidal anti-inflammatory drugs used as anti-inflammatory drugs) can weaken angiotensin-converting enzyme inhibitors against hypertension Effect. Furthermore, the use of non-steroidal anti-inflammatory drugs in combination with angiotensin-converting enzyme inhibitors may increase the risk of renal function degradation, including the risk of acute renal failure and elevated potassium levels, especially in patients who already have altered renal function . The combination of these two drugs needs to be used with caution, especially in elderly patients. Patients should be given adequate hydration and testing at the beginning of treatment and subsequent regular periods to monitor renal function levels.
Antihypertensive drugs and vasodilators:
Concomitant use of these drugs can increase the hypotensive effect of perindopril. Combining it with nitroglycerin, other nitrates, or other vasodilators can lower blood pressure even more.
Antidiabetic drugs:
Epidemiological studies show that the combination of angiotensin-converting enzyme inhibitors and anti-diabetic drugs (insulin, oral and hypoglycemic agents) can increase blood glucose lowering effect, and there is a risk of hypoglycemia. This phenomenon is more likely to occur in the first few weeks of combination therapy and in patients with renal insufficiency.
Acetylsalicylic acid. Thrombolytic drugs. Beta-blocker, nitroglycerin:
Perindopril can be used with acetylsalicylic acid and thrombolytic drugs. Beta-blockers and / or nitroglycerin are used in combination.
Tricyclic antidepressants / antipsychotics / narcotics:
Certain anesthetics, tricyclic antidepressants, and antipsychotics in combination with angiotensin-converting enzyme inhibitors can cause a further drop in blood pressure.
Sympathomimetics:
Sympathomimetics can reduce the antihypertensive effect of angiotensin-converting enzyme inhibitors.
gold:
Rare reports have suggested that patients with a combination of gold injections (such as gold sodium thiomalate) and angiotensin converting enzyme inhibitors (such as perindopril) may experience nitrite-like reactions (including facial flushing, nausea , Vomiting, and hypotension).
Estramustine:
Combination with angiotensin-converting enzyme inhibitors may increase the risk of angioedema.
Perindopril overdose
- There is less data on human overdose. Symptoms related to angiotensin-converting enzyme inhibitor overdose include hypotension, circulatory shock, electrolyte disturbance, and renal failure. Hyperventilation, tachycardia, palpitations, bradycardia, dizziness, anxiety, and cough.
The recommended treatment for overdose is an intravenous infusion of 0.9% saline. If hypotension occurs, the patient should remain in shock. If possible, infusion of angiotensin II and / or consider I intravenous catecholamine treatment. Perindopril can be eliminated from the systemic circulation by hemodialysis. Patients with bradycardia who do not respond to treatment require pacemaker therapy. Vital signs, serum electrolytes, and creatinine concentrations should be continuously monitored.
Perindopril clinical trial
- The EUROPA trial is an international, multicenter, randomized, double-blind, placebo-controlled clinical trial conducted in Europe for a period of 4 years. 12,218 subjects older than 18 years were randomly assigned to the Yashida 8mg group (n = 6110) or the placebo group (n = 6108).
The trial population was stable coronary heart disease patients without heart failure. Ninety percent of patients have a previous history of myocardial infarction and / or revascularization.
Most patients add research medications on top of conventional treatments (including: platelet suppression, lipid-lowering drugs, and beta-blockers).
The primary efficacy measure was a composite endpoint of cardiovascular death, nonfatal myocardial infarction, and / or cardiac arrest with successful resuscitation.
A composite endpoint was seen in 488 (8.0%) patients in the Yashida treatment group and a composite endpoint was seen in 603 (9.9%) patients in the placebo group. 8mg Yashida once daily reduced the incidence of the primary endpoint by 1.9% (relative risk reduction by 20%. 95% confidence interval [9.4; 28.6], P <0.001).
In patients with a previous history of myocardial infarction and / or revascularization, the incidence of composite endpoints in the Yashida group was definitely 2.2% lower than in the placebo group. Relative risk was reduced by 22.4% (95% confidence interval [12.0; 31.6]. P <O.OO1).
During the randomized period of the EUROPA trial, only severe adverse events were collected. Very few patients experienced serious adverse events: including 16 (0.3%) of 6,122 patients in the Yashida treatment group and 12 (0.2%) of 6,107 patients in the placebo group. In the Yashida treatment group. Hypotension occurred in 6 patients. Angioedema occurred in 3 patients and sudden cardiac arrest in 1 patient. More patients withdrew from the trial due to cough, hypotension, or other intolerance than in the placebo group, 6.0% (n = 366) and 2.1% (n = 129), respectively.
Perindopril pharmacology and toxicology
- Perindopril is an inhibitor of an enzyme (angiotensin converting enzyme) that converts angiotensin I to angiotensin II. This invertase or kinase is a peptide chain-endolytic enzyme that converts angiotensin I to angiotensin Il that constricts blood vessels. It also degrades bradykinin that relaxes blood vessels to inactive heptapeptides. Inhibition of angiotensin-converting enzyme results in a decrease in angiotensin II in the plasma, which can lead to increased plasma renin activity (by inhibiting the negative feedback effect of renin release) and reduce aldosterone secretion. Because angiotensin-converting enzyme inactivates bradykinin, inhibition of angiotensin-converting enzyme can also increase the activity of the circulating and local kallikrein-kinin system (thus prostaglandin system is also activated). This mechanism may be related to the effect of angiotensin-converting enzyme inhibitors on lowering blood pressure, or it may be related to some side effects such as cough.
Perindopril works through its active metabolite, perindopril. Other metabolites have no inhibitory effect on angiotensin-converting enzyme activity in vitro.
hypertension:
Perindopril is effective for mild, moderate and severe hypertension. Can reduce systolic and diastolic blood pressure in supine and upright positions.
Perindopril reduces the resistance of surrounding blood vessels, which causes blood pressure to drop. Increases peripheral blood flow without affecting heart rate.
Renal blood flow is increased, and glomerular filtration rate is usually unchanged.
It exerts its maximum antihypertensive effect in 4-6 hours after a single application, and can be maintained for at least 24 hours. The valley effect is about 87-100% of the peak effect.
The antihypertensive effect occurs quickly. For responding patients, blood pressure can reach normal within one month and can be maintained for a long time without drug resistance. There is no rebound effect after stopping treatment.
Perindopril reduces left ventricular hypertrophy.
In humans, perindopril has been shown to have diastolic blood vessels. It increases aortic elasticity and reduces the medial / lumen ratio of the arterial wall.
Combination with thiazide diuretics can produce synergistic effects. Angiotensin-converting enzyme inhibitors combined with thiazide diuretics can also reduce the risk of hypokalemia caused by diuretic therapy.
Heart failure:
Perindopril reduces cardiac work by reducing preload and postload.
Studies of patients with heart failure have shown that:
-Reduce left and right ventricular filling pressure,
-Reduce the total resistance of surrounding blood vessels,
-Increase cardiac output and increase cardiac index.
In a controlled study, patients with mild to moderate heart failure who took 2 mg of Yashida for the first time showed no significant reduction in blood pressure compared to the placebo group.
Toxicology study: In long-term oral drug toxicity studies (rats and monkeys), the target organ is the kidney and the damage is reversible. No mutagenicity was found in in vitro and in vivo studies.
Reproductive toxicity studies (rats, mice, rabbits and monkeys) did not suggest fetal toxicity and teratogenicity. However, angiotensin-converting enzyme inhibitors, as a class of drugs, have been shown to cause adverse reactions in late fetal development, leading to stillbirths and congenital effects in rodents and rabbits: kidney damage and perinatal deaths Strings increase.
No carcinogenicity has been found in long-term studies in rats and mice.
Perindopril pharmacokinetics
- After oral administration, perindopril was rapidly absorbed and reached a peak concentration within 1 hour. Perindopril has a plasma half-life of 1 hour.
Perindopril is a prodrug. 27% of perindopril taken orally enters the bloodstream as the active metabolite, perindopril. In addition to the active metabolite perindopril, perindopril also produces five metabolites, all of which are inactive. Perindopril reached peak concentrations in plasma in 3-4 hours.
Food intake reduces perindopril's conversion, which is bioavailability, and perindopril should be taken once daily before a meal start. A linear relationship has been demonstrated between the dose of perindopril and its plasma exposure.
The distribution volume of unbound perindopril is about 0.2 L / Kg, and the binding to plasma proteins is very slightly 20% (mainly binding to angiotensin-converting enzyme), but it is concentration-dependent.
Perindopril is eliminated by urine. The elimination half-life of the free part is about 17 hours, and a steady state can be reached within 4 days.
The elimination of perindopril is reduced in the elderly, patients with heart failure or renal failure. The dose for patients with renal insufficiency needs to be adjusted based on the degree of kidney damage (creatinine clearance).
Perindopril has a dialysis clearance of 70 ml / min.
Perindopril kinetics changed in patients with cirrhosis: the liver molecule's liver clearance was reduced by half. However, the amount of perindoprilil formed does not decrease, so no dose adjustment is required.
Perindopril tablets storage
- Store tightly below 30 ° C.
Perindopril tablets packaging
- 4mg: aluminum-plastic packaging, 10, 30 tablets / box.
8mg: aluminum-plastic packaging, 7, 15, 30 tablets / box.
Perindopril tablet expiration date
- 24 months.
Perindopril Tablets
- 4mg: WS l-(X-012) -2007Z
8mg: YBH03832010
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