What Is Ramipril?

Ramipril tablets, indications are-primary hypertension-mild to moderate heart failure (NYHA II and III) after acute myocardial infarction (days 2-9)-non-diabetic nephropathy patients, especially with associated diabetic nephropathy Patients with arterial hypertension-patients with an increased cardiovascular risk, such as a significant history of coronary heart disease, diabetes with at least one additional risk factor, peripheral arterial occlusive disease or stroke, reducing the likelihood of myocardial infarction, stroke or cardiovascular death .

Drug Name: Ramipril

Drug type: Prescription drugs, medicines for medical workers' injuries
Use classification: Angiotensin I converting enzyme inhibitor

Ramipril tablets ingredients

The main ingredient of this product is ramipril.
Chemical name: N- [1 (S) -carbonylethoxy-3-phenyl-propyl]-(S) -alanyl-cis-bridge-2-azabicyclo [3,3,0] octyl Alkan-3 (S) -carboxylic acid chemical structure formula:

Molecular formula: C ₂₃ H ₃₂ N ₂ O ₅
Molecular weight: 416.5

Ramipril film traits

Ruitai [sup] ® [/ sup] 5 is a pink shaped sheet with a score in the middle.

Ramipril tablets indications

-Essential hypertension-Mild to moderate heart failure after acute myocardial infarction (days 2-9) (NYHA II and III)
-Patients with non-diabetic nephropathy (creatinine clearance [70 ml / min / 1.73m ² , urinary protein> 1 g / day), especially those with arterial hypertension-Patients with increased cardiovascular risk, such as a significant history of coronary heart disease Diabetes has at least one additional risk factor, peripheral arterial occlusive disease or stroke, reducing the possibility of myocardial infarction, stroke or cardiovascular death.

Ramipril Tablet Specifications

5.0 mg

Ramipril tablets dosage

1. Dosage precautions:
Hyperlipidemia may occur at the beginning of ramipril treatment, especially in patients with salt and / or fluid loss (eg, vomiting / diarrhea, diuretic treatment), heart failure (especially after myocardial infarction) or severe hypertension phenomenon.
If possible, correct salt and / or fluid loss and reduce or discontinue diuretics for at least 2-3 days before starting treatment with ramipril (in patients with heart failure, the risk of volume overload must be weighed) .
Treatment for these patients should begin with the lowest single dose, taking 1.25 mg ramipril in the morning (eg, half a ramipril 2.5 mg).
When the dose of ramipril and / or diuretic is increased after the initial administration, patients should be given medical monitoring for at least 8 hours to prevent uncontrollable hypotension reactions.
Elderly patients (greater than 65 years of age) have a more pronounced response to ACE inhibitors than younger patients. Therefore, elderly patients and patients with a significant reduction in blood pressure may be at risk (such as patients with coronary or cerebral blood supply stenosis). The starting dose (1.25 mg of ramipril daily).
Patients with malignant hypertension or heart failure (especially after acute myocardial infarction) should be hospitalized when treated with this product.
Unless otherwise prescribed, the following dosage recommendations are recommended for patients with normal renal function:
* Initial dose for patients with essential hypertension is generally 2.5 mg of ramipril morning service. If this dose does not return to normal blood pressure, it can be increased to 5 mg per day. Increase the dose at least 3 weeks apart. The maintenance dose is generally 2.5-5 mg daily, and the maximum dose is 10 mg daily. If the antihypertensive effect of 5mg daily ramipril is not satisfactory, diuretics should be considered in combination. This can enhance the antihypertensive effect of Ramipril.
* Dose adjustment of ramipril in patients with mild to moderate heart failure (NYHA II and III) after acute myocardial infarction (days 2-9) can only be performed in patients with hemodynamic stability during hospitalization. Patients concomitant with antihypertensive drugs must be monitored very closely to avoid excessive lowering of blood pressure. The initial dose is usually divided into 2.5 mg sooner or later. If this initial dose is not tolerated by the patient (eg low blood pressure), 1.25 mg should be taken in the morning and evening. The dose can then be increased depending on the condition of the patient. The dose can be doubled at intervals of 1-2 days, up to a maximum daily dose of 5 mg of ramipril.
* The recommended starting dose of ramipril for non-diabetic nephropathy is 1.25 mg once daily. Increase the dose gradually according to the patient's tolerance.
It is recommended to double the dose after 2-3 weeks.
The maintenance amount is usually 5 mg daily. High doses do not have sufficient treatment experience. For patients with creatinine clearance <60 ml / min, the maximum daily dose cannot exceed 5 mg.
* The recommended starting dose of ramipril is 2.5 mg once daily in patients with increased cardiovascular risk to reduce the likelihood of myocardial infarction, stroke and cardiovascular death. Increase the dose gradually according to the patient's tolerance.
It is recommended to double the dose after 1 week and increase to 10 mg daily after 3 weeks.
Ramipril maintenance is generally 10mg daily.
* Patients with impaired renal function (creatinine clearance <60ml / min or serum creatinine concentration <1.2mg / dl)
The starting dose is 1.25 mg in the morning (see Dosage Precautions), and the maintenance amount is usually 2.5 mg per day. The maximum daily dose cannot exceed 5 mg.
2. Method of administration The absorption of this product is not affected by food. It can be taken with a sufficient amount of liquid before, during or after meals.
After acute myocardial infarction, patients with heart failure should take daily doses at the beginning, divided into two in the morning and evening. In other cases, the daily dose can be taken once in the morning.
For patients with heart failure after acute myocardial infarction, start taking ramipril not earlier than 2 days after the infarction, but not later than 10 days after the infarction. It is recommended to take this product for at least 15 months.

Ramipril adverse reactions

This product is an antihypertensive drug. Many adverse reactions are secondary to its blood pressure lowering effect, which will lead to negative feedback regulation of adrenaline or insufficient organ perfusion. Many other effects (such as effects on electrolyte balance, certain allergic reactions, or inflammatory reactions of the mucosa) are caused by ACE inhibition or other pharmacological effects of these drugs.
The incidence of adverse reactions is expressed as follows: very rare (1 / 10); common (1 / 100 to <1/10); occasional (1 / 1000 to <1/100); rare (1) / 10000 to <1/1000); very rare (<1/10000); unknown (cannot be evaluated based on known data). Within each incidence group, adverse reactions were ranked in descending order of severity.

Ramipril taboo

Ramipril tablets cannot be given in the following cases:
-People who are allergic to ramipril, other ACE inhibitors or any other component of ramipril tablets-Patients with a history of angioedema (such as those with angiotensinemia previously treated with an ACE inhibitor).
-Renal artery stenosis (bilateral or unilateral in patients with single kidney).
-After kidney transplantation-hemodynamically related aortic or mitral stenosis, or hypertrophic cardiomyopathy.
-Primary aldosteronism.
-Pregnancy (the possibility of pregnancy must be ruled out and contraceptive measures taken before starting treatment)
-Breastfeeding (requires weaning)
When Ramipril is used for mild to moderate heart failure after acute myocardial infarction, the following additional contraindications are available:
-Persistent hypotension (systolic blood pressure below 90mmHg)
-Orthostatic hypotension (systolic blood pressure reduced by 20mmHg after 1 minute of sitting)
-Severe Heart Failure (NYHA IV)
-Unstable angina pectoris-Fatal ventricular arrhythmias-Pulmonary heart disease Due to lack of treatment experience, ramipril tablets cannot be used in the following situations:
-Nephropathy being treated with steroidal, non-steroidal anti-inflammatory drugs, immunomodulators and / or cytotoxic compounds-dialysis-primary liver disease or impairment of liver function-untreated, decompensated heart failure- Children may have severe allergic reactions (such as life-threatening shock), so this product or other ACE inhibitors should be avoided at the same time as in vitro treatment that requires negative blood contact.
When using this product, do not use polyacrylonitrile or methallyl sodium sulfide high-throughput filter membranes (such as AN69) for dialysis or hemofiltration, nor use dextran sulfate for LDL (low density lipoprotein) separation. Clear.
If dialysis, hemofiltration or LDL separation is necessary, treatment must be replaced with a non-ACE inhibitor or another dialysis membrane (see "Precautions").
Desensitization of insect toxins (such as bees or wasps) while taking ACE inhibitors may trigger allergic-like reactions (such as decreased blood pressure, shortness of breath, vomiting, skin allergic reactions), and may sometimes be life threatening. Allergic reactions can also occur after insect bites (such as bee or wasp bites).
If insect toxin desensitization treatment is necessary, ACE inhibitors must be temporarily replaced with other types of suitable drugs (see "Precautions").

Precautions for ramipril tablets

1. Ramipril can be used only when the benefits clearly outweigh the risks and regular monitoring of representative clinical and laboratory indicators:
-Clinically relevant electrolyte disorders-immune response disorders or connective tissue disorders (such as lupus erythematosus, scleroderma)
-Simultaneous systemic use of drugs that suppress the immune response (such as corticosteroids, cytostatics, antimetabolites), allopurinol, procainamide or lithium.
2. In patients with higher renin-angiotensin system activity, there is a risk of sudden and significant drop in blood pressure and impaired renal function due to inhibition of ACE. In this case, if using ramipril for the first time or increasing the dose, blood pressure should be closely monitored until no further acute blood pressure drop is expected.
Higher renin-angiotensin activity is expected in the following situations:
-Patients already taking diuretics-Patients with salt and / or fluid loss-Patients with severe hypertension-Patients with heart failure, especially after acute myocardial infarction-Patients with obstruction of left ventricular inflow and outflow tract (such as aortic constriction or Cuspid stenosis, hypertrophic cardiomyopathy)
-Patients with hemodynamic-related renal artery stenosis (the diuretic may need to be discontinued)
3 The following patients should also be monitored particularly carefully at the beginning of treatment:
-Elderly patients (over 65 years of age)
-Patients at risk of a significant drop in blood pressure (eg, patients with coronary or cerebral stenosis)
4 Renal function must be checked before taking this product. Monitoring of renal function is recommended especially in the first few weeks of treatment.
Monitoring is particularly suitable for:
-Patients with heart failure-Patients with unilateral renal artery stenosis (in this case, a slight increase in serum inosine may mean failure of the affected kidney)
-Patients with impaired renal function. Patients with impaired renal function need to monitor the serum potassium concentration frequently. When taking this product, there is a danger of severe allergic reactions (such as life-threatening reactions) when in vitro treatment that requires negative electrical contact with blood (such as dialysis using a specific dialysis membrane, hemofiltration, or LDL separation and removal using dextran sulfate) Shock). This danger is also present with insect toxin desensitization treatments.
6. Use polyacrylonitrile or methallyl sodium sulfide high-throughput membranes (such as AN69) for dialysis or hemofiltration, use dextran sulfate for LDL (low density lipoprotein) separation and removal, or use insect toxin desensitization treatment Do not use this product for treatment (see "Contraindications").
7. If angioedema occurs during treatment, the drug must be discontinued immediately. Angioedema triggered by an ACE inhibitor may affect the throat, pharynx, and / or tongue (see "Adverse Reactions").
8. Impact on driving and operating mechanical ability / response. Treatment with this medicine requires regular medical examination. Due to differences in individual responses, some patients' responses may change significantly, so that their ability to drive, operate machines, or work without armrests or safety fulcrum is impaired, at the beginning of medication, when increasing doses, or when changing dosage forms or while drinking alcohol. This is especially true.
9. Keep medicines out of the reach of children.

Ramipril tablets for pregnant and lactating women

Taking this product during pregnancy, especially in the last 6 months of pregnancy, may cause fetal damage and even death, so pregnant women are prohibited from using this product. This product can be secreted through milk, so lactating women should not use this product.

Ramipril tablets for children

This product has not been studied in children, so this product is contraindicated in children.

Ramipril tablets for elderly

Elderly patients with congestive heart failure or liver and kidney dysfunction when using diuretics at the same time should be used with caution. When using this product, the dosage should be carefully adjusted according to the needs of blood pressure control.

Ramipril tablets drug interactions

Ramipril tablets or other ACE inhibitors in combination with the following drugs can have the following effects:
-Potassium salts, potassium-sparing diuretics (such as spironolactone, amiloride, amphitrazine): serum potassium concentrations have increased significantly (seropotassium concentrations must be closely monitored when used with these drugs).
-Antihypertensive drugs (especially diuretics) and other drugs with potential antihypertensive effects (such as nitrates, tricyclic antidepressants): the antihypertensive effect of ramipril is enhanced (during the concurrent use of diuretics, (Recommended periodic testing of serum sodium concentration)
-Hypnotics, sedatives, anesthetics: markedly decreased blood pressure (the anesthesiologist should be informed of the use of ramipril before surgery)
-Sympathomimetic vasopressors (such as epinephrine): may reduce the antihypertensive effect of ramipril (recommended close monitoring of blood pressure)
-Allopurinol, procainamide, cytostatics, immunosuppressants, systemic cortisols and other drugs that cause blood changes: increase the possibility of hematological reactions, especially decreased white blood cell counts, Leukopenia-Lithium: Increased serum lithium concentration, which increases the cardiac and neurotoxicity of lithium (requires regular monitoring of serum lithium concentration).
-Oral anti-glycemic drugs (such as sulfonylureas, biguanides), insulin: Due to the potential to reduce insulin resistance, this product can enhance the effect of hypoglycemic drugs, with the risk of hypoglycemia (especially in the early stages of treatment, blood glucose levels should be carefully monitored )
-Non-steroidal anti-inflammatory drugs, analgesics (such as indomethacin, acetylsalicylic acid): may reduce the antihypertensive effect of ramipril; it may also increase the risk of impaired renal function and elevated serum potassium concentrations.
-Heparin: May increase serum potassium concentration-Sodium chloride: Attenuate the antihypertensive effect of ramipril and relieve the symptoms of heart failure.
-Ethanol: Enhances blood pressure drop and effects of ethanol

Ramipril overdose

Symptoms of overdose vary depending on the degree of overdose, and the following symptoms may occur: severe hypotension, bradycardia, circulatory shock, electrolyte disturbances, and renal failure.
The treatment of overdose depends on the nature and timing of drug intake, and the type and severity of symptoms.
In addition to routine measures to remove ramipril (such as gastric lavage, taking absorbent and sodium sulfate within 30 minutes of taking ramipril tablets), vital parameters must be monitored and corrected under intensive care. Ramipril can hardly be removed by dialysis.
In the case of hypotension, sodium chloride and volume load are given first, and if there is no response, catecholamines should also be given intravenously. Consider angiotensin II treatment. If stubborn bradycardia occurs, pacing treatment should be performed.
The concentration of electrolytes and serum creatinine must be constantly monitored.

Ramipril tablets pharmacology and toxicology

Ramipril is a prodrug that is absorbed by the gastrointestinal tract and hydrolyzed in the liver to produce ramipril, an active, potent and long-acting angiotensin converting enzyme (ACE) inhibitor. Taking ramipril will lead to an increase in plasma renin activity and a decrease in angiotensin II and aldosterone plasma concentrations. Because of the reduction of angiotensin II, ACE inhibitors can cause peripheral vasodilation and decrease in vascular resistance, which can have beneficial hemodynamic effects. Evidence suggests that tissue ACE, especially the vascular system-not circulating ACE, is a major factor in determining hemodynamic effects.
Like kallikrein II, angiotensin converting enzyme can also degrade bradykinin. There is evidence that ACE inhibition caused by ramiprilra has certain effects on the kallikrein-kinin-prostaglandin system. Some speculate that this mechanism is involved in the antihypertensive and metabolic effects of ramipril.
Hypertensive patients' blood pressure in both supine and standing positions decreased after taking ramipril. A significant antihypertensive effect occurs within 1-2 hours after taking the drug; the peak effect appears 3-6 hours after taking the drug; it has been shown that the antihypertensive effect of the therapeutic dose can be maintained for at least 24 hours.
In a large sample endpoint study (HOPE), compared with placebo, ramipril significantly reduced the incidence of stroke, myocardial infarction and / or cardiovascular disease deaths. Studies have confirmed that most of these beneficial effects occur in patients with normal blood pressure, and that using standard regression analysis techniques has shown that only some of the beneficial effects are due to relatively small blood pressure drops. The 10 mg dose is the maximum safe dose currently approved, and this dose is considered to be the most likely dose to completely block the effects of the renin-angiotensin-aldosterone system, as has been done in previous dose-range studies (SECURE , HEART), and researchers in the HOPE trial also used this dose. This study and other studies together suggest that ACE inhibitors such as ramipril may have other direct effects on the cardiovascular system. These effects may include antagonizing angiotensin II-mediated vasoconstriction effects, inhibiting vascular smooth muscle proliferation and plaque Block rupture, enhance vascular endothelial function, reduce left ventricular hypertrophy and promote fibrinolysis. There may be other effects in diabetic patients, such as effects on insulin clearance and pancreatic blood flow.
Reproductive toxicology studies in rats, rabbits and monkeys have found no teratogenic effects. No damage to reproductive capacity was found in either male or female rats. Female rats during pregnancy and lactation, given daily doses of 50 mg / kg or more ramipril, will cause irreversible kidney damage (expanding of the renal pelvis) in offspring.

Pharmacokinetics of ramipril tablets

Ramipril can be quickly absorbed from the gastrointestinal tract after oral administration, and peak plasma concentrations can be reached within 1 hour. The peak plasma concentration of its active metabolite, ramipril, appeared within 2-4 hours after administration.
The peak plasma concentration of ramiprilat decreased in a heterogeneous manner. If Ramipril 5-10 mg is administered once a day, the effective half-life of Ramiprilat is 13-17 hours after a few days; it is administered at a lower dose (Ramipril 1.25-2.5 mg) The effective half-life was significantly prolonged. This difference is related to the long terminal phase of the concentration-time curve of ramiprilat observed at very low plasma concentrations. This terminal phase is independent of the dose of the drug, suggesting that the effect of the enzyme that binds to ramipril is saturable. The usual dose of ramipril, once a day, can reach the steady state plasma concentration of ramipril after about 4 days.
Ramipril is almost completely metabolized, and its metabolites are mainly excreted from the kidneys (about 60% are excreted in urine and 40% are excreted in feces). In addition to its active metabolite, ramipril, other inactive metabolites include diketopiperazine esters, diketopiperazine acids, and their conjugates.

Ramipril tablets storage

Store below 30 ° C. Keep medicines out of the reach of children.

Ramipril Tablet Packaging

Aluminum plastic packaging, 7 pieces / box.

The expiration date of ramipril tablets

60 months

Ramipril film implementation standards

YBH11652006 ^[1]