Linipril
Linipril Uses, Dosage, Side Effects, Food Interaction and all others data.
Linipril competitively inhibits ACE from converting angiotensin I to angiotensin II (a potent vasoconstrictor) resulting in increased plasma renin activity and reduced aldosterone (a hormone that causes water and Na retention) secretion. This promotes vasodilation and BP reduction.
Linipril is an angiotensin converting enzyme inhibitor used to treat hypertension, heart failure, and myocardial infarction. Linipril is not a prodrug, and functions by inhibition of angiotensin converting enzyme as well as the renin angiotensin aldosterone system. It has a wide therapeutic index and a long duration of action as patients are generally given 10-80mg daily.
Trade Name | Linipril |
Availability | Prescription only |
Generic | Lisinopril |
Lisinopril Other Names | Lisinopril, Lisinoprilum |
Related Drugs | amlodipine, aspirin, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, clopidogrel, spironolactone |
Type | |
Formula | C21H31N3O5 |
Weight | Average: 405.4879 Monoisotopic: 405.226371117 |
Protein binding | Lisinopril has not been demonstrated to bind to serum proteins. |
Groups | Approved, Investigational |
Therapeutic Class | Angiotensin-converting enzyme (ACE) inhibitors |
Manufacturer | |
Available Country | Bulgaria |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Hypertension: Linipril is used for the treatment of hypertension in adult patients and pediatric patients 6 years of age and older to lower blood pressure. Lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes.
Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than 1 drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).
Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.
Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.
Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease).
These considerations may guide selection of therapy.Linipril may be administered alone or with other antihypertensive agents.
Heart Failure: Linipril is used to reduce signs and symptoms of heart failure in patients who are not responding adequately to diuretics and digitalis.
Acute Myocardial Infarction: Linipril is used for the reduction of mortality in treatment of hemodynamically stable patients within 24 hours of acute myocardial infarction. Patients should receive, as appropriate, the standard recommended treatments such as thrombolytics, aspirin and beta-blockers
Linipril is also used to associated treatment for these conditions: Acute Myocardial Infarction (AMI), Cardiovascular Events, Congestive Heart Failure (CHF), Diabetic Nephropathy, High Blood Pressure (Hypertension), Migraine
How Linipril works
Angiotensin II constricts coronary blood vessels and is positively inotropic, which under normal circumstances, would increase vascular resistance and oxygen consumption. This action can eventually lead to myocyte hypertrophy and vascular smooth muscle cell proliferation.
Linipril is an angiotensin converting enzyme inhibitor (ACEI), preventing the conversion of angiotensin I to angiotensin II. This action prevents myocyte hypertrophy and vascular smooth muscle cell proliferation seen in untreated patients. Increased levels of bradykinin also exhibit vasodilating effects for patients taking ACEIs. Linipril also inhibits renin's conversion of angiotensin to angiotensin I.
Dosage
Linipril dosage
Oral (Adult)-
Hypertension:
Initially, 10 mg/day, 1st dose given preferably at bedtime to avoid precipitous fall in BP. Patient with renovascular HTN, volume depletion, severe HTN: Initially, 2.5-5 mg once daily. Patient on diuretic: Initially, 5 mg once daily. Maintenance: 20 mg once daily, up to 80 mg/day may be given if needed.
Diabetic nephropathy: Hypertensive type 2 diabetics with microalbuminuria: 10 mg once daily, may increase to 20 mg once daily to achieve a sitting diastolic BP
Heart failure: As adjunct: Initially, 2.5 or 5 mg/day, increased by increments of ≤10 mg at intervals of at least 2 wk to max maintenance dose of 40 mg/day.
Post-myocardial infarction: Initially, 5 mg once daily for 2 days started within 24 hr of the onset of symptoms. Increase to 10 mg once daily. Patients with low systolic BP: Initially, 2.5 mg once daily.
Oral (Child)-
Hypertension: ≥6 yr Initially, 0.07 mg/kg, up to 5 mg once daily.
Side Effects
Headache, fatigue, persistent and non-productive cough, chest and abdominal pain, dizziness, nausea, vomiting, diarrhoea, upper resp tract infection, asthenia, rash, orthostatic effects, hypotension, renal dysfunction, hyperkalaemia, intestinal angioedema; increased BUN and serum creatinine levels.
Toxicity
The oral and subcutaneous LD50 in rats is >8500mg/kg and in mice is >9100mg/kg. The oral LDLO in women is 1200µg/kg/16D and in men is 43mg/kg/43W.
Patients experiencing an overdose of lisinopril may present with hypotension. Patients should be treated with intravenous saline to restore blood pressure. Linipril can be removed from the blood by hemodialysis due to it not being protein bound.
Precaution
Bilateral renal artery stenosis or a single kidney with unilateral renal artery stenosis. Patients with collagen vascular disease, acute MI at risk of further haemodynamic deterioration, angioedema unrelated to ACE inhibitor therapy, aortic stenosis and hypertrophic cardiomyopathy. Increased risk of angioedema in black patients. Renal impairment. Lactation. Childn <6 yr.
Interaction
May enhance hypotensive effect with diuretics. May increase risk of renal function deterioration and decrease antihypertensive effect with NSAIDs. May increase serum levels and toxicity of lithium. Increased risk of hyperkalaemia with K-sparing diuretics and K supplements. May increase nitritoid reactions of gold Na thiomalate.
Food Interaction
- Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
- Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
- Limit salt intake. Salt may attenuate the antihypertensive effect.
- Take with or without food. The absorption is unaffected by food.
[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium can cause hyperkalemia in some patients who are using angiotensin converting enzyme (ACE) inhibitors.
In some cases, affected patients were using a potassium-rich salt substitute.
ACE inhibitors can promote hyperkalemia through inhibition of the renin-aldosterone-angiotensin (RAA) system.
MANAGEMENT: It is recommended that patients who are taking ACE inhibitors be advised to avoid moderately high or high potassium dietary intake.
Particular attention should be paid to the potassium content of salt substitutes.
Linipril Drug Interaction
Moderate: aspirin, aspirin, insulin glargine, furosemide, pregabalin, acetaminophen / hydrocodone, alprazolamUnknown: rosuvastatin, duloxetine, omega-3 polyunsaturated fatty acids, atorvastatin, metoprolol, metoprolol, clopidogrel, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Linipril Disease Interaction
Major: angioedema, bone marrow suppression, CHF, hemodialysis, hyperkalemia, hypotensionModerate: liver disease, renal dysfunction
Volume of Distribution
The apparent volume of distribution of lisinopril is 124L.
Elimination Route
Linipril is 6-60% orally bioavailable with an average of 25% bioavailability. Linipril reaches a Cmax of 58ng/mL with a Tmax of 6-8h. Linipril's absorption is not affected by food.
Half Life
Linipril has an effective half life of accumulation of 12.6h and a terminal half life of 46.7h.
Clearance
A 30kg child has a typical clearance of 10L/h, which increases with renal function. The mean renal clearance of lisinopril in healthy adult males is 121mL/min.
Elimination Route
Linipril is entirely eliminated exclusively in the urine.
Pregnancy & Breastfeeding use
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
History of angioedema related to previous ACE inhibitor treatment, hereditary or idiopathic angioedema. Concomitant use with aliskiren in patients with diabetes or renal impairment. Pregnancy. Children with GFR <30 mL/min/1.73 m2.
Special Warning
Adult:
- CrCl 10-30 ml/min: Initially, 2.5-5 mg once daily.
- CrCl 31-80 ml/min: Initially 5-10 mg once daily. Dose can be adjusted up to max 40 mg once daily based on patient's response.
Child: Do not give if GFR <30 mL/min/1.73 m2.
Acute Overdose
Symptoms: Hypotension, tachycardia, circulatory shock, palpitations, bradycardia, hyperventilation, renal failure, electrolyte disturbances, anxiety, dizziness and cough.
Management: Normal saline IV infusion may be used. Perform haemodialysis, emesis, gastric lavage, admin of absorbents and Na sulfate if recently taken. Consider admin of angiotensin II infusion and/or IV catecholamines if available.
Storage Condition
Store at below 25° C.
Innovators Monograph
You find simplified version here Linipril
Linipril contains Lisinopril see full prescribing information from innovator Linipril Monograph, Linipril MSDS, Linipril FDA label
FAQ
What is Linipril?
Linipril is a medication of the angiotensin-converting enzyme inhibitor class used to treat high blood pressure and heart failure and after heart attacks. For high blood pressure it is usually a first line treatment. It is also used to prevent kidney problems in people with diabetes mellitus.
What is the side effect of Linipril?
Common side effects of Linipril are: feeling dizzy or lightheaded, especially when you stand up or sit up quickly - this is more likely to happen when you start taking lisinopril or move on to a higher dose. headaches. diarrhoea or being sick (vomiting) itching or a mild skin rash.
Why should not take Linipril?
Taking certain blood pressure drugs with Linipril increases your risk for low blood pressure, high blood potassium, and kidney problems including kidney failure.
Is Linipril a good blood pressure medicine?
Linipril is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. It is also used to treat heart failure and to improve survival after a heart attack. Linipril belongs to a class of drugs known as ACE inhibitors.
What should I avoid while taking Linipril?
Linipril food interactions consist of foods high in potassium. Linipril can increase blood potassium levels. So, using salt substitutes or eating high-potassium foods may cause problems. Foods to avoid in excess include bananas, oranges, potatoes, tomatoes, squash, and dark leafy greens.
Should I drink more water when taking Linipril?
Drink plenty of water each day while you are taking Linipril.
Can Linipril cause bowel problems?
Linipril, a medication widely used to treat high blood pressure and other cardiovascular disorders, sometimes may trigger small bowel angioedema, suggests a case report.
Is Linipril bad for kidneys?
Taking certain blood pressure drugs with Linipril increases your risk for low blood pressure, high blood potassium, and kidney problems including kidney failure.
Does Linipril cause anxiety?
Linipril can cause nausea, headaches, anxiety, insomnia, drowsiness, nasal congestion and sexual dysfunction. Linipril should be stopped if there are symptoms or signs of an allergic reaction including feelings of swelling of the face, lips, tongue or throat.
How many hours does Linipril last?
The elimination half-life of Linipril is only 12 hours, but lisinopril has been shown to have some BP-lowering effects after 24 hours.
What vitamins affect Linipril?
It is recommended that if you are taking Linipril you should be advised to avoid moderately high or high potassium dietary intake. This can cause high levels of potassium in your blood. Do not use salt substitutes or potassium supplements while taking Linipril, unless your doctor has told you to.
Can I drink beer while taking Linipril?
It's not advised that you mix alcohol and Linipril for any reason because of the effects alcohol can have on your blood pressure, including making it drop too low or go too high. There is also the risk of increased dizziness and a risk of fainting when you mix alcohol and Linipril.
Why does Linipril cause a cough?
ACE inhibitors cause the body to increase nitric oxide production, and nitric oxide is known to irritate the lungs and possibly cause coughing.
How do I get off Linipril?
If a doctor recommends to stop taking Linipril, they may use a combination of reducing the dosage over a period of a few weeks or utilizing an ACE inhibitor substitute. The doctor can then discuss a withdrawal plan with the patient, where they Find the best treatment options.
Can I stop taking Linipril suddenly?
You should not stop taking the Linipril suddenly without your doctors permission - you could risk experiencing rebound hypertension, which is a sudden increase in blood pressure in response to stopping or reducing hypertension medications.
What herbs should not be taken with Linipril?
Herbs that have a diuretic effect should be avoided when taking diuretic medications, as they may increase the effect of these drugs and lead to possible cardiovascular side effects. These herbs include dandelion, uva ursi, juniper, buchu, cleavers, horsetail, and gravel root.
How long does Linipril stay in my body?
Linipril takes around 12 hours from the time you take lisinopril for half of the drug to be out of your blood.
Is Linipril safe during pregnancy?
Linipril can cause problems for a baby when it is taken during the second and third trimester of pregnancy. For this reason, it is recommended that a person who is pregnant should stop taking Linipril once a pregnancy is detected, but you should not stop Linipril without talking to your healthcare provider first.
Is Linipril safe during breastfeeding?
There are no studies looking at Linipril while breastfeeding. There are other high blood pressure medications that have been better studied for use while breastfeeding. Be sure to talk to your healthcare provider about all of your breastfeeding questions.