Benicar vs Lisinopril

October 25, 2015 at 12:55 PM

Benicar HCT (olmesartan medoxomil-hydrochlorothiazide) vs Lisinopril: comparison of drugs used for treatment of high pressure. The post compares medical uses, benefits, side effects and mechanism of action of both drugs. The drugs act in a different way as Benicar is a sartan group medicine while Lisinopril belongs to ACE inhibitor group of drugs.

Contents

  1. Benicar HCT
  2. Medical uses

Benicar HCT

The scientific name for Benicar HCT is Olmesartan Medoxomil-Hydrochlorothiazide. It is a combination of a sartan and a diuretic and it is a drug used for the treatment of high blood pressure.

Some other uses of this drug include its action against diabetes insipidus, renal tubular acidosis and to decrease the risk of kidney stones in people with high calcium levels in the urine. This drug is recommended as a good treatment against high blood pressure. Benicar HCT is usually taken through the oral route and should be combined with other blood pressure medications in order to increase its effectiveness.

There are some prominent side effects of this drug which include the imbalance of electrolytes, poor kidney function, high blood sugar, gout, low blood sodium, and feeling dizziness and fainting when standing up. There is also some research done which indicates that allergies are caused due to the intake of this drug. Benicar can be used during pregnancy but it shouldn’t be your first preference.

Benicar belongs to the thiazide medication family and normally functions by decreasing the ability of the kidney to retain water. First the blood volume is reduced which decreases the blood return to the heart which in turn decreases the cardiac output. But resistance develops due to the long term usage of this drug.

There is some controversy as to who are the real manufacturers of this drug. Merck and Ciba are the two companies which claimed that they made this drug. This drug became available for commercial use in 1959. This drug belongs to the World Health organization’s list of Essential Medicine as one of the most important drug needed in the healthcare system. This drug was the second most commonly used blood pressure medication in the United States in 2008. The good thing about this drug is that it isn’t that much expensive and is available for common use.

Medical uses

Benicar HCT is either given alone or prescribed with other drugs for the treatment of high blood pressure in adults or children greater than the age of 6 years (1).

High blood pressure is quite a serious condition and can cause many health related problems like damage to blood vessels, brain, kidneys and other body parts. The organs damage can cause heart attacks, heart disease, heart stroke, loss of vision, kidney failure and different other problems. You should remember one thing here and it is that this drug does have positive effects on blood pressure but it is more effective when positive life style changes are made like maintaining healthy weight, not smoking, eating a low fat diet, minimizing the intake of oil and using alcohol in moderate quantity.

Benicar controls high blood pressure but doesn’t completely cure it. You will see a change in your blood pressure in the first weeks but it will take two weeks to see some real benefits of this drug. You should continue taking Benicar even if you feel well.

Following are some other uses for this drug:

  • Benciar is also used for the treatment of heart failure which is a condition in which the heart fails to pump blood throughout the body.
  • Diabetic nephropathy can also be treated through this drug. Diabetic nephropathy is a kidney disease in people with high blood pressure and diabetes.
  • This drug is also used to prevent strokes.

Dosage and intake methods

The exact dosage of this drug depends on the individual needs. The starting recommended dosage is 20 mg once daily in patients who aren’t volume-contracted. The dose should be increased to about 40 mg in patients who need a reduction in their blood pressure after two weeks. There is no more effect on giving a dosage more than 40 mg. Taking the dosage twice a day will have the same effect as taking the same dose once a day.

There is no initial dosage adjustment in elderly patients. The dose can vary according to the individual needs. Patients with the depletion of intravascular volume should be kept under controlled medical supervision and should be given low starting dose.

Some other things which you should keep in mind while taking this medicine are mentioned below:

  • Benicar can be taken with or without food.
  • You should add a diuretic if blood pressure isn’t controlled with Benicar alone.
  • You should take Benicar about four hours before or after taking other drugs for lowering cholesterol like colesevelam, colestipol and cholestyramine.
  • You should take this drug regularly to get the most benefits. You should take the drug at the same time every day so that you won’t forget taking it. Remember to continue this medication even if you feel back to normal. Leave this drug only on the instructions of the doctor.
  • Inform your doctor as soon as you feel that you condition has worsened due to the drug.

Intake methods

There are two methods of taking this drug. It can either in tablet form or in liquid form. These methods have been discussed below:

Tablet form

Benicar comes in the form of 20 mg and 40 mg tablets. You should take the tablet exactly as directed by the doctor with water. It’s your choice to take it with meals or not. The dosage depends on your condition and your medical treatment.

Liquid form

This drug is also available in the form of syrup in the market. You should shake the bottle well before each dose. Measure the dosage strength by a measuring device or spoon. Using a household spoon isn’t recommended because you won’t get the correct dose that way.

Mechanism of action of benicar

Angiotensin II is made from angiotensin I which is a reaction catalyzed by an enzyme known as angiotensin converting enzyme or ACE. The principle presser agent of the renin-angiotensin system is Angiotensin II, which has effects thatinclude the stimulation and release of aldosterone, cardiac stimulation, renal absorption of sodium and vasoconstriction. The vasoconstriction effect of angiotensin are restricted and blocked by the binding of angiotensin II to the ATP1 receptor in the smooth muscles. Therefore, the pathways for the synthesis of angiotensin II receptors are quite independent.

AT2 receptors are present in many muscle tissues but they aren’t associated with cardiovascular homeostasis. This drug has more than 12,500 folds greater affinity for the AT1 receptors than the AT2 receptors.

In a nutshell, Benicar functions by blocking the binding on angiotensin to its receptors, which then blocks the action of angiotensin as well. It doesn’t directly block angiotensin converting enzyme, like other ACE inhibitors do. Instead, it blocks the site of action of angiotensin.

Mechanisms after intake – pharmacokinetics


The following steps take place after the intake of Benicar.

1. Absorption

Benicar is completely hydrolyzed by ester hydrolysis during the absorption in gastrointestinal tract. Benicar is eliminated in a biphasic manner with the terminal elimination half-life up to 13 hours. Linear pharmacokinetics are shown by different doses of Benicar including a single oral dose of 320 mg or multiple doses of 80 mg. The steady state of Benicar is reached within 3 to 5 days and no accumulation in the plasma occurs.

The bioavailability of Benicar is about 26%. The peak concentration of plasma is reached 1 to 2 hours after oral administration. The bioavailability of Benicar isn’t affected by the food you eat.

2. Distribution

Benicar is distributed in the body in the volume of about 17L. Benicar is bound tightly to the plasma proteins and doesn’t go through the red blood cells. The binding of protein remains constant when the Benicar concentration is higher than the recommended doses.

3. Metabolism and excretion

No metabolism occurs in Benicar after the complete conversion of Benicar medoxomil to Benicar during absorption. The clearance of Benicar is about 1.3 L/h and the renal clearance is about 0.6 L/h. 35 to 50 percent of the dose is recovered in the urine while the remainder is eliminated through the body in the form of feces.

Overdosage

The Benicar medication effects the blood pressure, so it is quite rare that a person overdoses on it. The effects of Benicar Overdosage varies and depends upon a number of factors which include how the dose is taken and whether the drug is taken with other medicines, drugs, or alcohol.

Some major symptoms of Benicar overdosage are:

  • Extremely low blood pressure
  • Increased potassium in blood
  • Kidney failure
  • Increased heart rate
  • Decrease in urine
  • Loss of consciousness
  • Dizziness or lightheadedness
  • Headache and drowsiness

There are a number of treatments of Benicar overdose. Your healthcare provider might give certain supplements or medicines which pump the stomach, in case the Overdosage happened recently. There is no treatment at present to remove Benicar from the body once a person has overdosed on it. So supportive care is needed in most of the cases. The main essence of this supportive care is to treat the symptoms which occur as a result of Overdosage. Some supportive care steps include:

  • Medicines to increase blood pressure
  • Treatment based on the complications
  • Fluids through intravenous line
  • Monitoring the heart and lungs closely

You should seek medical care as soon as you come to know that you have overdosed on Benicar.

Benicar side effects

Benicar has some major and severe side effects. The FDA gave a health safety alert for Benicar after viewing a data given by Mayo Clinic in 2012. Many Benicar users had reported that they suffered severe diarrhea and weight loss as a result of Benicar intake. Some people also suffered intestinal damage. The FDA clearly found in their evaluation that there is a relation between the intake of Benicar and developing spure-like enteropathy. The researchers from FDA were of the view that if a patient suffers from these side effects then he should discontinue this medicine. The researchers also reviewed this medication as a life-threatening drug.

Benicar also damages the walls of the intestine. This condition is known as villous atrophy and makes the villi in the intestinal walls to burst. This prevents the absorbing of food and makes the patient malnourished.

A study was published in the American Journal of Gastroenterology in May 2013 in which the researchers found that the patients who had Celiac disease suffered from Benicar-related atrophy. The patients who discontinued Benicar lost weight and had lesser symptoms.

A major side effect of this drug is that it can result in dizziness and light headedness. You should inform the doctor if any of these side effects occur to you. You should change your sitting position from sitting to lying to lessen this side effect.

You should also inform the doctor if you have certain side effects like faintness, slow and irregular heartbeat, symptoms of high potassium levels in the blood, persistent diarrhea, decrease in urine amount and high potassium blood level.

A recent research showed that higher death rates occur due to the intake of Benicar in people suffering from cardiovascular issues (2).

Sometimes allergic reactions are caused due to this drug. You should get medical help if you see any symptom of a serious allergic reaction like rashes, dizziness, itching, swelling and trouble breathing.

Moderate side effects

Some less severe side effects of Benicar intake have been mentioned below:

  • Flu-like symptoms
  • Head pain
  • Backache
  • High blood sugar
  • Throat irritation
  • Inflammation in nose
  • Hair loss
  • Indigestion
  • Muscle pain
  • Joint pain
  • Stomach cramps
  • Throwing up
  • Itching

You should immediately inform the doctor if you suffer from any of these side effects. You can also report to the doctor for medical advice. People living in the US should report their side effects to FDA at 1-800-FDA-1088. People living in Canada can also report their side effects to Health center Canada at 1-866-234-2345.

Decreased efficiency causes

The following things decrease the efficiency of Benicar:

  • The efficiency of Benicar is reduced when it interacts with other drugs. It is known that about 438 different drugs can interact with Benicar. Some common medications which need to be checked in combination with Benicar are amlodipine, metoprolol, metformin, simvastatin, gabapentin, fish oil, tramadol, vitamin D3 and many others.
  • Pregnant women should avoid taking Benicar because it can interact with other medications and reduce the overall efficiency of Benicar. Serious injuries can result if pregnant women take Benicar.

Lisinopril

Lisinopril belongs to the angiotensin-converting enzyme (ACE) inhibitor class of drugs and is commonly used in the treatment of high blood pressure, heart attacks and for the prevention of renal and retinal complication of diabetes. The indications, side effects and contraindications of this drug are the same as those for ACE inhibitors.

Lisinopril was the third ACE inhibitor made after captopril and enalapril and was introduced in therapy in the start of 1990s (3). There are a number of features which distinguish it from ACE inhibitors. This drug is hydrophilic, has a long life and isn’t metabolized by the liver.

Medical applications

Lisinopril is used in combination with other medications for the treatment of high blood pressure. It is also used with other medicines to treat heart failure. This drug improves the survival after heart attack. This drug belongs to the class of angiotensin converting enzyme (ACE) inhibitors. It decreases the level of angiotensin in the blood which tightens the blood vessels. This makes the blood flow more smoothly and the blood can easily be pumped throughout the body.

High blood pressure is a common condition which can cause severe medical problems when not treated. It can cause heart diseases, kidney failure, loss of vision, stroke and other problems. You should also make some lifestyle changes while taking this medicine. These include eating a low caloric diet, maintaining healthy weight, walking each morning and limiting the use of cigarette and alcohol.

Lisinopril is also beneficial for proper kidney functioning. It isn’t yet known how Lisinopril protects the kidneys. Some experts believe that the protective benefits of ACE inhibitors like Lisinopril are due to their ability to decrease the urine protein content. Reducing urine protein is quite important because the kidney patients usually have high urine content in their bodies. The kidneys prevent the proteins to go into urine. But this doesn’t happen in kidney patients. The glomeruli can be damaged when the proteins pass through them. Lisinopril lowers the urine protein and prolongs the kidney function.

Some studies have also shown that Lisinopril improves the functioning of heart muscles (4). The researchers observed improvement in the heart muscles of hypertensive patients who were treated with Lisinopril. The researchers have said that several ACE inhibitors are known to prevent heart failure.

Dosage and intake methods

Lisinopril comes in different dosage and strengths. The following are the main dosage and strengths of Lisinopril tablets:

  • 2.5 mg which are oval, white, biconvex, uncoated tablets, with “E25” written on one side and blank on the other
  • 5 mg which are pink, biconvex, uncoated tablets with “E54” written on one side and bisected on the other side
  • 10 mg tablets which are pink, oval, biconvex, uncoated tablets with “E101” written on one side and plain on the other side
  • 20 mg tablets which are peach, biconvex, oval, uncoated tablets with “E102” written on one side and plain on the other side
  • 30 mg which are red, biconvex, oval, uncoated tablets with “E103” written on one side and plain on the other side

The exact dosage for Lisinopril patients has been mentioned below:

  • The initial dosage for hypertension patients should be 10mg tablet taken orally. The patient should intake 20 to 40mg tablets for maintenance.
  • The initial dosage for patients with congestive heart failure is 5 mg tablet to be taken orally once a day. The maintenance dosage is from 5 to 20mg.
  • The initial dosage for patients with diabetes is 10 to 20 mg. The maintenance dosage is from 20 to 40 mg daily.
  • The initial dosage for myocardial infections is 5 mg to be taken orally. The maintenance dosage is 10 mg tablet to be taken once a day.

Intake methods

Following are the intake methods of Lisinopril:

  • Lisinopril is available in the market in the suspension form. You should shake the bottle well after each dose=. Carefully measure the dosage strength with a measuring spoon or cup. You shouldn’t use a household spoon because you won’t get the correct measurement that way.
  • Lisinopril is also available in the form of tablets of different strengths. You should always take the tablet with water. It’s your choice to take the tablet with or without food.

You should take the drug on regular basis in order to get the most health benefits. You should take it the same time every day. You should keep on taking this medicine even after you feel well. Patients with high blood pressure will start seeing the full effects of medication after two to four weeks. Heart patients will have to wait for weeks to months to see the full benefits of the drug.

Precautions

The following precautions should be noted before taking Lisinopril:

  • Lisinopril is popular for causing allergic reactions. There have been reports that people have suffered allergic reactions when taking Lisinopril during dialysis. You should seek help if you notice hives or unexplained rashes.
  • ACE inhibitors can cause swelling to the tongue and head. They can also cause swelling in the eyes, throats and lips. You should immediately seek help if you notice these side effects.
  • Lisinopril can also cause swelling in the intestines. This is called intestinal angioedema. The main symptoms are abdominal pain and vomiting. You should immediately seek help in such a situation.
  • You shouldn’t drive, operate heavy machinery or do other tasks which need focus.
  • People taking Lisinopril become prone to infections. You should immediately inform the doctor if you notice any infection like throat infection or fever.

Mechanism of action

The renin is synthesized by the kidneys and is then released into the circulation. There it acts with plasma precursor for producing angiotensin I, which is converted into angiotensin II which is a potent vasoconstriction and causes the release of aldosterone from the adrenals as well. Lisinopril doesn’t allow the conversion angiotensin I to angiotensin II, which leads to a decrease in the blood pressure levels and a small increase in the serum potassium levels and sodium and fluid loss.

Actions after intake – Pharmacokinetics

The following mechanism and actions take place after the consumption of Lisinopril:

1. Absorption

The serum levels reach their peak levels in 7 hours after the oral administration of Lisinopril. The decline in the serum concentrations show a long terminal phase which doesn’t contribute to the accumulation of drug. This terminal phase represents the saturable binding to the ACE and the does isn’t proportional. Lisinopril isn’t bound to other serum proteins. The extent of absorption of Lisinopril is about 25 percent with intersubject variability at all the tested doses. The food in the gastrointestinal tract doesn’t affect the absorption of Lisinopril.

2. Metabolism

Lisinopril doesn’t undergo the process of metabolism and is excreted unchanged in the urine.

3. Elimination

Lisinopril shows an effective half-life which is about 12 hours. The elimination of Lisinopril is decreased by impaired renal functioning. This decrease becomes quite important when the glomerular filtration rate is below 30 mL/min. The filtration rate is changed a bit above this glomerular filtration rate. Older patients have higher blood levels and the area under the plasma concentration curve (AUC) as compared to younger patients. It was found in a multiple study which involved elderly patients versus young hypertensive patients that the AUC increased about 120% for Lisinopril. Lisinopril can be removed from the body by hemodialysis.

Rat studies have shown that the blood-brain barrier is crossed poorly by Lisinopril. The multiple doses in rats doesn’t lead to the accumulation in any tissues but the milk of lactating rats contains radioactivity after administration of C14 lisinopril. Radioactivity was found in the placenta after the administration of the drug to pregnant rats. But no radioactivity was found in the fetus.

Overdosage

Lisinopril overdosage doesn’t normally happen. But a person can accidently take too much Lisinopril like other drugs. The Lisinopril Overdosage varies and depends upon a number of factors like how much Lisinopril is taken and whether it is taken with other drugs, medicines and alcohol.

Some major symptoms of Lisinopril overdosage include:

  • High levels of sodium and potassium in the blood
  • Extremely low blood pressure
  • Kidney failure

The treatment of overdosage varies from patient to patient. The doctor might advise you to take the Lisinopril out of your body through dialysis. The treatment also include supportive care. This usually includes treating the symptoms of Lisinopril overdose.

You should seek immediate help if you believe that you have overdosed on Lisinopril.

Side effects

Some major side effects of Lisinopril include tiredness, headache, and light headedness. You should immediately inform the doctor if any of these symptoms occur to you.

You should inform your doctor if you suffer from any symptoms like high potassium levels, fainting, irregular heartbeat, signs of infections and change in the amount of urine.

This drug can cause serious liver problems but it is quite rare. You should inform your doctor right away if you suffer from any side effects like dark urine, yellowing of eyes and skin, persistent nausea and vomiting and severe abdominal pain.

Moderate side effects

Some less severe side effects of the intake of Lisinopril have been mentioned below:

  • Cough
  • Cramps
  • Diarrhea
  • Feeling weak
  • Feeling like throwing up
  • Indigestion
  • Stomach problems
  • Inability to have an erection
  • Infrequent bowel movements

Decreased efficiency causes

The following things decreases the efficiency of Lisinopril:

  • The efficiency of Lisinopril is reduced when it reacts with other drugs. Some common drugs which can interact with Lisinopril include aspirin low strength, Nexium, xanax, Vitamin B12, Vitamin C, Lasix, Lantus, Norvasc and many others.
  • Allergic patients should avoid the intake of Lisinopril because this drug can cause severe side effects in allergic patients.
  • You should also check whether you have medical problems other than blood pressure because the efficiency of the drug is reduced if it is used for other medical problems.

Clinical studies of Benicar vs Lisinopril

A brief comparison of clinical trials of Benicar vs Lisinopril has been mentioned below:

  • There are about 7 studies which have approved the use of Benicar in which the doses range between 2.5 to 80 mg and the drugs were given from 6 to 12 weeks. There were more than 3000 hypertensive patients in the study. The studies showed a significant reduction in the diastolic and systolic blood pressure. The response of the drug was related to the dose. The patients who received more dose had a comparatively better effect as compared to the patients who took 20 mg tablets. It takes about 2 hours for this medicine to have some effect. The blood pressure remained under control throughout the 24 hours.
  • Many studies have shown that the effect of Lisinopril is seen one hour after the oral administration of the drug. It has also been seen that the effect of Lisinopril is more consistent as compared to other blood pressure medications. It has also been found out in the studies that the effect is more consistent in doses larger than 20 mg as compared to smaller doses. The effect of Lisinopril remained consistent throughout the day.

Conclusion

The comparison of Lisinopril and Benicar shows that Lisinopril is the better drug out of the two for the treatment of blood pressure. There are two reasons for it. The first reason is that Lisinopril has quicker effects compared to Benicar. The second reason which makes Lisinopril a better drug is that the effect of Lisinopril is more consistent than other blood pressure medications and that also includes Benicar (e.g. ACE inhibitors tend to be more consistent in effect than sartans and other high blood pressure treating drugs). So Lisinopril is a better drug than Benicar for the treatment of blood pressure and should be the first choice.

This is just an informative post comparing Benicar to Lisinopril. While we tried to be as accurate as possible in describing various effects and dosing of both drugs you should never rely on medical information found on the Internet. Only your physician is responsible for drug prescription and proper dosing. Go and see your doctor if you suffer from any health problems.

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Written by: Michal Vilímovský (EN)
Education: Physician
Article resources:

See numbered references within the article.

Image resources:

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Published: October 25, 2015 at 12:55 PM
Next scheduled update: October 25, 2017 at 12:55 PM
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