Olmisart

Olmisart Uses, Dosage, Side Effects, Food Interaction and all others data.

Olmisart medoxomil is a potent, orally active, selective angiotensin II receptor (type AT1) antagonist. It is expected to block all actions of angiotensin II mediated by the AT1 receptor, regardless of the source or route of synthesis of angiotensin II. The selective antagonism of the angiotensin II (AT1) receptors results in increases in plasma renin levels and angiotensin I and II concentrations, and some decrease in plasma aldosterone concentrations. Angiotensin II is the primary vasoactive hormone of the renin-angiotensin- aldosterone system (RAAS) and plays a significant role in the pathophysiology of hypertension via the type 1 (AT1) receptor.

Overall, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.

Hypotension in Volume- or Salt-Depleted Patients

In patients with an activated renin-angiotensin aldosterone system, such as volume-and/or salt-depleted patients (e.g., those being treated with high doses of diuretics), symptomatic hypotension may be anticipated after initiation of treatment with olmesartan. Initiate treatment under close medical supervision. If hypotension does occur, place the patient in the supine position and, if necessary, give an intravenous infusion of normal saline. A transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once the blood pressure has stabilized.

Trade Name Olmisart
Availability Prescription only
Generic Olmesartan
Olmesartan Other Names Olmesartan
Related Drugs amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide
Type Tablet
Formula C24H26N6O3
Weight Average: 446.5016
Monoisotopic: 446.206638728
Protein binding

Olmesartan is highly bound to plasma proteins. 99% of the administered dose is found in a bound state with no penetration in red blood cells.[L5566]

Groups Approved, Investigational
Therapeutic Class Angiotensin-ll receptor blocker
Manufacturer Nukind Healthcare Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Olmisart
Olmisart

Uses

Olmisart is used for the treatment of mild to moderate essential hypertension. Olmisart may be used alone or in combination with thiazide diuretic.

Olmisart is also used to associated treatment for these conditions: Diabetic Nephropathy, High Blood Pressure (Hypertension), Severe Hypertension, Moderate Hypertension

How Olmisart works

Olmisart belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, valsartan, and irbesartan. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects. As the principal pressor agent of the renin-angiotensin system, Angiotensin II causes vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. Olmisart blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis. Overall, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.

Olmisart also effects on the renin-angiotensin aldosterone system (RAAS) plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.

Dosage

Olmisart dosage

Adult:Dosage must be individualized. The usual initial dose is 10 mg once daily. In patients whose blood pressure is not adequately controlled at this dose, the dose may be increased to 20 mg once daily as the optimal dose. For patients requiring further reduction in blood pressure after 2 weeks of therapy, the dose of Olmisart may be increased to 40 mg. Doses above 40 mg do not appear to have greater effect.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: Of the total number of hypertensive patients receiving Olmisart Medoxomil in clinical studies, more than 20% were 65 years of age and over, while more than 5% were 75 years of age and older. No overall differences in effectiveness or safety were observed between elderly patients and younger patients.

Side Effects

Common or very common: Arthritis, chest pain, cough, fatigue, gastro-intestinal disturbances, haematuria, hypertriglyceridaemia, hyperuricaemia, influenza-like symptoms, musculoskeletal pain, peripheral edema, pharyngitis, rhinitis, urinary-tract infection.

Uncommon: Angina, rash, vertigo.

Very rare: Headache, myalgia, pruritus, thrombocytopenia, urticaria.

Toxicity

The reported LD50 of olmesartan in dogs was reported to be greater of 1500 mg/kg. Overdose is expressed as hypotension, tachycardia, and bradycardia when there is parasympathetic stimulation. In case of overdose, supportive treatment is recommended.

Olmisart was shown to be safe on carcinogenic and fertility studies. However, in in vitro mutagenic studies showed a potential to induce chromosomal aberrations in cells and it tested positive for thymidine kinase mutations in the mouse lymphoma assay.

Precaution

Fetal/Neonatal Morbidity and Mortality: Drugs that act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. Several dozen cases have been reported in the world literature of patients who were taking angiotensin converting enzyme inhibitors. When pregnancy is detected, Olmisart Medoxomil should be discontinued as soon as possible.

Hypotension in Volume- or Salt-Depleted Patients: In patients with an activated renin-angiotensin system, such as volume- and/or salt-depleted patients (e.g., those being treated with high doses of diuretics), symptomatic hypotension may occur after initiation of treatment with Olmisart Medoxomil. Treatment should start under close medical supervision. If hypotension does occur, the patient should be placed in the supine position and, if necessary, given an intravenous infusion of normal saline.

Interaction

No significant drug interactions were reported in studies in which Olmisart Medoxomil was co-administered with digoxin or warfarin in healthy volunteers. The bioavailability of Olmisart was not significantly altered by the co-administration of antacids [Al(OH)3/Mg(OH)2]. Olmisart Medoxomil is not metabolized by the cytochrome P450 system and has no effects on P450 enzymes; thus, interactions with drugs that inhibit, induce or are metabolized by those enzymes are not expected.

Food Interaction

  • Take with or without food. Food does not affect absorption.

[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium, especially salt substitutes, may increase the risk of hyperkalemia in some patients who are using angiotensin II receptor blockers (ARBs).

ARBs can promote hyperkalemia through inhibition of angiotensin II-induced aldosterone secretion.

Patients with diabetes, heart failure, dehydration, or renal insufficiency have a greater risk of developing hyperkalemia.

MANAGEMENT: Patients should receive dietary counseling and be advised to not use potassium-containing salt substitutes or over-the-counter potassium supplements without consulting their physician.

If salt substitutes are used concurrently, regular monitoring of serum potassium levels is recommended.

Patients should also be advised to seek medical attention if they experience symptoms of hyperkalemia such as weakness, irregular heartbeat, confusion, tingling of the extremities, or feelings of heaviness in the legs.

Volume of Distribution

17 L[L5566]

Elimination Route

When taken orally, the prodrug olmesartan medoxomil is rapidly absorbed in the gastrointestinal tract and metabolized to olmesartan. The esterification with medoxomil was created with the intention of increasing olmesartan bioavailability from 4.5% to 28.6%.

Oral administration of 10-160 mg of olmesartan has been shown to reach peak plasma concentration of 0.22-2.1 mg/L after 1-3 hours with an AUC of 1.6-19.9mgh/L. The pharmacokinetic profile of olmesartan has been observed to be nearly linear and dose-dependent under the therapeutic range. The steady-state level of olmesartan is achieved after once a day dosing during 3 to 5 days.[L5566]

Half Life

The mean plasma olmesartan half-life is reported to be from 10-15 hours after multiple oral administration.

Clearance

Total plasma clearance is 1.3 L/h and the renal clearance is 0.6 L/h.[L5566]

Elimination Route

The main elimination route of olmesartan is in the unchanged form through the feces. From the systemically bioavailable dose, about 10-16% is eliminated in the urine.

Pregnancy & Breastfeeding use

Pregnancy Categories C (first trimester) and D (second and third trimesters).

Nursing Mothers: It is not known whether Olmisart is excreted in human milk, but Olmisart is secreted at low concentration in the milk of lactating rats. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Olmisart is contraindicated in patients who are hypersensitive to any component of this product.

Special Warning

Hepatic Impairment: Dose should not exceed 20 mg daily in moderate impairment.

Renal Impairment: Max. 20 mg daily if eGFR 20–60 mL/minute/1.73 m2. Avoid if eGFR less than 20 mL/minute/1.73 m2.

Acute Overdose

Only limited information is available regarding overdosage in humans. The most likely effect of overdosage is hypotension. In the event of overdosage, the patient should be carefully monitored and treatment should be symptomatic and supportive. No information is available regarding the dialysability of olmesartan.

Storage Condition

Keep out of the reach of children. Keep in the original package in a cool & dry place. Protect from light and moisture.

Innovators Monograph

You find simplified version here Olmisart

Olmisart contains Olmesartan see full prescribing information from innovator Olmisart Monograph, Olmisart MSDS, Olmisart FDA label

FAQ

What is Olmisart used for?

Olmisart is a medicine used to treat high blood pressure. Olmisart helps prevent future strokes, heart attacks and kidney problems,and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure.

How safe is Olmisart ?

Olmisart is generally safe to take for a long time. In fact, it works best when you take it for a long time. Taking Olmisart long term can sometimes cause problems with your kidneys. This means they don't work as well as they should.

How does Olmisart work?

Olmisart is a type of blood pressure-lowering medicine called an angiotensin receptor blocker. Like other angiotensin receptor blockers, Olmisart relaxes and widens your blood vessels. This lowers your blood pressure and makes it easier for your heart to pump blood around your body.

What are the common side effects of Olmisart?

The main side effects of Olmisart are dizziness, headaches and flu-like symptoms, but they're usually mild and short-lived. If you're being sick or have severe diarrhoea because of a stomach bug or illness while taking Olmisart , tell your doctor.

Is Olmisart safe during pregnancy?

This Olmisart may be given to a pregnant woman if her healthcare provider believes that the benefits to the pregnant woman outweigh any possible risks to her unborn baby.

Is Olmisart safe during breastfeeding?

Olmisart isn't normally recommended in pregnancy or while breastfeeding. Talk to your doctor if you're trying to get pregnant, are already pregnant or you're breastfeeding. 

Can I drink alcohol with Olmisart ?

Drinking alcohol can increase the blood pressure-lowering effect of Olmisart, which can make you feel dizzy or lightheaded. During the first few days of taking Olmisart or after a dose increase, it's best not to drink alcohol until you see how the medicine affects you.

When Is the best taken of Olmisart?

Your doctor may suggest that you take your first dose before bedtime, as it can make you dizzy. After the very first dose you can take Olmisart at any time of day. Usually people take Olmisart in the morning, but it doesn't really matter.

How often can I take Olmisart?

For adults and children aged 6 years and over, the usual dose is 10mg taken once a day to start with. Your dose may eventually go up to 20mg or 40mg, taken once a day. Children weighing less than 35kg should not take more than 20mg daily.

How long does Olmisart take to work?

It may take 2 to 8 weeks to take effect fully.

Can I take Olmisart for a long time?

Olmisart works best when you take it for a long time. Taking Olmisart long term can sometimes cause problems with your kidneys. This means they don't work as well as they should. Your doctor will check how well your kidneys are working with regular blood tests.

Who should not take Olmisart?

Do not use if you are pregnant. Stop using Olmisart and tell your doctor right away if you become pregnant. If you have diabetes, do not take Olmisart with any medication that contains aliskiren (a blood pressure medicine).

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include fast heartbeats or fainting.

Is Olmisart good for kidneys?

This is due to the great number of studies, which have found that Olmisart and other ARBs protect the kidneys from the effects of inflammation and cytokine damage.

What happen If I suddenly stop taking Olmisart?

Stopping Olmisart may cause your blood pressure to rise. This may increase your chances of having a heart attack and stroke. If you're bothered by side effects, your doctor may be able to prescribe a different blood pressure-lowering medicine.

Can Olmisart affects my liver?

Olmisart is associated with a low rate of transient serum aminotransferase elevations, but has yet to be linked to instances of acute liver injury.

Can Olmisart cause heart attacks?

Don't stop taking Olmisart without talking to your doctor. Stopping the drug suddenly may cause your blood pressure to spike (rise suddenly). This may increase your risk of a heart attack or stroke.

*** Taking medicines without doctor's advice can cause long-term problems.
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