Losartanum 123ratio
Losartanum 123ratio Uses, Dosage, Side Effects, Food Interaction and all others data.
Losartanum 123ratio, the first of a new class of antihypertensives, is a specific and selective antagonist of angiotensin II at the AT1 sites. Angitensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. Losartanum 123ratio and its principal active metabolite block the vasoconstriction and aldosterone secreting effects of angiotensin II to the AT1 receptor found in many tissues. Losartanum 123ratio is now regarded as the first-line therapy option for treating high blood pressue.
Losartanum 123ratio is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke. Losartanum 123ratio has a long duration of action as it is given once daily. Patients taking losartan should be regularly monitored for hypotension, renal function, and potassium levels.
Trade Name | Losartanum 123ratio |
Availability | Prescription only |
Generic | Losartan |
Losartan Other Names | Losartan |
Related Drugs | amlodipine, lisinopril, metoprolol, furosemide, hydrochlorothiazide, atenolol, ramipril, captopril, enalapril, irbesartan |
Type | |
Formula | C22H23ClN6O |
Weight | Average: 422.911 Monoisotopic: 422.162187095 |
Protein binding | Losartan is 98.6-98.8% protein bound and the active metabolite (E-3174) is 99.7% protein bound in serum. |
Groups | Approved |
Therapeutic Class | Angiotensin-ll receptor blocker |
Manufacturer | |
Available Country | Poland |
Last Updated: | September 19, 2023 at 7:00 am |
![Losartanum 123ratio Losartanum 123ratio](https://www.medicinesfaq.com/media/png/losartanum-123ratio.png)
Uses
Losartanum 123ratio is an angiotensin II receptor blocker (ARB) used for:
- Treatment of hypertension, to lower blood pressure in adults and children greater than 6 years old. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
- Reduction of the risk of stroke in patients with hypertension and left ventricular hypertrophy. There is evidence that this benefit does not apply to Black patients.
- Treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria in patients with type 2 diabetes and a history of hypertension.
Losartanum 123ratio is also used to associated treatment for these conditions: Diabetic Nephropathy, Heart Failure, High Blood Pressure (Hypertension), Marfan Syndrome, Stroke
How Losartanum 123ratio works
Losartanum 123ratio reversibly and competitively prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland. Losartanum 123ratio and its active metabolite bind the AT1 receptor with 1000 times more affinity than they bind to the AT2 receptor. The active metabolite of losartan is 10-40 times more potent by weight than unmetabolized losartan as an inhibitor of AT1 and is a non-competitive inhibitor. Losartanum 123ratio's prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure.
Angiotensin II would otherwise bind to the AT1 receptor and induce vasoconstriction, raising blood pressure.
Dosage
Losartanum 123ratio dosage
Hypertension:
- Usual adult dose: 50 mg once daily.
- Usual pediatric starting dose: 0.7 mg per kg once daily (up to 50 mg).
Hypertensive Patients with Left Ventricular Hypertrophy:
- Usual starting dose: 50 mg once daily.
- Add hydrochlorothiazide 12.5 mg and/or increase Losartanum 123ratio to 100 mg followed by an increase to hydrochlorothiazide 25 mg if further blood pressure response is needed.
Nephropathy in Type 2 Diabetic Patients:
- Usual dose: 50 mg once daily.
- Increase dose to 100 mg once daily if further blood pressure response is needed.
Use in elderly:
- Patients up to 75 years: No initial dosage adjustment is necessary for this group of patients.
- Patients over 75 years: A lower starting dose of 25 mg once daily is recommended.
Side Effects
In controlled clinical trials in patients with essential hypertension, dizziness was the only side effect reported that occurred with an incidence greater than placebo in 1% or more of patients treated with Losartanum 123ratio. Rarely, rash was reported although the incidence in controlled clinical trials was less than placebo. Angioedema, involving swelling of the face, lips and/or tongue has been reported rarely in patients treated with Losartanum 123ratio. Serious hypotension (particularly on initiating treatment in salt-depleted patients) or renal failure (mainly in patients with renal artery stenosis) may be encountered during Losartanum 123ratio treatment.
Toxicity
The oral TDLO in mice is 1000mg/kg and in rats is 2000mg/kg. In humans the TDLO for men is 10mg/kg/2W and for women is 1mg/kg/1D.
Symptoms of overdose are likely to include hypotension, tachycardia, or bradycardia due to vagal stimulation. Supportive treatment should be instituted for symptomatic hypotension. Hemodialysis will not remove losartan or its active metabolite due to their high rates of protein binding.
Precaution
A lower dose should be considered for patients with a history of hepatic and renal impairment. Losartanum 123ratio should not be used with potassium-sparing diuretic
Interaction
No drug interaction of clinical significance has been identified. Compounds which have been studied in clinical pharmacokinetic trials include hydrochlorothiazide, digoxin, warfarin, cimetidine, ketoconazole and phenobarbital.
Food Interaction
- Take at the same time every day.
- Take with or without food. Food delays absorption, but does not affect the extent of 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.
MONITOR: Grapefruit juice may modestly decrease and delay the conversion of losartan to its active metabolite, E3174.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.
The clinical significance is unknown.
Moreover, pharmacokinetic alterations associated with interactions involving grapefruit juice are often subject to a high degree of interpatient variability.
MANAGEMENT: Patients who regularly consume grapefruits and grapefruit juice should be monitored for altered efficacy of losartan.
Grapefruits and grapefruit juice should be avoided if an interaction is suspected.
Orange juice is not expected to interact.
Losartanum 123ratio Drug Interaction
Moderate: aspirin, aspirin, pregabalin, alprazolamUnknown: ubiquinone, rosuvastatin, duloxetine, apixaban, omega-3 polyunsaturated fatty acids, furosemide, atorvastatin, metoprolol, metoprolol, clopidogrel, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Losartanum 123ratio Disease Interaction
Major: diabetes, angioedema, hypotensionModerate: CHF, hyperkalemia, renal artery stenosis, renal impairment, renal/liver disease
Volume of Distribution
The volume of distribution of losartan is 34.4±17.9L and 10.3±1.1L for the active metabolite (E-3174).
Elimination Route
Losartanum 123ratio is approximately 33% orally bioavailable. Losartanum 123ratio has a Tmax of 1 hour and the active metabolite has a Tmax of 3-4 hours. Taking losartan with food decreases the Cmax but does only results in a 10% decrease in the AUC of losartan and its active metabolite. A 50-80mg oral dose of losartan leads to a Cmax of 200-250ng/mL.
Half Life
The terminal elimination half life of losartan is 1.5-2.5 hours while the active metabolite has a half life of 6-9 hours.
Clearance
Losartanum 123ratio has a total plasma clearance of 600mL/min and a renal clearance of 75mL/min. E-3174, the active metabolite, has a total plasma clearance of 50mL/min and a renal clearance of 25mL/min.
Elimination Route
A single oral dose of losartan leads to 4% recovery in the urine as unchanged losartan, 6% in the urine as the active metabolite. Oral radiolabelled losartan is 35% recovered in urine and 60% in feces. Intravenous radiolabelled losartan is 45% recovered in urine and 50% in feces.
Pregnancy & Breastfeeding use
Although there is no experience with the use of Losartanum 123ratio in pregnant women, animal studies with Losartanum 123ratio potassium have demonstrated fetal and neonatal injury and death, the mechanism of which is believed to be pharmacologically mediated through effects on the renin angiotensinaldosterone system. Losartanum 123ratio should not be used in pregnancy and if pregnancy is detected Losartanum 123ratio should be discontinued as soon as possible.
It is not known whether Losartanum 123ratio is excreted in human breast milk. However, significant level of Losartanum 123ratio found in rat milk which suggests that the drug should not be used in lactating mother.
Contraindication
It is also contraindicated to patients who are hypersensitive to any component of this product. In patients who are intravenously volume depleted (e.g. those treated with high dose diuretics), symptomatic hypotension may occur. These conditions Losartanum 123ratio potassium should be corrected prior to administer Losartanum 123ratio or a lower starting dose (usually 25 mg) should be used.
Special Warning
No initial dosage adjustment is necessary in patients with mild renal impairment (CrCl 20-50 ml/min). For patients with moderate to severe renal impairment (CrCl <20 ml/min) or patients on dialysis, a lower starting dose of 25 mg is recommended.
Acute Overdose
Limited data are available regarding overdose in humans. The most likely manifestation of overdose would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. Supportive treatment should include repletion of the intravascular volume. Neither Losartanum 123ratio nor the active metabolite can be removed by hemodialysis.
Storage Condition
Store between 15-30°C
Innovators Monograph
You find simplified version here Losartanum 123ratio
Losartanum 123ratio contains Losartan see full prescribing information from innovator Losartanum 123ratio Monograph, Losartanum 123ratio MSDS, Losartanum 123ratio FDA label
FAQ
What is Losartanum 123ratio used for?
Losartanum 123ratio used to treat high blood pressure. It is also used for diabetic kidney disease, heart failure, and left ventricular enlargement. Losartanum 123ratio protect your kidneys if you have both kidney disease and diabetes.
How safe is Losartanum 123ratio?
Losartanum 123ratio is generally safe to take for a long time. In fact, Losartanum 123ratio works best when you take it for a long time. Taking Losartanum 123ratio for a long time can sometimes cause your kidneys not to work as well as they should. Your doctor will check how well your kidneys are working with regular blood tests.
How does Losartanum 123ratio work?
Losartanum 123ratio 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 Losartanum 123ratio?
Common side effects of Losartanum 123ratio are include:
- Blurred vision.
- difficult breathing.
- dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position.
- fast or irregular heartbeat.
- nausea or vomiting.
- numbness or tingling in the hands, feet, or lips.
- stomach pain.
- weakness or heaviness of the legs.
Is Losartanum 123ratio safe during pregnancy?
Do not take Losartanum 123ratio if you are pregnant. If you become pregnant while you are taking Losartanum 123ratio, stop taking Losartanum 123ratio and call your doctor immediately. Losartanum 123ratio may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.
Is Losartanum 123ratio safe during breastfeeding?
Losartanum 123ratio is not known if Losartanum 123ratio passes into breast milk. It is not recommended for women who are breastfeeding because other medicines with a more established safety profile are available.
Can I drink alcohol with Losartanum 123ratio?
Losartanum 123ratio may cause low blood pressure, resulting in dizziness, lightheadedness, and fainting. Moderate alcohol consumption while taking Losartanum 123ratio is generally considered safe, but alcohol may make the side effects of Losartanum 123ratio worse.
Can I drive after taking Losartanum 123ratio?
Avoid driving or using heavy machinery while dizzy. See a doctor if dizziness or lightheadedness persists or gets worse.
When should be taken of Losartanum 123ratio?
Take Losartanum 123ratio tablets once a day. Your doctor may suggest that you take your first dose before bedtime, because it can make you dizzy. After the very first dose, you can take Losartanum 123ratio at any time of day. Try to take it at the same time every day.
Can I take Losartanum 123ratio on an empty stomach?
You can take Losartanum 123ratio tablets with or without food. Swallow the tablets with a drink of water.
Is it better to take Losartanum 123ratio in the morning or in the evening?
For once daily dosing, there are no absolute recommendations about taking it in the morning vs. night. For high blood pressure, some research suggests taking medicines at night reduces the risk of cardiovascular events in the morning.
How long does Losartanum 123ratio take to work?
Losartanum 123ratio starts to reduce high blood pressure after about 6 hours but it may take 3 to 6 weeks to fully take effect. If you have high blood pressure, you may not have any symptoms.
How long does Losartanum 123ratio stay in my system?
The Losartanum 123ratio half-life is about 2 hours and the metabolite half-life is 6 to 9 hours. This means it can take a couple of days to clear Losartanum 123ratio and its metabolite from your system.
Can I take Losartanum 123ratio for a long time?
Losartanum 123ratio is generally safe to take for a long time. In fact, it works best when you take it for a long time. However taking Losartanum 123ratio for a long time can sometimes cause your kidneys not to work as well as they should. Your doctor will check how well your kidneys are working with regular blood tests.
Is Losartanum 123ratio bad for my kidney?
There is a risk of acute kidney failure developing in people taking Losartanum 123ratio.
Can I take Losartanum 123ratio every other day?
Your doctor may suggest that you take your first dose before bedtime, because it can make you dizzy. After the very first dose, you can take losartan at any time of day. Try to take it at the same time every day. You can take Losartanum 123ratio tablets with or without food.
How many hours does Losartanum 123ratio last?
Losartanum 123ratio taken once daily, does not last the full 24 hours at lower doses like 25 or 50 mg. At 100 mg daily Losartanum 123ratio does last the full 24 hours. If you take Losartanum 123ratio 50 mg in the morning, you may notice your blood pressure rises at night, because it's not covering you for a full 24 hours.
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happen If I overdose on Losartanum 123ratio?
An overdose of Losartanum 123ratio can cause dizziness, sleepiness and a pounding heartbeat.
What happen If I stop taking Losartanum 123ratio?
Stopping it suddenly can cause your blood pressure to increase quickly. This raises your risk of a heart attack or stroke. If you want to stop taking Losartanum 123ratio, talk with your doctor. They will slowly taper your dosage so that you can stop using the drug safely.
Can Losartanum 123ratio cause heart problems?
An irregular heartbeat has been reported with Losartanum 123ratio but is rare.
Can Losartanum 123ratio affects my liver?
Losartanum 123ratio is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.
Will Losartanum 123ratio affect my fertility?
One experimental animal study did not find effects on fertility.