Lortaan 100 mg
Lortaan 100 mg Uses, Dosage, Side Effects, Food Interaction and all others data.
Lortaan 100 mg, 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. Lortaan 100 mg and its principal active metabolite block the vasoconstriction and aldosterone secreting effects of angiotensin II to the AT1 receptor found in many tissues. Lortaan 100 mg is now regarded as the first-line therapy option for treating high blood pressue.
Lortaan 100 mg is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke. Lortaan 100 mg 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 | Lortaan 100 mg |
| 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 | Portugal |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lortaan 100 mg 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.
Lortaan 100 mg is also used to associated treatment for these conditions: Diabetic Nephropathy, Heart Failure, High Blood Pressure (Hypertension), Marfan Syndrome, Stroke
How Lortaan 100 mg works
Lortaan 100 mg reversibly and competitively prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland. Lortaan 100 mg 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. Lortaan 100 mg'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
Lortaan 100 mg 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 Lortaan 100 mg 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 Lortaan 100 mg. 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 Lortaan 100 mg. Serious hypotension (particularly on initiating treatment in salt-depleted patients) or renal failure (mainly in patients with renal artery stenosis) may be encountered during Lortaan 100 mg 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. Lortaan 100 mg 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.
Lortaan 100 mg 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
Lortaan 100 mg 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
Lortaan 100 mg is approximately 33% orally bioavailable. Lortaan 100 mg 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
Lortaan 100 mg 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 Lortaan 100 mg in pregnant women, animal studies with Lortaan 100 mg 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. Lortaan 100 mg should not be used in pregnancy and if pregnancy is detected Lortaan 100 mg should be discontinued as soon as possible.
It is not known whether Lortaan 100 mg is excreted in human breast milk. However, significant level of Lortaan 100 mg 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 Lortaan 100 mg potassium should be corrected prior to administer Lortaan 100 mg 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 Lortaan 100 mg nor the active metabolite can be removed by hemodialysis.
Storage Condition
Store between 15-30°C
Innovators Monograph
You find simplified version here Lortaan 100 mg
Lortaan 100 mg contains Losartan see full prescribing information from innovator Lortaan 100 mg Monograph, Lortaan 100 mg MSDS, Lortaan 100 mg FDA label
FAQ
What is Lortaan 100 mg used for?
Lortaan 100 mg used to treat high blood pressure. It is also used for diabetic kidney disease, heart failure, and left ventricular enlargement. Lortaan 100 mg protect your kidneys if you have both kidney disease and diabetes.
How safe is Lortaan 100 mg?
Lortaan 100 mg is generally safe to take for a long time. In fact, Lortaan 100 mg works best when you take it for a long time. Taking Lortaan 100 mg 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 Lortaan 100 mg work?
Lortaan 100 mg 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 Lortaan 100 mg?
Common side effects of Lortaan 100 mg 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 Lortaan 100 mg safe during pregnancy?
Do not take Lortaan 100 mg if you are pregnant. If you become pregnant while you are taking Lortaan 100 mg, stop taking Lortaan 100 mg and call your doctor immediately. Lortaan 100 mg may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.
Is Lortaan 100 mg safe during breastfeeding?
Lortaan 100 mg is not known if Lortaan 100 mg 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 Lortaan 100 mg?
Lortaan 100 mg may cause low blood pressure, resulting in dizziness, lightheadedness, and fainting. Moderate alcohol consumption while taking Lortaan 100 mg is generally considered safe, but alcohol may make the side effects of Lortaan 100 mg worse.
Can I drive after taking Lortaan 100 mg?
Avoid driving or using heavy machinery while dizzy. See a doctor if dizziness or lightheadedness persists or gets worse.
When should be taken of Lortaan 100 mg?
Take Lortaan 100 mg 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 Lortaan 100 mg at any time of day. Try to take it at the same time every day.
Can I take Lortaan 100 mg on an empty stomach?
You can take Lortaan 100 mg tablets with or without food. Swallow the tablets with a drink of water.
Is it better to take Lortaan 100 mg 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 Lortaan 100 mg take to work?
Lortaan 100 mg 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 Lortaan 100 mg stay in my system?
The Lortaan 100 mg 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 Lortaan 100 mg and its metabolite from your system.
Can I take Lortaan 100 mg for a long time?
Lortaan 100 mg is generally safe to take for a long time. In fact, it works best when you take it for a long time. However taking Lortaan 100 mg 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 Lortaan 100 mg bad for my kidney?
There is a risk of acute kidney failure developing in people taking Lortaan 100 mg.
Can I take Lortaan 100 mg 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 Lortaan 100 mg tablets with or without food.
How many hours does Lortaan 100 mg last?
Lortaan 100 mg taken once daily, does not last the full 24 hours at lower doses like 25 or 50 mg. At 100 mg daily Lortaan 100 mg does last the full 24 hours. If you take Lortaan 100 mg 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 Lortaan 100 mg?
An overdose of Lortaan 100 mg can cause dizziness, sleepiness and a pounding heartbeat.
What happen If I stop taking Lortaan 100 mg?
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 Lortaan 100 mg, talk with your doctor. They will slowly taper your dosage so that you can stop using the drug safely.
Can Lortaan 100 mg cause heart problems?
An irregular heartbeat has been reported with Lortaan 100 mg but is rare.
Can Lortaan 100 mg affects my liver?
Lortaan 100 mg is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.
Will Lortaan 100 mg affect my fertility?
One experimental animal study did not find effects on fertility.
