Losartan potassium, Discovery, Action, Uses, Uses in Urdu, Side effects, Dosage and Popular Brands.

Introduction

Losartan potassium is a widely used medication for managing high blood pressure (hypertension) ) and to lower the risk of strokes and heart attacks, particularly in patients with type 2 diabetes. It belongs to a class of drugs known as angiotensin II receptor blockers (ARBs), which help relax blood vessels and improve blood flow.

Losartan potassium is a prominent medication widely used in the medical field to manage hypertension (high blood pressure) and to protect kidney function in patients with type 2 diabetes, it plays a critical role in controlling blood pressure and maintaining cardiovascular health.

Hypertension is a major risk factor for serious health conditions such as heart attacks, strokes, and kidney failure. Therefore, effective management of high blood pressure is essential for reducing these risks and enhancing patients’ quality of life.

In addition, losartan is sometimes prescribed for heart failure and to reduce the risk of stroke in certain patient populations. Its versatility and effectiveness make it a valuable option in the therapeutic arsenal for cardiovascular and renal health management.

Discovery

Losartan Potassium was discovered by DuPont scientists in 1986. The research team was led by Dr. John M. Sasaki and Dr. James M. Roesgen. They were working on developing a new class of antihypertensive drugs that targeted the renin-angiotensin-aldosterone system (RAAS), a key regulator of blood pressure.

The discovery of Losartan Potassium was a result of a systematic search for compounds that could block the action of angiotensin II, a potent vasoconstrictor that raises blood pressure. The team used a combination of molecular modelling, chemical synthesis, and biological testing to identify potential leads.

Losartan Potassium was initially synthesized as a racemic mixture, but subsequent testing revealed that the potassium salt of the (-) enantiomer was the more active and potent form. This led to the development of Losartan Potassium as a single-enantiomer drug, which was approved by the FDA in 1995.

Impact

The discovery of Losartan Potassium has had a significant impact on the treatment of hypertension and related cardiovascular diseases. It has become a widely used medication worldwide, and its discovery has paved the way for the development of other angiotensin II receptor blockers (ARBs).

Mechanism of Action of Losartan Potassium

Angiotensin II Receptor Blockade

Losartan Potassium is a selective, competitive angiotensin II receptor type 1 (AT1) antagonist. It blocks the action of angiotensin II, a potent vasoconstrictor that raises blood pressure, by binding to the AT1 receptor in the following ways:

• Reducing vasoconstriction: Angiotensin II causes blood vessels to constrict, increasing blood pressure. It blocks this effect, allowing blood vessels to dilate and reducing blood pressure.
• Decreasing aldosterone production: Angiotensin II stimulates the production of aldosterone, a hormone that increases blood pressure by causing the kidneys to retain sodium and water. it reduces aldosterone production, leading to decreased sodium and water retention.
• Reducing renal reabsorption of sodium: Losartan decreases the reabsorption of sodium in the kidneys, leading to increased excretion of sodium and water, and a decrease in blood pressure.

Other Mechanisms

In addition to blocking the action of angiotensin II, Losartan Potassium has other mechanisms of action that contribute to its antihypertensive effects:

• Increasing renal blood flow: It increases blood flow to the kidneys, improving renal function and reducing blood pressure.
• Reducing sympathetic nervous system activity: It decreases the activity of the sympathetic nervous system, which can contribute to hypertension.
• Antioxidant effects: It has antioxidant properties, which can help protect against oxidative stress and inflammation, contributing to its antihypertensive effects.

Losartan potassium uses

Losartan potassium treats high blood pressure and reduces the risk of strokes and heart attacks. It’s mainly used for heart and blood vessel conditions. Its medical uses include:

Hypertension (High Blood Pressure) Management:

Losartan potassium is widely prescribed for the treatment of hypertension, a common cardiovascular condition characterized by elevated blood pressure levels. By blocking the action of angiotensin II on its receptors, It helps to relax blood vessels, reducing peripheral resistance and lowering blood pressure. Effective blood pressure control with Losartan reduce the risk of cardiovascular events such as stroke, heart attack, and heart failure.

Heart Failure:

Losartan is indicated for the treatment of heart failure with reduced ejection fraction (HFrEF), a condition in which the heart’s ability to pump blood is impaired. As an ARB, Losartan helps to improve cardiac function by reducing afterload (the resistance the heart must overcome to eject blood) and inhibiting adverse remodelling of the heart muscle. It can alleviate symptoms such as shortness of breath, fatigue, and fluid retention, thus improving quality of life and reducing the risk of hospitalization.

Diabetic Nephropathy (Kidney Disease):

Losartan potassium has demonstrated efficacy in the management of diabetic nephropathy, a common complication of diabetes characterized by kidney damage and proteinuria (excessive protein in the urine). By lowering blood pressure and inhibiting the progression of renal damage, Losartan helps to preserve kidney function and delay the onset of end-stage renal disease (ESRD) in patients with type 2 diabetes mellitus and proteinuria.

Post-Myocardial Infarction (Heart Attack) Protection:

In certain cases, Losartan is prescribed for secondary prevention in patients who have experienced a myocardial infarction (heart attack). It can help reduce the risk of future cardiovascular events and improve outcomes by stabilizing cardiac function, preventing adverse remodelling of the heart muscle, and lowering blood pressure.

Left Ventricular Hypertrophy:

Losartan potassium is used to treat left ventricular hypertrophy (LVH), a condition characterized by thickening of the heart’s left ventricle wall in response to chronic pressure overload, such as hypertension. By reducing blood pressure and inhibiting myocardial remodelling, Losartan can help regress LVH and improve cardiac function in affected individuals.

Prevention of Stroke:

Losartan can also be considered as part of a comprehensive strategy for stroke prevention in patients at high risk, particularly those with hypertension or a history of stroke or transient ischemic attack (TIA). Its ability to lower blood pressure and improve vascular function contributes to its potential benefit in reducing the risk of stroke and its complications.

Pregnancy and Breastfeeding

Pregnancy and breastfeeding are important considerations when it comes to taking Losartan potassium. there are significant considerations and potential risks that need to be understood:

Pregnancy:

• Losartan potassium is not recommended during pregnancy, especially during the second and third trimesters.
  Using Losartan potassium during pregnancy can cause serious harm or even death to an unborn baby. It leads to fetal injury or death if used during the second and third trimesters.
• If you become pregnant while taking Losartan, inform your doctor immediately. Your doctor need to switch you to a different medication that is safer during pregnancy.

Breastfeeding:

• It’s generally recommended to avoid using Losartan while breastfeeding.
• Losartan may pass into breast milk and could potentially harm a nursing infant.
• If you need to take Losartan while breastfeeding, discuss the risks and benefits with your doctor.
• it recommends alternative medications that are safer during breastfeeding.

Losartan potassium uses in Urdu

 لاسارٹن پوٹاشیم کا استعمال: ہائی بلڈ پریشر اور دیگر دل اور خون کی نالیوں کی بیماریوں کا علاج

لاسارٹن پوٹاشیم ایک وسیع پیمانے پر استعمال ہونے والی دوا ہے جو ہائی بلڈ پریشر اور دیگر دل اور خون کی نالیوں کی بیماریوں کے علاج میں مدد کرتی ہے۔ اس کی طبی استعمالات میں شامل ہیں

 ہائی بلڈ پریشر (ہائی بلڈ پریشر) کا انتظام

لاسارٹن پوٹاشیم کو ہائی بلڈ پریشر کے علاج کے لئے وسیع پیمانے پر تجویز کیا جاتا ہے، جو ایک عام قلبی بیماری ہے جس میں بلڈ پریشر کی سطح بلند ہوتی ہے۔ یہ انگیوٹینسن II کے رسیپٹرز پر اس کے عمل کو روک کر خون کی نالیوں کو آرام دیتا ہے، جس سے پیریفرل مزاحمت کم ہوتی ہے اور بلڈ پریشر کم ہوتا ہے۔ لاسارٹن کے ساتھ موثر بلڈ پریشر کنٹرول کرنے سے دل کے واقعات جیسے اسٹروک، دل کا دورہ، اور دل کی ناکامی کا خطرہ کم ہوتا ہے۔

 دل کی ناکامی

لاسارٹن کو کم ایجیکشن فریکشن کے ساتھ دل کی ناکامی کے علاج کے لئے تجویز کیا جاتا ہے، جو ایک حالت ہے جس میں دل کا خون پمپ کرنے کی صلاحیت متاثر ہوتی ہے۔ ایک اے آر بی کے طور پر، لاسارٹن دل کے افعال کو بہتر بنانے میں مدد کرتا ہے، آفٹرلوڈ کو کم کرتا ہے اور دل کے پٹھوں کی خراب تعمیر کو روکتا ہے۔ یہ سانس کی تنگی، تھکن، اور مائع کی برقرار رکھنے جیسے علامات کو دور کرتا ہے، جس سے زندگی کی کیفیت میں بہتری آتی ہے اور ہسپتال میں داخل ہونے کا خطرہ کم ہوتا ہے۔

 ذیابیطس نیفروپیتھی (گردوں کی بیماری)

لاسارٹن نے ذیابیطس نیفروپیتھی کے علاج میں مؤثر ثابت کیا ہے، جو ذیابیطس کا ایک عام پیچیدگی ہے جس میں گردے کی خرابی اور پروٹینیوریا (پیشاب میں زیادہ پروٹین) شامل ہیں۔ بلڈ پریشر کو کم کرکے اور گردے کی خرابی کی پیش رفت کو روک کر، لاسارٹن گردوں کے فنکشن کو محفوظ رکھنے میں مدد کرتا ہے اور ٹائپ 2 ذیابیطس میلیٹس اور پروٹینیوریا والے مریضوں میں آخری مرحلے کی گردے کی بیماری کے آغاز کو مؤخر کرتا ہے۔

دل کا دورہ کے بعد تحف

بعض صورتوں میں، لاسارٹن ان مریضوں کے لئے تجویز کیا جاتا ہے جنہوں نے دل کا دورہ (مائیوکارڈیل انفارکشن) کا سامنا کیا ہے۔ یہ مستقبل کے قلبی واقعات کے خطرے کو کم کرنے اور نتائج کو بہتر بنانے میں مدد کر سکتا ہے، دل کے افعال کو مستحکم کرتا ہے، دل کے پٹھوں کی خراب تعمیر کو روکتا ہے، اور بلڈ پریشر کو کم کرتا ہے۔

 بائیں وینٹریکلر ہائپر ٹرافی

لاسارٹن بائیں وینٹریکلر ہائپر ٹرافی  کے علاج کے لئے بھی استعمال کیا جا سکتا ہے، جو بلڈ پریشر کے بڑھتے ہوئے دباؤ کے جواب میں دل کی بائیں وینٹریکل کی دیوار کے موٹائی کی حالت ہے۔ بلڈ پریشر کو کم کرکے اور مائیوکارڈیل تعمیر کو روک کر، لاسارٹن  کو کم کرنے اور متاثرہ افراد میں دل کے فنکشن کو بہتر بنانے میں مدد کرتا ہے۔

اسٹروک کی روک تھام

لاسارٹن کو ان مریضوں میں اسٹروک کی روک تھام کے لئے ایک جامع حکمت عملی کے حصے کے طور پر بھی غور کیا جا سکتا ہے جو ہائی بلڈ پریشر یا اسٹروک یا عارضی اسکیمی حملہ کی تاریخ رکھتے ہیں۔ بلڈ پریشر کو کم کرنے اور خون کی نالیوں کے فنکشن کو بہتر بنانے کی صلاحیت کے ساتھ، لاسارٹن اسٹروک اور اس کی پیچیدگیوں کے خطرے کو کم کرنے میں مددگار ثابت ہو سکتا ہے۔

Side Effects

Losartan potassium can cause mild or severe side effects. Here are some side effects include:

Common Side Effects of Losartan:

• Upper Respiratory Infections: Like the common cold, you might experience a stuffy or runny nose.
• Dizziness: Feeling lightheaded or unsteady.
• Back Pain: Discomfort or pain in the back.
• Diarrhea: Loose or watery stools.
• Fatigue: Feeling tired or lacking energy.
• Low Blood Sugar: Might experience symptoms like shakiness, sweating, or confusion.
• Chest Pain: Any discomfort or tightness in the chest.
• High or Low Blood Pressure: Losartan affects blood pressure so levels might fluctuate.

Serious Side Effects of Losartan:

• High Potassium Blood Levels: This can lead to heart rhythm issues, muscle weakness, or a slow heart rate.
• Allergic Reactions: Look out for swelling of the face, lips, throat, or tongue, which can be signs of a serious allergic reaction.
• Low Blood Pressure: Feeling faint or dizzy could indicate low blood pressure.
• Kidney Disease: Swelling in the feet, ankles, or hands might suggest a problem with the kidneys.

If you experience any serious side effects, seek medical attention promptly. It’s essential to communicate any concerns or symptoms with your doctor or pharmacist for proper guidance and management.

Dosage

The dosage of Losartan potassium varies depending on the individual’s medical condition and response to treatment. Here’s a general guideline:

Hypertension (High Blood Pressure):

• The typical starting dose for adults is usually 50 milligrams (mg) once daily.
• Your doctor may adjust the dosage based on your blood pressure response, up to a maximum of 100 mg per day.

Heart Failure:

• The starting dose for heart failure is typically lower, around 25 mg once daily.
• Your doctor may gradually increase the dose up to 50 mg once daily, depending on your response.

Diabetic Nephropathy (Kidney Disease):

• The usual dose for diabetic nephropathy is 50 to 100 mg once daily.
• Dosage adjustments may be necessary based on kidney function and other factors.

Post-Myocardial Infarction (Heart Attack) Protection:

• The recommended starting dose after a heart attack is 50 mg once daily.
• Your doctor may increase the dose to 50 mg twice daily based on your response.

Always follow your doctor’s instructions regarding dosage, and do not adjust the dose without consulting them first. Taking more than the prescribed dose can increase the risk of side effects while taking too little may not effectively control your condition. It’s essential to take Losartan regularly, preferably at the same time each day, to maintain stable blood levels and maximize its effectiveness in managing your condition.

Losartan Potassium Interactions

Drugs:

• Potassium supplements or potassium-sparing diuretics: increased risk of hyperkalemia (high potassium levels)
• Lithium: increased risk of lithium toxicity
• Nonsteroidal anti-inflammatory drugs (NSAIDs): decreased antihypertensive effect
• Diuretics: increased risk of hypotension (low blood pressure)
• Angiotensin-converting enzyme (ACE) inhibitors: increased risk of hypotension and hyperkalemia
• Calcium channel blockers: increased risk of hypotension
• Beta-blockers: increased risk of hypotension.

Food:

• High potassium foods: increased risk of hyperkalemia (e.g., bananas, leafy greens, legumes)
• Salt substitutes containing potassium: increased risk of hyperkalemia.

Lab Tests:

• Potassium levels: monitor regularly
• Renal function tests: monitor regularly
• Blood pressure: monitor regularly

Losartan Potassium Warnings

Certainly, here are some important warnings and precautions to be aware of when taking Losartan potassium:

Pregnancy:

Losartan potassium is not recommended during pregnancy, especially during the second and third trimesters. Using Losartan during pregnancy can cause serious harm or even death to an unborn baby.

Kidney Function:

Losartan can affect kidney function, especially in individuals with pre-existing kidney disease. Regular monitoring of kidney function is recommended, particularly if you have kidney problems or are taking other medications that affect kidney function.

Hyperkalemia (High Potassium Levels):

Losartan potassium can increase potassium levels in the blood, especially when used with potassium supplements or salt substitutes containing potassium. This can lead to hyperkalemia, which can be dangerous and may require medical attention.

Hypotension (Low Blood Pressure):

Losartan can cause low blood pressure, especially in individuals who are volume-depleted (e.g., due to diuretic therapy, salt restriction, or dialysis). Use caution when initiating or adjusting the dosage of Losartan in these individuals.

Liver Function:

Losartan potassium may affect liver function, particularly in individuals with pre-existing liver disease. Liver function tests may be recommended before starting Losartan and periodically during treatment.

Heart Failure:

Losartan may not be suitable for all individuals with heart failure. It’s essential to discuss your medical history and condition with your doctor before starting Losartan for heart failure management.

Allergic Reactions:

Allergic reactions to Losartan, though rare, can occur. Seek medical attention immediately if you experience symptoms such as swelling of the face, lips, throat, or tongue, or difficulty breathing.

Interactions:

Losartan interact with other medications, supplements, or substances, potentially altering their effects or increasing the risk of side effects. Inform your doctor about all medications and supplements you are taking before starting Losartan.

Losartan potassium brands in Pakistan

In Pakistan, Losartan potassium is available under various brand names. Some common brand names of Losartan potassium in Pakistan include:

1. Cozaar (MERCK & CO)
2. Sartan 50mg Tablet (Barrett Hodgson Pakistan)
3. Tansin 50mg (PharmEvo)
4. Lozatin 50mg (Amarant Pharmaceuticals)
5. Xavor 50mg (Ferozsons Laboratories)
6. Qsartan 50mg (High-Q Pharmaceuticals)
7. Aceartin 50mg (Epla Laboratories)
8. Angilock 50mg (Venus Pharmaceuticals)
9. Anhibit 50mg (Medicraft Pharmaceuticals)
10. Bepsar Tablet 25mg (Bepsarol)
11. Eziday Tablet 25mg (WARRICK Pharmaceuticals)
12. Co-Eziday Tablet 50mg-12.5mg (WARRICK Pharmaceuticals)
13. Eziday 100mg Tablet (WARRICK Pharmaceuticals)
14. Losanta 25mg Tablet (Amarant Pharmaceuticals)
15. Corik-H Tablet (Medicraft Pharmaceuticals).