Cozaar 50 mg Tablets

Brand Name

This medication is marketed under the trade name Cozaar, a name well-known among clinicians for its cardiovascular applications.

International Nonproprietary Name (INN)

The active ingredient is identified globally as losartan, ensuring consistent recognition across medical systems worldwide.

Form of Release

The drug is offered as film-coated tablets, designed for oral use with varying strengths to meet individual treatment needs. This tablet form ensures ease of administration and stability under standard conditions.

Composition

Losartan potassium forms the core active substance, engineered to target specific physiological processes. Supporting this are excipients like microcrystalline cellulose, lactose monohydrate, magnesium stearate, and pregelatinized starch, which maintain tablet integrity and aid dissolution. The film coating, typically hydroxypropyl cellulose and titanium dioxide, improves swallowability and shields the active component from degradation. These ingredients are chosen to enhance losartan’s delivery and effectiveness.

Pharmacologic Properties

Pharmacodynamics

This medication functions as an angiotensin II receptor blocker (ARB), targeting the AT1 receptor to manage blood pressure and fluid levels. It blocks angiotensin II, preventing vessel constriction and aldosterone secretion, which relaxes blood vessels and reduces sodium retention. This lowers blood pressure and eases cardiovascular strain, making it effective for hypertension and organ protection. Effects start within hours, peaking over weeks with regular use. Losartan’s selective action minimizes disruption to other hormonal systems, enhancing its tolerability.

Pharmacokinetics

After oral intake, the drug absorbs from the digestive tract, with bioavailability around 33% due to initial liver metabolism. Food has little impact on uptake, allowing dosing flexibility. Losartan transforms in the liver via cytochrome P450 enzymes into an active metabolite, EXP3174, which drives much of its extended effect and peaks in plasma within three to four hours. It distributes broadly, binding about 98% to proteins, reaching tissues like the kidneys and heart. Elimination splits between urine (35%) and feces (60%), with losartan’s half-life at two hours and its metabolite’s at six to nine hours. Renal or liver issues may prolong these times, requiring oversight.

Indications for Use

The medication addresses several conditions linked to cardiovascular and kidney health. It effectively treats hypertension, lowering high blood pressure across diverse patients. It’s also used for heart failure, especially in those unable to take ACE inhibitors, supporting heart function and easing symptoms. In type 2 diabetes with proteinuria, it slows diabetic nephropathy progression by reducing glomerular pressure and protein loss. Additionally, it may reduce stroke risk in hypertensive patients with left ventricular hypertrophy, highlighting its wide-ranging protective benefits.

Contraindications

Certain conditions bar the use of this drug to avoid serious risks. Hypersensitivity to losartan or tablet ingredients prohibits it, as reactions could range from rashes to anaphylaxis. Severe liver impairment limits its use, as metabolism slows, risking buildup. It’s contraindicated in pregnancy, especially in later trimesters, due to potential fetal harm like renal issues or death. Combining it with aliskiren in diabetics is forbidden, as this raises renal and hypotension risks. Bilateral renal artery stenosis also rules it out, as reduced kidney blood flow could worsen function.

Method of Administration and Dosage

How to Take

Tablets are taken orally, with or without food, offering flexibility in daily schedules. Swallowing them whole with water ensures proper stomach delivery. Consistent timing each day maintains stable levels.

Dosage for Adults and Children

Adults with hypertension typically start at 50 mg once daily, adjusting to 25 mg or 100 mg based on response, with 100 mg as the usual cap. For heart failure, 12.5 mg daily is common initially, titrated to 50 mg if tolerated. In diabetic nephropathy, 50 mg daily may rise to 100 mg depending on proteinuria control. Children aged six and up with hypertension begin at 0.7 mg per kilogram daily, up to 50 mg, adjusted by weight and pressure under specialist care.

Dose Adjustment in Specific Conditions

Renal impairment usually needs no change unless severe, though hyperkalemia monitoring is wise in advanced cases. Liver dysfunction suggests a lower start, like 25 mg daily, due to slower metabolism. Elderly or volume-depleted patients may also begin lower to avoid steep pressure drops. Dosing should be tailored with regular checks to ensure safety and efficacy.

Side Effects

The medication may cause various unintended effects, mostly mild and short-lived. Dizziness or lightheadedness, tied to pressure decreases, is common, especially early on. Fatigue or headaches can occur but often fade with time. Hyperkalemia might develop, leading to muscle weakness or heart rhythm changes, notably in renal patients. Upper respiratory issues or congestion are reported, though links are uncertain. Rare severe reactions, like angioedema—swelling of the face or throat—or notable kidney decline, need urgent care. Routine evaluations help spot and manage these promptly.

Overdose

Symptoms of Overdose

Taking too much can cause significant hypotension, leading to dizziness, fainting, or circulatory failure from excessive vessel relaxation. Tachycardia might occur as compensation, though bradycardia is possible. Hyperkalemia could bring muscle cramps or heart irregularities, posing risks if ignored. Symptoms emerge within hours and worsen without action, reflecting strong vascular effects.

First Aid Measures

Stop the drug immediately in an overdose and seek prompt medical help. Recent ingestion may warrant activated charcoal under supervision to curb absorption. IV fluids can address low pressure, while heart and potassium monitoring corrects imbalances. Dialysis rarely removes losartan but may aid severe renal cases. Focus is on restoring pressure and organ function quickly.

Drug Interactions

Effects on Other Medications

This drug can influence other medications when used together. It may boost antihypertensive effects, risking sharp pressure drops, needing dose tweaks. NSAIDs might lessen its impact and stress kidneys, a concern over time. Potassium-sparing diuretics or supplements increase hyperkalemia odds, requiring electrolyte checks. Lithium levels could rise, risking toxicity, so plasma monitoring is advised. Effects on antidiabetic drugs are minor but worth watching for glucose changes.

Compatibility with Alcohol and Food

Alcohol might heighten the medication’s pressure-lowering effects, raising dizziness risks, so moderation is wise. Food doesn’t notably affect uptake, though high-salt intake could counter benefits, suggesting balance. Potassium-rich foods like bananas need care to avoid excess potassium.

Special Precautions

Use During Pregnancy and Breastfeeding

The drug is barred in pregnancy beyond the first trimester, as it risks fetal kidney damage or death, per extensive data. It appears in breast milk minimally, so nursing mothers should consult their doctor, possibly opting for alternatives to limit infant exposure.

Impact on Driving and Machinery Operation

Dizziness or fatigue, especially at start or dose shifts, may hinder driving or machinery use. Patients should gauge their response before such tasks, ensuring safety.

Considerations for Elderly and Pediatric Populations

Older adults may begin with lower doses due to potential renal or volume changes, with pressure monitoring. In children six and up, it’s approved for hypertension, with weight-based dosing adjusted carefully to avoid overeffects. Tailored care optimizes results across these groups.