Pyzacar 25mg Pymepharco anti -hypertension (2 blisters x 15 tablets)

Losartan is a competitive, reversible inhibitor of the AT1 receptor. The metabolic substance has the activity of the drug 10-40 times stronger than Losartan, calculated by weight and is a non -competitive, reversible inhibitor of the AT1 receptor. Angiotensin II antagonists also have hemodynamic effects such as ACE inhibitors, but there is no unwanted effect of the common ACE inhibitors are dry cough.

pharmacokinetics

After drinking, Losartan absorbs well and initially metabolized through the liver thanks to the cytochrom P450 enzymes.

Losartan's bioavailability is approximately 33%. About 14% of losartan dose taken into active metabolites. T1/2 of Losartan is about 2 hours, and of metabolites about 6 - 9 hours. The average peak concentration of Losartan reaches within 1 hour, and of the metabolites with activity within 3-4 hours.

both Losartan and active metabolites are highly linked to plasma proteins (> 99%), mainly albumin and not through blood -brain barriers.

Losartan's distribution volume is about 34 liters and of metabolites with activity about 12 liters.

LoSartan's total plasma clearance in the plasma is about 600 ml/min, of the metabolic substance with activity of 50ml/min, the renal clearance is about 75 ml/min and 25 ml/min.

In patients with mild to medium cirrhosis, the area under the curve of Losartan and of metabolites is 5 times higher than the corresponding activity and 2 times compared to patients with normal liver.

Children from 6 - 18 years old:

Elderly:

The starting dose is 25 mg/time/day for patients> 75 years old, usually does not need to adjust the dose in the elderly.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose? If symptoms of hypotension occur, supportive treatment. Both Losartan and metabolites are active, they cannot be removed by hemolysis.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when forgetting a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Do not drink twice as prescribed.

** ALT often returns to normal when stopping treatment.

Notice the unwanted effect when using the drug.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Caution when using

Hypersensitivity: Patients with a history of angioedema (swelling of the face, lips, throat and/or tongue) should be closely monitored.

Hypotension and water/electrolyte balance disorders: Hypotension with symptoms, especially after the starting dose or after increasing the dose, may occur in patients with a decrease in the volume of circulatory or hypoglycatic hematuria due to high doses of diuretics, salt low diet, vomiting or diarrhea. These conditions should be controlled before treatment with Losartan potassium, or should use the starting dose lower than the usual dose. This is also cautious in chestnuts from 6 to 18 years old.

Electrolyte disorders: Common in patients with renal failure, with or without diabetes. In a clinical study conducted in patients with diabetic diabetic diabetes 2, the treatment group with Losartan potassium has a higher rate of hyper -potassium hyperkemia than a placebo group. Therefore, plasma potassium concentration and creatinine clearance should be closely monitored in patients with heart failure, with creatinine clearance from 30 - 50ml/min. Do not simultaneously use potassium iOSartan with potassium -saving dtered, supplements and replacement containing potassium.

Losartan is indicated at lower doses than the common doses used for patients with a history of liver failure. Contraindicated in patients with severe liver failure and children with liver failure.

As a result of inhibiting the Renin - Angiotensin system, there has been reports on renal function changes, including renal failure (especially in patients with renal function dependent on the Renin - Angiotensin - Aldosteron system as patients with severe heart failure or renal dysfunction). Losartan potassium as well as other drugs on the Renin - Angiotensin - Aldosteron system can increase blood urea and serum creatinine in patients with kidney stenosis on both sides or kidney stenosis in patients with a single kidney. Therefore, it is necessary to be cautious when using Losartan Kali in the above patient group. These renal function changes can recover when stopped. Kidney function should be monitored during the treatment process, especially in patients who are having kidney function (such as fever, dehydration). Do not simultaneously use Losartan potassium and ACE inhibitors, due to increased renal function impairment.

No experience in using drugs in kidney transplant patients.

Patients with primary Aldosteron powerlessness do not respond to drugs to treat hypertension through inhibition of the Renin - Angiotensin system. Therefore, do not indicate Losartan for this patient group.

Like other medications for hypertension, Losartan Kali reduces excessive blood pressure in patients with ischemic heart disease and cerebrovascular disease, which can cause myocardial or mutant infarction. Inexperienced in using Losartan in patients with heart failure and at the same time severe renal failure, patients with severe heart failure IV (NYHA), as well as patients with heart failure and arrhythmia threatening symptoms. Therefore, be careful when using Losartan Kali in this patient group. Be cautious when coordinating simultaneously Losartan potassium and beta - adrenergic blockers.

Be cautious when indicating Losartan potassium in patients with aortic stenosis or mitral valve, obstructive hypertrophy of myocardial disease.

In the drug with lactose excipients, so patients have rare genetic problems that are not nap galactose, deficiency of lactase enzymes or malcose - galactose should not be used.

Dual inhibition of Renin - Angiotensin - Aldosteron (RAAS): There is evidence that combining ACE inhibitors, Angiotensin II and Aliskiren receptor antagonists increases the risk of lowering blood pressure, hyperkalemia and impaired renal function (including acute renal failure). Recommendations should not be used simultaneously. In case of need to be treated with the RAAS dual inhibitor regimen, it is necessary to closely monitor kidney, electrolyte and blood pressure. Ace ACE and Angiotensin II should not be used simultaneously in patients with diabetic kidney disease.

The ability to drive and operate machinery

There has been no research on the effect of the drug on the ability to drive and operate machinery. However, the drug may have a dizzy side effect, so it is necessary to consult a doctor if there is a driving and operating machinery.

Pregnancy

Use drugs that act on the Renin - Angiotensin system in the middle and the last three months of pregnancy can cause damage and death in infants. The use of drugs only in the first three months of pregnancy has not been related to the risk of the fetus, but anyway when detecting pregnancy, Losartan must be stopped as soon as possible.

Breastfeeding period

It is unknown whether Losartan is secreted into breast milk or not. Due to harmful potential for breastfeeding children, they must decide to stop breastfeeding or stop the drug, depending on the importance of the drug for the mother.

Drug interaction

Losartan oral with cimetidine increases the area under the curve (AUC) of Losartan by about 18%, but does not affect the pharmacokinetics of losartan's active metabolites.

Losartan oral with phenobarbital reduces about 20% of Losartan and of active metabolites.

Other hypertension drugs may increase the hypotension effect of Losartan. Simultaneously used with 3 -round antidepressants, psychotic drugs, Baclofen and amifostin may increase the risk of hypotension.

Losartan is metabolized mainly by CYP2C9 into carboxy metabolites - Active acids. In a clinical trial shows that fluconazole (CYP2C9 inhibitor) reduces the concentration and time of metabolic exposure of about 50%. Simultaneous treatment of losartan and rifampicin (CYP2C9 induction) reduces the concentration of active metabolites in plasma by about 40%. The above interactions are unclear in terms of clinical. There is no difference in concentration and contact time of the active metabolites of losartan when treated simultaneously with fluvastatin (weak inhibitor CYP2C9).

Do not simultaneously use Losartan with drugs that keep potassium (such as potassium -saving diuretic: Amilorid, triamteren, spironolacton), potassium -increasing drugs (such as heparin) or supplements and replacement substitutes containing potassium, as it can increase serum potassium level.

Should closely monitor serum lithium concentration when combining lithium salts with losartan.

Combining Angiotensin II receptor anti-receptor drugs with nonsteroidal anti-inflammatory drugs (NSAIDs) (selective inhibition of COX-2, acetylsalicylic acid anti-inflammatory doses and NSAIDs are not selective) can reduce the effect of lowering blood pressure. Simultaneous use of Angiotensin II receptor antagonists or diuretics with NSAIDs can impair kidney function, including acute renal failure, increased serum potassium concentration, especially in patients who have impaired renal function in advance. This combination needs to be cautious, especially in the elderly. Patients need to be fully rehydrated and monitoring the kidney function after the beginning of treatment and periodic treatment.

Clinical data shows that double inhibition RAAS through a combination of ACE inhibitors, Angiotensin II and Aliskiren receptor drugs, increases the frequency of hypotension, hyperkalemia and impaired kidney function (including acute renal failure) compared to single Raas inhibitors.