Cozaar drug 100mg MSD treats hypertension (3 blisters x 10 tablets)
Dosage form Box of 3 blisters x 10 tablets
Specifications Losartan
Ingredient Coronary artery disease, heart failure, high blood pressure
Ingredient
| Composition information | Content |
| Losartan | 100mg |
Uses
indications
Cozaar 100 drugs are indicated in the following cases:
Angiotensin II also stimulates smooth muscle cell proliferation. Biological tests of cohesion and pharmacological pharmacology have shown that Losartan is selected to the AT1 receptor. Through in vito and in vivo, both Losartan and carboxylic acid metabolites with pharmacological activity (E-3174) will inhibit all the physiological effects mentioned above of Angiotensin II, regardless of the origin or synthetic path of Angiotensin II.
When using Losartan, the negative response of Angiotensin II for renin secretion will no longer exist, leading to increased renin activity in plasma and eventually increasing the angiotensin II in plasma. Despite increased concentration of these substances, the effect of lowering blood pressure and keeping the concentration of Aldosteron is not high in plasma is still maintained, proving the effective inhibiting the Angiotensin II receptor.
Losartan is selectively attached to the AT1 receptor, which does not attach or inhibit other hormone receptors or important ion channels in the cardiovascular regulation.
Moreover, Losartan does not inhibit the enzyme transferring Angiotensin (ACE) (Kininase II), which is bradykinin decomposition. Therefore, what effects are not related to AT1 receptor inhibition, such as Bradykinin intermediaries or edema effects (1.7%Losartan; Placebo 1.9%) does not occur when using Losartan.
Losartan inhibits response to angiotensin I and II without affecting the response to Bradykinin, which is suitable for the specific mechanism of action of Losartan.
In contrast, the ACE inhibitors switch to the response to angiotensin I and increase the response to Bradykinin without inhibiting response to angiotensin II. This is the difference in pharmacological resources between Losartan and ACE transfer inhibitors.
In a specially designed study to evaluate the cough ratio in patients with Cozaar 100 compared to patients with ACE transferred inhibitors, the cough ratio in Cozaar 100 users or the Hydrochlorothiazide group is equal and significantly lower than in the ACE MEN -inhibitor group.
In addition, an integrated analysis from 16 clinical trials designed in double over 4,131 patients shows that the cough ratio according to the voluntary report in patients using Losartan (3.1%) is similar to that in patients using Placebo (2.6%) or hydrochlorothiazide (4.1%), while the cough ratio when using ACE inhibitors is 8.8%.In patients with hypertension without diabetes and proteinuria, Losartan significantly reduces proteinuria, reduces albumin and IgG. Losartan maintains glomerular filtration and reduces the filter volume. In general, Losartan reduces uric acid in serum (usually
Losartan has no effect on plant neurological reflexes and does not have a long -term effect on plasma norepinephrine.
For patients with left ventricular failure, dose of 25 mg and 50 mg Losartan causes positive effects on hemodynamics and nerves, characterized by an increase in the heart index and decreased pulmonary capillary pressure, body blood vessels, average body blood pressure, heart rate and decrease in respectively aldosteron and norepinephrine in the blood. Hypotension in people with heart failure depends on the dose.
In clinical studies, using Cozaar 100 once a day in patients with mild and moderate hypertension has reduced the significance of diastolic and systolic blood pressure; Hypotension effects are maintained up to one year in clinical studies. Measuring blood pressure at the bottom of the bottom (24 hours after taking the drug) compared to the peak (5-6 hours after taking the drug) proved that the blood pressure is reduced stable over 24 hours.
Hypotension effects corresponding to blood pressure biology. The effect of reducing blood pressure at the end of the dose is about 70-80% of the effect achieved after the drug 5-6 hours. Stop using Losartan in people with hypertension does not cause blood pressure to rise suddenly again. Despite the significant reduction of blood pressure, using Cozaar 100 has no clinical effects on the heart rate.
Take Cozaar 100, once a day, will cause more obvious hypotension than Captopril 50-100 mg, once a day.
The hypotension effect of cozaar 100 days of drinking can be comparable equivalent to Atenolol 50-100 mg, taken once a day. The effect of cozaar 100, drinking once a day is equivalent to felodipin release 5-10 mg in elderly patients with hypertension (≥65 years) after 12 weeks of treatment.
Cozaar 100 is also equivalent to use in men as well as women, in young people (
When combined with the diuretics of Thiazide, Cozaar 100 has a combination of energy to lower blood pressure.
Dynamic pharmacokinetics
absorption
After drinking, Losartan absorbs well and through the first metabolism that creates carboxylic acid metabolites and is active and other non -active metabolites. The whole body of Losartan tablets is about 33%.
The average peak concentration of Losartan and of the active metabolites is achieved after one hour (with Losartan) and 3-4 hours (with metabolites).
There is no clinical effect on losartan concentration in plasma, when taking the drug with normal meals.
distribution
Both Losartan and metabolites have an activity attaching ≥ 99% to plasma proteins, mainly on albumin.
Losartan's distribution volume is 34 liters. Research on rats shows that Losartan through a very poor brain barrier, may not be over.
transformation
About 14% of the intravenous or oral dose of Losartan is converted into biological metabolites. After drinking and intravenously Losartan Kali marked by 14C, the cycle marked in plasma is mainly losartan and active metabolites.
The minimum metabolism of Losartan into an active metabolite is about 1% of researchers.
In addition to active metabolites, there are also non-active metabolites formed, including two main substances created by the Butyl branch hydroxylation and an auxiliary metabolic substance, N-2 Tetrazole Glucuronide.
Elimination
Losartan's plasma purification is 600 ml/min, of the active metabolites of 50 ml/min.
Losartan's kidney purification is about 74 ml/min and the metabolic substance is active of 26 ml/min.
When using Losartan by oral, about 4% of the dose will be excreted intact through the urine and about 6% of the dose will be through urine in the form of active metabolites.
pharmacokinetics of Losartan and of metabolites are linear with oral dose of Losartan Kali to 200 mg.
After drinking, the concentration of Losartan and of the metabolites is active in plasma decreases according to multi -exponential functions with the final waste time about 2 hours (with Losartan) and 9 hours (with metabolites).
With a daily dose of 100 mg, both Losartan and metabolites are also active, not significant accumulation in plasma.
Losartan and metabolites are discharged through bile and urine. After taking a dose of Losartan marked with 14C, about 35% of the markers found in the urine, 58% found in feces.
Patient characteristics
In patients with mild and moderate cirrhosis due to alcoholism, Losartan concentration and of plasma metabolites are 5 times higher (with Losartan) and 1.7 times (with metabolites) compared to healthy volunteers after taking medicine.
Can not remove Losartan and metabolites that are active from the body by hemolysis.
Before taking Cozaar drug 100mg MSD treats hypertension (3 blisters x 10 tablets)
How to use
Cozaar 100 film tablets for oral.
Can drink cozaar 100 when hungry or full.
Can take Cozaar 100 with other hypertension medications.
Dosage
conventional dose for hypertension treatment:
The normal starting dose for patients with heart failure is 12.5 mg once daily. This dose should be adjusted slowly each week (for example, 12.5 mg daily, 25 mg daily, 50 mg per day, 100 mg per day, to the maximum dose of 150 mg per day per day depending on the patient's tolerance.
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? The most common expression of overdose is hypotension and fast heartbeat; It is also possible to have a slow heartbeat due to sympathetic nerve stimulation (vagus nerves). If symptomatic hypotension occurs, it is necessary to take supportive treatments.
Cannot remove Losartan or metabolites that are still active of Losartan by dialysis.
What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.
Side Effects
When using Cozaar 100, you may experience unwanted effects (ADR).
Common, ADR> 1/100
Muscle muscle: back pain, cramps, dizziness, headache, insomnia.
rare, 1/10000
Not determined frequency
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.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Cozaar 100 contraindications in the following cases:
Caution when using
Need to be very cautious when taking drugs for patients in the following cases:
Hypersensitivity:
Hypotension and electrolyte/epidemic imbalance:
Electrolyte imbalance:
Hepatic failure:
kidney failure:
Used in patients with kidney failure:
kidney transplantation:
Cuong Aldosteron Tien Phat:
coronary artery disease and cerebrovascular disease:
heart failure:
Aortic stenosis and narrow valve stenosis, hypertrophic cardiomyopathy:
excipients:
Warning and caution:
Double inhibition of the renin-ankiotensin-aldosteron (RAAS):
Use for children:
Babies have a history of cozaar 100 exposure in the uterus:
If urinary or hypotension occurs, pay directly on blood pressure support and kidney perfusion.
may need to replace blood or fertilize as a measure to reverse hypotension and/or instead of kidney function.
The hypotension effect of Cozaar 100 in children from> 1 month to 16 years old with hypertension has been proven.
Using Cozaar 100 in these age groups has been strengthened by evidence from good and appropriate control studies on children and adults using Cozaar 100 as well as by literature about drug use in children.
Losartan's pharmacokinetic properties have been studied over 50 children from> 1 month to
Losartan's pharmacokinetic properties and metabolites are similarly active in age groups that are studied and suitable for the pharmacokinetics of the drug in adults.
In a clinical study, there are 177 patients from 6 to 16 years old with hypertension, children weigh from ≥ 20 kg to
Response the dose of Losartan is recorded in all subgroups (for example, age, puberty stages according to the tanner, gender, race). However, the lowest dose studied is 2.5 mg and 5 mg, corresponding to the daily dose daily 0.07 mg/kg, seems to not bring stable hypotension effect. In this study, Cozaar 100 is well tolerated.
For children who can swallow the tablet, the recommended dose is 25 mg once a day in patients severely ≥ 20 kg to 50kg, the starting dose is 50 mg, once a day. Can increase the dose to up to 100 mg, once a day.
On the patients, there is a decrease in the volume of circulating, it is necessary to adjust this condition before using Cozaar 100.
Harmful reactions occur in children when using the drug is similar to the observed reactions in adults.
Do not recommend the use of cozaar 100 in patients with glomerular filtration
Used for the elderly:
Race:
Based on the study of the effect of reducing blood pressure when intervention with Losartan (Losartan Intermedion for Endpoint Reduction in Hypertension (Life), the benefit reduces the incidence and mortality due to cardiovascular disease in patients with cozaar 100 compared to the atenolol group that cannot be applied to black skin hypertension patients with hypertension, both effectively wearing both black and hypertension on these two groups of black skin patients with these two groups of black and hyperplasia on the two groups of black black patients with these two groups of black and hyperplasia in these groups of black black skin patients with these groups of black skin patients with these groups of black skin patients with these groups. are the same.
For the general population of the Life study (n = 9.193), Cozaar 100 reduces 13.0% of risk (P = 0.021) compared to the use of Atenolol for the main criterion of coordinating cardiovascular death events, stroke and myocardial infarction.
In this study, Cozaar 100 reduced the risk of cardiovascular disease and cardiovascular death compared to the use of Atenolol for patients who are not in black racial groups, suffer from hypertension with left ventricular hypertrophy (n = 8,660), which are assessed by the main criteria for combination of cardiovascular deaths, stroke, myocardial infarction (P = 0.003). However, in this study, black skin patients treated with Atenolol are less likely to have more coordinated events than the group of black skin patients using Cozaar 100 (P = 0.03).
In the division of black skin patients (n = 533, accounting for 6%of the patient in Life study), there were 29 cases of 263 patients using Atenolol encountered this group of incidents (11%; 25.9 for each 1,000 patients-in-year) and 46 cases among 270 patients using COZAAR 100 (17%; 41.8 for each patient-patient).
The ability to drive and operate machinery
There is no research on impact on the ability to drive and operate machinery has been done. However, when driving or operating machinery, it is important to note that dizziness or drowsiness can sometimes occur when using anti -hypertension therapy, especially when starting treatment or when increasing the dose.
Pregnancy
Medicines directly acting on the Renin-Anotensin system can cause damage and developing pregnancy. When detected pregnancy, must stop cozaar 100 as soon as possible.
Although there is no experience in using Cozaar 100 for pregnant women, studies with Losartan Kali have shown that the injury in the fetus, babies, and death, the mechanism of this influence is thought to be due to the intermediate pharmacological properties that act on the Renin-Anotensin system.
In humans, the fetal kidney perfusion depends on the development of the renin-analiotensin system, starting in the middle of the middle of pregnancy, so the risk of the fetus increases if using COZAAR 100 in the middle of the middle or the last three months of pregnancy.
The use of drugs on the Renin-Anotensin system in the middle and the last three months of pregnancy reduces the kidney function of the fetus, increases disease and death in the fetus and infants.
The amniotic fluid results may be associated with reduced lung production and skeletal deformation in fetus. The possible side effects in newborns include reducing skull production, anuria, hypotension, renal failure and death. When detected pregnancy, must stop cozaar 100 as soon as possible.
These harmful results are often associated with the use of these drugs in the middle and the last three months of pregnancy. Most epidemiological studies survey abnormalities in fetuses after exposure to anti-hypertension drugs used in the first three months of pregnancy, regardless of drugs that affect the renin-angiotensin system with other anti-hypertension drugs. The appropriate management of hypertension in the mother during pregnancy is important to optimize the results for both mother and pregnancy.
In special cases when there is no appropriate replacement treatment for drug treatments that affect the renin-angiotensin system for a separate patient, must notify the mother about the risk that may occur for fetuses.
It is necessary to conduct a mass ultrasound test to assess the environment in the amniotic fluid. Stop using cozaar 100 if observed with amniotic fluid unless this drug is considered a medicine to save life for the mother. The pregnancy test may be appropriate, based on the week of gestational age.
However, doctors and patients should know that amniotic fluid may not show until the pregnancy has been damaged for prolonged irreversible.
Need to closely monitor babies with a history of cozaar exposure 100 in the uterus on manifestations of hypotension, urinary discharge and hyperkalemia.
The period of breastfeeding
It is unclear whether Losartan will be secreted into the mother's milk. Because many drugs are secreted into the mother's milk and due to the potential for adultery effects to breastfeed, decide or stop the drug or stop breastfeeding, consider the importance of the drug for the mother.
Interactive drug
other hypertension medications may increase the hypotension effect of Losartan. Concomitant use with other substances that can cause lower blood pressure as a adverse reaction (such as three -round antidepressants, anti -psychotic drugs, Baclofen and amifostin) can increase the risk of hypotension.
Losartan is mainly converted by Cytochrom P450 (CYP) 2C9 into active carboxy acid conversion. In a clinical trial, fluconazole (CYP2C9 inhibitors) has reduced the concentration of metabolites with an activity of about 50%.
What has been found is the simultaneous treatment of losartan with rifampicin (drug -induced drugs of metabolic enzymes) provides a 40% reduction in plasma metabolic concentration.
unclear clinical significance of this effect. The difference in concentration is not found with the concentration of simultaneous treatment with fluvastatin (weak inhibitor CYP2C9).
Like other drugs Angiotensin II blockers or its effects, simultaneous use with other drugs that keep potassium (for example, potassium diuretics: amilorid, triamteren, spironolacton) or may increase potassium levels (for example, heparin), potassium supplements or salt replacement substances that contain potassium can lead to hyperlemia. Do not use the drug simultaneously.
Increased lachium and toxic lithium concentration has been reported while using simultaneously lithium with enzyme inhibitors.
Very rare cases have also been reported to Angiotensin II receptor antagonists. The simultaneous use of Lithium and Losartan should be done carefully. If this combination proves to be necessary, the recommendation to monitor serum lithium concentration when used simultaneously.
When using Angiotensin II antagonist simultaneously with nonsteroidal anti-inflammatory drugs (NSAID) (i.e., COX-2 inhibitors, acetylsalicylic acid in anti-inflammatory doses and non-selective steroid anti-inflammatory doses), reduced hypotension may occur.
Concentrated Angiotensin II antagonistic drugs or non -steroid anti -inflammatory drugs can lead to an increased risk of kidney function, including acute renal failure that may be encountered and increased serum potassium, especially in patients with poor kidney function before.
Be careful when using this combination, especially in the elderly. It should be fully rehydrated for patients and should consider monitoring kidney function after starting treatment simultaneously and periodically later.
Clinical testing data has shown double-analotensin-aldosteron (RAAS) inhibitors by using a combination of enzyme inhibitors, Angiotensin II or Aliskiren receptor blockers that are more involved in adverse frequencies such as hypotension, hyperpoint of blood potassium and reduced kidney function (including acute renal impairment) compared to a effect Renin-Anotensin-Aldosteron.
Storage
Storage below 30 ° C. Store in the original packaging. Avoid light.
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