Agilosart-H 100/25 Agimexpharm treatment for hypertension (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Losartan, hydrochlorothiazide
Ingredient Agimexpharm Pharmaceutical Joint Stock Company

Ingredient

Composition information	Content
Losartan	100mg
Hydrochlorothiazide	25mg

Uses

Indications

Agilosart-H 100/25 drugs are indicated in the following cases:

Treatment of idiopathic hypertension in adults, especially cases that do not control blood pressure with one drug. This drug is not indicated for initial treatment in the treatment of hypertension. When needed, Agilosart-H 100/25 can be combined with another anti-hypertension drug.

Pharmacokology

Agilosart-H 100/25 has ingredients of two active ingredients Losartan and hydrochlorothiazide used together in the form of oral dosage daily to control high blood pressure. This effect is thought to be the result of the mutual support effects of both ingredients that help the drug have a synergistic effect in lowering blood pressure, reducing blood pressure better when using each separate ingredient.

Losartan is a specific and selective antagonist on Angiotensin II receptor while hydrochlorothiazid is a thiazid diuretic. Both drugs have an impact on blood pressure. The effectiveness of high blood pressure treatment is often higher when combining a small dose of thiazid diuretics such as hydrochlorothiazid with Angiotensin II receptor antagonist.

Moreover, due to diuretic effects, hydrochlorothiazid increases plasma renin activity, increases aldosteron secretion, reduces serum potassium and increases angiotensin II levels. Using Losartan will prevent all the physiological effects of Angiotensin II and through Aldosteron inhibitors may tend to reduce the loss of potassium associated with this diuretics.

So the use of Losartan and hydrochlorothiazid combines increases the effect of anti -blood pressure of the drug, this effect is maintained for 24 hours, so it only needs to take it once a day.

losartan

Losartan is the first substance of the new anti -hypertension drug group, which is a receptor antagonist (Typ1) Angiotensin II.

Angiotensin II formed from angiotensin I in the reaction of the enzyme switching angiotensin (ACE) catalyzed, is a strong vasoconstrictor, which is the main vascular activation hormone of the Renin - Angiotensin system and is an important component in the pathophysiology of hypertension. Angiotensin II also stimulates the adrenal glands of Aldosteron.

Losartan and main metabolites have a clogging and aldosteron secretion of angiotensin II by preventing Angiotensin II selective, not attached to the AT1 receptor contained in many tissues (for example, blood vessel muscles, adrenal glands). Both Losartan and the main active metabolites do not show the local dominant effect in the AT1 receptor and have the affinity for the AT1 receptor, much larger (about 1,000 times) than the AT2 receptor.

Losartan is a competitive, reversible inhibitor of the AT1 receptor. The metabolic substance has the activity of drugs 10 to 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.

hydrochlorothiazide

hydrochlorothiazid is a drug in the group of thiazid diuretics that increases the secretion of sodium chloride and is accompanied by the mechanism of inhibiting the reabsorption of sodium and chlorine ions in the distance. The excretion of other electrolytes also increases, especially potassium and magnesi, and calcium decreases. Hydrochorothiazid also reduces the activity of the carbon dioxide should increase the secretion of bicarbonate but this effect is common compared to the effect of cloic secretion and does not significantly change the urine pH. Thiazid diuretics may also reduce the filtration rate of the glomerular. Thiazids have a moderate diuretic effect, because about 90% of sodium ions have been reabsorbed before arriving in the distance is the main position of the drug.

hydrochlorothiazid has the effect of lowering blood pressure, firstly due to a decrease in plasma volume and extracellular fluids related to sodium urine. Then, during the use of the drug, the effect of lowering blood pressure depends on the decrease in peripheral resistance, through the gradual adaptation of blood vessels from the reduction of Na+concentration. Therefore, the hypotension effect of hydrochlorothiazid is shown slowly after 1-2 weeks, while the diuretic effect occurs quickly and can be seen right after a few hours. Hydrochlorothiazid increases the effects of other antihypertensive drugs.

pharmacokinetics

Losartan

After drinking, Losartan absorbs well and initially metabolized through the liver thanks to the cytochrom P450 enzymes (CYP2C9 and CYP3A4). Losartan's bioavailability is approximately 33%. About 14% of losartan dose taken into active metabolites, this substance is mostly opposing the Angiotensin II receptor resistance. Losartan waste sale time is about 2 hours and of metabolites for 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 (> 98%), mainly albumin and they do not pass the brain blood barrier. The distribution of Losartan is about 34 l and of the metabolites with activity about 12L. Losartan's total plasma clearance is about 600ml/minute and of the metabolites with activity of 50ml/min, their clearance in the kidney corresponds to about 75ml/min and 25ml/min.

Losartan eliminates 35% by urine and about 60% in feces.

In patients with mild to medium cirrhosis, the area under the curve (AUC) of Losartan and of the metabolitus has a higher activity, 5 times and 2 times more than in patients with normal liver. Losartan and E-3174 metabolites are not excluded when hemolysis.

hydrochlorothiazide

After taken, hydrochlorothiazid is relatively fast, about 65 - 75% of the dose of use, but this ratio may decrease in heart failure people. Food can reduce the absorption of the drug. Hydrochlorothiazid accumulated in red blood cells. 40 - 68% of the drug is associated with plasma protein. The drug excreted mainly through the kidneys, largely in the form of non -metabolic.

The sale time of hydrochlorothiazid is about 9.5 - 13 hours but may last in the case of renal failure, so the dose adjustments need to be adjusted. Hydrochlorothiazid passes through the placenta, distributed and reached high concentrations in the fetus.

Diuretelli effects appear after drinking 2 hours, reaching maximum after 4 hours and lasting about 12 hours.

Anti -hypertension effect is much slower than diuretic effects and can only achieve adequate effect after 2 weeks, even with the optimal dose between 12.5 - 25mg/day. It is important to know that the anti -hypertension effect of hydrochlorothiazid is usually optimal at 12.5mg.

Modern clinical treatment and clinical trial guidelines emphasize the lowest and optimal use, which reduces the risk of harmful effects. The important issue is to wait enough time to assess the body's response to the hypotension effect of hydrochlorothiazid, because the effect on the peripheral resistance takes time to be clear.

Before taking Agilosart-H 100/25 Agimexpharm treatment for hypertension (3 blisters x 10 tablets)

How to use

Take oral use.

Dosage

Adults

Starting dose and maintenance dose: Take 1/2 single tablets a day.

For people who do not fully meet the dose of 50/125, can increase daily dose to 1 tablet Losartan 100mg/hydrochlorothiazide 25mg.

Maximum dose once a day only 1 tablet Losartan 100mg/ hydrochlorothiazid 25mg. In general, the hypotension effect is achieved within 3-4 weeks after the beginning of treatment.

Do not use this drug in people who lose the volume of circulatory fluid (such as high doses of doses).

Do not recommend the use of this drug for severe kidney failure (creatinine clearance

No need to adjust the initial dose of this drug in the elderly. Do not use losartan 100mg/hydrochlorothiazid 25mg is the starting dose for this patient group.

Used in children and adolescents (

Do not use Losartan/hydrochlorothiazide combination form for children and adolescents because they have not determined the safety and effectiveness of these drugs.

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?

Symptoms

Expression of overdose caused by Losartan. The most common manifestation of overdose is probably hypotension and tachycardia, which may also experience slow heart rate due to sympathetic nervous stimulation (vagus nerve).

Extremely manifestations of hydrochlorothiazid: The main manifestation is water and electrolyte disorders due to a lot of urinary tract. The most common signs and symptoms of overdose are nausea and drowsiness. If using digitalis, hypoglycemia increases arrhythmia.

Overdose

There is no specific information about treatment when overdose of the drug in combination with losartan and hydrochlorothiazid. Treatment methods are symptomatic and support. Need to stop the drug immediately and carefully monitor patients. The proposed measures are vomiting or gastric lavage if you have just taken medicine, use activated carbon, rehydration, electrolyte balancing, liver coma treatment, handling of blood pressure loss according to conventional processes. Elimination by hemorrhage is ineffective.

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 Agilosart-H 100/25, there are often unwanted effects (ADR).

Do Losartan

Most of the unwanted effects because Losartan is light and losing over time.

Common, ADR> 1/100

cardiovascular: lower blood pressure, chest pain Back, leg pain, muscle pain.

Cardiovascular: Hypotension, chest pain, Block A-V degree II, chest drum, sinus slow pace, fast heartbeat, face, blush. bruises, foreign bills. Perception, tremor, bone pain, muscle weakness, joint edema, muscle pain. throat.

Other effects: Sweating.

hydrochlorothiazid may cause excessive potassium loss. This effect depends on the dose and can be reduced when low doses (12.5mg/day), the best dose for hypertension treatment, while minimizing harmful reactions. Diuretics also often causes hypoglycemia.

Common, ADR> 1/100

Systemic: fatigue, dizziness, dizziness, headache.

circulating: Hypotenary pressure posture, arrhythmia.

Rare, ADR

Systemic body: Anaphylaxis reaction, fever.

liver: hepatitis, jaundice in the liver, pancreatitis The posture of hypotension may occur when used with alcohol, anesthesia and sedative.

Instructions on how to handle ADR

Dose or medication reduction when there are unwanted effects.

Excessive treatment of hypotension: Put the patient on your back, if the severe hypotension is necessary to infusion of the physiological saline solution to increase the volume of fluid.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Agilosart-H 100/25 contraindications in the following cases:

Hypersensitivity to Losartan, with thiazids and sulphonamid derivatives or any ingredients of the drug. 25mmol/liter or creatinine clearance ratio Precautions when using

by Losartan

Special monitoring or dose reduction in patients dehydration, diuretics and patients have other factors that can easily lead to hypotension. Patients with kidney stenosis on both sides or one side, only one kidney has a high risk of unwanted effects to increase creatinine and blood urea) and should be closely monitored in treatment.

Due to the risk of hyperkalemia, monitoring of blood potassium in the elderly and kidney failure, not used with diuretics to keep potassium.

Patients with lower doses of liver failure.

Due to hydrochlorothiazid

Due to the drug ingredient with hydrochlorothiazid, the patient must be regularly monitored in serum and urine, especially patients using corticosteroids, acth or digitalis, quinidine (risk of vibration -causing torsion), patients with vomiting or infusion.

Severe kidney failure: increased blood urea and may impair renal function.

Hepatic failure: prone to liver coma.

gout: severe illness.

Diabetes: Pay attention to adjust the drug (insulin, hypoglycemic drugs) because the drug can increase blood glucose.

Hypotension effect of hydrochlorothiazid increases in patients after removing sympathetic nerve.

hyperka cholesterol and triglycerides in the blood. Note when taking drugs in the elderly because it is easy to imbalance electrolytes.

The excipients of this drug have lactose: Do not use this drug for patients with rare genetic problems in galactose intolerance, lapp lactase deficiency or glucosegalactose.

The ability to drive and operate machinery

as well as for other anti -hypertension drugs should be cautious if taking the drug while driving or operating machinery because the drug can cause headaches, dizziness, fatigue, especially when starting treatment or when increasing the dose.

Pregnancy

Contraindicated Agilosart-H 100/25 for pregnant women. Using drugs directly on the Renin - Angiotensin system in the middle and the last three months of pregnancy can cause less amniotic fluid, hypotension, anuria, urinary discharge, face deformation and death in infants. Although, the use of drugs in the first three months of pregnancy has not been seen in the risk of the fetus, but when detected pregnancy, it must be stopped as soon as possible.

Breastfeeding period

I don't know if Losartan will be secreted into breast milk or not, but thiazid can be through breast milk. Because of the harmful effects for breastfeeding, it is necessary to decide or stop breastfeeding or stopping the drug, depending on the importance of using the drug with the mother.

Medicinal interaction

with other anti-hypertension drugs: The hypotension of Agilosart-H 100/25 can increase when used with other anti-hypertension drugs.

Medicines affecting potassium: The impact of potassium loss of hydrochlorothiazid is reduced due to the potassium retention effect of Losartan. However, this effect of hydrochlorothiazid on serum potassium is likely to occur when used in combination with other drugs that cause potassium loss and hypokalemia (for example, diuretic secretion of potassium urine, corticosteroid, acth, salbutamol, amphoticin). In contrast, when used with diuretics that keep potassium, potassium supplements, salt substitutes containing potassium or other potassium -causing drugs can increase serum potassium.

Lithi: Losartan increases serum lithium levels, in addition to lithium renal clearance reduced by thiazid. Should be cautious when shared lithium and Agilosart-H 100/25 and carefully monitor serum lithium concentration.

Losartan does not affect the pharmacokinetics of oral or intravenous digoxin.

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

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

rifampicin, aminoglutethimide, carbamazepin, nafcillin, nevirapin, phenytoin, reducing losartan and metabolites in plasma when used simultaneously.

Losartan increases the effect of drugs: amifostin, hypotension drugs, carvedilol, hypoglycemic drugs, lithium, diuretics holding potassium, rituximab.

Anti-inflammatory and pain relievers (NSAID) especially COX-2 used in combination with Losartan can cause kidney failure, so kidney function should be monitored.

Alcohol, barbiturate or addictive sleeping pills: Increasing the potential of hypotension.

Anti -diabetic drugs (oral and insulin drugs): The dose adjustment is needed due to hyperlem of blood glucose.

corticosteroid, ACTH: increase power outages, especially hypokalemia.

Amines of hypertension (eg norepinephrin): may reduce response to hypertension, but not enough to prevent use.

muscle relaxants (eg tuboCurarin): may increase response to muscle relaxants.

Non -steroid anti -inflammatory drugs: may reduce diuretic, sodium urinary and hypotension effect of thiazid in some patients. So if used together, you must monitor to see if it is effective for diuretic.

quinidine: easily causing torsion, vibration causes death.

Reduce the effects of anticoagulants, gout medications.

Increases the effects of anesthesia, glucoside, vitamin D.

cholestyramin or colestipol: The potential to attach thiazid diuretics, reducing the absorption of these drugs through the gastrointestinal tract.

Increases the toxicity of digitalis and increases the risk of arrhythmia with interpreted drugs such as Astemizol, Terfenadin, Halofantrin, Pimozid and Sotalol.

alopurinol, tetracyclin: Increased toxicity when used with thiazid.

Storage

Store in a dry place, avoid light, temperatures below 300C.

Other drugs

Disclaimer

Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.