Agimstan-H 80/25 Agimexpharm treatment for hypertension (4 blisters x 7 tablets)

Telmisartan 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 Telmisartan will prevent all the physiological effects of Angiotensin II and through Aldosteron inhibitors may tend to reduce the loss of potassium -related diuretics.

telmisartan

The chemical structure of Telmisartan belongs to benzimidazol derivatives, no peptides. Telmisartan is a specific antagonist of the Angiotensin II receptor (Typ1) in the smooth and adrenal muscle.

In the renin-ankiotensin system, angiotensin II is made up of angiotensin I thanks to the catalyst of the enzyme transferring Angiotensin (ACE). Angiotensin II is a vasoconstrictor, stimulating synthetic adrenal shells and releasing aldosteron, stimulating heart, aldosteron reduces sodium excretion and increases potassium excretion in the kidneys.

Telmisartan mainly prevents Angiotensin II into the AT1 receptor in the blood vessel and adrenal glands, causing vasodilation and reducing the effects of aldosteron.

In humans, the dose of 80mg Telmisartan inhibits almost completely acting causing hypertension of angiotensin II. Telmisartan dose is over 80 mg/day (to 160 mg/day) does not increase the effectiveness of Telmisartan treatment. Inhibiting effects (hypotension) are maintained for 24 hours and still measures 48 hours after drinking. After taking the first dose, the effect of reducing blood pressure manifests itself slowly within the first 3 hours. Typically, the maximum reduction of arterial blood pressure reaches 4-8 weeks after the treatment. The effect lasts for long -term treatment. In hypertension people, Telmisartan reduces systolic and diastolic blood pressure without changing the heart frequency. Telmisartan's anti -hypertension effect is equivalent to other anti -hypertension drugs.

As well as Angiotensin receptor blockers, Telmisartan shows the effectiveness of reducing the progression of kidney disease or microalbuminuria in patients with diabetes and is recommended to use in this patient group.

Telmisartan is also used in the treatment of congestive heart failure. However, like the Angiotensin II receptor blockers, Telmisartan should only be used for patients who are indicated for enzyme inhibitors but can not be tolerated with the drug (for example, on patients with cough or angiography).

hydrochlorothiazide

hydrochlorothiazid is a drug in the group of thiazid diuretics that increases the secretion of sodium chloride and water attached 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. Hydroclorothiazid also reduces the activity of the carbon dioxide, so it increases the secretion of bicarbonate but this effect is often weak compared to the effect of Cl- excretion 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.

Dynamic pharmacokinetics

Telmisartan

absorption

Telmisartan is rapidly absorbed through the gastrointestinal tract. Absolute oral bioavailability depends on the dose: about 42% after taking the dose of 40 mg and 58% after or taking the dose of 160 mg. The presence of food reduces the bioavailability of Telmisartan (down about 6% when using a dose of 40 mg). After drinking, the highest drug concentration in plasma is achieved after 0.5 - 1 hour.

Distribution

more than 99% of Telmisartan is attached to plasma proteins, mainly on albumin and A1-acid glycoprotein. The attachment to protein is constant, not affected by the change of dose. For example, about 500 liters.

Metabolism

After drinking, Telmisartan is converted into an inactive acylglucuronide.

Elimination

Most given doses (more than 97%) are eliminated in the form of constant biliary tract into the feces, only very small amount (less than 1%) discharged through the urine. Telmisartan waste time is about 24 hours, the peak rate of Telmisartan is about 15-20%.

Telmisartan's pharmacokinetics in children under 18 have not been studied. There is no difference in pharmacokinetics in the elderly and people under 65 years old.

hydrochlorothiazid

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, mostly in the form of non -metabolic. Half of the lifetime of hydrochlorothiazid is about 9.5 - 13 hours, but may last in the case of renal failure so the dose adjustment should 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 - 25 mg/day. It is important to know that the anti -hypertension effect of hydrochlorothiazid is usually optimal at 12.5 mg. Modern clinical treatment and clinical trial guidelines emphasize the lowest and optimal use of doses, 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.

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

Common, ADR> 1/100

Rare, ADR

Dose reduction or stopping 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.

Caution when using

Precautions when appointed Agimstan-H 80/25 for the following patients:

Do Telmisartan

Monitoring blood potassium concentration, especially in the elderly and people with kidney failure. Reduce the starting dose in these patients.

Aortic valve stenosis or mitral valve.

Concerted hypertrophic cardiomyopathy.

Severe congestive heart failure (may be particularly sensitive to changes in the Renin-Anotensin-aldosteron system, accompanied by a decrease in urine, hyper urea, acute renal failure that can cause death).

Dehydration (decreased volume and sodium caused by vomiting, diarrhea, prolonged use of diuretic, separation, salt restriction diet) increases the risk of excessive hypotension. This disorder must be adjusted before taking Telmisartan or reducing the dose and closely monitoring at the beginning of treatment. No contraindication to increase the dose of Telmisartan when there is a transient hypotension, but it is necessary to closely monitor treatment after blood pressure has stabilized (such as increased fluid volume).

Progressive stomach - duodenal ulcer or other stomach disease (increased risk of stomach bleeding).

Mild and moderate liver failure. Precautions in patients with bile clogged due to drugs are excreted through bile and reduce the clearance of the liver.

Kidney artery stenosis.

Mild and medium renal function.

Be cautious when used for patients with a history of angioedema or not related to enzyme inhibitors or Angiotensin II receptor blockers.

Telmisartan can cause porphyrin metabolism disorders, so it is only used when there are no other safer drugs to replace and be cautious in serious patients.

Due to hydrochlorothiazid

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

Hypotenoidal effect of hydrochlorothiazid increases in patients after sympathetic nerve removal.

hyperka cholesterol and triglycerides in the blood.

Attention when taking drugs in the elderly because it is easy to imbalance electrolytes.

The ability to drive and operate machinery

as well as for other anti -hypertension drugs, should be cautious if used when driving or operating machinery due to drugs can cause headaches, dizziness, fatigue, especially when starting treatment or when increasing dose.

Pregnancy

Contraindicated to use Agimstan -H 80/25 for pregnant women because the drug is directly acting on the Renin - Angiotensin system that can harm the fetus: lowering blood pressure, renal failure with recovery or non -recovery, reducing the production of skull bone in infants, causing pregnancy or infants. Little amniotic fluid in the mother (may be due to the reduction of the kidney function of the fetus) in combination with spastic spasm, deformed face and pulmonary lungs have been informed. When detecting pregnancy, this drug must be stopped as soon as possible.

The period of breastfeeding

It is not known whether Telmisartan will be secreted into breast milk, 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.

Interactive drug

with other anti-hypertension drugs: The hypotension effect of Agimstan-H 80/25 may increase when used with other anti-hypertension drugs. Do not use Aliskiren combination with Agimstan-H 80/25 in diabetic patients or renal failure (CLCR

Medicines affecting potassium: The impact of potassium loss of hydrochlorothiazid is reduced due to the potassium retention effect of telmisartan. 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). On the contrary, when used with potassium -keeping diuretics, potassium supplements, salt -containing substances containing potassium or other potassium -causing drugs may increase the effect of hyperkalemia of Telmisartan.

Lithi: Telmisartan increases serum lithium concentration, in addition to lithium renal clearance reduced by thiazid. Should be cautious when shared lithium and Agimstan-H 80/25 and carefully monitor serum lithium concentration.