Esseil-5 Davipharm medicine for hypertension (10 blisters x 10 tablets)

Dosage form Box of 10 blisters x 10 tablets
Specifications Cilnidipine

Ingredient

Composition information	Content
Cilnidipine	5mg

Uses

indicated

Esseil is indicated for hypertension treatment.

Pharmacokology

International name: cilnidipin.

Pharmacological group: Anti -hypertension drugs, antagonists of calcium channels. ATC code: C08CA14.

1. Anti -hypertension effect:

(1) In many different models of hypertension on animals (rats of spontaneous hypertension, rats and dogs hypertension due to kidney blood vessel disease, hypertension due to doca salt and rats with spontaneous hypertension easily stroke), a single -dose of oral cilnidipin shows that the effect of lowering blood pressure is slowly and prolonged at the dose of 1 mg/kg or higher. In contrast, it shows the effect of lowering blood pressure in rats with normal blood pressure.

The effect time does not last when taking an excessive high doses. In hypertension due to kidney blood vessel disease, cilnidipin shows the additional effect when used simultaneously with a beta blockers or enzyme inhibitors angiotensin.

(2) In spontaneous hypertension rats easily stroke and in dog hypertension due to kidney disease, repeated doses of cilnidipin used oral route have a stable antihypertensive effect without reducing decline. Stop using cilnidipine does not cause blood pressure.

(3) In rats, hypertension is awake and is not restrained, cilnidipine does not increase heart rate while hypotension. Cilnidipin does not increase plasma noradrenaline levels while hypotension, nor significantly reduces this concentration as caused by adrenergic guanethidine sulfate. Cilnidipine does not cause hypotension, although pentolinium (pentolinium) has caused in the tilt test (tilt test) using rabbits.

(4) In patients with idiopathic hypertension, a single dose of cilnidipin daily oral use shows that the hypotension effect is maintained in 24 hours and is still pronounced early in the morning. The analysis of the energy spectrum of the R-R interval in the 24-hour electrocardiogram has discovered that Cilnidipine does not increase the sympathetic activity or heart rate in the form of reflex response to lower blood pressure.

2. The above inhibitory effect responds to hypertension caused by stress:

(1) In the rats of hypertension, self -awake and uncontrolled, cilnidipine inhibits hypertension and norepinephrine levels in plasma caused by cold stress. Cilnidipin also inhibits hypertension caused by air jet stress (mental stress) in rats.

(2) In healthy adult male volunteers with 20% or higher blood pressure in cold stress test, Cilnidipin has inhibited hypertension caused by cold stress.

3. The above inhibitor effect responds to hypertension due to sympathetic stimulation:

(1) In spontaneous hypertension rats are poked the spinal cord, cilnidipine inhibits hypertension caused by electrocardiography.

(2) In spontaneous hypertension rats with the intestinal mesenteric artery isolated and infused, Cilnidipin also inhibits the release of norepinephrine caused by electrolyte stimulation.

4. Effect on brain circulation:

(1) In spontaneous hypertension rats, cilnidipine does not reduce the blood flow even when using the dose that reduces blood pressure by 30-40% in mice. The mechanism of self -regulating blood flow is still satisfactorily maintained while blood pressure drops.

(2) In patients with hypertension, it is complicated due to cerebrovascular disease, blood flow is still maintained while blood pressure is reduced.

5. Effects on heart function:

(1) In dogs, cilnidipine reduces heart rate and muscle contraction at higher doses than the dosage causing hypertension of arterial blood.

(2) In that it is anesthetized to open breasts, cilnidipine reduces the consumption of oxygen of the heart muscle at the dose of hypotension. At this time, Cilnidipine does not cause tachycardia, nor does it affect the contractions of the heart.

(3) In patients with idiopathic hypertension, cilnidipine does not affect the heart rate while blood pressure decreases, and in patients with abnormal rate of heart -acute (CTR), Cilnidipine improves the rate of heart - chest.

6. Effects on kidney function:

(1) In the rats of hypothalar hypertension is anesthetized, cilnidipine increases the volume of urine, blood flow through the kidneys and the filtration speed of the glomerular doses at the dose causing hypotension. Cilnidipine also increases the volume of urine, blood flow through the kidneys and the filtration rate of the glomerular when the kidney function is reduced by endothelin.

(2) In patients with idiopathic hypertension, cilnidipine does not affect kidney function while blood pressure is reduced.

7. Effects on cardiovascular disorders associated with hypertension

(1) In the rats of spontaneous hypertension easily stroke, a single dose of cilnidipine daily has prevented the appearance of stroke and improves the survival rate. In addition, Cilnidipin also reduces heart hypertrophy (increased heart weight), thick left ventricular walls, heart muscle fibrosis and kidney damage. Moreover, Cilnidipin also reduces the middle layer of the coronary wall walls and reduces the calcium content in the aorta.

(2) In patients with idiopathic hypertension, cilnidipine reduces atherosclerosis and lipid peroxide in serum.

8. Effective mechanism

(1) Experimental data has shown that cilnidipine is connected to the locations of the dihydropyridine of the calcium channel depending on the Type L voltage and inhibits the Ca2+ inhibitors through the cell membrane of the blood vessel smooth muscle through this channel (in vitro on rabbits). Therefore smooth blood vessel muscle relaxes, causing vasodilation. Through this mechanism, Cilnidipin is considered to have the effect of lowering blood pressure.

(2) Cilnidipin inhibits Ca2+ line coming into the calcium channel depending on the type N voltage in the sympathetic nerve cell membrane. The inhibition of the Ca2+ line entering through the calcium channel depends on the Type N voltage has been observed in a scope of the drug concentration similar to the Ca2+ inhibitor level depends on the Type L (In vitro on the rat).

Therefore, the release of norepinephrine from the beginning of the sympathetic nerve is inhibited. Cilnidipin is thought to inhibit the increase in reflex rate that can be intermediaries through sympathetic activation after reducing blood pressure and inhibiting hypertension associated with stress through this mechanism.

Dynamic pharmacokinetics

absorption

When taking a single dose of Cilnidipin 5 mg, 10 mg or 20 mg oral for 6 healthy volunteers, the highest concentration in plasma (CMAX) is recorded corresponding to 4.7 ng/ml; 5.4 ng/ml and 15.7 ng/ml, and the area under the curve (AUC0-24) corresponding to 23.7 ng.D/ml; 27.5 ng. Thus, both parameters increased in the way of dosage dependence.

When repeating a single dose of Cilnidipin 10 mg, 1 time/day for 6 healthy male volunteers to show that the plasma concentration is achieved in a stable state from the 4th day when taking the drug and no drug accumulation.

The pharmacokinetics of this drug have also been evaluated in patients with kidney failure (serum creatinine: 1.5 - 3.1 mg/dl) after taking a single 10 mg of oral doses in hypertension patients, and there is no significant difference on the dynamic data of this drug compared to data in patients with normal kidney function. The repetition of this medication is taken at a dose of 10 mg, 1 time/day for 7 days in patients with impaired renal function does not cause differences in pharmacokinetic data compared to data in patients with normal renal function.

distribution

cilnidipin binds 99.3% to human serum protein.

metabolism and elimination

Based on the identified metabolites in plasma and urine of healthy volunteers, it is thought that Cilnidipin's main metabolic line is the methyl reduction of methoxyethyl group, followed by the hydrolysis of Cinnamyl ester and oxidation of dihydropyridine. CYP3A4 is thought to be mainly related and CYP2C19 is partly related to the methyl reduction of the methoxyethyl group (in vitro).

The calcium channel blockage effect of metabolic substances has a methoxyethyl group that is reduced to methyl is only 1/100 the effect of the original compound.

When repeating a single dose of Cilnidipin 10 mg, 1 time/day orally for 7 days for men to volunteer healthy, without a constant cilnidipin compound, but 5.2% of the dose is excreted in urine in the form of metabolites.

Before taking Esseil-5 Davipharm medicine for hypertension (10 blisters x 10 tablets)

How to use

oral medication.

Dosage

Adults: Usually dose 5 - 10 mg Cilnidipin oral, 1 time/ day after breakfast. Dosage can be adjusted according to the age and symptoms of the patient. The dose can be increased to 20 mg/time/day if responding to the drug is not enough. Severe hypertension: Take dose 10 - 20 mg oral, 1 time/day after breakfast.

In case of forgetting to take medicine, take medicine as soon as you remember. However, if the time is close to the next dose, abandon the dose has forgotten to drink and continue at the next dose. Do not take double dose to compensate for the forgotten dose.

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?

Handling: If it is significantly reduced blood pressure, it is necessary to take appropriate measures such as improving the lower limb, treating fluid and taking hypertension drugs. Eliminate illness by hemolysis ineffective due to the high ratio of the drug to protein.

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

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

Clinical undesirable reactions.

Disorders of liver and jaundice (unknown frequency)

Disorders of liver and jaundice accompanied by an increase in AST (GOT), ALT (GPT) and (-GTP) may occur. Therefore, it is necessary to monitor closely, if observations see any abnormalities, it is necessary to take appropriate measures such as stopping cilnidipine.

platelet reduction (ratio:

Because platelets can occur, it is necessary to monitor closely, if observations see any abnormalities, it is necessary to take appropriate measures such as stopping cilnidipine.

Other undesirable reactions

If any of the following side effects occurs, it is necessary to take appropriate measures depending on symptoms.

liver (1):

Ratio 0.1 - The ratio of 0.1 - The ratio of 0.1 - The ratio of 0.1 - The ratio of 0.1 - The ratio of 0.1 - The ratio of 0.1 - The ratio of 0.1 -

Instructions on how to handle ADR:

Notify the physician the unwanted effects when using the drug.

Warnings

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

contraindicated

Esseil drugs contraindicated in the following cases:

Patients with hypersensitivity to cilnidipine or any ingredients of the drug.

Be cautious when used

Patients with severe liver dysfunction (plasma concentrations may increase).

Patients with a serious side of side effects with calcium antagonists.

Elderly patients.

Products containing castor oil: There has been an unwanted effect on castor oil, including nausea, abdominal pain and diarrhea.

Castor oils should not be used in case of obstruction or stenosis, loss of force (normal peristalsis in the intestine), appendicitis (a small part associated with the intestine), colitis (lower part of the intestine), abdominal pain that is unexplained and seriously dehydrated. Do not use during pregnancy and lactation.

Be important:

Because there is a report is a sudden stopping of calcium antagonism, several symptoms, so if it is necessary to stop cilnidipine, the dose must gradually reduce the dose under close monitoring.

If cilnidipine stops from a dose of 5 mg/day, it is advisable to take appropriate measures such as replacement with other anti -hypertension drugs.

Must guide the patient constantly this drug without the guidance of a doctor.

used in the elderly

cilnidipin should be used carefully under the closeness of the patient's condition and taking measures such as starting with a lower dose (for example 5 mg).

Should avoid excessive hypotension in the elderly.

Observed the side effects (including experimental results) in the elderly aged 65 and older at 152 out of 2,863 patients in studies using Cilnidipine.

used in children

Not yet determined the safety of cilnidipin in children's patients (without clinical experience).

To be out of reach of children.

Use drugs for women during pregnancy and lactation

Pregnancy

Do not use cilnidipine for pregnant women or women who are likely to be pregnant. There is a report that Cilnidipin extends the pregnancy and childbirth time in experimental animals.

Breastfeeding period

Avoid using this medication for breastfeeding women. If the treatment is necessary, advise patients not to breastfeed. There have been drugs for lactation in milk tests in animals (mice).

The effect of the drug on the ability to drive and operate machinery

Symptoms such as dizziness may occur due to the hypotension effect of this drug.

There is a need for a warning to participate in dangerous activities that need alertness such as working on high, operating machines or motor drivers.

Interactive drug 2>

drug interactions may affect the activity of the drug or cause side effects.

Patients should notify the doctor or pharmacist a list of the drugs and functional foods you are using. Do not use or increase or decrease the dose of the drug without the guidance of a doctor.

Other anti -hypertension drugs:

Symptoms and treatment: Blood pressure may be overreacted.

digoxin:

Symptoms and treatment: There is a report that some calcium antagonists (e.g. nifedipine) increases the concentration of digoxin in plasma. If observations see any signs of toxic symptoms can be attributed to digoxin (e.g. nausea, vomiting, headache, abnormal vision, arrhythmia), appropriate measures must be taken such as adjusting the dose of digoxin or stopping cilnidipine, depending on the patient condition.

cimetidine:

Symptoms and treatment: There is a report that is the effects of some other calcium antagonists (eg nifedipine) increased. Increase the absorption of calcium antagonists.

rifampicin:

Symptoms and treatment: There is a report that is the effect of other calcium antagonists (nifedipine).

Anti -fungal Azol group: Intraconazol, miconazole, ...

Symptoms and treatment: Cilnidipine concentration in the blood may increase.

grapefruit juice:

Symptoms of symptoms and treatment: proving the increased blood cilnidipine levels.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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