Esseil-10 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	10mg

Uses

Indications

Esseil-10 drugs are indicated in the following cases: Cilnidipin is indicated for hypertension treatment.

Pharmacokological

anti -hypertension effects

In many different models of hypertension on animals (rats with 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 lower blood pressure effects slowly and prolonged the dose dependent at 1mg/kg or higher.

On the contrary, it shows that the effect of lowering blood pressure in rats has normal blood pressure. The effect time does not last when taking an excessive high dose. In hypertension due to kidney blood vessel disease, cilnidipin shows the additional effect when used simultaneously with a beta blocker or angiotensin enamel inhibitor.

In spontaneous hypertension rats, stroke and hypertension dogs due to kidney blood vessel disease, repeated doses of cilnidipin used oral route have the effect of lowering stable blood pressure without showing a decrease. Stop using cilnidipine does not cause blood pressure regression.

In the rats of hypertension, self -awake and not restrained, cilnidipine does not increase heart rate while hypotension. Cilnidipin does not increase plasma noradrenalin concentrations while hypotension, nor significantly reduces this concentration as caused by adrenergic guanethidin sulfate. Cilnidipine does not cause hypotension, although pentolinium (pentolinium) has caused in the tilt test.

In patients with idiopathic hypertension, a single dose of cilnidipin every day orally shows that the hypotension effect is maintained in 24 hours and remains clearly early in the morning. The analysis of the energy spectrum of the R-R intervals 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 decrease.

The inhibitory effect on the hypertension response caused by stress

In the rats of hypertension, spontaneously awake and not restrained, cilnidipine inhibits hypertension and norepinephrin levels in plasma caused by cold stress. Cilnidipin also inhibits hypertension caused by air jet stress (mental stress) in rats.

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

The inhibitory effect on the hypertension response is caused by sympathetic stimulation

In spontaneous hypertension rats are poked the spinal cord, cilnidipin inhibits hypertension caused by electrolyte stimulation.

In spontaneous hypertension rats with isolated and fluid mesenteric artery, Cilnidipin also inhibits the release of norepinephrin caused by electric sympathetic stimulation.

Effects on brain circulation

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

In patients with hypertension, which is complicated due to cerebrovascular disease, the blood flow is still maintained while the blood pressure is reduced.

Effects on the heart function

In dogs, cilnidipine reduces heart rate and has a heart muscle at higher doses than the dosage causing hypertension of arterial blood.

In dogs with anesthesia, cilnidipine reduces the consumption of oxygen of the heart muscle at the dose causing hypotension. At this time, Cilnidipine does not cause tachycardia, nor does it affect the contractions of the heart.

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

Effects on kidney function

In spontaneous hypertension rats anesthetized, cilnidipine increases the volume of urine, blood flow through the kidneys and the filtration rate 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.

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

Effects on cardiovascular disorders associated with hypertension

In spontaneous hypertension rats that are easy to stroke, a single dose of cilnidipin 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 calcium content in the aorta.

In patients with idiopathic hypertension, cilnidipine reduces atherosclerosis and lipid peroxid in serum.

Mechanism of action

Experimental data has shown that cilnidipine is connected to the locations of the dihydropyridine of the calcium channel that depends on the Type L electrolyte and inhibits the Ca2+ inhibitors through the cell membrane of the blood vessel muscle through this channel (in vitro on rabbits).

Therefore, blood vessel muscles dilate, causing vasodilation. Through this mechanism, cilnidipine is considered to have the effect of lowering blood pressure.

Cilnidipin inhibits Ca2+ inhibiting 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 electrolyte has been observed in a scope of the drug concentration similar to the Ca2+ inhibitor concentration of Type L (In vitro on the rat).

Therefore, the release of norepinephrin 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.

pharmacokinetic

absorption

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

When repeating a single dose of Cilnidipin 10mg, 1 time/day for 6 healthy men to volunteer shows that the plasma concentration is achieved in a stable state from the 4th day when taking the drug and there is no signs of accumulation of drugs. The pharmacokinetics of this drug have also been evaluated in patients with kidney function (serum creatinine: 1.5 - 3.1mg/dl) after taking a single dose of 10mg oral in hypertension patients, and no difference is statistically significant about the pharmacokinetic data of this drug compared to data in patients with normal kidney function. The repetition of this medication is taken at a dose of 10mg, 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

cilnidipine connects 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. CYP 3A4 is thought to be mainly related and CYP 2C19 is partially related to the methyl reduction of the methoxyethyl group (in vitro).

The calcium channel blocker of metabolic channel 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 10mg, 1 time/day oral for 7 days for men to volunteer healthy, no Cilnidipin compound is unchanged, but 5.2% of the dose is eliminated in urine in the form of metabolites.

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

How to use

Oral drugs.

Dosage

Adults

Usually use 5 - 10mg 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 20mg/time/day if responding to the drug is not enough.

Severe hypertension

Take the dose of 10 - 20mg oral, 1 time/day after breakfast.

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.

What to do when forgetting a dose? 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.

Side Effects

When using ESSEIL-10, you may experience unwanted effects (ADR).

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 γ-AGP. 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.

0.1

Unknown frequency

liver (1)

Increase AST (GOT), ALT (GPT), LDH ...

Increase ALP

Increase creatinine or urea nitrogen, positive protein.

There are sediments in urine.

Headache, dull headache, dizziness, dizziness when standing up, stiff shoulder muscles.

Te.

Flushing, beating chest drum, hot feeling, abnormal electrocardiogram (sturgrust, reverse waves), blood pressure decreases.

Chest pain, heart - chest ratio, tachycardia, atrial fabric, cold feeling.

Extraordinary

digestive

Nausea, vomiting, abdominal pain.

Constipation, bloating, thirst, hypertrophy, heartburn, diarrhea.

red, itching.

Sensitive to light.

Increase or decrease in leukemia (WBC), Neutral leukocytes and haemoglobin.

Increase or decrease red blood cells (RBC), hematocrit, Eosin leukemia and lymphocytes.

edema (face, lower limb, ...), uncomfortable body, urine, serum hyperkemin, increase or decrease CK (CPK), Uric acid, potassium and serum phosphor.

The feeling of weakness, muscle spasm of the legs, dryness around the eyes, eye congestion and irritating sensation, taste disorders, positive urinary tract, increased or decreased blood sugar at hunger, total protein, calcium and CRP serum, cough.

(2) If any symptoms are found, cilnidipine must be stopped.

Instructions on how to handle ADR

Notice immediately to the doctor or pharmacist 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-10 drugs contraindicated in the following cases:

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

Pregnant women or women are likely to be pregnant.

Precautions 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 report 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 breastfeeding.

Be important

Because there is a report is a sudden stopping of calcium antagonism, several symptoms, so if it is necessary to stop cilnidipine, it is necessary to gradually reduce the dose under close monitoring. If cilnidipine stops from a dose of 5mg/day, appropriate measures should be taken such as replacing with other anti -hypertension drugs. The patient should be constantly instructed 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 (eg 5mg). Should avoid excessive hypotension in the elderly.

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

Use in children

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

The ability to drive and operate machinery

Symptoms such as dizziness may occur due to the hypotension effect of this drug. It is necessary to have a warning about participating in dangerous activities that need alertness such as working on high, operating machinery or motor drivers.

Pregnancy

must 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).

Medicinal interaction

cilnidipin is mainly metabolized by the enzyme metabolic CYP3A4 and partially by CYP2C19.

drug name

Signs, symptoms and treatment

Mechanisms and risk factors

Blood pressure can be overheated.

Includes the ability to have additional effects or coatings.

Digoxin

There have been reports that some calcium antagonists (e.g. nifedipine) increases the concentration of digoxin in plasma. If observations see any signs of toxic symptoms that can be attributed to digoxin (for example, nausea, vomiting, headache, abnormal vision, arrhythmia), must take appropriate measures such as adjusting digoxin or stop cilnidipine, depending on the patient condition.

The mechanism is not fully clarified, but is thought to be within the reduction of renal and external renal clearance.

There are reports that are the effects of some other calcium antagonists (e.g. nifedipine) increased.

It is thought that cimetidine reduces blood flow through the liver with the consequence of preventing the metabolism of calcium antagonists due to the liver enzyme, and cimetidine reduces the amount of stomach acid, thus increasing the absorption of calcium antagonists.

rifampicin

There is a report that is the effect of other calcium antagonists (NIFEDIPIN).

It is often thought that the enzyme metabolizes drugs in the liver (cytochrom p450) is induced by rifampicin, promoting the metabolism of calcium antagonists, thus increasing the clearance of these drugs.

Cilnidipine concentration in the blood may increase.

Anti -fungal Azol group is thought to inhibit CYP 3A4, a drug metabolic enzyme for cilnidipin.

grapefruit juice

There has been a shown that Cilnidipine concentration in the blood increased.

The details of the basic mechanism still need to be clarified, but some of the ingredients in grapefruit juice can inhibit CYP 3A4, which is an enzyme that transforms drugs for cilnidipine.

Storage

In a dry place, avoid light, the temperature does not exceed 30 ° C.

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