Atelec Tablets 10 Ea Pharma. Treatment of hypertension (10 blisters x 10 tablets)

Dosage form Box of 10 blisters x 10 tablets
Specifications Cilnidipine
Ingredient Ea Pharma

Ingredient

Composition information	Content
Cilnidipine	10mg

Uses

indications

Atelec Tablets 10 drug is indicated in the following cases:

Treatment of hypertension.

In many different models of hypertension on animals (spontaneous hypertension rats, rats and dogs hypertension due to kidney blood vessel disease, hypertension due to DOCA salts and rats with spontaneous hypertension easily stroke), a single dose of oral cilnidipine shows the effect of lowering blood pressure slowly and prolonged the dose dependent at 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 dose. In hypertension due to kidney blood vessel disease, Cilnidipine shows the additional effect when used simultaneously with a β blocker or angiotensin transferring enzyme inhibitors.

In spontaneous hypertension rats that are easy to stroke and in hypertension due to kidney blood vessels, repeated doses of cilnidipine use oral route has the effect of lowering stable blood pressure without showing a decrease. Stop using cilnidipine does not cause blood pressure.

In the rats of hypertension, self -awake and untreated, Cilnidipine does not increase the heart rate while hypotension. Cilnidipine does not increase plasma noradrenaline concentration while hypotension, nor significantly reduces this concentration as caused by adrenergic blockers (guanethidine sulfate). Cilnidipine does not cause hypotension, although pentolinium (pentolinium) has caused in tilt test.

In patients with idiopathic hypertension, a single dose of Cilnidipine 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 interval in the 24 -hour electrocardiogram has discovered that Cilnidipine does not increase the sympathetic activity or heart rate in the form of double reflex response with reduced blood pressure.

The inhibitory effect on the hypertension response caused by stress

In the rats of hypertension, self -consciousness and uncontrolled, cilnidipine inhibits hypertension and norepinephrine levels in plasma caused by cold stress. Cilnidipine 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 test, Cilnidipine inhibits blood pressure caused by cold stress.

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

In spontaneous hypertension rats poking the spinal cord, cilnidipine inhibits hypertension caused by electrolyte stimulation.

In spontaneous hypertension rats with isolated and fluid mesenteric artery, Cilnidipine also inhibits the release of norepinephrine caused by electrolyte 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 mice. 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, blood flow is still maintained while blood pressure is reduced.

Effects on the heart function

In dogs, cilnidipine reduces heart rate and muscle contraction at higher doses than the dosage causing hypertension.

In dogs with anesthesia, cilnidipine reduces the consumption of oxygen of the heart muscle in bureaucracy 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 ratio (CTR), Cilnidipine improves the rate of heart - chest.

Effects on kidney function

In the rats of spontaneous hypertension, cilnidipine increases the volume of urine, blood flow through the kidneys and the filtration speed of the glomerular 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 daily cilnidipine single dose prevents stroke appearance and improves the survival rate. In addition, Cilnidipine also reduces heart hypertrophy (heart weight increase), thick left ventricular walls, myocardial fibrosis and kidney damage. Moreover, Cilnidipine also reduces the middle layer of the coronary wall walls and reduces the calcium content in the aorta.

In patients with idiopathic hypertension, Cilnidipine reduces atherosclerosis and lipid peroxide in serum.

Mechanism of action

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 inhibit the Ca2+ inhibitors through the cell membrane of the blood vessel smooth 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.

Cilnidipine inhibits the Ca 2+ current coming through 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. Cilnidipine is said 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

Plasma concentration in plasma

When using a single dose of Cilnidipine 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) corresponds to 23.7 ng. NG.

So both parameters increase in the way of dosage dependence.

When repeating a single dose of Cilnidipine 10 mg, 1 time/day for 6 men to volunteer to be healthy, the pharmacokinetic parameters of Cilmdipine are expressed as below. The plasma concentration is achieved in a stable state from the 4th day when taking the drug and there is no sign of accumulation.

Parameters
Date of medicine

cmax (ng/ml)

TMAX (hour)

t ½ (α) (hour)

t ½ (β) (hour)

AUC0- ¥ (Ng.H/ML)

The first day

9.5 ± 1.6

2.8 ± 1.0

1.0 ± 0.2

5.2 ± 2.0

51.4 ± 12.7

13.5 ± 5.0

3.7 ± 0.8

101.8 ± 29.0

16.5 ± 7.9

3.0 ± 1.3

1.1 ± 0.6

8.1 ± 2.7

95.5 ± 34.5

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 oral dose in hypertension patients, and there is no significant difference in the dynamic data of this drug compared to data in patients with normal kidney function.

The repeated use of this medication at a dose of 10 mg, 1 time/day for 7 days in patients with impaired renal function does not cause differences in dynamic data compared to data in patients with normal renal function.

Metabolism and elimination

Based on the identified among plasma and urine of healthy volunteers, it is thought that Cilnidipine's main metabolic line is the methyl reduction of methoxyethyl group, followed by the hydrolysis of Cinnamyl ester hydrolysis 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).

Calcium channel blockers of metabolic substances have a methoxyethyl group that is reduced to methyl is only 1/100 the effect of the original compound (on rabbits).

When repeating a single dose of Cilnidipine 10 mg, 1 time/day orally for 7 days for men to volunteer healthy, without a constant Cilnidipine compound is eliminated but 5.2% of the dose is excreted in urine in the form of metabolites. (The use of Atelec has been approved as 1 time/day orally after breakfast).

A In vitro experiment has shown that Cilnidipine is connected to 99.3% to human serum protein.

Before taking Atelec Tablets 10 Ea Pharma. Treatment of hypertension (10 blisters x 10 tablets)

How to use

oral medication.

Dosage

Normally, for adults to use 5 - 10 mg Cilnidipine 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, 1 time/day, if not fully responded. For adults with severe hypertension, should use Atelec 10 - 20 mg, 1 time/day orally 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? If the blood pressure is reduced significantly, it is necessary to take appropriate measures such as improving the lower limb, the treatment of infusion and the use of hypertension drugs. Eliminate illness by hemolysis ineffective due to the high ratio of the drug to protein.

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. Do not drink twice as prescribed.

Side Effects

When using Atelec Tablets 10, you may experience unwanted effects (ADR).

Observed the side effects, including the test results in 414 patients (6.95%) out of 5958 patients in studies at the time of approved drugs and in after -sales studies (at the end of the re -testing period).

Clinical side effects

Disorders of liver and jaundice (unknown frequency)

Disorders of liver and jaundice accompanied by an increase in AST (GOT), ALT (GPT) and γ - GTP may occur.

Because platelet reduction may occur, it is necessary to monitor closely, if observations see any abnormalities, it is necessary to take appropriate measures such as stopping Atelec.

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

0.1 -

Unknown frequency

liver (note 1)

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

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), neutrophils and hemoglobin.

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

edema (face, lower limb, etc.), body discomfort, urination, serum cholesterol, increase or decrease CK (CPK), Uric acid, potassium and serum phosphorus.

Feeling weak, twin muscle spasms, dry eyes around the eyes, congestion and irritating sensation, taste disorders, positive urinary tract, increased or decreased blood sugar at eagerness, all -stooled protein, calcium and crp serum, cough.

Note 2: If any symptoms appear, stop using Atelec.

Notify the doctor with unwanted effects when using the drug.

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

Atelec Tablets 10 drug is contraindicated in the following cases:

Patients with hypersensitivity to the active ingredient or any component of excipients.

Pregnant women or women are likely to be pregnant.

Caution when using

Read the instructions carefully before use. If you need more information, please consult your doctor.

This drug is only used by a doctor.

Be careful when using Atelec in the following patients:

Patients with severe liver dysfunction.

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

Elderly patients.

Important caution

Because there is a report is a sudden stopping of calcium antagonism, several symptoms, so if they need to stop Atelec, the dose must be gradually reduced under close monitoring. If Attelec stops from 5 mg/day; Should 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

Atelec should be carefully used under the patient's close monitoring and taking measures such as starting with a lower dose (eg 5 mg).

Using in the elderly is often acknowledged to avoid excessive hypotension in the elderly.

Therefore, there have been a side effect (including test results) in the elderly aged 65 and older at 152 out of 2,863 patients in studies at the time of approved drugs and in after -sales studies (at the end of the re -examination period).

used in pediatrics

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

Precautions when using

When distributing this drug:

It is necessary to explain to the patient that first remove the pills from the PTP blister before taking the medicine. (There is a report that in the case of drinking ptp blisters, the hard, sharp edges of the blister can easily penetrate the esophagus mucosa and lead to serious complications, such as mediastitis).

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 against participating in dangerous activities that need alertness such as working on high, operating machinery or driving motor.

Pregnancy

must not use Atelec for pregnant women or women who are likely to be pregnant. The report has been reported that Atelec extends the pregnancy and childbirth time in experimental animals (on rats).

breastfeeding period

should avoid Attelec for breastfeeding women. However, if it is required to take the drug, it is necessary to instruct the patient to stop breastfeeding. There has been a report that this drug goes into breast milk in experimental animals (on rats).

Drug interaction

Atelec is mainly metabolized by the enzyme metabolism of CYP3A4 and partially by CYP2C19.

Be cautious when used simultaneously:

Medicinal name

Signs, symptoms and treatment

Mechanism and risk factors

Blood pressure can be overheated.

Includes the ability to have additional or union effects.

Digoxin

There has been a report that some calcium antagonistic drugs (eg nifedipine) increase the concentration of digoxin in plasma.

If observations see any signs/toxic symptoms that can be attributed to digoxin (e.g. nausea, vomiting, headache, abnormal vision, arrhythmia), appropriate measures must be taken such as adjusting Digoxin dose or stopping Attelec, depending on the condition of the patient.

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

cimetidine

There have been reports that are the effects of some other calcium antagonists (eg 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 enzymes in the liver microsoma, and cimetidine reduces gastric acid, thus increasing the absorption of calcium antagonists.

rifampicin

There is a report that is the effect of other calcium antagonists (eg nifedipine) decreased.

It is often thought that the enzyme metabolizes drugs in the liver (cytochrome p - 450) is induced by rifampicin, urging the metabolism of calcium antagonists, thus increasing the disposal of these drugs.

iTraconazole, miconazole, etc.

Atelec concentration may increase.

Anti -fungal Azole group is thought to inhibit CYP3A4, a drug metabolic enzyme for Atelec.

grapefruit juice

It has shown that Atelec concentration in plasma increased.

The details of the basic mechanism still need to be clarified, but some components in grapefruit juice can inhibit CYP3A4, which are drug metabolic enzymes for Atelec.

Storage

Store less than 30 ° C, avoid light.

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.