Stadovas 5 cap Stella medicine for hypertension, chronic angina (3 blisters x 10 tablets)

Amlodipine's blood pressure lowering mechanism is due to the effect of direct relaxation of blood vessel muscles. Amlodipine's exact mechanism reduces angina has not been determined enough, but Amlodipine reduces the burden of general anemia due to the following two effects:

1) Amlodipine relaxes peripheral arteries and thus reduces the peripheral resistance total of the heart (reducing the burden). Because the heart rate does not change, this burden reduces the heart consumption and oxygen needs of the heart muscle.

2) The mechanism of action of amlodipine may also include the relaxation of the main coronary arteries and coronary arteries, both in anemia and normal areas. This vasodilation increases the supply of oxygen to the heart muscle patients with coronary artery spasms (Prinzmetal angina or angina) and reduces smoking coronary spasms.

In patients with hypertension, one -time dose/day shows a significant clinical decrease in the clinical position in both lying and standing throughout the dose of 24 hours. Due to the slow -on -effect trigger, fasting blood pressure is not one of the effects of amlodipine.

In patients with angina, the use of amlodipine once a day increases the overall exertion time, the starting time of angina and time until the 1 mm ST segment inhibitors and reduces both the frequency of angina and reduces the use of nitroglycerin tablets.

Not yet detected that amlodipine is related to any adverse effects on metabolism or changes in plasma lipids and anlodipine suitable for use in patients, diabetes and gout.

Pharmacokinetics

absorption

After taking treatment doses, Amlodipine is well absorbed with peak concentration in plasma reaching about 6 - 12 hours after oral bioavailability is absolutely estimated to be about 64 - 80%. The distribution volume is about 21 l/kg. Amlodipine absorption is not affected by food.

In vitro studies show that about 97.5% amlodipine during circulation is associated with plasma proteins

Metabolism/ excretion

Amlodipine's semi -discharged time is in the range of 35 - 50 hours and is suitable for the dosage of 1 time/day. The concentration in a stable state in plasma is achieved after 7-8 days of continuous medication. Amlodipine is metabolized largely in the liver into non -active metabolites, with 10% of the initial substance and 60% of the metabolic substance eliminated through the urine.

Used in the elderly

Time to reach the peak concentration of amlodipine plasma is the same between the elderly and young people. However, Anlodipine's clearance tends to decrease with an increase in the area under the curve (AUC) and the sale time in elderly patients. The area under the curve and the sale time in patients with congested heart failure also increased as expected in the research group.

Use in children

In a long -term clinical study, 73 patients with hypertension from 12 months of age to less or 17 years old were used amlodipine at an average daily dose of 0.17 mg/kg. The clearance of the objects weighing on average 45 kg is 3.7 hours and 17.6 hours respectively in men and women. This index is similar to the announced estimates of 24.8 hours in adults 70 kg. The average distribution integral for a 45 kg patient is 130 l (25.11 l/kg). Observing the effect on the blood pressure is maintained throughout the 24 -hour bureaucracy, with a small difference in the variable effect in Dinh and the bottom. When compared to the information that has been dynamic in adults, the observed parameters in this study shows the one -time dosage/day is appropriate.

amlodipine well tolerated in children. These unwanted effects are similar to the unwanted effects to see in adults. In a study with 268 children, the most unwanted effects are:

Uncommon, 1/1000

Caution when used

used in patients with heart failure: In a long-term study, pretended to be studied by praise-2) using Amlodipine in patients with heart failure due to anemia origin, level III and V according to the New York cardiovascular Association (NYHA), amlodipine is reported related to increased lung rate. However, there is no significant difference in the proportion of patients with heart failure worse in the amlodipine group compared to the placebo group.

Used in patients with liver function impairment: Like all other calcium channel blockers, Amlodipine's waste sale time is long in patients with liver function impairment and recommended doses for these patients have not been set up. Therefore, Anlodipine needs to be used carefully in these patients.

The ability to drive and operate machinery

Amlodipine may have a slight or medium impact to the ability to drive and operate machinery. If the patient uses amlodipine dizziness, headache, fatigue or nausea, their reaction possibility may be impaired. Patients need to be carefully warned, especially from the beginning of treatment.

Pregnancy

The safety of Armlodipine in pregnant and lactating women has not been established. Amlodipine is not toxic in studies on animal reproductive systems, except for slowing labor and extending the time to live in mice at a dose of 50 times higher than the maximum use recommendations in humans. Therefore, Amlodipine should only be used during pregnancy when there is no safer replacement and when the disease itself contains greater risks for mothers and embryos. There is no effect on the ability to conceive on mice using amlodipine.

The period of breastfeeding

Experience used on humans shows that amlodipine has passed through breast milk. The median concentration ratio of amlodipine in milk/plasma in 31 women who are breastfeeding has hypertension due to pregnancy is 0.85 after using amlodipine at the starting dose of 5 mg once daily, this dose is adjusted if needed (average daily dose and daily dose in the form are 6 mg and 98.7 mcg/kg). The estimated daily dose of amlodipine that babies receives through breast milk is 4.17 mcg/kg.

Drug interaction

amiodipine has been shown to be safe to use with thiazid diuretics, A-adrenergic receptor inhibitors, β-adrenergic receptors, ACE inhibitors, long-lasting nitrates, nitroglycerin under the tongue, non-steroid anti-inflammatory drugs, antibodies and blood hypersensitivity drugs.

Intro data from plasma studies shows that amlodipine does not affect the cohesion of plasma proteins of research drugs (digoxin, phenytoin , warfarin or indomethacin).

Simvastatin : Use multiple doses of 10 mg amlodipine simultaneously with 80 mg of simvastatin increases 77% exposure rate with simvastatin compared to only simvastatin. For patients using amlodipine, the limit of simvastatin is 20 mg/day.

Grapefruit juice: Simultaneously use 240 ml of grapefruit juice with a single dose of 10 mg amlodipine in 20 healthy volunteers does not significantly affect the kinetics of Amlodipine. This study did not allow the testing of the effects of CYP3A4 genetic forms, the main enzyme is responsible for transforming amlodipine, so it should not be used amlodipine along with grapefruit or grapefruit juice because bioavailability may increase in some patients leading to increased hypotension.

CYP3A4 inhibitor: simultaneously use 180 mg daily dose of diltiazem with 5 mg of amlodipine in the elderly (69 - 87 years old) with hypertension increases 57% of the system exposure rate with amlodipite. Simultaneous use with erythromycin on a healthy lover (18 - 43 years old) does not significantly change the system exposure rate with amlodipine (up 22% AUC). Although clinically related to these studies is not sure, the change in kinetics may be more pronounced in elderly patients.

Strong CYP3A4 inhibitors (such as ketoconazole, iTraconazole, ritonavir) may increase the concentration of amlodipine in the blood larger than the diltiazem. Should be cautious when using amlodipine along with CYP3A4 inhibitors.

Clarithromycin : Clarithromycin is a CYP3A4 inhibitor. The risk of increased hypotension in patients using clarithromycin along with amlodipine. Should monitor patients closely when using simultaneously amlodipine with clarithromycin.

CYP3A4 induction substances: There is currently no data on the effects of CYP3A4 induction substances on Amlodipine. Simultaneous use with substances of CYP3A4 (such as rifampicin, hypercum Perforatum) can reduce amlodipine levels in plasma. Should be cautious when using amlodipine along with CYP3A4 touch substances.

In the following studies, there is no significant change in pharmacokinetics of amlodipine or other drugs in the study when used in combination.

Special studies: The effect of other drugs on amlodipine

cimetidine : simultaneously used amlodipine and cimetidine does not change the dynamics of amlodipine.

Aluminum/Magnesi salt (stomach acid neutralizing drugs): Concomitant use of antacids is aluminum salt and magnesium salt with a single dose of amlodipine does not significantly affect the dynamics of amlodipine.

Sidelnafil: Using a single dose of 100 mg of Sildenafil in objects with idiopathic hypertension does not affect the dynamic parameters of Amlodipine. When used in combination with amlodipine and sildenafil, each drug tries its own antihypertensive effect.

Special studies: The effect of amlodipine on other drugs.

Atorvastatin : simultaneously use 10 mg aloodipine doses with 30 mg atorvastatin does not significantly change the pharmacokinetic parameters of Atorvastatin in a stable concentration state in plasma.

digoxin: simultaneously use amlodipine with digoxin does not change the concentration of digoxin in plasma or the renal clearance of digoxin in healthy volunteers.

Ethanol (alcohol): Use of single -dose or multi -dose 10 mg of amlodipine does not significantly affect the dynamics of ethanol.

warfarin : simultaneous use of amlodipine with warfarin does not change the time of prothrombin inhibitors of warfarin.

Cyclosporin: There are no studies on interactive drugs cyclosporin and amlodipine in healthy volunteers or other groups of objects except for kidney transplant patients. Different studies in kidney transplantation show that the simultaneous use of amlodipine with cyclosporin affects the bottom concentration of cyclosporin from unchanged to an average increase of 40%. It is necessary to consider to monitor cyclosporin levels in kidney transplant patients using amlodipine.

tacrolimus : There is a risk of increasing the concentration of Tacrolimus in the serving area simultaneously with Anmodipire. To avoid the characteristics of Tacrolimus, when using Amlodipine in patients treated with Tacrolimus, the Agriculture and Agriculture of Tacrolimus should be monitored in the blood and adjust the dose of Tacrolimus if appropriate.

Mechanical goals of Rapamycin inhibitors (MTOR) MTOR inhibitors such as syrolimus, temsirolirus, and Everolimus are CYP3A. Amlodipine is a weak CYP3A inhibitor. When used simultaneously with MTor inhibitors, Amlodipine may increase the exposure of MTOR inhibitors.

Interactions between drugs and biochemical tests: unknown.

Tyeum of drugs

Due to the absence of studies on the correlation of the drug, not mixing this drug with other drugs.