"Amlotop": instructions for use, analogues, reviews

Hypertension, coronary heart disease, and angina pectoris are very common health problems for modern people today. Moreover, such diseases have become significantly “younger” - if previously mature patients suffered from them, today even young people are diagnosed with coronary artery disease and hypertension. To treat these health problems, the pharmaceutical industry produces many drugs, one of which is Amlotop. Instructions for use and reviews about it will be discussed below.

Pharmacological group of the drug

For the drug "Amlotop", the instructions for use included by the manufacturer in each package of the drug indicate a pharmaceutical accessory - a blocker of "slow" calcium channels. This is a fairly broad group of drugs, including several positions of active substances that have a similar effect, but differ in their effect on heart rate, pharmacokinetics, and tissue susceptibility.

Microelements play an important role in the human body. So, for example, upon penetration into tissue cells, calcium ions activate bioenergetics processes such as phosphorylation of proteins (one of the stages of biosynthesis), metabolism of ATP (adenosine triphosphoric acid - a source of energy for metabolic processes in the body) into cAMP (cyclic adenosine monophosphate, playing the role of an intermediary between certain hormones and tissue cells). But, like any other components, these substances must be present in the cells in a certain amount. If for some reason their concentration increases, then cellular metabolic processes require an increase in oxygen concentration, which can lead to destructive changes. The transfer of calcium Ca2+ ions (transmembrane transfer) occurs through special calcium channels, which are quite complex and diverse. Today, scientists have found that calcium channels, which have a complex structure of transmembrane proteins, can be divided into two types:

voltage-dependent, through which Ca ions pass when the membrane potential drops below a certain level;
receptor-dependent, allowing a flow of Ca ions through cell membranes when cell receptors interact with specific agonists, for example, acetylcholine, catecholamines, serotonin, histamine.

These chemical-physical processes play a vital function in cellular metabolism. Calcium channels are also divided into types that differ from each other in certain properties. They are designated by letter indices - L, N, P, Q, R, T.

L-type channels get their name from the English words long-lasting - long-lived, larde - large, depending on conductivity - they are slowly activated when the cell membrane is depolarized, which determines the entry of Ca2+ ions into the cell and the formation of a slow calcium potential.

L-type channels are found in cardiomyocytes, in smooth muscle cells of arterial vessels and most internal organs, as well as in cells of the cardiac conduction system, in skeletal muscles and in platelets. It is to the group of drugs that delay the work of these intercellular adapters that the drug “Amlotop” and analogues of this drug belong.

In what form can the drug be purchased?

The drug "Amlotop" is produced by several pharmaceutical companies. But there is only one form of release - in the form of tablets, which, however, have different contents of the active component. It can be 5 or 10 mg in one unit - a tablet. The drug "Amlotop", its analogues, produced in different dosage forms, have an antianginal (relieving angina pain and attack) and hypotensive (lowering blood pressure) effect. The group of drugs that have a similar effect is very extensive. But the question of which therapy to carry out for a particular patient can be resolved by the attending specialist, taking into account many circumstances. Taking Amlotop without consulting a doctor or on the advice of friends is strictly prohibited!

Compound

One of the antihypertensive drugs widely used in medical practice is the drug Amlotop. The instructions for it indicate the active substance - an amlodipine derivative - besylate. The following additional components are used:

calcium stearate;
colloidal silicon dioxide;
croscarmellose sodium;
lactose monohydrate;
microcrystalline cellulose.

These substances do not play any therapeutic role, performing only formative functions.

Amlotop tablets, both 5 and 10 mg, have a round shape, they are flat, and have beveled edges. Each unit of the drug is equipped with a median line on one side for ease of dividing the tablet. The medicine is packaged in 10 or 30 pieces in blister cells with aluminum protective film. Plates with tablets of 2, 3, 5, 10 pieces are folded into cardboard packs.

Action of the active component

As noted, the instructions for use of Amlotop indicate the active substance - amlodipine besylate. It is a white crystalline powder, practically insoluble in water. It has antianginal, hypotensive and vasodilating properties. This spectrum of activity is due to the fact that it blocks calcium channels, reducing the activity of the transition of calcium ions through the cell membrane into the cell. Amlodipine typically works in vascular smooth muscle cells, although it works somewhat worse in cardiomyocytes. This substance dilates coronary and peripheral arteries and arterioles, which determines its antianginal effect. Due to this effect, the drug reduces the severity of myocardial ischemia during angina pectoris, reduces peripheral vascular resistance and myocardial oxygen demand, prevents spasm of the coronary arteries, including those caused by smoking, thereby reducing the load on the heart muscle.

The hypotensive effect of the drug "Amlotop" is based on its vasodilating (relaxing) effect on vascular smooth muscles. For those who suffer from stable angina, using the drug in a single daily dosage can increase immunity to physical activity. The medicine also reduces the potential risk of developing angina attacks and ischemic depression, which has a direct impact on the use of nitroglycerin and other nitrates, reducing their dose and number of uses.

The drug "Amlotop" reduces the level of left ventricular myocardial hypertrophy, but does not affect its contractility and conductivity, does not cause an increase in heart rate at the reflex level, and inhibits aggregation, that is, sticking together of platelets. The drug also has a positive effect on kidney function, potentiating the glomerular filtration rate and having some natriuretic effect. The drug "Amlotop" has also found application in nephropathy associated with diabetes.

This medicine does not affect the metabolism in the body in any way, and therefore it can be taken by patients with diabetes, bronchial asthma, and gout. Also, taking this drug does not increase the risk of death for patients diagnosed with chronic heart failure of functional class III-IV, but with the same disease V-VI FC of non-ischemic origin, there is a potential for the development of pulmonary edema.

Amlotop Plus

Some undesirable effects observed with the use of the drug may affect the ability to drive vehicles and operate machinery.

In patients with reduced blood volume (for example, those receiving treatment with large doses of diuretics) or with severe aortic stenosis, symptomatic arterial hypotension may occur. Correction of such conditions must be carried out before prescription or treatment must begin with a lower dose of the drug. Acute arterial hypotension is unlikely due to the gradual onset of action of the drug.

Based on pharmacokinetic data that showed a significant increase in plasma concentrations of losartan in patients with cirrhosis, patients with a history of impaired liver function should be prescribed lower doses of losartan.

Since amlodipine is primarily metabolized in the liver and has a half-life of 56 hours in patients with hepatic impairment, dosage titration should be gradual when administering amlodipine to patients with severe hepatic impairment.

Amlodipine

Unstable angina and acute myocardial infarction may occur after initiation of therapy or an increase in the dose of amlodipine, especially in patients with severe hypertrophic obstructive cardiomyopathy.

If oliguria or arterial hypotension develops in newborns whose mothers took the drug during pregnancy, symptomatic therapy aimed at maintaining blood pressure and renal perfusion is necessary. Blood transfusions or dialysis may be required to prevent hypotension and/or maintain renal function.

Clinical studies have not revealed any particularities regarding the safety and effectiveness of losartan in elderly patients (over 65 years of age). In elderly patients, due to reduced clearance, amlodipine therapy is usually recommended to begin with a dose of 2.5 mg once daily. Since the drug does not have a dosage containing amlodipine 2.5 mg, this dose should be prescribed in monotherapy with amlodipine.

Losartan

In patients with a history of angioedema (swelling of the face, lips, pharynx/larynx and/or tongue), monitoring of the use of the drug is necessary.

Embryotoxicity: Use of drugs that affect the RAAS during the second and third trimester of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and mortality. The development of oligohydramnios may be associated with fetal lung hypoplasia and skeletal deformities. Possible adverse events in neonates include calvarial hypoplasia, anuria, hypotension, renal failure and death. If pregnancy is diagnosed, the drug should be discontinued immediately.

Fluid and electrolyte imbalance is common in patients with impaired renal function with or without diabetes mellitus, so careful monitoring of these patients is necessary. In clinical trials in patients with type 2 diabetes mellitus with proteinuria, the incidence of hyperkalemia was greater in the losartan group than in the placebo group. Several patients discontinued therapy due to hyperkalemia.

While taking losartan, patients should not take potassium supplements or potassium-containing salt substitutes without prior consultation with their doctor.

Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with aortic or mitral stenosis or hypertrophic obstructive cardiomyopathy.

Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with coronary heart disease or cerebrovascular diseases, since an excessive decrease in blood pressure in patients in this group can lead to the development of myocardial infarction or stroke.

As with the use of other drugs that act on the RAAS, in patients with CHF and with or without impaired renal function, there is a risk of developing severe arterial hypotension or acute renal failure.

Since there is insufficient experience with the use of losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias, losartan should be prescribed with caution in patients of these groups.

Since patients with primary hyperaldosteronism, as a rule, do not respond well to therapy with antihypertensive drugs that act by inhibiting the RAAS, the use of losartan is not recommended in patients in this group.

Data from pharmacokinetic studies indicate that the plasma concentration of losartan in patients with cirrhosis is significantly increased, therefore patients with a history of liver disease should be prescribed losartan at a lower dose. There is no experience with the use of losartan in patients with severe liver dysfunction, so the drug should not be used in patients in this group.

Due to inhibition of the RAAS, changes in renal function, including the development of renal failure, have been observed in some susceptible patients. These changes may subside after treatment is stopped.

Some drugs that affect the RAAS may increase blood urea and serum creatinine concentrations in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney. Similar effects have been reported with losartan. Such renal dysfunction may be reversible after discontinuation of therapy.

When is the drug prescribed?

The instructions for use of the drug "Amlotop" list the diseases and conditions for which this drug is prescribed:

arterial hypertension;
vasospastic angina;
stable angina;
essential hypertension.

This drug can be used both as a single agent and in complex therapy of these diseases. Only the attending physician can prescribe it for use, taking into account all the necessary nuances - medical history, concomitant diseases, state of health.

special instructions

For arterial hypertension, Amlotop can be combined with alpha- and beta-blockers, thiazide diuretics, antibiotics, nitrates, ACE inhibitors, and hypoglycemic drugs.

For angina pectoris, Amlotop can be used both as a single drug and in combination with other antianginal drugs, including in patients refractory to treatment with beta-blockers and/or nitrates.

In some cases, when using Amlotop, especially at the beginning of therapy and when changing the dosage, dizziness, drowsiness and similar symptoms may occur. Therefore, all patients are advised to exercise caution when driving.

How the drug works in the human body

One of the drugs that has a blocking effect on calcium channels is Amlotop. The instructions for its use indicate that the tablets are taken orally. The active component amlodipine is well absorbed in the gastrointestinal tract, with its bioavailability ranging from 64 to 80%.

In the patient's body, the active component of the drug is distributed mainly in the tissues and not in the blood. Metabolizes amlodipine in the liver, and the metabolites do not have significant pharmacological activity. The half-life is approximately 45 hours. In elderly patients over 65 years of age, this time is slightly longer - about 65 hours, but this indicator has no clinical significance. The same factor applies to patients suffering from renal and/or liver failure. The drug "Amlotop" is excreted from the body mainly by the kidneys, with 10% excreted unchanged. The rest is excreted with bile through the intestines. A doctor prescribing Amlotop for use should remember that the active substance of this medicine penetrates the blood-brain barrier. If necessary, it is also necessary to take into account that the medicine is not removed from the body during hemodialysis.

When should the drug not be taken?

Many people suffering from coronary heart disease and angina use Amlotop tablets for outpatient treatment. The instructions for use of this medicine indicate contraindications:

arterial hypotension if the measured systolic blood pressure is less than 90 mmHg. Art.;
heart failure after myocardial infarction, which is hemodynamically unstable;
cardiogenic shock;
collapse;
obstruction of the outflow tract of the left ventricle;
aortic stenosis;
increased sensitivity.

Also, the drug should not be taken in children under 18 years of age due to the lack of clinical studies. The use of this drug is not recommended for pregnant and lactating women. The drug is prescribed with extreme caution for hypertrophic cardiomyopathy, non-ischemic chronic heart failure of functional class III-IV, disorders of active liver function, mitral stenosis, sick sinus syndrome, expressed by tachycardia and bradycardia, acute myocardial infarction.

Contraindications

According to the annotation for the drug, the use of Amlotop is contraindicated in the following cases:

Collapse;
Severe arterial hypotension, if systolic blood pressure does not reach 90 mm Hg;
Cardiogenic shock;
Lactose intolerance;
Clinically significant aortic stenosis;
Lactase deficiency;
The presence of hypersensitivity to amlotop, any auxiliary component of the drug or other dihydroperidine derivatives;
Glucose-galactose malabsorption.

The drug should not be used during lactation, pregnancy, children and adolescents under 18 years of age.

Amlotop is prescribed, but strictly according to indications and under constant medical supervision, to elderly people, as well as to patients with:

Liver dysfunction;
Chronic heart failure of non-ischemic etiology;
Sick sinus syndrome (with tachycardia, severe bradycardia);
Arterial hypotension, if systolic pressure is more than 90 but less than 100 mmHg;
Aortic stenosis;
Acute myocardial infarction (within one month after the attack);
Hypertrophic obstructive cardiomyopathy;
Mitral stenosis.

Possible side effects

The use of Amlotop is possible only on the recommendation of a doctor. Like any medicine, it may cause side effects, including:

arthralgia;
arthrosis;
asthenia;
ataxia;
bradycardia;
Pain in the eyes;
chest pain;
backache;
vasculitis;
gastritis;
hypoesthesia;
gum hyperplasia;
headache;
dizziness;
dermatitis;
diplopia;
significant decrease in blood pressure;
itchy skin;
insomnia;
myocardial infarction;
nosebleeds;
flatulence;
atrial fibrillation;
myalgia;
myasthenia gravis;
visual impairment;
general malaise;
peripheral neuropathy;
fainting;
dyspnea;
orthostatic hypotension;
peripheral edema;
feeling of heartbeat,
paresthesia;
increased sweating;
rush of blood to the scalp (face);
thrombocytopenic purpura;
development or worsening of chronic heart failure;
vomit;
rhinitis;
drowsiness;
muscle cramps;
rash;
ventricular tachycardia;
nausea;
anxiety;
increased fatigue.

Side effects of Amlotop

According to patient reviews, Amlotop may have side effects:

More than 1% of patients experience peripheral edema, dizziness, a feeling of heat, rapid heartbeat, flushing of the face, increased fatigue, drowsiness, headache, insomnia, increased sweating, malaise, peripheral neuropathy, fainting, hypoesthesia, nervousness, emotional lability, tremor, depression, unusual dreams, paresthesia, nausea, abdominal pain;
Infrequently, i.e. in approximately 0.1% to 1% of cases of Amlotop use, vasculitis, excessive decrease in pressure, chills, orthostatic hypotension, asthenia, vomiting, anorexia, constipation, dry mouth, flatulence, diarrhea, thirst, dyspepsia, arthralgia, arthrosis, back pain, muscle cramps, myalgia, shortness of breath, nosebleeds, rhinitis, frequent urination, nocturia, painful urge to urinate, ringing in the ears, diplopia, conjunctivitis, visual impairment, xerophthalmia, eye pain, accommodation disturbances, taste perversion, alopecia , skin itching and rash, gynecomastia, impotence;
Rarely (more than 0.01% of patients, but less than 0.1%) develop apathy, convulsions, development of heart failure or worsening of its course, agitation, increased appetite, gingival hyperplasia, increased activity of liver transaminases, pancreatitis, jaundice, gastritis, hepatitis, dermatitis;
Very rarely - less than 0.01% of patients while taking Amlotop experience migraine, chest pain, ataxia, cardiac arrhythmias, myocardial infarction, amnesia, thrombocytopenia, leukopenia, thrombocytopenic purpura, hyperglycemia, cough, polyuria, dysuria, parosmia , skin pigmentation disorder, xeroderma, angioedema, urticaria, erythema multiforme, cold sweat.

How to take the medicine correctly?

The instructions for use for Amlotop tablets indicate that they are taken once, regardless of the time of meal. The tablets must be taken with a sufficient amount of plain water.

Usually start with 5 mg, then, if necessary, increase to 10 mg per day, this is considered the maximum allowable dose. This dosage change is carried out 1-2 weeks after the start of treatment with Amlotop. If you need to quickly increase the dose of this drug, then this should only be done under the supervision of a specialist. You cannot independently change the number of tablets per dose, or take this medicine more than once a day!

If the patient is treated with antihypertensive drugs, then the initial daily dose of Amlotop can be 2.5 mg, since the effect of lowering blood pressure will be cumulative.

Therapy with this medicine for special groups of people with low body weight, short stature, old age, and problems with liver function is carried out individually.

Directions for use and dosage of Amlotop

Amlotop tablets, according to the instructions, should be taken orally once a day with water, regardless of meals.

The initial daily dose of the drug is usually 5 mg. If necessary, taking into account the individual reaction of the patient's body, the dose can be increased to 10 mg per day. It is recommended to do this 1-2 weeks after the start of treatment. A faster increase in dosage requires special monitoring of the patient.

For elderly people, patients of short stature or low body weight, as well as persons with impaired liver function, Amlotop is prescribed as an antianginal drug in a dose of 5 mg, as an antihypertensive drug - 2.5 mg (1/2 tablet 5 mg). For people with renal failure, no dosage adjustment is required.

In combination with other antihypertensive medications, Amlotop is prescribed at an initial dose of 2.5 mg.

Interactions with other drugs

Be sure to read the instructions for use of Amlotop. At what pressure can and cannot be taken? The manufacturer of the drug indicates in its instructions that the medicine cannot be used if the systolic blood pressure is below 90 mm Hg. Art. It is also necessary to take into account the compatibility of the active component with other drugs that the patient is taking.

This medicine can be safely used with drugs such as alpha-blockers, beta-blockers, thiazide diuretics or angiotensin-converting enzyme (ACE) inhibitors, non-steroidal anti-inflammatory drugs, including indomethacin, antibiotics, hypoglycemic agents. It is important to remember that calcium supplements can significantly reduce the activity of the calcium channel blocker amlodipine. Neuroleptic drugs in combination therapy with Amlotop can enhance its hypotensive effect. If the patient is taking this drug and needs treatment with antiviral drugs, then the increase in the concentration of amlodipine in the blood should be taken into account and its single dosage should be reduced.

Amlotop®

Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that prolong the QT interval (eg, amiodarone and quinidine). Amlodipine can also be safely used concomitantly with antibiotics and oral hypoglycemic agents.

Single dose of 100 mg sildenafil

in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.

Repeated use of amlodipine 10 mg and atorvastatin

at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.

Simvastatin

: simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in simvastatin exposure by 77%. In such cases, the dose of simvastatin should be limited to 20 mg.

Ethanol (beverages containing alcohol):

amlodipine with single and repeated use at a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antivirals (ritonavir):

increases plasma concentrations of BMCC, including amlodipine.

Neuroleptics and isoflurane

: increased hypotensive effect of dihydropyridine derivatives.

Calcium preparations

may reduce the effect of BMCC.

When combined with BMCC and lithium preparations

(no data available for amlodipine) their neurotoxicity may increase (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Studies of the simultaneous use of amlodipine and cyclosporine in healthy volunteers and all groups of patients, with the exception of patients after kidney transplantation, have not been conducted.

Various studies of the interaction of amlodipine with cyclosporine in patients after kidney transplantation show that the use of this combination may not lead to any effect, or increase the minimum concentration of cyclosporine to varying degrees, up to 40%.

These data should be taken into account and cyclosporine concentrations should be monitored in this group of patients when cyclosporine and amlodipine are co-administered.

Does not affect serum digoxin

and its renal clearance.

Does not significantly affect the action of warfarin

(prothrombin time).

Cimetidine

does not affect the pharmacokinetics of amlodipine.

in vitro studies

of digoxin, phenytoin, warfarin and indomethacin
to plasma proteins Grapefruit juice:

A simultaneous single dose of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. However, it is not recommended to use grapefruit juice and amlodipine at the same time, since genetic polymorphism of the CYP3A4 isoenzyme may increase the bioavailability of amlodipine and, as a result, increase the hypotensive effect.

Aluminum or magnesium containing antacids:

their single dose does not have a significant effect on the pharmacokinetics of amlodipine.

CYP3A4 isoenzyme inhibitors

: with simultaneous use of diltiazem at a dose of 180 mg and amlodipine at a dose of 5 mg in patients from 69 to 87 years of age with arterial hypertension, an increase in systemic exposure of amlodipine by 57% was observed. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) does not lead to significant changes in amlodipine exposure (increase in area under the concentration-time curve (AUC) by 22%). Although the clinical significance of these effects is unclear, they may be more pronounced in older patients.

Potent inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) may increase the plasma concentration of amlodipine to a greater extent than diltiazem. Amlodipine and inhibitors of the CYP3A4 isoenzyme should be used with caution.

Clarithromycin:

CYP3A4 isoenzyme inhibitor. Patients taking clarithromycin and amlodipine at the same time have an increased risk of low blood pressure. Patients taking this combination are advised to be under close medical supervision.

Inducers of the CYP3A4 isoenzyme:

There is no data on the effect of inducers of the CYP3A4 isoenzyme on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored during concomitant use of amlodipine and inducers of the CYP3A4 isoenzyme.

Tacrolimus: When used concomitantly with amlodipine, there is a risk of increasing the concentration of tacrolimus in the blood plasma. To avoid toxicity of tacrolimus when used concomitantly with amlodipine, the concentration of tacrolimus in the blood plasma of patients should be monitored and the dose of tacrolimus should be adjusted if necessary.

Mammalian target of rapamycin (mTOR) inhibitors

mTOR inhibitors such as sirolimus, temsirolimus and everolimus are substrates of the CYP3A isoenzyme. Amlodipine is a weak inhibitor of the CYP3A isoenzyme. When used concomitantly with mTOR inhibitors, amlodipine may increase their exposure.

Some features of treatment with Amlotop

The use of the drug "Amlotop" requires the patient to follow the doctor's recommendations regarding dosage and regimen.

The treatment has not been studied in children or breastfeeding women, so the possibility of its danger or effectiveness for these categories of patients is not known. A pregnant woman should only be prescribed this medicine if the risk to the fetus is minimal compared to the benefit to the mother. It is better to choose another drug if necessary. The drug, when used once, does not have a negative effect on concentration, but during a course of treatment it is not recommended to drive a car or carry out work that requires increased concentration. Also, long-term treatment with this drug requires not only the strictest possible adherence to dental and oral hygiene, but also regular visits to the dentist in order to promptly eliminate the negative manifestation of its effect on the oral cavity, timely detect gum hyperplasia, their bleeding and take measures to preserve the health of teeth and gums .

Amlotop tablets 10 mg No. 30

Compound

Active substance: amlodipine besylate - 13.86 mg, equivalent to amlodipine - 10 mg.
Excipients: lactose monohydrate (lactose 200/flowlac 100), microcrystalline cellulose, calcium stearate, croscarmellose sodium (primellose), colloidal silicon dioxide (aerosil).

Pharmacokinetics

Suction. After oral administration, amlodipine is well absorbed from the gastrointestinal tract. Food intake does not affect the absorption of amlodipine. The maximum concentration in the blood serum is achieved 6-12 hours after administration. Bioavailability is 60-65%. The average volume of distribution is 21 l/kg body weight. Communication with plasma proteins is 90-97%. The drug penetrates the blood-brain barrier.

Metabolism and excretion. Amlodipine undergoes slow but significant metabolism (90%) in the liver to form inactive metabolites and has low hepatic clearance (first-pass effect through the liver). The half-life averages 35 hours (varies from 35 to 50 hours), which corresponds to the administration of the drug once a day. Total clearance - 500 ml/min. Stable equilibrium plasma concentrations are achieved after 7-8 days of therapy. It is excreted by the kidneys (10% unchanged, 60% in the form of metabolites), with bile and through the intestines - 20-25% in the form of metabolites, as well as in breast milk. It is not removed by hemodialysis.

In elderly patients, patients with liver failure and severe CHF, the half-life increases to 60-65 hours; in case of impaired renal function, it does not change.

Indications for use

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs).
Stable exertional angina and vasospastic angina (Prinzmetal's angina) (monotherapy or in combination with other antianginal drugs).

Contraindications

Hypersensitivity to amlodipine and other dihydropyridine derivatives, as well as to other components included in the drug.
Severe arterial hypotension (systolic blood pressure less than 90 mmHg).
Shock (including cardiogenic shock).
Left ventricular outflow tract obstruction (eg, severe aortic stenosis).
Hemodynamically unstable heart failure after myocardial infarction.
Age up to 18 years (efficacy and safety have not been studied).
Lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose).
Breastfeeding period.

With caution:
Impaired liver function, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of functional class III-IV according to the NYHA classification, arterial hypotension (systolic blood pressure more than 90 and less than 100 mm Hg), aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (HOCM), acute myocardial infarction (and within 1 month after myocardial infarction), use in elderly patients, simultaneous use with inhibitors or inducers of the CYP3A4 isoenzyme, pregnancy.

Directions for use and doses

Orally, once a day, regardless of meals, with a sufficient amount of water (100 ml).
The initial dose for arterial hypertension and angina pectoris is usually 5 mg. Depending on the individual response of the patient, the dose can be increased to a maximum of 10 mg per day. Dose increases are recommended 7-14 days after the start of therapy (faster dose increases require careful monitoring of the patient).

For patients with low body weight, short stature, elderly patients, patients with impaired liver function, amlodipine is prescribed as an antihypertensive agent in an initial dose of 2.5 mg (1/2 tablet 5 mg), and as an antianginal agent - 5 mg. A starting dose of 2.5 mg may also be used when amlodipine is added to therapy with other antihypertensive drugs.

In patients with renal failure, no dose adjustment is required.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25° C. Keep out of the reach of children.

Best before date

3 years. Do not use after expiration date.

special instructions

The effectiveness and safety of amlodipine in hypertensive crisis has not been established.
Patients with heart failure should use amlodipine with caution. In a long-term placebo-controlled study in patients with severe heart failure (NYHA functional class III or IV), the incidence of pulmonary edema was higher in the amlodipine group than in the placebo group. Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure as they may increase the risk of cardiovascular events and death. In patients with impaired liver function, T1/2 and AUC values of amlodipine may be increased; dosage recommendations have not been established. Therefore, the use of amlodipine should be started at the lower end of the therapeutic dose range and caution should be exercised both when starting treatment and when increasing the dose. In patients with severe hepatic impairment, gradual dosage titration and careful monitoring of the patient's condition may be necessary.

In elderly patients, T1/2 may increase and drug clearance may decrease. No dosage adjustment is required, but careful monitoring of patients is necessary.

During treatment, it is necessary to monitor body weight and sodium intake. It is necessary to maintain oral hygiene and regularly visit the dentist (to prevent pain, bleeding and gum hyperplasia).

Description

Blocker of “slow” calcium channels.

Use in children

There are no clinical data on the use of amlodipine in pediatrics.

Pharmacodynamics

The dihydropyridine derivative is a second generation blocker of “slow” calcium channels (SCCC), has an antianginal and hypotensive effect.
By binding to the segment S6III and IV domains of the alpha 1 subunit of the L-type calcium channel, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes). The antianginal effect is due to the expansion of peripheral and coronary arteries and arterioles. For angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces total peripheral vascular resistance (reduces afterload on the heart), without causing a reflex increase in heart rate, which helps reduce energy consumption; reduces myocardial oxygen demand. By expanding the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium during vasospastic angina; prevents the development of coronary spasm (including those caused by smoking).

In patients with angina pectoris, a single daily dose of amlodipine increases the time before the onset of the first ischemic episode during physical activity, prevents the development of an attack of angina and “ischemic” depression of the ST segment (by 1 mm) during physical activity, reduces the frequency of angina attacks and nitroglycerin consumption.

The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. It has a long-term dose-dependent hypotensive effect.

For arterial hypertension, a single daily dose of amlodipine provides a clinically significant reduction in blood pressure (BP) over 24 hours (in the patient’s “lying” and “standing” position). Does not cause a sharp decrease in blood pressure or left ventricular ejection fraction. Has no effect on myocardial contractility and conductivity. Reduces the degree of left ventricular myocardial hypertrophy.

In patients with coronary heart disease (CHD) (including coronary atherosclerosis with damage to one vessel and up to stenosis of 3 or more arteries and atherosclerosis of the carotid arteries), who have had myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (PTCA) or suffering from angina, the use of amlodipine prevents the development of intima-media thickening of the carotid arteries, reduces mortality from myocardial infarction, stroke, PTAP, coronary artery bypass grafting, leads to a decrease in the number of hospitalizations for unstable angina and progression of chronic heart failure, reduces the frequency of interventions aimed at restoring coronary blood flow.

Amlodipine does not increase the risk of death or complications leading to death in patients with chronic heart failure (CHF) (NYHA functional class III-IV) during therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors.

In patients with CHCH (III-IV functional class according to the NYHA classification) of non-ischemic etiology, when using amlodipine, there is a risk of pulmonary edema.

Amlodipine does not have any adverse effects on metabolism and plasma lipid concentrations. Inhibits platelet aggregation, increases glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria.

The onset of the effect is 2-4 hours, the duration of the effect is 24 hours.

Side effects

The frequency of the following possible side effects is indicated according to the classification of the World Health Organization (WHO):

very often - more than 1/10; often - from more than 1/100 to less than 1/10; uncommon - from more than 1/1000 to less than 1/100; rarely - from more than 1/10000 to less than 1/1000; very rarely - from less than 1/10000, including individual messages; frequency unknown—cannot be determined from available data.

Disorders of the blood and lymphatic system: very rarely - leukopenia, thrombocytopenic purpura, thrombocytopenia.

Immune system disorders: very rarely - allergic reactions.

Metabolic and nutritional disorders: very rarely - hyperglycemia.

Mental disorders: uncommon - insomnia, mood changes (including anxiety), depression; rarely confusion.

Nervous system disorders: often - drowsiness, dizziness, headache (especially at the beginning of treatment); infrequently - tremor, dysgeusia, fainting, hypoesthesia, paresthesia; very rarely - hypertonicity, peripheral neuropathy; frequency unknown - extrapyramidal disorders.

Visual disorders: often - visual impairment (including diplopia).

Hearing and labyrinthine disorders: uncommon - tinnitus.

Cardiac disorders: often - palpitations; uncommon - arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation); very rarely - myocardial infarction.

Vascular disorders: often - hyperemia; infrequently - arterial hypotension; very rarely - vasculitis.

Disorders of the respiratory system, chest and mediastinal organs: often - shortness of breath; infrequently - cough, rhinitis.

Disorders of the digestive system: often - abdominal pain, nausea, dyspepsia, change in bowel habits (including diarrhea and constipation); infrequently - vomiting, dryness of the oral mucosa; very rarely - pancreatitis, gastritis, hypertrophic gingivitis.

Disorders of the liver and biliary tract: very rarely - hepatitis, jaundice, increased activity of liver enzymes (mainly due to cholestasis).

Disorders of the skin and subcutaneous tissues: uncommon - alopecia, purpura, skin discoloration, increased sweating, itching, skin rash, exanthema, urticaria; very rarely - angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, photosensitivity.

Musculoskeletal and connective tissue disorders: often - swelling of the ankle joints, muscle cramps; infrequently - arthralgia, myalgia, back pain.

Renal and urinary tract disorders: infrequently, urinary problems. nocturia, increased frequency of urination.

Disorders of the genital organs and mammary gland: infrequently - impotence, gynecomastia.

General disorders and disorders at the injection site: very often - peripheral edema; often - increased fatigue, asthenia; Uncommon: chest pain, pain, malaise.

Laboratory and instrumental data: infrequently - increase in body weight, decrease in body weight.

Use during pregnancy and breastfeeding

The safety of amlodipine during pregnancy has not been established, so use is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.

There are no data indicating the excretion of amlodipine in breast milk. However, other calcium channel blockers (dihydropyridine derivatives) are known to be excreted in breast milk. In this regard, if it is necessary to use amlodipine during lactation, the issue of stopping breastfeeding should be decided.

Interaction

Amlodipine can be safely used for the treatment of arterial hypertension together with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors.
In patients with stable angina, amlodipine can be combined with other antianginal agents, for example, long- or short-acting nitrates, beta-blockers. Unlike other BMCCs, no clinically significant interaction of amlodipine was found when used together with non-steroidal anti-inflammatory drugs (NSAIDs), including indomethacin. It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when used together with alpha1-blockers, antipsychotics. Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that prolong the QT interval (eg, amiodarone and quinidine). Amlodipine can also be safely used concomitantly with antibiotics and oral hypoglycemic agents.

A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.

Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.

Simvastatin: simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in simvastatin exposure by 77%. In such cases, the dose of simvastatin should be limited to 20 mg.

Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiviral agents (ritonavir): increases plasma concentrations of BMCC, including amlodipine.

Neuroleptics and isoflurane: enhancing the hypotensive effect of dihydropyridine derivatives.

Calcium supplements can reduce the effect of BMCC.

When BMCC is used together with lithium preparations (no data are available for amlodipine), their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus) may increase. Studies of the simultaneous use of amlodipine and cyclosporine in healthy volunteers and all groups of patients, with the exception of patients after kidney transplantation, have not been conducted.

These data should be taken into account and cyclosporine concentrations should be monitored in this group of patients when cyclosporine and amlodipine are co-administered.

Does not affect the serum concentration of digoxin and its renal clearance.

Does not significantly affect the effect of warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In in vitro studies, amlodipine does not affect the plasma protein binding of digoxin, phenytoin, warfarin and indomethacin.

Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. However, it is not recommended to use grapefruit juice and amlodipine at the same time, since genetic polymorphism of the CYP3A4 isoenzyme may increase the bioavailability of amlodipine and, as a result, increase the hypotensive effect.

Aluminum- or magnesium-containing antacids: their single dose does not have a significant effect on the pharmacokinetics of amlodipine.

Inhibitors of the CYP3A4 isoenzyme: with simultaneous use of diltiazem at a dose of 180 mg and amlodipine at a dose of 5 mg in patients from 69 to 87 years of age with arterial hypertension, an increase in systemic exposure of amlodipine by 57% was observed. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) does not lead to significant changes in amlodipine exposure (increase in area under the concentration-time curve (AUC) by 22%). Although the clinical significance of these effects is unclear, they may be more pronounced in older patients.

Clarithromycin: CYP3A4 inhibitor. Patients taking clarithromycin and amlodipine at the same time have an increased risk of low blood pressure. Patients taking this combination are advised to be under close medical supervision.

Inducers of the CYP3A4 isoenzyme: there is no data on the effect of inducers of the CYP3A4 isoenzyme on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored during concomitant use of amlodipine and inducers of the CYP3A4 isoenzyme.

Mammalian target of rapamycin (mTOR) inhibitors

Overdose

Symptoms: pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of developing a pronounced and persistent decrease in blood pressure, including the development of shock and death).

Treatment: taking activated charcoal (especially in the first 2 hours after an overdose), gastric lavage (in some cases), maintaining the function of the cardiovascular system, monitoring indicators of heart and lung function, monitoring circulating blood volume and diuresis. The patient should take a horizontal position with the lower extremities elevated.

In the absence of contraindications, symptomatic therapy: vasoconstrictor drugs, intravenous administration of calcium gluconate. Hemodialysis is ineffective.

Impact on the ability to drive vehicles and operate machinery

In some patients, mainly at the beginning of treatment or when changing the dosage regimen, drowsiness, dizziness and other side effects may occur due to a possible pronounced decrease in blood pressure. If they occur, the patient must be careful when driving a car and working with complex mechanisms.

Are there any analogues?

All the information necessary for the doctor and the patient is contained in the instructions for use about the drug "Amlotop". Its analogues can be found in any pharmacy. These are such products as “Normodipin”, “Tenox”, “Amlodak”, “Norvask”. You can also purchase a generic version of Amlotop in pharmacy chains; this drug will be named after the active ingredient - Amlodipine, and some pharmaceutical companies add their own name to this name, for example, Amlodipine - Zentiva.

A doctor may prescribe a drug that has the same pharmacological activity, but has a different substance as an active component. For example, verapamil, lecranidipil, cinnarizine, which work in drugs called “Verogalid”, “Lerkamen”, “Stugeron”. The correct choice of medication, duration and completeness of the course of therapy, determined by the treating specialist, will help cope with the disease efficiently, without side effects.

What do experts say about the drug?

Amlotop tablets are often prescribed to patients with high blood pressure and the risk of developing myocardial infarction. Doctors speak of this drug as a fairly effective remedy that can provide the necessary effect even with a single use. For the drug "Amlotop", the instructions for use contain important information for the patient, in particular, the dosage. In some cases, it can be adjusted by the doctor in accordance with the patient's medical history and the course of the disease. Doctors note the high effectiveness of this drug for normalizing angina attacks, preventing the development of hypertension and reducing the potential danger of developing myocardial infarction. From the point of view of specialists, the occurrence of side effects is most often noted in the form of swelling of the lower extremities and dizziness. Other undesirable effects of the drug occur very rarely.

Patient Feedback

The drug "Amlotop" receives mostly grateful reviews from patients. Those who praise the medicine note its convenient once-a-day use, its effectiveness in normalizing blood pressure, relieving symptoms of angina pectoris and coronary heart disease. Some are upset by the appearance of side effects - swelling in the legs, dizziness, headaches. Some patients, due to the pronounced severity of such an unnecessary effect of the drug, were forced to abandon it, although almost everyone is satisfied with its price and Russian production. Many patients note that they use the drug only to lower blood pressure, although some thank the drug for its help during a course of fairly long-term use.

For the drug "Amlotop", the instructions for use contain important information that not only the specialist needs to know, but also the patient taking it for certain therapeutic purposes. We repeat, you can only take it as prescribed by a doctor!