Aladine 5 mg tablets number 50 *
Author Ольга Кияница
|Amount in a package
|Farmak OJSC (Ukraine, Kiev)
|The main medicament
Aladine (Amlodipine) Instructions for use
active ingredient : 1 tablet contains amlodipine besylate 13.90 mg or 6.95 mg (based on amlodipine 10 mg or 5 mg);
Aladine tablets 10 mg - lactose monohydrate, potato starch, crospovidone, coriander, silicon dioxide colloidal anhydrous, magnesium stearate;
tablets Aladine 5 mg - lactose monohydrate, corn starch, croscarmellose sodium, povidone, silicon dioxide colloidal anhydrous, magnesium stearate.
Selective calcium antagonists with a predominant effect on the vessels. Derivatives of dihydropyridine. Code АТС С08С А01.
- Arterial hypertension.
- Chronic stable angina pectoris.
- Vasospastic angina pectoris (angina pectoris).
- Known hypersensitivity to dihydropyridines, amlodipine or to any other component of the drug.
- Arterial hypotension of severe degree.
- Shock (including cardiogenic shock).
- Obstruction of the withdrawal tract of the left ventricle (for example, aortic stenosis of severe degree).
- Hemodynamically unstable cardiac insufficiency after acute myocardial infarction.
Method of administration and dose
Adults For the treatment of arterial hypertension and angina pectoris, the usual initial dose of Aladin is 5 mg of amlodipine once a day. Depending on the patient's response to therapy, the dose can be increased to a maximum dose of 10 mg once daily.
Patients with angina pectoris may be used as monotherapy or in combination with other antianginal drugs for resistance to nitrates and / or adequate doses of beta-blockers.
There is experience with the use of the drug in combination with thiazide diuretics, alpha-blockers, beta-blockers, or angiotensin converting enzyme inhibitors in patients with arterial hypertension.
There is no need to select a dose of the drug while co-administered with thiazide diuretics, beta-blockers and angiotensin converting enzyme inhibitors.
Children from 6 years of age with arterial hypertension. The recommended initial dose of Aladin for this category of patients is 2.5 mg once a day. If the required blood pressure level is not reached within 4 weeks, the dose can be increased to 5 mg per day. The use of the drug in doses above 5 mg for this category of patients has not been studied.
Older patients. There is no need to select a dose for this patient category. Dose increase should be done with caution.
Patients with impaired kidney function.
It is recommended to use the usual doses of the drug, since changes in the concentration of amlodipine in the blood plasma are not related to the severity of renal failure. Amlodipine is not eliminated by dialysis.
Patients with hepatic insufficiency.
Doses of the drug for use in patients with mild to moderate hepatic insufficiency have not been established, so the dose selection should be done with caution and start using at the lowest dose (see section "Special Features" and "Pharmacological Properties. Pharmacokinetics").
From the blood and lymphatic system. Thrombocytopenia, leukocytopenia.
From the side of the immune system. Allergic reactions.
Disorders of metabolism and alimentary disorders. Hyperglycemia.
From the psyche. Insomnia, mood swings (including anxiety), depression, confusion.
From the nervous system. Drowsiness, dizziness, headache (mainly at the beginning of treatment), fatigue, asthenia, convulsions, increased sweating, tremor, dysgnea, syncope, hypoesthesia, paresthesia, hypertonus, peripheral neuropathy.
From the side of the vision organs. Visual disturbance (including diplopia), tearing.
On the part of the hearing and labyrinth. Call in the ears.
From the heart. Heartburn, shortness of breath, chest pain. Like during the administration of other calcium antagonists, isolated undesirable phenomena have been described that can not be separated from the effects of the natural course of the underlying disease: myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia, and atrial fibrillation), as well as back pain.
From the vessels side. Face redness, flushing, arterial hypotension, vasculitis, peripheral edema.
Respiratory, thoracic and mediastinal disorders. Dyspnea, rhinitis, cough.
From the gastrointestinal tract. Nausea, vomiting, abdominal pain, dyspepsia, discomfort in the epigastric region, dry mouth, peristalsis of the intestine (including constipation, diarrhea and flatulence), pancreatitis, gastritis, gum hyperplasia.
From the hepatobiliary system. Hepatitis, jaundice, elevated liver enzymes (which is most often associated with cholestasis).
From the skin and subcutaneous tissues. Angioedema (Queinki's edema), rash, itching, erythema multiforme, urticaria, alopecia, purpura, skin discoloration, heat sensation, increased sweating, photosensitivity, exfoliative dermatitis, Stevens-Johnson syndrome.
On the part of the musculoskeletal and connective tissue. Sciatica, arthralgia, myalgia, muscle cramps, back pain.
From the kidneys and the urinary tract. A slight increase in diuresis, urticaria, urinary tract disruption, increased urinary frequency.
From the reproductive system and the mammary glands. Gynecomastia, sexual dysfunction.
General disorders and conditions at the injection site. Swelling, fatigue, pain, malaise, increase or decrease in body weight.
After the drug is discontinued, the side effects usually disappear completely.
Exceptional cases of extrapyramidal syndrome were reported.
Experience of intentional overdose of the drug is limited.
Overdose Symptoms: The available information suggests that a significant overdose of Aladin will lead to excessive peripheral vasodilation and, possibly, reflex tachycardia. Significant and possibly prolonged systemic hypotension, including fatal shock, has been reported.
Treatment: A clinically meaningful hypotension due to an overdose of amlodipine requires active support for the cardiovascular system, including frequent monitoring of cardiac and respiratory function, limb lifting, monitoring of volume of circulating fluid and urine output.
To restore vascular tone and blood pressure, you can use vasoconstrictor drugs, making sure that there are no contraindications to their use. The use of calcium gluconate intravenously may be useful for leveling the effects of blockade of calcium channels.
In some cases, gastric lavage may be beneficial. The use of activated charcoal for healthy volunteers within 2 hours after the administration of 10 mg of amlodipine significantly reduced its absorption.
Since amlodipine is highly bound to proteins, the effect of dialysis is negligible.
Use during pregnancy or breastfeeding
The safety of the use of amlodipine has not been established in women during pregnancy.
The use of amlodipine during pregnancy is recommended only in cases where there is no safer alternative and the risk associated with the disease itself exceeds the potential harm from treatment for the mother and the fetus.
It is not known whether amlodipine penetrates breast milk. When deciding whether to continue breast-feeding or on the use of amlodipine, it is necessary to evaluate the benefits of breast-feeding for the baby and the benefit of using the product for the mother.
Fertility. Reversible biochemical changes in the spermatozoa were reported in some patients with calcium channel blockers. Clinical information about the potential impact of amlodipine on fertility is not enough.
Where are you
The drug is for children from 6 years of age. The effect of amlodipine on arterial pressure in patients under 6 years of age is unknown.
You should start using the drug with the lowest dose. Care should be taken both at the start of the medication and during the dose increase. Patients with severe hepatic insufficiency may need a slow dose selection and careful monitoring of the patient's condition.
During the entire period of treatment, body weight and sodium intake, administration of the appropriate diet, and daily blood pressure monitoring should be monitored.
The safety and efficacy of the use of amlodipine in a hypertensive crisis has not been evaluated.
Application to patients with heart failure. This category of patients Aladin should be used with caution.
Application to patients with impaired liver function. The half-life of Aladin, like other calcium antagonists, is increased in patients with impaired liver function. For this reason, it is necessary to use the preparation for such a patient with extreme caution and only under careful supervision of the doctor.
Use of elderly patients. Increase the dose of the drug in this category of patients should be taken with caution.
Use in patients with renal insufficiency. For this category of patients, Aladin should be used in normal doses. Changes in the concentration of amlodipine in plasma do not correlate with the severity of renal insufficiency. Amlodipine is not eliminated by dialysis. Amlodipine does not affect the results of laboratory tests.
It is not recommended to use amlodipine with grapefruit or grapefruit juice, as some patients may have increased bioavailability, which will increase the hypotensive effect of the drug.
Drinking alcohol during contraction is contraindicated.
Ability to influence the reaction speed when driving or operating with other mechanisms
Aladin may moderately or moderately affect the ability to drive vehicles or work with other mechanisms. Care should be taken, especially at the start of therapy.
The reaction speed may be reduced if there are symptoms such as dizziness, headache, confusion or nausea.
Interaction with other drugs and other types of interactions
Effect of other drugs on amlodipine.
CYP3A4 inhibitors. At simultaneous administration of amlodipine and CYP3A4 inhibitors, such as erythromycin to younger patients or diltiazem in elderly patients, amlodipine plasma concentrations increased by 22% and 50%, respectively. The clinical significance of these data is unknown. It can not be ruled out that potent inhibitors of CYP3A4 (ketoconazole, itraconazole, ritonavir) increase the levels of amlodipine in blood plasma more than diltiazem. Amlodipine should be used with caution in combination with CYP3A4 inhibitors. However, the development of adverse reactions that are associated with the interaction in the application of such a combination, was not reported.
CYP3A4 inducers. There is no information on the effect of inducers of CYP3A4 on amlodipine. Simultaneous administration of amlodipine and substances that are inducers of CYP3A4 (eg, rifampicin, St. John's wort) may lead to a decrease in the concentration of amlodipine in plasma, therefore, such combinations should be used with caution.
Clinical studies of drug interactions showed that the use of bicimethin, antacids with aluminum or magnesium, and sildenafil did not affect the pharmacokinetics of amlodipine.
Dantrolene (infusion). In animals, ventricular fibrillation with fatal outcome and cardiovascular collapse, which were associated with hypercalcaemia, were observed after intravenous administration of verapamil and dantrolen. Due to the risk of hypercalemia, it is recommended to avoid the use of calcium channel blockers, such as amlodipine, prone to malignant hyperthermia in patients and in the treatment of malignant hyperthermia.
Effect of amlodipine on other medicines. The hypotensive effect of amlodipine potentiates the hypotensive effect of other antihypertensive agents.
Clinical studies of drug interaction have shown that amlodipine does not affect the pharmacokinetics of atorvastatin, digoxin, ethanol (alcohol), warfarin, and cyclosporin.
Amlodipine is an antagonist of calcium (a derivative of dihydropyridine) , which blocks the flow of calcium ions into myocardium and into smooth muscle cells.
The mechanism of hypotensive action of amlodipine is caused directly by a relaxing effect on the smooth muscles of the vessels. The exact mechanism of the antianginal effect of amlodipine has not been studied sufficiently, however, the following effects play a role.
Amlodipine expands peripheral arterioles and thus reduces peripheral resistance (post-load). As the heart rate remains stable, reducing heart load leads to a decrease in energy consumption and oxygen demand in the myocardium.
The expansion of major coronary arteries and coronary arterioles (normal and ischemic) may also play a role in the mechanism of action of amlodipine. Such an expansion increases the oxygen saturation of patients with coronary artery spasm (angina pectoris or variant angina pectoris).
In patients with arterial hypertension, the use of the drug once a day provides a clinically meaningful decrease in blood pressure for 24 hours in the position both lying and standing. Due to the slow onset of amlodipine, acute arterial hypotension is usually not observed.
In patients with angina pectoris, when using one daily dose of the drug, the total physical activity, time to the onset of angina and time to 1 mm depression of the ST segment increase. The drug reduces the frequency of seizures and reduces the need for nitroglycerin.
Amlodipine is not associated with any adverse metabolic actions or changes in the level of lipids in the blood plasma and can be used in patients with asthma, diabetes mellitus and gout.
Suction / distribution. After oral administration of therapeutic doses, amlodipine is gradually absorbed into the blood plasma. The absolute bioavailability of the unchanged molecule is about 64-80%. The maximum plasma concentration is reached within 6-12 hours after application. The volume of distribution is approximately 21 l / kg; The dissociation constant of acid (pKa) amlodipine is 8.6. The binding of amlodipine to blood plasma proteins is approximately 97.5%.
Simultaneous consumption of food does not affect the absorption of amlodipine.
Metabolism / Invention. The half-life of the blood plasma is about 35-50 hours. Equilibrium concentration in blood plasma is reached after 7-8 days of continuous use of the preparation. Amlodipine is mainly metabolized to the formation of inactive metabolites. About 60% of the administered dose is excreted in the urine, about 10% of which is amlodipine in the unmodified form.
Older patients. The time to achieve equilibrium concentrations of amlodipine in plasma is similar in elderly patients and in adult patients. The clearance of amlodipine is usually slightly reduced, which leads to an increase in the area under the "concentration / time" curve (AUC) and the half-life of the drug in elderly patients.
Patients with impaired kidney function. Amlodipine is extensively biotransformed to inactive metabolites. 10% of amlodipine is excreted unchanged in urine. Changes in the concentration of amlodipine in the plasma do not correlate with the degree of renal dysfunction. Patients with impaired renal function may use standard doses of amlodipine.Amlodipine is not removed by dialysis.
Patients with impaired liver function. Information on the use of amlodipine in patients with impaired liver function is very limited. In patients with hepatic insufficiency, clearance of amlodipine is reduced, which leads to an increase in the half-life and an increase in AUC by about 40-60%.
Where are you. Usually, oral clearance for children 6 to 12 years of age and from 13 to 17 years was 22.5 and 27.4 l / hr respectively for boys and 16.4 and 21.3 l / h respectively for girls. There is a significant variation in the exposure of different patients. Information for patients under 6 years of age is limited.
Basic physical and chemical properties: Aladine 10 mg - white or almost white tablets with a flat surface, with a rash and a chamfer; Aladine 5 mg is a round form tablet with a biconvex surface of white or almost white color. On the surface of the tablets, marble is allowed.
Aladine 10 mg - 3 years. Aladine 5 mg - 2 years. Do not apply after the expiry date stated on the packaging.
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
10 tablets in a blister. In 3 or 5 blister packs.