Amlodipine is a popular drug for rapidly lowering blood pressure. It is used exclusively for the treatment of adult patients. To achieve a stable effect, therapy involves the daily use of a medication.
Material Content:
Release form, composition of the drug
The medicine is available exclusively in tablet form intended for oral use. There are 2 dosage options, 5 mg or 10 mg of the active substance amlodipine besilate. Amlodipine tablets do not contain dyes, so they have a white tint. Packed in blisters, and they are placed in cardboard boxes with instructions. The medicine is sold in 10 or 30 tablets.
The composition of Amlodipine in addition to the active component:
- magnesium salts of fatty acids;
- potato starch;
- lactobiosis;
- povidone;
- cellulose microcrystals.
Amlodipine is a derivative blocker of the so-called slow calcium channels (BMCC), a typical dihydropyridine calcium antagonist. The use of the drug has a pronounced hypotensive effect, which is achieved by accelerated potassium nutrition of myocardial cells and the vascular system. It is characterized by a relaxing effect on the smooth muscles of blood vessels.
The active substances contained in the drug lead to the expansion of peripheral blood supply channels, without exerting a concomitant effect on the heart rhythm.
Pharmacological properties and pharmacokinetics
The range of pharmacological uses of Amlodipine is based on the ability to dilate blood vessels and saturate the tissues of the cardiovascular system with the necessary amount of oxygen. The drug affects the patient's body antianginally and hypotensively, optimizing the work of coronary and peripheral vessels, and also prevents the thickening of their walls. Increases the patency of arteries and arterioles.
After the administration of dihydropyridine, the therapeutic effect of lowering blood pressure persists throughout the day (the patient should be in a lying or sitting position). It has a positive effect on ischemia. It does not affect characteristics such as heart rate, conduction and myocardial contractility.
Amlodipine reduces platelet coagulation, intensifies glomerular filtration of the kidneys. It is characterized by a slight effect on the electrolyte balance and metabolic processes in adipose tissue. It does not adversely affect the metabolic reactions that occur in blood plasma.
The medication begins to provide a therapeutic effect after 2-4 hours after administration, which persists throughout the day. The maximum concentration of active substances in the blood is fixed 7 hours after consumption. The absorption of amlodipine occurs in the stomach and intestines, food intake does not affect the degree of absorption. The stabilization of the effect of therapy in most cases is recorded after 1 week.
The drug has a slow metabolism, characterized by high intensity. Inactive metabolites formed in the liver cells in this case do not have significant pharmacological activity.
The half-life depends on the age, characteristics of the patient's body and the amount of the drug taken:
- at the first use - 31–48 hours;
- with repeated admission - 45 hours;
- in people older than 64 years - 65 hours;
- with liver dysfunction - 60 hours.
The presence of pathologies in the work of the kidneys does not affect the pharmacokinetics of Amlodipine, by hemodialysis it is not excreted. Most of the drug is excreted with urine (60%) in the form of half-life products formed in the liver. The rest is excreted in feces and breast milk.
The drug does not cause hormonal disruptions and metabolic disorders. Therefore, it is often prescribed to patients with asthma and diabetes for the treatment of high blood pressure.
What helps amlodipine
According to the annotation to the drug, indications for its appointment are:
- arterial hypertension;
- hypertension or high blood pressure;
- angina pectoris;
- spasms of arteries and veins, causing a violation of the blood supply;
- bronchial asthma;
- attacks of myocardial ischemia;
- ischemia;
- non-ischemic cardiomyopathy.
To achieve a stable pressure effect, tablets should be taken daily, and not only at times of deterioration. It is strictly forbidden to cancel the drug sharply, because it can cause the return of symptoms. It is recommended to gradually reduce the dosage of Amlodipine, reducing its consumption to nothing.
Instructions for use and dosage
Only a specialist can determine the correct dosage. To do this, he considers a number of parameters:
- patient age;
- the presence of chronic diseases, their nature and symptoms;
- general state of health;
- the weight.
In the presence of high blood pressure and angina, Amlodipine is initially prescribed in a dosage of 5 mg. In the future, to achieve the desired therapeutic effect, it is increased (but not more than by a quarter) based on the general well-being of the patient and the reaction to the drug.
Instructions for use describe several regimens of Amlodipine:
- With increased pressure, a single dose of the medication is prescribed to achieve a single effect. The need for use is due to a jump in the indicator up to 150 mm RT. Art.
- In the presence of pathologies in the liver, a trial dosage of 5 mg is prescribed, which, with a normal reaction to the drug, increases to 10 mg.
- To prevent angina attacks, 5 mg is prescribed. Along with Amlodipine, diuretics, substances that block receptors for adrenaline mediators, ACE inhibitors are used.
- For angina pectoris, a dosage of 5–10 mg is indicated for treatment, and 10 mg per day for prophylaxis.
With a sharp and sudden jump in pressure, the relief of symptoms by Amlodipine is prohibited. It is indicated only as a prophylaxis or a chronic form of the disease.
During therapy, the patient should control their own weight, as well as dose sodium intake into the body. Therefore, in parallel with the use of Amlodipine, a diet is prescribed.
The drug can cause bleeding of the gums, therefore it is recommended not only to maintain oral hygiene, but also to visit the dentist often.
During pregnancy and lactation
A calcium channel blocker is not prescribed to women during gestation because of the clinically proven negative effect of the active components of the drug on the developing fetus. Therefore, while taking Amlodipine, women should thoroughly approach the issue of contraception.
The lactation period is also a contraindication to the use of the medication, since approximately 10% of the active substances are excreted through milk. Due to the fact that Amlodipine is contraindicated in children, and especially in infants, its use during feeding is extremely undesirable. If the achievement of the desired therapeutic effect is urgently necessary for the mother, then the medication is started, and the baby is transferred to artificial mixtures.
Drug interaction
The simultaneous use of Amlodipine and antioxidants causes an increase in the concentration of active substances in the blood, and also increases the risk of side effects. Phenobarbital, Rifampicin and a number of other inducers of liver enzymes, in contrast, reduce the activity of the drug.
Antihypertensive effect is stopped by non-steroidal anti-inflammatory drugs (indomethacin, estrogens, alpha-group adrenostimulants, sympathomimetics), as well as calcium preparations.
It is interesting:estrogens - female hormones, symptoms of deficiency
The antihypertensive effect on the body is enhanced by antipsychotics, quinidine, verapamil, amiodarone, diuretics and BMCC.
Joint administration with medications containing lithium is not recommended, because it leads to intoxication of the body (noise, headaches, nausea, accompanied by vomiting, ataxia).
Contraindications, side effects and overdose
In some cases, the use of the drug can harm the health of the patient. Amlodipine is contraindicated in such circumstances:
- individual intolerance to the components of the drug;
- the period of bearing or feeding the child;
- childhood;
- myocardial circulatory disturbance;
- acute arterial hypotension;
- extreme degree of left ventricular failure.
Under the strict supervision of the attending physician, the drug can be prescribed to patients with such disorders:
- diabetes mellitus;
- pathologies of the liver;
- primary isolated myocardial damage;
- SSSU;
- chronic heart failure;
- stenosis (mitral and aortic);
- impaired lipid metabolism.
In some cases, the use of Amlodipine can cause a negative reaction of the body. It can manifest itself on the part of the cardiovascular, central nervous system, digestive and genitourinary systems, as well as the musculoskeletal system and epidermis.
Possible side effects:
- increased swelling of the limbs;
- arrhythmia, heart palpitations;
- dyspnea;
- excessive decrease in pressure;
- headache;
- vasculitis;
- syncope;
- chest pains;
- general fatigue and mood swings;
- drowsiness;
- cramps
- depression;
- sleep disturbance;
- muscle or joint pain;
- osteoarthrosis;
- itching and rash on the skin;
- violation of the digestive tract (nausea, accompanied by vomiting, flatulence, constipation or diarrhea, uncontrolled appetite);
- xerostomia;
- hyperbilirubinemia;
- jaundice;
- pain during urination;
- sexual dysfunction.
The likelihood of developing a negative reaction of the body to taking Amlodipine significantly increases if the norms recommended by experts are not observed. To eliminate the consequences of an overdose, gastric lavage is done using the calcium salt of gluconic acid. To normalize the work of the cardiovascular system, Dopamine is taken. It also helps to eliminate the drug by intensive drinking pure boiled water and activated carbon.
Analogues of the drug to normalize pressure
There are a number of drugs that are similar in action to the drug in question.
Analogs of Amlodipine:
- Vero-Amlodipine;
- Amlodifarm;
- Valsartan;
- Lisinopril;
- Perindopril;
- Amlovel;
- Norvask
- Enalapril.
Only a specialist whose patient is observed can make a decision about replacing the drug. In this case, not only the manifested side effects are taken into account, but also the achieved therapeutic result. The independent use of drugs not prescribed by a doctor can lead to serious problems and involuntary hospitalization of the patient.
