Amlodipine Vertex pills 10mg, 60pcs

Composition

1 tablet contains an Active ingredient:

amlodipine besylate in terms of amlodipine 10 mg;

excipients:

microcrystalline cellulose,

lactose (milk sugar),

croscarmellose sodium (primellose),

calcium stearate (calcium octadecanoate).

Pharmacological action

Pharmacodynamics

Amlodipine, a dihydropyridine derivative, is a second-generation slow calcium channel blocker that has antianginal and antihypertensive effects. Binding to dihydropyridine receptors, it blocks calcium channels and reduces the transmembrane transition of ions. calcium into the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes).

Antianginal action is caused by the expansion of coronary and peripheral arteries and arterioles: with angina reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces the total peripheral vascular resistance; reduces preload on the heart, myocardial oxygen demand. Dilates the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents the development of coronary artery spasm (including caused by smoking). In patients with angina pectoris, a single daily dose increases exercise tolerance, delays the development of another angina attack and “ischemic” depression of the ST segment; reduces the frequency of angina attacks and nitroglycerin consumption.

Amlodipine has a long-term dose-dependent hypotensive effect, which is due to the direct vasodilating effect on vascular smooth muscles. In patients with arterial hypertension, a single daily dose of amlodipine provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the patient’s “lying” and “standing”positions).

Reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in coronary heart disease (CHD). It has no effect on myocardial contractility and conduction, inhibits platelet aggregation, increases glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not adversely affect the metabolism and concentration of blood lipids. The time of onset of the therapeutic effect is 2-4 hours, the duration is 24 hours.

Pharmacokinetics

After oral use, amlodipine is slowly absorbed from the gastrointestinal tract. Food intake does not affect the absorption of amlodipine. The average absolute bioavailability is 64%. The maximum concentration in the blood serum is observed after 6-9 hours. The equilibrium concentration is reached after 7-8 days of therapy. The binding to plasma proteins is 95%. The average volume of distribution is 21 l / kg of body weight. Amlodipine undergoes slow but active metabolism (90-97%) in the liver in the absence of a significant “first pass” effect. The metabolites do not have significant pharmacological activity.

The average half-life (T 1/2) is 35 hours. T 1/2 in patients with arterial hypertension — 48 hours, in elderly patients increases to 65 hours, in hepatic insufficiency-up to 60 hours, similar parameters of T 1/2 increase are observed in severe chronic heart failure, with impaired renal function-does not change.

About 60% of the oral dose is excreted by the kidneys mainly in the form of metabolites,10% in unchanged form,20-25% – with bile and through the intestine in the form of metabolites, as well as with breast milk.

The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg,0.42 l / h / kg).

Amlodipine penetrates the blood-brain barrier. It is not excreted during hemodialysis.

Indications

Arterial hypertension (monotherapy or in combination with other antihypertensive agents); Stable angina pectoris and Prinzmetal angina pectoris (monotherapy or in combination with other antianginal agents).

Use during pregnancy and lactation

No teratogenicity of amlodipine was detected in an animal study, but there is no clinical experience of its use during pregnancy and lactation.

Therefore, amlodipine should not be prescribed to pregnant and lactating women, as well as women of childbearing age, if they do not use reliable methods of contraception.

Contraindications

• hypersensitivity to amlodipine, other derivatives of dihydropyridine, other components of the drug;
• severe hypotension (systolic BP less than 90 mm Hg. calendar);
• collapse;
• cardiogenic shock;
• unstable angina (with the exception of prinzmetals angina);
• pronounced aortic stenosis;
• the age of 18 years (effectiveness and safety not established);
• lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• pregnancy;
• lactation.

With caution: impaired liver function, sinus node weakness syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of NYHA functional class III-IV, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), elderly age.

Side effects

From the cardiovascular system: often-palpitations, peripheral edema (swelling of the ankles and feet), infrequently-excessive decrease in blood pressure, orthostatic hypotension, vasculitis; rarely-development or aggravation of chronic heart failure; very rarely-rhythm disorders (bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, chest pain, migraine.

From the central nervous system: often-headache, dizziness, fatigue; infrequently. – malaise, fainting, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness, depression, anxiety; rarely-convulsions, apathy, agitation; very rarely-ataxia, amnesia.

Hematopoietic disorders: very rare — thrombocytopenia, leukopenia, thrombocytopenic purpura.

From the respiratory system: infrequently — shortness of breath, rhinitis; very rarely-cough.

From the digestive tract: often — nausea, abdominal pain; infrequently — vomiting, changes in bowel movements (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry oral mucosa, thirst; rarely — gum hyperplasia, increased appetite; very rarely — gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of “liver” transaminases, hepatitis.

From the genitourinary system: infrequently-pollakiuria, painful urination, nocturia, impotence; very rarely-dysuria, polyuria.

From the skin: rarely-increased sweating, very rarely-cold sticky sweat, xeroderma, alopecia, dermatitis, purpura, skin discoloration.

Allergic reactions: infrequently-pruritus of the skin, rash; very rarely-angioedema, erythema multiforme, urticaria.

From the musculoskeletal system: infrequently-arthralgia, muscle cramps, arthrosis, myalgia (with prolonged use), back pain; rarely-myasthenia gravis.

Others: infrequently-alopecia, tinnitus, gynecomastia, weight gain/loss, visual impairment, diplopia, accommodation disorders, xerophthalmia, conjunctivitis, eye pain, taste distortion, chills, nosebleeds, increased sweating; rarely — dermatitis; very rarely — cold sticky sweat, parosmia, skin pigmentation disorder, hyperglycemia.

Interaction

Inhibitors of microsomal oxidation can increase the concentration of amlodipine in blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes can reduce this indicator.

Unlike other BMCs, amlodipine has no clinically significant interaction with nonsteroidal anti-inflammatory drugs, especially Indometacin.

Thiazide and loop diuretics, beta-blockers, verapamil, ACE inhibitors, and nitrates enhance the antianginal or hypotensive effects of amlodipine.

Amiodarone, quinidine, alpha-1-blockers, antipsychotics (neuroleptics), and isoflurane may enhance the antihypertensive effect of amlodipine.

Calcium supplements may reduce the effect of BMCC.

When amlodipine is co-administered with lithium preparations, it is possible to increase the manifestations of neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

Antiviral agents (ritonavir) they contribute to an increase in the concentration of BMCC (including amlodipine) in blood plasma.

How to take it, course of use and dosage

Inside, regardless of food intake.

For the treatment of arterial hypertension and prevention of attacks of tension angina and vasospastic angina, the initial dose of Amlodipine is 5 mg once a day. If necessary, the daily dose can be increased to a maximum of 10 mg (once a day).

Patients with impaired liver function as a hypotensive agent, Amlodipine is prescribed with caution, at an initial dose of 2.5 mg (1/2 tablet of 5 mg), as an antiangial agent-5 mg.

In elderly patients, T 1/2 may increase and creatinine clearance (CC) may decrease. No dose changes are required, but patients should be monitored more closely.

No dose adjustment is required when co-administered with thiazide diuretics, beta-blockers, and angiotensin-converting enzyme (ACE) inhibitors. No dose adjustment is required in patients with renal insufficiency.

Overdose

Symptoms:

marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including shock and death).

Treatment:

gastric lavage, use of activated charcoal (especially in the first 2 hours after an overdose), maintenance of the cardiovascular system, monitoring of heart and lung function indicators, Trendelenburg pose, monitoring of the volume of circulating blood and diuresis. To restore vascular tone-the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade — intravenous use of calcium gluconate. Hemodialysis is not effective.

Special instructions

During treatment with Amlodipine, it is necessary to monitor the body weight of patients and the amount of sodium salt they consume; an appropriate low-salt diet is prescribed.

It is necessary to maintain dental hygiene and regularly visit the dentist (to prevent soreness, bleeding and gum hyperplasia).

The dosage regimen of Amlodipine in elderly patients is similar to that in patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.

Despite the absence of “withdrawal” syndrome in BMCC, a gradual dose reduction is recommended before discontinuing treatment.

Amlodipine does not affect the plasma concentrations of potassium, glucose, triglycerides, total cholesterol, low-density lipoproteins, uric acid, creatinine and urea nitrogen in the blood.

Abrupt discontinuation of the drug should be avoided due to the risk of worsening angina pectoris.

Amlodipine tablets are not recommended for hypertensive crisis.

Patients with low body weight, short stature, and severe hepatic impairment may require a lower dose.

Effects on the ability to drive vehicles and operate mechanisms: There have been no reports of the effect of Amlodipine on driving vehicles or working with mechanisms. However, some patients may experience drowsiness and dizziness, especially at the beginning of treatment. If they occur, you should be careful when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets are white or almost white in color, flat-cylindrical with a chamfer.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 ° C.

Shelf

life is 3 years.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Angina, Hypertension