Amlodipine-Teva, tablets 10 mg 30 pcs

Slow calcium channel blocker (SCB). Dihydropyridine derivative – II generation “slow” calcium channel blocker.

It has antianginal and hypotensive effects. It blocks calcium channels, reduces transmembrane transition of calcium ions into the cell (more in vascular smooth muscle cells than in cardiomyocytes).

The antianginal action is caused by the dilation of coronary and peripheral arteries and arterioles: in angina pectoris it reduces myocardial ischemia; by dilation of peripheral arterioles it reduces total peripheral resistance of vessels (TPRV), reduces post-load of the heart, reduces myocardial oxygen demand.

Dilating coronary arteries and arterioles in unchanged and in ischemic areas of the myocardium, increases the flow of oxygen to the myocardium (especially in vasospastic angina); prevents spasm of coronary arteries (including those caused by smoking).

In patients with stable angina a single daily dose increases exercise tolerance, increases time to angina attack and “coronary” ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilatory effect on the vascular smooth muscles. In arterial hypertension a single dose provides clinically significant reduction of blood pressure (BP) for 24 hours. (in patient’s “lying” and “standing” position). Orthostatic hypotension when prescribing amlodipine is quite rare. It does not cause decrease in left ventricular ejection fraction. It reduces the degree of left ventricular myocardial hypertrophy. It does not affect myocardial contractility and conduction, does not cause a reflex increase in heart rate (HR), inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect.

In diabetic nephropathy it does not increase the severity of microalbuminuria. It has no adverse effect on metabolism and concentration of blood plasma lipids and may be used for therapy of patients with bronchial asthma, diabetes mellitus and gout. Significant decrease in BP is observed after 6-10 hours, the duration of effect is 24 hours.

. In patients with diseases of the cardiovascular system, including coronary atherosclerosis with lesion of one vessel and up to stenosis of 3 or more arteries, atherosclerosis of carotid arteries, having had a myocardial infarction, percutaneous transluminal angioplasty (TLAP) of coronary arteries or patients with angina pectoris, the use of amlodipine prevents the development of intima-media thickening of carotid arteries, reduces mortality from myocardial infarction, stroke, TLAP, aorto-coronary bypass surgery; leads to a decrease in the incidence of unstable angina and progression of chronic heart failure (CHF); reduces the frequency of interventions aimed at restoring coronary blood flow.

Does not increase risk of death or complications and lethal outcomes in patients with CHF (functional class III – IV according to NYHA classification) during therapy with digoxin, diuretics and angiotensin-converting enzyme inhibitors (ACE). In patients with CHF (functional class III – IV according to NYHA classification) of non-ischemic etiology during amlodipine use there is a possibility of pulmonary edema development.

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

amlodipine besylate (in terms of amlodipine 10 mg) – 13.888 mg.

Auxiliary substances:

Microcrystalline cellulose,

calcium hydrophosphate (anhydrous),

sodium carboxymethyl starch (type A),

magnesium stearate.

How to take, the dosage

Overly, once daily with the required amount of water (100 ml).

In case of arterial hypertension and angina pectoris: the initial dose is 5 mg once daily. If there is no therapeutic effect within 2 to 4 weeks, the drug dose may be increased to 10 mg/day once.

In elderly patients: no dose adjustment is necessary.

In patients with hepatic impairment: although the T1/2 of amlodipine, like all BMCCs, is increased in patients with hepatic impairment, no dose adjustment is usually required.

In patients with renal impairment: Amlodipine-Teva is recommended at normal doses.

Interaction

Amelodipine interactions with hypotensive, antianginal and antiarrhythmic drugs

Amelodipine may be safely used for therapy of arterial hypertension together with thiazide diuretics, alpha-adrenoblockers or ACE inhibitors.

In patients with stable angina pectoris, amlodipine may be combined with other antianginal agents such as long-acting or short-acting nitrates.

The antianginal and hypotensive effects of DMARDs may be increased with thiazide and loop diuretics, ACE inhibitors and nitrates and their hypotensive effects may be increased with alpha1 – adrenoblockers.

Beta-adrenoblockers when used concomitantly with amlodipine may aggravate the course of heart failure.

While no negative inotropic effects have generally been observed with amlodipine, some BMCCs may exacerbate the negative inotropic effects of antiarrhythmic agents that cause QT interval prolongation (e.g., amiodarone and quinidine).

Interactions of amlodipine with NSAIDs

In contrast to other PBMCs, no clinically significant interaction of amlodipine (generation II PBMCs) has been found with nonsteroidal anti-inflammatory drugs (NSAIDs), including indomethacin.

Interactions not accompanied by changes in pharmacokinetics of amlodipine

Cimetidine does not affect the pharmacokinetics of amlodipine.

Grapefruit juice: Concomitant administration of 240 mg of grapefruit juice and 10 mg of oral amlodipine is not accompanied by significant changes in pharmacokinetics of amlodipine.

Aluminum- or magnesium-containing antacids: their single administration has no significant effect on amlodipine pharmacokinetics.

A single administration of 100 mg sildenafil in patients with arterial hypertension has no effect on the pharmacokinetic parameters of amlodipine.

Interactions not accompanied by changes in pharmacokinetics of other drugs

There is no effect on the serum concentration of digoxin and its renal clearance. There is no significant effect on the effect of warfarin (prothrombin time).

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

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

Ethanol (beverages containing alcohol): Amlodipine at a single and repeated use of 10 mg dose does not affect the pharmacokinetics of ethanol.

Amlodipine does not alter the pharmacokinetics of cyclosporine.

Interactions of amlodipine with antibiotics and antiviral drugs

Eritromycin when used together increases Cmax of amlodipine by 22% in younger patients and by 50% in older patients.

Antiretroviral agents (ritonavir) increase plasma concentrations of PBMCs, including amlodipine.

Interactions of amlodipine with lithium preparations and drugs for anesthesia

Neuroleptics and isoflurane – increase the hypotensive effect of dihydropyridine derivatives.

The co-administration of amlodipine with lithium preparations may increase the manifestation of neurotoxicity (nausea and vomiting, diarrhea, ataxia, intense tremor, tinnitus).

Special Instructions

Body weight and sodium intake should be controlled during therapy with Amlodipine-Teva and an appropriate diet should be prescribed.

Maintain oral hygiene and see a dentist (to prevent soreness, bleeding and gum hyperplasia).

Application in cardiovascular diseases: when using Amlodipine-Teva in patients with chronic heart failure of III and IV functional class according to NYHA classification pulmonary edema may develop.

In acute myocardial infarction Amlodipine-Teva is administered after hemodynamic stabilization.

Hepatic use: Patients with hepatic insufficiency should be under medical supervision if Amlodipine-Teva must be taken.

Perhaps increased T 1/2 and decreased drug clearance in elderly patients. No change in dosage is required, but closer monitoring of patients in this category is necessary.

Application in renal dysfunction: In patients with renal dysfunction, monitoring is necessary. The efficacy and safety of Amlodipine-Teva in hypertensive crisis have not been established.

Impact on the ability to drive motor transport and other complex mechanisms

. Although no adverse effect of Amlodipine-Teva on driving and other complex machines has been observed, however due to possible excessive decrease of BP, dizziness, somnolence and other adverse reactions, caution should be exercised in the above mentioned situations, especially at the beginning of treatment and when increasing dosage. Although there is no withdrawal in DMARDs, it is advisable to discontinue Amlodipine-Teva with a gradual reduction in dose.

Contraindications

With caution should be used: liver function disorders, sinus node weakness syndrome (marked bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of NYHA functional class III – IV, arterial hypotension, aortic stenosis, mitral stenosis, acute myocardial infarction (after first 28 days), elderly age, renal impairment.

Side effects

The frequency of adverse reactions below was determined according to the following (World Health Organization classification):

From the central nervous system: frequent – headache (especially at the beginning of treatment), dizziness, increased fatigue, somnolence; infrequent – general malaise, hypoesthesia, neuropsychiatric asthenization, paresthesia, acrodystrophic neuropathy, intensional tremor, insomnia, emotional lability, unusual dreams, nervousness, increased excitability, depression, anxiety, increased sweating; rarely – seizures, apathy, agitation; very rarely – ataxia, amnesia, migraine.

Digestive system disorders: frequent – nausea, abdominal pain; infrequent – vomiting, change of defecation mode (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry oral mucosa, thirst; rare – gum hyperplasia, increased appetite; very rare – pancreatitis, gastritis, jaundice (usually cholestatic), hyperbilirubinemia, increased activity of “liver” transaminases, hepatitis.

Cardiovascular system disorders: common – peripheral edema (ankles and feet), palpitations, “flushes” of blood to the skin of the face; infrequent – excessive reduction of BP, orthostatic hypotension , vasculitis; rare – development or aggravation of CHF course; very rare – fainting, shortness of breath, heart rhythm disorders (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, pain in the thorax, pulmonary edema.

Hematopoietic and lymphatic system disorders: very rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia.

The urinary system: infrequent – pollakiuria, painful urge to urinate, nycturia; very rare – dysuria, polyuria.

Reproductive system and mammary glands: infrequent – gynecomastia, impotence.

Respiratory system disorders: infrequent dyspnea, rhinitis; very rare – cough.

Motor system disorders: infrequent muscle cramps, myalgia, arthralgia, back pain, arthrosis; rarely – myasthenia.

Skin: infrequent alopecia; rarely dermatitis; very rare xeroderma, cold clammy sweat, impaired skin pigmentation.

Allergic reactions: rare – skin itching, rash (including erythematous, maculopapular rash); very rare – urticaria, angioedema, erythema multiforme.

Sensory system disorders: infrequent – tinnitus, visual disturbances, diplopia, accommodation disorders, xerophthalmia, conjunctivitis, eye pain; very rare – parosmia.

Metabolism disorders: very rarely – hyperglycemia.

Others: infrequent – weight loss, weight gain, perversion of taste, nasal bleeding, chills.

Overdose

Symptoms: marked BP decrease with possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including development of shock and death).

The treatment: gastric lavage, activated charcoal use (especially in the first 2 hours after overdose), maintenance of cardiovascular function, elevated position of the lower extremities, monitoring of heart and lung function parameters, control of circulating blood volume (CBV) and diuresis. To restore vascular tone – the use of vasoconstrictors (if there are no contraindications for their use). To eliminate the effects of calcium channel blockade – intravenous injection of calcium gluconate. Hemodialysis is ineffective.

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