Tenox® (Tenox® )

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspPills
Composition:

1 tablet contains:

Active substance: Amlodipine maleate 6.42 mg (corresponds to amlodipine 5 mg) and 12.84 mg (corresponds to amlodipine 10 mg).

Excipients: microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch, silicon dioxide colloidal, anhydrous, magnesium stearate.

Description:

Round, biconvex tablets are white or almost white with a facet and a risk on one side.

Pharmacotherapeutic group:blocker of "slow" calcium channels
Pharmacodynamics:

The dihydropyridine derivative blocking the "slow" calcium channels of the second generation, has an antianginal and hypotensive effect. Linking with dihydropyridine receptors, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes). Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral vascular resistance (OPSS), reduces preload on the heart, reduces the need for myocardium in oxygen. Expands the main coronary arteries and arterioles in unchanged and ischemic zones of the myocardium,increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including caused by smoking). In patients with stable angina, a single daily dose increases tolerance to physical exertion, slows the development of another attack of angina and "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin tablets.

Has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the patient's position "lying" and "standing"). Reduces the degree of myocardial hypertrophy of the left ventricle, has antiatherosclerotic and cardioprotective action in ischemic heart disease (CHD). Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the heart rate (HR), inhibits platelet aggregation, increases the rate of glomerular filtration,has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria. Does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout. A significant reduction in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours. With prolonged therapy, the maximum decrease in blood pressure occurs within 6-12 hours after taking amlodipine by mouth. If after prolonged treatment amlodipine cancel, the effective decrease in blood pressure persists for 48 hours after the last dose. Then the blood pressure indicators gradually return to the baseline within 5-6 days.
Pharmacokinetics:

After oral administration amlodipine slowly absorbed from the gastrointestinal tract (GIT). The average absolute bioavailability is 64%, the maximum concentration (Cmah) in the serum is observed after 6-9 hours. Equilibrium serum concentrations (Css) are achieved after 7-8 days of therapy. Food intake does not affect the absorption of amlodipine.

The average volume of distribution is 21 l / kg body weight, indicating that most of the drug is in the tissues, and relatively less in the blood.Most of the drug in the blood (95%), binds to blood plasma proteins. Amlodipine is subjected to a slow but active metabolism in the liver in the absence of a significant "first passage" effect. Metabolites do not have significant pharmacological activity.

After a single oral intake, the half-life (T 1 /2) varies from 31 to 48 hours, with the repeated appointment of T1 / 2 is approximately 45 hours. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% - through the intestine, as well as breast milk. The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg, 0.42 l / h / kg).

In elderly patients (over 65 years of age) the excretion of amlodipine is slowed down (T1 / 2 - 65 h) compared with young patients, but this difference has no clinical significance. Elongation T1 / 2 in patients with hepatic insufficiency, it is assumed that with prolonged administration, the cumulation of the drug in the body will be higher (T1 / 2 to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier.When hemodialysis is not removed.

Indications:

Arterial hypertension (monotherapy or in combination with other antihypertensive agents).

Stable exertional angina and vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antianginal drugs).

Contraindications:

Hypersensitivity to amlodipine, a derivative of dihydropyridine and other components of the drug;

severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

collapse, cardiogenic shock;

unstable angina (with the exception of Prinzmetal's stenocardia);

clinically significant aortic stenosis;

pregnancy and lactation;

age to 18 years (efficacy and safety not studied).

Carefully:hepatic dysfunction, sinus node weakness syndrome (SSSU) (pronounced bradycardia, tachycardia), chronic heart failure of non-ischemic etiology III-TV functional class by classification NYHA, mild or moderate degree of arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), acute myocardial infarction (and within 1 month after myocardial infarction), elderly age.
Pregnancy and lactation:

There was no evidence of teratogenicity of amlodipine in the study on animals, but there is no clinical experience of its use in pregnancy and lactation. therefore amlodipine should not be given to pregnant and lactating women, as well as to women of childbearing age, unless they use reliable methods of contraception.

Dosing and Administration:

Inside, the initial dose for treatment arterial hypertension and angina pectoris is 5 mg once a day. The maximum daily dose is 10 mg once.

With arterial hypertension, the maintenance dose can be 2.5 to 5 mg (1/2 tablets of 5 mg-1 tablet of 5 mg) per day.

With angina pectoris and vasospastic angina pectoris, 5-10 mg per day, once. In order to prevent attacks of angina pectoris - 10 mg / day.

Patients with impaired hepatic function as an antihypertensive agent Tenox® should be administered with caution, at an initial dose of 2.5 mg (1/2 tablet of 5 mg each), as an antianginal agent, 5 mg.

In elderly patients may increase T1 / 2 and decrease the clearance of the drug. Dose changes are not required, but more careful monitoring of patients is necessary.There is no need for dose changes with simultaneous administration with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors. Do not require dose changes in patients with renal insufficiency.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

sometimes from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

From the side of the cardiovascular system: often - palpitations, marked decrease in blood pressure, orthostatic hypotension, peripheral edema (swelling of the ankles and feet), "tides" of blood to the skin of the face, sometimes excessive decrease in blood pressure, orthostatic hypotension, vasculitis, dyspnea; rarely - development or exacerbation of heart failure; very rarely - migraine, syncope. Some adverse effects noted in individual patients can not be differentiated with symptoms the natural course of the underlying disease: myocardial infarction, arrhythmia (in a very rare cases: bradycardia, ventricular tachycardia and atrial fibrillation), pain in the thorax.

From the central and peripheral nervous system: often - headache, dizziness, drowsiness, fatigue; sometimes - tremor, insomnia, emotional lability, unusual dreams, nervousness, depression, anxiety, paresthesia; rarely - cramps, apathy, agitation; very rarely - ataxia, amnesia, asthenia, general malaise, peripheral neuropathy.

From the digestive system: often - nausea, abdominal pain; sometimes - vomiting, changing the regime of defecation (including constipation), flatulence, anorexia, thirst; rarely - increased appetite; very rarely - dyspepsia, diarrhea, gastritis, pancreatitis, hyperbilirubinemia, gingival hyperplasia, dry mouth, increased activity of "liver" transaminases, hepatitis, jaundice (caused by cholestasis).

From the genitourinary system: sometimes - gynecomastia, pollakiuria, painful urge to urinate, nocturia; very rarely - impotence, dysuria, polyuria.

From the skin: sometimes - alopecia; rarely - dermatitis; very rarely - a violation of skin pigmentation.

Allergic reactions: sometimes - itchy skin, rash (including erythematous, maculopapular rash); very rarely - hives, angioedema, erythema multiforme.

From the musculoskeletal system: sometimes - arthralgia, muscle cramps, myalgia, back pain, arthrosis; rarely - myasthenia gravis; very rarely - muscle cramps.

From the sense organs: sometimes - ringing in the ears, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, pain in the eyes, perversion of taste; very rarely - parosmia.

Other: sometimes - increase / decrease in body weight, chills, nosebleeds, rhinitis, increased sweating; very rarely - thrombocytopenic purpura, thrombocytopenia, leukopenia, hyperglycemia, increased sweating, cold sticky sweat (against arterial hypotension), cough.

Overdose:

Symptoms: excessive peripheral vasodilation with a pronounced and possibly long-term decline in blood pressure, collapse, shock.

Treatment: gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular function, control of heart and lung function, elevated, above the level of the head, the position of the lower extremities, control of the volume of circulating blood (BCC) and diuresis. To restore the vascular tone, the use of vasoconstrictors (in the absence of contraindications to their use); with the aim ofelimination of the effects of calcium channel blockade - intravenous calcium gluconate. Hemodialysis is not effective.

Interaction:

It is possible in the treatment of hypertension, the simultaneous use of amlodipine with thiazide diuretics, alpha-adrenoblockers, beta-adrenoblockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, with prolonged-action nitrates, beta-blockers or nitrates for oral administration.

Amlodipine can be used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration.

It is possible to increase the antianginal and hypotensive effect of blockers of "slow" calcium channels (BCCC) when combined with thiazide and "loop" diuretics, verapamil, ACE inhibitors, beta-adrenoblockers and nitrates, as well as strengthening their hypotensive effect when combined with alpha1-adrenoblockers, neuroleptics.

Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless, some BCCCs can increase the severity of the negative inotropic effect of antiarrhythmic agents that cause lengthening of the interval QT (eg, amiodarone and quinidine).

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

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

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

Antiviral drugs (ritonavir) increases the plasma concentrations of BCCI, incl. amlodipine.

Isoflurane is an increase in the hypotensive effect of dihydro pyridine derivatives. Calcium preparations can reduce the effect of BCCC.

When amlodipine is used together with lithium preparations, it is possible to intensify manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Amlodipine does not change the pharmacokinetics of cyclosporine.

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

Has no significant effect on the effect of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine.

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

Grapefruit juice: simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine inwards is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Special instructions:

During the treatment with the drug Tenox® it is necessary to control the body weight and sodium intake, the appointment of an appropriate diet. It is necessary to maintain dental hygiene and supervision at the dentist (to prevent soreness, bleeding and gingival hyperplasia).

Patients with low body weight, low growth patients and patients with severe liver dysfunction may need a lower dosage.

In elderly patients, T1 / 2 and the clearance of the drug may be prolonged. Dosage changes for elderly patients are not required; with increasing the dose, more careful monitoring of patients is necessary.

If the liver function is also impaired, T1 / 2 of the drug may be prolonged. Therefore, such patients Tenox® should be administered with caution.

The effectiveness and safety of the drug in hypertensive crisis is not established.

Effect on the ability to drive transp. cf. and fur:There have been no reports of the effects of Tenox® on vehicle management or work with machinery. However, some patients, mainly at the beginning of treatment, may experience drowsiness and dizziness. When they occur, the patient must be careful when driving and working with complex mechanisms.
Form release / dosage:

Tablets of 5 mg and 10 mg.

Packaging:10 tablets per blister (out-of-the-box). By 3 or 9 blisters (contour mesh packages) are placed in a pack of cardboard along with instructions for use.
Storage conditions:

List B.

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription
Registration number:П N015578 / 01
Date of registration:06.03.2009
The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
Manufacturer: & nbsp
Representation: & nbspKRKA KRKA Slovenia
Information update date: & nbsp02.12.2009
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