Equator, tablets 10 mg+20 mg 30 pcs

Equator is a combined antihypertensive drug containing lisinopril and amlodipine.

Lisinopril is an ACE inhibitor, reduces blood levels of angiotensin II and aldosterone while increasing levels of bradykinin, a vasodilatory mediator. Effects on tissue renin-angiotensin systems. It decreases RPS and BP, pre- and post-load, pulmonary capillary pressure, has no effect on HR, while it may increase cardiac output and increase blood flow in the kidneys. Dilates arteries more than veins. Improves blood supply to ischemic myocardium.

Long-term use promotes reduction of myocardial hypertrophy and resistive artery walls. Increases myocardial tolerance to exercise in patients with chronic heart failure. Plays a role in restoring endothelial function damaged due to hyperglycemia.

Lengthens life expectancy in chronic heart failure. Slows the progression of left ventricular dysfunction after myocardial infarction not complicated by heart failure.

Hypotensive effect is observed 1 hour after oral administration of the drug, reaching a maximum after 6 hours. The duration of action depends on the dose and is 24 hours. With long-term treatment the efficacy does not decrease. There is no withdrawal syndrome with a sharp increase in BP when the treatment is stopped abruptly.

Despite the primary effect manifested in the effect on the RAAS, it is also effective in arterial hypertension with low levels of renin.
Lisinopril decreases albuminuria not only due to BP decrease, but also due to the changes in hemodynamics of glomerular apparatus and its tissue structure. It does not affect blood sugar levels in diabetic patients and does not increase the incidence of hypoglycemia.
Amlodipine is a III generation slow calcium channel blocker, has antianginal and hypotensive effect. It prevents calcium influx into myocardial cells and, to a greater extent, into smooth muscle cells of the vascular wall. It reduces the tone of arteriolar smooth muscle, OPPS and, therefore, BP.

It has an antianginal effect by dilating the arterioles and arteries and reducing the afterload. It reduces the need for oxygen and myocardial energy expenditure, as it does not cause reflex tachycardia. Probably due to the expansion of coronary arteries and arterioles it increases the supply of oxygen to the intact (especially in vasospastic angina) and ischemic areas of the myocardium. In angina improves exercise tolerance, prevents the development of an attack of angina and the formation of ischemic ST interval, reducing the frequency of angina attacks and the need for nitroglycerin use.

It does not affect myocardial conduction and contractility.

It has a long-lasting, dose-dependent hypotensive effect. Does not reduce left ventricular ejection fraction. Reduces left ventricular hypertrophy. It has antiatherosclerotic and cardioprotective effect in CHD. Its usage along with digoxin, diuretics and ACE inhibitors does not increase the risk of death in patients with chronic heart failure (functional class III-IV according to NYHA classification).

Slow absorption, wide distribution in the body and slow excretion provides prolonged action, allowing to take the drug once/ For more than 24 hours provides significant clinically significant reduction of BP in sitting and lying position. The action develops gradually, 2-4 hours after administration and is not accompanied by arterial hypotension.

Inhibits platelet aggregation, increases glomerular filtration, has a weak natriuretic effect, in diabetic nephropathy it does not increase microalbuminuria.

It does not have adverse effects on metabolic processes, does not change the level of plasma lipids. It can be prescribed to patients with concomitant bronchial asthma, diabetes and gout.

Combining lisinopril with amlodipine in one drug prevents possible adverse effects caused by counterregulation of any of the active substances. For example, a slow calcium channel blocker, by directly dilating the arterioles, can lead to sodium and fluid retention in the body and, therefore, can activate the RAAS. ACE inhibitor blocks this process, normalizes the response to salt load.

Indications

Essential hypertension (patients who are indicated for combination therapy).

Active ingredient

Composition

1 tablet contains amlodipine 10 mg and lisinopril 20 mg.

How to take, the dosage

Ingestion, regardless of meals. It is recommended in cases when taking drugs containing separately the active components of Equator in the same doses does not provide proper BP control.

The daily dose for patients not taking antihypertensives is 1 tablet.

2-3 days before therapy, the diuretic should be discontinued if this treatment is given. If diuretic withdrawal is not possible, the initial dose of Equator is 1/2 tablet per day, after which the patient should be monitored by a physician for several hours because of the possible development of symptomatic hypotension.

In cases of heart failure and severe arterial hypertension, the maintenance dose is 1 tablet.

In cases of renal insufficiency, with a creatinine clearance of 30-70 ml/min, 1/2 of the usual starting dose is prescribed because lisinopril is eliminated by the kidneys. Maintenance dose of Equator depends on individual patient’s reaction; treatment requires regular monitoring of renal function, potassium and sodium levels in blood.

Interaction

Lisinopril
Potassium-saving diuretics (e.g., spironolactone, amiloride and triamterene), potassium supplements, potassium-containing salt substitutes and other medical drugs that may increase serum potassium levels (e.g., heparin) may lead to hyperkalemia when combined with ACE inhibitors, especially in patients with renal insufficiency and other renal diseases in the history. Serum potassium concentrations should be monitored when prescribing potassium-affecting drugs concomitantly with lisinopril.

Therefore, concomitant administration should be carefully justified and performed with extreme caution and regular monitoring of both serum potassium levels and renal function. Potassium-saving diuretics may be taken together with the drug Equator only under medical supervision. If a diuretic is prescribed to a patient receiving Equator, the hypotensive effect is usually enhanced. Therefore, extreme caution should be exercised when taking Equator® in combination with diuretics. Lisinopril mitigates potassium diuretic effect. concomitant use of other antihypertensive drugs may increase the hypotensive effect of the drug Equator.

Concomitant use with nitroglycerin, other nitrates or vasodilators may cause greater BP reduction.
Concomitant use with ACE inhibitors of tricyclic antidepressants/antipsychotics, general anesthetic agents, opioid analgesics: greater BP reduction may be possible.

Ethanol increases the hypotensive effect of the drug. Allopurinol, procainamide, cytostatics or immunosuppressants (systemic GCS) may increase the risk of leukopenia when combined with ACE inhibitors.

Aitacids and colestiramine decrease the bioavailability of ACE inhibitors concomitantly.

Sympathomimetics may decrease the hypotensive effect of ACE inhibitors; the desired effect should be carefully controlled. Concomitant use of ACE inhibitors and hypoglycemic drugs (insulin and hypoglycemic agents for oral administration) may increase the probability of decreased blood glucose concentration and the risk of hypoglycemia. This phenomenon is most often observed during the first week of combined treatment and in patients with renal insufficiency. With long-term use of NSAIDs, including acetylsalicylic acid in high doses, the effectiveness of ACE inhibitors may decrease.

Additive effect when taking NSAIDs and ACE inhibitors is manifested by increased serum potassium levels and may lead to worsening of renal function. These effects are usually reversible. Very rarely, acute renal failure may develop, especially in elderly patients and patients in a state of dehydration.

The excretion of lithium may be delayed during concomitant use with ACE inhibitors and therefore serum lithium concentration should be monitored during this period. Co-administration with lithium preparations may increase manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

In concomitant use of ACE inhibitors and gold drugs (sodium aurothiomalate) by IV has described a symptom complex including facial hyperemia, nausea, vomiting and arterial hypotension.

Amlodipine

Studies in elderly patients have shown that diltiazem inhibits the metabolism of amlodipine, probably through inhibition of the CYP3A4 isoenzyme (plasma concentrations are increased by almost 50% and amlodipine effects are increased). It is possible that stronger inhibitors of CYP3A4 isoenzyme (i.e. ketoconazole, itraconazole, ritonavir) can increase the plasma concentration of amlodipine to a greater extent than diltiazem.

Concurrent use should be used with caution.

Concomitant use with inducers of CYP3A4 isoenzyme – with antiepileptic drugs (e.g., carbamazepshum, phenobarbital, phenytoin, fosphenytoin, primidone), rifampicin, herbal drugs containing St. John’s wort – may decrease the plasma concentration of amlodipine. Clinical monitoring with possible correction of amlodipine dose during treatment with CYP3A4 isoenzyme inducers and after their withdrawal is indicated. Concomitant use should be performed with caution.

. As monotherapy, amlodipine has been well combined with thiazide and “loop” diuretics, general anesthetics, beta-adrenoblockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, Digoxin, warfarin, atorvastatin, sildenafil, antacids (aluminum hydroxide, magnesium hydroxide), simethicone, cimetidine, NSAIDs, antibiotics and oral hypoglycemic drugs.

Amlodipine has no significant effect on the pharmacokinetics of ethanol. Calcium preparations may reduce the effect of slow calcium channel blockers. Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine. The hypotensive effect of Equator may be reduced when concomitantly administered with estrogens, adrenostimulants. When concomitant use with the drug Equator® procainamide, quinidine and other drugs that prolong the QT interval may contribute to its significant prolongation.

Special Instructions

– Arterial hypotension
Significant BP decrease with the development of clinical symptoms may be observed in patients with decreased BOD and/or sodium content due to diuretics, fluid loss or other reasons, such as profuse sweating prolonged vomiting and/or diarrhea. In case of arterial hypotension, the patient should be laid down and the fluid loss replenished (intravenous infusion of 0.9% sodium chloride solution) if necessary.

Preferably, recovery of fluid and/or sodium loss should be performed before starting Equator therapy. BP should be monitored after the initial dose. This is especially true in patients with CHD or cerebrovascular disease, where a pronounced decrease in BP may lead to myocardial infarction or stroke.

– Aortic and mitral stenosis
Like all vasodilators, Equator® should be prescribed with caution in patients with left ventricular outflow tract obstruction and mitral valve stenosis.

– Renal dysfunction
In some patients with arterial hypertension without marked manifestations of renovascular disease, serum creatinine and urea were observed to increase, in most cases minimal or transient, more pronounced when concomitant administration of ACE inhibitors and diuretic. This is most common in patients with a history of kidney disease.

– Angioneurotic edema

Angioneurotic edema of the face, extremities, lips, tongue, vocal folds and/or larynx have been reported in patients who have taken an ACE inhibitor, including lisinopril. In these cases, Equator should be discontinued immediately and the patient should be closely monitored until the symptoms have completely disappeared.

The swelling of the face, lips, and extremities usually resolves on its own, but antihistamines should be used to reduce the severity of symptoms.

Contraindications

Side effects

The adverse reactions that occur are usually mild and transient, and withdrawal of treatment is rarely required.

Side effects caused by the combined drug do not occur more often than in cases of taking each component separately. The most common are: headache (8%), dry cough (5%) and dizziness (3%). Possible: weakness, diarrhea, nausea, vomiting, orthostatic hypotension, skin itching, skin rash, swelling of the ankles of the feet, facial redness, chest pain, arthralgia (1-3%). The frequency of other side effects is less than 1%.

In case of hypersensitivity, angioedema of the face, extremities, lips, tongue, epiglottis and larynx may develop (0.1%). In such cases the treatment should be stopped immediately and the patient should be observed until all symptoms have disappeared.

Laboratory findings: hyperkalemia, increased creatinine, urea nitrogen, liver enzymes activity and blood bilirubin, especially in renal disease, diabetes mellitus and renovascular hypertension.

Hematopoietic organs: leukopenia, neutropenia, agranulocytosis (effect of ACE inhibitor), thrombocytopenia, erythrocytopenia, with long-term treatment a slight decrease of hemoglobin concentration and hematocrit is possible.

Other rare adverse reactions:

Cardiovascular system: arrhythmias, increased palpitations, tachycardia, probably as a result of excessive BP reduction in patients with a high risk of myocardial infarction, cerebrovascular stroke.

Gastrointestinal tract: intestinal dysfunction, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gum hyperplasia, decreased appetite.

Skin disorders: urticaria, increased sweating, itching, alopecia.

Hypersensory system disorders: impaired renal function, frequent urination, oliguria, anuria, acute renal failure, uremia, proteinuria, impotence.

Immune system disorders: syndrome with the appearance of antinuclear antibodies, accelerated sedimentation rate and arthralgia; myalgia; erythema multiforme; fever.

CNS disorders: increased somnolence, muscle fasciculation of extremities and lips, asthenia, mood lability, confusion.

Overdose

Symptoms: excessive peripheral vasodilation with a marked decrease in BP, acute vascular failure, impaired water-electrolyte balance, renal failure, hyperventilation, tachycardia, bradycardia, dizziness, anxiety, cough.

The treatment: symptomatic therapy, control of cardiac activity, BP, diuresis and water-electrolyte balance, and its correction, if necessary. If BP is significantly decreased, the patient should be placed in the supine position, lower extremities should be elevated; if therapeutic response to IV fluid administration is unsatisfactory, dopamine administration may be required. Calcium gluconate may be administered intravenously to stop the effects of amlodipine.

If necessary, IV administration of angiotensin II. Because of the slow absorption of amlodipine in some cases the stomach is washed, use activated charcoal. Lisinopril is excreted by hemodialysis; the strong degree of binding to blood proteins makes dialysis of amlodipine ineffective.

Pregnancy use

Equator is contraindicated in pregnancy.

The treatment should be discontinued as soon as possible if pregnancy is detected.

The administration of lisinopril in the second and third trimesters of pregnancy may cause fetal damage and death due to its effect on the kidneys (arterial hypotension, renal failure, hyperkalemia).

The use of Equator may cause a decrease in amniotic fluid, lead to skull and facial deformities, impaired limb development, pulmonary hypoplasia and fetal death. There are no data on these and other effects earlier in pregnancy.

The drug is contraindicated during lactation due to excretion of amlodipine with breast milk. There are no data indicating penetration of lisinopril into breast milk.

Similarities