Lerkamen Duo (Coripren) tabs 10mg + 20mg #28

Lerkamen Duo instruction

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pharmachologic effect

The drug is a combination of an ACE inhibitor and a slow calcium channel blocker.

Lercanidipine

Lercanidipine, a derivative of the dihydropyridine series, inhibits transmembrane calcium flux into cardiac and smooth muscle cells. The mechanism of the antihypertensive effect is due to the direct relaxing effect on vascular smooth muscle, resulting in reduced round vascular disease. It has a prolonged antihypertensive effect. Due to the high selectivity to vascular smooth muscle cells, there is no negative inotropic effect.

Enalapril

Enalapril is an ACE inhibitor that inhibits the formation of angiotensin II and eliminates its vasoconstrictor effect. Reduces blood pressure, without causing an increase in heart rate and minute volume. Reduces the round neck, reduces afterload and preload on the heart. Reduces pressure in the right atrium and the pulmonary circulation.
It does not affect the metabolism of glucose, lipoproteins, as well as the function of the reproductive system.

Pharmacokinetics

Pharmacokinetic interaction with simultaneous use of enalapril and lercanidipine was not observed.

Lercanidipine

Suction
Lercanidipine is completely absorbed in the digestive tract after oral administration. With the "first pass" through the liver, due to high metabolism, the absolute bioavailability when administered after a meal is approximately 10%, when taken on an empty stomach, bioavailability decreases by 1/3. Bioavailability after administration of lercanidipine is increased 4 times if Lerkamen Duo is taken no later than 2 hours after ingestion of fatty foods. Therefore, the drug should be taken at least 15 minutes before meals. Cmax in the blood plasma is reached in 1.5-3 hours. It does not accumulate when re-used.
The duration of the therapeutic effect of lercanidipine is 24 hours. The concentration of lercanidipine in the blood plasma when administered orally is in a nonlinear dependence on the dose. When taking 10 mg, 20 mg or 40 mg Cmax of lercanidipine in the blood plasma was determined in the ratio 1: 3: 8, respectively, and AUC - in the ratio 1: 4: 18, which implies a progressive saturation during the "first passage" through the liver. Accordingly, bioavailability increases with increasing dose.
Distribution
The distribution of lercanidipine from blood plasma to tissues and organs occurs rapidly and intensively. The binding of lercanidipine to plasma proteins exceeds 98%.
Metabolism
Lercanidipine is metabolized by the liver isoenzyme CYP3A4 to form inactive metabolites.
Removal
Lerkamen Duo in its unchanged form is practically not detected in the urine and feces. About 50% of the dose of lercanidipine is excreted by the kidneys, the average T1 / 2 of lercanidipine is 8-10 hours.
Pharmacokinetics in special clinical situations
In elderly patients and patients with mild or moderate renal insufficiency or with mild or moderate hepatic insufficiency, the pharmacokinetic parameters of lercanidipine are the same as in the general group of patients.
In patients with severe renal insufficiency or in patients on hemodialysis, lercanidipine is eliminated by the kidneys in a higher amount (about 70%).
In patients with liver failure (moderate to severe), the systemic bioavailability of lercanidipine is increased because the drug is metabolized mainly in the liver.
In patients with renal and hepatic insufficiency, the plasma protein content is reduced, so the free fraction of lercanidipine may be increased.

Enalapril

Suction
The percentage of enalapril absorption after oral administration is about 60%. Cmax enalapril in plasma is observed after 1 h. Eating does not affect the absorption of enalapril.
Distribution
When ingested, it is rapidly hydrolyzed to enalaprilat, which has an inhibitory effect on ACE. Cmax enalaprilat in serum is observed in 3-4 hours after taking Lerkamen Duo. The binding of enalapril to plasma proteins does not exceed 60%.
Metabolism
When ingestion is hydrolyzed to the main metabolite - enalaprilat.
Removal
About 40% of enalapril in the form of enalaprilat and about 20% of unchanged enalapril is excreted by the kidneys.

Pharmacokinetics in special clinical situations

In patients with renal failure, the duration of exposure to enalapril and enalaprilat increased.
In patients with mild or moderate renal insufficiency (CK 40-60 ml / min) while taking 5 mg of enalapril 1 time / day, the AUC plateau stage of enalaprilat is doubled compared with patients with normal liver function.
In patients with severe renal insufficiency (CK≤30 ml / min), the AUC increases by about 8 times. In this stage of renal failure, T1 / 2 enalaprilat increases with repeated administration of enalapril maleate and the time to reach the AUC plateau stage is slowed down. Enalaprilat can be removed from the general bloodstream by hemodialysis. Dialysis clearance is 62 ml / min.

Indications

    Essential hypertension (with the ineffectiveness of lercanidipine monotherapy 10 mg) - dose 10 mg + 10 mg;
    essential hypertension (with the ineffectiveness of monotherapy with enalapril 20 mg) - a dose of 10 mg + 20 mg.

Contraindications for Lerkamen Duo

    Impaired outflow from the left ventricle, including aortic stenosis;
    chronic heart failure in the stage of decompensation;
    hereditary and / or idiopathic angioedema (including history);
    angioedema with the use of ACE inhibitors (in history);
    unstable angina;
    the first month after myocardial infarction (within 28 days);
    severe renal impairment (CC <30 ml / min), including patients on hemodialysis;
    severe liver failure;
    simultaneous use with powerful inhibitors of isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin), cyclosporine, grapefruit juice;
    lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome;
    children and adolescents up to 18 years;
    Hypersensitivity to lercanidipine, enalapril or to any other ACE inhibitor and other BCCA, a derivative of dihydropyridine, as well as to any other component of the drug.

Carefully

    sick sinus syndrome (without simultaneous use of an artificial pacemaker);
    dysfunction of the left ventricle and ischemic heart disease;
    renal failure (CC more than 30 ml / min);
    renovascular hypertension;
    condition after kidney transplantation (experience of use is limited);
    liver failure;
    oppression of bone marrow hematopoiesis;
    severe autoimmune diseases of the connective tissue (including scleroderma, systemic lupus erythematosus);
    simultaneous use with immunosuppressants, allopurinol, procainamide;
    diabetes;
    surgery and general anesthesia;
    patients on a diet restricting salt intake;
    hyperkalemia;
    conditions accompanied by a decrease in the BCC, incl. diarrhea, vomiting, primary aldosteronism.

Dosage and administration

Tablets are taken orally, preferably in the morning, at least 15 minutes before a meal, without chewing, with a sufficient amount of water. Do not drink grapefruit juice.
The drug Lerkamen Duo is not intended for the initial treatment of hypertension.
With the ineffectiveness of monotherapy with lercanidipine 10 mg, you should start taking Coripren® 10 mg of lercanidipine + 10 mg of enalapril.
If enalapril 20 mg monoterpy is ineffective, you should start taking Coripren® 10 mg of lercanidipine + 20 mg of enalapril. The dose of Lerkamen Duo is selected by the doctor.

Use during pregnancy and lactation

Use of the drug Lerkamen Duo is not recommended to be used at pregnancy.
ACE inhibitors can cause disease or death of the fetus or newborn when prescribed in the second and third trimesters of pregnancy. The use of ACE inhibitors during this period was accompanied by a negative effect on the fetus and newborn, including the development of arterial hypotension, renal failure, hyperkalemia and / or hypoplasia of the cranial bones in the newborn. Perhaps the development of oligohydramnios, apparently due to a decrease in renal function of the fetus. This complication can lead to contracture of the extremities, deformation of the bones of the skull, including its facial part, and lung hypoplasia. The teratogenic effect in the use of ACE inhibitors (enalapril) in the first trimester has not been proven, but this possibility should not be excluded. Patients on therapy with ACE inhibitors when planning pregnancy should switch to alternative antihypertensive treatment regimens.
The use of Lerkamen Duo in women of childbearing age who do not use reliable means of contraception is not recommended.
The use of the drug during breastfeeding is not recommended, because enalapril and its main metabolite - enalaprilat enter breast milk.

Side effects of Lerkamen Duo

The incidence of adverse events was classified as follows: very often (1/10), often (1/100), infrequently (1/1000), rarely (1/10 000), very rare (<1/10 000).

Lercanidipine + enalapril

From the side of the central nervous system: often - dizziness; infrequently - headache.
From the side of the psyche: rarely - anxiety.
On the part of the skin: infrequently - dermatitis, swelling of the lips, erythema, urticaria, rash.
On the part of the urogenital system: infrequently - erectile dysfunction, pollacuria, polyuria, nocturia.
On the part of the immune system: infrequently - hypersensitivity to one of the components of Lerkamen Duo, angioedema.
From the musculoskeletal system: infrequently - arthralgia.
On the part of the digestive system: infrequently - abdominal pain, nausea, constipation, dyspepsia, glossitis.
From the hemopoietic system: infrequently - thrombocytopenia.
On the part of the respiratory system: often - cough; infrequently - dry throat, pharyngeal-laryngeal pain.
Since the cardiovascular system: often - "tides" of blood to the skin of the face; infrequently - palpitations and tachycardia, marked reduction in blood pressure, circulatory collapse, congestive heart failure.
On the part of the organ of hearing: often - vertigo, incl. position dizziness.
Laboratory indicators: infrequently - decrease in hemoglobin level, increase in ALT activity, ACT.
Others: often - peripheral edema, infrequently - asthenia, fatigue, feeling of heat.

Enalapril

From the side of the central nervous system: very often - dizziness; often - headache; infrequently - paresthesia.
On the part of the psyche: often - depression; infrequently - confusion, drowsiness, insomnia, nervousness; rarely - pathological dreams, sleep disturbance.
For the skin: often - a rash; infrequently - increased sweating, itching, urticaria, alopecia; rarely - erythema multiforme, exfoliative dermatitis, Stevens-Jones syndrome, Lyell's syndrome, pemphigus.
From the genitourinary system: infrequently - renal failure, proteinuria, erectile dysfunction; rarely - gynecomastia, oliguria.
On the part of the immune system: often - hypersensitivity, angioedema of the face, extremities, lips, tongue, vocal folds and / or larynx; rarely, autoimmune disorders.
On the part of metabolism: infrequently - hypoglycemia, anorexia.
From the musculoskeletal system: Infrequently - muscle spasm.
On the part of the digestive system: very often - nausea; often - diarrhea, abdominal pain, taste disturbance; infrequently - intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, dryness of the oral mucosa, pain in the stomach, stomach ulcer or duodenal ulcer; rarely - stomatitis, aphthous stomatitis, glossitis; very rarely - intestinal angioedema.
On the part of the liver and biliary tract: rarely - liver failure, hepatitis (cholestatic or necrotic), cholestasis.
From the hemopoietic system: infrequently - anemia, incl. aplastic and hemolytic; rarely - thrombocytopenia, neutropenia, agranulocytosis, pancytopenia, lymphadenopathy, insufficiency of bone marrow hematopoiesis.
On the part of the respiratory system: very often - cough; often - shortness of breath; infrequently - rhinorrhea, pharyngeal and laryngeal pain, dysphonia, bronchospasm, asthma; rarely - lung infiltration, rhinitis, alveolar allergic / eosinophilic pneumonia.
On the part of the organ of vision: very often - a decrease in visual acuity.
On the part of the organ of hearing: infrequently - ringing in the ears, vertigo.
Since the cardiovascular system: often - arrhythmia, stenocardia, tachycardia, myocardial infarction, marked reduction in blood pressure, syncope, stroke, due to excessive reduction in blood pressure in patients with increased risk; infrequently, palpitations, flushing of blood to the skin of the face, orthostatic hypotension; rarely Raynaud's syndrome.
Laboratory indicators: often - hyperkalemia, an increase in creatinine in the blood; infrequently - an increase in the urea content in the blood, a decrease in the sodium content in the blood; rarely, an increase in hemoglobin and hematocrit, an increase in liver enzymes and a decrease in bilirubin concentration in the blood.
Other: very often - asthenia; often - increased fatigue, chest pain; infrequently - indisposition.
Also described is a symptom complex, including facial flushing, nausea, vomiting and a pronounced decrease in blood pressure and can develop with the simultaneous use of ACE inhibitors and a gold preparation (sodium aurothiomalate) IV.

Lercanidipine

From the side of the central nervous system: infrequently - dizziness, headache.
On the part of the psyche: rarely - drowsiness.
For the skin: rarely - a rash.
On the part of the immune system: very rarely - hypersensitivity.
From the genitourinary system: rarely - polyuria.
On the part of the musculoskeletal system: rarely - myalgia.
On the part of the digestive system: rarely - nausea, dyspepsia, diarrhea, abdominal pain, vomiting.
On the part of the cardiovascular system: infrequently - tachycardia, feeling of heartbeat, "flush" of blood to the skin of the face; rarely - angina; very rarely - fainting.
Other: infrequent - peripheral edema; rarely - asthenia, fatigue.

special instructions

Patients with severe arterial hypotension with systolic blood pressure less than 90 mm Hg, as well as patients with decompensated heart failure, require special attention in the treatment of hypertension.
Transient arterial hypotension is not a contraindication to the continuation of treatment, since After completing the BCC, we can expect an adequate response to taking the drug.
Special care must be taken in the initial stages of treatment of patients with mild and moderate renal failure.
Patients with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney are particularly at risk for developing hypotension or renal failure due to the use of ACE inhibitors. For this group of patients, treatment should take place under the strict supervision of a physician, with careful selection of the dose and the appointment of low doses of Lerkamen Duo. Before and during treatment it is necessary to monitor kidney function.
Special care should be taken at the initial stages of treatment of patients with mild and moderate severity of liver failure. In the event of jaundice and a significant increase in the activity of liver enzymes, it is necessary to urgently stop taking ACE inhibitors and consult a doctor.
Due to the increased risk of anaphylactic reactions, it should not be prescribed to patients undergoing hemodialysis using high-strength polyacrylonitrile membranes (AN69) undergoing low-density lipoprotein apheresis with dextran sulphate and immediately prior to desensitization to wasp or bee venom.
Like other ACE inhibitors, it has a less pronounced antihypertensive effect in patients of the Negroid race compared with other races.
Due to the use of enalapril, angioedema of the face, limbs, tongue, pharynx or larynx may develop. In this case, you should immediately stop taking the drug. Angioedema of the larynx can be fatal. Angioedema of the tongue, pharynx, or larynx can lead to airway obstruction, you must immediately enter 0.3-0.5 ml of epinephrine (adrenaline) solution in a 1: 1000 ratio and maintain airway patency (intubation or tracheostomy).
Among patients of the Negroid race, who receive treatment with an ACE inhibitor, the incidence of angioedema is higher than among patients of a different race.
Patients with a history of angioedema, not associated with the use of ACE inhibitors, have an increased risk of developing angioedema when using any ACE inhibitor.
Before surgery (including dentistry) it is necessary to warn the surgeon / anesthesiologist about the use of ACE inhibitors. During surgical interventions and / or during general anesthesia with the use of agents that cause hypotension, ACE inhibitors can block the formation of angiotensin II in response to compensatory release of renin. If this develops a pronounced decrease in blood pressure, explained by a similar mechanism, it can be adjusted by increasing the BCC.
Hyperkalemia can develop during therapy with ACE inhibitors, incl. and enalapril. Risk factors for hyperkalemia are renal failure, advanced age, diabetes mellitus, some concomitant conditions (reduced BCC, acute heart failure in the decompensation stage, metabolic acidosis), simultaneous use of potassium-sparing diuretics (such as spironolactone, eplerenone, triamterene, amyloride), as well as drugs potassium or potassium-containing substitutes for table salt and the use of other drugs that increase the content of potassium in the blood plasma (for example, heparin). Hyperkalemia can lead to serious cardiac arrhythmias, sometimes fatal. The combined use of the above preparations must be carried out with caution.
It is not recommended to take alcohol during drug therapy.
There is information about reversible biochemical changes in the heads of spermatozoa with the use of calcium channel blockers, which may impair their ability to fertilize.

Influence on ability to drive motor transport and control mechanisms

It should be borne in mind the possibility of weakness and drowsiness, so care must be taken when performing work that requires increased attention, especially at the beginning of treatment, when increasing the dose of Lerkamen Duo and when driving.

Interaction

The antihypertensive effect of Coriprene can be potentiated by other drugs that reduce blood pressure, such as diuretics, beta-blockers, alpha-blockers, and others.
In addition, the following effects of interaction can be observed when used simultaneously with other drugs.

Lercanidipine

The drug should not be taken in combination with inhibitors of CYP3A4, such as ketoconazole, itraconazole, erythromycin and others, with cyclosporine and grapefruit juice (increase the concentration in the blood and lead to potentiation of the antihypertensive effect).
Care must be taken when taken concurrently with drugs such as terfenadine, astemizole, class III antiarrhythmic drugs (eg, amiodarone) and quinidine.
Simultaneous use with anticonvulsants (for example, phenytoin, carbamazepine) and rifamycin can lead to a decrease in the antihypertensive effect of lercanidipine.
Reception of digoxin should be carefully monitored to identify the clinical signs of digoxin toxicity.
Taking Lerkamen Duo with midazolam leads to an increase in the absorption of lercanidipine in the gastrointestinal tract and a decrease in the rate of absorption.
Metaprolol reduces lercanidipine's bioavailability by 50%.
Cimetidine at a dose of 800 mg / day does not lead to significant changes in the content and concentration of lercanidipine in the serum, however, with such a combination, special caution is required, because with higher doses of cimetidine, the bioavailability of lercanidipine, and, consequently, its antihypertensive effect, may increase.
Fluoxetine has no effect on the pharmacokinetics of lercanidipine.
In the case of taking the drug with simvastatin, Lerkamen Duo should be taken in the morning, and simvastatin - in the evening.
Reception of lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter.

Enalapril

Simultaneous intake of the drug with potassium salts, with potassium-sparing diuretics (spironolactone, triamterene, eplerenone, amiloride), ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, heparins (low molecular weight or non-refractioned), cyclosporine, a figure and a figure I’ll be in a case I’ll be a case I’ll be a case I’ll be a case I’ll be a case.
He is recommended to use together with lithium salts (if the reception of such a combination is necessary, then carry out careful control over the concentration of lithium in the blood plasma).
Simultaneous use with antidiabetic drugs (both oral and insulin) can cause the development of hypoglycemia in the first week of treatment.
Diuretics ("loop" and thiazide) can cause a decrease in BCC and thus increase the risk of a pronounced decrease in blood pressure during drug treatment.
Prolonged use of NSAIDs can reduce the antihypertensive effect of ACE inhibitors.
Both NSAIDs and ACE inhibitors (enalapril) increase the potassium content in the blood, which can lead to impaired renal function.
Baclofen enhances the antihypertensive effect.
Cyclosporine increases the risk of hyperkalemia.
Ethanol enhances the antihypertensive effect of ACE inhibitors.
Tricyclic antidepressants, neuroleptics, drugs for general anesthesia, opioid analgesics can lead to a further decrease in blood pressure.
Corticosteroids (except hydrocortisone as a replacement therapy for Addison's disease) reduce the antihypertensive effect (fluid retention, followed by an increase in BCC).
Combined use with other antihypertensives can enhance the antihypertensive effect of enalapril.
Combined use with nitroglycerin and other nitrates and vasodilators leads to an even more pronounced decrease in blood pressure.
Allopurinol, cytostatics, immunosuppressants, systemic corticosteroids, and procainamide may lead to an increased risk of leukopenia.
Antacids help reduce the bioavailability of ACE inhibitors.
Sympathomimetics can reduce the antihypertensive effect.
Enalapril can be used simultaneously with acetylsalicylic acid (as an antiplatelet agent).
With simultaneous use of Lerkamen Duo gold (sodium aurothiomalate) in / in possible development of side effects.

Overdose

There is no information about drug overdose. Presumably, in the case of an overdose, it can cause states caused by an overdose of any of the active ingredients.

Lercanidipine

Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia, vomiting.
Treatment: symptomatic treatment, the choice of treatment method depends on the degree of overdose and the observed symptoms. The following methods of medical care are used: gastric lavage, taking high doses of catecholamines, furosemide, cardiac glycosides and plasma substitutes, activated carbon, laxatives, and iv administration of dopamine. Also, to prevent the development of bradycardia, it is possible in / in the introduction of atropine.

Enalapril

Symptoms: The main symptom of an overdose is a pronounced decrease in blood pressure, which is accompanied by a blockade of the renin-angiotensin-aldosterone system. Collapse, electrolyte imbalance, renal failure, hyperventilation, tachycardia, heart palpitations, bradycardia, dizziness, anxiety, and cough may also develop.
Treatment: symptomatic treatment. In severe cases, it is recommended to / in the introduction of a 0.9% solution of sodium chloride and, if possible, the infusion of angiotensin II and / or catecholamines. If overdose symptoms developed immediately after taking the drug, then it is necessary to induce vomiting, gastric lavage and taking drugs from the group of adsorbing agents or sodium sulfate.

Storage conditions

Lerkamen Duo should be stored out of reach of children at a temperature not higher than 25 ° C.
Shelf life - 2 years.

Release form and composition

The tablets covered with a film cover of white color, round, biconvex; on the cross-section - the core of a light yellow color.
1 tab.
lercanidipine hydrochloride 10 mg
enalapril maleate 10 mg
Excipients: lactose monohydrate - 102 mg, microcrystalline cellulose - 40 mg, sodium carboxymethyl starch - 20 mg, povidone K30 - 8 mg, sodium bicarbonate - 8 mg, magnesium stearate - 2 mg.
The composition of the shell: white opadry (02F29056) - 6 mg (hypromellose 5cP - 3.825 mg, titanium dioxide (E171) - 1.275 mg, talc - 300 µg, macrogol 6000 - 600 µg).
Tablets, film coated yellow, round, biconvex; on the cross-section - the core of a light yellow color.
1 tab.
lercanidipine hydrochloride 10 mg
enalapril maleate 20 mg
Excipients: lactose monohydrate - 92 mg, microcrystalline cellulose - 40 mg, sodium carboxymethyl starch - 20 mg, povidone K30 - 8 mg, sodium bicarbonate - 8 mg, magnesium stearate - 2 mg.
The composition of the shell: opadry yellow (02F22330) - 6 mg (hypromellose 5cP - 3.825 mg, titanium dioxide (E171) - 1.139 mg, talc - 300 µg, macrogol 6000 - 600 µg, dye quinoline yellow (E104) - 121 µg, iron dye yellow oxide (E172) - 15 μg).

Terms of sell

You can buy Lerkamen Duo without a prescription.