Description
Latin name
Coaprovel
Release form
Tablets.
Packing
In 1 blister pack of 14 tablets. In a cardboard bundle 2 blisters.
Pharmacological action
Coaproval is a combined antihypertensive drug containing the angiotensin II receptor antagonist irbesartan and the thiazide hydrochlorothiazide diuretic. The combination of these ingredients has additive antihypertensive effects, lowering blood pressure to a higher degree than each of them individually.
The selective antagonism of irbesartan against AT 1 receptors is manifested by an increase in the content of renin and angiotensin II and a decrease in the content of aldosterone in the blood serum. The level of potassium in the blood serum changes slightly during treatment with irbesartan with monotherapy in the recommended doses.
Irbesartan does not inhibit ACE (kininase II), which promotes the formation of angiotensin II, and also converts bradykinin into inactive metabolites. Irbesartan does not need metabolic activation to manifest its action.
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the renal mechanisms of reabsorption of electrolytes, increasing the excretion of sodium and chlorides in approximately equivalent amounts, inhibit reabsorption of sodium. Hydrochlorothiazide reduces plasma volume by increasing plasma renin activity and aldosterone secretion, followed by an increase in urine potassium and a decrease in serum potassium. Presumably, by blocking the renin-angiotensin-aldosterone system, the combined use of irbesartan leads to the prevention of the loss of serum potassium caused by this diuretic.
When taking hydrochlorothiazide, the onset of diuresis occurs in the first 2 hours after ingestion, reaches a peak within 4 hours, the effect lasts about 6-12 hours.
A decrease in blood pressure manifests itself after taking the first dose of Coaprovel, the maximum effect is observed after 6-8 weeks of treatment. The effect persists for prolonged use (1 year). The increase in blood pressure, although not studied during Coaprovel treatment, was not detected when irbesartan or hydrochlorothiazide was used separately.
There is no difference in response to Coaprovel depending on age or gender.
Indications
Arterial hypertension.
Contraindications
– Hereditary galactose intolerance, lactase deficiency or malabsorption of glucose and galactose.
– Pregnancy.
– Lactation period – 18 years and up to 18 years of age and up to 18 years. safety not established.)
– Hypersensitivity to the drug’s components
For the use of hydrochlorothiazide:
– Severe renal failure (CC – Refractory hypokalemia, hypercal cemia.
– Severe liver failure.
– Biliary cirrhosis.
– Cholestasis.
– Hypersensitivity to other sulfonamide derivatives.
Use during pregnancy and lactation
Coaproval is contraindicated in the second and third trimesters of pregnancy. If pregnancy is diagnosed, then Coaprovel should be canceled as soon as possible. The skull and renal function should be checked by ultrasound, if, inadvertently, the therapy lasted for a long time.
Coaproval is contraindicated throughout the lactation period.
Dosage and administration
Coaprovel can be used 1 time / day. before or during meals in patients whose blood pressure is not adequately controlled with irbesartan or hydrochlorothiazide alone.
Coaprovel 300/25 mg is prescribed for patients whose blood pressure is not sufficiently controlled by irbesartan (300 mg) or Coaprovel (300 / 12.5 mg).
Use of the drug in doses of more than 300 mg of irbesartan / 25 mg of hydrochlorothiazide 1 time / day. not recommended.
Before using Coaprovel, you need to adjust the reduced BCC and / or sodium content. If this fails, Consider taking a lower initial dose.
– Use in patients with impaired liver function: Coaproval is contraindicated in patients with severe hepatic impairment. In patients with impaired liver function, thiazides should be used with caution, but in patients with mild to moderate hepatic insufficiency, dose adjustment is not required.
– Use in patients with impaired renal function: Since the preparation includes hydrochlorothiazide Coaprovel is contraindicated in patients with severe impaired renal function (KK30 ml / min.
– Use in elderly patients: There is no need to adjust the dose of Coaprovel.
Side effects of
From the hemopoietic system: aplastic anemia, bone marrow depression, hemolytic anemia, leukopenia, neutropenia / agranulocytosis, thrombocytopenia.
From the side of the central nervous system and peripheral nervous system: depression, sleep disturbances, dizziness, paresthesia, anxiety.
From the side of the organ of vision: transient blurry vision, xanthopsia.
From the cardiovascular system: arrhythmias, postural hypotension.
From the respiratory system: respiratory distress syndrome (including pneumonitis and pulmonary edema).
From the digestive system: jaundice (intrahepatic cholestatic jaundice).
Allergic reactions: anaphylactic reactions, toxic necrosis of the epidermis, skin reactions such as lupus erythematosus, necrotic angiitis (vasculitis, skin vasculitis), photosensitivity reactions, rash, exacerbation of skin manifestations of lupus erythematosus, urticaria.
From the musculoskeletal system: muscle cramps, weakness.
From the urinary system: interstitial nephritis, renal dysfunction.
Other: fever.
On the part of laboratory indicators: electrolyte imbalance (including hypokalemia and hyponatremia), glucosuria, hyperglycemia, hyperuricemia, increase in cholesterol and TG.
Drug Interaction
It is possible to increase the antihypertensive effect of Coaprovel while using other antihypertensive drugs. The 300mg / 25mg irbesartan / hydrochlorothiazide combination should be used with caution in conjunction with other antihypertensive agents, including calcium channel blockers and beta-blockers. Prior high-dose diuretic therapy may lead to hypovolemia and the risk of arterial hypotension.
Reversible increases in serum lithium concentrations and toxic effects were observed with concomitant use of lithium with ACE inhibitors. With regard to irbesartan, similar effects have been extremely rare so far. In addition, renal clearance of lithium is reduced by thiazides, therefore, the risk of lithium toxicity may be increased in the case of Coaprovel. Therefore, the combination of lithium and Coaprovel is not recommended. Careful monitoring of serum lithium levels is recommended if the combination is necessary.
The hypokalemic effect of hydrochlorothiazide is attenuated by the potassium-sparing effect of irbesartan. However, this effect of hydrochlorothiazide may be exacerbated by other drugs that cause potassium loss and hypokalemia (eg, diuretics, laxatives, amphotericin, carbenoxolone, penicillin G sodium, salicylic acid derivatives). On the contrary, based on the experience of using other medicines that reduce the activity of the renin-angiotensin system, the concomitant use of potassium-sparing diuretics, dietary supplements, salt substitutes, containing potassium, or other drugs that can increase serum potassium levels (eg, sodium salt of heparin), may lead to increased serum potassium. Patients at risk are advised to have adequate control of serum potassium levels.
We recommend periodic monitoring of serum potassium levels when co-administered with co-administration of drugs and drugs that are affected by impaired serum potassium balance (eg, digitalis glycosides, antiarrhythmic agents).
When concomitant use of angiotensin II antagonists and NSAIDs (eg, selective COX-2 inhibitors, acetylsalicylic acid> 3 g / day and non-selective NSAIDs), antihypertensive effects may be attenuated.
As with ACE inhibitors, co-administration of angiotensin II antagonists and NSAIDs may increase the risk of renal dysfunction, including the likelihood of acute renal failure, and lead to increased serum potassium, especially in patients with impaired renal function. This combination should be used with caution, especially in elderly patients. Patients should not be dehydrated. Monitoring of kidney function should be performed after initiation of combination therapy and periodically thereafter.
Irbesartan pharmacokinetics are not exposed when co-administered with hydrochlorothiazide. Irbesartan is mainly metabolised by CYP2C9 and, to a lesser extent, by glucuronidation. No significant pharmacokinetic and pharmacodynamic interaction was observed, when irbesartan is co-administered with warfarin, a CYP2C9 metabolised drug. The effect of CYP2C9 inducers, such as rifampicin, on the pharmacokinetics of irbesartan has not been evaluated.
Digoxin pharmacokinetics did not change when co-administered with irbesartan.
Increased orthostatic hypotension may occur with concomitant use with thiazide diuretics of ethanol, barbiturates or anesthesia.
Hydrochlorothiazide may require dose adjustment of hypoglycemic agent.
The absorption of hydrochlorothiazide is reduced in the presence of anion exchange resins.
With the simultaneous use of hydrochlorothiazide and ACS or ACTH, a more pronounced electrolyte balance disturbance is possible, in particular, increased hypokalemia.
Hypokalemia and hypomagnesemia, caused by a thiazide diuretic, contribute to the manifestation of arrhythmias caused by the digitalis.
NSAIDs may reduce the effects of thiazide diuretics in some patients.
It is possible to reduce the effectiveness of catecholamines (eg, norepinephrine) under the influence of hydrochlorothiazide.
The effect of non-depolarizing muscle relaxants can be enhanced by hydrochlorothiazide.
Dosage adjustment may be required as well. hydrochlorothiazide may increase uric acid levels in the serum. It may be necessary to increase the doses of probenecid or sulfinpyrazone. Co-administration with thiazide diuretics may increase the incidence of allergic reactions to allopurinol.
Thiazide diuretics may increase serum calcium due to reduced excretion. If calcium supplements or drugs affecting calcium levels (for example, vitamin D therapy) are to be prescribed, serum calcium monitoring and appropriate dose adjustment of calcium should be performed.
The hyperglycemic effect of beta-blockers and diazoxide can be enhanced by thiazides.
Anticholinergics (eg, atropine) may increase the bioavailability of thiazide diuretics due to decreased gastrointestinal motility.
Thiazides may increase the risk of side effects caused by amantadine.
Thiazides may reduce urinary cytotoxic drugs (eg, cyclophosphamide, methotrexate) and enhance their myelosuppressive effects.
Overdose
There is no specific information on an overdose of Coaprovel.
– Symptoms: arterial hypotension, tachycardia, bradycardia with overdosage of hydrochlorothiazide – hypokalemia, hyponatremia, dehydration as a result of excessive diuresis are most likely with an overdose of irbesartan. The most common signs and symptoms of overdose are nausea and drowsiness. Hypokalemia can lead to convulsions and / or aggravation of arrhythmias in the case of concomitant use of digitalis glycosides and antiarrhythmic agents.
– Treatment: recommended measures depending on the time elapsed since taking the drug and on the severity of the symptoms – provoking vomiting and / or gastric lavage, use of activated charcoal, careful monitoring of the patient’s condition, carrying out symptomatic and supportive therapy. Frequent monitoring of serum electrolytes and creatinine should be performed. In case of hypotension of the patient it is necessary to lay on a back with the raised lower extremities and as soon as possible to carry out compensation of salts and liquids. Irbesartan is not excreted in hemodialysis. The degree of removal of hydrochlorothiazide in hemodialysis has not been established.
Storage conditions
– Store at a temperature not exceeding 30 ° C.
– Keep out of the reach of children.
– Do not use after the expiration date.
The Expiration of
is 3 years.
Active ingredient
Hydrochlorothiazide, Irbesartan
Pharmacy terms
Prescription
Dosage form
dosage form
tablets
Sanofi-Aventis, France
