Amiloride - characteristics, properties, instructions for use of the drug
Indications for use | Dosage regimen | Side effects and contraindications | Drug interactions
Amiloride is a loop diuretic with a pronounced potassium sparing effect. The drug is prescribed for diagnosed arterial hypertension, liver cirrhosis, and nephrotic syndromes. The drug is used in veterinary clinical practice for both cats and dogs. The selection of the correct dosage should be carried out by a qualified veterinarian based on laboratory and instrumental studies.
Indications for use
Amiloride is a diuretic with a pronounced potassium-sparing effect and is a loop drug, exerting an effect in the area of the distal renal tubules. Thanks to its pharmacological effects, the active substance provokes an increase in the excretion of chlorine and sodium ions, while reducing the excretion of potassium from the body. Compared to other thiazide-type diuretics, Amiloride has a less pronounced effect.
Experts prescribe the drug to patients along with diuretics that remove potassium from the body. This reduces the risk of developing pathological conditions such as hypokalemia and hypomagnesemia.
The main indications for the use of the diuretic drug Amiloride are:
- high blood pressure - hypertension;
- chronic heart failure;
- dystrophic processes in the liver (cirrhosis);
- nephrotic syndrome.
Amiloride dosage regimen used in human and veterinary medicine
The prescription of a diuretic is carried out by the attending physician of humane medicine, and for animals - by a veterinarian. The individual specialist selects the dosage of the drug, taking into account all the characteristics and diagnosis of the patient. For humans, the daily dose of the drug should not exceed 40 mg. The average daily dose ranges from 2.5 to 20 mg. Take the drug orally with a small amount of water.
Regarding veterinary medicine, Amiloride is used for both dogs and cats once a day. The dosage is calculated based on the body weight of the animal. On average, when taken orally, the amount of active substance should not exceed 1 mg/kg body weight.
Side effects and contraindications
Side effects while taking Amiloride may occur due to individual intolerance to the active component of the drug, as well as as a result of serious damage to internal organs (for example, hypokalemia, hepatic coma) or in case of overdose. The main side effects from internal organs in response to taking Amiloride are:
- attacks of nausea and eruption of gastric contents;
- a sharp decrease in the level of potassium ions in the blood;
- severe headaches in the animal;
- lethargy and apathy.
It is not recommended to use a systemic diuretic in the following conditions:
- hepatic coma;
- failure of renal structures in severe manifestations;
- chronic lack of potassium in the blood;
- hypersensitivity to the active substance.
It is worth noting that the greatest effectiveness when taking Amiloride is observed when the drug is combined with other diuretics that remove potassium ions from the blood. This allows you to minimize the risk of developing a serious condition - hypokalemia.
Drug interactions
Amiloride, when used in combination with Enalapril, Lisonopril, Ramipril and Captopril (ACE inhibitors - angiotensin-converting enzyme, prescribed for the prevention and treatment of heart and kidney failure, as well as to reduce pressure in the arteries) leads to the development of severe typical hyperkalemia. A fatal outcome is possible in a patient when using Amiloride with potassium preparations and potassium-sparing agents. Against this background, hyperkalemia develops, causing serious consequences, including the death of the patient.
The use of a loop diuretic in combination with an antibacterial agent from the penicillin series, Amoxicillin, leads to the fact that the absorption process of the antibiotic in the digestive tract is reduced. The likelihood of developing hyperkalemia increases in patients when using the diuretic Amiloride in combination with antihypertensive drugs - Eprosartan, Candesartan, Losartan.
After penetration into the body, the active substance begins to exert its effect after 2 hours, providing a pronounced diuretic effect for 24 hours. By acting on the distal region of the renal tubules, the modern diuretic drug Amiloride accelerates the process of removing chlorine and sodium from the body, while being a potassium-sparing agent. The diuretic effect of the drug is weaker than that of thiazide diuretics.
Uperio tablets 100 mg 56 pcs ➤ instructions for use
ACE inhibitors
Uperio is contraindicated for use concomitantly with ACE inhibitors, since inhibition of neprilysin simultaneously with the use of ACE inhibitors may increase the risk of developing angioedema. The use of the drug Uperio is possible no earlier than 36 hours after discontinuation of the ACE inhibitor. The use of ACE inhibitors is possible no earlier than 36 hours after the last dose of Uperio.
Aliskiren
The simultaneous use of Uperio with aliskiren-containing drugs is contraindicated in patients with diabetes mellitus or impaired renal function (eGFR <60 ml/min/1.73 m2 and not recommended in other patients.
Not recommended drug interactions
Angiotensin receptor antagonists
Since one of the active ingredients of the drug is ARA II, simultaneous use with another drug containing ARA II is not recommended.
Drug interactions to consider
HMG-CoA reductase inhibitors (statins)
Research data indicate that sacubitril inhibits the activity of the OATP1B1 and OATP1B3 transporters. Uperio may increase the systemic exposure of OATP1B1 and OATP1B3 substrates such as statins. In patients receiving Uperio simultaneously with atorvastatin, the maximum plasma concentration (Cmax) of atorvastatin and its metabolites increased up to 2 times, and AUC increased up to 1.3 times. Caution should be exercised when statins are used concomitantly with Uperio. No clinically significant drug interactions were observed with simultaneous use of Uperio with simvastatin.
Sildenafil
In patients with a marked increase in blood pressure receiving Uperio (until equilibrium concentrations were reached), a single dose of sildenafil enhanced the antihypertensive effect compared with the use of Uperio in monotherapy. For this reason, sildenafil or another phosphodiesterase type 5 inhibitor should be used with caution in patients receiving Uperio.
Suspected drug interactions to consider
Potassium
Concomitant use of potassium-sparing diuretics (for example, triamterene and amiloride), mineralocorticoid antagonists (for example, spironolactone and eplerenone), potassium supplements or potassium-containing salt substitutes may cause an increase in potassium and creatinine concentrations in the blood serum. In patients receiving Uperio concomitantly with these drugs, it is recommended to regularly monitor serum potassium levels.
Nonsteroidal anti-inflammatory drugs (NSAIDs), including selective ones
cyclooxygenase-2 inhibitors (COX-2 inhibitors)
The use of Uperio concomitantly with NSAIDs in patients over the age of 65 years, in patients with hypovolemia (including patients receiving diuretics) and in patients with impaired renal function may increase the risk of deterioration of renal function. In patients receiving Uperio concomitantly with NSAIDs, it is recommended to monitor renal function when using a similar treatment regimen and if it changes.
Lithium preparations
The possibility of drug interactions between Uperio and lithium preparations has not been studied. With the simultaneous use of lithium preparations with ACE inhibitors and ARB II, a reversible increase in the content of lithium in the blood serum and, in connection with this, increased toxic manifestations were noted. In patients receiving Uperio together with lithium preparations, it is recommended to carefully monitor the lithium content in the blood serum. If a diuretic drug is used additionally, the risk of lithium toxicity may increase.
Transport proteins
The active metabolite of sacubitril (sacubitrilate) and valsartan are substrates of the transporter proteins OATP1B1, OATP1B3 and OAT3; valsartan is also a substrate of the MRP2 transporter protein. In patients receiving Uperio concomitantly with inhibitors of OATP1B1, OATP1B3, OAT3 (eg, rifampicin and cyclosporine), or MPR2 (eg, ritonavir), the systemic exposure of sacubitrilate or valsartan, respectively, may be increased. Caution must be exercised at the beginning and at the end of the simultaneous use of Uperio and this group of drugs.
No significant drug interactions
When Uperio was used in combination with furosemide, digoxin, warfarin, hydrochlorothiazide, amlodipine, metformin, omeprazole, carvedilol, intravenous (IV) nitroglycerin or a combination drug of levonorgestrel and ethinyl estradiol, no clinically significant interactions were identified. Interactions with atenolol, indomethacin, glibenclamide (glyburide) or cimetidine are not expected when used simultaneously with Uperio.
Interactions with isoenzymes of the cytochrome P450 system
Available studies demonstrate that the likelihood of drug interactions mediated by cytochrome CYP450 isoenzymes is low, since the complex of active substances is metabolized to a small extent with the participation of CYP450 isoenzymes. The complex of active ingredients of the drug Uperio is not an inhibitor or inducer of CYP450 isoenzymes
Captopril Velpharm, 50 mg, tablets, 20 pcs.
Before starting, as well as regularly during treatment with Captopril Velpharm, blood pressure and kidney function should be regularly monitored. In patients with chronic heart failure, the drug is used under close medical supervision.
Arterial hypotension
In patients with arterial hypertension, when using the drug Captopril Velpharm, severe arterial hypotension is observed only in rare cases; the likelihood of developing this condition increases with a decrease in circulating blood volume and an imbalance in water and electrolyte balance (for example, after intensive treatment with diuretics), in patients with chronic heart failure or on hemodialysis. The possibility of a sharp decrease in blood pressure can be minimized by prior withdrawal (4-7 days) of the diuretic or replenishment of circulating blood volume (about a week before the start of treatment), or by using the drug Captopril Velpharm in small doses at the beginning of treatment (6.25 -12.5 mg/day).
A marked decrease in blood pressure when using antihypertensive drugs in patients with cerebrovascular accidents and cardiovascular diseases may increase the risk of myocardial infarction or stroke. If arterial hypotension develops, the patient should take a horizontal position with legs elevated. Sometimes it may be necessary to replenish the volume of circulating blood.
Renovascular hypertension
There is an increased risk of developing hypertension and renal failure in patients with bilateral renal artery stenosis of a solitary kidney when using ACE inhibitors. Impaired renal function can occur with moderate changes in serum creatinine concentrations. In such patients, therapy should be initiated under close medical supervision with low doses, carefully titrated and with monitoring of renal function.
The simultaneous use of ACE inhibitors (including the drug Captopril Velpharm) with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal failure (GFR less than 60 ml/min/1.73 m2 body surface area) and not recommended in other patients.
Concomitant use of ACE inhibitors with angiotensin II receptor antagonists is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.
Renal dysfunction
In patients with renal failure or when taking high doses of ACE inhibitors (including Captopril Wellpharm), proteinuria may occur. In most cases, proteinuria decreased or disappeared within 6 weeks, regardless of whether treatment with Captopril Velpharm was continued or not. Parameters of renal function, such as residual blood nitrogen and creatinine, rarely changed in patients with proteinuria. In patients with kidney disease, the protein content in the urine should be determined before starting therapy and periodically throughout the course of therapy.
Hyperkalemia
In some cases, when using the drug Captopril Velpharm, an increase in potassium levels in the blood serum is observed. The risk of developing hyperkalemia when using ACE inhibitors is increased in patients with renal failure and diabetes mellitus, as well as those taking potassium-sparing diuretics, potassium supplements and other drugs that cause an increase in potassium levels in the blood (for example, heparin). The simultaneous use of potassium-sparing diuretics and potassium supplements should be avoided. Use with caution in patients on a low-salt or salt-free diet (increased risk of hypotension and hyperkalemia).
Neutropenia/agranulocytosis
In the first 3 months of therapy, the number of leukocytes in the blood is monitored monthly, then once every 3 months. Neutropenia/agranulocytosis, anemia and thrombocytopenia have been reported in patients taking ACE inhibitors, including Captopril Velpharm. In patients with normal renal function and no other complicating factors, neutropenia rarely occurs. Captopril should be used with great caution in patients with connective tissue diseases who are simultaneously receiving immunosuppressive therapy (allopurinol or procainamide), especially with existing renal impairment. In such patients, a clinical blood test is monitored every 2 weeks in the first 3 months, then every 2 months. If the number of leukocytes is below 4.0 × 109 / L, a general blood test is indicated; below 1.0 × 109 / L, the drug is stopped. These patients may develop severe infections that do not respond to intensive antibiotic therapy. During treatment, all patients should be instructed that if signs of infection occur (eg, sore throat, fever), they should notify the physician and have a complete blood count performed. In most patients, the white blood cell count quickly returns to normal when treatment with Captopril is stopped.
Anaphylactoid reactions
Patients taking Captopril Velpharm against the background of desensitizing therapy with hymenoptera venom, etc., have an increased risk of developing anaphylactoid reactions. This can be avoided if you first temporarily stop taking the drug.
When performing hemodialysis in patients receiving Captopril Velpharm, the use of high permeability dialysis membranes (for example, AN69®) should be avoided, since in such cases the risk of developing anaphylactoid reactions increases.
In rare cases, life-threatening anaphylactoid reactions may occur in patients receiving ACE inhibitors during low-density lipoprotein (LDL) apheresis using dextran sulfate. To prevent anaphylactoid reactions, ACE inhibitor therapy should be discontinued before each LDL apheresis procedure using high-flux membranes.
Angioedema
In patients taking Captopril Velpharm, the appearance of abdominal pain must be differentiated from intestinal angioedema.
If angioedema develops, the drug is discontinued and careful medical observation and symptomatic therapy are provided. If the swelling is localized on the face, special treatment is usually not required (antihistamines can be used to reduce the severity of symptoms); in the event that the swelling spreads to the tongue, pharynx or larynx and there is a threat of developing airway obstruction and a threat to the patient’s life, epinephrine (adrenaline) should be immediately administered subcutaneously (0.5 ml in a dilution of 1:1000), and also make sure that airway patency.
It is recommended to stop taking ACE inhibitors, including Captopril Velpharm, 12 hours before surgery, warning the surgeon-anesthesiologist about the use of ACE inhibitors.
Cough
The development of a non-productive, prolonged cough when taking ACE inhibitors is reversible and resolves after discontinuation of treatment.
Diabetes
In patients with diabetes mellitus taking oral hypoglycemic agents or insulin, blood glucose concentrations should be regularly monitored during the first month of treatment with Captopril Velpharm.
Liver dysfunction
During therapy with ACE inhibitors, several cases of liver dysfunction with cholestatic jaundice, fulminant liver necrosis, sometimes fatal, have been reported.
If, during therapy with Captopril Velpharm, jaundice develops or the activity of “liver” transaminases increases, the drug should be discontinued immediately; the patient should be closely monitored and, if necessary, receive appropriate therapy.
Hypokalemia
The simultaneous use of an ACE inhibitor and a thiazide diuretic does not exclude the possibility of hypokalemia. It is recommended to regularly monitor potassium levels in the blood.
Surgery/anesthesia
Hypotension may occur in patients undergoing major surgery or during the use of anesthetics known to lower blood pressure. If arterial hypotension occurs, it is recommended to replenish the volume of circulating blood.
Ethnic differences
ACE inhibitors, including Captopril Welfarm, have a less pronounced antihypertensive effect in patients of the Black race, which is apparently due to the frequent occurrence of low renin activity in this group of patients.
Laboratory data
Captopril may cause a false-positive urine acetone test.
