What Is Amiloride?

Amiloride, also known as amlomipride, is a light yellow to yellow-green powder chemical. Chemical name N -fluorenyl-3.5-diamino-6-chloropyrazine-2-amide, molecular formula is C ₁₂ H ₁₈ ClN ₇ O, molecular weight is 311.777100, slightly soluble in water and absolute ethanol, insoluble in acetone and chloroform , Ether and ethyl acetate, easily soluble in dimethyl sulfoxide, slightly soluble in methanol, protected from light. Amiloride is a cardiovascular drug. It is mainly used to treat edema disease clinically, and it can also be used as an adjuvant treatment for refractory hypokalemia.

Chinese name: Amiloli
Foreign name: Amiloride

CAS number: 1428-95-1
Molecular formula: C12H18ClN7O
Molecular weight: 311.77100

Amiroli Basic Information

Chinese name

English name: 5- ( N, N -hexamethylene) amiloride

English alias: HMA; 3-amino-5-azepan-1-yl-6-chloro-pyrazine-2-carboxylic acid carbamimidoylamide; HMA-5; 3-amino-5- (azepan-1-yl) -6-chloro -N- (diaminomethylidene) pyrazine-2-carboxamide; Hexamethyleneamiloride;

CAS number: 1428-95-1

Molecular formula: C ₁₂ H ₁₈ ClN ₇ O

Chemical structure:

Molecular weight: 311.77100

Exact mass: 311.12600

PSA: 136.51000

LogP: 2.55300

Amilolide physical and chemical properties

Density: 1.63g / cm ³

Boiling point: 638.2ºC at 760mmHg

Flash point: 339.8ºC

Refractive index: 1.742

Storage conditions: 2-8ºC

Vapor pressure: 3.47E-16mmHg at 25 ° C ^[1]

Amiroli computing chemical data

1. Hydrophobic parameter calculation reference value (XlogP): 1.3

2.Number of hydrogen-bonded donors: 3

3.Number of hydrogen bond acceptors: 5

4.Number of rotatable chemical bonds: 2

5.Number of tautomers: 11

6.Topological molecular polar surface area: 137

7.Number of heavy atoms: 21

8.Surface charge: 0

9.Complexity: 393

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 0

12. Uncertain number of atomic stereocenters: 0

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15. Number of covalent bond units: 1 ^[2]

Information about Amilolide

Amiroli classification

Primary classification: Urinary system drugs Secondary classification: Diuretics Tertiary classification: Low-effect diuretics ^[3]

Amiloride pharmaceutical dosage form

Tablet: 5mg.

Pharmacological effects of amiloride

This product is a pyrazine derivative, and its effect is similar to that of ampicillin. The role is to interfere with epithelial sodium channels in the distal tubules and collecting ducts, and inhibit Na + -H + and Na + -K + exchange in the proximal tubules, thereby reducing potassium secretion. This product has no antagonistic effect on aldosterone. This product is a potent potassium-sparing diuretic. It does not depend on aldosterone to retain potassium and excrete sodium. It acts on the distal end of renal tubules, blocks the sodium-potassium exchange mechanism, promotes the excretion of sodium and chlorine, and reduces the secretion of potassium and hydrogen ions. Natriuretic and antihypertensive activities are weak, but they have a synergistic effect when combined with thiazide or myelin diuretics ^[4] .

Amiloride Pharmacokinetics

It is easy to be absorbed orally, and the absorption rate is 30% to 90%. When administered with food, bioavailability decreases. It started to work 3 hours after oral administration, peaked at 6-10 hours, and the effect lasted 24 hours. Its plasma half-life is 6-9 hours, and it is significantly prolonged in renal insufficiency. This product is not metabolized by the liver, 50% is excreted from the urine in its original form, and about 40% is excreted with feces. A small amount is excreted through the bile ^[4] .

Amiroli

Chronic congestive heart failure, cirrhosis with ascites, hypokalemia caused by primary aldosterone. Combined with other potassium-releasing diuretics can prevent hypokalemia ^[4] .

Amiloli disabled caution

(1) Animal experiments show that the drug has no adverse effects on fetuses, no teratogenic and tumorigenic effects. However, pregnant women should take medication under the guidance of a physician.

(2) No experiment has confirmed whether this drug can be secreted by milk.

(3) The elderly are more prone to hyperkalemia and renal damage when using this medicine, and should be closely observed during the medication.

(4) Disabled during hyperkalemia.

(6) Use with caution: no urine; renal impairment; diabetes; acidosis and hyponatremia.

Use with caution for pregnant women and married women of childbearing age. Severe liver and kidney dysfunction, those with a tendency to hyperkalemia are contraindicated.

This product has a significant effect on endocrine and water and salt metabolism, and may cause hyperkalemia in people with diabetes ^[4] .

Amiloli notes

1. Use with caution in diabetic patients and pregnant women. 2. When using this product alone, pay attention to monitoring potassium ^[4] .

Amiloride adverse reactions

Hyperkalemia is more common when used alone. This medicine can cause hyponatremia, hypercalcemia, mild metabolic acidosis, gastrointestinal reactions such as nausea, vomiting, abdominal pain, diarrhea or constipation, headache, dizziness, decreased sexual function, and allergic reactions. The rash even has trouble breathing.

Elevated blood potassium, kidney stones can occur in a small number of patients. Can cause gastrointestinal reactions: nausea, vomiting, loss of appetite, bloating, diarrhea. Giant cell anemia, lethargy, dry mouth, rash. Most appeared pale blue fluorescent urine.

Occasionally dry mouth, nausea, bloating, dizziness, chest tightness, etc. Long-term medication should regularly check blood potassium, sodium and chlorine levels ^[4] .

Amilo use

1. Adults usually take it orally. Start with 5-10mg once a day, and then adjust the dose as appropriate. The maximum daily dose is 20 mg.

2. Pediatric doses have not been determined.

[Preparation and specifications] Amirololi tablets 5mg

Oral, 10-20mg a day, divided into 2-3 times.

[Usage and Dosage] Orally, 1-2 tablets each time, once a day, if necessary, twice a day. In addition to being used for hypokalemia or preventing the occurrence of hypokalemia, it is generally used in combination with other diuretics or antihypertensive drugs for better efficacy.

[Formulation and specifications] Tablet: 2.5mg / tablet.

[Trade name] Wuduli tablet, containing 2.5mg of amiloride and 25mg of hydrochlorothiazide ^[4] .

Amiroli interaction

See Spironolactone.

Concomitant use with thiazines can cause severe hyponatremia.

Can counteract the positive inotropic effects of digoxin, but the clinical significance of these effects is unknown.

Indomethacin alone can cause severe hyperkalemia (> 6.0mmol / L) in about 12% of patients. It is best not to use it in combination with diuretics. Angiotensin-converting enzyme inhibitors combined with potassium-preserving diuretics can cause severe hyperkalemia and even cardiac block on both sides ^[4] .

Amiloli notes

(1) The administration should be individualized and used from the minimum effective dose to reduce side effects such as electrolyte disturbance.

(2) Interference with diagnosis: It can increase the following measured values: blood glucose (especially in patients with diabetes), blood creatinine, uric acid and urea nitrogen (especially in the elderly and those with pre-existing renal impairment) Plasma renin concentration. Decreased blood sodium concentration.

(3) Use with caution in the following cases: oliguria; renal impairment; diabetes; acidosis and hyponatremia.

(4) You should know the blood potassium concentration before taking the medicine, but in some cases the blood potassium concentration does not really reflect the amount of potassium in the body. For example, when potassium is transferred from the cell to the outside during acidosis, hyperkalemia is prone to occur After the poisoning is corrected, the potassium concentration can decrease.

(5) If hyperkalemia occurs during taking the medicine, the medicine should be stopped immediately and treated accordingly. Long-term application of this product should regularly check blood potassium, sodium and chlorine levels.

(6) Medication should be taken during or after meals to reduce gastrointestinal reactions.

(7) If administered once a day, it should be administered in the morning to avoid an increase in urine output at night ^[4] .

[Medication for pregnant and lactating women]

(1) It is unclear whether this medicine has adverse effects on pregnant women. If hypokalemia occurs, it should be administered under the guidance of a physician.

(2) No experiment has confirmed whether this drug can be secreted by milk.

[Children's medication] is not clear.

[Medication for elderly patients] Hyperkalemia and renal damage are more likely to occur in the elderly when using this drug, and should be closely observed during the medication ^[4] .

medicine interactions

(1) Adrenal corticosteroids, especially those with a strong mineralocorticoid effect, can reduce the diuretic effect of this drug, and antagonize the potassium-killer effect of this drug.

(2) Estrogen can cause water and sodium retention, thereby weakening the diuretic effect of this medicine.

(3) Non-steroidal anti-inflammatory analgesics, especially indomethacin, can reduce the diuretic effect of this drug and increase renal toxicity when combined.

(4) Sympathomimetic drugs reduce the hypotensive effect of this drug.

(5) Dopamine strengthens the diuretic effect of this drug.

(6) Combined with drugs that cause blood pressure drop, the diuretic and antihypertensive effects are enhanced.

(7) It should not be combined with potassium diuretics or potassium salts. When combined with the following drugs, the chance of developing hyperkalemia is increased, such as potassium-containing drugs, stock blood (20mmol / L potassium, such as potassium up to 65mmol / L for more than 10 days), angiotensin converting enzyme inhibitors, Angiotensin II receptor antagonist and cyclosporine A, etc. ^[4] .

(8) Combined with glucose insulin solution, alkaline agent, sodium type potassium reduction exchange resin, the chance of developing hyperkalemia is reduced.

(9) This medicine extends the half-life of digoxin.

(10) Combination with ammonium chloride is prone to metabolic acidosis.

(11) In combination with nephrotoxic drugs, nephrotoxicity increases.

(12) Sodium glycyrrhizinate and licorice preparations have aldosterone-like effects, which can reduce the diuretic effect of this drug ^[3] .

Amiloride Drug Evaluation

Long-term use of this drug often causes hyperkalemia, so it is combined with furosemide in the treatment of heart failure. The drug is currently the best drug in the role of sodium and potassium diuretics. When used alone, the blood potassium should be monitored, and the drug should be discontinued when the blood potassium is increased. This product is used in combination with thiazide or tincture diuretics. Serum potassium and creatinine levels should be monitored. Because this medicine can reduce H + excretion. Patients with moderate to severe diabetes can have impaired glucose tolerance and increased potassium during treatment. This product can also cause azotemia and hyperuricemia. ^[3-4]