Diuretics by strength. What are diuretics and what applies to them? Diuretics for renal failure

Diuretics are used to remove excess water from the body, cleanse it and normalize the acid-base balance. They are also called diuretics. Both synthetic and plant-based preparations are produced. Prescribed for hypertension, heart, kidney and liver diseases, which are accompanied by edema.

Diuretics - what are they?

Diuretics are medications designed to remove fluids from the body through urine. Their effect is that they can slow down the absorption of salts and water in the renal tubules, increase the formation and rate of urine output. This helps reduce fluid content in tissues and relieve swelling.
Diuretics have the following effects:

After a hypertensive patient takes a diuretic, sodium salts are retained in the body, excess water is removed, after some time the pressure becomes normal and remains for a long time.
Thanks to the use of diuretics, it is possible to normalize fundus pressure, as well as intracranial pressure.
They can inhibit the action of neurons, thereby preventing epilepsy attacks.
Some drugs act as protectors and become a kind of protection for the kidneys and. Others can relax the muscles of the muscles, thereby relieving spasms in them.
They reduce calcium levels in the blood, but retain magnesium. This improves microcirculation in the kidneys and relieves the load on the left ventricle of the heart, protecting the organs from complications.
Can alleviate the condition of a patient poisoned by toxic substances.

Classifications of diuretics

All diuretics are classified. They are divided depending on their origin. They can be:

Chemical . Available in the form of tablets and powders, solutions for intravenous administration.
Natural origin . Herbs, herbal teas, and food products are used for diuretic purposes.

Depending on the purpose, all diuretics have another classification according to their mechanism of action:

Potent drugs , necessary for providing emergency assistance, lowering blood pressure. They are mainly used once.
Medium strength , which have a long-term effect, are part of therapy in the treatment of internal organs - kidneys, heart. They are used in courses.
Weak drugs , controlling fluid accumulation, but preserving potassium in the body.

Thiazide diuretics

Thiazide drugs are one of the most common types. They are most often prescribed by attending physicians. The therapeutic effect begins to be observed after a few hours, as they are quickly absorbed in the intestine and are well tolerated by patients.

Thiazide diuretics may affect the distal tubules of the kidneys, resulting in the following:

Reabsorption (reabsorption) of chlorine and sodium is suppressed.
The excretion of potassium and magnesium increases.
The secretion of uric acid and the excretion of calcium ions and urine are reduced.

Prescribed for:

congestive heart failure;
essential hypertension;
kidney and liver diseases;
glaucoma and so on.

These drugs include:

Indapamide;
Indap;
Metolazone;
Klopamide;
Chlorthalidone.

To reduce dose-related side effects, thiazide diuretics are prescribed together with loop diuretics.

Potassium-sparing diuretics

Drugs that promote potassium retention in the body are called potassium-sparing diuretics. They are often used in combination with other drugs to enhance the effects of medications and conserve potassium. They lower systolic blood pressure.

They are prescribed for the following symptoms:

heart failure;
potassium-sparing diuretic therapy;
the appearance of edema (see also -).

These diuretics are:

Veroshpiron;
Spironolactone;
Aldactone.

These diuretics must be taken with caution as side effects may occur due to hormonal effects. Men may experience breast pain, women may experience breast pain, the menstrual cycle may be disrupted, or, even worse, bleeding may occur.

To avoid such hormone-related side effects, you can take Amiloride and Triampur. They affect everyone equally. At the level of the distal tubules, potassium is inhibited and magnesium is removed from the body. Therefore, these drugs produce a potassium-sparing effect. But they also have side effects– hyperkalemia occurs when taking them. Potassium passes from the cells into the blood. Its increase in large quantities can cause cardiac arrest or lead to muscle paralysis.

It is especially dangerous to prescribe these drugs to patients diagnosed with diabetes mellitus and renal failure. These medications should not be taken without the supervision of a physician and the dose should not be increased independently.

What are loop diuretics?

The most powerful diuretics are loop diuretics. The renal tubule, which is loop-shaped and directed towards the center of the kidney, is called the loop of Hengle. It performs the function of reabsorption of liquids and substances dissolved in it. Diuretics that act on this loop are called loop diuretics.

These diuretics do the following:

reduce the activity of reabsorption of potassium, sodium, chlorine, magnesium;
relax the muscles of blood vessels;
enhance glomerular filtration;
increase blood flow in the kidneys;
affect hemodynamic readings, especially if drugs are administered intravenously;
may gradually reduce the volume of extracellular fluid.

The effect of loop diuretics occurs quickly - after 30-40 minutes and lasts up to 6 hours. These drugs are prescribed very rarely, mainly in critical cases, as they have serious side effects:

cerebral edema;
hyperkalemia;
pulmonary edema;
heart and kidney failure;
hypertensive crisis;
cirrhosis of the liver.

Loop diuretics include the following medications:

Ethacrynic acid;
Furosemide;
Piretanide;
Bumetanide.

Osmotic diuretics

The effect of osmotic diuretics is based on reducing pressure in the blood plasma, which relieves swelling and removes excess water. In the renal glomeruli, the blood supply becomes greater, and there is an increase in filtration in the kidneys.

The following drugs are classified as osmotic drugs:

Sorbitol;
Urea;
Mannitol.

The most common is Mannitol. It has the longest therapeutic effect. Others are the weakest, and their effect does not last long. The drugs are prescribed intravenously for cerebral or pulmonary edema, drug poisoning, glaucoma, burns, and sepsis.

But their reception leads to the emergence side effects, these include:

the occurrence of pain in the head;
tissue necrosis if the drug gets under the skin;
increase in blood nitrogen;
nausea.

Herbal diuretics

Along with medications, diuretics of plant origin are widely used. They have a gentler effect on the body and do not have dangerous side effects.

Diuretics are used in the complex therapy of many ailments. A diuretic, what it is and how to take it, you need to find out from your doctor.

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Principles of classification

Diuretic medications are a group of drugs that have pronounced diuretic effects. The diuretic effect is the ability of substances to cause accelerated filtration of blood in the nephron channels, removing excess fluid from the body. This effect of drugs is achieved through different mechanisms of action, which forms the basis for the classification of diuretics.

Main groups of diuretic medications:

1. Loop diuretics (Furosemide, Ethacrynic acid).
2. Thiazide diuretics (benzothiazine derivatives - Thiazides).
3. Potassium-sparing medications.
4. Osmotic drugs.

But not all representatives of classical diuretic drugs are used in nephrology. Some drugs are prohibited due to their nephrotoxicity (mercury diuretics) and ineffectiveness (Theophylline, ammonium chloride).

Thiazide medications

Representatives of this group include diuretics: Hypothiazide, Dichlorothiazide, Hydrochlorothiazide, Cyclomethiazide. The mechanism of action is based on the suspension of sodium reabsorption in the cortical and distal parts of the nephron loop. The effect of the drug begins within an hour after their use, the duration of the effect is 12 hours or more, so each thiazide drug in this group is best taken once a day in the morning.

Thiazide diuretics include:

Brinaldix;
Chlorthalidone is a long-acting drug;
Renez.

Sodium excretion while taking these drugs is moderate (up to 10% of filtered sodium is released). The drugs are widely distributed due to the following characteristics:

ease of use;
hypotensive effect;
effectiveness in the treatment of nephrogenic diabetes insipidus, idiopathic hypercalciuria.

Undesirable effects from taking thiazides:

increased release of potassium with the development of hypokalemia and magnesium, possible development of metabolic alkalosis;
decreased excretion of calcium in the urine, increased its concentration in the blood plasma;
increase the risk of developing hyperuricemia due to decreased secretion of uric acid;
worsen the course of diabetes mellitus because they disrupt carbohydrate metabolism, causing hyperglycemia;
increase renal failure;
contribute to the development of toxic pancreatitis;
allergic manifestations with episodes of photosensitivity, necrotizing angiitis.

Loop drugs

A prominent representative of this group is Furosemide. It has a depressing effect on the active reabsorption of chlorine ions. The place of its action is the ascending part of the nephron, and when using large doses, the proximal tubules.

The drug has a quick, pronounced, but short-term effect. Its effect begins less than an hour after consumption. The maximum effect occurs after 20 minutes, the duration of action is about 4 hours.

When administered parenterally, the effect of the drug begins immediately and lasts up to 1 hour. Unlike thiazides and thiazide-like medications, Furosemide improves glomerular filtration, so it is considered the drug of choice in case of renal failure.

It is well tolerated by patients, but is not recommended for long-term use. There is a risk of developing the following pathologies:

hyperuricemia;
acute gout;
deafness (especially with simultaneous use of antibiotics);
thrombocytopenia;
disorders of the kidneys (with simultaneous use of antibiotics from the cephalosporin group);
hyponatremia.

The drug has a slight effect on carbohydrate metabolism. Uregit (or ethacrynic acid) is a lesser-known representative of the group of loop diuretics. It has a different chemical structure, but its mechanism of action is similar to Furosemide. Peak diuresis occurs two hours after taking the drug, the effect lasts up to 9 hours. It is better to take the drug after meals in the morning. Negative manifestations of Uregitis include:

hyperuricemia;
deafness (develops with simultaneous use of antibiotics).

Potassium-sparing group of diuretics

Representatives of this group include the following drugs: Spironolactone, Aldactone, Veroshpiron. All of them are artificial synthetic steroid hormones, competitive antagonists of aldosterone. They act at the level of the distal tubules, collecting ducts, and proximal tubules of the nephron. Spironolactone is able to directly inhibit the formation and release of aldosterone in the adrenal glands.

The diuretic effect of such drugs is very weak (they are able to release only 2% of the total sodium that is filtered in the kidneys). Such medical supplies often used in complex treatment various ailments. These drugs have the ability to potentiate the effect of other drugs on the proximal tubules, reducing the reabsorption of sodium that has passed through the proximal parts of the nephrons.

While maintaining the usual salt diet, isolated use of potassium-sparing medications will not work. For the effect of taking such drugs to occur, it is necessary to limit sodium intake. The diuretic effect of taking these drugs occurs gradually, starting from 2-3 days. The drugs are unique in that they increase the reabsorption of potassium back into the blood, which is why doctors often prescribe Spironolactone along with proximal diuretics (thiazides and thiazide-like drugs). This scheme leads to potentiation of the effect, prevents the development of hypokalemia, preserving potassium in the body.

Effective drugs

The daily dose of Veroshpiron ranges from 25 to 300 ml. While taking Spironolactone, the following undesirable reactions may develop:

increased potassium in the blood;
fast fatiguability;
constant drowsiness;
hirsutism;
gynecomastia;
interruptions in the menstrual cycle.

The drug should not be taken by patients with renal failure. late stages(especially in the presence of diabetic nephropathy). Potassium-sparing drugs also include Triamterene. It acts in the area of the distal tubules and affects only sodium transport. Triamterene is not involved in aldosterone metabolism in the kidneys. The drug has weak diuretic activity, which lasts up to 10 hours after administration.

The dose of the drug Triamterene can be from 50 to 300 ml per day. It is prescribed in two doses, combined with stronger diuretics. Adverse reactions of the drug include episodes of increased glucose and uric acid in the blood. Experts consider Amiloride to be similar in chemical structure and action to Triamterene. Its daily dosage is 5-20 mg.

Osmotic substances

Representatives of this group are not metabolizable at all and are not absorbed in the kidneys. They are only filtered in the nephron structures, increasing the osmolarity of urine in the nephron. This explains the decrease in reabsorption in nephron structures.

Mannitol is often used in nephrological practice. It is used to prevent the development of acute kidney failure or at the earliest stages of its development. Mannitol is used for forced diuresis if acute tubular necrosis is suspected. The drug is used only for parenteral administration, a 10-20% solution is administered slowly intravenously.

To combat minor edema and prevent their development, you can use decoctions of medicinal herbs that have diuretic properties. Herbal decoctions are often used:

bearberry;
juniper;
parsley;
lingonberries.

Pharmacokinetic differences

Each group of these drugs has different mechanisms of action.

If one drug is ineffective, another is used or a combination of them is used.

Approximate treatment regimens with diuretics:

1. Saluretics with proximal action and distal potassium-sparing medications. It is best to combine Veroshpiron, Triamterene with thiazides. The modern pharmaceutical market offers ready-made combination medications (Triamterene and Hypothiazide or Triamterene and Furosemide).
2. A combination of drugs with a similar effect against the background of the peak activity of thiazides is administered Furosemide, Ethacrynic acid is enhanced by the introduction of thiazides, Eufillin when administered intravenously significantly enhances the effect of Natriuretics (Furosemide, Ethacrynic acid).

Dangerous combinations of diuretic medications:

1. Ethacrynic acid, Furosemide is dangerous to combine with Kanamycin, Gentamicin, Streptomycin due to the risk of developing deafness.
2. Ethacrynic acid, Furosemide is dangerous to combine with Cephaloridine due to increased nephrotoxicity.
3. The combination of diuretics with acetylsalicylic acid disrupts the secretion of the latter by the kidneys.
4. Simultaneous use of diuretics with calcium can provoke the development of hypercalcemia.

Based on the works of N.E. de Wardener (1973) developed a sequence diagram for the use of diuretic medications:

1. Veroshpiron, Triamterene in the first few days to preserve potassium.
2. Then the addition of thiazides.
3. If their effectiveness is poor, thiazides are replaced with Furosemide, Ethacrynic acid. Their dosage is doubled daily until maximum diuresis occurs.
4. To enhance the effect, a certain dose of Furosemide can be used parenterally.
5. You can also add intravenous Mannitol.

To better understand the patient’s water balance, it is recommended to weigh him every day. This is more clear than measuring urine output and fluid intake for each day. After the swelling is eliminated, the use of diuretics is discontinued.

1. Most diuretic medications can cause hypokalemia and metabolic alkalosis. To prevent this condition, you should take additional potassium. Hypothiazide, Furosemide are best used in short, intermittent courses (2 times a week, every other day).
2. With the uncontrolled use of such medications, a sharp loss of chlorides, a drop in blood volume, and a decrease in reabsorption may occur. This will lead to increased secretion of renin and aldosterone.
3. Persistent swelling can be eliminated by using laxative medications (Sorbitol, Magnesium Sulfate) by puncturing the skin with sterile needles, by ultrafiltration of blood (with an assessment of the risk of a sharp decrease in CF).
4. Severe hyperaldosteronism is treated with the simultaneous use of potassium and Veroshpiron.
5. With long-term persistent swelling, there is a risk of developing hyponatremia, vascular insufficiency in the periphery, hyperaldosteronism, a drop in potassium concentration in the blood, alkalosis, a decrease in CP, and an increase in uric acid.
6. Against the background of a sharp drop in CF, the drug of choice is Furosemide (it acts on CF, enhancing it). Veroshpiron, Triamterene are dangerous to use due to the risk of hyperkalemia.
7. When treating chronic renal failure with diuretics, it is important to remember the risk of even greater kidney failure. In such patients, it is necessary to constantly monitor the levels of potassium, chlorine, calcium, uric acid and glucose in the blood.
8. With long-term use of significant doses of Furosemide, Ethacrynic acid, there is a risk of hearing loss (often transient).

Diuretics or diuretics are a special type of substances that increase the amount of urine excreted per unit of time. All diuretics are a heterogeneous group of compounds that either stimulate or inhibit (slow down) the action of various hormones. These hormones are naturally produced in the body to regulate urine production by the kidneys. Read about this and much more in this article.

A diuretic is any substance that stimulates urine production. For example, they include hypotonic aqueous solutions, including clean water, black and green tea, as well as decoctions and even tinctures. Yes, clean water is also a diuretic. Almost all herbs include a wide range of compounds, some of which are sure to have a diuretic effect.

Diuretics are divided into 5 main classes substances: thiazide, loop, osmotic, potassium-sparing diuretics and carbonic anhydrase inhibitors. Next, let's look in a little more detail at all of them.

Thiazide diuretics

They are a special class of diuretics that are most often used to treat hypertension and edema (caused, for example, by heart, liver or kidney failure). This group of diuretics is homogeneous in pharmacological action, and the substances differ from each other only in the duration and strength of action.

Loop diuretics

They are the most potent of all diuretics available in clinical practice. Most often, loop diuretics are used in the treatment of edema of various origins.

Potassium-sparing diuretics

They are a special class of diuretics that do not promote the excretion of potassium in the urine from the body. Potassium-sparing diuretics are most often used as adjuvant therapy in the management of congestive heart failure and the treatment of hypertension.

Osmotic diuretics

is a special type of diuretic that inhibits the reabsorption of water and sodium (Na) in the body. Osmotic diuretics, from a pharmacological point of view, are inert substances that are administered intravenously. They increase blood osmolarity and enhance renal filtration.

Carbonic anhydrase inhibitors

This is one of the types of diuretics that, paradoxically, are not used independently as diuretics (diuretics). Carbonic anhydrase inhibitors are mainly used for glaucoma.

Mechanism of action of diuretics

Diuretics exert their effect inside the nephron (inside the nerve cell) and affect the systems responsible for urine production. At the moment, 4 main targets of action of diuretics are known:

Target No. 1: transport proteins

Thiazide diuretics, loop diuretics, triamterene, amiloride affect specific transport proteins of the membrane of the epithelium of the renal tubules.

Loop diuretics, for example, act on the Na-K-2Cl symporter (transporter) in the luminal (ascending) part of the tubular epithelium of the ascending part of the loop of Henle. The strong diuretic effect is explained by the fact that it is in the ascending part of the loop of Henle that the bulk of sodium, and therefore water, is reabsorbed.

A symporter is a channel protein in cell membranes that transports substances across the membrane.

Target #2: Aldosterone receptors

Diuretics such as spironolactone block aldosterone receptors. This prevents this hormone from functioning fully.

Aldosterone is a hormone of the adrenal cortex, the physiological effect of which is to increase the volume of circulating blood and increase pressure in the circulatory system.

Target #3: water

The kidneys normally produce about 150 liters of primary urine and 1.5 - 2 liters of secondary urine. Why such difference? The fact is that the kidneys return many nutrients, including water, to the body from primary urine. This process is called reabsorption - reverse absorption. Due to this, the body does not lose a lot of fluid and nutrients. What if there is already enough liquid? Alternatively, slow down the reabsorption of water in the kidney tubules, and much more of it will be released. This mechanism of action is inherent in osmotic diuretics.

Target No. 4: carbonic anhydrase enzyme

There is a subclass of diuretics that inhibits the enzyme carbonic anhydrase, appropriately called carbonic anhydrase inhibitors.

Carbonic anhydrase in the epithelium of the proximal tubules of the nephron catalyzes the dehydration of carbonic acid, which is a key link in the reabsorption of bicarbonates. When carbonic anhydrase inhibitors act, sodium bicarbonate is not reabsorbed, but is excreted in the urine (urine becomes alkaline). Following sodium, potassium and water are excreted from the body in the urine. The diuretic effect of substances in this group is weak, since almost all of the sodium released into the urine in the proximal tubules is retained in the distal parts of the nephron. Therefore, carbonic anhydrase inhibitors are not currently used independently as diuretics.

Application in medicine

In medicine, diuretics are used to treat heart failure, arterial hypertension, influenza, liver cirrhosis, kidney disease, and hyperhydration. Some diuretics, such as acetazolamide, can slightly alkalinize the urine and are useful for increasing the excretion of various types of chemicals from the body, such as (aspirin) in cases of overdose or poisoning.

Diuretics for weight loss

Diuretics are often abused by people with an eating disorder, especially people with bulimia, in an attempt to lose weight. However, diuretics do not promote weight loss; in this case, they only promote the removal of fluid and imaginary weight loss due to a decrease in the volume of fluid in the body. Read more about this in our article: myths and reality.

Diuretics in sports

In sports, diuretics are usually used to hide the fact of drug use. Diuretics increase urine volume and dilute the concentration of doping substances and their metabolites. Also, diuretics in sports are used for rapid weight loss (by reducing the volume of fluid in the body) in order to enter competitions in a lower weight category, in sports such as boxing or wrestling.

Side effects of diuretics

Side effects of diuretics include a wide range of phenomena as related to them therapeutic effect and not related. Let's take a closer look at each of the groups.

Side effects of osmotic diuretics

Side effects of osmotic diuretics include disturbances in water-salt metabolism. They also make it difficult for the heart to work(therefore they cannot be used in heart failure, as discussed above).

Side effects of carbonic anhydrase inhibitors

Carbonic anhydrase inhibitors have the following main side effects:

hypokalemia;
hyperchloremic metabolic acidosis;
phosphaturia;
hypercalciuria with risk of kidney stones;
neurotoxicity (paresthesia and drowsiness);
allergic reactions.

Side effects of thiazide diuretics

Thiazide diuretics have the following main side effects

Hyperglycemia;
Hyperuricemia;
Hypokalemia (the mechanism of its development is described below);
Hyponatremia;
Hypomagnesemia;
Hypocalciuria;
Hyperuricemia, although rare. Women have a lower risk than men;
Gastrointestinal disorders: nausea, anorexia, diarrhea, cholecystitis, pancreatitis, abdominal pain, constipation;
Hyperlipidemia. An increase in plasma cholesterol levels by 5-15% and an increase in the levels of very low density lipoproteins (VLDL) and triglycerides (TG). In general, the risk of developing atherosclerosis is relatively low;
Violations of the central nervous system(CNS): weakness, xanthopsia, increased fatigue, paresthesia. Rarely encountered;
Impotence develops in 10% of men due to a decrease in fluid volume in the body;
Allergic reactions. Cross-allergy is observed with the sulfonamide group;
Occasionally, photosensitivity and dermatitis are observed, and extremely rarely, thrombocytopenia, hemolytic anemia and acute necrotizing pancreatitis.

Are common side effects of loop diuretics:

hypovolemia,
hypokalemia (it sharply increases the toxicity of cardiac glycosides),
hyponatremia,
hyperuricemia (can provoke a gout attack),
hypocalcemia,
hyperglycemia,
hypomagnesemia - loss of magnesium is considered possible reason occurrence of pseudogout (chondrocalcinosis),
dizziness,
fainting,
hypotension.

Rare side effects of loop diuretics:

dyslipidemia,
increase in serum creatinine concentration,
hypocalcemia,
rash.

Ototoxicity (ear damage) is a serious but rare side effect of loop diuretics. Tinnitus and dizziness may occur, but in severe cases it can also lead to deafness.

Side effects of potassium-sparing diuretics

Sodium channel blockers include amiloride and triamterene. Possible side effects include:

Cramps.
Dry mouth.
Dizziness or fainting, especially when standing up from a sitting or lying position (due to too low blood pressure).
Skin rash.
Drowsiness.
Headache.
Muscle spasms.
Diarrhea or constipation.
Amiloride in combination with thiazide diuretics can cause hyponatremia.

Aldosterone antagonists include spironolactone and eplerenone. Possible side effects include:

Sexual problems.
Breast augmentation (both men and women).
Irregular menstruation.
Confused consciousness.
Dizziness.
Skin rash.
Excessive hair growth.
Liver problems.
High potassium levels (hyperkalemia).

Comparative characteristics of diuretics

This table compares diuretics of different groups with each other, taking into account the site of action, route of administration, peak of action, release of electrolytes, strength of action, indications for use and main side effects. The table is taken from the book by V.P. Vdovichenko.
If the table is not completely visible, just scroll it to the side.

Options	Thiazide and thiazide-like	Loop	Potassium-sparing	Osmotic	Carbonic anhydrase inhibitors
Scene	Distal tubules	Ascending limb of loop of Henle	Collecting ducts	Distal tubules descending limb of the loop of Henle	Proximal tubules
Purpose	Inside	Inside, into a vein	Inside	into a vein	Inside
Peak action (in hours)	4-6 (up to 12)	1-2	2-8 or (spironolactone) 24-72	0.5	2-8
Release of electrolytes	Na(++)	Na (++++)	Na(+)	Minor	Na(++)
Force	Average	Strong	Weak	Strong	Weak
Main indications	1) Arterial hypertension 2) Edema, except severe renal 3) Hypercalciuria (reducing the risk of calcium nephrolithiasis due to a decrease in the concentration of Ca in the urine, as its reabsorption into the blood increases) 4) Osteoporosis (because Ca reabsorption in the kidneys increases) 5) Nephrogenic diabetes insipidus	Edema, especially for renal damage, edema of the brain, lungs, forced diuresis in case of poisoning, hypercalcemia.	Together with other diuretics to preserve K; spironolactone – for liver cirrhosis and CHF.	Acute poisoning, cerebral edema	Glaucoma, epilepsy, mountain sickness
Main side effects	Hypokalemia, hyperuricemia, gastrointestinal disorders, allergies	Hypokalemia, alkalosis, hypovolemia, hyperuricemia, ototoxicity	Hyperkalemia, acidosis	Dehydration	Hyperkalemia, acidosis

Note on the table: effect + – weak, ++ – moderate, +++ – strong, ++++ – very strong, 0 – absent.

If the text in the table is highlighted in bold, then this group of diuretics is the best of all diuretics for the treatment of this (highlighted) pathology.

Drugs that speed up the excretion of urine from the body are called diuretics. These drugs reduce the ability of the kidneys to reabsorb electrolytes, against the background of increasing concentrations of which fluid is released.

The first diuretic used by man was mercury. In the 19th century, this substance was used in the treatment of syphilis. It turned out to be practically powerless against this disease, but the diuretic effect of mercury did not escape the attention of doctors. Later, safer compounds appeared, the improvement of which made it possible to obtain effective and non-toxic diuretics.

Taking diuretics helps:

elimination of swelling in cardiac and vascular failure;
lowering blood pressure with hypertension;
alleviating the symptoms of kidney disease;
removal of toxins during intoxication.

Swelling is a frequent companion to diseases of the urinary and vascular systems, and the heart. Pathology develops as a result of sodium retention in the body. Diuretics help remove its excess. Thanks to this, swelling is noticeably reduced.

Hypotension (high blood pressure) against the background of increased sodium negatively affects blood vessels. They contract and narrow. Diuretics, used as blood pressure-lowering drugs, not only flush out sodium, but also dilate the walls of blood vessels. This effect of the drug leads to a decrease in blood pressure.

Removal of toxins through the use of diuretics is called “forced diuresis” in clinical medicine. This method consists in the fact that after intravenous administration of solutions to the patient, a certain dose of a highly effective diuretic drug is administered in a similar way. This leads to the fact that simultaneously with the fluid, toxic substances are washed out of the body.

There are several types of diuretic drugs, differing in their mechanism of action, used in the treatment of various pathologies.

There are three types of diuretics:

Affecting the functioning of epithelial tissue of the renal tubules. The group of these drugs includes the following: Triamterene, Hydrochlorothiazide, Bumetanide, Cyclomethiazide, Chlorthalidone, Bendroflumethiazide, Ethacrynic acid, Clopamide, Methyclothiazide, Amiloride, Metolazone, Furosemide, Indapamide, Torsemide.
Calcium sparing, related to aldosterone (mineralocorticoid) receptor antagonists. Diuretics of this type include Spironolactone, which is known under the trade name Veroshpiron.
Osmotic, for example, Mannitol (Monitol).

Diuretics are classified not only by their mechanism of action, but also by the degree of sodium leaching:

highly effective (washing out over 15%);
average efficiency (10%);
ineffective (5%).

The principle of action of diuretics

The effectiveness of diuretics for hypotension is directly related to the fact that they reduce sodium levels and dilate blood vessels. Maintaining vascular tone and reducing fluid concentration allows you to relieve arterial hypertension.

Taking diuretics relaxes myocardial cells, reduces platelet aggregation, improves microcirculation occurring in the kidneys, and reduces the load exerted on the left ventricle of the heart muscle. This mechanism of action leads to the fact that the myocardium needs much less oxygen. Osmotic diuretics, in addition to their intended purpose, increase the level of osmolar pressure nutrient medium cellular elements - interstitial fluid.

The antispasmodic effect of the drugs is based on the ability to relax the smooth muscles of the arteries, bile ducts, and bronchi.

The desire to get rid of hated kilograms pushes people to rather dubious experiments. Diuretic drugs also suffered this fate. Many people mistakenly believe that these drugs help you lose weight. This misconception is caused by the fact that ninety percent of adipose tissue consists of water.

Diuretics have an antiatherogenic effect. It lies in the ability to destroy cholesterol plaques. A drug such as Indapamide lowers the level of bad cholesterol in the blood. This in no way means that taking diuretics will help you lose fat. It stays in place, only the liquid leaves. The positive effect of the drug is that it reduces the risks of stroke, atherosclerosis, and heart failure.

Diuretics affect various systems, but mostly the urinary system. If medications are taken exclusively as directed, they normalize the balance of water and electrolytes. Uncontrolled use of diuretics, on the contrary, leads to numerous health problems, even death is possible.

It is impossible to remove fluid from the body without loss of ions. The latter regulate the work of everyone internal organ. Consequently, weight loss does not occur as a result of a decrease in body fat, but due to dehydration, which is accompanied by an ionic imbalance. Against this background, cardiac arrhythmia, hypotension develops, vision decreases, a general state of weakness is felt, and attacks of dizziness occur. With a severe overdose, hallucinations and collapse are possible.

Those wishing to use diuretics for the purpose of losing weight should remember that these drugs are included in the category prohibited for athletes. The reason for this was the death of an athlete who abused diuretics in order to get sculpted muscles. Only people far from medicine can recommend these drugs for weight loss.

Indications for the use of diuretics

Diuretics are prescribed to those suffering arterial hypertension, especially acute in old age, with an excess of sodium caused by the retention and accumulation of this substance in the body. The latter condition is observed in chronic heart and kidney failure, ascites. For those suffering from osteoporosis, it is recommended to take thiazides; for people with congenital Liddle syndrome, potassium-sparing diuretics are recommended for cardiac edema, glaucoma, intraocular pressure, cirrhosis - drugs affecting kidney function.

Diuretic thiazide-like drugs are indicated for therapy and as a prophylaxis for arterial hypotension. At moderate high blood pressure take small doses. Taking these drugs prophylactically reduces the risk of stroke. Taking large doses of these drugs unless necessary is not recommended. This may cause the development of hypokalemia. To prevent a drop in potassium levels in the blood, thiazide diuretics are combined with potassium-sparing diuretics.

Therapy with diuretics can be active or supportive. With active treatment with diuretics, patients are prescribed moderate dosages of potent drugs, for example, Furosemide, and with maintenance - regular use medicines with a diuretic effect.

Contraindications to taking diuretics

Contraindications to the use of diuretics are:

hypokalemia;
diabetes;
renal and respiratory failure;
decompensated cirrhosis.

These drugs should not be taken by patients who have an individual intolerance to sulfonamide derivatives. Thiazide group drugs, for example, Methyclothiazide, Bendroflumethiazide, Cyclomethiazide, Hydrochlorothiazide, can cause a sharp increase in blood sugar levels.

In patients suffering from ventricular arrhythmia, taking diuretics can cause a worsening of the condition and is strictly under medical supervision. Combining diuretic therapy with the use of lithium salts and cardiac glycosides requires maximum caution. Patients with heart failure are not prescribed osmotic diuretics.

Side effects and health risks

Thiazide drugs can increase uric acid in the blood. This side effect of using drugs in this group must be taken into account by patients with gout. The use of thiazides for this pathology can lead to an exacerbation of the disease and worsen the patient’s condition.

Moderately effective diuretics, for example, Hydrochlorothiazide or Hypothiazide, require strict dosage. If the dose is calculated incorrectly, the patient may feel nausea, weakness, increased drowsiness, headache, dry mouth. An overdose may be accompanied by diarrhea. Similar symptoms are observed in case of individual intolerance to the medication. Against the background of ion imbalance, muscle weakness, skeletal muscle spasms, arrhythmia, allergies develop, an increase in sugar and a decrease in male libido may occur.

Furosemide may have the following side effects: reduce magnesium, calcium, potassium, cause nausea, frequent urination, dizziness, dry the oral mucosa. Disturbances in ion exchange provoke an increase in glucose, uric acid, and calcium. High levels of these substances have a detrimental effect on hearing, manifested by paresthesia and skin rashes.

Uregit- a drug that has an increased irritant effect. Taking it may have a negative effect on hearing.

Aldosterone antagonists can cause cramps, diarrhea, vomiting, skin rashes, and gynecomastia. Incorrect purpose of these medications causes menstrual irregularities in women, and threatens impotence in men.

Osmotic With the wrong approach to the treatment of heart failure, medications can increase the load on the heart muscle by increasing plasma volumes. This side effect results in pulmonary edema.

Popular diuretics: how they affect the body

Drugs whose pharmacological action is aimed at the renal tubules remove sodium along with urine.

Thiazide-like diuretics, for example, Methyclothiazide, reduce the degree of absorption of not only sodium, but also chlorine. These drugs can often be found under the general name "saluretics", which they received from English word"salt" meaning "salt".

Moderately effective diuretics, promoting the removal of sodium, are prescribed, as a rule, for swelling and kidney disease, for patients with heart failure. Hypothiazide is most often used as an antihypertensive agent. This is due to the fact that this medication flushes out excess sodium and stabilizes high blood pressure. These drugs enhance the effect of hypertensive drugs.

To avoid effects on blood pressure, these diuretics are taken in large rather than moderate doses. The active substances present in Hypothiazide lower the level of calcium ions and prevent the accumulation of salts in the kidneys. It is often prescribed for the treatment of diabetes insipidus and urolithiasis.

Indapamide(known under the trade name as Arifon) is a drug that differs from other diuretics in its ability to dilate blood vessels and relieve spasms.

Furosemide(trade name Lasix) is the most effective diuretic, beginning to act within ten minutes after intravenous administration. It is prescribed to patients with arterial hypotension, peripheral edema, acute left ventricular failure with pulmonary edema, in order to remove toxins from the body. A diuretic such as Uregit also has similar pharmacological properties. The difference is that it lasts longer.

Competitive aldosterone antagonists, known under the trade names Aldactone or Veroshpiron, are diuretics whose action is based on reducing potassium and magnesium ions and preventing the absorption of sodium ions. Indications for the use of diuretics from this group are: hypertension, edema, congestive processes against the background of acute or chronic disorders of the heart muscle.

Osmotic diuretics have low permeability through membranes. The most common and effective drug This group of diuretics is Monitol, administered intravenously. It reduces intracranial and intraocular pressure, but increases plasma osmotic pressure. It is prescribed to patients with oliguria, which causes severe blood loss, trauma, burns, cerebral edema, glaucoma, including during the rehabilitation period after glaucoma surgery.

Diuretics of natural origin

There are many natural diuretics that are inferior in action to artificial analogues, but were used by humans long before the advent of synthetic diuretics. Lower efficiency traditional methods compensated by harmlessness and gentleness. Correctly selected dosage allows you to use decoctions for quite a long time without any side effects or harm. You should take natural diuretics, as well as synthetic drugs, only after finding out the true reason why fluid is retained in the body.

If fluid retention is caused by swelling and heart failure, drink a decoction made from birch leaves or strawberries. Birch leaves are used as compresses for swelling of the upper and lower limbs. Inflammation Bladder and kidney problems are treated with tansy, lingonberry, and shepherd's purse. Flaxseeds, bearberry, rose hips, and orthosiphon are most often used in the treatment of swelling. Rosehip tea is taken during long-term antibacterial treatment and recovery after surgery.

Orthosiphon is a traditional kidney tea that has both a diuretic and antispasmodic, anti-inflammatory effect. Natural diuretics are not only herbs, but also other vegetables. The removal of fluid is facilitated by the use of pumpkin, melons, celery, and parsley. Instead of fresh herbs, you can use cucumber and dandelion leaves to make a salad that reduces swelling.

Taking diuretics during pregnancy and lactation

Many expectant mothers, especially in the last months of pregnancy, suffer from swelling. They appear as a result of the expanding uterus compressing the vena cava. Puffiness cannot be ignored. It can signal the development of pathological conditions such as renal failure and gestosis. When compliance dietary nutrition does not bring visible results, the pregnant woman is prescribed synthetic or natural diuretics.

Most diuretics are contraindicated for use at any stage of pregnancy. You should take diuretics only as prescribed by a doctor and with extreme caution. On early stages Almost all drugs are prohibited, and in later years only a few are allowed, which are prescribed by a specialist. An incorrectly selected diuretic or dosage can change the composition of the blood, causing problems with the kidneys, hearing, vision, and even lead to a disease such as jaundice.

They can even harm a pregnant woman and the fetus folk remedies. Regular use of herbal teas disrupts the electrolyte balance and negatively affects future pregnancy. You should not take juniper, strawberries, or parsley root. The safest remedy is orthosiphon. It can be used both during pregnancy and lactation.

If it is impossible to do without taking diuretics, the attending physician prescribes Canephron tablets. This medicine can be taken at almost any stage of pregnancy. Drops of this drug are not prescribed because they contain alcohol. If swelling occurs without acute inflammatory processes in the kidneys, a herbal medicine such as Phytolysin may be prescribed.

An alternative to diuretics can be the bronchodilator Eufillin, which has a diuretic effect. It is contraindicated for women suffering from hypotension, epileptic seizures, and heart disease. When prescribing it during lactation, the specialist assesses the risk and the real need for taking this drug.

Diuretics are a traditional group of drugs widely used for the treatment of arterial hypertension (AH). They are most popular in the USA and other English-speaking countries. Impressive advances in the treatment of hypertension have been demonstrated in large randomized trials in which diuretics have been the mainstay or essential addition to long-term antihypertensive therapy. Attitudes towards diuretics are currently very ambiguous. Many experts continue to consider them, along with, first-line antihypertensive drugs. Others consider diuretics as one of the equivalent groups of antihypertensive drugs. Still others tend to consider them tools of yesterday. Along with the undoubted advantages - a pronounced hypotensive effect, ease of dosing, low cost, many diuretics also have a number of disadvantages associated with imbalance of electrolytes, lipid and carbohydrate metabolism and activation of the SAS.

There are three known groups of diuretics, differing in chemical structure and localization of action in the nephron:

thiazide;
loop;
potassium-sparing diuretics.

The pharmacological effect of thiazide and thiazide-like diuretics is realized at the level distal tubules, loop diuretics - at the level ascending part of the loop Henle, potassium-sparing - in the most remote departments distal tubules.

All diuretics, except spironolactone, “work” on the surface facing the lumen of the nephron. Since diuretics circulate in the blood in a protein-bound form, they do not pass through the glomerular filter, but reach their sites of action through active secretion by the epithelium of the corresponding parts of the nephron. The inability of the renal epithelium to secrete one or another group of diuretics in certain pathological conditions (for example, acidosis) becomes of paramount importance and predetermines their choice.

Mechanism of action

The antihypertensive effect of diuretics is determined by the natriuretic and diuretic action itself. These groups of diuretics have different indications for use. Thiazide diuretics are the drugs of choice for the treatment of uncomplicated hypertension. Loop diuretics for hypertension used only in patients with concomitant chronic renal failure (CRF) or circulatory failure. Potassium-sparing compounds have no independent significance and are used only in combination with loop or thiazide diuretics.

The mechanism of action and side effect profile of thiazide and loop diuretics are the same and will be discussed together. The antihypertensive effect of diuretics occurs at the beginning of therapy, gradually increases and reaches a maximum after 24 weeks of systematic use. In the first days of treatment, the decrease in blood pressure is due to a decrease in plasma volume and cardiac output. Then the volume of blood plasma increases slightly (without, however, reaching the initial level), and cardiac output practically normalizes. The antihypertensive effect is enhanced, which is associated with a decrease in peripheral vascular resistance. Its cause is believed to be a decrease in sodium content in the vessel wall, which reduces its reactivity in response to pressor influences. Thus, diuretics can be classified (of course, very conditionally) as vasodilators with a unique mechanism of action. An indispensable condition for this vasodilation is the stable maintenance of a slightly reduced blood plasma volume. An inevitable consequence of this decrease is the activation and increase in tone of the SAS. Activation of these neurohumoral pressor mechanisms limits the effectiveness of diuretics and underlies such side effects as hypokalemia, hyperlipidemia, and impaired carbohydrate tolerance.

Side effects

Side effects of diuretics are numerous and may have important clinical implications. A well-known side effect is hypokalemia. It is caused by reflex activation of the RAAS, namely an increase in the secretion of aldosterone. Hypokalemia is considered to be a decrease in the concentration of K+ in the blood plasma less than 3.7 mmol/l. It is possible, however, that a less significant decrease in K+ is potentially unfavorable.

Symptoms of hypokalemia are muscle weakness, up to paresis, polyuria, tonic convulsions, as well as an arrhythmogenic effect associated with the risk of sudden death. The real possibility of developing hypokalemia exists in all patients taking diuretics, which makes it necessary to determine the level of K+ in the blood before starting treatment with diuretics and periodically monitor it. One of the measures to prevent hypokalemia during diuretic therapy is to limit consumption table salt. The classic recommendation remains the consumption of foods rich in potassium. Maintains a certain value and intake of potassium in capsules. One of the best measures to prevent hypokalemia is to use the minimum effective dose of diuretics. The likelihood of hypokalemia and other side effects of diuretics is significantly reduced when they are combined with ACE inhibitors or potassium-sparing drugs.

Approximately half of patients with hypokalemia also have hypomagnesemia(magnesium level less than 1.2 mEq/L), which contributes to the occurrence of arrhythmias. It is important to note that in some cases, hypokalemia cannot be eliminated without correcting magnesium deficiency. For this purpose, magnesium oxide is prescribed at 200-400 mg per day.

Diuretics induce hyperuricemia by increasing the reabsorption of uric acid. This problem is very relevant, since even without the prescription of diuretics, the level of uric acid is elevated in approximately 25% of patients. Prescribing diuretics to patients with hyperuricemia is undesirable, and gout - contraindicated. Asymptomatic, moderate increases in uric acid levels do not require discontinuation of diuretics.

Diuretic therapy may cause adverse effects changes in lipid composition: increased levels of total cholesterol, low-density lipoprotein cholesterol and triglycerides. The content of high-density lipoproteins does not change. The mechanism for this effect of diuretics is unclear. A number of researchers believe that the hyperlipidemic effect of diuretics correlates with hypokalemia and does not develop with its effective prevention.

Taking diuretics leads to increased glucose levels blood on an empty stomach and after a sugar load, as well as to the development of insulin resistance. Therefore, diuretics are not prescribed to patients with diabetes.

Postural hypotension(a sharp decrease in blood pressure when moving from a horizontal to a vertical position) occurs in 5-10% of patients taking diuretics, especially in old age. This effect is due to relative hypovolemia and decreased cardiac output.

Thiazide diuretics

Thiazide diuretics include compounds that have a cyclic thiazide group. Non-thiazide sulfonamides that do not have this group are very close to thiazide diuretics and will be considered together. Thiazide diuretics began to be used as antihypertensive agents in the late 50s of the last century. During this period, there was a radical revision of ideas about their effective dosages. So, if 30 years ago the optimal daily dose of the most popular thiazide diuretic, hydrochlorothiazide, was considered 200 mg, now it is 12.5-25 mg.

The dose-effect curve of thiazide diuretics has a gentle slope - as the dose increases, the hypotensive effect increases minimally, and the risk of side effects increases significantly. Forcing diuresis makes no sense, since for optimal blood pressure reduction it is important to ensure a relatively small but stable decrease in circulating blood volume.

Widely used in the treatment of hypertension combinations of thiazide diuretics with other drugs- (beta-blockers, alpha-blockers. At the same time, the combination of diuretics with calcium antagonists is not very effective, since the latter themselves have some natriuretic effect.

Main reasons for refractoriness to thiazide diuretics are excessive consumption of table salt and chronic renal failure. Acid metabolites (lactic and pyruvic acids) formed in excess quantities during renal failure compete with thiazide diuretics, which are weak acids, for common secretion pathways in the epithelium of the renal tubules.

The diuretic xipamide (Aquaphor), which is structurally similar to thiazides, has appeared on the pharmaceutical market. Aquaphor has been well studied abroad and has been used in clinical practice for 25 years. The mechanism of action of aquaphor is to suppress sodium reabsorption in the initial part of the distal tubule, however, unlike thiazides, the point of application of aquaphor is the peritubular part of the nephron. This property ensures that aquaphor remains effective in renal failure when thiazide diuretics do not work. When taken orally, aquaphor is rapidly absorbed, the peak concentration is reached after 1 hour, the half-life is 7-9 hours. The diuretic effect of aquaphor reaches a maximum between 3 and 6 hours, and the natriuretic effect lasts 12-24 hours. When treating hypertension, the drug is prescribed 5- 10 mg once daily. The antihypertensive effect of aquaphor persists in patients with concomitant circulatory failure. In case of edema syndrome, the dose of aquaphor can be increased to 40 mg per day. The drug has been shown to be effective in patients with chronic failure blood circulation, as well as chronic renal failure, refractory to thiazide and loop diuretics.

A special place among the drugs in this series is occupied by a thiazide-like diuretic. indapamide(ariphon). Due to the presence of a cyclic indoline group, arifon reduces vascular resistance to a greater extent than other diuretics. The hypotensive effect of arifon is observed against the background of a relatively weak diuretic effect and minimal changes in the balance of electrolytes. Therefore, hemodynamic and metabolic side effects characteristic of thiazide diuretics and related sulfonamides are practically absent or only slightly expressed during Arifon therapy. Arifon does not affect cardiac output, renal blood flow and the level of glomerular filtration, does not violate carbohydrate tolerance and blood lipid composition. Arifon is not inferior in efficiency to others antihypertensive drugs and it can be prescribed to a wide range of patients, including patients with concomitant diabetes and hyperlipoproteinemia. Arifon compares favorably with thiazide diuretics in its clearly documented ability to reverse the development of left ventricular hypertrophy. The half-life of arifon is about 14 hours, due to which it has a prolonged hypotensive effect. Arifon therapy provides control of blood pressure levels for 24 hours, including in the early morning hours. Arifon is prescribed in a standard dosage - 2.5 mg (1 tablet) once a day.

Loop diuretics

Loop diuretics include three drugs: furosemide, ethacrynic acid and bumetanide. Loop diuretics have a powerful saluretic effect due to the blockade of the Ma2+/K+/Cl- cotransport system in the ascending limb of the loop of Henle. The main indication for their use in hypertension is concomitant renal failure, in which thiazide diuretics are ineffective. Prescribing loop diuretics to patients with uncomplicated hypertension makes no sense due to their short duration of action and toxicity. All side effects typical of thiazide diuretics are not to a lesser extent and loop diuretics, which also have an ototoxic effect.

The most popular drug from the group of loop diuretics is furosemide has a powerful but short-term (4-6 hours) effect, so it should be taken twice a day. For hypertension with chronic renal failure, the dose of furosemide is selected individually, according to the doubling rule (40, 80, 160, 320 mg).

Potassium-sparing diuretics

This group of drugs consists of spironolactone(veroshpiron), amiloride And triamterene, which have a purely auxiliary value in hypertension. Triamterene and amiloride are direct inhibitors of potassium secretion in the distal tubules and have a very weak diuretic and hypotensive effect. They are used in combination with thiazide diuretics to prevent hypokalemia. Doctors are familiar with the drug triampur(combination of 25 mg hypothiazide and 50 mg triamterene). Less known is the drug moduretic, containing 50 mg of hypothiazide and 5 mg of amiloride. Triamterene and amiloride are contraindicated in chronic renal failure due to the high risk of hyperkalemia. It is known that co-administration of triamterene and indomethacin can cause reversible acute renal failure. During therapy with amiloride, side effects such as nausea, flatulence, and skin rash occasionally occur.

Mechanism of action of spironolactone consists of competitive antagonism with aldosterone, of which it is a structural analogue. In fairly high doses (100 mg per day), spironolactone has a pronounced diuretic and hypotensive effect. However, spironolactone has no independent value in the treatment of hypertension, since its long-term use is often accompanied by the development of hormonal side effects (gynecomastia in men and amenorrhea in women). When taking lower doses (50 mg per day), the frequency of side effects decreases, but both the diuretic and hypotensive effects are significantly weakened.

What diuretics are currently used to treat patients with hypertension?

The main drugs of this class in the treatment of hypertension are thiazides and thiazide-like diuretics. The most commonly used drugs include hydrochlorothiazide, chlorthalidone and indapamide (Arifon-retard).

Thiazide diuretics can be used in a wide range of patients, both with uncomplicated and complicated hypertension. Clinical situations in which the use of diuretics is preferable:

Heart failure
Diabetes
Systolic hypertension
Prevention of recurrent strokes
Postmenopause
Cerebrovascular diseases
Elderly age
Black race

The only contraindications to the use of thiazides are pregnancy And hypokalemia. Caution is required when used in patients with gout, dyslipidemia, diabetes mellitus and with severe renal failure.

Which drug from this group is the best?

Currently, significant interest in an antihypertensive diuretic, which has a weak diuretic effect and a pronounced vasoprotective effect, is clear and justified. Arifonu-retard(indapamide). Metabolic concerns regarding thiazide diuretics do not concern Arifon-retard, which in a dose reduced to 1.5 mg does not worsen the parameters of lipid and carbohydrate metabolism and is therefore more preferable when choosing a diuretic. For patients with hypertension in combination with diabetes mellitus, the use of Arifon-retard for combination treatment is necessary, given the very low target level of blood pressure reduction (130/80) and metabolic neutrality.