Diuretic drugs. The principle of action and effect of diuretics. Diuretics that function at the glomerular level

It is customary to call diuretics synthetic drugs that inhibit the reabsorption of salts and water, increasing their excretion in the urine, and also increasing the rate of its formation, thereby reducing the total amount of fluid in the body. Since these drugs are widely used in various branches of medicine, the list of diuretic drugs is replenished every year. All diuretics can be divided into 4 groups.

Diuretics - names of drug groups

Saluretics;
Potassium-sparing drugs;
Osmotic agents;
Calcium-saving tablets.

Diuretics - a list of saluretics

It is difficult to remember all the diuretic names of saluretics, since 3 types of drug subgroups are combined under this general concept. They are prescribed for glaucoma and hypertension.

Saluretics (diuretics) list of drug subgroups:

loop diuretics;
carbonic anhydrase inhibitors.

The trade name of the diuretics included in these groups:

Chlorthalidone,
Bumetonide,
Diakarb,
Hydrochlorothiazide,
Bumetonide,
Fonurite,
Indapamed,
Furosemide,
Acetamoc,
Chlortizide,
Ethacrynic acid,
Dehydratin,
Prirethanides.

Potassium-sparing diuretics, drug names

Potassium-sparing diuretics are prescribed for the treatment of patients with hypertension in combination with other drugs. Potassium-sparing diuretics are usually combined with thiazide and loop drugs. The main effect of potassium-sparing tablets, as the name suggests, is to prevent the elimination of potassium salts along with the removal of excess fluid from the body when taking strong diuretics.

Pharmacological names of diuretic drugs in this group:

Triamur,
Veroshpiron,
Amiloride,
Spironolactone,
Triamteren,
Aldactone.

Osmotic drugs - a list of diuretics

To date, osmotic agents have the shortest list of diuretics. Their names boil down to:

Sorbit,
Manitou,
Urea.

The peculiarity of diuretics, the names of which are given above, are that they are able to quickly reduce the pressure in the plasma, due to which water is removed from the edematous area. This mechanism of action of osmotic drugs was the reason for their frequent prescription for edema of the larynx, lungs, brain, glaucoma, peritonitis, pill poisoning, burns and sepsis.

From the above list of osmotic diuretics, Manit is most often used, since it has the longest duration of action and the least number of side effects.

Calcium-sparing diuretics, names of drugs and their features

This group of diuretics is especially recommended for elderly people, patients with osteoporosis and children. That is, to all those for whom the loss of calcium by the body, and hence the bones, is fraught with fractures in the future. In addition, calcium-sparing tablets have shown themselves well in the treatment of postmenopausal hypertension in women and in the treatment of IDDM (some patients with this form of diabetes feel worse when their calcium levels are low). In addition, this group of drugs has one interesting feature - to catalyze the actions of other diuretics when taken together, which allows you to achieve a high effect without resorting to increasing the dosage.

Calcium-sparing diuretics (tablets) drug names:

Oxodolin,
Hygroton,
Hypothiazide,
Hydrochlorothiazide,
Tenzar,
Acrylamide,
Retapres,
Akuter-Sanovel,
Pamid,
Arindap,
Lorvas,
Arifon,
Ionic,
Indap,
Indiour,
Indapres,
Indapsan and others.

Diuretics or diuretics are a special type of substance that increases the amount of urine produced 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 absolutely any substance that stimulates the production of urine. For example, they include hypotonic aqueous solutions, including pure 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 will certainly 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 dwell in a little more detail on all of them.

Thiazide diuretics

They are a special class of diuretics that are most commonly 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 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 to treat edema of various origins.

Potassium-sparing diuretics

They are a special class of diuretics that does not promote the excretion of potassium in the urine from the body. Potassium-sparing diuretics are most commonly used as adjuvant therapy (adjuvant) 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 independently used as diuretics (diuretics). Basically, carbonic anhydrase inhibitors are used in glaucoma.

The mechanism of action of diuretics

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

Target number 1: transport proteins

Thiazide diuretics, loop diuretics, triamterene, amiloride act on specific transport proteins of the epithelial membrane of the renal tubules.

Loop diuretics, for example, act on the Na-K-2Cl symporter in the luminal (ascending) tubular epithelium of the ascending loop of Henle. The strong diuretic effect is explained by the fact that it is in the ascending part of Henle's loop that most of the 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. Thus, they do not allow this hormone to function fully.

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

Target number 3: water

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

Target number 4: the enzyme carbonic anhydrase

There is a subclass of diuretics that inhibits the enzyme carbonic anhydrase, it is called accordingly - 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. Under the action of carbonic anhydrase inhibitors, sodium bicarbonate is not reabsorbed, but excreted in the urine (urine becomes alkaline). Following sodium, potassium and water are excreted in the urine. The diuretic effect of substances of this group is weak, since almost all sodium excreted in the urine in the proximal tubules is retained in the distal parts of the nephron. Therefore, carbonic anhydrase inhibitors are currently not used independently as diuretics.

Application in medicine

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

Diuretics for weight loss

Diuretics are often overused by people with an eating disorder, especially people with bulimia, in an effort to lose weight. However, diuretics do not contribute to weight loss, they promote, in this case, only the elimination of fluid and imaginary weight loss by reducing the volume of fluid in the body. Read more about this in our article: myths and reality.

Diuretics in sports

In sports, diuretics are commonly used to disguise drug use. Diuretics increase the volume of urine and dilute the concentration of doping substances and their metabolites. Also, diuretics in sports are used to lose weight quickly (by reducing the volume of fluid in the body) in order to get to competitions in a smaller weight category, in sports such as boxing or wrestling.

Side effects of diuretics

The side effects of diuretics include a wide range of phenomena, both related to their 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 are disorders of water-salt metabolism. They also make it difficult for the heart (therefore, they cannot be used for 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 the risk of kidney stones;
neurotoxicity (paresthesia and drowsiness);
allergic reactions.

Side effects of thiazide diuretics

Thiazide diureticshave the following main side effects

Hyperglycemia;
Hyperuricemia;
Hypokalemia (the mechanism of its development is described below);
Hyponatremia;
Hypomagnesemia;
Hypocalciuria;
Hyperuricemia, although rare. Women have less 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 very low density lipoprotein (VLDL) and triglyceride (TG) levels. In general, the risk of developing atherosclerosis is relatively low;
Central nervous system (CNS) disorders: weakness, xanthopsia, fatigue, paresthesia. They are rare;
Impotence develops in 10% of men due to a decrease in the volume of fluid in the body;
Allergic reactions. Cross-allergy occurs with the sulfa group;
Photosensitization and dermatitis are rarely observed, and extremely rarely, thrombocytopenia, hemolytic anemia, and acute necrotizing pancreatitis.

Are common side effects of loop diuretics:

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

Rare side effects of loop diuretics:

dyslipidemia,
increased 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:

Convulsions.
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 (for 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 various groups with each other, taking into account the location 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 fully visible, just scroll to the side.

Options	Thiazide and thiazide-like	Loopback	Potassium-sparing	Osmotic	Carbonic anhydrase inhibitors
Scene	Distal tubules	Ascending part of the loop of Henle	Collecting ducts	Distal tubules descending part of Henle's loop	Proximal tubules
Appointment	Inside	Inside, into a vein	Inside	Into the 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 (++)
Power	Average	Strong	Weak	Strong	Weak
Main indications	1) Arterial hypertension 2) Edema, except for severe renal 3) Hypercalciuria (a decrease in the risk of calcium nephrolithiasis due to a decrease in the concentration of Ca in the urine, since its reabsorption into the blood increases) 4) Osteoporosis (because the reabsorption of Ca in the kidneys increases) 5) Nephrogenic diabetes insipidus	Swelling, especially with renal damage, edema of the brain, lungs, forced diuresis in case of poisoning, hypercalcemia.	Together with other diuretics to preserve K; spironolactone - with cirrhosis of the liver and with CHF.	Acute poisoning cerebral edema	Glaucoma, epilepsy, altitude sickness
Major side effects	Hypokalemia, hyperuricemia, gastrointestinal disorders, allergies	Hypokalemia, alkalosis, hypovolemia, hyperuricemia, ototoxicity	Hyperkalemia, acidosis	Dehydration	Hyperkalemia, acidosis

Note to the table: action + - weak, ++ - moderate, +++ - strong, ++++ - very strong, 0 - no.

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

Diuretics increase urination (diuresis)

- filtration enhancement(formation of primary urine)

- inhibition of electrolyte reabsorption processes (primarily Na +, Cl -) and water in the kidney tubules(formation of secondary urine).

In medical practice, they are used for edema of various etiologies (acute and chronic). In addition, diuretics are used in case of poisoning with drugs and other chemical compounds to accelerate their excretion from the body (the so-called forced diuresis), and also as antihypertensive drugs.

Diuretic classification:

By localization of action in the nephron:

Thiazide- act on the initial part of the distal renal tubules (hydrochlorothiazide).

Thiazide-like- act on the initial part of the distal renal tubules (clopamide (brinaldix), indapamide (arifon), chlorthalidone (oxodoline)).

Loop diuretics- act on the ascending part of Henle's loop (furosemide (lasix), bumetanide (bufenox), ethacrynic acid (uregit)).

Potassium-sparing diuretics- act on the distal tubule and collecting ducts (triamterene (pterofen), amiloride, spironolactone (aldactone, veroshpiron).

Osmotic- act on the proximal tubule, the descending part of Henle's loop, collecting ducts (mannitol (mannitol), sorbitol, urea).

Carbonic anhydrase inhibitors- act on the proximal tubule

(diacarb (acetazolamide)).

Watercolors- demeclocin (an ADH antagonist).

Herbs with a diuretic effect- bearberry leaf (foliumUvaeursi), lingonberry leaf (foliumVitisidaei), birch buds (gemmaeBetulae), field horsetail herb (herbaEquisetiArvensis), juniper fruits (fructus Juniperi).

Medicines with a diuretic effect:cardiac glycosides,

xanthines - enhance glomerular filtration;

By the strength of the action:

Strong(cause the excretion of 15-25% of filtered sodium) - loop diuretics, osmotic (natriuresis is not great).

Medium strength(excretion of 5-10% of filtered sodium) - thiazide, thiazide-like diuretics.

Weak(excretion of not -5%) - diacarb (fonurite), potassium-sparing (triamterene, amiloride, spironolactone).

By the nature of the effect:

Hydrouretics

Saluretics

Potassium-sparing

Carbonic anhydrase inhibitors.

By speed and duration of action:

- fast and short-term effect: loop, osmotic.

- medium strength and duration: thiazide, potassium-sparing (triamterene),

inhibitors of carbonic anhydrase, xanthines.

- delayed and prolonged action: thiazide-like, potassium-sparing (spironolactone).

Comparative characteristics, distinctive properties and features of the appointment of diuretics are presented in table 1.

Table 1

Comparative characteristics of diuretics

A drug

Features of appointment

Dehydration (after intravenous administration, initially increases the osmotic pressure of the blood, ie, "pulling fluid" from the tissues, useful for cerebral edema) \u003d\u003e an increase in BCC, which decreases with development

diuretic effect

Increases BCC

Alkalizes urine

Increase the osmotic pressure of blood and primary urine, cause tissue dehydration, which reduces water reabsorption;

increase renal blood circulation, glomerular filtration.

Used for local edema (brain, larynx, lungs)

Not used for cardiovascular

vascular insufficiency.

It is used in acute hemolytic conditions, to prevent the precipitation of proteins and hemoglobin.

Acute poisoning with water-soluble poisons

Furosemide

prostacyclin and reduces preload.

Dramatically displays K + and

increases the threshold of sensitivity to cardiac

glycosides.

Changes the ionic balance in the lymph of the inner ear.

Improves metabolism in

damaged brain tissue.

Blocking sulfhydryl groups of enzymes in the loop of Henle, which leads to

a decrease in the reabsorption of Na +, Mg 2+, K + ions and reduces the reabsorption of H 2 O. Promote the excretion of K +, Mg 2+, Ca 2+, Na + ions.

It is prescribed for pulmonary edema on

background of pulmonary

failure.

Exclude concurrent use.

Causes an ototoxic effect;

exclude combination with

aminoglycoside antibiotics.

Used for traumatic brain injury.

Arterial hypertension,

hypertensive crisis;

Cirrhosis of the liver with portal

hypertension and ascites;

Acute poisoning (forced diuresis);

Hydrochlorothiazide

Increases the reabsorption of Ca 2+

Washes Na + from

vascular wall.

Delays urinary

They inhibit the activity of Na + -K + -ATP-ase, succinate dehydrogenase, bind carbonic anhydrase. As a result, the supply of energy to the sodium pump is disrupted.

Suppress reabsorption

ions Na +, Cl - and water. Promote elimination

ions K + and Mg 2+ and detain Ca 2+ ions.

Combine with furosemide,

removing Ca 2+

It is prescribed for hypertensive

There is a danger of provocation of gout.

Diabetes insipidus;

Subcompensated glaucoma;

Arterial hypertension

(in complex therapy)

Congestive heart failure (reduces preload)

Indapamide

Indapamide stimulates the synthesis of prostaglandin E 2 in the endothelium, weakens

the reaction of smooth muscles to pressor amines, prevents the entry of calcium ions into them through voltage-dependent L-type channels, exhibits properties

antiplatelet agent, causes regression of left ventricular hypertrophy.

Used for arterial hypertension. It has only a hypotensive effect, since 80% of the molecules accumulate in the arterial wall.

Reduces blood pressure in 80% of patients resistant to inhibitor therapy

angiotensin converting

enzyme.

Moderate diuretic effect

indapamide occurs by the end of the first week of course therapy and becomes maximum after 3 months.

Acetazolamide

Reduces the secretion of cerebrospinal fluid and intracranial pressure.

Inhibits secretion

intraocular fluid.

Displays bicarbonates.

Reduces HCl secretion

Inhibits the activity of carbonic anhydrase of the kidneys, central nervous system and ciliary body, which disrupts the exchange reabsorption of Na + and H + ions,

increases diuresis.

Promotes elimination

K +, R 5+, Ca 2+ development

It is used for hydrocephalus and epilepsy.

Used for glaucoma.

It is prescribed together with sodium bicarbonate.

Control the release of HCl

Edema associated with chronic cardiopulmonary failure;

Emphysema of the lungs;

Metabolic alkalosis;

Spironolactone

Violates the entry of Na + into the vascular wall.

Reduces afterload on the heart.

Strengthens processes

biotransformation

cardiac glycosides.

Competitively blocks intracellular aldosterone receptors that facilitate the transfer of Na + across cell membranes,

enhances its excretion from the body and inhibits

elimination of K + and Mg. 2 +

It is used for hypertension.

It is used for angina pectoris.

It is used for prevention

intoxication.

Hypokalemia;

Heart failure;

Arterial hypertension

(in combination with thiazides);

table 2

Indications for the use of diuretics.

Indications	Drug of choice
Swelling with cardiovascular failure	Triampur, triamterene, spironolactone, furosemide
Renal edema	Furosemide, hydrochlorothiazide
Acute pulmonary edema	Furosemide, beckons (with toxic pulmonary edema)
Cerebral edema	Mannitol, furosemide
Ascites in liver cirrhosis	Hydrochlothiazide, acetazolamide
Glaucoma	Hydrochlothiazide, acetazolamide
Epilepsy	Hydrochlothiazide, acetazolamide
Hypertonic disease	Hydrochlothiazide, Triampur, Amiloride
Forced diuresis	Furosemide, mannitol, ethacrynic acid
Metabolic acidosis	Hydrochlorothiazide, sodium bicarbonate
Metabolic alkalosis	Diacarb, sodium chloride, potassium chloride
Inflammatory diseases urinary tract	Decoction of bearberry leaves, juniper berries, field horsetail, knotweed

The side effects of diuretics are mainly associated with a direct effect on the electrolyte balance and acid-base balance of the body.

Table 3

Side effects of diuretics

Types of adverse reactions	Funds causing side effects	Remedy and warnings
Associated with electrolyte disturbances
Hypokalemia		Combining with potassium-sparing diuretics. Using a diet rich in potassium.
Hyperkalemia	Triampur, spironolactone	Potassium restriction in the diet. The use of glucose with insulin, calcium gluconate.
Hyponatremia	Hydrochlorothiazide, furosemide	Application of sodium chloride
Associated with a violation of acid-base balance
	Acetazolamide	Appointment together with sodium bicarbonate. Dose reduction or drug withdrawal.
	Hydrochlorothiazide, furosemide, ethacrynic acid.	The use of triampur, ammonium chloride, calcium chloride.
Other side effects
Provocation	Hydrochlorothiazide, furosemide, ethacrynic acid.	Exclude long-term use. Appointment of uricosuric agents.
Hyperglycemia	Hydrochlorothiazide, furosemide	Exclude the appointment of patients with diabetes mellitus.
	Furosemide, ethacrine	To exclude long-term use and combination with aminoglycoside antibiotics.
Azotemia	Triamterene, amiloride	Appointment of Lespenefril
Formation of phosphate and oxalate stones.	Furosemide, ethacrine	Simultaneous appointment hydrochlorothiazide warns excretion of Ca 2+ in the urine.

General principles of prescribing diuretics

The daily diuresis during treatment should not exceed 2-2.5 liters.

Rational choice considering:

- severity of edematous syndrome

- imbalance of hemodynamics

- baseline electrolyte balance

- features of the pharmacological characteristics of the diuretic, its undesirable effects

- individual tolerance

Combination of diuretics

In urgent cases, intravenous administration of strong and fast-acting diuretics

Control and correction of electrolyte and acid-base balance

Diuretics

		Method of appointment,
Hydrochlorothiazide (hypothiazide, dichlothiazide) Dichlothiazidum (B)	Tablets of 0.025 and 0.1 No. 20	Inside at 0.025-0.05 in the morning before meals.
Chlorthalidone (oxodoline) Chlortalidonum (B)	0.05 N tablets. 50	Inside, 1-2 tablets in the morning before meals.
Furosemide (lasix) Furosemidum (B)	Tablets of 0.04 N. 50 Ampoules 1% solution of 2 ml N.10	Inside, 1 tablet in the morning before meals. Into the muscle, into the vein, 2-3 ml 1-2 times a day.
Spironolactone (veroshpiron) Spironolactonum (B)	Tablets 0.025	Inside, 1 tablet 2-4 times a day.
Indapamide (arifon) Indapamidum (B)	Dragee 0.0025	Inside, 1 tablet in the morning before meals.
	Vials of 30.0	Dissolve the contents of the vial in 5% glucose solution or water for injection and inject into a vein drip (in the form of 10-15-20% solution)

Anti-gout remedies

Gout is a disorder of purine metabolism that results in a high concentration of uric acid in the serum (hyperuricemia). As a result of the deposition of crystals of uric acid salts (urates) in the synovial tissue of the joints and cartilage, repeated episodes of acute arthritis occur. In addition, the formation of uric acid stones in the kidneys is possible.

With the pharmacotherapy of gout, it is necessary to eliminate the acute attack as quickly as possible, as well as the prevention of repeated exacerbations and the formation of urate crystals in the tissues and kidneys.

Means for stopping an acute attack of gout:

Non-steroidal anti-inflammatory drugs:colchicine, naproxen, indomethacin, diclofenac, etc.

Steroid anti-inflammatory drugs: prednisolone, methylprednisolone, etc.

Remedies for gout:

Uricodepressive(inhibit xanthine oxidase \u003d\u003e uric acid synthesis decreases) : allopurinol

Uricosuric(enhancing the excretion of uric acid by reducing the reabsorption of uric acid in the renal tubules) : etamide, sulfinpyrazone.

Mixed type: ugly.

The name of the product, its synonyms, storage conditions and the procedure for dispensing from pharmacies.	Release form (composition), amount of the drug in the package.	Method of appointment, average therapeutic doses.
Cistenal Cystenalum (B)	10 ml vials	Inside 3-4 (up to 10) drops. 3 times a day (with sugar, before meals).
Aethamidum (B)	0.35 pills	Inside, 1 tablet 4 times a day.
	Powder (granules) in vials of 100.0	Inside, 1 teaspoon in half a glass of water 3-4 times a day before meals.
Allopurinol Allopurinolum (B)	0.1 tablets	Inside, 1 tablet 2-3 times a day after meals.

Means that affect the tone and contractile activity of the myometrium.

Classification of drugs affecting the myometrium.

Uterine remediesweaken or increase the contraction of the uterus. They are used to maintain pregnancy, stimulate labor and stop uterine bleeding.

Many have heard the term “diuretic” more than once. What it is, we will try to figure it out below. This group of drugs has its own classification, properties and features.

Diuretic - what is it?

Diuretics are also called diuretics. They are drugs of synthetic or herbal origin that can increase the excretion of urine by the kidneys. Due to this, along with urine, water also increases, and the level of fluid in the cavities and tissues of the body decreases. Because of this, edema decreases or disappears altogether. Diuretics are drugs that are widely used in the treatment of hypertension (high blood pressure). They are often used to treat mild congestive heart failure, as well as a number of liver ailments and diseases associated with circulatory disorders, which provoke congestion in the body. Often, diuretic medications are used to reduce or completely eliminate the symptoms of flatulence, which sometimes accompanies PMS or appears already during menstruation. With strict adherence to the treatment regimen and dosages, they do not cause severe side effects. They are fairly safe to use.

during pregnancy

Many gynecologists advise against drinking diuretics during pregnancy. The drugs can be unsafe for the fetus and maternal health. Negative action was discovered not so long ago. Previously, diuretic drugs were used to reduce edema in pregnant women, counteract preeclampsia, etc.

Diuretics: classification

There are different types of diuretic medications. Each category has its own disadvantages. Today there are such groups of medicines:

Loop medication.

Thiazide medicines.
... Thiazide-like drugs.

These groups will be discussed in more detail below.

Loop diuretics

This category of drugs is the most common. It includes drugs such as Ethacrynic acid, Torasemide, Furosemide, Pyretanid, Bumetanid. Despite the fact that they can differ significantly in chemical structure, these diuretics have the same mechanism of action. These medications inhibit the reabsorption of substances such as sodium, chlorine and potassium. The name "loop diuretics" is related to their mechanism of action. Resorption occurs in the ascending lobe of the Henle loop. It is carried out due to the blockade of sodium, chlorine, potassium ions in the apical membrane of the tubular epithelium of cells. Due to this, the work of the turn-countercurrent system in the kidneys is suppressed. In addition, diuretics of this type are able to dilate the vessels of the cortex.

Side effects of loop diuretics

The strength of the effect of these medications is unusually great: they can increase urine output by 25%. Unlike other drugs that lose their effect with the normalization of the BCC, loop-type diuretics continue to function under these conditions. It is due to their strong diuretic effect that they can provoke such side effects. The most rare and severe are a drop in blood pressure, hypovolemia, a decrease in GFR and renal blood flow. Due to the increased level of excretion of hydrogen, chlorine and potassium, metabolic alkalosis is not excluded. Sometimes loop diuretics provoke hyponatremia and hypokalemia. In rare cases - hyperglycemia, hyperuricemia. Other side effects include lightheadedness, nausea, and weakness. The medicine often provokes permanent or temporary deafness, as well as neutropenia. All medications of this type, which were listed above, are excreted from the body by the kidneys, metabolized in the liver.

Indications for loop diuretics

These medications are prescribed for any type of heart failure. And they are especially necessary for diseases such as refractory heart failure and pulmonary edema. The drugs are also effective for hyponatremia, hypoalbuminemia, hypokalemia, hypochloremia, and renal failure. Loop diuretics continue to work when other diuretic groups and combinations are ineffective. This is their great value. Therefore, this type is so common - a loop diuretic. We have already figured out what it is.

Thiazide diuretics

These medications and their derivatives (Indapamide, Chlorthalidone and Metolazone) are used quite often. First of all, this is due to their high rate of absorption in the gastrointestinal tract, as well as a good level of tolerance by patients. Thiazide diuretics are less powerful than loop diuretics, but due to their long duration of action, they are indicated for people with chronic ailments such as essential hypertension and mild congestive heart failure. Thiazide diuretics are prescribed for oral administration. Diuresis, as a rule, begins after 1-2 hours, but the therapeutic antihypertensive effect in some cases can be observed only after 3 months of continuous treatment. The parent of this group is chlorothiazide. It is characterized by low fat solubility, and, consequently, low bioavailability. Because of this, higher dosages of the drug are required for the therapeutic effect. The drug "Chlorthalidone" is absorbed rather slowly, therefore its duration of action is somewhat longer. Means "Metolazone" is often very effective in patients with reduced renal function, in contrast to other medications in this category.

Potassium-sparing diuretics

There is also a potassium-preserving diuretic. What it is? These drugs are used to treat hypertension in combination with other types of drugs. They prevent excess potassium from being excreted from the body, which is a common side effect of other diuretic drugs. Hypokalemia is a decrease in plasma potassium levels. She is a constant companion of thiazide diuretics, which are often prescribed for the treatment of hypertension. When the level of potassium is greatly reduced, the patient begins to feel weak, gets tired faster, he has cardiac arrhythmia. To prevent this, potassium-sparing diuretics are often prescribed along with thiazide drugs. They retain in the body along with potassium other essential minerals - magnesium and calcium. However, they practically do not delay the withdrawal of excess fluid and sodium. The disadvantage of potassium-sparing medicines is as follows. Plasma potassium levels may increase excessively (more than 5 mmol / L). This condition is called hyperkalemia. It is capable of causing muscle paralysis and heart rhythm disturbances, up to and including its complete stop. The development of pathology is most possible in patients with renal failure.

Use for the treatment of hypertension

Diuretics for hypertension have worked well. They help remove fluid from the body, which reduces blood pressure. It is a proven fact that diuretic drugs are more effective for the treatment of elderly patients in comparison with beta-blockers. Diuretic medications are included in the list of first-line medications that are used to normalize blood pressure. This category should be used for the initial therapy of hypertension (uncomplicated) according to the recommendations of US physicians. Due to the great importance of blood pressure control, as well as reducing cardiovascular risks during treatment, special attention is paid to the metabolic effects that are characteristic of antihypertensive medications. Their influence on the course of associated diseases and organoprotective characteristics is also important.

Thiazide-like and thiazide medicines for hypertension

In the past, hypertension was usually treated with loop diuretics. But now they are more used to treat kidney, heart failure and edema. Research results have shown good efficacy of thiazide-type drugs. They improve the prognosis of hypertension. However, the reduction in the risk of coronary complications when using these drugs was not so pronounced in comparison with the expected results. The use of thiazide drugs increases the likelihood of developing arrhythmias. In some patients, even sudden arrhythmic death is possible. Disorders of carbohydrate and lipid metabolism, as well as hyperuricemia, are also common. The course of atherosclerosis and diabetes mellitus may worsen. Medications of this group are often combined with potassium-sparing diuretics.

Thiazide-like drugs became the next level of evolution of diuretics for the treatment of hypertension. In particular, the drug Indapamid, synthesized in 1974, has proven itself well. The advantage is that thiazide-like agents have much less effect on sodium reabsorption, which means that they remove much less potassium from the body. Therefore, there are practically no negative metabolic and diabetogenic effects. It has now been proven that the drug "Indapamide" used in small dosages, in addition to the diuretic action, can play a role due to the vasodilator activity and stimulation of the production of prostaglandin E2.

In modern conditions, thiazide and thiazide-like medications are very widely used not only to reduce blood pressure, but also for prophylactic purposes, as well as for the treatment of target organ damage. These drugs are very often prescribed as part of combination therapy courses. They have proven themselves well and therefore are widely used in different countries of the world.

To date, there is no such classification of diuretics that would take into account all aspects of the action of these types of medications. So, groups can be divided according to:

chemical structure;
place of action;
mechanism of action;
the strength of the action;
the speed of appearance of effects;
duration of exposure;
by side effect.

The very first classification of diuretics was based on differences in the chemical structure of drugs. Then there was an attempt to generalize the types of diuretics by the nature of their effect on the kidneys. However, some diuretic drugs have extrarenal effects. Also, an attempt to classify diuretics according to which part of the nephron they affect was unsuccessful, since osmotic drugs, Ethacrynic acid, Furosemide, Xanthines and others act not on a specific part of the nephron, but throughout its entire length. In connection with such features of diuretics, the classification by the mechanism of action is the most rational.

When treating a patient, it is no less important, from a clinical point of view, to classify diuretics according to the duration of exposure, the speed of onset of the effect, and also according to the strength of the action.

Thiazide diuretics

Thiazide and thiazide-like diuretics have become widespread due to their effectiveness and the fact that their use does not require too strict restriction of salt intake in patients with moderate and mild heart failure.

In fact, thiazide diuretics are medium-strength diuretics, the main difference of which from loop drugs is to reduce calcium excretion and increase sodium concentration in the distal nephron, which allows increasing the exchange of sodium for potassium, increasing the excretion of the latter.

When prescribing thiazide diuretics, the list of drugs mainly consists of Hydrochlorothiazide and Chlothiazide, after taking which the maximum concentration of active substances in the body is reached after 4 hours and does not decrease for 12 hours.

Many derivative drugs have been created on the basis of Chlothiazide, however, it is most convenient to prescribe Chlorthalidone, since this thiazide diuretic is taken only once a day, while the same Chlothiazide must be taken 500 mg every 6 hours.

Loop diuretics

Loop diuretics are diuretic drugs, which include drugs such as Torasemide, Pyrethanide, Bumetonide, Ethacrynic acid and Furosemide. Usually, these drugs are taken either orally on an empty stomach (in this case, their absorption is about 65%) or intramuscularly / intravenously (in this application, the absorption reaches 95%, due to good binding to blood proteins).

Loop diuretics differ in their mechanism of action from thiazide diuretics in that they reduce calcium reabsorption, thereby increasing the excretion of the latter with urine from the patient's body. These drugs should be taken no more than 2 times a day, despite the fact that half-elimination from the blood occurs on average in 60 minutes.

When prescribing loop diuretics together with other drugs, one should take into account the fact that they are well combined with both cardiovascular drugs and other diuretics. But the simultaneous use with nephrotoxic and ototoxic drugs, as well as with nonsteroidal anti-inflammatory drugs, is contraindicated, since loop diuretics in this case will increase the undesirable effect of the former on the patient, and in the case of nonsteroidal anti-inflammatory drugs, the diuretic will act as a pharmacodynamic antagonist.

Potassium-sparing diuretics

To preserve potassium in the human body, the diuretic must act on the distal tubule, where it either inhibits potassium secretion or acts as a direct antagonist of aldosterone. Diuretics that do not excrete potassium are often prescribed for hypertension in order to lower blood pressure, but you should be aware that this group of diuretics has a weak effect, therefore, its appointment as the only treatment for high blood pressure is ineffective.

Therefore, diuretics that do not excrete potassium are used not in isolation, but in combination with thiazide and loop diuretics to prevent hypokalemia. The most commonly used potassium-sparing diuretics are Veroshpiron, Aldactone, Spironolactone, Amiloride and Triampur.

Unlike potassium-sparing diuretics, potassium-sparing diuretics have one serious side effect - the risk of hyperkalimia, especially in patients with diabetes mellitus, renal failure, or if these drugs are combined with ARA inhibitors, ACE inhibitors, or with potassium preparations. In addition, if the prescribed potassium-sparing drugs were hormonal antagonists of aldosteronam, then gynecomastia and impotence in men and menstrual irregularities, pain in the mammary glands and postmenopausal bleeding in women can be added to the negative consequences.

Osmotic diuretics

The mechanism of action of osmotic diuretics is based on an increase in the osmotic pressure in the blood plasma, as a result of which water extraction begins from the edematous tissues, and as a result, the volume of circulating blood increases. As a result of an increase in the total volume of circulating blood, there is an increase in blood flow in the glomeruli of the kidneys, an increase in filtration, while a violation in the functioning of the countercurrent-rotary system of the Henle loop is observed, which leads to the suppression of passive reabsorption of chlorine and sodium in the ascending knee of the Henle loop.

Osmotic diuretics include Urea, Sorbitol, Mannitol. Today, of these drugs, Mannitol is most often used, since Sorbitol and Urea have a shorter duration of action and have a weaker effect. In addition, it is worth considering the side diseases of the patient, since the same Urea cannot be prescribed to patients with impaired liver or kidney function.

Side effects of taking osmotic diuretics include an increase in blood pressure, vomiting, the risk of developing bilirubin encephalopathy, nausea, headaches, and with the use of urea and an increase in the level of nitrogen in the blood.

Lungs diuretics

Light diuretics are widely used in gynecology and pediatrics in the fight against edema of the hands and feet in pregnant women, in the normalization of slightly elevated blood pressure in children and in the treatment of elderly people. In the first case, osmotic drugs can be used as mild diuretics, since their main action is aimed precisely at removing fluid from edematous tissues. Children and the elderly are often prescribed potassium-sparing diuretics as a weak diuretic, which in most cases is sufficient when it is required to lower the child's blood pressure by 10-20 mm.hrs. In elderly people, due to changes in the course of biochemical processes, which in all respects belong to mild diuretics, they are able to provide the maximum possible positive result.

It should be noted that it is better to give preference to those drugs that fall under the classification of "lungs" and do not have various side effects of the hormonal plan, which is especially important when it comes to small children and pregnant women. Also, various herbal infusions can be attributed to light diuretics.

Strong diuretics

Unlike light diuretics, which have been used in folk medicine in the form of infusions from various herbs for a long time, strong synthetic diuretics were created relatively recently, but have already become widespread in the treatment of various diseases.

To date, the most powerful diuretics are drugs:

Lasix;
Spironolactone;

Lasix can be used both parenterally and orally. The undoubted advantage of this remedy is the rapid onset of a positive effect after its use. For example, if Lasix is \u200b\u200btaken orally, then the improvement will come within one hour, and if taken parenterally within a few minutes. At the same time, the duration of action of this diuretic when taken orally reaches 8 hours, and when administered intravenously - only three.

The diuretic effect of another strong diuretic drug - Spironolactone, used for edema of various origins, including edema of the heart, usually occurs on the 3rd day of medication. However, this time can be greatly shortened by prescribing Flurosemide or Hypothiazide with Spironolactone.

Manitol comes in the form of a dry powder and is considered one of the most powerful diuretics used for edema of the brain, lungs, heart and barbiturate poisoning.

Combined diuretics

Combined diuretic drugs include:

Vero-Triamtesid;
Diazid;
Diursan;
Diursan Mite;
Isobar;
Lasilactone;
Moduretic;
Thialoride;
Triam-Ko;
Triampur compositum;
Triamteside;
Triamtel;
Furesis compositum;
Furo-Aldopur;
EcoDurex;
Aldactone Saltucin;
Amyloside;
Amiloretic;
Amiloride + Hydrochlorothiazide;
Amitrid;
Amitrid Mite;
Apo-Triazide.

All of these combined diuretics have both hypotensive and diuretic effects. The advantage of combined drugs is the speed of onset of positive changes after taking them (from 1 to 3 hours) and the maintenance of the achieved effect for 7 to 9 hours.

Combined diuretics are mainly used for chronic venous insufficiency, toxicosis in the last weeks of pregnancy, liver cirrhosis, nephrotic syndrome, CHF, as well as for arterial hypertension.

Diuretic, non-excreting calcium

Diuretic tablets that do not excrete calcium are prescribed for those patients in whom high blood pressure is combined with osteoporosis. This is a necessary measure to prevent the progression of osteoporosis in patients, and as a result, the appearance of new fractures. Loop and potassium-sparing diuretics flush out calcium, while thiazide diuretics, on the contrary, reduce the excretion of calcium ions in the urine. That is why patients with osteoporosis are prescribed only thiazide-like and thiazide diuretics. However, calcium-sparing diuretics are necessary not only for people with osteoporosis, but also for other people at high risk of developing OPA injuries, for example, older people. Studies have shown that people who take thiazide-like diuretics to treat chronic hypertension are less likely to have fractures than those who are prescribed other types of diuretics.

But, despite the described advantages of diuretics that save calcium, they may be contraindicated in some groups of patients, since their intake is associated with an increase in the excretion of magnesium and potassium from the body, which means that patients with hyperuricemia, gout, hypokalemia, and others cannot be prescribed them.

Antihypertensive diuretics

A rather promising direction in the treatment of hypertension in patients is the intake of hyotensive diuretics. And the point is not only that almost all diuretics are able to lower blood pressure, in some cases not inferior in effectiveness to highly specialized drugs prescribed in the treatment of chronic forms of hypertension, but also that treatment with antihypertensive diuretics compared, for example, with b blockers , will cost the patient 9-15 times cheaper, which is important, given the fact that basically the group of people suffering from hypertension is a pensioner, whose financial wealth in most cases does not allow them to pay for expensive long-term treatment.

When taking diuretics, the hypotensive effect is achieved due to the fact that at the initial stage of treatment there is a decrease in the amount of circulating blood and cardiac output (the supply of sodium chlorides is depleted), and even after a few months the blood flow is normalized, the blood vessels by this time reduce peripheral resistance, thereby maintaining the antihypertensive effect achieved during treatment.

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