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Furosemidum

Category: Blood Pressure

Description

Furosemide is used for treating fluid build-up and swelling caused by congestive heart failure, liver cirrhosis, or kidney disease.

Active Ingredient: furosemide

Furosemide (Furosemidum) as known as: Apo-furosemide, Diurin, Froop, Frusemide, Frusid, Frusol, Furorese, Furosemida, Furosemidum, Furoside, Fusid, Impugan, Myrosemide, Novosemide, Rusyde, Seguril, Tenkafruse, Uritol

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Furosemidum Indications

Furosemidum is used for treating fluid build-up and swelling caused by congestive heart failure, liver cirrhosis, or kidney disease. It is also used in combination with other medicines to treat fluid build-up in the lungs. Furosemidum is a loop diuretic. Loop diuretics make the kidneys eliminate larger amounts of electrolytes (especially sodium and potassium salts) and water than normal (diuretic effect). Loop diuretics are useful for treating many conditions in which salt and water retention (eg, edema, swelling) is a problem.

Furosemidum Instructions

Use Furosemidum as directed by your doctor.

  • Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
  • Your doctor may occasionally change your dose to make sure you get the best results from this medication.
  • Take Furosemidum by mouth with or without food.
  • To be sure Furosemidum is not causing harmful effects, your blood will need to be tested on a regular basis. Your kidney or liver function may also need to be tested. Do not miss any scheduled appointments.
  • If you are being treated for high blood pressure, keep using this medication even if you feel fine. High blood pressure often has no symptoms.
  • Furosemidum may increase the amount of urine or cause you to urinate more often when you first start taking it. To keep this from disturbing your sleep, try to take your dose before 6 pm.
  • If you miss a dose of Furosemidum, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Furosemidum.

Furosemidum Storage

Store Furosemidum at room temperature between 68 and 77 degrees F (20 and 25 degrees C) in a tightly closed container. Brief periods at temperatures of 59 to 86 degrees F (15 to 30 degrees C) are permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Furosemidum out of the reach of children and away from pets.

Do NOT use Furosemidum if:

  • you are allergic to any ingredient in Furosemidum
  • you are unable to urinate.

Contact your doctor or health care provider right away if any of these apply to you.

Some medical conditions may interact with Furosemidum. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

  • if you are pregnant, planning to become pregnant, or are breast-feeding
  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
  • if you have allergies to medicines, foods, or other substances
  • if you have fluid in your abdomen, hearing impairment, liver disease, diabetes mellitus, low urine output, high blood uric acid levels, a blood disorder, kidney disease, or lupus; you have had a heart attack; or you are dehydrated.

Some medicines may interact with Furosemidum. Tell your health care provider if you are taking any other medicines, especially any of the following:

  • Nonsteroidal anti-inflammatory drugs (NSAIDs) (eg, ibuprofen, indomethacin) because they may decrease Furosemidum's effectiveness
  • Aminoglycosides (eg, gentamicin), angiotensin-converting enzyme (ACE) inhibitors (eg, captopril), ethacrynic acid, or salicylates (eg, aspirin) because serious side effects to the kidneys (decreased ability to urinate) and ears (hearing loss) may occur
  • Chloral hydrate because side effects, such as excessive sweating, rapid heart beat, and changes in blood pressure, may occur
  • Digoxin or lithium because the risk of their side effects may be increased by Furosemidum.

This may not be a complete list of all interactions that may occur. Ask your health care provider if Furosemidum may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

Important Furosemidum Safety Information
  • Furosemidum may cause dizziness. These effects may be worse if you take it with alcohol or certain medicines. Use Furosemidum with caution. Do not drive or perform other possible unsafe tasks until you know how you react to it.
  • Furosemidum may cause dizziness, lightheadedness, or fainting; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.
  • Diabetes patients - Furosemidum may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.
  • Blood pressure should be monitored when taking Furosemidum.
  • Your doctor may also prescribe a potassium supplement while you use Furosemidum. Check with your doctor before you use a salt substitute or other product that also has potassium in it.
  • Furosemidum may cause you to become sunburned more easily. Avoid the sun, sunlamps, or tanning booths until you know how you react to Furosemidum. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.
  • Lab tests, including complete blood cell counts, may be performed while you use Furosemidum. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.
  • Caution is advised when using Furosemidum in children; they may be more sensitive to its effects.
  • Pregnancy and breast-feeding: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Furosemidum while you are pregnant. Furosemidum is found in breast milk. If you are or will be breast-feeding while you use Furosemidum, check with your doctor. Discuss any possible risks to your baby.

All medicines may cause side effects, but many people have no, or minor, side effects.

Check with your doctor if any of these most common side effects persist or become bothersome:

Abnormal skin sensations; bladder spasm; blurred vision; constipation; cramping; dizziness; dizziness when rising from a seated or lying position; feeling of whirling motion; fever; headache; lightheadedness; mouth and stomach irritation; muscle spasm; nausea; redness; restlessness; ringing in the ears; seeing a yellow color; sensitivity to sunlight; vein inflammation.

Seek medical attention right away if any of these severe side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); confusion; diarrhea; drowsiness; dry mouth; excessive urination; hearing loss; loss of appetite; muscle pain/cramps/weakness; rapid or irregular heartbeat; restlessness; sudden joint pain; unusual bleeding or bruising; unusual thirst; unusual tiredness or weakness; vomiting; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.

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Furosemidum of a tablet 0, 04 g

The latin name: Tabulettae Furosemidi 0, 04 g
Pharmacological groups: Diuretics
Nosological classification (MKB-10): E87. 5 Hyperpotassemia. G93. 6 wet brain. I10-I15 the illnesses or diseases, described the raised or increased blood pressure. I50 a heart failure. I50. 0 congestive or stagnant heart failure. I50. 1 left ventricular failure. J81 a pulmonary edema. K74 a fibrosis and a cirrhosis of a liver. K76. 6 Portal hypertensia. N04 a nephrotic syndrome. N17 an acute renal failure. N18 a chronic renal failure. N19 a renal failure not specified. N94. 3 syndrome of a premenstrual strain. O10-O16 edemas, a proteinuria and hypertensive frustration during pregnancy, sorts or labors and in the postnatal or puerperal period. O14. 9 preeclampsia [nephropathy] not specified. O15 an eclampsia. R18 an ascites. R39. 2 Extrarenal uremia. R60 the edema which has been not classified in other headings. T36-T50 a poisoning with medical products, medicines and biological substances. T42 The Poisoning anticonvulsant, sedative, somnolent and protivoparkinsonicheskimi agents. T42. 3 barbiturates
Pharmacological action


Operating or Working substance (MNN) * (Furosemide*)

Application: the Chronic heart failure, a fluid lungs, a hypertonic crisis, otechno-an ascitic syndrome at a cirrhosis of a liver, a renal failure, the nephrotic syndrome, the expressed hypernatremia, a hypercalcemia and gipermagniemija.
Contraindications: the Hypersensitivity (including to sulfonamidam), a hepatic coma, serious disturbances of electrolytic balance, a hypopotassemia, the expressed failure of function of a liver and kidneys, an oliguria during more 24 ch, anurija, a gout, a hyperuricemia, a diabetes mellitis or disturbance of tolerance to carbohydrates, dekompensirovannyj a mitral or aortal stenosis, rising of pressure in a bulbar vein over 10 mm hg, a hypertrophic cardiomyopathy with obstruction of a target tract of a left ventricle, a hypotension, a myocardial infarction, a systemic lupus erythematosus, a pancreatitis, a metabolic alkalosis.
Side effects: the Hypotension, including posturalnaja, a collapse, a thromboembolism, a thrombophlebitis (mainly at elderly), a hypopotassemia, a hypomagnesiemia, a hyponatremia, disturbance of tolerance to a glucose, a hyperuricemia, a gout, rising of a level of cholesterin LPNP (at greater or big doses), disturbance KSHCHS (gipohloremichesky an alkalosis), a hypercalcuria, disturbance of function of a liver, an intrahepatic cholestasia, a pancreatitis, a diarrhea, a constipation, a nausea, a vomiting, an anorexia, a lesion of an internal ear, a hearing loss, misting or caligation of vision, confusion of consciousness, nervousness, a headache, a giddiness, parestezija, delicacy, a spastic stricture of muscles, a spastic stricture of a bladder, a cold fit, a fever, a thrombocytopenia, an aplastic anemia, a leukopenia, a systemic vasculitis, an intersticial or interstitial nephritis, a hematuria, a necrotizing angiitis, an exfoliative dermatitis, mnogoformnaja an erythema, an impotency, a photosensitization, a urticaria, a dermal itch.
Interaction: Aminoglycosides, Acidum etacrynicum and Cisplatinum raise or increase ototoksichnost (especially at the broken or disturbed function of kidneys). Strengthens danger of a lesion of kidneys on a background of Amphotericinum B. At purpose or appointment of high doses of Salicylases the risk of development salitsilizma (a competitive renal egestion), intimate or cardiac glycosides - hypopotassemias and the arrhythmia connected with her, corticosteroids - electrolytic disbalansa increases or is enlarged. Reduces miorelaksirujushchuju activity of a tubocurarine, potentsiruet effect suktsinilholina. Reduces a renal clearance (and raises or increases probability of an intoxication) lithium. Under influence of Furosemidum the effect of inhibitors APF and antihypertensive agents, warfarin, diazoxide, Theophyllinum increases, is weakened or easied - antidiabetic preparations, Noradrenalinum. Sukralfat and Indomethacinum (due to inhibition of synthesis PG, disturbances of a level of a renin in plasma and egestions of Aldosteronum) reduce efficiency. probenetsid increases or enlarges concentration in Serum (blocks an egestion).
Overdosage: Signs: a hypotension, depression OTSP, a hypopotassemia and gipohloremichesky an alkalosis.
Treatment: maintenance of the vital functions.
Way of application and dose: Inside, in a daily dose of 20 60 mg; the augmentation of a dose at 20 40 mg through everyone 6 8 ch (greater or big doses divide or share;part into 2 3 receptions) is if necessary possible or probable. V/m or v/in - unitary, 20 40 mg (if necessary - rising of a dose on 20 mg everyone 2). Jet v/in introduction make slowly, during 1 2 minutes In high doses (80 240 mg and more) enter v/in dropwise or driply, with rate not above 4 mg/minutes the Maximal daily dose - 600 mg.
Safety measures: At presence of an ascites without peripheric edemas it is recommended to apply in the doses providing an additional diuresis in volume no more 700 900 ml/sut in order to prevent development of an oliguria, an azotemia and disturbances of an electrolytic exchange. With the purpose of exception of a phenomenon of "rebound" at treatment of an arterial hypertensia appoint or nominate not less than 2 times day. It is necessary to mean, that long reception can lead to occurrence of delicacy, weariness, depression of a BP and intimate or cardiac emission, and the excessive diuresis at a myocardial infarction with developments of stagnation in a small circle of a circulation can promote development of a cardiogenic shock. The time or temporary cancelling (for some days) before purpose or appointment of inhibitors APF is necessary. Within the first months of treatment the control of a BP, a level of electrolytes (especially a potassium), CO2, a creatinine, a urea nitrogen, a urinary acid, periodic definition of activity of hepatic enzymes, a level of a calcium and a magnesium, the maintenance or contents of a glucose in a blood and in urine (is recommended at a diabetes mellitis). At conservation of an oliguria during 24 ch Furosemidum should be cancelled. It is not necessary to apply during job to drivers of vehicles and people which trade is connected with the raised or increased concentration of attention.
Special indicatings: For delution it is necessary to use isotonic solutions of sodium of Sodium chloridum or a glucose with pH not below 5, 5.
Year of last updating: 1999


Trading names of preparations with operating or working substance * (Furosemide*)

Lasixum (Lasix) Furosemid-Milve (Furosemide-Milve) Furosemid-a Ferein (Furosemide-Ferein)
Furosemidum (Furosemide) Furosemid-N. (Furosemide-N. S.) Furosemidum a solution for injections of 1 % (Solutio Furosemidi pro injectionibus 1 %)
Furosemidum Nikomed (Furosemide Nycomed) Furosemid-ratiofarm (Furosemid-ratiopharm) Furosemidum of a tablet 0, 04 g (Tabulettae Furosemidi 0, 04 g)
Furosemid-Darnitsa (Furosemid-Darnitsa) Furosemid-Teva (Furosemide-Teva) Furosemidum of a tablet of 40 mg (Furosemide tablets 40 mg)

Furosemid Biotika Forte

4. CLINICAL PARTICULARS

4. 1 Therapeutic indications

Clinical conditions where is no standard dose of furosemide effective, such as acute and chronic edema, the heart insufficiency, nephrotic syndrome or liver cirrhosis, late gestosis. Acute left ventricular failure (pulmonary edema), cerebral edema, chronic renal insufficiency, hypercalcaemia and hyperkalemia, forced diuresis in some poisonings ( by salicylates, barbiturates, tricyclic antidepressants, halides).

4.2 Posology and method of administration

a) Dosage for children:

In children the intravenous dose of 1-2 mg / kg per day is given, if necessary, repeatedly. The maximum daily dose is 6 mg / kg of body weight.

b) Dosage for adults:

Dosage is individual and depends on the functional state of the kidney ,on the previous diuretic therapy and the desired diuretic effect. When higher doses needed, 250 mg of furosemide is administered intravenously by injection or infusion. Individually, the dose may be higher than 1000 mg of furosemide daily. During forced diuresis 500-1000 mg of furosemide in 400 ml of electrolyte solution is administered by intravenous infusion such with infusion rate, which depends on the achievement of diuretic effect. It is necessary to apply electrolyte solution to replace sodium, potassium, chloride and water losses. Infusion rate should not exceed 4 mg of furosemide per minute

Hypersensitivity to furosemide and to sulfonamides (the possibility of cross-sensitivity). Acute glomerulonephritis, renal insufficiency with hepatic coma accompanied with anuria. Hyponatremia and hypokalemia, metabolic alkalosis.

4.4 Special warnings and precautions for use

Intravenous form of administration is chosen if oral administration is not possible (coma, vomiting), if absorption from the gastrointestinal tract is insufficient, or if rapid onset of therapeutic response is necessary(forced diuresis in intoxications).

In patients with liver cirrhosis and ascites, furosemide may cause severe electrolyte imbalance (hypokalemia, hyponatremia, azotemia), and coma. Treatment should be initiated only when the current laboratory control and treatment of electrolyte imbalance are managed.

In diabetes mellitus is necessary to adjust glycemia with oral antidiabetic agents or insulin and in hyperuricemia simultaneous administration of allopurinol is needed. Caution is necessary in patients treated with cardiac glycosides

4.5 Interactions with other medicinal products and other forms of interaction

Furosemide-induced hypokalemia may enhance the arrhythmogenic effect cardiac glycosides. Furosemide enhances the hypotensive effect of antihypertensive therapy. Ototoxic effects of furosemide may be potentiated by the current application of aminoglycoside antibiotics with ototoxic effect (eg, gentamicin).

Nephrotoxic effect of some cephalosporin antibiotics (Cefalotin) might be potentiated by furosemide administration. Diuretics of different types can increase plasma levels of lithium to toxic levels. If a long-term treatment with lithium medication is necessary, the dose of lithium need to be reduced and plasma levels of lithium shall be regularly checked. Repeated administration of furosemide may increase plasma levels of barbiturates in patients with epilepsy.

Long-term antiepileptic medication reduces the diuretic effect. Furosemide may reduce plasma levels of theophylline.

Probenecid and indomethacin can reduce the diuretic and hypotensive effect of furosemide. Furosemide reduces the vasoconstrictive effects of norepinephrine. Co-administration of furosemide and sucralphate may reduce diuretic and hypotensive effect of furosemide. Both substances should be applied at two-hour interval. In patients who received chloral hydrate during the previous 24 hours, furosemide injection may cause tachycardia, elevate blood pressure, flushing heat and sweating. Furosemide may increase the toxicity of simultaneously administrated high doses of acetylsalicylic acid.

4.6 Pregnancy and lactation

Furosemide crosses the placenta and may increase the production of fetal urine. In pregnancy furosemide can be used only in case when the benefits of treatment outweigh the possible adverse effect in fetus (eg, pulmonary edema or heart failure). Furosemide passes at low concentrations into breast milk, therefore the patient treated with furosemide should not breastfeed. The diuretic effect of furosemide can be reduced in newborns, and thus the risk of ototoxicity might be increased. Furosemide passes at low concentrations into breast milk, therefore the patient treated with furosemide should not breastfeed. The diuretic effect of furosemide can be reduced in newborns, and thus the risk of ototoxicity might be increased.

4.7 Effects on ability to drive and use machines

Furosemide does not affect ability to drive or operate machinery.

4.8 Undesirable effects

Furosemide may cause hypokalemia in patients. Risk group are people with low potassium intake in the diet, or patients where the loss of potassium is not replaced by oral or parenteral form, or potassium-sparing diuretics are not used. Decreased level of potassium is manifested by various symptoms: usually it's fatigue, lethargy and muscle weakness. Severe hypokalemia is associated with cardiac arrhythmias of ventricular type (ventricular extrasystoles, ventricular tachycardia). Furosemide may cause acute hyponatremia due to excessive loss of sodium if inappropriately high doses are used. Chronic sodium depletion results from the prolonged use of potent diuretics. Both disorders are characterized by weakness, lethargy, somnolence, muscle spasms, postural hypotension, hyponatremia, hyperkalemia, elevated serum urea and elevated hematocrit. A serious complication is dilutional hyponatremia, which puts patients at risk.

Furosemide may cause a loss of magnesium (hypomagnesaemia) in patients. Decreased levels of magnesium in serum and tissues may result, as in the case of increased potassium loss, to heart arrhythmias. Furosemide increases Furosemidexcretion in the urine. In patients with latent or manifest symptoms of hypoparathyroidism tetany symptoms may arise. The long-term treatment may develop osteoporosis. Current kidney disease with reduced formation of 1.25 OH-cholecalciferol which results to decrease in Furosemidabsorption from the gut, might develop osteoporosis. In about 7% of patients anorexia, nausea, vomiting and epigastric pain are present. Constipation or diarrhea occurs in about 4% of patients. Furosemide in high doses increases levels of amylase, cases of acute pancreatitis and cholestatic jaundice. Leukopenia, agranulocytosis, thrombocytopenia, anemia, hemolytic anemia, or aplastic anemia have been reported occasionally.

Furosemide may like thiazide diuretics cause carbohydrate metabolism disorders, hyperglycemia, glycosuria and might aggravate diabetes mellitus. These disorders occur mainly in patients with latent diabetes, with hypokalemia, and in prolonged use of furosemide. The course is usually reversible.

Hyperosmolar coma in high doses has been rarely described. In this case a high hyperglycemia, hypokalemia, and dehydration are developed. Furosemide increased serum uric acid. This may cause hyperuricemia attack in predisposed patients. Like other diuretics, furosemide may alter lipid spectrum. Furosemide increases serum triglycerides and cholesterol. It increases concentration of low density lipoprotein, LDL-cholesterol and decreases HDL-cholesterol. Furosemide in high doses causes tinnitus and deafness in patients Particularly affected are middle and upper acoustic frequencies, the perception of deep tones is slightly damaged only. Damage is usually transitory, but it can also cause permanent hearing loss. Danger of permanent hearing damage is increased by concomitant use of other ototoxic drugs and in patients with renal insufficiency who are treated with high doses of furosemide. To prevent this undesirable effect it is necessary to follow the dosage and rate of administration. Infusion rate should not exceed 4 mg / min. Adverse reactions to skin are often characterized by rashes of various types, by pruritus, urticaria and by fotoalergic reactions. Most of them are of light nature, but rarely erythema multiforme, exfoliative dermatitis and purpura might occur. Rarely at high doses blurred vision or xanthopia (yellow vision) are found. In patients with micturition disorders, eg due to prostatic hypertrophy, can occur acute urinary retention. Increased urination may bother patients during night. Cases of interstitial nephritis have been reported. Changes in water and electrolyte balance, particularly hypokalaemia and hypomagnesaemia can lead to arrhythmias. Hypotensive effect and increased hematocrit, may be involved in the development of cerebral or peripheral ischemia in patients with the advanced atherosclerosis.

After rapid intravenous administration cardiac arrest has been reported.

Furosemide overdose may cause hypokalemia, hyponatremia, hypocalcaemia and hypomagnesemia (see section 4.8) in patients. Furosemide in high doses causes tinnitus and deafness (see section 4.8)in patients.

Treatment of overdosage consists of treatment of internal environment dysbalance. Furosemide can not be dialyzed.

5. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Sulphonamide diuretic

ATC code: C03CA01

Mechanism of effect

Furosemide belongs to the loop diuretics. It is also effective in significantly reduced kidney function. Furosemide inhibits the reabsorption of chloride and sodium in the medullary part of ascending limb of loop of Henle. Another site of action are distal and proximal tubule. It increases excretion of sodium, chloride and water, as well as potassium, Furosemidand magnesium. Furosemide increases the blood flow in the kidney and its redistribution in the kidney cortex. It reduces left ventricular filling pressure, which is achieved earlier than the diuretic effect. It acts hypotensively.

5.2 Pharmacokinetic properties

Furosemide in plasma is largely bound to plasma proteins, on average 97% and only 2-4% are unbound fraction of the drug. Volume of distribution is approximately 170-270 ml / kg. Diseases leading to decrease in plasma albumin levels (eg, nephrotic syndrome or liver cirrhosis), increase the amount of unbound fraction and increase the volume of distribution. Plasma clearance is approximately 200 ml / min. The half-life in healthy individuals is 45-60 minutes. The greater part of the dose is excreted unchanged into urine. Approximately 7-15% of the applied dose is transformed to glucuronide. Part of furosemide is excreted unchanged in the faeces (approximately 10%). Clearance of furosemide is influenced by different factors. Clearance is reduced in neonates and in elderly, likely due to reduced glomerular filtration.

Kidney disesase or heart disease, reduce the clearance. The half-life in renal, heart or liver impairment is extended. It can reach up to 20-24 hours. Pharmacological effect of furosemide correlates better with the concentration of the substance in the urine than in plasma. The effect depends on the amount of unbound fraction, which gets to the site of action in kidney tubules. After intravenous administration, the pharmacological effect is reached approximately in 5 minutes and lasts about 2 hours. Furosemide passes into the placenta and breast milk. Clearance of furosemide can not be affected by hemodialysis.

5.3 Preclinical safety data

Experiments on pregnant females of several animal species at doses exceeding the therapeutic dose have documented an increased incidence of fetal death and abortion. In mice and rabbits, the increased incidence of renal pelvic distension and ureteral distension has been observed.

6. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Sodium hydroxide, water for injection.

Sodium content in the product: 0.736 mg / ml, corresponding to 0.032 mmol / ml.

During infusion preparation, furosemide must not be mixed with substances which reduce the pH of the solution (eg, vitamin B, vitamin C, adrenaline, noradrenaline, local anesthetics, antihistamines, etc.). pH of the solution must not drop below 7, because the active ingredient may precipitate.

6.4 Special precautions for storage

Position statement: Lifestyle changes - O

Position statement: Lifestyle changes

  • Lifestyle measures should be instituted, whenever appropriate, in all patients, including those who require drug treatment. The purpose is to lower BP, to control other risk factors and to reduce the number of doses of antihypertensive drugs to be subsequently administered.

  • Lifestyle measures are also advisable in subjects with high normal BP and additional risk factors to reduce the risk of developing hypertension.

  • The lifestyle measures that are widely recognized to lower BP or cardiovascular risk, and that should be considered are:

    • smoking cessation

    • weight reduction (and weight stabilization)

    • reduction of excessive alcohol intake

    • physical exercise

    • reduction of salt intake

    • increase in fruit and vegetable intake and decrease in saturated and total fat intake

Position statement: Choice of antihypertensive drugs

  • The main benefits of antihypertensive therapy are due to lowering of BP per se.

  • Five major classes of antihypertensive agents - thiazide diuretics, calcium antagonists, ACE inhibitors, angiotensin receptor antagonists and -blockers – are suitable for the initiation and maintenance of antihypertensive treatment, alone or in combination. -blockers, especially in combination with a thiazide diuretic, should not be used in patients with the metabolic syndrome or at high risk of incident diabetes.

  • Because in many patients more than one drug is needed, emphasis on identification of the first class of drugs to be used is often futile. Nevertheless, there are many conditions for which there is evidence in favor of some drugs versus others either as initial treatment or as part of a combination.

  • The choice of a specific drug or a drug combination, and the avoidance of others, should take into account the following:

  1. The previous favorable or unfavorable experience of the individual patient with a given class of compounds.

  2. The effect of drugs on cardiovascular risk factors in relation to the cardiovascular risk profile of the individual patient.

  3. The presence of subclinical organ damage, clinical cardiovascular disease, renal disease or diabetes which may be more favorably treated by some drugs than others (Box 1 and Table 4).

  4. The presence of other disorders that may limit the use of particular classes of antihypertensive drugs (Table 5).

  5. The possibilities of interactions with drugs used for other conditions.

  6. The cost of drugs, either to the individual patient or to the health provider, but cost considerations should never predominate over efficacy, tolerability, and protection of the individual patient.

  • Continuing attention should be given to side effects of drugs, because they are the most important cause of non-compliance. Drugs are not equal in terms of adverse effects, particularly in individual patients.

  • The BP lowering effect should last 24 hours. This can be checked by office or home BP measurements at trough or by ambulatory BP monitoring.

  • Drugs which exert their antihypertensive effect over 24 hours with a once-a-day administration should be preferred because a simple treatment schedule favors compliance.


Box 1 Position statement: Antihypertensive treatment: Preferred drugs


Subclinical organ damage

LVH ACEI, CA, ARB

Microalbuminuria ACEI, ARB


Renal dysfunction ACEI, ARB

Clinical event any BP lowering agent

Previous stroke BB, ACEI, ARB

Previous Ml BB, CA

Angina pectoris diuretics, BB, ACEI, ARB,

Heart failure antialdosterone agents

- Recurrent ARB, ACEI

- Permanent BB, non-dihydropiridine CA

ESRD/proteinuria ACEI, ARB, loop diuretics

Peripheral artery CA

ISH (elderly) diuretics, CA

Metabolic syndrome ACEI, ARB, CA

Diabetes mellitus ACEI, ARB

Pregnancy CA, methyldopa, BB

Blacks diuretics, CA


Abbreviations: LVH: left ventricular hypertrophy; ISH: isolated systolic hypertension; ESRD: renal failure; ACEI: ACE inhibitors; ARB: angiotensin receptor antagonists; CA: calcium antagonists; BB: -blockers

Table 4. Conditions favoring use of some antihypertensive drugs versus others

Thiazide diuretics

  • Isolated systolic
    hypertension

  • Heart failure

  • Hypertension in blacks

ACE inhibitors

  • Heart failure

  • LV dysfunction

  • Post-myocardial infarction

  • Diabetic nephropathy

  • Non-diabetic nephropathy

  • LV hypertrophy

  • Carotid atherosclerosis

  • Proteinuria/
    Microalbuminuria

  • Atrial fibrillation

  • Metabolic syndrome

Beta-blockers

  • Angina pectoris

  • Post-myocardial infarction

  • Heart failure

  • Tachyarrhythmias

  • Glaucoma

  • Pregnancy

Angiotensin receptor antagonists

  • Heart failure

  • Post-myocardial infarction

  • Diabetic nephropathy

  • Proteinuria/Microalbuminuria

  • LV hypertrophy

  • Atrial fibrillation

  • Metabolic syndrome

  • ACEl-induced cough

Calcium antagonists (dihydropyridines )

  • Isolated systolic hypertension
    (elderly)

  • Angina pectoris

  • LV hypertrophy

  • Carotid/Coronary
    Atherosclerosis

  • Pregnancy

  • Hypertension in blacks

Diuretics (antialdosterone)

  • Heart failure

  • Post-myocardial infarction

Calcium antagonists (verapamil/diltiazem)

  • Angina pectoris

  • Carotid atherosclerosis

  • Supraventricular tachycardia

Loop diuretics

  • End stage renal disease

  • Heart failure


ACEI: ACE Inhibitors; LV: Left Ventricle.


Table 5. Compelling and possible contraindications to use of antihypertensive drugs


T hiazide diuretics Beta-blockers

Calcium antagonists (dihydropiridines) Calcium antagonists (verapamil, diltiazem) ACE inhibitprs

Angiotensin receptor antagonists Diuretics (antialdosterone)

A-V block (grade 2 or 3 )

Figure 3. Possible combinations between some classes of antihypertensive drugs.


The preferred combinations in the general hypertensive population are represented as thick lines. The frames indicate classes of agents proven to be beneficial in controlled intervention trials.

V. MATERIALS FOR METHODICAL MAINTENANCE OF THE LESSON


5.1. Control materials of a preparatory stage of the lesson


5.1.1. Theoretical questions to the lesson:


  1. The reasons and mechanisms of occurrence of artetial hypertension.

  2. Pathogenesis of various types of artetial hypertension.

  3. Methods of diagnostics, differential diagnostics and treatment of these diseases.

  4. Classification of artetial hypertension.

  5. Aetiologic factors causing development of artetial hypertension

  6. Data additional laboratory and instrumental methods of diagnostics.

  7. The diagnostic criteria's of the different forms of artetial hypertension.

  8. ECG-changes typical for artetial hypertension with different origin.

  9. Principles of artetial hypertension treatment.

  10. Indications for surgical treatment of patients with this pathology.


5.1.2. Practical tasks on the lesson:


    1. To be able to make inquiry of complaints and to take the anamnesis of patients with artetial hypertension.

    2. To be able to make the objective examination of patients with artetial hypertension (survey, palpation, percussion, auscultation).

    3. To be able to formulate the preliminary diagnosis.

    4. To be able to make the plan of inspection of the patient.

    5. To be able to realize the differential diagnosis of artetial hypertension.

    6. To be able to prove drug treatment of the patient.

5.2 Materials for the control of the final stage of the lesson:


1. A male patient complains of reccurent headaches, rises in BP lasting 2 years. Clinically: BP – 160/100 mmHg, Ps – 80 beats/min, tense. Auscultation: heart tones are weakened, a loud aortic second sound. Point out the most probable changes on the ECG.

A. Signs of hypertrophy of the left ventricle of the heart.

B. Signs of hypertrophy of the right ventricle of the heart.

C. Block of right bundle of His.

D. Signs of myocardial ischemia.

E. Signs of hypertrophy of the left atrium.


2. A female patient of 52 years complains of the anginal pain, which appears at hightened physical loading. Rises in BP for 15 years, last year BP was constantly hightened to the levels of 175/100 – 180/110 mmHg. What combination of drugs should be prescribed to the patient?

A. ACE inhibitor and beta-blocker.

B. ACE inhibitor and diuretic drug.

C. ACE inhibitor and calcium antagonist.

D. ACE inhibitor and imidazoline receptors agonist.

E. ACE inhibitor and  -adrenoreceptor agonist.


3. A female patient of 52 years of age, who suffers from hypertensive disease, developed after stress a sudden headache, palpitation, pain in heart area, a feeling of anxiety, fear. Clinically: the patient is excited, Ps – 120 beats/min, BP – 210/110 mmHg. Heart tones are rhythmic, a loud aortic second sound. The prescription of what drugs is the most favorable in the given case?

A. ACE inhibitors.

B. Thiaside diuretic.


4. A female patient, 52 years, complains of the headache, giddiness, a shroud of mist before her eyes, sickness, dull pain in the heart area. She is followed up by a pulmonologist about the bronchial asthma, often resorts to salbutamol. Clinically: BP – 180/110 mmHg. What group of drug cannot you apply while treating this patient?

A. Calcium antagonists.

B. Nitrates of prolonged action.

C. .ACE inhibitors.

D. Muscle spasmolytics.


5. A male patient of 22 years revealed at auscultation of the heart a systolic murmur in the second right intercostal space radiating into the interscapular area. BP in both arms 160/100 mmHg, BP in the legs 110/70 mm Hg. What is the most probable diagnosis?

A. Ventricular septal defect.

B. Aortic coarctation.

C. Fallot’s tetrad.

D. Pulmonary artery stenosis.

E. Renovascular hypertension.


1.  A 2.  A 3.  C 4.  A 5.  B

The report of clinical investigation of the patient


Full name of patient -_________________________________________

Age___________________ Profession ___________________________


1. 2007 Guidelines for the Management of Arterial Hypertension. The task force for the management of arterial Hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). / European Heart Journal Advance Access, June 11, 2007.

2. Fedosyeva V.M. Khrenov A.A. Therapy. The course of lectures. / Simferopol, 2003.


Topic 2. “ Clinical analysis of patients with Ischemic Heart Disease

(Coronary Heart Disease, Coronary Artery Disease)

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