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Furosemide, 40 mg tablets

Drug formTablets

ATC categoryCardiology, angiology

ATC subcategoryDiuretics

Brand nameFurosemide

Generic nameFurosemide

Composition

Each tablet contains:

active ingredient: furosemide 40mg;

excipients: microcristalline cellulose, lactose monohydrate , magnesuim stearate , sodium starch glycolate , povidone , maize starch.

Pharmacological group and ATC code
Diuretic, C03CA01.

Pharmacology

The all mechanism of action is not investigated, but it is known that furosemide inhibits reabsorbtion of sodium and water in the ascending limb of the loop of Henle by interfiering with the chloride binding site of the Na+, K+, 2CL- contransport system. Loop diuretics increase the rate of delivery of tubular fluid and electrolites to the distal sites of hydrogen and potassium ion secretion, while plasma volume contraction increases aldosterone production. The increased delivery and high aldosterone levels promote sodium reabsorbtion in the distal tubules, thus increasing the loss of potasium and hydrogen ions.Sodium and chloride decreases in the proximal and distal tubules. Еfficacy is largely due to the unique site of action, which include limb of the loop of Henle, proximal and distal tubules The action on the distal tubule is independent of any inhibitory effect on carbonic anhydrase and aldosterone.

Reabsorbtion of K ions is more less, than Na. Furosemid doesn’t suppress carboanhydrous ferment. It’s effective in both conditions of acidity and alkalinity equally. The diuretic effect of furosemide is more effective during two first days, It does not disappear at once and may lasts long time, but with diminishing aktion.

CLINICAL PHARMACOLOGY

Furosemid indicated in patients who has a moderate to severe level fluid retention, connected with hearth failure, liver disease or some kidney disorders. It is also lower the high blood pressure as it reduces the plasma and extracellular fluid and cardiac output. Cardiac output returns to normal with an accompanying decrease in peripheral resistance and decreased swelling volume and fluid retention in body. Decreased concentration of Na lessen the volume of blood plasma and circulatory blood. Furosemide may be effective in patients unresponsive to thiazide diuretics. In some patients, especially when there is diuretic resistance, may be needed combination treatment with diuretics that behave synergistically by acting at different sites (the principle of sequential nephron blockade).In high doses Furosemide is used for management of oliguria.

Pharmacokinetics

Furosemide is fairly rapidly absorbed from the gastrointestinal tract. glucuronide is the only or at least the major biotransformation product of furosemide in man. Furosemide is extensively bound to plasma proteins, mainly to albumin. Plasma concentrations ranging from 1 to 400 μg/mL are 91 to 99% bound in healthy individuals. The unbound fraction averages 2.3 to 4.1% at therapeutic concentrations.. In fasted normal men, the mean bioavailability of furosemide from tablets is 60% to 70%, respectively, of that from an intravenous injection of the drug. Although furosemide is more rapidly absorbed from the oral solution (50 minutes) than from the tablet (87 minutes), absorbtion is variable and erratic.Peak plasma levels and area under the plasma concentration-time curves do not differ significantly. The onset of diuresis following oral administration is within 1-2 hours. The peak effect occurs within the first or second hour. But the duration of diuretic effect is 6 to 8 hours Peak plasma concentrations increases with increasing dose but times-to-peak do not differ among doses. Significantly more furosemide is excreted in urine following the IV injection than after the tablet or oral solution. Renal excretion is 88%, biliary/fecal is 12%.Excretion via the bile is conciderably increased in severe renal impairment.and renal clearance is reduced, but overall plasma clearance may be unchanged because nonrenal clearance is increased. In patient with uremia, both renal and nonrenal clearance are reduced, and elimination is delayed. There are no significant differences between the two oral formulations in the amount of unchanged drug excreted in urine.

Uses
Edemas: Furosemide is indicated in adults and pediatric patients for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, , including the nephritic syndrome, oliguria. Furosemide is particularly useful when an agent with greater diuretic potential is desired.

Hypertension: Oral furosemide may be used in adults for the treatment of hypertension alone or in combination with other antihypertensive agents. Hypertensive patients who cannot be adequately controlled with thiazides will probably also not be adequately controlled with furosemide alone. Hypercalciemia, Hypernatriemia, Hypermagniemia.Artificial diuresis.

Dosage and administration

It is given by mouth usualy in the morning. In the treatment of edema initial dose is 40mg daily, adjusted as necessary. Mild cases -20.0mg. Some patients may require the 80,0 mg per day, given at one or two doses, or intermittently.

In chronic renal insufficiency initial dose is 50 mg every 4 or 6 hours. In exceptional cases up to 2g in 24hours may be given, according to the patient’s response with careful laboratory control.

In the management of oliguria treatment with infusion in severe cases may be maintained by oral doses up to 500mg for each 250 mg required by injection.

Pediatric

Caution must be exercised in using furosemide in infants, particularly for long periods. The immaturity of the renal system can result in unexpectedly high blood concentrations and extended half-lives. Fluid and electrolyte balances should therefore be monitored carefully. Neonates appear to be particularly susceptible to increases in urinary calcium concentrations after long-term use.

Overdosage
Symptoms

Overdosage connected with increasing diuresis, arterial hypotension with bradicardia, circulating plasma volume reduction, low level of electrolits in plasma, hypocholaemic alkalinity. Symptoms may include ringing in ears, loss of appetite, weakness, dizziness, confusion, feeling light-headace, or fainting.

Treatment

Seek emergency medical attention if you think you have used too much of this medicine No special measures have to be taken in case of accidental ingestion.

Adverse effects

CNS system:

Dry mouth, thirst, nausea, vomiting, feeling weak, restless, teengly feeling, blurred vision, тinnitus and permanent deafness.

Cardiovascular system

Most adverse effects of furosemide occur with high doses, and serious effects are uncommon. The most common adverse effect is fluid and electrolyte imbalance including hyponatraemia, hypokalaemia, and hypochloraemic alkalosis, particularly after large doses or prolonged use. Signs of electrolyte imbalance include headache, hypotension, muscle cramps, dry mouth, thirst, weakness, lethargy, drowsiness, restlessness, oliguria, cardiac arrhythmias, and gastrointestinal disturbances. Hypovolaemia and dehydration may occur, especially in the elderly. Because of their shorter duration of action, the risk of hypokalaemia may be less with loop diuretics such as furosemide than with thiazide diuretics.

Urological effects
– Glucosuria, glucosaemia,symptomatic hyperurikaemia, dark urine Unlike the thiazides, furosemide increases the urinary excretion of calcium and nephrocalcinosis has been reported in preterm infants., Adison deseas.

Gastrointestinal tract
– Diarea, constipation, pancreatitis, jaundice (yellowing of the skin or eyes)

Haemopoetic system
– Trombocytopenia, agranulocytosis

Allergic reactions
– Skeen rash, photosensitivity reactions, bullous pemphigoid,interstitial nephritis and vasculitis
– Sencitivity to any component of drug.

Precautions

Furosemide is sometimes used only once, so patient may not be on a dosing schedule. If he is using the medication regularly, he should take the missed dose as soon as he remember, if it is not a time to take the next dose. During treatment with Furosemid patient should avoid becaming dehydrating and must followed doctor’s instruction about the type and amount of liquids. During treatment with Furosemid there is a danger of more sensitivity to sunlight and sunburn may result. In case of ascyt without peripheric edemas it is recommended to take doses, which submit the formulation of 700-900ml urine in a day for avoidance of oliguria, azotemia and electrolits’s metabolism. For exclusion the “Ricochet’ syndrom drug must be used not less than twice daily. Furosemid can digress the attention concentration during the driving and control of machine

Periodic testing is needed in kidneys function disorders, diabetеs an gоut.

Contraindications
Although furosemide is used in high doses for oliguria due to chronic or acute renal impairment it should not be given in anuria or in renal failure caused by nephrotoxic or hepatotoxic drugs nor in renal failure associated with hepatic coma. Furosemide should not be given in pre-comatose states associated with hepatic cirrhosis. It should be used with care in patients with prostatic hyperplasia or impairment of micturition since it can precipitate acute urinary retention. Furosemid is contraindicated in .allergic reactions on sulfa drugs,:hives; difficulty of breathing;unability to urinate.

Dose adjustment or special tests to safely take furosemide is needed when patient has a kidney disease, lupus diabetes; gout.

Diuretics do not prevent development of toxemia of pregnancy.

High –dose furosemide therapy is contraindicated in renal failure caused by nephrotoxic or hepatotoxic drugs, and in renal failure associated with hepatic coma.

Drug interactions

Dose correction with hypoglycemic drugs is necessary.. The risk of development of glycosides toxic effects may be increased, when Furosemid used with glycosides. Тhereafter risk of hypokaliemia with concomitant usage of glucocorticoides. When used with aminoglycosides, cefalosporines and cysplatin the concentration of mentioned drugs in plasma may be increased and it may lead to development of ortotoxic and toxic effects in kidneys. Furosemid may strengthen lithium reabsorbtion in kidney tubules and cause toxic effects. NSAID can reduce diuretic effect of Furosemid. Taken with antihypertensive drugs Furosemid can potentiate their action.

If you take sucralfate (Carafate), take it at least 2 hours before or after you take furosemide. Before taking this medication, tell your doctor if you are using any of the following drugs:

  • lithium;
  • digoxin (Lanoxin);
  • steroids (prednisone and others);
  • ethacrynic acid (Edecrin);
  • diet pills or cold medicine;
  • other blood pressure medications;
  • amikacin (Amikin), gentamicin (Garamycin), netilmicin (Netromycin), streptomycin,
  • salicylates such as aspirin.


  • This list is not complete and there may be other drugs that can interact with furosemide. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

    Pregnancy and breast feeding

    FDA pregnancy category C. Furosemide may compromise placental perfusion by reducing maternal blood volume; it may also inhibit lactatio

    This medication may be harmful to an unborn baby. Doctor advice is needed if patient is pregnant or plans to become pregnant during treatment.

    Breast feesding
    – Furosemide can pass into breast milk and may harm a nursing baby.

    Pediatric Precautions
    – Usual dose by mouth 1-3mg per kg body- weight daily up to a maximum of 40mg daly.

    Presentation

    1 blister packet with 40 tablets in the cardboard box.

    Expiry date

    3 years. Do not use after the expiration date.

    Prescription status

    To be dispensed with prescription.

    Storage conditions

    Store at a room temperature (15-250C), in a dry place, out of the reach of children. Protect from light.