Fludapamide
Fludapamide Uses, Dosage, Side Effects, Food Interaction and all others data.
Fludapamide is a diuretic antihypertensive. It appears to cause vasodilation, probably by inhibiting the passage of calcium and other ions (sodium, potassium) across membranes. It has an extra-renal antihypertensive action resulting in a decrease in vascular hyperreactivity and a reduction in total peripheral and arteriolar resistance.
Classified as a sulfonamide diuretic, indapamide is an effective antihypertensive agent and by extension, has shown efficacy in the prevention of target organ damage.Administration of indapamide produces water and electrolyte loss, with higher doses associated with increased diuresis. Severe and clinically significant electrolyte disturbances may occur with indapamide use - for example, hypokalemia resulting from renal potassium loss may lead to QTc prolongation. Further electrolyte imbalances may occur due to renal excretion of sodium, chloride, and magnesium.
Other indapamide induced changes include increases in plasma renin and aldosterone, and reduced calcium excretion in the urine. In many studies investigating the effects of indapamide in both non-diabetic and diabetic hypertensive patients, glucose tolerance was not significantly altered. However, additional studies are necessary to assess the long term metabolic impacts of indapamide, since thiazide related impaired glucose tolerance can take several years to develop in non-diabetic patients.
| Trade Name | Fludapamide |
| Availability | Prescription only |
| Generic | Indapamide |
| Indapamide Other Names | Indapamid, Indapamida, Indapamide, Indapamidum, Metindamide |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, spironolactone, Lasix, chlorthalidone, torsemide |
| Type | |
| Formula | C16H16ClN3O3S |
| Weight | Average: 365.835 Monoisotopic: 365.06008979 |
| Protein binding | Approximately 76-79% of indapamide is protein bound. Indapamide binds primarily to alpha 1-acid glycoprotein and less significantly to serum albumin and lipoproteins. In the blood, indapamide is extensively and preferentially bound to erythrocytes. |
| Groups | Approved |
| Therapeutic Class | Thiazide diuretics & related drugs |
| Manufacturer | |
| Available Country | Switzerland |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fludapamide is used for the treatment of essential hypertension . It is effective in treating hypertension in patients with renal function impairment, although its diuretic effect is reduced. Fludapamide is also used for the treatment of salt and fluid retention associated with congestive heart failure.
Fludapamide is also used to associated treatment for these conditions: High Blood Pressure (Hypertension), Recurrent Nephrolithiasis, Sodium and fluid retention
How Fludapamide works
Fludapamide acts on the nephron, specifically at the proximal segment of the distal convoluted tubule where it inhibits the Na+/Cl- cotransporter, leading to reduced sodium reabsorption. As a result, sodium and water are retained in the lumen of the nephron for urinary excretion. The effects that follow include reduced plasma volume, reduced venous return, lower cardiac output, and ultimately decreased blood pressure.
Interestingly, it is likely that thiazide-like diuretics such as indapamide have additional blood pressure lowering mechanisms that are unrelated to diuresis. This is exemplified by the observation that the antihypertensive effects of thiazides are sustained 4-6 weeks after initiation of therapy, despite recovering plasma and extracellular fluid volumes.
Some studies have suggested that indapamide may decrease responsiveness to pressor agents while others have suggested it can decrease peripheral resistance. Although it is clear that diuresis contributes to the antihypertensive effects of indapamide, further studies are needed to investigate the medication’s ability to decrease peripheral vascular resistance and relax vascular smooth muscle.
Dosage
Fludapamide dosage
One tablet daily preferably in the morning. In more sever case Fludapamide can be combine with other categories of anti-hypertensive agent. The safety and effectiveness in pediatric patients have not been established
Side Effects
Side effects of Fludapamide include headache, anorexia, gastric irritation,nausea, vomiting, constipation, diarrhoea etc.
Toxicity
Fludapamide overdose symptoms may include but are not limited to nausea, vomiting, gastrointestinal disorders, electrolyte disturbances and weakness. Other signs of overdose include respiratory depression and severe hypotension. In cases of overdose, supportive care interventions may be necessary to manage symptoms. Emesis and gastric lavage may be recommended to empty the stomach; however, patients should be monitored closely for any electrolyte or fluid imbalances.
Precaution
Monitoring of potassium and uric acid serum levels is recommended, especially in subjects with a predisposition or sensitivity to hypokalemia and in patients with gout. Although no allergic manifestations have been reported during clinical trials, patients with a history of allergy to sulfonamide derivatives should be closely monitored.
Interaction
Other antihypertensive: Fludapamide may add to or potentiate the action of other antihypertensive drugs.
Norepinephrine: Fludapamide like thiazides, may decrease arterial responsiveness to norepinephrine.
Lithium: In general, diuretics should not be given concomitantly with lithium because they reduce its renal clearance and add a high risk of lithium toxicity.
Food Interaction
- Avoid alcohol. Alcohol may potentiate orthostatic hypotension.
- Increase consumption of potassium-rich foods. Fludapamide my cause potassium depletion leading to hypokalemia.
- Take with or without food.
Fludapamide Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Fludapamide Cholesterol interaction
[Moderate] Thiazide diuretics may increase serum triglyceride and cholesterol levels, primarily LDL and VLDL.
Whether these effects are dose-related and sustained during chronic therapy are unknown.
Patients with preexisting hyperlipidemia may require closer monitoring during thiazide therapy, and adjustments made accordingly in their lipid-lowering regimen
Fludapamide Drug Interaction
Moderate: metoprolol, metoprolol, cholecalciferol, cholecalciferolUnknown: aspirin, aspirin, rosuvastatin, rosuvastatin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, atorvastatin, atorvastatin, acetaminophen, acetaminophen, levothyroxine, levothyroxine, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid
Fludapamide Disease Interaction
Major: anuria, electrolyte losses, liver disease, lupus erythematosus, renal function disordersModerate: asthma, diabetes, hyperlipidemia, hyperparathyroidism, hyperuricemia, thyroid function tests
Volume of Distribution
Some sources report an apparent volume of distribution of 25 L for indapamide, while others report a value of approximately 60 L.
Elimination Route
The bioavailability of indapamide is virtually complete after an oral dose and is unaffected by food or antacids. Fludapamide is highly lipid-soluble due to its indoline moiety - a characteristic that likely explains why indapamide’s renal clearance makes up less than 10% of its total systemic clearance. The Tmax occurs approximately 2.3 hours after oral administration. The Cmax and AUC0-24 values are 263 ng/mL and 2.95 ug/hr/mL, respectively.
Half Life
Fludapamide is characterized by biphasic elimination. In healthy subjects, indapamide's elimination half-life can range from 13.9 to 18 hours. The long half-life is conducive to once-daily dosing.
Clearance
Fludapamide's renal and hepatic clearance values are reported to be 1.71 mL/min and 20-23.4 mL/min, respectively.
Elimination Route
An estimated 60-70% of indapamide is eliminated in the urine, while 16-23% is eliminated in the feces.
Pregnancy & Breastfeeding use
There are no adequate and well-controlled studies in pregnant women and so Fludapamide is not recommended. Mothers taking Fludapamide should not breast feed.
Contraindication
This drug must not be taken in the following conditions:
- Hypersensitivity to sulfonamides
- Severe renal failure
- Hepatic encephalopathy or severe hepatic failure
- Hypokalaemia
Acute Overdose
Symptoms: These could include: allergies, skin rashes, epigastric pain, nausea, photosensitivity, dizziness, weakness and paraesthesia.Treatment: Treatment is supportive and symptomatic, directed at correcting the electrolyte abnormalities.
Storage Condition
Store in a cool and dry place. Protect from light and moisture.
Innovators Monograph
You find simplified version here Fludapamide
Fludapamide contains Indapamide see full prescribing information from innovator Fludapamide Monograph, Fludapamide MSDS, Fludapamide FDA label
FAQ
What is Fludapamide used for?
Fludapamide is a thiazide-like diuretic drug generally used in the treatment of hypertension, as well as decompensated heart failure.
How safe is Fludapamide ?
Fludapamide is safe to take for a long time. You will have to see your doctor or nurse every so often to get your blood pressure checked and have blood and urine tests. This is to make sure the chemicals in your blood are balanced properly and your kidneys are working well.
How does Fludapamide work?
Fludapamide make your body get rid of extra fluid through your kidneys. This increases the amount of salts (such as sodium and potassium) and water you pee out. This means you have less fluid in your body and blood, which helps reduce blood pressure.
What are the common side effects of Fludapamide?
Common side effects of Fludapamide are include:
peeing more than normal - most people need to pee a couple of times within a few hours of taking indapamide, and you may also lose a bit of weight as your body loses water. mild skin rash. feeling or being sick. feeling dizzy or faint.
Is Fludapamide safe during pregnancy?
Fludapamide should not normally be used during pregnancy. Thiazide diuretics can reduce blood flow to the baby through the placenta and, if used in the third trimester, can cause problems such as jaundice, disturbances in the baby's electrolyte levels and problems with the growth of the baby.
Is Fludapamide safe during breastfeeding ?
Fludapamide is not recommended for women who wish to breastfeed because it passes into breast milk and could have side effects on a nursing infant. Fludapamide may also affect the production of breast milk.
Can I drink alcohol with Fludapamide?
If you have high blood pressure, it's best not to drink alcohol in large amounts while you're taking Fludapamide. It may raise your blood pressure, make you feel dizzy and cause dehydration.
When is the best time to take Fludapamide ?
It's usual to take it once a day, in the morning. Do not take Fludapamide too late in the day (after 4pm) or at night, otherwise you may have to wake up to go to the toilet.
How often can I take Fludapamide?
It's usual to take Fludapamide once a day, in the morning.
Can I take Fludapamide on empty stomach?
Fludapamide tablets can be taken either with or without food, on a full or empty stomach.
How long does Fludapamide take to work?
This means you have less fluid in your body and blood, which helps reduce blood pressure. Fludapamide will start to work within 2 hours of taking it. However, it may take up to a week to see an initial effect on your blood pressure and up to 12 weeks for the full effect to be seen.
How long does Fludapamide stay in my system?
Fludapamide keeps working to reduce your blood pressure for as long as you take it. It stays in the body for 3 to 4 days after you stop taking it.
Can I take Fludapamide for a long time?
Fludapamide oral tablet is used for long-term treatment of high blood pressure. It's used for short-term or long-term drug treatment of edema.
Is Fludapamide safe for kidneys?
Fludapamide is a safe and effective agent to use in lowering the blood pressure of hypertensive patients with normal renal function.
Can Fludapamide affect my kidneys?
Fludapamide can cause kidney problems. This Fludapamide should be used with caution if you have kidney disease. For people with liver disease: Fludapamide can cause fluid and electrolyte imbalances. These imbalances can worsen your liver disease.
Can Fludapamide affects my heart ?
Fludapamide may increase your risk of a heart attack or stroke.
What happen If I stop taking Fludapamide?
If you stop taking the drug or don't take it at all: Don't stop taking Fludapamide without talking to your doctor. Stopping this drug suddenly may cause your blood pressure to spike. This may increase your risk of a heart attack or stroke. If you have heart failure, you may experience fluid buildup.
Can Fludapamide affects my liver?
Fludapamide can cause fluid and electrolyte imbalances. These imbalances can worsen your liver disease. People with liver disease should use this drug with caution.
Can Fludapamide cause cancer?
Fludapamide increased risk of developing specific types of skin cancer.
Can Fludapamide cause eye problems?
This Fludapamide can cause certain eye problems. If left untreated, this can lead to lasting eyesight loss.
What are the common side effects of Fludapamide?
You should not use this Fludapamide if you are allergic to sulfa drugs or if you are unable to urinate.
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention. Overdose symptoms may include vomiting, weakness, dizziness, dry mouth, thirst, and muscle pain or weakness.
