Leodrine

Leodrine Uses, Dosage, Side Effects, Food Interaction and all others data.

A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822)

Leodrine is an oral thiazide used to treat hypertension and edema. High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. Like other thiazides, Leodrine promotes water loss from the body (diuretics). Thiazides inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Trade Name Leodrine
Availability Discontinued
Generic Hydroflumethiazide
Hydroflumethiazide Other Names Dihydroflumethazide, Hidroflumetiazid, Hidroflumetiazida, Hydrofluméthiazide, Hydroflumethiazide, Hydroflumethiazidum, Idroflumetiazide, Metforylthiadiazin
Related Drugs amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, spironolactone, Lasix, chlorthalidone, torsemide
Type
Formula C8H8F3N3O4S2
Weight Average: 331.292
Monoisotopic: 330.990831754
Protein binding

74%

Groups Approved, Investigational, Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Leodrine
Leodrine

Uses

Leodrine is a thiazide diuretic used to treat hypertension as well as edema due to congestive heart failure and liver cirrhosis.

Used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Also used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension.

Leodrine is also used to associated treatment for these conditions: Edema, High Blood Pressure (Hypertension)

How Leodrine works

Leodrine is a thiazide diuretic that inhibits water reabsorption in the nephron by inhibiting the sodium-chloride symporter (SLC12A3) in the distal convoluted tubule, which is responsible for 5% of total sodium reabsorption. Normally, the sodium-chloride symporter transports sodium and chloride from the lumen into the epithelial cell lining the distal convoluted tubule. The energy for this is provided by a sodium gradient established by sodium-potassium ATPases on the basolateral membrane. Once sodium has entered the cell, it is transported out into the basolateral interstitium via the sodium-potassium ATPase, causing an increase in the osmolarity of the interstitium, thereby establishing an osmotic gradient for water reabsorption. By blocking the sodium-chloride symporter, Leodrine effectively reduces the osmotic gradient and water reabsorption throughout the nephron.

Toxicity

Overdoses lead to diuresis, lethargy progressing to coma, with minimal cardiorespiratory depression and with or without significant serum electrolyte changes or dehydration.

Food Interaction

  • Increase consumption of potassium-rich foods. This medication may cause a loss of potassium.

Leodrine 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.

Leodrine 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

Elimination Route

Leodrine is incompletely but fairly rapidly absorbed from the gastrointestinal tract

Half Life

It appears to have a biphasic biological half-life with an estimated alpha-phase of about 2 hours and an estimated beta-phase of about 17 hours

Innovators Monograph

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https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5784
http://www.hmdb.ca/metabolites/HMDB0014912
http://www.genome.jp/dbget-bin/www_bget?drug:D00654
http://www.genome.jp/dbget-bin/www_bget?cpd:C07763
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3647
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505220
https://www.chemspider.com/Chemical-Structure.3521.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25897
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=5495
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=5784
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1763
https://zinc.docking.org/substances/ZINC000000897225
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000747
http://www.pharmgkb.org/drug/PA164752557
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/HFZ
http://www.rxlist.com/cgi/generic2/hydroflumethiazide.htm
https://en.wikipedia.org/wiki/Hydroflumethiazide
*** Taking medicines without doctor's advice can cause long-term problems.
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