Actions of Olmefast H in details
Pharmacology: Pharmacodynamics: Losartan Potassium: It is an angiotensin II receptor blocker with antihypertensive activity due mainly to selective blockage of AT1 receptors and the consequent reduced pressure effect of angiotensin II.
Olmefast H: It is a diuretic antihypertensive.
Pharmacokinetics: Losartan Potassium: It is readily absorbed from the gastrointestinal tract (GIT) following oral administration, with an oral bioavailability of about 33%. It undergoes first-pass metabolism to form an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than losartan and some inactive metabolites. Metabolism is primarily by cytochrome P-450 isoenzyme CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and E-3174 occur about 1 hr and 3-4 hrs, respectively, after an oral dose. Both losartan and E-3174 are >98% bound to plasma proteins. Losartan is excreted in the urine and in the feces via bile, as unchanged drug and metabolites. Following oral dosing, about 35% of the dose is excreted in the urine and about 60% in the feces. The terminal elimination t½ of losartan and E-3174 are about 1.5-2.5 hrs and 3-9 hrs, respectively.
Olmefast H: It is fairly rapidly absorbed from the GIT. It is reported to have a bioavailability of about 65-70%. It has been estimated to have a plasma t½ of between about 5-15 hrs and appears to be preferentially bound to red blood cells. It is excreted mainly unchanged in the urine. Olmefast H crosses the placental barrier and is distributed into breast milk.
How should I take Olmefast H?
Take Olmefast H exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.
Olmefast H is usually taken once per day. Follow your doctor's dosing instructions very carefully.
Call your doctor if you have ongoing vomiting or diarrhea, or if you are sweating more than usual. You can easily become dehydrated while taking this medicine, which can lead to severely low blood pressure or a serious electrolyte imbalance.
While using Olmefast H, you may need frequent medical tests and blood pressure be checks. Your blood and urine may both be tested if you have been vomiting or are dehydrated.
If you need surgery, tell the surgeon ahead of time that you are using Olmefast H. You may need to stop using the medicine for a short time.
Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medicine for the rest of your life.
Store Olmefast H t room temperature away from moisture, heat, and freezing. Keep the bottle tightly closed when not in use.
Olmefast H administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results.
Your blood pressure will need to be checked often. Visit your doctor regularly.
Conditions that may cause very low blood pressure include: vomiting, diarrhea, heavy sweating, heart disease, dialysis, a low salt diet, or taking diuretics (water pills). Follow your doctor's instructions about the type and amount of liquids you should drink while taking Olmefast H. Tell your doctor if you have a prolonged illness that causes diarrhea or vomiting.
Your blood and urine may both be tested if you have been vomiting or are dehydrated.
If you need medical tests, tell the doctor ahead of time that you are taking medication that contains Hydrochlorothiazide. You may need to stop using the medicine for a short time.
If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
Store at room temperature away from moisture, heat, and light.
Olmefast H pharmacology
Olmefast H blocks the reabsorption of sodium and chloride ions, and it thereby increases the quantity of sodium traversing the distal tubule and the volume of water excreted. A portion of the additional sodium presented to the distal tubule is exchanged there for potassium and hydrogen ions. With continued use of Olmefast H and depletion of sodium, compensatory mechanisms tend to increase this exchange and may produce excessive loss of potassium, hydrogen and chloride ions. Olmefast H also decreases the excretion of calcium and uric acid, may increase the excretion of iodide and may reduce glomerular filtration rate. Metabolic toxicities associated with excessive electrolyte changes caused by Olmefast H have been shown to be dose-related.
Pharmacokinetics and Metabolism
Olmefast H is well absorbed (65% to 75%) following oral administration. Absorption of Olmefast H is reduced in patients with congestive heart failure.
Peak plasma concentrations are observed within 1 to 5 hours of dosing, and range from 70 to 490 ng/mL following oral doses of 12.5 to 100 mg. Plasma concentrations are linearly related to the administered dose. Concentrations of Olmefast H are 1.6 to 1.8 times higher in whole blood than in plasma. Binding to serum proteins has been reported to be approximately 40% to 68%. The plasma elimination half-life has been reported to be 6 to 15 hours. Olmefast H is eliminated primarily by renal pathways. Following oral doses of 12.5 to 100 mg, 55% to 77% of the administered dose appears in urine and greater than 95% of the absorbed dose is excreted in urine as unchanged drug. In patients with renal disease, plasma concentrations of Olmefast H are increased and the elimination half-life is prolonged.
When Olmefast H (Olmefast H capsule) is administered with food, its bioavailability is reduced by 10%, the maximum plasma concentration is reduced by 20%, and the time to maximum concentration increases from 1.6 to 2.9 hours.
Pharmacodynamics
Acute antihypertensive effects of thiazides are thought to result from a reduction in blood volume and cardiac output, secondary to a natriuretic effect, although a direct vasodilatory mechanism has also been proposed. With chronic administration, plasma volume returns toward normal, but peripheral vascular resistance is decreased. The exact mechanism of the antihypertensive effect of Olmefast H is not known.
Thiazides do not affect normal blood pressure. Onset of action occurs within 2 hours of dosing, peak effect is observed at about 4 hours, and activity persists for up to 24 hours.
Clinical Studies
In an 87 patient 4-week double-blind, placebo controlled, parallel group trial, patients who received Olmefast H (Olmefast H capsule) had reductions in seated systolic and diastolic blood pressure that were significantly greater than those seen in patients who received placebo. In published placebo-controlled trials comparing 12.5 mg of Olmefast H to 25 mg, the 12.5 mg dose preserved most of the placebo-corrected blood pressure reduction seen with 25 mg.
References
- DailyMed. "AMLODIPINE BESYLATE; HYDROCHLOROTHIAZIDE; OLMESARTAN MEDOXOMIL: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Hydrochlorothiazide: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Hydrochlorothiazide: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
