Product Information
Registration Status: ActiveOLMETEC PLUS 20 / 12.5MG is approved to be sold in Singapore with effective from 2007-05-22. It is marketed by PFIZER PTE LTD, with the registration number of SIN13283P.
This product contains Hydrochlorothiazide 12.50mg, and Olmesartan 20mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by DAIICHI SANKYO EUROPE GmbH in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It has been used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism. [PubChem]
Indication
For the treatment of high blood pressure and management of edema.
Mechanism of Action
Hydrochlorothiazide, a thiazide diuretic, 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, hydrochlorothiazide effectively reduces the osmotic gradient and water reabsorption throughout the nephron.
Pharmacokinetics
- Absorption
- 50-60%
- Distribution
- Metabolism
- Hydrochlorothiazide is not metabolized.
- Elimination
Toxicity
The most common signs and symptoms observed are those caused by electrolyte depletion (hypokalemia, hypochloremia, hyponatremia) and dehydration resulting from excessive diuresis. If digitalis has also been administered, hypokalemia may accentuate cardiac arrhythmias. The oral LD50 of hydrochlorothiazide is greater than 10 g/kg in the mouse and rat.
Active Ingredient/Synonyms
HCTZ | Hydrochlorothiazide |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
Olmesartan is an antihypertensive agent, which belongs to the class of medications called angiotensin II receptor blockers. It is indicated for the treatment of high blood pressure and is marketed under the name Olmetec®. The FDA label includes a black-box warning of injury and death to the fetus, so women of child-bearing age need to be warned and take the necessary precautions. Olmesartan is also contraindicated in diabetes mellitus patients taking aliskiren.
Indication
For the treatment of hypertension.
Mechanism of Action
Olmesartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Olmesartan is selective for AT1 and has a 12,500 times greater affinity for AT1 than the AT2 receptor. Also unlike the well-known ARB losartan, olmesartan does not have an active metabolite or possess uricosuric effects.
Pharmacokinetics
- Absorption
- Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
- Distribution
- The volume of distribution is 17 L and olmesartan poorly crosses the blood brain barrier.
- Metabolism
- Olmesartan is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. There is virtually no further metabolism of olmesartan.
- Elimination
Clearance
* Total plasma cl=1.3 L/h * Renal cl=0.6 L/h
Toxicity
The main symptoms of overdose include low blood pressure and fast heartbeat.
Active Ingredient/Synonyms
4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid | 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid | Olmesartan |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.