Irbesartan
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2019-09-19
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Clinical Pharmacology
Antihypertensive agent, angiotensin II receptor antagonist. Blocks AT1-receptors, which leads to a decrease in the biological effects of angiotensin II, incl. vasoconstrictor action, stimulating effect on the release of aldosterone and activation of the sympathetic nervous system. As a result, blood pressure decreases.
Reduces the round robin, reduces afterload. Reduces blood pressure (with a minimum change in heart rate) and pressure in the pulmonary circulation, with a decrease in blood pressure is dose-dependent.
Does not affect the concentration of triglycerides, cholesterol, glucose, uric acid in the blood plasma or the excretion of uric acid in the urine.
Indications
Arterial hypertension.
Nephropathy in patients with hypertension and type 2 diabetes mellitus (as part of combination antihypertensive therapy).
Composition
One tablet contains:
active ingredient: irbesartan (form A) 150.00 mg
excipients: microcrystalline cellulose 33.50 mg, carmellose calcium 9.00 mg, povidone K-30 (collidon 30) 3.50 mg, silicon colloidal dioxide 1.00 mg, calcium stearate 3.00 mg;
shell: onadray white OY-S-38956 - 4.00 mg.
Opadry white OY-S-38956: hypromellose (HPMC 2910, E 464) 72.00%, talc (E553b) 14.00%, titanium dioxide (E171) 14.00%.
Irbesartan is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Irbesartan | pills | ||
| Irbesartan | Canonpharma | Russia | pills |
| Aprovel | Sanofi-aventis | France | pills |
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Dosage and Administration
The initial dose is 150 mg, if necessary, the dose is increased to 300 mg. In some cases (hypochlorite diet, treatment with some diuretics, prior to treatment with vomiting or diarrhea, hemodialysis) a lower starting dose is used.
Irbesartan is taken orally once a day, preferably at the same time of day.
Adverse reactions
CNS: headache, dizziness.
On the part of the digestive system: nausea, vomiting.
Others: indisposition, weakness.
Contraindications
Pregnancy, childhood, hypersensitivity to irbesartan.
Drug interactions
With simultaneous use with potassium-sparing diuretics, potassium preparations may increase the content of potassium in the blood plasma.
With simultaneous use with hydrochlorothiazide, the additive nature of the hypotensive effect is manifested.
With simultaneous use of lithium carbonate may increase the concentration of lithium in the blood plasma.
With simultaneous use of fluconazole can inhibit the metabolism of irbesartan.
Pregnancy and Lactation
Contraindicated for use in pregnancy.
If necessary, use during lactation should decide on the termination of breastfeeding.
Special instructions
It is used with caution in patients with impaired renal function, after severe vomiting or diarrhea, and also against the background of simultaneous therapy with potassium-saving diuretics or potassium preparations.
In experimental studies on laboratory animals, mutagenic, clastogenic and carcinogenic effects of irbesartan have not been established.
Influence on ability to drive motor transport and control mechanisms
There are no indications about the effect of irbesartan on the ability to drive vehicles and control mechanisms.
- Brand name: Irbesartan
- Active ingredient: Irbesartan
- Manufacturer: Canonpharma
Studies and clinical trials of Irbesartan (Click to expand)
- Synthesis of Amido-N-imidazolium Salts and their Applications as Ligands in Suzuki–Miyaura Reactions: Coupling of Hetero- aromatic Halides and the Synthesis of Milrinone and Irbesartan
- ChemInform Abstract: Radiosynthesis of (Tetrazoyl-11C)irbesartan, a Non-Peptidic Angiotensin II Antagonist.
- ChemInform Abstract: NMR Study of Desmotropy in Irbesartan (I), a Tetrazole-Containing Pharmaceutical Compound.
- ChemInform Abstract: Irbesartan Crystal Form B.
- Improved Synthesis of Irbesartan, an Antihypertensive Active Pharmaceutical Ingredient
- New Synthesis of Analogues of the Antihypertensive Active Pharmaceutical Ingredient Irbesartan.
- ChemInform Abstract: Improved Methods for the Synthesis of Irbesartan, an Antihypertensive Active Pharmaceutical Ingredient.
- ChemInform Abstract: Molecular Sieves-Supported Palladium(I) Catalyst: Suzuki Coupling of Chloroarenes and an Easy Access to Useful Intermediates for the Synthesis of Irbesartan, Losartan and Boscalid.
- ChemInform Abstract: Synthesis of Amido-N-imidazolium Salts and Their Applications as Ligands in Suzuki—Miyaura Reactions: Coupling of Heteroaromatic Halides and the Synthesis of Milrinone and Irbesartan.
- The synthesis of radiolabeled Irbesartan using N,N-dimethyl[14C]formamide as a source of carbon-14 isotope
- Irbesartan: FTIR and Raman spectra. Density functional study on vibrational and NMR spectra
- Hydrophilic interaction chromatography-tandem mass spectrometric analysis of irbesartan in human plasma: Application to pharmacokinetic study of irbesartan
- Inulin and poly(acrylic acid) grafted inulin for dissolution enhancement and preliminary controlled release of poorly water-soluble Irbesartan drug
- Electrochemical determination of antihypertensive drug irbesartan in pharmaceuticals
- Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: Derivatives of irbesartan key intermediate
- Comparison of irbesartan versus atorvastatin therapy on angiotensin II (ANG II)-induced venoconstriction and plasma levels of angiotensin-(1?7)[ANG-(1?7)] in healthy volunteers
- Individual and joint association of α-adrenergic receptor Arg347Cys polymorphism and plasma irbesartan concentration with blood pressure therapeutic response in Chinese hypertensive subjects
- Simultaneous determination of the acid/base antihypertensive drugs celiprolol, bisoprolol and irbesartan in human plasma by liquid chromatography
- Liquid chromatographic determination of irbesartan in human plasma
- Simultaneous quantification of losartan and active metabolite in human plasma by liquid chromatography–tandem mass spectrometry using irbesartan as internal standard
- Simultaneous determination of irbesartan and hydrochlorothiazide in human plasma using HPLC coupled with tandem mass spectrometry: Application to bioequivalence studies
- Extractive-spectrophotometric determination of disopyramide and irbesartan in their pharmaceutical formulation
- Spectroscopic and spectrofluorimetric studies on the interaction of irbesartan with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone and iodine
- Molecular sieves-supported palladium(II) catalyst: Suzuki coupling of chloroarenes and an easy access to useful intermediates for the synthesis of irbesartan, losartan and boscalid
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