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1.
Article in English | MEDLINE | ID: mdl-32164965

ABSTRACT

Azilsartan is used for treatment of the high blood pressure (hypertension). Reducing high blood pressure enables avoid strokes, heart attacks and problems of kidneys. Azilsartan comes under the name angiotensin receptor blocker (ARBs) as a class of drugs. It acts by relaxing blood vessels to make it easier for blood to flow. Azilsartan Medoxomil's a comprehensive profile containing the description, formulae, Elemental Analysis, Uses and application. Furthermore, methods and schemes are outlined for the preparation of the drug substance. The physical properties of the medication include constant of ionization, solubility, X-ray powder diffraction pattern, differential scanning calorimetry, thermal conduct and spectroscopic studies are investigated. The methods employed in bulk medicines and/or in pharmaceutical formulations to analyze the drug substance include spectrophotometric, electrochemical and the chromatographic methods. Other studies on this drug substance include drug stability, Pharmaceutical Applications, Mechanism of Action, Pharmacodynamics, and a Dosing Information are reviewed. At the end of this profile, there are more than sixty references were listed.


Subject(s)
Angiotensin Receptor Antagonists/pharmacology , Antihypertensive Agents/pharmacology , Benzimidazoles/pharmacology , Oxadiazoles/pharmacology , Blood Pressure , Drug Stability , Humans , Hypertension/drug therapy
2.
Article in English | MEDLINE | ID: mdl-32164970

ABSTRACT

Emtricitabine (Emtriva, FTC) is an antiviral medicine which decreases the body's amount of HIV. Emtricitabine on of Anti-HIV drugs slow down or protect the immune system against damage and reduce the risk of diseases related to developing of AIDS. Emtricitabine use also for treatment of hepatitis B virus. Emtricitabine is a drug class known as nucleoside reversing transcriptase inhibitors (NRTIs). In view of Emtricitabine's clinical significance, a thorough review of the physical and pharmaceutical characteristics and details of the multiple analytical techniques used to test the drug in pharmaceutical and biological systems was conducted. The methods investigated include identification test, Spectroscopy, chromatography, electrochemicals, and Thermal. Beside the analytical profile, the degradation and stability of Emtricitabine, its pharmacology and pharmacokinetics, Pharmaceutical Applications, Mechanism of Action, dosage forms and dose, ADME profile, and interactions have been debated.


Subject(s)
Anti-HIV Agents/pharmacology , Emtricitabine/pharmacology , Reverse Transcriptase Inhibitors/pharmacology , HIV Infections/drug therapy , Hepatitis B/drug therapy , Humans
3.
Article in English | MEDLINE | ID: mdl-28431778

ABSTRACT

Olmesartan is an angiotensin receptor blockers with actions similar to those of losartan; it is used for the treatment of high blood pressure by relaxing blood vessels for this reason blood can flow more easily. It could be used alone or in combination with other antihypertensive drugs. This chapter gives a comprehensive profile of olmesartan, containing detailed nomenclature, formulae, elemental analysis, and appearance of the drug. In addition this chapter also describes several methods of synthesis and usage of the olmesartan. The profile covers the physicochemical properties including pKa value, solubility, X-ray powder diffraction, melting point, and procedures of analysis (compendial, spectroscopic, electrochemical, and chromatographic techniques of analysis). Comprehensive pharmacology is also presented (pharmacological actions, therapeutic uses and dosing, interactions, and adverse effects and precautions). Eighty references were given as a proof of the above-mentioned studies.


Subject(s)
Angiotensin II Type 1 Receptor Blockers , Antihypertensive Agents , Imidazoles , Tetrazoles , Humans , Hypertension/drug therapy
4.
Article in English | MEDLINE | ID: mdl-28431779

ABSTRACT

Propranolol is a noncardioselective ß-blocker. It is reported to have membrane-stabilizing properties, but it does not own intrinsic sympathomimetic activity. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. It is also used to control symptoms of sympathetic overactivity in the management of hyperthyroidism, anxiety disorders, and tremor. Other indications cover the prophylaxis of migraine and of upper gastrointestinal bleeding in patients with portal hypertension. This study provides a detailed, comprehensive profile of propranolol, including formulas, elemental analysis, and the appearance of the drug. In addition, the synthesis of the drug is described. The chapter covers the physicochemical properties, including X-ray powder diffraction, pK, solubility, melting point, and procedures of analysis (spectroscopic, electrochemical, and chromatographic). In-depth pharmacology is also presented (pharmacological actions, therapeutic dosing, uses, Interactions, and adverse effects and precautions). More than 60 references are given as a proof of the abovementioned studies.


Subject(s)
Adrenergic beta-Antagonists , Propranolol , Adrenergic beta-Antagonists/chemistry , Adrenergic beta-Antagonists/pharmacokinetics , Adrenergic beta-Antagonists/pharmacology , Adrenergic beta-Antagonists/therapeutic use , Drug Stability , Humans , Hypertension/drug therapy , Molecular Structure , Propranolol/chemistry , Propranolol/pharmacokinetics , Propranolol/pharmacology , Propranolol/therapeutic use
5.
Article in English | MEDLINE | ID: mdl-26051689

ABSTRACT

Telmisartan is an angiotensin-II receptor antagonist (ARB) used in the treatment of hypertension. Generally, angiotensin-II receptor blockers such as telmisartan bind to the angiotensin-II type 1 receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. The present study gives a comprehensive profile of telmisartan, including detailed nomenclature, formulae, elemental analysis, and appearance of the drug are mentioned. The uses and applications and the several methods described for its preparation of the drug are outlined. The profile contains the physicochemical properties including: pKa value, solubility, X-ray powder diffraction, melting point, and methods of analysis (including compendial, electrochemical, spectroscopic, and chromatographic methods of analysis). Developed validated stability-indicating (HPLC and biodiffusion assay methods under accelerated acidic, alkaline, and oxidative conditions, in addition to effect of different types of light, temperature, and pH. Detailed Pharmacology also presented (Pharmacological actions, Therapeutic uses and Dosing, Interactions, and adverse effects and precautions). More than 80 references were given as a proof of the above-mentioned studies.


Subject(s)
Angiotensin II Type 1 Receptor Blockers/chemistry , Antihypertensive Agents/chemistry , Benzimidazoles/chemistry , Benzoates/chemistry , Angiotensin II Type 1 Receptor Blockers/administration & dosage , Angiotensin II Type 1 Receptor Blockers/adverse effects , Angiotensin II Type 1 Receptor Blockers/pharmacokinetics , Animals , Antihypertensive Agents/administration & dosage , Antihypertensive Agents/adverse effects , Antihypertensive Agents/pharmacokinetics , Benzimidazoles/administration & dosage , Benzimidazoles/adverse effects , Benzimidazoles/pharmacokinetics , Benzoates/administration & dosage , Benzoates/adverse effects , Benzoates/pharmacokinetics , Blood Pressure/drug effects , Chemistry, Pharmaceutical , Drug Interactions , Drug Stability , Humans , Hypertension/drug therapy , Hypertension/physiopathology , Molecular Structure , Technology, Pharmaceutical/methods , Telmisartan
6.
Article in English | MEDLINE | ID: mdl-24794904

ABSTRACT

Azithromycin is an azalide, a subclass of macrolide antibiotics. It is derived from erythromycin, with a methyl-substituted nitrogen atom incorporated into the lactone ring, thus making the lactone ring 15-membered. It prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome and thus inhibits translation of mRNA. Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, bronchitis, and sinusitis. In recent years, it has been used primarily to prevent bacterial infections in infants and those with weaker immune systems. It is also effective against certain sexually transmitted infections, such as nongonococcal urethritis, chlamydia, and cervicitis. Recent studies have indicated it also to be effective against late-onset asthma, but these findings are controversial and not widely accepted. The present study gives a comprehensive profile of azithromycin, including detailed physico-chemical properties, nomenclature, formulae, methods of preparation, and methods of analysis (including compendial, electrochemical, spectroscopic, and chromatographic methods of analysis). Developed validated stability-indicating (HPLC and biodiffusion assay methods under accelerated acidic, alkaline, and oxidative conditions, in addition to effect of different types of light, temperature, and pH. Detailed clinical applications also presented (mechanism of action, ADME profile, clinical uses and doses, side effects, and drug interactions). Each of the above stages includes appropriate figures and tables. More than 80 references were given as a proof of the above-mentioned studies.


Subject(s)
Anti-Bacterial Agents/analysis , Anti-Bacterial Agents/chemistry , Azithromycin/analysis , Azithromycin/chemistry , Animals , Anti-Bacterial Agents/adverse effects , Anti-Bacterial Agents/therapeutic use , Azithromycin/adverse effects , Azithromycin/therapeutic use , Chemistry, Pharmaceutical , Drug Interactions , Drug Resistance, Bacterial , Drug Stability , Humans , Molecular Structure
7.
Article in English | MEDLINE | ID: mdl-24794909

ABSTRACT

Imatinib (INN), marketed by Novartis as Gleevec (United States) or Glivec (Europe/Australia/Latin America), received Food & Drug Administration (FDA) approval in May 2001 and is a tyrosine kinase inhibitor used in the treatment of multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia. Like all tyrosine kinase inhibitors, imatinib works by preventing a tyrosine kinase enzyme. Because the BCR-Abl tyrosine kinase enzyme exists only in cancer cells and not in healthy cells, imatinib works as a form of targeted therapy-only cancer cells are killed through the drug's action. In this regard, imatinib was one of the first cancer therapies to show the potential for such targeted action and is often cited as a paradigm for research in cancer therapeutics. This study presents a comprehensive profile of imatinib, including detailed nomenclature, formulae, physico-chemical properties, methods of preparation, and methods of analysis (including compendial, electrochemical, spectroscopic, and chromatographic methods of analysis). Spectroscopic and spectrometric analyses include UV/vis spectroscopy, vibrational spectroscopy, nuclear magnetic resonance spectrometry ((1)H and (13)C NMR), and mass spectrometry. Chromatographic methods of analyses include electrophoresis, thin layer chromatography, and high-performance liquid chromatography. Preliminary stability investigations for imatinib have established the main degradation pathways, for example, oxidation to N-oxide under oxidative stress conditions. Stability was also carried out for the formulation by exposing to different temperatures 0°C, ambient temperature, and 40°C. No remarkable change was found in the drug content of formulation. This indicates that the drug was stable at the above optimized formulation. Stability studies under acidic and alkaline conditions have established the following main degradation products: α-(4-Methyl-1-piperazinyl)-3'-{[4-(3-pyridyl)-2-pyrimidinyl] amino}-p-tolu-p-toluid-ide methanesulfonate and 4-(4-methylpiperazin-1-ylmethyl)-benzoic acid. The main degradation products under oxidation conditions, that is, 4-[(4-methyl-4-oxido-piperazin-1-yl)-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-enzamide, 4-[(4-methyl-1-oxido-piperazin-1-yl)-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide, and 4-[(4-methyl-1,4-dioxido-piperazin-1-yl)-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-enzamide. Clinical application studies for pharmacodynamics, pharmacokinetics, mechanism of action, and clinical uses of the drug were also presented. Each of the above stages includes appropriate figures and tables. More than 50 references were given as proof of the above-mentioned studies.


Subject(s)
Antineoplastic Agents/analysis , Antineoplastic Agents/chemistry , Benzamides/analysis , Benzamides/chemistry , Piperazines/analysis , Piperazines/chemistry , Pyrimidines/analysis , Pyrimidines/chemistry , Animals , Antineoplastic Agents/pharmacokinetics , Antineoplastic Agents/therapeutic use , Benzamides/pharmacokinetics , Benzamides/therapeutic use , Chemistry, Pharmaceutical , Drug Resistance, Neoplasm , Drug Stability , Humans , Imatinib Mesylate , Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy , Molecular Structure , Piperazines/pharmacokinetics , Piperazines/therapeutic use , Pyrimidines/pharmacokinetics , Pyrimidines/therapeutic use
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