Synonyms: Omeprazole, INN, Antra, Losec, Audazol, Omapren, Belmazol, Ceprandal, Emeproton, Gastrimut, Indurgan



6-methoxy-2-[(4-methoxy-3, 5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole

Functional Activity:

Omeprazole is a proton pump (H+,K+-ATPase, IC50=5.8 μM) inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux (LPR) and Zollinger-Ellison syndrome. Omeprazole is one of the most widely prescribed drugs internationally and is available over the counter in some countries.

Omeprazole is a competitive inhibitor of the enzymes CYP2C19 and CYP2C9, and CYP3A ((Ki values are 3.1, 40.1 and 84.4 μM respectively) and may therefore interact with drugs that depend on them for metabolism, such as diazepam, escitalopram, and warfarin; the concentrations of these drugs may increase if they are used concomitantly with omeprazole.

Omeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole in penicillin-hypersensitive patients) in the 7 to 14 day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is the causative factor in the majority of peptic and duodenal ulcers.

Technical Data:

M.Wt: 345.42

Formula: C17H19 N3O3S

Solubility: Soluble in DMSO at 19mg/mL and soluble in ethanol at 4.5mg/mL, and soluble in water at 0.5mg/mL

Purity: >98%

Storage: Dessicate at 4°C

CAS No.: 73590-58-6

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References for Omeprazole:

1. Freeman, K. L. and Trezevant, M. S. Interaction between liquid protein solution and omeprazole suspension. Am J Health Syst Pharm, 66: 1901-1902, 2009.

2. Fang, H. M., Xu, J. M., Mei, Q., Diao, L., Chen, M. L., Jin, J., and Xu, X. H. Involvement of cytochrome P450 3A4 and P-glycoprotein in first-pass intestinal extraction of omeprazole in rabbits. Acta Pharmacol Sin, 30: 1566-1572, 2009.

3. Haffey, M. B., Buckwalter, M., Zhang, P., Homolka, R., Martin, P., Lasseter, K. C., and Ermer, J. C. Effects of omeprazole on the pharmacokinetic profiles of lisdexamfetamine dimesylate and extended-release mixed amphetamine salts in adults. Postgrad Med, 121: 11-19, 2009.

4. Panti, A., Bennett, R. C., Corletto, F., Brearley, J., Jeffery, N., and Mellanby, R. J. The effect of omeprazole on oesophageal pH in dogs during anaesthesia. J Small Anim Pract, 50: 540-544, 2009.

5. Cuisset, T., Frere, C., Quilici, J., Poyet, R., Gaborit, B., Bali, L., Brissy, O., Morange, P. E., Alessi, M. C., and Bonnet, J. L. Comparison of omeprazole and pantoprazole influence on a high 150-mg clopidogrel maintenance dose the PACA (Proton Pump Inhibitors And Clopidogrel Association) prospective randomized study. J Am Coll Cardiol, 54: 1149-1153, 2009.

6. Van Der Straeten, F., Al-Afandi, A., De Paepe, K., Bovy, J., and Plaizier-Vercammen, J. [Pharmacy compounding of an omeprazole suspension]. J Pharm Belg: 54-63, 2009.

Certificate of Analysis/MSDS is available upon request with lot number

References for Diltiazem:

1. Sultana, Y., Mall, S., Maurya, D. P., Kumar, D., and Das, M. Preparation and in vitro characterization of diltiazem hydrochloride loaded alginate microspheres. Pharm Dev Technol, 14: 321-331, 2009.

2. Demir, M., Ozaydin, M., Varol, E., Dogan, A., and Altinbas, A. Effects of metoprolol and diltiazem on plasma homocysteine levels in patients with isolated coronary artery ectasia. Anadolu Kardiyol Derg, 9: 69-70, 2009.

3. Ezeugo, U. and Glasser, S. P. Clinical benefits versus shortcomings of diltiazem once-daily in the chronotherapy of cardiovascular diseases. Expert Opin Pharmacother, 10: 485-491, 2009.

4. Rigat, B. and Mahuran, D. Diltiazem, a L-type Ca(2+) channel blocker, also acts as a pharmacological chaperone in Gaucher patient cells. Mol Genet Metab, 96: 225-232, 2009.

5. Matsumura, C. Y., Pertille, A., Albuquerque, T. C., Santo Neto, H., and Marques, M. J. Diltiazem and verapamil protect dystrophin-deficient muscle fibers of MDX mice from degeneration: a potential role in calcium buffering and sarcolemmal stability. Muscle Nerve, 39: 167-176, 2009.

6. Bertera, F. M., Mayer, M. A., Opezzo, J. A., Taira, C. A., and Hocht, C. Increased sensitivity to diltiazem hypotensive effect in an experimental model of high-renin hypertension. J Pharm Pharmacol, 61: 79-87, 2009.

7. Bojanic, V., Bojanic, Z., Najman, S., Savic, T., Jakovljevic, V., Najman, S., and Jancic, S. Diltiazem prevention of toxic effects of monosodium glutamate on ovaries in rats. Gen Physiol Biophys, 28 Spec No: 149-154, 2009.

Certificate of Analysis/MSDS is available upon request with lot number

References for Clotrimazole :

1. Parmar, P. and Mehta, A. Development and Validation of HPTLC Method for the Estimation of Clotrimazole in Bulk drug and Tablet Formulation. Indian J Pharm Sci, 71: 451-454, 2009.

2. Harish, N. M., Prabhu, P., Charyulu, R. N., Gulzar, M. A., and Subrahmanyam, E. V. Formulation and Evaluation of in situ Gels Containing Clotrimazole for Oral Candidiasis. Indian J Pharm Sci, 71: 421-427, 2009.

3. Sholapurkar, A. A., Pai, K. M., and Rao, S. Comparison of efficacy of fluconazole mouthrinse and clotrimazole mouthpaint in the treatment of oral candidiasis. Aust Dent J, 54: 341-346, 2009.

4. Iannelli, A., de Sousa, G., Zucchini, N., Peyre, L., Gugenheim, J., and Rahmani, R. Clotrimazole protects the liver against normothermic ischemia-reperfusion injury in rats. Transplant Proc, 41: 4099-4104, 2009.

5. Furrow, E. and Groman, R. P. Intranasal infusion of clotrimazole for the treatment of nasal aspergillosis in two cats. J Am Vet Med Assoc, 235: 1188-1193, 2009.

6. Rasouli, M. R., Rahimi-Movaghar, V., and Vaccaro, A. R. Re: Usul H, Arslan E, Cansever T, et al. Effects of clotrimazole on experimental spinal cord ischemia/reperfusion injury in rats. Spine 2008;33:2863-7. Spine (Phila Pa 1976), 34: 1884, 2009.

Certificate of Analysis/MSDS is available upon request with lot number

References for 8-Phenyltheophylline:

1. Murray, S., Odupitan, A. O., Murray, B. P., Boobis, A. R., and Edwards, R. J. Inhibition of human CYP1A2 activity in vitro by methylxanthines: potent competitive inhibition by 8-phenyltheophylline. Xenobiotica, 31: 135-151, 2001.

2. Lee, S. C., Mallet, R. T., Shizukuda, Y., Williams, A. G., Jr., and Downey, H. F. Canine coronary vasodepressor responses to hypoxia are attenuated but not abolished by 8-phenyltheophylline. Am J Physiol, 262: H955-960, 1992.

3. Sawynok, J., Espey, M. J., and Reid, A. 8-Phenyltheophylline reverses the antinociceptive action of morphine in the periaqueductal gray. Neuropharmacology, 30: 871-877, 1991.

4. Wei, H. M., Kang, Y. H., and Merrill, G. F. Canine coronary vasodepressor responses to hypoxia are abolished by 8-phenyltheophylline. Am J Physiol, 257: H1043-1048, 1989.

5. Wormald, A., Bowmer, C. J., Yates, M. S., and Collis, M. G. Pharmacokinetics of 8-phenyltheophylline in the rat. J Pharm Pharmacol, 41: 418-420, 1989.

6. Nicholson, C. D. and Wilke, R. 8-phenyltheophylline as an inhibitor of cyclic AMP hydrolysis by cyclic nucleotide phosphodiesterase. J Auton Pharmacol, 9: 159-165, 1989.

Certificate of Analysis/MSDS is available upon request with lot number

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