Diltiazem hydrochloride

Synonyms: Diltiazem, Cardizem, Dilacorxr, Tiazac, Cardizem

IUPAC Name:

(2S-cis)-3-(Acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5 -benzothiazepin-4(5H)-one hydrochloride

Functional Activity:

Diltiazem is a non-dihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.

It is also an effective preventive medication for migraine. It is a class 3 anti-anginal drug, and a class IV antiarrhythmic. It is a common adulterant of cocaine, and has been found to reduce cocaine cravings in rats, indicating that it may prolong the "high". It incites very minimal reflex sympathetic changes. It is based upon a 1,4-thiazepine ring.

Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

Technical Data:

M.Wt: 450.98

Formula: C22H26N2O4S.HCl

Solubility: Soluble to 100 mM in water and to 100 mM in DMSO

Purity: >99%

Storage: Dessicate at RT

CAS No.: 33286-22-5

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.