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The structure-activity relationship of the drug class has been explored to a reasonable extent. The optimal substitution pattern is fairly tightly defined (i.e. N,N-diethyl on the amine nitrogen, 4-ethoxy on the benzyl ring and 5-nitro on the benzimidazole ring), but even derivatives incorporating only some of these features are still potent opioids.
Benzimidazole was discovered during research on vitamin B 12. The benzimidazole nucleus was found to be a stable platform on which drugs could be developed. [3] Benzimidazole is produced by condensation of o-phenylenediamine with formic acid, [4] or the equivalent trimethyl orthoformate: C 6 H 4 (NH 2) 2 + HC(OCH 3) 3 → C 6 H 4 N(NH)CH + 3 CH ...
Researchers have explored the pharmacological properties of benzimidazole derivatives, with some displaying antimicrobial, antiviral, anticancer, and antifungal activities. [medical citation needed] The specific medicinal properties of 5,6-dimethylbenzimidazole may vary based on its structural features and substituent. [vague]
It is a member of the benzimidazole family of medications for worms. [1] Triclabendazole was approved for medical use in the United States in 2019. [3] [4] It is on the World Health Organization's List of Essential Medicines. [5] For human use, it can be obtained from the World Health Organization. [2] It is also used in animals. [6]
Albendazole is a broad-spectrum antihelmintic and antiprotozoal agent of the benzimidazole type. [3] It is used for the treatment of a variety of intestinal parasite infections, including ascariasis, pinworm infection, hookworm infection, trichuriasis, strongyloidiasis, taeniasis, clonorchiasis, opisthorchiasis, cutaneous larva migrans, giardiasis, and gnathostomiasis, among other diseases.
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Print/export Download as PDF; Printable version; ... Pages in category "Benzimidazole opioids" The following 23 pages are in this category, out of 23 total.
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.