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Ospemifene is a selective estrogen receptor modulator (SERM) [4] acting similarly to an estrogen on the vaginal epithelium, building vaginal wall thickness which in turn reduces the pain associated with dyspareunia. Dyspareunia is most commonly caused by "vulvar and vaginal atrophy." [5]
It was approved for prevention and treatment of osteoporosis and was the first clinically available SERM to prevent both osteoporosis and breast cancer. [7] Ospemifene was approved on February 26, 2013, for the treatment of moderate to severe dyspareunia, which is a symptom, due to menopause, of vulvar and vaginal atrophy.
Dyspareunia (/ d ɪ s p ə r ˈ u n i ə / dis-pər-OO-nee-ə) is painful sexual intercourse due to somatic or psychological causes. [1] The term dyspareunia covers both female dyspareunia and male dyspareunia, but many discussions that use the term without further specification concern the female type, which is more common than the male type.
Drug resistance is the reduction in effectiveness of a medication such as an antimicrobial or an antineoplastic in treating a disease or condition. [1] The term is used in the context of resistance that pathogens or cancers have "acquired", that is, resistance has evolved.
Drug resistance, such as antimicrobial resistance or antineoplastic resistance, may make the first-line drug ineffective, especially in case of multidrug-resistant pathogens and tumors. Such an alternative may be outside of extant regulatory requirements or medical best practices, in which case it may be viewed as salvage therapy .
Many drugs are eliminated from the body by this mechanism. Some of these drugs pass through the MRP2 transporter slowly. This may cause a buildup of organic anions in the cytoplasm of the cells. Drugs that inhibit the MRP2 transporter can cause a buildup of organic anions inside renal proximal tubule cells.
Multiple drug resistance (MDR), multidrug resistance or multiresistance is antimicrobial resistance shown by a species of microorganism to at least one antimicrobial drug in three or more antimicrobial categories. [1] Antimicrobial categories are classifications of antimicrobial agents based on their mode of action and specific to target ...
This causes repetitive excitation that lasts longer than a normal acetylcholine excitation and is most likely explained by the resistance of depolarizing agents to the enzyme acetylcholinesterase. The constant depolarization and triggering of the receptors keeps the endplate resistant to activation by acetylcholine.