DDInter458 DDInter676
Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions. It is isolated from the fungus _Beauveria nivea_. Initially manufactured by Sandoz and approved for use by the FDA in 1983, cyclosporine is now available in various products by Novartis (previously known as Sandoz).[L11097,L3734,L11118]
Esomeprazole, sold under the brand name Nexium, is a proton pump inhibitor (PPI) medication used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of _H. pylori_ infections along with other antibiotics including , , and , for example.[A177271, F4498] Its efficacy is considered similar to other medications within the PPI class including , , , , and . Esomeprazole is the s-isomer of , which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as , without any significant differences between the two compounds _in vitro_. Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect persists longer than 24 hours.[FDA Label] PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes.[A177577, A177580] Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients such as iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life. Rapid discontinuation of PPIs such as esomeprazole may cause a rebound effect and a short term increase in hypersecretion. Esomeprazole doses should be slowly lowered, or tapered, before discontinuing to prevent this rebound effect.
Cyclosporine {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) downregulates {v} (Gene) THAP11
THAP11 {u} (Gene) is downregulated by {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) causes {v} (Side Effect) Muscle spasms
Muscle spasms {u} (Side Effect) is caused by {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Lansoprazole
Lansoprazole {u} (Compound) resembles {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) downregulates {v} (Gene) THAP11
THAP11 {u} (Gene) is downregulated by {v} (Compound) Rabeprazole
Rabeprazole {u} (Compound) resembles {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) causes {v} (Side Effect) Muscle spasms
Muscle spasms {u} (Side Effect) is caused by {v} (Compound) Lansoprazole
Lansoprazole {u} (Compound) resembles {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) causes {v} (Side Effect) Depression
Depression {u} (Side Effect) is caused by {v} (Compound) Omeprazole
Omeprazole {u} (Compound) resembles {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) downregulates {v} (Gene) THAP11
THAP11 {u} (Gene) is downregulated by {v} (Compound) Omeprazole
Omeprazole {u} (Compound) resembles {v} (Compound) Esomeprazole
Cyclosporine {u} (Compound) causes {v} (Side Effect) Rigors
Rigors {u} (Side Effect) is caused by {v} (Compound) Duloxetine
Duloxetine {u} may cause a minor interaction that can limit clinical effects when taken with {v} Esomeprazole
Cyclosporine {u} (Compound) causes {v} (Side Effect) Cyst
Cyst {u} (Side Effect) is caused by {v} (Compound) Raltegravir
Raltegravir {u} may cause a minor interaction that can limit clinical effects when taken with {v} Esomeprazole
Cyclosporine (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Esomeprazole (Compound)
Cyclosporine (Compound) downregulates THAP11 (Gene) and THAP11 (Gene) is downregulated by Esomeprazole (Compound)
Cyclosporine (Compound) causes Muscle spasms (Side Effect) and Muscle spasms (Side Effect) is caused by Esomeprazole (Compound)
Cyclosporine (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Lansoprazole (Compound) and Lansoprazole (Compound) resembles Esomeprazole (Compound)
Cyclosporine (Compound) downregulates THAP11 (Gene) and THAP11 (Gene) is downregulated by Rabeprazole (Compound) and Rabeprazole (Compound) resembles Esomeprazole (Compound)
Cyclosporine (Compound) causes Muscle spasms (Side Effect) and Muscle spasms (Side Effect) is caused by Lansoprazole (Compound) and Lansoprazole (Compound) resembles Esomeprazole (Compound)
Cyclosporine (Compound) causes Depression (Side Effect) and Depression (Side Effect) is caused by Omeprazole (Compound) and Omeprazole (Compound) resembles Esomeprazole (Compound)
Cyclosporine (Compound) downregulates THAP11 (Gene) and THAP11 (Gene) is downregulated by Omeprazole (Compound) and Omeprazole (Compound) resembles Esomeprazole (Compound)
Cyclosporine (Compound) causes Rigors (Side Effect) and Rigors (Side Effect) is caused by Duloxetine (Compound) and Duloxetine may cause a minor interaction that can limit clinical effects when taken with Esomeprazole
Cyclosporine (Compound) causes Cyst (Side Effect) and Cyst (Side Effect) is caused by Raltegravir (Compound) and Raltegravir may cause a minor interaction that can limit clinical effects when taken with Esomeprazole