74.有關verapamil與digoxin之交互作用,下列敘述何者正確?
(A)digoxin血中濃度降低
(B)digoxin的代謝增加
(C)verapamil抑制小腸中的P-glycoprotein
(D)digoxin在腸道的吸收降低
答案:登入後查看
統計: A(60), B(48), C(3011), D(53), E(0) #2972668
統計: A(60), B(48), C(3011), D(53), E(0) #2972668
詳解 (共 6 筆)
#5870880
| 限制 | 抑制P-gp |
| VIP | Verapmil Itraconazole Propafenone |
| 訪問 (ASK) |
Amiodarone Spironolactone Ketoconazole |
| 賽 (RACE) |
Ritonavir Azithromycin Clarithromycin Erythromycin |
| 車 | Carvedilol |
| Queen | Quinidine |
72
1
#5715704
抑制P-gp
Amiodarone、verapamil、quinidine、ketoconazole、erythromycin
23
1
#6159427
給跟我一樣對D有疑問的
P-gp是外排型的pump,digoxin會透過p-gp排到小腸中而非透過p-gp吸收進入體內
P-gp是外排型的pump,digoxin會透過p-gp排到小腸中而非透過p-gp吸收進入體內
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Both its location at the apical membrane of enterocytes and its function as an efflux pump suggest a particular role of intestinal P-gp for the disposition of digoxin. Inhibition of intestinal P-gp by oral treatment with the P-gp inhibitor PSC833 (18) increases bioavailability of concomitantly administered drugs. In contrast to such inhibition, recent experimental evidence obtained from human colon carcinoma cell lines indicates that P-gp expression is upregulated by rifampin (19). If rifampin induces intestinal P-gp in humans, and digoxin is transported from apical duodenal cells during absorption back into the lumen of the intestine, then coadministration of rifampin should affect digoxin disposition predominantly after oral administration.
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Ref: Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, Kroemer HK. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest. 1999 Jul;104(2):147-53. doi: 10.1172/JCI6663. Erratum in: J Clin Invest 2002 Aug;110(4):571. PMID: 10411543; PMCID: PMC408477. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC408477/
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另外補充,digoxin會受到食物影響吸收速率但不影響吸收總量
Digoxin is approximately 70-80% absorbed in the first part of the small bowel.6 The bioavailability of an oral dose varies from 50-90%, however, oral gelatinized capsules of digoxin are reported to have a bioavailability of 100%.10 Tmax, or the time to reach the maximum concentration of digoxin was measured to be 1.0 h in one clinical study of healthy patients taking 0.25 mg of digoxin with a placebo.19 Cmax, or maximum concentration, was 1.32 ± 0.18 ng/ml−1 in the same study, and AUC (area under the curve) was 12.5 ± 2.38 ng/ml−1.19 If digoxin is ingested after a meal, absorption is slowed but this does not change the total amount of absorbed drug. If digoxin is taken with meals that are in fiber, absorption may be decreased.24
Digoxin is approximately 70-80% absorbed in the first part of the small bowel.6 The bioavailability of an oral dose varies from 50-90%, however, oral gelatinized capsules of digoxin are reported to have a bioavailability of 100%.10 Tmax, or the time to reach the maximum concentration of digoxin was measured to be 1.0 h in one clinical study of healthy patients taking 0.25 mg of digoxin with a placebo.19 Cmax, or maximum concentration, was 1.32 ± 0.18 ng/ml−1 in the same study, and AUC (area under the curve) was 12.5 ± 2.38 ng/ml−1.19 If digoxin is ingested after a meal, absorption is slowed but this does not change the total amount of absorbed drug. If digoxin is taken with meals that are in fiber, absorption may be decreased.24
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7
0
#6545200
補充個
P-gp inhibitor : AAACCC MNOPQ
Amiodarone, Atovastatin, Amphotericin B, Clartithromycin, Cyclosporine, CCB(verapamil, Diltiazem)
Macrolide, KetocoNazole, ItracoNazole, Propafenone, Quinidine
1
0