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赛洛多辛(Silodosin)的注意事项和药物相互作用
Silodosin is a highly selective α1A-adrenergic receptor antagonist that mainly targets lower urinary tract symptoms caused by benign prostatic hyperplasia (BPH).
Precautions for Silodosin
1. Orthostatic hypotension
Silodosin may cause orthostatic hypotension, dizziness or syncope.
2. Prostate cancer
The possibility of prostate cancer needs to be ruled out before starting treatment.
3. Intraoperative flaccid iris syndrome
Intraoperative iris flaccid syndrome (IFIS) occurs in some patients currently or previously treated with α1-adrenergic blockers during phacoemulsification cataract surgery.
Male patients scheduled to undergo cataract surgery should be specifically asked whether they have used silodosin or other α1-adrenergic blockers.
If the patient has used such drugs, the ophthalmologist should consider modifying the surgical technique (such as the use of iris hooks, iris dilation rings, or pharmacological intervention (intracameral phenylephrine or preoperative atropine)) to reduce the risk of IFIS. There is currently no proven benefit from discontinuing α1-blockers preoperatively.
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Silodosin drug interactions
1. Interactions with CYP3A4 inhibitors
(1) Strong CYP3A4 inhibitors: such as ketoconazole, clarithromycin, itraconazole, and ritonavir will significantly inhibit the metabolism of silodosin and increase its plasma concentration by 3 .2 to 3.8 times, so combined use is prohibited.
(2) Moderate CYP3A4 inhibitors: such as diltiazem, erythromycin, and verapamil may also increase the concentration of silodosin, and adverse reactions should be carefully monitored during combined use.
2. Interaction with P-glycoprotein inhibitors
Silodosin is a substrate of P-gp, and ketoconazole (which simultaneously inhibits CYP3A4 and P-gp) is known to significantly increase its plasma concentration. , it is not recommended to use silodosin in combination with strong P-gp inhibitors (such as cyclosporine)
3. Interactions with other α-blockers
Silodosin should not be used in combination with other α-blockers due to possible side effects. Enhance the antihypertensive effect and increase the risk of adverse reactions such as hypotension and dizziness.
Pharmacokinetics of Silodosin
1. Absorption
Time to peak after oral administration. (Tmax) is about 2.6 hours, and the absolute bioavailability is about 32%. When taken with food, Cmax and AUC may decrease, but it is still recommended to take it after meals to improve tolerance.
2. Distribution
The distribution volume of silodosin is 49.5L, and the plasma protein binding rate is as high as 97%, so it is not easily removed by dialysis.
3. Metabolism
The main metabolite of silodosin is glucuronic acid conjugates. (KMD-3213G), mainly metabolized by CYP3A4, UGT, ADH/ALDH to generate glucuronic acid conjugates and oxidative metabolites
4, excretion
5. Pharmacokinetics in Special Populations
(1 ), Elderly people: AUC and half-life are slightly higher than those of young adults, but no dose adjustment is required.
(2) Patients with renal insufficiency: AUC and Cmax increase approximately 3 times in patients with moderate renal impairment (Clcr30-50mL/min), and the dose needs to be reduced to 4mg/day; it is contraindicated in patients with severe liver dysfunction.
(3) Patients with mild to moderate impairment do not need to adjust the dose; no studies have been conducted in patients with severe impairment, and use is contraindicated.
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