赛洛多辛(Silodosin)的详细说明书：作用与功效,用法用量,副作用,注意事项等

Silodosin was developed by Kissei Pharmaceutical Co., Ltd. of Japan.

Indications for Silodosin

It is not suitable for the treatment of hypertension.

Silodosin usage and dosage

1. Dosage information

The recommended dose is 8 mg once a day, taken orally with food.

2. How to take the medicine

Patients who have difficulty swallowing tablets or capsules can carefully open the silodosin capsule and sprinkle the contained powder on a tablespoon of applesauce. Applesauce should be swallowed immediately (within 5 minutes) without chewing, followed by drinking 8 ounces of cool water to ensure complete swallowing of the powder. The applesauce should not be hot and should be soft enough to be swallowed without chewing. Any powder/applesauce mixture should be used immediately (within 5 minutes) and should not be stored for later use.

3. Dose adjustment for special groups

(1) Renal insufficiency: Silodosin capsules are contraindicated in patients with severe renal insufficiency (creatinine clearance CCr<30mL/min).

In patients with moderate renal insufficiency (CCr30-50mL/min), the dose should be reduced to 4 mg once daily with meals.

No dose adjustment is required for patients with mild renal insufficiency (CCr50-80mL/min).

(2) Hepatic insufficiency: Silodosin capsules have not been studied in patients with severe hepatic insufficiency (Child-Pugh score ≥ 10), so it is contraindicated in such patients.

No dose adjustment is required in patients with mild or moderate hepatic impairment.

4. Dosage forms and specifications

The 4 mg capsules have a white opaque cap and body, with a size of "3". Cap is stamped "479" in black ink. The bag is stamped with "4" in black ink. The 8 mg capsule has a white opaque cap and body, with a size of "1". Cap is stamped "480" in black ink. The bag is stamped with "8" in black ink.

The pictures are from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Contraindications of Silodosin

1. Severe renal insufficiency (CCr<30mL/min).

2. Severe liver insufficiency (Child-Pugh score ≥ 10).

3. Use potent cytochrome P4503A4 (CYP3A4) inhibitors (for example: ketoconazole, clarithromycin, itraconazole, ritonavir) at the same time.

4. Patients with a history of allergies to silodosin or any component of silodosin capsules.

Precautions for Silodosin

1. Orthostatic effect

When starting treatment with Silodosin capsules, orthostatic hypotension with or without symptoms (such as dizziness) may occur. As with other alpha-blockers, there is a potential risk of syncope. Patients should be cautioned about driving, operating machinery, or performing hazardous tasks when starting treatment.

2. Renal insufficiency

The dose of silodosin capsules in patients with moderate renal insufficiency should be reduced to 4 mg. Exercise caution and monitor for adverse reactions in such patients.

Silodosin capsules are contraindicated in patients with severe renal insufficiency.

3. Hepatic insufficiency

Silodoxin capsules have not been tested in patients with severe hepatic insufficiency and should not be prescribed to such patients.

4. Prostate cancer

Prostate cancer and BPH can cause many of the same symptoms. The two diseases often coexist. Therefore, patients thought to have BPH should be examined to rule out the presence of prostate cancer before starting treatment with silodosin capsules.

5. Laboratory test interactions

No laboratory test interactions were observed during the clinical evaluation, and treatment with silodosin capsules for up to 52 weeks had no significant effect on prostate-specific antigen (PSA).

Adverse reactions of Silodosin

1. Skin and subcutaneous tissue: toxic skin rash, purpura, rash, itching and urticaria.

2. Liver and gallbladder: jaundice, liver function damage accompanied by elevated transaminases.

3. Immune system: allergic reactions, not limited to skin reactions, including tongue swelling and pharyngeal edema, and can lead to serious consequences.

Silodosin drug interactions

1. Moderate and strong CYP3A4 inhibitors

The use of strong CYP3A4 inhibitors (such as itraconazole or ritonavir) may lead to an increase in the plasma concentration of silodosin. Concomitant use of strong CYP3A4 inhibitors and silodosin capsules is prohibited.

The effects of moderate CYP3A4 inhibitors on the pharmacokinetics of silodosin have not been evaluated. Concomitant use of moderate CYP3A4 inhibitors (such as diltiazem, erythromycin, verapamil) may increase the concentration of silodosin capsules. Exercise caution and monitor patients for adverse reactions when coadministering silodosin capsules with moderate CYP3A4 inhibitors.

2. Potent P-glycoprotein (P-gp) inhibitor

In vitro studies have shown that silodosin is a substrate of P-gp. Ketoconazole is a CYP3A4 inhibitor that also inhibits P-gp, resulting in a significant increase in silodosin exposure. Inhibition of P-gp may result in increased silodosin concentrations. Therefore, the use of silodosin capsules is not recommended in patients who are taking strong P-gp inhibitors (such as cyclosporine).

3. Alpha-blockers

The pharmacodynamic interaction between silodosin and other alpha-blockers has not been determined. However, a possible interaction is expected and silodosin capsules should not be used in combination with other alpha-blockers.

4. Digoxin

Concurrent administration of silodosin capsules and digoxin does not significantly change the steady-state pharmacokinetics of digoxin, and no dose adjustment is required.

Silodosin (Silodosin) Medication for Special Populations

1. Pregnancy

Silodosin capsules are not suitable for women.

2. Lactation period

Silodosin capsules are not suitable for women.

3. Males of reproductive potential

Based on findings in rats with exposures at least twice the MRHD based on AUC, effects on male fertility may be observed. These findings may be reversible and their clinical relevance is unknown.

4. Pediatric use

Silodoxin capsules are not suitable for pediatric patients. Safety and effectiveness in pediatric patients have not been established.

5. Medication for the elderly

In the 12-week double-blind, placebo-controlled clinical study of silodosin capsules, 259 (55.6%) patients were under 65 years old, 207 (44.4%) patients were 65 years old and above, and 60 (12.9%) patients were 75 years old and above.

Orthostatic hypotension was reported in 2.3% of silodosin patients aged <65 years (1.2% in the placebo group), 2.9% in silodosin patients aged ≥65 years (1.9% in the placebo group), and 5.0% in patients aged ≥75 years (0% in the placebo group). Otherwise, there were no significant differences in safety or effectiveness between older and younger patients.

6. Renal insufficiency

The plasma concentration of silodosin in subjects with moderate renal insufficiency was approximately three times higher than that in subjects with normal renal function.

In patients with moderate renal insufficiency, the dose of silodosin capsules should be reduced to 4 mg daily. Caution should be exercised and patients should be monitored for adverse reactions.

Silodoxin capsules have not been studied in patients with severe renal insufficiency. Silodosin capsules are contraindicated in patients with severe renal insufficiency.

7. Hepatic insufficiency

Patients with mild or moderate hepatic insufficiency do not need to adjust the dose.

Silodosin capsules have not been studied in patients with severe hepatic impairment. Silodosin capsules are contraindicated in patients with severe hepatic insufficiency.

Silodosin (Silodosin) mechanism of action

Silodosin is a selective postsynaptic α-1 adrenergic receptor antagonist. These receptors are found in the human prostate, bladder base, bladder neck, prostate capsule and prostatic urethra. Blocking these alpha-1 adrenergic receptors causes the smooth muscles in these tissues to relax, thereby improving urinary flow rate and reducing BPH symptoms.

Silodosin packaging

Silodosin capsules for oral administration have the following specifications:

1. 4 mg: white opaque capsule cap and capsule body. Cap is stamped "479" in black ink. The bag is stamped with "4" in black ink. The packaging is as follows:

30-capsule bottle with child-resistant cap. NDC82619-113-01.

2. 8 mg: white opaque cap and body. Cap is stamped "480" in black ink. The bag is stamped with "8" in black ink. The packaging is as follows:

30-capsule bottle with child-resistant cap. NDC82619-114-01.

90-capsule bottle with child-resistant cap. NDC82619-114-02.

Storage of Silodosin

Store at 20° to 25°C (68° to 77°F); allowed to move within the range of 15° to 30°C (59° to 86°F), protected from light and moisture.

Please keep out of the reach of children.