RAPAFLO Capsule (2020)

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Allergan, Inc.

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1. Indications and Usage

RAPAFLO, a selective alpha-1 adrenergic receptor antagonist, is indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH) [see CLINICAL STUDIES (14)]. RAPAFLO ...

2. Dosage and Administration

2.1 Dosing Information The recommended dose is 8 mg orally once daily with a meal. Patients who have difficulty swallowing pills and capsules may carefully open the RAPAFLO capsule and sprinkle the powder ...

3. Dosage Forms and Strengths

The 8 mg capsules are white, opaque, hard #1 gelatin capsules imprinted with WATSON 152 in green on the cap and 8 mg in green on the body. The 4 mg capsules are white, opaque, hard #3 gelatin capsules ...

4. Contraindications

Severe renal impairment (CCr <30 mL/min) Severe hepatic impairment (Child-Pugh score >10) Concomitant administration with strong Cytochrome P450 3A4 (CYP3A4) inhibitors (e.g., ketoconazole, clarithromycin, ...

5. Warnings and Precautions

5.1 Orthostatic Effects Postural hypotension, with or without symptoms (e.g., dizziness) may develop when beginning RAPAFLO treatment. As with other alpha-blockers, there is potential for syncope. Patients ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

6.2. Postmarketing Experience

The following adverse reactions have been identified during post approval use of silodosin. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible ...

7. Drug Interactions

7.1 Moderate and Strong CYP3A4 Inhibitors In a clinical metabolic inhibition study, a 3.8-fold increase in silodosin maximum plasma concentrations and 3.2-fold increase in silodosin exposure were observed ...

8.1. Pregnancy

Risk Summary RAPAFLO is not indicated for use in females.

8.2. Lactation

RAPAFLO is not indicated for use in females.

8.3. Females and Males of Reproductive Potential

Infertility Males Possible effects on male fertility could be observed based on findings in rats at exposures that were at least two times higher than at the MRHD (based on AUC). These findings may be ...

8.4. Pediatric Use

RAPAFLO is not indicated for use in pediatric patients. Safety and effectiveness in pediatric patients have not been established.

8.5. Geriatric Use

In double-blind, placebo-controlled, 12-week clinical studies of RAPAFLO, 259 (55.6%) were under 65 years of age, 207 (44.4%) patients were 65 years of age and over, while 60 (12.9%) patients were 75 years ...

8.6. Renal Impairment

The effect of renal impairment on silodosin pharmacokinetics was evaluated in a single dose study of six male patients with moderate renal impairment and seven male subjects with normal renal function. ...

8.7. Hepatic Impairment

In a study comparing nine male patients with moderate hepatic impairment (Child-Pugh scores 7 to 9), to nine healthy male subjects, the single dose pharmacokinetics of silodosin were not significantly ...

10. Overdosage

RAPAFLO was evaluated at doses of up to 48 mg/day in healthy male subjects. The dose-limiting adverse event was postural hypotension. Should overdose of RAPAFLO lead to hypotension, support of the cardiovascular ...

11. Description

RAPAFLO is the brand name for silodosin, a selective antagonist of alpha-1 adrenoreceptors. The chemical name of silodosin is 1-(3-Hydroxypropyl)- 5-[(2R)2({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1 ...

12.1. Mechanism of Action

Silodosin is a selective antagonist of post-synaptic alpha-1 adrenoreceptors, which are located in the human prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Blockade of ...

12.2. Pharmacodynamics

Orthostatic Effects A test for postural hypotension was conducted 2 to 6 hours after the first dose in the two 12-week, double-blind, placebo-controlled clinical studies. After the patient had been at ...

12.3. Pharmacokinetics

The pharmacokinetics of silodosin have been evaluated in adult male subjects with doses ranging from 0.1 mg to 24 mg per day. The pharmacokinetics of silodosin are linear throughout this dosage range. ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

In a 2-year oral carcinogenicity study in rats administered doses up to 150 mg/kg/day [about 8 times the exposure at the MRHD based on AUC of silodosin], an increase in thyroid follicular cell tumor incidence ...

14. Clinical Studies

14.1 Benign Prostatic Hyperplasia Two 12-week, randomized, double-blind, placebo-controlled, multicenter studies were conducted with 8 mg daily of silodosin. In these two studies, 923 patients [mean age ...

16.1. How Supplied

White, opaque, hard gelatin 8 mg capsules: Cap is imprinted with WATSON 152 in green. Body is imprinted with 8 mg in green. 8 mg capsules are supplied in unit of use HDPE bottles of: 30 capsules ...

16.2. Storage and Handling

Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). [See USP controlled room temperature]. Protect from light and moisture. Keep out of reach of children.

17. Patient Counseling Information

Advise patients to take RAPAFLO once daily with a meal [see Dosage and Administration (2.1)]. Advise patients about the possible occurrence of symptoms related to postural hypotension (such as ...