Tamsulosin Hydrochloride Information
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Indications And Usage
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH) . Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are not indicated for the treatment of hypertension.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Dosage And Administration
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg once daily is recommended as the dose for the treatment of the signs and symptoms of BPH. It should be administered approximately one-half hour following the same meal each day.
For those patients who fail to respond to the 0.4 mg dose after 2 to 4 weeks of dosing, the dose of Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules can be increased to 0.8 mg once daily. Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg should not be used in combination with strong inhibitors of CYP3A4 (e.g., ketoconazole) .
If Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules administration is discontinued or interrupted for several days at either the 0.4 mg or 0.8 mg dose, therapy should be started again with the 0.4 mg once-daily dose.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Dosage Forms And Strengths
Capsule: 0.4 mg, hard-shell gelatin capsule with a blue opaque cap and a blue opaque body filled with white to off-white beads. The capsule is axially printed with over in black ink on both the cap and the body.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Contraindications
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are contraindicated in patients known to be hypersensitive to Tamsulosin hydrochloride (Tamsulosin hydrochloride) or any component of Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules. Reactions have included skin rash, urticaria, pruritus, angioedema and respiratory symptoms
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Warnings And Precautions
Tamsulosin is extensively metabolized, mainly by CYP3A4 and CYP2D6. Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg should not be used in combination with strong inhibitors of CYP3A4 (e.g., ketoconazole) . Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules should be used with caution in combination with moderate inhibitors of CYP3A4 (e.g., erythromycin), in combination with strong (e.g., paroxetine) or moderate (e.g., terbinafine) inhibitors of CYP2D6, in patients known to be CYP2D6 poor metabolizers particularly at a dose higher than 0.4 mg (e.g., 0.8 mg) .
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules should be used with caution in combination with cimetidine, particularly at a dose higher than 0.4 mg (e.g., 0.8 mg) .
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules should not be used in combination with other alpha adrenergic blocking agents .
Caution is advised when alpha adrenergic blocking agents including Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are coadministered with PDE5 inhibitors. Alpha-adrenergic blockers and PDE5 inhibitors are both vasodilators that can lower blood pressure. Concomitant use of these two drug classes can potentially cause symptomatic hypotension .
Caution should be exercised with concomitant administration of warfarin and Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules .
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Adverse Reactions
Because clinical studies are conducted under widely varying conditions, adverse reactions rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.
The incidence of treatment-emergent adverse events has been ascertained from six short-term U.S. and European placebo-controlled clinical trials in which daily doses of 0.1 to 0.8 mg Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules were used. These studies evaluated safety in 1,783 patients treated with Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules and 798 patients administered placebo. Table 1 summarizes the treatment-emergent adverse events that occurred in ≥ 2% of patients receiving either Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg or 0.8 mg and at an incidence numerically higher than that in the placebo group during two 13-week U.S. trials (US92-03A and US93-01) conducted in 1,487 men.
The following adverse reactions have been identified during post-approval use of Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Decisions to include these reactions in labeling are typically based on one or more of the following factors: (1) seriousness of the reaction, (2) frequency of reporting, or (3) strength of causal connection to Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules.
Allergic-type reactions such as skin rash, urticaria, pruritus, angioedema and respiratory symptoms have been reported with positive rechallenge in some cases. Priapism has been reported rarely. Infrequent reports of palpitations, hypotension, skin desquamation, constipation and vomiting have been received during the postmarketing period.
During cataract surgery, a variant of small pupil syndrome known as Intraoperative Floppy Iris Syndrome (IFIS) has been reported in association with alpha blocker therapy .
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Use In Specific Populations
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are not indicated for use in pediatric populations.
A description of the data from pediatric studies of Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules is contained in the approved labeling for Boehringer Ingelheim’s Flomax capsules. However, due to Boehringer Ingelheim’s marketing exclusivity rights, a description of these pediatric studies is not contained in the approved labeling for this Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Overdosage
Should overdosage of Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules lead to hypotension , support of the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in the supine position. If this measure is inadequate, then administration of intravenous fluids should be considered. If necessary, vasopressors should then be used and renal function should be monitored and supported as needed. Laboratory data indicate that Tamsulosin hydrochloride (Tamsulosin hydrochloride) is 94% to 99% protein bound; therefore, dialysis is unlikely to be of benefit.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Description
Tamsulosin hydrochloride (Tamsulosin hydrochloride) is an antagonist of alpha adrenoceptors in the prostate.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) is (-)-()-5-[2-[[2-(-Ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfonamide, monohydrochloride. Tamsulosin hydrochloride (Tamsulosin hydrochloride) , USP is a white to off-white powder that melts with decomposition at approximately 230°C. It is sparingly soluble in water and methanol, slightly soluble in glacial acetic acid and ethanol, and practically insoluble in ether.
The molecular formula of Tamsulosin hydrochloride (Tamsulosin hydrochloride) is CHNOS • HCl. The molecular weight of Tamsulosin hydrochloride (Tamsulosin hydrochloride) is 444.97. Its structural formula is:
Each Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsule, USP for oral administration contains Tamsulosin hydrochloride (Tamsulosin hydrochloride) 0.4 mg, and the following inactive ingredients: calcium stearate, D&C Red No. 28, FD&C Blue No. 1, gelatin, methacrylic acid copolymer, microcrystalline cellulose, polysorbate 80, sodium hydroxide, sodium lauryl sulfate, talc, titanium dioxide and triethyl citrate.
The imprinting ink contains the following: black iron oxide, D&C Yellow No. 10 Aluminum Lake, FD&C Blue No. 1 Aluminum Lake, FD&C Blue No. 2 Aluminum Lake, FD&C Red No. 40 Aluminum Lake, propylene glycol and shellac glaze.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Clinical Pharmacology
The symptoms associated with benign prostatic hyperplasia are related to bladder outlet obstruction, which is comprised of two underlying components: static and dynamic. The static component is related to an increase in prostate size caused, in part, by a proliferation of smooth muscle cells in the prostatic stroma. However, the severity of BPH symptoms and the degree of urethral obstruction do not correlate well with the size of the prostate. The dynamic component is a function of an increase in smooth muscle tone in the prostate and bladder neck leading to constriction of the bladder outlet. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha adrenoceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in symptoms of BPH.
Tamsulosin, an alpha adrenoceptor blocking agent, exhibits selectivity for alpha receptors in the human prostate. At least three discrete alpha adrenoceptor subtypes have been identified: alpha, alpha, and alpha; their distribution differs between human organs and tissue. Approximately 70% of the alpha receptors in the human prostate are of the alpha subtype.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules are not intended for use as an antihypertensive drug.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Clinical Studies
Four placebo-controlled clinical studies and one active-controlled clinical study enrolled a total of 2,296 patients (1,003 received Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg once daily, 491 received Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.8 mg once daily, and 802 were control patients) in the U.S. and Europe.
In the two U.S. placebo-controlled, double-blind, 13-week, multicenter studies [Study 1 (US92-03A) and Study 2 (US93-01)], 1,486 men with the signs and symptoms of BPH were enrolled. In both studies, patients were randomized to either placebo, Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg once daily, or Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.8 mg once daily. Patients in Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.8 mg once-daily treatment groups received a dose of 0.4 mg once daily for one week before increasing to the 0.8 mg once-daily dose. The primary efficacy assessments included: 1) total American Urological Association (AUA) Symptom Score questionnaire, which evaluated irritative (frequency, urgency, and nocturia), and obstructive (hesitancy, incomplete emptying, intermittency, and weak stream) symptoms, where a decrease in score is consistent with improvement in symptoms; and 2) peak urine flow rate, where an increased peak urine flow rate value over baseline is consistent with decreased urinary obstruction.
Mean changes from baseline to Week 13 in total AUA Symptom Score were significantly greater for groups treated with Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg and 0.8 mg once daily compared to placebo in both U.S. studies (Table 3, Figures 2A and 2B). The changes from baseline to Week 13 in peak urine flow rate were also significantly greater for the Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg and 0.8 mg once-daily groups compared to placebo in Study 1, and for the Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.8 mg once-daily group in Study 2 (Table 3, Figures 3A and 3B). Overall there were no significant differences in improvement observed in total AUA Symptom Scores or peak urine flow rates between the 0.4 mg and the 0.8 mg dose groups with the exception that the 0.8 mg dose in Study 1 had a significantly greater improvement in total AUA Symptom Score compared to the 0.4 mg dose.
Mean total AUA Symptom Scores for both Tamsulosin hydrochloride (Tamsulosin hydrochloride) capsules 0.4 mg and 0.8 mg once-daily groups showed a rapid decrease starting at one week after dosing and remained decreased through 13 weeks in both studies (Figures 2A and 2B).
In Study 1, 400 patients (53% of the originally randomized group) elected to continue in their originally assigned treatment groups in a double-blind, placebo-controlled, 40-week extension trial (138 patients on 0.4 mg, 135 patients on 0.8 mg and 127 patients on placebo).
Three hundred twenty-three patients (43% of the originally randomized group) completed one year. Of these, 81% (97 patients) on 0.4 mg, 74% (75 patients) on 0.8 mg and 56% (57 patients) on placebo had a response ≥ 25% above baseline in total AUA Symptom Score at one year.
Tamsulosin hydrochloride (Tamsulosin hydrochloride) How Supplied/storage And Handling
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Capsules, USP are available containing 0.4 mg of Tamsulosin hydrochloride (Tamsulosin hydrochloride) , USP. The 0.4 mg capsule is a hard-shell gelatin capsule with a blue opaque cap and a blue opaque body filled with white to off-white beads. The capsule is axially printed with over in black ink on both the cap and the body. They are available as follows:
NDC 51079-294-20 - Unit dose blister packages of 100 (10 cards of 10 capsules each).
NDC 51079-294-56 - Unit dose punch cards of 300 (10 punch cards of 30 capsules each).
NDC 51079-294-19 - Robot Ready blister packages of 25 (25 cards of 1 capsule each).
Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]
Protect from moisture.
Manufactured by:Mylan Pharmaceuticals Inc.Morgantown, WV 26505
Distributed by:UDL Laboratories, Inc.Rockford, IL 61103
S-10709 R14/10
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Patient Counseling Information
Tamsulosin hydrochloride (Tamsulosin hydrochloride)
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Principal Display Panel
Tamsulosin hydrochloride (Tamsulosin hydrochloride) Capsules, USP
0.4 mg
10 Capsules
