Lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH)
 

One capsule a day after breakfast or the first meal of the day. The capsule is swallowed
whole with a glass of water while standing or sitting (not lying down). The capsule should
not be broken or pulled apart as this may have an effect on the release of the long-acting
active ingredient.
No dose adjustment is warranted in renal impairment. No dose adjustment is warranted in
patients with mild to moderate hepatic insufficiency (see also 4.3
Contraindications).
The safety and efficacy of tamsulosin in children < 18 years have not been established.
Currently available data are described in section 5.1.
 

As with other α1-adrenoceptor antagonists, a reduction in blood pressure can occur in individual cases during treatment with tamsulosin as a result of which, rarely, syncope can occur. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down until the symptoms have disappeared.

Before therapy with tamsulosin is initiated, the patient should be examined in order to exclude the presence of other conditions, which can cause the same symptoms as benign prostatic hyperplasia.

Digital rectal examination and, when necessary, determination of prostate specific antigen (PSA) should be performed before treatment and at regular intervals afterwards.

The treatment of patients with severe renal impairment (creatinine clearance of < 10 ml/min) should be approached with caution, as these patients have not been studied. Angio-oedema has been rarely reported after the use of tamsulosin. Treatment should be discontinued immediately, patient should be monitored until disappearance of the oedema, and tamsulosin should not be re-administered.

The 'Intraoperative Floppy Iris Syndrome' (IFIS, a variant of small pupil syndrome) has been observed during cataract surgery in some patients on or previously treated with tamsulosin. IFIS may increase the risk of eye complications during and after the operation. The initiation of therapy with tamsulosin in patients for whom cataract surgery is scheduled is not recommended.

Discontinuing tamsulosin 1-2 weeks prior to cataract surgery is anecdotally considered helpful, but the benefit of treatment discontinuation has not yet been established. IFIS has also been

reported in patients who had discontinued tamsulosin for a longer period prior to cataract surgery.

During pre-operative assessment, cataract surgeons and ophthalmic teams should consider whether patients scheduled for cataract surgery are being or have been treated with tamsulosin in order to ensure that appropriate measures will be in place to manage the IFIS during surgery.

Tamsulosin hydrochloride should not be given in combination with strong inhibitors of CYP3A4 in patients with poor metaboliser CYP2D6 phenotype.

Tamsulosin hydrochloride should be used with caution in combination with strong and moderate inhibitors of CYP3A4.

Tamsulosin is extensively metabolized, mainly by CYP3A4 and CYP2D6. (e.g., ketoconazole). (e.g., paroxetine) or moderate (e.g., terbinafine) inhibitors of CYP2D6, particularly at a dose higher than 0.4 mg (e.g., 0.8 mg). Drug capsules should be used with caution in combination with

cimetidine, particularly at a dose higher than 0.4 mg (e.g., 0.8 mg). Drug should not be used in combination with other alpha adrenergic blocking agents Caution is advised when alpha

adrenergic blocking agents including Tamsulosin hydrochloride are co-administered 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 capsules

Interaction studies have only been performed in adults.

No interactions have been seen when tamsulosin was given concomitantly with either atenolol, enalapril, nifedipine or theophylline.

Concomitant cimetidine brings about a rise in plasma levels of tamsulosin, whereas furosemide a fall, but as levels remain within the normal range posology need not be adjusted. In vitro, neither diazepam nor propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin change the free fraction of tamsulosin in human plasma. Neither does tamsulosin change the free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone.

Diclofenac and warfarin, however, may increase the elimination rate of tamsulosin.

Strong and Moderate Inhibitors of CYP3A4 or CYP2D6

Tamsulosin is extensively metabolized, mainly by CYP3A4 and CYP2D6.

Concomitant treatment with ketoconazole (a strong inhibitor of CYP3A4) resulted in an increase in the Cmax and AUC of tamsulosin by a factor of 2.2 and 2.8, respectively. The effects of concomitant administration of a moderate CYP3A4 inhibitor (e.g., erythromycin) on the pharmacokinetics of Tamsulosin have not been evaluated

Concomitant treatment with paroxetine (a strong inhibitor of CYP2D6) resulted in an increase in the Cmax and AUC of tamsulosin by a factor of 1.3 and 1.6, respectively. A similar increase in

exposure is expected in CYP2D6 poor metabolizers (PM) as compared to extensive metabolizers (EM). Since CYP2D6 PMs cannot be readily identified and the potential for significant increase in tamsulosin exposure exists when Tamsulosin is co-administered with strong CYP3A4 inhibitors in CYP2D6 PMs, Tamsulosin should not be used in combination with strong inhibitors of CYP3A4 (e.g., ketoconazole)

The effects of concomitant administration of a moderate CYP2D6 inhibitor (e.g., terbinafine) on the pharmacokinetics of Tamsulosin have not been evaluated

The effects of co-administration of both a CYP3A4 and a CYP2D6 inhibitor with Tamsulosin capsules have not been evaluated. However, there is a potential for significant increase in tamsulosin exposure when Tamsulosin is co-administered with a combination of both CYP3A4 and CYP2D6 inhibitors

Cimetidine: Treatment with cimetidine resulted in a significant decrease (26%) in the clearance of tamsulosin hydrochloride, which resulted in a moderate increase in tamsulosin hydrochloride AUC (44%)

Tamsulosin hydrochloride should not be given in combination with strong inhibitors of CYP3A4 in patients with poor metaboliser CYP2D6 phenotype.

Tamsulosin hydrochloride should be used with caution in combination with strong and moderate inhibitors of CYP3A4.

Concurrent administration of other α1-adrenoceptor antagonists could lead to hypotensive effects.

Tamsulosin is intended for males only.
Ejaculation disorders have been observed in short and long term clinical studies with
tamsulosin. Events of ejaculation disorder, retrograde ejaculation and ejaculation failure
have been reported in the post authorization phase.
 

No studies on the effects on the ability to drive and use machines have been performed.
However patients should be aware of the fact that dizziness can occur.
 

a) Summary of safety
Not Applicable
b) Tabulated adverse reactions

c) Description of selected adverse events:
During cataract surgery a small pupil situation, known as Intraoperative Floppy Iris Syndrome
(IFIS), has been associated with therapy of tamsulosin during post-marketing surveillance
d) Pediatric use:
Not applicable
e) Other special population:
Renal Patients:
The treatment of severely renally impaired patients (creatinine clearance of < 10 ml/min)
should be approached with caution as these patients havenot been studied.
IFIS:
The 'Intraoperative Floppy Iris Syndrome' (IFIS, a variant of small pupil syndrome) has been
observed during cataract surgery in some patients on or previously treated with tamsulosin.
IFIS may lead to increased procedural complications during the operation. The initiation of
therapy with tamsulosin in patients for whom cataract surgery is scheduled is not
recommended.
 

To report any side effect(s):

Saudi Arabia

The National Pharmacovigilance Centre (NPC):

-  SFDA Call Center: 19999

-  E-mail: npc.drug@sfda.gov.sa

-  Website: https://ade.sfda.gov.sa

Other GCC States

Please contact the relevant competent authority.

Acute overdose with 5 mg tamsulosin hydrochloride has been reported. Acute hypotension
(systolic blood pressure 70 mm Hg), vomiting and diarrhoea were observed, which were
treated with fluid replacement and the patient could be discharged the same day. In case of
acute hypotension occurring after overdosage cardiovascular support should be given. Blood
pressure can be restored and heart rate brought back to normal by lying the patient down. If
this does not help then volume expanders and, when necessary, vasopressors could be
employed. Renal function should be monitored and general supportive measures applied.
Dialysis is unlikely to be of help as tamsulosin is very highly bound to plasma proteins.
Measures, such as emesis, can be taken to impede absorption if large quantities of the medicinal
product are involved, gastric lavage may be performed and activated charcoal and an osmotic
laxative, such as sodium sulphate, may be given.
 

Pharmacotherapeutic group: α1A adrenoreceptor antagonist. ATC code: G04CA02 Mechanism
of action Tamsulosin binds selectively and competitively to postsynaptic α1A adrenoreceptors,
which convey smooth muscle contraction, thereby relaxing prostatic and urethral smooth
muscle.
o Please contact the relevant competent authority.
Pharmacodynamic effects
Tamsulosin increases the maximum urinary flow rate by relaxing prostatic and urethral smooth
muscle, thus relieving obstruction.
The medicinal product also improves the irritative and obstructive symptoms in which the
contraction of smooth muscle in the lower urinary tract plays an important role.
Alpha-blockers can reduce blood pressure by lowering peripheral resistance. No reduction in
blood pressure of any clinical significance was observed during studies with tamsulosin in
normotensive patients.
The medicinal product's effect on storage and voiding symptoms are also maintained during
long-term therapy, as a result of which the need for surgical treatment is significantly
postponed.
Paediatric population
A double-blind, randomized, placebo-controlled, dose ranging study was performed in
children with neuropathic bladder. A total of 161 children (with an age of 2 to 16 years) were
randomized and treated at 1 of 3 dose levels of tamsulosin (low [0.001 to 0.002 mg/kg],
medium [0.002 to 0.004 mg/kg], and high [0.004 to 0.008 mg/kg]), or placebo. The primary
endpoint was number of patients who decreased their detrusor leak point pressure (LPP) to
<40 cm H2O based upon two evaluations on the same day. Secondary endpoints were:
Actual and percent change from baseline in detrusor leak point pressure, improvement or
stabilization of hydronephrosis and
hydroureter and change in urine volumes obtained by catheterisation and number of times
wet at time of catheterisation as recorded in catheterisation diaries. No statistically
significant difference was found between the placebo group and any of the 3 tamsulosin
dose groups for either the primary or any secondary endpoints. No dose response was
observed for any dose level.
 

Absorption
Tamsulosin is rapidly absorbed from the intestines and its bioavailability is almost complete.
Absorption is slowed down if a meal has been eaten before taking the medicinal product.
Uniformity of absorption can be assured by always taking tamsulosin after breakfast.
Tamsulosin shows linear kinetics.
Peak plasma levels are achieved at approximately six hours after a single dose of tamsulosin
taken after a full meal. The steady state is reached by day five of multiple dosing, when
Cmax in patients is about two-thirds higher than that reached after a single dose. Although
this has been demonstrated only in the elderly, the same result would also be expected in
youngerpatients.
There are huge inter-patient variations in plasma levels of tamsulosin, both after single as
well as multiple dosing.
Distribution
In humans, tamsulosin is more than 99% bound to plasma proteins and the volume of
distribution is small (about 0.2 l/kg).
Biotransformation
Tamsulosin has a low first pass metabolic effect. Most tamsulosin is found unaltered in
plasma. The substance is metabolised in the liver.
In studies on rats, tamsulosin was found to cause only a slight induction of microsomal liver
enzymes.
The metabolites are not as effective and toxic as the active medicinal product itself.
Excretion
Tamsulosin and its metabolites are mainly excreted in the urine with about 9% of the dose
being present in unchanged form.
The elimination half-life of tamsulosin in patients is approximately 10 hours (when taken
after a meal) and 13 hours in the steady state.
 

Toxicity after a single dose and multiple dosing has been investigated in mice, rats and
dogs. Reproductive toxicity has also been investigated in rats, carcinogenicity in mice and
rats, and genotoxicity in vivo and in vitro.
The common toxicity profile found with large doses of tamsulosin is equivalent to the
pharmacological effect associated with alpha adrenergic antagonists.
Changes in ECG readings were found with very large doses in dogs. This is not, however,
assumed to be of any clinical significance. Tamsulosin has not been found to have any
significant genotoxic properties.
Greater proliferative changes in the mammary glands of female rats and mice have been
discovered on exposure to tamsulosin. These findings, which are probably indirectly linked
to hyperprolactinaemia and only occur as a result of large doses having been taken, are
considered clinically insignificant.
 

Microcrystalline cellulose (Avicel PH101), Eudragit L30D-55, Polysorbate 80,
Sodium lauryl sulphate, Triacetin, Calcium Stearate, Talc
Empty gelatin capsule
 

Not applicable
 

Store below 25° C.
 

Aluminium / aluminium foil blister packs containing 30 Capsules
 

No special requirements.