Consumer medicine information

Blooms the Chemist Tamsulosin SR

Tamsulosin hydrochloride

BRAND INFORMATION

Brand name

Blooms the Chemist Tamsulosin SR

Active ingredient

Tamsulosin hydrochloride

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Blooms the Chemist Tamsulosin SR.

What is in this leaflet

This leaflet answers some common questions about BLOOMS THE CHEMIST TAMSULOSIN SR.

It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking this medicine against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, talk to your doctor or pharmacist.

Keep this leaflet with our medicine. You may need to read it again.

What this medicine is used for

BLOOMS THE CHEMIST TAMSULOSIN SR is a medicine for use by men only. Tamsulosin SR is used in men who have a medical condition called benign prostatic hyperplasia (also known as BPH). In BPH the prostate gland is bigger than normal. BPH is NOT prostate cancer.

Tamsulosin SR belongs to a group of medicines called alpha-blockers.

Your doctor has prescribed Tamsulosin SR for you because you have symptoms caused by an enlarged prostate gland. BPH occurs only in men. It is common in men over the age of 50 years.

The prostate gland is at the outlet of your urinary bladder. Because your prostate has become bigger than it should be, it is affecting how well you are able to pass your urine.

This causes some, or all of the following symptoms:

  • urine flow is slow
  • the urine stream may become a trickle, or it may stop and start
  • you find a delay when you try to pass urine, and you must strain to do so
  • you feel that you cannot empty your bladder completely
  • you may dribble at the end of passing urine
  • you need to pass urine often during the day
  • you need to get up often during the night to pass urine
  • you feel an urgency to pass urine as soon as you first feel the need to do so

These symptoms usually start gradually and increase in severity.

Ask your doctor if you have any questions about why Tamsulosin SR has been prescribed for you.

Tamsulosin SR is available only with a doctor’s prescription.

Before you take this medicine

When you must not take it

Do not take this medicine if you have an allergy to:

  • medicines containing tamsulosin hydrochloride
  • any of the ingredients listed at the end of this leaflet

Some of the symptoms of an allergic reaction may include:

  • shortness of breath
  • wheezing or difficulty breathing
  • swelling of the face, lips, tongue or other parts of the body
  • rash, itching or hives on the skin

Tamsulosin SR is for use by MEN only. If you are a woman or a child, do not take Tamsulosin SR. If you are not sure whether you should start taking Tamsulosin SR you should contact your doctor.

Do not take this medicine if you have or have had any of the following medical conditions:

  • you become dizzy or light-headed or have low blood pressure when you stand up, after sitting or lying down. This is called orthostatic hypotension
  • you have serious liver problems
  • you have serious kidney function problems
  • you are taking other medication which relaxes the smooth muscle of blood vessels (e.g. prazosin).

Do not take this medicine after the expiry date printed on the pack or if the packaging is torn or shows signs of tampering. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you start to take it

Tamsulosin SR does not treat prostate cancer. BPH and prostate cancer may have similar symptoms. A man can have prostate cancer and BPH at the same time. You should be checked for prostate cancer before you start Tamsulosin SR. It is recommended that men be checked for prostate cancer once a year, from 50 years of age onwards.

These checks should continue while you are on Tamsulosin SR.

Tell your doctor if you have allergies to any other medicines, foods, preservatives, or dyes including medicines containing sulfa.

Tell your doctor if you have or have had any of the following medical conditions:

  • angina (severe pain in the chest, usually on exertion) or have had a heart attack during the last six months
  • high, or low blood pressure, or your blood pressure is controlled by medication
  • ejaculation problems
  • are suffering from any other illness

Your doctor may want to take special care if you have any of these conditions.

Tell your doctor if you plan to have surgery. If you are going to have eye surgery for cataracts or glaucoma, please tell your surgeon that you are taking or have taken Tamsulosin SR.

If you have not told your doctor about any of the above, tell them before you start taking this medicine.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you get without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may be affected by this medicine or may affect how well it works. These include:

  • cimetidine, used to treat stomach ulcers or reflux.

Taking these medicines with Tamsulosin SR may increase the risk of possible side effects.

Other medications can also interfere with Tamsulosin SR and make you feel drowsy.

If you are not sure whether you are taking any of these medicines, check with your doctor or pharmacist.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

How to take this medicine

How much to take

Your doctor will tell you how many tablets you need to take each day and when to take them. This depends on your condition and whether you are taking any other medicines. It is important that you take this medicine as directed by your doctor.

The usual dose is one tablet a day.

Patients with severe liver or kidney problems should not take these tablets.

Continue taking your medicine for as long as your doctor tells you.

How to take this medicine

Swallow the tablets whole, preferably with a glass of water.

Do not crush, bite or chew the tablet, as this changes how this medicine works.

If you forget to take this medicine

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take the missed dose as soon as you remember, and then go back to taking your tablets as you would normally.

Do not take a double dose to make up for the dose that you missed. This may increase the chance of you getting an unwanted side effect.

If you are not sure what to do, ask your doctor or pharmacist.

If you take too much (overdose)

Immediately telephone your doctor or the Poisons Information Centre (telephone 13 11 26) or go to Accident and Emergency at your nearest hospital, if you think you or anyone else may have taken too much Tamsulosin SR. Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

If you take too many Tamsulosin SR tablets, this may result in vomiting, diarrhoea and low blood pressure leading to dizziness or fainting.

If you experience any of these symptoms, seek urgent medical attention.

While you are taking this medicine

Things you must do

Before starting any new medicine, tell your doctor or pharmacist that you are taking this medicine.

Tell all the doctors, dentists and pharmacists who are treating you that you are taking this medicine.

Tell your doctor if, for any reason, you have not taken your medicine exactly as prescribed. Otherwise your doctor may think it is not working effectively and change your treatment unnecessarily.

If you are going to have eye surgery for cataracts or glaucoma, please tell your surgeon that you are taking or have taken this medicine.

Things you must not do

Do not use this medicine to treat any other conditions unless your doctor tell you to.

Do not give this medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage without checking with your doctor.

Things to be careful of

Be careful when driving or operating machinery until you know how this medicine affects you. This medicine may cause dizziness and may impair your reactions.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking this medicine.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor if you notice any of the following and they worry you:

  • "retrograde ejaculation" – when this happens, the ejaculation fluid is not squirted out, most of it runs back into the bladder. Retrograde ejaculation is painless.
  • dizziness

Tell your doctor as soon as possible if you notice any of the following:

  • headache
  • skin rash (red spots or patches), itching, hives
  • weakness
  • dizziness on standing
  • nausea, vomiting, diarrhoea, constipation
  • fast heart beats
  • blocked nose
  • faintness

This medicine can occasionally cause people to feel faint and dizzy. You should get up slowly from the sitting or lying position to reduce the risk of dizziness or light-headedness. If you do feel faint on standing up, you should lie down for a short while. If the dizziness persists you should contact your doctor. You must not drive a car or operate machinery if you feel dizzy.

If you are having an operation on your eyes because of cataracts or glaucoma and are already taking or have taken this medicine, the pupil may dilate poorly and the iris (the coloured part of the eye) may become floppy during the procedure. This can be managed if your surgeon knows before carrying out the operation. If you are going to have eye surgery for cataracts or glaucoma, please tell your surgeon that you are taking or have taken this medicine.

This medicine may also occasionally cause blurred or reduced vision, inflammation and blistering of the skin and/or mucous membranes of the lips, eyes, mouth, nasal passages or genitals, or nose bleeds.

Tell your doctor immediately or go to Accident and Emergency at the nearest hospital if you notice any of the following:

  • prolonged painful erection of the penis, which is unrelated to sexual activity
  • symptoms of an allergic reaction including cough, shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue, throat or other parts of the body; rash, itching or hives on the skin

The above list includes very serious side effects. You may need urgent medical attention or hospitalisation. These side effects are very rare.

Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Other side effects not listed above may also occur in some people.

After using this medicine

Storage

Keep your tablets in the blister pack until it is time to take them.

Keep your tablets in a cool, dry place where the temperature stays below 25°C.

Do not store this medicine or any other medicine in the bathroom or near a sink.

Do not leave this medicine in a car or on windowsill. Heat and dampness can destroy some medicines.

Keep it where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking this medicine, or the expiry date has passed, ask your pharmacist what to do with any tablets that are left over.

Product description

What it looks like

BLOOMS THE CHEMIST TAMSULOSIN SR tablets

White to off-white round tablets with a diameter of approximately 9 mm, debossed with “TSLN” on one side and “0.4” on the other side. AUST R 313163.

Each pack contains 30 tablets.

Ingredients

This medicine contains 400 micrograms of tamsulosin hydrochloride as the active ingredient.

This medicine also contains the following:

  • microcrystalline cellulose
  • polyethylene oxide
  • magnesium stearate

This medicine does not contain gluten, lactose, sucrose, tartrazine or any other azo dyes.

Supplier

This medicine is supplied in Australia by:

Apotex Pty Ltd
16 Giffnock Avenue
Macquarie Park NSW 2113
Tel: (02) 8877 8333
Web: www1.apotex.com/au

This leaflet was last updated in May 2020.

Published by MIMS October 2020

BRAND INFORMATION

Brand name

Blooms the Chemist Tamsulosin SR

Active ingredient

Tamsulosin hydrochloride

Schedule

S4

 

1 Name of Medicine

Tamsulosin hydrochloride.

2 Qualitative and Quantitative Composition

Blooms the Chemist Tamsulosin SR modified release tablets contain the active ingredient tamsulosin hydrochloride.
Each Blooms the Chemist Tamsulosin SR modified release tablet contains 400 micrograms of tamsulosin hydrochloride.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Blooms the Chemist Tamsulosin SR 400 micrograms tablets are white to off-white round tablets with a diameter of approximately 9 mm, debossed with "TSLN" on one side and "0.4" on the other side.

4 Clinical Particulars

4.1 Therapeutic Indications

For the relief of lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH).

4.2 Dose and Method of Administration

One tablet daily.
The tablet must be swallowed whole and not be broken, crunched or chewed, as this compromises the modified release properties of the tablet for the active ingredient.
Blooms the Chemist Tamsulosin SR can be taken on an empty stomach, or before, with or after food.

4.3 Contraindications

Hypersensitivity, including drug induced angioedema to tamsulosin hydrochloride or any other component of the product.
A history of orthostatic hypotension.
Severe hepatic impairment (Child-Pugh scores > 9).
Severe renal impairment with creatinine clearance of less than 10 mL/min.
Concurrent use of another α1-adrenoceptor inhibitor.

4.4 Special Warnings and Precautions for Use

Syncope and postural hypotension.

Patients beginning treatment with Tamsulosin tablets should be cautioned to avoid situations where injury could result should syncope occur. Postural hypotension can occur during treatment with Tamsulosin tablets, but rarely results in syncope. However, the patient should be warned of this possibility and advised to sit or lie down if symptoms of hypotension should occur.

Exclusion of prostatic carcinoma and other urological conditions.

Carcinoma of the prostate and other conditions which can cause the same symptoms as benign prostatic hyperplasia should be excluded before starting therapy with Tamsulosin tablets. Digital rectal examination and, as considered appropriate, determination of prostate specific antigen should be performed before treatment and at regular intervals afterwards.

Myocardial ischaemia.

Patients with myocardial infarction or angina pectoris within the preceding six months were excluded from the Phase III clinical studies. As a result, the safety of Tamsulosin tablets in these patients has not been formally assessed.

Dizziness.

As Tamsulosin tablets may cause dizziness, patients should be warned to take care whilst operating machinery or driving.

Intra-operative floppy iris syndrome.

Intra-operative Floppy Iris Syndrome (IFIS) has been observed during cataract and glaucoma surgery in some patients taking or who have previously been treated with α1-adrenoceptor antagonists, including tamsulosin. This variant of small pupil syndrome is characterised by the combination of a flaccid iris that billows in response to intra-operative irrigation currents, progressive intra-operative miosis despite pre-operative dilation with standard mydriatic drugs, and potential prolapse of the iris toward the phaco-emulsification incisions.
During pre-operative assessment, ophthalmologists and ophthalmic teams should consider whether patients scheduled for cataract or glaucoma surgery are being, or have been, treated with α1-adrenoceptor antagonists in order to ensure that appropriate measures will be in place to manage IFIS during surgery if it occurs. The patient's ophthalmologist should be prepared for possible modifications to their surgical technique, such as the utilisation of iris hooks, iris dilator rings, or visco-elastic substances. The benefit of stopping α1-adrenoceptor antagonist therapy prior to cataract or glaucoma surgery has not been established.

Sulfa allergy.

Cases of allergic reaction to tamsulosin in patients with a past history of sulphonamide allergy have been reported. If a patient reports a sulfa allergy, caution is warranted when administering Tamsulosin tablets.

Use in hepatic impairment.

In a study of patients with moderate hepatic impairment, free tamsulosin levels remained unchanged after treatment with 400 micrograms tamsulosin hydrochloride in a sustained release capsule formulation when compared to normal subjects. Since the type of formulation will not affect the disposition of tamsulosin no dose adjustment for Tamsulosin tablets is expected in patients with mild to moderate hepatic impairment.
Severe hepatic impairment (Child-Pugh scores > 9) is a contraindication, see Section 4.3 Contraindications.

Use in renal impairment.

Severe renal impairment, with creatinine clearance of less than 10 mL/min is a contraindication, as these patients have not been studied, see Section 4.3 Contraindications.

Use in the elderly.

See Section 4.2 Dose and Method of Administration.

Paediatric use.

Blooms the Chemist Tamsulosin SR is not indicated for use in children.

Other populations.

Blooms the Chemist Tamsulosin SR is not indicated for use in women.

Effects on laboratory tests.

Interactions with laboratory tests have not been established.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Drugs known to interact with tamsulosin.

Concomitant cimetidine leads to a rise in plasma levels of tamsulosin, while furosemide leads to a fall (about 12% following a single 20 mg intravenous dose). However, as levels remain within the normal range, dosage need not be adjusted.
Concurrent administration of tamsulosin with other α1-adrenoceptor antagonists is contraindicated because of the potential for hypotensive effects, see Section 4.3 Contraindications.

Drugs which may interact with tamsulosin.

Tamsulosin binds extensively to plasma proteins and may displace other protein-bound drugs. Clinical trial data are not available.
No interactions at the level of hepatic metabolism have been seen during in vitro studies with liver microsomal fractions (representative of the cytochrome P450-linked drug metabolising enzyme system), involving amitriptyline, salbutamol, glibenclamide and finasteride. Diclofenac and warfarin, however, may increase the elimination rate of tamsulosin.

Drugs which do not interact significantly with tamsulosin.

Tamsulosin did not affect the pharmacokinetics of a single intravenous dose of digoxin 0.5 mg.
No interactions have been seen when tamsulosin hydrochloride was given concomitantly with either atenolol, enalapril, nifedipine or theophylline.

General.

Tamsulosin is metabolised in the liver, and may be expected to interact with other hepatically-metabolised drugs. Pharmacokinetic studies in healthy volunteers revealed that concomitant administration with strong inhibitors of CYP3A4 or CYP2D6 may lead to increased exposure to tamsulosin. Concomitant administration with ketoconazole (a known CYP3A4 inhibitor) resulted in an increased Cmax and AUC of tamsulosin. Tamsulosin 400 micrograms should not be used in combination with strong inhibitors of CYP3A4 in patients known to be CYP2D6 poor metabolizers. Concomitant administration with paroxetine (a known CYP2D6 inhibitor) resulted in an increased Cmax and AUC of tamsulosin. Tamsulosin should therefore be used with caution in patients who are taking other drugs, particularly those which undergo hepatic metabolism.

Other in vitro findings.

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.
An in vitro study using human liver microsomal fractions showed no effect of amitriptyline, salbutamol, glibenclamide and finasteride on the rate of disappearance of tamsulosin. The clinical relevance of these findings is uncertain.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

α-adrenoceptor antagonists are known to reduce male fertility by affecting penile erection, emission and/or ejaculation. In male rats, a severe reduction in male copulation rate and fertility was observed after a single dose or after repeated oral doses of tamsulosin. Spermatogenesis was not affected in the rat studies, and the effect on fertility was reversible. The no effect dose on male rat fertility was associated with plasma tamsulosin levels (AUC) at least 50% of those expected in human males treated with tamsulosin.
Treatment of female rats with tamsulosin caused disruption of the oestrus cycle and a severe reduction in fertility, due to interference of fertilisation with the ova. These effects were shown to be reversible.
(Category B2)
Tamsulosin is intended for use only in males.
Tamsulosin, at oral doses causing maternal toxicity, was not embryotoxic or teratogenic when administered during gestation in rats (doses up to 300 mg/kg/day) or rabbits (doses up to 50 mg/kg/day). However, administration of tamsulosin during the peri-/post-natal period was associated with a higher incidence of stillbirths and reduced pup weight gain after birth. No adverse effects on development or reproductive performance were observed on surviving pups, however, there is some evidence for impairment of offspring reproductive capacity when maternal treatment with tamsulosin is started before pregnancy.
 Tamsulosin is intended for use only in males.
In female rats, tamsulosin and/or its metabolites were shown to pass into milk after oral administration of the drug during lactation. The effect on the newborn is not known.

4.7 Effects on Ability to Drive and Use Machines

As Tamsulosin tablets may cause dizziness, patients should be warned to take care whilst operating machinery or driving.

4.8 Adverse Effects (Undesirable Effects)

Priapism.

Rarely, tamsulosin, like other alpha-1 antagonists, has been associated with priapism (persistent painful penile erection unrelated to sexual activity). Patients should be informed that this reaction is extremely rare, but if not brought to immediate medical attention, can lead to permanent erectile dysfunction.

Abnormal ejaculation.

Patients should be advised on the potential for abnormal ejaculation to occur upon commencement of Tamsulosin treatment. Retrograde ejaculation is the most commonly reported abnormal ejaculation event associated with the use of Tamsulosin tablets (see Table 1).

Clinical trials.

Table 4 shows the incidence of undesirable effects following 400 micrograms Tamsulosin tablet treatment. This data is based on a phase 3 clinical study in which there were no relevant differences between the treatment and placebo groups in the percentage of patients reporting at least 1 Treatment Emergent Adverse Event (TEAE). Most TEAEs were of mild or moderate intensity.
The most frequent TEAEs were ejaculation disorders. These are TEAEs that are often associated with α1-AR antagonists.
The following treatment-related adverse events were reported from clinical trials, where Common is ≥ 1% and < 10%; Uncommon is ≥ 0.1% and < 1%; Rare is ≥ 0.01% and < 0.1%; and Very rare is < 0.01%.

Cardiac disorders.

Uncommon: palpitations.

Gastro-intestinal disorders.

Uncommon: constipation, diarrhoea, nausea, vomiting.

General disorders.

Uncommon: asthenia.

Nervous system disorders.

Common: dizziness (1.3%), insomnia.
Uncommon: headache.
Rare: syncope.

Reproductive system disorders.

Common: ejaculation disorder.
Very rare: priapism.

Respiratory, thoracic and mediastinal disorders.

Uncommon: rhinitis.

Skin and subcutaneous tissue disorders.

Uncommon: rash, pruritus, urticaria.
Rare: angioedema.

Vascular disorders.

Uncommon: postural hypotension.

Post-marketing experience.

The following events have also been reported during the post-marketing period. These events are reported voluntarily from a population of uncertain size, therefore it is not possible to reliably estimate their frequency.

Vision disorders.

Blurred vision, vision impairment.
During cataract and glaucoma surgery, a variant of small pupil syndrome known as Intra-operative Floppy Iris Syndrome (IFIS) has been reported in association with α1-adrenoceptor antagonist therapy, see Section 4.4 Special Warnings and Precautions for Use, Intra-operative floppy iris syndrome.

Skin and subcutaneous tissue disorders.

Skin desquamation, dermatitis exfoliative, erythema multiforme, Stevens-Johnson syndrome, photosensitivity reaction.

Respiratory, thoracic and mediastinal disorders.

Epistaxis.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

Acute overdose with 5 mg tamsulosin hydrochloride has been reported. Acute hypotension (systolic blood pressure 70 mmHg), vomiting and diarrhoea were observed, which were treated with fluid replacement and the patient could be discharged the same day. If acute hypotension occurs after overdosage, cardiovascular support should be given and maintained. Blood pressure can be restored and heart rate brought back to normal by lying the patient down. If this is insufficient then volume expanders and, when necessary, vasopressors could be administered. 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.
Tamsulosin tablet is a modified release formulation. The signs and symptoms of overdose may be delayed or modified from the time of ingestion.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

The tone of the human prostate smooth muscle is maintained primarily by noradrenaline released from adrenergic nerves and stimulating post-junctional α1-adrenoceptors. This provides the rationale for the use of α1-adrenoceptor antagonists for lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH).
Pharmacological studies have established that tamsulosin is a selective, potent and competitive α1- adrenoceptor antagonist and that it has a greater affinity for the α1A-receptor subtype, predominantly present in the human prostate.
α1-adrenoceptor antagonists generally can reduce blood pressure by lowering peripheral resistance. However, no reduction in blood pressure of any clinical significance was observed during studies with Tamsulosin.
The binding of tamsulosin to α1-adrenoceptors in the prostate results in relaxation of prostate smooth muscle followed by improvements in urodynamics. Thus, Tamsulosin increases maximum urinary flow rate by reducing smooth muscle tension in the prostate and urethra and thereby relieving obstruction.
It also improves the symptoms related to bladder instability and tension of the smooth muscle of the lower urinary tract.
These effects on urinary storage and voiding symptoms are maintained during long-term therapy.
The need for surgery or catheterisation is significantly delayed.

Clinical trials.

The efficacy of Tamsulosin tablets has been evaluated in 2 randomised, placebo-controlled studies: the phase 2 dose-response study 617-CL-303 and the phase 3 study 617-CL-307. A total of 2962 patients were studied, of which 560 were treated with 0.4 mg of Tamsulosin tablets and 564 were treated with placebo. The remaining subjects were treated with 0.4 mg (capsules), 0.8 mg and 1.2 mg (tablets) doses of tamsulosin hydrochloride.

Inclusion criteria.

In both studies the inclusion criteria were: male patients aged ≥ 45 years, diagnosed as having lower urinary tract symptoms (LUTS) suggestive of BPH, with voiding/obstructive symptoms (including incomplete emptying of the bladder, intermittency, poor stream or hesitancy), and/or storage/irritative/filling symptoms (including daytime frequency, urgency or nocturia).
These patients had a total International Prostate Symptom Score (I-PSS) of ≥ 13, both at enrolment (Visit 1) and at baseline after the 2-week placebo run-in period (Visit 2). At enrolment, they also had to have a maximum flow rate (Qmax) of ≥ 4.0 mL/s and ≤ 12.0 mL/s, with a voided volume ≥ 120 mL during free flow.
Patients with cardiac ischaemia were excluded from participation in these trials. Safety in such patients has not been formally assessed.

Study 617-CL-303.

Study 617-CL-303 was a multi-center, double-blind, randomised, placebo-controlled, parallel group, dose-response study. In this study, 211 patients received placebo and 203 patients received 400 micrograms of Tamsulosin tablets once daily for 12 weeks of the double-blind randomised treatment. The results of study 617-CL-303 are summarised in Table 2.

Study 617-CL-307.

Study 617-CL-307 was a multi-center, double-blind, randomised, placebo and active-controlled, parallel group study. In this study, 353 patients received placebo and 357 patients received 400 micrograms of Tamsulosin tablets once daily for 12 weeks of the double-blind randomised treatment. The results of study 617-CL-307 are summarised in Table 3.
The primary efficacy parameter in both studies following 400 micrograms Tamsulosin treatment was the change from baseline to endpoint in total I-PSS scores. The secondary efficacy analyses contained the changes from baseline in voiding and storage I-PSS sub-scores, and I-PSS Quality of Life scores.
The I-PSS questionnaire was developed and validated by the American Urological Association (I-PSS previously called the AUA Symptom Index) and consisted of 7 questions evaluating the frequency of 7 urinary symptoms. These included 4 voiding symptoms (poor stream, hesitancy, intermittency and incomplete bladder emptying) and 3 storage symptoms (daytime frequency, nocturia and urgency). The patient rated each of the 7 symptoms on a scale of 0-5 of increasing symptom severity. The total score could therefore range from 0-35, the voiding sub-score from 0-20 and the storage sub-score from 0-15. The questionnaire was adopted by the World Health Organization, who added a further question assessing the impact of the urinary symptoms on the Quality of Life. The Quality of Life question asked how the patient would feel about his current level of symptoms for the rest of his life, ranging from 1 (delighted) to 6 (terrible).

5.2 Pharmacokinetic Properties

Absorption.

Tamsulosin is a modified release tablet of the non-ionic gel matrix type. The tamsulosin formulation provides consistent slow release of tamsulosin, which is maintained over the whole pH range encountered in the gastro-intestinal tract, resulting in an adequate exposure, with little fluctuation, over 24 hours.
Tamsulosin administered is absorbed from the intestine. Of the administered dose, approximately 55 to 59% is estimated to be absorbed. The rate and extent of absorption of tamsulosin hydrochloride administered as Tamsulosin tablets are only slightly affected by food, but this is unlikely to be clinically significant.
Tamsulosin hydrochloride administered as Tamsulosin tablets exhibits near linear pharmacokinetics (plasma concentrations Cmax and AUC vs dose) over the dosage range 0.4 mg through 0.8 mg to 1.2 mg once daily. Steady state is reached by day 4 of multiple dosing. The pharmacokinetics of a 400 micrograms once daily dose of tamsulosin hydrochloride as Tamsulosin tablets as a single dose under fasted conditions, and steady state under fed and fasted conditions, are shown in Table 4.
As a result of the modified release characteristic of Tamsulosin, the trough concentrations - at steady state, of tamsulosin hydrochloride in plasma amount to approximately 40% of the peak plasma concentrations, under fasted and fed conditions.
There is a considerable inter-patient variation in the plasma concentrations of tamsulosin hydrochloride, after both single and multiple dosing.

Distribution.

In man, tamsulosin is about 99% bound to plasma proteins. The volume of distribution is small (about 0.2 L/kg).

Metabolism.

Tamsulosin 400 ug modified release tablet contains tamsulosin as the R(-) isomer. In humans, there is no in vivo conversion to the less active S(+) isomer. Tamsulosin has a low first pass effect, being metabolised slowly. Most tamsulosin is present in plasma in the form of unchanged drug. Tamsulosin is metabolised in the liver. In vitro results suggest that CYP3A4 and also CYP2D6 are involved in metabolism, with possible minor contributions to tamsulosin metabolism by other CYP isozymes. Inhibition of hepatic drug metabolising enzymes may lead to increased exposure to tamsulosin, see Section 4.4 Special Warnings and Precautions for Use; Section 4.5 Interactions with Other Medicines and Other Forms of Interactions. In rats, tamsulosin was seen to cause minimal induction of microsomal liver enzymes. No dose adjustment is warranted in hepatic insufficiency, see Section 4.3 Contraindications.
None of the metabolites is more active than the original precursor compound.

Excretion.

Tamsulosin and its metabolites are mainly excreted in the urine. The amount excreted as unchanged drug is estimated to be about 4 - 6% of the dose administered as Tamsulosin.
No dose adjustment is warranted in renal impairment see Section 4.3 Contraindications.

5.3 Preclinical Safety Data

Genotoxicity.

In vivo and in vitro genotoxicity studies have been conducted.
Tamsulosin HCI produced no evidence of genotoxic potential in assays for gene mutation (Ames reverse mutation test and mouse lymphoma thymidine kinase assay), chromosomal damage (Chinese hamster ovary cells and mouse micronucleus assay) and other genotoxic effects (unscheduled DNA repair synthesis and in vivo sister chromatid exchange).

Carcinogenicity.

Reproduction toxicity studies in rats and carcinogenicity studies in mice and rats have been conducted. Oral (dietary) administration of tamsulosin for up to 2 years in rats and mice was associated with an increased incidence of pituitary adenoma, mammary gland hyperplasia, mammary gland fibroadenoma and (in mice only) mammary gland adenocarcinoma. These effects occurred at plasma tamsulosin concentrations (AUC) up to 10 times lower than those expected in men undergoing treatment with Tamsulosin, but they were observed only in female animals and are probably due to the hyperprolactinaemic effect of tamsulosin. It is not known if Tamsulosin elevates prolactin during modified administration in humans. The relevance for human risk of the findings of prolactin-mediated endocrine tumours in female rodents is unknown.

6 Pharmaceutical Particulars

6.1 List of Excipients

Blooms the Chemist Tamsulosin SR 400 micrograms modified release tablets contain the following inactive ingredients: microcrystalline cellulose, polyethylene oxide and magnesium stearate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Blooms the Chemist Tamsulosin SR 400 micrograms modified release tablets should be stored below 25°C and protect from light.

6.5 Nature and Contents of Container

Blooms the Chemist Tamsulosin SR is available in OPA/Al/PVC blister packs of 30 tablets.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Chemical Name: 5-[(2R)-2-[2-(2-ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide hydrochloride.
Molecular Formula: C20H29CIN2O5S.
Molecular Weight: 445.0.

CAS number.

106463-17-6.

7 Medicine Schedule (Poisons Standard)

S4 (Prescription Only Medicine).

Summary Table of Changes