Tamsulosin (Flomax) is an alpha-adrenergic receptor inhibitor. Since alpha receptors are mostly present in the lower urinary system, tamsulosin primarily causes smooth muscle relaxation in the bladder and prostate. It causes an increase in urinary flow by relaxing the smooth muscles of the lower urinary tract. It is used to treat the following conditions:
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Benign prostatic hyperplasia:
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It is used in the treatment of signs and symptoms of benign prostatic hyperplasia (BPH)
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It is not indicated for the treatment of hypertension.
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Off Label Use of Tamsulosin in Adults:
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It is also used in the following conditions:
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Chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) in males;
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Lower urinary tract symptoms (LUTS) in males;
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Ureteral calculi expulsion;
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Ureteral stent-related urinary symptoms, treatment
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Tamsulosin (Flomax) dose in Adults
- Tamsulosin capsules should be given ~30 minutes following the same meal each day.
Dose in the treatment of Benign prostatic hyperplasia (BPH):
- Capsule: Initial and Maintenance:
- 0.4 mg once daily given.
- If the response is inadequate after 2 to 4 weeks, then increase to 0.8 mg once daily.
- If therapy is stopped or interrupted for several days, restart with 0.4 mg once daily.
- The controlled-release tablet is given at 0.4 mg once daily
Dose in the treatment of chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) in males (off-label):
- Oral: Initial:
- 0.4 mg once daily given in combination with antibiotic treatment
- an antibiotic is given for the initial 6 weeks
- If a response to initial therapy is inadequate, referral to a urologist is recommended
Dose in the treatment of lower urinary tract symptoms (LUTS) in males (off-label):
- Bladder outlet obstruction (BOO) and low postvoid residual (PVR):
- Oral: Initial:
- 0.4 mg once daily given
- It can be combined with an anticholinergic agent if symptoms of an overactive bladder persist
Dose in the treatment of Ureteral calculi expulsion (off-label):
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Medical expulsive therapy (MET) to facilitate the passage of lower ureteral calculi:
- Stones >5 and ≤10 mm: Oral:
- 0.4 mg once daily given until stone passage occurs or for up to 4 weeks.
- Stones >5 and ≤10 mm: Oral:
-
Adjunctive therapy following shock wave lithotripsy to facilitate the clearance of residual stones:
- 0.4 mg once daily given
- start therapy immediately after extracorporeal shock wave lithotripsy
- duration of therapy in trials ranged from 14 days to 3 months
Dose in the treatment of Ureteral stent-related urinary symptoms, treatment (off-label):
- 0.4 mg once daily given
Tamsulosin (Flomax) dose in Children
Dose in the treatment of distal stones Nephrolithiasis:
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Children 2 to 4 years:
- Oral: 0.2 or 0.4 mg once daily given at bedtime
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Children >4 years and Adolescents:
- Oral: 0.4 mg once daily given at bedtime
Dose in the treatment of Primary bladder neck dysfunction:
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Children ≥3 years and Adolescents:
- Oral: Initial dose:
- 0.2 mg once daily given
- increase by 0.2 mg increments according to response (symptoms and urodynamic studies) and tolerability.
- The mean effective dose is 0.4 mg daily
- maximum reported daily dose is 0.8 mg/day.
- Oral: Initial dose:
Tamsulosin (Flomax) Pregnancy Risk Factor: C
- There is insufficient information on the use of Tamsulosin to treat ureteral calculi during pregnancy
- If stone removal is required, other treatments like stents and ureteroscopy are recommended.
Tamsulosin (Flomax) dose in kidney disease:
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CrCl ≥10 mL/minute:
- No dosage adjustment is required.
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CrCl <10 mL/minute:
- There are no dosage adjustments given in the manufacturer’s labeling (has not been studied).
Tamsulosin (Flomax) dose in Liver disease:
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Mild-to-moderate impairment:
- No dosage adjustment is required.
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Severe impairment:
- There are no dosage adjustments given in the manufacturer’s labeling (has not been studied).
Common Side Effects of Tamsulosin (Flomax) Include:
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Cardiovascular:
- Orthostatic Hypotension
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Central Nervous System:
- Headache
- Dizziness
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Genitourinary:
- Ejaculation Failure
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Infection:
- Infection
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Respiratory:
- Rhinitis
Less Common Side Effects of Tamsulosin (Flomax) Include:
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Central Nervous System:
- Drowsiness
- Insomnia
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Vertigo
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Endocrine & Metabolic:
- Loss Of Libido
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Gastrointestinal:
- Diarrhea
- Nausea
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Neuromuscular & Skeletal:
- Weakness
- Back Pain
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Ophthalmic:
- Blurred Vision
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Respiratory:
- Pharyngitis
- Cough
- Sinusitis
Contraindications to Tamsulosin Include:
- Hypersensitivity to Tamsulosin, or any component of it, can result in angioedema and rash.
- Use with strong CYP3A4 inhibitors (including ketoconazole) concurrently
Warnings and precautions
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Angina
- Stop if you feel that your symptoms of angina are getting worse.
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Floppy iris syndrome:
- IFIS was seen in patients undergoing cataract or glaucoma surgery who had been on alpha-blockers. This included tamsulosin.
- It has not been proven that stopping alpha-blocker therapy before cataract or glaucoma surgery is beneficial.
- IFIS may increase the likelihood of ocular complications after and during surgery.
- It might be necessary to modify the surgical procedure. Instruct patients to tell their ophthalmologist about any alpha-blocker or current use before considering eye surgery.
- Patients with planned cataract surgery or glaucoma are not advised to initiate tamsulosin treatment.
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Syncope/orthostatic hypotension:
- It may cause significant orthostatic hypotension and syncope, especially with the first dose; anticipate a similar effect if therapy is stopped for a few days, if the dosage is rapidly increased, or if another antihypertensive drug (particularly vasodilators) or a PDE-5 inhibitor (eg, sildenafil, tadalafil, vardenafil) is introduced.
- The "first dose" of orthostatic hypotension is 4-8 hours after dosing. It may also be dose-related.
- When initiating new therapies or increasing dosages, patients should be cautious about driving or performing dangerous tasks.
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Priapism
- Rarely, was Priapism seen in conjunction with drug use.
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Allergy to sulfonamide
- Rarely, do patients with a sulfa allergy also develop an allergic reaction to Tamsulosin.
- Avoid using it if the reaction is severe or life-threatening.
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Heart failure:
- Tamsulosin was found to be an agent that can exacerbate myocardial dysfunction.
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Prostate cancer:
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Screening for prostatic carcinoma is strongly recommended before beginning therapy. Then, screen regularly.
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Tamsulosin: Drug Interaction
Risk Factor C (Monitor therapy) |
|
Alpha-/Beta-Agonists |
Alpha1-Blockers may diminish the vasoconstricting effect of Alpha-/BetaAgonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. |
Alpha1-Agonists |
Alpha1-Blockers may diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. |
Antipsychotic Agents (Second Generation [Atypical]) |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). |
Aprepitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Barbiturates |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Benperidol |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Beta-Blockers |
May enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Exceptions: Levobunolol; Metipranolol. |
Blood Pressure Lowering Agents |
May enhance the hypotensive effect of Hypotension-Associated Agents. |
Bosentan |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Brimonidine (Topical) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Calcium Channel Blockers |
Alpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers. |
Cimetidine |
May increase the serum concentration of Tamsulosin. |
Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
CYP2D6 Inhibitors (Moderate) |
May increase the serum concentration of Tamsulosin. |
CYP2D6 Inhibitors (Strong) |
May increase the serum concentration of Tamsulosin. |
CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
CYP3A4 Inhibitors (Moderate) |
May increase the serum concentration of Tamsulosin. |
Dapoxetine |
May enhance the orthostatic hypotensive effect of Alpha1-Blockers. |
Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Diazoxide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
DULoxetine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. |
Duvelisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Erdafitinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Fosaprepitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Fosnetupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Herbs (Hypotensive Properties) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Hypotension-Associated Agents |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. |
Ivosidenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Larotrectinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Levodopa-Containing Products |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. |
Lormetazepam |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Molsidomine |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Netupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Nicorandil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Nitroprusside |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. |
Palbociclib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Pentoxifylline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Pholcodine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. |
Phosphodiesterase 5 Inhibitors |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Phosphodiesterase 5 Inhibitors |
Alpha1-Blockers (Uroselective) may enhance the hypotensive effect of Phosphodiesterase 5 Inhibitors. |
Prostacyclin Analogues |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Quinagolide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Rilmenidine |
Alpha1-Blockers may enhance the hypotensive effect of Rilmenidine. |
Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Simeprevir |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
Risk Factor D (Consider therapy modification) |
|
Amifostine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. |
CYP3A4 Inducers (Strong) |
May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
Dabrafenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
Enzalutamide |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. |
Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
Mitotane |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
Obinutuzumab |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. |
Pitolisant |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Combined use of pitolisant with a CYP3A4 substrate that has a narrow therapeutic index should be avoided. Other CYP3A4 substrates should be monitored more closely when used with pitolisant. |
St John's Wort |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
Risk Factor X (Avoid combination) |
|
Alpha1-Blockers |
May enhance the antihypertensive effect of other Alpha1-Blockers. |
Bromperidol |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. |
Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
CYP3A4 Inhibitors (Strong) |
May increase the serum concentration of Tamsulosin. |
Fusidic Acid (Systemic) |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Monitor:
- Blood pressure
- urinary symptoms
How to administer Tamsulosin (Flomax)?
- Give capsules 30 minutes after the same mealtime each day.
- Capsules should be swallowed whole
- do not crush, chew, or open.
- The controlled-release tablet should be administered at the same time each day with or without food and should be swallowed whole.
Mechanism of action of Tamsulosin:
- Tamsulosin blocks alpha-adrenoreceptors from the prostate.
- Alpha-adrenoreceptors maintain the tone of the prostate's smooth muscles.
- Blocking them causes relaxation of the bladder neck and prostate, which results in improved urine flow and reduced symptoms of BPH.
- About 75% of alpha-receptors found in the prostate belong to the alpha subtype.
Absorption:
- >90%
Distribution: V :
- 16 L
Protein binding:
- protein binding is 94% to 99%, primarily to alpha-1 acid glycoprotein (AAG)
Metabolism:
- Mainly Hepatic (extensive) via CYP3A4 and 2D6; metabolites undergo extensive conjugation to glucuronide or sulfate
Bioavailability:
- Fasting: 30% increase
- Steady-state: By the fifth day of once-daily dosing
Half-life elimination:
- Healthy volunteers: 9 to 13 hours
- Target population: 14 to 15 hours
Time to peak:
- Fasting: 4 to 5 hours
- With food: 6 to 7 hours
Excretion:
- Via Urine (76%, <10% as unchanged drug); feces (21%)
International Brands of Tamsulosin:
- APO-Tamsulosin CR
- Flomax CR
- MYLAN-Tamsulosin
- RATIO-Tamsulosin
- SANDOZ Tamsulosin
- SANDOZ Tamsulosin CR
- TEVA-Tamsulosin
- TEVA-Tamsulosin CR
- Adenorm
- Alna
- Bazetham
- Bestflo
- Comadex
- Contiflo OD
- Curepro XR
- Eziflo
- Flectone XL
- Flomax
- Flomaxtra
- Flomaxtra XL
- Flosin
- Flosure
- Fokusin
- Harnal
- Harnal D
- Harnal OCAS
- Harnalidge D
- Harusin SR
- Inreq
- Josir
- Kirnom
- Libert
- Losiprost
- Lostam
- Lutsnal
- Maxflow
- Maxrin
- Mecir LP
- Mingo
- Omexel LP
- Omic
- Omix Ocas
- Omnexel
- Omnic
- Omnic OCAS
- Omnic Tocas
- Omsal
- Petyme
- Pimax
- Pinexel PR
- Promnix
- Prosta-Tab PR
- Prozelax
- Ranomax
- Sasolin
- Sebrane
- Secotex
- Secotex OCAS
- Sulosin
- Sultam
- Tabphyn MR
- Talusin
- Tamic
- Tamlosin
- Tamlosin SR
- Tamnexyl
- Tamodof
- Tamsin
- Tamsnal SR
- Tamsol
- Tamsu
- Tamsulid
- Tamsulin
- Tamsulo
- Tamsulon
- Tamsustad
- Tamunal
- Tarunal
- Urimax
- Urnal
- Uroflo
- Uroflow
- Urostad
- Urotams SR
- Xalgetz
- Zotan
- Zuantrip
Tamsulosin (Flomax) Brands in Pakistan:
Tamsulosin Hydrochloride [Susp 0.4 Mg] |
|
Kolac | Asian Continental (Pvt) Company |
Tamsulosin Hydrochloride [Tabs 0.4 Mg] |
|
Flosure | Ferozsons Laboratoies Ltd. |
Tamsol-D | Global Pharmaceuticals |
Tamsulosin Hydrochloride [Caps 0.2 Mg] |
|
Maxiflo | Ferozsons Laboratoies Ltd. |
Sintam | Hilton Pharma (Pvt) Limited |
Uroflo | Novartis Pharma (Pak) Ltd |
Tamsulosin Hydrochloride [Caps 0.4 Mg] |
|
Alfamax | Platinum Pharmaceuticals (Pvt.) Ltd. |
Easypas | Valor Pharmaceuticals |
Easypas | Valor Pharmaceuticals |
Eziflo | Asian Agencies |
Healpros Sr | Cirin Pharmaceuticals (Pvt) Ltd. |
Maxflow | Consolidated Chemical Laboratories (Pvt) Ltd. |
Maxron | Navegal Laboratories |
Maylan | Mcolson Research Laboratories |
Optiflo | Hansel Pharmacueutical Pvt (Ltd) |
Prostam | Highnoon Laboratories Ltd. |
Prostreat | Asian Continental (Pvt) Company |
Sydapros | Sayyed Pharmaceuticals |
Tamsol | Global Pharmaceuticals |
Tamsolin | Getz Pharma Pakistan (Pvt) Ltd. |
Tamsomax | Tagma Pharma (Pvt) Ltd. |
Tamusin | Adcare Pharma |
Tamusin | Aims Pharmaceuticals |
Uflo | Noa Hemis Pharmaceuticals |
Uriflow | Mission Pharmaceuticals |
Uroflo | Novartis Pharma (Pak) Ltd |
Tamsulosin Hydrochloride [Caps Sr 0.4 Mg] |
|
Talsin | Pharmedic (Pvt) Ltd. |
Tamflo | Foray Pharmaceuticals |