Tamsulosin hydrochloride is an alpha-1A and alpha-1D adrenoceptor antagonist used to treat benign prostatic hyperplasia by relaxing smooth muscles in the prostate and bladder. It is administered orally and works by selectively blocking alpha-1A and alpha-1D receptors, improving urinary flow. Common side effects include dizziness, headache, and diarrhea. Due to its selectivity, tamsulosin has fewer cardiovascular side effects than older non-selective alpha-blockers but can still cause hypotension. It is contraindicated in patients with orthostatic hypotension or taking other alpha-blockers and interactions may occur with cimetidine or sildenafil.

1. DRUG PRESENTATION
TAMSULOSIN
HYDROCHLORIDE
Presented by :
Dakshta
MSc. (N) 1st Year
Date – 16th Sept’2021

2. CONTENTS
• Introduction
• Chemical name
• Chemical formula
• Structure
• Generic name
• Trade name
• Available forms
• Classification
• Uses
• Mechanism of Action
• Indications
• Contraindications
• Route and Dosage
• Pharmacodynamics
• Pharmacokinetics
• Adverse Effects
• Toxicity
• Drug Interactions
• Nursing Implications

3. INTRODUCTION
• Tamsulosin is a selective alpha-1A and alpha-1D adrenoceptor antagonist that exerts its greatest
effect in the prostate and bladder, where these receptors are most common.
• It is indicated for treating the signs and symptoms of benign prostatic hypertrophy. Antagonism
of these receptors leads to relaxation of smooth muscle in the bladder trigone, sphincter and
prostate, allowing for better urinary flow.
• Other alpha-1 adrenoceptor antagonists developed in the 1980s were less selective and more
likely to act on the smooth muscle of blood vessels, resulting in hypotension. For eg. Prazosin
and Terazosin.
• Tamsulosin was first approved by the FDA on April 15, 1997.

4. Chemical Name –
• 5-[(2R)-2-[2-(2-ethoxyphenoxy)ethylamino]propyl]-2-
methoxybenzenesulfonamide;hydrochloride
Chemical Formula –
• C20H28N2O5S
Structure –
Generic Name –
• Tamsulosin hydrochloride
Trade Names –
• Flomax, Jalyn, Contiflo, Urimax, Dynapres

5. Available forms –
0.2 mg capsules
0.4 mg capsules

6. • Classification
Sympatholytics
( alpha and beta Blockers)
Alpha blockers
Non-selective Alpha-1 selective
(Phenoxybenzamine, (Prazosin, Terazosin
Phentolamine) Tamsulosin)

7. • Uses of Alpha Blockers
Hypertension – Prazosin, Terazosin
Pheochromocytoma – diagnosis (Phentolamine)
treatment (Phenoxybenzamine)
BPH – Tamsulosin
CHF – Prazosin
Secondary Shock – Phenoxybenzamine, Prazosin
PVD – Phenoxybenzamine, Prazosin

8. MECHANISM OF ACTION
• Tamsulosin is a blocker of alpha-1A and alpha-1D adrenoceptors. About
70% of the alpha-1 adrenoceptors in the prostate are of the alpha-1A
subtype. By blocking these adrenoceptors, smooth muscle in the prostate is
relaxed and urinary flow is improved.
• The blocking of alpha-1D adrenoceptors relaxes the trigone smooth muscles
of the bladder which prevents storage symptoms. The specificity of
tamsulosin focuses the effects to the target area while minimizing effects in
other areas.

9. Continued…

10. Continued…

11. INDICATIONS
• For symptoms of Benign prostatic hyperplasia.
difficulty urinating (hesitation, dribbling, weak stream, and incomplete bladder
emptying)
painful urination
urinary frequency and urgency.
• Prostatitis
• Ureteral stones
• Urethral stricture

12. CONTRAINDICATIONS
• Orthostatic hypotension
• Cataract surgery
• Hypersensitivity to tamsulosin
• In conjunction with another alpha1A-adrenergic blocking agent
• Lactation
• Pediatric patients
Cautious use –
• Pregnancy (category B)
• History of Syncope and hypotension

13. ADMINISTRATION
Oral route:
• Give 30 min after the meal each day.
• Instruct to swallow capsules whole; not to crush, chew, or open.
• If dose is interrupted for several days, reinitiate at the lowest dose, 0.4 mg.
• Store at 20°–25° C (68°–77° F).
DOSAGE
Adult Dose:
PO 0.4 mg q.i.d. 30 min after a meal, may increase up to 0.8 mg q.i.d.

14. PHARMACODYNAMICS
Tamsulosin is an alpha adrenoceptor blocker with specificity for the alpha-1A and
alpha-1D subtypes, which are more common in the prostate and submaxillary
tissue. The final subtype, alpha-1B, are most common in the aorta and
spleen. Tamsulosin binds to alpha-1A receptors 3.9-38 times more selectively than
alpha-1B and 3-20 times more selectively than alpha-1D. This selectivity allows for a
significant effect on urinary flow with a reduced incidence of adverse reactions like
orthostatic hypotension.

15. PHARMACOKINETICS
Absorption
• Rapidly absorbed from GI tract.
• The maximum plasma concentration is 3.1-5.3ng/mL for a 0.4mg oral dose and 2.5-3.6ng/mL
for a 0.8mg oral dose.
• >90% bioavailability.
Peak
• 4–5 hr. fasting
• 6–7 hr. fed
Volume of Distribution
• 16L after intravenous administration.
• Widely distributed in body tissues, including kidney and prostate

16. Continued…
Protein Binding
• Tamsulosin is 94%-99% protein bound, mostly to alpha-1-acid glycoprotein.
Metabolism
• Tamsulosin is mostly metabolized in the liver by cytochrome P-450 (CYP) 3A4
and 2D6, with some metabolism by other CYPs.
Route of Elimination
97% of an orally administered dose is recovered in studies, which 76% in the urine
and 21% in the feces after 168 hours.

17. Continued…
• Half Life
The apparent half life is 14-15 hours.
• Clearance
2.88L/h.

18. ADVERSE EFFECTS
Body as a Whole:
• Asthenia, back or chest pain
CNS:
• Headache, Dizziness,
insomnia
CVS:
• Orthostatic hypotension
(especially with first dose)
GI:
Diarrhea, Nausea
Respiratory:
Rhinitis, pharyngitis, increased cough,
sinusitis
Urogenital:
Decreased libido, abnormal ejaculation
Special Senses:
Amblyopia.

19. TOXICITY
• Hypotension
In the event of overdose, patients may experience hypotension and should lie down in a
supine position to maintain blood pressure and heart rate.
If further measures are required intravenous fluids should be considered.
If further progression is required, vasopressors may be used and renal function should be
monitored.
Dialysis is unlikely to assist in treating overdose because tamsulosin is extensively protein
bound.
• Carcinogenic
Tamsulosin is not mutagenic but may be carcinogenic at levels above the maximum
recommended human dose.
• Fertility problems
In men, tamsulosin is associated with abnormal ejaculation.

20. DRUG INTERACTIONS
• Acetaminophen - Acetaminophen may decrease the excretion rate of Tamsulosin which
could result in a higher serum level.
• Acetazolamide – Acetazolamide may increase the excretion rate of Tamsulosin which could
result in a lower serum level and potentially a reduction in efficacy.
• Chlorpropamide - The therapeutic efficacy of Chlorpropamide can be increased when used
in combination with Tamsulosin.
• Cimetidine may decrease clearance of tamsulosin.
• Sildenafil, vardenafil, and tadalafil may enhance hypotensive effects.
Food Interactions
Take after a meal. Take 30 minutes after the same meal each day to reduce plasma level
variations.

21. MISSED DOSE OF TAMSULOSIN
• If a dose of tamsulosin is missed, it should be taken immediately as long as it is not too close
to bed time or to the usual time of taking next dose.
• In case it is the time for next dose, then usual schedule should be resumed missing that dose.
It’s dose shouldn’t be doubled up to make up for the missed dose.

22. NURSING IMPLICATIONS
Assessment & Drug Effects
•Monitor for signs of orthostatic hypotension; take BP lying down, then upon standing. Report a systolic pressure drop
of 15 mm Hg or more and a HR of 15 beats or more upon standing.
•Monitor patients on warfarin therapy closely.
Patient & Family Education
• Make position changes slowly to minimize orthostatic hypotension.
• Report dizziness, vertigo, or fainting to physician. Exercise caution with hazardous activities until response to drug is
known.
• Be aware that concurrent use of cimetidine may increase the orthostatic hypotension adverse effect of Tamsulosin.
• Advise patient that urinary symptoms (retention, dribbling, hesitancy, urgency) should improve, and to contact the
physician if these symptoms continue to worsen.
• Instruct patient or family/caregivers to report other bothersome side effects such as severe or prolonged headache,
nasal irritation, or problems with ejaculation.

23. Clinical trials
The phase 4 clinical trials has been completed for Tamsulosin for it to be used safely for :
• the prevention of Post Operative Urinary Retention (POUR).
• the treatment of BPH, of Kidney and Ureteral stones.
• the treatment of Lower Urinary Tract Symptoms (LUTS).

24. RELATED RESEARCH ARTICLE
A research was conducted by Yoshinori Nishino et al, published on 9th March’ 2006 to
compare the efficacy of two α1-adrenoceptor antagonists, α1A-adrenoceptor-selective
tamsulosin hydrochloride and α1D-adrenoceptor-selective naftopidil, in the treatment of lower
urinary tract symptoms (LUTS) with benign prostatic hyperplasia (BPH).
34 patients with LUTS secondary to BPH were enrolled in a randomized crossover study. 17
patients were initially prescribed naftopidil 50 mg for 4 weeks, followed by tamsulosin 0.2 mg
for 4 weeks (group A); another 17 were initially prescribed tamsulosin 0.2 mg, followed by
naftopidil 50 mg (group B).
It was concluded that, the two agents provided similar efficacy in the treatment of LUTS with
BPH. However, naftopidil was better than tamsulosin for nocturia. The disappearance of
involuntary contraction and the greater increase in first-desire volume with naftopidil may be
associated with the relief of nocturia. The α1D-adrenoceptor antagonist is effective in
alleviating both voiding and storage symptoms. The α1D-adrenoceptor antagonist may be more
effective than the α1A-adrenoceptor antagonist in LUTS with BPH.

25. Summary
In today’s drug presentation, we discussed all the characteristics and specifications of the drug TAMSULOSIN
HYDROCHLORIDE. We covered its introduction, chemical name, chemical formula, structure, generic name,
trade name, available forms, classification, uses, mechanism of action, indications, contraindications, route and
dosage.
Conclusion
Tamsulosin hydrochloride is an Alpha 1 adrenergic receptor blocker drug which is routinely used in urology
department for relieving the symptoms associated with BPH and other obstructive uropathies i.e. prostatitis,
ureteral stones or urethral strictures.

26. BIBLIOGRAPHY
• KD Tripathi; Essentials of Medical Pharmacology 7th Edition. New Delhi; Jaypee
Publications, 2014, Pg no. 144-146.
• Williams and Wilkins; Nursing Drug Handbook 41st Edition; Philadephia; Walters Kluwer
Publications, 2021, Pg no. 342-348.
• Wishart DS, Feunang YD, Guo AC, Wilson M. Drug Bank 5.0 : A major update to the Drug
Bank database for 2018. Nucleic acids Res. 2017 Nov 8. Available from :
https://go.drugbank.com/drugs/DB00706.
• Tamsulosin hydrochloride ; No date. Available from :
https://www.robholland.com/Nursing/Drug_Guide/data/monographframes/T005.html.