Tamsulosin

Tamsulosin Uses, Dosage, Side Effects, Food Interaction and all others data.

Tamsulosin is an antagonist of α1A-adrenoreceptors in the prostate. It binds selectively and competitively to postsynaptic α1A-adrenoreceptors, which convey smooth muscle contraction, thereby relaxing prostatic and urethral smooth muscle.

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.

Trade Name Tamsulosin
Availability Prescription only
Generic Tamsulosin
Tamsulosin Other Names Tamsulosin, Tamsulosina, Tamsulosine, Tamsulosinum
Related Drugs finasteride, Flomax, prazosin, tadalafil, doxazosin, Cialis
Weight 400mcg, , 0.4mg
Type Capsule Medlife Pure Generics, + Dutasteride Tablet Medlife Pure Generics, Slow Release Tablet, Capsule
Formula C20H28N2O5S
Weight Average: 408.512
Monoisotopic: 408.171892706
Protein binding

Tamsulosin is 94%-99% protein bound, mostly to alpha-1-acid glycoprotein.

Groups Approved, Investigational
Therapeutic Class BPH/ Urinary retention/ Urinary incontinence
Manufacturer Tulip Lab Pvt Ltd, Novell Pharmaceutical Lab, Bharat Parenterals Limited, Pell Tech Health Care Pvt Ltd
Available Country India, United States, Indonesia, Switzerland, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Tamsulosin
Tamsulosin

Uses

Tamsulosin Hydrochloride is used for the treatment of the signs and symptoms of Benign Prostatic Hyperplasia (BPH).

Tamsulosin is also used to associated treatment for these conditions: Benign Prostatic Hyperplasia (BPH), Benign Prostatic Hypertrophy, Bladder Outlet Obstruction, Ureteral Calculus

How Tamsulosin works

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 detrusor 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.

Dosage

Tamsulosin dosage

The recommended dose of Tamsulosin is 0.4 mg once daily. It should be administered approximately half/hour following the same meal each day. For those patients who fail to respond to the 0.4 mg dose after two to four weeks of dosing, the dose of Tamsulosin can be increased to 0.8mg once daily. If Tamsulosin 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.

Side Effects

The following adverse reactions have been reported during the use of Tamsulosin: dizziness, abnormal ejaculation, and less frequently (1-2%) headache, asthenia, postural hypotension, palpitations, and rhinitis.

Gastrointestinal reactions such as nausea, vomiting, diarrhoea, and constipation can occasionally occur. Hypersensitivity reactions such as rash, pruritus, and urticaria can occur occasionally. As with other alpha-blockers, drowsiness, blurred vision, dry mouth, or edema can occur. Syncope has been reported rarely, and there have been very rare reports of angioedema and priapism.

Toxicity

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.

The oral LD50 in rats is 650mg/kg.

Tamsulosin is not indicated for use in women and no studies have been performed in pregnancy, though animal studies have not shown fetal harm. Tamsulosin is excreted in the milk of rats but there is no available data on what the effect of this tamsulosin exposure may be. Animal studies have shown male and female rat fertility is affected by tamsulosin due to impairment of ejaculation and fertilization. In men, tamsulosin is associated with abnormal ejaculation. Tamsulosin is not mutagenic but may be carcinogenic at levels above the maximum recommended human dose. Female rats experience a slight increase in the rates of mammary gland fibroadenomas and adenocarcinomas.

Precaution

Not indicated for use in women. Severe renal impairment (CrCl <10 mL/min). Pregnancy and lactation.

Interaction

Increased plasma concentration with strong CYP3A4 inhibitors (e.g. ketoconazole). Moderate CYP3A4 inhibitors (e.g. erythromycin), strong (e.g. paroxetine) or moderate (e.g. terbinafine) CYP2D6 inhibitors may increase exposure of tamsulosin. Increased plasma concentration with cimetidine. Additive effect with other α-adrenergic blocking agents. Concomitant use with PDE5 inhibitors may lead to symptomatic hypotension. Decreased plasma concentration with furosemide.

Food Interaction

  • Take after a meal. Take 30 minutes after the same meal each day to reduce plasma level variations.

[Moderate] ADJUST DOSING INTERVAL: Food may delay the gastrointestinal absorption of tamsulosin.

The time to maximum plasma concentration (Tmax) is reached by 4 to 5 hours under fasted conditions and by 6 to 7 hours when tamsulosin is administered with food.

The delay in Tmax has the desirable effect of smoothing the tamsulosin plasma concentration profile, thereby reducing fluctuation of the plasma peak and trough concentrations with multiple dosing.

Food may also affect the extent of absorption of tamsulosin.

It has been reported that taking tamsulosin under fasted conditions results in a 30% increase in bioavailability (AUC) and 40% to 70% increase in peak plasma concentration (Cmax) compared to fed conditions.

The effects of food on the pharmacokinetics of tamsulosin are consistent regardless of whether tamsulosin is taken with a light meal or a high-fat meal.

MANAGEMENT: To ensure uniformity of absorption, tamsulosin should be administered approximately one-half hour following the same meal each day.

Tamsulosin Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of ethanol and alpha-1 adrenergic blockers may cause increased hypotensive effects.

Patients with aldehyde dehydrogenase deficiencies (primarily Asians) may be at a higher risk of this interaction.

The mechanism has not been determined.

Data exist for prazosin and other alpha adrenergic blockers are expected to interact also.

In addition, any patients taking alpha adrenergic blockers may experience excessive orthostatic hypotension with ethanol ingestion, due to ethanol's unopposed vasodilatory effects in the presence of alpha adrenergic blockade.

Patients who develop

a flushing reaction after ethanol ingestion (indicates a possible aldehyde dehydrogenase deficiency) should be advised to avoid ethanol or limit their intake.

All patients should be warned about the possibility of orthostatic hypotension with concurrent ethanol use.

Volume of Distribution

16L after intravenous administration.

Elimination Route

Oral tamsulosin is 90% absorbed in fasted patients. The area under the curve is 151-199ng/mL*hr for a 0.4mg oral dose and 440-557ng/mL*hr for a 0.8mg oral dose. 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. Taking tamsulosin with food increases the time to maximum concentration from 4-5 hours to 6-7 hours but increases bioavailability by 30% and maximum plasma concentration by 40-70%.

Half Life

The half life in fasted patients is 14.9±3.9 hours. The elimination half life is 5-7 hours and the apparent half life is 9 to 13 hours in healthy subjects. In patients who require tamsulosin, the apparent half life is 14-15 hours.

Clearance

2.88L/h.

Elimination Route

97% of an orally administered does is recovered in studies, which 76% in the urine and 21% in the feces after 168 hours. 8.7% of the dose is excreted as unmetabolized tamsulosin.

Pregnancy & Breastfeeding use

Tamsulosin Hydrochloride capsules are not indicated for use in women.

Contraindication

History of orthostatic hypotension. Severe hepatic impairment.

Special Warning

Tamsulosin Hydrochloride capsules are not indicated for use in pediatric populations.

Acute Overdose

As overdose of Tamsulosin Hydrochloride capsules lead to hypotension, support the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in supine position. If this measure is inadequate, then administration of intravenous fuid should be considered. Measures, such as emesis, can be taken to impede absorption. When large quantities are involved, gastric lavage can be applied and activated charcoal and an osmotic laxative, such as sodium sulphate, can be administered.

Storage Condition

Store between 20-25° C.

Innovators Monograph

You find simplified version here Tamsulosin

Tamsulosin contains Tamsulosin see full prescribing information from innovator Tamsulosin Monograph, Tamsulosin MSDS, Tamsulosin FDA label

FAQ

What is Tamsulosin used for?

Tamsulosin used to treat men with symptoms of an enlarged prostate . It's also occasionally taken to treat kidney stones.Tamsulosin helps reduce the symptoms of an enlarged prostate gland by relaxing the muscles in the bladder and prostate so you can pee more easily.

How safe is Tamsulosin?

Long-term treatment with Tamsulosin is safe and well tolerated in patients with lower urinary tract symptoms/benign prostatic hyperplasia.

What are the common side effects of Tamsulosin?

Dizziness, lightheadedness, drowsiness, runny/stuffy nose, or ejaculation problems may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Can I take Tamsulosin while pregnant?

Tamsulosin is not for use by women. This medicine can cause birth defects if a woman is exposed to it during pregnancy.Tamsulosin capsules should not be handled by a woman who is pregnant or who may become pregnant.

Is Tamsulosin safe during breastfeeding?

If you take Tamsulosin while breastfeeding there's a risk of the Tamsulosin getting into your breast milk. This may mean your baby gets some side effects from the medicine.

How quickly does Tamsulosin work?

Tamsulosin are reached within four to five hours when a Tamsulosin capsule is taken on an empty stomach, or within six to seven hours when Tamsulosin is taken with food.

Can Tamsulosin affect memory?

Recently shown that men taking Tamsulosin have a higher risk of developing dementia when compared to men taking other α-adrenergic antagonists or no α-adrenergic antagonists at all.

Is Tamsulosin safe for long term use?

Long-term treatment with Tamsulosin is safe and well tolerated in patients with lower urinary tract symptoms/benign prostatic hyperplasia.

Does Tamsulosin affect sleep?

Tamsulosin improves nocturia and sleep disturbances by increasing the number of hours of undisturbed sleep

Does Tamsulosin make me pee more?

Tamsulosin helps relax the muscles in the prostate and the opening of the bladder. This may help increase the flow of urine or decrease the symptoms.

Does Tamsulosin break kidney stones?

Tamsulosin can boost the passage of large kidney stones, but not small ones.

Can I drink alcohol with Tamsulosin?

It's usually safe to drink alcohol with Tamsulosin. However, during the first few days of taking Tamsulosin, It's best not to drink alcohol. Alcohol can increase the blood pressure-lowering effect and this can make you feel dizzy or lightheaded.

Can I drive after taking Tamsulosin?

Tamsulosin can make some people feel dizzy or lightheaded, especially when they first start taking it. If this happens to you, do not drive a car, ride a bike, or use tools or machinery.

How long should a man take Tamsulosin?

The low incidence of acute urinary retention in patients treated with Tamsulosin for up to 6 years suggests that Tamsulosin may reduce the risk of AUR in patients with BPH.

When is the best time to take Tamsulosin?

Tamsulosin will be taken approximately one half hour following the same meal each day.

When should I stop taking Tamsulosin?

For kidney stones – your doctor may tell you to stop taking it if your stones have gone or if the medicine is not helping you.

*** Taking medicines without doctor's advice can cause long-term problems.
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