Tamsulosin

Tamsulosin is an alpha-blocker medication approved by the US FDA on April 15, 1997. Tamsulosin is a medicine that treats benign prostatic hyperplasia. The problem is with men's prostate glands. Urinary problems are caused by the prostate gland's expanding muscles getting tense and clogging the tube that empties the bladder of pee. Tamsulosin helps to relax the muscles around the prostate gland and bladder, making urination simpler and less frequent. It also works to cure kidney stones.

BRAND NAMES:

Flomax - Flomax is a drug composition of tamsulosin hydrochloride available in oral capsules with a strength of 0.4 mg.

Jalyn –Jalyn contains two active ingredients, dutasteride 0.5 mg and tamsulosin 0.4 mg oral capsules.

MECHANISM OF ACTION:

Tamsulosin is involved in the selective inhibition of alpha-1 adrenergic receptors. By blocking these receptors, it prevents norepinephrine from binding to them; as a result, it helps in reducing the contraction of smooth muscles in the prostate and bladder neck. The relaxation of smooth muscles leads to an improvement in urine flow and a reduction in the symptoms. The non-selective alpha-blockers affect alpha-1 receptors throughout the body. Tamsulosin specifically targets alpha-1A receptors, which are mainly located in the prostate. This selectively minimizes the impact on blood vessels and reduces the risk of side effects such as orthostatic hypotension.

PHARMACOKINETICS:

Absorption: The maximum plasma concentration is 3.1 – 5.3ng/ml for orally administered 0.4mg. The maximum plasma peak concentration time increases from 4 -5 hours to 6-7 hours when tamsulosin is taken with food. The bioavailability increases by 30% and the maximum plasma concentration by 40-70%.

Distribution: The distribution's mean apparent volume is 16 liters.

Metabolism: Tamsulosin is metabolized in the liver by the cytochrome P450 enzyme. The metabolites of tamsulosin Hcl undergo extensive conjugation to glucuronide or sulfate to renal excretion.

Excretion: 76% of the drug is excreted through urine and 21% through feces.

PHARMACODYNAMICS:

Alpha adrenoceptor blockers, such as tamsulosin, are specific for alpha-1A and alpha-1D receptors, which are more prevalent in the prostate and submaxillary tissue. Tamsulosin binds to alpha-1A receptors with a selectivity that is 3.9–38 times greater than that of alpha-1B and 3–20 times greater than that of alpha-1D.

DOSAGE AND ADMINISTRATION:

Tamsulosin is often supplied in the form of capsules. The dose varies according to the patient's disease state.

The recommended dose for benign prostatic hyperplasia in adults is 0.4 mg orally once a day, which can be increased to 0 mg orally once a day depending on the patient's health and response to treatment.

CONTRAINDICATIONS:

Tamsulosin is contraindicated in patients with hypersensitivity and its related compounds.

DRUG INTERACTIONS:

While using tamsulosin it is needed to discuss with the physician the medicines that have been already used for other treatments Below are some drugs with which tamsulosin interacts.