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Alpha-1 Blocker

Tamsulosin

A prostate-selective alpha-1 blocker used for urinary symptoms of an enlarged prostate (BPH); it is not a treatment for high blood pressure.

Drug card

How it works
Blocking alpha-1 receptors, relaxing blood vessels and prostate muscle
Used for
  • Urinary symptoms of an enlarged prostate (BPH)
  • Kidney stones, to help them pass (off-label)
Known for
  • Abnormal ejaculation: less or no semen
  • Dizziness, especially on standing
  • Floppy iris syndrome during cataract surgery

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Mechanism of action

How does tamsulosin work?

Tamsulosin is selective for the alpha-1A subtype, which makes up roughly 70% of prostatic alpha-1 receptors, so it acts mainly on the prostate, prostatic urethra and bladder neck and is not used to lower blood pressure. It is a sulfonamide, broken down by CYP3A4 and CYP2D6.

Like other alpha-1 blockers: They block alpha-1 adrenergic receptors on smooth muscle, so norepinephrine can no longer contract it. In arterioles and veins this lowers peripheral resistance and blood pressure; in the prostate, its capsule and the bladder neck the muscle relaxes and urine flows more easily. Tamsulosin favors the alpha-1A subtype that dominates the prostate and is not used for blood pressure.

Uses

What is tamsulosin used for?

  • Urinary symptoms of an enlarged prostate (BPH)
  • Kidney stones, to help them pass (off-label)

Side effects

Side effects of tamsulosin

  • Abnormal ejaculation: less or no semenKnown for
  • Dizziness, especially on standingKnown for
  • Floppy iris syndrome during cataract surgeryKnown for
  • Headache
  • Runny or stuffy nose (rhinitis)
  • Weakness and tiredness
  • Back pain
  • Palpitations or a fast heartbeat (rare)
  • Blurred vision
  • PriapismSerious
  • Allergic reactions, including angioedemaSerious
  • Stevens-Johnson syndrome (rare)Serious

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Not for high blood pressure, and not to be combined with another alpha blocker.
  • Avoid with strong CYP3A4 inhibitors such as ketoconazole; take care with CYP2D6 inhibitors such as paroxetine.
  • Before cataract or glaucoma surgery, tell the eye surgeon: floppy iris syndrome can occur even after stopping.
  • Take care in serious sulfa allergy, and with PDE5 inhibitors or warfarin.

Good to know: The prostate-selective member of the class: used for BPH, not for high blood pressure. It does not change PSA, and ejaculation problems and floppy iris syndrome are its best-known effects.

Remember it

A way to remember it

FAINT

F
First-dose fall in blood pressure, with fainting
A
Abnormal ejaculation, most with tamsulosin
I
Intraoperative floppy iris syndrome in cataract surgery
N
Nasal stuffiness
T
Tiredness and weakness

Written for biofideX

Its class

Alpha-1 blockers

Sources

Checked against

Written for biofideX in plain words, after checking these references:

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.

Practice it

Blood pressure

Tamsulosin is one of 27 drugs practiced together here: their classes, how they work, what they treat and what they're known for.

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