Tamsulosin

tam-sool′o-sin

Flomax

Do not confuse Flomax with Fosamax or Volmax.

CATEGORY AND SCHEDULE

Pregnancy Risk Category: B (not indicated for use in women.)

Classification: Urinary tract agents, antiadrenergics, specific peripheral α-blockers

Table of contents:

MECHANISM OF ACTION

PHARMACOKINETICS

AVAILABILITY

‣ Dosage with strong CYP3A4 inhibitors

‣ Severe hepatic impairment

CONTRAINDICATIONS

DIAGNOSTIC TEST EFFECTS

SERIOUS REACTIONS

MECHANISM OF ACTION

An α1 antagonist that targets receptors around the bladder neck and prostate capsule. Therapeutic
Effect: Relaxes smooth muscle and improves urinary flow and symptoms of prostatic hyperplasia.

PHARMACOKINETICS

Well absorbed and widely distributed. Protein binding: 94%-99%. Metabolized in the liver primarily by
CYP3A4 and CYP2D6. Excreted primarily in urine. Unknown whether it is removed by hemodialysis. Half-
life: 9-13 h.

AVAILABILITY

Capsules: 0.4 mg.

INDICATIONS AND DOSAGES

‣ Benign prostatic hyperplasia

PO

Adults. 0.4 mg once a day, approximately 30 min after same meal each day. May increase dosage to 0.8
mg if inadequate response in 2-4 wks.

‣ Dosage with strong CYP3A4 inhibitors

Limit dosage to 0.4 mg once daily.

‣ Severe hepatic impairment

Do not use.

CONTRAINDICATIONS

History of sensitivity to tamsulosin.

INTERACTIONS

Drug

α-Adrenergic blocking agents (such as doxazosin, prazosin, terazosin): May increase the α-blockade
effects of both drugs.

β-Blockers, calcium channel blockers, phosphodiesterase-5 inhibitors: May increase the potential for
hypotension.

CYP3A4 inducers: May reduce tamsulosin levels, decrease effect.

CYP3A4 inhibitlors: May increase tamsulosin levels and increase side effects such as hypotension risk;
tamsulosin dose adjustment required with strong inhibitors.

Warfarin: May alter the effects of warfarin.

Herbal

Herbs with hypotensive properties (black cohosh, coleus, golden seal, hawthorn, mistletoe, periwinkle,
quinine): May increase the potential for hypotension.

Saw palmetto: Unknown whether it will interact but it is recommended to avoid use.

St. John’s wort: May decrease tamsulosin’s effects.

Food

None known.

DIAGNOSTIC TEST EFFECTS

None known.

SIDE EFFECTS

Frequent (7%-9%)

Dizziness, somnolence.

Occasional (3%-5%)

Headache, anxiety, insomnia, orthostatic hypotension.

Rare (< 2%)

Nasal congestion, pharyngitis, rhinitis, nausea, vertigo, impotence.

SERIOUS REACTIONS

• Severe orthostatic hypotension with syncope may be preceded by tachycardia.

• Rare reports of jaundice, impaired hepatic function, and increased transaminases.

• α-blockers associated with intraoperative floppy iris syndrome during cataract surgery.

• Priapism (very rare).

• Toxic skin eruptions (very rare).

PRECAUTIONS & CONSIDERATIONS

Caution is warranted in patients with hepatic impairment. Tamsulosin is not indicated for use in women
or children. No age-related precautions have been noted in elderly patients.

Dizziness and light-headedness may occur. Tasks that require mental alertness or motor skills should be
avoided until response to the drug is established. Caution should be used when getting up from a sitting
or lying position. BP should be monitored.

Storage

Store capsules at room temperature.

Administration

Take at the same time each day,

30 min after the same meal. Do not crush or open capsule.