dutasteride/tamsulosin (Rx)

Brand and Other Names:Jalyn
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

dutasteride/tamsulosin

capsule

  • 0.5mg/0.4mg

Benign Prostatic Hyperplasia

1 capsule (dutasteride 0.5 mg/ tamsulosin 0.4 mg) PO qDay

Dosage Modifications

Renal impairment

  • Mild-to-severe (CrCl 10 to <70 mL/min/1.73 m2): No dosage adjustment necessary
  • End-stage renal disease (CrCl <10 mL/min/1.73 m2): Not studied

Hepatic impairment

  • Pharmacokinetics has not been studied
  • Dutasteride is extensively metabolized; exposure may be higher in hepatically impaired patients

Dosing Considerations

Limitations of Use: Dutasteride-containing products are not approved for prostate cancer prevention

Not indicated

Safety and efficacy not established

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Interactions

Interaction Checker

and dutasteride/tamsulosin

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    Contraindicated

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            Adverse Effects

            1-10%

            Year 1

            • Ejaculation disorders (1.6-7.8%)
            • Impotence (1.1-5.4%)
            • Decreased libido (≤4.5%)
            • Breast disorders (≤1.1%)
            • Dizziness (≤1.1%)

            Year 2-4

            • Impotence (1.1-5.4%)
            • Ejaculation disorders (≤1%)

            <1%

            Cardiac failure

            Year 2-4

            • Decreased libido
            • Breast disorders
            • Dizziness

            Postmarketing Reports

            Dutasteride

            • Immune system disorders: Hypersensitivity reactions, including rash, pruritus, urticaria, localized edema, serious skin reactions, and angioedema
            • Neoplasms: Male breast cancer
            • Psychiatric disorders: Depressed mood
            • Reproductive system and breast disorders: Testicular pain and testicular swelling

            Tamsulosin

            • Immune system disorders: Hypersensitivity reactions, including rash, urticaria, pruritus, angioedema, and respiratory problems have been reported with positive rechallenge in some cases
            • Cardiac disorders: Palpitations, dyspnea, atrial fibrillation, arrhythmia, and tachycardia
            • Skin disorders: Skin desquamation, including Stevens-Johnson syndrome, erythema multiforme, dermatitis exfoliative
            • Gastrointestinal disorders: Constipation, vomiting, dry mouth
            • Reproductive system and breast disorders: Priapism
            • Vascular disorders: Hypotension
            • Ophthalmologic disorders: During cataract surgery, a variant of small pupil syndrome known as intraoperative floppy iris syndrome (IFIS) associated with alpha adrenergic antagonist therapy, blurred vision, visual impairment, glaucoma
            • Respiratory: Epistaxis
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            Warnings

            Contraindications

            Clinically significant hypersensitivity (eg, serious skin reactions, angioedema, urticaria, pruritus, respiratory symptoms) to dutasteride, other 5 alpha-reductase inhibitors, or tamsulosin

            Females who are pregnant

            Cautions

            Orthostatic hypotension and/or syncope can occur

            Reduces total serum prostate-specific antigen (PSA) concentration by ~50%, evaluate any confirmed increases in PSA levels from nadir, even if those values are within normal range, for the presence of prostate cancer

            Caution patients about the possibility and seriousness of priapism

            Advise patients to not donate blood until 6 months after their last dose

            Intraoperative floppy iris syndrome has been observed during cataract surgery after alpha-adrenergic antagonist exposure

            5-ARIs and prostate cancer risk

            • June 9, 2011: Recent data from 2 large, randomized, controlled trials, Prostate Cancer Prevention Trial (PCPT) and the Reduction by Dutasteride of Prostate Cancer Events (REDUCE) trial, observed an increased risk of being diagnosed with a more serious form of prostate cancer (high-grade prostate cancer) in trial participants taking 5-alpha reductase inhibitors (5-ARIs)
            • Revised prescribing information recommends that before initiating 5-ARIs, rule out other urological conditions, including prostate cancer that might mimic benign prostatic hyperplasia (BPH)

            Drug interaction overview

            • Tamsulosin: CYP3A4 and CYP2D6 substrate
            • Dutasteride: CYP3A4 and CYP3A5 substrate
            • Additive hypotensive effects
              • Coadministration with PDE-5 inhibitors (eg, sildenafil) or other alpha-antagonists (eg, doxazosin, terazosin may increase risk of hypotension
            • CYP3A4 and CYP2D6 inhibitors
              • Strong CYP3A4 inhibitors (eg, ketoconazole): Avoid coadministration
              • Less potent CYP3A4 inhibitors (eg, terbinafine), strong or moderate (eg, terbinafine, paroxetine) CYP2D6 inhibitors, a combination of both CYP3A4 and CYP2D6 inhibitors, or poor metabolizers of CYP2D6: Use caution
              • Ketoconazole (strong CYP3A4 inhibitor) and paroxetine (strong CYP2D6 inhibitor) resulted in increased in plasma levels of tamsulosinEffects of CYP3A4 inhibitors on dutasteride has not been studied
            • Calcium channel blockers
              • No dosage adjustment recommended
              • Coadministration of verapamil or diltiazem decreases clearance and increases effects of dutasteride
            • Warfarin
              • Use caution; monitor INR
              • Limited studies showed inconclusive results regarding coadministration of tamsulosin with warfarin
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            Pregnancy & Lactation

            Pregnancy

            Not indicated for use in females; contraindicated for use in pregnancy because may cause harm to male fetus; dutasteride is a 5-alpha-reductase inhibitor that prevents conversion of testosterone to dihydrotestosterone (DHT), a hormone necessary for normal development of male genitalia

            Abnormalities in genitalia of male fetuses is an expected physiological consequence of inhibition of this conversion; these results are similar to observations in male infants with genetic 5-alpha-reductase deficiency

            Animal data

            • In animal reproduction studies, dutasteride inhibited normal development of external genitalia in male offspring when given to rats or rabbits during organogenesis at less than maximum recommended human dose (MRHD) of 0.5 mg daily, in absence of maternal toxicity; at 15 times MRHD, prolonged pregnancy, decreased reproductive organ weights, and delayed puberty in male offspring were observed in rats, with no-effect levels less than the MRHD of 0.5 mg daily
            • Increased placental weights in rabbits were also observed, with no-effect levels less than the MRHD of 0.5 mg daily
            • Although dutasteride is secreted into human semen, drug concentration in human female partner is approximately 100 times less than concentrations producing abnormalities of male genitalia in animal studies
            • In monkeys dosed during organogenesis at blood concentrations comparable to or above levels to which a human female partner is estimated to be exposed, male offspring external genitalia was not adversely affected
            • No feminization occurred in male offspring of untreated female rats mated to treated male rats even though detectable blood levels of dutasteride were observed in the female rats
            • No adverse developmental effects were observed in animal studies in which tamsulosin hydrochloride was administered to rats or rabbits during period of organogenesis

            Reproductive potential

            • Effects of dutasteride 0.5 mg/day on semen characteristics were evaluated in normal volunteers aged 18 to 52 years (n = 27 dutasteride, n = 23 placebo) throughout 52 weeks of treatment and 24 weeks of post-treatment follow-up; at 52 weeks, mean percent reductions from baseline in total sperm count, semen volume, and sperm motility were 23%, 26%, and 18%, respectively, in the dutasteride group when adjusted for changes from baseline in placebo group; sperm concentration and morphology were unaffected
            • After 24 weeks of follow-up, mean percent change in total sperm count in dutasteride group remained 23% lower than baseline, while mean values for all semen parameters at all timepoints remained within normal ranges and did not meet predefined criteria for a clinically significant change (30%), 2 subjects in the dutasteride group had decreases in sperm count of greater than 90% from baseline at 52 weeks, with partial recovery at 24-week follow-up; clinical significance of these effects on semen characteristics for an individual patient’s fertility is not known

            Lactation

            Therapy not indicated for use in females

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Dutasteride: Selective inhibitor of type 1 and type 2 isoforms of 5-alpha-reductase

            Tamsulosin: Alpha-adrenergic antagonist; blocks alpha-1a adrenergic receptor in smooth muscle of prostate, decreasing bladder neck & urethral resistance

            Absorption

            Bioavailability: 60% (dutasteride); 10% (tamsulosin)

            Peak Plasma Time: 2-3 hr (dutasteride); 4-5 hr fasting; 6-7 hr with food (tamsulosin)

            Onset: 1-2 weeks (dutasteride); 4-8 hr (tamsulosin)

            Distribution

            Protein Bound: 99% (dutasteride and tamsulosin)

            Vd: 300-500 L (dutasteride); 0.2 L (tamsulosin)

            Metabolism

            Dutasteride

            • Metabolism: hepatic P450 enzyme CYP3A4 and CYP2D6
            • Metabolites, major: 4'-hydroxydutasteride, 6-hydroxydutasteride (as active as parent), 6,4'-dihydroxydutasteride

            Tamsulosin

            • Metabolism: liver
            • Metabolites: glucuronide and sulfate conjugates (inactive)

            Elimination

            Half-Life: 5 weeks at steady state (dutasteride); 14-15 hr (tamsulosin)

            Excretion: mainly feces (dutasteride); urine 76%, feces 21% (tamsulosin)

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            Administration

            Oral Administration

            Swallow capsules whole; do not chew, crush, or open

            High temperatures may deform and/or discolored capsules; discard if this occurs

            Missed dose

            • Take later that same day, 30 min after a meal; do not take 2 capsules in the same day
            • Missed doses for several days: Contact healthcare provider before restarting

            Storage

            Store at 25ºC (77ºF); excursions permitted 15-30ºC (59-86ºF)

            Capsules may become deformed and/or discolored if kept at high temperatures

            Dutasteride is absorbed through the skin

            Females who are pregnant or who could become pregnant should not be handling capsules

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.