testosterone (Rx)

Brand and Other Names:Aveed, Depo-Testosterone, more...Testopel, Xyosted, Jatenzo
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

oral capsule (undecanoate): Schedule III

  • 158mg (Jatenzo)
  • 198mg (Jatenzo)
  • 237mg (Jatenzo)

injectable solution (cypionate): Schedule III

  • 100mg/mL (Depo-Testosterone)
  • 200mg/mL (Depo-Testosterone)

injectable solution (enanthate): Schedule III

  • 50 mg/0.5mL (Xyosted)
  • 75 mg/0.5mL (Xyosted)
  • 100 mg/0.5mL (Xyosted)
  • 200mg/mL (generic)

injectable solution (undecanoate): Schedule III

  • 750mg/3mL (Aveed)

pellet implant: Schedule III

  • 75mg (Testopel)
  • 12.5mg, 25mg, 37.5mg, 50mg (generic)

Hypogonadism

Primary hypogonadism (congenital or acquired): Testicular failure due to conditions such as cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter Syndrome, chemotherapy, or toxic damage from alcohol or heavy metals; these men usually have low serum testosterone concentrations and gonadotropins (FSH, LH) above normal range

Hypogonadotropic hypogonadism (congenital or acquired): Gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency or pituitary-hypothalamic injury from tumors, trauma, or radiation; these men have low testosterone serum concentrations but have gonadotropins in the normal or low range

Testosterone cypionate: 50-400 mg IM every 2-4 weeks

Testosterone enanthate (generic): 50-400 mg IM every 2-4 weeks

Testosterone undecanoate (restricted availability): 750 mg IM initial dose, repeat after 4 weeks, and then q10wk thereafter

Pellet: 150-450 mg SC every 3-6 months; 150 mg of pellet approximately equivalent to 25 mg of testosterone propionate weekly

Xyosted

  • Starting dose: 75 mg SC qWeek
  • Adjust dose based upon total testosterone minimum (trough) concentrations (Cmin) (measured 7 days after most recent dose) obtained following 6 weeks of dosing and periodically thereafter
  • Trough concentration (350-650 ng/dL) generally provides testosterone exposures in normal range during entire dosing interval
  • Decrease dose by 25 mg if (Cmin) is ≥650 ng/dL Increase dose by 25 mg if the total testosterone Cmin <350 ng/dL
  • Maintain same dose if total testosterone Cmin ≥350 ng/dL and <650 ng/dL

Jatenzo

  • Starting dose: 237 mg PO BID with food
  • To ensure proper dose adjustment, measure serum testosterone concentrations 6 hr after morning dose in plain tubes, clotted at room temperature for 30 minutes prior to centrifugation; adjust dose based on serum testosterone measurement
  • Wait 7 days after starting treatment or adjusting the dose before checking the serum testosterone concentration; thereafter, periodically monitor serum testosterone concentrations 6 hr after morning dose
  • Adjust dose based on testosterone level as follows
  • <425 ng/dL
    • Current BID dose 158 mg: Increase to 198 mg BID
    • Current BID dose 198 mg: Increase to 237 mg BID
    • Current BID dose 237 mg: Increase to 316 mg (two 158-mg cap) BID
    • Current BID dose 316 mg: Increase to 396 mg (two 198-mg cap) BID
  • 425-970 ng/dL
    • No dose change
  • >970 ng/dL
    • Current BID dose 396 mg: Decrease to 316 mg BID
    • Current BID dose 316 mg: Decrease to 237 mg BID
    • Current BID dose 237 mg: Decrease to 198 mg BID
    • Current BID dose 198 mg: Decrease to 158 mg BID
    • Current BID dose 158 mg: Discontinue treatment

Delayed Puberty in Males

Testosterone enanthate (generic): 50-200 mg IM every 2-4 weeks for 4-6 months

Inoperable Mammary Cancer in Women

Testosterone enanthate (generic): 200-400 mg IM every 2-4 weeks

Androgen Deficiency in HIV+ Patients (Orphan)

Physiologic testosterone replacement in androgen-deficient HIV+ patients with associated weight loss

Orphan sponsor

  • Watson Laboratories, Research Park, 417 Wakara Way, Salt Lake City, UT 8410

Delayed Growth (Orphan)

Treatment of constitutional delay in growth and puberty in adolescent boys aged 14-17 years (testosterone undecanoate)

Orphan sponsor

  • SOV Therapeutics, Inc, 101 Guymon Court, Morrisville, NC 27560

Dosing Considerations

Before initiating: Confirm diagnosis of hypogonadism by ensuring serum testosterone has been measured in the morning on at least 2 separate days and that these concentrations are below the normal range

Dosage Forms & Strengths

injectable solution (cypionate): Schedule III

  • 100mg/mL (Depo-Testosterone)
  • 200mg/mL (Depo-Testosterone)

injectable solution (enanthate): Schedule III

  • 200mg/mL (generic)

injectable solution (undecanoate): Schedule III

  • 250mg/mL (Aveed)

pellet implant: Schedule III

  • 75mg (Testopel)
  • 12.5mg, 25mg, 37.5mg, 50mg (generic)

Hypogonadism

<12 years

  • Safety and efficacy not established

≥12 years

  • Testosterone cypionate: 50-400 mg IM every 2-4 weeks
  • Testosterone enanthate (generic): 50-400 mg IM every 2-4 weeks
  • Pellet: 150-450 mg SC every 3-6 months; 150 mg of pellet approximately equivalent to 25 mg of testosterone propionate weekly

Delayed Puberty in Males

<12 years

  • Safety and efficacy not established

≥12 years

  • 50-200 mg IM every 2-4 weeks for 4-6 months

Dosing Considerations

Limitations of use (Xyosted, Aveed)

  • Safety and efficacy not established in adult males with “age-related hypogonadism” (also referred as “late-onset hypogonadism”) and males <18 years
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Interactions

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            Adverse Effects

            Frequency Not Defined

            Acne

            Abnormal dreams

            Aggressive behavior

            Alopecia

            Anaphylaxis

            Anger

            Amnesia

            Anxiety

            Bladder irritability

            Breast soreness

            Deep venous thrombosis

            Excessive frequency and duration of erection

            Fatigue

            Growth acceleration

            Gynecomastia

            Headache

            Hirsutism

            Hot flashes

            Hypersensitivity

            Hypercholesterolemia

            Hypertension

            Insomnia

            Liver function alterations

            Male pattern baldness

            Menstrual irregularities

            Priapism

            Pruritus

            Rash

            Seborrhea

            Suppression of factors II, V, VII, X

            Vasodilation

            Virilization

            Water retention

            Postmarketing Reports

            Vascular Disorders: Venous thromboembolism

            Reproductive system: Azoospermia, benign prostatic hyperplasia

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            Warnings

            Black Box Warnings

            Blood pressure increase

            • Blood pressure (BP) increases reported that can increase the risk for major adverse cardiovascular events (MACE) (eg, nonfatal myocardial infarction, nonfatal stroke, cardiovascular death) with greater risk for MACE in patients with cardiovascular risk factors or established cardiovascular disease
            • Before initiating treatment, consider patient’s baseline cardiovascular risk and ensure adequate blood pressure controlled
            • Starting ~6 weeks after initiating therapy, periodically monitor for and treat new onset hypertension or exacerbations of pre-existing hypertension
            • Re-evaluate whether benefits outweigh its risks in patients who develop cardiovascular risk factors or cardiovascular disease while on treatment
            • Due to this risk, use only for treatment of men with hypogonadal conditions associated with structural or genetic etiologies

            Serious pulmonary oil microembolism reactions and anaphylaxis

            • Aveed only
            • Serious pulmonary oil microembolism reactions (POME) (eg, urge to cough, dyspnea, throat tightening, chest pain, dizziness, syncope reactions and episodes) of anaphylaxis reported during or immediately after administration; may occur after first dose
            • Observe patients for 30 minutes in healthcare setting to provide immediate medical treatment in event of serious POME reactions or anaphylaxis
            • Because of risks of serious POME reactions and anaphylaxis, testosterone undecanoate is available through restricted program under a risk evaluation and mitigation strategy (REMS) called the Aveed REMS Program

            Contraindications

            Hypersensitivity to product or formulation components

            Men with carcinoma of the breast or known or suspected carcinoma of the prostate

            Men with hypogonadal conditions (eg, “age-related hypogonadism”) that are not associated with structural or genetic etiologies; efficacy has not been established for these conditions, and testosterone can increase BP which can increase the risk of MACE

            Women: Pregnancy or prospect of pregnancy

            Cautions

            May increase blood pressure (BP); before initiating, consider baseline cardiovascular (CV) risk and ensure BP is adequately controlled; check BP ~3 weeks after initiating or increasing dose and periodically thereafter; treat new-onset hypertension or exacerbations; reassess whether the benefits of continued treatment outweigh risks

            Increased hematocrit (polycythemia) reflective of increases in RBC mass may require lower dose or discontinuation; evaluate hematocrit ~q3Months, and if elevated hold testosterone until hematocrit returns to normal; if testosterone restarted and again hematocrit increase, permanently discontinue testosterone; increased RBC mass may increase thromboembolic risk

            Patients with BPH treated with androgens are at an increased risk for worsening of BPH signs and symptoms

            Androgens may increase risk for prostate cancer; evaluate patients for prostate cancer before initiating and during treatment with testosterone

            Venous thromboembolic events (VTE) reported, including deep vein thrombosis (DVT) and pulmonary embolism (PE), in patients using testosterone replacement; evaluate patients who report symptoms of pain, edema, warmth, and erythema in the lower extremity for DVT and those who present with acute shortness of breath for PE; if VTE suspected, discontinue testosterone and initiate appropriate workup and management

            Testosterone has been subject to abuse, typically at doses higher than recommended for approved indication and in combination with other anabolic androgenic steroids; anabolic androgenic steroid abuse can lead to serious cardiovascular and psychiatric adverse reactions; if testosterone abuse suspected, check serum testosterone concentrations to ensure they are within therapeutic range; consider possibility of testosterone and anabolic androgenic steroid abuse in suspected patients who present with serious cardiovascular or psychiatric adverse events

            Prolonged use of high dose testosterone associated with serious hepatic adverse effects (peliosis hepatis, hepatic neoplasms, cholestatic hepatitis, and jaundice); peliosis hepatis can be life-threatening or fatal; long-term therapy with IM testosterone enanthate has produced multiple hepatic adenomas; although not reported with other administration routes, monitor for signs or symptoms of hepatic dysfunction; promptly discontinue testosterone if jaundice occurs while evaluating cause

            Gynecomastia may develop and persist in patients treated for hypogonadism

            May alter serum lipid profile and require dose adjustment of lipid lowering drugs or discontinuing testosterone; monitor lipid profile, especially after starting testosterone

            Androgens may promote sodium and water retention; edema, with or without CHF, may be a serious complication if pre-existing cardiac, renal, or hepatic disease exists; may necessitate discontinuing drug; consider diuretic therapy

            Large doses may suppress spermatogenesis

            May potentiate sleep apnea in some patients, especially patients who are obese or with chronic lung disease

            Use androgens cautiously in patients with cancer with risk of hypercalcemia (and associated hypercalciuria); monitor serum calcium concentrations regularly during treatment

            May decrease concentrations of thyroxine-binding globulin, resulting in decreased total T4 serum concentrations and increased resin uptake of T3 and T4; free thyroid hormone concentrations remain unchanged, however, and there is no clinical evidence of thyroid dysfunction

            Due to lack of controlled evaluations in women and potential virilizing effects, not indicated for use in women

            Depression and suicidal ideation and behavior, including completed suicide, have occurred during clinical trials

            Aveed only: Serious POME reactions reported to occur during or immediately after IM injection of testosterone undecanoate 1000 mg (see Black Box Warnings)

            Testopel only: Postmarketing cases associated pellet(s) insertion with implant site infection (cellulitis and abscess), and/or pellet extrusion at or near implantation site; most reported cases occurred within the first month after implantation

            Cardiovascular risk

            • Long term clinical safety trials have not been conducted to assess CV outcomes of testosterone replacement therapy
            • As of March 2019, epidemiologic studies and randomized controlled trials have been inconclusive for determining the risk of MACE (eg, non-fatal MI or stroke, CV death) with testosterone use compared with non-use
            • Some studies, but not all, reported an increased risk of MACE associated with testosterone replacement therapy
            • Testosterone can cause BP increases that can increase the risk of MACE

            Drug interactions overview

            • In diabetic patients, metabolic effects of androgens may decrease blood glucose and, therefore, may necessitate a decrease in dose of antidiabetic medication
            • Changes in anticoagulant activity may be seen with androgens, therefore more frequent monitoring of international normalized ratio (INR) and prothrombin time are recommended in patients taking warfarin, especially at initiation and termination of androgen therapy
            • Concurrent use of testosterone with corticosteroids may result in increased fluid retention and carefully monitor, particularly in patients with cardiac, renal or hepatic disease
            • Some prescription medications and nonprescription analgesic and cold medications contain drugs known to increase blood pressure; coadministration of these medications may lead to additional increases in blood pressure
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            Pregnancy & Lactation

            Pregnancy

            Contraindicated in pregnant women

            Teratogenic; may cause fetal harm when administered to a pregnant woman based on data from animal studies and its mechanism of action

            Exposure of a female fetus to androgens may result in varying degrees of virilization

            Animal data

            • In animal developmental studies, exposure to testosterone in utero resulted in hormonal and behavioral changes in offspring and structural impairments of reproductive tissues in female and male offspring
            • These studies did not meet current standards for nonclinical development toxicity studies

            Infertility

            • During treatment with large doses of exogenous androgens, spermatogenesis may be suppressed through feedback inhibition of the hypothalamic-pituitary-testicular axis
            • Observed reduced fertility in some men taking testosterone replacement therapy; impact on fertility may be irreversible

            Lactation

            Not indicated for women

            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

            Endogenous androgen; promotes growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males

            Absorption

            Peak plasma concentration: 790 ng/dL (Xyosted)

            Peak plasma time: 11.9 hr (Xyosted)

            AUC: 92,955 ng·hr/dL (Xyosted)

            Steady state reached: 14 days (Aveed)

            Distribution

            Circulating testosterone is primarily bound in serum to sex hormone-binding globulin (SHBG) and albumin

            Protein bound

            • Xyosted and Aveed: ~40% (SHBG), 2% (free), and remaining is loosely bound to albumin and other proteins
            • Depo-Testosterone and Testopel: 98% (SHBG); 2 % (free)

            Metabolism

            Testosterone undecanoate: Metabolized to testosterone via ester cleavage of undecanoate group

            Testosterone enanthate: Metabolized to testosterone via ester cleavage of enanthate group

            Testosterone is metabolized to various 17-keto steroids through two different pathways; major active metabolites of testosterone are estradiol and DHT

            Elimination

            Half-life: 8 days (Depo-Testosterone); 10-100 minutes (Testopel)

            Excretion: Urine (90%); feces (6%)

            Inactivation of testosterone occurs primarily in the liver

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            Administration

            Oral Administration

            Jatenzo only

            Take with food

            Implant Administration

            Testopel only

            Number of pellets to implant depends upon minimal daily requirements of testosterone propionate determined by a gradual reduction of amount administered parenterally

            With lower requirements by injection, correspondingly lower amounts may be implanted; found approximately one-third of material is absorbed in the first month, one-fourth in the second month and one-sixth in the third month

            Adequate effect of pellets ordinarily continues for 3-4 months, sometimes as long as 6 months

            SC Administration

            Xyosted only

            SC use only; administer in abdominal region only

            Avoid IM or IV injection

            Visually inspect for particulate matter and discoloration prior to administration

            Do not use if liquid is cloudy or if visible particles are present

            Do not use if seal is broken

            IM Administration

            Depo-Testosterone and Aveed only

            IM use only; administer IM deep in the gluteal muscle

            Do not give IV

            The various testosterone salts are not interchangeable; check prescribing information if switching product

            Between consecutive injections, alternate injection site between left and right buttock

            Visually inspect for particular matter and discoloration prior to administration

            Warming and shaking the vial redissolves any crystals that may have formed during storage at temperatures lower than recommended

            Storage

            All formulations: Store at room temperature 25°C (77°F); excursions permitted to 15-30°C (59-86°F) in its original carton until the date indicated

            Xyosted: Protect from light

            Jatenzo: Avoid exposing the capsules to moisture (store in a dry place)

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            Images

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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.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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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.