Xyosted 75mg/0.5ml Auto Inj 4x0.5ml

Manufacturer ANTARES PHARMA Active Ingredient Testosterone Enanthate (Subcutaneous)(tes TOS ter one) Pronunciation zye-OH-sted (for Xyosted); tes-TOS-ter-own EN-an-thate
WARNING: High blood pressure has happened with this drug. Have your blood pressure checked as you have been told by your doctor.High blood pressure can raise the chance of heart attack, stroke, or death from heart disease. If you have high blood pressure or heart disease, talk with your doctor. @ COMMON USES: It is used to treat low testosterone levels.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Androgen
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Pharmacologic Class
Androgen receptor agonist
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Pregnancy Category
Category X
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FDA Approved
Oct 2018
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DEA Schedule
Schedule III

Overview

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What is this medicine?

Xyosted is a prescription medicine containing testosterone, a male hormone. It is used to treat adult men who have low testosterone levels due to certain medical conditions (primary hypogonadism or hypogonadotropic hypogonadism). It helps restore testosterone levels to normal, which can improve symptoms like low energy, decreased libido, and muscle weakness.
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How to Use This Medicine

Proper Administration of This Medication

To ensure safe and effective use, follow your doctor's instructions and read all provided information carefully. This medication is administered via injection into the fatty tissue on either side of your abdomen. If you will be self-administering the injection, your doctor or nurse will provide guidance on the proper technique.

Before administering the injection, wash your hands thoroughly. Avoid injecting into skin within 2 inches (5 cm) of your belly button or into areas that are irritated, tender, bruised, red, scaly, hard, scarred, or have stretch marks. Do not use the medication if the solution appears cloudy, is leaking, or contains particles. The solution should be colorless to faintly yellow; discard it if the color changes.

After use, dispose of needles in a designated needle/sharp disposal box. Do not reuse needles or other materials. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.

Storage and Disposal

Store this medication at room temperature, avoiding freezing. Keep it in its original container, protected from light, and in a dry location. Do not store it in a bathroom.

Missed Dose Instructions

If you miss a dose, administer it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at once or use extra doses to make up for a missed dose.
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Lifestyle & Tips

  • Administer Xyosted exactly as prescribed by your doctor, typically once weekly. Do not inject more often than prescribed.
  • Learn proper injection technique from your healthcare provider. Xyosted is given as a subcutaneous (under the skin) injection in the abdomen, thigh, or upper arm.
  • Rotate injection sites to avoid skin irritation.
  • Do not inject into blood vessels or muscles.
  • Keep all appointments for blood tests and follow-up visits to monitor your testosterone levels, blood pressure, blood count, and prostate health.
  • Inform your doctor about all other medications, supplements, and herbal products you are taking.
  • Maintain a healthy lifestyle, including regular exercise and a balanced diet, as advised by your doctor.

Dosing & Administration

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Adult Dosing

Standard Dose: 75 mg (0.5 mL) administered subcutaneously once weekly
Dose Range: 75 - 75 mg

Condition-Specific Dosing:

hypogonadism: Initial dose: 75 mg (0.5 mL) subcutaneously once weekly. Dose adjustments may be made based on serum testosterone levels and clinical response, but the maximum recommended dose is 100 mg (0.67 mL) once weekly.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Safety and efficacy not established in pediatric patients. Use in males under 18 years of age is not recommended.)
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, but use with caution.
Moderate: No specific dose adjustment recommended, but use with caution.
Severe: No specific dose adjustment recommended, but use with caution. Monitor for fluid retention.
Dialysis: Not available. Use with caution and monitor for fluid retention.

Hepatic Impairment:

Mild: No specific dose adjustment recommended, but use with caution.
Moderate: No specific dose adjustment recommended, but use with caution.
Severe: Contraindicated in patients with severe hepatic impairment due to potential for fluid retention and exacerbation of liver disease.
Confidence: Medium

Pharmacology

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Mechanism of Action

Testosterone is an endogenous androgen. Androgens are responsible for the normal growth and development of male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of the prostate, seminal vesicles, penis, and scrotum; the development of male hair distribution (pubic, axillary, chest, and beard); laryngeal enlargement, vocal cord thickening, and alterations in body musculature and fat distribution. Testosterone also promotes retention of nitrogen, sodium, potassium, and phosphorus, and decreases urinary excretion of calcium. Androgens increase protein anabolism and decrease protein catabolism. The mechanism of action of testosterone enanthate administered subcutaneously is the same as that of endogenous testosterone.
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Pharmacokinetics

Absorption:

Bioavailability: Not directly quantified for subcutaneous testosterone enanthate, but absorption is sustained.
Tmax: Approximately 10-14 hours after a single subcutaneous dose.
FoodEffect: Not applicable for subcutaneous administration.

Distribution:

Vd: Approximately 1 L/kg (for testosterone)
ProteinBinding: Approximately 98% (to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration: Limited (Testosterone can cross the blood-brain barrier, but its distribution into the CNS is complex and influenced by various factors.)

Elimination:

HalfLife: Approximately 8-10 days (for testosterone enanthate after subcutaneous administration)
Clearance: Approximately 13.2 Β± 3.9 mL/min/kg (for testosterone)
ExcretionRoute: Mainly renal (approximately 90% as conjugates of testosterone and its metabolites), fecal (approximately 6%)
Unchanged: Less than 6% of a testosterone dose is excreted unchanged in the urine.
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Pharmacodynamics

OnsetOfAction: Gradual, with therapeutic effects typically observed within weeks to months.
PeakEffect: Serum testosterone levels peak approximately 10-14 hours after a dose, with steady-state levels achieved after approximately 3 weeks of weekly dosing.
DurationOfAction: Weekly administration maintains therapeutic testosterone levels.

Safety & Warnings

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BLACK BOX WARNING

Increases in Blood Pressure: XYOSTED can increase blood pressure, which can increase the risk of major adverse cardiovascular events (MACE), including non-fatal myocardial infarction, non-fatal stroke, and cardiovascular death. Before initiating XYOSTED, consider the patient’s baseline cardiovascular risk and ensure blood pressure is adequately controlled. Monitor blood pressure during XYOSTED treatment and manage new-onset or worsening hypertension. Discontinue XYOSTED in patients who develop uncontrolled hypertension.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Prolonged or frequent erections
Urination problems, such as:
+ Trouble passing urine
+ Pain while passing urine
+ Weak or dripping urine stream
+ Frequent urination
Loss of bladder control
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
Enlarged breasts or breast pain
Shortness of breath, significant weight gain, or swelling in the arms or legs
Upset stomach or vomiting
Trouble breathing while sleeping
Excessive daytime sleepiness
Weakness on one side of the body, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Skin color changes
Changes in testicle size or shape
Signs of a blood clot, including:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color changes, or pain in a leg or arm
+ Trouble speaking or swallowing
Liver problems, which can be life-threatening. Seek medical help if you experience:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:

Headache
Acne
Diarrhea
Emotional changes
Fatigue or weakness
Sleep disturbances
* Irritation at the site of application

This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Signs of increased blood pressure: severe headache, blurred vision, pounding in your ears or neck.
  • Signs of blood clots: pain, swelling, warmth, or redness in your leg; sudden shortness of breath; sudden chest pain.
  • Signs of prostate problems: difficulty urinating, frequent urination (especially at night), weak or interrupted urine stream, painful urination.
  • Signs of liver problems: yellowing of the skin or eyes (jaundice), dark urine, light-colored stools, nausea, vomiting, unusual tiredness.
  • Signs of fluid retention: swelling in your ankles, feet, or hands; sudden weight gain.
  • Signs of sleep apnea: new or worsening snoring, daytime sleepiness.
  • Signs of breast enlargement or tenderness (gynecomastia).
  • Mood changes, aggression, irritability, or depression.
  • Frequent or persistent erections, or erections that are painful.
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
If you are a male with a history of breast or prostate cancer.
If you have been diagnosed with any of the following health conditions: heart disease, kidney disease, or liver disease.
If you are a female who is pregnant, plans to become pregnant, or is breastfeeding. This medication is not approved for use in pregnant or breastfeeding women. If you are in one of these categories, discuss your situation with your doctor.
* If the patient is a child, as this medication is not approved for pediatric use.

This list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems to your doctor and pharmacist. They will help you determine whether it is safe to take this medication in conjunction with your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

If you have diabetes, it is crucial to closely monitor your blood sugar levels while using this drug.

There may be an increased risk of developing prostate cancer associated with this medication. You should discuss this with your doctor.

Men with an enlarged prostate should be aware that their symptoms may worsen while taking this medication. If this occurs, contact your doctor promptly.

Individuals with sleep apnea should consult their doctor, as this condition may deteriorate in some people using testosterone.

Treatment with this medication may lead to elevated cholesterol and triglyceride levels. Although the impact of these changes on heart health is not fully understood, it is vital to discuss this with your doctor.

Regular blood work and other laboratory tests, as directed by your doctor, are necessary to monitor your health while taking this medication.

Additionally, this medication may interfere with certain laboratory tests. Therefore, it is essential to inform all your healthcare providers and laboratory personnel that you are taking this drug.

There is a risk of blood clots associated with this medication. If you have a history of blood clots, you should inform your doctor and discuss this further.

As this medication is an anabolic steroid, it is crucial to be aware that anabolic steroid drugs have been misused and abused, leading to dependence and severe health problems. These problems can include cardiovascular issues, stroke, liver damage, and mental or mood disorders. It is vital to discuss these risks with your doctor.

In some individuals with cancer, medications like this one have caused high calcium levels. If you experience symptoms such as weakness, confusion, fatigue, headache, nausea, vomiting, constipation, or bone pain, you should contact your doctor immediately.

If you are 65 years or older, you should use this medication with caution, as you may be more susceptible to side effects.

It is essential to note that this medication is not approved for treating low testosterone levels caused by aging. You should discuss this with your doctor.

Large doses of this medication may affect sperm production in males, potentially impacting fertility. This effect may be irreversible, even after stopping the medication. If you have concerns, you should discuss them with your doctor.
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Overdose Information

Overdose Symptoms:

  • Irritability
  • Nervousness
  • Weight gain
  • Acne
  • Frequent or prolonged erections

What to Do:

Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is supportive and symptomatic. Discontinuation of the drug may be necessary.

Drug Interactions

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Major Interactions

  • Anticoagulants (e.g., Warfarin): May increase anticoagulant activity, leading to increased risk of bleeding. Close monitoring of INR/PT is required.
  • Corticosteroids: Concomitant use may increase the risk of edema, especially in patients with cardiac, renal, or hepatic disease.
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Moderate Interactions

  • Insulin and Oral Hypoglycemics: Androgens may decrease blood glucose and insulin requirements in diabetic patients.
  • Thyroid Hormones: Androgens may decrease levels of thyroxine-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged.
  • Immunosuppressants (e.g., Cyclosporine): May increase cyclosporine levels.

Monitoring

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Baseline Monitoring

Serum Testosterone (total and free)

Rationale: To confirm diagnosis of hypogonadism and establish baseline levels.

Timing: Prior to initiation of therapy

Hematocrit (Hct) and Hemoglobin (Hgb)

Rationale: To assess for polycythemia, a common adverse effect of testosterone therapy.

Timing: Prior to initiation of therapy

Prostate-Specific Antigen (PSA)

Rationale: To screen for prostate cancer and benign prostatic hyperplasia (BPH) before initiating therapy, especially in men over 40.

Timing: Prior to initiation of therapy

Lipid Panel (Total Cholesterol, HDL, LDL, Triglycerides)

Rationale: Testosterone therapy can affect lipid profiles.

Timing: Prior to initiation of therapy

Liver Function Tests (LFTs)

Rationale: To assess baseline liver function, especially given potential for hepatic effects.

Timing: Prior to initiation of therapy

Blood Pressure

Rationale: Testosterone therapy can increase blood pressure.

Timing: Prior to initiation of therapy

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Routine Monitoring

Serum Testosterone (total)

Frequency: At 3 months after initiation, then periodically (e.g., every 6-12 months) or as clinically indicated. Measure trough levels (just before next dose).

Target: Maintain levels within the normal range (e.g., 300-1000 ng/dL).

Action Threshold: If levels are consistently above or below target range, adjust dose or frequency.

Hematocrit (Hct)

Frequency: At 3 months after initiation, then periodically (e.g., annually).

Target: <54%

Action Threshold: If Hct >54%, discontinue therapy until Hct decreases, then restart at a lower dose or consider phlebotomy.

Prostate-Specific Antigen (PSA)

Frequency: At 3-6 months after initiation, then annually for men over 40 or as clinically indicated.

Target: Stable or within normal limits for age.

Action Threshold: Significant increase in PSA or abnormal prostate exam warrants further urological evaluation.

Lipid Panel

Frequency: Periodically (e.g., annually).

Target: Within normal limits.

Action Threshold: Significant adverse changes may require intervention or re-evaluation of therapy.

Blood Pressure

Frequency: Regularly, especially during the initial weeks of therapy and with dose adjustments.

Target: Within normal limits.

Action Threshold: Persistent or significant increase in blood pressure may require dose adjustment or discontinuation.

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Symptom Monitoring

  • Signs of fluid retention (edema, weight gain)
  • Symptoms of benign prostatic hyperplasia (BPH) such as urinary urgency, frequency, nocturia, decreased stream
  • Signs of prostate cancer (e.g., urinary symptoms, bone pain)
  • Symptoms of cardiovascular events (chest pain, shortness of breath, leg swelling)
  • Mood changes, irritability, aggression
  • Sleep apnea (worsening or new onset)
  • Gynecomastia
  • Skin changes (acne, oily skin)
  • Changes in libido or sexual function

Special Patient Groups

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Pregnancy

Contraindicated in pregnant women. Testosterone can cause virilization of the female fetus.

Trimester-Specific Risks:

First Trimester: High risk of virilization of female fetus (e.g., clitoral enlargement, abnormal vaginal development).
Second Trimester: High risk of virilization of female fetus.
Third Trimester: High risk of virilization of female fetus.
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Lactation

Contraindicated in breastfeeding women. It is not known if testosterone is excreted in human milk. However, testosterone and other androgens can have virilizing effects on the breastfed infant.

Infant Risk: High risk of virilization (e.g., clitoral enlargement, hirsutism) in breastfed female infants. Potential for adverse effects on male infant development.
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Pediatric Use

Safety and effectiveness have not been established in pediatric patients. Not indicated for use in males under 18 years of age. Use in children could result in premature epiphyseal closure and precocious puberty.

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Geriatric Use

No specific dose adjustment is required based on age. However, geriatric patients may be at increased risk for prostate enlargement and prostate cancer. Close monitoring of PSA and prostate exams is essential. Increased risk of cardiovascular events and fluid retention should also be considered.

Clinical Information

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Clinical Pearls

  • Xyosted is a subcutaneous formulation of testosterone enanthate, offering a less frequent dosing schedule (once weekly) compared to daily topical gels or twice-weekly intramuscular injections.
  • The Black Box Warning for increased blood pressure is critical; baseline and ongoing blood pressure monitoring is essential. Discontinue if hypertension becomes uncontrolled.
  • Patients should be thoroughly educated on proper self-injection technique and rotation of injection sites.
  • Regular monitoring of hematocrit is crucial due to the risk of polycythemia. If Hct exceeds 54%, therapy should be interrupted or dose reduced.
  • Prostate monitoring (PSA and DRE) is vital, especially in older men, due to the potential for testosterone to stimulate prostate growth or unmask prostate cancer.
  • Patients should be advised about potential mood changes, irritability, and aggression, which can occur with testosterone therapy.
  • Consider the patient's cardiovascular risk profile before initiating and throughout therapy, given the potential for adverse cardiovascular events.
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Alternative Therapies

  • Other testosterone formulations (e.g., intramuscular injections of testosterone cypionate/enanthate, topical gels/solutions, transdermal patches, buccal tablets, nasal gel, implantable pellets)
  • Human Chorionic Gonadotropin (hCG) (for secondary hypogonadism, to stimulate endogenous testosterone production)
  • Clomiphene citrate (off-label for secondary hypogonadism, to stimulate endogenous testosterone production)
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Cost & Coverage

Average Cost: Varies widely, typically $500-$1000+ per 4x0.5ml auto-injector pack
Insurance Coverage: Tier 2 or 3 (Brand-name prescription drug, may require prior authorization)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a crucial resource for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, we encourage you to discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.