Xyosted 100mg/0.5ml Auto Inj4x0.5ml

Manufacturer ANTARES PHARMA Active Ingredient Testosterone Enanthate (Subcutaneous)(tes TOS ter one) Pronunciation zye-OH-sted (for Xyosted); tes-TOS-ter-own (for Testosterone)
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
Sep 2018
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DEA Schedule
Schedule III

Overview

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What is this medicine?

Xyosted is a medication containing testosterone, a male hormone. It is used to treat men who have low testosterone levels due to certain medical conditions. It is given as a shot under the skin once a week using an auto-injector.
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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 accompanying information carefully. This medication is administered via injection into the fatty tissue on either side of the abdomen.

If you will be self-administering the injection, your doctor or nurse will provide guidance on the proper technique. Before each use, wash your hands thoroughly. Avoid injecting into skin within 2 inches (5 cm) of the navel or into areas that are irritated, tender, bruised, red, scaly, hard, scarred, or have stretch marks.

Inspect the solution before use; do not administer if it 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 sharps container. Do not reuse needles or other materials. When the container is full, follow local regulations for 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 the missed dose is near the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not administer two doses at once or take extra doses.
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Lifestyle & Tips

  • Maintain a healthy diet and exercise regularly to support overall health and manage potential side effects like weight gain or lipid changes.
  • Report any new or worsening symptoms, especially those related to heart problems, blood clots, or prostate issues, to your doctor immediately.
  • Do not share your auto-injector with anyone else.
  • Store Xyosted at room temperature, away from light and moisture.

Dosing & Administration

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Adult Dosing

Standard Dose: 100 mg (0.5 mL) administered subcutaneously once weekly
Dose Range: 50 - 100 mg

Condition-Specific Dosing:

initial: 100 mg (0.5 mL) subcutaneously once weekly
dose_adjustment: Adjust dose based on serum testosterone levels and clinical response. Serum testosterone levels should be measured approximately 7 days after the previous dose (just prior to the next dose). If the average trough serum testosterone concentration is below 350 ng/dL, the dose may be increased to 120 mg (0.6 mL) once weekly. If the average trough serum testosterone concentration is above 650 ng/dL, the dose may be decreased to 80 mg (0.4 mL) once weekly. If the average trough serum testosterone concentration is above 1000 ng/dL, discontinue Xyosted until levels return to normal, then restart at 50 mg (0.25 mL) once weekly. The maximum recommended dose is 120 mg once weekly.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Safety and effectiveness in pediatric patients less than 18 years of age have not been established. Use in pediatric patients is not recommended.)
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: Not studied. Use with caution and monitor closely.
Dialysis: Not studied. Use with caution and monitor closely.

Hepatic Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: Not studied. Use with caution and monitor closely.
Severe: Not studied. Contraindicated in severe hepatic impairment due to potential for fluid retention and exacerbation of liver disease.

Pharmacology

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Mechanism of Action

Endogenous androgens, including testosterone, are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. Testosterone enanthate is an ester of the androgen testosterone. Following subcutaneous injection, testosterone enanthate is hydrolyzed to release testosterone. Testosterone then binds to androgen receptors in target tissues, activating gene transcription and protein synthesis, leading to the development and maintenance of male characteristics.
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Pharmacokinetics

Absorption:

Bioavailability: Not directly quantified for SC, but slowly absorbed from the subcutaneous depot.
Tmax: Approximately 2 days (for total testosterone after SC injection)
FoodEffect: Not applicable (parenteral administration)

Distribution:

Vd: Approximately 1 L/kg (for testosterone)
ProteinBinding: Approximately 98% (to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration: Yes (testosterone can cross the blood-brain barrier)

Elimination:

HalfLife: Approximately 8.4 days (for total testosterone after SC injection of Xyosted)
Clearance: Approximately 13.2 mL/min/kg (for testosterone)
ExcretionRoute: Urine (approximately 90%) and feces (approximately 6%)
Unchanged: Less than 6% (of testosterone excreted unchanged in urine)
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Pharmacodynamics

OnsetOfAction: Gradual (weeks to months for full therapeutic effect)
PeakEffect: Within 2-3 months of consistent dosing
DurationOfAction: Approximately 1 week (due to enanthate ester and SC depot)

Safety & Warnings

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BLACK BOX WARNING

Venous Thromboembolism (VTE): Cases of serious VTE, including deep vein thrombosis (DVT) and pulmonary embolism (PE), have been reported in patients using testosterone products. Evaluate patients with symptoms of VTE. If a VTE is suspected, discontinue Xyosted and initiate appropriate workup and management.
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Side Effects

Serious Side Effects: Seek Medical Attention Immediately

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 medical help right away:

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 attention 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. Many people may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:

Headache
Acne
Diarrhea
Emotional changes
Fatigue or weakness
Trouble sleeping
* Irritation at the site of application

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact 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:

  • Chest pain, shortness of breath, or discomfort in the upper body (signs of heart attack)
  • Sudden weakness or numbness on one side of the body, sudden severe headache, or vision changes (signs of stroke)
  • Pain, swelling, warmth, or redness in the leg (signs of deep vein thrombosis)
  • Sudden shortness of breath, chest pain, or coughing up blood (signs of pulmonary embolism)
  • Difficulty urinating, frequent urination, or weak urine stream (signs of prostate enlargement or cancer)
  • Swelling in the ankles, feet, or hands (signs of fluid retention)
  • Yellowing of the skin or eyes, dark urine, or severe stomach pain (signs of liver problems)
  • Increased irritability, aggression, or mood swings
  • New or worsening sleep apnea (loud snoring, gasping for air during sleep)
  • Breast tenderness or enlargement (gynecomastia)
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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, so it is crucial to discuss this 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 vital 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 with your other medications and health conditions. Never start, stop, or adjust the dose 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. Discuss this potential risk with your doctor.

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

Individuals with sleep apnea should consult their doctor, as this condition may be exacerbated by testosterone treatment.

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 essential to discuss this with your doctor.

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

Additionally, inform all your healthcare providers and laboratory personnel that you are taking this medication, as it may affect the results of certain lab tests.

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

As this medication is an anabolic steroid, it is crucial to be aware that anabolic steroid abuse can lead to dependence and severe health problems, including cardiovascular issues, stroke, liver damage, and mental or mood disorders. Discuss the risks and benefits with your doctor.

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

If you are 65 years or older, 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. Discuss the rationale for your treatment with your doctor.

Lastly, high doses of this medication may affect sperm production in males, potentially impacting fertility. This effect may be irreversible even after the medication is discontinued. If you have concerns, consult your doctor.
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Overdose Information

Overdose Symptoms:

  • Irritability
  • Nervousness
  • Weight gain
  • Acne
  • Polycythemia (high red blood cell count, symptoms like headache, dizziness, fatigue)
  • Priapism (prolonged, painful erection)

What to Do:

Seek immediate medical attention. Overdose symptoms are typically managed by discontinuing the medication and providing supportive care. Call 1-800-222-1222 (Poison Control) for advice.

Drug Interactions

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Major Interactions

  • Anticoagulants (e.g., warfarin): May increase anticoagulant activity, leading to increased risk of bleeding. Monitor INR/PT closely.
  • Corticosteroids: Concomitant use may increase the risk of edema.
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Moderate Interactions

  • Insulin and oral hypoglycemics: Testosterone may decrease blood glucose, requiring adjustment of antidiabetic medication dosage.
  • Thyroid hormones: May decrease levels of thyroid-binding globulin, leading to increased free thyroid hormone levels. No clinical significance usually, but monitor thyroid function if symptoms arise.
  • Adrenocorticotropic hormone (ACTH): May increase risk of edema.

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.

Timing: Prior to initiation of therapy

Prostate-Specific Antigen (PSA)

Rationale: To screen for prostate cancer and benign prostatic hyperplasia (BPH) in men over 40-50 years, especially those with risk factors.

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 in patients with pre-existing hepatic conditions.

Timing: Prior to initiation of therapy

Bone Mineral Density (BMD)

Rationale: Consider in hypogonadal men with risk factors for osteoporosis.

Timing: Prior to initiation of therapy

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Routine Monitoring

Serum Testosterone (trough)

Frequency: Approximately 7 days after the previous dose (just prior to the next dose) at Weeks 6 and 12, then periodically (e.g., every 3-6 months) thereafter.

Target: 350-650 ng/dL

Action Threshold: Below 350 ng/dL (consider dose increase); Above 650 ng/dL (consider dose decrease); Above 1000 ng/dL (discontinue and restart at lower dose).

Hematocrit (Hct)

Frequency: At Weeks 6 and 12, then periodically (e.g., every 3-6 months) thereafter.

Target: <54%

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

Prostate-Specific Antigen (PSA)

Frequency: At 3-6 months, then annually thereafter (or more frequently based on age and risk factors).

Target: Stable or within normal limits for age

Action Threshold: Significant increase from baseline or age-specific normal range, or abnormal prostate exam (refer to urologist).

Lipid Panel

Frequency: Annually or as clinically indicated.

Target: Within normal limits

Action Threshold: Significant adverse changes (consider intervention or therapy adjustment).

Liver Function Tests (LFTs)

Frequency: Periodically, especially if symptoms of liver dysfunction develop.

Target: Within normal limits

Action Threshold: Significant elevation (investigate cause, consider therapy adjustment).

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Symptom Monitoring

  • Signs of polycythemia (e.g., headache, dizziness, fatigue, shortness of breath)
  • Signs of benign prostatic hyperplasia (BPH) progression (e.g., urinary frequency, urgency, nocturia, weak stream)
  • Signs of prostate cancer (e.g., urinary symptoms, bone pain)
  • Cardiovascular symptoms (e.g., chest pain, shortness of breath, edema, leg pain/swelling)
  • Mood changes (e.g., irritability, aggression, depression)
  • Sleep apnea (worsening or new onset)
  • Gynecomastia (breast tenderness or enlargement)
  • Fluid retention/edema (swelling in ankles, feet, hands)
  • Skin changes at injection site (pain, bruising, irritation)

Special Patient Groups

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Pregnancy

Contraindicated in pregnant women. Testosterone can cause virilization of the female fetus, including clitoral enlargement, abnormal vaginal development, and fusion of genital folds.

Trimester-Specific Risks:

First Trimester: High risk of virilization of female fetus.
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, due to the potential for serious adverse reactions in the breastfed infant, including virilization, Xyosted is contraindicated during lactation.

Infant Risk: High (potential for virilization)
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Pediatric Use

Safety and effectiveness have not been established in pediatric patients less than 18 years of age. Use in pediatric patients is not recommended. Androgen therapy in prepubertal males may accelerate bone maturation without producing compensatory gain in linear growth, resulting in compromised adult stature.

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Geriatric Use

Geriatric patients treated with androgens may be at an increased risk for the development of prostate hypertrophy and prostate carcinoma. Increased risk of cardiovascular events and fluid retention. Close monitoring of PSA, Hct, and cardiovascular status is essential.

Clinical Information

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Clinical Pearls

  • Xyosted is a subcutaneous auto-injector, offering a convenient alternative to intramuscular injections or daily topical applications for testosterone replacement.
  • Trough testosterone levels should be measured approximately 7 days after the previous dose (just prior to the next dose) to guide dose adjustments.
  • Patients should be educated on proper injection technique for the auto-injector.
  • Emphasize the importance of regular monitoring for hematocrit, PSA, and lipid profiles due to potential adverse effects.
  • Counsel patients on the black box warning regarding venous thromboembolism and the general class warning for cardiovascular risks.
  • Not indicated for age-related decline in testosterone without a clear diagnosis of hypogonadism.
  • Consider alternative formulations if injection site reactions are problematic or if weekly administration is not preferred.
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Alternative Therapies

  • Testosterone cypionate (IM injection)
  • Testosterone enanthate (IM injection)
  • Testosterone undecanoate (IM injection, oral capsule)
  • Testosterone transdermal patches (Androderm)
  • Testosterone topical gels (AndroGel, Testim, Fortesta, Vogelxo)
  • Testosterone buccal system (Striant)
  • Testosterone subcutaneous pellets (Testopel)
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Cost & Coverage

Average Cost: Approximately $500 - $800 per 4x0.5ml auto-injector pack
Insurance Coverage: Tier 2 or Tier 3 (Specialty drug, may require prior authorization)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.

This medication is accompanied by a Medication Guide, a patient fact sheet that provides crucial information. Please read it carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult 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. Be prepared to provide detailed information about the incident, including the medication taken, the amount, and the time it occurred.