Xyosted 50mg/0.5ml Auto Inj 4x0.5ml
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.
Drug Class
Androgen
Pharmacologic Class
Androgen receptor agonist
Pregnancy Category
Category X
FDA Approved
Oct 2018
DEA Schedule
Schedule III
Overview
What is this medicine?
Xyosted is a medicine containing testosterone, a male hormone. It is used to treat men who have low testosterone levels due to certain medical conditions. It comes as an auto-injector that you give yourself as a shot under the skin, usually once a week. It helps to restore testosterone levels, which can improve symptoms like low energy, low sex drive, and muscle weakness.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. 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 injecting, wash your hands thoroughly. Avoid injecting into skin that is:
Within 2 inches (5 cm) of your belly button
Irritated, tender, bruised, red, scaly, hard, scarred, or has stretch marks
Inspect the solution before use. Do not use if it is:
Cloudy
Leaking
Contains particles
Has changed color (the solution should be colorless to a faint yellow)
Properly dispose of used needles in a designated needle/sharp disposal box. Do not reuse needles or other items. When the box is full, follow local regulations for disposal. If you have any questions, consult your doctor or pharmacist.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in its original container and avoid storing it in a bathroom. Do not freeze the medication.
Missing a Dose
If you miss a dose, take 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 the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. 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 injecting, wash your hands thoroughly. Avoid injecting into skin that is:
Within 2 inches (5 cm) of your belly button
Irritated, tender, bruised, red, scaly, hard, scarred, or has stretch marks
Inspect the solution before use. Do not use if it is:
Cloudy
Leaking
Contains particles
Has changed color (the solution should be colorless to a faint yellow)
Properly dispose of used needles in a designated needle/sharp disposal box. Do not reuse needles or other items. When the box is full, follow local regulations for disposal. If you have any questions, consult your doctor or pharmacist.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in its original container and avoid storing it in a bathroom. Do not freeze the medication.
Missing a Dose
If you miss a dose, take 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 the same time or take extra doses.
Lifestyle & Tips
- Administer the injection exactly as prescribed by your doctor, usually once a week. Do not inject more often than prescribed.
- Rotate injection sites (abdomen, thigh) to avoid skin irritation.
- Follow up with your doctor for regular blood tests to monitor testosterone levels, blood count, prostate health, and lipids.
- Report any new or worsening symptoms, especially those related to heart problems, blood clots, or prostate issues.
- Maintain a healthy lifestyle, including regular exercise and a balanced diet, to support overall health and manage potential side effects like blood pressure changes.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
50 mg (0.5 mL) administered subcutaneously once weekly
Dose Range:
50 - 100 mg
Condition-Specific Dosing:
initial_dose:
50 mg (0.5 mL) once weekly
dose_adjustment:
Dose may be adjusted based on serum testosterone levels and clinical response, up to a maximum of 100 mg (1 mL) once weekly. Serum testosterone levels should be measured approximately 7 days after the previous dose (just prior to the next dose). If the serum testosterone concentration is below 350 ng/dL, the dose may be increased to 75 mg (0.75 mL) once weekly. If the serum testosterone concentration is 350 to 800 ng/dL, the dose should remain at 50 mg once weekly. If the serum testosterone concentration is greater than 800 ng/dL, the dose should be decreased to 25 mg (0.25 mL) once weekly or therapy should be temporarily withheld. If the serum testosterone concentration is greater than 1000 ng/dL, therapy should be temporarily withheld and restarted at a lower dose once the testosterone concentration returns to the normal range.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Safety and efficacy not established in pediatric patients <18 years of age. Use in pediatric patients is not recommended.)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but caution advised.
Moderate:
No specific dose adjustment recommended, but caution advised.
Severe:
No specific dose adjustment recommended, but caution advised. Monitor closely for adverse effects.
Dialysis:
Considerations: Not specifically studied. Use with caution and monitor testosterone levels and adverse effects.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended, but caution advised.
Moderate:
No specific dose adjustment recommended, but caution advised.
Severe:
Contraindicated in patients with severe hepatic impairment due to potential for fluid retention and exacerbation of liver disease.
Pharmacology
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 testosterone, which is converted to testosterone in vivo. Testosterone acts by binding to androgen receptors in target tissues, leading to gene transcription and protein synthesis, mediating its effects on sexual differentiation, spermatogenesis, muscle mass, bone density, and erythropoiesis.
Pharmacokinetics
Absorption:
Bioavailability:
Not directly quantifiable for subcutaneous injection, but provides sustained release.
Tmax:
Approximately 2 days (for testosterone after subcutaneous injection of testosterone enanthate).
FoodEffect:
Not applicable for subcutaneous injection.
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 and effects in the CNS are complex).
Elimination:
HalfLife:
Approximately 8.4 days (for testosterone after subcutaneous injection of testosterone enanthate).
Clearance:
Approximately 13.2 mL/min/kg (for testosterone).
ExcretionRoute:
Mainly renal (approximately 90% as conjugates of testosterone and its metabolites), fecal (approximately 6%).
Unchanged:
Less than 6% (excreted unchanged in urine).
Pharmacodynamics
OnsetOfAction:
Gradual, typically within weeks for clinical effects (e.g., increased libido, energy).
PeakEffect:
Serum testosterone levels peak within 2 days after injection, but clinical effects are more gradual.
DurationOfAction:
Approximately 1 week (due to the enanthate ester providing sustained release).
Safety & Warnings
BLACK BOX WARNING
Increases in Blood Pressure: Xyosted can cause increases in blood pressure that can increase the risk of major adverse cardiovascular events, 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 treat new-onset hypertension or exacerbations of pre-existing hypertension.
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 during sleep
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, such as:
+ 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. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, 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.
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 during sleep
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, such as:
+ 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. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, 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.
Seek Immediate Medical Attention If You Experience:
- Sudden chest pain or discomfort
- Shortness of breath
- Weakness or numbness on one side of the body
- Slurred speech
- Sudden severe headache
- Pain, swelling, or redness in a leg (signs of a blood clot)
- Difficulty urinating, frequent urination, or weak urine stream
- Swelling in ankles, feet, or hands
- Unexplained weight gain
- Changes in mood, aggression, or irritability
- Sleep disturbances, especially worsening sleep apnea
- Yellowing of skin or eyes (jaundice)
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. Be sure to describe the allergic reaction you experienced.
If you are a male with breast or prostate cancer.
If you have a history of certain health conditions, including heart disease, kidney disease, or liver disease.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in pregnant or breastfeeding women, so it is crucial to discuss this with your doctor.
* If you are 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 consulting your doctor first.
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. Be sure to describe the allergic reaction you experienced.
If you are a male with breast or prostate cancer.
If you have a history of certain health conditions, including heart disease, kidney disease, or liver disease.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in pregnant or breastfeeding women, so it is crucial to discuss this with your doctor.
* If you are 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 consulting your doctor first.
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, you will need to closely monitor your blood sugar levels.
There is a potential increased risk of prostate cancer associated with this medication. You should discuss this with your doctor. Additionally, if you have an enlarged prostate, your symptoms may worsen while using this drug. If this occurs, contact your doctor promptly.
If you have sleep apnea, consult with your doctor, as this condition may worsen with testosterone treatment. This medication may also lead to elevated cholesterol and triglyceride levels, and the impact of these changes on heart health is not fully understood. Discuss this with your doctor.
As directed by your doctor, have your blood work and other laboratory tests checked regularly. Be aware that this medication may affect certain lab tests, so 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, inform your doctor. This medication is an anabolic steroid, and misuse or abuse of anabolic steroids can lead to dependence and severe health problems, including cardiovascular issues, stroke, liver problems, and mental or mood disorders. Discuss the 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, contact your doctor immediately.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. This medication is not approved for treating low testosterone levels caused by aging. Discuss this with your doctor.
High doses of this medication may affect sperm production in males, potentially impacting fertility. This effect may not be reversible after stopping the medication. If you have concerns, discuss them with your doctor.
There is a potential increased risk of prostate cancer associated with this medication. You should discuss this with your doctor. Additionally, if you have an enlarged prostate, your symptoms may worsen while using this drug. If this occurs, contact your doctor promptly.
If you have sleep apnea, consult with your doctor, as this condition may worsen with testosterone treatment. This medication may also lead to elevated cholesterol and triglyceride levels, and the impact of these changes on heart health is not fully understood. Discuss this with your doctor.
As directed by your doctor, have your blood work and other laboratory tests checked regularly. Be aware that this medication may affect certain lab tests, so 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, inform your doctor. This medication is an anabolic steroid, and misuse or abuse of anabolic steroids can lead to dependence and severe health problems, including cardiovascular issues, stroke, liver problems, and mental or mood disorders. Discuss the 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, contact your doctor immediately.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. This medication is not approved for treating low testosterone levels caused by aging. Discuss this with your doctor.
High doses of this medication may affect sperm production in males, potentially impacting fertility. This effect may not be reversible after stopping the medication. If you have concerns, discuss them with your doctor.
Overdose Information
Overdose Symptoms:
- Headache
- Nausea
- Vomiting
- Diarrhea
- Fluid retention (edema)
- Irritability
- Nervousness
- Increased blood pressure
- Polycythemia (high red blood cell count)
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Discontinue the medication and monitor for adverse effects.
Drug Interactions
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.
Moderate Interactions
- Insulin and oral hypoglycemics: Androgens may decrease blood glucose, requiring adjustment of antidiabetic medication dosage.
- Adrenocorticotropic hormone (ACTH): May increase risk of edema.
- Thyroid hormones: May decrease levels of thyroid-binding globulin, leading to increased free thyroid hormone levels (clinical significance usually minimal).
Monitoring
Baseline Monitoring
Serum Testosterone (total and free)
Rationale: To confirm diagnosis of hypogonadism and establish baseline levels.
Timing: Prior to initiation of therapy (usually 2-3 morning samples).
Hematocrit (Hct) and Hemoglobin (Hgb)
Rationale: Testosterone can stimulate erythropoiesis, increasing risk of polycythemia.
Timing: Prior to initiation of therapy.
Prostate-Specific Antigen (PSA)
Rationale: To screen for prostate cancer and benign prostatic hyperplasia (BPH). Testosterone can stimulate prostate growth.
Timing: Prior to initiation of therapy (in men ≥40 years with BPH or ≥50 years without BPH).
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 hepatic metabolism.
Timing: Prior to initiation of therapy.
Blood Pressure
Rationale: Xyosted has a Black Box Warning for increased blood pressure.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum Testosterone (total)
Frequency: At 6 weeks, then periodically (e.g., every 3-6 months) after dose stabilization.
Target: 350-800 ng/dL (trough level, prior to next dose).
Action Threshold: If <350 ng/dL, consider dose increase. If >800 ng/dL, consider dose decrease or temporary cessation. If >1000 ng/dL, temporarily withhold.
Hematocrit (Hct)
Frequency: At 3-6 months, then 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, then annually (or more frequently if clinically indicated).
Target: Age-dependent, stable.
Action Threshold: Significant increase from baseline or age-specific normal range, or abnormal digital rectal exam (DRE), warrants further urological evaluation.
Lipid Panel
Frequency: Annually.
Target: Normal ranges.
Action Threshold: Significant adverse changes may require intervention or re-evaluation of therapy.
Blood Pressure
Frequency: Regularly, especially during initial treatment and dose adjustments.
Target: Normal ranges.
Action Threshold: Significant increase warrants intervention and re-evaluation of therapy.
Symptom Monitoring
- Signs of polycythemia (e.g., headache, dizziness, fatigue, shortness of breath)
- Signs of prostate enlargement (e.g., urinary hesitancy, frequency, nocturia, decreased stream)
- Signs of fluid retention (e.g., edema, weight gain)
- Signs of cardiovascular events (e.g., chest pain, shortness of breath, leg pain, weakness on one side of the body)
- Mood changes, irritability, aggression
- Sleep apnea exacerbation
- Breast tenderness or enlargement (gynecomastia)
- Skin changes (e.g., acne, oily skin)
Special Patient Groups
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.
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 breastfeeding.
Infant Risk:
L5 (Contraindicated - high risk of adverse effects, including virilization, in breastfed infant).
Pediatric Use
Safety and efficacy have not been established in pediatric patients (<18 years of age). Use in pediatric patients is not recommended. Androgen therapy in prepubertal males can cause premature epiphyseal closure and precocious puberty.
Geriatric Use
Geriatric patients treated with androgens may be at an increased risk for the development of prostate hyperplasia and prostate carcinoma. Increased monitoring for prostate health (PSA and DRE) is recommended. Older patients may also be more susceptible to fluid retention and cardiovascular effects.
Clinical Information
Clinical Pearls
- Xyosted is the first and only FDA-approved subcutaneous testosterone enanthate auto-injector for once-weekly administration.
- It is crucial to monitor blood pressure regularly due to the Black Box Warning for increased blood pressure.
- Patients should be trained on proper subcutaneous injection technique and rotation of injection sites.
- Trough testosterone levels should be measured approximately 7 days after the previous dose (just prior to the next dose) to guide dose adjustments.
- Polycythemia is a common side effect; regular hematocrit monitoring is essential. If Hct >54%, therapy should be temporarily discontinued.
- Testosterone therapy is contraindicated in men with known or suspected prostate cancer or breast cancer.
- Patients should be advised about the potential for abuse and misuse of testosterone, especially by athletes or bodybuilders.
Alternative Therapies
- Other testosterone formulations (e.g., intramuscular injections of testosterone cypionate or enanthate, transdermal patches, gels, buccal systems, 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)
Cost & Coverage
Average Cost:
Approximately $1000 - $1500 per 4x0.5ml auto-injector pack
Insurance Coverage:
Tier 2 or 3 (Specialty drug, may require prior authorization)
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 important 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 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. Be prepared to provide critical information, including the name of the medication taken, the amount, and the time it happened, to help healthcare professionals provide the best possible care.
This medication is accompanied by a Medication Guide, a patient fact sheet that provides important 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 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. Be prepared to provide critical information, including the name of the medication taken, the amount, and the time it happened, to help healthcare professionals provide the best possible care.