Testosterone 1.62%(40.5mg/2.5gm)pkt

Manufacturer ACTAVIS Active Ingredient Testosterone Gel(tes TOS ter one) Pronunciation tes TOS ter one
WARNING: Wash the site where the drug was used before it touches anyone else's skin.Do not let this drug or the treated area touch anyone else's skin. They could have side effects from touching this drug. Cover the treated area with clothes.If a female or a child touches the gel, they will need to wash their skin with soap and water. @ COMMON USES: It is used to treat low testosterone levels.
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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
Aug 2009
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DEA Schedule
Schedule III

Overview

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What is this medicine?

Testosterone gel is a medication applied to the skin daily to replace the hormone testosterone in men who have low levels (hypogonadism). It helps improve symptoms like low energy, reduced sex drive, and muscle weakness.
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How to Use This Medicine

Proper Use of This Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. Use this medication only on your skin, as directed. It is essential to wash your hands before and after applying the medication.

Application Instructions

Apply the medication at the same time every day.
Be aware that different products may have varying strengths, so carefully read and follow the label instructions.
Avoid getting the medication on other parts of your body or on other people.
Do not apply the medication to the genital area.
Keep the medication out of your eyes.

Special Instructions for Pump and Packet Products

If you are using a pump, prime it before the first use, following the instructions in the package insert.
If you are using a packet, follow the instructions provided.

Post-Application Instructions

After applying the medication, wait for a specified amount of time before bathing, showering, or swimming. Refer to the package insert for details on the waiting period.
Allow the medication to dry completely before covering the treated area with clothing.
Avoid exposure to fire, flames, or smoking until the medication is dry.
Apply the medication to clean, dry, healthy skin.

Specific Application Sites

Certain products are designed for use on specific areas of the body. Be sure to read the package insert to understand where to apply the medication.

Storage and Disposal

Store the medication at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding storage in a bathroom.
Protect the medication from heat or open flames.

Missed Dose Instructions

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

  • Apply the gel to clean, dry, intact skin of the shoulders, upper arms, or abdomen once daily, preferably in the morning.
  • Wash hands thoroughly with soap and water immediately after applying the gel.
  • Allow the application site to dry completely before dressing. Cover the application site with clothing to prevent transfer to others.
  • Avoid swimming, showering, or washing the application site for at least 2-5 hours after application (check specific product instructions).
  • Avoid skin-to-skin contact with women or children at the application site to prevent accidental transfer of testosterone.
  • If contact occurs, the exposed individual should wash the affected skin area immediately with soap and water.
  • Regular exercise and a balanced diet can support overall health during therapy.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial dose: 40.5 mg (one packet or 2 pump actuations) applied once daily to shoulders, upper arms, or abdomen. Dose adjustment based on serum testosterone levels.
Dose Range: 40.5 - 81 mg

Condition-Specific Dosing:

hypogonadism: Initial dose 40.5 mg daily. Adjust based on serum testosterone levels (target 300-1000 ng/dL) and clinical response. Maximum recommended dose is 81 mg daily.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Safety and efficacy not established for hypogonadism. Use in delayed puberty is off-label and requires careful consideration.)
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment, monitor for fluid retention.
Moderate: No specific adjustment, monitor for fluid retention.
Severe: No specific adjustment, monitor for fluid retention and adverse effects. Use with caution.
Dialysis: Considerations: Use with caution, monitor closely for fluid retention and other adverse effects.

Hepatic Impairment:

Mild: No specific adjustment, monitor liver function.
Moderate: Use with caution, monitor liver function and adverse effects.
Severe: Contraindicated or use with extreme caution; testosterone is extensively metabolized by the liver.

Pharmacology

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Mechanism of Action

Testosterone and its active metabolite, dihydrotestosterone (DHT), bind to androgen receptors in target tissues. This hormone-receptor complex translocates to the cell nucleus, where it binds to specific DNA sequences (androgen response elements), stimulating gene transcription and protein synthesis. This leads to the development and maintenance of male primary and secondary sexual characteristics.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 9-14% (transdermal absorption varies)
Tmax: 4-12 hours (for serum testosterone after application)
FoodEffect: Not applicable (topical administration)

Distribution:

Vd: Approximately 1 L/kg
ProteinBinding: Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Endogenous testosterone: 10-100 minutes; Effective half-life from gel: approximately 24 hours (due to reservoir effect in skin)
Clearance: Not readily quantifiable for transdermal
ExcretionRoute: Approximately 90% in urine (as glucuronic and sulfuric acid conjugates), approximately 6% in feces (unconjugated metabolites)
Unchanged: <6% (in urine)
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Pharmacodynamics

OnsetOfAction: Clinical effects (e.g., libido, energy) may take weeks to months; serum levels reach steady state within days.
PeakEffect: Serum testosterone levels peak within 4-12 hours after daily application.
DurationOfAction: Approximately 24 hours (requiring daily application)

Safety & Warnings

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BLACK BOX WARNING

WARNING: SECONDARY EXPOSURE TO TESTOSTERONE. Cases of secondary exposure resulting in virilization of children and women have been reported. Testosterone gel can transfer from the patient to others in close contact. Patients should be advised to strictly adhere to recommended application instructions to minimize the potential for secondary exposure.
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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 medical attention immediately:

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
Changes in skin color
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
Signs of liver problems, including:
+ 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

Reporting Side Effects

This list is not exhaustive, and you may experience other 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:

  • Signs of virilization in women or children (e.g., new or increased body hair, acne, voice changes, increased libido, enlarged clitoris in females; enlarged penis, pubic hair, aggressive behavior in children).
  • Swelling in your ankles, feet, or hands (fluid retention).
  • Difficulty breathing, especially at night (worsening sleep apnea).
  • Chest pain, shortness of breath, or pain/swelling in your leg (signs of blood clot or cardiovascular event).
  • Frequent or difficult urination, changes in urine stream (signs of prostate issues).
  • Breast tenderness or enlargement.
  • Nausea, vomiting, yellowing of skin or eyes (signs of liver problems).
  • Unexplained weight gain.
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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. Be sure to describe the allergic reaction you experienced.
If you are a male with a history of breast or prostate cancer.
If you have any pre-existing medical conditions, such as heart disease, kidney disease, or liver disease.
If you are female, as this medication is not approved for use in women. Additionally, if you are pregnant, plan to become pregnant, or are breastfeeding, discuss the potential risks with your doctor, as this medication may harm an unborn baby.
* If the patient is a child, as this medication is not intended for pediatric use.

This is not an exhaustive list of all possible interactions. Therefore, it is crucial to inform your doctor and pharmacist about all the medications you are taking (including prescription and over-the-counter drugs, natural products, and vitamins) and any health problems you have. This will help ensure your safety while taking this medication. Never start, stop, or change 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, you will need to closely monitor your blood sugar levels.

There may be an increased risk of developing prostate cancer. Discuss this with your doctor.

If you have an enlarged prostate, your symptoms may worsen while using this medication. Contact your doctor if you experience any changes.

If you have sleep apnea, consult with your doctor, as this medication may exacerbate the condition.

This medication may cause high blood pressure, which can increase the risk of heart attack, stroke, or death from heart disease. Have your blood pressure checked regularly, as advised by your doctor. If you have pre-existing high blood pressure or heart disease, discuss this with your doctor.

Treatment with this medication may lead to increased cholesterol and triglyceride levels. The impact of these changes on heart health is unknown, so it is crucial to discuss this with your doctor.

Regularly undergo blood work and other laboratory tests as directed by your doctor. This medication may affect the results of certain lab tests, so inform all your healthcare providers and laboratory personnel that you are taking this medication.

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 damage, 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 a child or female accidentally comes into contact with the gel or solution, they may experience adverse effects. In children, these can include aggressive behavior, enlarged sex organs, and premature pubic hair growth. In females, these can include a deepened voice, changes in body hair, or acne. If this occurs, contact your doctor right away.

If a pregnant individual is exposed to the gel or solution, 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 be irreversible, even after stopping the medication. If you have concerns, discuss them with your doctor.
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Overdose Information

Overdose Symptoms:

  • Irritability
  • Nervousness
  • Acne
  • Hair loss
  • Headache
  • Priapism (prolonged, painful erection)

What to Do:

Discontinue the medication and seek medical attention. Treatment is supportive. Call 1-800-222-1222 (Poison Control Center).

Drug Interactions

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Major Interactions

  • Oral anticoagulants (e.g., warfarin): May increase anticoagulant activity, leading to increased risk of bleeding. Monitor INR/PT closely.
  • Corticosteroids (e.g., prednisone): 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: Testosterone may decrease blood glucose levels, potentially requiring a reduction in insulin or oral hypoglycemic dosage.
  • Thyroid hormones: May decrease levels of thyroid-binding globulin, leading to increased free thyroid hormone levels. No change in thyroid hormone dose is usually needed, but monitor for signs of hyperthyroidism.
  • Immunosuppressants (e.g., cyclosporine): Potential for altered metabolism, though clinical significance is often low.

Monitoring

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Baseline Monitoring

Serum Testosterone (total and free)

Rationale: To confirm diagnosis of hypogonadism and establish baseline for therapy.

Timing: Before initiation of therapy (morning levels, ideally two separate measurements)

Prostate-Specific Antigen (PSA)

Rationale: To screen for prostate cancer before initiating therapy, especially in men over 40.

Timing: Before initiation of therapy

Hematocrit (Hct)

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

Timing: Before initiation of therapy

Lipid Panel

Rationale: To assess cardiovascular risk factors.

Timing: Before initiation of therapy

Liver Function Tests (LFTs)

Rationale: To assess baseline liver function, as testosterone is metabolized by the liver.

Timing: Before initiation of therapy

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Routine Monitoring

Serum Testosterone (total)

Frequency: 2-4 weeks after initiation or dose adjustment, then every 3-6 months, then annually

Target: 300-1000 ng/dL (or within normal physiological range)

Action Threshold: If consistently >1000 ng/dL, reduce dose or discontinue. If consistently <300 ng/dL, consider dose increase.

Hematocrit (Hct)

Frequency: At 3 and 6 months after initiation, then annually

Target: <54%

Action Threshold: If Hct >54%, reduce dose, temporarily discontinue, or consider phlebotomy.

Prostate-Specific Antigen (PSA)

Frequency: Annually (more frequently in men >50 or with prostate risk factors)

Target: Stable or within age-appropriate limits

Action Threshold: Significant increase from baseline or abnormal findings warrant further urological evaluation.

Digital Rectal Exam (DRE)

Frequency: Annually (in men >50 or with prostate risk factors)

Target: Normal findings

Action Threshold: Abnormal findings warrant further urological evaluation.

Lipid Panel

Frequency: Annually

Target: Within normal limits

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

Liver Function Tests (LFTs)

Frequency: Periodically, especially if signs of hepatic dysfunction or with concomitant hepatotoxic drugs

Target: Within normal limits

Action Threshold: Significant elevations may require dose reduction or discontinuation.

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Symptom Monitoring

  • Signs of virilization in women or children (e.g., voice deepening, hirsutism, clitoromegaly)
  • Fluid retention/edema (swelling of ankles, feet, hands)
  • Signs of prostate enlargement (e.g., urinary frequency, urgency, nocturia, decreased stream)
  • Breast tenderness or enlargement (gynecomastia)
  • Mood changes (e.g., irritability, aggression)
  • Sleep apnea (worsening or new onset)
  • Skin reactions at application site (e.g., irritation, rash)
  • Signs of cardiovascular events (e.g., chest pain, shortness of breath, leg pain/swelling)

Special Patient Groups

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Pregnancy

Contraindicated. Testosterone can cause virilization of a female fetus.

Trimester-Specific Risks:

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

Contraindicated. It is unknown if testosterone is excreted in human milk. Due to the potential for serious adverse reactions in the breastfed infant, testosterone is not recommended during lactation.

Infant Risk: High risk of virilization in breastfed infant.
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Pediatric Use

Not indicated for the treatment of hypogonadism in pediatric patients. Safety and efficacy have not been established. Use in delayed puberty is off-label and requires careful consideration due to potential for premature epiphyseal closure and virilization.

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Geriatric Use

Increased risk of prostate enlargement (BPH), prostate cancer, and cardiovascular events. Careful monitoring of PSA, DRE, hematocrit, and cardiovascular status is essential. Lower starting doses and slower titration may be considered.

Clinical Information

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Clinical Pearls

  • Emphasize strict adherence to application instructions to prevent secondary exposure to women and children.
  • Monitor hematocrit closely due to the risk of erythrocytosis, which may require dose reduction or phlebotomy.
  • Testosterone therapy is contraindicated in men with known or suspected prostate cancer or breast cancer.
  • Educate patients on signs of fluid retention and advise them to report these symptoms.
  • Consider baseline and regular monitoring of PSA and DRE, especially in older men, due to the potential impact on prostate health.
  • Patients should be aware that clinical benefits (e.g., improved libido, energy) may take several weeks to months to become apparent.
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Alternative Therapies

  • Testosterone injections (e.g., testosterone cypionate, enanthate)
  • Testosterone patches (e.g., Androderm)
  • Testosterone buccal system (e.g., Striant)
  • Testosterone pellets (e.g., Testopel)
  • Testosterone nasal gel (e.g., Natesto)
  • 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: $300 - $600+ per 30-day supply (for brand)
Generic Available: Yes
Insurance Coverage: Varies by insurance plan (often Tier 2 or 3 for brand, Tier 1 for generic)
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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, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or other healthcare provider for clarification.

In the event of a suspected overdose, it's crucial to seek immediate medical attention or contact your local poison control center. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred. This information will help healthcare professionals provide you with the most effective treatment.