Dosing & Uses
Dosage Forms & Strengths
tablet: Schedule III
- 10mg
capsule: Schedule III
- 10mg
Androgen Deficiency (Male)
Oral: 10-50 mg/day
Buccal: 5-25 mg/day
Hypogonadism, Climacteric & Impotence (Male)
Oral: 10-40 mg/day
Postpubertal Cryptorchidism (Male)
Oral: 30 mg/day
Inoperable Breast Carcinoma (Female)
Oral: 50-200 mg/day
Buccal: 25-100 mg/day
Postpartum Breast Pain & Engorgement (Female)
Oral: 80 mg/day x 3-5 days post-parturition
Buccal: 40 mg/day x 3-5 days
Other Information
Buccal absorption produces twice androgenic activity as oral tablets
Monitor: Virilization in females; priapism & excessive sexual arousal in males
Other Indications & Uses
Females: Inoperable metastatic breast cancer 1-5 years postmenopausal; post-partum breast pain & engorgement
Males: Delayed puberty
Off-label: Male climacteric impotence
Dosage Forms & Strengths
tablet: Schedule III
- 10mg
capsule: Schedule III
- 10mg
To Induce Pubertal Changes in Hypogonadal Males
10 mg PO qDay
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (4)
- cyclosporine
methyltestosterone increases effects of cyclosporine by decreasing metabolism. Avoid or Use Alternate Drug. Androgens may potentiate the hepatoxic effects of cyclosporine, when coadministered.
- pexidartinib
methyltestosterone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.
- pretomanid
methyltestosterone, pretomanid. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Pretomanid regimen associated with hepatotoxicity. Avoid alcohol and hepatotoxic agents, including herbal supplements and drugs other than bedaquiline and linezolid.
- warfarin
methyltestosterone increases effects of warfarin by anticoagulation. Avoid or Use Alternate Drug.
Monitor Closely (10)
- albiglutide
methyltestosterone increases effects of albiglutide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- epoetin alfa
methyltestosterone increases effects of epoetin alfa by pharmacodynamic synergism. Use Caution/Monitor. Concurrent administration of androgens can increase the patient's response to epoetin alfa, reducing the amount required to treat anemia. Because of potential adverse effects drug combination should be avoided.
- insulin aspart
methyltestosterone increases effects of insulin aspart by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- insulin glargine
methyltestosterone increases effects of insulin glargine by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- insulin glulisine
methyltestosterone increases effects of insulin glulisine by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- insulin regular human
methyltestosterone increases effects of insulin regular human by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- liraglutide
methyltestosterone increases effects of liraglutide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
- siponimod
siponimod and methyltestosterone both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- tacrolimus
methyltestosterone increases effects of tacrolimus by decreasing metabolism. Use Caution/Monitor.
- tolazamide
methyltestosterone increases effects of tolazamide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.
Minor (26)
- acarbose
methyltestosterone increases effects of acarbose by pharmacodynamic synergism. Minor/Significance Unknown.
- chlorpropamide
methyltestosterone increases effects of chlorpropamide by pharmacodynamic synergism. Minor/Significance Unknown.
- cortisone
methyltestosterone, cortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- dexamethasone
methyltestosterone, dexamethasone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- fludrocortisone
methyltestosterone, fludrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- glimepiride
methyltestosterone increases effects of glimepiride by pharmacodynamic synergism. Minor/Significance Unknown.
- glipizide
methyltestosterone increases effects of glipizide by pharmacodynamic synergism. Minor/Significance Unknown.
- glyburide
methyltestosterone increases effects of glyburide by pharmacodynamic synergism. Minor/Significance Unknown.
- hydrocortisone
methyltestosterone, hydrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- insulin detemir
methyltestosterone increases effects of insulin detemir by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin lispro
methyltestosterone increases effects of insulin lispro by pharmacodynamic synergism. Minor/Significance Unknown.
- insulin NPH
methyltestosterone increases effects of insulin NPH by pharmacodynamic synergism. Minor/Significance Unknown.
- metformin
methyltestosterone increases effects of metformin by pharmacodynamic synergism. Minor/Significance Unknown.
- methylprednisolone
methyltestosterone, methylprednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- miglitol
methyltestosterone increases effects of miglitol by pharmacodynamic synergism. Minor/Significance Unknown.
- nateglinide
methyltestosterone increases effects of nateglinide by pharmacodynamic synergism. Minor/Significance Unknown.
- pioglitazone
methyltestosterone increases effects of pioglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- prednisolone
methyltestosterone, prednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- prednisone
methyltestosterone, prednisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
- repaglinide
methyltestosterone increases effects of repaglinide by pharmacodynamic synergism. Minor/Significance Unknown.
- rosiglitazone
methyltestosterone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- saw palmetto
saw palmetto decreases effects of methyltestosterone by pharmacodynamic antagonism. Minor/Significance Unknown.
- saxagliptin
methyltestosterone increases effects of saxagliptin by pharmacodynamic synergism. Minor/Significance Unknown.
- sitagliptin
methyltestosterone increases effects of sitagliptin by pharmacodynamic synergism. Minor/Significance Unknown.
- tolbutamide
methyltestosterone increases effects of tolbutamide by pharmacodynamic synergism. Minor/Significance Unknown.
- triamcinolone acetonide injectable suspension
methyltestosterone, triamcinolone acetonide injectable suspension. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.
Adverse Effects
>10%
Edema
Acne
Breast soreness
Priapism
Menstrual irregularities
Virilization
Frequency Not Defined
Edema wiith or without congestive heart failure
Gynecomastia
Suppression of clotting factors II, V, VII & X, Erythrocytosis
Cholestatic jaundice syndrome
Neoplasm of liver
Anaphylaxis
Warnings
Contraindications
Known or suspected prostate CA, males w/ breast cancer
Pregnancy
Cautions
Cardiac dz, hepatic dz, renal dz, elderly
Hypercalcemia may occur in breast CA pts
Risk of jaundice, cholestatic hepatitis, abnl LFTs & potentially fatal hepatic peliosis - discontinue if any of these occur
Pts. easily sexually aroused
Pregnancy & Lactation
Pregnancy Category: X
Lactation: excreted into breast milk, avoid
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Half-Life: 10-100 min
Peak Plasma Time: 1-2 hr
Bioavailability: absorbed from GI tract & oral mucosa
Protein Bound: 98%
Metabolism: less extensively undergoes first-pass hepatic metabolism than testosterone, suitable for PO admin
Excretion
Urine: 90%
Feces: 6%
Mechanism of Action
Synthetic testosterone derivatives with anabolic & androgenic activity; promoting growth & development of male sex organs & maintaining secondary sex characteristics in androgen-deficient males
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Methitest oral - | 10 mg tablet |  | |
| methyltestosterone oral - | 10 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
methyltestosterone oral
METHYLTESTOSTERONE - ORAL
(METH-ill-tess-TOSS-ter-own)
COMMON BRAND NAME(S): Android, Testred
USES: This medication is used in men who do not make enough of a natural substance called testosterone. In males, testosterone is responsible for many normal functions, including growth and development of the genitals, muscles, and bones. It also helps cause normal sexual development (puberty) in boys. Methyltestosterone is similar to the natural testosterone produced by your body. It belongs to a class of drugs known as androgens. It works by affecting many body systems so that the body can develop and function normally.Methyltestosterone may also be used in certain adolescent boys to cause puberty in those with delayed puberty. It may also be used to treat certain types of breast cancer in women.
HOW TO USE: Take this medication by mouth with or without food, usually 1 to 4 times a day, as directed by your doctor.Dosage is based on your medical condition, testosterone blood levels, and response to treatment.Use this medication regularly in order to get the most benefit from it. To help you remember, take it at the same times each day.Misuse or abuse of testosterone or testosterone-like products can cause serious side effects such as heart disease (including heart attack), stroke, liver disease, mental/mood problems, abnormal drug-seeking behavior, or improper bone growth (in adolescents). Do not increase your dose or use this drug more often or for longer than prescribed. When testosterone is misused or abused, you may have withdrawal symptoms (such as depression, irritability, tiredness) when you suddenly stop using the drug. These symptoms may last from weeks to months.Tell your doctor if your condition does not improve or worsens.
SIDE EFFECTS: Nausea, vomiting, headache, skin color changes, increased/decreased sexual interest, oily skin, hair loss, and acne may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as anxiety, depression, increased anger), trouble sleeping/snoring, signs of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), hands/ankles/feet swelling, unusual tiredness, fast/irregular heartbeat.Get medical help right away if you have any very serious side effects, including: shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden/severe headaches, trouble speaking, weakness on one side of the body, sudden vision changes.If you are male, tell your doctor right away if you have any serious side effects, including: trouble urinating, breast swelling/tenderness, too frequent/prolonged erections.Rarely, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.If you are female, tell your doctor right away if you have any serious side effects, including: deepening of the voice, hoarseness, unusual facial/body hair growth, enlarged clitoris, irregular menstrual periods.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using methyltestosterone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: cancer (such as breast cancer in men, prostate cancer), blood clots (such as in the leg, lungs), heart disease (such as heart failure, chest pain, heart attack), stroke, liver problems, kidney problems, certain mineral imbalance (high calcium blood level), high cholesterol, high blood pressure, enlarged prostate, breathing problems (such as sleep apnea, chronic obstructive pulmonary disease-COPD), diabetes.If you have diabetes, this product may lower your blood sugar. Check your blood sugar regularly as directed and share the results with your doctor. Tell your doctor right away if you have symptoms of low blood sugar, such as sudden sweating, shaking, fast heartbeat, hunger, blurred vision, dizziness, or tingling hands/feet. Your doctor may need to adjust your diabetes medication, exercise program, or diet.This drug may affect your cholesterol and may increase your risk of heart or blood vessel problems (coronary artery disease). Your doctor will monitor your cholesterol level closely.Tell your doctor if you become bed-ridden (unable to walk) for a prolonged time while using this medication. Your doctor may monitor your blood calcium level to prevent problems.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially prostate/liver problems, swelling of arms/legs.Caution is advised when using this drug in children because bone growth may be affected, causing shorter adult height. Your child's doctor will monitor growth and bone development during treatment.This medication can affect fertility in males. Ask your doctor for more details.This medication must not be used during pregnancy. It may harm an unborn baby. Discuss the use of reliable forms of birth control (such as condoms, birth control pills) with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this drug passes into breast milk. It may affect milk production and it may harm a nursing infant. Breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: "blood thinners" (such as warfarin).This medication may interfere with certain laboratory tests (including thyroid function tests), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others. Sharing it is against the law.Lab and/or medical tests (such as blood testosterone levels, red blood cell counts, liver function, blood cholesterol levels, PSA test) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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