Methitest (methyltestosterone)

Dosage of methyltestosterone is variable and should be individualized according to the condition being treated, the severity of symptoms, and the patient's age, gender, and history of prior androgenic therapy.

Diagnosis of male hypogonadism must be confirmed by laboratory testing prior to initiation of methyltestosterone therapy. To confirm this diagnosis, serum testosterone concentrations should be measured in the morning on at least 2 separate days and must be consistently below the normal range. Serum testosterone concentrations may be low later in the day in men with or without hypogonadism; therefore, measuring testosterone concentrations later in the day should be avoided.

Methyltestosterone is administered orally; the drug usually is given in divided daily doses. Methyltestosterone also has been administered intrabuccally.

No dosing information is available for this tab.

Methyltestosterone may potentiate the action of oral anticoagulants, causing bleeding in some patients. When methyltestosterone therapy is initiated in patients receiving oral anticoagulants, dosage reduction of the anticoagulant may be required to prevent an excessive hypoprothrombinemic response. Patients receiving oral anticoagulants also should be closely monitored when androgen therapy is discontinued.

The metabolic effects of androgens may decrease blood glucose concentrations and insulin requirements in patients with diabetes.

There are no contraindication interactions for this drug.

Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

Selected Androgens/Cyclosporine

SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

MECHANISM OF ACTION: Danazol and methyltestosterone may inhibit the metabolism of cyclosporine.

CLINICAL EFFECTS: Concurrent therapy may result in increased levels of cyclosporine, which may produce hepatic and renal dysfunction.

PREDISPOSING FACTORS: None determined.

PATIENT MANAGEMENT: If possible, avoid giving patients receiving cyclosporine danazol or methyltestosterone. If concurrent therapy is warranted, monitor cyclosporine levels as well as renal and hepatic function carefully. Cyclosporine dosage adjustments may be necessary when these agents are initiated or discontinued, as well as during concurrent therapy. Discontinuation of the androgen may be necessary.

DISCUSSION: Four case reports have documented increased cyclosporine levels during concurrent therapy with danazol.(1-4) In two of these reports, elevated cyclosporine levels persisted even after decreases in cyclosporine dosages.(1,2) One patient also experienced decreased renal function, as indicated by an increase in serum creatinine levels.(1) Cyclosporine levels returned to baseline following the discontinuation of danazol.(1-4) Two case reports have documented increased cyclosporine levels during concurrent therapy with methyltestosterone. Both patients experienced elevated cyclosporine, bilirubin, and serum creatinine levels during concurrent therapy.(5,6) In one patient, elevated cyclosporine levels persisted despite a 40% decrease in cyclosporine dosage.(5) Discontinuation of methyltestosterone resulted in a gradual return of cyclosporine levels to previous values.(5,6)

Slt Anabolic Steroids/Slt Anticoagulants (Vit K Antagonists)

SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

MECHANISM OF ACTION: The exact mechanism is unknown. It has been hypothesized that the C-17 alkylated androgens may increase turnover of clotting factors and decrease their synthesis. Increased affinity for the anticoagulant receptor site has also been hypothesized. The C-17 alkylated androgens have not been shown to alter the metabolism of anticoagulants.

CLINICAL EFFECTS: The concurrent use of anticoagulants and anabolic steroids may result in an increased risk for bleeding.

PREDISPOSING FACTORS: The risk for bleeding episodes may be greater in patients with disease-associated factors (e.g. thrombocytopenia). Drug associated risk factors include concurrent use of multiple drugs which inhibit anticoagulant/antiplatelet metabolism and/or have an inherent risk for bleeding (e.g. NSAIDs).

PATIENT MANAGEMENT: Patients should be closely monitored for increased anticoagulant activity. The dose of the anticoagulant may need to be adjusted. The time of highest risk for a coumarin-type drug interaction is when the precipitant drug is initiated or discontinued. Contact the prescriber before initiating, altering the dose or discontinuing either drug. When concurrent therapy is warranted, also monitor patients receiving concurrent therapy for signs of blood loss, including decreased hemoglobin, hematocrit, fecal occult blood, and/or decreased blood pressure and promptly evaluate patients with any symptoms. Discontinue anticoagulation in patients with active pathologic bleeding. Instruct patients to report any signs and symptoms of bleeding, such as unusual bleeding from the gums or nose; unusual bruising; red or black, tarry stools; red, pink or dark brown urine; acute abdominal or joint pain and/or swelling.

DISCUSSION: Danazol, methandrostenolone, methyltestosterone, oxymetholone, and stanozolol have been shown to increase the hypoprothrombinemic actions of warfarin. Methyltestosterone has also been shown to increase the effects of dicumarol. Oxymetholone and ethylestrenol have been shown to increase the effects of phenindione. Limited data suggest that the non-C-17-alkylated androgens do not affect anticoagulants.

There are no moderate interactions for this drug.

There is no enhanced messaging for this drug.

• Lactation
• Malignant tumor of male breast
• Pregnancy
• Prostatic carcinoma

• Acute myocardial infarction
• Benign prostatic hyperplasia
• Cerebrovascular accident
• Chronic heart failure
• Coronary artery disease
• Disease of liver
• Hypercalcemia

• Diabetes mellitus
• Edema
• Hypertension
• Kidney disease with reduction in glomerular filtration rate (GFr)
• Neoplasm of liver

There is no enhanced messaging for this drug.

More Frequent

• Amenorrhea
• Bladder irritability
• Gynecomastia
• Irregular menstrual periods
• Mastalgia
• Priapism
• Urinary tract infection
• Virilism

Less Frequent

• Benign prostatic hyperplasia
• Dizziness
• Edema
• Epididymitis
• Fatigue
• Flushing
• Headache disorder
• Hypercalcemia
• Hypertension
• Nausea
• Prostatic carcinoma
• Vomiting

Rare or Very Rare

• Abnormal hepatic function tests
• Acute myocardial infarction
• Cerebrovascular accident
• Cholestatic hepatitis
• Deep venous thrombosis
• Drug-induced hepatitis
• Erythrocytosis
• Heart failure
• Hepatic necrosis
• Jaundice
• Leukopenia
• Malignant neoplasm of liver
• Peliosis hepatis
• Pulmonary thromboembolism
• Venous thrombosis

Less Frequent

• Acne vulgaris
• Diarrhea
• Erectile dysfunction
• Increased pubic hair
• Insomnia
• Libido changes
• Testicular atrophy

Rare or Very Rare

• Aggressive behavior
• Anorexia
• Depression
• Hostility
• Irritability
• Oligospermia

No enhanced messaging available.

No enhanced messaging available.

Methyltestosterone may cause fetal harm when administered to pregnant women. Androgenic effects including clitoral hypertrophy, labial fusion of the external genital fold to form a scrotal-like structure, abnormal vaginal development, and persistence of a urogenital sinus have occurred in the female offspring of women who were given androgens during pregnancy. The degree of masculinization is related to the amount of drug given to the woman and the age of the fetus; masculinization is most likely to occur in a female fetus when exposure to androgens occurs during the first trimester. Since the risks clearly outweigh the possible benefits in women who are or may become pregnant, methyltestosterone is contraindicated in such women. Women who become pregnant while receiving the drug should be informed of the potential hazard to the fetus.

It is not known whether methyltestosterone is distributed into milk. Because of the potential for serious adverse reactions to androgens in nursing infants, a decision should be made whether to discontinue nursing or to not use methyltestosterone, taking into account the importance of the drug to the woman.

No enhanced messaging available.