Depostat (Solution) Instructions for Use

Marketing Authorization Holder

Schering, AG (Germany)

ATC Code

L02AB03 (Gestonorone)

Active Substance

Gestonorone caproate (Rec.INN registered by WHO)

Dosage Form

Depostat

Solution for intramuscular injection oil-based 200 mg/2 ml: amp. 5 pcs.

Dosage Form, Packaging, and Composition

2 ml – ampoules of dark glass (5) in a set with an ampoule knife or scarifier – contour plastic packaging (1) – cardboard packs.

Clinical-Pharmacological Group

Gestagen – depot form. Antineoplastic drug

Pharmacotherapeutic Group

Antineoplastic agent – progestogen

Dosage Regimen

Depostat is administered exclusively as a deep intramuscular injection into the gluteal muscle. The contents of one ampoule (2 ml containing 200 mg of gestonorone caproate) constitute a single dose.

The standard dosage regimen for the treatment of hormone-dependent malignancies is 200 mg to 400 mg, administered once every one to two weeks. The exact dosage and frequency must be strictly individualized by the attending physician based on the type and severity of the disease, the patient’s response to therapy, and overall tolerability.

It is imperative that the injection is performed by a qualified healthcare professional using proper aseptic technique. The oil-based solution should be inspected visually for particulate matter or discoloration prior to administration. The injection should be administered slowly.

Adverse Reactions

The use of Depostat, like all potent hormonal therapies, is associated with a range of potential adverse reactions. The frequency and severity of these reactions are often dose-dependent and may vary significantly from patient to patient.

Common adverse reactions are primarily related to its progestogenic activity and may include: weight changes (increase or decrease), edema (fluid retention), nausea, headache, dizziness, drowsiness, nervousness, changes in libido, breast tenderness or discomfort, and breakthrough bleeding or spotting in women.

Less frequently, more significant reactions may occur, such as: thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism), hypertension, jaundice, pruritus, skin rashes, alopecia, hirsutism, depression, and insomnia. Local reactions at the injection site, including pain, induration, or sterile abscess formation, are also possible due to the depot nature of the formulation.

Patients should be monitored regularly for the development of these and other adverse effects. Any unusual or severe symptoms should be reported to a physician immediately.

Indications

• Palliative treatment of advanced, hormone-dependent carcinoma of the prostate in men.
• Palliative treatment of advanced, hormone-dependent endometrial carcinoma (cancer of the uterine body) in women.
• Palliative treatment of advanced, hormone-dependent breast cancer in postmenopausal women or in premenopausal women in whom ovarian function has been therapeutically ablated.

The use of Depostat is indicated in cases where the tumor has been shown to be hormone-receptor positive or is suspected to be hormonally responsive. Treatment decisions should be made by an oncologist following a comprehensive assessment of the patient’s condition.

Drug Interactions

Concomitant use of Depostat with other medications requires careful monitoring due to potential interactions. Gestonorone caproate is metabolized in the liver, and its efficacy and toxicity profile can be altered by drugs that affect hepatic microsomal enzymes.

Enzyme-inducing agents, such as rifampicin, phenobarbital, phenytoin, and carbamazepine, may increase the metabolic clearance of gestonorone caproate, potentially leading to a reduced therapeutic effect. Dose adjustment of Depostat may be necessary.

Conversely, inhibitors of hepatic metabolism might increase the plasma concentrations of gestonorone caproate, potentially enhancing both its therapeutic and adverse effects.

Gestagens may also interfere with the metabolism of other drugs, potentially altering their plasma levels. Caution is advised when co-administering with drugs that have a narrow therapeutic index. Patients should inform their doctor about all medications they are taking, including prescription, over-the-counter, and herbal products.

Contraindications

• Known hypersensitivity to gestonorone caproate, any other components of the formulation, or other progestogens.
• Patients with a history of or active thromboembolic disorders (e.g., deep vein thrombosis, pulmonary embolism, cerebrovascular accident).
• Patients with severe hepatic dysfunction or liver disease where liver function tests are significantly impaired.
• Patients with undiagnosed abnormal vaginal bleeding.
• Known or suspected progestogen-dependent neoplasms, other than those for which the drug is being therapeutically used.
• This medication is not indicated for use during pregnancy. If pregnancy is suspected or confirmed, treatment must be discontinued.

Overdose

Acute overdose with Depostat following intramuscular administration is unlikely due to the route of administration and the depot release profile. However, in the event of suspected excessive dosing, the manifestations would be an exaggeration of the known pharmacological and adverse effects.

Expected symptoms could include severe nausea, vomiting, dizziness, marked drowsiness, and significant fluid retention. There is no specific antidote for gestonorone caproate overdose.

Management should be symptomatic and supportive. Medical supervision is essential. Given the prolonged action of the depot formulation, effects may persist for several weeks. Monitoring of vital signs and appropriate symptomatic treatment is the mainstay of management.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.