Https://www.accessda Ta.fda.gov/drugsatfd A_docs/label/2007/01 7362s104lbl.pdf

Summary

Indication: Treats amenorrhea (absence of menstrual periods) and abnormal uterine bleeding due to hormonal imbalance, excluding organic causes like fibroids or cancer.

Formulation & Administration: Sterile solution of progesterone (50 mg/mL) in sesame oil for intramuscular injection.

Key Properties:

Chemical: Pregn-4-ene-3,20-dione (C21H30O2)
Structure: White or creamy white powder, odorless.
Solubility: Practically insoluble in water; soluble in alcohol, acetone, and dioxane; sparingly soluble in vegetable oils.

Pharmacodynamics:

Converts proliferative endometrium to secretory endometrium.
Inhibits gonadotropin secretion, preventing follicular maturation and ovulation.

Pharmacokinetics:

Absorption: Maximum plasma concentrations reached within 8 hours; cleared primarily by the liver (metabolized to pregnanediol, pregnanetriol, and pregnanolone).
Distribution: Extensively bound to plasma proteins (50-54% albumin, 43-48% cortisol-binding protein).

Contraindications:

History of thrombophlebitis, thromboembolic disorders, cerebral apoplexy, liver dysfunction or disease, known or suspected genital organ cancer, undiagnosed vaginal bleeding, missed abortion, known sensitivity to progesterone injection.

Warnings & Precautions:

Thrombotic risk: Monitor for signs of thrombosis (thrombophlebitis, cerebrovascular accidents, pulmonary embolism, retinal thrombosis). Discontinue immediately if suspected.
Visual changes: Discontinue medication if sudden partial or complete loss of vision, proptosis, diplopia, or migraine occurs.
Other precautions:

Careful monitoring in patients with epilepsy, migraine, asthma, cardiac, or renal dysfunction due to potential fluid retention.
Evaluate for non-progestational causes of irregular bleeding.
Monitor patients with a history of psychic depression.
Inform pathologists about progestin therapy when relevant specimens are submitted.

Adverse Reactions:

Breakthrough bleeding, spotting, amenorrhea, edema, changes in weight, cervical erosion/secretions, cholestatic jaundice, breast tenderness, galactorrhea, injection site reactions (irritation, redness), skin sensitivity reactions, acne, alopecia, hirsutism, rash (allergic), anaphylactoid reactions, mental depression, pyrexia, insomnia, nausea, somnolence.
Increased risk of pulmonary embolism and cerebral thrombosis/embolism with estrogen-progestin combination therapy.
Possible association with neuro-ocular lesions (retinal thrombosis, optic neuritis).