Consumer medicine information

1. Why am I using RALOVERA?

RALOVERA contains the active ingredient medroxyprogesterone acetate. RALOVERA is used to treat endometriosis, the absence of menstrual periods (not due to pregnancy), abnormal bleeding from the uterus, certain types of cancer including cancer of the breast, kidney and endometrium, and in combination with an estrogen containing medicine to relieve symptoms of menopause in women with an intact uterus.
For more information, see Section 1. Why am I using RALOVERA? in the full CMI.

2. What should I know before I use RALOVERA?

Do not use if you have ever had an allergic reaction to medroxyprogesterone acetate or any of the ingredients listed at the end of the CMI.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.
For more information, see Section 2. What should I know before I use RALOVERA? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with RALOVERA and affect how it works.
A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use RALOVERA?

• Swallow the tablets whole with a full glass of water at about the same time each day that you need to take it.

5. What should I know while using RALOVERA?

6. Are there any side effects?

Side effects include: dizziness, increased heart rate, changes to mood or mental state, sleepiness or difficulty sleeping, skin conditions, changes to menstrual period or vaginal secretions, changes to breasts, changes in sex drive, weight and/or appetite changes, fluid retention, yellowing of the skin or eyes, swollen or tender veins, painful swelling in the arms or legs, severe headaches or changes to speech or vision, allergic reactions, chest pain or shortness of breath, hand tremors or cramps.
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

1 Name of Medicine

Medroxyprogesterone acetate (MPA).

2 Qualitative and Quantitative Composition

Ralovera tablets contain 2.5 mg, 5 mg or 10 mg medroxyprogesterone acetate as the active ingredient.
Excipient(s) with known effect. Lactose monohydrate.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

2.5 mg tablets: orange, circular, scored on one side, marked U64 on the other side.
5 mg tablets: pale blue, circular, scored on one side and marked 286 on both sides of the score line, marked U on the other side.
10 mg tablets: white, circular, scored on one side, marked UPJOHN 50 on the other side.

4 Clinical Particulars

4.9 Overdose

Oral doses up to 3 g per day have been well tolerated. Patients receiving pharmacological doses of MPA for treatment of neoplasms (400 mg/day or greater) may occasionally exhibit effects resembling those of glucocorticoid excess.
As with the management of any overdosage, the physician should carefully observe the patient for the potential side effects. Overdose treatment is symptomatic and supportive.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. No data available.
Carcinogenicity. Long-term toxicology studies in the monkey, dog and rat with parenteral MPA have disclosed:
Beagle dogs receiving 75 mg/kg and 3 mg/kg every 90 days for 7 years developed mammary nodules, as did some of the control animals. The nodules appearing in the control animals were intermittent in nature, whereas the nodules in the drug treated animals were larger, more numerous, persistent, and there were 2 high dose animals that developed breast malignancies.
Two monkeys receiving 150 mg/kg every 90 days for 10 years developed undifferentiated carcinoma of the uterus. No uterine malignancies were found in monkeys receiving 30 mg/kg, 3 mg/kg, or placebo every 90 days for 10 years. Transient mammary nodules were found during the study in the control, 3 mg/kg and 30 mg/kg groups, but not in the 150 mg/kg group. At sacrifice (after 10 years), the only nodules extant were in 3 of the monkeys in the 30 mg/kg group. Upon histopathological examination these nodules were determined to be hyperplastic.
No uterine or breast abnormalities were revealed in the rat after 2 years.
The relevance of any of these findings with respect to humans has not been established.
Animal toxicology. Acute toxicity. The oral LD₅₀ of MPA was found to be > 10,000 mg/kg in the mouse. The intraperitoneal LD₅₀ in the mouse was 6985 mg/kg.
Subacute and chronic toxicity. MPA administered orally to rats and mice (334 mg/kg/day) and dogs (167 mg/kg/day) for 30 days was found to be nontoxic.
MPA was administered orally to dogs and rats at 3 mg/kg/day, 10 mg/kg/day and 30 mg/kg/day for 6 months. The drug was considered to be nontoxic at these levels but with anticipated hormonal effects at the higher dose.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

MPA is a progestogen and a derivative of progesterone. It is a white to off white, odourless crystalline powder, stable in air, melting between 200°C and 210°C. It is freely soluble in chloroform, soluble in acetone and dioxane, sparingly soluble in ethanol and methanol, slightly soluble in ether and insoluble in water.
Chemical structure. MPA is 6α-methyl- 3,20-dioxopregn- 4-en-17α-yl acetate, and its structural formula is as follows:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSMEDPRO.gif CAS number. 71-58-9.

7 Medicine Schedule (Poisons Standard)

S4, Prescription Only Medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/RALOVEST.gif