The P-I-E-N-O Parkinsn's List Drug Database
medroxyprogesterone / ProveraTM , Depo-ProveraTM
AMENORRHEA:
Endometriosis
Description: Medroxyprogesterone is a synthetic progestational agent with 15 times the potency of progesterone. Medroxyprogesterone can be administered orally or parenterally. Medroxyprogesterone can be used for the treatment of amenorrhea, abnormal uterine bleeding, endometriosis believed to be secondary to hormonal imbalances, and endometrial and renal cell carcinomas. The IM injection is a sustained-release (i.e., "depo") product available in 2 forms: one for use as a contraceptive similar to the subcutaneous implant NorplantTM , and the other for the treatment of endometrial and renal cell carcinoma. Progestational agents including medroxyprogesterone may be useful as a respiratory stimulant in certain pulmonary disorders such as chronic obstructive pulmonary disease (COPD), Pickwickian syndrome, polycythemia, and other hypercapnic pulmonary conditions. Medroxyprogesterone was originally approved by the FDA in 1959.
Mechanism of Action: Medroxyprogesterone inhibits secretion of pituitary gonadotropins, which prevents follicular maturation and ovulation. The drug converts a proliferative endometrium into a secretory state. The mode of action against certain cancers has not been determined. Progestins also can demonstrate estrogenic, anabolic, and androgenic activity.
Progestins are also mild, direct stimulants of the respiratory center. During pregnancy and the luteal phase of the menstrual cycle, women can hyperventilate and become hypocapnic due to elevated concentrations of endogenous progestins. Therapeutically, medroxyprogesterone has been used successfully in patients with COPD and hypercapnia, in patients with Pickwickian syndrome, and in patients with sleep apnea.
Pharmacokinetics: Medroxyprogesterone is administered both orally and parenterally. Oral bioavailability is not known. Following a single IM dose, concentrations increase progressively for 3 weeks, then begin to decrease exponentially to undetectable levels at 120-200 days following the injection. The half-life following IM administration of the depot form is 50 days. Metabolism is hepatic, and elimination is primarily fecal.
CONTRAINDICATIONS/PRECAUTIONS: Medroxyprogesterone is absolutely contraindicated in patients with hepatic disease, hepatic dysfunction, incomplete abortion, suspected pregnancy, or abnormal and undiagnosed vaginal bleeding.
The relative risk of developing breast cancer in patients receiving depot medroxyprogesterone for contraception has been investigated in a number of trials. Pooled data from two trials indicates the relative risk of breast cancer appears to be increased (2.2) if depot medroxyprogesterone is used within the previous 5 years, but there is no increased risk overall. The duration of use was not a factor, that is, the incidence with a single dose was the same as with multiple doses. Depot medroxyprogesterone may accelerate the growth of occult cancers, but is not necessarily a risk factor for breast cancer.D Medroxyprogesterone is contraindicated in patients with pre-existing breast carcinoma or carcinoma of reproductive organs, except for palliative therapy in selected patients.
Medroxyprogesterone is relatively contraindicated in patients with asthma, cardiac disease, seizure disorder, migraine, or renal disease because it can cause fluid retention, which could aggravate these conditions.
Medroxyprogesterone is relatively contraindicated in patients with hyperlipidemia because some progestins increase LDL concentration, particularly with long-term use.
Medroxyprogesterone is relatively contraindicated in patients who have progestin intolerance, major depression, thrombophlebitis, thromboembolic disease, or a history of cerebrovascular accident including cerebral hemorrhage.
Medroxyprogesterone should not be used if there is a history of ectopic pregnancy, during the first four months of pregnancy, or in diagnostic tests for pregnancy. It is secreted in milk, so alternative methods to breast-feeding should be employed.
DRUG INTERACTIONS: Medroxyprogesterone can cause amenorrhea and/or galactorrhea, which would counteract the desired effect of bromocriptine. These drugs should not be used together.
ADVERSE REACTIONS: Frequent adverse effects that can occur during therapy with medroxyprogesterone and may require medical attention include: changes in vaginal bleeding pattern including spotting or breakthrough bleeding, or menstrual irregularities including dysmenorrhea or amenorrhea.
Adverse effects that are rare but may require medical attention include: thromboembolism including deep venous thrombosis (DVT) or pulmonary embolism, galactorrhea, hepatitis, gallbladder obstruction, hypersensitivity, major depression, and neuro-ocular lesions.
Adverse reactions that occur commonly during therapy with medroxyprogesterone but that require medical attention only if prolonged or bothersome include: anorexia or appetite stimulation, weight loss or weight gain, edema, and unusual fatigue or weakness.
Other adverse reactions that can occur during therapy with medroxyprogesterone are hirsutism, breast tenderness, impotence, anxiety, and diarrhea.
PATIENT INFORMATION:
What do medroxyprogesterone tablets do?
Medroxyprogesterone (ProveraTM ) helps to treat an irregular menstrual cycle, lack of menstrual periods, or abnormal uterine bleeding caused by a hormonal imbalance. Medroxyprogesterone is a man-made steroid that acts like the natural hormone progesterone. Natural progesterone is essential to normal reproductive functioning of the womb and reproductive system. Generic medroxyprogesterone tablets are not yet available.
What should my doctor, dentist, or pharmacist know before I take medroxyprogesterone?
They need to know if you have any of these conditions:
How should I take this medicine?
Take medroxyprogesterone tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Bleeding generally begins in 3 to 7 days after completing the drug treatment.
Special precautions for use in children:
This medicine is not for children.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with medroxyprogesterone?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking medroxyprogesterone?
Serious side effects with medroxyprogesterone include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with medroxyprogesterone include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take medroxyprogesterone?
Visit your doctor for regular checks on your progress. You should have a complete check-up every 6 to 12 months. Stop taking medroxyprogesterone at once and contact your doctor if you think you are pregnant.
The effect of medroxyprogesterone on fertility can last for a long time. If you want to get pregnant when you have stopped taking this medicine it may be some time before you can conceive.
Progestins can cause swelling, tenderness, or bleeding of the gums; be careful when brushing and flossing teeth. See your dentist regularly for routine dental care
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30C (59 and 86F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
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