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Megestrol Contraindications; Pregnancy Category

Megestrol Contraindications is a synthetic derivative of progesterone with an antiestrogenic activity. Megestrol binds to and activates nuclear receptors which subsequently bind to and activate target genes for transcription. As an antiestrogen, this agent may inhibit the growth-stimulating effects of estrogen on estrogen-sensitive tumor cells. In addition, megestrol stimulates appetite in cachectic subjects.

Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia. (From Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)

Mechanism of Action of Megestrol

Megestrol acetate shares the actions of the progestins: induction of secretory changes in the endometrium, increase in basal body temperature, pituitary inhibition, and production of withdrawal bleeding in the presence of estrogen. In animals, the drug suppresses ovulation and produces antigonadotrophic, antiuterotrophic and antiandrogenic/amyotrophic effects. It has slight glucocorticoid activity and a very slight degree of mineralocorticoid activity. Megestrol acetate has no estrogenic, androgenic, or anabolic activity.

The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time, but its progestin antitumor activity may involve suppression of luteinizing hormone by inhibition of pituitary function. Studies also suggest that the megestrol’s weight gain effect is related to its appetite-stimulant or metabolic effects rather than its glucocorticoid-like effects or the production of edema. It has also been suggested that megestrol may alter metabolic pathways via interferences with the production or action of mediators such as cachectin, a hormone that inhibits adipocyte lipogenic enzymes.

Megestrol Indications

For the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
Breast Cancer-Palliative
Endometrial Carcinoma
Abnormal Uterine Bleeding
Anorexia
AIDS-Related Wasting
Breast Cancer, Palliative
Cachexia
Endometrial Cancer
Endometrial Hyperplasia
Hot Flashes
Weight Loss

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Therapeutic Uses

Antineoplastic Agents, Hormonal; Progestational Hormones, Synthetic
Megestrol Acetate Tablets USP is indicated for the palliative treatment of advanced carcinoma of the breast or endometrium (ie, recurrent, inoperable, or metastatic disease). It should not be used in lieu of currently accepted procedures such as surgery, radiation, or chemotherapy.
Megestrol Acetate Oral Suspension USP is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS).
Anorexia is a common disorder in patients treated with regular hemodialysis and is a contributing factor to malnutrition. The aim of this study was to evaluate the effectiveness of megestrol acetate, an appetite stimulant used in cancer patients, as a treatment for anorexia in dialysis patients.

Megestrol Contraindications

Severe infection
Diabetes
Anemia
Decreased Function of the Adrenal Gland
High blood pressure
Chronic heart failure
Obstruction of a Blood Vessel by a Blood Clot
High Blood Sugar
Decreased Blood Platelets
Severely Decreased Platelets
Decreased Neutrophils a Type of White Blood Cell
Peripheral neuropathy
Disease of Inadequate Blood Flow to the Heart Muscle
Abnormal heart rhythm
Heart Disease
Liver problems
Severe liver disease
High Amount of Bilirubin in the Blood
Abnormal liver function tests
Pregnancy
A mother who is producing milk and breastfeeding
Severely Decreased Levels of Neutrophils in the Blood

Megestrol Dosage

Strengths: 40 mg/mL; 20 mg; 40 mg; 625 mg/5 mL

Breast Cancer-Palliative

Megestrol tablets are indicated for use in the palliative treatment of advanced carcinoma of the breast: 160 mg/day (40 mg of oral tablets four times a day)

Endometrial Carcinoma

Megestrol tablets are indicated for use in the palliative treatment of advanced carcinoma of the endometrium: 40 to 320 mg/day of oral tablets in divided doses

Anorexia

Megestrol oral suspension is indicated for use in the treatment of anorexia at a dose of 800 mg/day.
Alternatively, 625 mg/5 mL of the concentrated formula (Megace ES formula) may be given.
Note: 800 mg/20 mL of the regular formula is equivalent to 625 mg/ 5 mL of the concentrated formula.

Cachexia

Megestrol oral suspension is indicated for use in the treatment of cachexia at a dose of 800 mg/day.
Alternatively, 625 mg/5 mL of the concentrated formula (Megace ES formula) may be given.
Note: 800 mg/20 mL of the regular formula is equivalent to 625 mg/ 5 mL of the concentrated formula.

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Weight Loss

Megestrol oral suspension is indicated for use in the treatment of unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS) at a dose of 800 mg/day.
Alternatively, 625 mg/5 mL of the concentrated formula (Megace ES formula) may be given.
Note: 800 mg/20 mL of the regular formula is equivalent to 625 mg/ 5 mL of the concentrated formula.

Abnormal Uterine Bleeding

5 to 10 mg/day for 5 to 10 days

Side Effects of Megestrol

The Most Common

Abdominal or stomach pain or tenderness
diarrhea
symptoms of heart problems (e.g., shortness of breath, swelling of the ankles or feet, chest pain, irregular heartbeat)
symptoms of liver problems (e.g., nausea, vomiting, abdominal pain, yellowing of the skin and eyes, itchy skin, dark urine)
symptoms of lung problems (e.g., shortness of breath or difficulty breathing, chest pain, cough)
symptoms of a severe allergic reaction (e.g., hives; difficulty breathing; swelling of the face, mouth, tongue, or throat)
signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort

More Common

Acid or sour stomach
back pain
belching
cracked lips
diarrhea (mild)
dry skin
heartburn
indigestion
pain in the arms or legs
redness, swelling, or painful skin
scaling of the skin on the hands and feet
sores, ulcers, or white spots on the lips, tongue, or the inside of the mouth

Rare

Black, tarry stools
body aches or pain
burning, numbness, tingling, or painful sensations
burning pain on urination
chest pain
chills
cough
difficult or labored breathing
ear congestion
fever
headache
loss of voice
lower back or side pain
nasal congestion
painful or difficult urination
pale skin
red, swelling, or painful skin

Drug Indications of Megestrol

Megestrol Acetate may interact with following drugs, supplements & may change the efficacy of drugs

calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
carbamazepine
cyclosporine
diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin, nateglinide, rosiglitazone)
corticosteroids (e.g., prednisone, dexamethasone)
cyclosporine
dexamethasone
domperidone
everolimus
“gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
“glitazone” diabetes medications
hydrocortisone
loperamide
macrolide antibiotics (e.g., clarithromycin, erythromycin)
methotrexate
metronidazole
mirabegron
phenobarbital
phenytoin
prazosin
progesterone
propranolol
protein kinase inhibitors (e.g., pazopanib, sunitinib)
quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
“statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
tacrolimus
testosterone and androgens(for men taking megestrol to treat prostate cancer)
estrogen (for women taking megestrol for breast or endometrial cancer)
ulipristal
warfarin

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Pregnancy Category

US FDA Pregnancy Category: X

Pregnancy

Megestrol acetate is not recommended for use during the first 4 months of pregnancy. Women should use effective birth control when taking megestrol. If you become pregnant while taking megestrol, tell your doctor right away.

Lactation

This medication may pass into breast milk. If you are a breast-feeding mother and are taking megestrol acetate, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.