megestrol

BEERS REMS, High Alert

Palliative treatment of endometrial and breast carcinoma, either alone or with surgery or radiation (tablets only).
Anorexia, weight loss, and cachexia associated with AIDS (oral suspension only).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Undiagnosed vaginal bleeding;
Severe hepatic impairment;
Suspension contains alcohol and should be avoided in patients with known intolerance;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Diabetes;
Mental depression;
Renal impairment;
History of thromboembolism;
Cardiovascular disease;
Seizures;
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. ↑ risk of thrombotic events and possibly death in older adults. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: DEEP VEIN THROMBOSIS (DVT), edema

Derm: alopecia

Endo: asymptomatic adrenal suppression (chronic therapy)

GI: GI irritation

GU: vaginal bleeding

MS: carpal tunnel syndrome

Resp: PULMONARY EMBOLISM (PE)

Interactions ⬆ ⬇

Drug-drug:

May ↑ INR and risk of bleeding when used with warfarin.

Availability ⬆ ⬇

(Generic available)

Oral suspensionlemon-lime flavor: 40 mg/mL; 125 mg/mL
Tablets: 20 mg; 40 mg; 160 mg

Route/Dosage ⬆ ⬇

Breast Carcinoma

PO (Adults ): 160 mg/day as a single dose or divided doses.

Endometrial Carcinoma

PO (Adults ): 40–320 mg/day in divided dose.

Anorexia Associated With AIDS

PO (Adults ): 40 mg/mL suspension: 800 mg once daily; may ↓ to 400 mg/day after 1 mo (range 400–800 mg/day); 125 mg/mL suspension: 625 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Antineoplastic effect may result from inhibition of pituitary function.

Therapeutic effects:

Regression of tumor.
Increased appetite and weight gain in patients with AIDS.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics, hormones

Pharmacologic Classification: progestins

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed from the GI tract.

Distribution: Unknown.

Protein Binding: ≥90%.

Metabolism/Excretion: Completely metabolized by the liver.

Half-Life: 38 hr (range 13–104 hr).

Time/Action Profile ⬆ ⬇

(antineoplastic activity)

ROUTE	ONSET	PEAK	DURATION
PO	week–months	2 mo	unknown

Patient/Family Teaching ⬆ ⬇

Explain the purpose and side effects of megestrol. Instruct patient to take as directed; do not skip or double up on missed doses. Missed doses may be taken as long as not right before next dose. Gradually decrease dose prior to discontinuation. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
Advise patient to report to health care provider any unusual vaginal bleeding or signs of DVT or PE.
Discuss with patient the possibility of hair loss. Explore methods of coping.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception during and for ≥4 mo after therapy is completed. Advise patient to notify health care provider immediately if pregnancy is planned or suspected and to avoid breastfeeding during therapy.

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Indications ⬇