hydroxyprogesterone caproate (hye-drox-ee-pro-jess-te-rone kap-roe-ate) Makena

 Indications

Topthe risk of preterm birth in women with a singleton

pregnancy who have a history of previous singleton

preterm birth.

Action

A synthetic analog of progesterone. Produces secretory

changes in the endometrium.qs basal temperature.

Produces changes in the vaginal epithelium. Relaxes

uterine smooth muscle. Stimulates mammary alveolar

growth. Inhibits pituitary function. Action in reducing

risk of recurrent preterm birth is unknown. Therapeutic

Effects:prisk of preterm birth in women at

risk.

Pharmacokinetics

Absorption: Slowly absorbed following IM administration.

Distribution: Unknown.

Protein Binding: Extensively bound to plasma proteins.

Metabolism and Excretion: Extensively metabolized

by the liver.

Half-life: 7.8 days.

TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK DURATION

IM unknown 4.6 days 7 days

Contraindications/Precautions

Contraindicated in: Hypersensitivity to hydroxyprogesterone

or castor oil; History of or known thrombosis/

thromboembolic disorder; History of or known/

suspected breast cancer or other hormone-sensitive

cancer; Unexplained abnormal vaginal bleeding unrelated

to pregnancy; Cholestatic jaundice of pregnancy;

Benign/malignant liver tumors or active liver disease;

Uncontrolled hypertension.

Use Cautiously in: Risk factors for thromboembolic

disorders (mayqrisk); Diabetes mellitus or risk

factors for diabetes mellitus (may impair glucose tolerance);

History of preeclampsia, epilepsy, cardiac or renal

impairment (may be adversely affected by fluid retention);

History of depression (may worsen); Safe and

effective use in children 16 yr has not been established.

Adverse Reactions/Side Effects

CNS: depression. CV: hypertension. GI: diarrhea,

jaundice, nausea. Derm: urticaria, pruritus. F and

E: fluid retention. Hemat: THROMBOEMBOLISM. Local:

injections site reactions. Misc: allergic reactions

including ANGIOEDEMA.

Interactions

Drug-Drug: Mayqmetabolism andpblood levels

and effectiveness of drugs metabolized by the

CYP1A2, CYP2A6, and CYP2B6 enzyme systems. 

Route/Dosage

IM (Adults): 250 mg once weekly starting between 16

wks, 0 days and 20 wks, 6 days continuing until wk 37

of gestation or delivery, whichever occurs first.

Availability

Solution for IM injection (contains castor oil):

1250 mg/5 mL vial (250 mg/mL).