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Prometrium (Progesterone) - Drug Interactions, Contraindications, Overdosage, etc

 
 



DRUG INTERACTIONS

G. Drug Interactions

The metabolism of progesterone by human liver microsomes was inhibited by ketoconazole (IC50 < 0.1 μM). Ketoconazole is a known inhibitor of cytochrome P450 3A4, hence these data suggest that ketoconazole or other known inhibitors of this enzyme may increase the bioavailability of progesterone. The clinical relevance of the in vitro findings is unknown.

Co administration of conjugated estrogens and PROMETRIUM Capsules to 29 postmenopausal women over a 12-day period resulted in an increase in total estrone concentrations (Cmax 3.68 ng/mL to 4.93 ng/mL) and total equilin concentrations (Cmax 2.27 ng/mL to 3.22 ng/mL) and a decrease in circulating 17β estradiol concentrations (Cmax 0.037 ng/mL to 0.030 ng/mL). The half-life of the conjugated estrogens was similar with coadministration of PROMETRIUM Capsules. Table 2 summarizes the pharmacokinetic parameters.

TABLE 2. Mean (± S.D.) Pharmacokinetic Parameters for Estradiol, Estrone, and Equilin Following Coadministration of Conjugated Estrogens 0.625 mg and PROMETRIUM Capsules 200 mg for 12 Days to Postmenopausal Women
a Total estrogens is the sum of conjugated and unconjugated estrogen.
  Conjugated Estrogens Conjugated Estrogens plus PROMETRIUM Capsules
Drug Cmax
(ng/mL)
Tmax
(hr)
AUC(0-24h)
(ng × h/mL)
Cmax
(ng/mL)
Tmax
(hr)
AUC(0-24h)
(ng × h/mL)
Estradiol 0.037
± 0.048
12.7
± 9.1
0.676
± 0.737
0.030
± 0.032
17.32
± 1.21
0.561
± 0.572
Estrone
Total a
3.68
± 1.55
10.6
± 6.8
61.3
± 26.36
4.93
± 2.07
7.5
± 3.8
85.9
± 41.2
Equilin
Total a
2.27
± 0.95
6.0
± 4.0
28.8
± 13.0
3.22
± 1.13
5.3
± 2.6
38.1
± 20.2

OVERDOSAGE

No studies on overdosage have been conducted in humans. In the case of overdosage, PROMETRIUM Capsules should be discontinued and the patient should be treated symptomatically.

CONTRAINDICATIONS

PROMETRIUM Capsules should not be used in women with any of the following conditions:

  1. PROMETRIUM Capsules should not be used in patients with known hypersensitivity to its ingredients. PROMETRIUM Capsules contain peanut oil and should never be used by patients allergic to peanuts.
  2. Undiagnosed abnormal genital bleeding.
  3. Known, suspected, or history of breast cancer.
  4. Active deep vein thrombosis, pulmonary embolism or history of these conditions.
  5. Active arterial thromboembolic disease (for example, stroke and myocardial infarction), or a history of these conditions.
  6. Known liver dysfunction or disease.
  7. Known or suspected pregnancy.

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