Mecpro – 200/400 capsules (oral progesterone)

MECPRO NAFDAC NO: B4 – 1131

Progesterone soft gelatin capsules for oral/vaginal/rectal use.

 

THERAPEUTIC CATEGORY: Female Sex Hormone.

COMPOSITION

Each soft gelatin capsule contains:

Progesterone   BP        200/400mg

(Micronized)

Excipient                       q.s

 

PHARMACOKINETICS

Absorption

(i) Vaginal/ rectal route

MECPRO is well absorbed when administered vaginally or rectally. Rectal or vaginal administration of 200-400mg produces concentration in luteal range which is maximal within 1-8 hours and then decline over a period of 24 hours.

(ii) Oral route

After oral administration progesterone as a micronized soft gelatin capsule formulation, maximum serum concentrations were attained within 3 hours. The absolute bioavailability of micronized progesterone is not known. Serum progesterone concentrations appeared linear.

Distribution

Progesterone is approximately 96%-99% bound to serum proteins, primarily to serum albumin (5%-54%) and transcortin (40%-48%).

Metabolism

Progesterone is metabolized by the liver largely to pregnanediols and pregnanolones. Pregnanediols and pregnanolone are conjugated in the liver to glucuronide and sulfate metabolites .progesterone metabolites which are excreted in the bile may be deconjugated and may be further metabolized in the gut via reduction, dehydroxylation, and epimerization.

Excretion

The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the bile and urine.

Progesterone metabolities which are excreted in the bile may undergo entero-hepatic recycling or may be excreted in the feces.

 

DOSAGE AND ADMINISTRATION

Flexible dosage regimen can be followed depending on the indication and requirement of patients. Lower dose is required when vaginal route is used.

Vaginal/Rectal Administration

Each capsule should be inserted deeply into the vagina. Rectal administration should be considered when ever vaginal administration is not possible.

Luteal support during assisted reproductive techniques (IVF-ET): MECPRO 200mg thrice a day from the day of embryo transfer till pregnancy is confirmed. If pregnant; it is continued till 12th week of pregnancy.

To provide luteal support in luteal phase defects: MECPRO 100mg thrice a day from the 17th day of the cycle for 10days. If pregnant, it is continued till12th week of pregnancy.

 

Oral Administration

The evening dose/once daily is preferably taken at bedtime.

In secondary amenorrhoea: MECPRO 400mg daily at bedtime for 10 days.

Dysfunctional uterine bleeding (DUB): MECPRO 300mg once daily from 12th day of the cycle for 10 days

Postmenopausl women with intact uterus (in addition to estrogen treatment): MECPRO 200mg at bed time for 12 days sequentially per 28 days cycle.

Premenstrual syndrome: MECPRO 100-200 mg once daily from 14th days of the cycle for 10 days.

SIDE EFFECTS

Breakthrough bleeding, spotting and menstrual irregularity,

Breast tenderness, Fatigue, Vertigo, Headache, light headedness or migraine have been reported rarely.

CONTRAINDICATIONS

Mecpro is contraindicated in

-Patients with known sensitivity to progesterone or its ingredients.

-Thrombophlebitis and Thromboembolic disorders.

-Severe liver disease.

-Known or suspected malignancy of the breast or genital organs, undiagnosed vaginal bleeding and missed abortion.

 

 

INTERACTION

The metabolism of progesterone by human liver microsomes was inhibited by ketoconazole.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.

OVER DOSAGE

There is wide margin of safety with progesterone but overdose may produce euphoria or dysmenorrhea.

 

STORAGE

Store in a cool, dry place.

Protect from sunlight

Keep out of children.

PRESENTATION

Mecpro is available as 200/400mg in blister strip of 10 soft gelatin capsules.