Medroxyprogesterone

ATC CodeG03AC06, G03DA02, L02AB02
CAS number520-85-4
PUB number10631
Drugbank IDDB00603
Empirical formulaC22H32O3
Molar mass (g·mol−1)344,488
Physical statesolid
Density (g·cm−3)1,1
Melting point (°C)221,75
Boiling point (°C)488
PKS value17,73
Solubility0.00221 mg/mL

Basics

Medroxyprogesterone is an active ingredient used for contraception in the three-month injection. It is a synthetically produced preparation that is injected into the thigh muscle every 3 months. The active ingredient is designed to prevent ovulation and therefore pregnancy. In the injection suspension, it is used as medroxyprogesterone acetate and is available as a white, crystalline powder that is insoluble in water. The active ingredient is also used as hormone replacement therapy during the menopause and is said to alleviate menopausal symptoms such as hot flushes or sweating.

Graphic structural formula of the active substance medroxyprogesterone

Effect

Medroxyprogesterone works by suppressing gonadotropin hormone production. Gonadotropin is responsible for the release of the hormone FSH (follicle-stimulating hormone). FSH in turn ensures follicle maturation. The follicle contains the egg cell. The follicle matures between the end of the last menstrual period and ovulation. During ovulation, it bursts and releases the egg, which can then be fertilized within around 48 hours. If the follicle does not mature, ovulation does not occur and the egg cannot be fertilized. Medroxyprogesterone can therefore be used as a contraceptive.

Medroxyprogesterone is mainly metabolized in the liver and excreted via the kidneys. The half-life, i.e. the time the body needs to excrete half of the active substance, is around 40-60 hours. The active substance is 86% protein-bound. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood), is 4.69 nmol/L and is reached after about 4-5 days.

Dosage

Always take medroxyprogesterone exactly as described in the package leaflet or as advised by your doctor.

Adults:

The usual recommended dose for adults is 104 mg medroxyprogesterone every 13 weeks.

If the interval is 14 weeks or more, additional contraceptive methods should be used.

When using for the first time, care should be taken to ensure that the injection is given within the first 5 days of a normal menstrual cycle.

It can generally be used within the first 5 days after childbirth, but should be used with caution due to reports of heavy and prolonged bleeding.

When switching to other contraceptives, care should be taken to ensure continuous contraception.

Children&adolescents:

The usual recommended dose in young women from menarche (first menstrual period) is also 104 mg medroxyprogesterone every 13 weeks .

As adolescents are still growing and medroxyprogesterone can lead to a decrease in bone density, a careful risk-benefit assessment must be carried out.

When using for the first time, care should be taken to ensure that the injection is given within the first 5 days of a normal menstrual cycle.

It can generally be used within the first 5 days after childbirth, but should be used with caution due to reports of heavy and prolonged bleeding.

When switching to other contraceptives, care should be taken to ensure continuous contraception.

Side effects

The following side effects may occur:

Common:

  • Depression
  • insomnia
  • anxiety
  • Affective disorders
  • irritability
  • weakened sexual desire
  • dizziness
  • headaches
  • abdominal pain
  • nausea
  • acne
  • Back pain
  • Pain in the extremities
  • Absence of menstruation
  • Heavy, frequent and/or unexpected bleeding
  • irregular bleeding
  • period pain
  • Pain in the chest
  • exhaustion
  • Reactions at the injection site
  • Dimpling or lump formation at the injection site
  • Pain at the injection site
  • weight gain
  • Changed vaginal smear

Occasionally:

  • Decrease in bone density
  • Decreased glucose tolerance
  • Altered liver enzymes
  • Fever attacks
  • ovarian cysts
  • uterine bleeding
  • vaginal discharge
  • sexual dysfunction
  • milk production without breastfeeding
  • pelvic pain
  • vaginal dryness
  • premenstrual syndrome
  • breast tenderness
  • breast enlargement
  • muscle cramps
  • joint pain
  • hives
  • rash
  • skin disorders
  • Excessive hair growth or hair loss
  • flatulence
  • bloating
  • high blood pressure
  • formation of varicose veins
  • hot flushes
  • rapid heart rate
  • migraine
  • somnolence
  • nervousness
  • emotional disturbances
  • absence of orgasms
  • drug hypersensitivity
  • Excretion of too little fluid
  • Increased or decreased appetite

Rarely:

  • Breast cancer
  • Decrease in fatty tissue
  • Loss of strength
  • Discoloration at the injection site

Frequency unknown:

Interactions

No known interactions.

Contraindications

Medroxyprogesterone must NOT be taken in the following cases:

  • if you are allergic to medroxyprogesterone
  • if pregnancy is suspected
  • vaginal bleeding of unknown cause
  • liver disease
  • breast cancer or cancer of the reproductive organs, currently or in the past
  • for deep vein thrombosis
  • pulmonary embolism
  • circulatory problems
  • for blood clotting disorders
  • metabolic diseases of the bones
  • for cerebrovascular diseases

Age restriction

Medroxyprogesterone can be used during the first menstrual period (menarche).

Pregnancy & breastfeeding

Medroxyprogesterone should NOT be used during pregnancy. As medroxyprogesterone is a contraceptive, it is contraindicated in pregnancy. No increased risk of malformation in the unborn baby has been observed when it is usually taken accidentally at the beginning of pregnancy (when you do not yet know that you are pregnant). Even if injected after conception, there is no increased risk.

Medroxyprogesterone should NOT be used in the 2nd and 3rd trimester of pregnancy . No experience is available.

Medroxyprogesterone should not be used during breastfeeding until 6 weeks after delivery. Although there are no reports or studies on negative effects within the first 6 weeks, the enzyme system of infants is better developed 6 weeks after birth.

History of the active ingredient

A scandal involving medroxyprogesterone broke in the summer of 2002, when it became known that a pharmaceutical producer had delivered industrial waste containing the active ingredient to an environmental technology company. The waste was incorporated into animal feed by a Belgian organic sugar company and sold in Germany. Medroxyprogesterone was subsequently detected in glucose syrup and pork.

Thomas Hofko

Thomas Hofko



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