Mercilon 28
Mercilon 28 Uses, Dosage, Side Effects, Food Interaction and all others data.
Desogestrel is a progestogen structurally related to levonorgestrel that has been shown to reliably inhibit ovulation.
The effects of desogestrel are divided on reproductive including modification of luteinizing hormone and follicle stimulating hormone, declines on the onset of menstruation, and increases the viscosity of the vaginal fluid; and on metabolic that includes increase insulin secretion and resistance, increased lipase activity, and increased fat deposition. The effect of desogestrel on the lipids has been studied extensively and the results are contradictory.
Desogestrel main therapeutic effect due to its mechanism of action is known to be related to the inhibition of the ovulation in 97% of the cycles. This effect was proven in clinical trials in non-breastfeeding women from which the Pearl failure rate was reported to be of 0.17 per 100 women-years. This result indicated that desogestrel is more efficient when compared to other progestogen-only pills. All the therapeutic effect is produced by a transformation of the endometrium followed by an inhibition of the ovulation due to the suppression of other hormones.
Desogestrel has been widely confirmed to be related to an increase in the risk of venous thromboembolism due to the driven increased in blood coagulation factors, leading to a pronounced prothrombotic state. However, the effects of desogestrel are known to not impact significantly the level of total cholesterol remaining in the range of change of 10% which allows it to be a molecule that presents a favorable lipid profile.
| Trade Name | Mercilon 28 |
| Generic | Desogestrel + ethinyl estradiol |
| Type | |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Sweden, Thailand |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Desogestrel used for prevention of pregnancy or oral contraception.
Mercilon 28 is also used to associated treatment for these conditions: Contraception
How Mercilon 28 works
Desogestrel enters the cell passively and acts by binding selectively to the progesterone receptor and generating low androgenic activity. Its binding produces an effect like a transcription factor and thus, it produces modifications in the mRNA synthesis.
The active metabolite of desogestrel, etonogestrel, presents a combination of high progestational activity with minimal intrinsic androgenicity.
Dosage
Mercilon 28 dosage
When used alone: 75 mcg daily when used alone.
For monophasic combined oral contraceptives: Typically, 150 mcg daily;
For triphasic combined oral contraceptives: 50-150 mcg daily.
Side Effects
Common- Irregular bleeding, amenorrhoea, headache, weight gain, breast pain, nausea, acne, mood changes, decreased libido. Less common- Vaginitis, dysmenorrhea, vomiting, alopecia, fatigue, difficulty wearing contact lenses. Rare- Rash, urticaria, erythema nodosum.
Toxicity
Administration of large quantities of desogestrel has been shown to produce strong hormonal effects but to lack chronic toxicity. The reported LD50 in rats after oral administration of desogestrel is higher than 2000 mg/kg. Overdose hasn't reported serious effects but only symptoms of nausea and withdrawal of bleeding.
Most reports haven't linked the administration of desogestrel with the increased risk of breast cancer. The increased risk has been reported to be related to the duration of use. However, several reports indicate a desogestrel-driven increased risk in cervical intra-epithelial neoplasia but the results are still not conclusive.
Precaution
Heart disease, sex-steroid dependent cancer, past ectopic pregnancy, malabsorption syndromes, functional ovarian cysts, active liver disease, recurrent cholestatic jaundice, history of jaundice in pregnancy, history of CV or renal impairment, DM, asthma, epilepsy, migraine, depression and thromboembolism; lactation.
Interaction
Reduced efficacy with enzyme-inducing drugs; aminoglutethimide. May inhibit ciclosporin metabolism.
Volume of Distribution
The apparent volume of distribution of desogestrel is of 1.5 L/kg.
Elimination Route
After oral administration, desogestrel is rapidly absorbed and it reaches a peak concentration of 2 ng/ml after 1.5 hours. The bioavailability of desogestrel is reported to be in the range of 60-80% and the reported AUC is of 3000 ng.h/ml. Almost all the administered dose is modified to the active metabolite, etonogestrel.
Half Life
The terminal half-life of desogestrel is determined to be of 30 hours.
Clearance
The metabolic clearance rate of desogestrel is reported to be of about 2 ml/min/kg.
Elimination Route
The elimination of desogestrel is found to be mainly renal corresponding to about 6 times the dose eliminated in the bile. The elimination of desogestrel is only done as the metabolites and not as the unchanged drug and about 85% of the administered dose can be excreted as metabolites after 6-8 days.
Pregnancy & Breastfeeding use
Incase of known or suspected Desogestrel is contraindicated. Desogestrel does not influence the production or the quality (protein, lactose, or fat concentrations) of breast milk. From clinical trial it has been seen that it has no effect on the development and growth of a nursing infant.
Contraindication
Desogestrel is contraindicated in the following conditions: Known or suspected pregnancy; Active venous thromboembolic disorder; Presence or history of severe hepatic disease as long as liver function values have not returned to normal; Known or suspected sex-steroid sensitive malignancies; Undiagnosed vaginal bleeding; Hypersensitivity to the active substance or to any of the excipients.
Acute Overdose
There have been no reports of serious deleterious effects from overdose. Symptoms that may occur in this case are nausea, vomiting and, in young girls, slight vaginal bleeding. There are no antidotes and further treatment should be symptomatic.
Storage Condition
Store below 25° C in a cool, dry place. Keep away from light & out of reach of children.
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