Desogestrel
Desogestrel 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 | Desogestrel |
| Generic | Desogestrel |
| Desogestrel Other Names | Desogestrel, Désogestrel, Desogestrelum |
| Type | |
| Formula | C22H30O |
| Weight | Average: 310.473 Monoisotopic: 310.229665582 |
| Protein binding | The main metabolite of desogestrel is mainly found bound to albumin and sex-hormone binding globulin. Around 96-98% of the administered dose of desogestrel is found bound to plasma proteins from which 40-70% is found bound to sex-hormone binding globulin. |
| Groups | Approved |
| Therapeutic Class | Oral Contraceptive preparations |
| Manufacturer | |
| Available Country | Netherlands |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Desogestrel used for prevention of pregnancy or oral contraception.
Desogestrel is also used to associated treatment for these conditions: Contraception
How Desogestrel 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
Desogestrel 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.
Food Interaction
No interactions found.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.
Innovators Monograph
You find simplified version here Desogestrel
Desogestrel contains Desogestrel see full prescribing information from innovator Desogestrel Monograph, Desogestrel MSDS, Desogestrel FDA label
FAQ
What are the side effects of Desogestrel?
Nausea, vomiting, headache, bloating, breast tenderness, swelling of the ankles/feet (fluid retention), or weight change may occur. Vaginal bleeding between periods (spotting) or missed/irregular periods may occur, especially during the first few months of use.
Does Desogestrel cause weight gain?
With regards to changing your Pill to one less likely to affect weight, the Pills containing Desogestrel and gestodene types of progesterone hormone are suggested as less likely to cause weight gain.
What does Desogestrel do to my body?
The traditional progestogen-only pill (POP) prevents pregnancy by thickening the mucus in the cervix to stop sperm reaching an egg. The Desogestrel progestogen-only pill can also stop ovulation. The progestogen-only pill needs to be taken every day to work.
Does Desogestrel stop periods?
The Desogestrel pill (12-hour pill, Desogestrel) stops ovulation in 97% of menstrual cycles.
Does Desogestrel affect my mood?
Desogestrel is known to be commonly associated with mood changes, depressed mood and decreased libido Anxiety and panic attacks have however not yet been described with Desogestrel use.
Does Desogestrel make my breasts bigger?
Birth control pills Desogestrel can affect your breast size, they don't change breast size permanently.
At what age should I stop taking Desogestrel?
If you're healthy and you don't smoke, you can continue taking birth control pills after age 35. However, birth control pills aren't recommended if you're 35 or older and you smoke because of the risk of cardiovascular disease.
Is it normal to bleed on the Desogestrel pill?
Irregular bleeding or spotting is common in the first three to four months after you start taking the Desogestrel. This should subside once your body adjusts to the medication. You may experience spotting later on if you've missed or skipped a dose.
Can Desogestrel cause hair growth?
Desogestrel is low on the androgen index, and they can actually stimulate hair growth by keeping your hair in the anagen phase longer. Low-androgen birth control pills include: desogestrel-ethinyl estradiol (Desogen, Reclipsen)
Can Desogestrel cause night sweats?
Desogestrel appears to be associated with dry eyes, vulvovaginal dryness (atrophic vaginitis) and night sweats (nocturnal hyperhidrosis), according to a signal reported in the WHO Pharmaceutical Newsletter.
How long does Desogestrel take to work?
Desogestrel takes two days for the pill's contraceptive effect on cervical mucus to be re-established after missing a pill. If you are taking a 12-hour pill that stops ovulation (a desogestrel pill, such as Desogestrel), you will need additional contraception for two days.
Does Desogestrel cause water retention?
Desogestrel have previously been shown to increase sodium excretion3, demonstrating that sodium and associated fluid retention does not occur in the body during use of oral contraceptives containing 'traditional' progestogens.
Can Desogestrel make me crazy?
For some women, being on the Desogestrel can magnify these feelings, leading to anxiety disorders and depression. But if these things happen to you, it doesn't mean you're crazy; it just means you're on the wrong pill. Mood-related issues like anxiety and depression are super-common among women on the Desogestrel.
Can Desogestrel help with anxiety?
Hormonal contraception can cause feelings of anxiety in some people. But other users may find their birth control relieves anxiety symptoms.
Does Desogestrel make my boobs grow?
Starting to take Desogestrel can stimulate the breasts to grow. However, any increase in size is typically slight. Within a few months of taking the pill, the breasts generally return to their regular size. This usually also happens if a person stops taking Desogestrel.
Does Desogestrel cause blood clots?
Among those ages 25 to 49 taking Desogestrel, drospirenone or cyproterone, an additional 17 women per 10,000 will develop a blood clot.
Why is Desogestrel prescribed for?
Desogestrel is used to prevent pregnancy. It is a birth control pill when taken properly, prevents pregnancy. It works by stopping a woman's egg from fully developing each month.
Can I push my period out faster?
The best way to make your period come faster is to take your placebo birth control pills earlier than usual. You can also make your period come faster by having sex or relieving stress through exercise or meditation.
Can Desogestrel cause weight gain?
Desogestrel containing desogestrel and gestodene types of progesterone hormone are suggested as less likely to cause weight gain.
