Ethinyl Estradiol + Desogestrel + Ferrous Fumarate

Uses

Ethinyl Estradiol + Desogestrel + Ferrous Fumarate is also used to associated treatment for these conditions: ContraceptionFolic acid antagonist overdose, Iron Deficiency (ID), Iron Deficiency Anemia (IDA), Oral Contraceptives

How Ethinyl Estradiol + Desogestrel + Ferrous Fumarate 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.

Iron is necessary for the production of hemoglobin. Iron-deficiency can lead to decreased production of hemoglobin and a microcytic, hypochromic anemia.

Dosage

Ethinyl Estradiol + Desogestrel + Ferrous Fumarate 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.

Iron-deficiency anemia:

• Adult: Usual dose range: Up to 600 mg daily. May increase up to 1.2 g daily if necessary.
• Child:Preterm neonate: 0.6-2.4 ml / kg daily; up to 6 yr: 2.5-5 ml bid.

Should be taken on an empty stomach. Best taken on an empty stomach. May be taken with meals to reduce GI discomfort.

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.

Like all medicines, Ferrous Fumarate Tablets can sometimes cause side effects, although not everybody gets them. They might be:

• Heartburn
• Feeling sick or being sick
• Diarrhoea or constipation.

Also, you might find your stools are darker in color after you have taken this medicine. This is quite commonly seen with all iron preparations and is normal.

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.

Acute iron overdosage can be divided into four stages. In the first stage, which occurs up to six hours after ingestion, the principal symptoms are vomiting and diarrhea. Other symptoms include hypotension, tachycardia and CNS depression ranging from lethargy to coma. The second phase may occur at 6-24 hours after ingestion and is characterized by a temporary remission. In the third phase, gastrointestinal symptoms recur accompanied by shock, metabolic acidosis, coma, hepatic necrosis and jaundice, hypoglycemia, renal failure and pulmonary edema. The fourth phase may occur several weeks after ingestion and is characterized by gastrointestinal obstruction and liver damage. In a young child, 75 milligrams per kilogram is considered extremely dangerous. A dose of 30 milligrams per kilogram can lead to symptoms of toxicity. Estimates of a lethal dosage range from 180 milligrams per kilogram and upwards. A peak serum iron concentration of five micrograms or more per ml is associated with moderate to severe poisoning in many.

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.

Patients with intestinal strictures and diverticular disease. May worsen diarrhoea in patients with inflammatory bowel disease. May cause constipation and faecal impaction in elderly. Avoid prolonged admin (>6 mth) except in patients with continued bleeding, menorrhagia or repeated pregnancies. Not for routine use in treatment of haemolytic anaemia unless an iron-deficient state exists. Parenteral iron should not be used concurrently with oral iron treatment. Avoid use in patients receiving repeated blood tranfusions. Pregnancy.

Interaction

Reduced efficacy with enzyme-inducing drugs; aminoglutethimide. May inhibit ciclosporin metabolism.

Oral absorption of iron may be increased when taken with ascorbic acid. May reduce the absorption of quinolones and tetracyclines when taken concurrently via the oral route. Concurrent admin with antacids may reduce the absorption of ferrous fumarate from the GI tract. May reduce the absorption of penicillamine in the gut when taken concurrently.

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.

The efficiency of absorption depends on the salt form, the amount administered, the dosing regimen and the size of iron stores. Subjects with normal iron stores absorb 10% to 35% of an iron dose. Those who are iron deficient may absorb up to 95% of an iron dose.

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.

Pregnancy Category- Not Classified. FDA has not yet classified the drug into a specified pregnancy category

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.

Patients with a known hypersensitivity to any of the ingredients. Hemochroma

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.

Symptoms: Nausea, vomiting, abdominal pain, diarrhoea, haematemesis and rectal bleeding. Hypotension, coma and hepatocellular necrosis may occur later.

Treatment: Empty stomach contents by gastric lavage within 1 hr of ingestion. In severe toxicity, IV desferrioxamine may be given. Whole bowel irrigation may also be considered in severe poisoning.

Storage Condition

Store below 25° C in a cool, dry place. Keep away from light & out of reach of children.

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