Nectrapill

Nectrapill Uses, Dosage, Side Effects, Food Interaction and all others data.

Nectrapill is a synthetic steroid which blocks the effects of progesterone by competitively binding to the intracellular progesterone receptor. It sensitises the myometrium to the contraction-inducing action of prostaglandin. At higher doses, it blocks the effect of cortisol at the glucocorticoid receptor while increasing circulating cortisol concentrations.

Nectrapill is a synthetic steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through 49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the myometrium to the contraction-inducing activity of prostaglandins. Nectrapill also exhibits antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol.

Trade Name Nectrapill
Availability Prescription only
Generic Mifepristone
Mifepristone Other Names Mifepriston, Mifepristona, Mifépristone, Mifepristone, Mifepristonum
Related Drugs dexamethasone, Decadron, misoprostol, cyproheptadine, oxytocin, Cytotec, Pitocin, Cervidil, Hemabate
Type Tablet
Formula C29H35NO2
Weight Average: 429.5937
Monoisotopic: 429.266779369
Protein binding

98% (bound to plasma proteins, albumin and a 1-acid glycoprotein)

Groups Approved, Investigational
Therapeutic Class Drugs acting on the Uterus
Manufacturer Nectar Lifesciences Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Nectrapill
Nectrapill

Uses

Nectrapill is used for:

  • As a medical alternative to surgical termination of intra-uterine pregnancy
  • Softening and dilatation of the cervix uteri prior to surgical pregnancy termination
  • Preparation for the action of prostaglandin analogues in the termination of pregnancy for medical reasons
  • Labour induction for the expulsion of a dead fetus (fetal death in utero).

Nectrapill is also used to associated treatment for these conditions: Hyperglycemia, Pregnancy Termination

How Nectrapill works

The anti-progestational activity of mifepristone results from competitive interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the compound inhibits the activity of endogenous or exogenous progesterone. The termination of pregnancy results.

In the treatment of Cushing's syndrome, Nectrapill blocks the binding of cortisol to its receptor. It does not decrease cortisol production but reduces the effects of excess cortisol, such as high blood sugar levels.

Dosage

Nectrapill dosage

As a medical alternative to surgical termination of intra-uterine pregnancy in early pregnancy: 600 mg Nectrapill in a single oral dose followed 36-48 hrs later, by the administration of a prostaglandin analogue Misoprostol 400 mcg orally (up to 49 days) or Gemeprost 1 mg vaginally (up to 63 days).

Softening and dilatation of the cervix uteri prior to surgical pregnancy termination: 200 mg Nectrapill, followed 36-48 hrs later (but not beyond) by a surgical termination of pregnancy.

Preparation for the action of prostaglandin analogues in the termination of pregnancy for medical reasons (to reduce the doses of prostaglandin): 600 mg of Nectrapill taken in a single oral dose, 36-48 hrs prior to scheduled prostaglandin administration which will be repeated as often as indicated.

Labour induction for expulsion of a dead fetus (fetal death in utero): 600 mg of Nectrapill in a single oral daily dose for 2 consecutive days. Nectrapill alone leads to expulsion in about 60%. Labour should be induced by the usual methods if it has not started within 72 hrs following the first administration of Nectrapill.

There are no precautions for timing in relation to food.

Side Effects

It is very common for women to experience uterine contractions or cramping (10-45%) in the hours following prostaglandin intake. Bleeding increases with gestational age. Heavy bleeding occurs in about 5% of cases and from 0-1.4% may require haemostatic curettage. Uterine rupture, hypotension, skin rashes, urticaria, hot flashes and dizziness have been uncommonly reported.

Toxicity

Nearly all of the women who receive mifepristone will report adverse reactions, and many can be expected to report more than one such reaction. About 90% of patients report adverse reactions following administration of misoprostol on day three of the treatment procedure. Side effects include more heavy bleeding than a heavy menstrual period, abdominal pain, uterine cramping, nausea, vomiting, and diarrhea.

Precaution

Nectrapill is available only in single dose packaging. Administration must be under the supervision of a qualified physician. There are no data on the safety and efficacy of Nectrapill in women with chronic medical conditions such as cardiovascular, hypertensive, hepatic, respiratory or renal disease; insulin-dependent diabetes mellitus; severe anemia or heavy smoking. Women who are more than 35 years of age and who also smoke 10 or more cigarettes per day should be treated with caution because such patients were generally excluded from clinical trials of Nectrapill. Although there is no clinical evidence, the effectiveness of Nectrapill may be lower if Misoprostol is administered more than two days after Nectrapill administration.

Interaction

ketoconazole, itraconazole, erythromycin and grapefruit juice may inhibit its metabolism (increasing serum levels of mifepristone). Furthermore, rifampicin, dexamethasone, St John's Wort and certain anticonvulsants (phenytoin, phenobarbital, carbamazepine) may induce mifepristone metabolism (lowering serum levels of Nectrapill). Based on invitro inhibition information, co-administration of mifepristone may lead to an increase in serum levels of drugs that are CYP3A4 substrates.

Limited evidence suggests that co-administration of NSAIDs on the day of prostaglandin administration does not adversely influence the effects of Nectrapill or the prostaglandin on cervical ripening or uterine contractility and does not reduce the clinical efficacy of medical termination of pregnancy.

Food Interaction

  • Avoid grapefruit products. Grapefruit inhibits the metabolism of mifepristone through the CYP3A4 pathway causing increased serum levels of mifepristone.
  • Take with food. Taking mifepristone with meals has been shown to increase serum levels of mifepristone.

[Moderate] ADJUST DOSING INTERVAL: Food may significantly increase the plasma concentrations of mifepristone.

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of mifepristone.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Because pharmacokinetic interactions involving grapefruit juice are often subject to a high degree of interpatient variability, the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: When mifepristone is used daily to control hyperglycemia secondary to hypercortisolism in patients with endogenous Cushing's syndrome, it should be taken with food to achieve consistent plasma drug levels.

Patients should be advised to avoid consuming grapefruit or grapefruit juice during treatment with mifepristone, as it may cause increased adverse effects such as headache, dizziness, fatigue, nausea, vomiting, cramping, diarrhea, hypokalemia, adrenal insufficiency, vaginal bleeding, arthralgia, peripheral edema, and hypertension.

Because mifepristone is eliminated slowly from the body, the interaction with grapefruit juice may be observed for a prolonged period.

Elimination Route

The absolute bioavailability of a 20 mg oral dose is 69%

Half Life

18 hours

Elimination Route

Fecal: 83%; Renal: 9%.

Pregnancy & Breastfeeding use

Pregnancy: Nectrapill is indicated for use in the termination of pregnancy (through 49 days’ pregnancy) and has no other approved indication for use during pregnancy.

Lactation: It is not known whether Nectrapill is excreted in human milk. Many hormones with a similar chemical structure, however, are excreted in breast milk. Since the effects of Nectrapill on infants are unknown, breast-feeding women should consult with their health care provider to decide if they should discard their breast milk for a few days following administration of the medications.

Contraindication

Nectrapill must not be administered if there is doubt as to the existence or age of the pregnancy or if an extra-uterine pregnancy is suspected. An ultrasound scan and/or measurement of Beta-hCG must be performed before administration. For first trimester abortions, Nectrapill is contraindicated if the pregnancy is beyond 49 days of amenorrhoea when used with Misoprostol, or beyond 63 days of amenorrhoea when used with Gemeprost. Nectrapill should never be prescribed in patients with chronic adrenal failure, known allergy to Nectrapill or to any component of the product, severe asthma uncontrolled by corticosteroid therapy, porphyrias and renal failure, liver failure or malnutrition, or during breast feeding. Nectrapill is a lipophilic compound and may theoretically be excreted in the mother\'s breast milk, however no data is available.

Special Warning

Use in children: Safety and effectiveness in pediatric patients have not been established.

Acute Overdose

Single doses of Nectrapill up to 2 gm caused no unwanted reaction. In the event of massive ingestion, signs of adrenal failure might occur. Acute intoxication may require admission to hospital and if relevant treatment with dexamethasone.

Storage Condition

Store at 25° C.

Innovators Monograph

You find simplified version here Nectrapill

Nectrapill contains Mifepristone see full prescribing information from innovator Nectrapill Monograph, Nectrapill MSDS, Nectrapill FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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