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Norethisterone; Uses, Side Effects, Interactions, Pregnancy

Norethindrone is a synthetic progestational substance with some anabolic, estrogenic, and androgenic properties. Norethindrone binds to the progesterone intracellular receptors in the reproductive system and the resultant activated complex interacts with specific DNA sites. This leads to an alteration in protein synthesis and results in an inhibition of LH release. Consequently, it inhibits ovulation and changes the normal cycle of cervical mucus and endometrium.

Norethindrone is a synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception.

Norethisterone, also known as norethindrone is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders.

Mechanism of Action of Norethisterone

Progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin-releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.

Norethindrone shares the actions of progestins. Although the exact mechanism of action of progestin-only oral contraceptives is not known, norethindrone, when administered in usual contraceptive doses, appears to act principally by altering cervical mucus so that sperm migration into the uterus is inhibited. Progestational changes in the endometrium also occur which may inhibit implantation of the fertilized ovum in the uterus. In addition, continuous administration of low doses of norethindrone alters the rate of ovum transport by changing motility and secretion in fallopian tubes. Norethindrone prevents pregnancy even in the presence of ovulation. Norethindrone suppresses ovulation and causes ovarian and endometrial atrophy at high doses; the drug does not consistently suppress ovulation when administered in a continuous low-dose regimen. In low doses, norethindrone causes variable suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). Norethindrone has mild androgenic activity. At low doses, norethindrone also has some estrogenic activity.

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Indications of Norethisterone

Amenorrhea secondary
Dysfunctional Uterine Bleeding
Endometriosis
Endometriosis related pain
Estrogen deficiency
Postmenopausal osteoporosis
Vasomotor symptoms
Vulvovaginal atrophy
Use as a contraceptive,
Treat premenstrual syndrome,
Dysmenorrhea,
Menorrhagia,
Irregular menstruation,
Menopausal symptoms (in combination with estrogen), or to postpone a period.
It is also commonly used to help prevent uterine hemorrhage in complicated non-surgical or pre-surgical gynecologic cases and in treating nonresponsive cyclical mastalgia.
Oral contraceptives are indicated for the prevention of pregnancy in women who elect to use this product as a method of contraception
Indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathologies, such as submucous fibroids or uterine cancer.

Contra-Indications of Norethisterone

Diabetes
Excessive fat in the blood
Porphyria
Overweight
Depression
Migraine Headache
Poor Vision
Optic Disk Edema
High blood pressure
Heart Attack
Lung embolism
Chronic Heart Failure
Stroke
Obstruction of a Blood Vessel by a Blood Clot
Blood Clot in Vein
Liver Problems
Kidney disease with reduction in kidney function
seizures
Visible water retention
Pregnancy
Increased cardiovascular event risk

Dosage of Norethisterone

Strengths: 0.35 mg; 5 mg

Abnormal Uterine Bleeding

2.5 to 10 mg orally once a day
Duration of therapy: 5 to 10 days

Amenorrhea

2.5 to 10 mg orally once a day
Duration of therapy: 5 to 10 days

Contraception

0.35 mg orally once a day

Endometriosis

Initial dose: 5 mg orally once a day for 2 weeks
Maximum dose: 15 mg/day

Side Effects of Norethisterone

The most common

chest pain, irregular heartbeat, or shortness of breath
rapid or irregular heartbeat or pulse
heart palpitations
increased appetite
weight loss
dizziness
drowsiness
dry mouth
headache
joint pain
nausea and vomiting
Severe stomach ache
diarrhoea,
anorexia,
flatulence,
headache,
fainting, fast or pounding heartbeats.

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More common

weight loss
Syndrome of inappropriate secretion of antidiuretic hormone
Fast or irregular heartbeat
dizziness
headache
increased cough
Acid or sour stomach
decreased appetite
Agitation
chest congestion
chest pain
cold sweats
confusion
decreased sexual ability or desire
diarrhea or loose stools
heartburn
sleepiness or unusual drowsiness
stomach or abdominal cramps, gas, or pain
trouble sleeping

Less common

Abnormal dreams
change in sense of taste
congestion
discouragement, feeling sad, or empty
Acting on dangerous impulses
Aggressive or violent behavior
Thoughts about suicide or dying
New or worse depression
New or worse anxiety or panic attacks
Agitation, restlessness, anger, or irritability
Trouble sleeping
An increase in activity or talking more than normal

Drug Interactions of Norethisterone

Norethisterone may interact with following drugs, supplements & may decrease the efficacy of the drug

anticonvulsants (e.g., carbamazepine, phenytoin, phenobarbital)
antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
birth control pills containing estrogen
cyclosporine
estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
“gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
macrolide antibiotics (e.g., clarithromycin, erythromycin)
phenytoin
proton pump inhibitors (e.g., lansoprazole, omeprazole)
ranitidine
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
tramadol
warfarin

Pregnancy & Lactation of Norethisterone

FDA Pregnancy Category – X

Pregnancy

Birth control pills should not be taken by pregnant women. If you are taking birth control pills and discover that you are pregnant, stop the birth control pills and see your doctor. However, there is no conclusive evidence that the progestin contained in this medication will be harmful to the unborn child.

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Lactation

If the use of birth control pills is started after breastfeeding has begun, there does not appear to be any effect on the quantity and quality of the milk. There is no evidence that progestin-only birth control pills such as this medication are harmful to the nursing infant. No side effects have been found on breastfeeding performance or on the health, growth, or development of the infant.