Levonorgestrel
Generic Name: levonorgestrel
Brand Name: Plan B
Drug class : progestogen,progestin
Introduction:
Levonorgestrel is used to prevent pregnancy after unprotected sexual intercourse
(sex without any method of birth control or with a birth control method that failed
or was not used properly [e.g., a condom that slipped or broke or birth control pills
that were not taken as scheduled]). Levonorgestrel should not be used to prevent
pregnancy on a regular basis. This medication is to be used as an emergency
contraceptive or backup in case regular birth control fails or is used incorrectly.
Levonorgestrel is in a class of medications called progestins. It works by
preventing the release of an egg from the ovary or preventing fertilization of the
egg by sperm (male reproductive cells). It also may work by changing the lining of
the uterus (womb) to prevent development of a pregnancy. Levonorgestrel may
prevent pregnancy, but it will not prevent the spread of human immunodeficiency
virus (HIV, the virus that causes acquired immunodeficiency syndrome [AIDS])
and other sexually transmitted diseases.
Pharmacokinetics
• Absorption: proximal part of small intestine.
• Onset: 0.5-1 hour
• Metabolism: metabolized in liver.
• Elimination: urine
Mechanism of action:
Mechanism of action on ovulation
Oral contraceptives containing levonorgestrel suppress gonadotropins, inhibiting
ovulation. Specifically, levonorgestrel binds to progesterone and androgen
receptors and slows the release of gonadotropin-releasing hormone (GnRH) from
the hypothalamus. This process results in the suppression of the normal
physiological luteinizing hormone (LH) surge that precedes ovulation. It inhibits
the rupture of follicles and viable egg release from the ovaries. Levonorgestrel has
been proven to be more effective when administered before ovulation.
Mechanism of action in cervical mucus changes
Similar to other levonorgestrel-containing contraceptives, the intrauterine (IUD)
forms of levonorgestrel likely prevent pregnancy by increasing the thickness of
cervical mucus, interfering with the movement and survival of sperm, and inducing
changes in the endometrium, where a fertilized ovum is usually implanted.
Levonorgestrel is reported to alter the consistency of mucus in the cervix, which
interferes with sperm migration into the uterus for fertilization. Levonorgestrel is
not effective after implantation has occurred. Interestingly, recent evidence has
refuted the commonly believed notion that levonorgestrel changes the consistency
of cervical mucus when it is taken over a short-term period, as in emergency
contraception. Over a long-term period, however, levonorgestrel has been proven
to thicken cervical mucus. The exact mechanism of action of levonorgestrel is not
completely understood and remains a topic of controversy and ongoing
investigation.
Mechanism of action in hormone therapy
When combined with estrogens for the treatment of menopausal symptoms and
prevention of osteoporosis, levonorgestrel serves to lower the carcinogenic risk of
unopposed estrogen therapy via the inhibition of endometrial proliferation.
Unregulated endometrial proliferation sometimes leads to endometrial cancer after
estrogen use.
Indications:
Emergency contraception
Levonorgestrel, in the single-agent emergency contraceptive form, is indicated for
the prevention of pregnancy after the confirmed or suspected failure of
contraception methods or following unprotected intercourse. It is distributed by
prescription for patients under 17, and over the counter for those above this
age. This levonorgestrel-only form of contraception is not indicated for regular
contraception and must be taken as soon as possible within 72 hours after
intercourse. It has shown a lower efficacy when it is used off label within 96 hours.
Long-term contraception or nonemergency contraception
In addition to the above indication in emergency contraception, levonorgestrel is
combined with other contraceptives in contraceptive formulations designed for
regular use, for example with ethinyl estradiol. It is used in various hormone-
releasing intrauterine devices for long-term contraception ranging for a duration of
3-5 years.
Hormone therapy and off-label uses
Levonorgestrel is prescribed in combination with estradiol as hormone therapy
during menopause to manage vasomotor symptoms and to prevent
[Link]-label, levonorgestrel may be used to treat menorrhagia,
endometrial hyperplasia, and endometrios
Dose
Method of administration
For oral administration.
One tablet should be taken as soon as possible, preferably within 12 hours, and no
later than 72 hours after unprotected intercourse
If vomiting occurs within three hours of taking the tablet, another tablet should be
taken immediately.
Women who have used enzyme-inducing drugs during the last 4 weeks and need
emergency contraception are recommended to use a non-hormonal EC (emergency
contraception), i.e. Cu-IUD or take a double dose of levonorgestrel (i.e. 2 tablets
taken together) for those women unable or unwilling to use Cu-IUD
Levonorgestrel 1.5mg tablets can be used at any time during the menstrual cycle
unless menstrual bleeding is overdue.
Contraindication
leukemia
uterine fibroids
breast cancer
carcinoma cancer of the cervix
cancer of the uterus
cancer in the lining of the uterus
diabetes
inflammation of the cervix
inflammation or infection of the vagina
an infection of the vagina called bacterial vaginosis
an ovarian cyst
absence of menstrual periods
abnormal bleeding from the uterus
pregnancy to occur outside of womb
abnormal pap smear results
IUD insertion with active vaginitis
Side effect
heavier or lighter than usual menstrual bleeding
spotting or bleeding between menstrual periods
nausea
vomiting
diarrhea
tiredness
headache
dizziness
breast pain or tenderness
Nursing Consideration
Monitor for decreased pulse, perspiration, or pallor during insertion.
Keep patient supine until these signs have disappeared.
Monitor BP especially with preexisting hypertension.
Monitor diabetics for loss of glycemic control.
Report S&S of Pelvic Inflammatory Disease immediately: (e.g.,
prolonged or heavy bleeding, unusual vaginal discharge, abdominal or
pelvic pain or tenderness, painful sexual intercourse, chills, fever, and
flu-like symptoms).
Assess for mentioned cautions and contraindications.
Monitor closely diabetics Patient for blood glucose indications of
loss of control.
Inform patient not to use this drugs while breastfeed
Monitor for patient adverse effects
Reference
[Link]
[Link]
[Link]
disorders-amp-supplementation-e
[Link]
health/levonorgestrel-13-08-2004/
(Retrived on:-october 3)
Bimla shrestha
Roll no 8
