Postinor 1.5 Mg 1 Tablet

Postinor (1.5 Mg 1 Tablet)

1. What is Postinor and what is it used for?

ACTION AND MECHANISM
- Emergency contraceptive. Levonorgestrel is a synthetic progestin, with progestagenic agonist effects. Its contraceptive effects could be due to an inhibition of ovulation and / or a decrease in fertilization due to alterations in the transport of sperm or ovule due to thickening of the cervical mucus. On the other hand, it inhibits embryo implantation by induction of endometrial alterations.

PHARMACKINETICS
Orally:

- Absorption: after a dose of 1.5 mg, it is absorbed rapidly (tmax 2 h) and almost completely (near 100% bioavailability). The cmax is 18.5 ng / ml.

Food effect: they do not seem to affect significantly.

- Distribution: high plasma protein binding (> 97.5%), especially sex hormone binding globulin (65%) and albumin. The Vd is 1.8 l / kg. It is excreted in small amounts in breast milk (0.1% of the breast dose).

- Metabolism: it is extensively metabolized in the liver by the usual steroid routes, by hydroxylation by CYP3A4. Several metabolites that are subsequently glucuronated have been described. There are no active metabolites.

Enzyme inducing / inhibiting ability: does not appear to have a significant effect.

- Excretion: in urine (45%) and feces (32%), mainly as glucuronated metabolites. The CLt is 7.7 +/- 2.7 L / h, while the t1 / 2 is 26 h.

Pharmacokinetics in special situations:

- Other situations: there are no specific data in girls, elderly women or patients with renal or hepatic impairment.

INDICATIONS
- [EMERGENCY CONTRACEPTION] within 72 hours (3 days) after having had unprotected sex or having produced a contraceptive failure.

POSOLOGY
- Adults: 1.5 mg administered as soon as possible, and never after 72 hours (3 days) after having had unprotected sexual intercourse or having produced the contraceptive failure.

It can be administered at any time during the menstrual cycle, as long as there has been no delay in the cycle.

The dose repetition in the same menstrual cycle has not been evaluated, so it is not advised.

- Girls and adolescents <18 years:

* Adolescents from 16 years: no specific dosage recommendations have been established.

* Girls and adolescents <16 years: very limited clinical experience. Levonorgestrel is not intended for premenarchic patients.

- Elderly women: it is not intended for these patients once menopause is reached.

Measures to be taken in case of vomiting: if the patient vomits within 3 hours after administration, administer a new dose.

Posology in special situations:

- Women treated with potent CYP3A4 inducers in the last 4 weeks: in case of not being possible or wishing to use non-hormonal emergency contraceptives, a dose of 3 mg could be administered. However, the safety and efficacy of this dose has not been evaluated.

POSOLOGY IN RENAL INSUFFICIENCY
It does not require dosage adjustment, regardless of the degree of renal functionality.

POSOLOGY IN HEPATIC INSUFFICIENCY
- Mild to moderate hepatic impairment (Child-Pugh classes A and B): no specific dosage recommendations could be established due to lack of studies.

- Severe hepatic impairment (Child-Pugh class C): not recommended.

RULES FOR THE CORRECT ADMINISTRATION
Swallow the tablet whole, without chewing, with enough water.

Administration with food: can be taken with or without food.

CONTRAINDICATIONS
- Hypersensitivity to levonorgestrel or any other component of the medicine.

PRECAUTIONS
- [LIVER FAILURE]. Safety and efficacy have not been specifically evaluated, so it has not been possible to verify whether women with mild to moderate insufficiency (Child-Pugh classes A and B) have different safety or efficacy profiles than those with normal liver function. Its use is not advised in severe hepatic impairment (Child-Pugh class C).

- [OVERWEIGHT]. There are very limited data that suggest that women who are overweight or obese may be less effective with levonorgestrel.

- Women at risk of ectopic pregnancy, as a previous history of said pregnancy or [SALPINGITIS]. It is unlikely that an ectopic pregnancy will occur due to its contraceptive effects. However, the appearance of menstrual bleeding does not eliminate the probability of ectopic pregnancy.

- [INTESTINAL MALABSORTION]. There could be a decrease in the absorption of levonorgestrel in patients with impaired intestinal absorption, such as [CROHN'S DISEASE].

- [THROMBOEMBOLISM]. Cases of thromboembolic events have been reported after administration of this medication. The possibility of a thromboembolic episode in women presenting with other risk factors for thromboembolism, especially personal or family history indicative of thrombophilia, should be considered.

PRECAUTIONS RELATING TO EXCIPIENTS
- This medicine contains lactose. Patients with hereditary or galactose [INTOLERANCE TO LACTOSE], Lapp lactase insufficiency or glucose or galactose malabsorption should not take this medicine.

- This medicine contains lactose. The intake of amounts greater than 5 g daily should be taken into account in patients with [DIABETES] and with intolerance to certain sugars.

PATIENT ADVICE
- Emergency contraceptives are intended exclusively for occasional employment to reduce the risk of pregnancy during sexual intercourse without contraceptive methods or in case of failure of a contraceptive method (eg rupture of condoms, forgetting to take oral contraceptives) . Levonorgestrel also does not protect against sexually transmitted diseases. Therefore, it should never replace other alternative contraceptive methods.

- Levonorgestrel delays ovulation, resulting in a contraceptive and non-abortive effect, so it should be taken as soon as possible after sexual intercourse, and never later than 3 days (72 h) later. Its administration once ovulation had occurred would not prevent pregnancy. Keep in mind that no contraceptive method is 100% effective, so it does not prevent pregnancy in all patients.

- After the use of levonorgestrel, fertility can be recovered quickly in a few days. Continue using contraceptives for the rest of the menstrual cycle to avoid pregnancy. Levonorgestrel can be used together with oral contraceptives.

- If, despite the use of levonorgestrel, you suspect that you may be pregnant, consult your doctor. Levonorgestrel does not exert any abortion effects.

- If you are breastfeeding, you should avoid breastfeeding for 8 hours after administration.

SPECIAL WARNINGS
- Confirm a possible pregnancy in case of delayed menstruation, lack of bleeding due to deprivation, abnormal menstruation or any other symptoms. Levonorgestrel can have an effect on the menstrual cycle itself, advancing it or delaying it a few days.

INTERACTIONS
Strong CYP3A4 inhibitors are not expected to result in a significant increase in levonorgestrel levels after a single dose.

- Cyclosporine. Levonorgestrel may inhibit the metabolism of cyclosporine, increasing the possibility of toxicity. The actual clinical impact of the administration of a single dose of levonorgestrel is unknown.

- CYP3A4 inductors. Levonorgestrel levels and their effects may decrease due to increased metabolism by drugs such as carbamazepine, efavirenz, phenytoin, phenobarbital, rifampicin or hypericum. Due to the prolonged enzymatic induction, other emergency contraceptive methods are advised in women who have received a potent CYP3A4 inducer in the previous 4 weeks, such as copper IUDs.

If the woman cannot or does not want to use these IUDs, a double dose of levonorgestrel may be administered (see Dosage; dosage in special situations). However, the efficacy of this dose is not evaluated.

- Ulipristal. Levonorgestrel and ulipristal could interfere with its effects, so association is not advised.

PREGNANCY
Safety in animals: the administration of high-dose progestogens in rats has resulted in virilization phenomena of female fetuses.

Safety in humans: adequate and well-controlled studies in humans are not available. There are limited data that suggest that levonorgestrel would not have embryotoxic effects on the fetus, but the consequences of dose administration> 1.5 mg are unknown. Nor is the influence of a single dose used as emergency contraception known. Levonorgestrel is not intended for use in pregnant women, and should not be used during this period. Despite this, it does not exert abortive effects.

If there is suspicion of pregnancy (period delay> 5 days, abnormal menstruation or any other symptoms) a test should be performed to rule it out or confirm it. Keep in mind that levonorgestrel could alter the menstrual cycle, shortening or delaying it.

In the event that the woman became pregnant, and as with any contraceptive, the possibility of ectopic pregnancy should be assessed.

Fertility effects: no specific studies have been conducted in humans. The woman is likely to recover fertility quickly after administration.

LACTATION
Animal safety: no data available.

Safety in humans: levonorgestrel is excreted in milk in small amounts (0.1% maternal dose). The consequences that it could have for the infant are unknown. It is advisable to administer levonorgestrel immediately after an intake, and stop breastfeeding for at least 8 hours.

CHILDREN
The clinical experience in girls and adolescents <16 years is very limited.

It is not intended for employment in pre-hierarchical girls, so it is recommended to avoid its use.

ELDERLY
Levonorgestrel is intended for emergency contraception, so there is no recommendation for use in women after menopause.

EFFECTS ON DRIVING
It is unlikely to have important effects, although it is very common to lead to fatigue or headache, and often dizziness.

ADVERSE REACTIONS
Adverse reactions are described according to each frequency range, being considered very frequent (> 10%), frequent (1-10%), rare (0.1-1%), rare (0.01-0.1%) , very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data).

- Digestive: very common [NAUSEAS], [ABDOMINAL PAIN]; Frequent [VOMITING], [DIARRHEA].

- Cardiovascular: frequency unknown [THROMBOEMBOLISM].

- Neurological / psychological: very frequent [CEFALEA]; Frequent [MAREO].

- Genitourinary: very common [UTERINE HEMORRAGY], [VAGINAL HEMORRAGY]; frequent irregular menstruation, [MASTALGIA], delay in menstruation; very rare [DISMENORREA], [PELVIC PAIN].

- Dermatological: very rare [EXANTEMATIC ERUPTIONS], [PRURITO], [URTICARIA].

- General: very frequent [FATIGUE]; very rare [EDEMA] facial.

ADVERSE REACTIONS CONCERNING EXCIPIENTS
- This medicine contains lactose, which may have milk proteins. It could cause [HYPERSENSITIVITY REACTIONS] in people with a cow's milk protein allergy.

OVERDOSE
Symptoms: The administration of high doses of oral contraceptives has not resulted in serious adverse reactions, and is usually limited to nausea or withdrawal bleeding.

Measures to take:

- Antidote: there is no specific antidote.

- General measures of elimination: it does not seem necessary to take any action.

- Monitoring: clinical status of the patient.

- Treatment: symptomatic.

Postinor 1.5 Mg 1 Tablet Leaflet