1. Name of the medicinal product

   

   Levonorgestrel 1.5mg Tablets – G-pill by Taj Pharma

G-Pill (Levonorgestrel) 1.5mg Tablets

2. Qualitative and quantitative composition

Each tablet contains 1.5mg of G-Pill (Levonorgestrel)

Excipient(s) with known effect:

Each tablet contains 140.10 mg of lactose monohydrate.

For a full list of excipients, see section 6.1.

3. Pharmaceutical form

Tablet.

Pink Colour round shaped tablets, debossed with “Taj” on one side and plain on the other side.

4. Clinical particulars

4.1 Therapeutic indications

Emergency contraception within 72 hours of unprotected sexual intercourse or failure of a contraceptive method.

4.2 Posology and 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 (see section 5.1).

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, i.e. Cu-IUD or take a double dose of G-Pill (Levonorgestrel) (i.e. 2 tablets taken together) for those women unable or unwilling to use Cu-IUD (see section 4.5).

G-Pill (Levonorgestrel) 1.5mg tablets can be used at any time during the menstrual cycle unless menstrual bleeding is overdue.

After using emergency contraception it is recommended to use a local barrier method (e.g. condom, diaphragm, spermicide, cervical cap) until the next menstrual period starts. The use of G-Pill (Levonorgestrel) does not contraindicate the continuation of regular hormonal contraception.

Paediatric population

There is no relevant use of G-Pill (Levonorgestrel) for children of prepubertal age in the indication emergency contraception.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

4.4 Special warnings and precautions for use

If pregnancy occurs after treatment with G-Pill (Levonorgestrel), the possibility of an ectopic pregnancy should be considered. The absolute risk of ectopic pregnancy is likely to be low, as G-Pill (Levonorgestrel) prevents ovulation and fertilisation. Ectopic pregnancy may continue, despite the occurrence of uterine bleeding.

Therefore, G-Pill (Levonorgestrel) is not recommended for patients who are at risk of ectopic pregnancy (previous history of salpingitis or of ectopic pregnancy).

G-Pill (Levonorgestrel) is not recommended in patients with severe hepatic dysfunction.

Severe malabsorption syndromes, such as Crohn’s disease, might impair the efficacy of G-Pill (Levonorgestrel).

This medicinal product contains lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

After G-Pill (Levonorgestrel) intake, menstrual periods are usually normal and occur at the expected date. They can sometimes occur earlier or later than expected by a few days. Women should be advised to make a medical appointment to initiate or adopt a method of regular contraception. If no withdrawal bleed occurs in the next pill-free period following the use of G-Pill (Levonorgestrel) after regular hormonal contraception, pregnancy should be ruled out.

Repeated administration within a menstrual cycle is not advisable because of the possibility of disturbance of the cycle.

G-Pill (Levonorgestrel) is not as effective as a conventional regular method of contraception and is suitable only as an emergency measure. Women who present for repeated courses of emergency contraception should be advised to consider long-term methods of contraception.

Use of emergency contraception does not replace the necessary precautions against sexually transmitted diseases.

4.5 Interaction with other medicinal products and other forms of interaction

The metabolism of G-Pill (Levonorgestrel) is enhanced by concomitant use of liver enzyme inducers, mainly CYP3A4 enzyme inducers. Concomitant administration of efavirenz has been found to reduce plasma levels of G-Pill (Levonorgestrel) (AUC) by around 50%.

Drugs suspected of having similar capacity to reduce plasma levels of G-Pill (Levonorgestrel) include barbiturates (including primidone), phenytoin, carbamazepine, herbal medicines containing Hypericum perforatum (St.John’s Wort), rifampicin, ritonavir, rifabutin, griseofulvin.

For women who have used enzyme-inducing drugs in the past 4 weeks and need emergency contraception, the use of non-hormonal emergency contraception (i.e. a Cu-IUD) should be considered. Taking a double dose of G-Pill (Levonorgestrel) (i.e. 3000 mcg within 72 hours after the unprotected intercourse) is an option for women who are unable or unwilling to use a Cu-IUD, although this specific combination (a double dose of G-Pill (Levonorgestrel) during concomitant use of an enzyme inducer) has not been studied.

Medicines containing G-Pill (Levonorgestrel) may increase the risk of cyclosporine toxicity due to possible inhibition of cyclosporin metabolism.

4.6 Fertility, pregnancy and lactation

Pregnancy

G-Pill (Levonorgestrel) should not be given to pregnant women. It will not interrupt a pregnancy. In the case of continued pregnancy, limited epidemiological data indicate no adverse effects on the fetus but there are no clinical data on the potential consequences if doses greater than 1.5 mg of G-Pill (Levonorgestrel) are taken (see section 5.3.).

Breast-feeding

G-Pill (Levonorgestrel) is secreted into breast milk. Potential exposure of an infant to G-Pill (Levonorgestrel) can be reduced if the breast-feeding woman takes the tablet immediately after feeding and avoids nursing at least 8 hours following G-Pill (Levonorgestrel) administration.

Fertility

G-Pill (Levonorgestrel) increases the possibility of cycle disturbances which can sometimes lead to earlier or later ovulation date. These changes can result in modified fertility date; however, there are no fertility data in the long term.

4.7 Effects on ability to drive and use machines

No studies on the effect on the ability to drive and use machines have been performed.

4.8 Undesirable effects

The most commonly reported undesirable effect was nausea.

All adverse drug reactions are listed by system, organ class and frequency.

Frequencies are defined as Very common (≥ 1/10), Common (≥ 1/100 to <1/10), Uncommon (≥ 1/1,000 to <1/100), Rare (≥ 1/10,000 to <1/1,000) and Very rare (<1/10,000), not known (cannot be estimated from the available data).

* Bleeding patterns may be temporarily disturbed, but most women will have their next menstrual period within 7 days of the expected time.

** If the next menstrual period is more than 5 days overdue, pregnancy should be excluded.

From Post-marketing surveillance additionally, the following adverse events have been reported:

Gastrointestinal disorders

Very rare (<1/10,000): abdominal pain

Skin and subcutaneous tissue disorders

Very rare (<1/10,000): rash, urticaria, pruritus,

Reproductive system and breast disorders

Very rare (<1/10,000): pelvic pain, dysmenorrhoea

General disorders and administration site conditions

Very rare (<1/10,000): face oedema

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme, website: www.mhra.gov.uk/yellowcard.

4.9 Overdose

Serious undesirable effects have not been reported following acute ingestion of large doses of oral contraceptives. Overdose may cause nausea, and withdrawal bleeding may occur. There are no specific antidotes and treatment should be symptomatic.

5. Pharmacological properties

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Sex hormones and modulators of the genital system, emergency contraceptives, ATC code: G03AD01

Mechanism of action

Levonorgestrel 1.5mg Tablets – G-pill by Taj Pharma

Levonorgestrel 1.5mg Tablets – G-pill by Taj Pharma

The precise mode of action of G-Pill (Levonorgestrel) as an emergency contraceptive is not known. At the recommended regimen, G-Pill (Levonorgestrel) is thought to work mainly by preventing ovulation and fertilisation if intercourse has taken place in the preovulatory phase, when the likelihood of fertilisation is the highest. G-Pill (Levonorgestrel) is not effective once the process of implantation has begun.

Clinical efficacy and safety

Results from a randomised, double-blind clinical study conducted in 2001 (Lancet 2002; 360: 1803-1810) showed that a 1500 microgram single dose of G-Pill (Levonorgestrel) (taken within 72 hours of unprotected sex) prevented 84% of expected pregnancies (compared with 79% when the two 750 microgram tablets were taken 12 hours apart).

There was no difference between pregnancy rates in case of women who were treated on the third or the fourth day after the unprotected act of intercourse (p>0.2).

Another study conducted in 1997 (Lancet 1998; 352: 428–33) showed that two 750 microgram doses taken 12 hours apart prevents 85% of expected pregnancies

At the recommended regimen, G-Pill (Levonorgestrel) is not expected to induce significant modification of blood clotting factors, and lipid and carbohydrate metabolism.

Paediatric population

A prospective observational study showed that out of 305 treatments with G-Pill (Levonorgestrel) emergency contraceptive tablets, seven women became pregnant resulting in an overall failure rate of 2.3%. The failure rate in women under 18 years (2.6% or 4/153) was comparable to the failure rate in women 18 years and over (2.0% or 3/152).

5.2 Pharmacokinetic properties

Absorption

Orally administered G-Pill (Levonorgestrel) is rapidly and almost completely absorbed.

Distribution

The results of a pharmacokinetic study carried out with 16 healthy women showed that following ingestion of single dose of 1.5 mg G-Pill (Levonorgestrel) maximum drug serum levels of G-Pill (Levonorgestrel) of 18.5 ng/ml were found at 2 hours. After reaching maximum serum levels, the concentration of G-Pill (Levonorgestrel) decreased with a mean elimination half-life of about 26 hours.

Biotransformation

G-Pill (Levonorgestrel) is not excreted in unchanged form but as metabolites.

Elimination

G-Pill (Levonorgestrel) metabolites are excreted in about equal proportions with urine and faeces. The biotransformation follows the known pathways of steroid metabolism, the G-Pill (Levonorgestrel) is hydroxylated in the liver and the metabolites are excreted as glucuronide conjugates.

No pharmacologically active metabolites are known.

G-Pill (Levonorgestrel) is bound to serum albumin and sex hormone binding globulin (SHBG). Only about 1.5% of the total serum levels are present as free steroid, but 65% are specifically bound to SHBG.

The absolute bioavailability of G-Pill (Levonorgestrel) was determined to be almost 100% of the dose administered.

About 0.1% of the maternal dose can be transferred via milk to the nursed infant.

5.3 Preclinical safety data

Animal experiments with G-Pill (Levonorgestrel) have shown virilisation of female fetuses at high doses.

Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeat-dose toxicity, genotoxicity and carcinogenicity potential, beyond the information included in other sections of the SmPC.

6. Pharmaceutical particulars

6.1 List of excipients

Lactose monohydrate, Maize starch, Povidone K30, Silica, colloidal anhydrous, Magnesium stearate

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

2 years

6.4 Special precautions for storage

Store below 25°C. Store in the original package in order to protect from light.

6.5 Nature and contents of container

PVC/PVDC/aluminium blister containing one tablet, which is further packed in to a carton.

6.6 Special precautions for disposal and other handling

No specific requirements.

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.