Description overdue on 10/27/2014
- Latin name: Zoely
- ATC code: G03AA14
- Active substance: Nomegestrol plus estradiol (Nomegestrol + Estradiol)
- Manufacturer: Organon (Ireland) Ltd (Ireland)
- Composition
- Product form
- Pharmacological action
- Pharmacodynamics and pharmacokinetics
- Indications
- Contraindications
- Side effects
- Instructions for use Zoeli
- Overdose
- Cooperation
- Terms of sale
- Storage conditions
- Shelf life
- Cautions
- Analogs
- Babies
- With alcohol
- During pregnancy (and lactation)
- Reviews
- Price, where to buy
Composition
Tablet 1 - 2, 5 mg nomegestrola acetate and 1 55 mg of estradiol Hemihydrate (respectively 1 and 5 mg Estradiol ) - Active substances.
Auxiliary ingredients:
- 0, 7 mg - talc;
- 14 mg - microcrystalline cellulose;
- 0, 7 mg - magnesium stearate;
- 2, 4 mg - crospovidone;
- 57, 71 mg - lactose monohydrate;
- 0, 44 mg - colloidal silica.
Sheath:
- 1, 6 mg - Opadry II white.
Pills placebo :
- 0, 7 mg - talc;
- 14 mg - microcrystalline cellulose;
- 0, 7 mg - magnesium stearate;
- 2, 4 mg - crospovidone;
- 61.76 mg - lactose monohydrate;
- 0, 44 mg - colloidal silica.
Sheath:
- 2, 4 mg - Opadry II yellow.
Product form
Zoeli drug comes in the form of tablets in a film coating on 28 or 84 pills in a single package. The blister containing the tablets numbered days of the week.
Pharmacological action
The contraceptive.
Pharmacodynamics and pharmacokinetics
Zoeli - combined hormonal contraceptive medicament consisting than additional substances of the active components: estradiol (17β) and nomegestrola.
Estradiol is a natural estrogen Identical to human endogenous 17β-estradiol (E2) . The main difference from ethinyl estradiol , Included in the structure of other COCs (combined oral contraceptives), it is the absence of 17α-position methyl group. Receiving drugs Zoeli cause the average concentrations E2 Which correspond to those in the initial phase and the final follicular luteal phase of the menstrual cycle.
A derivative of natural progesterone - nomegestrol Similar thereto in structure and is highly selective progestogen . With a marked affinity for the receptor progesterone (Human), exhibits high antigonadotropnym and moderate anti-androgenic activity, without having with the androgen, glucocorticoid, estrogen and mineralocorticoid activity.
The contraceptive effect of the drug Zoeli is a combination of several effects, the most significant of which is the change secretion mucous cervix and suppression of ovulation . E2 increases effects progestogen , a nomegestrol It is involved in the suppression of ovulation. After the end of reception of a preparation Zoeli, the normal ovulation , Most women recovered pretty quickly.
Serum folate during reception Zoeli unchanged for six months and consecutive administration remains at a basic level.
Clinical studies found Pearl Index 0, 66 - to the age group of women 18 - 50 years 0, 75 - to 18 - 35 years, the upper boundary of the respective 95% confidence interval 1, 1.7, 23.
In the studies undertaken it was proved that preparation reception Zoeli not leads to meaningful changes metabolism lipids, does not affect on sensitivity to Insulin , Portability Glucose and hemostasis . The drug increases the number of proteins that transport CBG (corticosteroid-binding) and TBG (thyroxine-binding) globulins , But to a much lesser extent than the compound ethinyl estradiol from levonorgestrel . Also, significantly reduced the content of free and total of testosterone, dehydroepiandrosterone, of androstenedione and marginally increased concentration globulin Sex hormone binding (SHBG). During the histological examination endometrial After application Zoeli for 13 cycles, it was observed pathological changes.
Nomegestrol receiving at an internal rapidly absorbed and exhibits Cmax (7 ng / ml) in plasma after 2 hours. When receiving a single, absolute bioavailability is not dependent on food intake is equal to 63%.
At 97-98% binds albumin , While not binding to CBG or SHBG. Vss - 1 645 ± 576 liters.
It is metabolized by cytochrome P450 to several hydroxylated metabolites are inactive, which in turn, together with nomegestrolom Form a sulfate and glucuronide conjugates. In equilibrium, the ground clearance is 26 l / h.
At equilibrium, T1 / 2, the average - 46 hours (28 to 83 hours). Nomegestrol output means for renal lower intestine and a greater degree. About 80% of output to 4 days and is almost completely for 10 days.
Linear pharmacokinetics nomegestrola It depends on the dose (range 0 mg 625-5).
On the pharmacokinetics of nomegestrola SHBG is not affected. The equilibrium state is observed after 5 days. Average Css - 4 ng / ml. Plasma Cmax of about - 12 ng / ml and manifested through 90 minutes after administration.
Nomegestrol It does not react with glycoprotein P and no significant inhibitory action on or inducing cytochrome P450.
Estradiol , When taken orally, it lends itself to expressed metabolize when of his the first passage. Absolute bioavailability, regardless of the meal, about 5%.
Actively distributed throughout the body. The highest content of shows in target organs GHG ( hormones ). In the blood 37% bound to SHBG, 61% of albumin . Only 1-2% Estradiol found in unbound form.
When taken orally, exogenous Estradiol actively biotransformed and the similarity due to the endogenous estradiol , Is rapidly converted in the liver and intestine, several metabolites (mainly estrone ). Recent conjugated, undergoing intestinal and hepatic circulation. Oxidation occurs thanks to cytochrome P450 isoenzymes.
Cmax serum is observed after 6 hours and is equal to - 90 pg / ml. The average concentration of serum - 50 pg / ml.
Derived from the blood rapidly, T1 / 2 varies within a wide range, and after / in the administration of 8 ± 4 6 4 hours.
Indications
Birth control pills are prescribed for the purpose of Zoeli Contraception .
Contraindications
Precise data on contraindications oral contraceptives Containing 17β-estradiol does not exist. However, it can be assumed that they correspond to those when receiving etinilestradiolsoderzhaschih means. When receiving Zoeli, in cases of any of the following conditions, you should immediately stop taking it.
- hypersensitivity to any component of the tablet;
- thromboembolism pulmonary artery thrombosis deep veins, as in the present time and in the past;
- arterial thrombosis (Circulation Pathology of the brain, myocardial infarction );
- migraine with focal neurological symptoms, including the anamnesis;
- prodromal state ( angina, transient ischemic attack ), Including the anamnesis;
- multiple and / or severe factors of arterial or venous thrombosis ( severe hypertension, diabetes with vascular symptoms, severe dyslipoproteinemia );
- pancreatitis when in severe hypertriglyceridemia, in this time and in the past;
- acquired or genetic predisposition of the patient to the arterial or venous thrombosis For example: antithrombin III deficiency, and protein C and S, protein C resistance, hyperhomocysteinemia and the presence of antiphospholipid antibodies (Lupus anticoagulant antibodies to cardiolipin);
- tumor and heavy pathology liver, including in anamnesis;
- implied or diagnosed malignant hormone-dependent tumors ( tumors of the breast or genital );
- during breast feeding;
- the assumed or diagnosed pregnancy ;
- vaginal bleeding of unknown etiology;
- lactose intolerance, the deficit lactase, glucose-galactose malabsorption;
- postmenopause .
With extreme caution:
- serious condition depression , As a history;
- diabetes Passing without vascular pathology;
- systemic lupus erythematosus;
- ulcerative colitis ;
- Crohn's disease;
- pathology of the liver;
- hypertriglyceridemia , Now present or seen in the family history;
- risk factors for ischemic heart disease ( smoking, obesity, hypertension );
- the presence of a family history arterial embolism and venous thrombosis ;
- major surgery and prolonged immobilization.
Side effects
As shown, the tolerability of contraceptive Zoeli mostly good and safety of others is at the level of the combined drugs with similar effects. The following are the possible adverse effects that were observed at the reception Zoeli.
Metabolism:
- weight gain;
- fluid retention;
- increase or decrease in appetite.
CNS:
- decrease or increase libido ;
- depression;
- migraine ;
- violation of of attention;
- headache.
The bodies of:
- dryness of of the eyeballs;
- intolerance to contact lens wear.
Vascular system:
- tides .
Digestive system:
- bloating;
- nausea ;
- increase in liver enzymes;
- dryness in the oral cavity.
Skin and subcutaneous tissue disorders:
- acne ;
- alopecia ;
- hyperhidrosis ;
- itching;
- seborrhea ;
- dry skin;
- hypertrichosis ;
- chloasma .
Musculoskeletal system:
- a feeling of heaviness.
Reproductive organs and breasts:
- withdrawal bleeding;
- menorrhagia ;
- pain in the pelvic area;
- gipomenoreya ;
- engorgement of mammary glands;
- metrorrhagia ;
- galactorrhea ;
- premenstrual syndrome ;
- spasm of the uterus;
- seals in the mammary glands;
- dryness of the vagina and vulva;
- dyspareunia;
- discomfort in the vagina;
- unpleasant odor from the vagina.
General:
- edema ;
- irritability;
- hunger.
Adverse effects seen with KOC (combined oral contraceptives) that contain ethinyloestradiol:
- an increase in blood pressure ;
- arterial and venous thromboembolism ;
- chloasma ;
- hormone-dependent tumors ( breast cancer, liver tumors ).
The frequency of diagnosis of breast cancer in women using COCs slightly higher than that of women using other methods and means of contraception.
Communication between breast cancer and reception COCs is not installed.
Instructions for use Zoeli
Instructions on Zoeli recommends a daily intake of pills inside at the same time, without taking into account food intake. The tablets are in the sequence shown on the blister and washed down with water.
For all women's recommendations for use of the drug Zoeli same. Throughout 28 days is necessary to Streak to take 1 tablet every day. During the first 24 days of a tablet white color comprising active substance, and then, over the next 4 tablets yellow ( placebo ), Which do not contain active components.
The initial tablet from each of the following blister (or packaging) must be taken in the next day after the final of the last pill blister. The drug is carried out regardless of the presence or absence withdrawal bleeding Which usually occurs within 24-36 hours after the last consumption of pills of white color and can continue to use the start of the next blister.
Home use
For women not previously treated with hormonal contraceptives, it is best to start taking the first day Zoeli menstrual cycle . In this case additional contraceptive protection is needed. The application shall start from the 2nd-5th day of the cycle, but for a week, you need to use additional contraceptive barrier methods.
When switching from other hormonal contraceptives combined action (other COCs patches transdermal, vaginal rings ), In the case of other COCs recommends taking Zoeli the next day after the last active tablet ( no placebo ) Not later than the next day at the end of the normal range between cycles or taking pills placebo . When previous use of tons ransdermalnogo patch or vaginal rings Switching to pills Zoeli desirable to begin on the date of withdrawal (deletion), but not later than during the next recommended sticking plaster or entering the ring.
With the right and constant application of the preceding contraceptive methods and under the guarantee of lack of pregnancy, is possible the transition to Zoeli in any day of the. Bezgormonalny exceed the recommended period of the previous contraceptive method, it is impossible in any case.
In the case of switching from contraceptives containing one progestogen ( Implants Tablets, injections or IUD - intrauterine system ) During the previous use of other tablets, you can go to Zoeli any day, the next day after the termination of the adoption of progestogen tablets. When switching from injectables, taking pills Zoeli replaced by the following recommended injection. Navy or Implant removed at any convenient day, and which are beginning to take Zoeli. In all the above-described cases, it recommends to, throughout a week, to use additional barrier contraceptives.
After the abortion In the first trimester You can start the application Zoeli immediately after the procedure, while the additional contraceptive measures are required.
After abortion Second trimester or childbirth, you should start to use the drug between 21 and 28 days. In the case of later use, better, during the week, further use barrier contraceptives . At previous sexual contact, it is necessary to exclude possible pregnancy , Prior to use.
In the event of missed tablets
In the case of skip the next acting (of white color) tablets lead the following recommendations.
At delay following reception of at least 12 hours to take the tablet without correction desired sequence and subsequent reception time of tablets.
With more than 12-hour delay adhere to two rules:
- acting tablets should be taken for at least 7 consecutive days;
- the greater the number of missed active tablets and close during use placebo , The higher the possibility of pregnancy.
Omitting the first pill to take it as soon as possible, even in the case of receiving 2 subsequent tablets simultaneously. In the future continue to the usual scheme of application, without additional measures.
If you pass 2 or more tablets in the absence of withdrawal bleeding while taking placebo , Should be excluded pregnancy .
When you pass over the 1 st - 7 th days of the cycle should take the last missed tablet as soon as possible, even in the case of receiving 2 tablets at the same time later. Subsequently, to continue to use a conventional circuit using barrier contraception , During the first week. In the case of sexual intercourse at this time, it is possible pregnancy .
When you pass over the 8 th - 17 th day of the cycle should take the last missed tablet as soon as possible, even in the case of receiving 2 tablets at the same time later. Subsequently, to continue to use a conventional circuit using barrier contraception , During the first week.
When skipping over the 18th - 24th day of the cycle should take the last missed tablet as soon as possible, even in the case of receiving 2 tablets at the same time later. It is impossible to carry out a simultaneous reception of more than 2 active tablets. During the first week should be used barrier contraception And the first action of the next pill blister, take after the last active tablet of the previous one, that is, the phase of receiving minuyu placebo . In this scheme, withdrawal bleeding often occurs following reception phase placebo However during the current cycle, can be observed spotting or breakthrough bleeding.
Given the uncertainty in the amount of missed pills, you need to use barrier contraceptives , For at least a week of continuous reception of existing tablets.
Skipping pills placebo It does not lead to a lowering of contraceptive effect.
When gastrointestinal disease states, such as diarrhea or vomiting, may suffer the process of absorption of the drug Zoeli, in this connection, it is necessary to resort to auxiliary measures of contraception.
In case of vomiting over 3-to 4 hours after ingestion of tablets, this equates to a missed reception. If this painful condition lasts for several days, you should use the above recommendations. If you would not change the typical patterns of use can take additional steps tablet or tablet from another blister.
To delay the moment menstrualnopodobnoe bleeding you must start taking white tablets from the next blister immediately end their own from the previous blisters, that is, that the admission of placebo . White pills from the second blister, you can take full. Upon receiving placebo from the second blister, resume normal regimen Zoeli. In the case of the extended application may appear spotting and / or breakthrough bleeding . To move the start date of occurrence menstrualnopodobnoe bleeding It can reduce reception phase placebo (maximum of 4 days). Smaller increases the risk of a lack of break bleeding cancel and development of spreadable spotting and breakthrough bleeding.
Overdose
Serious side effects with the drug overdose Zoeli observed. 5 multiple repeated dose and single dose greater than 40 times the dose, showed no adverse effects.
You can prevent the emergence of nausea . emetic urges, bleeding from the vagina.
It is shown that symptomatic therapy.
Cooperation
In order to completely eliminate the potential interaction should carefully read the instructions to them, in the instructions for use of the drugs used in parallel.
Interaction of COCs, including Zoeli with other drugs can cause bleeding and / or decrease contraceptive effectiveness. The following summarizes the interaction of other drugs with COCs.
Hepatic metabolism
Possible interactions with inducers of microsomal liver enzymes, which may cause increase GHG clearance ( sex hormones). Definitely cooperation with barbiturates, phenytoin, primidone, rifampin, carbamazepine . Possible interactions with Griseofulvin . Of topiramate . Oxcarbazepine . Felbamate and drugs St. John's wort. Ritonavir Nevirapine
Ketoconazole
tetracyclines and ampicillin ethinylestradiol . and placebo
Cyclosporine .
Terms of sale
Prescription.
Storage conditions
Shelf life
36 months.
Cautions
ethinylestradiol .
thromboembolism thrombosis ( embolism thrombosis .
With the development of thrombosis
- edema
- breathlessness ;
- cough ;
- diplopia ;
- collapse
- .
embolism and thrombosis :
- obesity ;
- thrombophlebitis ;
- phlebeurysm ;
:
- ;
- arterial hypertension ;
- obesity ;
- migraine ;
- ;
- ;
thrombosis
- Crohn's disease;
- anemia.
migraine
and endometrial no.
Breast Cancer
pancreatitis .
hypertension .
jaundice .
Steroids
and . diabetes .
HIV infection
or . or pregnancy .
Femoden
Jess
Jess Plus
Dimia
Mersilon
Lindinet
Miniziston
Silest
Rigevidon
Yarina
+ Estradiol + at
Babies
With alcohol
During pregnancy and lactation
pregnancy
Lactation
.
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