Tricquilar, 21 pcs.

Triquilar is a low-dose, three-phase oral combined estrogen-gestagen contraceptive.

The contraceptive effect of Triquilar is achieved through three complementary mechanisms:

• inhibiting ovulation at the level of hypothalamic-pituitary regulation;
• changing the properties of the cervical secretion, making it impermeable to sperm;
• changes in the endometrium, which makes implantation of a fertilized egg impossible.

Women taking combined oral contraceptives have a more regular menstrual cycle, less frequent painful menstruation, less heavy bleeding, and as a result the risk of iron deficiency anemia is reduced.

Pharmacokinetics

Levonorgestrel

Intake

Intake

. After oral administration, levonorgestrel is rapidly and completely absorbed, its serum Cmax of 2.3 ng/ml is reached after about 1 hour. After a single oral administration of 0.125 mg of levonorgestrel together with 0.33 mg of ethinylestradiol (corresponding to the highest levonorgestrel content of the triphasic drug), the highest serum concentration of 4.3 ng/ml was determined after approximately one hour. Levonorgestrel is almost completely bioavailable when taken orally.

Distribution

Levonorgestrel is bound by serum albumin and sex hormone-binding globulin (hGBS). Only 1.4% of total serum concentrations are free; whereas 55% are specifically bound to HSPH and about 44% are not specifically bound to albumin. As a result of the induction of binding protein synthesis by ethinylestradiol, the HSPH-bound fraction increases, whereas the albumin-bound fraction decreases. The apparent Vd of levonorgestrel is approximately 128 L after a single oral tablet of Tricquilar containing the highest dose of levonorgestrel.

The equilibrium concentration. The pharmacokinetics of levonorgestrel are influenced by serum hGH levels, which increase about 2-fold over a 21-day course of Triquilar. Daily administration of the drug increases serum levels by about 2-fold, and the equilibrium concentration is reached in the second half of the course. At equilibrium concentration, the volume of distribution and clearance rate are reduced to 52 L and 0.5 ml/min/kg, respectively.

Metabolism

Levonorgestrel is fully metabolized through steroid-specific metabolic pathways. After a single oral dose of the highest dose of levonorgestrel, the serum clearance rate is approximately 1.0 mL/min/kg.

The levonorgestrel serum content undergoes a biphasic decrease. The T1/2 in the terminal phase is about 22 h. Levonorgestrel is not excreted unchanged but only as metabolites, which are excreted with a T1/2 of about 24 h in the urine and bile at a ratio of about 1:1.

Ethinylestradiol

Intake

Ethinylestradiol is quickly and completely absorbed after oral administration. A serum Cmax of approximately 116 pg/mL is reached in 1.3 hours. During absorption and the first passage through the liver, ethinylestradiol is metabolized, resulting in a mean bioavailability of about 45% when ingested, with significant individual differences ranging from 20-65%.

Distribution

Ethinylestradiol is almost completely (98%), although non-specific, bound by albumin. Ethinylestradiol induces the synthesis of HSPC. The apparent Vd of ethinylestradiol is 2.8-8.6 L/kg.

The equilibrium concentration is reached after one week.

Metabolism

Ethinylestradiol undergoes presystemic conjugation both in the small intestinal mucosa and in the liver. The main metabolic pathway is aromatic hydroxylation. The metabolic clearance rate from plasma is 2.3-7 ml/min/kg.

The concentration of ethinylestradiol in blood serum decreases, and the decrease is biphasic; the first phase is characterized by a T1/2 of about 1 h, the second – 10-20 h. It is not excreted from the body unchanged. Metabolites of ethinylestradiol are excreted by the kidneys and liver in a ratio of 4:6; with a T1/2 of about 24 h.

Indications

Contraception

Preventing pregnancy; mid-cycle pain, irregular periods.

Active ingredient

Ethinylestradiol, Levonorgestrel

Composition

Active substances:

levonorgestrel,

ethinylestradiol;

Associates:

calcium carbonate,

iron oxide pigment red,

Iron oxide pigment yellow,

Glycerol 85%,

Lactose monohydrate,

Magnesium stearate,

Corn starch,

Montanglicol wax,

MacroGol 6000,

Povidone 25,000, <

povidone 700,000,

sucrose,

talc,

titanium dioxide.

How to take, the dosage

Ingestion. Tablets should be taken in the order listed on the package (blister), every day at about the same time, with a little water. Take one tablet a day continuously for 21 days. The pills from the next package start after a 7-day break from the pills, during which you usually have a bleeding discontinuation. Menstrual bleeding usually begins on the 2nd or 3rd day after taking the last pill and may not end until the pills from the new pack start.

How to start Triquilar^®

If you have not taken any hormonal contraceptive medicine in the previous month. The use of Triquilar® begins on the 1st day of the menstrual cycle (i.e., the first day of menstrual bleeding). It is allowed to start taking the drug on days 2-5 of a menstrual cycle, but in this case it is recommended to use an additional barrier method of contraception during the first 7 days of taking tablets from the first package.

If you are switching from other OCs, vaginal ring, or contraceptive patch. It is preferable to start Triquilar^® the day after taking the last active pill from the previous package, but never later than the day after the usual 7-day interval (for products containing 21 tablets) or after taking the last inactive pill (for products containing 28 tablets in a package). The use of Triquilar^® should be started on the day the vaginal ring or patch is removed, but no later than the day a new ring or patch is to be inserted.

When switching from a contraceptive containing only gestagens (“mini-pills,” injectable forms, implant) or from a gestagen-releasing intrauterine contraceptive (Mirena^®). A woman may switch from the “mini-pill” to Triquilar® on any day (without a break), from the implant or intrauterine contraceptive with gestagen – on the day of its removal, from the injectable form – from the day when the next injection is to be made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the pills.

After an abortion in the first trimester of pregnancy. A woman can start taking the drug immediately. If this condition is met, the woman does not need additional contraceptive protection.

After delivery or abortion in the second trimester of pregnancy. It is recommended that the drug be started on day 21-28 after childbirth if the woman is not breastfeeding or after a second trimester abortion. If you start taking the drug later, you should additionally use a barrier method of contraception during the first 7 days of taking the pills. However, if sexual intercourse occurs, pregnancy must be ruled out or the first menstrual period must be awaited before starting Triquilar^®.

Missed pills

If the delay in taking the drug is less than 12 hours, contraceptive protection is not reduced. The woman should take the pill as soon as possible, and the next one is taken at the usual time.

If pills are taken more than 12 hours late, contraceptive protection may be reduced. The more pills missed, and the closer the miss is to a 7-day break in taking the pills, the greater the chance of pregnancy. The following two basic rules can guide you in this process:

– taking the drug should never be interrupted, for more than 7 days;

– 7 days of continuous pills are required to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

The following recommendations may be made accordingly:

The first week of taking the drug. The woman should take the last pill she missed; as soon as she remembers (even if that means taking two pills at once). The next pill is taken at the usual time. Additionally, a barrier method of contraception (such as a condom) must be used for the next 7 days. If sexual intercourse took place during the week before skipping the pill, it is necessary to consider the possibility of pregnancy.

The second week of taking the drug. The woman should take the last missed pill as soon as she remembers (even if it means taking two pills at once). The next pill is taken at the usual time. Provided that the woman has taken the pills correctly in the 7 days preceding the first missed pill, no additional contraceptive measures are necessary. Otherwise, and if two or more pills are missed, additional barrier methods of contraception (e.g., a condom) should be used for 7 days.

The third week of taking the drug. The risk of decreased reliability is inevitable because of the upcoming break in taking the pills. The woman must strictly adhere to one of the following two options. That said, if all pills were taken correctly in the 7 days preceding the first missed pill, there is no need to use additional contraceptive methods:

1. The woman should take the last missed pill as soon as she remembers (even if that means taking two pills at once). The next pills are taken at the usual time until the pills from the current package run out. The pills from the next package should be started immediately. Bleeding cancellation is unlikely until the pills from the second package are finished, but bleeding of varying degrees of intensity (from smeary to breakthrough) may occur while taking the pills.

2. A woman can also stop taking the pills from her current package. She must then take a break for 7 days, including the day she missed the pills and then start taking the pills from the new package. If the woman misses taking the pills and then has no bleeding cancellation during the break, pregnancy should be ruled out.

Recommendations in case of gastrointestinal distress

If a woman has had vomiting or diarrhea within 3 to 4 h after taking the pills, absorption may be incomplete and additional contraceptive measures should be taken. In these cases, the recommendations for skipping the pills should be followed.

To change the day menstrual bleeding begins

In order to delay the onset of menstrual bleeding, a woman should continue taking the drug using the last 10 pills (numbered 12 to 21) from another package of Triquilar ^® without taking a break in the drug. In this way, the cycle can be lengthened by up to 10 days until the end of the second dose. While taking the drug from the second package, a woman may experience a mucous bloody discharge or breakthrough uterine bleeding. Regular use of Triquilar^® is then resumed after the usual 7-day break from taking the pills.

In order to reschedule menstrual bleeding to another day of the week, a woman should shorten her next pill interval by the desired number of days. The shorter the interval, the greater the risk that she won’t have a withdrawal bleed and will have future menses or breakthrough bleeding while taking pills from the second pack (just like when she would like to delay the start of her menstrual-like bleeding).

Additional information for specific patient groups

Children and adolescents

The drug Triquilar^® is contraindicated until ovulatory cycles are established.

Patients in postmenopause

Not applicable. Triquilar^® is contraindicated after the onset of menopause.

Patients with liver disorders

Triquilar^® is contraindicated in women with severe liver disease until liver function returns to normal.

Patients with renal impairment. Tricquilar^® has not been specifically studied in patients with renal impairment. The available data do not suggest a dosing regimen adjustment in these patients.

Interaction

Some medications may decrease the effectiveness of Triquilar.

These include drugs used to treat epilepsy (e.g., primidone, phenytoin, barbiturates, carbamazepine, oxcarbazepine, topiramate, felbamate), tuberculosis (e.g., rifampicin, rifabutin) and HIV infection (ritonavir); antibiotics to treat some other infectious diseases (e.g., ampicillin, tetracyclines, griseofulvin), and St. John’s wort-based medications (used primarily in the treatment of depression).

Sulfonamides, pyrazolone derivatives can increase the metabolism of steroid hormones included in the drug.

Special Instructions

If you miss taking Triquilar for more than 12 hours, take the next pill as soon as possible and use additional methods of contraception until the end of the cycle. The effectiveness of the drug decreases with the simultaneous use of drugs that activate the liver enzyme function, vomiting, diarrhea. The drug Triquilar should be withdrawn in case of prolonged immobilization and 6 weeks before planned surgical intervention.

Triquilar is not recommended for women over 35 years of age who smoke. For women under 18 and over 35-40 years of age, a three-phase, low-dose formulation is recommended.

The monophasic drugs are recommended for therapeutic and preventive purposes. The frequency and severity of side effects depend on the doses and ratios of the active ingredients in each drug.

Contraindications

• hepatitis, cholecystitis
• diabetes mellitus
• arterial hypertension
• anemia
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• chronic colitis
• tumors of the breast and genital organs
• intolerance of the drug.

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Side effects

Pain and tightness in the mammary glands, breast enlargement, mammary discharge; oozing and breakthrough uterine bleeding; headache; migraine; change in libido; decrease/change in mood; poor tolerance of contact lenses; visual disturbances; nausea; vomiting; abdominal pain; changes in vaginal secretion; skin rash; erythema nodosa; erythema multiforme; generalized pruritus; cholestatic jaundice; fluid retention; weight changes; allergic reactions.

Rarely – increased fatigue, diarrhea.

Sometimes chloasma may develop, especially in women with a history of pregnancy chloasma.

As with other combined oral contraceptives, thrombosis and thromboembolism may occur in rare cases.

Overdose

Symptoms that may occur in case of overdose: nausea, vomiting, bleeding from the genital tract.

In case of overdose, seek medical attention.