Ginipral

Ginipral is a medicine used mainly to prevent or stop preterm labor. It has a tocolytic action, i.e. It relaxes the uterine muscles, reducing the frequency and intensity of contractions, which helps to delay labor until a safer time.

The active ingredient in Ginipral is hexoprenaline, which is categorized as a beta-adrenomimetic. Hexoprenaline acts on the uterine musculature to reduce its tone and prevent contractions, which is used to manage preterm labor, as well as in some other situations that require relaxation of the uterine musculature, such as before a cesarean section or when it is necessary to turn the fetus in the womb.

The drug is contraindicated in hypersensitivity to its components, thyrotoxicosis, cardiovascular diseases, severe liver and kidney diseases, closed-angle glaucoma, premature placental abruption, uterine bleeding, intrauterine infections, as well as in the first trimester of pregnancy and during lactation.

Among the side effects of Ginipral may occur tachycardia, hypokalemia, hyperglycemia, tremor, headache, dizziness and other manifestations associated with the action on the cardiovascular system and metabolic changes in the body.

It is important to take Ginipral only as prescribed and under the supervision of a doctor, taking into account possible risks and side effects.

Indications Ginipral

Ginipral is used in obstetric practice to eliminate and prevent preterm labor. The action of ginipral is aimed at relaxation of smooth muscles, including myometrium (muscle layer of the uterus), due to which a decrease in uterine tone and suppression of its contractile activity is achieved. This helps to delay the onset of labor, which is important in cases of threatened preterm labor to prevent possible complications in a premature baby.

The use of Ginipral may be indicated in the following cases:

1. Threat of preterm labor.
2. The need to delay labor for medical reasons, such as cervical insufficiency or for emergency medical manipulations during pregnancy.
3. Uterine hypertonicity, causing pain or other unfavorable symptoms.

Release form

Ginipral is available in the form of a solution for intravenous administration. The composition of one ampoule (2 ml of solution) includes hexoprenaline sulfate in the amount of 0.01 mg, as well as additional substances such as sodium pyrosulfite, edetate dihydrate, sodium chloride, sulfuric acid for pH optimization and water for injection. The drug is a clear colorless solution packed in contoured cell packs of 5 ampoules of colorless glass with a break point; the carton pack may contain 1 or 5 packs.

Pharmacodynamics

Ginipral is a selective β2-adrenomimetic, the action of which is aimed at stimulation of β2-adrenergic receptors. Its use in obstetric practice is due to its ability to relax smooth muscle, including uterine muscle, which provides its tocolytic (antinociceptive) effect.

Mechanism of Action:

1. Stimulation of β2-adrenergic receptors. Ginipral binds to β2-adrenergic receptors in uterine smooth muscle cells, activating them. This leads to activation of adenylate cyclase, an enzyme that catalyzes the conversion of ATP (adenosine triphosphate) to cAMP (cyclic adenosine monophosphate).
2. Increase in the level of cAMP. An increase in the concentration of cAMP leads to activation of protein kinase A, which phosphorylates certain proteins and leads to a decrease in the intracellular level of calcium ions.
3. Decreased calcium levels in cells. Calcium plays a key role in the contraction of smooth muscles, including the uterus. A decrease in its concentration in the cells causes smooth muscle fibers to relax.
4. Tocolytic effect. The result is relaxation of the myometrium (the muscular layer of the uterus), which leads to a decrease in tone and suppression of uterine contractile activity. This helps prevent or delay preterm labor, providing additional time for fetal development in cases of threatened preterm labor.

Pharmacokinetics

Although the exact details of Ginipral pharmacokinetics may vary depending on various factors, including route of administration and individual patient characteristics, the following are general aspects of its pharmacokinetics:

1. Absorption: Ginipral is usually administered orally as tablets. After administration, it is usually well absorbed from the gastrointestinal tract.
2. Metabolism: Ginipral is metabolized in the liver to form active metabolites. The main route of metabolism is hydroxylation in the liver to form the active metabolite terbutaline sulfate.
3. Excretion: Metabolites are excreted mainly through the kidneys.
4. Half-life: The half-life of terbutaline sulfate may be about 3-4 hours, but this may vary depending on individual patient characteristics.
5. Duration of action: The effect of Ginipral can last for several hours, which helps to reduce the contractile activity of the uterus and prevent premature contractions.

Dosing and administration

The route of administration and dosage may vary depending on the individual patient, the severity of the condition and clinical indications. Nevertheless, the following are general recommendations for the use of Ginipral to manage the threat of preterm labor. It is important to remember that specific doses and treatment regimen should be prescribed only by the attending physician.

Oral administration:

• Thestarting dose is usually 1 tablet (0.5 mg hexoprenaline) 3 times daily.
• Depending on clinical response and tolerability, the dose may be gradually increased to a maximum daily dose of 4 tablets (2 mg).

Intravenous administration:

• Ginipral may also be administered intravenously, especially in situations requiring an immediate tocolytic effect.
• Thestarting dose for intravenous administration is usually 1-2 mcg per minute.
• The dose may be gradually increased at 10-20 minute intervals until the desired effect is achieved, but no more than 4 mcg per minute.

Important Notes:

• When taking orally, the tablet should be swallowed whole, without chewing, drinking enough liquid.
• Intravenous administration should be carried out only in hospital settings under continuous monitoring of heart rate and blood pressure.
• The dosage and duration of treatment is determined by the physician based on an assessment of the patient's condition and response to treatment.

Use Ginipral during pregnancy

Hexoprenaline is a synthetic adrenomimetic that is sometimes used to reduce preterm labor in cases of preterm labor. However, its use during pregnancy requires extreme caution and strict medical supervision.

In some cases, when preterm labor poses a serious risk to the health of the mother and/or baby, the doctor may decide to prescribe hexoprenaline to reduce contractions and delay labor. However, this decision should be made after careful discussion of the benefits and risks with the patient.

The use of hexoprenaline during pregnancy may be associated with some risks and side effects for both mother and fetus. Possible side effects include rapid heartbeat, increased blood pressure, anxiety, dizziness, and others. In addition, hexoprenaline can cause fetal contractions, which can also have negative effects.

Contraindications

1. Hypersensitivity to the drug: Any known or suspected hypersensitivity to terbutaline or any of the drug components is a contraindication.
2. Tachyarrhythmias: Ginipral is contraindicated in the presence of tachyarrhythmias such as atrial fibrillation or paroxysmal tachycardia.
3. Thyrotoxicosis: In the presence of thyrotoxicosis (increased thyroid function), Ginipral should be used with caution or avoided altogether.
4. Gestosis: Ginipral is contraindicated in the presence of gestosis (severe pre-eclampsia and eclampsia).
5. Glaucoma: Ginipral should be used with caution in glaucoma because the drug may increase intraocular pressure.
6. Heart failure: In the presence of heart failure, the use of Ginipral also requires caution and monitoring.
7. Hypokalemia: An increased risk of hypokalemia (low blood potassium levels) is an additional factor to consider when using Ginipral.
8. Severe lung disease: In the presence of severe lung disease, such as bronchial asthma or chronic obstructive pulmonary disease (COPD), Ginipral may be contraindicated because of its possible effects on the bronchial system.

Side effects Ginipral

• Endocrine system: Rarely may cause lipolysis.
• Metabolic disorders: Hypokalemia is frequently observed. Rarely, hyperglycemia may occur, especially in patients with diabetes mellitus.
• Nervous system: Tremor is very common. Headache, dizziness, and anxiety may also occur, although the frequency of these effects has not been established.
• Cardiovascular system: Tachycardia is very common. Palpitations, decreased diastolic pressure, arterial hypotension may occur frequently.

Overdose

An overdose of Ginipral can lead to serious undesirable effects, including an increase in its adrenergic effects. Symptoms of overdose may include palpitations (tachycardia), arterial hypertension, heart rhythm disturbances, shaking, dizziness, headache, hyperglycemia, hypokalemia and others. In case of overdose, immediate medical attention should be sought.

Interactions with other drugs

1. Antihypertensive drugs (drugs that lower blood pressure): Ginipral may increase the hypotensive effect of these drugs, which can lead to dangerously low blood pressure.
2. Antidepressants and other drugs that increase serotonin levels in the body: When combined with Ginipral, they can increase serotoninergic activity, which can lead to serious side effects known as serotonin excess syndrome.
3. Drugs that increase arrhythmias or cause tachycardia: Ginipral may increase these effects, which can lead to cardiac arrhythmias or palpitations.
4. Monoamine oxidase inhibitors (MAOIs): Co-administration of MAOIs with Ginipral may result in significant increases in blood pressure, tachycardia, and other serious side effects.
5. Drugs that increase hypokalemia (low blood potassium levels): Ginipral may increase the loss of potassium in the urine, so its use in combination with other potassium-losing drugs may increase this effect.

Storage conditions

The storage conditions for Ginipral are usually specified in the instructions for use provided by the manufacturer. In general, here are typical recommendations for storage conditions:

1. Temperature: The drug should be stored at room temperature, usually between 15°C and 30°C.
2. Humidity: It is recommended to store the drug in a place where there is no high humidity to prevent damage to the tablets.
3. Light: Store Ginipral in the original package or in a dark container to prevent exposure to direct sunlight.
4. Children's access: It is important to keep the drug out of the reach of children to avoid accidental use.
5. Packaging conditions: Ensure that the product container is tightly closed to prevent foreign matter and moisture.
6. Do not freeze: Avoid freezing the preparation.