Pabal

General characteristics. Structure:

Active agent: карбетоцин 100 mkg (oksitotsinovy activity about 50 ME of oxytocin/ml) 

Excipients: sodium chloride of 9 mg, acetic acid ice to pH 3.8, water for and to 1 ml.

Pharmacological properties:

Karbetotsin (1-deamino-1-monokarba-[2-0 methyltyrosine] - oxytocin) is an agonist of oxytocin of long action.
Like oxytocin, карбетоцин selectively contacts oxytocin receptors in smooth muscles of a uterus, stimulates rhythmical reductions of a uterus, increases the frequency of the available pains and raises a tone of uterine muscles.
In a puerperal uterus карбетоцин increases the speed and force of spontaneous uterine reductions. After introduction of a karbetotsin of reduction of a uterus become frequent, and in two minutes there comes the sharp fight.
One dose of a karbetotsin of 100 mkg enough in order that remained adequate reductions of a uterus, the warning uterine atony and plentiful bleeding that it is possible to compare to the introduction of oxytocin operating within several hours.

Pharmacokinetics. Distribution. Cmax in plasma is reached within 15 min. after introduction and makes 1035±218 pg/ml within 60 min. Karbetotsin gets into breast milk, at this its Cmax is about 56 times lower, than in a blood plasma in 120 min.

Metabolism. By analogy with oxytocin, карбетоцин it is hydrolyzed by proteinases.

Removal. Removal of a karbetotsin has two-phase character with linear pharmacokinetics in the range of doses of 400-800 mkg. T1/2 makes about 40 min. The renal clearance of not changed form low, less than 1% of the entered dose is removed by kidneys in not changed look.

Indications to use:

— the prevention of an atony of a uterus after extraction of the child at operational delivery by operation of Cesarean section;
— the prevention of an atony of a uterus at women in labor with the increased risk of puerperal bleeding after the delivery in natural patrimonial ways.

Route of administration and doses:

Pabal is entered 1 time in/in or only the child, in oil after the birth. It is not necessary to use drug repeatedly. It is not necessary to mix Pabal with other drugs in one syringe. It is not necessary to use drug if in solution insoluble particles are observed or solution changed color.

Unused drug is liable to destruction.

During operation of Cesarean section one dose of drug Pabal (100 mkg/ml) is entered right after extraction of the child, it is desirable to department of a placenta.

At delivery in natural patrimonial ways 1 dose of drug Pabal (100 mkg/ml) is entered into an upper part of a hip at once after allocation of an afterbirth.

Features of use:

Pabal enter in oil or in/in only in specialized akusherskikh.otdeleniye, according to equipped and having the qualified and experienced medical staff in the state.

Drug use Pabal at any stage of childbirth till the birth of the child is forbidden as the promoting effect of a karbetotsin on a uterus after single introduction of 100 mkg/ml lasts several hours unlike bystry decrease in effect of oxytocin.

In case of ongoing uterine bleeding, after drug use Pabal, it is necessary to exclude such reasons as not separated fragments of a placenta and disturbance of coagulability of blood.

Pabal is entered only 1 time. In case of hypotonia or the atony of a uterus which are followed plentiful bleeding it is necessary to consider the possibility of use of oxytocin and/or ergometrine.

As Pabal possesses a certain antidiuretic action, it is necessary to reveal the first signs of development of a hyponatremia (drowsiness, apathy and a headache) for prevention of spasms and a coma.

Influence on ability to driving of motor transport and to control of mechanisms

It is not applicable, considering indications to use.

Side effects:

Character and frequency of development of side effects at use of a karbetotsin are comparable to side effects of oxytocin:

Type of system of an organism	Very often> 1/10	Often> 1/100 and <1/10
From hemopoietic and lymphatic system		Anemia
From a nervous system	Headache, tremor	Dizziness
From cardiovascular system	Increase in the ABP, hyperemia of the person
From a respiratory organs		Stethalgia, asthma
From the alimentary system	Nausea, abdominal pain	Metal smack in a mouth, vomiting
From integuments	Itch
From a musculoskeletal system		Dorsodynia

General reactions: a fever, pain in the place of an injection.

Interaction with other medicines:

Cases of medicinal interaction with analgetics, spasmolysants and means which are used for carrying out epidural or spinal anesthesia were not observed. However it is not necessary to mix Pabal in one syringe with other drugs.

As карбетоцин is oxytocin analog, the interaction cases characteristic of oxytocin can be observed. Sharp raising of the ABP at administration of drug Pabal in 3-4 h after preventive use of vasoconstrictors, in combination with caudal and conduction anesthesia is possible. Increase in the ABP and strengthening of effect of a karbetotsin at combined use of drug Pabal with ergot drugs is also possible (methylergometrine).

Pabal along with prostaglandins in connection with possible strengthening of action of a karbetotsin is not recommended to apply. If nevertheless their simultaneous use is necessary, then for the patient constant observation has to be conducted.

Means for inhalation anesthesia (a halothane, cyclopropane) can strengthen hypotensive effect and reduce drug influence Pabal on a uterus.

At simultaneous use of drug Pabal with oxytocin development of arrhythmia is possible.

Contraindications:

— the period of pregnancy and childbirth till the child's birth;
— abnormal liver function or kidneys;
— serious violations of cardiovascular system (disturbance of a rhythm and conductivity);
— epilepsy;
— for induction of childbirth;
— hypersensitivity to a karbetotsin, oxytocin or to one of drug components.

With care карбетоцин possesses a certain antidiuretic action. Therefore follows
to consider a possibility of development of a hyponatremia at drug use Pabal especially at the patients receiving large volumes in/in injections.
It is necessary to pay attention to the first signs of a hyponatremia (drowsiness, apathy, a headache) for prevention of spasms and a coma.
Pabal has to be applied with care at migraine, bronchial asthma and cardiovascular diseases, and also at any states at which bystry increase in volume, extracellular liquid can provoke the complications connected with an overhydratation. Pabal the doctor has to make the decision on drug use taking into account a ratio risk advantage in each case. Constant control of the ABP is necessary at patients with gestoses of the II half of pregnancy of heavy degree, an eclampsia and a preeclampsia.

Use at pregnancy and feeding by a breast
Drug use Pabal is contraindicated at pregnancy and childbirth until the child's birth.
A small amount of a karbetotsin can get into breast milk of mother and then collapse the newborn's enzymes.

Use at abnormal liver functions
It is contraindicated at an abnormal liver function.

Use at renal failures
It is contraindicated at a renal failure.

Overdose:

Symptoms: overdose cases at a single injection of the recommended dose of 100 mkg/ml are very rare. Administration of drug Pabal in a dose of 800 mkg/ml can cause tachycardia. Disturbance of the recommended mode of dosing can provoke a myometrium hyper tone regardless of existence or lack of hypersensitivity to a karbetotsin or puerperal bleeding. In hard cases drug overdose Pabal can, lead to a hyponatremia and an overhydratation, especially in combination with simultaneous large volume in the infusion of solutions which is carried out to delivery time.

Treatment: consists in a symptomatic and maintenance therapy. At emergence of signs, or overdose symptoms the woman in labor needs to provide adequate oxygenation. At water intoxication it is necessary to limit intake of liquid, to stimulate a diuresis, to carry out correction of electrolytic disturbances, and also to pay attention to clinical signs of a hyponatremia (drowsiness, apathy, a headache) for prevention of spasms and a coma.

Storage conditions:

To store in the place, unavailable to children, at a temperature of 2-8 °C.

Issue conditions:

Without recipe

Packaging:

Solution for in/in and in oil введ. 100 mkg/ml: amp. 5 pieces.