Pipolphen, solution 25mg/ml 2ml ampoules 10pcs

Composition

1 ml: – promethazine hydrochloride 25 mg

Auxiliary substances:

hydroquinone,

potassium disulfite,

sodium sulfite anhydrous,

sodium chloride,

water for d / I.

Pharmacological action

of the pharmaceutical group:

Histamine H1-receptor blocker. An anti-allergic drug.

Pharmaceutical action:  

Pipolphen is a histamine H1-receptor blocker, a phenothiazine derivative. It has a pronounced antihistamine activity and has a significant effect on the central nervous system (it has sedative, hypnotic, antiemetic, antipsychotic and hypothermic effects). Prevents and soothes hiccups.

Prevents histamine-mediated effects (including hives and pruritus). Anticholinergic action causes a drying effect on the mucous membranes of the nose and mouth.

The antiemetic effect of promethazine is due to its central anticholinergic effect, reduced excitability of the vestibular system, suppression of labyrinth function, and direct inhibitory effect on the trigger chemoreceptor zones of the medulla oblongata.

The sedative effect is caused by inhibition of histamine-K-methyltransferase and blockade of central histamine receptors. It is also possible to block other CNS receptors, such as serotonin and cholinergic receptors; stimulation of alpha-adrenergic receptors indirectly weakens the stimulation of the reticular formation of the brain stem. Since its chemical structure is different from that of other antipsychotic drugs from the phenothiazine group, promethazine has a weaker antipsychotic effect.

In therapeutic doses, it does not affect the cardiovascular system.

The clinical effect manifests itself 20 minutes after oral use (on average 15-60 minutes),2 minutes after intravenous use or 3-5 minutes after intravenous use and usually lasts for 4-6 hours (sometimes lasting up to 12 hours).

Indications

-allergic diseases (including urticaria, serum sickness, hay fever, allergic rhinitis, allergic conjunctivitis, angioedema, pruritus);- auxiliary therapy of anaphylactic reactions (after stopping acute manifestations by other means, for example, epinephrine/epinephrine/);— as a sedative in the pre-and postoperative period— – for the prevention or relief of nausea and vomiting associated with anesthesia and/or appearing in the postoperative period;- postoperative pain (in combination with analgesics);- kinetosis (to prevent and eliminate dizziness and nausea during transport trips);— as a component of lytic mixtures used for potentiation of anesthesia in surgical practice (for parenteral use).

Contraindications

-comatose states or other types of deep depression of the central nervous system; – simultaneous use of MAO inhibitors for 14 days after the end of their use— – angle-closure glaucoma— – alcohol intoxication, acute intoxication with sleeping pills, opioid analgesics— – sleep apnea syndrome— – episodic vomiting in children of unspecified origin;— pregnancy; – lactation period; – children under 2 months of age (for parenteral use);- children under 6 years of age (for oral use);- hypersensitivity to promethazine, other phenothiazine derivatives and any other component of Pipolphen. The drug should be used with caution in acute and chronic respiratory diseases (due to suppression of the cough reflex), open-angle glaucoma, bone marrow suppression, diseases of the cardiovascular system, liver and kidney disorders, peptic ulcer with pyloroduodenal obstruction, bladder neck stenosis and / or prostatic hypertrophy, predisposition to urinary retention, epilepsy, Reye’s syndrome, as well as in elderly patients.

Side effects

From the central nervous system: sedation, drowsiness, nightmares, increased nocturnal apnea, visual acuity disorders, anxiety, psychomotor agitation, dizziness, confusion, disorientation; after taking high doses – extrapyramidal disorders, increased convulsive activity (in children).

From the cardiovascular system: possible decrease in blood pressure, tachycardia, bradycardia.

From the digestive system: nausea, vomiting, constipation, dry mouth, nose, pharynx, anesthesia of the oral mucosa, cholestasis are possible.

From the hematopoietic system: rarely-thrombocytopenia and / or leukopenia, agranulocytosis.

Dermatological reactions: possible skin rash and / or photosensitization.

From the sensory organs: noise or ringing in the ears, paresis of accommodation, visual impairment.

Allergic reactions: urticaria, dermatitis, photosensitivity, bronchospasm.

Others: increased sweating, difficulty or painful urination.

Interaction

Pipolphen® enhances the effects of opioid analgesics, sleeping pills, anxiolytics (tranquilizers) and antipsychotics (neuroleptics), as well as drugs for general anesthesia, local anesthetics, m-holinoblockers and antihypertensive drugs (dose adjustment is required).

Pipolphen ® weakens the effect of amphetamine derivatives, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine.

Barbiturates accelerate elimination and reduce promethazine activity.

Beta-blockers increase (mutually) the concentration of promethazine in blood plasma.

Pipolphen ® weakens the effect of bromocriptine and increases the concentration of prolactin in the blood serum.

Tricyclic antidepressants and anticholinergic drugs enhance the m-holinoblocking activity of promethazine.

Ethanol, clonidine, and antiepileptic drugs enhance the depressing effect of promethazine on the central nervous system.

MAO inhibitors (concomitant use is not recommended) and phenothiazine derivatives increase the risk of hypotension and extrapyramidal disorders. Quinidine increases the likelihood of cardiodepressive effects of promethazine.

How to take, course of use and dosage

Assign inside, in / m and in/V.

The maximum daily dose for adults is 150 mg.

In / m, the drug is prescribed for adults at 25 mg 1 time/day, if necessary 12.5-25 mg every 4-6 hours. In the treatment of allergic diseases, Pipolphen® is prescribed orally at a dose of 25 mg 1 time/day. in the evening or 25 mg 2 times/day (morning and evening). The drug should be administered at the minimum effective dose.

For the prevention and treatment of nausea and vomiting, the drug is prescribed orally or in / m at a dose of 25 mg once. If necessary, you can prescribe 25 mg every 4-6 hours.

With kinetosis, Pipolphen® is prescribed orally at 25 mg 2 times/day, the first dose is 0.5 – 1 h before the trip, the subsequent one is 8-12 hours later. As a sedative in surgery, on the eve of surgery, it is prescribed orally or in / m at a dose of 25-50 mg once a night. For preoperative preparation,50 mg of Pipolphen is administered intravenously 2.5 hours before surgery as part of lytic mixtures, and if necessary, the use can be repeated after 1 hour.

For the induction of anesthesia and analgesia in certain diagnostic and surgical procedures, such as repeated bronchoscopy, ophthalmic surgery, Pipolphen® can be administered intravenously in doses of 0.15-0.3 mg/kg of body weight.

For children over 2 months of age, the drug can be administered intravenously 3-5 times a day. in a dose of 0.5-1 mg / kg of body weight. In severe cases, the single dose for intravenous use can be increased to 1-2 mg/kg of body weight.

Children aged 6 to 14 years are prescribed inside 25 mg (1 tablet) 3-4 times a day. Pipolphen pills are not recommended to be divided, so the use of this dosage form for children under 6 years of age is not indicated.

Overdose

Symptoms: in children – agitation, anxiety, hallucinations, convulsions, mydriasis and immobility of the pupils, hyperemia of the facial skin, hyperthermia; in adults-psychomotor agitation, convulsions, lethargy. In acute overdose – a marked decrease in blood pressure, vascular collapse, respiratory depression, coma.

Treatment: due to the lack of antidotes, symptomatic and supportive therapy is performed. Gastric lavage, use of activated charcoal inside (during detoxification in the early stages after ingestion); according to indications-antiepileptic drugs. Dialysis is ineffective. Ingestion of sodium or magnesium sulfate may have a beneficial effect.

Measures should be taken to restore adequate pulmonary ventilation by ensuring airway patency and providing assisted or artificial ventilation. Correction of acidosis and/or electrolyte balance is necessary. In case of severe hypotension, norepinephrine (norepinephrine) or mezaton should be administered. Epinephrine (epinephrine) can paradoxically increase arterial hypotension.

Special instructions

With prolonged use of the drug, it is necessary to systematically monitor the peripheral blood formula and liver function.

With extreme caution, especially in high doses, Pipolphen® should be prescribed to elderly patients, since this category of patients has an increased risk of side effects.

When used concomitantly with Pipolphen, analgesics and sleeping pills should be prescribed in smaller doses. Pipolphen® should be used under strict medical supervision simultaneously with opioid analgesics, sedatives and hypnotics, anesthetics, tricyclic antidepressants and tranquilizers.

Pipolphen® may mask the ototoxic effects (tinnitus and dizziness) of co-administered medications.

Pipolphen ® reduces the threshold of convulsive readiness.This should be taken into account when prescribing the drug to patients who are prone to developing seizures, or simultaneously with other drugs with a similar effect.

As an antiemetic, Pipolphen should only be used for prolonged vomiting of known etiology. With prolonged use, the risk of developing dental diseases (caries, periodontitis, candidiasis) increases due to a decrease in salivation.

Alcohol consumption is prohibited during the treatment period.

During the period of taking Pipolphen, a diagnostic pregnancy test may give a false positive result. A possible increase in blood glucose levels in patients taking Pipolphen® should be considered when performing a glucose tolerance test.

To prevent distortion of the results of skin scarification tests for allergens, the drug should be discontinued 72 hours before the allergological tests.

Each tablet contains 95 mg of lactose, which should be taken into account if you are lactose intolerant.

Use in pediatrics Caution should be exercised when prescribing Pipolphen® to children, as this makes it difficult to diagnose the underlying disease. Symptoms of undiagnosed encephalopathy and Reye’s syndrome can be mistaken for side effects of Pipolphen.

Influence on the ability to drive motor vehicles and control mechanisms During the initial period of Pipolphen use, it is necessary to refrain from driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, the degree of restrictions is determined depending on the individual tolerance of the patient.

Form of production

Pipolphen solution for intravenous and intramuscular use is clear, colorless or with a green tint, odorless or almost odorless.

Storage conditions

List B. The drug should be stored in a place protected from light, out of the reach of children at a temperature of 15° to 25°C.

Shelf

life is 5 years.

Active ingredient

Promethazine

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For children over 2 months of age, For adults as prescribed by a doctor, For children as prescribed by a doctor

Indications

Allergy, Hay Fever