Pipolfen, 25 mg/ml 2 ml 10 pcs

Pharmgroup:

Histamine H1-receptor blocker. Antiallergic drug.

Pharm Action:

Pipolphen is a blocker of histamine H1-receptors, a phenothiazine derivative. It has pronounced antihistamine activity and has a significant effect on the CNS (has sedative, hypnotic, antiemetic, antipsychotic and hypothermic effects). It prevents and calms hiccups.

Prevent histamine-mediated effects (including urticaria and itching). 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, decrease in excitability of the vestibular system, suppression of labyrinth function and direct inhibitory effect on trigger chemoreceptor areas of the medulla oblongata.

The sedative effect is due to inhibition of histamine-K-methyltransferase and blockade of central histamine receptors. Blockade of other CNS receptors such as serotonin and choline receptors is also possible; stimulation of α-adrenoreceptors indirectly attenuates brainstem reticular formation stimulation. Because its chemical structure is different from that of other phenothiazine antipsychotics, promethazine has a weaker antipsychotic effect.

In therapeutic doses, it has no effect on the cardiovascular system.

The clinical effects appear 20 min after ingestion (15-60 min on average), 2 min after IUI or 3-5 min after IUI and usually last for 4-6 h (sometimes persisting up to 12 h).

Indications

Active ingredient

Composition

How to take, the dosage

Prescribe orally, v/m and intravenously.

The maximum daily dose for adults is 150 mg.

In/m the preparation is indicated in adults in dose 25 mg once daily, if necessary 12.5-25 mg every 4-6 hours.
In treatment of allergic diseases Pipolfen® is indicated orally in dose 25 mg once daily in the evening or in dose 25 mg twice daily (morning and evening). (in the morning and in the evening). The drug should be prescribed in the minimum effective dose.

To prevent and treat nausea and vomiting, the drug is administered orally or IM in a dose of 25 mg once. If necessary, 25 mg every 4-6 hours may be prescribed.

In kinetosis Pipolphen® is prescribed orally in 25 mg 2 times per day, the first dose 0.5-1 hours before the trip, the subsequent dose 8-12 hours later.
As a sedative in surgery on the eve of surgery it is prescribed orally or in m/m in a dose of 25-50 mg once at night. For preoperative preparation 2.5 hours before surgery 50 mg of Pipolfen is administered as part of lytic mixtures in an intravenous mode; if necessary after 1 hour the administration can be repeated.

In order to induce anesthesia and analgesia during certain diagnostic and surgical interventions such as repeated bronchoscopy, ophthalmic surgery, Pipolfen® may be administered in an IV dose of 0.15-0.3 mg/kg body weight.

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

Children from 6 to 14 years of age are indicated by oral administration of 25 mg (1 tablet) 3-4 times daily. It is not recommended to divide Pipolfen tablets; therefore this dosage form is not indicated for children under 6 years of age.

Interaction

Pipolpfen® enhances the effects of opioid analgesics, hypnotics, anxiolytics (tranquilizers) and antipsychotics (neuroleptics), as well as medicines for general anesthesia, local anesthetics, m-cholinoblockers and hypotensive drugs (dose adjustment is required).

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

Barbiturates accelerate elimination and decrease promethazine activity.

Beta-adrenoblockers increase (reciprocally) the plasma concentration of promethazine.

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

Tricyclic antidepressants and anticholinergic drugs increase the m-cholin-blocking activity of promethazine.

Ethanol, clopheline, antiepileptic drugs increase the CNS depressant effect of promethazine.

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

Special Instructions

In long-term use of the drug peripheral blood count and liver function should be systematically monitored.

Pipolphen® should be used with special caution, especially in high doses, in elderly patients, because this category of patients has an increased risk of side effects.

In concomitant use with Pipolfen, analgesics and hypnotics should be prescribed in lower doses.
Pipolfen® should be used under close 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 drugs.

Pipolphen® lowers the seizure threshold. This should be considered when prescribing the drug in patients who are prone to seizures or concomitantly with other medicinal products with similar effects.

Pipolphen® should be used only in case of prolonged vomiting of known etiology.
With long-term use the risk of dental diseases (caries, periodontitis, candidiasis) may increase due to reduction of salivary flow.

The use of alcohol is prohibited during treatment.

The diagnostic test for pregnancy may give false positive results while taking Pipolfen.
Possible increase in blood glucose levels in patients who have taken Pipolfen® should be considered when performing a glucose tolerance test.

In order to prevent distortion of the results of skin allergen scarification tests the drug must be discontinued 72 hours before allergy tests.

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

Pediatric use
Caution should be exercised when prescribing Pipolphen® in children because it makes it difficult to diagnose the underlying disease. Symptoms of undiagnosed encephalopathy and Reye syndrome may be mistaken for side effects of Pipolfen.

Influence on driving and operating machinery

In the initial period of Pipolphen use it is necessary to refrain from driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions. Thereafter, the degree of restriction is determined depending on the individual tolerance of the patient.

Contraindications

Side effects

CNS disorders: sedation, somnolence, nightmares, increased nighttime apnea, visual disturbances, anxiety, psychomotor agitation, dizziness, confusion, disorientation; after high doses – extrapyramidal disorders, increased seizure activity (in children).

Cardiovascular system disorders: decreased BP, tachycardia, bradycardia may occur.

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

Hematopoietic system: rarely – thrombocytopenia and/or leukopenia, agranulocytosis.

Dermatological reactions: skin rash and/or photosensitization are possible.

Sensory organs: tinnitus or ringing in the ears, accommodation paresis, visual impairment.

Allergic reactions: urticaria, dermatitis, photosensitization, bronchospasm.

Others: increased sweating, difficulty or painful urination.

Overdose

Symptoms: in children – agitation, anxiety, hallucinations, seizures, mydriasis and fixed pupils, facial hyperemia, hyperthermia; in adults – psychomotor agitation, seizures, lethargy. In acute overdose – marked BP decrease, vascular collapse, respiratory depression, coma.

Treatment: in connection with the absence of antidotes, symptomatic and supportive therapy is carried out. Gastric lavage, oral administration of activated charcoal (if detoxification is carried out early after ingestion); antiepileptic drugs if indicated. Dialysis is ineffective. Oral administration of sodium or magnesium sulfate may have a beneficial effect.

Make measures to restore adequate pulmonary ventilation by ensuring airway patency and assisted or artificial ventilation. Correction of acidosis and/or electrolyte balance is necessary. Norepinephrine (noradrenaline) or mesaton should be administered in severe arterial hypotension. Epinephrine (adrenaline) may paradoxically increase arterial hypotension.

Pregnancy use