Pipolzine (Solution) Instructions for Use

Marketing Authorization Holder

Bryntsalov-A, JSC (Russia)

ATC Code

R06AD02 (Promethazine)

Active Substance

Promethazine (Rec.INN registered by WHO)

Dosage Form

Pipolzine

Solution for intravenous and intramuscular administration 2.5% (50 mg/2 ml): amp. 10 pcs.

Dosage Form, Packaging, and Composition

2 ml – ampoules (5) – contour cell packs (2) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Histamine H₁-receptor blocker, possesses high antihistamine activity and a pronounced blocking effect on the CNS. It causes a sedative effect and has an antiemetic action. It also exerts a pronounced adrenergic blocking effect and a moderate peripheral and central anticholinergic action. The effect begins to develop 20 minutes after administration and lasts for 6 hours, sometimes up to 12 hours.

Pharmacokinetics

After oral administration, it is rapidly and well absorbed from the gastrointestinal tract.

Plasma protein binding is more than 90%. It penetrates the blood-brain barrier and the placental barrier.

It is metabolized in the liver, forming mainly sulfoxides and N-demethylated derivatives of promethazine.

After oral administration, the T_1/2 is 7-12 hours. It is excreted mainly by the kidneys; to a lesser extent, through the intestines.

Indications

Allergic diseases and reactions: rash, itching, eczema, drug rash, serum sickness, angioedema, hay fever, anaphylactic shock, bronchospastic syndrome (as part of complex therapy).

Skin diseases (including eczema, neurodermatitis, diathesis, contact dermatitis, and toxicoderma).

In anesthesiology: as a sedative before and after surgical interventions, as an adjunct to analgesics; for the prevention and treatment of nausea and vomiting during anesthesia and surgery; for artificial hibernation.

As part of combination therapy or as an adjunct: motion sickness, migraine, sleep disorders, states of agitation; gastric and duodenal ulcer.

In pediatrics: skin and mucous membrane changes in infants against the background of exudative diathesis, eczema, asthmatic bronchitis, false croup, various types of allergic dermatoses, serum sickness.

ICD codes

Dosage Regimen

When taken orally, the daily dose for adults is 75-100 mg.

Maximum doses for oral administration: single – 75 mg, daily – 500 mg; for intramuscular administration: single – 50 mg, daily – 250 mg.

Intravenous administration is used as part of lytic mixtures.

For children aged 1 to 2 years, orally – 5-10 mg 1-2 times/day; from 2 to 5 years – 5-10 mg 1-3 times/day; from 5 to 10 years – 5-15 mg 1-3 times/day; over 10 years and adolescents 5-20 mg 1-3 times/day. For intramuscular administration, the dose is 0.5-1 mg/kg, frequency of administration – 3-5 times/day. In emergency cases (status asthmaticus, false croup), the dose can be increased to 1-2 mg/kg. For intravenous administration (usually as part of a lytic cocktail), the dose is 1/3 of the dose for intramuscular administration.

Adverse Reactions

From the digestive system: moderately pronounced numbness of the oral mucosa, dry mouth, nausea, constipation, diarrhea, discomfort; rarely – jaundice.

From the CNS and peripheral nervous system: drowsiness, dizziness, anxiety, lethargy, fatigue, impaired coordination of movements, blurred vision; rarely – tinnitus, euphoria, nervousness, insomnia, convulsions, oculogyric crisis, catatonic state, hysteria, psychomotor agitation, extrapyramidal disorders, headache, nystagmus.

From the cardiovascular system: rarely – tachycardia, bradycardia, palpitation, fainting, arterial hypotension (with intravenous administration), arrhythmias.

Dermatological reactions: rarely – contact dermatitis, photosensitivity, urticaria.

From the hematopoietic system: rarely – leukopenia, agranulocytosis, aplastic anemia, thrombocytopenic purpura.

Allergic reactions: rarely – exanthema, urticaria, angioedema, anaphylactic reactions.

Other: rarely – irregular breathing, urinary retention.

Local reactions: with intramuscular administration, painful infiltrates may occur.

Contraindications

Simultaneous use of MAO inhibitors, coma (including due to alcohol intoxication), severe liver dysfunction, first trimester of pregnancy, lactation (breastfeeding), early childhood under 2 months, hypersensitivity to promethazine or other phenothiazine derivatives.

Use in Pregnancy and Lactation

Promethazine is contraindicated for use in the first trimester of pregnancy. If therapy is necessary for clinical indications in the third trimester of pregnancy, Promethazine is used in minimal maintenance doses, reducing them towards the end of the term to prevent the development of drowsiness or psychomotor agitation in newborns.

If it is necessary to use promethazine during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction.

Pediatric Use

Contraindicated in early childhood under 2 months.

Use with caution in children with acute or chronic respiratory diseases, since Promethazine suppresses the cough reflex.

Not recommended for use in children to relieve occasional vomiting of unspecified origin.

Special Precautions

Use with caution in acute or chronic respiratory diseases, since Promethazine suppresses the cough reflex.

The use of promethazine in combination with opioid analgesics and tranquilizers for comprehensive preoperative preparation of patients is possible only under strict medical supervision.

During long-term treatment, systematic complete blood count and monitoring of liver function parameters are recommended.

During treatment, alcohol consumption is not allowed.

Use with caution in children with acute or chronic respiratory diseases, since Promethazine suppresses the cough reflex.

Not recommended for use in children to relieve occasional vomiting of unspecified origin.

Effect on ability to drive vehicles and operate machinery

During the initial, individually determined period of promethazine use, driving vehicles and engaging in other potentially hazardous activities requiring speed of psychomotor reactions are not permitted. During further treatment, the degree of restrictions is determined depending on individual tolerance to promethazine.

Drug Interactions

With simultaneous use, Promethazine potentiates the action of opioid analgesics, hypnotics, and local anesthetics.

With simultaneous use of promethazine with tricyclic antidepressants, an enhancement of the anticholinergic effect, as well as the depressant effect on the CNS, is possible; with antihypertensive drugs – an enhancement of the effect of the latter is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.