Pipolfen - Instructions For Use, Tablets, Ampoules, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Pipolfen

Pipolfen: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Terms of dispensing from pharmacies
19. 19. Reviews
20. 20. Price in pharmacies

Latin name: Pipolphen

ATX code: R06AD02

Active ingredient: promethazine (Promethazine)

Producer: EGIS CJSC Pharmaceutical Plant (EGIS Pharmaceuticals, Plc) (Hungary)

Description and photo update: 02.10.2019

Prices in pharmacies: from 899 rubles.

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Pipolfen is a drug with antihistamine, antiallergic, hypnotic, sedative and antiemetic effects.

Release form and composition

Dosage forms of Pipolfen release:

• Dragee (coated tablets): light blue, with a shiny surface, lenticular shape, almost odorless or odorless (20 pieces in blisters, 1 blister in a cardboard box or 25 blisters in a cardboard box);
• Solution for intravenous and intramuscular administration: with a green tint or colorless, transparent, almost odorless or odorless (2 ml each in colorless glass ampoules with a blue code ring and a break point, 5 ampoules in blister strip packaging, 2 packages in a cardboard box).

Each pack also contains instructions for the use of Pipolfen.

The composition of 1 tablet contains:

• Active ingredient: promethazine hydrochloride - 25 mg;
• Auxiliary components: potato starch, stearic acid, gelatin, magnesium stearate, talc, lactose monohydrate;
• Cover: sucrose, ariavit blue, glycerol, talc, gelatin, macrogol 35,000, titanium dioxide.

The composition of 1 ml of injection solution includes:

• Active ingredient: promethazine hydrochloride - 25 mg;
• Auxiliary components: potassium disulfite - 0.75 mg, hydroquinone - 0.2 mg, sodium chloride - 7 mg, anhydrous sodium sulfite - 1 mg, water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

The active component of Pipolfen is promethazine, a phenothiazine derivative. A substance with a high antihistamine activity, which has a pronounced effect on the central nervous system (central nervous system), with a sedative, hypnotic, antiemetic, antipsychotic, hypothermic, preventive / calming effect.

Promethazine helps to prevent histamine reactions (such as hives, itching, etc.), but does not eliminate them. Due to the anticholinergic action, the effect of drying the mucous membranes of the nasal and oral cavities is ensured.

The antiemetic (antiemetic) effect of promethazine is due to its central anticholinergic effect, inhibition of the excitability of the vestibular apparatus and the function of the labyrinth, as well as direct inhibition of the trigger chemoreceptor zones of the medulla oblongata.

The sedative (sedative) effect is based on the inhibition of histamine-N-methyltransferase and blockade of central histaminergic receptors. Blockade of other CNS receptors - serotonin and acetylcholine; stimulation of α-adrenergic receptors indirectly reduces the stimulation of the reticular formation of the brainstem. Due to the fact that the chemical structure of promethazine differs from the structure of antipsychotic phenothiazines, it has a weaker antipsychotic effect.

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

The duration of the clinical action of promethazine is usually 4-6 hours, in some cases it lasts up to 12 hours.

The onset of action of Pipolfen, depending on the method of its administration:

• Oral administration (pills / tablets): after 20 minutes (average 15-60 minutes);
• Parenteral administration (solution): intramuscularly - after 2 minutes; intravenously - 3-5 min.

Pharmacokinetics

After taking pills / tablets Pipolfen inside from the gastrointestinal tract, promethazine is well absorbed. Protein binding ~ 90%.

Promethazine actively undergoes presystemic elimination (the effect of the first passage through the liver), mainly through S-oxidation, with the formation of promethazine sulfoxides and N-demethyl promethazine, the main metabolites excreted in the urine.

The half-life (T _1/2) of the main compound is from 7 to 15 hours. It is excreted mainly by the kidneys, to a lesser extent - with bile.

Promethazine crosses the blood-brain and placental barriers.

Indications for use

• Anaphylactic reactions (as additional therapy after relief of acute manifestations with other drugs, for example, adrenaline);
• Allergic diseases, including urticaria, angioedema, serum sickness, hay fever, allergic rhinitis and conjunctivitis, pruritus;
• Pre- and postoperative period (as a sedative);
• Kinetosis (to eliminate and prevent nausea and dizziness while traveling by transport);
• Postoperative pain (along with pain medications);
• Nausea and vomiting, which is associated with anesthesia and / or appears in the postoperative period (to stop or prevent development).

Injection solution in surgical practice is also prescribed as a component of lytic mixtures, which are used to potentiate anesthesia.

Contraindications

Absolute:

• Coma or other types of deep depression of the central nervous system;
• Sleep apnea;
• Alcohol intoxication, acute intoxication with opioid analgesics and / or hypnotics;
• Closed-angle glaucoma;
• Occasional vomiting of unspecified genesis in children;
• Simultaneous use with monoamine oxidase inhibitors, as well as a period of 2 weeks after the end of their use;
• Pregnancy and lactation;
• Children under 2 months of age (injection solution) or 6 years (dragee);
• Hypersensitivity to promethazine, other phenothiazine derivatives, and other components of the drug.

Relative (Pipolfen is prescribed with caution in the presence of the following diseases / conditions):

• Peptic ulcer with pyloroduodenal obstruction;
• Acute and chronic respiratory diseases (due to suppression of the cough reflex);
• Depression of bone marrow function;
• Open-angle glaucoma;
• Diseases of the cardiovascular system;
• Predisposition to urinary retention;
• Functional disorders of the kidneys and liver;
• Bladder neck stenosis and / or prostatic hypertrophy;
• Reye's syndrome;
• Epilepsy;
• Advanced age (due to the high risk of adverse reactions).

Pipolfen, instructions for use: method and dosage

Dragee / Pipolfen tablets are used orally, the solution is administered intramuscularly and intravenously.

The maximum adult daily dose is 150 mg.

Intramuscularly Pipolfen in ampoules is prescribed for adults at 25 mg 1 time per day, if necessary, it is possible to introduce 12.5-25 mg solution every 4-6 hours.

Recommended dosage regimen:

• Allergic diseases: inside, 25 mg 1 (evening) or 2 (morning and evening) times a day (recommended - in the lowest effective dose);
• Nausea and vomiting (treatment and prevention): a single dose of 25 mg orally or intramuscularly. If necessary, it is possible to reapply Pipolfen every 4-6 hours;
• Kinetosis: inside, 2 times a day, 25 mg (the first dose - 30-60 minutes before the trip, the next - after 8-12 hours);
• Surgical operations (as a sedative): once at night, 25-50 mg (orally or intramuscularly) on the eve of the operation. As part of lytic mixtures for preoperative preparation, 50 mg of Pipolfen is injected intramuscularly 2.5 hours before the operation, the same dose can be re-administered after 60 minutes;
• Diagnostic and surgical interventions, including ophthalmic operations, repeated bronchoscopy (for induction of anesthesia and analgesia): intravenously at 0.15-0.3 mg / kg.

For children from 2 months old, Pipolfen can be administered 3-5 times a day intramuscularly at 0.5-1 mg / kg. In severe cases, a single dose may be increased to 1-2 mg / kg.

Children 6-14 years old Pipolfen is prescribed orally 3-4 times a day, 25 mg. It is not recommended to share dragees, therefore, Pipolfen in this dosage form is not prescribed for younger children.

Side effects

• Digestive system: cholestasis, nausea, anesthesia of the oral mucosa, constipation, vomiting, dry mouth, pharynx, nose;
• Central nervous system: drowsiness, sedation, disorientation, impaired visual acuity, nightmares, increased sleep apnea, anxiety, agitation, confusion, dizziness; the use of high doses - increased seizure activity (in children), extrapyramidal disorders;
• Hematopoietic system: rarely - agranulocytosis, leukopenia and / or thrombocytopenia;
• Cardiovascular system: bradycardia, decreased blood pressure, tachycardia;
• Sense organs: paresis of accommodation, ringing or noise in the ears, visual impairment;
• Dermatological reactions: photosensitivity and / or skin rash;
• Allergic reactions: bronchospasm, dermatitis, urticaria, photosensitivity;
• Others: painful or difficult urination, increased sweating.

Overdose

Symptoms of a promethazine overdose depend on the age of the patient. In children, it is manifested by agitation, anxiety, hallucinations, convulsions, mydriasis and immobility of the pupils, hyperemia of the skin of the face, hyperthermia; in adults - psychomotor agitation, convulsions, lethargy. In acute overdose, there is a pronounced decrease in blood pressure, respiratory depression, vascular collapse, coma.

Since the antidote to promethazine is unknown, symptomatic and supportive treatment is recommended. In case of an overdose of oral forms of the drug, detoxification in the early stages includes gastric lavage and the intake of activated carbon. Further, according to indications, it is possible to use antiepileptic drugs. Oral sodium / magnesium sulfate may be beneficial. Dialysis is ineffective.

It may be necessary to carry out measures to restore adequate pulmonary ventilation with the provision of airway patency and the provision of auxiliary or mechanical ventilation. Correction of acidosis / electrolyte balance is required. Severe hypotension is relieved by parenteral administration of norepinephrine (norepinephrine) or Mezaton. It should be borne in mind that the introduction of adrenaline (epinephrine) can paradoxically aggravate arterial hypotension.

special instructions

Pipolfen can mask the ototoxic effect (in the form of tinnitus and dizziness) of co-administered drugs.

With prolonged therapy, it is necessary to systematically monitor the functional state of the liver and the peripheral blood count.

Pipolfen can lower the seizure threshold, which should be taken into account when prescribing it to patients prone to the development of seizures, or in conjunction with other drugs with a similar effect.

As an antiemetic, Pipolfen should be used only with prolonged vomiting of a known etiology.

With a long course, due to a decrease in salivation, the likelihood of developing dental diseases (periodontitis, caries, candidiasis) increases.

During therapy, alcohol is prohibited.

It is possible to get a false positive result when performing a diagnostic pregnancy test. You also need to consider the possible increase in blood glucose levels when performing a glucose tolerance test.

To prevent distortion of the results of skin scarification tests for allergens, Pipolfen should be canceled 72 hours before the allergy tests.

In case of lactose intolerance, it must be borne in mind that the composition of the dragee contains lactose.

Pipolfen should be used with caution in children, since it can complicate the diagnosis of the underlying disease (symptoms of Reye's syndrome and undiagnosed encephalopathy can be mistaken for side effects of the drug).

At the beginning of therapy, one should refrain from driving vehicles and performing other potentially hazardous types of work. Further, the degree of restriction is determined individually.

Application during pregnancy and lactation

Due to the lack of data from clinical studies, it is not recommended to use Pipolfen during pregnancy.

Due to the use of the drug during breastfeeding, there is a risk of developing extrapyramidal disorders in a child due to the penetration of promethazine into breast milk. If it is necessary to use Pipolfen during lactation, breastfeeding must be stopped.

Pediatric use

Parenteral administration of Pipolfen is contraindicated in children under 2 months of age; taking tablets / pills inside - children under 6 years old.

The drug is prescribed with caution to children, since its use makes it difficult to diagnose the underlying disease. The side effects of promethazine can be mistaken for symptoms of undiagnosed encephalopathy and Reye's syndrome.

With impaired renal function

Pipolfen is prescribed with caution for renal failure (impaired renal function).

For violations of liver function

Pipolfen is prescribed with caution in liver failure (liver dysfunction).

Use in the elderly

Elderly patients should be careful while using Pipolfen.

Drug interactions

With the combined use of Pipolfen with certain drugs / substances, the following effects may be observed:

• Derivatives of m-cholinomimetics, ephedrine, amphetamine, anticholinesterase drugs, levodopa, guanethidine, dopamine: weakening their action;
• Opioid analgesics, hypnotics, anxiolytic (tranquilizers) and antipsychotic drugs (neuroleptics), as well as drugs for general anesthesia, local anesthetics, m-anticholinergics and antihypertensive drugs: enhancement of their effects (medical supervision and dose adjustment is required);
• Beta-blockers: increasing the concentration of promethazine in the blood plasma;
• Barbiturates: acceleration of elimination and decrease in the activity of promethazine;
• Prolactin: increasing its concentration;
• Bromocriptine: weakening of its action;
• Clonidine, ethanol, antiepileptic drugs: increasing the inhibitory effect of promethazine on the central nervous system;
• Anticholinergic drugs and tricyclic antidepressants: increased m-anticholinergic activity of promethazine;
• Quinidine: increasing the likelihood of a cardiodepressant effect of promethazine;
• Monoamine oxidase inhibitors, phenothiazine derivatives: an increase in the likelihood of developing extrapyramidal disorders and arterial hypotension (simultaneous administration with monoamine oxidase inhibitors is not recommended).

Analogs

Pipolfen's analogues are: Avomin, Fargan, Fenergan, Prometegan, Protiazin, Pipolzin, Rinathiol.

Terms and conditions of storage

Store in a dark place, out of reach of children, at a temperature of 15-25 ° C.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Pipolfen

Since the drug belongs to the first generation antihistamines, it is not used as often now as the second and third generation drugs. In isolated reviews of Pipolfen from patients, a fairly large list of adverse reactions and contraindications is especially noted, which in some cases forces to stop therapy. Other patients point to the high efficacy of the drug.

Experts note the rapid and effective action of promethazine, thanks to which it is successfully used in emergency situations (after intramuscular administration, the effect is noted within 2 minutes). Therefore, Pipolfen's solution is included in the mandatory composition of first aid kits for providing ambulance for anaphylactic shock. It is important that in therapeutic doses the drug does not affect the function of the cardiovascular system. And its sedative effect is quite significant in the postoperative period. In addition, the use of promethazine in combination with analgesics helps relieve postoperative pain. Long-term use of the drug requires monitoring of the peripheral blood count and hepatic function.

Price for Pipolfen in pharmacies

The approximate price of Pipolfen in ampoules in the form of a solution for intravenous and intramuscular administration of 50 mg / 2 ml (10 ampoules per pack) varies from 714 to 1067 rubles.

The term for registration of tablets in Russia has expired, therefore, in this form of release, Pipolfen is not available for free sale.

Pipolfen: prices in online pharmacies

Drug name Price Pharmacy

Pipolfen 50 mg / 2 ml solution for intravenous and intramuscular administration 2 ml 10 pcs. 899 RUB Buy

Pipolfen solution for in. 25mg / ml 2ml 10 pcs. 1,024 RUB Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!