Product Overview
Structure
1 ml:
- promethazine hydrochloride 25 mg
Excipients :
hydroquinone,
potassium disulfite,
sodium sulfite anhydrous,
sodium chloride,
water d / i.
pharmachologic effect
Pharmaceutical group:
Blocker of histamine H1 receptors. Antiallergic drug.
Pharmaceutical action:
Pipolfen 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 a sedative, hypnotic, antiemetic, antipsychotic and hypothermic effect). Prevents and soothes hiccups.
Prevents histamine-mediated effects (including hives and pruritus). The anticholinergic effect causes a drying effect on the mucous membranes of the nasal cavity and mouth.
The antiemetic effect of promethazine is due to its central anticholinergic effect, a decrease in the excitability of the vestibular system, suppression of the labyrinth function, as well as a direct inhibitory effect on the trigger chemoreceptor zones of the medulla oblongata.
The sedative effect is due to inhibition of histamine-K-methyltransferase and blockade of central histamine receptors. It is also possible blockade of other CNS receptors, such as serotonin and cholinergic receptors; stimulation of α-adrenergic receptors indirectly weakens the stimulation of the reticular formation of the brainstem. Since its chemical structure is different from that of other antipsychotics 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 administration (on average 15-60 minutes), 2 minutes after intramuscular administration or 3-5 minutes after intravenous administration and usually lasts for 4-6 hours (sometimes persisting up to 12 hours).
Indications
- allergic diseases (including urticaria, serum sickness, hay fever, allergic rhinitis, allergic conjunctivitis, angioedema, itching);
- auxiliary therapy of anaphylactic reactions (after relief of acute manifestations by other means, for example, epinephrine / adrenaline /);
- 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 while traveling by transport);
- as a component of lytic mixtures used to potentiate anesthesia in surgical practice (for parenteral use).
Contraindications
- coma or other types of deep depression of the central nervous system;
- the simultaneous use of MAO inhibitors and a period of 14 days after the end of their intake;
- angle-closure glaucoma;
- alcohol intoxication, acute intoxication with hypnotics, opioid analgesics;
- sleep apnea syndrome;
- episodic vomiting in children of unspecified genesis;
- pregnancy;
- lactation period;
- children's age up to 2 months (for parenteral administration);
- children under 6 years of age (for oral administration);
- hypersensitivity to promethazine, other phenothiazine derivatives and any other component of Pipolfen.
The drug should be prescribed 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, impaired liver and kidney function, peptic ulcer disease with pyloroduodenal obstruction, bladder neck stenosis and / or prostatic hypertrophy, predisposition to urinary retention, epilepsy, Reye's syndrome, as well as elderly patients.
Side effects
From the side of the central nervous system: sedation, drowsiness, nightmares, increased sleep apnea, impaired visual acuity, anxiety, psychomotor agitation, dizziness, confusion, disorientation; after taking in high doses - extrapyramidal disorders, increased seizure activity (in children).
From the side of the cardiovascular system: a decrease in blood pressure, tachycardia, bradycardia is possible.
From the digestive system: possible nausea, vomiting, constipation, dry mouth, nose, throat, anesthesia of the oral mucosa, cholestasis.
From the hematopoietic system: rarely - thrombocytopenia and / or leukopenia, agranulocytosis.
Dermatological reactions: possible skin rash and / or photosensitization.
From the senses: 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
Pipolfen® enhances the effects of opioid analgesics, hypnotics, anxiolytics (tranquilizers) and antipsychotics (neuroleptics), as well as drugs for general anesthesia, local anesthetics, m-anticholinergics and antihypertensive drugs (dose adjustment is required).
Pipolfen® weakens the effect of amphetamine derivatives, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine.
Barbiturates accelerate elimination and decrease the activity of promethazine.
Beta-blockers increase (mutually) the concentration of promethazine in the blood plasma.
Pipolfen® weakens the effect of bromocriptine and increases the concentration of prolactin in the blood serum.
Tricyclic antidepressants and anticholinergic drugs increase the m-anticholinergic activity of promethazine.
Ethanol, clonidine, antiepileptic drugs increase the inhibitory effect of promethazine on the central nervous system.
MAO inhibitors (simultaneous administration is not recommended) and phenothiazine derivatives increase the risk of arterial hypotension and extrapyramidal disorders. Quinidine increases the likelihood of the cardiodepressant effect of promethazine.
How to take, course and dosage
Assign orally, intramuscularly and intravenously.
The maximum daily dose for adults is 150 mg.
The intramuscular 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, Pipolfen® is prescribed orally at a dose of 25 mg 1 time / day. in the evening or 25 mg 2 times / day. (in the morning and in the evening). The drug should be prescribed in the minimum effective dose.
For the prevention and treatment of nausea and vomiting, the drug is prescribed orally or intramuscularly in a dose of 25 mg once. If necessary, you can prescribe 25 mg every 4-6 hours.
In kinetosis, Pipolfen® is prescribed orally at 25 mg 2 times / day, the first dose - 0.5-1 hours before the trip, the next one - after 8-12 hours.
As a sedative in surgery on the eve of the operation, it is prescribed by mouth or intramuscularly in a dose 25-50 mg once at night. For preoperative preparation, 50 mg of Pipolfen is administered as part of lytic mixtures in the composition of lytic mixtures 2.5 hours before the operation; if necessary, the administration can be repeated after 1 hour.
For the induction of anesthesia and analgesia during certain diagnostic and surgical interventions, such as repeated bronchoscopy, ophthalmic operations, Pipolfen® can be administered intravenously at doses of 0.15-0.3 mg / kg body weight.
For children over the age of 2 months, the drug can be administered IM 3-5 times / day. at a dose of 0.5-1 mg / kg body weight. In severe cases, a single dose for intramuscular injection can be increased to 1-2 mg / kg of body weight.
Children aged 6 to 14 years are prescribed by mouth 25 mg (1 tablet) 3-4 times / day. Dragee Pipolfen is not recommended to be divided, therefore 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 pronounced decrease in blood pressure, vascular collapse, respiratory depression, coma.
Treatment: due to the lack of antidotes, symptomatic and supportive therapy is carried out. Gastric lavage, the appointment of activated charcoal inside (when detoxification is carried out in the early stages after ingestion); according to indications - antiepileptic drugs. Dialysis is ineffective. Ingestion of sodium or magnesium sulfate may be beneficial.
Steps should be taken to restore adequate pulmonary ventilation by maintaining an airway and providing assisted or mechanical ventilation. Correction of acidosis and / or electrolyte balance is required. In severe arterial hypotension, norepinephrine (norepinephrine) or mezatone should be administered. Epinephrine (adrenaline) can paradoxically increase hypotension.
Special instructions
With prolonged use of the drug, it is necessary to systematically monitor the peripheral blood count and liver function.
With extreme caution, especially in high doses, Pipolfen® should be prescribed to elderly patients, because this category of patients has an increased risk of side effects.
When used simultaneously with Pipolfen, analgesics and hypnotics should be prescribed in smaller doses.
Pipolfen® should be used under strict medical supervision simultaneously with opioid analgesics, sedatives and hypnotics, anesthetics, tricyclic antidepressants and tranquilizers.
Pipolfen® can mask the ototoxic effect (tinnitus and dizziness) of concomitant drugs.
Pipolfen® lowers the seizure threshold. This should be taken into account when prescribing the drug to patients prone to the development of seizures, or simultaneously with other drugs with a similar effect.
As an antiemetic drug, Pipolfen® should be used only with prolonged vomiting of known etiology.
With prolonged use, the risk of developing dental diseases (caries, periodontitis, candidiasis) increases due to a decrease in salivation.
During the period of treatment, alcohol is prohibited.
During the period of taking Pipolfen, a diagnostic pregnancy test can give a false positive result.
A possible increase in blood glucose levels in patients taking Pipolfen® should be taken into account when performing a glucose tolerance test.
To prevent distortion of the results of skin scarification tests for allergens, the drug must be canceled 72 hours before the allergological tests.
Each dragee contains 95 mg of lactose, which should be taken into account in case of lactose intolerance.
Use in pediatrics
Pipolfen® should be prescribed with caution to children, as this makes it difficult to diagnose the underlying disease. Symptoms of undiagnosed encephalopathy and Reye's syndrome can be mistaken for Pipolfen's side effects.
Influence on the ability to drive vehicles and control mechanisms
In the initial period of Pipolphen's use, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous 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 patient's tolerance.
Release form
Pipolfen solution for intravenous and intramuscular administration is transparent, colorless or with a green tinge, without or almost odorless.
