Composition, form of production and packaging
The solution for intravenous and / or injections is clear, colorless or with a green tinge, without or almost no odor.
1 ml of 1 amp.
Promethazine hydrochloride 25 mg 50 mg
Excipients: hydroquinone - 0.4 mg, potassium disulphite - 1.5 mg, sodium sulfite anhydrous - 2 mg, sodium chloride - 14 mg, water d / and - up to 2 ml.
2 ml - ampoules of colorless glass with a break point and a blue code ring (5) - packs of cellular plastic (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
The blocker of histamine H 1 -receptors, a phenothiazine derivative. Has a pronounced antihistaminic activity and has a significant effect on the central nervous system (has a sedative, hypnotic, antiemetic, antipsychotic and hypothermic effect). Warns and soothes hiccups.
Prevents effects mediated by histamine (including hives and itching). Anticholinergic action 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, and a direct inhibitory effect on the trigger chemoreceptor zones of the medulla oblongata.
Sedative action is due to 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 ОІ-adrenoreceptors indirectly weakens the stimulation of the reticular formation of the brain stem. Since its chemical structure is different from the structure of other antipsychotic agents from the phenothiazine group, promethazine has a weaker antipsychotic effect.
In therapeutic doses does not affect the cardiovascular system.
The clinical effect is manifested after 2 min after IM or 3-5 min after IV introduction and usually lasts for 4-6 hours (sometimes remaining up to 12 hours).
PHARMACOKINETICS
Suction
After oral administration, it is quickly and well absorbed from the digestive tract.
Distribution
The binding of promethazine to plasma proteins is about 90%.
It penetrates the GEB and the placental barrier.
Metabolism
Intensively metabolized in the liver during the "first passage", mainly by S-oxidation. Sulfoxides prometazina and N-demetil-prometazin are the main metabolites, which are determined in urine.
Excretion
T 1/2 of promethazine is 7-15 hours. It is excreted mostly by the kidneys; to a lesser extent - through the intestines.
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 / epinephrine);
- as a sedative in the pre- and postoperative period;
- to prevent or arrest 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 on transport);
- as a component of lytic mixtures used to potentiate anesthesia in surgical practice (for parenteral use).
DOSING MODE
Assign in / m and / in.
The maximum daily intake for adults is 150 mg.
In / m the drug is prescribed to adults at 25 mg 1 time / day, if necessary 12.5-25 mg every 4-6 hours.
For the prevention and treatment of nausea and vomiting, the drug is administered orally or intravenously at a dose of 25 mg once. If necessary, you can appoint 25 mg every 4-6 hours.
As a sedative in surgery on the eve of surgery, I / m in a dose of 25-50 mg once a night. For preoperative preparation 2.5 hours before the operation, 50 mg of Pipolphen is administered as a part of lymphatic mixtures in / m, if necessary, after 1 h, the administration can be repeated.
For the induction of anesthesia and analgesia with certain diagnostic and surgical interventions, such as repeated bronchoscopy, ophthalmic operations, PipolpheneВ® can be administered IV in doses of 0.15-0.3 mg / kg body weight.
For children over 2 months of age, the drug can be injected intravenously 3-5 times a day at a dose of 0.5-1 mg / kg body weight. In severe cases, a single dose for I / m administration can be increased to 1-2 mg / kg body weight.
SIDE EFFECT
From the side of the central nervous system: sedative effect, drowsiness, nightmares, increased nighttime apnea, visual acuity, anxiety, psychomotor agitation, dizziness, confusion, disorientation; after taking in high doses - extrapyramidal disorders, increased convulsive activity (in children).
From the cardiovascular system: it is possible to reduce blood pressure, tachycardia, bradycardia.
On the part of the digestive system: nausea, vomiting, constipation, dry mouth, nose, pharynx, anesthesia of the oral mucosa, cholestasis are possible.
From the hemopoietic system: rarely - thrombocytopenia and / or leukopenia, agranulocytosis.
Dermatological reactions: skin rash and / or photosensitivity are possible.
From the senses: noise or ringing in the ears, paresis of accommodation, visual impairment.
Allergic reactions: urticaria, dermatitis, photosensitivity, bronchospasm.
Other: increased sweating, difficulty or painful urination.
CONTRAINDICATIONS
- comatose conditions or other forms of deep depression of the central nervous system;
- simultaneous use of MAO inhibitors and a period of 14 days after completion of their admission;
- an angle-closure glaucoma;
- alcohol intoxication, acute intoxication with hypnotic drugs, opioid analgesics;
- sleep apnea syndrome;
- Occasional vomiting in children of unspecified genesis;
- Pregnancy;
- lactation period;
- Children under 2 months of age (for parenteral administration);
- hypersensitivity to promethazine, other phenothiazine derivatives and any other component of the drug.
Caution should be given to the drug in acute and chronic respiratory diseases (due to suppression of cough reflex), open-angle glaucoma, suppression of bone marrow function, diseases of the cardiovascular system, violations of the liver and kidney function, peptic ulcer with pyloroduodenal obstruction, stenosis of the neck of the bladder and / or prostatic hypertrophy, predisposition to urinary retention, epilepsy, Reye's syndrome, and elderly patients.
PREGNANCY AND LACTATION
Clinical data on the use of the drug Pipolfen В® in pregnancy are absent, therefore its use is contraindicated.
If it is necessary to use the drug during lactation, breastfeeding should be discontinued due to the risk of extrapyramidal disorders in the child.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for violations of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for violations of liver function.
APPLICATION FOR CHILDREN
Contraindication: children under 2 months (for parenteral administration); children under 6 years (for oral administration).
Caution should be used to administer Pipolphen В® to children, since it is difficult to diagnose the underlying disease. Symptoms of undiagnosed encephalopathy and Reye's syndrome may be mistaken for the side effects of Pipolphen.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
SPECIAL INSTRUCTIONS
With prolonged use of the drug, it is necessary to systematically monitor the formula of peripheral blood and liver function.
With extreme caution, especially in high doses, Pipolphene В® should be given to elderly patients; In this category of patients, the risk of side effects is increased.
When used simultaneously with Pipolphenom analgesics and hypnotics should be given in smaller doses.
Pipolphene В® should be used under strict medical supervision simultaneously with opioid analgesics, sedatives and hypnotics, anesthesia, tricyclic antidepressants and tranquilizers.
Pipolphene В® can mask the ototoxic effect (tinnitus and dizziness) of the medications used together.
Pipolphen В® reduces the threshold of convulsive readiness. This should be taken into account when appointing the drug to patients prone to developing seizures, or simultaneously with other drugs with a similar effect.
As an antiemetic, Pipolphen В® should be used only with prolonged vomiting of a known etiology.
With prolonged use, the risk of developing dental diseases (caries, periodontitis, candidiasis) is increased due to a decrease in salivation.
During the period of treatment, alcohol is not allowed.
During the period of taking Pipolphen, a diagnostic test for pregnancy can give a false positive result.
Consideration should be given to the possible increase in blood glucose levels in patients taking Pipolphene В® when performing a test for glucose tolerance.
To prevent distortion of the results of skin scarification tests for allergens, the drug must be discontinued 72 hours before the allergological tests.
Each pellet contains 95 mg of lactose, which should be taken into account when lactose intolerance.
Use in Pediatrics
Caution should be used to administer Pipolphen В® to children, since it is difficult to diagnose the underlying disease. Symptoms of undiagnosed encephalopathy and Reye's syndrome may be mistaken for the side effects of Pipolphen.
Impact on the ability to drive vehicles and manage mechanisms
In the initial period of application of Pipolphen, it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. Further, the degree of restriction is determined depending on the patient's individual tolerability.
OVERDOSE
Symptoms: in children - excitement, anxiety, hallucinations, convulsions, mydriasis and immobility of the pupils, hyperemia of the facial skin, hyperthermia; in adults - psychomotor agitation, convulsions, inhibition. In acute overdose - a marked decrease in blood pressure, vascular collapse, respiratory depression, coma.
Treatment: in connection with the lack of antidotes, symptomatic and supportive therapy is performed. Gastric lavage, the appointment of activated charcoal inside (with detoxification in the early periods after ingestion); on indications - antiepileptic drugs. Dialysis is ineffective. A beneficial effect can be taken orally in the form of sodium or magnesium sulphate.
Steps should be taken to restore adequate pulmonary ventilation by providing airway patency and assisted or artificial ventilation. Correction of acidosis and / or electrolyte balance is necessary. In severe arterial hypotension, norepinephrine (norepinephrine) or mezaton should be administered. Epinephrine (adrenaline) paradoxically can enhance arterial hypotension.
DRUG INTERACTION
Pipolphene В® enhances the effects of opioid analgesics, hypnotics, anxiolytic (tranquilizers) and antipsychotics (neuroleptics), as well as drugs for general anesthesia, local anesthetics, m-holinoblokatorov and antihypertensive drugs (dose adjustment is required).
Pipolphene В® weakens the action of derivatives of amphetamine, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine.
Barbiturates accelerate elimination and reduce prometazine activity.
Beta-adrenoblockers increase (mutually) the concentration of promethazine in the blood plasma.
Pipolphene В® weakens the effect of bromocriptine and increases the concentration of prolactin in the blood serum.
Tricyclic antidepressants and anticholinergic drugs increase m-cholinoblocking activity of promethazine.
Ethanol, clonidine, antiepileptic drugs increase the oppressive effect of promethazine on the CNS.
MAO inhibitors (concurrent use is not recommended) and phenothiazine derivatives increase the risk of arterial hypotension and extrapyramidal disorders. Quinidine increases the likelihood of cardiodepressant action of promethazine.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a place protected from light, inaccessible to children at a temperature of 15 В° to 25 В° C. Shelf life - 5 years.
