Pipolphen solution for intravenous and intramuscular administration of 50 mg 2 ml ampoules 2 ml 10 pcs
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Active ingredients
Promethazine
Composition
Promethazine hydrochloride 25 mg per 1 ml. Excipients: hydroquinone - 0.4 mg, potassium disulfite - 1.5 mg, sodium anhydrous sulfite - 2 mg, sodium chloride - 14 mg, water d / up to 2 ml.
Pharmacological effect
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). Warns and soothes hiccups. Prevents effects mediated by histamine (including urticaria and pruritus). 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, reduction in the excitability of the vestibular system, suppression of the maze function, as well as a direct inhibitory effect on the trigger chemoreceptor zones of the medulla oblongata. Sedative effect due to inhibition of histamine-K-methyltransferase and blockade of central histamine receptors. It is also possible blockade and other receptors of the CNS, such as serotonin and cholinergic receptors; stimulation of α-adrenoreceptors indirectly weakens the stimulation of the brainstem reticular formation. Since its chemical structure is different from that of other antipsychotics from the phenothiazine group, promethazine has a weaker antipsychotic effect. In therapeutic doses, does not affect the cardiovascular system. The clinical effect is manifested 2 min after i / m administration or 3-5 min after i / v administration and usually lasts 4-6 h (sometimes lasts up to 12 h).
Pharmacokinetics
Absorption After ingestion, it is rapidly and well absorbed from the gastrointestinal tract. Distribution The binding of promethazine to plasma proteins is about 90%. It penetrates the BBB and placental barrier. Metabolism Intensively metabolized in the liver during the "first pass" mainly by S-oxidation. Promethazine sulfoxides and N-demethyl-promethazine are the main metabolites that are detected in urine. Withdrawal of T1 / 2 of promethazine makes 7-15 h. It is removed mainly by kidneys; to a lesser extent through the intestines.
Indications
- Allergic diseases (including urticaria, serum sickness, hay fever, allergic rhinitis, allergic conjunctivitis, angioedema, pruritus); - adjuvant 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; - to prevent or relieve 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 vehicle); - as a component of lytic mixtures used to potentiate anesthesia in surgical practice (for parenteral use).
Contraindications
- coma or other types of deep CNS depression; - simultaneous use of MAO inhibitors and the period within 14 days after completion of their admission; - angle-closure glaucoma; - alcohol intoxication, acute intoxication with hypnotic drugs, opioid analgesics; - sleep apnea syndrome; - occasionally occurring vomiting in children of unspecified genesis; - pregnancy; - lactation period; - children's age up to 2 months (for parenteral administration); - Hypersensitivity to promethazine, other phenothiazine derivatives and any other component of the drug. Precautions should be prescribed for acute and chronic respiratory diseases (due to suppression of the cough reflex), open-angle glaucoma, bone marrow suppression, cardiovascular diseases, liver and kidney function disorders, peptic ulcer with piloroduodenal obstruction, bladder neck stenosis and / or prostatic hypertrophy, predisposition to urinary retention, epilepsy, Reye's syndrome, as well as elderly patients.
Use during pregnancy and lactation
Clinical data on the use of the drug Pipolphen during pregnancy are not available, so its use is contraindicated. If necessary, the use of the drug during lactation breastfeeding should be discontinued due to the risk of extrapyramidal disorders in the child.
Dosage and administration
Assign IM / IV. The maximum daily dose for adults is 150 mg. V / m drug is prescribed to adults 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 intramuscularly in a dose of 25 mg once. If necessary, you can prescribe 25 mg every 4-6 hours. As a sedative in surgery, on the eve of the operation, an intramuscular dose of 25-50 mg is prescribed once a night. For preoperative preparation, 2.5 mg of Pipolphen is injected into the composition of the lytic mixtures 2.5 hours before the operation, and if necessary, the administration can be repeated after 1 hour. For induction of anesthesia and analgesia with certain diagnostic and surgical procedures, such as repeated bronchoscopy, ophthalmic surgery, Pipolphen can be administered IV dose of 0.15-0.3 mg / kg body weight. For children over the age of 2 months, the drug can be administered intramuscularly 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 effects
From the side of the central nervous system: sedation, drowsiness, nightmares, increased sleep apnea, visual acuity, anxiety, agitation, dizziness, confusion, disorientation; after administration in high doses - extrapyramidal disorders, increased seizure activity (in children). Since the cardiovascular system: may decrease blood pressure, tachycardia, bradycardia. On the part of the digestive system: nausea, vomiting, constipation, dry mouth, nose, throat, anesthesia of the oral mucosa, cholestasis are possible. On the part of the blood system: rarely - thrombocytopenia and / or leukopenia, agranulocytosis. Dermatological reactions: skin rash and / or photosensitization are possible. On the part of the senses: noise or tinnitus, accommodation paresis, blurred vision. Allergic reactions: urticaria, dermatitis, photosensitivity, bronchospasm. Other: increased sweating, difficulty or painful urination.
Overdose
Symptoms: in children - excitement, anxiety, hallucinations, convulsions, mydriasis and stiffness of the pupils, flushing of the skin of the face, hyperthermia; in adults - psychomotor agitation, convulsions, lethargy.In acute overdose - marked reduction in blood pressure, vascular collapse, respiratory depression, coma. Treatment: due to the absence of antidotes, symptomatic and supportive therapy is carried out. Gastric lavage, the appointment of activated carbon inside (when carrying out detoxification in the early stages after ingestion); According to indications - antiepileptic drugs. Dialysis is ineffective. Intake of sodium sulfate or magnesium may have a beneficial effect. Measures should be taken to restore adequate pulmonary ventilation by ensuring the airway is passable and conducting auxiliary or artificial ventilation of the lungs. Correction of acidosis and / or electrolyte balance is necessary. In severe hypotension, norepinephrine (norepinephrine) or mezaton should be administered. Epinephrine (adrenaline) in a paradoxical way can increase arterial hypotension.
Interaction with other drugs
Pipolphen enhances the effects of opioid analgesics, hypnotics, anxiolytics (tranquilizers) and antipsychotics (neuroleptics), as well as general anesthetic drugs, local anesthetics, m-anticholinergics and antihypertensive drugs (dose adjustment is required). Pipolphen reduces the effects of amphetamine derivatives, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine. Barbiturates accelerate elimination and reduce the activity of promethazine. Beta-blockers increase (mutually) the concentration of promethazine in the blood plasma. Pipolphen weakens the effect of bromocriptine and increases the concentration of prolactin in the serum. Tricyclic antidepressants and anticholinergic drugs enhance the m-anticholinergic activity of promethazine. Ethanol, clofelin, 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 cardiodepressive action of promethazine.
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, should appoint Pipolphen elderly patients, because this category of patients has an increased risk of side effects.When used simultaneously with Pipolphen analgesics and hypnotics should be prescribed in smaller doses. Pipolphen should be used under strict medical supervision simultaneously with opioid analgesics, sedatives and hypnotics, anesthetics, tricyclic antidepressants and tranquilizers. Pipolphen may mask the ototoxic effect (tinnitus and dizziness) of commonly used drugs. Pipolphen reduces the threshold of convulsive readiness. 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 Pipolphen should be used only with prolonged vomiting of known etiology. With prolonged use increases the risk of developing dental diseases (caries, periodontitis, candidiasis) due to a decrease in salivation. Alcohol is prohibited during treatment. During the period of taking Pipolphen, a diagnostic pregnancy test may give a false positive result. Consideration should be given to a possible increase in the blood glucose level of patients taking Pipolphen when performing a glucose tolerance test. To prevent distortion of the results of skin scarification tests for allergens, the drug should be canceled 72 hours before the allergological tests. Each dragee contains 95 mg of lactose, which should be considered when lactose intolerance. Use in pediatrics. Pipolphen should be prescribed with care to children, as this makes it difficult to diagnose the underlying disease. The symptoms of undiagnosed encephalopathy and Reye's syndrome may be mistaken for the side effects of Pipolphen. Influence on the ability to drive motor vehicles and control mechanisms In the initial period of Pipolphen use, it is necessary to refrain from driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and quickness of psychomotor reactions. In the future, the degree of restriction is determined depending on the individual tolerance of the patient.