Promethazine - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

H1-antihistamines

Included in the formulation

Pipolphen®

solution w / m in / in

Egis Pharmaceutical Plant OJSC Hungary

Pipolphen®

pills inwards

Egis Pharmaceutical Plant OJSC Hungary

АТХ:

R.06.A.D. Phenothiazine derivatives

R.06.A.D.02 Promethazine

Pharmacodynamics:

The action is anti-allergic, antihistamine, sedative, antiemetic, antipruritic, hypnotic, locally anesthetic.

Competitively blocks H1-histamine receptors, has antiexudative, anti-allergic, anti-inflammatory. Reduces the permeability of capillaries, swelling of the mucous membranes, itching. It blocks alpha-adrenoreceptors, M-holinoretseptory. Inhibits histamine-N-methyltransferase, blocks central histamine H3 receptors. Oppresses the central nervous system, has a sedative, anxiolytic, antipsychotic and hypnotic effect, lowers body temperature. Reduces the excitability of the vestibular receptors, depresses the function of the labyrinth, eliminates dizziness. The antiemetic effect is due to blockade of the M-receptors of the chemoreceptor zone of the emetic center of the medulla oblongata. Penetrates through the BBB. At appointment for 2 weeks before sorts or labors can oppress an aggregation of thrombocytes at newborns. In experimental studies, there was no mutagenic effect and adverse effects on fetal development.

Pharmacokinetics:Quickly and completely absorbed from the digestive tract. When ingestion effects appear after 15-60 minutes, with intramuscular injection - after 20 minutes, with intravenous - in 3-5 minutes. The duration of the action is 4-6 hours (after oral administration - up to 12 hours). It binds to blood plasma proteins by 65-90%. Metabolized in the liver and, partially, in the kidneys, with the formation of prometazine sulfoxides, N-desmethylprometazine and other derivatives. The half-life is 7-14 hours. It is excreted mostly with urine, incl. in the form of metabolites.

Indications:Allergic dermatoses, prurigo, eczema, exudative diathesis, urticaria, rash and other skin allergic reactions to medicinal and chemical preparations, pruritus, allergic conjunctivitis, allergic rhinitis, pollinosis, bites of bees, bees, scorpions, bumblebees, serum sickness, angioedemaedema, false croup, asthmatic bronchitis, atopic bronchial asthma, anaphylactic and anaphylactoid reactions (as part of complex therapy), rheumatism with a pronounced allergic component; Meniere's syndrome, dizziness, nausea and vomiting, motion sickness syndrome; anxiety, neuroses and neurosis-like conditions, psychoses, insomnia,extrapyramidal disorders (against the background of neuroleptics), trigeminal neuralgia, migraine, chorea, hyperthermia; premedication and postoperative(as a sedative, for artificial hibernation, potentiation of anesthesia and local anesthesia), study of gastric secretion (when used as a stimulant secretion of histamine).

ICD-10

V.F20-F29.F29 Inorganic psychosis, unspecified

VI.G20-G26.G25.5 Other types of chorea

VI.G40-G47.G43 Migraine

VI.G50-G59.G50.0 Neuralgia of the trigeminal nerve

VIII.H80-H83.H81.0 Ménière's disease

X.J30-J39.J30 Vasomotor and allergic rhinitis

X.J40-J47.J44 Other chronic obstructive pulmonary disease

X.J40-J47.J45 Asthma

XII.L20-L30.L20 Atopic dermatitis

XII.L20-L30.L23 Allergic contact dermatitis

XII.L20-L30.L28 Simple chronic lichen and prurigo

XII.L20-L30.L29 Itching

XII.L20-L30.L30.9 Dermatitis, unspecified

XIII.M70-M79.M79.0 Rheumatism, unspecified

XVIII.R10-R19.R11 Nausea and vomiting

XVIII.R40-R46.R42 Dizziness and dizziness

XVIII.R40-R46.R45.1 Anxiety and Excitement

XVIII.R50-R69.R50 Fever of unknown origin

XIX.T66-T78.T75.3 Motion Slicking

XIX.T66-T78.T78.2 Anaphylactic shock, unspecified

XIX.T66-T78.T78.3 Angioedema

XIX.T66-T78.T78.4 Allergy, unspecified

XIX.T80-T88.T80.6 Other serum reactions

XX.W50-W64.W57 Bite or sting with a non-toxic insect or other non-venous arthropod

XIX.T66-T78.T78.8 Other adverse reactions, not elsewhere classified

Contraindications:Hypersensitivity(including other phenothiazines), coma, simultaneous use of MAO inhibitors and a period of 14 days after completion of their intake, alcohol intoxication, hepatic and / or renal failure, pregnancy, breast-feeding, episodic vomiting in children unspecified genesis, early childhood to 2 months (for parenteral administration), children under 6 years of age (for oral administration).

Carefully:Jaundice, prostatic hypertrophy, predisposedThere is a delay in urine, stenosis of the neck of the bladder, open-angle or closed-angle glaucoma, peptic ulcer with pyloroduodenalobstruction, lower respiratory tract diseases, bone marrow depression, cardiovascular diseasessystem (severe angina, hypertension, decompensatedchronic heart failure, ciliary tachyarrhythmia), epilepsy, sleep apnea syndrome, Reye syndrome,elderly age.

Pregnancy and lactation:

Contraindicated in pregnancy. Action category on the fetus by FDA - C.

For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:Inside (after meal), intramuscularly, intravenously. Adults: 12.5-25 mg 3-4 times daily and 25-50 mg per night (maximum dose: single dose - 75 mg, daily - 500 mg). With kinetosis, 12.5-25 mg 3-4 times a day orally. With nausea and vomiting - at the beginning of 25 mg, then - 12.5-25 mg every 4-6 hours. Children: at the age of 2-6 years - 12.5 mg, 6-14 years - 25 mg 3-4 times in day. Parenteral (emergency cases, anesthesia(deep in the muscle) at a dose of 0.5-1 mg / kg 3-5 times a day (in severe cases at an initial dose of 1-2 mg / kg), the maximum daily dose is 250 mg; in / in (for hibernation) 0,15-0,3 mg / kg (maximum permissible concentration) - 25 mg / ml, the speed of administration - 25 mg / min). To prepare for surgery - on the evening before 25-50 mg orally together with other drugs; on the day of surgery 2.5 hours before it - 50 mg IM (in combination with an analgesic and anticholinergic), it is possible to re-introduce after 1 hour; children in a dose of 1.1 mg / kg. For the prevention of motion sickness syndrome, once for 1 hour before the trip, adults - 25-50 mg, children - 10-20 mg. For auxiliary therapy of anaphylaxisabout shock - 10-20 mg IV slowly (after injection of epinephrine) and then for the next 24-48 hours to prevent relapse.

Side effects:

From the nervous system and sensory organs: sedation, dizziness, drowsiness, anxiety, agitation, nightmares, more frequent nighttime apneas; rarely - disorientation, confusion, extrapyramidal disorders, increased convulsive activity (in children); disturbance of accommodation and vision, noise or ringing in the ears.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): Orthostatic hypotension (with intravenous administration), hypertension, tachycardia, or bradycardia; rarely - leukopenia, thrombocytopenia, agranulocytosis.

On the part of the digestive system: anesthesia and dry mouth, nausea, vomiting, cholestasis, constipation.

On the part of the respiratory system: dryness in the nose, pharynx.

From the genitourinary system: rarely - labored or painful urination.

Allergic reactions: urticaria, dermatitis, asthma.

Other: increased sweating, photosensitivity, soreness (with the / m introduction).

Overdose:

Symptoms: hyperemia of the skin of the face, dyspnea,dryness of mucous membranes, mydriasis, restlessness, motor hyperactivity, agitation, delirium (in children), extrapyramidal disorders, tremor, epileptiform seizures (rarely), hypotension, respiratory depression, loss of consciousness.

Treatment: induction of vomiting, gastric lavage, the appointment of activated charcoal, saline laxatives (with ingestion), intravenous fluids; monitoring and maintenance of vital functions; symptomatic therapy: vasoconstrictor (with hypotension), oxygen (to maintain adequate oxygenation).

It is not recommended the use of analeptics (can cause seizures) and epinephrine (possibly strengthening hypotension). With the development of extrapyramidal reactions, anticholinergics are used to treat Parkinson's disease, diphenhydramine or barbiturates. Dialysis is ineffective.

Interaction:

β-Adrenoblockers - increase (mutual) of plasma concentrations, severe arterial hypotension, arrhythmias, irreversible retinopathy, tardive dyskinesia.

Analgesics, hypnotics, tranquilizers, antipsychotics, anesthetics, local anesthetics, m-holinoblokatory, hypotensive drugs, other means, depressing breathing - enhancing effects, correction of doses is required.

Barbiturates - acceleration of elimination and reduction of prometazine activity.

Bromocriptine - weakening of its action, increasing serum prolactin concentration.

Hepatotoxic agents - increased hepatotoxicity.

MAO inhibitors (concurrent use is not recommended), phenothiazine derivatives - increased risk of developing arterial hypotension and extrapyramidal disorders.

Ototoxic agents - enhancement of ototoxicity.

Derivatives of amphetamine, m-cholinomimetics, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine - weakening of their action.

Riboflavin - it is necessary to increase its dose.

Means that depress the appetite - decrease in anorexigensal effect.

Tricyclic antidepressants, anticholinergics - enhance m-cholinoblocking activity.

Quinidine - increased likelihood of cardiodepressive action.

Epinephrine - blockade of α-adrenergic effect, risk of serious hypotension.

Ethanol, clonidine, anticonvulsants - increased oppression of the central nervous system.

Special instructions:

In newborns whose mothers took promethazine, there was a violation of platelet aggregation.

With long-term treatment, it is recommended that a systematic analysis of the blood and control of liver function parameters is recommended.

During the treatment period, do not drink alcohol.

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

It is not recommended for use in children for relief of episodic vomiting of unspecified genesis.

The use of promethazine in combination with opioid analgesics and tranquilizers for the complex preoperative preparation of patients is possible only under the strict supervision of a physician.

With long-term treatment, it is recommended that a systematic analysis of the blood and control of liver function parameters is recommended.

During the treatment period, do not drink alcohol.

The solution is not intended for intra / a and / or administration. Some dosage forms of promethazine contain sodium metabisulphite, which can cause allergic reactions, including anaphylactoid and asthmatic. To prevent distortion of skin scarification test results for allergens, it is necessary to cancel 72 hours prior to allergological testing.During treatment, false-positive pregnancy test results are possible.

It can suppress the cough reflex, therefore caution is necessary in patients (especially children) with exacerbation of chronic respiratory diseases.

With caution should be used in people with impaired liver function, diseases of the cardiovascular system and oppression of bone marrow hematopoiesis.

In the elderly, caution is necessary for parenteral administration of high doses, because extrapyramidal disorders and acute retention of urine are possible.

As antiemetics should be used only with prolonged vomiting of a known etiology.

To prevent oppression of the central nervous system, caffeine is recommended. With prolonged use, the risk of developing dental diseases (caries, periodontitis, candidiasis) is increased due to a decrease in salivation. May mask ototoxic effect (tinnitus and dizziness) of the drugs used together. Increases the need for riboflavin.

Impact on the ability to drive vehicles and manage mechanisms

Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention (especially at the beginning of the course)

Instructions

Promethazine (Promethazinum)