Pipolfen

Active material: Promethazine
When ATH: R06AD02
CCF: Gistaminovыh blocker H₁-receptors. Allergy medication
ICD-10 codes (testimony): H10.1, H81, J30.1, J30.3, L29, L50, R11, R52.0, R52.2, T78.2, T78.3, T80.6, T88.7, Z51.4
When CSF: 11.06.04
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)

Pharmaceutical form, composition and packaging

Drop light blue, čečeviceobraznoj form, with shiny surface, with little or no odor.

Excipients: stearic acid, magnesium stearate, gelatin, talc, potato starch, lactose monohydrate.

The composition of the shell: ariavit blue, glycerol, gelatin, Titanium dioxide, macrogol 35 000, talc, sucrose.

20 PC. – blisters (1) – packs cardboard.
20 PC. – blisters (25) – cardboard boxes.

Solution for in / and the / m clear, colourless or with a green tint, with little or no odor.

Excipients: Hydroquinone, potassium disul′fit, sodium sulfite, anhydrous, sodium chloride, water d / and.

2 ml – colorless glass vials (5) – packings Valium plastic (2) – packs cardboard.

Pharmacological action

Gistaminovыh blocker H₁-receptors, derived fenotiazina. Has expressed antigistaminna activity and has a considerable impact on the central nervous system (has a sedative, snotvornoe, antiemetic, antipsihoticescoe and gipotermicescoe action). Prevents and relieves hiccups.

Prevents effects, indirect gistaminom (including the hives and itching). Antiholinergicescoe effect causes podsushiwauschee effect on mucous membranes cavity of the nose and mouth.

Protivorvotnoe effect promethazine due to its central antiholinergicakim effect, decrease in excitability of the vestibular system, suppressing function of labyrinth, as well as a direct inhibitory effect on the chemoreceptor trigger zone oblong brain.

Sedative effect due to the inhibition of histamine-to-methyltransferase and blockade of Central histamine receptors. It is also possible to blockade and other receptors in the CENTRAL NERVOUS SYSTEM, such as serotoninove and holinoretseptora; α-adrenoceptor stimulation indirectly weakens the retikuliarna formations barrel brain stimulation. Because its chemical structure different from other antipsychotic means of group fenotiazinov, promethazine has weaker antipsihotičeskim action.

In therapeutic doses does not affect the cardiovascular system.

The clinical effect is manifested through 20 minutes after ingestion (average 15-60 m), through 2 minutes after the on/m introduction or through 3-5 minutes after the on/in the introduction and usually continues for 4-6 no (sometimes persisting up to 12 no).

Pharmacokinetics

Absorption

After intake of rapidly and well absorbed from the digestive tract.

Distribution

Promethazine binding to plasma proteins is about 90%.

Penetrates the GEB and placental barrier.

Metabolism

Intensive metabolised in the liver, with the “first pass” mainly through the S-oxidation. Sulfoxide promethazine and N-demetil-promethazine are major metabolites, that are defined in the Moche.

Deduction

T_1/2 promethazine is 7-15 no. Write mainly kidneys; less – through the intestine.

Testimony

- Allergic diseases (incl. hives, serum sickness, hay fever, nasal allergy, allergic conjunctivitis, angioedema, itch);

— adjuvant therapy anaphylactic reactions (After cupping acute manifestations of other means, eg, Epinephrine/adrenaline/);

— as a sedative in the pre- and postoperative;

is to prevent or relieve nausea and vomiting, associated with anesthesia and/or appearing in the postoperative period;

-post-operative pain (in combination with analgesics);

— kinetosis (for the prevention and elimination of dizziness and nausea during trips to transport);

as the political component mixtures, used for potenzirovania narcosis in surgical practice (for parenteral application).

Dosage regimen

Assign inside, / m and / in.

The maximum daily dose Adult is 150 mg.

In/m product shall adult by 25 mg 1 time / day, if necessary 12.5-25 mg every 4-6 no.

At treatment of allergic diseases Pipol′fen^® administered orally at a dose 25 mg 1 times/day in the evening or on 25 mg 2 times / day (in the morning and in the evening). The agent should be appointed at the minimum effective dose.

To Prevention and treatment of nausea and vomiting the agent shall inside or/m in a dose of 25 mg dose. Optionally, you can assign 25 mg every 4-6 no.

At kinetoze Pipol′fen^® appointed interior 25 mg 2 times / day, the first reception – for 0.5-1 hours before the trip, subsequent – through 8-12 no.

As sedative in surgery on the eve of the operation or appoint inwards in/m in a dose of 25-50 mg once at night. To Preoperative preparation for 2.5 hours before the operation, comprising lytic mixes/m impose 50 mg Pipol′fena^®, if necessary through 1 h introduction can be repeated.

To induction of anesthesia and analgesia during certain diagnostic and surgical interventions, such as repeated Bronchoscopy, ophthalmologic operation, Pipol′fen^® You can assign/in the dose 0.15-0.3 mg / kg body weight.

Children under the age of 2 Months the drug can be administered intramuscularly 3-5 times/day dose calculation 0.5-1 mg / kg body weight. In severe cases, single dose for the on/m introduction can be increased up to 1-2 mg / kg body weight.

Children aged 6 to 14 years appointed interior 25 mg (1 drop) 3-4 times / day. Bonbons share is not recommended, Therefore, the use of this dosage form children under the age of 6 years not shown.

Side effect

CNS: sedation, drowsiness, nightmares, increased frequency of sleep apnea, violation of visual acuity, anxiety, psychomotor agitation, dizziness, confusion, disorientation; After taking high doses – extrapyramidal disorder, increase in seizure activity (children).

Cardio-vascular system: You may decline ad, tachycardia, bradycardia.

From the digestive system: nausea, vomiting, constipation, dry mouth, nose, glotke, anaesthesia mucous membranes of the oral cavity, cholestasis.

From the hematopoietic system: rarely – thrombocytopenia and/or Leucopenia, agranulocytosis.

Dermatological reactions: possible skin rash and/or photosensitization.

From the senses: noise or ringing in the ears, Parez akkomodacii, blurred vision.

Allergic reactions: hives, dermatitis, photosensitivity, bronchospasm.

Other: increased perspiration, difficult or painful urination.

Contraindications

— komatosnye State or other kinds of deep oppression CNS;

-the simultaneous use of MAO inhibitors and the period during 14 days after their reception;

- Zakrыtougolynaya glaucoma;

— alcohol intoxication, acute intoxication hypnotics drugs, opioid analgesics;

-sleep apnea syndrome;

-sporadically appearing vomiting in children of an unspecified origin;

- Pregnancy;

- Lactation;

- Children up to age 2 months (for parenteral administration);

- Children up to age 6 years (orally);

-hypersensitivity to prometazinu, other derivatives fenotiazina and any other component of the drug.

FROM caution should designate product in acute and chronic respiratory diseases (due to suppression of kashlevogo reflex), open-angle glaucoma, suppression of bone marrow function, diseases of the cardiovascular system, human liver and kidneys, peptic ulcer with piloroduodenal′noj obstruction, stenosis of the cervix bladder and/or prostate hypertrophy, predisposition to delay incontinence, epilepsy, Reye's syndrome, and elderly patients.

Pregnancy and lactation

Clinical data on the use of drugs Pipol′fen^® when pregnancy is missing, therefore its use is contraindicated.

If necessary, the use of the drug during lactation breastfeeding should be discontinued because of the risk of extrapiramidale disorders in child.

Cautions

With long-term use drugs should systematically monitor formula peripheral blood and liver function.

With extreme caution, especially in high doses, assign Pipol′fen^® elderly patients, tk. This category of patients have increased risk of side effects.

Together with the application Pipol′fenom^® analgesics and hypnotics should designate smaller doses.

Pipol′fen^® should be used under strict medical supervision simultaneously with opioid analgesics, sedatives and hypnotics drugs, means to narcosis, tricyclic antidepressants and tranquilizers.

Pipol′fen^® can mask the ototoxic effect (tinnitus and dizziness) jointly used drugs.

Pipol′fen^® reduces threshold sudorojna preparedness. This should be taken into account when appointing drug patients, prone to the development of seizures, or simultaneously with other drugs with similar action.

As protivorvotny drug Pipol′fen^® should be used only when the protracted vomiting known etiology.

Prolonged use increases the risk of dental diseases (caries, periodontitis, candidiasis) due to a decrease salivation.

During treatment, it is forbidden to consume alcohol.

During the reception Pipol′fena^® pregnancy diagnostic test may give a false positive result.

Should take into account the possible increase in the level of glucose in the blood of patients, taking Pipol′fen^®, When you run a test on the tolerance to glukoze.

To prevent distortion of the skin skarifikih samples for drug allergens you must cancel 72 h to conduct allergy tests.

Each tablet contains 95 Lactose mg, What to consider when lactose intolerance.

Use in Pediatrics

The caution should appoint Pipol′fen^® children, Since this can be difficult to diagnose the disease. Symptoms of encephalopathy and nediagnostirovannoj Reyes syndrome can be mistaken for side effects Pipol′fena^®.

Effects on ability to drive vehicles and management mechanisms

In the initial period of application Pipol′fena^® to refrain from driving motor vehicles and other potentially hazardous activities, require high concentration and speed of psychomotor reactions. Further the degree of limitation determine depending on individual tolerance of the patient.

Overdose

Symptoms: children – excitation, anxiety, hallucinations, convulsions, midriaz and stiffness pupils, facial flushing, hyperthermia; adult – psychomotor agitation, convulsions, lethargy. In acute overdose – marked reduction in blood pressure, vascular collapse, respiratory depression, coma.

Treatment: due to the lack of antidotes symptomatic and supportive therapy. Gastric lavage, appointment of activated charcoal inside (When conducting a detox in the early periods after ingestion); testimony-antiepileptic drugs. Dialysis nyeeffyektivyen. Beneficial effect can have ingestion of sodium sulfate or magnesium.

Measures should be taken to restore adequate pulmonary ventilation by ensuring the road respiratory tract and adjuvant or mechanical ventilation. A correction of the acidosis and/or electrolyte imbalance. With severe arterial hypotension should be norapinefrin (noradrenaline) or mezaton. Epinephrine (adrenaline) Paradoxically it may exacerbate hypertension hypotension.

Drug Interactions

Pipol′fen^® do effects of opioid analgesics, hypnotics, anccioliticakih (trankvilizatorov) and antipsychotic means (neuroleptics), as well as drugs for general anesthesia, local anesthetics, m-holinoblokatorov and gipotenziveh drugs (dose adjustments).

Pipol′fen^® ters of amphetamine derivatives, Mr. holinomimetikov, anticholinesterase drugs, ephedrine, guanethidine, levodopa, dopamine.

Barbiturates eliminatiu up and reduce the activity of promethazine.

Beta-blockers increase (mutually) promethazine concentration in blood plasma.

Pipol′fen^® ters bromokriptina and increases the concentration of prolactin in serum.

Tricyclic antidepressants and antiholinergicakie drugs increase the m-holinoblokirutuyu activity of promethazine.

Ethanol, clonidine, antiepileptic tools reinforce psychological impact promethazine on the central nervous system.

MAO inhibitors (co-administration is not recommended) and derivatives fenotiazina risk of arterial hypotension and extrapiramidale disorders. Quinidine increases the likelihood of the cardiodepressive actions promethazine.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in the dark, inaccessible to children at temperature from 15 ° to 25 ° C. Shelf life – 5 years.