Neosinephrine-PIC - instructions for use, doses, side effects, contraindications

Phenylephrine is a non-selective a-adrenomimetic. Has a pronounced α-adrenomimetic activity. With topical application in ophthalmology causes the dilatation of the pupil, improves the outflow of intraocular fluid and narrows the vessels of the conjunctiva.

Phenylephrine has a pronounced stimulating effect on postsynaptic α-adrenoceptors, has a very weak effect on β-adrenergic receptors of the heart.

The drug has a vasoconstrictive effect, similar to the action of norepinephrine (noradrenaline), while it has virtually no chronotropic and inotropic effects on the heart. The vasopressor effect of phenylephrine is weaker than that of norepinephrine, but is more prolonged. Causes vasoconstriction after 30-90 seconds after instillation, duration 2-6 hours.

After instillation phenylephrine reduces the muscle dilating the pupil, and the smooth muscles of the arterioles of the conjunctiva, thereby causing a dilated pupil. Mydriasis occurs within 10-60 minutes after a single instillation and lasts for 2 hours. Mydriaz, caused by phenylephrine, is not accompanied by cycloplegia.

Pharmacokinetics:

Phenylephrine easily penetrates the tissues of the eye, the maximum concentration in the plasma occurs 10 to 20 minutes after topical application. Phenylephrine is excreted by the kidneys in unchanged form (<20%) or in the form of inactive metabolites.

Indications:

- Iridocyclitis (for prevention of the appearance of posterior synechia and reduction of exudation from the iris);

- dilated pupil in ophthalmoscopy and other diagnostic procedures necessary to monitor the state of the posterior segment of the eye (including in the postoperative period); Conducting a provocative test in patients with a narrow anterior chamber angle profile and suspected closure angle glaucoma;

- differential diagnosis of superficial and deep injection of the eyeball.

Contraindications:

- Hypersensitivity to the components of the drug;

- narrow-angle or angle-closure glaucoma;

- arterial hypertension, ischemic heart disease, aortic aneurysm, atrioventricular blockade of I-III degree, arrhythmia;

- tachycardia;

- Type I diabetes mellitus in history;

- a constant intake of monoamine oxidase inhibitors, tricyclic antidepressants, antihypertensive drugs;

- additional mydriasis during surgery in patients with impaired integrity of the eyeball, as well as in violation of tear production;

- hyperthyroidism;

- hepatic porphyria;

- congenital deficiency of glucose-6-phosphate dehydrogenase;

- pregnancy;

- the period of breastfeeding;

- rhinitis;

- age up to 12 years;

- elderly age.

Carefully:

In patients with type 2 diabetes mellitus because of the increased risk of high blood pressure.

Due to the fact that phenylephrine causes hypoxia of the conjunctiva - in patients with sickle cell disease, with contact lenses, after surgical interventions (decreased healing).

At a cerebral atherosclerosis, long-term existing bronchial asthma.

Pregnancy and lactation:

Application during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

In adults and children over 12 years of age to expand the pupil in the conduct of diagnostic procedures - 1 drop of 5% solution once, if necessary (to maintain mydriasis), it is possible to re-instillation after 1 h.

With insufficient expansion of the pupil, as well as in patients with a rigid iris for diagnostic dilatation of the pupil, a 10% solution can be used in the same dose.

For diagnostic procedures:

- as a provocative test in patients with a narrow angle profile of the anterior chamber

and suspicion of a closed-angle glaucoma is buried 1 drop 5% solution of the drug once. If the difference between the values of intraocular pressure before instillation of the drug and after dilating the pupil is from 3 to 5 mm Hg. the provocative test is considered positive;

- for differential diagnosis of the type of injection of the eyeball - 1 drop of 5% or 10% of the solution of the drug is instilled once: if 5 minutes after instillation there is a narrowing of the vessels of the eyeball, then the injection is classified as superficial. If the redness of the eye is preserved, the patient should be carefully examined for the presence of iridocyclitis or sclerite, as this indicates the expansion of more deeply lying vessels.

With iridocyclitis, to prevent the development and rupture of the already formed posterior synechia and to reduce exudation into the anterior chamber of the eye, a drop of 5% or 10% solution of the drug is digested into the conjunctival sac of the diseased eye 2-3 times a day 5-10 days depending on the severity of the disease.

When preparing patients for surgical interventions to achieve mydriasis - single instillation of 5% or 10% solution for 30-60 minutes before surgery (after autopsy shells of the eyeball re-instillation of the drug is not allowed).

Side effects:

Local

Conjunctivitis, keratitis, periorbital edema, pain in the eye, burning during instillation; lacrimation, blurred vision; irritation of the eye; a feeling of discomfort in the eye; increased intraocular pressure, blocking the angle of the anterior chamber (with a narrowing angle), allergic reactions, reactive hyperemia (after drug withdrawal).

Phenylephrine may cause a reactive miosis the next day after application. Repeated instillations of the drug at this time may give less pronounced mydriasis than the day before.

Due to a significant reduction in the pupil dilator under the influence of phenylephrine, in 30-45 minutes after instillation in the moisture of the anterior chamber of the eye, pigment particles from the iris pigment sheet can be detected. The suspension in the chamber moisture must be differentiated with the manifestations of anterior uveitis or with the ingress of the formed elements of blood into the moisture of the anterior chamber.

System

Contact dermatitis.

From the cardiovascular system:

tachycardia, increased blood pressure, reflex bradycardia, coronary artery occlusion, pulmonary embolism. When using a 10% solution (in elderly patients with diseases of the cardiovascular system) - ventricular arrhythmias, myocardial infarction.

From the side of the central nervous system:

headache, vomiting, tremor, insomnia, weakness.

Overdose:

Symptoms of overdose are anxiety, nervousness, dizziness, sweating, vomiting, tachycardia, weak or shallow breathing.

When a systemic effect of phenylephrine occurs, it is possible to quench unwanted effects by using α-blockers, for example, 5 to 10 mg of phentolamine intravenously. If necessary, the injection can be repeated.

Interaction:

The mydriatic effect of phenylephrine is enhanced when used in combination with topical application of atropine. Because of the increased vasopressor effect, tachycardia can develop.

The use of phenylephrine within 21 days after discontinuation of patients with monoamine oxidase inhibitors and tricyclic antidepressants should be performed withcaution, since in this case there is the possibility of an uncontrolled rise in blood pressure.

The vasopressor effect of phenylephrine can also be potentiated when combined with tricyclic antidepressants, βadrenoblockers, reserpine, guanethidine, methyldopa, and m-holinoblokatorami.

Phenylephrine can potentiate the inhibition of cardiovascular activity during inhalation anesthesia as a result of increased myocardial sensitivity to adrenomimetics and the occurrence of ventricular fibrillation.

The use together with other adrenomimetics can increase the cardiovascular effects of phenylephrine.

The use of phenylephrine can cause weakening of concomitant antihypertensive therapy and lead to an increase in blood pressure, tachycardia.

Pre-instillation of local anesthetics can increase systemic absorption and prolong mydriasis.

Special instructions:

During treatment, contact lenses are not recommended.

Effect on the ability to drive transp. cf. and fur:

After applying the drug,due to a change in accommodation and the width of the pupil, it is possible to reduce visual acuity, therefore it is not recommended to drive and engage in activities requiring increased attention before it is restored.

Form release / dosage:Eye drops, 5%, 10%.

Packaging:

To 10 ml in polyethylene bottles-droppers with a screwing protective cap, equipped with a safety ring.

For 1 bottle-dropper along with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

In closed original packaging: 2.5 years.

After opening the bottle: 4 weeks.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001147

Date of registration:11.11.2011

The owner of the registration certificate:Ursafarm Artsnaymittel GmbHUrsafarm Artsnaymittel GmbH Germany

Manufacturer: & nbsp

URSAPHARM Arzneimittel, GmbH Germany

Representation: & nbspURSAFARM ARTSNAYMITTEL GmbH URSAFARM ARTSNAYMITTEL GmbH Germany

Information update date: & nbsp19.09.2015

Illustrated instructions

Instructions

Neosinephrine-PIC® (Neosinefrin-POS®)