Phenylephine hydrochloride

Мезатон Drug photo

The description is actual on 23.12.2015

  • Latin name: Mesaton
  • ATH code: C01CA06
  • Active ingredient: Fenilefrin (Phenylephrine)
  • Producer: GNTsLS Experimental plant of Ltd company (Ukraine)

Structure

1 ml of eye drops contains 25 mg of Phenylephrinum (in the form of a hydrochloride) that in terms of 100% of substance – 25 mg. Decamethoxynum, a macrogoal, dinatrium edetat, the purified water are auxiliary.

1 ml of the solution intended for injections contains 10 mg of Phenylephrinum (in the form of a hydrochloride) and auxiliary connections: glycerin and injekts. water.

Release form

Eye drops on 5 ml in bottles droppers, and also other form of release – in the form of solution for injections which is issued in ampoules (volume of 1 ml) packed on 10 ampoules in the cardboard packs completed with the ampullary scarificator or the cutting ceramic disk.

Pharmacological action

Pharmacological group of drug: α-adrenomimetik. Besides, vasopressor action is characteristic of Mezoton.

Pharmacodynamics and pharmacokinetics

Phenylephine hydrochloride (MNN Phenylephrine) the known α-adrenostimulyator which has small influence on β-adrenoceptors, located in heart. Is not a catecholamine as has only one hydroxylic group in the aromatic kernel, it is capable to narrow arterioles and to increase the ABP that can lead to development of reflex bradycardia. In comparison with Norepinephrinum or Epinephrinum raises the ABP not so sharply and works is much longer because catechol-au-methyltransferase is affected more weakly. Therapy by the Phenylephine hydrochloride does not lead to increase in minute volume of blood. Drug shows vasopressor action, similar to noradrenaline, however, less expressed and longer, at the same time practically does not exert chronotropic and inotropic impact on heart.

After instillation the pupil dilator is reduced that causes its expansion, and unstriated muscles of arterioles of a conjunctiva. There is no impact on a tsiliarny muscle therefore the mydriasis is observed without tsikloplegiya.

The therapeutic effect comes right after in/in introductions and is observed for the next 5–20 minutes, at a hypodermic way of introduction — 50 min., intramuscular – 60-120 min.

Data on pharmacokinetics

Phenylephrinum is capable to get easily into eye tissues, expanding pupils within 10-60 min. Thanks to considerable reduction of the dilator pupils in 30-45 min. after instillation in moisture of an anterior chamber of an eye can be defined parts of a pigment of a leaf of an iris of the eye that demands differentiation of a uveitis or hit of uniform elements of blood in moisture of an anterior chamber.

The metabolism of Phenylephrinum occurs in a liver, and also a gastrointestinal tract (without participation of enzyme-catechol-au-methyltransferase)))))))))). Removal of metabolites is provided by kidneys.

Indications to use of the Phenylephine hydrochloride

Use in ophthalmology

  • iridocyclitis, front uveitis (treatment and prevention of emergence of back commissures, an asthenopia, reduction of exudation from an iris);
  • mydriasis for the purpose of diagnosis at the oftalmoskopiya and other procedures necessary for definition of a condition of back department of an eye, and also for laser interventions and vitreo-retinal surgery;
  • for carrying out provocative tests at people with a narrow profile of a corner of an anterior chamber of an eye and suspicion on closed-angle glaucoma;
  • differential diagnosis like eyeglobe injections;
  • reduction of a hyperemia and irritation at a syndrome of "a red eye";
  • complex treatment of a spasm of accommodation at children.

For parenteral use

  • arterial hypotension;
  • depressed case (including traumatic and toxic shock);
  • vascular form of insufficiency which can also arise at overdose by vazodilatator;
  • as vasoconstrictor of local anesthesia.

For intranasal use

Contraindications

  • pheochromocytoma;
  • hypertrophy at a subaortic stenosis;
  • fibrillation of ventricles;
  • hypersensitivity to components.

Use in ophthalmology is contraindicated:

  • at narrow or zakrytougolony angle glaucoma;
  • if there are considerable disturbances of cardiovascular system (including heart troubles, hypertensia, aneurisms, tachycardia);
  • at an insulin-dependent diabetes mellitus;
  • at a thyrotoxicosis, a hyperthyroidism;
  • existence of disturbances of integrity of an eyeground or dysfunctions of lacrimation, inborn deficit glyukozo-6-fosfatgidrogenazy, hepatic porphyria;

Mezoton's use with care is possible

  • at a metabolic acidosis;
  • at a hypercapnia;
  • at a hypoxia;
  • at fibrillation of auricles;
  • at arterial hypertension, and also hypertensia in a small circle of the blood circulatory system;
  • at a hypovolemia;
  • at a heavy stenosis of the mouth of an aorta;
  • at an acute myocardial infarction;
  • at a tachyarrhythmia and ventricular arrhythmia;
  • at an occlusal disease of vessels (including in the anamnesis): at an arterial thromboembolism, atherosclerosis, an obliterating thromboangitis (Thrombangiitis obliterans), a Raynaud's disease, tendency of vessels to spasms, and also at freezing injury, at a diabetic endarteritis, a diabetes mellitus, combined use of inhibitors of monoaminoxidase;
  • when using the general anesthesia (ftorotanovy), renal failures;
  • at advanced or children's age (≤ 18 years).

Attention! The phenylephine hydrochloride in the form of eye drops can be used in pediatrics — except for newborn children with small body weight.

Side effects

  • increase of the ABP;
  • fibrillation of ventricles;
  • heartbeat;
  • arrhythmia;
  • cardialgia;
  • bradycardia;
  • dizziness;
  • feeling of fear;
  • sleeplessness;
  • weakness;
  • concern;
  • headache;
  • paresthesia;
  • hematencephalon;
  • tremor;
  • spasms;
  • pale face skin;
  • local escharosis at hit in fabric;
  •  skin ischemia in an injection site;
  • allergic reactions.

Undesirable reactions from organs of sight when using in ophthalmology are possible

Burning, reactive hyperemia, sight zatumanennost, irritation, diskomofort, increase in intraocular pressure, dacryagogue, reactive miosis.

Application instruction of the Phenylephine hydrochloride (Way and dosage)

Drops eye are recommended to be used in the form of instillations: it is necessary to enter 1 drop into a conjunctival sac of an eye.

Intravenous or jet administration injekts. solution it is recommended to carry out slowly.

In a condition of a collapse

  • Ampoules the Phenylephine hydrochloride, the application instruction at intravenous drop administration: use 1 ml of 1% the solution divorced in 250 or 500 ml of 5 percent solution of a dextrose.
  • 0,1/0,3/0,5 ml of 1 percent solution should be parted in 20 ml of 5-percentage solution of a dextrose or 0,9 percent solution of sodium chloride. If there is a need — to repeat introduction.
  • Dosage at hypodermic or intramuscular use for adult patients — from 0,3 to 1 ml of 1 percent solution to 2–3 times a day; for children of 15 flyings (with arterial hypotension) at spinal anesthesia — from 0,5 to 1 mg on 1 kg of body weight of the child.

For the purpose of vasoconstriction in mucous membranes and for reduction of manifestations of the inflammatory phenomena

It is necessary to grease or dig in drug kontsentr. solution
— 0,125/0,25 / 0,5/1%.

For local anesthesia

It is recommended to add on 0,3–0,5 ml of 1 percent solution to 10 ml of solvent-anesthetic.

The maximum admissible dose for adults: one-time for hypodermic and intramuscular introduction — no more than 10 mg, daily — no more than 50 mg, for intravenous administration: the single dose makes up to 5 mg, a daily dose — 25 mg.

Attention!

For the purpose of prevention of repeated lowering of the ABP connected with drug withdrawal a dose reduce gradually, in particular — after carrying out long infusion. Infusions can be resumed if the sist was succeeded to lower. The ABP to 70–80 mm hg.

Overdose

Clinical picture

The ventricular ekstrasistoliya, short paroxysmal displays of ventricular tachycardia, "weight" of the head and extremities, essential increase of the ABP develops.

Treatment actions

In/in administration of α-adrenoblockers ((((((((((for example, Phentolamine). If disturbances of a cordial rhythm reasonablly use of β-adrenoblockers are observed..........

Interaction

Reactions of medicinal interaction are observed at a therapy combination with the following drugs:

  • With diuretics and anti-hypertensive means — the anti-hypertensive effect of diuretic and anti-hypertensive drugs decreases, for example: Guanadrela, Guanetidin, Methyldopums, Mekamilamina.
  • With fenotiazina, α-adrenoblockers ((((((((((Phentolamine) hypertensive influence decreases.
  • With MAO Inhibitors, for example, with Furasolidone, Procarbazinum, Selegilin, and also Oxytocin, ergot alkaloids, tricyclic antidepressants, Methylphenidate, adrenostimulyator – essential strengthening of pressor effect and an aritmogennost of Phenylephrinum is observed.
  • With β-adrenoblockers the cardiostimulating activity decreases, with Reserpinum development of the arterial hypertension arising at the expense of exhaustion of depot of the catecholamines localized in the adrenergic terminations that raises the answer to adrenomimetik is possible.
  • With inhalation anesthetics (Chloroform, Enfluran, the Halothane, Izofluran, Metoksifluran) the probability of heavy atrial, and also ventricular arrhythmia in connection with sharp increase in sensitivity of a myocardium to drugs — sympathomimetics increases.
  • With Ergometrine, Ergotamine, Metilergometrin, oxytocin, Doksapram — expressiveness of vasopressor influence increases.
  • With nitrates — their anti-anginal action decreases that, in an effect leads to decrease in pressor influence of sympathomimetics and risk of development of arterial hypotension.
  • To thyroid hormones there is a mutual potentsiation of effects and risk of coronary insufficiency that is aggravated at coronary atherosclerosis.
  • Mydriatic influence of Phenylephrinum increases under the influence of Atropine.

Terms of sale

The recipe is necessary (on Latin Recipe: Mesatonum).

Storage conditions

  • the protected place from rays of light;
  • temperature is no more than +25 °C.

Storage has to be made in the place, unavailable to juvenile children.

Period of validity

Till 3 flyings.

Period of storage of the drug Drop Phenylephine Hydrochloride for eyes differs and makes – no more than 2 years, the opened bottle dropper – till 2 weeks.

Special instructions

During therapy control of indicators of extremities of an ECG, the ABP, minute volume of a blood-groove, blood circulation in extremities and in an injection site is necessary.

The beginning and on the course of therapy of a depressed case correction of a hypoxia, a hypercapnia, hypovolemia and acidosis is necessary.

During use of the Phenylephine hydrochloride it is recommended to refrain from driving of the car, and other types of activity demanding high speed, motor and mental reactions, and also other dangerous types of activity (control of difficult mechanisms, work behind machines).

At pregnancy and a lactation

Therapy at respect for care is possible: only according to strict instructions and under supervision of the attending physician who objectively estimated a ratio of advantage and risks for mother, a fruit, future child. Besides, it is established that use of vasoconstrictors during patrimonial activity for correction of arterial hypotension, and also additives to anesthetics of local action against such drugs which are capable to stimulate sokratitelny ability of a uterus (for example: Vasopressin, Metilergometrin, Ergotamine, Ergometrine), can lead to permanent increase of the ABP in a puerperal period.

  • Irifrin of 2,5%, (the approximate price is from 450 rub);
  • Nazol kids spray, Germany (the approximate price is from 150 rub).

Responses

Responses of people are various, but the majority agrees in opinion that eye drops have too frequent manifestation of side reactions – discomfort, a sight zatumanennost. In respect of effectiveness of drug of opinion dispersed – part of patients praised and noted improvements, and some were forced to refuse the Phenylephine hydrochloride due to the lack of therapeutic effect.

The Phenylephine hydrochloride price where to buy

The average price of eye drops the Phenylephine hydrochloride of 5 ml – 25-40 rub, solution of 10 amp. — 44 rub.

Zdravzona

  • Phenylephine hydrochloride of 1% 1 ml No. 10 of amp. Opytny zavod GNTSLS, LLC
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Apteka24

  • Phenylephine hydrochloride eye drops of 2.5% 5mloz GNTsLS (Ukraine, Kharkiv)
  • Mezatonoz GNTSLS (Ukraine, Kharkiv)

Paniapteka

  • Phenylephine hydrochloride of hot-smoked 2.5% 5mloz GNTsLS
  • Phenylephine hydrochloride of hot-smoked 2.5% 5mloz GNTsLS

BIOSPHERE

  • Phenylephine hydrochloride of 1%/1 ml No. 10 solution for in.amp. OZ GNTsLS (Ukraine)
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Section: For eyes Cardiovascular
in more detail

Education: Graduated from the Nikolaev national university of V. A. Sukhomlinsky, gained the diploma of the specialist with honors as "An embryologist, a cytologist, a histologist". Also, the human physiology and animals, the teacher of biology" graduated from a magistracy majoring in ". The course on discipline "Pharmacology" is with honors passable.

Experience: Worked as the senior laboratory assistant of department of Physiology and biochemistry of the Nikolaev national university of V. A. Sukhomlinsky in 2010 - 2011.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use the Phenylephine hydrochloride surely consult with the attending physician.
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