Dikain description according to gf. Dikain: instructions for use of eye drops

Dikain is a drug with the properties of a local anesthetic. It is mainly used in ophthalmology.

Release form and composition

The active substance of the drug is tetracaine.

Dosage forms of Dikain:

• Powder;
• eye films;
• Solutions with concentration active substance from 0.25 to 3%.

Indications for use

Dikain is a local anesthetic intended for terminal anesthesia. The anesthetic effect develops 30-90 seconds after Dikain is applied to the mucosal surface and persists for another 15-20 minutes.

According to the instructions for Dikain, the use of the remedy is shown:

• In some ENT diseases, when the patient requires surgery due to the need to remove polyps, puncture maxillary cavity, middle ear surgery, conchotomy;
• When performing short-term operations on the anterior segment eyeball, as well as manipulations associated with the removal of a foreign body from the eye, etc.;
• For anesthetizing the larynx during intubation (in general anesthesiology), as well as bronchography, esophago- and bronchoscopy procedures;
• For epidural (epidural) anesthesia;
• For anesthesia of the urinary tract before catheterization.

Contraindications

The instructions for Dikain indicate that the drug is contraindicated in persons with individual intolerance to its components, as well as children under 10 years old.

In ophthalmology, Dikain is not prescribed for keratitis.

Do not use the drug for people undergoing treatment with sulfonamides.

It is unacceptable to use Dikain as part of nasal drops.

With caution, the drug is used for:

• AV blockade;
• Violation of the heart rhythm;
• Decrease in the level of cholinesterase in the blood plasma;
• Shock.

Method of application and dosage

The drug is used mainly for terminal, rarely for epidural anesthesia. The substance is very toxic, so the solution is practically unsuitable for conduction and infiltration anesthesia. The highest dose at topical application- 0.1 grams.

In accordance with the instructions, in ophthalmic practice, Dikain is used in 2-3 drops. A strong analgesic effect develops after 1-2 minutes.

To achieve the desired anesthetic effect during eye surgery, as a rule, a 0.5% solution is sufficient. To prolong the action and enhance the effectiveness of the drug, a 0.1% solution of epinephrine is added to Dikain (at the rate of 3-5 drops per 10 ml of tetracaine).

For pain relief when measuring intraocular pressure, it is usually limited to a 0.1% solution.

In otolaryngology, in most cases, a solution of 0.25-0.5% is sufficient. Adult patients at the discretion of the doctor may be prescribed up to 3 ml of a 1% solution. 2 and 3% solutions are used only when absolutely necessary. Pulverization or lubrication of the larynx and pharynx is carried out gradually, maintaining intervals and monitoring the patient's condition. To reduce the overall response to the drug 30-60 minutes before anesthesia, the patient is given 0.1 grams of barbamyl.

In the absence of contraindications to the use of vasoconstrictors, epinephrine hydrochloride is added to Dikain (1 drop of a 0.1% solution for every 1-2 ml of tetracaine). A swab is impregnated with a solution and the surface of the mucosa is treated. Do not leave the swab in the nasal cavity for a long time.

The use of Dikain for epidural anesthesia requires caution. The preparation of a 0.25-0.3% solution is carried out under aseptic conditions, mixing Dikain with sterile water for injection and isotonic sodium chloride solution, a stabilized hydrochloric acid solution. Before use, the drug is sterilized by boiling for half an hour, after which a 0.1% solution of epinephrine hydrochloride is added to it at the rate of 1 cap. 5 ml solution for anesthesia. The agent is administered in stages - 15-20 ml. The interval between injections is 5 minutes.

For anesthesia of the urinary tract, up to 10 ml of a 0.1% solution of Dikain is used.

Side effects

With topical application of Dikain, mild symptoms are possible. allergic reactions, burning sensation, swelling after instillation.

Dikain is very toxic (10 times more toxic than novocaine, and 2-5 times more toxic than cocaine). Intoxication with the drug is manifested by anxiety, agitation, convulsions, cardiovascular insufficiency, respiratory disorders, nausea, vomiting, hypotension. In case of an overdose, the mucosa at the site of application should be washed (for this, an isotonic NaCl solution is used) and a caffeine preparation and / or another analeptic should be injected subcutaneously.

special instructions

If possible, novocaine should be used instead of Dicaine, as it is less toxic.

It is important to remember that solutions containing more than 2% tetracaine can damage the corneal epithelium and cause significant vasodilation of the conjunctiva.

Dikain can weaken the effect of sulfonamide drugs.

Since the agent is very quickly absorbed by the mucous membranes of the respiratory tract, extreme caution must be exercised when using it in ENT practice and the patient's condition should be carefully monitored. 4.92 Rating: 4.9 - 24 votes

Molecular formula. Ci5H24N202-HC1.

Relative molecular weight. 300.8.

Structural formula.

CH3(CHg)3NH-Q-COOCH2CH2N(CH3)2

Chemical name. 2-(dimethylamino)ethyl p-(butylamino)benzoate monohydrochloride; 2-(dimethylamino)ethyl 4-(butylamino)benzoate monohydrochloride; per.

CAS No. 136-47-0.

Synonyms. Amethocaine hydrochloride; dikain.

Description. White crystalline powder, odorless.

Solubility. Soluble in about 8 parts of water; soluble in ethanol (−750 g/l) TS; sparingly soluble in chloroform R; practically insoluble in ether R.

Storage. Tetracaine hydrochloride should be kept in a tightly closed container, protected from light.

Additional Information. Tetracaine hydrochloride is hygroscopic; it has a slightly bitter taste and causes local numbness of the tongue. Even in the dark, it gradually decomposes in a humid atmosphere, and the destruction accelerates with increasing temperature.

Tetracaine hydrochloride melts at about 148°C or can be in one of two polymorphic forms, one of which melts at 134°C and the other at 139°C. Mixtures of these forms melt in the range of 134-147°C.

REQUIREMENTS

General requirement. Tetracaine hydrochloride contains at least

98.0 and not more than 101.0% Сі5Н24^02-HC1 in terms of the dried substance.

Authenticity

A. Dissolve 0.2 g in 10 ml of water and add 1 ml of ammonium thiocyanate (75 g/l) TS. The precipitate is collected on a filter, recrystallized from water and dried for 2 hours at 80°C; melting point is about 131 °C.

B. A 20 mg/mL solution of the test substance gives reaction A, characteristic of chlorides, as described in General Identity Tests (vol. 1, p. 129).

Transparency and color of the solution. A solution of 0.20 g in 10 ml of carbon dioxide-free water R is clear and colorless.

sulfate ash. Not more than 1.0 mg/g.

Loss on drying. Dry to constant weight at 105°C; loss no more than 10 mg/g.

solution pH. The pH of a solution of the test substance in carbon dioxide-free water R at a concentration of 10 mg/ml is 4.5-6.0.

foreign impurities. Carry out the test as described in Thin Layer Chromatography (Vol. 1, p. 92), using silica gel R4 as the sorbent and a mixture of 80 volumes of dibutyl ether R, 16 volumes of hexane R, and 4 volumes of ice-cold as the mobile phase. acetic acid R. Place the plate in the chromatographic chamber, immersing it 5 mm into the liquid. After the solvent front reaches a height of about 12 cm, remove the plate from the chamber and dry it for several minutes in a stream of warm air. Allow the plate to cool and apply separately 5 µl of each of 2 solutions containing (A) 0.10 g of the test substance per ml and (B) 0.050 mg of 4-aminobenzoic acid R per ml. Allow the solvent front to rise 10 cm above the application line. After removing from the chromatographic chamber, the plate is dried for 10 min at 105°C and the chromatogram is evaluated in ultraviolet light (254 nm). Any stain that solution A gives, other than the main stain, should not be more intense than the stain that dart solution B produces. The main stain remains on the application line.

Quantitation. Carry out the test as described in Nitritometry (vol. 1, p. 153) using about 0.5 g of the test substance (accurately weighed) dissolved in a mixture of 50 ml of water and 5 ml of hydrochloric acid (-420 g/l ) TS, and titrate with sodium nitrite (0.1 mol/l) VS. Each milliliter of sodium nitrite (0.1 mol/l) VS corresponds to 30.08 mg of Ci5H24N202-HC1.

Synonyms

Amethocaine, Anethaine, Decicain, Felicain, Foncaine, Intercain, Medicain, Pantocain, Pontocaine hydrochloride, Rexocaine, Tetracaini hydrochloridum, Tetracaine hydrochloride.

Physical properties

White crystalline powder, odorless. Easily soluble in water (1:10), alcohol (1:6). The solutions are sterilized at +100 "C for 30 minutes; to stabilize the solutions, a solution of hydrochloric acid is added to pH 4.0 - 6.0.

Application

Dikain is used only for superficial anesthesia. Instead of dicaine, it is preferable to use less toxic local anesthetics(lidocaine, pyromecaine, etc.).

In ophthalmic practice, it is used in the form of a 0.1% solution when measuring intraocular pressure (one drop 2 times with an interval of 1-2 minutes). Anesthesia usually develops in 1-2 minutes. When removed foreign bodies and surgical interventions use 2 - 3 drops of 0.25 - 0.5 - 1% or 2% solution. After 1 - 2 minutes, severe anesthesia develops. It should be borne in mind that solutions containing more than 2% dicaine can cause damage to the corneal epithelium and significant vasodilation of the conjunctiva. Usually for anesthesia with surgical interventions on the eyes, it is enough to use a 0.5% solution. To lengthen and enhance the anesthetic effect, add 0.1% - a solution of adrenaline (3 - 5 drops per 10 ml of dicaine). With keratitis, dikain is not used.

In ophthalmic practice, if prolonged anesthesia is necessary, eye films with dicain (Membranulae orhthalmicae cum Dicaino) are used. Each film contains 0.00075 g (0.75 mg) of dicaine. The basis of the films is a biosoluble polymer.

Dikain is also used for surface anesthesia in otorhinolaryngological practice during some surgical interventions (puncture maxillary sinus, removal of polyps, conchotomy, middle ear surgery). Due to the rapid absorption of dicaine by mucous membranes respiratory tract great care should be exercised in its use and carefully monitor the patient's condition. Children under 10 years of age are not given anesthesia with dicaine. In older children, no more than 1 - 2 ml of a 0.5 - 1% solution is used, in adults - up to 3 ml of a 1% solution (sometimes a 0.25 - 0.5% solution is sufficient) and only if absolutely necessary - 2% or 3% solution. To a solution of dicaine (in the absence of contraindications to the use of vasoconstrictor substances), add 1 drop of a 0.1% solution of adrenaline hydrochloride per 1-2 ml of dicaine.

The highest doses of dicain for adults during anesthesia of the upper respiratory tract are 0.09 g once (3 ml of a 3% solution). Doses of dicaine should not be exceeded in order to avoid severe toxic effects. The literature describes cases of deaths associated with overdose and misuse of dicaine. Dikain is contraindicated in children under the age of 10 years and in the general serious condition of patients.

Features of work

When working with dicain, instruments and syringes should not contain alkali residues, since dicain precipitates in the presence of alkali.

Release forms

Powder and eye films with dikain (30 pieces in dispensers).

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See what "Dikain" is in other dictionaries:

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DICAIN- Dicainum. Synonyms: amethocaine, intercaine, pantocaine. Properties. White or white with a yellowish color, odorless crystalline powder, bitter taste. It causes a feeling of numbness on the tongue. Soluble in water (1:10), easily soluble in alcohol (1:6) ... Domestic veterinary drugs

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Authentication and Quantification of Dicaine Hydrochloride (Tetracaine Hydrochloride)

Authenticity reaction equations

• A) General reactions of esters of n-aminobenzoic acid having a substituted primary aromatic amino group
• - Secondary amines under the action of sodium nitrite form nitroso compounds:

An azo dye can also be obtained by adding a slightly acidic solution of an aromatic amine to a diazonium salt.

These reactions form the basis of the nitritometric method for the analysis of aromatic amines.

Condensation reactions. Aromatic amines enter into condensation reactions with 2,4-dinitrochlorobenzene, aldehydes and other substances. As a result of the interaction of amines with aldehydes, Schiff bases are formed - compounds painted in yellow or orange-yellow color.

Where R-FROM 4 H 9

• - Halogenation reactions. Substitution occurs in the ortho and para positions relative to the amino group. As a result of the bromination reaction, white or yellow precipitates are formed, and bromine water becomes decolorized.
• - Oxidation reactions. Under the action of various oxidizing agents, aromatic amines form indophenol dyes.
• - Reaction to the aromatic nitro group.

Under the action of alkali on a compound containing a nitro group, the color intensifies to yellow, yellow-orange or red as a result of the formation of an aci-salt.

• - Tetracaine hydrochloride from solutions is precipitated by potassium iodide in the form of hydroiodine salt
• - Under the action of ammonium isothiocyanate, isothiocyanate tetracaine precipitates, the melting point of which is 130-132 ° C
• - Tetracaine hydrochloride, when interacting with potassium iodate in a phosphoric acid medium, when heated, forms a violet-colored oxidation product with a light absorption maximum at 552 nm. The reaction is specific for qualitative and quantitative determination.
• B) Private reactions to tetracaine hydrochloride:

Tetracaine hydrochloride, after heating with concentrated nitric acid and adding potassium hydroxide solution to the residue, acquires a blood-red color. The reaction is based on its nitration and subsequent formation of a potassium salt of an orthoquinoid compound.

(Dicainum; syn.: Tetracaini Hydrochloridum, Amethocaine, Decicain, Felicain, Intercain, Medicain, Pantocain, Rexocaine and etc.; GF X, sp. A) is a local anesthetic. 2-Dimethylaminoethyl ether para-butylaminobenzoic to-you hydrochloride, C 15 H 24 N 2 O 2 -HCl:

White crystalline powder, odorless, soluble in water and alcohol, insoluble in ether.

By D.'s activity surpasses novocaine (see), cocaine (see), ksikain (see) and trimekain (see). Highly toxic (2-3 times more toxic than cocaine and 10-15 times more toxic than novocaine, xicaine, trimecaine). The drug is rapidly absorbed by the mucous membranes: anesthesia occurs in 1-3 minutes. and lasts 20-40 minutes. (depending on the concentration of the solution).

D. is used only for surface (in ophthalmology and otorhinolaryngology) and epidural (in surgery) anesthesia.

In ophthalmology, D. is used in the removal of foreign bodies and various surgical interventions in the form of 0.25; 0.5; 1 and 2% solution, 2-3 drops in the eye. Higher concentrations of the solution can cause damage to the corneal epithelium.

In otorhinolaryngology, the drug is used in some operations and manipulations (puncture maxillary sinus, conchotomy, removal of polyps, middle ear surgery, tonsillectomy) as 0.25; 0.5; one; 2 and 3% solution (no more than 3 ml); to lengthen and enhance the anesthetic effect, as well as to reduce the absorption of D., adrenaline (0.1% solution, 1 drop per 1-2 ml of D.) or ephedrine (2-3% solution) is added to its solutions. 1 drop per 1 ml solution D.). D.'s solution is impregnated with a tampon and the mucous membranes are lubricated with it. Lubrication or spraying of the pharynx and larynx is carried out at intervals, observing the patient's condition.

In surgery, D. is used for broncho- and esophagoscopy and bronchography in the form of a 2% solution; for epidural anesthesia - 0.3% solution in isotonic solution of sodium chloride; 15-20 ml are administered fractionally (5 ml each) with an interval of 5 minutes. Weakened patients and elderly people are administered no more than 15 ml. Only freshly prepared solutions are used (shelf life is no more than 2 days). Higher doses for adults: with anesthesia of the upper respiratory tract 0.09 g, or 3 ml of 3% solution (once), with epidural anesthesia - 0.075 g, or 25 ml of 0.3% solution (once).

When applying D. are often observed side effects and complications: pallor of the face, cyanosis, vomiting, dizziness, cold extremities, slow heart rate, weakening of cardiac activity and respiration, blurred vision, loss of consciousness, allergic reactions; there are cases of individual intolerance. At D.'s overdose the lethal outcome as a result of an apnea is possible. To reduce the overall reaction of the body to D., it is recommended to take 30-60 minutes in advance. before anesthesia, give the patient 0.1 g of barbamil. In case of D.'s intoxication, the mucous membranes are washed with a solution of sodium bicarbonate or isotonic solution of sodium chloride, caffeine-sodium benzoate is injected under the skin, other measures - depending on the picture of poisoning.

D.'s use requires great care. The drug is not prescribed for children under 10 years of age, with cardiovascular insufficiency, impaired liver and kidney function, bronchial asthma, keratitis.

Release form: powder. Store in a well-closed container.

Bibliography: Pryanishnikova H. T. and Likhosherstov A. M. Chemistry and mechanism of action of anesthetics, Zhurn. All-Union, chem. about them. Mendeleev, vol. 15, N° 2, p. 207, 1970, bibliography; Cherkasova E. M. et al. Advances in the chemistry of anesthetics (1961-1971), Usp. chem., v. 42, c. 10, p. 1892, 1973, bibliography; Wiedling S.a. T e g n e r C. Local anaesthetics, Progr, med. Chem., v. 3, p. 332, 1963, bibliogr.

H. T. Pryanishnikova.