Laboratory class 13

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Date

Topic:TOXICOLOGICAL ASPECTS OF NEUROLEPTICS, TRANQUILIZERS AND LOCAL ANESTHETICS

APPLICATION. EXAMINATION OF THE BASIC CHLOROFORM EXTRACT FOR DERIVATIVES OF
1,4-BENZODIAZEPINE, PHENOTHIAZINE, P-AMINOBENZOIC ACID
Using the reference literature give a toxicological characteristic to the drugs that suppress the CNS and local anesthetics:
 neuroleptics (antipsychotic drugs) (derivatives of phenothiazine: chlorpromazine, diprazine, levomepromazine)
 tranquilizers (derivatives of 1,4-benzodiasepine: chlorodiazepoxide, diazepam, nitrazepam)
 local anesthetics (p-aminobenzoic acid derivatives).
To summarize the material is in the form of table (see Table 1).

Table 24 – Toxicological characteristics of neuroleptics, tranquilizers and local anesthetics

Prevention of an
Toxic and leathal Mechanism of the The main symptoms Treatment of a intoxication
Drugs
doses toxic action of an intoxication poisoning (factors that
increase toxicity)
1 2 3 4 5 6
1 2 3 4 5 6
 Table 25 – Chemical reactions for derivatives of 1,4-benzodiazepine, phenothiazine, p-aminobenzoic acid

Specificity
and
No. Method Observation Chemical reaction equation(s)
sensitivity of
the reaction
Derivatives of 1,4-benzodiazepine
Acidic hydrolysis
Method. Evaporate 2 ml of the chloroform extract to dryness in
a water bath. Add 5 ml of 6 M hydrochloric acid solution to the
residue and reflux the solution at 100 °C for 60 min. Cool the
hydrolyzate obtained, neutralize it with saturated sodium
hydroxide solution to adjust the pH to 7–9. Place the solution
into a separating funnel and extract the products of 1,4-
benzodiazepine hydrolysis (aminobenzophenones) with the
equal volume of chloroform. Filter the organic phase through
anhydrous sodium sulphate. Evaporate the extract to the
volume of 0.2 ml and examine.
Examination in UV light
1. Place a few drops of the extract on a chromatographic plate and
examine in UV light. Observe fluorescence.
Azo dye coupling reaction
Method. Apply a few drops of the extract on a piece of
chromatographic plate and treat the spot with 1 % sodium
2. nitrite solution, then with 2 M hydrochloric acid solution and Specificity:
-naphthol alkaline solution.
 Derivatives of phenothiazine (aminazine, levomepromazine)

The reaction with concentrated sulphuric acid Specificity:

Method. Place 4–5 drops of the chloroform extract
examined in a porcelain cup, evaporate chloroform to
dryness. Add a drop of concentrated sulphuric acid.
1.
Observe appearance of colour

The reaction with concentrated nitric acid Specificity:

Method. Place 4–5 drops of the chloroform extract
examined in a porcelain cup and evaporate chloroform to
2.
dryness. Add a drop of concentrated nitric acid. Observe
appearance of colour

The reaction with concentrated hydrochloric acid Specificity:

Method. Place 4–5 drops of the chloroform extract
examined in a porcelain cup and evaporate chloroform to
3.
dryness. Add a drop of concentrated hydrochloric acid.
Observe appearance of colour

Derivatives of p-aminobenzoic acid (procaine)

Azo dye coupling reaction Specificity:

Method. Apply the chloroform extract examined on a
piece of chromatographic plate, evaporate to dryness,
1. apply a drop of 2 M hydrochloric acid and a drop of 1 %
sodium nitrite solution, then treat the spot with a drop of
-naphthol alkaline solution. Observe appearance of
colour.