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MINISTRY OF PUBLIC HEALTH OF UKRAINE

MINISTRY OF EDUCATION, SCIENCE, YOUTH AND SPORTS OF UKRAINE

SUMY STATE UNIVERSITY


3078 METHODOLOGICAL INSTRUCTIONS

for practical training

on the topic “DRUGS AFFECTING

PERIPHERAL AND CENTRAL NERVOUS SYSTEM”


in Pharmacology course

for foreign students

of speciality 7.110101 «Medical science»

full-time training


Sumy

Sumy State University

2011

Methodological instructions for practical training on the topic “Drugs affecting peripheral and central nervous system” / compiler A.A. Kachanova. – Sumy : Sumy State University, 2011. – 46 p.


Biological chemistry and pharmacology departmentThematic Module “Drugs Affecting Peripheral Nervous System”


Drugs Affecting the Afferent Innervation


Topical questions


  1. The classification of drugs affecting the afferent innervation.

  2. The classification of local anesthetics according to chemical structure.

  3. The types of local anesthesia. Primary use of local anesthetics for this or that type of local anesthesia.

  4. The mechanism of action of local anesthetics.

  5. Expediency of combination of local anesthetics with adrenoceptor agonists.

  6. The comparison characteristics of local anesthetics: duration of anesthesia, clinical use, influence on the central nervous system and internals, biotransformation in organism, and side effects.

  7. Astringent drugs: classification, mechanism of action, local effects, and clinical use.

  8. The characteristic of covering drugs and adsorbents: mechanism of action, local effects, and clinical use.

  9. Irritant drugs: mechanism of action, effects, and clinical use.
^

Tasks for prescription


Prescribe the following drugs and list the indications for their use:


  1. Novocaine (procaine) in ampoules for different types of anesthesia.

  2. Anesthesin (benzocaine) in suppositories, powders for internal use, in ointment.

  3. Lidocaine in ampoules for different types of anesthesia.

  4. Trimecaine in ampoules for different types of anesthesia.

  5. Tannin in ointment and in solution for the gastric lavage at a poisoning.

  6. Bismuth subnitrate in tablets, ointment and powders for external use.

  7. Activated charcoal (Carbo activatus) in tablets and non-dosage powders for internal use.

  8. Menthol in alcoholic solution and in ointment.


^ Table 1 – Drugs for prescription


Drug name

Single dose and mode of administration

Drug product

Anaesthesinum

Orally 0.3 g

through rectum 0.05–0.1 g;

on the skin 5–10% ointment

Powder;

tablets 0.3 g;

suppositories 0.05 and 0.1 g;

5% ointment

Novocainum

For infiltration anesthesia 0.25-0.5% solution;

for conduction anesthesia 1–2% solution;

for permeation anesthesia 10–20% solution and 5–10% ointment;

through rectum – suppository containing 0.1 g



Ampoules 0.25% and 0.5% solution – 1, 2, 5, 10 and 20 ml; 1% and 2% solution – 1, 2, 5, and 10 ml;

bottle 200 or 400 ml of 0.25% or 0.5% solution;

suppositories 0.1 g;

5% and 10% ointments

Trimecainum

For infiltration anesthesia – 0.125%, 0.25% or 0.5% solution;

for conduction anesthesia – 1–2% solution;

for permeation anesthesia – 2–5% solution;

for epidural anesthesia –
1–2% solution;

for spinal anesthesia – 5% solution

Ampoules 10 ml of 0.25% solution; 2, 5, or 10 ml 0.5% or 1% solution; 1, 2, 5, or
10 ml 2% solution;
1 or 2 ml 5% solution

Lidocainum

For infiltration anesthesia –0.25% or 0.5% solution;

for conduction anesthesia – 0.5–2% solution;

for permeation anesthesia – 1–5% solution


Ampoules 10 or 20 ml of 1% solution; 2 or 10 ml of 2% solution; 2 ml of 10% solution

Table 1 continuation

Tanninum

For oral, nasal, a pharyngeal rinsing, and throat gargling – 1–2% water or glyceric solutions;

for application on injured surfaces – 3–10% solution or ointment;

for gastric lavage – 0.5% solution

There are no made forms at the plant. Pharmacist prepares these forms (the prescriptions can be written in short or full forms)

Bismuthi subnitras

Orally – 0.25–0.5 g;

on the skin – 5–10% ointment and aspersion

Powder;

tablets 0.25 or 0.5 g; 10% ointment

Carbo activatus

Orally – 1–2 g for meteorism;

20–30 g (in the form of suspension in water) for poisonings

Powder;

tablets 0.25 or 0.5 g

Mentholum

For applying on the skin – 0.5–2% alcoholic solution, 1% ointment;

sublingually – 2–3 drops of 5% alcoholic solution (on a slice of sugar)

1%, 2% or 5% alcoholic solution;

1% ointment



Cholinomimetics. Cholinesterase Inhibitors


Topical questions


1. The types of efferent nerves. The peculiarities of structure and physiology of vegetative nervous system.

2. The structure and work of cholinergic synapse. Different types of cholinoceptors and their localization.

3. The classification of cholinergic drugs depending on their influence upon different types of cholinoceptors.

4. Direct M-, N-cholinomimetics: mechanism of action, pharmacological effects, peculiarities of pharmacokinetics, clinical applications, adverse effects.

5. Cholinesterase inhibitors: drugs classification, mechanism of action, pharmacological effects, peculiarities of pharmacokinetics, clinical applications, adverse effects. The symptoms and treatment of poisoning with cholinesterase inhibitors. Mechanism of action of cholinesterase regenerators; peculiarities of their use.

6. M-cholinomimetics: mechanism of action, pharmacological effects, peculiarities of pharmacokinetics, clinical applications, and adverse effects. The comparison characteristics of pilocarpine and aceclidine.

7. N-cholinomimetics: mechanism of action, pharmacological effects, peculiarities of pharmacokinetics, clinical applications. The toxicology of nicotine. The treatment of nicotine abuse.

Situational tasks in pharmacodynamics and pharmacokinetics


1. An eye was denervated. Describe the carbacholine effects on this eye.

2. An eye was denervated. Describe the proserin effects on this eye.

3. M-cholinoceptor antagonist was administered to animal. Describe the change in its blood pressure owing to the following acetylcholine administration.

4. M- cholinoceptor antagonist was administered to animal. Describe the change in its blood pressure owing to the following proserin administration.

5. The doctor has 3 preparations. All of them are miotic, reduce intraocular pressure, cause bradycardia, and increase glands secretion and tone of smooth muscles.

Two preparetions also have an ability to ease the neuromuscular transmission and transmission through autonomic ganglia. But one of them acts in full loss of function, while another – only in decreased function. What groups do these drugs belong to?

6. Patient with poisoning was hospitalized with the following symptoms: profuse sweating, myosis, nausea, vomiting, diarrhea, and bradycardia. Blood pressure is low. What is the cause of poisoning? Institute treatment for this patient.

7. The side effects in digestive system and in bronchi develop in patient suffering from myasthenia that is treated with proserin. What are these side effects? What drug should be administered for prevention of these side effects?

8. A patient suffers from glaucoma. What drugs may be used for reduction of intraocular pressure? Explain the mechanism of drugs action.

9. A patient suffers from myasthenia. Choose drugs for treatment of patient. Explain the mechanism of drugs action.


Tasks for prescription


Prescribe the following drugs and list indications for their use:


  1. Proserin in tablets, eye drops, and ampoules.

  2. Galantamine in ampoules.

  3. Pilocarpine in eye drops and eye ointment.

  4. Aceclidine in ampoules, eye drops, and eye ointment.

  5. Carbacholine in eye drops.

  6. Dipiroxim in ampoules.

  7. Lobeline in ampoules.

  8. Cytitonum in ampoules.


Fill in the following tables


Table 2 – Localization of cholinergic synapses and cholinoceptors


Synapses localization

^ Receptors localization

M-cholinoceptor

N-choliniceptor

Synapses of sympathetic and parasympathetic ganglia







Synapses of sympathetic fibers in adrenal medulla







Carotid bodies







Synapses of postganglionic parasympathetic fibers in innervated organs







Synapses of postganglionic sympathetic fibers in genital glands and vessels of skeletal muscles







Synapses of motor nerves in skeletal muscles







Synapses of central nervous system








Table 3 – Organs reaction upon the excitation of vegetative nerves


^ Organ, tissue, function

Change of function owing to excitation of

sympathetic nerve

parasympathetic nerve

Heart:

  • heart rate;

  • force of cardiac contraction;

  • automatism;

  • conductibility







Vessels







Smooth muscles:

  • bronchi;

  • gastrointestinal tract;

  • urinary tract;

  • biliary tract;

  • uterus;

- sphincters of GIT







Excretory glands activity







Eye muscles:

  • muscle – sphincter of pupil;

  • radial muscle;

- ciliary muscle








Table 4 – Comparison characteristics of M-cholinomimetics


Effect

Pilocarpine

Aceclidine

Reduction of intraoccular pressure







Increase of tone and peristalsis of intestine







Increase of tone and contractibility of uterus







Increase of secretion of excretory glands







Bradycardia







Indications for use








“+” – weak effect;

“++” – moderate effect;

“+++” – marked effect


Table 5 – Comparison characteristics of cholinesterase inhibitors





Physostigmine

Proserin

Galantamine

Armin

Mode of
administration













Duration of action













Indications for use













Symptoms of poisoning













Antidotes














Table 6 – Drugs for prescription


Drug name

Single dose and mode of administration

Drug product

Proserinum

Orally 0.01–0.015 g;

subcutaneously 0.0005 g;

in eyes 1–2 drops

Tablets 0.015 g;

ampoules 1 ml of 0.05% solution;

eye drops: 0.5% solution

Galanthamini hydrobromidum

Subcutaneously 0.0025–0.005 g

Ampoules 1 ml of 0.1%, 0.25%, 0.5% or 1% solution

Pilocarpini hydrochloridum

In eyes: 1–2% solution (1–2 drops) or eye ointment

Eye drops: 1% or 2% solution in bottles 5 or 10 ml;

1% or 2% eye ointment

Aceclidinum

In eyes: 2-5% solution (1–2 drops) or 3–5% eye ointment;

subcutaneously 0.002 g

2-5% solution of eye drops;

3% and 5% eye ointment;

ampoules 1 or 2 ml of 0.2% solution

Carbacholinum

In eyes 1–2 drops of 0.5–1% solution

Eye drops: 0.5% or 1% solution in bottles 5 or 10 ml

Dipiroximum

Subcutaneously, intramuscularly or intravenously 0.15–0.3 g

Ampoules 1 ml of 15% solution

Lobelini hydrochloridum

Intravenously slowly 0.005 g

Ampoules 1 ml of 1% solution

Cytitonum

Intravenously slowly 0.5 ml

Ampoules 1 ml

M-Cholinoceptor Antagonists


Topical questions

1. Types and localization of M-cholinoceptors. The effects of excitation of different M-cholinoceptors types.

2. Classification of М-cholinoceptor antagonists.

3. The mechanism of action of М-cholinoceptor antagonists.

4. Influence of М-cholinoceptor antagonists upon the eye.

5. Influence of М-cholinoceptor antagonists upon cardiovascular system.

6. Influence of М-cholinoceptor antagonists upon the smooth muscular organs (the gastrointestinal tract, bronchi, and urinary ways).

7. Influence of М-cholinoceptor antagonists upon the functions of excretory glands.

8. Central effects of М-cholinoceptor antagonists (influence upon CNS).

9. The comparison characteristics of М-cholinoceptor antagonists (peculiarities of atropine, scopolamine, platyphyllin, methacin).

10. Indication for application of М-cholinoceptor antagonists.

11. Adverse effects of М-cholinoceptor antagonists and contraindications to their use.

12. The symptoms and treatment of poisoning with М-cholinoceptor antagonists.


Situational tasks in pharmacodynamics and pharmacokinetics

1. An eye was denervated. Describe the effects of pilocarpine and atropine on this eye.

2. A child with poisoning was hospitalized with the following symptoms: tachycardia, marked mydriasis, dry mouth, agitation, and hallucinations. What substance is the cause of poisoning? Institute treatment for this child.

3. A patient suffers from spastic pain owing to urolithiasis. What drugs may be used for pain relief of spasm? Explain mechanism of drugs action.

4. A patient suffers from atrioventricular blockade. What drugs may be used for improving of conductivity?

5. A patient with ulcer disease suffers from hypersecretion and pain owing to pylorus spasm. Propose drugs for treatment of this patient. Explain the mechanism of drugs action.


Fill in the following table


Table 7 – Comparison characteristics of М-cholinoceptor antagonists effects


Effects

Drug

Atropine

Scopolamine

Platyphyllin

Methacin

Relaxation of bronchi













Decrease of bronchial and digestive glands secretion













Reduction of spasm of intestine, biliary and urinary tracts













Degree of
М-cholinoceptor antagonists action













Direct myotropic antispasmodic action













Tachycardia













Reduction of vestibular disturbances













Antiparkinsonian action













Mydriasis













Duration of paralysis of accommodation













Indications for use














“+” – weak action;

“++” – moderate action;

“+++” – marked action.

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