1

PHARMACOLOGY – 3rd TOT

DRUGS THAT INFLUENCE PERIPHERAL INNERVATION

B. QUESTIONS ON GENERAL AND MEDICAL PRESCRIPTION

1. Pilocarpine hydrochloride:
Ointment 1%-5,0;
Films 0,0027

2. Aceclidine:
Amp. 0,2%-1ml,
ointment 3%-5,0,
non-dosage powder

3. Cytiton:
Amp 1 ml ; 2ml

4. Neostigmine:
Granules 60, 0;
tab/powder 0,015,
amp. 0,05%-1ml

5. Galanthamine bromhydrate:
Amp. 1%-1ml.
2

6. Paraoxon:

7. Atropine sulphate:
powder Tab 0,0005
Ampoules 1%-1ml
Ung 10%- 5,0
Drops 0,1%-5,0

8. Scopolamine bromhydrate:
“aeron”Nr 10 powder
ampoules 0,05%-1 ml
drops 1%-10 ml

9. Platyphylline hydrotartrate:
powder
Tab. 0,005
Supp- 0,01
Sol. 0,2%-1ml

10. Benzohexonium:
Sol. 0,5%-20 ml
Drops 1%-10ml
Tab. 0,1 or 0,25
Amp. 2,5%-1 ml s/c
3

11. Triperium iodide:

Flacon –0,1% -1ml or 1%- 10ml
Amp. –0,1% -1ml or 1%- 10ml

12. Suxamethonium:
Powder Amp. 2%-5ml i/v

13. Mellictine:
Tab. 0,02

14. Norepinephrine hydrotartrate:

Amp 0.2% - 1ml

15. Isoprenaline:
F(inhalation) 0.5%/1%-25ml/100ml
T(sublingual) 0.005/0.01
Amp 0.5%-1ml

16. Salbutamol:
Amp(inhalation) 0.1%-2.5ml
F(inhalation) 0.1%-2.5ml/5ml/10ml/50ml
Tab 0.002/0.004/0.006/0.007/0.008
Amp 0.1%-5ml
SR 0.04%-150ml
Aer 10ml
K(inhalation) 0.0001/0.0002/0.0004
4

17. Epinephrine hydrochloride:

Amp 0.1% - 1ml
Focal 0.1%-10ml

18. Phentolamine:
Tab 0.025

19. Propranolol:
Tab 0.01/0.02/0.04/0.08/0.16
Amp 0.25%-1ml ; 0.1%-1.5ml/5ml
K* 0.04/0.08
F(pie oft) 1%-5ml/10ml

20. Reserpine:
Tab 0.0001/0.00025
Amp 0.1%-1ml or 0.25%-1ml

21. Procaine:
Amp 0.25%/0.5% - 1ml/2ml/5ml/10ml/20ml ; 1%/2%-1ml/2ml/5ml/10ml

22. Benzocaine:
Tab 0.3

23. Lidocaine:
Amp 0.5%-5ml/10ml ; 1%-10ml ; 2%-2ml/10ml ; 10%-2ml
5

24. Armine:
Amp 0,01%-10 ml

25. Dopamine:
Amp 0.5%/1%-2ml or 0.5%/2%-10ml ; 4%-5ml
F 0.25

26. Phenylephrine:
Amp 1%-1ml
F 012%-15ml ; 1%-5ml ; 0.25%/2.5%-10ml

27. Prazosin:
Tab 0.0005/0.001/0.002/0.005

28. Dobutamine:
Amp 0.5%-50ml ; 1,25%-20ml ; 5%-5ml
F 0.25/0.53

29. Guanethidine:
Tab 0.025
F 5%-10ml

30. Dihydroergotoxine:
Tab 0.005/0.01
Amp 0.03%-1ml or 0.1%-1ml
F (po) 0.1%-10ml/50ml
6

31. Ephedrine hydrochloride:

Tab 0.002/0.003/0.025/0.05
Amp 1%-1ml or 5%-1ml
F(intranasal) 2%-10ml or 3%-10ml
Aer 20ml

32. Tetracaine:
Tab .0,05;
caps 0,1
ung 3%-15g ; ung ophthalmic 1%-10g

33. Trimecaine.

34. Bupivacrine:
Amp 0.25/ 0.5/ 0.75

35. Physostigmine salicylate:

Amp. 1%-10 ml

36. Metocinium iodide:

Tab. 0,002:
Ampoules 0,1%-1 ml s/c
7

37. Pirenzerpine:
Tab. 0,025 or 0,05 Amp. 0,01 or. 0,5%- 2 ml
38. Ipratropium bromide:
Spray 0,025%- 20 ml:
tab. 0,01

39. Trihexyphenidyl hydrochloride:

Tab. 0,001 Nr 50

40. Nebivolol:
Tab 0.005/0.01

41. Cizaprid:
Tab. 0,005; 0,01;
amp. 0,001%-1 ml

42. Trimedoxime:
Amp, Sol. 15%-1ml

43. Lobeline hydrochloride:

Amp. 1%-1ml; tab. 0,002
8

C. ADMINISTERED DRUGS USED IN (FOR):

PRESCRIPTION

1. Glaucoma
-pilocaroine
-aciclidine
-carbachol

2. atonia of the intestine and urinary bladder

-neostigmine
-physostigmine
-aciclidine

3. inhibition of the respiratory center

-lobeline
-lobesil
-citotine

4. residual phenomena of poliomyelitis

-neostigmine
-physostigmine
-galautamine

5. gastric ulcer
-pirenzepine
-ipratropium
-metacine

6. bronchial asthma seizure

-pirenzepine
-ipratropium
- metacine

7. intoxication with fly-agarics

-atropine
-homatropine
-scopolamine

GROUP 1439
9

8. research of the eye bottom

- neostigmine
- physostigmine
- galatamine

9. relaxation of skeletal muscles during intubation

-tubocurarine
-galamine
-pancuronium

10.biliary colic
-atopine
-homatropine
-scopolamine

11.hypertensive crisis
-trimetaphan
-decamethonium
-asamethonium

12.acute hypotension
-phenylephrine
-epinephrine
-norepinephrine

13.cardiac arrhythmia
-propranolol
-timolol
-nadolol

14.hypoglycemic coma
-epinephrine
-ephedrine
-norepinephrine
10

15.arterial hypertension
-prazosine
-terazosine
-doxazosine

16.anaphylactic shock
-epinephrine
-ephedrine
-norepinephrine

17.angina pectoris
-propranolol
-timolol
-nadolol

18.Pheochromocytoma
-propranolol
-timolol
-nadolol

19.vascular spasms
-prazosine
-terazosine
-doxazosine

20.infiltrative , peripheral and conjuctive anesthesia’s

-ledocaine
-procaine
-trelicaine

21.Endarteritis
-prazosine
-terazosine
-doxazosine
11

22.Rhinitis
-naphasoline
-tetrahydrozoline
-xelomethezdine

23.menace of spontaneous absorption

-adsorbine
-medicase
-carbosem

24.radiological diagnostics of gastrointestinal tract

-aprophenum
-arprenolum
-gastrosepine

25.Conjunctivitis
-phenylephrine
-ethylephrine
-mydodrine

26.controlled hypotension.
-trimetaphan
-decamethonium
-asamethonium

GROUP 1439
12

*LOCAL ANESTHESIA *

-Is condition that results when sensory transmission from local area of the body to the CNS is blocked
*CLASSIFICATION*

I.According to the origin

1. naturale : cocaine
2. synthetic : tetracaine , - procaine , -lidocaine
3. various : phenol, diphenylhydramine
II.According to the chemical structure
• Derivates of paraaminobenzoic acid:
– procaine
– tetracaine
– benzocaine
III.According to the activity
• very active : tetracaine
• active: lidocaine
• less active : procaine

IV.According to use
1. With superficial action :benzocaine , dicaine , lidocaine

2. for infiltrative anesthesia: procaine

3. for Rachyanesthesia (Peridural )

-occurring or applied about the dura mater sofcaine, lidocaine
4. All type of anesthesia : lidocaine, trimecaine
13

*MECHANISM OF ACTION*
• Blocks the sodium channel
-Wide ranging effects on the nervous system

• Local anesthetics blocks the channel from the intracellular side

-Must enter the neuron to work

-increased lipophilicity is associated with increased potency

-Increased un-ionized fraction increases potency

-The un-ionized molecule crosses the cell membrane

-Adding bicarbonate increases the un ionized fraction

• Tetrodotoxin binds the sodium channel from the outside

 LA often combined with vasoconstrictors to extend duration of action (also to minimize bleeding)

• Local anesthetics activity is strongly PH-dependent, being increased at alkaline PH and vice versa.

*SIDE EFFECTS:
• -tremor
• -euphoria
• -heart depression
• -vasodilatation
• -tachycardia
• -convulsion
• -respiratory depression
• -hypotension
• -hypersensitivity reaction (allergic, anaphylactic reaction)
14

*ASTRINGENTS: *
• any of a group of substances that cause contraction or shrinkage of tissues & that dry up secretions

• Classification:
- Organic astringents (Tanninum)
- Non-organic astringents (Plumbi acetas, Alumen), Used to reduce swollen mucous membranes
that result from inflammations or to stop bleeding.

*ADSORBENTS: *

• A drug, usually a powder, capable of attaching other substances to its surface without any chemical
action , administered to adsorb gases, toxins and bacteria in the stomach and intestines. Examples
include activated charcoal and medicas E.

*Mucilagines (coating drugs):*

• any solution of a thick and adhesive nature, resembling in its appearance the solutions of gum.
• Mucilage of Starch
• used in: gastrointestinal inflammatory processes; associated to topical irritation agents.
• mucilages cover the mucous membranes and prevent irritation of the nerve endings.
• Mucilages does not exert resorptive action

*Counterirritants : *
• an agent used to produce an irritation in one part of the body intended to relieve irritation in some
other part.

• Drugs:
- Menthol
- Oleum Terebinthinae
- Solution Ammonii Caustici
- capsaicin from chili peppers
15 Cholinoblockers
*Mechanism of drug action

-Cholinoblockers are competitive antagonists to acetylcholine on cholinergic receptors, thus

blocking the effect of the parasympathetic nervous system
-due to no parsympathetic innervation of vascular smooth muscle (vasodilation is due to
circulating acetylcholine))

*Cholinoblockers (CB) Classification*

-
 1) M, N CB (CENTRALS)
trihexyphenidyl
*  3) M. CB

a) naturals
- denezine
- atropine
- benactisine
- scopolamine
- homatropine
 2) M,N CB (PERIPHERALS)
- adiphenine
b) synthetics
- aprophenum
- metacine
- arprenolum
- pirenzepine
- gastrosepine
- ipratropium
- fubraphoniu
- tropicamide
- troventol
4) N-CB
A) GANGLION-BLOCKNG DRUGS
- trimetaphan - dimechine
- hexamethonium - triperium iodide
- decamethonium
- asamethonium
- cwateron
16

B) NEUROMUSCULAR-BLOCKING DRUGS

1) non depolarizing drugs:

- tubocurarine
- pancuronium
- pipecuronium
- melicitine
- gallamine

2) depolarizing drugs:
-suxamethonium

3) mixed:
- dioxonium
17

*Effects of Anticholinergic Drugs

 CNS stimulation followed by depression
 Tachycardia
 Bronchodilation and decrease respiratory secretions
 Antispasmodic effects in GI system
 Eyes (increase intraoculary pressure, cycloplegya, midriasis).

*USES
 GI disorders – peptic ulcer disease, gastritis, increased gastric acid secretion – relax
gastric smooth muscle (replaced by newer drugs)
 Genitourinary – anti-spasmodic – urgency
 Excessive secretions
 Ophthalmology – relax eye for exam
 Respiratory disorder – asthma or bronchitis – inhaled form only
 Cardiac disorders – bradycardia or heart block
 Parkinson’s disease

*SIDE EFFECTS
 Hyperthermia,
 hot, dry flushed skin,
 dry mouth,
 tachycardia,
 delirium,
 paralytic ileus
 urinary retention
18

* ATROPINE - GENERAL INFORMATION *

- found naturally in nightshade (“atropa belladonna”)
• Clinical uses
- treatment of irreversible cholinesterase inhibitor poisoning
- treatment of bradycardia
- treatment of spasms of the GI tract
- supplement to anaesthesia (by reduced exocrine gland secretions)
• Side effects
- midriasis (due to relaxation of the pupillary sphincter)
- cycloplegia (due to relaxation of the ciliary muscle leading to inhibition of accomodation)
- urine retention (due to relaxation of the detrusor muscle)
- dry mouth (due to inhibition of salivation)
- dry skin (due to inhibition of sweating)
*Muscarinic antagonism - - used in the renaissance

*SCOPOLAMINE*
• General information
- found naturally in thorn apple (“datura stramonium”),
Lipophilic, thus may cross the blood-brain barrier
• Clinical uses
- same as atrophine
- treatment of motion sickness (“antiemetic effect”)
• Side effects
- sedation (due to CNS depression)
19

 Intoxication with M -Cholinoblockers

*Symptoms:
mydriasis, photophobia ,dry skin, hyperthermia ,hyperemia ,dry mouth ,hydrophobia change
of the voice coma ,anuria and olygouria ,convulsions ,dysphagia ,tachycardia ,muscle atonia
constipation ,dry eyes hallucinations
*Treatment:
• to transfer the patients in a cold room
• to wash out a stomach
• tranqiulisators
• antidotes : anticholinesterases: neostigmine, galantamine
• catheterization
20

 NEUROMUSCULAR BLOCKING AGENTS.

*Classification after duration of action

• Short (5-10 min.)
suxamethonium
• Medium (20-50 min)
tubocurarine, anatruxonium, melictine, pipecuronium, pancuronium, diplacine.
• Long (over 60 min)
anatruxonium, pipecuronium, pancuronium (in high doses)

NON-DEPOLARIZING - drugs that competitively inhibit nicotinic receptors at the

neuromuscular junction, thus causing flaccid muscle paralysis (however, they do not block
the awareness of pain

*Reversal of Blockade:
• The action of NON-DEPOLARIZING Drugs is reversed by increasing the concentration
of normal transmitter at the receptors.
• This is best accomplished by administration of cholinesterase inhibitors such as
neostigmine or pyridostigmine.
TUBOCURARINE - GENERAL INFORMATION
- onset: 5-10 minutes, duration: 1-2 hours
- found naturally in curare (“south american indian arrow poison”)
• Medical uses
- supplement to anaesthesia (by skeletal muscle paralysis)
• Side effects
- hypotension (due to inhibition of ganglion type nicotinic receptors)
- bronchoconstriction (due to histamine release from mast cells due to its strongly basic
character)
21

*DEPOLARIZING DRUGS:
• - are nicotinic receptor agonists
• Mecanism of action
A) bind to the active site, thus triggering an initial depolarization leading to initiation of
an action potential and following muscle twitches
B) however, they remain bound to the receptor due to inability of acetylcholinesterase
to degrade them, thus causing inability
*Pharmacokinetics:
• These drugs are hydrolyzed by pseudocholinesteraze and have a T0,5 of a few minutes in
persons with normal plasma cholinesterase.
• Approximately one in 2500 individuals produces a genetically determinated form of
abnormal cholinesterase.
*Reversal of Blockade:
• Such drugs have no antagonists. It is possible to use a fresh blood that contains
butyrilcholineserase.
SUXAMETHONIUM - GENERAL INFORMATION
- onset: immediately, duration: 10 minutes
• Medical uses
- supplement to anaesthesia (by skeletal muscle paralysis)
• Side effects
- bradycardia (muscarinic agonist effect)
- cardiac dysrythmias (due to muscle denervation leading to nicotinic receptor spread
outside the neuromuscular junction, continuous depolarization, continously opened k+
channels, and continuous leakage of k+ out of the skeletal muscle fibers)
- increased intraoccular pressure (due to simultaneous contraction of extraoccular
muscles)
 therapeutic uses of neuromuscular blocking agents
-Adjuvant in surgical anesthesia
-Orthopedic procedures for alignment of fractures
-To facilitate intubations – use one with a short duration of action
-In electroshock treatment of psychiatric disorders
22

*DRUGS ACTING ON AUTONOMIC GANGLIA

drugs acting on autonomic ganglia act both on the sympathetic- and parasympathetic
autonomic nervous system, thus giving very complex effects in the body.

*Classification after duration of action*

• Short action (10-20 min)
-trepirium, trimetafan
• Medium action (2-4 h)
-Hexamethonium, azamethonium, cvateron
• Long action (4-6-12 h)
-pempidine, dimecoline, trimetidine, temechine

*GANGLION BLOCKERS
• are ganglion-type nicotinic receptor competitive pharmacologic antagonists
• through there is evidence that they can also block the nicotinic channel pore.
• (Both sympathetic and parasympathetic divisions are blocked)

*EFFECTS:
– Vasodilatation and hypotension
– Tachycardia
– Relaxation of the smooth muscles and contraction of the sphincters
– Hyposecretion
– Mydriasis
– Increase of intraoculary pression
– Paralyses of accommodation (cycloplegia)
23

*Indications:
• hypertension crises, for the treatment of hypertension,
• malignant hypertension,
• to produce controlled hypotension in anesthesia,
• lungs edema,

*Side effects:
• collapse, postural hypotesion
• atonia, constipation
• mydriasis, blurred vision
• increase of intraoculary pression
• paralyses of accommodation (cycloplegia)
• urinary retention
• tolerance
• respiratory depression
• convulsions
• hyposecresion, dry mouth

*Pharmacokinetics:
• lipid-soluble drugs,
• inactive orally,
• short half-life.
• used intravenously.

*TRIMETAPHAN
Clinical uses
• - emergency treatment of malignant hypertension (by vasodilation)
• - supplement to anaesthesia (minimizes bleeding due to vasodilation)
 *Drug Acting On PNS*
24
-cholinomimetic and anticholinesterasic drugs-

CLASSIFICATION OF CHOLINOMIMETICS
1.With direct action

*M-N CHOLINOMIMETICS
- Acetylcholine chloride
- Carbachol
- cisapride

*M- CHOLINOMIMETICS
- Pilocarpine hydrochloride
- Aceclidine

*N-CHOLINOMIMETICS
- Lobeline
- Lobesil
- Tabex
- Anabazina hydrochloride
- Citizina (cititon)
- Gamibazina

2. With indirect MN cholinomimetics

(inhibits the hydrolysis of endogenous Ach )

a) with reversible action b) with irreversible action

- Neostigmine(prozerine)
*organophosphate agents
- physostigime(ezerine)
- Armin
- Galantamine
- Paraoxon(phosfacol)
- Pyridostigmin bromide
- Eserine *organophosphates substances (non-drug)

- aminostigmine - insecticides
- pesticides
- distigmine bromide (ubretid)
- ambenoniu (oxazil) *organophosphates substances used with military
- amiridin purposes
- sarin
25 *Cholinoblockers (CB) Classification*
 1) M, N CB (CENTRALS) *  3) M. CB
- trihexyphenidyl
- denezine a) naturals
- benactisine - atropine
 2) M,N CB (PERIPHERALS) - scopolamine
- adiphenine
- aprophenum - homatropine
- arprenolum
- gastrosepine b) synthetics
- fubraphoniu
- metacine
- pirenzepine

4) N-CB - ipratropium

A) GANGLION-BLOCKNG DRUGS - tropicamide

- trimetaphan - troventol
- hexamethonium
- decamethonium
- asamethonium
- cwateron
- dimechine
- triperium iodide

B) NEUROMUSCULAR-BLOCKING DRUGS

1) non depolarizing drugs:

- tubocurarine
- pancuronium
- pipecuronium
- melicitine
- gallamine

2) depolarizing drugs:
-suxamethonium

3) mixed:

GROUP 1439
26
Adrenomimetics (AM)
- dioxonium
*
**CLASSIFICATION ACCORDING TO THE SITE OF ACTION**
*drugs with direct action on the receptor of the postsynaptic membrane
- adrenomimetics:
- norepinephrine
- phenylephrine
- dobutamine
- adrenoblockers
-phentolamine
-propranolol
*drugs with presynaptic action “acting on release and/or storage of noradrenaline ”
- indirect sympathomimetic or adrenomimetics drugs
- ephedrine
- tyramine
- sympatholytics
- reserpine
- guanethidine sulphate
27

**CLASSIFICATION OF ADRENOMIMETICS**
A. alpha + beta ADRENOMIMETICS

1.direct action
- Epinephrine (adrenaline hydrochloride)
- Norepinephrine (noradrenaline hydrochloride)
- Dopamine
2.indirect action(sympathomimetics)
-Ephedrine hydrochloride

B. alpha ADRENOMIMETICS

1.with peripheral action

*alpha-1 *alpha-2
-phenylephrine (mezaton) - naphazoline
-ethylephrine (fetanol, efortill) - xylometazoline hydrochloride
-metoxamne
-methoraminol
2.with central action

*alpha-1
- clonidine hydrochloride
- alfa-methyldopa
C. Beta - ADRENOMIMETICS

*1.1+ 2-AM
- isoprenaline
- orciprenaline sulphate

*2.1-AM
-dobutamine hydrochloride
-dopamine (middle dose)

*3.2-AM
-terbutaline sulphate
- salbutamol (ventolin)
- fenoterol
- hexoprenaline
- ritodrine
28

**CLASSIFICATION ACCORDING TO THE CHEMICAL STRCTURE**

A.catecholamines
1.natural
*of animal origin
- epinephrine
- norepinephrine

*of vegetal origin

- ephedrine

2.synthetic
- phenylephrine
- ethylephrine

B.non-catecholamines
- naphazoline
- xylomethazoline
- oxymethazoline

GROUP 1439
29
Adrenoblockers
A. a - adrenoblockers
*
(α -receptor competitive antagonists)

1.nonselective (α 1+ α 2)

a)hydrogenated derivates of ergo alkaloids

- dihydroergotamine
- dihidroergotoxine
-nicergoline (sermion)

b)synthetic

-phenoxybenzamine
-phentolamine
-butiroxan
-tropodiphen (tropafen)
-proroxan(pyroxan)

2.selective (α 1)
-prazosin
-doxazosin
-terazosin
-alfuzosin
-tamsulosin (α 1A) (omnic)
-indoramin

3.selectve(α 2)
-yohimbine
30

B .  - adrenoblockers
( - receptor competitive antagonists)

1.nonselective (B1+B2)without intrinsic sympathomimetic activity (ISA)

-propranolol
-timolol
-nadolol
-sotalol

2.nonselective (1+2) with (ISA)

- alprenolol
- oxprenolol
- pindolol

3.selective (1) without (ISA) – (cardioselective)

-atenolo
-metoprolol
-talinolol
-betaxolol
-bisoprolol

4.selective (1) with (ISA)

-acebutolol
-practolol

5.supraselective (1) – (3rd generation)

-nebivolol (nebilet)
31

C. α, β-adrenoblockers

-labetolol
-proxodolol
-carvedilo

D. Acting on multiple receptors

-urapadil (α1,2 and 5-HT)

-chlorpromazine
-haloperidol
-levomepromazine

E. Sympatholytic

**central acting
-methyldopa

**peripherally acting
-guanethidine
-bretylium

**with central and peripheral action

-reserpine
32

F.Dopaminergic drugs

1. Dopaminomimetics
-dopamine
-levodopa
-apomorphine
-bromocriptine

2. Dopaminolytics

A) Neuroleptics
-chlorpromazine
-droperidol
-haloperidol
-sulpiride

B) anti-vomiting drugs
-metoclopramide (reglan, cerucal)
-domperidone
-dimetpramid
33
*LOCAL ANESTHESIA - CLASSIFICATION*
I.According to the origin
1. naturale : cocaine *
2. synthetic : tetracaine , - procaine , -lidocaine
3. various : phenol, diphenylhydramine

II.According to the chemical structure

• Derivates of paraaminobenzoic acid: – procaine
– tetracaine
– benzocaine

III.According to the activity

• very active : tetracaine
• active: lidocaine
• less active : procaine

IV.According to use
1. With superficial action :benzocaine , dicaine , lidocaine
2. for infiltrative anesthesia: procaine
3. for Rachyanesthesia (Peridural ) -occurring or applied about dura mater
sofcaine, lidocaine
4. All type of anesthesia : lidocaine, trimecaine