Drugs affecting the afferent and efferent nervous system. Cholinergic drugs

LOCAL (REGIONAL) ANAESTHETICS
1. For Terminal (Superficial) Anaesthesia:
Cocaine Anaesthesine (Benzocaine)
Dicaine

According to the Chemical structure:
1. Esters of aromatic acids:
Natural

LAs are Weak Bases.
In order that a drug manifests its

+ Vasoconstrictor
Adrenaline hydrochloride 0.1% - 1 drop in 2-10 ml

Cocaine blockades:
Noradrenaline
Serotonin
Dopamine
reuptake into the Presynaptic Terminals.
?Dopamine in brain’s Pleasure System

COCAINE:
✶ POTENTIATES the action of Noradrenaline
✶ the «FIGHT OR FLIGHT» SYNDROME

Adverse Effects of COCAINE:

1. Anxiety Reactions:
?BP, ?HR, Sweating, Paranoia.
2. Depression Reactions
3.

Dicaine (Tetracaine) is used topically for:
∙ Eye Mucous Anesthesia

Novocaine => System Effects :

∙ ↓Acetylcholine Formation
∙ Block of the

For infiltration anesthesia:
Novocaine 0.25-0.5% - 200-1000 ml
For conductive

Lidocaine (amp 2%-10 ml; 10%-2 ml) -
a Local Anesthetic and

Astringents

1. Organic Compounds:
Tannin
Tannalbin
Oak Bark [Cortex Quercus]
Grass of st. Johns wort

2. Inorganic Compounds:
Bismuth subcitrate [DE-NOL]
Silver nitrate
Zinc oxide

Range of SHMIDEBERG: Pb, Al, Bi, Zn Cu, Ag, Hg

Left Part

ADSORBENTs:
TALC
WHITE CLAY ( Bolus Alba)
ACTIVATED CHARCOAL
IRRITATING AGENTS:
MUSTARD PLASTER

Mustard plaster
∙ Distracting action: Inflammation Zone on the skin =>

Validol – 25–30% Menthol solution
in Menthol Ether of Isovalerianic acid
✶

Cholinergic Drugs
Location of Muscarinic M-Receptors:
M1 – Gastric Parietal Cells
Vegetative

Location of Nicotinic N-receptors:
N neuronal : (Nn)
∙ CNS
∙

Cholinergic Drugs
I. M,N-cholinergic Agents of Direct Action:
1. M, N- Cholinomimetics:
Acetylcholine

II. Anticholinesterase Agents:- M, N - Cholinomimetics of Indirect action

1. Reversible Action:

Acethylcholine

Stimulation M1 and M3 Receptors => Stimulating Action:
the Receptor interacts with

Stimulation of M2 Receptors => Inhibiting Action:
the Receptor interacts with Ginhibitory-Protein

Stimulation of M3 Receptors in the Blood Vessels => VASODILATION
Mechanism:
PIP2

Stimulation of N - Receptors
Phase I: The opening of the

Proserin (Neostigmine)– Polar Compound => does not enter the CNS.
Pharmacologic Effects:
Pupil

Clinical uses of Proserine:
Myasthenia Gravis
Glaucoma
Intestines, Urinary, Gall Bladder

Galantamine - the alkaloid from the roots of Snowdrop – Galanthus

Reactivators of Acetylcholinesterase:

Alloxim (amp. 0.075 g)
Dipiroxime (amp. 15%-1 ml)
Isonitrosin (amp.

Central M,N-Cholinoblockers:

CYCLODOL
NORAKIN
Clinical use: Parkinson’s Disease Parkinsonism
Adverse effects:
Dry Mouth,

Overdose with Pilocarpine
Taking 100 mg PO is considered fatal
Muscarinic symptoms:
Nausea,

M - Cholinoblockers
Atropine sulfate – amp. 0,1%-1 ml
Scopolamine – amp. 0.05%-1

Clinical Uses of Cholinoblockers
●Hypersecretory Conditions: Atropine sulfate,
Scopolamine, Platyphyllin, Pirenzepine
● Sinus

Lobeline and Cytiton-
- Respiratory stimulants with reflector type of action
Mechanism

Ganglioblockers
1.The Quaternary Ammonium Compounds:
Benzohexonium
Pentamin
Hygronium
2. The Tertiary Ammonium

Myorelaxants
1. Non-depolarizing type:
Tubocurarine
Diplacin
Anatruxonium
Pipecuronium (Arduan)
Mellictin
2. Depolarizing type: Dythiline
3.