(12).

Ganglionic stimulators and blockers

GANGLIONIC STIMULANTS
Selective nicotine agonists:
Nicotine (small dose)
Lobeline
Dimethyl phenyl piperazinium
iodide (DMPP)
Tetramethyl ammonium (TMA)
Nonselective/muscarinic agonists:
AGetylcholine
Carbachol
Piocarpine
Anticholinesterases
MCN 343-A
GANGLION BLOCKING AGENTS
1.Competitive blockers:
Quarternary ammonium compounds
Hexamethonium
Pentolinium
Amines (secondary/tertialy)
Mecamylamine
Pempidine
Monosulfonium compound
Trimethaphan
camforsulfonate
2.Persistent depolarizing blockers
Nicotine (large dose)
Anticholinesterases (large dose)
table on side effect of ganglionic blockers:

Side effects of ganglionic stimulators:

1. CVS: bradycardia, vasoconstriction.
2. Eye: myosis, blurring of far vision
3.GIT: increase motility
4.Bladder : increase tone
5.Salivary and sweat gland : stimulation of secretion of saliva and sweat
Effects of nicotine and tobacco
=>Dose related responses , higher dose direct stimulation nicotinic N1 receptor on
autonomic ganglia. Even higher dose act as ganglionic blocking agent ANS depression,
CNS effects : activation mesocortical + mesolimbic dopaminergic system responsible
for dependence rapid tolerance to nicotine effects.
Tobacco components including nicotine have effects on a number of organ systems.
Respiratory effects. The lungs are the first area to be in contact with the chemical
components and are also exposed to particles and gases.
1. Reduction of activity of cilia in bronchi decreases clearance of lung secretions.
2. An increase in carboxyhaemoglobin concentration in blood reduces oxygen carrying
capacity. This may be important in patients with ischaemic heart disease, increasing the
chance of provoking angina.
3. Increased mucus secretion leads to chronic bronchitis and chronic obstructive lung
disease. Progressive destruction of the supporting tissue in the bronchioles produces
emphysema and airway obstruction.
4. The risk of lung cancer is increased to about 20 times that of a non-smoker. Inhalation
of tobacco smoke is a major contributory factor and explains the greater risk in cigarette
smokers. Giving up smoking reduces the risk progressively over about 10 years of
abstinence. The constituent of tobacco smoke responsible for altering DNA structure and
initiating the cancer process remains controversial, but the relationship between smoking
and lung cancer has been confirmed by numerous epidemiological studies. Compared
with non smokers, passive smokers also have a 2025% increased risk of lung cancer.
Psychological effects. The psychological effects of smoking are substantial, as indicated
by the difficulties experienced by those giving up smoking.
1.Decreased appetite, with weight gain on stopping smoking.
2.Emotional dependence on nicotine and the physical act of smoking is powerful.
Physical withdrawal is less marked but includes restlessness, irritability, anxiety,
depression, difficulty concentrating, decreased heart rate and increased appetite.
Cardiovascular effects. The risk of cardiovascular disease is increased and it occurs at a
younger age. The overall risk of death from coronary artery disease is doubled in smokers
compared with non-smokers, but the magnitude of the effect is related to the numbers of
cigarettes smoked. The risk falls over the first 35 years after stopping smoking to a
level close to that of non smokers. Peripheral vascular disease and stroke are also
increased. Even passive smokers have an excess risk of vascular disease of 25%.
Contributory effects to the increased risk include increased plasma fatty acids and
enhanced platelet aggregability.
Other effects. Nicotine and smoking have a number of other effects:
1.peptic ulceration is twice as common in smokers

2.smoking during pregnancy has several effects, the most important of which is an
increased risk of a low-birth weight child
3.smoking induces a number of the cytochrome P450 isoenrymes and increases the
clearance of drugs such as theophylline and imipramine
4.nicotine patches are sometimes used to reduce the symptoms of ulcerative colitis; they
have no effect in Crohns disease.