Documenti di Didattica
Documenti di Professioni
Documenti di Cultura
Dr A J Karki
Tutor,Anesthesiology
NAMS,Bir Hospital
PARASYMPATHETIC DIVISION OUTFLOW
M2
Atria, conducting tissues of heart and smooth muscle
Decrease cAMP and increase K+ conductance
M3
Excitatory effect=exocrine gland and visceral smooth muscle contraction by
stimulation of IP3
Drugs with muscarinic actions preferentially stimulate muscarinic receptors on
these tissues, but at high concentration they may show some activity at
nicotinic receptors
NICOTINIC RECEPTOR
Sub-types:
N1: Present in autonomic ganglia, adrenal medulla, CNS
N2: Present in neuromuscular junction
NICOTINIC RECEPTORS
Belong to the superfamily of ligand gated ion channels
5 subunits ;2-alpha, beta, epsilon, delta sub-units.
Channel opens when Ach occupies both the alpha
Channel closes when Ach occupies only 1 alpha subunit
In addition to binding acetylcholine, has weak affinity for
muscarine
CHOLINERGIC AGONISTS
DIRECT-ACTING CHOLINERGIC AGONISTS/
PARASYMPATHOMIMETICS
mimic the effects of acetylcholine by binding directly to
cholinoceptors
All of the direct-acting cholinergic drugs have longer
durations of action than acetylcholine
ACETYLCHOLINE
Although it is the neurotransmitter of parasympathetic
and somatic nerves as well as autonomic ganglia
it is therapeutically of no importance because of its rapid
inactivation by the cholinesterases.
Acetylcholine has both muscarinic and nicotinic activity.
EFFECTS OF ACH OTHER
EFFECTS
CVS;
on the heart mimic the
effects of vagal
stimulation; Decrease in
heart rate and cardiac
output
Decrease BP(vasodilation )
OTHER CHOLINERGIC DRUGS
Non-selective actions
Rapid hydrolysis
As miotic
Atropine fever
CHOLINERGIC ANTAGONISTS
CHOLINERGIC BLOCKERS, PARASYMPATHOLYTICS OR
ANTICHOLINERGIC DRUGS
T1/2=45min
Derivative of atropine
Quarternary amine
0.5mg/2.5ml-Rx of COPD asthma along with B-
agonist
GLYCOPYRROLATE
Quaternary compd
Dose=0.005-0.01mg/kg upto=0.2-0.3mg in adults
Sol=0.2mg/ml
Duration of action=2-4hrs
INDICATION OF ANTICHOLINERGICS
Bradycardia
Rx of op poisoning
Premed
antiemetic
As an antispasmodic
anti-parkinsonism
COPD/asthma
C/I
Acute cong glucoma
CCF
Enlarged prostrate
GOO
S/E OF ANTI CHOLINERGICS
Blurred vision
Confusion,restlessness,anxiety
Mydriasis
Constipation
Urinary retention
Dry mouth
restlessness
hallucinations
dry mouth
somnolence
unconsciousness
atropine fever