Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system (PSNS)
Also called cholinergic blocking agents or parasympatholytics
Often referred to as anticholinergics or antimuscarinics
 Drugs thatblock or inhibit the actions of
acetylcholine (ACh) in the parasympathetic
nervous system (PSNS)
 Also called cholinergic blocking agents or
parasympatholytics
 Often referred to as anticholinergics or
antimuscarinics
4.
 Competitive antagonists
Compete with acetylcholine
 Block acetylcholine at the muscarinic
receptors in the PSNS
 Reversible blockade of acetylcholine at
muscarinic receptors by competitive binding
 Once these drugs bind to receptors, they
inhibit nerve transmission at these receptors.
Mechanism of Action
5.
 Nicotinic receptorantagonists also block
certain actions of Ach
 Referred as GANGLION BLOCKERS/
NEUROMUSCULAR BLOCKERS
7.
 Prototype antimuscarinicdrug - derived from
Atropa belladonna (deadly nightshade) and
Datura stramonium (thorn apple)
 History:
 during the Italian renaissance dilated pupils
were considered desirable
 plant extracts were used as cosmetic eye drops
 hence the name belladonna or "beautiful lady"
in Italian
Atropine
 Tachycardia
 Vascular– no (direct) effect – except, dilate
cutaneous vessels (red as a beet) – block
hypotensive effect of muscarinic agonists
Actions Cardiovascular effects-
11.
 At normaldoses atropine stimulates medullary
centers
 At higher doses produce excitement, agitation,
hallucinations and coma.
 Depresses vestibular excitation and has anti
motion sickness properties
 Supresses tremor and rigidity of
parkinsonism by blocking cholinergic
overactivity in basal ganglia.
Actions On CNS
12.
 Dilated pupils(mydriasis)
 Blocks muscarinic innervations on the circular
muscles (Mydriasis) and relaxes cilairy muscles
(Cycloplegia)
 worsens glaucoma
Actions on Eye
13.
 Relax smoothmuscles of GI tract
 Decrease intestinal and gastric secretions
 Decrease motility and peristalsis
 antispasmodic effect
 Sphincter contraction
Gastrointestinal
14.
 Decreases bronchialsecretion (used as
preanesthetic Medication,COPD)
 Dilated bronchial airways (used for treatment
of Asthma)
Actions Respiratory system
15.
 Relaxes detrusormuscle
 Increased constriction of internal sphincter
 Result: urinary retention
 Relaxation of smooth muscles of ureters
 contraindicated for prostate hypertrophy
patients.
Genitourinary
16.
 Salivary secretion(Dry mouth)
 Decreases Gastric Acid (used for Peptic Ulcer )
 Sweating
 Dry skin
 Fever in infants and children.
 Dec. Bronchial Secretion (used for COPD)
Glandular
 Anticholinergic overdosesyndrome (Belladona
poisoning- consumption of seeds or berries of
belladona or dhatura plant)
 characterized by: Hyperthermia, delirium, dry
mouth, tacycardia, ileus, urinary retention.
 Seizures, coma and respiratory arrest may occur.
 Treatment – Gastric lavage with tannic acid, cold
sponging or ice bags, Physostigmine s.c. or i.v.,
diazepam to control convulsions.
Toxicity of Anticholinergics
 Atropine
 Prototype.
Antidote in OP Poisoning.
 Ipratropium
 Useful in rhinorrhea.
 Also excellent bronchodilator.
Individual Drugs
30.
 Scopolamine
 DepressesCNS and causes amnesia,
drowsiness, euphoria, relaxation and sleep.
 Motion sickness.
 Given parenterally, orally and transdermally.
 Benztropine
 Temporary use in Parkinson’s disease.
 Useful for dystonic reactions caused by
antipsychotics.
31.
 Trihexyphenidyl
 Alsoused for treating EPS by some antipsychotics.
 Contraindicated in glaucoma.
 Flavoxate
 relieves dysuria, urgency, frequency, and pain with
GU infections
 Oxybutynin
 has direct antispasmodic effects on smooth muscle
and anticholinergic effects.
 Decreases frequency of voiding.
 Acetylcholine isthe primary exitatory
neurotransmitter in both sympathetic and
parasympathetic ganglia
 both Sympathetic and parasympathetic
ganglia stimulated
 No therapeutic application
35.
 Principal alkaloidin tobacco
 Acts as an agonist on both Nn and Nm
subtypes of nicotinic cholinergic receptors
 Only use- short term replacement therapy in
tobacco abstinent subjects.
NICOTINE
36.
 Wish toquit but fail due to nicotine
dependance
 Goals for such pharmacotherapy-
 to reduce craving
 Suppress physical withdrawl symptoms like
anxiety, depressed mood ,irritability,inability to
concentrate,tremors
Treatment of smoking
cessation