ANTICHOLINERGIC
DRUGS
BY-DR.STUTI SINGH
ASSISTANT PROFESSOR
UNSASMC,JAUNPUR
 MUSCARINIC RECEPTOR ANTAGONISTS/
 ATROPINIC/
 PARASYMPATHOLYTIC/
OTHER NAMES
 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
 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
 Nicotinic receptor antagonists also block
certain actions of Ach
 Referred as GANGLION BLOCKERS/
NEUROMUSCULAR BLOCKERS
 Prototype antimuscarinic drug - 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
ATROPA BELLADONA
DATURA
 Tachycardia
 Vascular – no (direct) effect – except, dilate
cutaneous vessels (red as a beet) – block
hypotensive effect of muscarinic agonists
Actions Cardiovascular effects-
 At normal doses 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
 Dilated pupils (mydriasis)
 Blocks muscarinic innervations on the circular
muscles (Mydriasis) and relaxes cilairy muscles
(Cycloplegia)
 worsens glaucoma
Actions on Eye
 Relax smooth muscles of GI tract
 Decrease intestinal and gastric secretions
 Decrease motility and peristalsis
 antispasmodic effect
 Sphincter contraction
Gastrointestinal
 Decreases bronchial secretion (used as
preanesthetic Medication,COPD)
 Dilated bronchial airways (used for treatment
of Asthma)
Actions Respiratory system
 Relaxes detrusor muscle
 Increased constriction of internal sphincter
 Result: urinary retention
 Relaxation of smooth muscles of ureters
 contraindicated for prostate hypertrophy
patients.
Genitourinary
 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
THERAPEUTIC
USES
 Parkinson’s disease – Benztropine,
Trihexyphenidyl ,biperdine
 Motion Sickness (Scopolamine/hyoscine)
 Drug-induced extrapyramidal reactions(due to
antipsychotics)
Central Nervous System
 Atropine is used to increase heart rate in
symptomatic bradycardias.
 Sinus node dysfunction
 Symptomatic second-degree heart block
 Sinus or nodal bradycardia (due to myocardial
infarction)
CVS
 Chronic bronchitis
 Asthma
 Exercise-induced bronchospasms
 Chronic obstructive pulmonary disease -
Ipratropium , Tiotropium
Respiratory system-
 Peptic Ulcer: Pirenzepine ,telenzepine
 As antispasmodic :Dicyclomine
 Irritable bowel disease: Propantheline
 GI hypersecretory states
Gastrointestinal
 Antispasmodic effects seen in overactive
bladder and in urinary incontinence -
Oxybutynin
 Detrusor hyper-reflexia
 Enuresis -Increase bladder capacity -Decrease
bladder pressure
 Urge incontinence-Darifenacine,Solufenacine
Urologic disorders
Homatropine,tropicamide –
 Accurate measurement of refractive error in
uncooperative patients (e.g, children)
 Examination of retina (Mydriasis)
Opthalmological Disorders-
SIDE EFFECTS
 Anticholinergic overdose syndrome (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
 Glaucoma
 Prostatic hypertrophy
 Urinary tract obstruction
 Gastrointestinal tract obstruction
 Infectious diarrhea
 Reflux esophagitis
 Tachyarrhythmias
 Angina
 Hyperthyroidism
 Pregnancy
Contraindications
 Atropine
 Prototype.
 Antidote in OP Poisoning.
 Ipratropium
 Useful in rhinorrhea.
 Also excellent bronchodilator.
Individual Drugs
 Scopolamine
 Depresses CNS 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.
 Trihexyphenidyl
 Also used 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.
DRUGS ACTING ON AUTONOMIC
GANGLIA
 Acetylcholine is the primary exitatory
neurotransmitter in both sympathetic and
parasympathetic ganglia
 both Sympathetic and parasympathetic
ganglia stimulated
 No therapeutic application
 Principal alkaloid in 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
 Wish to quit 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
 NICOTINE REPLACEMENT
 PARTIAL AGONISTS OF α4β2 NRs-varenicline
 ANTIDEPRESSANTS- Bupropion
Drugs
 HEXAMETHONIUM
 PENTOLINIUM
 MECAMYLAMINE
 PEMPIDINE
GANGLIONIC BLOCKING
AGENTS
 Used earlier for HTN and peptic ulcer
 Totally replaced now
 Produces intolerable side effects

anticholinergic sysytem and drugs .pptx

  • 1.
  • 2.
     MUSCARINIC RECEPTORANTAGONISTS/  ATROPINIC/  PARASYMPATHOLYTIC/ OTHER NAMES
  • 3.
     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
  • 8.
  • 9.
  • 10.
     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
  • 18.
  • 19.
     Parkinson’s disease– Benztropine, Trihexyphenidyl ,biperdine  Motion Sickness (Scopolamine/hyoscine)  Drug-induced extrapyramidal reactions(due to antipsychotics) Central Nervous System
  • 20.
     Atropine isused to increase heart rate in symptomatic bradycardias.  Sinus node dysfunction  Symptomatic second-degree heart block  Sinus or nodal bradycardia (due to myocardial infarction) CVS
  • 21.
     Chronic bronchitis Asthma  Exercise-induced bronchospasms  Chronic obstructive pulmonary disease - Ipratropium , Tiotropium Respiratory system-
  • 22.
     Peptic Ulcer:Pirenzepine ,telenzepine  As antispasmodic :Dicyclomine  Irritable bowel disease: Propantheline  GI hypersecretory states Gastrointestinal
  • 23.
     Antispasmodic effectsseen in overactive bladder and in urinary incontinence - Oxybutynin  Detrusor hyper-reflexia  Enuresis -Increase bladder capacity -Decrease bladder pressure  Urge incontinence-Darifenacine,Solufenacine Urologic disorders
  • 24.
    Homatropine,tropicamide –  Accuratemeasurement of refractive error in uncooperative patients (e.g, children)  Examination of retina (Mydriasis) Opthalmological Disorders-
  • 26.
  • 27.
     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
  • 28.
     Glaucoma  Prostatichypertrophy  Urinary tract obstruction  Gastrointestinal tract obstruction  Infectious diarrhea  Reflux esophagitis  Tachyarrhythmias  Angina  Hyperthyroidism  Pregnancy Contraindications
  • 29.
     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.
  • 33.
    DRUGS ACTING ONAUTONOMIC GANGLIA
  • 34.
     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
  • 37.
     NICOTINE REPLACEMENT PARTIAL AGONISTS OF α4β2 NRs-varenicline  ANTIDEPRESSANTS- Bupropion Drugs
  • 38.
     HEXAMETHONIUM  PENTOLINIUM MECAMYLAMINE  PEMPIDINE GANGLIONIC BLOCKING AGENTS
  • 39.
     Used earlierfor HTN and peptic ulcer  Totally replaced now  Produces intolerable side effects