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Anticholinergics
Anticholinergics




Drugs that block or inhibit the actions of
acetylcholine (ACh) in the parasympathetic nervous
syste...
Cholinergic Blocking Agents:
Mechanism of Action




Competitive antagonists
Compete with ACh
Block ACh at the muscarin...
Classification


Natural:

Atropine,
Hyoscine (Scopolamine)



Semisynthetic:

Homatropine
Atropine methonitrate
Ipratro...


Synthetic:

a)

Mydriatics: Cyclopentonate, Tropicamide

b) Antisecretory antispasmodic:
I) Quaternary compounds:
Propa...
Pharmacological actions
Atropine as prototype



CNS
Overall CNS stimulant effect
 Small doses: These effects are not ap...


Cardiovascular
Small doses: decrease heart rate
 Large doses: increase heart rate, facilitates AV
conduction.
 No con...


Gastrointestinal






Relax smooth muscle tone of GI tract
Decrease intestinal and gastric secretions
Decrease mot...
Atropine substitutes
Quaternary compounds
 Hyoscine butyl bromide- 20-40mg oral, i.m.,
Use- oesophageal, Gi spastic condi...
Quaternary compounds


Glycopyrrolate: 0.1-0.3 mg im,1-2 mg oral
No central effect
 Potent and rapidly acting antimuscar...
Tertiary amines


Dicyclomine :20mg oral/im
Direct smooth muscle relaxant action
 Antispasmodic action
 Antiemetic
 Us...
Vasicoselective drugs


Oxybutinin
High affinity for receptors of urinary bladder, and
salivary glands
 Uses : Neurogeni...


Atropine




Potent
Slow & Longer acting
Undesirable for refraction tesing






10 times less potent than atropi...
Uses


As antisecretory
Preanaesthetic medication-(Atropine, glycopyrolate, hyosine)
 Peptic ulcers
 Pulmonary embolism...



Bronchial asthma, COPD
As mydriatic and cycloplegic





As cardiac vagolytic





Diagnostic
therapeutic
In pa...
Cholinergic Blocking Agents:
Therapeutic Uses

CNS

Decreased muscle rigidity and muscle tremors
 Parkinson’s disease
 D...
Cholinergic Blocking Agents:
Therapeutic Uses
Cardiovascular
Affect the heart’s conduction system



Low doses: slow the...
Cholinergic Blocking Agents:
Therapeutic Uses
Atropine
Used primarily for cardiovascular disorders




Sinus node dysfu...
Cholinergic Blocking Agents:
Therapeutic Uses

Respiratory

Blocking the cholinergic stimulation of the PSNS
allows unoppo...
Cholinergic Blocking Agents:
Therapeutic Uses
Respiratory agents are used to treat:





Exercise-induced bronchospasm...
Cholinergic Blocking Agents:
Therapeutic Uses
Gastrointestinal
PSNS controls gastric secretions and smooth
muscles that pr...
Cholinergic Blocking Agents:
Therapeutic Uses
Gastrointestinal agents are used to treat:




Peptic ulcer disease
Irrit...
Cholinergic Blocking Agents:
Therapeutic Uses
Genitourinary





Relaxed detrusor muscles of the bladder
Increased con...
Cholinergic Blocking Agents:
Side Effects
Body System

Side/Adverse Effects

Cardiovascular

Increased heart rate,
dysrhyt...
Cholinergic Blocking Agents:
Side Effects
Body System

Side/Adverse Effects

Eye

Dilated pupils, decreased
visual accommo...
Cholinergic Blocking Agents:
Side Effects
Body System

Side/Adverse Effects

Genitourinary

Urinary retention

Glandular

...
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Anticholinergics (VK)

  1. 1. Anticholinergics
  2. 2. Anticholinergics   Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system (PSNS) i.e. on muscarinic receptors: Autonomic effectors CNS Nicotinic antagonists also block certain actions of Ach, they are generally referred to as- Ganglionic blockers / NMBs
  3. 3. Cholinergic Blocking Agents: Mechanism of Action    Competitive antagonists Compete with ACh Block ACh at the muscarinic receptors in the PSNS  As a result, ACh is unable to bind to the receptor site and cause a cholinergic effect.
  4. 4. Classification  Natural: Atropine, Hyoscine (Scopolamine)  Semisynthetic: Homatropine Atropine methonitrate Ipratropium bromide Hyoscine butylbromide
  5. 5.  Synthetic: a) Mydriatics: Cyclopentonate, Tropicamide b) Antisecretory antispasmodic: I) Quaternary compounds: Propantheline, Clidinium, Oxyphenonium, Pipenzolate methyl bromide, Glycopyrolate. II) Tertiary compounds: Dicyclomine, Pirenzepine c) Vasicoselective: Oxybutinin, Flavoxate, Tolterodine d) Antiparkinsonian: Trihexyphenidyl, Biperidin.
  6. 6. Pharmacological actions Atropine as prototype  CNS Overall CNS stimulant effect  Small doses: These effects are not appericiable, decrease muscle rigidity and tremors  Large doses: stimulates medullary centres- vagal , respiratory, vasomotor centres    drowsiness, disorientation, hallucinations –(cortical excitation) Depresses vestibular excitation- antimotion sickness property.
  7. 7.  Cardiovascular Small doses: decrease heart rate  Large doses: increase heart rate, facilitates AV conduction.  No considerable effect on BP   Eye Dilated pupils (mydriasis)  Decreased accommodation due to paralysis of ciliary muscles (cycloplegia lasting for 7-10 days)  This results into long lasting blurring of vision and photophobia   Body temperature   Rise in body temp.high doses Local anaesthetic
  8. 8.  Gastrointestinal     Relax smooth muscle tone of GI tract Decrease intestinal and gastric secretions Decrease motility and peristalsis Genitourinary   Increased constriction of internal sphincter   Relaxed detrusor muscle Result: urinary retention Glandular   Decreased bronchial secretions, salivation, sweating Respiratory  Decreased bronchial secretions  Dilated bronchial airways
  9. 9. Atropine substitutes Quaternary compounds  Hyoscine butyl bromide- 20-40mg oral, i.m., Use- oesophageal, Gi spastic conditions.  Atropine methonitrate-2.5-10mg orally, im Use-abdominal colic, hyperacidity  Ipratropium bromide-40-80microgram inhalational Use-COPD, Bronchial asthma
  10. 10. Quaternary compounds  Glycopyrrolate: 0.1-0.3 mg im,1-2 mg oral No central effect  Potent and rapidly acting antimuscarinic  Use- For preanaesthetic medication and during anaesthesia   Propanthelin, Clidinium, OxyphenoniumUse- peptic ulcer , gastritis, irritable bowel syndrome, colic, gi hypermotility
  11. 11. Tertiary amines  Dicyclomine :20mg oral/im Direct smooth muscle relaxant action  Antispasmodic action  Antiemetic  Use: Dysmenorrhea, irritable bowel syndrome, motion sickness, morning sickness.   Pirenzepine :Use-relief of peptic ulcer pain
  12. 12. Vasicoselective drugs  Oxybutinin High affinity for receptors of urinary bladder, and salivary glands  Uses : Neurogenic bladder  spina bifida nocturnal enuresis overactive bladder-urinary urgency, frequency, dysuria
  13. 13.  Atropine    Potent Slow & Longer acting Undesirable for refraction tesing    10 times less potent than atropine Dilatation takes 45-60mins last for 1-3 days Cyclopentonate     Pupils dilates in 30-40mins,cycloplegia in 1-3 hrs last for a week Homatropine   Mydriatics Potent and fast acting (dilatation 30-60mins and last for 1day) Preffered for cycloplegic refraction, uveitis, iritis Adverse effects-transient behavioral abnormalities Tropicamide   Quickest (onset-20-40mins , brief duration for 3-6 hrs) Satisfactory for refraction testing in adults and for fundoscopy
  14. 14. Uses  As antisecretory Preanaesthetic medication-(Atropine, glycopyrolate, hyosine)  Peptic ulcers  Pulmonary embolism  To check sweating , salivation in parkinsonism   As antispasmodic Intestinal, biliary, renal colic, abdominal cramps  Nervous , functional diarrheoa  Irritable bowel syndrome, spastic constpation  Pylorospasm, gastric hypermotility, gastritis, gastric dyspepsia  Urinary frequency, urgency, enuresis in children  dysmenorrhea 
  15. 15.   Bronchial asthma, COPD As mydriatic and cycloplegic    As cardiac vagolytic    Diagnostic therapeutic In partial AV block AMI, digitalis toxicity For central action    Motion sickness Antiparkinsonian OPPs
  16. 16. Cholinergic Blocking Agents: Therapeutic Uses CNS Decreased muscle rigidity and muscle tremors  Parkinson’s disease  Drug-induced extrapyramidal reactions
  17. 17. Cholinergic Blocking Agents: Therapeutic Uses Cardiovascular Affect the heart’s conduction system   Low doses: slow the heart rate High doses: block inhibitory vagal effects on the SA and AV node pacemaker cells  Result: increased heart rate
  18. 18. Cholinergic Blocking Agents: Therapeutic Uses Atropine Used primarily for cardiovascular disorders    Sinus node dysfunction Symptomatic second-degree heart block Sinus bradycardia with hemodynamic compromise (advanced life support)
  19. 19. Cholinergic Blocking Agents: Therapeutic Uses Respiratory Blocking the cholinergic stimulation of the PSNS allows unopposed action of the SNS.  Results:  Decreased secretions from nose, mouth, pharynx, bronchi  Relaxed smooth muscles in bronchi and bronchioles  Decreased airway resistance 
  20. 20. Cholinergic Blocking Agents: Therapeutic Uses Respiratory agents are used to treat:     Exercise-induced bronchospasms Chronic bronchitis Asthma Chronic obstructive pulmonary disease
  21. 21. Cholinergic Blocking Agents: Therapeutic Uses Gastrointestinal PSNS controls gastric secretions and smooth muscles that produce gastric motility.  Blockade of PSNS results in:  Decreased secretions  Relaxation of smooth muscle  Decreased GI motility and peristalsis
  22. 22. Cholinergic Blocking Agents: Therapeutic Uses Gastrointestinal agents are used to treat:    Peptic ulcer disease Irritable bowel disease GI hypersecretory states
  23. 23. Cholinergic Blocking Agents: Therapeutic Uses Genitourinary     Relaxed detrusor muscles of the bladder Increased constriction of the internal sphincter Reflex neurogenic bladder Incontinence
  24. 24. Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Cardiovascular Increased heart rate, dysrhythmias CNS CNS excitation, restlessness, irritability, disorientation, hallucinations, delirium
  25. 25. Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Eye Dilated pupils, decreased visual accommodation, increased intraocular pressure Gastrointestinal Decreased salivation, decreased gastric secretions, decreased motility
  26. 26. Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Genitourinary Urinary retention Glandular Decreased sweating Respiratory Decreased bronchial secretions
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