ANTICHOLINERGIC DRUGS
Those drugs which blocks the action of Acetylcholine transmitter (neuroeffector).
1.Natural Classification
Prototype drug of this class :Atropine
Atropin is selective for :Muscarinic receptors
& Nictotinic receptor
Classification of Anticholinergic Drugs
1.Natural alkaloids Atropine , Hyoscine
2.Semisynthetic Homatropine,tiotropiume
Etc.
3.Synthetic Compounds A].Mydriatics
eg. Tropicamide
B].Antisecretory –antispasmodic
1].Quoaternary compund
2].tertiary amine compound
C]. Vasoselective
D]. Antiperkinsonian
Pharmacological Action of Anticholinergic Drugs
Acts as parasympatic responses
Affected organ Pharmacological actionCNS Suppresses tremor and rigidity
CVS Tachycardia(blockade of M2 receptor)
so tend to high Bp
Eyes Abolition of light reflex
Cycloplegia
Leads to blurring of vision and photophobia,increased intraoccular pressure
Smooth muscle All viscera like stomach, intestine, bronchi get relaxed by it
Cont…
Glands Decrease the secretion of lachrymal, sweat,tracheobroncheal
Body temperature Rise in body temperature due to decreased sweat
Local anesthetic Mild anesthetic on the cornea
Pharmakynetics
Absorbed by GIT,Cornea .(50% Absobed by Liver)
Slightly Restricted by Blood brain barrier.
3rd class :Synthetic Class
1. Mydriatics
2. Antisecretory –antispasmodic
a).Quaternary compounds
b). Tertiary amines
3. Vasico selective
4. Antiperkinsonian
1. MydriaticsCompound name
Available in market with name of
Action on Used For
Homatropine Homatropine eye, Homide
Eye Cycloplegia
Cyclopentolate Cyclomid eye, Cyclogyl (eye drops)
Eye Same
Tropicamide Optimide,Tropicamet, Tromide (eye drops)
Eye Same
2.Antisecretory-antispasmodica). Quaternary compounds
Compound name
Available in market with name of
Location of action
Indicated in
Hyoscine butyl bromide
Buscopan tab Oesopahagus, GIT
Spastic condition of that
Atropine menthnitrate
Mydrindon (tab), Spasmolysin(tab)
Abdomen, Pain and acidity
Ipratropium bromide
Ipravent (inhaler),
Ipranase(nasal spray)
Respiratory secretion
COPD,Rhinorrhaoea
Titropium bromide
Tiova(rotacaps)
Bronchioles Bronchial asthma
Oxyphenonium Antrenyl (tab) Gastric mucousa, GIT
Peptic ulcer
Cidinium Spasril,Equirex, Normaxin(tab)
GIT Peptic ulcer, irritable bowel syndrome, dyspepsia.
Pipenzolate methyl bromide
Piptal ,Pipen, (drops)
GIT Dyspepsia , infantile colics
Isopropamide Gastabid,stelabid(tab)
GIT GIT PROBLEMS WITH EMOTIONAL PROBLEMS
Glycopyrrolate Glyco –p General anaesthesia
b) Tertiary Amine group
Compound name
Available in market with name of
Site of action Indicated in
Dicyclomine Cyclominol(tab) Cyclopam(inj) ,Colimex
Bowel (movements), Guts, female genitalia
Morning and motion sickness, Dysmenorrhoea,
Velethamate Valamate(inj)
Epidosin(inj)
Cervix, visceras Spasmodic condition
3.Vasicoselective Drugs
Compound name
Available in market with name of
Site of action Indicated in
Oxybutynin Oxybutin ,cystran , Oxyspas (tab)
Urinary bladder. And Salivary gland
Urge incontinence, spina bifida, and nocturanal enuresis
Tolterodine Roliten,TORQ(tab)
Urinary bladder, Overactive bladder,urinary urgency
Flavoxate Uripas ,Flavate(tab)
Same UTI, Dysuria
4.Antiperkinsonian Drugs
1. Antisecretory
a). Preanesthetic medication
b).Peptic ulcer
c).Pulmonary embolism
2. Antispasmodic
3.Bronchial asthma, COPD
4.Mydriatic and Cycloplegic
Side Effects and Toxicity
-Children are more susceptible-Dry mouth-Dry flushed and hot skin-Fever-Difficulty in micturation-decreased bowel sounds-Dialated pupil-Hypotension
Cont….
- Cardiovascular collapse
- Respiratory Depression
- Convulsions ,
- Coma
Treatment of Overdose
-Gastric Lavage with Tannic Acid(KmNO4)
-Physostigmine 1-3 mg s.c or i.v.
Contraindication
Elderly male with prostatic hypertrophy
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