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. A].Mydriatics eg. Tropicamide B].Antisecretory antispasmodic 1].Quoaternary compund 2].tertiary amine compound C]. Vasoselective D]. Antiperkinsonian

3.Synthetic Compounds

Pharmacological Action of Anticholinergic Drugs Acts as parasympatic responses Affected organ

CNS CVS Eyes

Pharmacological action
Suppresses tremor and rigidity
Tachycardia(blockade of M2 receptor) so tend to high Bp Abolition of light reflex Cycloplegia Leads to blurring of vision and photophobia,increased intraoccular pressure All viscera like stomach, intestine, bronchi get relaxed by it

Smooth muscle

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 Vasico selective Antiperkinsonian

3. 4.

1. Mydriatics
Compound 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,Tropica Eye met, Tromide (eye drops)

Same

2.Antisecretory-antispasmodic a). Quaternary compounds

Compound name
Hyoscine butyl bromide Atropine menthnitrate

Available in market with name of

Buscopan tab

Location of action

Indicated in

Oesopahagu Spastic s, GIT condition of that Pain and acidity

Mydrindon Abdomen, (tab), Spasmolysin(t ab) Ipravent Respiratory (inhaler), secretion Ipranase(nasa l spray) Tiova(rotacap s) Bronchioles

Ipratropium bromide

COPD,Rhinorrh aoea

Titropium bromide

Bronchial asthma

Oxyphenonium

Antrenyl (tab)

Gastric mucousa, GIT

GIT

Peptic ulcer

Cidinium

Spasril,Equirex, Normaxin(tab)

Peptic ulcer, irritable bowel syndrome, dyspepsia. Dyspepsia , infantile colics GIT PROBLEMS WITH EMOTIONAL PROBLEMS

Pipenzolate methyl bromide Isopropamide

Piptal ,Pipen, (drops)

GIT

Gastabid,stelabid( GIT tab)

Glycopyrrolate

Glyco p

General anaesthesia

b) Tertiary Amine group

Compound name
Dicyclomine

Available in market with name of

Cyclominol(tab) Cyclopam(inj) ,Colimex Valamate(inj) Epidosin(inj)

Site of action Indicated in

Bowel (movements), Guts, female genitalia Cervix, visceras

Morning and motion sickness, Dysmenorrhoea, Spasmodic condition

Velethamate

3.Vasicoselective Drugs
Compound name
Oxybutynin

Available in market with name of

Oxybutin ,cystran , Oxyspas (tab)

Site of action Indicated in

Urinary bladder. And Salivary gland

Urge incontinence, spina bifida, and nocturanal enuresis Overactive bladder,urinary urgency UTI, Dysuria

Tolterodine

Roliten,TORQ(tab )

Urinary bladder,

Flavoxate

Uripas ,Flavate(tab)

Same

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