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