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Atropine

Atropine


ATROPINE

  • Alkaloid of the belladonna plant.
MECHANISM OF ACTION:
  • Competitive antagonist at muscarinic receptor.
  • Does not distinguish between M1, M2, & M3 subgroups of muscarinic receptors.
  • Tissues most sensitive to atropine:
  • Salivary, bronchial, & sweat glands.
  • Acts on central & peripheral cholinergic receptors.
METABOLISM:
  • Rapidly absorbed from GI tract.
  • Freely penerates cornea on eye application.
  • Restricted BBB passage.
  • 50% metabolized in liver & remaining excreted unchanged via urine.
  • t1/2 – 3-4 hours.

DOSAGE:

  • Atropine 1% eye ointment/drops.
  • Atropine sulfate inj (IM/IV)  – 0.5mg for 1 ml in children.
ACTION:

CNS: 

  • Low doses: Minimal stimulant effects. 
  • In toxic/high doses: Maximal excitaory effect.
  • Cause excitement, agitation, hallucinations, & coma.  
  • Reduces Parkinson’s tremor.

Eye: 

  • Mydriasis – Paralysis of sphincter pupillae.
  • Cycloplegia – Paralysis of accommodation.
  • Abolition of light reflex.
  • Photophobia & blurring of near vision.
  • Increased intraocular pressure in people with shallow anterior chamber.
  • It gives comfort & rest to eye by relieving spasm of iris sphincter & ciliary muscle.
  • Prevents synechiae formation & demolishes already formed synechiae.
  • Increases blood supply to anterior uvea.
  • By relieving pressure on anterior ciliary arteries.

CVS:  

  • Tachycardia – Due to M2 bloackade.
  • Heart rate decreases transiently.
  • Counteracts the peripheral vasodilation and sharp fall in blood pressure caused by choline esters.
  • Increased A-V conduction

GIT:

  • Inhibitory effects on motor activity of the stomach, duodenum, jejunum, ileum, and colon. 
  • Reduction in tone and in amplitude and frequency of peristaltic contractions
  • Cause relaxation of LES.

Respiratory System:

  • Causes bronchodilatation.
  • Reduces airway resistance (In COPD & asthma)
  • Inhibits secretions of nose, mouth, pharynx, & bronchi. 
  • Inhibits mucociliary clearance. 
  • Dry secretions result in mucus plugs. 

Excretory system:

  • Relaxant action on ureter & urinary bladder.
  • Urinary retention in older males with prostatic hypertrophy.

Secretions: 

  • Reduces salivarylacrimal and gastric secretions.
  • Due to M3 blockade.

ADVERSE EFFECTS:

  • Due to extension of its pharmacological actions.
  • Dryness of mouth, difficult swallowing
  • Tachycardia
  • Fever
  • Constipation
  • Blurring of vision – Glaucoma (elderly)
  • Retention of urine (elderly)
  • Local allergy: Dermatitis, conjunctivitis, swelling of eyelids

Festooned pupil:

  • Due to irregular dilatation of pupil with atropine in presence of segmental posterior synechiae.

USES:

  • As an anti-spasmodic drug.

In eyes:

  • As mydriatic and cyclopegic, both for diagnostic & therapeutic purposes.
  • Fundoscopic examination
  • Acute iritis
  • Iridocyclitis
  • Fungal corneal ulcer
  • Keratitis

Pre-anesthetic medications:

  • Reduce secretions.

As an anti-dote:

  • OP poisioning (competitive antagonist of acetylcholine)
  • Mushroom poisoning
  • Carbamates poisoning
  • In Parkinsonism

CVS: 

  • As a cardiac vagolytic:
  • Useful in AV block, bradycardia.
  • Urinary incontinence.
  • Motion sickness
  • Hyosine – most effective drug.
  • Prophylactically 0.2 mg orally.

CONTRAINDICATION:

Age > 40yrs.

  • In patients with narrow iridocorneal angle.
  • May precipitate acute congestive glaucoma.
  • Elderly patient with prostatatic hypertrophy.
  • Fear of urinary retention.
  • Cyanosed patient.
  • due to danger of respiratory arrest

BELLADONA POISIONING:

  • Resultant of drug overdose/consumption of seeds & berries of belladonna/datura plant.
  • Children highly susceptible.

Lethal drug dose: 

  • Children: 10-30mg.
  • Adults: 80-130mg

Peripheral muscarinic blockade

  • Dryness of mouth, difficult swallowing, thirst
  • Tachycardia, palpitations
  • Hyperpyrexia (inhibition of sweating)
  • Dilatation of pupils, blurred vision, photophobia
  • Urinary urgency, difficult micturition, retention
  • Rash (Scarlet type) – face, neck , upper trunk

Central actions

  • Excitement, restlessness
  • Motor incoordination
  • Slurring of speech, memory disturbance
  • Confusionhallucination, mania, delirium
  • Hypotension.
  • Coma, paralysis of resp centre

Diagnosis

  • Methacholine 5 mg or neostigmine 1 mg s.c. fails to induce typical muscarinic effects.
  • Pupillary dilatation.

Treatemnt:

Ingestion: 

  • Gastric lavage with Tannic acid.
  • Physostigmine 1-4mg (children 0.5-1mg) IV (preferred in CNS symp)
  • Neostigmine 2-5mg sc (No effect on CNS symp.)
  • Diazepam to control convulsions.
  • Repeated at intervals of 1-2hrs
  • Other symptomatic management:
  •  Dark room, tepid sponging, oxygen, artificial ventilation, catheterisation.
Exam Question
 
  • Atropine is used as Mydriatic, Cyclopegic & Preanaesthetic medication
  • An antidote for Mushroom poisoning, Organophosphates poisoning & Carbamates poisoning.
  • Percentage of atropine in “Atropine eye drops” as cycloplegic is 1%
  • Atropine is most sensitive to mucous & pharyngeal secretions.
  • Atropine is derived from Atropa belladonna.
  • Atropine cause relaxation of lower oesphageal sphincter.
  • Atropine in anterior uveitis causes rest to ciliary muscle, increases antibody supply & prevents posterior synechia formation.
  • Atropine therapy in elderly may be hazardous because risk of elevating intraocular pressure in patients with glaucoma
  • Atropine should never be started when patient is cyanosed due to danger of respiratory arrest.
  • Atropine is useful in organophosphate poisoning because is a competitive antagonist of acetylcholine
  • Rise of body temperature, Decrease bowel sound,Decreased salivary secretion & Increased A-V conduction  are the effects of atropine
  • Atropine when used as a pre-medication causes Skin flush,Prevents bradycardia & Dryness of mouth
  • Atropine-mechanism of action in organophosphate poisoning is that it Acts on central and peripheral cholinergic receptors
  • Treatment of atropine toxicity Physostigmine
  • Agent used for dilatation of pupil in children is atropine
  • Mydriatic used in 3 years old child for refraction is 1 % Atropine ointment
  • Drug of choice for increased IOT in acute anterior uveitis is atropine
  • Atropine is drug of choice in Iridocyclitis.
  • Features of atropine poisoning are Mydriasis, Confusion & Hallucinations.
  • Atropine is contraindicated in glaucoma
  • A farmer visiting an orchard gets unconscious, excessive salivation, constricted pupils and fasciculation of muscles. Treatment is started with:   Atropine
  • Atropine and acetylcholine show Competitive antagonism
Don’t Forget to Solve all the previous Year Question asked on Atropine
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