
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 salivary, lacrimal 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
- Confusion, hallucination, 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