ATROPINE
DR GEETANJALI S VERMA
DR GEETANJALI VERMA
ANTI CHOLINERGICS
• Natural : Atropine, Scopolamine
• Semisynthetic: Homatropine, Atropine
methonitrate, Hyoscine butylbromide,
Ipratropium bromide, Tiotropium bromide
• Synthetic: Cyclopentolate, Tropicamide,
Oxybutinin, Trihexphenidyl, Glycopyrrolate
DR GEETANJALI VERMA
• Origin:
– Atropa belladona
– Datura stramonium
• Ester of tropic acid and tropine
• MoA
– Block muscarinic effects of Ach (competitive
antagonist)
– Do not interfere with release of Ach at cholinergic
nerve endings
– Does not distinguish between the M 1 , M 2 , and M 3
DR GEETANJALI VERMA
DR GEETANJALI VERMA
PHARMACOKINETICS
• Absorbed from the gut, parenteral sites and
mucous membranes
• Distribution: widely distributed in the body
• Metabolism: in liver (conjugation)
• 60% excretes unchanged in urine
• Effects disappear quickly within 2 Hrs except eye
• Crosses placental barrier & secreted in milk &
saliva
DR GEETANJALI VERMA
PHARMACODYNAMICS
SECRETIONS
• Salivary: dry mouth, difficult swallowing
• Gastric: reduces vol & total acidity
– Psychic, gastric & intestinal phases of gastric secretion
blocked partially
– Reduced secretion of mucin & gastric enzymes
• Others:
– Reduces secr in nose, mouth, pharynx, bronchi (viscid)
– Decr sweat
– No lacrimal inhibition
– Little effect on pancreatic & intestinal juices & bile
DR GEETANJALI VERMA
SMOOTH MUSCLE
• GI
– Reduces tone & motility (antispasmodic)
– Doesn’t interfere significantly with normal peristalsis
• Biliary tract : weak anti spasmodic
• Urinary tract: reduce tone of fundus of bladder &
enhance tone of trigonal sphincter -- uri retention
• Bronchi: relaxes musc of bronchi & bronchioles
• Uterus : -
• Eye: mydriasis (sphincter of iris & ciliary musc) –
paralysis of accomodation or cyclopegia
DR GEETANJALI VERMA
CVS
• Initially decreases HR – partial agonist of Ach
or stimulation of vagal nuclei
• Foll by tachy (↑ by 30-40 bpm) – blocking of
M2 ® in SA node
• Toxic doses: dilatation of cutaneous blood
vessels – atropine flush & hypotension
(depression of vasomotor center or periph
vasomotor paralysis)
DR GEETANJALI VERMA
CNS
• Mild stimulation of medullary vagal nuclei &
higher cerebral centres – ↓HR,↑ rate & depth
of resp
• Toxic doses: marked excitation
• Mod doses: controls tremors & rigidity in
parkinsonism
DR GEETANJALI VERMA
DR GEETANJALI VERMA
DR GEETANJALI VERMA
ADVERSE EFFECTS
• Due to extension of its pharma actions
– Dryness of mouth, difficult swallowing
– tachycardia
– Fever
– Constipation
– Blurring of vision, ppts glaucoma (elderly)
– Retention of urine (elderly)
– Local allergy: dermatitis, conjunctivitis, swelling of
eyelids
– Drugs causing synd of acute atropine intox: TCAs,
phenothiazines, anti histaminics
DR GEETANJALI VERMA
ACUTE BELLADONA POISONING
• Lethal dose: children 10-30mg, adults: 80-130mg
• Periph muscarinic blockade
– Dryness of mouth, difficult swallowing, thirst
– Tachy, palpitations
– Hyperpyrexia (inhibitino of sweating)
– Dil of pupils, blurred vision, photophobia
– Uri urgency, difficult micturition, retention
– Rash –face, neck , upper trunk
• Central actions
– Excitement, restlessness
– Motor incoord
– Slurring of speech, memory disturbance
– Confusion, hallucination, mania, delirium
– n/v, HTN
– Coma, paralysis of resp centre
DR GEETANJALI VERMA
• Diagnosis
Adding drop of pt’s urine in cat’s eye
pupillary dilatation
• t/t:
– Ingestion: gastic lavage
– Physostigmine 1-4mg (children 0.5-1mg) IV (pref
in CNS symp)
– Neostigmine 2-5mg sc
– Repeated at intervals of 1-2hrs
– Other symptomatic mgmt (dark room, tepid
sponging, oxygen, artificial vent, catheterisation)
DR GEETANJALI VERMA
PREPARATIONS
• Belladona dry extract (1%)
• Belladona tincture : dose 0.6-2ml
• Atropie sulfate 0.5 mg tab or powder 0.25-
2mg
• Atropine eye oint 1%
• Atropine sulfate inj 0.5mg in 1ml
• Atropine methonitrate (0.6% alcoholic soln in
dose 0.2-0.6mg)
DR GEETANJALI VERMA
USES
• GI
– Biliary colic (morphine)
– Cystitis (allay freq & urgency)
• Ocular
– Fundosc examn
– Acute iritis
– Iridocyclitis
– Keratitis
DR GEETANJALI VERMA
• Pre anesth med:
– Reduce secretions
• OP poisioning
• Parkinsonism
• CVS: AV block, hypersensitive carotid sinus
(counters syncope & brady)
• Uri incontinence
DR GEETANJALI VERMA
CONTRAIND
• Age > 40yrs (acute congestive glaucoma)
• Enlarged prostate (retention)
• Chronic lung condn
• Congestive cardiac condn
• Pyloric obstr, pylorospasm, cardiospasm
DR GEETANJALI VERMA
DR GEETANJALI VERMA

Atropine

  • 1.
    ATROPINE DR GEETANJALI SVERMA DR GEETANJALI VERMA
  • 2.
    ANTI CHOLINERGICS • Natural: Atropine, Scopolamine • Semisynthetic: Homatropine, Atropine methonitrate, Hyoscine butylbromide, Ipratropium bromide, Tiotropium bromide • Synthetic: Cyclopentolate, Tropicamide, Oxybutinin, Trihexphenidyl, Glycopyrrolate DR GEETANJALI VERMA
  • 3.
    • Origin: – Atropabelladona – Datura stramonium • Ester of tropic acid and tropine • MoA – Block muscarinic effects of Ach (competitive antagonist) – Do not interfere with release of Ach at cholinergic nerve endings – Does not distinguish between the M 1 , M 2 , and M 3 DR GEETANJALI VERMA
  • 4.
  • 5.
    PHARMACOKINETICS • Absorbed fromthe gut, parenteral sites and mucous membranes • Distribution: widely distributed in the body • Metabolism: in liver (conjugation) • 60% excretes unchanged in urine • Effects disappear quickly within 2 Hrs except eye • Crosses placental barrier & secreted in milk & saliva DR GEETANJALI VERMA
  • 6.
    PHARMACODYNAMICS SECRETIONS • Salivary: drymouth, difficult swallowing • Gastric: reduces vol & total acidity – Psychic, gastric & intestinal phases of gastric secretion blocked partially – Reduced secretion of mucin & gastric enzymes • Others: – Reduces secr in nose, mouth, pharynx, bronchi (viscid) – Decr sweat – No lacrimal inhibition – Little effect on pancreatic & intestinal juices & bile DR GEETANJALI VERMA
  • 7.
    SMOOTH MUSCLE • GI –Reduces tone & motility (antispasmodic) – Doesn’t interfere significantly with normal peristalsis • Biliary tract : weak anti spasmodic • Urinary tract: reduce tone of fundus of bladder & enhance tone of trigonal sphincter -- uri retention • Bronchi: relaxes musc of bronchi & bronchioles • Uterus : - • Eye: mydriasis (sphincter of iris & ciliary musc) – paralysis of accomodation or cyclopegia DR GEETANJALI VERMA
  • 8.
    CVS • Initially decreasesHR – partial agonist of Ach or stimulation of vagal nuclei • Foll by tachy (↑ by 30-40 bpm) – blocking of M2 ® in SA node • Toxic doses: dilatation of cutaneous blood vessels – atropine flush & hypotension (depression of vasomotor center or periph vasomotor paralysis) DR GEETANJALI VERMA
  • 9.
    CNS • Mild stimulationof medullary vagal nuclei & higher cerebral centres – ↓HR,↑ rate & depth of resp • Toxic doses: marked excitation • Mod doses: controls tremors & rigidity in parkinsonism DR GEETANJALI VERMA
  • 10.
  • 11.
  • 12.
    ADVERSE EFFECTS • Dueto extension of its pharma actions – Dryness of mouth, difficult swallowing – tachycardia – Fever – Constipation – Blurring of vision, ppts glaucoma (elderly) – Retention of urine (elderly) – Local allergy: dermatitis, conjunctivitis, swelling of eyelids – Drugs causing synd of acute atropine intox: TCAs, phenothiazines, anti histaminics DR GEETANJALI VERMA
  • 13.
    ACUTE BELLADONA POISONING •Lethal dose: children 10-30mg, adults: 80-130mg • Periph muscarinic blockade – Dryness of mouth, difficult swallowing, thirst – Tachy, palpitations – Hyperpyrexia (inhibitino of sweating) – Dil of pupils, blurred vision, photophobia – Uri urgency, difficult micturition, retention – Rash –face, neck , upper trunk • Central actions – Excitement, restlessness – Motor incoord – Slurring of speech, memory disturbance – Confusion, hallucination, mania, delirium – n/v, HTN – Coma, paralysis of resp centre DR GEETANJALI VERMA
  • 14.
    • Diagnosis Adding dropof pt’s urine in cat’s eye pupillary dilatation • t/t: – Ingestion: gastic lavage – Physostigmine 1-4mg (children 0.5-1mg) IV (pref in CNS symp) – Neostigmine 2-5mg sc – Repeated at intervals of 1-2hrs – Other symptomatic mgmt (dark room, tepid sponging, oxygen, artificial vent, catheterisation) DR GEETANJALI VERMA
  • 15.
    PREPARATIONS • Belladona dryextract (1%) • Belladona tincture : dose 0.6-2ml • Atropie sulfate 0.5 mg tab or powder 0.25- 2mg • Atropine eye oint 1% • Atropine sulfate inj 0.5mg in 1ml • Atropine methonitrate (0.6% alcoholic soln in dose 0.2-0.6mg) DR GEETANJALI VERMA
  • 16.
    USES • GI – Biliarycolic (morphine) – Cystitis (allay freq & urgency) • Ocular – Fundosc examn – Acute iritis – Iridocyclitis – Keratitis DR GEETANJALI VERMA
  • 17.
    • Pre anesthmed: – Reduce secretions • OP poisioning • Parkinsonism • CVS: AV block, hypersensitive carotid sinus (counters syncope & brady) • Uri incontinence DR GEETANJALI VERMA
  • 18.
    CONTRAIND • Age >40yrs (acute congestive glaucoma) • Enlarged prostate (retention) • Chronic lung condn • Congestive cardiac condn • Pyloric obstr, pylorospasm, cardiospasm DR GEETANJALI VERMA
  • 19.