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ATROPINE
Hamad Emad Hamad Dhuhayr
Dr. Sayed Sardar & Prof. Asgher Mehdi
Contents
1 Name
2 Medical uses
2.1 Ophthalmic use
2.2 Heart medicine
2.3 Secretions and bronchodilatation
2.4 Organophosphate and nerve agent poisoning
3 Side-effects and overdose
4 Contraindications
5 Mechanism of action
Name
Atropine
is a naturally occurring tropane alkaloid extracted from
deadly nightshade (Atropa belladonna), Jimson weed
(Datura stramonium), mandrake (Mandragora officinarum)
and other plants of the family Solanaceae. It is a secondary
metabolite of these plants and serves as a drug with a wide
variety of effects.
Natural Sources of Atropine & Hyoscine
Atropa belladonna
( Solanaceae)
Hyoscyamus niger
( Solanaceae)
Datura stramonium
Indication
Ophthalmic use
 Topical atropine is used as a cycloplegic, to temporarily paralyze the accommodation
reflex, and as a mydriatic, to dilate the pupils. Atropine degrades slowly, typically wearing
off in 7 to 14 days, so it is generally used as a therapeutic mydriatic, whereas
tropicamide (a shorter-acting cholinergic antagonist) or phenylephrine (an α-adrenergic
agonist) is preferred as an aid to ophthalmic examination.
 In refractive and accommodative amblyopia, when occlusion is not appropriate sometimes
atropine is given to induce blur in the good eye.
Heart medicine
 Injections of atropine are used in the treatment of bradycardia (an extremely low heart
rate).
 Atropine was previously included in international resuscitation guidelines for use in
cardiac arrest associated with asystole and PEA, but was removed from these
guidelines in 2010 due to a lack of evidence. For symptomatic bradycardia, the
usual dosage is 0.5 to 1 mg IV push, may repeat every 3 to 5 minutes up to a total dose
of 3 mg (maximum 0.04 mg/kg).
 Atropine is also useful in treating second-degree heart block Mobitz Type 1
(Wenckebach block), and also third-degree heart block with a high Purkinje or AV-
nodal escape rhythm. It is usually not effective in second-degree heart block Mobitz
type 2, and in third-degree heart block with a low Purkinje or ventricular escape
rhythm.
Secretions and bronchodilatation
 Atropine's actions on the parasympathetic nervous system inhibit salivary and
mucus glands.
 The drug may also inhibit sweating via the sympathetic nervous system. This
can be useful in treating hyperhidrosis, and can prevent the death rattle of dying
patients.
 Even though atropine has not been officially indicated for either of these
purposes by the FDA, it has been used by physicians for these purposes.
Organophosphate and nerve agent poisoning
Atropine is not an actual antidote for organophosphate
poisoning.
However, by blocking the action
of acetylcholine at muscarinic receptors, atropine also
serves as a treatment for poisoning
by organophosphate insecticides and nerve gases, such
as tabun (GA), sarin (GB), soman (GD) and VX.
Side-effects and overdose
 Adverse reactions to atropine include
ventricular fibrillation,
supraventricular or ventricular tachycardia,
 dizziness, nausea, blurred vision, loss of balance, dilated
pupils,photophobia,
dry mouth and potentially extreme confusion,
dissociative hallucinations and excitation especially amongst the
elderly. These latter effects are because atropine is able to cross
the blood–brain barrier. Because of the hallucinogenic properties,
some have used the drug recreationally, though this is potentially
dangerous and often unpleasant.
In overdoses, atropine is poisonous.
Atropine is sometimes added to potentially addictive drugs,
particularly anti-diarrhea opioid drugs.
 such as diphenoxylate or difenoxin, where in the secretion-
reducing effects of the atropine can also aid the anti-
diarrhea effects.
Contraindications
 Myasthenia Gravis, Closed Angle Glaucoma, Dysreflexia, High
Blood Pressure, Disease of the Arteries of the Heart, Chronic Heart
Failure, Depression of the Function of the Heart, Chronic Lung
Disease, Down Syndrome, Drowsiness, Fast Heart beat, Cannot
Empty Bladder, Toxin from Microorganisms causing Diarrhea,
Overactive Thyroid Gland, Bleeding causing Blood Pressure or
Heart Problems
 Allergies:
BELLADONNA ALKALOIDS
Mechanism Of Action of Atropine
Atropine and other muscarinic antagonists are competitively
binds to receptors with Ach or other agonists. Muscarinic
receptors are GPCRs. They have 7-helicalamino acid
structure, the aspartate present on the –NH2 end of the
receptor. This form link between agonist/antagonist with the
receptor. If concentration of Ach is increased, effect of
antagonist overcomes. But chE antagonist along with M-
antagonist works in right way.
Absorption Atropine is rapidly and well absorbed after intramuscular
administration. Atropine disappears rapidly from the blood and is
distributed throughout the various body tissues and fluids.
Protein binding The protein binding of atropine is 14 to 22% in plasma.
Metabolism Much of the drug is destroyed by enzymatic hydrolysis, particularly in
the liver. From 13 to 50% is excreted unchanged in the urine.
Route of elimination Much of the drug is destroyed by enzymatic hydrolysis, particularly in
the liver; from 13 to 50% is excreted unchanged in the urine.
Half life 3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter
(approximately 20 minutes) in females than males.
References
 http://www.drugbank.ca/drugs/DB00572
 http://en.wikipedia.org/wiki/Atropine#Medical_uses
 http://www.webmd.com/drugs/2/drug-6687/atropine-oral/details/list-contraindications

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Atropine

  • 1. ATROPINE Hamad Emad Hamad Dhuhayr Dr. Sayed Sardar & Prof. Asgher Mehdi
  • 2. Contents 1 Name 2 Medical uses 2.1 Ophthalmic use 2.2 Heart medicine 2.3 Secretions and bronchodilatation 2.4 Organophosphate and nerve agent poisoning 3 Side-effects and overdose 4 Contraindications 5 Mechanism of action
  • 3. Name Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects.
  • 4. Natural Sources of Atropine & Hyoscine Atropa belladonna ( Solanaceae) Hyoscyamus niger ( Solanaceae) Datura stramonium
  • 5. Indication Ophthalmic use  Topical atropine is used as a cycloplegic, to temporarily paralyze the accommodation reflex, and as a mydriatic, to dilate the pupils. Atropine degrades slowly, typically wearing off in 7 to 14 days, so it is generally used as a therapeutic mydriatic, whereas tropicamide (a shorter-acting cholinergic antagonist) or phenylephrine (an α-adrenergic agonist) is preferred as an aid to ophthalmic examination.  In refractive and accommodative amblyopia, when occlusion is not appropriate sometimes atropine is given to induce blur in the good eye.
  • 6. Heart medicine  Injections of atropine are used in the treatment of bradycardia (an extremely low heart rate).  Atropine was previously included in international resuscitation guidelines for use in cardiac arrest associated with asystole and PEA, but was removed from these guidelines in 2010 due to a lack of evidence. For symptomatic bradycardia, the usual dosage is 0.5 to 1 mg IV push, may repeat every 3 to 5 minutes up to a total dose of 3 mg (maximum 0.04 mg/kg).  Atropine is also useful in treating second-degree heart block Mobitz Type 1 (Wenckebach block), and also third-degree heart block with a high Purkinje or AV- nodal escape rhythm. It is usually not effective in second-degree heart block Mobitz type 2, and in third-degree heart block with a low Purkinje or ventricular escape rhythm.
  • 7. Secretions and bronchodilatation  Atropine's actions on the parasympathetic nervous system inhibit salivary and mucus glands.  The drug may also inhibit sweating via the sympathetic nervous system. This can be useful in treating hyperhidrosis, and can prevent the death rattle of dying patients.  Even though atropine has not been officially indicated for either of these purposes by the FDA, it has been used by physicians for these purposes.
  • 8. Organophosphate and nerve agent poisoning Atropine is not an actual antidote for organophosphate poisoning. However, by blocking the action of acetylcholine at muscarinic receptors, atropine also serves as a treatment for poisoning by organophosphate insecticides and nerve gases, such as tabun (GA), sarin (GB), soman (GD) and VX.
  • 9. Side-effects and overdose  Adverse reactions to atropine include ventricular fibrillation, supraventricular or ventricular tachycardia,  dizziness, nausea, blurred vision, loss of balance, dilated pupils,photophobia, dry mouth and potentially extreme confusion, dissociative hallucinations and excitation especially amongst the elderly. These latter effects are because atropine is able to cross the blood–brain barrier. Because of the hallucinogenic properties, some have used the drug recreationally, though this is potentially dangerous and often unpleasant.
  • 10. In overdoses, atropine is poisonous. Atropine is sometimes added to potentially addictive drugs, particularly anti-diarrhea opioid drugs.  such as diphenoxylate or difenoxin, where in the secretion- reducing effects of the atropine can also aid the anti- diarrhea effects.
  • 11. Contraindications  Myasthenia Gravis, Closed Angle Glaucoma, Dysreflexia, High Blood Pressure, Disease of the Arteries of the Heart, Chronic Heart Failure, Depression of the Function of the Heart, Chronic Lung Disease, Down Syndrome, Drowsiness, Fast Heart beat, Cannot Empty Bladder, Toxin from Microorganisms causing Diarrhea, Overactive Thyroid Gland, Bleeding causing Blood Pressure or Heart Problems  Allergies: BELLADONNA ALKALOIDS
  • 12. Mechanism Of Action of Atropine Atropine and other muscarinic antagonists are competitively binds to receptors with Ach or other agonists. Muscarinic receptors are GPCRs. They have 7-helicalamino acid structure, the aspartate present on the –NH2 end of the receptor. This form link between agonist/antagonist with the receptor. If concentration of Ach is increased, effect of antagonist overcomes. But chE antagonist along with M- antagonist works in right way.
  • 13. Absorption Atropine is rapidly and well absorbed after intramuscular administration. Atropine disappears rapidly from the blood and is distributed throughout the various body tissues and fluids. Protein binding The protein binding of atropine is 14 to 22% in plasma. Metabolism Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver. From 13 to 50% is excreted unchanged in the urine. Route of elimination Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver; from 13 to 50% is excreted unchanged in the urine. Half life 3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter (approximately 20 minutes) in females than males.
  • 14. References  http://www.drugbank.ca/drugs/DB00572  http://en.wikipedia.org/wiki/Atropine#Medical_uses  http://www.webmd.com/drugs/2/drug-6687/atropine-oral/details/list-contraindications