Respiratory Tract infections. PROF. AzzA ELMedany Department of pharmacology.
ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology...
-
Upload
jesse-austin -
Category
Documents
-
view
251 -
download
1
Transcript of ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology...
![Page 1: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/1.jpg)
ANTICHOLINERGIC DRUGSANTICHOLINERGIC DRUGSANTICHOLINERGIC DRUGSANTICHOLINERGIC DRUGS
Prof. Hanan HagarPharmacology Department
Prof. Alhaider Pharmacology Department
![Page 2: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/2.jpg)
What students should know:What students should know:Student should be able to : Student should be able to :
• Describe Kinetics of muscarinic antagonists Describe Kinetics of muscarinic antagonists • The effects of atropine on the major organ systems.The effects of atropine on the major organ systems.• To list the clinical uses of muscarinic antagonistsTo list the clinical uses of muscarinic antagonists.• To know adverse effectsTo know adverse effects & contraindications of anticholinergic & contraindications of anticholinergic drugs.drugs.• To identify at least one antimuscarinic agent for each of theTo identify at least one antimuscarinic agent for each of the following special uses as peptic ulcer & parkinsonism, motion following special uses as peptic ulcer & parkinsonism, motion sickness.sickness.
Anticholinergic drugsAnticholinergic drugs
![Page 3: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/3.jpg)
are drugs that block cholinergic receptors
Anticholinergic drugsAnticholinergic drugs
![Page 4: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/4.jpg)
Antimuscarinics Antinicotinics
synthetic atropine substitutes
Ganglionic blockers
Neuromuscular blockers
Anticholinergic drugs Anticholinergic drugs
Naturally occurring alkaloids e.g. atropine, hyoscine
![Page 5: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/5.jpg)
synthetic atropine substitutes
AntimuscarinicsAntimuscarinics
Naturally occurring alkaloids
Antimuscarinics
![Page 6: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/6.jpg)
Natural alkaloids
Drugs as : Atropine - Hyoscine
• Lipid soluble
• Good oral absorption
• Good distribution
• Cross blood brain barrier (have CNS actions)
AntimuscarinicsAntimuscarinicsMuscarinic antagonistsMuscarinic antagonists
![Page 7: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/7.jpg)
Synthetic atropine substitutes
AntimuscarinicsAntimuscarinicsMuscarinic antagonistsMuscarinic antagonists
Benztropine
Homatropine
Tropicamaide
Pirenzepine
Ipratropium
Glycopyrrolate
Oxybutynin
![Page 8: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/8.jpg)
Mechanism of action
• Reversible competitive blockade of
muscarinic receptors.
• Atropine& hyoscine can block all
muscarinic receptors (not selective).
Antimuscarinic drugs Antimuscarinic drugs
![Page 9: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/9.jpg)
CNS– CNS depression (Sedation). – Antiemetic effect (block vomiting center)– Antiparkinsonian effect (block basal
ganglia).
– Toxic dose: Hyperthermia - excitement-hallucination.
Pharmacological effects ofPharmacological effects ofatropine atropine
![Page 10: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/10.jpg)
Cardiovascular system (CVS) Tachycardia (increase in heart rate) AV conduction ( + ve dromotropic effect) Therapeutic dose: Vasodilatation induced
by cholinomimetics. Toxic dose: Cutaneous vasodilatation
(atropine flush).
Respiratory system
Relaxation of bronchial muscles (bronchodilator)
Bronchial secretion viscosity
![Page 11: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/11.jpg)
EyePassive mydriasis
due to paralysis of circular muscleCycloplegia (loss of near accommodation)
due to paralysis of ciliary muscle.Loss of light reflex. increase I.O.P # glaucoma. Lacrimal secretion sandy eye
![Page 12: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/12.jpg)
Secretions
Salivary secretion ( Dry mouth ).
Sweating dry skin Fever in infants and
children.
Bronchial secretion Viscosity
Lacrimal secretion Sandy eye
![Page 13: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/13.jpg)
GIT– Relaxation of smooth muscles. GIT motility Antispasmodic effect. Sphincter contractions– Constipation
Urinary Tract– Relaxation of smooth muscles of urinary
bladder.– Sphincter contraction. – Urinary retention.
![Page 14: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/14.jpg)
Side effects
Eye: Blurred vision – mydriasis
CVS: Tachycardia - atropine flush
UT: Urinary retention
GIT: Constipation, paralytic ileus
Secretions: dryness of mouth , sandy eye, increased body temperature.
CNS: sedation, hallucination, excitation (toxic dose).
![Page 15: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/15.jpg)
Treatment of toxicity– Gastric lavage.– Anticonvulsant.– Cooling blanket.
Antidote: Physostigmine ( IV slowly)
(direct acting anticholinesterase).
![Page 16: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/16.jpg)
Hyoscine (scopolamine)
What are the differences between atropine and hyoscine?
Hyoscine has• Shorter duration of action• Less CVS effect• More CNS depressant action• More antiemetic action used in motion sickness• Can produce amnesia.
![Page 17: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/17.jpg)
Contraindications
– Glaucoma (angle closure glaucoma)
– Tachycardia
– Prostate hypertrophy in old patients.
– Constipation
– Children in case of atropine
![Page 18: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/18.jpg)
Cholinergic actions Anticholinergic actionsEyeCircular muscle of iris Contraction (miosis)
Ciliary muscles Contractionaccommodation for near vision
relaxation (mydriasis)
relaxation (cycloplegia) loss of accommodation
Heartbradycardia ( H.R.) Tachycardia ( H.R)
Urinary bladderContraction of musclesRelaxation of sphincterUrination
Relaxation of musclescontraction of sphincter Urinary retention
![Page 19: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/19.jpg)
Cholinergic drugs Anticholinergic drugsExocrine glands
Increase of sweat, saliva, lacrimal, bronchial, intestinal secretions
Decrease all secretions
GIT
peristalsis
secretion
relaxation of sphincter
Diarrhea
peristalsis secretionContraction of sphincter
constipation
Lung
1. Bronchoconstriction
2. bronchial secretion
1. Bronchodilatation2. Decrease secretion
![Page 20: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/20.jpg)
Drugs organ Uses
Atropine CNS Pre-anesthetic medicationAntispasmodic
Hyoscine CNS Pre-anesthetic medication, Motion sickness, antispasmodic
Benztropine CNS Parkinson's disease
HomatropineTropicamide
Eye Fundus examination of eye
Ipratropium Respiratory system
asthma, COPD, inhalation
Pirenzepine Stomach Peptic ulcer
Glycopyyrolate GIT Antispasmodics in hypermotility
Oxybutynin UT Urinary urgency, Urinary incontinence
Uses of antimuscarinic drugs Uses of antimuscarinic drugs
![Page 21: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/21.jpg)
Clinical uses of antimuscarinic drugs
– Parkinsonism
– Vomiting
– Asthma
– Peptic ulcer.
– Intestinal spasm as antispasmodics
– Constipation
– Urinary urgency
![Page 22: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/22.jpg)
Can antimuscarinic drugs reverse the action
of neostigmine on skeletal muscles?
![Page 23: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/23.jpg)
SUMMARY
– Antimuscarinics reverse action of
cholinomimetics on muscarinic receptors.
– Are useful in many applications including
intestinal spasm, urinary urgency, vomiting,
parkinsonism, asthma and peptic ulcer.
– Are contraindicated in constipation, Prostate
hypertrophy, tachycardia and glaucoma.
![Page 24: ANTICHOLINERGIC DRUGS Prof. Alhaider Pharmacology Department Prof. Hanan Hagar Pharmacology Department.](https://reader033.fdocuments.us/reader033/viewer/2022061605/56649d6e5503460f94a4e986/html5/thumbnails/24.jpg)
Thank you
Questions ?