PROF A K SAKSENA CLASSIFICATION All are competitive antagonist at M I Natural Alkaloids Atropine Hyoscine II Semisynthetic Homatropine Ipratropium Br ID: 216997
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Slide1
ANTICHOLINERGIC DRUGS
-PROF. A. K. SAKSENASlide2
CLASSIFICATIONAll are competitive antagonist at ‘M’
I. Natural Alkaloids:- Atropine, HyoscineII. Semisynthetic:-
Homatropine
, Ipratropium Br,
Tiotropium
,
Hyoscine
Butyl Br, Atropine
MethonitrateSlide3
CLASSIFICATION (contd.)
III. Syntetic:- A. Mydriatics:-
Cyclopentolate
,
Tropicamide
B.
Antisecretory
–Antispasmodic
:-
Methantheline
,
Propantheline
,
Clidinium
,
Oxyphenonium
,
Isopropamide
,
Pipenzolate
,
Dicyclomine
,
Flavoxate
,
Oxybutynin,
Telenzepine
,
Pirenzepine
.
C.
Antiparkinsonian
-
Trihexyphenidyl
,
Benztropine
.Slide4
PHARMACOLOGICAL ACTIONSCNS:-Atropine-
less entry → stimulation of CNS High dose- excitation, disorientation, hallucinationHyoscine- freely enters → depression of CNS ↓ of vestibular excitation- emesisSynthetic – Antiparkinsonian
drugs
CVS:-
Tachycardia due to ↓ vagal tone
(
Bradycardia
?)
Facilitation of AV conduction
Blood Pressure – minor changeSlide5
PHARMACOLOGICAL ACTIONS(contd.)SMOOTH MUSCLES:-
GIT- Vagus Vs. Morphine induced GNS - local mediators (5-HT, Enkephalin)
Biliary tract-
Weak
relax
n
Urinary-
↓ tone of ureter
↓ tone of fundus→ ↓contraction(prostate)
Bronchi-
Relax
n
–
BronchodilationSlide6
PHARMACOLOGICALACTIONS(contd.)EYE –
Relaxn of circ. mus. → Mydriatic Paralysis of ciliary mus
.→
Cycloplegia
,
photophobia & blurring.
EXOCRINE GLANDS:-
↓ secretions
Salivary≥ Sweat ≥ Bronchial˃˃
Lacrimal
≥ Gastric
BODY
TEMPERATURE:-
is
↑
↑ Thermostat + ↓ Sweating
GANGLIA
:-
M1 (
Pirenzepine
)Slide7
OTHER DRUGSHomatropine
Cyclopentolate OphthalmicTropicamideHyoscine
Butyl
Br
:- G .I. smooth muscles
Atropine
Methonitrate
:- Oral
Methantheline
:-
Oral, long duration
Ganglion block→ postural hypo.
Urinary retn, impotence.Propantheline:- Less S/EOxyphenonium:- Potent antispasmodicPirenzepine:- M1 selective (Telenzepine)Slide8
OTHER DRUGS (contd.)Dicyclomine
:- Direct relaxant also + antiemeticOxybutynin :- Urinary bladder & salivationGlycopyrrolate:-
Potent
,
rapid
Flavoxate
:- Analgesic,
L.A. & Anticholinergic
urinary pathologies
Clidinium
:-
With
chlordiazepoxide
Isopropamide:- Long durationIpratropium:- Bronchi (inhalation) TiotropiumDrotavarine:- Selective PDE4Slide9
THERAPEUTIC USESAnti-secretory:-
a)GIT – Hyperacidity, peptic ulcer, nervous diarrhea, IBS, Emotional b)Bronchi:- Preanaesthetic med. (Laryngeal spasm) (Glycopyrrolate
)
Anti-spasmodic
a)
Intestinal colic, biliary colic, pyloric stenosis, spasm
b
)
Nervous diarrhea,
IBS
, spastic colon
c)
Urinary urgency, Dyspepsia, ↑ frequency, cystitis,
supra-pubic pain (Tolterodine, Trospium Cl.)Slide10
THERAPEUTIC USES (contd.)Bronchial Asthma:- Ipratropium/ tiotropium
low efficacy/ thickness of mucous, cf- β2 agonistsVaso-vagal syncope:- Atropine(AV block) d/t vagal stimulation
Anti-
parkinsonian
:-
Ophthalmic:-
Refractory error,
iridocyclitis
,
fundoscopic
examination-
α
1 ago., Antiemetic:- Motion sickness Poisonings:- mushroom poisoning, organophosphorous poisoningSlide11
Hot as a hare
blind as a bat
dry as a bone
red as a beet
mad as a
wet
hen !!