Pharmacology

Level-1
Dr. Mohammad Dammage

Muscarinic antagonists (Parasympatholytics)

Compete with Ach for muscarinic receptors

Classification according
to nature
A) Natural
alkaloids

B) Synthetica-Mydriatics derivatives

-1
Atropin = scopolamine .
2-Hyoscine
e

b-Antisecretory- antispasmodic
c-Antiasthmatic (bronghodilator)
d-Urinary
incontinenace
E-Anti-parkinsonism

Natural alkaloids:
1-Atropine:
Eye:- passive mydriasis.
-ve light reflex cycloplegia, IOP.
Lacrimation. 7-10 days local.
Secretions (salivary, gastric, bronchial and sweat).
Bronchodilatation.
H.R., A.V conduction. Toxic dose flushing.
gut motility and urinary retention.
R.C., cardio-inhibitory center (C.I.C). (initial
H.R) also due to block of pre-synaptic receptors.
Vomiting center.
Basal ganglia.
Large dose cortex Hallucination.

Uses :
1-Preanaestheic medication to decrease secretions &
prevents bronchospasm, protect heart from
bradycardia, to R.C. & prevent vomiting.
2-Fundus examination, errors of refraction &iritis.
3-Bradycardia, heart block & carotid sinus syndrome.
4-Bronchial asthma (iparatropium is better).
5-Duodenal ulcer, colics, diarrhea.
6-Nocturnal enuresis.
7-Antidote to parasympathomimetics (parathion.).
8-Parkinsonism.
9-Motion sickness (hyoscine is better).
10-Hyperhiderosis (excessive sweating).

Toxicity :
1- dry mouth (xerostomia)
2- blurred vision
3- H.R.
4-mydriasis , flushing,
7-dry skin
8- hyperthermia,
9- excitation.
Ttt by physostigmine, cold fomentations.
Contraindications :- glaucoma prostatic
enlargement.

2-Hyoscine = scopolamine .
Shorter duration.
Less effect on heart.
More C.N.S depressant. sedation, amnesia.
If used alone in presence of pain delirium,
confusion.
Uses as atropine & preferred in
1-preanaesthesia of cardiac and thyrotoxic patients
2- in labour (+analgesic)
3- motion sickness
4- Miniere's disease
5- peptic ulcer,
6-colics.

2-Synthetic

derivatives

a-Mydriatics :
1-Homatropine (24 hrs).
2-Tropicamide.
3-Cyclopentolate (6hrs).
Used for fundus examination .
Contraindicated in glauocma.

b-Antisecretory- antispasmodic
1-Pirenzepine and Telenzepine
(M1 blocker).
2-Propantheline.
3-Oxyphenonium.
4-Hyoscine butylbromide(Buscopan)
Used in peptic ulcer & in colics .

c-Antiasthmatic (bronghodilator)
1-Ipratropium is quaternary
amine, given by inhalation, dilates
bronchi. With no dryness of
secretions, used in bronchial
asthma.
2-Tiotropium is similar and used
in chronic obstructive pulmonary
diseases ( COPD).

d-Urinary incontinenace
1-Emepronium and oxybutynin
(uripan)
Useful in Nocturnal enuresis ,to
prevent bladder spasm after urosurgery.
E-Anti-parkinsonism
Benzhexol = Trihexyhpendine and
benztropine

Autonomic Ganglia
A)Ganglion stimulants

B)Ganglion blockers

Nicotine, lobeline in small dose.

1-Nicotine: plant origin, it H.R.,
B.P. Antiduretic
hormone( ADH), R.C reflexly,
gut.
Tobacco smoking is enzyme
inducer.
2-Lobeline is used in treatment of
neonatal asphyxia

B)Ganglion blockers

Nicotine

-1
Depolarizin
g
, lobeline in larg dose

Uses : Trimethaphan in
ttt of emergency
hypertension & to induce
controlled hypotension
during surgery.

2-Non depolarizing
(competitive).
1-Trimethaphan: release histamine,
given by I.V. infusion, no C.N.S.
action.
2-Mecamylamine (Secondary amine,
affects C.N.S).
3-Quaternary amines: Tetra-EthylAmmonium(TEA), hexamethonium,
ecolid = chlorisondamine .
Actions:- as atropine + orthostatic
(postural) hypotension + impotence

THANK YOU