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Anticholinergic Drugs or Parasympatholytic Drugs

Anticholinergic drugs, also known as parasympatholytic drugs, block the actions of acetylcholine (Ach) on autonomic effectors and muscarinic receptors in the central nervous system. They are classified into natural alkaloids like atropine and hyoscine, semisynthetic derivatives, and synthetic compounds used as mydriatics, antisecretory drugs, antispasmodics, and for conditions like Parkinson's disease. Atropine has various pharmacological actions through muscarinic receptor blockade including drying secretions, dilating pupils, increasing heart rate, relaxing smooth muscles, and increasing body temperature. It is absorbed rapidly, metabolized in the liver, and excreted unchanged

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81 views4 pages

Anticholinergic Drugs or Parasympatholytic Drugs

Anticholinergic drugs, also known as parasympatholytic drugs, block the actions of acetylcholine (Ach) on autonomic effectors and muscarinic receptors in the central nervous system. They are classified into natural alkaloids like atropine and hyoscine, semisynthetic derivatives, and synthetic compounds used as mydriatics, antisecretory drugs, antispasmodics, and for conditions like Parkinson's disease. Atropine has various pharmacological actions through muscarinic receptor blockade including drying secretions, dilating pupils, increasing heart rate, relaxing smooth muscles, and increasing body temperature. It is absorbed rapidly, metabolized in the liver, and excreted unchanged

Uploaded by

Nishant Katiyar
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Anticholinergic Drugs or Parasympatholytic Drugs

The term ‘anticholinergic drugs’ is restricted to those which block actions of


Ach on autonomic effectors and in the CNS exerted through muscarinic
receptors. Though nicotinic receptor antagonists also block certain actions of
ACh, they are generally referred to as ‘ganglion blockers’ and
‘neuromuscular blockers’.

CLASSIFICATION-

1. Natural alkaloids- Atropine, Hyoscine (Scopolamine).


2. Semisynthetic derivatives- Homatropine, Atropine methonitrate, Hyoscine
butyl bromide, Ipratropium bromide, Tiotropium bromide.
3. Synthetic compounds-
(a) Mydriatics- Cyclopentolate, Tropicamide
(b) Antisecretory- antispasmodics:
(i) Quaternary compounds: Propantheline, Oxyphenonium, Clidinium,
Pipenzolate methyl bromide, Isopropamide, Glycopyrrolate.
(ii) Tertiary amines: Dicyclomine, Valethamate, Pirenzepine.
(c)Vasicoselective- Oxybutynin, Flavoxate, Tolterodine.
(d)Antiparkinsonian- Trihexyphenidyl (Benzhexol), Procyclidine, Biperiden.
Atropine-
PHARMACOLOGICAL ACTIONS-
CNS- Atropine has an overall CNS stimulant action. However, these
effects are not appreciable at low doses which produce only peripheral
effects because of restricted entry into the brain.
CVS- The most prominent effect of atropine is tachycardia. It is due
to blockade of M2 receptors on the SA node through which vagal tone
decreases HR. Higher the existing vagal tone— more marked is the
tachycardia.
Eye- Topical instillation of atropine causes mydriasis, abolition of
light reflex and cycloplegia lasting 7–10 days. This results in
photophobia and blurring of near vision. The ciliary muscles recover
somewhat earlier than sphincter pupillae. The intraocular tension
tends to rise, especially in narrow angle glaucoma. However,
conventional systemic doses of atropine produce minor ocular effects.
Smooth muscles- All visceral smooth muscles that receive
parasympathetic motor innervation are relaxed by atropine (M3
blockade). Tone and amplitude of contractions of stomach and
intestine are reduced; the passage of chyme is slowed—constipation
may occur, spasm may be relieved.
Atropine causes bronchodilatation and reduces airway resistance,
especially in COPD and asthma patients.
Atropine has relaxant action on ureter and urinary bladder; urinary
retention can occur in older males with prostatic hypertrophy.
However, this relaxant action can be beneficial for increasing bladder
capacity and controlling detrusor hyperreflexia in neurogenic bladder.
Glands- Atropine markedly decreases sweat, salivary,
tracheobronchial and lacrimal secretion (M3 blockade). Skin and eyes
become dry, talking and swallowing may be difficult. Atropine
decreases secretion of acid, pepsin and mucus in the stomach, but the
primary action is on volume of secretion so that pH of gastric contents
may not be elevated unless diluted by food.

Body temperature- Rise in body temperature occurs at higher doses.


It is due to both inhibition of sweating as well as stimulation of
temperature regulating centre in the hypothalamus. Children are
highly susceptible to atropine fever.

PHARMACOKINETICS- Atropine and hyoscine are rapidly


absorbed from g.i.t. Applied to eyes they freely penetrate cornea.
Passage across blood-brain barrier is somewhat restricted. About 50%
of atropine is metabolized in liver and rest is excreted unchanged in
urine. It has a t½ of 3–4 hours.

USES-
 As antisecretory in preanaesthetic medication.

 In peptic ulcer

 As antispasmodic

 In bronchial asthma and COPD

 To antagonize muscarinic effects of drugs and poisons


Adverse Effects-
 Dry mouth
 Difficulty in swallowing and talking
 Dry, flushed and hot skin
 Difficulty in micturition
 Dilated pupil, photophobia, blurring of near vision
 Excitement, psychotic behaviour, delirium, visual
hallucinations.
 Hypotension, weak and rapid pulse
 Respiratory depression
 Convulsions and coma occur only in severe
poisoning.

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