SMOOTH MUSCLE ANTISPASMODICS

(SPASMOLYTICS)

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 Definitions
• Definition:
– ANTISPASMODICS are drug that suppress
smooth muscle contraction, especially in
tubular organs. The effect is to prevent spasms
of the stomach, intestine or urinary bladder
• Uses
– Drugs used to relieve spasms of smooth muscle
in the GIT
– Specific indications
• Irritable bowel syndrome
• Flatulent distension of the abdomen (meteorism),
• Painful smooth muscle spasms some organs (Analgo-
spasmolytics), examples
– biliary, renal and intestinal colics
– (also in spastic dysmenorrhoea etc.) 2

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 CLASSIFICATION OF ANTISPASMODICS

• Two main groups of drugs:

A. Drugs affecting autonomic innervations
anticholinergics and parasympatolytics
B. Drugs directly affecting smooth muscle
function

– Combination of drugs from the both groups gives

synergism
– Combination with analgesics (pethidine, codeine,
tramadol) = analgo-spasmolytic preparations

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 Antispasmodics
affecting autonomic innervations
• Parasympatolytics (Anticholinergics)
– Antagonists on M – receptors
• Spasmolytic effect on smooth muscle
– Drugs: atropine, trospium, tolterodine , Scopolamine
butylbromide (also known as Hyoscine butylbromide
(Buscopan®)
– Adverse effects (relatively frequent): xerostomia, mydriasis,
cycloplegia, increased ocular pressure, urinary retention and

– Antagonists on both M and N types of cholinergic

receptors
• Spasmolytic effects on both smooth muscle and sphincters
• Often in combination with other drugs
• Quarternary amines – low/slow absorption (low adverse effects on
the CNS)
– Drugs: otilonium, fenpiverine, tiemonium (Visceralgine®), Prifinium (Riabal)

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 Antispasmodics
directly affecting smooth muscle

• Different mechanisms of action are

involved: inhibition of Ca2+ channels,
activation of K+ channels, stimulation of
NO synthesis
• Drugs: papaverine and drotaverine (No-
Spa®), mebeverine,
alverine(Meteospasmyl®)

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 Newer Therapies
• GABA agonists – baclofen (Lioresal®)
– This is a muscle relaxant used for the treatment of
spasticity
– Could also be used for the treatment of Achalasia-
(lower esophageal sphincter (LES) fails to relax)
– The mechanism of action : Baclofen exerts its effects
as an agonist at presynaptic GABA-B (bicuculline-
insensitive) receptors
• Agents that inhibit contractility – Ca2+
channel blockers, organic nitrates, local
injection of botulinum toxin (inhibits ACh
release)
• cholecystokinin (CCK) receptor antagonist –
loxiglumide
– to suppress transient lower esophageal relaxations
(tLESRs) (in gastroesophageal reflux disease - GERD)
– (still in Phase 111 Clinical Trial) 6

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