Level 2

Semester 4

Module : Gastrointestinal system, liver, Nutrition& Metabolism(GLNM411)

 Tutorial
Antispasmodic drugs
 Instructor information

▪ Contact: Rehab M. Elshahat

▪ Department: pharmacology
▪ Official email: rehab@azhar.edu.eg
▪ Mobile: 01006833432
 Learning Outcomes

By the end of the session, the students will be able to:

➢ Discuss Clinical cases related to GIT spasm (colic)
 Antispasmodic drugs

Antispasmodic drugs are a group (class) of medicines that can

relieve cramps or spasms of the stomach, intestines, and bladder.

There are two main types:

I-Antimuscarinics
II-Smooth muscle relaxants
I-Antimuscarinics such as:
➢ Atropine
➢ Propantheline
➢ Dicyclomine and Hyoscyamine
➢ Glycopyrrolate and methscopolamine (quaternary ammonium compounds)
➢ Dicycloverine
➢ Otilonium bromide (quaternary ammonium, block Ca2+ channels and
neurokinin NK2 receptors).

II-Smooth muscle relaxants such as:

➢ Mebeverine
➢ Papaverine
➢ Peppermint oil
➢ Alverine
I-Antimuscarinics

Mechanism of action:
➢ Antimuscarinics act by attaching to the receptors and prevent binding
of Ach to M receptors.
➢ Which resulting in inhibition of smooth muscle contractions.

➢ SO, they help to relax the muscle and relieve the pain associated with a
contraction of the gut.
N.B: Mechanism of smooth muscle contraction by cholinomimetics
 Antimuscarinics: Anticholinergic agents (spasmolytics or
antispasmodics) are used in patients with IBS but should not be used
over the long term.

The most common agents of this class available are nonspecific

antagonists of the muscarinic receptor and include the tertiary amines
dicyclomine and hyoscyamine and the quaternary ammonium
compounds glycopyrrolate and methscopolamine (off-label use).
Dicyclomine: is given in 20-mg doses orally every 6 h, increasing to 40 mg
every 6 h unless limited by side effects.

Hyoscyamine: is available as sublingual tablets, orally disintegrating

tablets, immediate-release oral capsules, tablets, elixir, and drops (all
administered as 0.125–0.25 mg every 4 h as needed),
as extended-release forms for oral use (0.25–0.375 mg every 12 h, or
0.375 mg every 8 h, as needed), and
as an injection for intramuscular, intravenous, or subcutaneous use
(0.25–0.5 mg every 4 h as needed).
 Glycopyrrolate: is rarely used but is available as immediate-release
tablets, oral solution, and injectable forms.

Methscopolamine: is provided tablets; the dose is 2.5 mg a half hour

before meals and 2.5 to 5 mg at bedtime.

last two compounds is that they have a limited propensity to cross the
BBB and hence have a lower risk for neurological side effects such as
light-headedness, drowsiness, or nervousness.

These agents typically are given on either an as-needed basis or

before meals to prevent the pain and fecal urgency that occur in some
patients with IBS.
 Cimetropium and acotiamide are muscarinic antagonists that are
effective in patients with IBS.
Acotiamide appears to be a promising agent for the treatment of
postprandial distress syndrome, one of two major forms of functional
dyspepsia.

Otilonium bromide is a quaternary ammonium salt with

antimuscarinic effects that also appears to block Ca2+ channels and
neurokinin NK2 receptors.
 Dicycloverine
Dicycloverine: it is an anticholinergic drug and also it block histaminic and
bradykinin receptors
Pharmacological action:

1-GIT : smooth muscle relaxation (antispasmodic effect)

decrease salivary secretion
2-CVS : blocking M2 receptors
increase heart rat and may leads to tachyarrhythmia
3- Other secretion: decrease lacrimal and sweat secretion
Precautions:
1- It decrease sweat secretions so it may ppt fever and heat stork.
2- Drowsiness hallucination and alteration of mental status and blurred
of vision
All of these can decrease the working performance of the patient.

N.B : On long use should be close monitoring to CNS &CVS side effects
Side effects:
A-common side effects
1-CNS: drowsiness, dizziness, and hallucination
2-Eye: blurred vision & dry eyes
3-GIT: dry mouth, nausea, vomiting, constipation,
& abdominal bloating

B-Serious side effects :

1-Decreased Sweating
2-Irregular heartbeat
3-Slurred speech
4-Agitation
Mostly, the doctor will provide medicines looking at the benefit
and their side effects.
Contraindications:
1. Obstructive uropathy
2. Obstructive disease of the gastrointestinal tract
3. Severe ulcerative colitis
4. Reflux esophagitis
5. Cardiovascular disease
6. Glaucoma
7. Myasthenia gravis
8. Hypersensitivity to dicyclomine
II-Smooth muscle relaxants: Mebeverine
Directly relaxes intestinal smooth muscle without
anticholinergic effects.

Mechanism of action:
➢ Is a muscolotropic spasmolytic with a strong and selective action on
the smooth muscle spasm of the gastrointestinal tract, particularly of
the colon.
Mebeverine hydrochloride, a derivative of hydroxybenzamide,
appears to have a direct effect on the smooth muscle cell, blocking K+,
Na+, and Ca2+ channels.
Mebeverine is used as an antispasmodic agent. It is given orally, 100 to
135 mg three times daily or 200 mg twice daily, before meals.
N.B: It does not have the acetyl choline side effect commonly seen in an
anticholinergic antispasmodic drugs.
Side effects
➢ Skin rash
➢ Facial Swelling
➢ Angioedema
➢ Dizziness
➢ Drowsiness
➢ Headache
Papaverine
Papaverine is an opium alkaloid

➢ Mechanism of action: due to its potency to inhibit phosphodiesterase

(PDE 10A)

➢ Used to treat Visceral spasm

Erectile dysfunction and
Investigated as antipsychotic drug
Peppermint oil

➢ Peppermint oil is an herbal extract of peppermint made from the

essential oil of peppermint leaves. Relaxes intestinal smooth
muscle and is given in an enteric-coated capsule which releases its
contents in the distal small bowel.

➢ It has been traditionally used as an antispasmodic.

It is given before meals three times daily.

And for symptom relief in IBS (as an antispasmodic)

Case 1
A 43-year-old woman with a history of recurrent abdominal pain and she
take antispasmodic drugs

There is no family history of irritable bowel syndrome or colon cancer.

Physical examinations and laboratory test reports showed
no signs of weight loss,
no blood in stool,
laboratory tests negative for celiac disease,
colonoscopy with biopsy was negative, and fecal calprotectin was
negative.
Q1- Mention the antispasmodic drugs.

Q2-What is the mechanism of anticholinergic drugs as antispasmodic action.

Q3-Mention the precaution of Dicycloverine.

Q4- What is the adverse effects of Dicycloverine

 Q1- Mention the antispasmodic drugs.
Antispasmodic drugs are a group (class) of medicines
that can
relieve cramps or spasms of the stomach, intestines, and
bladder.
There are two main types:
I-Antimuscarinics
II-Smooth muscle relaxants
Q2-What is the mechanism of anticholinergic drugs as antispasmodic
action.
Mechanism of action:
➢ Antimuscarinics act by attaching to the receptors and prevent binding
of Ach to M receptors.
➢ Which resulting in inhibition of smooth muscle contractions.

➢ SO, they help to relax the muscle and relieve the pain associated with a
contraction of the gut.
Q3-Mention the precaution of Dicycloverine.

Precautions:
1- It decrease sweat secretions so it may ppt fever and heat stork.
2- drowsiness hallucination and alteration of mental status and blurred
of vision
All of these can decrease the working performance of the patient.

N.B : On long use should be close monitoring to CNS &CVS side effects
Q4- What is the adverse effects of Dicycloverine
Adverse effects:
A-common side effects
1-CNS: drowsiness, dizziness, and hallucination
2-Eye: blurred vision & dry eyes
3-GIT: dry mouth, nausea, vomiting, constipation,
& abdominal bloating

B-Serious side effects :

1-Decreased Sweating
2-Irregular heartbeat
3-Slurred speech
4-Agitation
Mostly, the doctor will provide medicines looking at the benefit
and their side effects.
Case 2
A 32-year-old male with no significant past medical history, presents to
the emergency department with abdominal pain.

He states the pain began a few days ago in the right lower quadrant of
the abdomen, and now feels as though it is spreading to the mid-abdomen.

He describes the pain as coming on suddenly and sharp in

nature. Since onset, his pain started to improve until the morning of
presentation to the emergency department when it acutely worsened. He
says that the pain is much worse with movement.
 The patient is concerned for a possible hernia as he does heavy lifting
at work. Review of systems is negative including no anorexia, no nausea
or vomiting, no testicular pain or swelling, no urinary or bowel
complaints, and no fevers or chills.

The patient take Mebeverine as antispasmodic which relive the pain

temporary.
He does smoke a half pack of cigarettes a day, drinks alcohol socially,
and denies any recreational drug use.
He notes no inherited medical conditions in his family.
 Vital signs on arrival:
•Blood pressure (BP) 120/73
•Heart rate (HR) 60
•RR 18
•Temperature: 35.6 C
•Oxygen saturation: 98% on room air
 Physical Exam
General: Alert and oriented, in no apparent distress, although ambulates into the
emergency room holding his abdomen.

Cardiovascular (CV): Regular rate and rhythm, no murmurs, rubs, gallops

Pulmonary: clear to auscultation bilaterally

Abdomen: moderate tenderness to palpation in the right lower quadrant without

rebound, guarding, or rigidity. Bowel sounds are present throughout.
Negative psoas and obturator signs.
Q1-what is Mebeverine
Q2-Mention the mechanism of action and its adverse effects
Mebeverine
Directly relaxes intestinal smooth muscle without anticholinergic effects.

Mechanism of action:
➢ Is a muscolotropic spasmolytic with a strong and selective action on the
smooth muscle spasm of the gastrointestinal tract, particularly of the colon.
N.B: It does not have the acetyl choline side effect commonly seen in an
anticholinergic antispasmodic drugs.
Side effects
➢ Skin rash
➢ Facial Swelling
➢ Angioedema
➢ Dizziness
➢ Drowsiness
➢ Headache
Thank you

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