42 Piromide

Piromide (tiropramide)Piromide (tiropramide)

Oscar Ty Cabahug, M.D., FPCP, FPSG, FPSDE

UERM Medical Center

MCU Medical Center

Oscar Ty Cabahug, M.D., FPCP, FPSG, FPSDE

UERM Medical Center

MCU Medical Center

PiromidePiromide

100 mg tablets

• Manufactured by Kyung Dong Pharm., Co., Ltd.

• Imported by 1 GN Trade Corporation

• Repackaged by Ashford Pharmaceutical Laboratories

100 mg tablets

• Manufactured by Kyung Dong Pharm., Co., Ltd.

• Imported by 1 GN Trade Corporation

• Repackaged by Ashford Pharmaceutical Laboratories

Piromide PharmacodynamicsPiromide Pharmacodynamics

Is pharmacologically characterized as a calmodulin-independent broad-spectrum antispasmodic

Is regarded as a “eukinetic” agent as it has greater potency in the inhibition of pathological smooth muscle contractions than of physiological contractions

Is pharmacologically characterized as a calmodulin-independent broad-spectrum antispasmodic

Is regarded as a “eukinetic” agent as it has greater potency in the inhibition of pathological smooth muscle contractions than of physiological contractions


Its smooth muscle relaxant activity as observed in isolated detrusor muscle of rats is predominantly due to inhibition of Ca++ influx into the smooth muscle cells via voltage dependent Ca++ channels and to a lesser extent related to an increase in intracellular cyclic AMP due to inhibition of phosphodiesterase activity.

Its smooth muscle relaxant activity as observed in isolated detrusor muscle of rats is predominantly due to inhibition of Ca++ influx into the smooth muscle cells via voltage dependent Ca++ channels and to a lesser extent related to an increase in intracellular cyclic AMP due to inhibition of phosphodiesterase activity.


Shows very little calcium channel blocking activity in the vascular smooth muscle indicating its selectivity of its calcium channel blockade in the smooth muscles of non-vascular hollow organs

Does not compete with acetylcholine in muscarinic receptors and would therefore be expected to be devoid of anticholinergic effects as observed with muscarinic receptor antagonists including tachycardia, dry mouth, blurring of vision and inhibition of micturition.

Shows very little calcium channel blocking activity in the vascular smooth muscle indicating its selectivity of its calcium channel blockade in the smooth muscles of non-vascular hollow organs

Does not compete with acetylcholine in muscarinic receptors and would therefore be expected to be devoid of anticholinergic effects as observed with muscarinic receptor antagonists including tachycardia, dry mouth, blurring of vision and inhibition of micturition.


Has been shown to be efficacious in controlling spastic conditions involving the small and large intestines, in normalizing the intestinal transit times in diarrhea-dominant irritable bowel syndrome, in normalizing the motor activity of the gallbladder in biliary dyskinesia and in alleviating spasms of the urinary bladder.

Has been shown to be efficacious in controlling spastic conditions involving the small and large intestines, in normalizing the intestinal transit times in diarrhea-dominant irritable bowel syndrome, in normalizing the motor activity of the gallbladder in biliary dyskinesia and in alleviating spasms of the urinary bladder.


Since the urinary bladder is mainly innervated by non-cholinergic excitatory neurons, antispasmodics of the muscarinic receptor antagonist class of drugs are ineffective whereas tiropramide, because of its pure musculotropic smooth muscle relaxant activity has been found useful in controlling spasms of the urinary bladder.

Since the urinary bladder is mainly innervated by non-cholinergic excitatory neurons, antispasmodics of the muscarinic receptor antagonist class of drugs are ineffective whereas tiropramide, because of its pure musculotropic smooth muscle relaxant activity has been found useful in controlling spasms of the urinary bladder.


Because of its lack of anticholinergic effects, tiropramide has been shown to be an excellent premedication drug in patients undergoing diagnostic or therapeutic endoscopic procedures including ERCP, colonoscopy and flexible procto providing control of intestinal peristalsis without the frequently observed adverse effect of tachycardia.

Because of the higher threshold for the inhibition of gastric peristalsis, tiropramide inhibits intestinal, biliary and urinary spasms without affecting gastric emptying time.

Because of its lack of anticholinergic effects, tiropramide has been shown to be an excellent premedication drug in patients undergoing diagnostic or therapeutic endoscopic procedures including ERCP, colonoscopy and flexible procto providing control of intestinal peristalsis without the frequently observed adverse effect of tachycardia.

Because of the higher threshold for the inhibition of gastric peristalsis, tiropramide inhibits intestinal, biliary and urinary spasms without affecting gastric emptying time.

Piromide PharmacokineticsPiromide Pharmacokinetics

Peak plasma concentrations (Tmax) are reached 1 to 1.7 hours after the oral administration of tiropramide tablets.

Orally administered tiropramide undergoes first pass metabolism in the liver resulting in an AUC ratio between orally and intravenously administered tiropramide of 0.67.

Peak plasma concentrations (Tmax) are reached 1 to 1.7 hours after the oral administration of tiropramide tablets.

Orally administered tiropramide undergoes first pass metabolism in the liver resulting in an AUC ratio between orally and intravenously administered tiropramide of 0.67.


About 35% of orally or intravenously administered tiropramide is excreted in the urine either as unchanged drug or as metabolites while the rest are recovered in the feces.

Of the total amount of drug excreted in the urine, about 16% of intravenously administered and 20% of orally administered tiropramide are in the form of unchanged drug while the rest are in the form of metabolites.

About 35% of orally or intravenously administered tiropramide is excreted in the urine either as unchanged drug or as metabolites while the rest are recovered in the feces.

Of the total amount of drug excreted in the urine, about 16% of intravenously administered and 20% of orally administered tiropramide are in the form of unchanged drug while the rest are in the form of metabolites.


Its metabolites retain biologic activity but have significantly less potency than the parent drug.

Its elimination half-life (T1/2) is about 2.5 hours after a single oral dose.

Its metabolites retain biologic activity but have significantly less potency than the parent drug.

Its elimination half-life (T1/2) is about 2.5 hours after a single oral dose.

Piromide IndicationsPiromide Indications

Symptomatic relief of painful spastic conditions involving the hepatobiliary, gastrointestinal and urinary tracts.

Symptomatic relief of painful spastic conditions involving the hepatobiliary, gastrointestinal and urinary tracts.

Piromide DosagePiromide Dosage

Usual adult dose is 100 mg tablets given one tablet three times daily.

Dosage may be adjusted according to the patient's age or symptoms or as prescribed by a physician.

Usual adult dose is 100 mg tablets given one tablet three times daily.

Dosage may be adjusted according to the patient's age or symptoms or as prescribed by a physician.

Piromide Adverse EventsPiromide Adverse Events

The most commonly encountered adverse events include xerostomia, dyspepsia, nausea and vomiting. Hypersensitivity reactions characterized by pruritus and erythema have also occasionally been observed.

The most commonly encountered adverse events include xerostomia, dyspepsia, nausea and vomiting. Hypersensitivity reactions characterized by pruritus and erythema have also occasionally been observed.

Piromide Special Warnings and Precautions


Although tiropramide is expected to be devoid of anticholinergic side effects at the usual therapeutic doses, caution should still be exercised when administering the drug to patients with glaucoma or benign prostatic hyperplasia.

Tiropramide administered at supra-therapeutic doses may have additive hypotensive effects when given concomitantly with other antihypertensive medications.

Although tiropramide is expected to be devoid of anticholinergic side effects at the usual therapeutic doses, caution should still be exercised when administering the drug to patients with glaucoma or benign prostatic hyperplasia.

Tiropramide administered at supra-therapeutic doses may have additive hypotensive effects when given concomitantly with other antihypertensive medications.



Large intravenous doses of tiropramide may likewise have depressive effects on the cardiovascular system but are less pronounced after oral administration.

Though specific safety parameters have not been established among patients with mild to moderate renal insufficiency, it would be prudent to undertake dosage reduction in such a situation.

Large intravenous doses of tiropramide may likewise have depressive effects on the cardiovascular system but are less pronounced after oral administration.

Though specific safety parameters have not been established among patients with mild to moderate renal insufficiency, it would be prudent to undertake dosage reduction in such a situation.



Although animal studies have not demonstrated any teratogenic effect, it should not be prescribed during pregnancy, unless there are compelling reasons for doing so.

Its safety in lactating women and in pediatric patients has not been established and therefore should not be used in these patients.

Although animal studies have not demonstrated any teratogenic effect, it should not be prescribed during pregnancy, unless there are compelling reasons for doing so.

Its safety in lactating women and in pediatric patients has not been established and therefore should not be used in these patients.

Piromide Contraindications

Piromide Contraindications

Patients who have exhibited a history of hypersensitivity reaction to tiropramide

Severe renal insufficiency

Gastrointestinal obstruction or megacolon

Patients who have exhibited a history of hypersensitivity reaction to tiropramide

Severe renal insufficiency

Gastrointestinal obstruction or megacolon

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42 Piromide

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