Ple-Spa (Tablets) Instructions for Use

Marketing Authorization Holder

Plethico Pharmaceuticals, Ltd. (India)

ATC Code

A03AD02 (Drotaverine)

Active Substance

Drotaverine (Rec.INN registered by WHO)

Dosage Form

Ple-Spa

Film-coated tablets, 40 mg: 10, 20, or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets yellow in color, round, biconvex.

Excipients: lactose monohydrate 31.75 mg, calcium phosphate 25 mg, calcium hydrogen phosphate 13 mg, sodium carboxymethyl starch 11 mg, sodium lauryl sulfate 2 mg, colloidal silicon dioxide 1.75 mg, povidone 2 mg, magnesium stearate 1.5 g.

Film coating:
Ready-made mixture for film coating [hypromellose 35.0 %, macrogol-6000 12.0 %, titanium dioxide 23.0 %, lactose monohydrate 25.0 % talc 5.0 %] 3.9 mg, quinoline yellow dye 0.1 mg.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (10) – cardboard packs.

Clinical-Pharmacological Group

Myotropic antispasmodic

Pharmacotherapeutic Group

Spasmolytic agent

Pharmacological Action

Myotropic antispasmodic. In chemical structure and pharmacological properties, it is similar to papaverine, but surpasses it in efficacy and duration of action.

Drotaverine is effective for spasms of smooth muscle of both neurogenic and muscular origin. Regardless of the type of autonomic innervation, Drotaverine relaxes the smooth muscle of the gastrointestinal tract, biliary tract, and genitourinary system. Due to its vasodilatory action, Drotaverine improves blood supply to tissues.

Pharmacokinetics

After oral administration, Drotaverine is rapidly absorbed from the gastrointestinal tract. After presystemic metabolism, 65% of the dose enters the systemic circulation. C_max of drotaverine in blood plasma is reached within 45-60 minutes. Plasma protein binding is 95-98%. It is evenly distributed in tissues and penetrates smooth muscle cells. It does not cross the blood-brain barrier; Drotaverine and/or its metabolites may slightly cross the placental barrier. Drotaverine is almost completely metabolized in the liver. T_1/2 of drotaverine is 8-10 hours. Within 72 hours, Drotaverine is almost completely eliminated from the body. About 50% is excreted by the kidneys and about 30% via the gastrointestinal tract. Drotaverine is mainly excreted as metabolites; the unchanged form of drotaverine is not detected in urine.

When administered parenterally, Drotaverine is rapidly absorbed. Bioavailability is 100%. Onset of action is within 2-4 minutes. C_max in blood plasma is reached within 30-40 minutes.

Indications

Spasms of smooth muscle in diseases of the biliary tract (cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis); spasms of smooth muscle of the urinary tract (nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder spasms). As adjunctive therapy for spasms of smooth muscle of the gastrointestinal tract (gastric and duodenal ulcer, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation, irritable bowel syndrome with flatulence); for tension-type headache; for dysmenorrhea; for performing certain instrumental examinations, including cholecystography.

ICD codes

Dosage Regimen

Administer orally, intramuscularly, or intravenously. The dose, method, and regimen of administration are determined individually, depending on the indications, clinical situation, and age.

When taken orally, adults are prescribed 40-80 mg 2-3 times/day. The maximum daily dose for adults is 240 mg. The dose for children is determined depending on age.

For parenteral administration, the average daily dose is 40-240 mg, divided into 1-3 doses per day, intramuscularly. For acute colic (renal or biliary) a dose of 40-80 mg is administered intravenously by slow bolus (injection duration approximately 30 seconds).

Adverse Reactions

Nervous system disorders rarely – headache, dizziness, insomnia.

Cardiovascular system disorders: rarely – palpitations, decreased blood pressure; with parenteral administration – arrhythmia, tachycardia, collapse (with intravenous administration).

Gastrointestinal system disorders rarely – nausea, constipation.

Allergic reactions rarely – angioedema, urticaria, rash, itching; with parenteral administration in isolated cases – anaphylactic shock.

Local reactions with parenteral administration rarely – reactions at the injection site.

Contraindications

Hypersensitivity to drotaverine; severe renal impairment, severe hepatic impairment, severe heart failure (low cardiac output syndrome); lactation period (breastfeeding); children under 6 years of age (for oral administration), children under 18 years of age (for parenteral administration).

For parenteral administration: AV block II-III degree; labor period.

With caution: in arterial hypotension; in children (insufficient clinical experience of use); during pregnancy. For parenteral administration – in severe atherosclerosis of coronary arteries, prostate adenoma, glaucoma.

Use in Pregnancy and Lactation

Use during pregnancy is possible only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.

Contraindicated for use during lactation (breastfeeding). If use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment.

Use in Renal Impairment

Contraindicated in severe renal impairment.

Pediatric Use

Oral administration of drotaverine is contraindicated in children under 6 years of age.

Parenteral administration of drotaverine is contraindicated in children and adolescents under 18 years of age.

Geriatric Use

Should be prescribed with caution to elderly patients to avoid worsening of concomitant diseases.

Special Precautions

During intravenous administration of drotaverine, the patient should be in a horizontal position due to the risk of collapse.

Use in pediatrics

Use Drotaverine (for oral administration) with caution in children. Parenteral administration in children is contraindicated.

Effect on ability to drive vehicles and operate machinery

During the use of drotaverine, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions (for 1 hour after parenteral administration, especially intravenous).

Drug Interactions

With simultaneous use with tricyclic antidepressants, quinidine, procainamide, the blood pressure-lowering effect caused by tricyclic antidepressants, quinidine, and procainamide is enhanced.

With simultaneous use, the spasmogenic activity of morphine is reduced.

With simultaneous use with levodopa, a decrease in the antiparkinsonian effect of levodopa is possible.

With simultaneous use, the action of papaverine, bendazole, and other antispasmodics (including m-anticholinergics) is enhanced.

With simultaneous use with phenobarbital, the severity of the antispasmodic action of drotaverine is increased.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.