Pantoprazole sodium sesquihydrate, domperidone.
Green coloured cap and clear transparent body hard gelatin capsules filled with orange and blue coloured pellets.
Pantoprazole Sodium Sesquihydrate BP eq. to Pantoprazole 40 mg (as enteric coated pellets), Domperidone BP 30 mg (as sustained release pellets).
Pharmacotherapeutic group: Pantoprazole: Proton pump inhibitors, ATC code: A02BC02.
Domperidone: Domperidone is a peripheral dopamine (D2) and (D3) receptor antagonist, ATC Code: A03FA03.
Pharmacology: Mechanism of Action: Pantoprazole, a benzimidazole sulphoxide derived prodrug, is an irreversible proton pump inhibitor. Pantoprazole, being a weak base, is highly ionized at low pH and readily accumulated in the highly acidic canalicular lumen of the stimulated parietal cell in the stomach. In this acidic environment, it is protonated and rapidly converted to a cationic cyclic sulphonamide. The sulphonamide binds covalently to cysteine residues on the luminal (acidic) surface of H+/K+-ATPase to form a mixed disulphide; thus causing irreversible inhibition of the gastric proton pump. This inhibition of the gastric proton pump or H+ / K+ -ATPase (which represents the final step in the secretory process), suppress gastric acid secretion.
Domperidone, a benzimidazole derivative (structurally related to the butyrophenones), acts by selectively antagonizing the peripheral dopaminergic 0, receptors in the gastrointestinal (G.I.) wall, thereby enhancing gastrointestinal peristalsis and motility and increasing Lower Esophageal Sphincter (LES) tone.
Pharmacokinetics: Pantoprazole: Pantoprazole is rapidly absorbed after oral administration, with peak plasma concentrations (Cmax) of 1.1 to 3.1 (mean 2.1) m/L occurring within 2 to 4 (mean 2.7) hours (tmax) after ingestion of an enteric coated 40 mg tablet. The volume of distribution is low (mean 0.16 L/kg at steady state) due to high degree of plasma protein binding (-98%). Plasma Pantoprazole concentrations decline monophasically after oral administration, with a mean plasma terminal half-life (ty,P) of 0.9 to 1.9 hours. However, since inhibition of acid secretion is non-competitive or irreversible, there is no correlation between plasma levels and the duration of action of Pantoprazole. Concomitant intake of food has no influence on the bioavailability of Pantoprazole, and any possible retardant effect of food on the rate of drug absorption is not of clinical relevance, considering the prolonged antisecretory action of Pantoprazole. The enteric coating does not influence the bioavailability of Pantoprazole. Pantoprazole undergoes extensive hepatic metabolism via cytochrome P450 oxidase followed by sulphate conjugation. Elimination of Pantoprazole is predominantly renal, with -80% of an oral dose being excreted as urinary metabolite; the remainder is excreted in the feces and originates primary from biliary secretion.
Domperidone: Domperidone is rapidly and almost completely (93%) absorbed after oral administration. Peak plasma concentrations occur within 30 min. after oral administration. The peak plasma concentration value after a 20 mg oral dose is in the range of 15 to 19 ng/ml. The mean elimination half-life ranges from 12-16 hours for an oral dose. Oral bioavailability of Domperidone is 13-17% because of extensive presystemic metabolism in gut wall and liver. Administration of Domperidone 90 minutes after a meal increases bioavailability whereas Cimetidine or alkali pretreatment reduces bioavailability. Domperidone is strongly bound to olasma proteins (90-93%). Domperidone undergoes extensive biotransformation with <1% excreted unchanged in urine.
Special populations: Pantoprazole: Hepatic impairment: There is a slight increase (1.5 fold) in a maximum drug concentrations in patients with mild to severe hepatic impairment. No dosage adjustment is needed in patients with mild to severe hepatic impairment.
Renal impairment: Pharmacokinetic parameters for Pantoprazole in patients with severe renal impairment are similar to those of healthy subjects. No dosage adjustment is needed in patients with renal impairment.
Gender: No dosage adjustment is needed based on gender.
Pediatrics: The pharmacokinetics of Pantoprazole have not been investigated in patients <18 years of age.
Geriatrics: No dosage adjustment is recommended based on age.
Domperidone: Hepatic impairment: There is no published pharmacokinetic data in patients with hepatic impairment. Because Domperidone is extensively metabolized, response to the drug should be carefully monitored in this patient population.
Neonates: Domperidone is not recommended for use in neonates.
Breast milk: Domperidone may precipitate galactorrhea and improve postnatal lactation. It is secreted in breast milk in very small quantities and thus insufficient to be considered harmful.
Pediatrics: Domperidone is not recommended other than for treatment of nausea and vomiting in patients undergoing cancer therapy. There may be an increased risk for extrapyramidal reactions in young children because of an incompletely developed blood brain barrier.
Pregnant women: The safety of Domperidone has not been proven, therefore its use is not recommended in pregnant women.
Geriatrics: No special precautions are necessary in older patients. Pantoprazole + Domperidone should be used with caution in conditions where the individual drugs have been used with precautionary approach.
It is indicated in the management of gastroesophageal reflux disease; gastritis, non-ulcer dyspepsia, gastric or duodenal ulcer, dyspepsia, bloating, fullness, belching, NSAID-induced dyspepsia.
The usual recommended dose of Pantoprazole + Domperidone is one capsule daily before breakfast. Swallow capsule as a whole, do not chew the capsule.
Administration: Can be taken with or without meals.
For the most effective treatment take 30-60 minutes before the first daily intake of food.
Take at around the same time everyday.
Or as prescribed by the physician.
In the event of overdosage, gastric lavage should be performed. Symptomatic and supportive measures are recommended.
It is contraindicated in patients with known hypersensitivity to Pantoprazole or Domperidone.
Use in Pregnancy and Lactation: See Use in Pregnancy and Lactation section for further information.
Lactation. Pantoprazole: Not recommended in children <12yrs. Longterm therapy may lead to bacterial overgrowth in GIT.
Domperidone: Increases serum prolactin levels resulting to galactorrhoea in females and gynaecomastia in males.
Due to lack of controlled studies in pregnant and lactating women, use of Pantoprazole + Domperidone is contraindicated in this group of patients.
Pantoprazole: Diarrhoea, dizziness, pruritus, skin rashes, GIT Infections; anaphylaxis, angioedema, chest pain, dyspnea, erythema multiforme, gastroenteritis, hyperglycaemia, infection, jaundice, optic neuropathy, anterior ischemia, pancreatitis, speech disorder.
Domperidone: Headache, insomnia, nervousness, dizziness, thirst, lethargy, irritability, GP disturbances, hot flushes, mastalgia, galactorrhoea, gynecomastia, menstrual irregularities, rash, pruritus, urticaria, stomatitis, conjunctivitis, urinary frequency, dysuria, oedema, palpitations, leg cramps, asthaenia, drug intolerance.
Pantoprazole: Pantoprazole is metabolized through the cytochrome P450 system, primarily the CYP2C19 and CYP3A4 isoenzymes, and subsequently undergoes phase II conjugation. Based on studies evaluating possible interactions of Pantoprazole with other drugs metabolized by the cytochrome P450 system, no dosage adjustment is needed with concomitant use of the following drugs: theophylline, cisapride, antipyrine, caffeine, carbamazepine, diazepam, diclofenac, digoxin, ethanol, glyburide, oral contraceptives (levonorgestrel ethynylestradiol), metoprolol, nifedipine, phenytoin or warfarin. Clinically relevant interactions of Pantoprazole with other drugs with the same metabolic pathways are not expected. Therefore, when co-administered with Pantoprazole, adjustment of the dosage of Pantoprazole with such drags may not be necessary. There was also no interaction with concomitantly administered antacids. Because of profound and long lasting inhibition of gastric acid secretion, it is theoretically possible that Pantoprazole may interfere with absorption of drags where gastric pH is an important determinant of their bioavailability (e.g. Ketoconazole, Ampicillin esters, and iron salts).
Domperidone: Anti-cholinergic drugs may inhibit the anti-dyspeptic effects of Domperidone. Antimuscarinic agents and opioid analgesics may antagonize the effect of Domperidone. Domperidone suppresses the peripheral effects (digestive disorders, nausea and vomiting) of dopaminergic agonists. Since Domperidone has gastro-kinetic effects, it could influence the absorption of concomitant orally administered drugs, particularly those with sustained release or enteric coated formulations. As Domperidone interferes with serum prolactin levels, it may interfere with other hypoprolactinaemic agents and with some diagnostic tests. Antacids and anti-secretory agents lower the oral bioavailability of Domperidone. They should be taken after meals and not before meals, i.e. they should not be taken simultaneously with Domperidone. Reduced gastric acidity impairs the absorption of Domperidone. Oral bioavailability is decreased by prior administration of Cimetidine or Sodium Carbonate.
Store at temperatures not exceeding 30°C.
A02BC02 - pantoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Cytoran Plus MR cap
100's;30's
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