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Klacid-HP7

Klacid Hp7

 

PRODUCT INFORMATION

This document refers to the use of pantoprazole, clarithromycin and amoxycillin in combination for the treatment of patients with peptic ulcer disease. The components of this therapy are frequently used to treat other conditions. For information about the treatment of conditions other than peptic ulcer disease, refer to full Product Information for the appropriate component.

 

Name of Drug

KLACID Hp7 is a combination pack containing Klacid ( active ingredient clarithromycin ) 500mg tablet, Controloc ( active ingredient pantoprazole sodium sesquihydrate 45.1mg which is equivalent to pantoprazole 40mg ) 40mg tablet, and Ospamox ( active ingredient amoxicillin ) 1gm tablet.

 

Description

KLACID pale yellow ovaloid film-coated tablet.

CONTROLOC yellow, oval, biconvex enteric-coated tablets with a white to off-white core printed with brown ink, on one side : P40.

OSPAMOX white to cream coloured tablet, oblong, biconvex, with break cores on both sides.

 

Pharmacology

KLACID Hp7 Helicobacter pylori is a spiral, flagellated, Gram-negative rod, primarily colonising the antrum of the stomach, it congregates at, and around intercellular junctions. The natural habitat of H.pylori is the gastric mucosa, where the bacterium attaches itself via adhesion pedestals. H.pylori is associated with duodenal and gastric ulcer disease in about 95% and 70% of patients, respectively. H.pylori is the major factor in the development of gastritis and ulcers in such patients. Eradication of H.pylori is associated with reduced peptic ulcer recurrence. Eradication of H.pylori is therefore appropriate therapy in most patients with duodenal and gastric ulcer where the latter is not caused by non-steriodal anti-inflammatory drug ( NSAID ) ingestion. Eradication of H.pylori was achieved in approximately 95% of patients following therapy with clarithromycin, pantoprazole and amoxycillin.

 

KLACID Clarithromycin is active in vitro and in vivo against H.pylori. Clarithromycin exerts its antibacterial action by binding to the 50s ribosomal sub-unit of susceptible bacteria and suppresses protein synthesis. The 14-hydroxy metabolite of clarithromycin also has antimicrobial activity. The minimum inhibitory concentrations ( MICs ) of this metabolite are equal or two-fold higher than the MICs of the parent compound.

 

CONTROLOC is an irreversible proton pump inhibitor which has been developed for the treatment of acid-related gastrointestinal disorders. Pantoprazole reduces gastric acid secretion through inhibition of the proton pump on the gastric parietal cell. As a weak base, pantoprazole is highly ionised at low pH and readily accumulates in the highly acidic canalicular lumen of the stimulated parietal cell. In this acidic environment pantoprazole is rapidly converted to the active species, a cationic cyclic sulphonamide, which binds covalently to cysteine residues on the luminal ( acidic ) surface of H+, K+-ATPase to form a mixed disulphide, thereby causing irreversible inhibition of gastric proton pump function. As H+, K+-ATPase represents the final step in the secretory process, inhibition of this enzyme suppresses gastric acid secretion regardless of the primary stimulus.

 

OSPAMOX Amoxycillin is a highly potent, broad spectrum penicillin with a particularly rapid onset and a broad spectrum of action ( active against both gram-positive and gram-negative micro-organism ). Like other penicillins, it acts by inhibiting cell wall synthesis.

 

Pharmacokinetics

A summary of the pharmacokinetic parameters for KLACID Hp7 are provided below. For further information regarding pharmacokinetics of KLACID, CONTROLOC or OSPAMOX, refer to full Product Information for the appropriate component.

 

Pharmacokinetic Parameter   KLACID   CONTROLOC   OSPAMOX
Peak plasma levels   2 hrs   2.7 hrs   1 - 2 hrs
Systemic bioavailability ( single dose )   approximately 50%   77%   70-90%
Plasma protein binding   80%   98%   17%
T1/2   5 - 7 hrs   0.9 - 1.9 hrs   1 - 2 hrs
Average peak plasma levels   1.6+0.6mg/mL ( fasting )   2.1 mg/L   30mg/L
    2.5+0.8mg/mL ( non-fasting )        
             

KLACID Clarithromycin is rapidly and well absorbed from the gastro-intestinal tract after oral administration of Klacid tablets. The microbiologically active metabolite 14-hydroxycalrithromycin is formed by first pass metabolism. Klacid may be given without regard to meals as food does not affect the extent of bioavailability of Klacid tablets. Food does slightly delay the onset of absorption of clarithromycin and formation of the 14-hydroxymetabolite. The pharmacokinetics of clarithromycin are non linear; however, steady-state is attained within 2 days of dosing. At 250mg bid 15-20% of unchanged drug is excreted in the urine. With 500mg bid daily dosing urinary excretion is greater ( approximately 36% ). The 14-hydroxy-clarithromycin is the major urinary metabolite and accounts for 10-15% of the dose. Most of the remainder of the dose is eliminated in the faeces, primarily via the bile 5-10% of the parent drug is recovered from the faeces.

Klacid provides tissue concentrations that are several times higher than the circulating drug levels. Increased levels have been found in both tonsillar and lung tissue. Klacid also penetrates the gastric mucus. Levels of clarithromycin in gastric mucus and gastric tissue are higher when clarithromycin is co-administered with proton pump inhibitor than when clarithromycin is administered alone.

CONTROLOC Pantoprazole is subjected to low first-pass hepatic extraction, as reflected in an estimated absolute oral bioavailability of 77%. Concomitant intake of food has no influence on the bioavailability of pantoprazole. Plasma pantoprazole concentrations decline monophasically after oral administration, with a mean plasma terminal elimination half life of 0.9 to 1.9 hours. Despite the short half life of pantoprazole, inhibition of acid secretion, once accomplished, is long lasting, persisting long after the drug has been cleared from the circulation. On repeated ( 7 days ) oral administration, the pharmacokinetics of pantoprazole ( 20msg and 40mg/ day ) do not differ appreciably from those on single dose administration, suggesting that drug accumulation does not occur. In keeping with its high degree of plasma protein binding ( 98% ), pantoprazole has a relatively low apparent volume of distribution ( mean 0.16 L/kg at steady-state ), suggesting limited tissue distribution. Pantoprazole is subject to extensive hepatic metabolism via cytochrome P450 ( CYP ) - mediated oxidation followed by sulphate conjugation. Elimination is renal, with 80% of an oral dose being exreted as urinary metabolites, the remainder is excreted in the faeces and originates primarily from biliary secretion. The pharmacokinetics of pantoprazole do not appear to be modified to any clinically relevant extent by renal impairment. Haemodialysis does not appear to significantly influence the pharmacokinetics of pantoprazole or its main metabolite M2 in patients with renal disease or end stage renal failure. The metabolism of pantoprazole is impaired in patients with hepatic dysfunction. However, Cmax was only marginally elevated ( 50% ), indicating that pantoprazole may be given without dosage adjustment to patients with hepatic impairment.

OSPAMOX The absorption of amoxycillin is unaffected by meals. The drug is almost completely absorbed from the small intestine. Peak serum levels are reached within 1 to 2 hours after ingestion. Amoxycillin readily distributes in body tissues and fluid including the sputum and purulent bronchial secretions. If liver function is intact, high biliary drug concentrations are reached. Amoxycillion is eliminated at a half life of approximately 1 to 2 hours. Elimination is predominantly renal. More than half of the oral dose is excreted with the urine in a therapeutically active form.

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