Usage
This triple therapy combines an antibiotic (Amoxycillin), a proton pump inhibitor (Lansoprazole), and an antiprotozoal/antibacterial agent (Tinidazole). It is primarily prescribed for Helicobacter pylori (H. pylori) eradication in patients with peptic ulcers (duodenal and gastric ulcers) and other gastrointestinal infections associated with H. pylori. It is also used for the treatment of other bacterial infections of the stomach and digestive system.
Pharmacological Classification:
- Amoxycillin: Antibiotic (Aminopenicillin, Beta-lactam)
- Lansoprazole: Proton Pump Inhibitor (PPI)
- Tinidazole: Antiprotozoal, Antibacterial (Nitroimidazole)
Mechanism of Action:
Amoxycillin inhibits bacterial cell wall synthesis, leading to bacterial death. Lansoprazole reduces gastric acid production by inhibiting the proton pump (H+/K+ ATPase) in the parietal cells of the stomach lining. Tinidazole disrupts DNA synthesis and other cellular processes in susceptible microorganisms, leading to their death. The combined effect of the medications works synergistically to eradicate the infection.
Alternate Names
There is no single international nonproprietary name (INN) for this specific combination. However, the individual components have several alternate names:
- Amoxycillin: Amoxicillin, Amox, α-amino-p-hydroxybenzylpenicillin, p-Hydroxyampicillin
- Lansoprazole: Prevacid, Takecab, Zoton
- Tinidazole: Fasigyn, Simplotan, Tindamax
Brand Names: Several brand names are available depending on the manufacturer and region, including LANZOL KT, HELIKIT-LT, LANSIKIT, PYLOMOX and STANCARE.
How It Works
Pharmacodynamics:
- Amoxycillin: Bactericidal action against susceptible bacteria by inhibiting cell wall synthesis.
- Lansoprazole: Suppresses gastric acid secretion by inhibiting the proton pump, providing relief from symptoms and promoting ulcer healing.
- Tinidazole: Disrupts DNA and other cellular processes in bacteria and protozoa, causing cell death.
Pharmacokinetics:
- Amoxycillin: Well-absorbed orally, widely distributed in tissues and fluids, primarily excreted renally.
- Lansoprazole: Activated in the acidic environment of parietal cells, metabolized by CYP2C19 and CYP3A4, excreted hepatically and renally.
- Tinidazole: Well-absorbed orally, metabolized in the liver, excreted in urine and feces.
Mode of Action (Cellular/Molecular):
- Amoxycillin: Binds to penicillin-binding proteins (PBPs) in bacterial cell walls, inhibiting transpeptidation and peptidoglycan synthesis, leading to cell lysis.
- Lansoprazole: Irreversibly binds to the H+/K+ ATPase in parietal cells, blocking the final step of gastric acid secretion.
- Tinidazole: Forms cytotoxic metabolites that interact with microbial DNA, causing strand breakage and impairing cellular function.
Elimination Pathways:
- Amoxycillin: Primarily renal excretion.
- Lansoprazole: Hepatic metabolism (CYP2C19, CYP3A4) and renal excretion.
- Tinidazole: Hepatic metabolism and excretion in urine and feces.
Dosage
Standard Dosage
This medication is commonly prescribed for adults and not usually for children younger than 12 years. The optimal dose may vary depending on the particular infection and its severity. It’s vital to follow the doctor’s prescription and complete the full course of treatment, even if symptoms improve before the medication is finished.
Adults:
A standard regimen for H. pylori eradication includes:
- Lansoprazole: 30 mg
- Amoxycillin: 1000 mg
- Tinidazole: 500 mg
This combination is usually administered twice daily (every 12 hours) for 7-14 days.
Children:
The combination is generally not recommended for children younger than 12 years. For older children, dosage must be determined by a doctor and based on the child’s weight and the specific infection being treated.
Special Cases:
- Elderly Patients: Dosage adjustments may be necessary in cases of severe hepatic impairment or other significant comorbidities.
- Patients with Renal Impairment: Amoxycillin dosage adjustment is needed for severe renal impairment (creatinine clearance < 30 mL/min).
- Patients with Hepatic Dysfunction: Lansoprazole dosage adjustment is necessary for severe hepatic impairment (Child-Pugh Class C).
- Patients with Comorbid Conditions: Consider potential drug interactions and adjust dosages accordingly.
Clinical Use Cases
The combination is not specifically indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary use is for H. pylori eradication and certain bacterial infections in the stomach and digestive system.
Dosage Adjustments
Dosage adjustments should be individualized based on patient factors such as renal function, hepatic function, age, and other medical conditions.
Side Effects
Common Side Effects:
Nausea, diarrhea, vomiting, abdominal pain, headache, metallic taste, dark urine, fatigue.
Rare but Serious Side Effects:
Severe allergic reactions (anaphylaxis, angioedema), liver dysfunction (jaundice, hepatitis), blood disorders (leukopenia, thrombocytopenia), neurological effects (peripheral neuropathy, seizures).
Long-Term Effects:
Long-term use of PPIs may be associated with an increased risk of osteoporosis-related fractures, vitamin B12 deficiency, and Clostridium difficile infection.
Adverse Drug Reactions (ADR):
Any signs of hypersensitivity (rash, itching, swelling), severe gastrointestinal issues, neurological symptoms, or blood disorders should prompt immediate medical attention.
Contraindications
Hypersensitivity to any component of the medication, porphyria, history of drug-induced liver injury with a PPI, concomitant use of cisapride, pimozide, astemizole, or terfenadine.
Drug Interactions
Amoxicillin may interact with oral contraceptives, warfarin, methotrexate, probenecid. Lansoprazole interacts with drugs metabolized by CYP2C19 and CYP3A4. Tinidazole can cause a disulfiram-like reaction with alcohol.
Pregnancy and Breastfeeding
Amoxycillin is generally considered safe during pregnancy. The safety of lansoprazole and tinidazole during pregnancy has not been fully established. All components are excreted in breast milk and may cause adverse effects in nursing infants. The use of this combination during pregnancy and breastfeeding should be discussed with a physician to assess the benefit versus risk.
Drug Profile Summary
- Mechanism of Action: Amoxycillin: Inhibits bacterial cell wall synthesis; Lansoprazole: Inhibits proton pump, reducing gastric acid; Tinidazole: Disrupts microbial DNA.
- Side Effects: Nausea, diarrhea, headache, metallic taste, allergic reactions.
- Contraindications: Hypersensitivity, porphyria, use of cisapride, pimozide, astemizole, or terfenadine.
- Drug Interactions: Interactions with CYP2C19 and CYP3A4 substrates, alcohol (Tinidazole), oral contraceptives (Amoxycillin).
- Pregnancy & Breastfeeding: Consult physician; all components are excreted in breast milk.
- Dosage: Adult: Lansoprazole 30mg, Amoxycillin 1000mg, Tinidazole 500mg twice daily for 7-14 days. Not typically recommended for children <12 years.
- Monitoring Parameters: Liver function tests, complete blood count, renal function tests (if necessary).
Popular Combinations
This specific combination is itself a popular combination for H. pylori eradication.
Precautions
- Hypersensitivity reactions, liver disease, renal disease, blood dyscrasias, neurological disorders. Avoid alcohol consumption during tinidazole treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Amoxycillin + Lansoprazole + Tinidazole?
A: The typical adult dosage for H. pylori eradication is: Lansoprazole 30 mg, Amoxycillin 1000 mg, and Tinidazole 500 mg, taken twice daily (every 12 hours) for 7-14 days.
Q2: What are the common side effects?
A: Common side effects include nausea, diarrhea, abdominal discomfort, headache, and changes in taste perception.
Q3: What are the contraindications to this combination?
A: Contraindications include known hypersensitivity to any of the components, porphyria, concomitant use with drugs like cisapride or pimozide, and severe liver disease.
Q4: Can this combination be used in pregnant or breastfeeding women?
A: Amoxycillin is generally considered safe during pregnancy. The safety of the other components in pregnancy has not been fully established. All components are excreted in breast milk. Consult a physician before use during pregnancy or breastfeeding.
Q5: How does this combination work to eradicate H. pylori?
A: Amoxycillin kills the bacteria, Lansoprazole reduces acid production creating a less hospitable environment for H. pylori, and Tinidazole disrupts the bacteria’s DNA.
Q6: What should patients be advised regarding lifestyle while taking this combination?
A: Patients should avoid alcohol while taking Tinidazole due to the risk of a disulfiram-like reaction.
Q7: What should be done if a patient misses a dose?
A: Patients should take the missed dose as soon as they remember, unless it is almost time for the next dose. They should not double the dose to catch up.
Q8: Are there any specific drug interactions I should be aware of?
A: Yes, numerous potential drug interactions exist. Inform your healthcare provider about all current medications, including over-the-counter drugs and supplements, to avoid adverse events. Some key interactions involve medications metabolized by the liver enzymes CYP2C19 and CYP3A4.
Q9: What are the long-term implications of Lansoprazole use?
A: Long-term Lansoprazole use has been linked to an increased risk of osteoporosis-related fractures, vitamin B12 deficiency, and Clostridium difficile infection.
