Pylera

— THERAPEUTIC CATEGORIES —
  • Hyperacidity, GERD, and ulcers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Pylera Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Bismuth subcitrate potassium 140mg, metronidazole 125mg, tetracycline HCl 125mg; caps.

    Pharmacological Class

    Antimicrobial/antibiotics.

    How Supplied

    Caps—120

    How Supplied

    Pylera is supplied as a white opaque capsule containing 140 mg bismuth subcitrate potassium, 125 mg metronidazole, and 125 mg tetracycline hydrochloride, with the APTALISTM logo printed on the body and “BMT” printed on the cap. 

    • Pylera capsules are supplied as bottles of 120 capsules.

    • Pylera capsules are supplied as a 10 day Therapy pack containing 10 blister cards, with each card containing 12 Pylera capsules for a total of 120 capsules.

    Storage

    Store at controlled room temperature [68° to 77°F or 20° to 25°C]. 

    Manufacturer

    AbbVie

    Generic Availability

    YES

    Mechanism of Action

    Tetracycline interacts with the 30S subunit of the bacterial ribosome and inhibits protein synthesis. Metronidazole’s antibacterial mechanism of action in an anaerobic environment is not fully understood but possibly includes reduction by intracellular electron transport proteins after entry into the organism. Because of this alteration to the metronidazole molecule, a concentration gradient is created and maintained which promotes the drug’s intracellular transport. Presumably, free radicals are formed which, in turn, react with cellular components resulting in death of bacteria. The antibacterial action of bismuth salts is not well understood.

    Pylera Indications

    Indications

    To eradicate H. pylori, in combination with omeprazole, in patients with H. pylori infection and duodenal ulcer disease (active or history of).

    Pylera Dosage and Administration

    Adult

    Swallow whole with 8 oz water. 3 caps 4 times daily after meals and at bedtime for 10 days (give with omeprazole 20mg twice daily with breakfast and dinner for 10 days).

    Children

    Not established.

    Pylera Contraindications

    Contraindications

    Concomitant methoxyflurane. During or within 14 days of disulfiram. Alcohol or propylene-glycol containing products (during and for ≥3days after treatment). Cockayne syndrome. Severe renal impairment. Pregnancy.

    Pylera Boxed Warnings

    Boxed Warning

    Potential for carcinogenicity.

    Pylera Warnings/Precautions

    Warnings/Precautions

    May cause permanent teeth discoloration during 2nd/3rd trimester of pregnancy and children up to 8yrs of age; avoid. Discontinue if superinfection, skin erythema or cutaneous reaction occurs. Blood dyscrasias. Monitor CBC with differential before and after treatment. Avoid sun, UV light. Severe hepatic impairment: not recommended; monitor in mild to moderate. Children ≤8yrs: avoid. High tetracycline doses may cause hepatotoxicity in pregnancy. Nursing mothers: not recommended.

    Warnings/Precautions

    Potential for Carcinogenicity

    • In mice and rats, metronidazole, a component of Pylera, has been shown to be carcinogenic. It is unknown whether metronidazole is associated with carcinogenicity in humans.

    Fetal Toxicity

    • Tetracycline may cause fetal harm when used during pregnancy.

    • May cause permanent teeth discoloration (yellow-gray brown) and possibly inhibit bone development if Pylera is used during the 2nd/3rd trimester of pregnancy.

    • Advise the patient of the potential risk to the fetus if Pylera is used during pregnancy, or if the patient becomes pregnant during treatment.

    Maternal Toxicity

    • Rare but serious cases of maternal hepatotoxicity have been reported when tetracycline is used during pregnancy at high doses (>2g IV), resulting in stillborn or premature birth due to maternal pathology.

    Tooth Enamel Discoloration and Hypoplasia

    • May cause permanent discoloration of the teeth (yellow-gray-brown) if Pylera is used during tooth development (last half of the pregnancy, infancy, and childhood to the age of 8 years).

    • Pylera should not be used in this age group unless other drugs are not likely to be effective or are contraindicated.

    Central and Peripheral Nervous System Effects

    • Metronidazole: Convulsive seizures, encephalopathy, aseptic meningitis and peripheral neuropathy (including optic neuropathy) have been reported.

    • Tetracycline: Intracranial hypertension (IH), including pseudotumor cerebri, has been associated with the use of tetracyclines. Increased risk for IH in women of childbearing age who are overweight or have a history of IH. Avoid concomitant use with isotretinoin. IH usually resolves after discontinuation of treatment, but there is a risk for permanent visual loss. Perform ophthalmologic evaluation if visual disturbance occurs during treatment.

    • Bismuth-containing products: Cases of neurotoxicity associated with excessive doses of various bismuth-containing products have been reported.

    Development of Potential for Microbial Overgrowth

    • Use of tetracycline may result in overgrowth of nonsusceptible organisms, including fungi. Discontinue Pylera if superinfection occurs and institute appropriate therapy.

    Photosensitivity

    • Avoid exposure to the sun or sun lamps. Discontinue Pylera at the first sign of skin erythema.

    Darkening of the Tongue and/or Black Stool

    • May cause temporary and harmless darkening of the tongue and/or black stools. This is usually reversible within several days after discontinuing treatment.

    Use in Patients with Blood Dyscrasias

    • Use Pylera with care in patients with evidence of or history of blood dyscrasia.

    • Total and differential leukocyte counts are recommended before and after therapy.

    Increased Drug Plasma Concentrations in Patients with Hepatic Impairment  

    • Monitor patients with mild to moderate hepatic impairment for metronidazole associated adverse events.

    • Do not use Pylera in patients with severe hepatic impairment.

    Laboratory Test Interactions

    • May interfere with x-ray diagnostic procedures of the GI tract.

    • May cause a temporary and harmless darkening of the stool. This does not interfere with standard tests for occult blood.

    • May interfere with certain types of determinations of serum chemistry values (eg, AST, SGOT, ALT, SGPT, LDH, triglycerides, and hexokinase glucose). Values of zero may be observed.

    Development of Drug Resistant Bacteria

    • Prescribing Pylera in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.

    Cutaneous Reactions

    • Skin and subcutaneous disorders (eg, SJS, TEN, DRESS syndrome) have been reported. Discontinue treatment at the first evidence of a cutaneous reaction.

    Drug Interactions

    • Oral Contraceptives: Pylera may make oral contraceptives less effective. Advise women of child-bearing potential to use a different or additional form of contraception during treatment.

    • Anticoagulants: Pylera may change the effects of warfarin and other anticoagulants. Metronidazole has shown to potentiate the effects of warfarin and anticoagulants leading to a prolongation of prothrombin time. Monitor closely prothrombin time, INT, or other suitable tests if Pylera is used with warfarin. Monitor for evidence of bleeding.

    • Lithium: In patients stabilized on relatively high doses of lithium, short-term use of Pylera may cause elevation of serum lithium concentrations and signs of lithium toxicity due to the interaction between metronidazole and lithium. Monitor lithium and serum creatinine concentrations daily for several days after starting treatment.

    • Busulfan: Metronidazole may increase plasma concentrations of busulfan and lead to busulfan toxicity. Avoid concomitant use of Pylera with busulfan, unless the benefit outweighs the risk. If unavoidable, then monitor for busulfan toxicity and busulfan plasma concentrations and adjust busulfan dose.

    • Drugs that prolong the QT interval: May prolong QT interval when used with drugs with a risk for prolonging the QT interval.

    Pregnancy Considerations

    Risk Summary

    • Pylera is contraindicated in pregnant women.

    • May cause permanent teeth discoloration (yellow-gray brown) and possibly inhibit bone development if Pylera is used during the 2nd/3rd trimester of pregnancy.

    • Advise the patient of the potential risk to the fetus if Pylera is used during pregnancy, or if the patient becomes pregnant during treatment.

    Clinical Considerations

    • Maternal Adverse Reactions: Rare but serious cases of maternal hepatotoxicity have been reported when tetracycline is used during pregnancy at high doses (>2g IV), resulting in stillborn or premature birth due to maternal pathology.

    Nursing Mother Considerations

    Risk Summary

    • It is not known whether bismuth subcitrate, the third component of Pylera, is present in human milk. It is not known what effect metronidazole, tetracycline or bismuth has on the breastfed infant or on milk production.

    • Due to the potential risk, women should pump and discard human milk during Pylera therapy, and for 2 days after the last dose.

    Pediatric Considerations

    Safety and efficacy have not been established.

    Geriatric Considerations

    Because elderly patients are more likely to have decreased renal function, additional monitoring may be required.

    Renal Impairment Considerations

    Severe renal impairment: higher serum concentration of tetracycline may lead to azotemia, hyperphosphatemia, and acidosis.

    Hepatic Impairment Considerations

    Mild to moderate hepatic impairment: monitor for metronidazole associated adverse events.

    Severe hepatic impairment: not recommended.

    Pylera Pharmacokinetics

    Absorption

    Metronidazole

    • Peak plasma concentrations are reached between 1 to 2 hours.

    Tetracycline Hydrochloride

    • 60% to 90% absorbed in the stomach and upper small intestine.

    Distribution

    Bismuth Subcitrate Potassium (Bismuth)

    • Distributed throughout the entire body. Highly plasma protein bound (>90%).

    Metronidazole

    • Distributed in CSF, saliva, and breast milk. Less than 20% is bound to plasma proteins.

    Tetracycline Hydrochloride

    • Distributed into most body tissues, fluids, bile, and undergoes varying degrees of enterohepatic recirculation. Readily crosses the placenta and is excreted in high amounts in breast milk.

    Elimination

    Bismuth Subcitrate Potassium (Bismuth)

    • Elimination half-life: ~5 days in both blood and urine.

    Metronidazole

    • Elimination half-life: 8 hours. Renal (60–80%), fecal (6–15%). Renal clearance: ~10 mL/min/1.73m2.

    Tetracycline Hydrochloride

    • Renal, fecal.

    Pylera Interactions

    Interactions

    See Contraindications. May antagonize oral contraceptives (use non-hormonal backup method). Absorption reduced by antacids containing aluminum, magnesium, or calcium; and by iron, zinc, sodium bicarbonate, and dietary calcium (clinical significance unknown). Potentiated by CYP450 inhibitors (eg, cimetidine). Antagonized by CYP450 inducers (eg, phenytoin, phenobarbital); monitor phenytoin levels. Potentiates busulfan; avoid or monitor if clinically indicated. Monitor lithium, warfarin. QT prolongation esp. when concomitant drugs that prolong the QT interval. Intracranial hypertension with concomitant isotretinoin; avoid. May interfere with GI X-rays, liver function tests, others.

    Pylera Adverse Reactions

    Adverse Reactions

    Abnormal stool, diarrhea, nausea, headache; encephalopathy, peripheral neuropathy, aseptic meningitis, intracranial hypertension (monitor), neurotoxicity, tongue darkening, leukopenia, rash.

    Pylera Clinical Trials

    Clinical Trials

    The approval was based on an open-label, parallel-group, active-controlled, multicenter study in Helicobacter pylori positive patients with current duodenal ulcer or a history of duodenal ulcer disease was conducted in the United States and Canada (the North American Study). 

    Patients were randomly assigned to receive 1 of the following 10-day treatment regimens:

    • Three Pylera capsules four times daily, after meals and at bedtime plus 20 mg omeprazole twice a day after the morning and evening meals (OBMT). 

    • Clarithromycin 500 mg plus 1000 mg amoxicillin plus 20 mg omeprazole twice a day before the morning and evening meals (OAC).  

    Results showed the following H. pylori eradication rates for OBMT vs OAC at 8 weeks after the 10-day treatment regimen, respectively:

    • Per Protocol: 92.5% vs 85.7% (difference, 6.8% [95% CI, -0.9, 14.5])

    • Modified Intent-to-Treat: 87.7% vs 83.2% (difference, 4.5% [95% CI, -3.9, 12.8])

    Pylera Note

    Not Applicable

    Pylera Patient Counseling

    Patient Counseling

    Lactation

    • Advise the lactating women to pump and discard their milk during treatment with Pylera and for 2 days after the therapy ends.

    Hypersensitivity

    • Inform patients that Pylera may cause allergic reactions and to discontinue Pylera at the first sign of urticaria, erythematous rash, flushing, and fever or other symptoms of an allergic reaction.

    Central Nervous System Effects

    • Inform patients of the risk of central and peripheral nervous system effects with Pylera and to discontinue Pylera and report immediately to their health-care provider if any neurologic symptoms occur. 

    Photosensitivity

    • Avoid exposure to sun or sun lamps while taking Pylera. 

    Darkening of the Tongue and/or Stool

    • Inform patients that Pylera may cause temporary and harmless darkening of the tongue and/or black stool generally reversible within several days after treatment is stopped. Stool darkening should not be confused with melena (blood in the stool).

    Administration with Fluids

    • Instruct patients to swallow the Pylera capsules whole with a full glass of water (8 ounces). Ingestion of adequate amounts of fluid,particularly with the bedtime dose, is recommended to reduce the risk of esophageal irritation and ulceration by  tetracycline hydrochloride.

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