Telithromycin (Ketek) is a macrolide antibiotic that inhibits bacterial protein synthesis.
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It is used in the treatment of mild to moderate community-acquired pneumonia (CAP) due to:
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Streptococcus pneumoniae (including multidrug-resistant isolates)
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Chlamydophila (also known as Chlamydia) pneumoniae
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Haemophilus influenzae
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Moraxella catarrhalis
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Mycoplasma pneumoniae in patients 18 years and older.
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Telithromycin Dose in Adults
Telithromycin dosage in the treatment of Community-acquired pneumonia (CAP):
- 800 mg orally once daily given for 7-10 days
Telithromycin Dose in Childrens
Not recommended for use in children.
Pregnancy Risk Factor C
- Animal reproduction studies have shown that adverse events can be observed
Use of telithromycin while breastfeeding
- It is unknown if telithromycin excreted in breastmilk or not.
- If the product is being administered to a nursing mother, it is recommended that caution be taken.
Telithromycin dose in Renal disease:
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CrCl ≥ 30 mL/minute:
- No dosage adjustment required
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CrCl <30 mL/minute:
- 600 mg once daily given
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CrCl <30 mL/minute and concomitant hepatic impairment:
- 400 mg once daily given
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Hemodialysis:
- 600 mg once daily given
- administer after dialysis on dialysis days
Telithromycin dose in liver disease:
- No dosage adjustment required, unless concurrent renal impairment (eg.,CrCl <30 mL/minute) is present.
Common Side Effects of Telithromycin Include:
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Gastrointestinal:
- Diarrhea
Less Common Side Effects of Telithromycin Include:
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Central Nervous System:
- Headache
- Dizziness
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Gastrointestinal:
- Nausea
- Vomiting
- Dysgeusia
- Loose Stools
Rare side effects of Telithromycin:
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Central Nervous System:
- Drowsiness
- Fatigue
- Insomnia
- Vertigo
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Dermatologic:
- Diaphoresis
- Skin Rash
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Gastrointestinal:
- Abdominal Distension
- Abdominal Pain
- Anorexia
- Constipation
- Dyspepsia
- Flatulence
- Gastric Distress
- Gastritis
- Gastroenteritis
- Glossitis
- Oral Candidiasis
- Stomatitis
- Xerostomia
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Genitourinary:
- Fungal Vaginosis
- Vaginitis
- Vulvovaginal Candidiasis
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Hematologic & Oncologic:
- Thrombocythemia
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Hepatic:
- Abnormal Hepatic Function Tests
- Increased Serum Transaminases
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Ophthalmic:
- Accommodation Disturbance
- Blurred Vision
- Diplopia
Contraindication to Telithromycin (Ketek) Include:
- Hypersensitivity to telithromycin or macrolide antibiotics or any component of the formulation
- myasthenia gravis
- Previous history of hepatitis and/or jaundice associated with telithromycin or other macrolides antibiotic use
- concurrent use of colchicine (if the patient has concomitant renal or hepatic impairment), cisapride, pimozide, lovastatin, or simvastatin
Warnings and precautions
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Modified cardiac conduction
- It can prolong QTc interval and increase the risk of ventricular arrhythmias including torsades-de-pointes.
- Patients with congenital prolongation or QTc interval, ongoing hypokalemia, hypomagnesemia, significant bradycardia or concurrent QTc-prolonging drug therapy (eg class Ia or class III antiarrhythmics) should be avoided
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Hepatic effects
- In some cases, acute hepatic failure or severe liver injury (some fatal) were seen.
- If you notice signs or symptoms of hepatitis, stop treatment and get liver function testing.
- Permanently stop if clinical hepatitis, transaminase or transaminase testing are combined with other systemic symptoms.
- Patients with a history of hepatitis or jaundice due to the use of telithromycin, any macrolide antibiotic, should not be readministered.
- We have also seen less severe hepatic dysfunction due to increased liver enzymes, hepatitis with or with out jaundice.
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Superinfection
- Extended use can lead to fungal or bacterial overinfections, such as C. difficile-associated diarrhea(CDAD) and pseudomembranous collitis. CDAD can be observed up to 2 months after antibiotic treatment.
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Syncope
- It can cause loss of consciousness (possibly vagal-related).
- These events can cause impairments in the ability to drive or operate machinery. Patients should be advised to exercise caution while waiting for results.
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Visual disturbances:
- It can cause visual disturbances, such as blurred vision, altered accommodation ability, diplopia or changes in sight.
- Most cases are mild to moderate in severity, though severe cases have been reported.
- These events could affect the ability to drive or operate machinery. Patients should be advised to exercise caution until they are fully understood.
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Myasthenia gravis: [U.S. Boxed Warning]:
- Patients with myasthenia Gravis have been diagnosed with life-threatening (including fatal!) respiratory failure. It is not recommended that they be treated.
- Myasthenia gravis may be exacerbated within hours after the first dose.
- It has been observed that respiratory failure can quickly progress from onset to progression.
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Renal impairment
- Patients with impaired renal function should be cautious
- severe impairment (CrCl <30 mL/minute) needs dosage adjustment.
Telithromycin: Drug Interaction
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Alosetron |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron. |
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Apixaban |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Apixaban. |
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BCG Vaccine (Immunization) |
Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). |
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Benperidol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benperidol. |
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Benzhydrocodone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benzhydrocodone. Specifically, the concentration of hydrocodone may be increased. |
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Betamethasone (Ophthalmic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Betamethasone (Ophthalmic). |
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Bictegravir |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bictegravir. |
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Bortezomib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bortezomib. |
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Bosentan |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Bosentan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bosentan. Management: Concomitant use of both a CYP2C9 inhibitor and a CYP3A inhibitor or a single agent that inhibits both enzymes with bosentan is likely to cause a large increase in serum concentrations of bosentan and is not recommended. See monograph for details. |
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Brentuximab Vedotin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. |
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Brinzolamide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brinzolamide. |
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Budesonide (Nasal) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Nasal). |
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Budesonide (Oral Inhalation) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Oral Inhalation). |
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Buprenorphine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Buprenorphine. |
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Calcifediol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Calcifediol. |
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Cannabidiol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabidiol. |
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Cannabis |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased. |
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Cardiac Glycosides |
Macrolide Antibiotics may increase the serum concentration of Cardiac Glycosides. |
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Cinacalcet |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cinacalcet. |
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Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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CloZAPine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of CloZAPine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Codeine |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Codeine. |
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Corticosteroids (Orally Inhaled) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Corticosteroids (Orally Inhaled). Management: Orally inhaled fluticasone propionate with a strong CYP3A4 inhibitor is not recommended. Exceptions: Beclomethasone (Oral Inhalation); Triamcinolone (Systemic). |
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Corticosteroids (Systemic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Corticosteroids (Systemic). Exceptions: MethylPREDNISolone; PrednisoLONE (Systemic); PredniSONE. |
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CycloSPORINE (Systemic) |
Telithromycin may increase the serum concentration of CycloSPORINE (Systemic). |
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CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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CYP3A4 Inhibitors (Moderate) |
May increase the serum concentration of Telithromycin. |
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CYP3A4 Inhibitors (Strong) |
May increase the serum concentration of Telithromycin. |
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Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Dexamethasone (Ophthalmic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dexamethasone (Ophthalmic). |
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Dienogest |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dienogest. |
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Dofetilide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide. |
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Doxercalciferol |
CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Doxercalciferol. |
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Dronabinol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronabinol. |
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Dutasteride |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dutasteride. |
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Estrogen Derivatives |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Estrogen Derivatives. |
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Evogliptin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Evogliptin. |
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Fosnetupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Fostamatinib |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fostamatinib. |
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Galantamine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Galantamine. |
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Gefitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Gefitinib. |
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HYDROcodone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of HYDROcodone. |
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Ifosfamide |
CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ifosfamide. |
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Imatinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imatinib. |
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Imidafenacin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imidafenacin. |
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Lacosamide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lacosamide. |
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Lactobacillus and Estriol |
Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. |
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Levobupivacaine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levobupivacaine. |
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Lumefantrine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lumefantrine. |
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MedroxyPROGESTERone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of MedroxyPROGESTERone. |
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Mirtazapine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Mirtazapine. |
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Naldemedine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Naldemedine. |
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Nalfurafine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nalfurafine. |
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Netupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Ospemifene |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ospemifene. |
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Oxybutynin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Oxybutynin. |
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Parecoxib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Parecoxib. |
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Paricalcitol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Paricalcitol. |
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Perhexiline |
CYP2D6 Inhibitors (Weak) may increase the serum concentration of Perhexiline. |
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Pimecrolimus |
CYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus. |
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Pitavastatin |
Telithromycin may increase the serum concentration of Pitavastatin. |
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Polatuzumab Vedotin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Polatuzumab Vedotin. Exposure to unconjugated MMAE, the cytotoxic small molecule component of polatuzumab vedotin, may be increased. |
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Pranlukast |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pranlukast. |
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Pravastatin |
Telithromycin may increase the serum concentration of Pravastatin. |
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Praziquantel |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Praziquantel. |
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PrednisoLONE (Systemic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of PrednisoLONE (Systemic). |
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PredniSONE |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of PredniSONE. |
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Propafenone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Propafenone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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QT-prolonging Agents (Highest Risk) |
QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
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Ramelteon |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ramelteon. |
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Repaglinide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Repaglinide. Management: The addition of a CYP2C8 inhibitor to this drug combination may substantially increase the magnitude of increase in repaglinide exposure. |
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Retapamulin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Retapamulin. Management: Avoid this combination in patients less than 2 years old. No action is required in other populations. |
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RomiDEPsin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of RomiDEPsin. |
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Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Sibutramine |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Sibutramine. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sibutramine. |
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Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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SORAfenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of SORAfenib. |
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Tacrolimus (Topical) |
Macrolide Antibiotics may increase the serum concentration of Tacrolimus (Topical). |
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Tasimelteon |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tasimelteon. |
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Tetrahydrocannabinol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol. |
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Tetrahydrocannabinol and Cannabidiol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol and Cannabidiol. |
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Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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TraMADol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of TraMADol. |
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Upadacitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Upadacitinib. |
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Vilanterol |
May increase the serum concentration of CYP3A4 Inhibitors (Strong). |
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Vitamin K Antagonists (eg, warfarin) |
Macrolide Antibiotics may increase the serum concentration of Vitamin K Antagonists. |
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Zolpidem |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zolpidem. |
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Risk Factor D (Consider therapy modification) |
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Abemaciclib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Abemaciclib. Management: In patients taking abemaciclib at a dose of 200 mg or 150 mg twice daily, reduce the dose to 100 mg twice daily when combined with strong CYP3A4 inhibitors. In patients taking abemaciclib 100 mg twice daily, decrease the dose to 50 mg twice daily. |
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Alitretinoin (Systemic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alitretinoin (Systemic). Management: Consider reducing the alitretinoin dose to 10 mg when used together with strong CYP3A4 inhibitors. Monitor for increased alitretinoin effects/toxicities if combined with a strong CYP3A4 inhibitor. |
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Almotriptan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Almotriptan. Management: Limit initial almotriptan adult dose to 6.25 mg and maximum adult dose to 12.5 mg/24-hrs when used with a strong CYP3A4 inhibitor. Avoid concurrent use in patients with impaired hepatic or renal function. |
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ALPRAZolam |
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Antineoplastic Agents (Vinca Alkaloids) |
Macrolide Antibiotics may increase the serum concentration of Antineoplastic Agents (Vinca Alkaloids). Macrolides may also increase the distribution of Vinca Alkaloids into certain cells and/or tissues. Management: Consider an alternative to using a macrolide antibiotic when possible in order to avoid the potential for increased vinca alkaloid toxicity. |
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ARIPiprazole |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of ARIPiprazole. Management: See full interaction monograph for details. |
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ARIPiprazole Lauroxil |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of ARIPiprazole Lauroxil. Management: Please refer to the full interaction monograph for details concerning the recommended dose adjustments. |
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AtorvaSTATin |
Telithromycin may increase the serum concentration of AtorvaSTATin. Management: Consider limiting atorvastatin to a max (adult) dose of 20 mg/day when used with telithromycin. Although not a specific recommendation in atorvastatin labeling, this is consistent with dosing for other strong CYP3A4 inhibitors, including clarithromycin. |
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Bedaquiline |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bedaquiline. Management: Limit duration of concurrent use of bedaquiline with CYP3A4 inhibitors to no more than 14 days, unless the benefit of continued use outweighs the possible risks. Monitor for toxic effects of bedaquiline. Exceptions discussed in separate monographs. |
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Brexpiprazole |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brexpiprazole. Management: Reduce brexpiprazole dose 50% with strong CYP3A4 inhibitors; reduce to 25% of usual if used with both a moderate CYP3A4 inhibitor and a CYP2D6 inhibitor in patients not being treated for MDD, or strong CYP3A4 inhibitor used in a CYP2D6 poor metabolizer. |
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Brigatinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brigatinib. Management: Avoid concurrent use of brigatinib with strong CYP3A4 inhibitors when possible. If combination cannot be avoided, reduce the brigatinib dose by approximately 50%, rounding to the nearest tablet strength (ie, from 180 mg to 90 mg, or from 90 mg to 60 mg). |
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Budesonide (Topical) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Topical). Management: Per US prescribing information, avoid this combination. Canadian product labeling does not recommend strict avoidance. If combined, monitor for excessive glucocorticoid effects as budesonide exposure may be increased. |
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BusPIRone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg daily and monitor patients for increased buspirone effects/toxicities if combined with strong CYP3A4 inhibitors. |
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Cabazitaxel |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cabazitaxel. Management: Concurrent use of cabazitaxel with strong inhibitors of CYP3A4 should be avoided when possible. If such a combination must be used, consider a 25% reduction in the cabazitaxel dose. |
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Cabozantinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cabozantinib. Management: Avoid use of a strong CYP3A4 inhibitor with cabozantinib if possible. If combined, cabozantinib dose adjustments are recommended and vary based on the cabozantinib product used and the indication for use. See monograph for details. |
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Calcium Channel Blockers |
Macrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers. Management: Consider using a noninteracting macrolide. Felodipine Canadian labeling specifically recommends avoiding its use in combination with clarithromycin. Exceptions: Clevidipine. |
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Cariprazine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cariprazine. Management: Cariprazine dose reductions of 50% are required; specific recommended management varies slightly for those stable on cariprazine versus those just starting cariprazine. See prescribing information or full interaction monograph for details. |
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Ceritinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ceritinib. Management: If such combinations cannot be avoided, the ceritinib dose should be reduced by approximately one-third (to the nearest 150 mg). Resume the prior ceritinib dose after cessation of the strong CYP3A4 inhibitor. Exceptions discussed in separate monographs. |
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Cilostazol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol. Management: Consider reducing the cilostazol dose to 50 mg twice daily in adult patients who are also receiving strong inhibitors of CYP3A4. |
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Cobicistat |
Telithromycin may increase the serum concentration of Cobicistat. Cobicistat may increase the serum concentration of Telithromycin. Management: Seek alternatives to telithromycin. US prescribing information for the combination product containing elvitegravir, cobicistat, emtricitabine, and tenofovir does not address this potential interaction. |
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Colchicine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Colchicine. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a strong CYP3A4 inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. See full monograph for details. |
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Copanlisib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Copanlisib. Management: If concomitant use of copanlisib and strong CYP3A4 inhibitors cannot be avoided, reduce the copanlisib dose to 45 mg. Monitor patients for increased copanlisib effects/toxicities. |
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Crizotinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Crizotinib. Management: Avoid concomitant use of crizotinib and strong CYP3A4 inhibitors whenever possible. If combined use cannot be avoided, decrease the crizotinib dose to 250 mg daily. Exceptions are discussed in separate monographs. |
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CYP3A4 Inducers (Strong) |
May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
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CYP3A4 Substrates (High risk with Inhibitors) |
CYP3A4 Inhibitors (Strong) may decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Exceptions: Alitretinoin (Systemic); AmLODIPine; Benzhydrocodone; Buprenorphine; Gefitinib; HYDROcodone; Mirtazapine; Praziquantel; Telithromycin; Vinorelbine. |
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Daclatasvir |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Daclatasvir. Management: Decrease the daclatasvir dose to 30 mg once daily if combined with a strong CYP3A4 inhibitor. No dose adjustment is needed when daclatasvir is used with darunavir/cobicistat. |
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Dasatinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib. Management: This combination should be avoided if possible. If combined, dasatinib dose reductions are recommended. See full monograph for details. Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Deflazacort |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Deflazacort. Management: Administer one third of the recommended deflazacort dose when used together with a strong or moderate CYP3A4 inhibitor. |
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Delamanid |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Delamanid. Management: Increase ECG monitoring frequency if delamanid is combined with strong CYP3A4 inhibitors due to the risk for QTc interval prolongation. Continue frequent ECG assessments throughout full delamanid treatment period. Exceptions discussed separately. |
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DOCEtaxel |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of DOCEtaxel. Management: Avoid the concomitant use of docetaxel and strong CYP3A4 inhibitors when possible. If combined use is unavoidable, consider a 50% docetaxel dose reduction and monitor for increased docetaxel toxicities. |
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DOXOrubicin (Conventional) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to strong CYP3A4 inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided. |
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Drospirenone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Drospirenone. Management: Drospirenone use is contraindicated specifically when the strong CYP3A4 inhibitors atazanavir and cobicistat are administered concurrently. Caution should be used when drospirenone is coadministered with other strong CYP3A4 inhibitors. |
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Duvelisib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Duvelisib. Management: Reduce the dose of duvelisib to 15 mg twice a day when used together with a strong CYP3A4 inhibitor. |
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Elagolix |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Elagolix. Management: Use of the elagolix 200 mg twice daily dose with a strong CYP3A4 inhibitor for longer than 1 month is not recommended. Limit combined use of the elagolix 150 mg once daily dose with a strong CYP3A4 inhibitor to a maximum of 6 months. |
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Eliglustat |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eliglustat. Management: Use should be avoided under some circumstances. See full drug interaction monograph for details. |
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Encorafenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Encorafenib. Management: Avoid concomitant use of encorafenib and strong CYP3A4 inhibitors whenever possible. If concomitant administration is unavoidable, decrease the encorafenib dose. See monograph for details. |
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Entrectinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Entrectinib. Management: Avoid strong CYP3A4 inhibitors during treatment with entrectinib. Reduce dose to 100 mg/day if combination cannot be avoided in adults and those 12 yrs of age or older with a BSA of at least 1.5 square meters. No alternative dosing provided for others. |
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Enzalutamide |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. |
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Erdafitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Erdafitinib. Management: Avoid concomitant use of erdafitinib and strong CYP3A4 inhibitors when possible. If combined, monitor closely for erdafitinib adverse reactions and consider dose modifications accordingly. |
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Ergot Derivatives |
Macrolide Antibiotics may increase the serum concentration of Ergot Derivatives. Cabergoline and Clarithromycin may interact, see specific monograph for full details. Exceptions: Cabergoline; Nicergoline; Pergolide. |
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Erlotinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements). |
|
Estazolam |
Macrolide Antibiotics may increase the serum concentration of Estazolam. Management: Consider an alternative less likely to interact. Azithromycin is likely a lower-risk macrolide, and benzodiazepines less dependent on CYP3A metabolism (e.g., lorazepam, oxazepam) are similarly less likely to interact. |
|
Eszopiclone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eszopiclone. Management: Limit the eszopiclone dose to 2 mg daily when combined with strong CYP3A4 inhibitors and monitor for increased eszopiclone effects and toxicities (eg, somnolence, drowsiness, CNS depression). |
|
Etizolam |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Etizolam. Management: Consider use of lower etizolam doses when using this combination; specific recommendations concerning dose adjustment are not available. Monitor clinical response to the combination closely. |
|
Fedratinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fedratinib. Management: Consider alternatives when possible. If used together, decrease fedratinib dose to 200 mg/day. After the inhibitor is stopped, increase fedratinib to 300 mg/day for the first 2 weeks and then to 400 mg/day as tolerated. |
|
FentaNYL |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of FentaNYL. Management: Monitor patients closely for several days following initiation of this combination, and adjust fentanyl dose as necessary. |
|
Fesoterodine |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fesoterodine. Management: Avoid fesoterodine doses greater than 4 mg daily in adult patients who are also receiving strong CYP3A4 inhibitors. |
|
Fluticasone (Oral Inhalation) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fluticasone (Oral Inhalation). Management: Use of orally inhaled fluticasone propionate with strong CYP3A4 inhibitors is not recommended. Use of orally inhaled fluticasone furoate with strong CYP3A4 inhibitors should be done with caution. Monitor patients using such a combination more closely. |
|
Gilteritinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Gilteritinib. Management: Consider alternatives to the use of a strong CYP3A4 inhibitor with gilteritinib. If the combination cannot be avoided, monitor more closely for evidence of gilteritinib toxicities. |
|
Glasdegib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Glasdegib. Management: Consider alternatives to this combination when possible. If the combination must be used, monitor closely for evidence of QT interval prolongation and other adverse reactions to glasdegib. |
|
GuanFACINE |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of GuanFACINE. Management: Reduce the guanfacine dose by 50% when initiating this combination. |
|
Iloperidone |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolites P88 and P95 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Management: Reduce iloperidone dose by half when administered with a strong CYP3A4 inhibitor. |
|
Ivacaftor |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivacaftor. Management: Ivacaftor dose reductions are required; consult full monograph content for specific age- and weight-based recommendations. |
|
Ivosidenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivosidenib. Management: Avoid use of a strong CYP3A4 inhibitor with ivosidenib whenever possible. When combined use is required, reduce the ivosidenib dose to 250 mg once daily. Drugs listed as exceptions are discussed in further detail in separate drug interaction monographs. |
|
Ixabepilone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ixabepilone. |
|
Larotrectinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Larotrectinib. Management: Avoid use of strong CYP3A4 inhibitors with larotrectinib. If this combination cannot be avoided, reduce the larotrectinib dose by 50%. Increase to previous dose after stopping the inhibitor after a period of 3 to 5 times the inhibitor half-life. |
|
Levomilnacipran |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levomilnacipran. Management: Do not exceed a maximum adult levomilnacipran dose of 80 mg/day in patients also receiving strong CYP3A4 inhibitors. |
|
Lorlatinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lorlatinib. Management: Avoid use of lorlatinib with strong CYP3A4 inhibitors. If the combination cannot be avoided, reduce the lorlatinib dose from 100 mg once daily to 75 mg once daily, or from 75 mg once daily to 50 mg once daily. |
|
Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
|
Manidipine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Manidipine. Management: Consider avoiding concomitant use of manidipine and strong CYP3A4 inhibitors. If combined, monitor closely for increased manidipine effects and toxicities. Manidipine dose reductions may be required. |
|
Maraviroc |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Maraviroc. Management: Reduce the adult dose of maraviroc to 150 mg twice daily when used with a strong CYP3A4 inhibitor. Do not use maraviroc with strong CYP3A4 inhibitors in patients with Clcr less than 30 mL/min. |
|
Meperidine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Meperidine. Management: Consider reducing meperidine dose if concomitant use with strong CYP3A4 inhibitors is required. Monitor for signs and symptoms of respiratory depression and sedation when these agents are combined. |
|
MethylPREDNISolone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of MethylPREDNISolone. Management: Consider methylprednisolone dose reduction in patients receiving strong CYP3A4 inhibitors and monitor for increased steroid related adverse effects. |
|
Midazolam |
Macrolide Antibiotics may increase the serum concentration of Midazolam. Management: Consider an alternative less likely to interact. Azithromycin is likely a lower-risk macrolide, and benzodiazepines less dependent on CYP3A metabolism (e.g., lorazepam, oxazepam) are similarly less likely to interact. |
|
Midostaurin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Midostaurin. Management: Seek alternatives to the concomitant use of midostaurin and strong CYP3A4 inhibitors if possible. If concomitant use cannot be avoided, monitor patients for increased risk of adverse reactions. Exceptions are discussed in separate monographs. |
|
MiFEPRIStone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of MiFEPRIStone. Management: Limit mifepristone adult dose, when used for treatment of hyperglycemia in Cushing's syndrome, to a maximum of 600 mg/day when combined with a strong CYP3A4 inhibitor. Monitor for increased mifepristone toxicity regardless of dose or indication. |
|
MiFEPRIStone |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. |
|
Mirodenafil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Mirodenafil. Management: Consider using a lower dose of mirodenafil when used with strong CYP3A4 inhibitors. Monitor for increased mirodenafil effects/toxicities with the use of this combination. |
|
Mitotane |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
|
Nilotinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nilotinib. Management: Avoid if possible. If combination needed, decrease nilotinib to 300 mg once/day for patients with resistant or intolerant Ph+ CML or to 200 mg once/day for patients with newly diagnosed Ph+ CML in chronic phase. Exceptions discussed in separate monograph. |
|
Olaparib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Olaparib. Management: Avoid use of strong CYP3A4 inhibitors in patients being treated with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib should be reduced to 100 mg twice daily. |
|
OxyCODONE |
CYP3A4 Inhibitors (Strong) may enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Strong) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite oxymorphone may also be increased. |
|
Panobinostat |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Panobinostat. Management: Reduce the panobinostat dose to 10 mg when it must be used with a strong CYP3A4 inhibitor. |
|
PAZOPanib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of PAZOPanib. Management: Avoid concurrent use of pazopanib with strong inhibitors of CYP3A4 whenever possible. If it is not possible to avoid such a combination, reduce pazopanib adult dose to 400 mg. Further dose reductions may also be required. |
|
Pexidartinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pexidartinib. Management: Avoid use of pexidartinib with strong CYP3A4 inhibitors if possible. If combined use cannot be avoided, the pexidartinib dose should be reduced. Decrease 800 mg or 600 mg daily doses to 200 mg twice daily. Decrease doses of 400 mg/day to 200 mg/day. |
|
Pimavanserin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimavanserin. Management: Decrease the pimavanserin dose to 10 mg daily when combined with strong CYP3A4 inhibitors. |
|
Piperaquine |
CYP3A4 Inhibitors (Strong) may enhance the QTc-prolonging effect of Piperaquine. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Piperaquine. Management: Avoid concomitant use of piperaquine and strong CYP3A4 inhibitors when possible. If the combination cannot be avoided, frequent ECG monitoring is recommended due to the risk for QTc prolongation. Exceptions are discussed separately. |
|
PONATinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib. Management: Per ponatinib U.S. prescribing information, the adult starting dose of ponatinib should be reduced to 30 mg daily during treatment with any strong CYP3A4 inhibitor. |
|
QUEtiapine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of QUEtiapine. Management: In quetiapine treated patients, reduce quetiapine to one-sixth of regular dose after starting strong CYP3A4 inhibitor. In those on strong CYP3A4 inhibitors, start quetiapine at lowest dose and up-titrate as needed. Exceptions discussed separately. |
|
QuiNINE |
Telithromycin may enhance the QTc-prolonging effect of QuiNINE. Telithromycin may increase the serum concentration of QuiNINE. Management: Concomitant therapy with quinine and telithromycin should be avoided, if possible, due to the risk of elevated quinine serum levels and potential adverse cardiac effects. If combined, monitor for QT prolongation and quinine toxicities. |
|
Reboxetine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Reboxetine. |
|
Ribociclib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ribociclib. Management: Avoid use of ribociclib with strong CYP3A4 inhibitors when possible; if combined use cannot be avoided, reduce ribociclib dose to 400 mg once daily. Exceptions are discussed in separate monographs. |
|
Rifamycin Derivatives |
Macrolide Antibiotics may decrease the metabolism of Rifamycin Derivatives. Exceptions: Rifapentine. |
|
Rilpivirine |
Macrolide Antibiotics may increase the serum concentration of Rilpivirine. Management: Consider the use of azithromycin or another non-macrolide alternative when appropriate to avoid this potential interaction. |
|
Ruxolitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ruxolitinib. Management: This combination should be avoided under some circumstances. See monograph for details. |
|
SAXagliptin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of SAXagliptin. Management: Saxagliptin U.S. product labeling recommends limiting saxagliptin adult dose to 2.5 mg/day when used with a strong CYP3A4 inhibitor. Monitor for increased saxagliptin levels/effects. A similar recommendation is not made in the Canadian product labeling. |
|
Sildenafil |
Telithromycin may increase the serum concentration of Sildenafil. |
|
Sirolimus |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sirolimus. Management: Consider avoiding concurrent use of sirolimus with strong CYP3A4 inhibitors in order to minimize the risk for sirolimus toxicity. Concomitant use of sirolimus and voriconazole or posaconazole is contraindicated. |
|
Sodium Picosulfate |
Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. |
|
Solifenacin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Solifenacin. Management: Limit solifenacin doses to 5 mg daily when combined with strong CYP3A4 inhibitors. |
|
St John's Wort |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
|
Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
|
SUFentanil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of SUFentanil. Management: If a strong CYP3A4 inhibitor is initiated in a patient on sufentanil, consider a sufentanil dose reduction and monitor for increased sufentanil effects and toxicities (eg, respiratory depression). |
|
SUNItinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of SUNItinib. Management: Avoid when possible. If such a combination cannot be avoided, sunitinib dose decreases are recommended, and vary by indication. See full monograph for details. |
|
Tacrolimus (Systemic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tacrolimus (Systemic). Management: Monitor clinical tacrolimus response closely and frequently monitor tacrolimus serum concentrations with concurrent use of any strong CYP3A4 inhibitor. Tacrolimus dose reductions and/or prolongation of the dosing interval will likely be required. |
|
Tadalafil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tadalafil. Management: Recommendations regarding use of tadalafil in patients also receiving strong CYP3A4 inhibitors may vary based on indication and/or international labeling. Consult appropriate product labeling. |
|
Temsirolimus |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Temsirolimus. Management: Avoid concomitant use of temsirolimus and strong CYP3A4 inhibitors whenever possible. If combined, decrease temsirolimus dose to 12.5 mg per week and monitor patients for increased temsirolimus effects and toxicities. |
|
Tezacaftor |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tezacaftor. Management: When combined with strong CYP3A4 inhibitors, tezacaftor/ivacaftor should be administered in the morning, twice a week, approximately 3 to 4 days apart. No evening doses of ivacaftor alone should be administered. |
|
Thiotepa |
CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Thiotepa. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Thiotepa. Management: Thiotepa prescribing information recommends avoiding concomitant use of thiotepa and strong CYP3A4 inhibitors. If concomitant use is unavoidable, monitor for adverse effects and decreased efficacy. |
|
Tofacitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tofacitinib. Management: Tofacitinib dose reductions are recommended when combined with strong CYP3A4 inhibitors. Recommended dose adjustments vary by tofacitinib formulation and therapeutic indication. See full monograph for details. |
|
Tolterodine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tolterodine. Management: The maximum recommended adult dose of tolterodine is 2 mg/day when used together with a strong CYP3A4 inhibitor. |
|
Toremifene |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Toremifene. Management: Use of toremifene with strong CYP3A4 inhibitors should be avoided if possible. If coadministration is necessary, monitor for increased toremifene toxicities, including QTc interval prolongation. Exceptions are discussed in separate monograph. |
|
TraZODone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of TraZODone. Management: Consider the use of a lower trazodone dose and monitor for increased trazodone effects (eg, sedation, QTc prolongation) if combined with strong CYP3A4 inhibitors. |
|
Typhoid Vaccine |
Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. |
|
Valbenazine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Valbenazine. Management: Reduce the valbenazine dose to 40 mg daily when combined with strong CYP3A4 inhibitors. |
|
Vardenafil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vardenafil. Management: Recommendations regarding concomitant use of vardenafil with strong CYP3A4 inhibitors may vary depending on brand name (e.g., Levitra, Staxyn) or by international labeling. See full drug interaction monograph for details. |
|
Vemurafenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vemurafenib. Management: Avoid concurrent use of vemurafenib with strong CYP3A4 inhibitors when possible. Consider use of an alternative that is not a strong inhibitor of CYP3A4 as clinically appropriate. Exceptions are discussed in separate monographs. |
|
Venetoclax |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Venetoclax. Management: This combination is contraindicated during venetoclax initiation and ramp-up in patients with CLL/SLL. Reduced venetoclax doses are required during ramp-up for patients with AML, and reduced doses are required for all patients during maintenance therapy. |
|
Verapamil |
Telithromycin may enhance the bradycardic effect of Verapamil. Telithromycin may enhance the hypotensive effect of Verapamil. |
|
Vilazodone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. Management: Limit maximum adult vilazodone dose to 20 mg daily in patients receiving strong CYP3A4 inhibitors. The original vilazodone dose can be resumed following discontinuation of the strong CYP3A4 inhibitor. |
|
Zopiclone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zopiclone. Management: The initial starting adult dose of zopiclone should not exceed 3.75 mg if combined with a strong CYP3A4 inhibitor. Monitor patients for signs and symptoms of zopiclone toxicity if these agents are combined. |
|
Zuclopenthixol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zuclopenthixol. Management: Consider zuclopenthixol dosage reduction with concomitant use of a strong CYP3A4 inhibitor (eg, ketoconazole) in poor CYP2D6 metabolizers or with strong CYP2D6 inhibitors (eg, paroxetine). Monitor for increased zuclopenthixol levels/toxicity. |
|
Risk Factor X (Avoid combination) |
|
|
Acalabrutinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Acalabrutinib. |
|
Ado-Trastuzumab Emtansine |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Ado-Trastuzumab Emtansine. Specifically, strong CYP3A4 inhibitors may increase concentrations of the cytotoxic DM1 component. |
|
Alfuzosin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alfuzosin. |
|
Aprepitant |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Aprepitant. |
|
Astemizole |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Astemizole. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Asunaprevir |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Asunaprevir. |
|
Avanafil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Avanafil. |
|
Axitinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Axitinib. Management: Avoid concurrent use of axitinib with any strong CYP3A inhibitor whenever possible. If a strong CYP3A inhibitor must be used with axitinib, a 50% axitinib dose reduction is recommended. |
|
Barnidipine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Barnidipine. |
|
BCG (Intravesical) |
Antibiotics may diminish the therapeutic effect of BCG (Intravesical). |
|
Blonanserin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Blonanserin. |
|
Bosutinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bosutinib. |
|
Bromocriptine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bromocriptine. |
|
Budesonide (Systemic) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Systemic). |
|
Cholera Vaccine |
Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. |
|
Cisapride |
Telithromycin may increase the serum concentration of Cisapride. |
|
Cobimetinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cobimetinib. |
|
Conivaptan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan. |
|
Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Dabrafenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dabrafenib. |
|
Dapoxetine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dapoxetine. |
|
Disopyramide |
Telithromycin may enhance the QTc-prolonging effect of Disopyramide. Telithromycin may increase the serum concentration of Disopyramide. |
|
Domperidone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Domperidone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Dronedarone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronedarone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Eletriptan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eletriptan. |
|
Eplerenone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eplerenone. |
|
Everolimus |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Everolimus. |
|
Flibanserin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Flibanserin. |
|
Fluticasone (Nasal) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fluticasone (Nasal). |
|
Fosaprepitant |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fosaprepitant. |
|
Fusidic Acid (Systemic) |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Halofantrine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Halofantrine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Ibrutinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ibrutinib. Management: Avoid concomitant use of ibrutinib and strong CYP3A4 inhibitors. If a strong CYP3A4 inhibitor must be used short-term (eg, anti-infectives for 7 days or less), interrupt ibrutinib therapy until the strong CYP3A4 inhibitor is discontinued. |
|
Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Irinotecan Products |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Irinotecan Products. Specifically, serum concentrations of SN-38 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Irinotecan Products. |
|
Isavuconazonium Sulfate |
CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Isavuconazonium Sulfate. Specifically, CYP3A4 Inhibitors (Strong) may increase isavuconazole serum concentrations. Management: Combined use is considered contraindicated per US labeling. Lopinavir/ritonavir (and possibly other uses of ritonavir doses less than 400 mg every 12 hours) is treated as a possible exception to this contraindication despite strongly inhibiting CYP3A4. |
|
Itraconazole |
May increase the serum concentration of Telithromycin. Telithromycin may increase the serum concentration of Itraconazole. |
|
Ivabradine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivabradine. |
|
Ketoconazole (Systemic) |
May increase the serum concentration of Telithromycin. Telithromycin may increase the serum concentration of Ketoconazole (Systemic). |
|
Lapatinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lapatinib. Management: If an overlap in therapy cannot be avoided, consider reducing lapatinib adult dose to 500 mg/day during, and within 1 week of completing, treatment with the strong CYP3A4 inhibitor. |
|
Lefamulin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets and strong inhibitors of CYP3A4. |
|
Lercanidipine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lercanidipine. |
|
Lomitapide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lomitapide. |
|
Lovastatin |
Telithromycin may increase the serum concentration of Lovastatin. |
|
Lurasidone |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lurasidone. |
|
Macitentan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Macitentan. |
|
Mizolastine |
Macrolide Antibiotics may increase the serum concentration of Mizolastine. |
|
Naloxegol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Naloxegol. |
|
Neratinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Neratinib. |
|
NiMODipine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of NiMODipine. |
|
Nisoldipine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nisoldipine. |
|
Palbociclib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Palbociclib. |
|
Pimozide |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimozide. |
|
Radotinib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Radotinib. |
|
Ranolazine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ranolazine. |
|
Red Yeast Rice |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Red Yeast Rice. Specifically, concentrations of lovastatin and related compounds found in Red Yeast Rice may be increased. |
|
Regorafenib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Regorafenib. |
|
Rupatadine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Rupatadine. |
|
Salmeterol |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol. |
|
Silodosin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Silodosin. |
|
Simeprevir |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Simeprevir. |
|
Simvastatin |
Telithromycin may increase the serum concentration of Simvastatin. |
|
Sonidegib |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sonidegib. |
|
Suvorexant |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Suvorexant. |
|
Tamsulosin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tamsulosin. |
|
Terfenadine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Terfenadine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Ticagrelor |
CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ticagrelor. |
|
Tolvaptan |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tolvaptan. |
|
Trabectedin |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Trabectedin. |
|
Triazolam |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Triazolam. |
|
Udenafil |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Udenafil. |
|
Ulipristal |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ulipristal. Management: This is specific for when ulipristal is being used for signs/symptoms of uterine fibroids (Canadian indication). When ulipristal is used as an emergency contraceptive, patients receiving this combo should be monitored for ulipristal toxicity. |
|
VinCRIStine (Liposomal) |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of VinCRIStine (Liposomal). |
|
Vinflunine |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vinflunine. |
|
Vorapaxar |
CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vorapaxar. |
Monitor:
- Liver function tests
- signs/symptoms of liver failure (eg, jaundice, fatigue, malaise, anorexia, nausea, bilirubinemia, acholic stools, liver tenderness, hepatomegaly)
- visual acuity
How to administer Telithromycin (Ketek)?
Oral:
- It may be administered with or without food.
Mechanism of action of Telithromycin (Ketek):
- It inhibits the synthesis of bacterial proteins by binding to two locations on the 50S subunit of the ribosomal ribosomal ribosomal.
- Telithromycin can also alter TNF-alpha and IL-1alpha secretion.
- This immunomodulatory effect is not clinically significant.
Absorption:
- Rapid
Distribution:
- 2.9 L/kg
Protein binding:
- 60% to 70%; primarily to albumin
Metabolism:
- mainly Hepatic, via CYP3A4 (50%) and non-CYP-mediated pathways
Bioavailability:
- 57%
Half-life elimination:
- 10 hours
Time to peak, plasma:
- 1 hour
Excretion:
- Via Urine (13% unchanged drug, remainder as metabolites); feces (7% unchanged drug
International Brands of Telithromycin:
- Engtel
- Ketek
- Levviax
Telithromycin Brands in Pakistan:
Telithromycin is not available in Pakistan.