Telithromycin (Ketek) - Complete Drug Information

A macrolide antibiotic called telithromycin (Ketek) prevents bacteria from synthesising proteins.

  • Mild to moderate community-acquired pneumonia (CAP) is treated with it because:

    • Streptococcus pneumoniae (including multidrug-resistant isolates)

    • Chlamydophila (also known as Chlamydia) pneumoniae

    • Haemophilus influenzae

    • Moraxella catarrhalis

    • Mycoplasma pneumoniae in 18 years and older patients

Telithromycin Dose in Adults

Telithromycin dosage in the treatment of Community-acquired pneumonia (CAP):

  • 800 mg administered orally once daily for 7 to 10 days

Telithromycin Dose in Children

Not recommended for use in children.

Pregnancy Risk Factor C

  • Studies on animal reproduction have demonstrated that negative outcomes are possible.

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:

  • CrCl ≥ 30 mL/minute:

    • Dosage adjustment not required
  • CrCl <30 mL/minute:

    • administered 600 mg once daily
  • CrCl <30 mL/minute and concomitant hepatic impairment:

    • administered 400 mg once daily
  • Hemodialysis:

    • On dialysis days, 600 mg is administered once per day.

Telithromycin dose in liver disease:

  • There is no need to alter the dosage unless there is concomitant renal impairment (e.g., CrCl 30 mL/minute).

Common Side Effects of Telithromycin Include:

  • Gastrointestinal:

    • Diarrhea

Less Common Side Effects of Telithromycin Include:

  • Central Nervous System:

    • Headache
    • Dizziness
  • Gastrointestinal:

    • Nausea
    • Vomiting
    • Dysgeusia
    • Loose Stools

Rare side effects of Telithromycin:

  • Central Nervous System:

    • Drowsiness
    • Fatigue
    • Insomnia
    • Vertigo
  • Dermatologic:

    • Diaphoresis
    • Skin Rash
  • Gastrointestinal:

    • Abdominal Distension
    • Abdominal Pain
    • Anorexia
    • Constipation
    • Dyspepsia
    • Flatulence
    • Gastric Distress
    • Gastritis
    • Gastroenteritis
    • Glossitis
    • Oral Candidiasis
    • Stomatitis
    • Xerostomia
  • Genitourinary:

    • Fungal Vaginosis
    • Vaginitis
    • Vulvovaginal Candidiasis
  • Hematologic & Oncologic:

    • Thrombocythemia
  • Hepatic:

    • Abnormal Hepatic Function Tests
    • Increased Serum Transaminases
  • Ophthalmic:

    • Accommodation Disturbance
    • Blurred Vision
    • Diplopia

Contraindication to Telithromycin (Ketek) Include:

  • hypersensitivity to any ingredient in the treatment for myasthenia gravis, including telithromycin, macrolide antibiotics, or both
  • When taking colchicine (if the patient has concurrent renal or hepatic impairment), cisapride, pimozide, lovastatin, or simvastatin, a prior history of hepatitis and/or jaundice connected to the use of telithromycin or other macrolides antibiotics is present.

Warnings and precautions

 

  • Modified cardiac conduction

    • It can lengthen the QTc interval and make ventricular arrhythmias such torsades de pointes more likely.
    • Avoid using class Ia or class III antiarrhythmics on patients with congenital prolongation of the QTc interval, ongoing hypokalemia, hypomagnesemia, severe bradycardia, or concurrent QTc-prolonging medication therapy.
  • Hepatic effects

    • Acute liver failure or severe liver damage, some of which were fatal, were observed in some cases.
    • Stop taking your medication and seek a liver function test if you experience any hepatitis symptoms or signs.
    • If clinical hepatitis, transaminase, or transaminase testing are accompanied with additional systemic symptoms, cease the medication permanently.
    • Readministering any macrolide antibiotic to patients who have already experienced hepatitis or jaundice is not advised.
    • Additionally, we have observed hepatitis with or without jaundice and less severe hepatic dysfunction brought on by elevated liver enzymes.
  • Superinfection

    • Extended use can result in fungal or bacterial overinfections including pseudomembranous collitis and C. difficile-associated diarrhoea (CDAD). CDAD can be seen for up to two months following antimicrobial therapy.
  • 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.
  • Visual disturbances:

    • It can cause visual disturbances, such as blurred vision, altered accommodation ability, diplopia or changes in sight.
    • Though there have been reports of severe cases, the majority of cases are mild to moderate in intensity.
    • These events could affect the ability to drive or operate machinery. Patients should be advised to exercise caution until they are fully understood.
  • 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.
  • Renal impairment

    • Patients who have severely compromised renal function (CrCl 30 mL/minute) should exercise caution and alter their dosage.

Telithromycin: Drug Interaction

Risk Factor C (Monitor therapy)

Alosetron

The serum levels of Alosetron may rise in response to CYP3A4 Inhibitors (Strong).

Apixaban

The serum levels of apixaban may rise in response to CYP3A4 Inhibitors (Strong).

BCG Vaccine (Immunization)

Antibiotics may reduce the BCG vaccine's therapeutic effect (Immunization).

Benperidol

The serum concentration of Benperidol may rise in response to CYP3A4 Inhibitors (Strong).

Benzhydrocodone

The serum levels of Benzhydrocodone may rise in response to CYP3A4 Inhibitors (Strong). In particular, there might be an increase in hydrocodone concentration.

Betamethasone (Ophthalmic)

Betamethasone serum levels may rise in response to strong CYP3A4 inhibitors (Ophthalmic).

Bictegravir

Bictegravir's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Bortezomib

The serum levels of bortezomib may rise in the presence of CYP3A4 Inhibitors (Strong).

Bosentan

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Bosentan

The serum concentration of bosentan may rise in response to CYP3A4 Inhibitors (Strong). Management: It is not advised to use a CYP2C9 inhibitor and a CYP3A inhibitor concurrently, or to use a single medication that inhibits both enzymes, with bosentan because this will likely result in a significant rise in the drug's serum concentrations. Monograph for more information.

Brentuximab Vedotin

The serum concentration of Brentuximab Vedotin may rise in response to CYP3A4 Inhibitors (Strong). More specifically, levels of the substance's active monomethyl auristatin E (MMAE) component might rise.

Brinzolamide

Brinzolamide's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Budesonide (Nasal)

The serum concentration of Budesonide may rise in response to CYP3A4 Inhibitors (Strong) (Nasal).

Budesonide (Oral Inhalation)

The serum concentration of Budesonide may rise in response to CYP3A4 Inhibitors (Strong) (Oral Inhalation).

Buprenorphine

Buprenorphine's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Calcifediol

The serum levels of calcifediol may rise in response to CYP3A4 Inhibitors (Strong).

Cannabidiol

The content of cannabidiol in the serum may rise in response to CYP3A4 Inhibitors (Strong).

Cannabis

Cannabis serum concentrations may rise in response to strong CYP3A4 inhibitors. Serum concentrations of cannabidiol and tetrahydrocannabinol may rise particularly.

Cardiac Glycosides

The serum levels of cardiac glycosides may rise in response to macrolide antibiotics.

Cinacalcet

Cinacalcet's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Clofazimine

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

CloZAPine

The serum levels of CloZAPine may rise in response to CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Codeine

The active metabolite(s) of codeine may be present in higher serum quantities while taking CYP3A4 Inhibitors (Strong).

Corticosteroids (Orally Inhaled)

Corticosteroids may be present in greater amounts in the serum while taking strong CYP3A4 inhibitors (Orally Inhaled). Treatment: It is not advised to use an effective CYP3A4 inhibitor with orally administered fluticasone propionate. Exceptions include triamcinolone and beclomethasone (oral inhalation) (Systemic).

Corticosteroids (Systemic)

Corticosteroids may be present in greater amounts in the serum while taking strong CYP3A4 inhibitors (Systemic). MethylPREDNISolone, PrednisoLONE (Systemic), and PredniSONE are exceptions.

CycloSPORINE (Systemic)

Telithromycin may elevate CycloSPORINE levels in the serum (Systemic).

CYP3A4 Inducers (Moderate)

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

CYP3A4 Inhibitors (Moderate)

Telithromycin serum levels can rise.

CYP3A4 Inhibitors (Strong)

Telithromycin serum levels can rise.

Deferasirox

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Dexamethasone (Ophthalmic)

Dexamethasone serum levels may rise in response to strong CYP3A4 inhibitors (Ophthalmic).

Dienogest

The serum concentration of Dienogest may rise in response to CYP3A4 Inhibitors (Strong).

Dofetilide

The serum levels of Dofetilide may rise in response to CYP3A4 Inhibitors (Strong).

Doxercalciferol

The active metabolite(s) of doxercalciferol may have lower serum concentrations when taken with CYP3A4 Inhibitors (Strong).

Dronabinol

The serum concentration of dronabinol may rise in response to strong CYP3A4 inhibitors.

Dutasteride

The serum concentration of dutasteride may rise in response to CYP3A4 Inhibitors (Strong).

Estrogen Derivatives

The serum concentration of oestrogen derivatives may rise in response to strong CYP3A4 inhibitors.

Evogliptin

Evogliptin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Fosnetupitant

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Fostamatinib

The active metabolite(s) of foamamatinib may be present in higher serum quantities while taking CYP3A4 Inhibitors (Strong).

Galantamine

Galantamine's serum levels may rise in response to strong CYP3A4 inhibitors.

Gefitinib

It's possible that CYP3A4 Inhibitors (Strong) will raise the level of gefitinib in the blood.

HYDROcodone

CYP3A4 Inhibitors (Strong) may raise the level of HYDROcodone in the blood.

Ifosfamide

The active metabolite(s) of ifosfamide may be present in lower serum quantities when CYP3A4 Inhibitors (Strong) are used.

Imatinib

Imatinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong).

Imidafenacin

Imidafenacin's serum levels may rise in response to CYP3A4 Inhibitors (Stro

Lacosamide

CYP3A4 Inhibitors (Strong) may raise the level of lacosamide in the serum.

Lactobacillus and Estriol

The therapeutic effects of Lactobacillus and Estriol may be reduced by antibiotics.

Levobupivacaine

Levobupivacaine's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Lumefantrine

Lumefantrine's serum levels may rise when taken with CYP3A4 Inhibitors (Strong).

MedroxyPROGESTERone

The blood concentration of medroxyPROGESTERone may rise in response to CYP3A4 Inhibitors (Strong).

Mirtazapine

The quantity of Mirtazapine in the serum may rise after taking CYP3A4 Inhibitors (Strong).

Naldemedine

The serum concentration of Naldemedine may rise in response to CYP3A4 Inhibitors (Strong).

Nalfurafine

The serum levels of nalfurafine may rise in response to CYP3A4 Inhibitors (Strong).

Netupitant

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Ospemifene

Ospemifene's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Oxybutynin

The serum levels of oxybutynin may rise in response to CYP3A4 Inhibitors (Strong).

Parecoxib

The serum concentration of parecoxib may rise in response to CYP3A4 Inhibitors (Strong).

Paricalcitol

The concentration of paricalcitol in the serum may rise in response to CYP3A4 Inhibitors (Strong).

Perhexiline

The quantity of perhexiline in the serum may rise in response to CYP2D6 Inhibitors (Weak).

Pimecrolimus

The metabolism of pimecrolimus may be decreased by strong CYP3A4 inhibitors.

Pitavastatin

Pitavastatin's serum levels may rise in response to telithromycin.

Polatuzumab Vedotin

CYP3A4 Inhibitors (Strong) may raise Polatuzumab Vedotin's serum levels. The harmful small molecule in polatuzumab vedotin, unconjugated MMAE, may be exposed to more people.

Pranlukast

Pranlukast's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Pravastatin

Pravastatin's serum levels might be raised by telithromycin.

Praziquantel

Praziquantel's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

PrednisoLONE (Systemic)

PrednisoLONE serum levels may rise in response to strong CYP3A4 inhibitors (Systemic).

Propafenone

Propafenone serum levels may rise after taking CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

QT-prolonging Agents (Highest Risk)

The QTc-prolonging action of QT-prolonging Agents may be enhanced by QT-prolonging Agents (Indeterminate Risk - Avoid) (Highest Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors.

Ramelteon

The serum levels of Ramelteon may rise in response to CYP3A4 Inhibitors (Strong).

Repaglinide

Repaglinide's serum levels may rise in response to strong CYP3A4 inhibitors. Management: The extent of the rise in repaglinide exposure may be significantly increased by adding a CYP2C8 inhibitor to this medication combination.

Retapamulin

Retapamulin's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Patients under the age of two should not take this combination. Other populations don't need to take any action.

RomiDEPsin

RomiDEPsin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Sarilumab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Sibutramine

The active metabolite(s) of sibutramine may be present in higher serum quantities while taking CYP3A4 Inhibitors (Strong). The serum concentration of sibutramine may rise in response to CYP3A4 Inhibitors (Strong).

Siltuximab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

SORAfenib

The serum levels of SORAfenib may rise when taken with CYP3A4 Inhibitors (Strong).

Tacrolimus (Topical)

Tacrolimus serum levels may rise in response to macrolide antibiotics (Topical).

Tasimelteon

Tasimelteon's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Tetrahydrocannabinol

Tetrahydrocannabinol's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Tetrahydrocannabinol and Cannabidiol

Tetrahydrocannabinol and cannabidiol's serum concentrations may rise in response to CYP3A4 Inhibitors (Strong).

Tocilizumab

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

TraMADol

The serum levels of TraMADol may rise in response to CYP3A4 Inhibitors (Strong).

Upadacitinib

Upadacitinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong).

Vilanterol

Could raise the serum level of CYP3A4 inhibitors (Strong).

Vitamin K Antagonists (eg, warfarin)

The serum concentration of Vitamin K antagonists may rise in response to macrolide antibiotics.

Zolpidem

Zolpidem's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Risk Factor D (Consider therapy modification)

Abemaciclib

Abemaciclib's serum levels may rise in response to strong CYP3A4 inhibitors. Treatment: When paired with potent CYP3A4 inhibitors, individuals taking abemaciclib at doses of 200 mg or 150 mg twice daily should lower their dosage to 100 mg twice daily. Reduce the dosage of patients receiving abemaciclib from 100 mg twice day to 50 mg twice daily.

Alitretinoin (Systemic)

Alitretinoin serum levels may rise in response to strong CYP3A4 inhibitors (Systemic). Management: If alitretinoin is combined with potent CYP3A4 inhibitors, think about lowering the dose to 10 mg. If you take alitretinoin with a potent CYP3A4 inhibitor, keep an eye out for any enhanced effects or toxicities.

Almotriptan

Almotriptan's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: When taken with a potent CYP3A4 inhibitor, limit the initial adult dose of almotriptan to 6.25 mg and the maximum adult dose to 12.5 mg/24 hours. In individuals with impaired renal or hepatic function, avoid concomitant usage.

ALPRAZolam

The serum levels of ALPRAZolam may rise in response to CYP3A4 Inhibitors (Strong). Management: Take into account utilising a different agent that interacts less frequently. If coupled, keep an eye out for alprazolam's potentially hazardous or increased therapeutic effects.

Antineoplastic Agents (Vinca Alkaloids)

The serum concentration of antineoplastic agents may rise in response to macrolide antibiotics (Vinca Alkaloids). Macrolides may also spread vinca alkaloids more widely throughout some tissues and/or cell types. When feasible, avoid using a macrolide antibiotic in order to minimise the risk of infection.

ARIPiprazole

The serum concentration of ARIPiprazole may rise in response to CYP3A4 Inhibitors (Strong). Management: For information, see the complete interaction monograph.

ARIPiprazole Lauroxil

The blood concentrations of the active metabolite(s) of ARIPiprazole Lauroxil may rise in response to CYP3A4 Inhibitors (Strong). Management: For further information on the suggested dose modifications, please see the complete interaction monograph.

AtorvaSTATin

The serum levels of AtorvaSTATin may rise in response to telithromycin. Management: When used with telithromycin, limit the intake of atorvastatin to a maximum of 20 mg/day for adults. This is similar with the dosage for other potent CYP3A4 inhibitors, such as clarithromycin, despite not being an explicit suggestion in the atorvastatin labelling.

Bedaquiline

The serum levels of bedaquiline may rise in response to CYP3A4 Inhibitors (Strong). Management: Only take bedaquiline concurrently with CYP3A4 inhibitors for no longer than 14 days, unless the potential benefits outweigh the potential hazards. Benacquiline's hazardous effects should be monitored. A separate monograph is discussed for the exceptions.

Brexpiprazole

Brexpiprazole's serum levels may rise in response to CYP3A4 Inhibitors (Strong). In patients not receiving treatment for MDD, the dose of brexpiprazole should be reduced by 50% when combined with strong CYP3A4 inhibitors; it should be reduced to 25% of the usual dose when combined with both a moderate CYP3A4 inhibitor and a CYP2D6 inhibitor; or it should be used in patients who have poor CYP2D6 metabolism.

Brigatinib

Brigatinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong). Management: When possible, avoid taking brigatinib at the same time as potent CYP3A4 inhibitors. Reduce the brigatinib dosage by roughly 50%, rounding to the nearest tablet strength, if combination cannot be avoided (ie, from 180 mg to 90 mg, or from 90 mg to 60 mg).

Budesonide (Topical)

The serum concentration of Budesonide may rise in response to CYP3A4 Inhibitors (Strong) (Topical). Management: Avoid this combination, according to US prescribing advice. Canadian goods labels do not expressly advise against anything. If used in conjunction, keep an eye out for too glucocorticoid effects as budesonide exposure may rise.

BusPIRone

The serum concentration of BusPIRone may rise in response to CYP3A4 Inhibitors (Strong). Buspirone dosage should be kept to 2.5 mg per day, and patients should be watched for any heightened side effects or toxicities if coupled with potent CYP3A4 inhibitors.

Cabazitaxel

It's possible that CYP3A4 Inhibitors (Strong) will raise the serum level of Cabazitaxel. Management: When at all feasible, avoid using cabazitaxel at the same time as potent CYP3A4 inhibitors. Consider lowering the dose of the cabazitaxel by 25% if such a combination is required.

Cabozantinib

Cabozantinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: If at all feasible, refrain from taking cabozantinib with a potent CYP3A4 inhibitor. Depending on the cabozantinib product used and the intended use, cabozantinib dose modifications are advised if taken in conjunction. Monograph for more information.

Calcium Channel Blockers

Calcium Channel Blockers may have a slower metabolism when using macrolide antibiotics. Use a noninteracting macrolide as a possible management strategy. The Canadian labelling for felodipine expressly advises against using it in conjunction with clarithromycin. Clevidipine is an exception.

Cariprazine

Cariprazine's serum levels may rise in response to strong CYP3A4 inhibitors. Cariprazine dose reductions of 50% are necessary for management; the precise recommended management differs slightly depending on whether a patient is stable on the medication or just starting it. To learn more, consult the entire interaction monograph or the prescription information.

Ceritinib

Ceritinib's serum levels may rise in response to strong CYP3A4 inhibitors. Management: The ceritinib dose should be lowered by around one-third if such interactions cannot be avoided (to the nearest 150 mg). After stopping the potent CYP3A4 inhibitor, go back to your previous ceritinib dosage. A separate monograph is discussed for the exceptions.

Cilostazol

Cilostazol's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: When treating adult patients who are also taking potent CYP3A4 inhibitors, it may be appropriate to reduce the dose of cilostazol to 50 mg twice daily.

Cobicistat

The serum levels of Cobicistat may rise when telithromycin is used. Telithromycin's serum levels may rise in response to cobicistat. Management: Look for telithromycin substitutes. This potential interaction is not included in the US prescribing material for the combination drug that contains elvitegravir, cobicistat, emtricitabine, and tenofovir.

Colchicine

The serum concentration of colchicine may rise in response to CYP3A4 Inhibitors (Strong). Treatment: Patients who are concurrently receiving a potent CYP3A4 inhibitor and have poor renal or hepatic function should not take colchicine. Colchicine dosage should be decreased in patients with normal renal and hepatic function as instructed. For information, see the entire monograph.

Copanlisib

The serum levels of Copanlisib may rise in response to strong CYP3A4 inhibitors. Treatment: Reduce the dose of copanlisib to 45 mg if concurrent usage with potent CYP3A4 inhibitors cannot be avoided. Watch out for increasing copanlisib side effects or toxicities in your patients.

Crizotinib

Crizotinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong). Management: Whenever possible, refrain from using powerful CYP3A4 inhibitors and crizotinib concurrently. Cryotinib dosage should be reduced to 250 mg per day if concomitant use cannot be avoided. Exceptions are covered separately.

CYP3A4 Inducers (Strong)

May speed up CYP3A4 substrate metabolism (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label.

CYP3A4 Substrates (High risk with Inhibitors)

The metabolism of CYP3A4 Substrates may be reduced by strong CYP3A4 Inhibitors (High risk with Inhibitors). Alitretinoin (Systemic), Amlopidine, Benzhydrocodone, Buprenorphine, Gefitinib, Hydrocodone, Mirtazapine, Praziquantel, Telithromycin, and Vinorelbine are exceptions.

Daclatasvir

Daclatasvir's serum levels may rise in response to strong CYP3A4 inhibitors. Treatment: If daclatasvir is coupled with a potent CYP3A4 inhibitor, reduce the dose to 30 mg once day. When administered with darunavir/cobicistat, daclatasvir does not require a dose change.

Dasatinib

Dasatinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: If at all possible, stay away from this combo. Dasatinib dose decreases are advised when used in conjunction. For information, see the entire monograph. Separate drug interaction monographs go into further depth about the medications indicated as exceptions to this monograph.

Deflazacort

The blood concentrations of the active metabolite(s) of Deflazacort may rise in response to CYP3A4 Inhibitors (Strong). When taking deflazacort with a strong or moderate CYP3A4 inhibitor, only take one-third of the prescribed dose.

Delamanid

The serum levels of Delamanid may rise in the presence of CYP3A4 Inhibitors (Strong). Management: Due to the possibility of QTc interval lengthening when delamanid is taken with potent CYP3A4 inhibitors, increase the frequency of ECG monitoring. Throughout the whole delamanid therapy duration, continue periodic ECG evaluations. Distinctive discussions of exceptions.

DOCEtaxel

CYP3A4 Inhibitors (Strong) may raise the level of DOCEtaxel in the serum. Management: Whenever feasible, avoid using docetaxel and potent CYP3A4 inhibitors together. Consider a 50% dose decrease of docetaxel and keep an eye out for increased docetaxel toxicities if combination usage is inevitable.

DOXOrubicin (Conventional)

The serum levels of DOXOrubicin may rise when taking strong CYP3A4 Inhibitors (Conventional). Treatment: Whenever possible, try to find alternatives to powerful CYP3A4 inhibitors for patients receiving doxorubicin. Pfizer Inc., a U.S. manufacturer, advises against using certain mixtures.

Drospirenone

Drospirenone's serum levels may rise with the use of CYP3A4 Inhibitors (Strong). Administration of the potent CYP3A4 inhibitors atazanavir and cobicistat at the same time is specifically contraindicated when using drospirenone. When drospirenone is used alongside other potent CYP3A4 inhibitors, caution should be exercised.

Duvelisib

It's possible that CYP3A4 Inhibitors (Strong) will raise Duvelisib's serum levels. Treatment: If duvelisib is used with a potent CYP3A4 inhibitor, lower the dose to 15 mg twice daily.

Elagolix

The serum levels of Elagolix may rise when using CYP3A4 Inhibitors (Strong). Treatment: It is not advised to take elagolix 200 mg twice daily along with a potent CYP3A4 inhibitor for more than a month. Use of elagolix 150 mg once daily in combination with a potent CYP3A4 inhibitor should be limited to no more than 6 months.

Eliglustat

Eliglustat's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: There are specific situations when use should be avoided. For information, consult the entire medication interaction monograph.

Encorafenib

Encorafenib's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Management: Whenever feasible, avoid using powerful CYP3A4 inhibitors and encorafenib concurrently. Reduce the encorafenib dose if concurrent administration is necessary and cannot be avoided. Monograph for more information.

Entrectinib

The serum levels of Entrectinib may rise when taking CYP3A4 Inhibitors (Strong). Management: When taking entrectinib, stay away from potent CYP3A4 inhibitors. If the combination cannot be avoided in adults and children 12 years of age and older with a BSA of at least 1.5 square metres, reduce the dose to 100 mg/day. There isn't a substitute dosage offered for others.

Enzalutamide

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: Enzalutamide should not be used concurrently with CYP3A4 substrates that have a limited therapeutic index. Enzalutamide use, like with the use of any other CYP3A4 substrate, should be done cautiously and under close observation.

Erdafitinib

Erdafitinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong). Management: Whenever possible, avoid using powerful CYP3A4 inhibitors and erdafitinib concurrently. If coupled, closely watch for erdafitinib side effects and take appropriate dose adjustments.

Ergot Derivatives

Ergot derivatives' serum levels may rise in response to macrolide antibiotics. Clarithromycin and cabergoline may interact; detailed information is available in the relevant monograph. Exceptions: Nicergoline, Pergolide, and Cabergoline.

Erlotinib

The serum concentration of erlotinib may rise in response to strong CYP3A4 inhibitors. Management: When feasible, steer clear of using this combo. When the combination must be used, keep a close eye out for the onset of any serious side effects, and if they happen, cut the erlotinib dose (in 50 mg decrements).

Estazolam

Estazolam's serum levels may rise in response to macrolide antibiotics. Management: Take into account a less likely to interact option. Azithromycin is most likely a lower-risk macrolide, while benzodiazepines (such as lorazepam and oxazepam) that are less dependent on CYP3A metabolism are also less likely to interact.

Eszopiclone

Eszopiclone's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). When used with potent CYP3A4 inhibitors, the dose of eszopiclone should be restricted to 2 mg per day. Eszopiclone effects and toxicities should also be closely monitored (eg, somnolence, drowsiness, CNS depression).

Etizolam

The serum levels of Etizolam may rise when using CYP3A4 Inhibitors (Strong). Management: If using this combination, think about utilising lower etizolam doses; there are no precise guidelines for dose reduction. Keep a watchful eye on the combination's clinical reaction.

Fedratinib

Fedratinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong). Management: When feasible, take into account alternatives. Fedratinib dosage should be reduced if combined to 200 mg daily. Increase fedratinib dosage to 400 mg/day as tolerated when the inhibitor is withdrawn, starting at 300 mg/day for the first two weeks.

FentaNYL

The serum levels of FentaNYL may rise when using CYP3A4 Inhibitors (Strong). Management: After starting this combination, keep a watchful eye on the patients for a few days and alter the fentanyl dosage as necessary.

Fesoterodine

The serum concentrations of the active metabolite(s) of fesoterodine may rise in response to CYP3A4 Inhibitors (Strong). Management: In adult patients receiving potent CYP3A4 inhibitors, do not exceed a daily dose of 4 mg of fesoterodine.

Fluticasone (Oral Inhalation)

Fluticasone serum levels may rise in response to CYP3A4 Inhibitors (Strong) (Oral Inhalation). Treatment: It is not advised to use oral fluticasone propionate in combination with potent CYP3A4 inhibitors. Fluticasone furoate should be used cautiously when combined with potent CYP3A4 inhibitors. When utilising such a combination, keep a closer eye on the patients.

Gilteritinib

The serum levels of Gilteritinib may rise in response to CYP3A4 Inhibitors (Strong). Management: Take into account alternatives to gilteritinib in combination with a potent CYP3A4 inhibitor. If the combination must be avoided, keep a closer eye out for any harmful effects of gilteritinib.

Glasdegib

Glasdegib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: When possible, look into alternatives to this pairing. If the combination must be used, keep a cautious eye out for signs of QT interval lengthening and other glasdegib side effects.

GuanFACINE

The content of GuanFACINE in the serum may rise in response to CYP3A4 Inhibitors (Strong). When starting this combo, cut the guanfacine dose in half.

Iloperidone

The active metabolite(s) of iloperidone may be present in higher serum quantities while using CYP3A4 Inhibitors (Strong). In particular, levels of the metabolites P88 and P95 may rise. Iloperidone's serum levels may rise in response to strong CYP3A4 inhibitors. Treatment: When given with a potent CYP3A4 inhibitor, cut the dose of iloperidone in half.

Ivacaftor

Ivacaftor's serum levels may rise in response to strong CYP3A4 inhibitors. Management: Ivacaftor dosage reductions are necessary; for complete monograph material and specific recommendations based on age and weight.

Ivosidenib

Ivosidenib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Whenever possible, avoid taking ivosidenib with a potent CYP3A4 inhibitor. Ivosidenib dosage should be decreased to 250 mg once daily when combination use is necessary. Drugs that are specifically mentioned as exceptions are covered in further detail in their own drug interaction monographs.

Ixabepilone

Ixabepilone's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Larotrectinib

CYP3A4 Inhibitors (Strong) may raise larotrectinib's serum levels. Management: Larotrectinib should not be used with potent CYP3A4 inhibitors. Reducing the larotrectinib dosage by 50% should be done if this combination cannot be avoided. after quitting the inhibitor, increase the dose to the previous level

Levomilnacipran

Levomilnacipran's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: In patients who are already taking potent CYP3A4 inhibitors, a maximum adult dose of 80 mg/day of levomilnacipran should not be exceeded.

Lorlatinib

Lorlatinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Avoid combining lorlatinib with potent CYP3A4 inhibitors. Reduce the dose of lorlatinib from 100 mg once daily to 75 mg once daily or from 75 mg once daily to 50 mg once daily if the combination cannot be avoided.

Lorlatinib

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in serum levels of the substrate could result in therapeutic failure and negative clinical outcomes.

Manidipine

Manidipine's serum levels may rise in response to strong CYP3A4 inhibitors. Management: Take into account avoiding using manidipine and potent CYP3A4 inhibitors together. If coupled, keep a watchful eye out for any increased toxicities and effects of manidipine. Reduced doses of manidipine might be necessary.

Maraviroc

The serum levels of Maraviroc may rise in response to strong CYP3A4 inhibitors. When used with a potent CYP3A4 inhibitor, reduce the adult dose of maraviroc to 150 mg twice daily. With powerful CYP3A4 inhibitors, do not use maraviroc in individuals with Clcr less than 30 mL/min.

Meperidine

Meperidine's serum levels may rise in response to strong CYP3A4 inhibitors. Management: If concurrent usage with potent CYP3A4 inhibitors is necessary, take into account lowering the dose of meperidine. When these medications are taken together, keep an eye out for any signs and symptoms of sedation and respiratory depression.

MethylPREDNISolone

MethylPREDNISolone's levels in the serum may rise in response to CYP3A4 Inhibitors (Strong). Treatment: If a patient is using a potent CYP3A4 inhibitor, consider lowering the dose of methylprednisolone and keep an eye out for any increased steroid-related side effects.

Midazolam

Midazolam's serum levels may rise in response to macrolide antibiotics. Management: Take into account a less likely to interact option. Azithromycin is most likely a lower-risk macrolide, while benzodiazepines (such as lorazepam and oxazepam) that are less dependent on CYP3A metabolism are also less likely to interact.

Midostaurin

Midostaurin's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: If at all possible, look for alternatives to using midostaurin and potent CYP3A4 inhibitors simultaneously. If concurrent use cannot be avoided, keep an eye on the patients' risk of adverse responses increasing. A separate monograph is dedicated to discussing exceptions.

MiFEPRIStone

The serum concentration of MiFEPRIStone may rise in response to CYP3A4 Inhibitors (Strong). Management: When paired with a potent CYP3A4 inhibitor, the adult dose of mifepristone for treating hyperglycemia in Cushing's syndrome should not exceed 600 mg/day. Regardless of dose or indication, keep an eye out for increased mifepristone toxicity.

MiFEPRIStone

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: During and two weeks after mifepristone treatment, reduce doses of CYP3A4 substrates and keep an eye out for elevated amounts or toxicity. Fentanyl, pimozide, quinidine, sirolimus, and tacrolimus should all be avoided. Cyclosporine should also be avoided.

Mirodenafil

The serum concentration of Mirodenafil may rise in response to CYP3A4 Inhibitors (Strong). When used with potent CYP3A4 inhibitors, mirodenafil dosage may want to be reduced. When using this combination, keep an eye out for any increased toxicities or side effects from mirodenafil.

Mitotane

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: When administered in individuals receiving mitotane, doses of CYP3A4 substrates may need to be significantly modified.

Nilotinib

Nilotinib's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Avoid if at all feasible. Nilotinib dosage should be reduced, if necessary, to 200 mg once daily for newly diagnosed Ph+ CML patients or 300 mg once daily for patients with resistant or intolerable Ph+ CML. Exceptions are covered in a different monograph.

Olaparib

Olaparib's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Management: If at all feasible, refrain from administering potent CYP3A4 inhibitors to patients receiving olaparib. Olaparib dosage should be decreased to 100 mg twice if such concomitant use cannot be avoided.

OxyCODONE

CYP3A4 Inhibitors (Strong) may intensify OxyCODONE's harmful/toxic effects. CYP3A4 Inhibitors (Strong) may raise OxyCODONE's serum levels. The active metabolite oxymorphone's serum concentrations may also rise.

Panobinostat

The serum levels of Panobinostat may rise in response to strong CYP3A4 inhibitors. Management: If a potent CYP3A4 inhibitor is required, reduce the dose of panobinostat to 10 mg.

PAZOPanib

The serum concentration of PAZOPanib may rise in response to CYP3A4 Inhibitors (Strong). Management: Whenever feasible, avoid using pazopanib at the same time as potent CYP3A4 inhibitors. Reduce the adult dose of pazopanib to 400 mg if avoiding such a combination is not possible. There might also be a need for further dose decreases.

Pexidartinib

Pexidartinib's serum levels may rise when taken with CYP3A4 Inhibitors (Strong). Management: If at all feasible, avoid taking pexidartinib with potent CYP3A4 inhibitors. Pexidartinib dosage should be decreased if concomitant use cannot be avoided. Reduce daily doses of 800 mg or 600 mg to 200 mg twice day. Reduce 400 mg/day doses to 200 mg/day.

Pimavanserin

Pimavanserin's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: If pimavanserin is taken with potent CYP3A4 inhibitors, reduce the dose to 10 mg per day.

Piperaquine

Piperaquine's ability to prolong QTc may be enhanced by CYP3A4 Inhibitors (Strong). The serum concentration of piperaquine may rise in response to CYP3A4 Inhibitors (Strong). Management: Whenever feasible, avoid using powerful CYP3A4 inhibitors and piperaquine concurrently.

PONATinib

PONATinib's serum levels may rise when used with CYP3A4 Inhibitors (Strong). Management: Ponatinib's adult beginning dose should be decreased to 30 mg per day while being treated with any potent CYP3A4 inhibitor, according to the U.S. prescribing guidelines.

QUEtiapine

CYP3A4 Inhibitors (Strong) may raise QUEtiapine's serum levels. Treatment: After initiating a potent CYP3A4 inhibitor, patients taking quetiapine should reduce their dose to one-sixth of the usual amount. Start quetiapine at the lowest dose and increase it as necessary in those who are taking potent CYP3A4 inhibitors. Distinctive discussions of exceptions.

QuiNINE

Telithromycin may increase QuiNINE's ability to prolong QTc. The serum concentration of QuiNINE may rise in response to telithromycin. Treatment: If at all feasible, avoid concurrent therapy with quinine and telithromycin due to the risk of higher quinine serum levels and potential cardiac side effects.

Reboxetine

Reboxetine's serum levels may rise with the use of strong CYP3A4 inhibitors.

Ribociclib

The serum levels of ribociclib may rise in response to CYP3A4 Inhibitors (Strong). Management: If using ribociclib in combination with potent CYP3A4 inhibitors cannot be avoided, reduce the dose to 400 mg once daily. A separate monograph is dedicated to discussing exceptions.

Rifamycin Derivatives

The metabolism of derivatives of rifamycin may be slowed down by macrolide antibiotics. Exceptions: Rifapentine.

Rilpivirine

The serum levels of Rilpivirine may rise in response to macrolide antibiotics. Management: To prevent this potential interaction, take into account using azithromycin or another non-macrolide alternative when necessary.

Ruxolitinib

Ruxolitinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: There are specific situations where this combination should be avoided. Monograph for more information.

SAXagliptin

It's possible that CYP3A4 Inhibitors (Strong) will raise SAXagliptin's serum levels. The U.S. product labelling for saxagliptin advises restricting the adult dose to 2.5 mg/day when used with a potent CYP3A4 inhibitor. Keep an eye out for elevated saxagliptin levels or effects. The product labelling in Canada does not include an advice of this nature.

Sildenafil

Telithromycin may raise the level of sildenafil in the blood.

Sirolimus

The serum levels of Sirolimus may rise when taking CYP3A4 Inhibitors (Strong). Management: To reduce the risk of sirolimus toxicity, take into account avoiding concomitant use of sirolimus and potent CYP3A4 inhibitors. It is not advised to use voriconazole or posaconazole with sirolimus together.

Sodium Picosulfate

Antibiotics may reduce Sodium Picosulfate's therapeutic impact. In the event that a patient recently took or is now taking an alternate product for bowel cleansing prior to a colonoscopy,

Solifenacin

The blood levels of Solifenacin may rise in response to CYP3A4 Inhibitors (Strong). Management: When coupled with potent CYP3A4 inhibitors, limit solifenacin dosages to 5 mg per day.

St John's Wort

May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label.

Stiripentol

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: Due to the increased potential for side effects and toxicity, stiripentol should not be used with CYP3A4 substrates that are thought to have a narrow therapeutic index. Use of stiripentol with any CYP3A4 substrate necessitates closer observation.

SUFentanil

CYP3A4 Inhibitors (Strong) may raise the level of SUFentanil in the serum. Treatment: If a powerful CYP3A4 inhibitor is started in a patient on sufentanil, consider lowering the dose and keep an eye out for any toxicities and side effects that may become more severe (eg, respiratory depression).

SUNItinib

Serum concentrations of SUNItinib may rise in response to CYP3A4 Inhibitors (Strong). Management: Avert wherever you can. If this combination cannot be avoided, sunitinib dose reductions, which vary depending on the indication, are advised. For information, see the entire monograph.

Tacrolimus (Systemic)

Tacrolimus serum levels may rise when taking strong CYP3A4 Inhibitors (Systemic). Treatment: When using a potent CYP3A4 inhibitor at the same time as tacrolimus, closely monitor the clinical tacrolimus response and frequently check tacrolimus serum concentrations. It is likely that Tacrolimus dose adjustments and/or interval extensions will be necessary.

Tadalafil

Tadalafil's serum levels may rise in the presence of strong CYP3A4 inhibitors. Treatment: Depending on the indication and/or international labelling, recommendations for the usage of tadalafil in patients who are simultaneously taking potent CYP3A4 inhibitors may change. Check the relevant product labels.

Temsirolimus

Temsirolimus' serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Whenever feasible, avoid using powerful CYP3A4 inhibitors and temsirolimus concurrently. If both are present, reduce the dose of temsirolimus to 12.5 mg per week and keep an eye on the patients for any worsening side effects and toxicities.

Tezacaftor

Tezacaftor's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Treatment: Tezacaftor/ivacaftor should be administered twice a week, three to four days apart, in the morning, when paired with potent CYP3A4 inhibitors. Ivacaftor alone shouldn't be taken in the evening.

Thiotepa

Thiotepa's active metabolite(s) may have lower serum concentrations when used with CYP3A4 Inhibitors (Strong). Thiotepa's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: The prescribing literature for thiotepa advises against combining it with potent CYP3A4 inhibitors. Keep an eye out for negative side effects and lower efficacy if concurrent use is unavoidable.

Tofacitinib

Tofacitinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: When used with potent CYP3A4 inhibitors, tofacitinib dose decreases are advised. Depending on the tofacitinib formulation and the intended use, different dose changes are advised. For information, see the entire monograph.

Tolterodine

The blood levels of tolterodine may rise after taking CYP3A4 Inhibitors (Strong). Treatment: When used with a potent CYP3A4 inhibitor, the maximum daily dose of tolterodine for adults is 2 mg.

Toremifene

The serum levels of toremifene may rise in response to CYP3A4 Inhibitors (Strong). Treatment: If at all feasible, avoid using toremifene with potent CYP3A4 inhibitors. Monitor for increased toremifene toxicities, especially QTc interval prolongation, if coadministration is required. Exceptions are covered in a different monograph.

TraZODone

The serum levels of TraZODone may rise in response to CYP3A4 Inhibitors (Strong). Treatment: If coupled with potent CYP3A4 inhibitors, take into account using a lower dose of trazodone and keep an eye out for any enhanced adverse effects (such as sedation and QTc prolongation).

Typhoid Vaccine

The Typhoid Vaccine's therapeutic benefits may be reduced by antibiotics. The only strain impacted is the live attenuated Ty21a strain. Treatment: Patients receiving systemic antibacterial drugs should refrain from receiving the live attenuated typhoid vaccination (Ty21a). This vaccine should not be used for at least 3 days after receiving it.

Valbenazine

The serum concentration of Valbenazine may rise in response to CYP3A4 Inhibitors (Strong). Treatment: When used in conjunction with potent CYP3A4 inhibitors, reduce the dose of valbenazine to 40 mg daily.

Vardenafil

Vardenafil's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Depending on the brand name (e.g., Levitra, Staxyn) or by international labelling, recommendations on concurrent use of vardenafil with potent CYP3A4 inhibitors may differ. For information, consult the entire medication interaction monograph.

Vemurafenib

Vemurafenib's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Management: Whenever possible, avoid using vemurafenib at the same time as potent CYP3A4 inhibitors. Consider using a substitute that doesn't significantly inhibit CYP3A4 as being clinically appropriate. A separate monograph is dedicated to discussing exceptions.

Venetoclax

Venetoclax's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: In patients with CLL/SLL, this combination is contraindicated during venetoclax commencement and ramp-up. Patients with AML must take lower doses of venetoclax during ramp-up, and lower dosages of the drug are needed for all patients throughout maintenance therapy.

Verapamil

Telithromycin might make Verapamil's bradycardic action more potent. Telithromycin might make Verapamil's hypotensive impact even stronger.

Vilazodone

Vilazodone's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: In patients using potent CYP3A4 inhibitors, the daily maximum adult dose of vilazodone should be 20 mg. After stopping the potent CYP3A4 inhibitor, the original vilazodone dosage can be resumed.

Zopiclone

It's possible that CYP3A4 Inhibitors (Strong) will raise the serum level of Zopiclone. Management: If coupled with a potent CYP3A4 inhibitor, the first starting dose of zopiclone for adults should not be higher than 3.75 mg. If these medications are taken together, patients should be kept an eye out for any zopiclone toxicity symptoms.

Zuclopenthixol

The serum levels of Zuclopenthixol may rise in response to CYP3A4 Inhibitors (Strong). Management: If the patient is a poor CYP2D6 metabolizer, consider reducing the dosage of zuclopenthixol while also taking a potent CYP3A4 inhibitor (such as ketoconazole) (eg, paroxetine). Keep an eye out for rising zuclopenthixol levels or toxicity.

Risk Factor X (Avoid combination)

Acalabrutinib

Acalabrutinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Ado-Trastuzumab Emtansine

Ado-Trastuzumab Emtansine's active metabolite(s) may be present in higher concentrations in the serum when used with CYP3A4 Inhibitors (Strong). Strong CYP3A4 inhibitors in particular may raise levels of the cytotoxic DM1 component.

Alfuzosin

Alfuzosin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Aprepitant

The serum concentration of aprepitant may rise in response to CYP3A4 Inhibitors (Strong).

Astemizole

Astemizole's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Asunaprevir

Asunaprevir's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Avanafil

Avanafil's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Axitinib

The serum concentration of Axitinib may rise when using CYP3A4 Inhibitors (Strong). Management: Whenever feasible, avoid taking axitinib at the same time as any potent CYP3A inhibitor. A 50% dose reduction of axitinib is advised if a potent CYP3A inhibitor must also be administered.

Barnidipine

The serum concentration of barnidipine may rise in response to strong CYP3A4 inhibitors.

BCG (Intravesical)

Antibiotics may lessen BCG's therapeutic effects (Intravesical).

Blonanserin

Blonanserin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Bosutinib

The serum concentration of bosutinib may rise when taking CYP3A4 Inhibitors (Strong).

Bromocriptine

The serum levels of bromocriptine may rise in response to CYP3A4 Inhibitors (Strong).

Budesonide (Systemic)

The serum concentration of Budesonide may rise in response to CYP3A4 Inhibitors (Strong) (Systemic).

Cholera Vaccine

The therapeutic benefit of the cholera vaccine may be reduced by antibiotic use. Management: Cholera vaccine should not be administered to individuals taking systemic antibiotics or within 14 days after taking oral or parenteral antibiotics.

Cisapride

The serum levels of cisapride may rise in response to telithromycin.

Cobimetinib

Cobimetinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Conivaptan

Conivaptan serum concentrations may rise in response to CYP3A4 Inhibitors (Strong).

Conivaptan

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Dabrafenib

The serum levels of Dabrafenib may rise in response to CYP3A4 Inhibitors (Strong).

Dapoxetine

Dapoxetine's serum levels may rise in response to strong CYP3A4 inhibitors.

Disopyramide

Telithromycin may increase Disopyramide's ability to prolong QTc. Disopyramide's serum levels may rise in response to telithromycin.

Domperidone

Domperidone's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Dronedarone

The serum concentration of dronedarone may rise in response to CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Eletriptan

Eletriptan's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Eplerenone

The serum levels of eplerenone may rise in response to CYP3A4 Inhibitors (Strong).

Everolimus

CYP3A4 Inhibitors (Strong) may raise the level of Everolimus in the serum.

Flibanserin

The serum levels of Flibanserin may rise in response to CYP3A4 Inhibitors (Strong).

Fluticasone (Nasal)

Fluticasone serum levels may rise in response to CYP3A4 Inhibitors (Strong) (Nasal).

Fosaprepitant

The serum levels of Fosaprepitant may rise in response to CYP3A4 Inhibitors (Strong).

Fusidic Acid (Systemic)

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Halofantrine

The serum concentration of halofantrine may rise in response to CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Ibrutinib

Ibrutinib's serum levels may rise when used with CYP3A4 Inhibitors (Strong). Avoid taking ibrutinib and potent CYP3A4 inhibitors together. If a strong CYP3A4 inhibitor must be taken for a brief period of time (for example, antibiotics for 7 days or fewer), ibrutinib medication should be interrupted until the strong CYP3A4 inhibitor is stopped.

Idelalisib

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Irinotecan Products

The active metabolite(s) of irinotecan products may be present in higher serum quantities when CYP3A4 Inhibitors (Strong) are used. Particularly, there may be an increase in SN-38 serum concentrations. Irinotecan products may have a higher serum concentration when taken with CYP3A4 Inhibitors (Strong).

Isavuconazonium Sulfate

The blood concentrations of the active metabolite(s) of isavuconazonium sulphate may rise in response to CYP3A4 Inhibitors (Strong). Particularly, CYP3A4 Inhibitors (Strong) may raise the blood concentrations of isavuconazole. Management: According to US labelling, combined usage is not recommended. Despite severely suppressing CYP3A4, lopinavir/ritonavir (and maybe other applications of ritonavir doses less than 400 mg every 12 hours) is viewed as a potential exception to this contraindication.

Itraconazole

Telithromycin serum levels can rise. The serum levels of itraconazole may rise in response to telithromycin.

Ivabradine

Ivabradine's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Ketoconazole (Systemic)

Telithromycin serum levels can rise. Ketoconazole's serum levels may rise in response to telithromycin (Systemic).

Lapatinib

Lapatinib's serum levels may rise in response to CYP3A4 Inhibitors (Strong). Treatment: If a therapeutic overlap cannot be avoided, think about lowering the adult dose of lapatinib to 500 mg/day both during and immediately after the completion of treatment with the potent CYP3A4 inhibitor.

Lefamulin

The serum levels of lefamulin may rise in response to CYP3A4 Inhibitors (Strong). Avoid using lefamulin pills and potent CYP3A4 inhibitors simultaneously as treatment.

Lercanidipine

Lercanidipine's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Lomitapide

The serum concentration of lomitapide may rise in response to CYP3A4 Inhibitors (Strong).

Lovastatin

The serum levels of lovastatin may rise in response to telithromycin.

Lurasidone

The serum levels of lurasidone may rise in response to strong CYP3A4 inhibitors.

Macitentan

The serum concentration of Macitentan may rise in response to strong CYP3A4 inhibitors.

Mizolastine

The serum levels of Mizolastine may rise in response to macrolide antibiotics.

Naloxegol

The serum levels of Naloxegol may rise in response to CYP3A4 Inhibitors (Strong).

Neratinib

Neratinib serum levels may rise when taking CYP3A4 Inhibitors (Strong).

NiMODipine

The serum levels of NiMODipine may rise in response to CYP3A4 Inhibitors (Strong).

Nisoldipine

The serum levels of nisoldipine may rise in response to CYP3A4 Inhibitors (Strong).

Palbociclib

The serum levels of palbociclib may rise in response to CYP3A4 Inhibitors (Strong).

Pimozide

Pimozide's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Radotinib

The presence of CYP3A4 Inhibitors (Strong) may raise the level of Radotinib in the serum.

Ranolazine

The serum levels of ranolazine may rise in response to CYP3A4 Inhibitors (Strong).

Red Yeast Rice

The blood concentration of Red Yeast Rice may rise in response to CYP3A4 Inhibitors (Strong). Particularly, levels of lovastatin and other associated substances present in red yeast rice may be elevated.

Regorafenib

Regorafenib's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Rupatadine

Rupatadine's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Salmeterol

Salmeterol's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Silodosin

The serum levels of Silodosin may rise in response to CYP3A4 Inhibitors (Strong).

Simeprevir

Simeprevir's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Simvastatin

Simvastatin's serum levels may rise in response to telithromycin.

Sonidegib

Sonidegib's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).

Suvorexant

Suvorexant's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Tamsulosin

Tamsulosin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Terfenadine

Terfenadine's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book.

Ticagrelor

The active metabolite(s) of ticagrelor may have lower serum concentrations when used with CYP3A4 Inhibitors (Strong). Ticagrelor's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Tolvaptan

The serum levels of tolvaptan may rise in response to CYP3A4 Inhibitors (Strong).

Trabectedin

The serum levels of Trabectedin may rise in response to CYP3A4 Inhibitors (Strong).

Triazolam

Triazolam's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Udenafil

The serum levels of udenafil may rise in response to CYP3A4 Inhibitors (Strong).

Ulipristal

Ulipristal's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong). Treatment: This is specific to the use of ulipristal for indications or symptoms of uterine fibroids (Canadian indication). Patients who get this combination and ulipristal as an emergency contraception should be watched for ulipristal toxicity.

VinCRIStine (Liposomal)

VinCRIStine serum levels may rise in response to CYP3A4 Inhibitors (Strong) (Liposomal).

Vinflunine

Vinflunine's serum levels may rise in response to CYP3A4 Inhibitors (Strong).

Vorapaxar

It's possible that CYP3A4 Inhibitors (Strong) will raise the serum level 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.