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Dear Readers! I started this blog when my daughter was in the NICU. She had ventriculitis. Her CSF report grew E.coli. But, she was injected Teicoplanin directly into her brain. The doctors made two errors here:

Teicoplanin is for gram-positive bacteria only. It does not treat E.coli.
Teicoplanin is not for intraventricular use. The manufacturer strongly discourage injecting Teicoplanin into the brain.

My daughter bled into the brain. She lived for another two years and ultimately died.

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Indinavir (Crixivan) - Class, Uses, Dosage, Side effects

Indinavir (Crixivan) is a protease inhibitor that is used in combination with other antiretroviral drugs for the treatment of HIV-1 infection.

Indinavir Uses:

HIV-1 infection:
- Treatment of HIV infection in fusion with other antiretroviral agents

Indinavir dose in adults:

Indinavir dose in the treatment of HIV-1 infection: Oral:

Unboosted regimen:
- 800 mg every 8 hours
ritonavir-boosted regimen (off-label dose):
- Ritonavir 100 to 200 milligrammes twice daily in addition to 800 milligrammes of indinavir.
Missed dose:
- If the time between doses is less than two hours, take the dose right away and resume your regular dosing plan; if more than two hours have passed, resume with your next regularly scheduled dose.
Dosage adjustments for indinavir when administered in combination therapy: Note:
- Delavirdine, itraconazole, or ketoconazole:
  - Reduce indinavir dose to 600 milligrams after every 8 hours.
- Rifabutin:
  - Reduce rifabutin to the recommended dose + increase indinavir to 1,000 mg every 8 hours.

Indinavir dose in childrens:

Note:

It is recommended to assess gene mutation and antiretroviral (ARV) resistance patterns as needed (for more information, go to https://www.iasusa.org).

Indinavir dose in the treatment of HIV-1 infection:

Note:

Indinavir is not advised for use in adults, children, or adolescents, according to the recommendations of AIDS Info, because of its adverse toxicity profile, paucity of efficacy data, hazy pharmacokinetics, and the availability of substitute medications.
Usage in conjunction with additional ARV medications.
Children: Limited data available; optimal dose not established:
- Oral:
  - Ritonavir-boosted:
    - Ritonavir doses of 100 to 125 mg/m2/dose (maximum of 100 milligramme) every 12 hours in addition to indinavir 400 mg/m2/dose (maximum of 800 milligramme) are recommended.
    - In clinical trials, this dosage generated AUCs that were comparable to adult exposure to indinavir 800 mg/ritonavir 100 mg twice day.
    - Yet, studies show that paediatric patients experience substantial levels of toxicity and interindividual heterogeneity.
    - With supratherapeutic (indinavir 500 milligrams/m2/dose every 12 hours) and subtherapeutic (indinavir 234 to 250 milligram/m2/dose every 12 hours) indinavir serum concentrations reported, a number of additional ritonavir-boosted dosage regimens have been tested.
Adolescents:
- Oral:
  - Unboosted:
    - 800 milligram/dose every 8 hours.
  - Ritonavir-boosted:
    - Indinavir 800 mg plus ritonavir 100 to 200 mg twice a day.
Indinavir dosing adjustment for concomitant therapy:
- Adolescents:
  - The manufacturer's labelling for adults makes the following suggestions, which should also be taken into account for adolescent patients receiving the adult dose.

Pregnancy Risk Category: C

The amount of placental transfer that can be done to humans is very minimal.
Data from the antiretroviral pregnancy registry show that there is no increase in overall birth defects.
Despite the possibility that maternal antiretroviral therapy (ART) increases the risk of preterm birth, information is not readily available since maternal variables can vary (disease severity and gestational age at therapy initiation).
While some studies have shown an increase in stillbirths, low birth weights, and infants of small gestational age, these findings are not consistent across all studies.
Because of the clear benefits to maternal ART, it should not be withheld.
Long-term monitoring is important for all infants who have been exposed to antiretroviral medication.
It is important to test kids for mitochondrial dysfunction if they have major organ abnormalities, especially in the heart or central nervous system.
Therapy has been associated with hyperbilirubinemia; it is unknown if this will happen in neonates exposed to indinavir in utero.
Protease inhibitors have been linked to hyperglycemia, diabetes mellitus, and new onsets of diabetes mellitus. It is unclear if pregnancy increases the risk.
The use of Indinavir during pregnancy is not advised by the Perinatal HIV Guidelines published by the Health and Human Services (HHS). This is due to the existence of other sensible alternatives.
If a female becomes pregnant while taking indinavir, she should switch to the recommended regimen.
If it is to be administered during pregnancy, it must be combined with low-dose, ritonavir boosting. The ideal dosage hasn't yet been determined, though. During pregnancy, unboosted Indinavir's plasma concentrations fall.
ART is highly advised for all pregnant HIV-positive women. This will reduce the risk of perinatal transmission and keep the viral burden below the limit of detection.
Monitoring during pregnancy is more common than monitoring in adults who are not pregnant. All females with HIV should continue ART postpartum. This can be modified after delivery.

Indinavir use during breastfeeding:

Indinavir can be found in breast milk.
Breast milk concentrations indinavir in breast milk were as high as 54% to 55% in a woman who took 600 mgs of ritonavir and 200 mgs twice daily for five days after birth.
Postnatal HIV transmission is not preventable by infant or maternal antiretroviral treatment. A multiclass-resistant virus was also detected in breastfed infants, despite maternal therapy.
In the United States, where infant mortality from diarrhea and respiratory infections is low, the formula is affordable, safe and sustainable. Therefore, pregnant women with HIV should not breastfeed to reduce the chance of HIV transmission.

Indinavir Dose in Kidney Disease:

No dosage modifications are mentioned in the manufacturer's labelling (has not been studied).

Indinavir Dose in Liver disease:

Mild to moderate impairment due to cirrhosis (unboosted regimen):
- 600 milligram every 8 hours
Severe impairment:
- In the manufacturer’s labeling, there are no dosage adjustments provided (has not been studied).

Common Side Effects of Indinavir:

Gastrointestinal:
- Abdominal pain
- Nausea
Hepatic:
- Hyperbilirubinemia
Renal:
- Nephrolithiasis
- Urolithiasis

Less Common Side Effects of Indinavir:

Central Nervous System:
- Headache
- Dizziness
- Drowsiness
- Malaise
- Fatigue
Dermatologic:
- Pruritus
- Skin Rash
Gastrointestinal:
- Vomiting
- Anorexia
- Diarrhea
- Dysgeusia
- Gastroesophageal Reflux Disease
- Dyspepsia
- Increased Appetite
- Increased Serum Amylase
Genitourinary:
- Dysuria
Hematologic & Oncologic:
- Neutropenia
- Anemia
Hepatic:
- Increased Serum Transaminases
- Jaundice
Neuromuscular & Skeletal:
- Back Pain
- Weakness
Renal:
- Hydronephrosis
Respiratory:
- Cough
Miscellaneous:
- Fever

Contraindications to Indinavir:

Hypersensitivity
Alfuzosin, amiodarone, and ergot derivatives (dihydroergotamines,ergonovines,ergotamines, methylergonovine), simvastatins, simvastatins, lovastatins, simvastatins, cisapride.

Canadian labeling:

Additional contraindications not listed in the US labeling:
- Coadministration with atazanavir, rifampin, and St. John wort.

Warnings and precautions

Fat redistribution
- Fat distribution may change (e.g., buffalo hump; peripheral wasting with an increased abdominal girth; cushingoid appearance).
Hemolytic anemia
- Acute hemolytic anaemia, which can occasionally be fatal, can result from it.
- Stop using if hemolytic anaemia appears.
Hyperbilirubinemia:
- Direct and indirect hyperbilirubinemia are frequently seen. Nonetheless, elevated serum transaminases have infrequently been linked to it.
- Use atazanavir alone.
Immune reconstitution syndrome:
- During treatment, patients run the risk of developing an immune reconstitution syndrome, which causes an inflammatory reaction to a dormant, persistent opportunistic HIV infection or the activation of autoimmune illnesses (such as Graves' disease or polymysitis).
- Additional evaluation and treatment may still be necessary.
Nephrolithiasis/urolithiasis:
- Sometimes associated with renal impairment, may cause nephrolithiasis/urolithiasis, acute renal failure, or pyelonephritis (with or without bacteremia).
- It is important to hydrate properly.
- Pediatric patients are at significantly higher risk than adults.
- Temporary interruption of therapy (1-3 days) may be necessary for certain signs and symptoms.
Tubulointerstitial nephritis:
- Medullary calciumification and cortical atrophy have been identified in patients with severe nephritis (>100 cells/high-power field).
- Perform a thorough examination of patients suffering from asymptomatic severe Leukocyturia.
- Additional diagnostic testing may be necessary.
- For all patients suffering from severe leukocyturia, it is important to consider discontinuing treatment.
Diabetes:
- Patients who have received protease inhibitors have reported changes in glucose tolerance, hyperglycemia and exacerbation or new-onset diabetes mellitus.
Hemophilia A and B:
- Patients with hemophilia A and B should be cautious.
- During protease inhibitor therapy, there have been reports of increased bleeding.
Hepatic impairment
- It can cause hepatitis and sometimes lead to fatal hepatic impairment.
- Patients with underlying liver disease should be cautious and patients suffering from cirrhosis should reduce their dosage.

Indinavir: Drug Interaction

Risk Factor C (Monitor therapy)
Abacavir	Protease Inhibitors may decrease the serum concentration of Abacavir.
Alosetron	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron.
AmLODIPine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of AmLODIPine.
Antidiabetic Agents	Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents.
Apixaban	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Apixaban.
Atovaquone	May decrease the serum concentration of Indinavir.
Benperidol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benperidol.
Benzhydrocodone	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benzhydrocodone. Specifically, the concentration of hydrocodone may be increased.
Betamethasone (Ophthalmic)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Betamethasone (Ophthalmic).
Bictegravir	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bictegravir.
Bortezomib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bortezomib.
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.
Brinzolamide	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brinzolamide.
Budesonide (Nasal)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Nasal).
Budesonide (Oral Inhalation)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Oral Inhalation).
Buprenorphine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Buprenorphine.
Calcifediol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Calcifediol.
Cannabidiol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabidiol.
Cannabis	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased.
Cinacalcet	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cinacalcet.
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.
Codeine	CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Codeine.
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).
Corticosteroids (Systemic)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Corticosteroids (Systemic). Exceptions: MethylPREDNISolone; PrednisoLONE (Systemic); PredniSONE.
Cyclophosphamide	Protease Inhibitors may enhance the adverse/toxic effect of Cyclophosphamide. Specifically, the incidences of neutropenia, infection, and mucositis may be increased.
CYP3A4 Inducers (Moderate)	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Deferasirox	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
DexAMETHasone (Ophthalmic)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of DexAMETHasone (Ophthalmic).
Dienogest	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dienogest.
Dofetilide	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
Doxercalciferol	CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Doxercalciferol.
Dronabinol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronabinol.
Dutasteride	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dutasteride.
Enfortumab Vedotin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Enfortumab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased.
Enfuvirtide	Protease Inhibitors may increase the serum concentration of Enfuvirtide. Enfuvirtide may increase the serum concentration of Protease Inhibitors.
Estrogen Derivatives	The serum concentration of oestrogen derivatives may rise in response to strong CYP3A4 inhibitors.
Etravirine	Protease inhibitors may lower the level of etravirine in the serum. With the use of lopinavir, saquinavir, and darunavir, this impact is anticipated (with low-dose ritonavir). The serum levels of protease inhibitors may rise after using etravirine. The drug nelfinavir is expected to have this effect. Management: When using any protease inhibitor in combination with etravirine, low-dose ritonavir boosting is required. Etravirine shouldn't be taken in conjunction with tipranavir, atazanavir, fosamprenavir, or full-dose ritonavir (600 mg twice daily for adults).
Evogliptin	Evogliptin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).
Fostamatinib	CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fostamatinib.
Galantamine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Galantamine.
Gefitinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Gefitinib.
Histamine H2 Receptor Antagonists	Indinavir's serum concentration can drop.
HYDROcodone	CYP3A4 Inhibitors (Strong) may increase the serum concentration of HYDROcodone.
Idelalisib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Idelalisib.
Ifosfamide	CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ifosfamide.
Imatinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imatinib.
Imidafenacin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imidafenacin.
Lacosamide	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lacosamide.
Levamlodipine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levamlodipine.
Levobupivacaine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levobupivacaine.
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).
Meperidine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Meperidine.
Mirtazapine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Mirtazapine.
Naldemedine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Naldemedine.
Nalfurafine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nalfurafine.
Orlistat	May decrease the serum concentration of Antiretroviral Agents.
Ospemifene	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ospemifene.
Oxybutynin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Oxybutynin.
Parecoxib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Parecoxib.
Paricalcitol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Paricalcitol.
P-glycoprotein/ABCB1 Inhibitors	May increase the serum concentration of Pglycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of pglycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.).
Pimecrolimus	CYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus.
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.
Pranlukast	Pranlukast's serum levels may rise in response to CYP3A4 Inhibitors (Strong).
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).
PredniSONE	PredniSONE's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).
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.
Proton Pump Inhibitors	Indinavir's serum concentration can drop.
QuiNIDine	Indinavir may increase the serum concentration of QuiNIDine.
Ramelteon	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ramelteon.
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.
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.
Rilpivirine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Rilpivirine.
RomiDEPsin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of RomiDEPsin.
Sarilumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
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.
Siltuximab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
SORAfenib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of SORAfenib.
Tacrolimus (Topical)	Protease Inhibitors may decrease the metabolism of Tacrolimus (Topical).
Tasimelteon	Tasimelteon's serum levels may rise in the presence of CYP3A4 Inhibitors (Strong).
Telithromycin	Telithromycin's serum levels may rise in response to CYP3A4 Inhibitors (Strong).
Tetrahydrocannabinol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol.
Tetrahydrocannabinol and Cannabidiol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol and Cannabidiol.
Tocilizumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
TraMADol	CYP3A4 Inhibitors (Strong) may increase the serum concentration of TraMADol.
Tricyclic Antidepressants	Protease Inhibitors may increase the serum concentration of Tricyclic Antidepressants.
Upadacitinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Upadacitinib.
Valproate Products	Protease Inhibitors may decrease the serum concentration of Valproate Products.
Venlafaxine	May decrease the serum concentration of Indinavir.
Vilanterol	May increase the serum concentration of CYP3A4 Inhibitors (Strong).
Vindesine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vindesine.
Vinorelbine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vinorelbine.
Zidovudine	Protease Inhibitors may decrease the serum concentration of Zidovudine.
Zolpidem	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zolpidem.
Risk Factor D (Consider therapy modification)
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.
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.
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.
ARIPiprazole	CYP3A4 Inhibitors (Strong) may increase the serum concentration of ARIPiprazole. Management: See full interaction monograph for details.
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.
AtorvaSTATin	Protease Inhibitors may increase the serum concentration of AtorvaSTATin. Management: See full monograph for recommended dose limits. Avoid atorvastatin with tipranavir/ritonavir.
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.
Bosentan	The serum levels of bosentan may rise when indinavir is used. The serum concentration of Indinavir may drop while taking bosentan. Treatment: Begin or adjust bosentan at 62.5 mg once daily or every other day (depending on tolerability) in patients receiving indinavir (see ritonavir for dosing if that agent is used). Watch out for any potential changes in indinavir's response as well.
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.
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).
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.
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.
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.
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.
Calcium Channel Blockers (Nondihydropyridine)	Protease Inhibitors may decrease the metabolism of Calcium Channel Blockers (Nondihydropyridine). Increased serum concentrations of the calcium channel blocker may increase risk of AV nodal blockade. Management: Avoid concurrent use when possible. If used, monitor for CCB toxicity. The manufacturer of atazanavir recommends a 50% dose reduction for diltiazem be considered. Saquinavir, tipranavir, and darunavir/cobicistat use with bepridil is contraindicated.
CarBAMazepine	Protease inhibitors may have a faster metabolism. The metabolism of CarBAMazepine may be slowed down by protease inhibitors.
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.
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.
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.
Clarithromycin	Protease Inhibitors may diminish the therapeutic effect of Clarithromycin. Specifically, certain protease inhibitors may decrease formation of the active 14-hydroxyclarithromycin metabolite, which may negatively impact clarithromycin effectiveness vs. H. influenzae and other non-MAC infections. Protease Inhibitors may increase the serum concentration of Clarithromycin. Clarithromycin dose adjustment in renally impaired patients may be needed. Clarithromycin may increase the serum concentration of Protease Inhibitors. Management: Saquinavir is contraindicated with clarithromycin. Avoid clarithromycin adult doses over 1000 mg/day with a protease inhibitor. Further dose reductions may be needed with impaired renal function. Consider alternative antimicrobial for a non-MAC infection.
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.
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.
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.
CycloSPORINE (Systemic)	Protease Inhibitors may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Protease Inhibitors.
CycloSPORINE (Systemic)	CYP3A4 Inhibitors (Strong) may increase the serum concentration of CycloSPORINE (Systemic).
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.
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.
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.
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.
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.
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.
Delavirdine	Protease Inhibitors may decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Protease Inhibitors.
Didanosine	Indinavir's serum concentration can drop. Treatment: Formulations of didanosine that contain a buffer should be given at least an hour apart from indinavir.
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.
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.
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.
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.
Efavirenz	Indinavir's serum concentration can drop. Treatment: It is unknown how indinavir should be dose-adjusted when combined with efavirenz. Indinavir doses that are higher and unboosted are probably not the best course of action. Consider using an indinavir regimen that is enhanced by ritonavir.
Elagolix	The serum levels of Elagolix may rise when using CYP3A4 Inhibitors (Strong). Usage of elagolix 200 mg twice day together with a potent CYP3A4 inhibitor for more than one month is the recommended course of treatment.
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.
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.
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.
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.
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.
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).
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	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	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.
Garlic	May decrease the serum concentration of Protease Inhibitors. Management: Concurrent use of garlic supplements with protease inhibitors is not recommended. If this combination is used, monitor closely for altered serum concentrations/effects of protease inhibitors, and particularly for signs/symptoms of therapeutic failure.
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.
Istradefylline	The blood levels of istradefylline may increase after taking CYP3A4 Inhibitors (Strong). When taken with potent CYP3A4 inhibitors, the maximum daily dose of istradefylline should be limited to 20 mg, and istradefylline effects and toxicities should be well monitored.
Itraconazole	Indinavir's serum concentration can rise. Itraconazole's serum levels may rise as a result of indinavir. When taking itraconazole, reduce the standard adult dose of indinavir to 600 mg every 8 hours. Keep an eye out for any increased systemic effects of itraconazole, especially harmful or toxic ones.
Ivacaftor	Ivacaftor's serum levels may rise in response to strong CYP3A4 inhibitors. Management: Ivacaftor dose reductions are necessary; for product-specific advice, refer to the entire monograph information.
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. Medications 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).
Ketoconazole (Systemic)	Indinavir's serum concentration can rise. Ketoconazole's serum levels may rise in response to indinavir (Systemic). When given with ketoconazole, the standard adult dose of indinavir should be decreased to 600 mg every 8 hours. Keep an eye out for any increased systemic effects, including harmful or toxic ones,
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.
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.
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 900 mg/day when combined with a strong CYP3A4 inhibitor. Monitor for increased mifepristone toxicity regardless of dose or indication.
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.
Nefazodone	Protease Inhibitors may increase the serum concentration of Nefazodone. Management: Consider alternatives to, or reduced doses of, nefazodone in patients treated with HIV protease inhibitors. Monitor patients receiving these combinations closely for toxic effects of nefazodone.
Nevirapine	May decrease the serum concentration of Indinavir. Management: Increased indinavir doses may be needed when used with nevirapine; however, specific dosing guidelines have not been established.
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.
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	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.
Protease Inhibitors	May increase the serum concentration of other Protease Inhibitors. Management: Atazanavir--indinavir combination contraindicated. Tipranavir/ritonavir or atazanavir/ritonavir not recommended with other protease inhibitors (PI). Darunavir/cobicistat not recommended with PI that require boosting.Other combos may require dose changes.
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.
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.
Rifabutin	Indinavir may increase serum concentrations of the active metabolite(s) of Rifabutin. Rifabutin may decrease the serum concentration of Indinavir. Indinavir may increase the serum concentration of Rifabutin.
Rifapentine	Indinavir's serum concentration can drop. Management: Because of the potential for lower indinavir concentrations, decreased efficacy, and the emergence of resistance, you should think about avoiding the combination of indinavir and rifapentine whenever you can. Keep an eye out for indinavir treatment failure if coupled.
Riociguat	Protease Inhibitors may increase the serum concentration of Riociguat. Management: Consider starting with a reduced riociguat dose of 0.5 mg three times a day (for adults). Patients receiving such a combination should also be monitored extra closely for signs or symptoms of hypotension.
Rosuvastatin	Protease Inhibitors may increase the serum concentration of Rosuvastatin. Management: Start at the lowest rosuvastatin dose and monitor for toxicity. See full drug interaction monograph for details.
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: Limit the saxagliptin dose to 2.5 mg daily when combined with strong CYP3A4 inhibitors. When using the saxagliptin combination products saxagliptin/dapagliflozin or saxagliptin/dapagliflozin/metformin, avoid use with strong CYP3A4 inhibitors.
Sildenafil	Protease Inhibitors may increase the serum concentration of Sildenafil. Management: Erectile dysfunction: sildenafil max = 25 mg/48 hrs with ritonavir, atazanavir, or darunavir; starting dose = 25 mg with other protease inhibitors (adult doses). Contraindicated if sildenafil being used for pulmonary arterial hypertension.
Sildenafil	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sildenafil. Management: Use of sildenafil for pulmonary hypertension should be avoided with strong CYP3A4 inhibitors. When used for erectile dysfunction, starting adult dose should be reduced to 25 mg. Maximum adult dose with ritonavir or cobicistat is 25 mg per 48 hours.
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.
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.
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)	Protease Inhibitors may decrease the metabolism of Tacrolimus (Systemic).
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	Protease Inhibitors may enhance the adverse/toxic effect of Temsirolimus. Levels of sirolimus, the active metabolite, may be increased, likely due to inhibition of CYP-mediated metabolism.
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.
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.
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.
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.
Voxelotor	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Voxelotor. Management: Avoid concomitant use of voxelotor and strong CYP3A4 inhibitors. If concomitant use is unavoidable, reduce the voxelotor dose to 1,000 mg once daily.
Zanubrutinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zanubrutinib. Management: Decrease the zanubrutinib dose to 80 mg once daily during coadministration with a strong CYP3A4 inhibitor. Further dose adjustments may be required for zanubrutinib toxicities, refer to prescribing information for details.
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.
Alfuzosin	Protease Inhibitors may increase the serum concentration of Alfuzosin.
ALPRAZolam	Indinavir may increase the serum concentration of ALPRAZolam.
Amiodarone	Indinavir may increase the serum concentration of Amiodarone.
Aprepitant	The serum concentration of aprepitant may rise in response to CYP3A4 Inhibitors (Strong).
Astemizole	Astemizole's serum concentration 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).
Atazanavir	Could make Indinavir's harmful or hazardous effects worse. Atazanavir's harmful or hazardous effects may be exacerbated by indinavir.
Avanafil	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Avanafil.
Avapritinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Avapritinib.
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.
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).
Cisapride	Protease Inhibitors may increase the serum concentration of Cisapride. This may result in QTc prolongation and malignant cardiac arrhythmias. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Cobimetinib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cobimetinib.
Conivaptan	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
Dabrafenib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dabrafenib.
Dapoxetine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dapoxetine.
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.
Ergot Derivatives	Protease Inhibitors may increase the serum concentration of Ergot Derivatives. Exceptions: Cabergoline; Nicergoline; Pergolide.
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.
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.
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.
Ivabradine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivabradine.
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.
Lasmiditan	May increase the serum concentration of P-glycoprotein/ABCB1 Substrates.
Lefamulin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets and strong inhibitors of CYP3A4.
Lemborexant	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lemborexant.
Lercanidipine	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lercanidipine.
Lomitapide	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lomitapide.
Lovastatin	Protease Inhibitors may increase the serum concentration of Lovastatin.
Lovastatin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
Lumateperone	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lumateperone.
Lurasidone	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lurasidone.
Macitentan	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Macitentan.
Midazolam	Protease Inhibitors may increase the serum concentration of Midazolam. Management: Oral midazolam contraindicated with all protease inhibitors. IV midazolam contraindicated with f nelfinavir; other protease inhibitors recommend caution, close monitoring, and consideration of lower IV midazolam doses with concurrent use.
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	Protease Inhibitors may increase the serum concentration of Pimozide.
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.
RifAMPin	May decrease the serum concentration of Indinavir.
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.
Simeprevir	Protease Inhibitors may increase the serum concentration of Simeprevir. Simeprevir may increase the serum concentration of Protease Inhibitors.
Simvastatin	Protease Inhibitors may increase the serum concentration of Simvastatin.
Simvastatin	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Simvastatin.
Sonidegib	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sonidegib.
St John's Wort	May increase the metabolism of Protease Inhibitors.
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.
Tipranavir	May decrease the serum concentration of Protease Inhibitors.
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.
Ubrogepant	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ubrogepant.
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.

Monitoring parameters:

Monitor viral load, triglycerides, liver function tests, CD4 count, cholesterol, glucose, CBC, urinalysis.
Patients should be monitored habitually who suffers from severe leukocyturia.

How to administer Indinavir?

Drink at least 48 oz of water every day.
Give with water one or two hours after a meal.
Perhaps given together with a small meal or other liquids (such skim milk, juice, coffee, or tea) (eg, toast, corn flakes).
Administer continuously to prevent a noticeable change in serum levels.
When used in conjunction with ritonavir, it can be taken with food.

Mechanism of action of Indinavir:

By attaching to the HIV-1 protease site, it prevents the viral GagPol polyprotein precursors from being converted into the functional proteins required for HIV infection.
Immature, non-contagious virus particles are created as a result.

Absorption:

Diets high in fat and calories caused a drop in AUC and maximum serum concentration (77 percent & 84 percent, respectively).
Lighter meals had no impact on these variables.

Protein binding:

plasma: ~60%

Metabolism:

Hepatic via CYP3A4 to inactive metabolites.
The identification of 6 oxidative and 1 glucuronide conjugate metabolites have occurred.

Bioavailability:

Good
Wide interpatient variability in children: 15 percent to 50 percent.

Half-life elimination:

Children 4 to 17 years (n=18): 1.1 hours
Adults: 1.8 ± 0.4 hours
hepatic insufficiency: 2.8 ± 0.5 hours

Time to peak: 0.8 ± 0.3 hours

Excretion:

Feces (83 percent; 19.1 percent as unchanged drug)
urine (19 percent; 9.4 percent as unchanged drug)

International Brands of Indinavir:

Crixivan
Aviran
Avural
Crixivan
Elvenavir
Inavir
Indilan
Indivan
Indivir
Virxit

Indinavir Brands Names in Pakistan:

No Brands Available in Pakistan.

Disclaimer Notice:

Emedz.net is not an online pharmacy:

We are not affiliated with any pharmaceutical companies:

Indinavir (Crixivan) - Class, Uses, Dosage, Side effects

Indinavir Uses:

HIV-1 infection:

Indinavir dose in adults:

Indinavir dose in the treatment of HIV-1 infection: Oral:

Unboosted regimen:

ritonavir-boosted regimen (off-label dose):

Dosage adjustments for indinavir when administered in combination therapy: Note:

Indinavir dose in childrens:

Indinavir dose in the treatment of HIV-1 infection:

Children: Limited data available; optimal dose not established:

Adolescents:

Oral:

Indinavir dosing adjustment for concomitant therapy:

Pregnancy Risk Category: C

Indinavir use during breastfeeding:

Indinavir Dose in Kidney Disease:

Indinavir Dose in Liver disease:

Common Side Effects of Indinavir:

Gastrointestinal:

Hepatic:

Renal:

Less Common Side Effects of Indinavir:

Central Nervous System:

Dermatologic:

Gastrointestinal:

Genitourinary:

Hematologic & Oncologic:

Hepatic:

Neuromuscular & Skeletal:

Renal:

Respiratory:

Miscellaneous:

Contraindications to Indinavir:

Warnings and precautions

Hemolytic anemia

Hyperbilirubinemia:

Immune reconstitution syndrome:

Nephrolithiasis/urolithiasis:

Tubulointerstitial nephritis:

Diabetes:

Hemophilia A and B:

Hepatic impairment

Monitoring parameters:

How to administer Indinavir?

Mechanism of action of Indinavir:

International Brands of Indinavir:

Indinavir Brands Names in Pakistan:

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