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Cobicistat

Pharmacokinetic enhancer (CYP3A inhibitor, no antiviral activity) · Antiretroviral Booster

START
150 mg PO once daily with food (with boosted ARV)
TYPICAL MAX
150 mg/day
STOP IF
Serious interacting-drug toxicity or true renal decline
WATCH
Full interaction review; baseline/periodic creatinine (interpret eGFR shift)
CDSCO approvedSchedule HATC V03AX03
Renal dose adjustmenteGFR mL/min/1.73m²
CAUTIONUsual; expect small non-…70REDUCEAvoid starting certain tenofovir-DF combos90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET3.5hPEAK3.5h1dDURATION
ONSET
1h · absorption
PEAK
3.5h · Tmax
3.5h ·
DURATION
1d · once-daily
EXCRETION
Mainly faecal; minor renal
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Boosted regimens may give inadequate levels in pregnancy — alternative regimens often preferred.
FDA category + note
Top interactionssee all 12
  • CilostazoleContraindicatedTextbookKDT 7e · p555
  • AlfuzosinContraindicatedDatabaseKimi deep-research + Cla
  • Ergot AlkaloidsContraindicatedDatabaseKimi deep-research + Cla
  • SimvastatinContraindicatedDatabaseKimi deep-research + Cla

Mechanism

Potent mechanism-based inhibitor of CYP3A (and weak CYP2D6); has no antiviral activity itself but boosts plasma levels of co-administered CYP3A-metabolised antiretrovirals (elvitegravir, atazanavir, darunavir).

Indications

Pharmacokinetic booster for selected HIV antiretrovirals (elvitegravir, atazanavir, darunavir)

Dosing

Adult
150 mg PO once daily with food, co-administered with the boosted antiretroviral (fixed-dose combinations common).
Pediatric
Per weight-banded fixed-dose combination products (specialist).
Renal adjustment
Inhibits tubular creatinine secretion (apparent eGFR fall ~10 mL/min, non-progressive); avoid starting certain TDF combos if CrCl <70.
Hepatic adjustment
Severe hepatic impairment: not recommended.
Geriatric
No specific adjustment.
Max dose
150 mg/day

Pharmacokinetics

Onset
CYP3A inhibition within hours
Peak effect
~3–4 h (Tmax)
Duration
~24 h (once-daily)
Half-life
~3–4 h
Bioavailability
Enhanced with food
Protein binding
~97–98%
Metabolism
CYP3A (and CYP2D6) — substrate and inhibitor
Excretion
Mainly faecal; minor renal

Contraindications

  • Co-administration with drugs highly CYP3A-dependent with serious/life-threatening toxicity (e.g., certain ergot alkaloids, lovastatin/simvastatin, some sedatives, alfuzosin)
  • Hypersensitivity

Side effects

Common
NauseaDiarrhoeaHeadacheReduced estimated GFR (creatinine secretion inhibition, non-pathologic)
Serious
  • Serious interactions via CYP3A inhibition
  • True nephrotoxicity (with tenofovir DF combinations)
  • Severe hypersensitivity

Pregnancy & lactation

Pregnancy

Boosted regimens may give inadequate levels in pregnancy — alternative regimens often preferred.

Lactation

Breastfeeding not recommended in HIV (per regional guidance).

Drug interactions

Cilostazole
Contraindicated
Textbook

Increased plasma levels and toxicity of cilostazole.

Should not be administered along with inhibitors of CYP3A4.

Source: KDT 7e · p555

Alfuzosin
Contraindicated
Database

Increased levels

Contraindicated per label

Source: Kimi deep-research + Cla

Ergot Alkaloids
Contraindicated
Database

CYP3A inhibition

Contraindicated

Source: Kimi deep-research + Cla

Simvastatin
Contraindicated
Database

CYP3A inhibition

Contraindicated; use pravastatin/low-dose alternative

Source: Kimi deep-research + Cla

Ebastine
Severe
Textbook

Increased risk of arrhythmogenic potential.

Exercise caution with coadministration.

Source: KDT 7e

Abemaciclib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Acalabrutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Amiodarone
Severe
Database

Increase amiodarone levels.

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apixaban
Severe
Database

Drug interaction classified as: absorption, metabolism

Source: DDInter

Artemether
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Ask House about Cobicistat

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Sources: BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20