Cilostazole
Contraindicated
Textbook
Increased plasma levels and toxicity of cilostazole.
Should not be administered along with inhibitors of CYP3A4.
Source: KDT 7e · p555
Drug reference
Imatinib
Tyrosine kinase inhibitor (TKI) — BCR-ABL, PDGFR, c-KIT inhibitor · Antineoplastic
Also known as Imatinib mesylate
START
Baseline CBC, LFTs, creatinine, electrolytes, cardiac function (ECHO if cardiac history). Verify not pregnant. Counsel on taking with food and large glass of water to reduce GI irritation. BCR-ABL transcript monitoring at baseline.
TYPICAL MAX
800mg/day. Dose-limiting toxicity is typically myelosuppression or fluid retention. Dose interruption/reduction is common during therapy.
STOP IF
ANC <1000, platelets <50,000 (hold until recovery), severe fluid retention, hepatotoxicity (bilirubin >3x ULN or transaminases >5x ULN), SJS/TEN, severe CHF.
WATCH
CBC weekly for first month, then biweekly, then monthly. LFTs monthly. Weigh patient regularly (fluid retention). BCR-ABL transcript levels q3 months to monitor molecular response (major molecular response = goal). Many drug interactions via CYP3A4.
CDSCO approvedSchedule HATC L01EA01
KDIGO 2024 + manufacturer label
- ONSET
- 1h · Onset ~1 hour
- PEAK
- 3h · Tmax 2-4 hours
- t½
- 18h · t½ ~18 hours; metabolite ~40h
- DURATION
- 1d · 24 hours (QD)
EXCRETION
Fecal as parent + metabolites (~68%)
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Contraindicated in pregnancy—teratogenic in animals. Effective contraception required during and for 15 days after treatment (both sexes).
FDA category + note
Top interactionssee all 12 →
- CilostazoleContraindicatedTextbookKDT 7e · p555
- EbastineSevereTextbookKDT 7e
- AcalabrutinibSevereDatabaseDDInter
- AdalimumabSevereDatabaseDDInter
Available in India
68 branded formulations. Look up specific brands in the Drugs workspace.
Mechanism
Competitively inhibits ATP binding to tyrosine kinase domains of BCR-ABL (Philadelphia chromosome fusion protein), platelet-derived growth factor receptor (PDGFR), and stem cell factor receptor (c-KIT). Blocks downstream signaling pathways (RAS/MAPK, PI3K/AKT, STAT5), inhibiting proliferation and inducing apoptosis of malignant cells.
Indications
Chronic myeloid leukemia (CML) — all phases (chronic, accelerated, blast crisis)Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL)Gastrointestinal stromal tumor (GIST) — c-KIT positiveDermatofibrosarcoma protuberans (DFSP)Myelodysplastic/myeloproliferative diseases (MDS/MPD) with PDGFR rearrangementsAggressive systemic mastocytosis (ASM)Hypereosinophilic syndrome (HES) / chronic eosinophilic leukemia (CEL)Pediatric Ph+ ALL and CML
Dosing
- Adult
- CML chronic phase: 400mg PO daily. CML accelerated/blast crisis: 600mg PO daily (may increase to 800mg daily). Ph+ ALL: 600mg PO daily. GIST (adjuvant/metastatic): 400mg PO daily. DFSP: 800mg PO daily. MDS/MPD, ASM, HES/CEL: 400mg PO daily.
- Pediatric
- CML/Ph+ ALL: 340mg/m²/day (max 600mg). DFSP: 400mg/m² BID (max 800mg/day).
- Renal adjustment
- CrCl ≥20: no adjustment. CrCl <20 or HD: reduce dose 25-50% and monitor closely.
- Hepatic adjustment
- Mild-moderate: no adjustment. Severe: reduce dose 25% and monitor.
- Geriatric
- No specific adjustment; monitor for fluid retention and cardiac toxicity.
- Max dose
- 800mg/day (CML blast crisis, DFSP)
Pharmacokinetics
Onset
Hematologic response in CML: 1-3 months; cytogenetic response: 6-12 months; molecular response: 12-18 months
Peak effect
Tmax 2-4 hours; steady-state in ~7 days
Duration
24 hours (QD dosing)
Half-life
~18 hours (imatinib); ~40 hours (active metabolite N-desmethyl imatinib / CGP74588)
Bioavailability
~98%
Protein binding
~95% (albumin, alpha-1-acid glycoprotein)
Metabolism
Hepatic via CYP3A4 (major) to active N-desmethyl metabolite (CGP74588, equipotent); also CYP1A2, CYP2D6
Excretion
~68% fecal (unchanged 20% + metabolites); ~13% renal
Contraindications
- Hypersensitivity to imatinib
- Pregnancy (teratogenic in animals)
- Breastfeeding
Side effects
Common
Edema / fluid retention (periorbital, peripheral, pleural effusion)Nausea and vomitingMuscle crampsFatigueDiarrheaRashHeadacheMyelosuppression (anemia, neutropenia, thrombocytopenia)
Serious
- Severe fluid retention / pleural effusion / pericardial effusion / ascites
- Hepatotoxicity (elevated LFTs, hepatic failure rare)
- Severe myelosuppression
- Tumor lysis syndrome
- Cardiac toxicity (left ventricular dysfunction, CHF—rare)
- Hemorrhage (GI, CNS—especially with thrombocytopenia)
- Severe skin reactions (SJS/TEN)
- Hypothyroidism (when used with levothyroxine in thyroid cancer)
Pregnancy & lactation
Pregnancy
Contraindicated in pregnancy—teratogenic in animals. Effective contraception required during and for 15 days after treatment (both sexes).
Lactation
Excreted in breast milk; discontinue breastfeeding during treatment.
Drug interactions
Ebastine
Severe
Textbook
Increased risk of arrhythmogenic potential.
Exercise caution with coadministration.
Source: KDT 7e
Acalabrutinib
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Adalimumab
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Alfentanil
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Aminolevulinic Acid
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Apalutamide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Avanafil
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Avapritinib
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Avatrombopag
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Baricitinib
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Benzhydrocodone
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Related guidelines
Empirical antimicrobial use in common syndromes
ICMR · Infectious Diseases · 2019
Acute coronary syndrome in chronic kidney disease
CSI · Cardiology · 2020
Extrapulmonary tuberculosis
ICMR · Infectious Diseases · 2022
Sjögren's syndrome
EULAR · Rheumatology · 2025
Glomerular diseases
KDIGO · Nephrology · 2021
Ask House about Imatinib
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19