[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/microtubule-inhibitors/) › Vincristine

[Pharmacology](https://durgical.com/en/pharmacology/) · [Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/microtubule-inhibitors/)

# Vincristine

Vinca alkaloid that blocks the mitotic spindle. Key in childhood leukaemia and lymphoma; it injures nerves, spares the marrow, is fatal given intrathecally.

Updated 2026-11-01

- Class: [Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/microtubule-inhibitors/)
- Target: β-tubulin (vinca site, at the junction between tubulin dimers)
- ATC code: L01CA02
- WHO Model List of Essential Medicines

## ⚠ High-alert medication

An error with this medicine can cause serious harm: double checks and protocols are used.

◆**β-tubulin (vinca site, at the junction between tubulin dimers)**Vincristine

ⓘ The figure shows vinblastine, which occupies the same vinca site, bound to bovine tubulin; no vincristine–tubulin structure is available.

**Target in 3D:** β-tubulin (vinca site, at the junction between tubulin dimers). PDB structure 5J2T (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/5J2T) · Drag to rotate · pinch to zoom

## Mechanism of action

Vincristine binds β-tubulin at the vinca site and stops tubulin dimers from adding to microtubules. Without a mitotic spindle, dividing cells arrest in metaphase and die. Nerve axons also depend on microtubules to transport material, so the same action causes a dose-related sensory, motor and autonomic neuropathy.

- Vincristine binds tubulin at the vinca site
- Microtubules cannot assemble: no spindle
- Cells arrest in metaphase and die
- Axonal transport fails too: neuropathy

## Pharmacokinetics

**Absorption**
Intravenous only.

**Distribution**
Leaves the blood quickly and binds tightly in tissues; enters the cerebrospinal fluid poorly.

**Metabolism**
Liver, by CYP3A; also a P-glycoprotein substrate.

**Elimination**
Mostly in the faeces (bile); a smaller part in the urine.

**Half-life**
Long terminal half-life, about 85 hours on average, varying widely between people.

## Indications

- Acute leukaemia.
- Hodgkin and non-Hodgkin lymphoma, in combination.
- Rhabdomyosarcoma, neuroblastoma and Wilms tumour, in combination.

## Adverse effects

### Common

- Hair loss (the most common effect)
- Constipation and abdominal cramps
- Tingling and numbness, loss of tendon reflexes, foot drop
- Jaw, throat and bone pain
- Urinary retention from bladder atony

### Serious (rare, important)

- Death or ascending paralysis if given intrathecally
- Paralytic ileus, especially in young children
- Cranial nerve palsies, including bilateral vocal cord paralysis
- Hyponatraemia from inappropriate ADH secretion
- Hepatic veno-occlusive disease in children; tissue injury after extravasation

## Contraindications

- Demyelinating form of Charcot–Marie–Tooth disease
- Any route other than intravenous

## Key interactions

**Strong CYP3A inhibitors (e.g. itraconazole); moderate ones such as fluconazole**
Earlier and more severe neurotoxicity; strong inhibitors are avoided.

**Strong CYP3A inducers (e.g. St John's wort) and P-glycoprotein inhibitors or inducers**
Change vincristine exposure; avoided.

**Phenytoin**
Chemotherapy combinations with vincristine have lowered phenytoin levels and increased seizures.

**Mitomycin**
Acute bronchospasm and breathlessness occur most often with this combination.

**Live vaccines**
Not recommended during treatment.

## What is monitored

- Neurological examination: sensation, reflexes, gait, hoarseness
- Bowel movements and abdominal examination
- Sodium (SIADH) and blood counts in combination regimens
- Liver tests, especially in children

## Administration and safety

- Intravenous use only: given intrathecally it is usually fatal. The bag is labelled «for intravenous use only – fatal if given by other routes».
- Dispensed diluted in a flexible plastic container, which lowers the risk of a fatal wrong-route error.
- Vesicant: if leakage occurs, the injection is stopped and the rest given in another vein; local hyaluronidase and moderate heat help disperse the drug.
- Mixed only with normal saline (sodium chloride); the needle position is confirmed before injecting.
- Hazardous drug: prepared and given following hazardous-drug handling procedures (impervious gloves, no skin contact) and disposed of as cytotoxic waste.

## Nursing care

- Before giving it, confirm the route is intravenous with a second nurse; it is never taken to a lumbar puncture or intrathecal procedure.
- Bowel regimen from the start (fluids, fibre, stool softeners); ask about stools every day and report abdominal pain or no bowel movement.
- Ask about tingling, weakness, trouble walking or buttoning, jaw pain and hoarseness before each dose.
- Check that the patient is passing urine normally.
- Avoid eye contact with the drug; if it happens, rinse the eye immediately and thoroughly.

## Pregnancy and breastfeeding

Can cause fetal harm; pregnancy is avoided during treatment.

## Memory aid

VinCRIStine «CRIppleS the nerves» and spares the marrow; VinBLAStine «BLASts the bone marrow». And the vinca rule: «veins only – never the spine».

## Test yourself

Think of the answer, then tap the question to see it.

## What is the dose-limiting toxicity of vincristine?

Neurotoxicity: peripheral neuropathy, constipation and ileus, cranial nerve palsies. Marrow suppression is minor.

## Why is vincristine dispensed diluted in a flexible plastic container labelled for intravenous use only?

To prevent a fatal wrong-route error: intrathecal vincristine is usually fatal.

## A child on vincristine has colicky abdominal pain and an empty rectum. What should be suspected?

Constipation with upper-colon impaction or paralytic ileus from vincristine's autonomic neurotoxicity.

## Which antifungals raise vincristine toxicity, and why?

Azoles such as itraconazole (and fluconazole) inhibit CYP3A, which metabolises vincristine, so neurotoxicity comes earlier and is more severe.

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## Related drugs

- [Vinblastine](https://durgical.com/en/pharmacology/vinblastine/)
- [Vinorelbine](https://durgical.com/en/pharmacology/vinorelbine/)
- [Paclitaxel](https://durgical.com/en/pharmacology/paclitaxel/)

[← Back to the class: Microtubule inhibitors](https://durgical.com/en/pharmacology/classes/microtubule-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - VINCRISTINE SULFATE injection, solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b22e4c8e-dbe1-4d4b-a026-e1812974071c) (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 70 (McGraw Hill, 2023); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01CA02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/vincristine/
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