Capecit

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Capecit

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Capecit

Quick Facts

Property Description
Active ingredient Capecitabine (INN)
Form Tablet (Film-coated, Oral form)
Pharmacological class Antineoplastic Agent, Antimetabolite
Common purpose To disrupt the growth of malignant cells
Origin Synthetic (Chemically synthesized)

Capecit is a specialized, prescription-only medication whose active component is the substance Capecitabine (INN), used in oncology to address abnormal cell proliferation. It is classified as an antineoplastic agent, belonging specifically to the group of antimetabolites, a class of chemotherapy agents.


The Identity of Capecit: A Synthetic Antimetabolite Prodrug

Capecitabine is chemically a fluoropyrimidine antimetabolite and is fundamentally a prodrug. This means the compound is chemically inactive upon ingestion; it must undergo a sequence of internal enzymatic conversion steps to be transformed into its potent, cytotoxic form, 5-Fluorouracil (5-FU).

This prodrug mechanism is a key differentiating feature, as it is designed to achieve tumor-selective activation by exploiting the higher concentration of certain enzymes, like thymidine phosphorylase, often present within malignant tumors to concentrate the active drug at the disease site. This feature is clinically recognized for its potential to optimize the delivery of the therapeutic compound.


Composition and Oral Form

The medication is a single-ingredient product and is prepared as an orally administered tablet for systemic absorption, in contrast to the intravenous delivery required for many other antineoplastic agents. The oral form, available under the original brand Xeloda and generic versions, is considered bioequivalent.


General Purpose and Action Principle

The general purpose of this medicine is to cause growth disruption by interfering with the vital processes of rapidly dividing cells, such as those in neoplasms. The activated metabolite, 5-Fluorouracil (5-FU), acts as a nucleoside metabolic inhibitor by blocking the synthesis and repair of DNA and RNA, which is necessary for cancer cell proliferation.

Regulatory References

  1. antineoplastic

What side effects are possible with Capecit?

The safety profile of Capecit (Capecitabine) is established through official regulatory documentation, classifying adverse effects based on the frequency and the physiological system affected. The profile is characterized by the systemic effects of its active metabolite on rapidly dividing cells, particularly within the gastrointestinal tract and skin.


Frequency-Classified Adverse Reactions

Adverse reactions are formally grouped by the frequency of their occurrence in patient populations:

Classification Examples of Effects
Very Common (ge 10%) Diarrhea, Palmar-Plantar Erythrodysesthesia Syndrome (Hand-Foot Syndrome), Stomatitis, Nausea, Vomiting, Fatigue/Asthenia, Anemia.
Common (ge 1% to <10%) Neutropenia, Thrombocytopenia, Dehydration, Constipation, Rash, Alopecia, Headache, Dizziness.
Rare/Very Rare Serious Cutaneous Adverse Reactions (SJS, TEN), Cardiotoxicity (cardiac failure, myocardial infarction).

Key Safety Constraints and Serious Risks

Official labeling defines significant constraints on the use of Capecit. The drug is contraindicated in patients with a confirmed complete Dihydropyrimidine Dehydrogenase (DPD) deficiency due to the high risk of acute, life-threatening toxicity. Use is also restricted in cases of severe renal impairment (creatinine clearance below 30 mL/min). The label explicitly documents the potential for serious Cardiotoxicity and the risk of severe, sometimes fatal, bleeding events when the medicine is used concurrently with oral Vitamin K antagonists.

Population-Specific Notes

The safety profile is differentiated for certain patient groups. Older adults (ge 65 years) may experience a higher incidence of severe adverse reactions, including severe diarrhea and Hand-Foot Syndrome. Safety considerations also dictate that the substance carries warnings regarding embryo-fetal toxicity.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose with Capecit is characterized by acute, unusually severe manifestations of systemic toxicity, as documented in official regulatory labeling. Documented presentations typically involve severe Gastrointestinal Toxicities, including intense diarrhea, vomiting, and inflammation of the mouth (stomatitis). The overdose may also lead to profound Hematologic Toxicity such as myelosuppression and neutropenia.

The most severe, life-threatening outcomes formally documented are Cardiotoxicity and Neurotoxic complications, which can include acute encephalopathy and cerebellar ataxia. Immediate medical attention is required upon recognizing that an overdose has occurred, or if unusually severe, early-onset toxicities appear, regardless of the immediate presence of all symptoms.

Regulatory guidance mandates that emergency treatment must be initiated as soon as possible, and specifically within a 96-hour window from the last dose. An approved antidote, Uridine Triacetate, is available for the emergency management of Capecit overexposure. Patients who undergo emergency management require continuous hospital monitoring, including daily laboratory value assessment.

A critical population-specific note highlights that individuals with a genetic deficiency in the DPD enzyme are at an extremely high risk for acute, life-threatening systemic toxicity, which can mimic a severe overdose even when standard doses are administered.

Therapeutic Uses of Capecit

What Capecit Treats: Main Uses and Benefits

This medication is generally used to provide systemic support across therapeutic domains involving advanced conditions, specifically advanced or metastatic disease of the colon and rectum, certain gastric (stomach) and breast cancers, and as adjuvant therapy after surgery for Stage III colon cancer. The medication is applied to stabilize the condition in contexts marked by increased physiological stress. It helps manage symptomatic domains related to systemic imbalance, assisting with easing the overall symptom load related to the condition.


The drug is commonly applied in the adjuvant setting for patients who have undergone surgery, aiming to address the high-risk clinical status where microscopic residual disease may remain. This supportive benefit is relevant for addressing the potential for disease return, which assists with maintaining functional stability over time. The medication is generally used in situations involving advanced breast cancer when prior systemic treatment has been followed by disease progression. It offers a subsequent line of therapy to stabilize the condition and may assist with the goal of providing sustained disease control when initial treatments have failed.

“The primary goal is to provide systemic support in managing the condition, which assists with easing the overall symptom load.”


Quick Fact: Relief for Uncontrolled Malignant Growth

Property Description
Symptom Axis Addressed Symptoms related to systemic imbalance caused by rapid cell proliferation.
Key Therapeutic Domain Adjuvant and systemic oncology support for advanced solid tumors.
Typical Clinical Context Used during phases when symptoms become more noticeable or the patient requires additional management of discomfort.
Patient-Oriented Benefit Contributes to maintaining stable health and supports general well-being during symptomatic phases.

Regulatory References

  1. European Medicines Agency summary

Eligibility and Restrictions for Use

The official regulatory profile for Capecit (capecitabine) defines eligibility based on specific conditions, organ function, and enzyme status, adhering strictly to government prescribing information.

Populations Strictly Contraindicated

Capecit must not be used in patients with:

  • Severe Renal Impairment (creatinine clearance below 30 mL/min).
  • Complete Absence of Dihydropyrimidine Dehydrogenase (DPD) activity.
  • Known Hypersensitivity to capecitabine, its components, or to 5-Fluorouracil.
  • Pregnancy or Lactation (breastfeeding).

Eligibility Constraints

Constraint Category Official Regulatory Statement
Baseline Blood Counts Treatment must not be initiated if baseline neutrophil counts are below 1.5 imes 10^9/ L or thrombocyte counts are below 100 imes 10^9/ L.
Age Groups The medicine is approved for Adults; however, safety and efficacy have not been established in the pediatric population (under 18 years).
Conditional Use Patients with moderate renal impairment, partial DPD deficiency, or a history of coronary artery disease are eligible but require close medical monitoring and potential adjustment protocols.

All patients of reproductive potential are required to use effective contraception during and for a specified time following treatment, as documented in the label.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile of Capecit (Capecitabine) is officially documented by regulatory authorities, highlighting several necessary constraints and restrictions on co-administration.

Formal Contraindications and Prohibitions

Co-administration with Sorivudine or its chemically related analogues (e.g., brivudine) is formally prohibited due to the risk of a potentially fatal drug interaction resulting from Dihydropyrimidine Dehydrogenase (DPD) enzyme inhibition. Additionally, individuals with a known DPD deficiency are listed as being absolutely contraindicated due to the severe, toxic risk posed by increased metabolite exposure.

Drug–Drug Interaction Patterns

Capecit acts as an inhibitor of the CYP2C9 enzyme. This interaction is documented to increase the systemic exposure of co-administered medicines that are CYP2C9 substrates, such as Phenytoin, leading to increased plasma levels and a potential for intoxication.

Another significant pharmacodynamic interaction occurs with Vitamin K Antagonists (e.g., Warfarin), where co-administration is associated with an increased risk of severe bleeding events due to altered coagulation parameters (elevated INR/PT). The combination of Capecit with Leucovorin (Folinic Acid) is also documented to increase the concentration of the active metabolite, resulting in enhanced toxicity.

Drug–Food Interaction

Co-administration with a meal significantly reduces both the rate and the extent of absorption of the Capecitabine parent drug and its active metabolite. This pharmacokinetic change is the basis for specific administration timing requirements relative to food intake.

Mechanism of Action

Capecitabine (Capecit) is a fluoropyrimidine prodrug that interferes with key biological processes by acting as an antimetabolite, targeting cell replication and function through a unique three-step activation cascade. This activation results in the physiological consequence of cellular growth cessation.

Enzymatic Prodrug Activation and Differential TP Expression

This domain covers the conversion of the prodrug into its active form, utilizing the differential expression of Thymidine Phosphorylase (TP). Capecitabine is initially inactive and requires a three-step enzymatic cascade to yield the cytotoxic agent, 5-Fluorouracil (5-FU). The final, critical step is driven by the enzyme TP, which is typically found in higher concentrations in specific cells. This concentration of the active drug at the site of high TP expression influences the local molecular action.

Inhibition of DNA Replication

The resulting active metabolite, 5-fluorodeoxyuridine monophosphate (FdUMP), targets and irreversibly inhibits the enzyme Thymidylate Synthase (TS). By blocking TS, the drug prevents the production of thymidine triphosphate (dTTP), a vital building block for DNA synthesis and repair. This scarcity of essential components disrupts the function of DNA repair mechanisms in highly proliferative cells, resulting in cellular growth cessation.

Functional RNA Disruption

This domain outlines the complementary mechanism involving interference with protein synthesis machinery. A second active metabolite, 5-fluorouridine triphosphate (FUTP), is mistakenly incorporated into the cell’s RNA (Ribonucleic Acid) structures, particularly ribosomal RNA. This incorporation of a "fraudulent" nucleotide disrupts the normal functioning and processing of RNA, consequently inhibiting protein synthesis and adding a secondary, critical layer to the cytotoxic mechanism.

Dosage and Administration Information

How to use Capecit — Official Administration Guidelines

Capecit is an oral medication administered in strict cycles, with the dosage precisely determined by the patient's body size.


Administration Scope

Feature Official Instruction
Route of administration Oral administration only, via film-coated tablets in 150 mg and 500 mg strengths.
Dosing schedule Dosing is calculated per Body Surface Area (m^2) and is administered twice daily (BID), approximately 12 hours apart. Standard starting doses generally range from 1000 mg/m^2 to 1250 mg/m^2 BID.
Timing in relation to meals Must be taken with water and within 30 minutes after completing a meal.
Preparation requirements The tablets must be swallowed whole and should not be crushed, chewed, or cut. The dose is rounded to the nearest whole tablet increment.
Age-group administration rules No specific starting dose adjustment is mandated based on advanced age alone.
Missed-dose rules If a dose is missed, it must not be taken later; the next dose should be taken at the regularly scheduled time.
Special procedural conditions The standard regimen is administered in 21-day cycles, consisting of 14 consecutive days of dosing followed by a 7-day rest period.

Instruction Classifications (High-Level)

Classification Detail
Administration method type Oral.
Frequency pattern Twice daily (BID) administration in an intermittent (cyclic) pattern.
Regulatory basis Established clinical and pharmaceutical standards.
Use-context constraints Patients with moderate renal impairment (creatinine clearance 30 to 50 mL/min) require a 25% reduction of the starting dose.

Resulting Procedural Structure

Official step sequence:

  • The total daily dose is divided and taken twice daily, calculated based on the individual's Body Surface Area.
  • The oral doses must be taken whole, with water, and within 30 minutes of eating (morning and evening).
  • The active dosing is conducted for 14 days, which is then followed by a 7-day unmedicated rest period to complete a standardized 21-day cycle.

Connection to the overall use protocol: The official administration guidelines establish a cyclic, oral regimen with a BSA-dependent dose taken specifically with meals, which dictates the structured manner in which the medicine is to be systemically delivered. This framework includes predetermined adjustments for moderate kidney function impairment and explicit rules for handling missed doses to maintain the integrity of the prescribed schedule.

Recent Clinical Evidence

Research evidence / Overview of studies for Capecit

This section provides an overview of the official research that has studied Capecitabine, focusing on the types of trials conducted, the populations included, and the areas where research is still ongoing. The information below reflects patterns observed in the studies but provides no clinical guidance.


Evidence for Use in Colorectal Cancer

Research exploring the use of Capecitabine in colorectal cancer has focused on its use after surgery (the adjuvant setting) for Stage III disease and its use in advanced disease (metastatic colorectal cancer). These evaluations primarily utilized large, international Randomized Controlled Trials (RCTs).

Studies for patients who had surgery for Stage III colon cancer compared Capecitabine monotherapy to the traditional intravenous regimen, 5-Fluorouracil (5-FU) plus leucovorin. The findings describe patterns observed in the studies where measurements for disease-free status (DFS) and long-term survival (OS) for Capecitabine were reported to be consistent with the measurements observed for the intravenous standard. In the metastatic setting, Capecitabine-based combinations were generally reported to be consistent with the measures of disease progression seen with 5-FU-based regimens.


Research in Specific Patient Groups

The research has included specific study analyses to address the needs of certain patient groups, such as older adults (typically aged 70 or older) with colon cancer. Studies demonstrate that the data show patterns related to similar outcomes as those measured in younger adults in patients included in the study who met the criteria for overall physical health and organ function. However, the available evidence is limited regarding the drug's role in patients with reduced kidney function, and data for certain groups remain insufficient (e.g., pregnant patients or children), reflecting the specialized nature of the drug's use.


What the Research Landscape Still Needs to Clarify

Despite a substantial foundation of evidence, certain aspects of Capecitabine's use remain uncertain. Research is ongoing to determine the optimal duration of treatment for adjuvant colon cancer; for instance, research has explored whether a shorter course (e.g., 3 months) can provide similar measurements as the longer 6-month course. Additionally, comparative evidence for direct comparison with other newer oral agents is lacking in some settings, and for advanced breast cancer, there is still research exploring different treatment schedules to assess how this may influence the reported patterns of change in outcomes.

Key Studies & References

  1. Final results of a randomized trial comparing capecitabine with fluorouracil (5-FU)/leucovorin (LV) for adjuvant therapy of stage III colon cancer: the X-ACT trial
  2. Capecitabine-based chemotherapy for metastatic colorectal cancer - Database of Abstracts of Reviews of Effects (DARE)
  3. The Role of Capecitabine in the Treatment of Colorectal Cancer in the Elderly

Frequently Asked Questions (FAQ)

Common questions about Capecit (FAQ)


Q: What should I know about Capecit before I start taking it?

Official product information includes specific warnings that patients should be aware of before starting treatment. Regulatory documents indicate the drug may cause fetal harm and its use is contraindicated during pregnancy. Warnings also relate to potential severe side effects, like diarrhea, and the risk of drug interactions, especially with blood thinners.


Q: Does Capecit cause hair loss?

Hair thinning or loss, also called alopecia, is listed as a possible side effect of this medicine. However, according to the official product information, it is not reported among the most common adverse reactions (ge30%) seen in clinical studies.


Q: Is it normal to feel very tired when taking Capecit?

Yes, according to official regulatory documents, feeling very tired or weak (known as fatigue and asthenia) is a very common adverse reaction. It was reported in a significant number of patients in clinical studies.


Q: Can Capecit affect my liver function?

Official information indicates that the medicine can affect liver function. Monitoring is recommended for patients who already have existing liver problems (hepatic impairment). Elevated bilirubin, which is a sign of changes in liver function, is listed as an adverse reaction.


Q: What are the most commonly reported side effects of Capecit?

The most commonly reported side effects in clinical studies include stomach issues such as diarrhea, nausea, and abdominal pain. Other very common adverse reactions include fatigue and a specific skin reaction known as hand-and-foot syndrome.


Q: Is Capecit considered a chemotherapy drug?

Yes, according to its official classification, Capecit is considered an antineoplastic agent, which is a type of medicine used to treat cancer. It is specifically a cytotoxic medicine, which is a key characteristic of antineoplastic agents.


Q: Why do official documents describe Capecit as a 'pro-drug'?

Official documents describe Capecit as a 'pro-drug' because the medicine itself is inactive when taken. It must be converted by specific enzymes inside the body to become the active drug, 5-fluorouracil. This conversion process is known to involve specific enzymes in the body.


Q: Are there any long-term effects of Capecit treatment that I should be aware of?

Most side effects are known to be temporary and resolve after treatment is reduced or discontinued. However, the official patient information mentions a rare potential for permanent effects. This may include the loss of fingerprints in cases where the hand-and-foot syndrome becomes severe and chronic.


Q: Can men use Capecit?

The regulatory label indicates the medicine for use in conditions that affect both men and women. There are no restrictions on its use based on gender found in the official product information.


Q: Does Capecit interact with common pain relievers like ibuprofen?

The official product label lists specific drug-to-drug interactions, but it does not list a direct interaction with ibuprofen. However, a general caution exists regarding the use of Non-Steroidal Anti-inflammatory Drugs (NSAIDs) due to risk factors for gastrointestinal bleeding.


Q: What kind of studies support the use of Capecit for its main purpose?

The uses of this medicine, as authorized by regulatory bodies, are supported by clinical trials. These studies examined the drug's effectiveness and safety profile in treating specified stages of various cancers, including colorectal and breast cancer.


Q: Is it possible for Capecit to cause a skin reaction on the hands and feet?

Yes, official product information indicates that a skin reaction is very common. This reaction is known as Hand-and-Foot Syndrome (palmar-plantar erythrodysesthesia), and usually affects the palms of the hands and the soles of the feet.


Q: How is Capecit stored?

Regulatory guidance states that the medicine should be stored at room temperature, which is typically between 68 F and 77 F (20 C to 25 C). The tablets should remain in a closed container and be protected from heat, moisture, and direct light.


Q: Can I drink alcohol while I am on Capecit therapy?

Official patient information suggests discussing the consumption of alcohol with a healthcare professional. This is because both the medicine and alcohol can cause similar adverse effects, such as dizziness or nausea, which could potentially become worse when consumed together.


Q: Is Capecit safe for older adults?

Studies have examined the use of this medicine in older adults (aged 65 and over). Official data indicates that this population had a higher frequency of severe adverse reactions (Grade 3 or 4) when compared to younger patients. This difference often leads to closer monitoring during treatment.


Q: Do patients always get side effects when taking Capecit?

No, not all patients experience side effects. While regulatory data reports some adverse reactions are very common, no single side effect has been reported to affect 100% of patients in clinical studies.


Q: Can Capecit affect my ability to drive or operate machinery?

Official documents warn that the medicine may affect a patient’s ability to drive or operate machinery. This is due to potential adverse reactions such as dizziness and fatigue.


Q: Why is it sometimes combined with other medicines?

Official documents indicate that Capecit is authorized for use in combination regimens, not just as a standalone treatment. It may be combined with other medicines, such as docetaxel or platinum-based agents, for treating specific conditions.


Q: Is Capecit safe to use during pregnancy?

No. According to regulatory documents, the medicine can cause fetal harm. Therefore, its use is specifically contraindicated (should not be used) during pregnancy.


Q: Is it true that Capecit can cause mouth sores?

Yes, the official product information lists stomatitis, which involves soreness or ulcers inside the mouth, as a commonly reported adverse reaction.


Q: What are the official guidelines about sun exposure while on Capecit?

Official information warns that treatment can lead to increased sensitivity of the skin to sunlight, which is known as photosensitivity. Patients should be aware of this potential adverse effect.


Q: How does the body break down Capecit?

The body first breaks down (metabolizes) the medicine into 5-fluorouracil, which is the active drug. The resulting compounds, or metabolites, are then predominantly passed out of the body through the urine.


Q: What kind of monitoring is done while a patient is on Capecit?

Throughout the course of treatment, monitoring of the patient's health is required. This often includes blood tests to check blood cell counts, liver and kidney function, and the assessment for specific adverse effects like severe diarrhea.


Q: Does Capecit interfere with blood thinners?

Yes, a clinically important interaction is reported with coumarin-derivative blood thinners, such as warfarin. This interaction necessitates frequent monitoring of blood clotting parameters (like INR) and may require adjustment of the blood thinner's dose.


Q: Is Capecit the generic or brand name of the medicine?

Capecitabine is the name of the generic active substance in the medicine. Capecit is the name used in this document, and other trade names under which the drug is marketed include XELODA.


Q: Can Capecit affect my sense of taste?

Changes or disturbance to the sense of taste are listed in the official patient information as a common effect that can occur during treatment.


Q: Are there specific symptoms that require immediate medical attention while on Capecit?

Yes, official regulatory information notes that treatment interruption is generally necessary if severe adverse reactions occur. Examples of severe toxicities include severe diarrhea, vomiting, fever, or severe skin reactions.


Q: Is Capecit allowed for use in people with kidney problems?

The use of Capecit is addressed in regulatory documents regarding kidney function (renal impairment). Use is allowed for people with moderate impairment but requires a lower starting dose. However, it is contraindicated (not allowed) for people with severe kidney impairment.


Q: Can taking Capecit cause dehydration?

Yes, dehydration is listed as an adverse reaction in the official safety information. This can be a severe condition and often occurs as a consequence of other side effects like severe diarrhea and vomiting.


Q: What is the risk of serious infection while on Capecit?

Severe neutropenia, which is a significant drop in the number of white blood cells in the body, is a known adverse event. This reduction in immune cells increases the risk of developing a serious infection.


Q: Does Capecit affect fertility?

Studies conducted in animals have indicated that the medicine may lead to decreased fertility.


Q: Are there different forms of Capecit available?

The medicine is supplied as film-coated tablets. According to the official description, these tablets are available in two specific strengths: 150 mg and 500 mg.


Q: Is there a maximum time a person can be treated with Capecit?

For certain uses, such as adjuvant colon cancer, treatment is recommended for a total duration of six months (eight cycles). For other authorized uses, treatment typically continues until there is evidence of disease progression or the patient experiences intolerable side effects.


Q: What are the most important things to mention to my doctor about my health history before starting Capecit?

Official contraindications and warnings highlight the importance of discussing certain elements of your health history. These relate to a prior history of severe reactions to similar medicines (fluoropyrimidines), a known DPD deficiency, and any existing severe kidney or liver problems.


Q: Can Capecit be taken by children?

The official label provides indications and dosing information for use in adult populations, such as for the treatment of colorectal and breast cancer. It does not provide information regarding the use or appropriate dosing for pediatric patients (children).


Q: Does Capecit cause weight changes?

Yes, a change in body weight is reported in clinical data. Specifically, decreased weight is a finding documented in the official product information.


Q: What is the purpose of the routine blood tests during Capecit treatment?

Routine blood monitoring is required throughout treatment to check for changes in the blood, such as a drop in blood cell counts (neutropenia). The tests also help monitor for signs of changes in liver function, such as elevated bilirubin levels.


Q: Is there an official patient leaflet available for Capecit?

Yes, the official Prescribing Information for the medicine includes references to patient labeling. This documentation is provided to ensure patients receive adequate information about the medicine.


Q: Are the side effects of Capecit temporary or permanent?

Most side effects are temporary and typically resolve once the treatment dose is adjusted or the medicine is stopped. However, official information does mention that in rare cases, severe skin reactions like hand-foot syndrome have been associated with permanent physical effects.

How should Capecit be stored and disposed of?

How to Store and Dispose of Capecitabine

Capecitabine tablets must be stored at Controlled Room Temperature, defined as 20 C to 25 C (68 F to 77 F). The medicine must be kept in its original, tightly closed container and protected from heat, moisture, and freezing.

To ensure safety, the medication must be stored out of the sight and reach of children.

Capecitabine is classified as a cytotoxic agent, requiring specific handling and disposal. The tablets must not be crushed or cut by the patient. Unused or expired tablets must not be thrown in the household trash or flushed down the toilet. Instead, disposal must follow official guidelines for regulated medical waste, typically requiring return to a pharmacy or healthcare provider for proper handling.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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