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Drug presentation

Agnel George

Roll no 02

Anticancer Drugs

Imatinib

Intro

Pharmacology

What is Pharmacology ?

The study of drugs or chemicals and the effects they have on living animals is called pharmacology. Pharmacology explains what drugs are, what they do to body functions and what the body does to them.

What is it?

General idea

In life everyone at once will relay on some kind of pharmaceutical product, whether if it was for self-use or someone else, therefore it is useful to know the basic understanding of pharmacology and the drug uses. The general idea behind a drug is a chemical that interacts with proteins in the body to affect a physiological function.

Drug

Drug: Imatinib

Name of the Drug

Imatinib is also known as “Gleevec” or “Glivec”

Anticancer drug Imatinib

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Info

Imatinib is an oral chemotherapy medication used to treat cancer. Imatinib was identified in the late 1990s by Dr Brian J. Druker. Specifically, it is used for Chronic myelogenous leukemia (CML), Acute lymphocytic leukemia (ALL), and Gastrointestinal stromal tumor (GISTs) and a number of other malignancies

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cont...

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it was called the magic bullet when it revolutionized the treatment of chronic myeloid leukemia when it was released in 2001. The first clinical trial of Imatinib took place in 1998 and the FDA approved in May of 2001 and generic version became available in the UK as of 2017.

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Due in part to the development of Imatinib and related drugs, the five-year survival rate for people with chronic myeloid leukemia (CML) increased from 31% in 1993, to 59% in 2009, to 70% in 2016. Proving the success-fulness of the drug.

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Different drug names

Dose Frequency & Route

Drug name:-------------- Imatinib

Generic name:----------- Imatinib Mesylate

Pharmalogical name:--------- Gleevec

Administration

Imatinib is taken orally

Give with meal and large glass of water (at least 8 oz).

Store at 15°–30° C (59°–86° F).

Route & Dosage

Dosage

CML Chronic Phase

Adult: PO 400–800 mg q.d. with a meal and large glass of water

Child: PO >3 y, 260 mg/m2/d in 1 or 2 divided dose(s) (max: 340 mg/m2/d)

CML Accelerated Phase or Blast Crisis

Adult: PO 600 mg q.d. with a meal and large glass of water

GISTs

Adult: PO 400–600 mg q.d. times up to 24 mo

Hepatic Impairment

Reduce dose to 300 mg q.d. (chronic) or 400 mg q.d. (accelerated, blast crisis)

Pharmacokinetics

PHARMACOKINETICS

Pharmacokinetics is the study of what happens to drugs once they enter the body.

Includes the following

- The absorption of the drug into the blood and across cell membranes to enter the cells. 98% reaches systemic circulation in around 2 – 4 hours.

- The distribution of the drug throughout the body;

- The metabolism or breakdown of the drug primarily by CYP3A4 in liver.

- The excretion of the drug from the body primarily excreted in feces.

- Half-Life: 18 h imatinib, 40 h active metabolite.

Icludes...

Pharmacodynamics

described as what a drug does to the body

- Imatinib binds to BCR/Abl protein very close to the binding site of ATP, blocking ATP from binding. Without the binding of ATP, Bcr/Abl cannot phosphorylate substrate proteins.

- Imatinib is very specific to this sub-family of receptor tyrosine kinases

- Blocking the ability of Bcr/ Abl stops several transduction pathways that cause the excessive proliferation of partially differentiated cells that lead to CML

PHARMACODYNAMICS

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ADVERSE DRUG REACTIONS

Drug Reaction

An adverse drug reaction (ADR) is an injury caused by taking medication. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs.

Side Effects

The most frequently reported adverse reactions (>30%) were edema, nausea, vomiting, muscle cramps, musculoskeletal pain, diarrhea, rash, fatigue and abdominal pain.

Side Effects

Contraindication

Contraindication

-Hypersensitivity to imatinib or any of its components; viral infections, including herpes and chickenpox; intramuscular injections with concurrent thrombocytopenia; pregnancy (category D), lactation; children.

Cautions include...

-Hepatic impairment

- Risk of severe CHF or left ventricular dysfunction, especially in patients with comorbidities

- pregnancy, risk of embryo-fetal toxicity

- Risk of fluid retention

- Risk of growth stunting in children or adolescents

Cautions include

Nursing responsibility

Nursing Responsibility

-Monitor for S&S of fluid retention. Weigh daily and report rapid weight gain immediately.

- Lab test: CBC with platelet count and differential weekly.

- Review concurrent medications.

conclusion

conclusion

Using the drug Imatinib has shown improvement in patients and doctors continue to prescribe them. As of now long-term survivals is a reality now. imatinib has revolutionized the management of Chronic Myeloid Leukemia (CML)

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