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Agnel George
Roll no 02
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.
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.
Imatinib is also known as “Gleevec” or “Glivec”
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
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.
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.
Drug name:-------------- Imatinib
Generic name:----------- Imatinib Mesylate
Pharmalogical name:--------- Gleevec
Imatinib is taken orally
Give with meal and large glass of water (at least 8 oz).
Store at 15°–30° C (59°–86° F).
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 is the study of what happens to drugs once they enter the body.
- 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.
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
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.
The most frequently reported adverse reactions (>30%) were edema, nausea, vomiting, muscle cramps, musculoskeletal pain, diarrhea, rash, fatigue and abdominal pain.
-Hypersensitivity to imatinib or any of its components; viral infections, including herpes and chickenpox; intramuscular injections with concurrent thrombocytopenia; pregnancy (category D), lactation; children.
-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
-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.
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)