Health
A Toxicologist Explains the Details
many adults take prescription drugsthe utilization is keep increasingApproximately 1.3 million emergency department visits in the United States caused by adverse drug events Patient education is becoming more and more important every year.
all prescription drugs Comes with instructions on how to use them safely and effectivelyDepending on the drug, there may be. some kind of information Includes: Patient Information Sheets, Medication Guides, and Instructions for Use. You can fold one or more of these documents into a box or attach them as printed pages provided by your pharmacist.
i am a scientist I study how drugs and other chemicals affect human health. While it may seem intimidating, package inserts (especially prescribing information) help patients better understand the contents of pill bottles, blister packs, and the like.
What can you learn from the attached document?
The part of the attachment that is often overlooked is Prescribing informationAlthough written primarily for medical professionals, it contains a wealth of information about how drugs interact with the body.
If the prescribing information is not included with your prescription, you can often find a copy on the National Institutes of Health site. Daily Med website or other Drug information website.
As an example, consider any of the following: The most widely prescribed drug in the United States, atorvastatin (Lipitor). Among other effects, it increases overall cholesterol levels and lowers low-density lipoprotein cholesterol (LDL) levels. “Bad” Cholesterol.
By reading the insert, you can answer some important questions about this drug. If you want to follow Click here for a prescription for Lipitor.
how do the drugs work?
To answer this question, see the subsections Mechanism of Action and Pharmacodynamics. prescription insert.
of Mechanism of action and pharmacodynamics are related concepts. Mechanism of action describes the chemical and molecular interactions that cause a drug’s therapeutic or toxic effects. Pharmacodynamics is “Effects of drugs on the bodyThis includes mechanism of action and how other factors, such as drug concentration, affect its efficacy.
In many cases, a drug’s mechanism of action is related to how it interacts with cellular receptors and enzymes involved in mediating specific signals and biochemical reactions in the body.
For Lipitor, the prescribing information tells us three important things about how the drug works. First, the liver is the main site of cholesterol production in the body and is the area targeted by the drug. HMG-CoA reductase.And third, the drug increases the number of LDL cholesterol receptors on the cell surface, ultimately catabolismor the metabolic breakdown of LDL cholesterol.
Where do drugs go in the body?
Before answering this question, let’s start with some background information in the “Pharmacokinetics” subsection.
pharmacokinetics iswhat the body does to drugsIt focuses on four major processes that the body undergoes in response to chemicals. distribution, or how the drug is distributed throughout the body; metabolism, or how the drug is transformed into other chemical forms. and excretion, or how the drug is removed from the body.
A drug’s pharmacokinetics are determined by factors related to the chemical itself and the person taking the drug. For example, the same drug may work differently in different people depending on their disease state, age, gender, and genetic makeup.
Now let’s take a look at the “Distribution” subsection.
In the case of Lipitor, the prescription does not specifically say where the drug will go in the body. Distribution volume 381 liters. The volume of distribution is the ratio of the total amount of drug in the body to the drug concentration in the blood.
Values ​​above about 30 liters indicate that the drug entered the body Not limited to blood flow.For reference, the medicine WarfarinIt prevents blood clots, binds tightly to proteins in the blood and has a volume of distribution of just 8 liters. chloroquinethe value of antimalarial drugs entering body fat is 15,000 liters.
Does the drug cause an effect or its by-products?
Although most drugs derive their therapeutic effect from the compounds that make them up, many are broken down into active metabolites in the body and also have associated biological effects.
Some drugs are Inactive forms called prodrugs conversion by the body into metabolites that have the desired therapeutic effect. Pharmaceutical companies generally use prodrugs because their pharmacokinetics are superior to the active form, including improved absorption and distribution in the body.
For Lipitor, the ‘Metabolism’ subsection under ‘Pharmacokinetics’ shows that the drug is broken down into several products and that these metabolites contribute significantly to its therapeutic effect.
How long does the drug stay in the body?
Important drug properties to consider in this case are: half lifewhich is the length of time required for the concentration of a drug to decrease to half of its initial amount in the body. Information on drug half-lives can be found in the Excretion subsection under Pharmacokinetics. .
The half-life of Lipitor is approximately 14 hours. When you stop taking the drug, 97% of the drug is cleared from the blood in about 3 days, or 5 half-lives.
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Since Lipitor’s active metabolite has a longer half-life than the drug itself, the cholesterol enzyme inhibitory effect has a half-life of 20-30 hours. This means that the effects of the drug can persist even after the drug itself has left the body.
Why should I take my medicine with meals or at certain times?
Eating food can alter the amount and rate at which drugs are absorbed into the body in several ways, including changing the acidity of the digestive system, altering the release of bile, and increasing blood flow to the intestines. .
Specifically for Lipitor, the answer to this question can be found in the Pharmacokinetics, Absorption subsection. Diet reduces the rate and extent of absorption of Lipitor, but does not significantly affect LDL cholesterol reduction.
Interestingly, this insert also notes that the blood levels of the drug were significantly lower when taken in the evening than in the morning, whereas the reduction in LDL cholesterol levels was observed irrespective of drug intake. Is the same.
All these conclusions are written on the drug label outside the package. Lipitor can be taken with or without food. There is no specified morning or evening, but it is recommended to take Lipitor at the same time each day.
Why is my doctor asking about other medicines I’m taking?
Drugs can interact in ways that affect their safety and efficacy. For example, two drugs may rely on the same enzymatic system in the body to break down.
Taking them at the same time may eventually result in higher than expected levels of either or both drugs in the body.
Information to answer this question can be found in the Drug Interactions section.
One of Lipitor’s drug categories of concern is “potent inhibitors of CYP 3A4,” an enzyme that plays a key role in the metabolism of many drugs. Because Lipitor itself is degraded by this enzyme, its use with drugs that block CYP 3A4, such as the antibiotic clarithromycin and the fungal infection drug itraconazole, can increase blood levels and cause side effects. I have.
Brad Reisfeld is Professor of Chemical and Bioengineering, Biomedical Engineering, and Public Health at Colorado State University. His research focuses on pharmacology and toxicology.
conversation is a non-profit independent news organization that publishes articles written by academic experts in partnership with universities.
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