Pharmacology and The Opioid Crisis

Mini-Med Fall 2019

Basic Pharmacology

Name some common medicines found at home!

Here are a few, but there are many more!● Advil● Tylenol● Motrin● Aleve● Excedrin● Benadryl● Mucinex● NyQuil/DayQuil

● Visine● Pepto-Bismol● TUMS● Allegra● Flonase● Claritin● Sudafed● Robitussin

Naming of Drugs

It is important to understand the different namings of the same drug.

Generic Name

● The name of the active ingredient of the drug

● Has the same effect as the brand name (more on this next slide)

● A pharmacological drug only has one generic name!

Example: Ibuprofen

Brand Name

● A name given by the company that manufactures the drug

● Usually a name that is easy to use for sales and marketing

● There can be multiple brand names for the same drug!

Example: Advil, Motrin

The “Generic” and “Brand name” medications in stores do the same thing but for different prices!

Why? - During development a company will put a patent on a particular drug so other companies can not sell the same drug- Once that patent runs out, other companies will begin manufacturing the same drug but at a lower cost to compete- “In order for the FDA to approve a generic version of a brand, the FDA requires that generic medications have the same dosage form, safety, strength, route of administration, quality, performance characteristics and intended use as the brand-name drug.”

Advil - 100 tablets

$7.99 at Target

Active ingredient: Ibuprofen

Up & Up Ibuprofen - 100 tablets

$1.99 at Target

Active ingredient: Ibuprofen

http://info.iwpharmacy.com/generic-vs.-brand-whats-the-difference

There are situations where a physician will prescribe a specific Brand Name but that is beyond the scope of this lecture.

How Does it Work?Ibuprofen

Ibuprofen facts● Common brand names include Motrin and Advil

● Is classified as an NSAID (Non-steroidal anti-inflammatory drug)

● Used mostly for pain, fever, and inflammation

● Ibuprofen purchased over-the-counter (OTC) comes in tablets or capsules of 200 mg, while prescription doses are available in 400, 600, and 800 mg tablets.

Ibuprofen is a COX enzyme inhibitor● Ibuprofen is a non-selective inhibitor of the

cyclooxygenase (COX) enzymes○ It will inhibit both COX-1 and COX-2

● This enzyme converts arachidonic acid into prostaglandin

● Therefore, ibuprofen inhibits the production of prostaglandins

● Prostaglandins are promoters of inflammation, so when they are not produced, inflammation is reduced○ This leads to a decrease in symptoms

such as fever, swelling, and pain, which are results of inflammation

How Does it Work?Acetaminophen

Acetaminophen facts● A common brand name is Tylenol● Is considered an analgesic (pain reducer) and an antipyretic (fever reducer)● It is used to relieve aches, pains, and reduce fever

○ It is commonly used in the treatment of pain associated with arthritis● Proper dosing for acetaminophen often confuses people based on the

variety of different types of tablets

Acetaminophen DOES NOT reduce inflammation like ibuprofen● The exact mechanism is not known

● It is believed this drug works mostly on the central nervous system in the brain centers responsible for pain and fever

● Studies show acetaminophen indirectly inhibits the COX enzymes just like NSAIDs.○ However, since they only work

centrally, and not in the peripheral body, it does not have effects on inflammation

● The effect of acetaminophen on the heat centers of the brain are believed to cause the body to sweat and lose body heat which reduces fever

How Does it Work?Naproxen

Naproxen facts● The common brand name is Aleve

● Is classified as an NSAID (Non-steroidal anti-inflammatory drug)

● Naproxen is used as an analgesic (what does this mean?), antipyretic (and this?), and an anti-inflammatory○ It is commonly used in the management of rheumatoid arthritis

Ibuprofen is also an NSAID so what do you think the difference is?

The difference is how long they act on the body!Ibuprofen

● Short-acting NSAID

● Better suited for acute pain

● Most appropriate NSAID for children

● Higher doses are associated with increased cardiovascular risk

Naproxen

● Long-acting NSAID

● Better suited for chronic conditions

● Has a higher risk of causing GI side effects such as stomach ulcers

More on COX-1 and COX-2● Ibuprofen and Naproxen are both

“non-selective COX inhibitors” meaning they inhibit both COX-1 and COX-2

● COX-2 is responsible for producing the prostaglandins responsible for pain, fever, and inflammation, so it is the desired COX enzyme to inhibit

● COX-1 is located in tissue such as the lining of the stomach, so the inhibition of this COX can lead to stomach ulcers and other bad GI side effects

● Why not just use drugs that only inhibit COX-2 then?

- Several studies found COX-2 inhibitors (AKA Coxibs) had an extremely negative effect on cardiovascular health

- In fact, it was shown to almost DOUBLE a patient’s risk for a heart attack or stroke

- Celecoxib (Celebrex) is a COX-2 inhibitor used in practice today but under VERY STRICT conditions

The Opioid Crisis

Run time - 2:02

What is an opioid?● A class of drugs that interact with opioid receptors in the body and brain

○ These receptors control pain, reward, and addictive behaviors● These drugs are used as strong pain relievers

○ However, these drugs also produce a euphoria which can leadto abuse and dependence

● Heroin is an example of an opioid that is illegal● There are also several synthetic opioids that are used

in medicine legally○ Examples: Fentanyl, morphine, oxycodone, codeine

Why is it a crisis?● Opioids are a highly addictive substance

○ They work on the reward/pleasure centers of the brain○ They cause euphoria along with pain-relief

● This leads to patients misusing them, and eventually overdosing○ Overdosing on opioids causes a person to stop breathing (more on this next slide)

How does death by overdose occur?● The fundamental drive for

breathing is generated in the brainstem

● There are opioid receptors in the brainstem that can alter this respiratory drive

● This can lead to respiratory distress and eventual death since the person cannot breath

● Three common symptoms of an opioid overdose:○ Pinpoint pupils○ Unconsciousness○ Respiratory depression

In 2017...

So why are opioids still prescribed?● Opioids are some of the strongest pain relievers available

● There are conditions that cause patients A LOT of pain that can not be managed by medications such as ibuprofen, acetaminophen, or naproxen○ Post-surgical pain○ Pain from severe accidents○ Pain from a cancer○ Pain from a variety of chronic conditions such as lupus

● It is up to the physician to fully evaluate the patient and to responsibly choose when an opioid should be prescribed○ Whenever possible, opioids should be avoided

How Does it Work? Naloxone

Naloxone facts● Brand names include Narcan and Evzio

● Naloxone is an opioid antagonist

● It is used to to treat opioid overdoses in and out of the hospital

● It takes 2-5 minutes to begin working

● Naloxone can cause withdrawal symptoms so it should be used with caution

What is a drug antagonist?● A drug that binds to a receptor

in the body and blocks it, rather than activating it

● This dampens the biological response of certain chemicals that usually bind to that same receptor

● Naloxone antagonizes opioids by binding to opioid receptors and blocking them

Narcan in the world today● In recent years, laws have been

passed in several states that allow non-medical professionals to get access to Narcan

● Narcan can be obtained for free from certain organizations and participating pharmacies in New York and New Jersey

● It can also be purchased at most pharmacies or prescribed by medical professionals

● Training for Narcan use is also widely available

Run time - 2:31

Questions?