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Chapter 5
Drugs for Pain Control
74
Pharmacology
Professional
02/17/2013

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Term
What is pain?
Definition
a sensation that may indicate pathology
Term
Where is the pain stimulus from?
Definition
the peripheral nervous system
Term
What is pain interpreted by?
Definition
the central nervous system
Term
Is all pain the same?
Definition
no, it may be perceived differently, there are different treatment options for individualized pain relief
Term
What pain is considered a standard that allows for comparison for clinical studies?
Definition
dental pain from a tooth extraction
Term
What are the two types of orofacial pain?
Definition
neuropathic and nociceptive
Term
What type of pain is neuropathic? What does it cause?
Definition
-chronic pain
-causes damage to the nerve tissue(in or out of CNS)
Term
Does neuropathic pain occur in or outside of the CNS?
Definition
can occur in both inside or outside of the CNS
Term
What are some causes of neuropathic pain?
Definition
-diabetic peripheral neuropathy
-trigiminal neuralgia
Term
What types of medications is neuropathic pain treated with?
Definition
-analgesics
-antidepressants
-anticonvulsants
Term
Where do analgesics work? Can they effectively cross the blood brain barrier?
Definition
Work effectively in the PNS, can't effectively cross the blood brain barrier
Term
What is a nocioreceptor?
Definition
sensory receptor for painful stimulus found in the peripheral nervous system
Term
What type of pain is nociceptive? What is it caused from?
Definition
-acute pain
-caused from injury or stimulus
Term
What are some causes of nociceptive pain?
Definition
toothache, surgery, lesions
Term
What is nociceptive pain treated with?
Definition
-NSAIDs
-acetaminophen
-narcotics(opioids)
Term
What are some big differences between opioids and nonopioids?
Definition
-Different sites of action
-Different mechanisms of action
Term
What are the sites of action for opioids? Nonopioids?
Definition
Opioids- within CNS
Nonopioids- within PNS
Term
What are the mechanisms of action for opioids? Nonopioids?
Definition
Opioids- depresses the CNS
Nonopioids- inhibits prostaglandin synthesis
Term
What can nonopioids be divided into?
Definition
-salicylates
-acetaminophen
-NSAIDs
Term
What does NSAIDs stand for?
Definition
non-steroidal anti-inflammatory drugs
Term
What is prostaglandin synthesis?
Definition
phospholipids converted to arachidonic acid by phospholipase A
Term
What is prostaglandin synthesis inhibited by?
Definition
corticosteroids
Term
What do corticosteroids treat?
Definition
chronic inflammation(asthma, arthritis
Term
What are two common corticosteroids?
Definition
-Prednisone
-Dexamethasone
Term
What happens in prostaglandin synthesis after arachidonic acid is made?
Definition
converted by cyclooxygenase enzymes to prostglandins
Term
What is the abbreviation for cyclooxygenase enzymes?
Definition
COX
Term
What does COX-1 produce?
Definition
prostaglandins that assist platelets, kidneys, and GI tract
Term
What is COX-3?
Definition
A variant of COX-1
Term
What does COX-2 do?
Definition
produces prostaglandins that cause pain, fever, and inflammation
Term
What is COX-2 produced in response to?
Definition
injury or other stimulus
Term
What are salicylates?
Definition
aspirin
Term
What is another nae for aspirin?
Definition
acetylsalicylic acid(ASA)
Term
What type of receptor is aspirin?
Definition
noncompetitive enzyme inhibitors
Term
What is the mechanism of aspirin? What is the administration of aspirin?
Definition
Mechanism-irreversibly inhibits COX enzymes(binds to and blocks COX 1,2,3 enzymes)
Administration-predominantly oral
Term
How quickly is aspirin absorbed? When are the peak effects seen?
Definition
Absorption- 30 mins after ingestion
**Peak effects seen 2 hours**
Term
What are the pharmacologic effects of salicylates?
Definition
relieves pain, fever, inflammation, reduced clotting
Term
What are the adverse reactions of salicylates? Why do these occur?
Definition
-GI tract distress
-bleeding problems
-Reye's Syndrome
-hepatic and renal effects
-teratogenicity
-allergies
*Occur because these are related to COX 1 enzyme and aspirin blocks this enzyme*
Term
Does GI tract distress indicate an allergy to salicylates?
Definition
no, it is a normal side effect
Term
What is Reye's syndrome? Who should not take aspirin?
Definition
kids under age 6 should not take it due to possible development of Reye's syndrome which is buildup of fluid in the skull related to a virus
Term
Can Reye's syndrome be fatal?
Definition
yes
Term
What can frequent use of aspirin in pregnant people result in?
Definition
can result in still borns, shows teratogenic effects
Term
What are the symptoms of toxicity of aspirin? What causes it?
Definition
-due to overdose
-headache
-dizziness
-nausea
-vision problems
Term
What can the breakdown of liver cause?
Definition
liver toxicity
Term
What happens when aspirin is taken with warfarin?
Definition
increases bleeding
Term
What happen when aspirin is taken with alcohol?
Definition
hepatic toxicity
Term
What happens when aspirin is taken with probcecid(treats gout)?
Definition
a decrease in aspirin excretion
Term
What happens when aspirin is taken with methotrexate (taken with cancer and autoimmune diseases)?
Definition
increased bleeding, and aspirin decreases methotrexate excretion
Term
What happens when aspirin is taken with sulfonylureas(taken for diabetes) ?
Definition
decreased sulfonylrea excretion
Term
What happens when aspirin is taken with antihypertensives?
Definition
the aspirin decreases the antihypertensive effectiveness
Term
Why do a majority of these drug to drug interactions occur with aspirin?
Definition
because of an increased risk of bleeding
Term
What is another name for acetaminophen?
Definition
paracetamol
Term
What is the mechanism of acetaminophen? Administration?
Definition
Mechanism- competitive inhibitor of COX enzymes
Administration- predominately oral
Term
When does absorption of acetaminophen occur? What are the pharmacologic effects?
Definition
Absorption- peak effects at 30-60 mins
Pharmacologic effects- relieves pain and fever
Term
Does acetaminophen relieve inflammation?
Definition
NO
Term
What are the adverse reactions of acetaminophen?
Definition
hepatic and renal toxicity, methemoglobinemia
Term
What is methemoglobinemia? What is a sign of this?
Definition
hemoglobin that cannot bind to oxygen, cynanosis around lips is a sign of this
Term
When does toxicity occur? What are signs of this?
Definition
-occurs after overdose
-nausea, vomiting, anorexia, renal necrosis(kills kidney)
Term
What are the drug interactions of acetaminophen?
Definition
other than alcohol, essentially none, but some may exacerbate hepatic toxicity
Term
What does alcohol do when taken with acetaminophen?
Definition
forces/induces acetaminophen to use Phase I metabolism, cytochrome P450 enzyme metabolite produced is toxic to the liver
Term
What type of receptor is acetaminophen? Is it reversible? What type of metabolism does it generally go through?
Definition
competitive inhibition, reversible, generally goes through phase II metabolism
Term
What is the mechanism of NSAIDS?
Definition
reversibly inhibits COX-1/3 and COX-2 enzymes
Term
How are NSAIDs administered?
Definition
predominately orally
Term
When does absorption of NSAIDs occur? What does it depend on?
Definition
absorption occurs 1-2 hours after ingestion, depends on food
Term
Are NSAIDs competitive? Reversible?
Definition
they are competitive and reversible
Term
Are NSAIDs better absorbed in a full or empty stomach? Why?
Definition
better absorbed on an empty stomach because they are weak acids
Term
What are the pharmacologic effects of NSAIDs?
Definition
-relieves pain
-fever
-inflammation
-reduced clotting
Term
How are NSAIDs compared to acteaminophen? Aspirin?
Definition
does more then acetaminophen, works as well as aspirin but it is not as harsh
Term
What are some adverse reactions of NSAIDs?
Definition
-ulceration
-CNS depression
-sedation
-convulsions
-renal effects in people with renal disorders
-oral effects
-allergy
Term
If you are allergic to aspirin should you take NSAIDs?
Definition
no, if you are allergic to aspirin you are likely allergic to NSAIDs
Term
What is the toxicity of NSAIDs?
Definition
similar to those with salicylates (aspirin)
Term
What happens when NSAIDs are taken with lithium?
Definition
decreased lithium excretion
Term
What happens when NSAIDs are taken with digoxin(treats cardiovascular conditions)?
Definition
it increases digoxin effects
Term
What happens when NSAIDs are treated with antihypertensive medications?
Definition
opposes antihypertensive effects
Term
What happens when NSAIDs are taken with methotrexate?
Definition
increased bleeding, decreased mehotrexate excretion
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