Pain Medications Flashcards
What do NSAIDs work on?
1) NSAIDs inhibit cycloxygenase enzyme
2) Results in the inhibition of prostaglandin synthesis
Define analgesic
Pain relief medication
Define Antipyretic
Anti-fever
Drug that is selective for COX-2 enzyme; no effect on bleeding time/platelets
Celecoxib (celebrex)
Drug that irreversibly inhibits COX enzyme
Aspirin
Where is Thromboxane A2 produced and what is its functions?
1) Platelets
2) Vasoconstrictor
3) Activator of platelet aggregation
How long does it take for platelet aggregation to recover in a patient who has taken aspirin?
1) Aspirin irreversibly inhibits COX enzyme resulting in decreased production of Thromboxane A2
2) 8-11 days
What prostaglandin is involved with sensitization of pain nerve endings, causes vasodilation, inhibits gastric acid secretion, and Promotes mucosal blood flow
Prostaglandin E2
When should NSAIDs and COX-2 inhibitors be used with caution?
Pt. has:
1) Reduced renal function
2) Heart failure
3) Liver dysfunction
4) Pt. on ACEi or diruetics
Why should NSAIDs and COX-2 inhibitors be used with caution in states of high levels of vasoconstrictors?
1) NSAIDs and COX-2 inhibit prostaglandin synthesis
2) Prostaglandins cause vasodilation of the afferent arteriole
What is contraindicated to children with chicken pox or influenza?
1) Salicylates
2) Can cause Reye’s syndrome
What prostaglandin keeps a patent ductus areteriosus open? What drug is used to close it? What is this drug also used for?
1) PGE2
2) Indomethacin
3) Suppression of uterine contraction
What are the two main contraindications for NSAIDs/aspirin?
1) Aspirin allergy
2) Third trimester of pregnancy
What are the uses for indomethacin?
1) Closure of a patent ductus arteriosus
2) Decrease uterine contractions
3) Can only be used episodically because stronger than aspirin
Most efficacious NSAID analgesic, weak anti-inflammatory effect; used for post op pain
Ketorolac
Non-narcotic analgesic and antipyretic with weak anti-inflammatory acitivty
Acetaminophen (tylenol)
What is used to treat an overdose of acetaminophen?
1) N-acetylcysteine
Drugs that bind to opioid receptors
Opioids
Natural products and derivatives obtained from the opium poppy
Opiates
What are the types of opioid receptors
1) Mu
2) Kappa
3) Delta
What opioid receptor binds to endorphins?
1) Mu
2) Stronger than enkephalin
What opioid receptor binds to enkephalins?
1) Mu
2) Delta
What opioid receptor binds to dynorphins?
1) Kappa
What are endorphins derived from?
POMC
What are enkephalins derived from?
1) POMC (met-enkephalin)
2) Preproenkephalin (6-met and 1-leu)
What are dynorphins derived from?
Prodynorphins
What are the classic effects of opioids? (6 total)
1) Analgesia
2) Euphoria
3) Miosis
4) Respiratory distress
5) Physiological dependence
6) Reduced GI motility
Why is Meperidine only used for short periods of time?
1) Because its metabolite causes seizures
What are the high efficacy mu opioids?
1) Morphine
2) Meperidine
3) Methadone
4) Fentanyl
5) Heroin
Opioid that has a long half life, blocks NMDA receptors and monoamine reuptake pumps, used in rehab for opioid abuse
Methadone
Most lipid soluble mu opioid; highest potency; effective with a transdermal patch
Fentanyl
What are the high efficacy kappa opioids?
1) Butorphanol
2) Nalbuphine
What are two of the main effects on the kappa opioid receptor?
1) Dysphoria
2) Psychotomimetic response
What drug is a kappa agonist and a Mu antagonist? Used post op for pt. with respiratory depression.
1) Nalbuphine
What are opioids with intermediate efficacy?
1) Hydrocodone
2) Oxycodone
3) Pentazocine
What is more efficacious with oral intake? Morphine or Oxycodone?
1) Oxycodone
2) Morphine has a low oral:parenteral potency
Characterized by signs and symptoms when drug use is stopped; not an addiction
Dependence
Using a drug for its euphoric effect, observed as escalation in drug dose unrelated to pain level
Abuse
Moderate Kappa agonist; partial Mu agonist/pure Mu antagonist
Pentazocine
Opioids with low efficacy
1) Buprenorphine
2) Codeine
Low efficacy opioid; long duration of action, slow to dissociate from Mu receptors; not readily reversed
Buprenorphine
Enzyme that is involved with converting codeine to morphine
1) CYP2D6
2) Responsible for demethylation
What is the MOA for Tramadol?
1) Weak Mu agonist
2) CNS serotonin releaser
3) Norepinephrine re-uptake inhibitor
What given with serotonin selective reuptake inhibitors can cause a serotonin syndrome?
1) Tramodol
How do weak partial agonists act when given with a full agonist?
Weak partial agonist become antagonists
What are three opioid antagonists?
1) Naloxone (injection only)
2) Naltrexone (oral only)
3) Nalmefene
What is the triad of primary findings observed in opioid overdose?
1) Lethargy/coma
2) Miosis
3) Depressed respiration
What is the drug of choice for opioid overdose?
Naloxone
What opioids are used for treatment of Diarrhea?
1) Ioperamide
2) Diphenoxylate
3) Difenoxin
What drug is used to treat the reactive (affective) portion of pain?
Amitriptyline
What are the adverse effects of salicylism?
1) Nausea
2) Vomiting
3) Tinnitus
4) Hyperventilation
