[PHARM] Pharm approach to Pain [Iszard] Flashcards
Define:
Analgesics
Drugs that relieve pain without causing loss of consciousness
What are examples of MSK indications for NSAIDs?
Osteoarthritis
Bursitis
Gout ‘flare’
Ankylosing spondylitis
What are (2) other indications for NSAIDs?
Headache
Dysmenorrhea
What are the (2) isoenzyme forms of COX?
Cyclooxygenase 1 (COX1)
Cyclooxygenase 2 (COX2)
What are the similarities between COX1 and COX2?
Both…
- Use same substrates
- Make the same products
- Role in inflammation
- Physiological role in renal function
What are the features of COX1 that make it distinct?
Its expressed in all tissues all the time [constituitive]
Prominant role in responding to physiological stimuli
ALSO contributes to a response in any pathological stimuli that release AA from cells
What are the features of COX2 that make it distinct?
Induced in SOME tissues SOMEtimes
Physiological role in kidney, complements COX1
Prominant role in response to any pathological stimuli that release AA from cells
All NSAIDs, but particularly COX2 selective agents should be avoided in patients with:
Cardiovascular risk factors
What is the NSAID of choice to give a patient that needs NSAID thearpy but also has cardiovascular risk factors?
Naproxen
In addition to cardiovascular risk, what ar the other contraindications for NSAID use?
Chronic kidney disease
Active duodenal or gastric ulcer
NSAID allergy
Warfarin use
What are the beneficial actions of NSAIDs (Aspirin)?
Supression of inflammation
Relief of mild to moderate pain
Reduction of fever
Prevention of MI and stroke
How does aspirin prevent MI/stroke?
Inhibition of COX-1 in platelets
This suppresses platelet aggregation
Aspirin causes ________ inhibition of cyclooxygenase
Aspirin causes irreversible inhibition of cyclooxygenase
Because of it’s anti-platelet effects, aspirin can ____________ in patients taking warfarin, heparin and other anticoagulants
Because of it’s anti-platelet effects, aspirin can INCREASE THE RISK OF BLEEDING in patients taking warfarin, heparin and other anticoagulants
By impairing renal function, aspirin can cause ______________, ___________
By impairing renal function, aspirin can cause Sodium and water retention, edema and hypertension
What population should NOT take aspirin due to REYE SYNDROME risk?
Chilren w/ chicken pox or influenza
What is the MOA of non-aspirin NSAIDs?
Same as aspirin:
Inhibit COX-1 and COX-2
What are the major differences of non-aspirin NSADIS from aspirin?
- They are REVERSIBLE
- Suppress platelet aggregation but actually INCREASE RISK OF MI and STROKE
Ketorolac
Indications:
Warnings:
Risks:
Indications: Short term management of moderately severe acute pain, usually postoperative
Warnings: Peptic ulcers, GI bleeding
Risks: Bleeding, CV thrombotic events, Renal risk
Indomethacin
MOA:
Indications:
Warnings:
Contraindicated:
MOA: NSAID
Indications: RA, Ankylosing spondylitis, Osteoarthritis, Bursitis, Gouty arthritis
Warnings: C/V and GI risks
Contraindicated: Peri-operative pain in setting of coronary artery bypass graft (CABG) surgery
Ibuprofen
Indications:
Contraindications:
Warnings/precautions:
Adverse effects:
Indications: Fast effective relief of (millions of things); HA, menstrual pain, dental pain, minor aches and pains in muscles, reduction of fever
Contraindications: Active gastric or duodenal ulcer
Warnings/precautions: Pts with heart dz or HTN
Adverse effects: Decreased appetite, edema, fluid retention
Flurbiprofen
Indications:
Contraindications:
Indications: Opthalmic use; indicated for inhibition of intraoperative miosis
Contraindications: Pts who are hypersentitive to any components of the med; including ibuprofen
Naproxen
Contraindications:
Warnings/precautions:
Contraindications: Hx. of asthma, uticaria or other allergic type reactions after taking aspirin or other NSAIDs
Warnings/precautions: Hepatotoxicity, Thrombotic effects (BBW)
Diclofenac
Warnings/precautions?
Increased risk of serious cardiovascular thrombotic events;
Including MI and Stroke
BBW
Coxibs
Class:
Benefit:
Risk:
Class: 2nd gen NSAID
Benefit: May cause less gastric ulceration than non selective inhibitors
Risk: Increases risk of MI and stroke
Acetaminophen
Suppresses?
DOES NOT SUPPRESS?
Suppresses = Pain and fever
DOES NOT SUPPRESS = Inflammation
Acetaminophen
MOA
Benefits?
Inhibition of prostaglandin synthesis in the CNS, but not in the periphery
As a result:
- Does NOT cause GI ulceration
- Does NOT suppress platelet aggregation
- Does NOT impair renal function
What is the major risk in taking acetaminophen?
Hepatic necrosis
What is acetaminophen overdose treated with?
Acetylcysteine
What is a class of drugs used for patients that have depression and pain symptoms?
Tricyclic antidepressants (TCAs)
Duloxetine
MOA:
Indications:
Contraindications:
Warnings:
MOA: SNRI
Indications: Chronic MSK pain, fibromyalgia, diabetic neuropathic pain, GAD, MDD
Contraindications: MAO inhibitor use
Warnings: Suicidality, Hepatotoxicity
Pregabalin
Indications:
Func fact?
Indications : Neuropathic pain w/ diabetic neuropathy, postherpetic neuralgia, adjunctive therapy for partial seizures, fibromyalgia
Func fact : First drug approved for fibromyalgia
Gabapentin
MOA?
Indications?
Caution?
MOA : Anticonvulsant
Indications : Post-herpetic neuralgia, Diabetic neuropathy, prophylaxis for migraine, treatment of fibromyalgia, restless legs syndrome
Caution : Can intensify depressant effects
Tramadol
MOA:
Indications:
Side effects:
MOA: Codeine analog, weak mu agonist, block NE and 5-HT reuptake
Indications: Moderate to moderately severe pain, more effective than codeine, less effective than morphine
Side effects: Rare, seizures in epileptics, precipitate HTN crisis, Serotonin syndrome w/ SSRI, TCA etc
Tapentadol
Who is this drug reserved for?
Patients who are not effectively treated with other non-opioids and opioids
Ketamine
MOA:
Indications:
Side effects:
Tendencies:
MOA: NDMA antagonist
Indications: Starting and maintaining anesthesia, post-operative pain
Side effects: Psychological reactions
Tendencies: Elevate blood pressure
Dexmedetomidine
MOA:
Indications:
MOA: Alpha2 adrenergic agnoist
Indications: Analgesia and sedation
Clonidine
MOA:
Indications:
Route:
Side effects:
MOA: Alpha2 adrenergic agonist
Indications: HTN, Relief of severe pain, SEVERE CANCER PAIN
TEST Q***Route: Continuous infusion through epidural catheter***
Side effects: Enhances hypotensive and depressive effects of other drugs
Ziconotide
MOA:
Indications:
Adverse effects:
MOA: Prevents transmission of pain signals from periphery to brain; Antagonist of N-type voltage sensitive calcium channels
Indications: ***ONLY for chronic severe pain in those whom INTRATHECAL ADMIN is warrented and refractory to other treatments
Adverse effects: CNS effects w/ cognitive impairment
What are the topical anti-pain agents?
Capsaicin
Camphor
Menthol
Topical NSAIDs
Topical Na+ channel blocker
Pentazocine
Indications:
Precautions:
Reversed by?
Indications: Agonist-antagonist opioid used to treat mild to moderate pain
Precautions: Unpleasant reactions (nightmares), respiratory depression
Reversed by: Naloxone
Butorphanol
Indications:
Reversed by?
Contraindications:
Indications: mild to moderate pain
Reversed by: Naloxone
Contraindications: MI
Buprenorphine
Indications:
Side effects:
Indications: Treat addicts, mild to moderate pain
Side effects: Respiratory depression
What are the (3) Anti-migraine agents?
Ergotamine
Dihydroergotamine
Sumatriptan
What is the drug of choice for terminating an ongoing migraine attack?
Ergotamine
What are the adverse effects of ergotamine?
N/V, weakness in legs, myalgia, numbness and tingling of fingers
What is a benefit of using dihydroergotamine over ergotamine?
Does NOT cause N/V, has NO physical dependence and MINIMAL peripheral vasoconstriction
What is the 5-HT agonist used for terminating migraine attacks?
Triptans
