[PHARM] Pharm approach to Pain [Iszard] Flashcards by A. Ozumba

Define:

Analgesics

Drugs that relieve pain without causing loss of consciousness

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What are examples of MSK indications for NSAIDs?

Osteoarthritis

Bursitis

Gout ‘flare’

Ankylosing spondylitis

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What are (2) other indications for NSAIDs?

Headache

Dysmenorrhea

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What are the (2) isoenzyme forms of COX?

Cyclooxygenase 1 (COX1)

Cyclooxygenase 2 (COX2)

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What are the similarities between COX1 and COX2?

Both…

Use same substrates
Make the same products
Role in inflammation
Physiological role in renal function

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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

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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

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All NSAIDs, but particularly COX2 selective agents should be avoided in patients with:

Cardiovascular risk factors

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What is the NSAID of choice to give a patient that needs NSAID thearpy but also has cardiovascular risk factors?

Naproxen

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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

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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

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How does aspirin prevent MI/stroke?

Inhibition of COX-1 in platelets

This suppresses platelet aggregation

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Aspirin causes ________ inhibition of cyclooxygenase

Aspirin causes irreversible inhibition of cyclooxygenase

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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

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By impairing renal function, aspirin can cause ______________, ___________

By impairing renal function, aspirin can cause Sodium and water retention, edema and hypertension

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What population should NOT take aspirin due to REYE SYNDROME risk?

Chilren w/ chicken pox or influenza

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What is the MOA of non-aspirin NSAIDs?

Same as aspirin:

Inhibit COX-1 and COX-2

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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

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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

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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