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PAIN MEDS

2 types of pain
o Nociceptive = normal processing
o Neuropathic = abnormal processing
Physiologic Effects = Inc catabolic demands, dec limb movement, respiratory effects,
tachycardia, and elev BP
Acute Pain Goal = pt comfort and min ADRs
Chronic Pain Goal= pt comfort (poss not pain free) and min ADRs + integrate normal life and
ADLs
Drug options = non-opiods (acetaminophen and NSAIDs), opiods ( agonists & mixed agonist-
antagonists), adjuvants (multipurpose & specific)

**Controlled Substance Schedules
I = cant prescribe, research only
II = more likely to abuse
III = safer, less likely to abuse
IV = as effective as acetaminophen
V = may help with cough

**Opiods (narcotics) = meperidine and morphine w/ active/toxic metabolites
No max dose
Acute and chronic pain
If morphine and derivative allergy (codeine) then use meperidine, fentanyl, or methadone
MOA = opium derived from poppies, relieves pain and induces euphoria by binding to opiod
receptors (mu, delta, kappa), mimics actions of endogenous opiod compounds (enkephalins,
dynorphins, endorphins)

1.) Morphine = MS Contin, MSIR (immediate rel), Avinza, Kadian (long-acting)
Severe pain, use IR to establish dose needed then switch to CR formulations
Avinza and Kadian 24 hr SR fewer fluctuations and less freq dosing
Altering drug deliver sys daily drug supply rel immed = pot OD and death
SR should not be crushed/chewed
Active metabolites may accumulate in renal dysfunction

2.) Hydromorphone (Dilaudid)
Mod-severe pain
? < sedating than morphine

3.) Oxycodone Products
? > addictive than heroin
1.) OxyCONtin
Tampering for IV abuse = gel-coded so cant draw into syringe, now you cant crumble it
Test ?: NOT for acute pain mgmt
2.) OxyIR and Roxicodone = only readily available oxycodone only immed-rel products
3.) With APAP:
a. Percocet = oxycodone + APAP, beware of combos w/ acetaminophen
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b. Roxicet (soln, +APAP)
c. Percodan (+ ASA)
4.) Fentanyl very short acting
Fentanyl Patch (Duragesic) = mcg dosage, us change q3 days, crappy adhesive
a. Pt may want brand-name only
b. Well absorbed topically (avoid sun exposure, heat)
c. 6-12 hrs until significant systemic levels, 14+ before plateau
d. Blackbox for acute pain
e. Test ?: Never use in an opiod-nave pt
Fentanyl lozenge on a stick (ACTIQ)
f. Breakthru pain or if have trouble swallowing
g. NOT for opiod-nave!
h. Good in hospice ppl who have trouble swallowing
5.) Codeine - weak
a. + APAP/aspirin = III
b. + expectorant = V
6.) Hydrocodone + APAP (Norco, Vicodin, Lortab), Hydrocodone + IBU (Vicoprofen)
a. If pt was on oxycodone + APAP, this will be inadequate pain control

**APAP and opiod analgesic combos
Synergistic pain control
1.) Meperidine
a. Euphoric, stimulates drug seeking
b. No longer pref for acute or chronic pain
c. M for metabolites CNS stimulant, seizures, visual disturbances, twitching, anxiety
d. May only be appropriate in morphine allergic pt
2.) Methadone
a. Biphasic alpha (analgesic) and beta phase (prev withdrawal, pain control)
b. For mgmt opiod abuse and chr pain
c. Equianalgesic dose of methadone will dec progressively as morphine equivalents inc

***Other Opiod Agonists***
1.) Tramadol (Ultram) and Tramadol + APAP (Ultracet)
o Dual action = mu receptors & inhibits neuronal uptake of serotonin and norepinephrine
o PO mod pain, also used for chronic pain
o Lowers seizure threshold, inc serotonin levels (2 ss)
o Not controlled
o Test ?: DOES NOT tx 7-10
2.) Tapentadol

**Opioid Equivalency
Morphine IV 3x > morphine PO. So 10 mg IV = 30 mg PO
Oxycodone PO 1.5x > morphine PO. So 20 mg oxy = 30 mg morphine
o Example ?: 60 mg morphine PO = 40 mg oxycodone PO
Hydrocodone 1.5x > morphine PO. So 20-30 mg = 30 mg morphine
Methadone PO 3-5mg = 30 mg morphine PO. Higher doses of morphine means less linear
transition of methadone to morphine
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Hydromorphone PO 7-7.5 mg = 30 mg morphine PO
Fentanyl is super strong. If on high-dose 50 mg morphine PO then can switch to lowest dose
fentanyl

**Pain Scales
Numerical: 0 10
o Mild 1-3: APAP, Ibuprofen
o Moderate 4-6: APAP/codeine, APAP/oxycodone, tramadol
o Severe 7-10: morphine, hydromorphone, morphine controlled release
o Example ?: Tramadol least effective for which type of pain? Severe. It is best for a 3 or 4
(mild or mod)
Faces: children and elderly
Colors: blue/white red (10)

**Considerations of Dosing Formulations
Long vs. short-acting: basal rate w/ breakthru = CR (or long-acting) + something for breakthru
pain
Approx 10% of daily-dose long-acting is given as breakthru
Example: 60 mg oxycontin BID so 120 mg total, look for 6-9 mg oxycodone for breakthru pain,
could do 1-2 5 mg tablets or 2 mg hydromorphone tablets

***Pt Controlled Analgesia = PCA
IV or SC cont infusion narc w/ breakthru doses pt can control
Locked button that delivers dose
For acute pain
May use less total narc than traditional PRN dosing (morphine, fentanyl, hydromorphone)

**Opioid Effects/ADRs
Constipation (give stool softener + stimulant combo live docusate + senna)
Pruritis - . IV more likely to cause
N/V triggers CTZ
Sedation
Respiratory depression deadly
Inhibition of cough reflex
Confusion
Dysphoria/euphoria
Hallucinations
Prolongation of labor
Urinary retention
miosis

**Opioid Drug Interactions
Other CNS depressants
Methadone has CYP450 3A4 drug interactions
ETOH + opiod = respiratory depression


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**Withdrawal from Opioids
Time of onset, intensity, and duration of abstinence sx depends on drug prev used (t1/2)
Muscular aches and yawning
Administration of opiod at time of withdrawal sx = suppression of abstinence s/sx almost
immediately

**Opioid Antagonists = naloxone and naltrexone
Quickly reverses fx morphine and other opioid agonists, tx opioid overdose
Antagonist-precipitated withdrawal w/in 3 min after injection withdrawal sx appears, peaks
10-20 mins, subsides 1 hr
ADRs = insomnia, HA, nervous, low energy

**Mixed Opioid Agonist-Antagonist = buprenorphine, butorphanol, nalbuphine, pentazocine
Partial agonist or antagonist activity at mu receptors, agonist or antagonist activity at kappa
receptors
Buprenorphine/Naloxone (Suboxone) = Tx opioid abuse .. But can eventually abuse this too!
ADRs: less respiratory depression and abuse potential?
Precipitiate withdrawal in an opioid-dependent pt

**Adjuvant Analgesics and Co-Analgesics
Enhance analgesic efficacy, work on specific pain types, relieve concurrent sx that exacerbate
pain
NSAIDs, antidep/convulsants, corticosteroids, benzos, muscle relaxers

**Dependence (formerly physical dep) = Occurs in all pts on chronic opioids
**True addiction (formerly psychological dep) = Compulsive use despite harm
**Pseudoaddiction = end result of under-tx pain, drug-seeking behavior (demanding doses before
scheduled time, hoarding), go to 1+ pharmacy/Dr., cured by inc daily dose and monitoring pt
**Tolerance = escalation of dose to maintain effect (analgesia or euphoria may be life threatening bc
res dep doesnt show much tolerance)
**If opioid intolerance, use meperidine, methadone, or morphine

WOMENS HEALTH

**Other Hormonal Contraceptives
1) Depo-provera
o progesterone-only IM q3 mos
o most common and widely used
o weight gain after 5 yrs of chronic use (gain 3-5 lbs/yr)
2) Implanon
o implantable subdermal rod, up to 3 yrs
o progestin only
o ? Efficacy in morbid obesity
3) NuvaRing
o in for 3 wks, out for 1
o can be stacked
4) Mirena
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o umbrella-like IUS
o very effective
5) ParaGard IUD (Copper-T)
o IUD up to 10 yrs
o non-hormonal
o Issue for Mirena and ParaGard is nonparity bc more likely to have chronic pain from
products
6) Ortho Evra
o transdermal patch q1 wk x 3 wks, week 4 is patch free
o Issues: overweight, thromboembolism, lousy adhesive in some (us bc lotion)

**Menopause
Intact uterus must get most estrogen and progesterone [unopposed estrogen can lead to
endometrial CA]
Good candidates = osteoporosis [worry about cardiac issues]

**Major sx of estrogen withdrawal
2 most common sx = vasomotor instability (hot flushes, sweating) and vaginal atrophy
(discomfort)
Other sx are loss of concentration and libido, wt gain, depression, thinning hair, joint discomfort,
disrupted sleep

**HRT = CV risk!!!
**Soy products = phytoestrogens. Can eat enough to be in HRT state. Bad bc high pesticides

OSTEOPOROSIS

**Institute of Medicine
F 50-70: 1200 mg Ca, 600 IU Vit D, 800-1000 IU Vit D rec daily intake (National Osteoporosis
Foundation)
F > 70: 1200 mg Ca, 800 IU Vit D
M 50-70: 1000 mg Ca, 600 IU Vit D (note diff here)
M > 70: 1200 mg Ca, 800 IU Vit D

**Commonly Used Ca Salts
Take sm amts throughout days, NOT with high fiber meals, consider TUMS
Recommended 3-5 tablets/day
1.) Calcium Carbonate (40% elemental Ca) Tums, Caltrate, Oscal
Needs acid to absorb (take w/ food)
Not good for ppl on PPIs (or those who take antacids regularly) and elderly (lack of acid)
#1 complaint is gas and bloating in F
2.) Calcium Citrate (21%) Citracal
Does NOT need acid to absorb

**Vit D deficiency tx = 50,000 IU PO 1x/wk x 6-8 wks, re-level in 8 wks, weight-bearing exercise (walking,
weight training)

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**Drug Therapy: 2 Major Categories
1.) Antiresorptive Meds (bisphosphonates, calcitonin, estrogen, and SERMs) slow bone loss
2.) Anabolic Drugs (teriparatide/Forteo) only one that inc rate of bone formation

**HRT - premarin, estrace, prempro, femhrt
For post-menopausal F, works too just not used. Inhibit bone resorption

**SERMS Raloxifene (Evista)
Prevention and tx osteoporosis in postmenopausal women only, also for breast CA
Benefits of estrogen w/o ADRs
MOA estrogen agonist in bone, none in breast and uterus, anti-resorptive
Other: reduces risk breast CA by 65% over 8 yrs

**Bisphosphonates
Prev and tx in post-menopausal women and in M, steroid-induced in both (Fosamax)
MOA inhibit osteoclast activity and dec bone resorption. Dec bone loss and risk fx, inc bone
density, anti-resorptive
Oral:
o 1.) Alendronate (Fosamax) prev is tx
o 2.) Ibandronate (Boniva)
o 3.) Risedronate (Actonel)
o 4.) Risedronate (Atelvia) H sensitive coating so can travel thru stomach and rel in sm
intestine, has EDTA to pick-up stray cations, can be taken after breakfast instead of 30
min before, Needleless injection
Parenteral:
o 1.) Ibandronate (Boniva)
o 2.) Zoledronic Acid (Reclast)
Side Fx: GI upset in PO agents (N, diff swallow, heartburn, irritate esophagus, gastric ulcer,
esophageal CA)
ALL FORMS: musculoskeletal pain, uveitis, femur fx
ONJ: bisphosphonates inhibit bone turnover to heal these injuries, some ppl more at risk
(improper fitting dentures can form ulcers), use chlorhexidine gluconate rinse (Peridex) qd and
before dental sx to help
Contraindications: hypocalcemia, hx esophageal dis, gastritis, PUD, renal impairment (SCr > 2.5
mg/dl), inability to sit/stand uprt for > 30 min
Other Considerations: take first thing in the morning with 8 oz H2O, sit/stand 30 min, do not
eat/drink anything else for 30 min, do not take in a fasting state (inc risk ab pain and GI issues)
Clinical Pearls: take for 5 yrs and d/c. Then check DEXA scan in 2 yrs (if stable then d/c 1-2 more
yrs and recheck DEXA)

**Calcitonin - Calcimar SC/IM, Miacalcin intranasally
Tx osteoporosis in postmenopausal F who are at least 5 yrs beyond menopause
Nat occuring hormone for Ca regulation and bone metabolism = slow bone loss, inc bone
density in spine and red risk spine fx, least effective of all
Target: post-menopausal F, M, bone pain
Contraindications: hypersensitivity to salmon protein
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Side Fx: N, H/A, nasal dryness, nasal and skin irritation, allergy, flushing of face and hands,
urinary freq, N, bloody nose

**Miscellaneous
1.) Denosumab (Prolia) psotmenopausal F at hi risk for rx or those who failed/intolerant to
other meds like bisphosphonates
MOA: human IgG2 monoclonal ab which inhibits RANKL (cytokine member of TNF family)
Dose SQ 2x/yr

**Bone Forming (Anabolic) Meds
1.) Teriparatide (Forteo)
Parathyroid hormone, take max 2 yrs
Postmenopausal F and men hi risk fx
Rebuilds bone (only one!) and sig inc bone mineral density (esp spine)
ADRs leg cramps and dizziness