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Pharm Exam # 2
Pain,Heart,GI
38
Other
Undergraduate 2
03/19/2007

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Term
COX Inhibitors
Definition
Acetaminophen (Tylenol)
-Analgesic & antipyretic properties
-Not anti-inflammatory
MOA: inhibits PG synthesis in CNS to block pain impulse
**DOC for osteoarthritis
Preferred agent for fever, pain in ped pt's w/influenza or chicken pox
INTERACTIONS
-Alcohol, Warfarin
Term
Salicylates
Definition
Aspirin (ASA)
-anti-inflammatory, antipyretic, and analgesic properties
MOA: irreversible inhibition of COX
Adverse reactions:
-GI events are the most common (gastric distress, heartburn, nausea)
Reye's Syndrome
-Not to be used in pregnancy
Interactions: Anticoagulants, glucocorticoids, alcohol, NSAIDS
Term
Non-acetylated salicylates
Definition
Salsalate (Disalcid, Amigestic)
Choline Magnesium Trisalicylate (Trilisate
Advantages over ASA:
-Less platelet inhibition: less bleeding
-Less GI irritation
-Less hypersensitivity
but less anti-inflammatory action
Term
Non-steroidal anti-inflammatory agents
NSAIDS
Definition
Ibuprofen, ketorolac, indomethacin, naproxen, nambumetone
-MOA: reversable inhibition of COX, decreased PG syn, trans effect platelets
-Cost more than ASA, CV events (naproxen, COX-2 inhibitors)
A.R- GI: N/V, ulceration, bleeding
Risk factors: age, hx, female, high dose
Interactions: AntiHPT meds
Contraindictions: heart failure, kidney disease, hx of ulcer, pregnancy Cat. D in 3rd trimester
Monitor: s/s of bleeding, blood counts (platelets, hemoglobin), renal func,pain
Term
Pure Agonists (Opioid Analgesics)
Definition
Morphine, oxycodone, codeine, fentanyl, methadone
-activate u & k receptors
-strong/ moderately strong
-typically high potential for abuse
Term
Partial Agonists (Opioid)
Definition
Buprenorphine, pentazocine
-partial agonist or antagonist at u & k
-generally produce analgesia as mono-tx
-can decrease analgesic effect of the pure opioid when admin. together
-generally low abuse potential
Term
Combination Products
Definition
Codeine + acetaminophen (cough/cold)
Hydrocodone + acetam. or ibuprofen
Oxycodone + acetam or ASA
Propoxyphene + acetam.
-Antagonists: reverse A.R, toxicity
-Agonists- pain, diarrhea, cough
Term
Adverse Reactions of Opioids
Definition
-Respiratory Depression
-**Constipation: all pt's should be on a laxative and stimulant bowel regimen w/ chronic use
-Orthostatic hypotension
-Urinary retention, emesis, cough supress, elevation of intercranial pressure, euphoria/disphoria, sedation and miosis.
Term
Other centrally acting analgesics
Definition
Tramadol (Ultram)
Tricyclic antidepressants (amitriptyline)
Anticonvulsants (carbamezapine/ gabapentin)
Term
Goals for Rheumatoid Arthritis Tx
Definition
-Relieve sx
-maintain/improve joint function
-delay disease progression
Term
RA- NSAID effects
Definition
-Rapid relief of pain
-Do not slow or delay disease progression
Term
RA- Disease Modifying Antirheumatic Agents
effects (DMARDS)
Definition
-Decrease joint destruction
-Slow disease progression
-Longer onset of therapeutic effect
Term
RA- Glucocorticoids effects
Definition
-Provide rapid relief of pain
-Can slow disease progression
-Generally try not to use long term due to adverse effects
Term
Drug Selection for RA
Definition
-Start with NSAID
-Add a DMARD if sx aren't controlled
-Add glucocorticoids for flare ups when DMARDS are used
Term
Glucocorticoids
Definition
Cortisone, hydrocortisone, prednisone, methylprednisone, triamcinolone, betamethasone, dexamethasone
-Anti-inflammatory & immunosuppressive properties when used in high doses
MOA: inhibit syn of PG's, suppression of immune func (neutrophils, macrophages, lymphocytes), effects on adrenal cortex
-Oral for systemic sx
-Intra-articular injections for a few joints that are affected
-Intermediate acting (prednisone & prednisolone) are most common
Long-term adverse effects: hyperglycemia, wt. gain, osteoporosis, adrenal insufficiency, HPT
Other uses: SLE, IBS, allergies, asthma, neoplasms, transplant, RDS, inflam cond
Term
DMARDS- non-biological agents (1st two)

**see chart (table 4)
Definition
1st- methotrexate (rheumatrex): most rapid acting, effects in 3-6 weeks, cont. in pregnancy
A.E-hepatic fibrosis, bone marrow sup, nephrotoxicity
2nd- Cyclosporine: reserved for severe sx, used in combo with methotrexate.
Term
DMARDS- non-biological agents cont.
**see chart (table 4)
Definition
Hydroxychloroquine (Plaquenil): good for mild sx, delayed onset of action (3-6 mo
-retinal damage, nausea, diarrhea, blood dyscrasia

Sulfasalazine (Azulfidine): mild-moderate disease, can delay progression & onset
-derm reactions, orange stool or urine, hepatotoxicity, bone marrow sup.
Term
DMARDS- Biological Agents
Definition
Entanercept (Enbrel): TNF blocker, effects in ~ 2 wks, very expensive; increased risk of infection, injection site reactions

Infliximab: TNF blocker, avoid use in pt's w/ HF, very expensive; infusion reactions, headache, increased infection risk, worsening of HF
Term
DMARDS- Biological Agents
Definition
Adalimumab (Humira): TNF blocker, reduces sx & decreases disease progression, combo or monotherapy, expensive; immunosuppres effects, increased infection risk

Anakinra (Kineret): Blocks interleukin-1 receptors, decreases joint destruction & inflam., not to be used w/TNF blockers, avail. in prefilled syringes; increased site reactions, increased infection risk, neutropenia
Term
Leflunomide (Arava) -DMARD
Definition
-Small molecule DMARD
-decreases immune response
A.E.-diarrhea, resp. infection, alopecia, hepatotoxicity, Steven Johnson,severe HPT
Interactions: NSAIDS, methotrexate, cholestyramine
***Contraindicted during pregnancy
-If pregnancy is desired for M/W: take cholestyramine (8g TID) for 11 days
-verify plasma level <0.02 mg/dl
Term
Osteoarthritis
Definition
-May or may not have an inflammatory component (generally less w/ RA)
Tx: relieve pain, minimize disability, pt education
***Acetaminophen is first line tx***
-Salicylates
-NSAIDS
-Corticosteriods (s.t. for pt's who dont respond to other tx, lowest possible dose, not to exceed 5-10 days)
Term
Synovial Fluid Replacement Agents (Hyaluronadase)
Definition
-Synvisc (hylan G-F 20)
-Hylagan (sodium hyaluronate)
-Glucosamine +/- chondroitin
-Capsaicin cream
Term
Treatment Goals for Gout
Definition
treat acute attacks, eliminate/ treat underlying cause, prophylaxis
Term
Gout Treatment
Definition
1) NSAIDS: INDOMETHACIN is DOC*** but they do not decrease uric acid levels
2) Cholchicine: limited use do to toxicity, can decrease amount of uric acid in joint; low dose- too much with cause major diarrhea, vomiting,abdominal pain, blood dyscrasias; IV available to avoid GI problems but can cause tissue necrosis
-avoid in elderly, pregnancy
Term
Preventing attacks of Gout
Definition
-Some pt's may go yrs w/out another attack(up to 10)
-Need to determine who is an overproducer vs. underexcretor
-Goal is to decrease uric acid levels below 7mg/dl in men and 6mg/dl in women
-Low purine diet (low saturated fat and intake of meats)
Term
Pharmalogic Tx for preventing attacks of Gout
Definition
-Cholchicine in low doses
-Uricosurics- promote excretion of uric acid (underexcretors)- Probenacid (Benemid) & Sulfinpyrazone (Auturane)
A.E.
P:GI effects N/V, Rash (generally well tolerated)
S: more common GI effects, ulcers
**avoid use in pt's w/ CrCl < 20-30ml/min
Term
Pharmalogic Tx for preventing attacks of Gout Cont'd
Definition
Allopurinol (Zyloprim) -for overproducers
-adjust dose if renal impairment
-A.E: rash-need to d/c at first site
GI, drowsiness, headache
Interactions- combo w/ amipicillin increases risk of rash
Exp. Tx
-Febuxostat (similar to above, except renal impairment adjustment)
Term
Migraines/ non-pharm tx
Definition
-Without aura is more common
-Eliminate or control triggers
-Maintain reg eating, sleep, exercise patterns
-Dark quiet room helps
-Ice pack on neck and scalp
Term
Abortive therapy
Definition
-goal is to eliminate headache pain
-begin at earliest onset of attack or when first signs of aura start
-Routes: PO,IM, nasal, rectal
-Should not be used <1-2 times per week due to risk of rebound headache
-Antiemtics used for N/V- metoclopramide, prochlorperazine
-Analgesics: Aspirin, IBP, Acetaminophen (not to be used alone- Acet. ASA Caffeine- exedrin migraine)
Term
Barbiturate containing products
Definition
-Butlbital, ASA, Caffeine (Fiornal)
-Butalbital, Acetam, Caffeine (Floricet)
-Rebound headaches
-Not typically recommended
Term
Opioid Analgesics for Headaches
Definition
-Reserved for severe migraine pain that has not responded to first line tx
-Meperidine
-Butorphanol nasal spray (Stadol NS)
Term
Sympathomimetic Combinations
Definition
-Isometheptene, acetam, dichloralphenazone
(Midrin)
-Can lead to rebound headaches
-Alt. for mild-moderate headaches
Not to be used w/ pt's who have HPT
Term
Ergot Alkaloids
Definition
-Ergotamine- oral (Cafergot)
SL- Ergomar
rectal- (Cafergot supp)
-Dihydroergotamine: IM/IV (D.H.E. 45) or intranasal (Migranal)
*non-selective serotonin (5-HT) agonist, constriction of intracranial BV
A.E.
N/V- should be used in combo w/ antiemetic (M&P)
Peripheral vascular effects
Chest pain and angina
-Not to be used w/ Triptans (24 hrs)
Contraindications:
-Peripheral vascular disease, uncontrolled HPT, CAD, Pregnancy & lactation, hepatic or renal problems, Elderly (<60)
Term
Serotonin Receptor Agonists (Triptans)
Definition
**DOC for mod-severe that dont respond to NSAIDS
Sumatriptan,Almotriptan etc, table 5
-Different pharmacokinetic properties: duration, onset, route
-A.E,: parathesia, tingling, flushing, burning, chest pain, MI possible, dizziness, fatigue
**do cardiac assess prior to use
Interactions:Ergots, other triptans (24h
Contraindications:
Pregnancy, CAD, ischemic bowel
Term
Serotonin Receptor Agonists (Triptans)
Drug Selection (onset of action)
Definition
Fast Acting: rizatriptan, zomatriptan, eletriptan, sumatriptan (REZS)
(Sum SC is expensive)
Long Acting: naratriptan & frovatriptan (FN) those with reccurent headaches)
Term
Preventive tx for headaches
Definition
-Indicated for those who have frequent attacks (>2/ month)
-Propanolol, valproic acid, amitriptyline
Beta Blockers: Propanolol (Inderal) most commonly used; those that contain ISA arent effective (acebutolol, pindolol)
-Anticonvulsants: Valproic Acid (Depakote ER) 1st line if Beta or antidepressant cant be used
-Topirimate (Topamax)
-Tricyclic antidepressants: amitriptyline (anticholinergic effects, orthostatic hypotension)
-Calcium Channel Blockers: Verapamil (Calan)
**see S.E. in handout
Term
Cluster Headaches
Definition
-Unilateral, throbbing, usually behind eyes and more common in men
-Tx: oxygen & prophylaxis w/ Lithium or verapamil
Term
Tension-type Headaches
Definition
-Most common form of headache
-Mod, non-throbbing, headband dist.
-caused by stress, eyestrain, aggravation
-Acetaminophen or NSAIDS; prophylaxis w/ amitriptyline
Non-pharm: biofeedback, baths, massage,etc
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