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4Qpharm3-test1 > analgesic, antipyretic, NSAIDs and DMARDS > Flashcards

analgesic, antipyretic, NSAIDs and DMARDS Flashcards

1
Q

clinical signs of inflammation (4)

A

erythema
edema
tenderness
pain

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2
Q

3 phases of inflammation

A

acute inflammation
immune response
chronic inflammation

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3
Q

Aspirin: mechanism of action

A

nonselective, irreversible inhibitor of COX-1 & COX-2

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4
Q

Aspirin: pharmokinetics

A

acid, pKa=3.5
fast oral absorbtion
[ASA] in mucosal cell=20 times [ASA] in stomach
-readily crosses placenta
-SLOWLY crosses BBB
rapidly hydrolyzed inplasema, liver & erythrocytes
binds to plasma proteins

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5
Q

ASA drug interactions

A

COMPETES w/T3, Pen G, thiopental, bilirubin, phenytoin, sulfinpyrazone, naproxen, etc for PROTEIN PLASMA BINDING SITES->drug interactions

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6
Q

ASA metabolism

A

low doses: first order kinetics
high doses: zero order kinetics (>600mg body burden; 2 ASA/day=zero order kinetics)

RENAL EXCRETION-alkalinization of urine promotes excretion

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7
Q

Aspirin effects

A

ANTIINFLAMMATORY- ↓sxs of inflammation
ANALGESIC: most effective in mild-moderate pain
ANTIPYRETIC:↓elevated temp
ANTIPLATELET: irreversible inhibition of platelet COX enzymes; platelets can’t synthesize new enzyme, effect lasts 8-10 days

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8
Q

Aspirin uses

A 
mild-moderate pain
antipyresis
anti-inflammatory (NSAID)
MI, thrombosis prophylaxis
long term use ↓colon CA
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9
Q

Aspirin adverse effects

A

respiratory alkalosis
then
metabolic & respiratory acidosis

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10
Q

ASA platelet effects

A

ASA (but not sodium salicylate) inhibits platelet aggregation, thereby ↑ bleeding time
single 650 mg dose of ASA DOUBLES bleeding time (may last 8-10d)

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11
Q

ASA should be avoided or d/c in which pts? (6)

A 
hypoprothrombinemia
vitamin K deficiency
hemophilia
severe hepatic damage
prior to labor

stop AT LEAST ONE WEEK prior to elective surgery

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12
Q

Uricosuric effects of ASA

A 
biphasic & dose dependant
LOW DOSES (1-2g/day): ASA ↓ uric acid excretion & ↑plasma urate excretion
LARGE DOSES (>5g/day): ASA ↑uric acid excretion (uricosuria) & lowers plasma urate levels
***such large doses of ASA are POORLY TOLERATED b/c ASA causes stomach irritation, gastric bleeding, etc
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13
Q 
ASA effects:
Cardiovascular
Lungs
GI
renal
A

Cardio: minimal in regular doses

Lungs: ASA asthma due to ↑leukotriene synthesis

GI upset, gastritis, ulcer, bleeding (buffering, food, misoprostol used to reduce damage; but miso=abortion so no pregos)

Kidneys: renal damage, acute renal failure, interstitial nephritis

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14
Q

ASA & pregnancy

A

NO TERATOGENIC EFFECTS

withhold ASA several days prior to deliver to prevent excessive & prolonged post partum bleeding

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15
Q

salicylic acid local irritant effects

A 
salicylic acid (but NOT ASA) irritant to skin, mucosa, epithelial cells, ketolytic effect used to remove wards, corns, funga, exzematous dermatitis
*but salts of salicyclic acid=no effect on skin
methyl salicylates (oil of Wintergreen) is irritating to skin
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16
Q

ASA should be DECREASED in whom?

A

↓ ASA during long term therapy w/oral anticoagulants, hypoglycemic agents, etc

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17
Q

Salicylate: fatal dose

A 
ASA: abt 20g (10-30g)
methyl salicylate (oil of Wintergreen): 4-5mL fatal in kids
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18
Q

Reye’s syndrome

A

cerebral edema in kids w/viral infections who take ASA

so DOC is acetaminophen

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19
Q

Nonacetylated salicylates (3)

A

magnesium chloine salicylate
sodium salicylate
salicyl salicylate

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20
Q

Nonacetylated salicylates: effects

A

effective anti-inflammatory
salicylic acid is the active drug
less effective analgesics than ASA
NO irreversible COX inhibition

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21
Q

Diflunisal: what is it, what is its action

A

salicylic acid derivative, but NOT metabolized to salicylic acid
does NOT have significant antipyretic effects, prob due to POOR penetration into CNS

22
Q

NSAIDs: 2 major types based on action

A
  1. Specific reversible inhibitors of COX-2 enzymes

2. Nonspecific reversible inhibitors of COS-1 & COX-2 enzymes

23
Q

Celecoxib (Celebrex): class, admin, AEs, contraindication

A

Selective reversible COX-2 inhibitors=less gastropathy & risk of GI bleed
-but FDA says risk of GI ulceration, bleeding and perforation
ORAL admin
AEs: GI disturbances including ulceration & bleeding, ↑risk of cardiovascular dz
CONTRA: GI dz, asthma, breast feeding, prego, renal failure

24
Q

Nonspecific reversible inhibitors of COX-1 & COX-2 effects

A

various chem structures
sim to ASA but NOT irreversible
variable SE frequency but basically same
variable PHK

25
Nonspecific reversible inhibitors of COX-1 & COX-2: the best (2) and the worst (2)
first DOC: ibuprofen-best SE profile worst (but potent): Indomethacin, Phenylbutazone (not in US)
26
Nonspecific reversible inhibitors of COX-1 & COX-2 toxicities
GI: pain, bleeding, ulcer, pancreatitis, diarrhea CNS: HA, dizziness, confusion, depression Lung: bronchoconstriction Bone marrow: agranulocytosis, aplastic anemia Nephrotox: acute renal failure, interstitial nephritis, nephrotic sxs Hepatotox: enzyme elevation, hepatitis Hypersensitivity rxns
27
Indomethacin (Indocin)
nonselective, reversible inhibitor of COX-1 & COX-2 ↓ PMN migration inhibit phospholipase A very potent ant-inflammatory agent, high incidence of SEs used for patent ductus arteriosus (others work too)
28
Note that a lot of cards were lost when not saved, so I'm skipping from Indomethacin to Acetominophen now
yup, a lot like Naproxen=long half life, no pregos Ibuprofen (Motrin) 1st DOC b/c low SEs half life 2-4h
29
Acetominophen
often preferred to ASA b/c better tolerated no COX inhibition so no ulvers, blood clotting defects, acid-base imbalance auditory toxicity but OD can cause FATAL HEPATIC NECROSIS so, be careful with kids
30
Best NSAID for NO hx of PUD: PUD in hx but not active: active PUD:
NO hx: any NSAID hx of PUD, not active: celecoxib w/or without antacids, some NSAIDS w/misoprostol or "-prazols" (PPIs) active PUD: acetaminophen &/or opioids
31
Acetaminophen PHK
ORAL absorption half-life: 2-3 hours (inc. w/high doses) liver metabolism, conjugation, renal excretion dose dependent free radical production-eliminated by GSH (reduced glutathione)
32
Acetaminophen effects
antipyretic action analgesic action NO ANTIINFLAMMATORY ACTION
33
Acetaminophen uses
DOC: fever in kids mild-moderate pain adjunct to anti-inflammatory therapy dose not influence urate excretion combined w/codeine & derivatives, sedatives, cough suppressants, tramadol, diphenhydramine, caffeine etc NO anti-inflammatory effect, no platelet effects
34
Acetaminophen AEs:
occasional SKIN RASH & allergic rspsonse, CROSS-SENSITIVITY w/ salicylcates few cases of NEUTROPENIA ****DOSE-DEPENDENT FATAL HEPATIC NECROSIS*** (in adults, 10-15g at once=hepatotoxicity, 25 g=fatal) hepatotoxicity->encephalopathy, coma & death ↑serum transaminase, lactic acid dehydrogenase hydroxylated INTERMEDIATE METABOLITE is rspsnble for liver damage
35
When does Acetaminophen toxicity become serious
when METABOLITES EXCEED THE AVAILABLE REDUCED GLUTATHIONE in body chronic ETOH consumption ↑toxicity`
36
tx of acetaminophen intoxication
gastric emptying forced diuresis hemodialysis SPECIFIC ANTIDOTE: N-acetylcysteine (Mucomyst) N-acetylcysteine must be administered parenterally, ASAP within 10-12 hours after intoxication
37
Goals of therapy for Chronic Inflammatory Conditions
``` pain relief ↓inflammation protect articular structures maintain fxn control systemic involvement ```
38
Gold Salts: action, toxicity
inhibit phagocytosis, inhibit cellular respiration, inhibit proteolytic eyzmyes of leukocytes, prevent PGI synthesis SUPPRESS CELLULAR IMMUNITY toxicity: BONE MARROW DAMAGE, dermatitis, ENTEROCOLITIS, jaundice, peripheral neuropathy
39
Penicillamine (Cuprimine): action, toxicity
chelating drug effective in RA & Wilson's mechanism unknown, maybe it works like gold salts TOXICITIES: high inc. of adv. rxns; pruritis, rash, alteration in taste, thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, proteinurin, hypoalbuminemia, nephrotic syndrome, lupus like dz, pemphigus, Goodpasture's syndrome, myasthenia gravis, polymyositis, stenosing alveolitis PTs OVER 65 YEARS HAVE HIGHER RISKS
40
Hydroxychloroquine (PLaquenil)
possess antihistaminic, anticholinesterse & antiprotease props inhibits prostaglandin synthesis inhibits biosynth of mycopolysaccharide, inhibits responses to chemotactic stimuli & phagocytosis stabilizes lysosomes REACTS w/NUCLEIC ACIDS and TISSUE PROTEINS Toxicity: pruritus, hemolysis (G6PD deficient), ototoxicity, retinopathy, peripheral neuropathy
41
Sulfasalazine (Azulfidine): use, effectiveness, toxicities
Rheumatoid Arthritis, IBS as effective Penicillamine, less toxic As affective as injected gold compounds & better tolerated TOX: Gi disturbance, rash, RARE hepatitis & blood dyscrasias MONITORING for HEPATITIS & BONE MARROW SUPPRETION recommended for 2-3 weeks during first 3 mos of tx & less frequently therafter
42
Infliximab (Remicade): description, use, AE, contraindications
IgG1k monoclonal antibody targeted against TNFalpha human constant + murine variable regions use: Crohn's dz & RA combined with methotrexate IV admine AE: HA & infusion rxns Contra: prego, breast feeding, kids, infections
43
Rituximab (Rituxan): description, use, admin
IgG immunoglobin that BINDS TO CD20, a B-LYMPHOCYTE DIFFERENTIATE ANTIGEN on pre-B & mature B-lymphocyte CD20 antigen expressed on >90% of B-cell non-Hodgkin's lymphoma (NHL), but not on hematopoietic stem cells, pro-B cells, normal plasma cells or other normal tissues USE: NHL, other B-cell malignancies including chronic lyphocytic leukemia ADMIN: IV
44
Adalimumab (Humira): description use, admin, AEs
recomh. HUMAN IgG1 MAB specific for TNG-alpha MONOTHERAPY in tx of RA (is formally approved for this, unlike infliximab) subQ , t1/2=8-10days AEs: rash, flu sxs, fatigue, HA, pruritis, N/V
45
Etanercept (Enbrel)
not a MAB, instead a FAKE TNFalpha receptor, so fewer can bind to real TNF receptor -inhibits TNF subQ AE: injection site rxn, infections, increased incidence of antibody formation CONTRA: bone marrow suppression, breast-feeding, kids, DM, infection, sepsis, vaccination, varicella, active TB
46
Abatacept (Orencia)
FULLY HUMAN recombinant fusion protein 2nd signal blocker of T cell activations competes w/ CD28 (on T cell) for CD80 & CD86 (on APC) binding Rheumatoid Arthritis IV mean t1/2=13.1 days
47
Leflunomide (Arava): Action, Admin, SEs, Contra
inhibits dihydrooratate dehydrogenase (DHODH) INHIBITS INDUCTION OF COX-2 oral admin, t1/2=16 hours SE: N/V/D, dyspepsia, abdominal pain, back pain, weight loss, anorexia, oral ulceration elevated hepatic enzymes CONTRA: prego, breast feeding, heapatic, renal failure
48
Mycophenolate mofetil (Cellcept)
INHIBITS LYMPHOCYTE PURINE SYNTHESIS by reversible & noncompetitively inhibiting IMPDH admin: ORAL or IV AE: diarrhea, emesis, GI bleed CONTRA: active GI dz, diarrhea, prego, breast feeding, infections
49
Anakinra (Kineret)
INTERLEUKIN-1 RECEPTOR AGONIST RA subQ t1/2: 4-6h, eliminated renally CONTRA: breastfeeding, kids, hypersensitivity rxns, renal dz
50
Tofacitinib (Xeljanz)
xelJANZ=janus kinase inhibitor prim inhibits JAK1& JAK3, to a lesser extent JAK2 Use: adults MOD-SEVERE w/ACTIVE RA who have had inadequate response or intolerance to methotrexate ORAL admin, t1/2=3h AEs: serious infections & malignancy

4Qpharm3-test1 (9 decks)

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