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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
Q

Nonspecific reversible inhibitors of COX-1 & COX-2: the best (2) and the worst (2)

A

first DOC: ibuprofen-best SE profile

worst (but potent): Indomethacin, Phenylbutazone (not in US)

26
Q

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

A

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
Q

Indomethacin (Indocin)

A

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
Q

Note that a lot of cards were lost when not saved, so I’m skipping from Indomethacin to Acetominophen now

A

yup, a lot
like Naproxen=long half life, no pregos
Ibuprofen (Motrin) 1st DOC b/c low SEs half life 2-4h

29
Q

Acetominophen

A

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
Q

Best NSAID for
NO hx of PUD:
PUD in hx but not active:
active PUD:

A

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
Q

Acetaminophen PHK

A

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
Q

Acetaminophen effects

A

antipyretic action
analgesic action
NO ANTIINFLAMMATORY ACTION

33
Q

Acetaminophen uses

A

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
Q

Acetaminophen AEs:

A

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
Q

When does Acetaminophen toxicity become serious

A

when METABOLITES EXCEED THE AVAILABLE REDUCED GLUTATHIONE in body

chronic ETOH consumption ↑toxicity`

36
Q

tx of acetaminophen intoxication

A

gastric emptying
forced diuresis
hemodialysis
SPECIFIC ANTIDOTE: N-acetylcysteine (Mucomyst)
N-acetylcysteine must be administered parenterally, ASAP within 10-12 hours after intoxication

37
Q

Goals of therapy for Chronic Inflammatory Conditions

A 
pain relief
↓inflammation
protect articular structures
maintain fxn
control systemic involvement
38
Q

Gold Salts: action, toxicity

A

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
Q

Penicillamine (Cuprimine): action, toxicity

A

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
Q

Hydroxychloroquine (PLaquenil)

A

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
Q

Sulfasalazine (Azulfidine): use, effectiveness, toxicities

A

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
Q

Infliximab (Remicade): description, use, AE, contraindications

A

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
Q

Rituximab (Rituxan): description, use, admin

A

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
Q

Adalimumab (Humira): description use, admin, AEs

A

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
Q

Etanercept (Enbrel)

A

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
Q

Abatacept (Orencia)

A

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
Q

Leflunomide (Arava): Action, Admin, SEs, Contra

A

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
Q

Mycophenolate mofetil (Cellcept)

A

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
Q

Anakinra (Kineret)

A

INTERLEUKIN-1 RECEPTOR AGONIST

RA

subQ
t1/2: 4-6h, eliminated renally

CONTRA: breastfeeding, kids, hypersensitivity rxns, renal dz

50
Q

Tofacitinib (Xeljanz)

A

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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