Pharm #5 Flashcards
Body’s Protective response to tissue injury and infection
Inflammation Patho
A vascular reaction occurs causing fluid, blood, leukocytes, and chemical mediators to accumulate at the injured site
Inflammation Patho
3 Chemical Mediators
Histamine, Kinins, and Prostaglandins
Not all inflammations caused by ___
illness
anti-inflammatory med goal is to-
decrease and inhibit mediators from occurring
Cardinal signs of inflammation
Erythema, Edema, Heat, Pain, Loss of function
Erythema-
Redness occurs in first phase of inflammation
Edema-
Swelling, 2nd phase of inflammation.
Plasma is leaking into the tissues at the site of injury
Heat-
resulting from increase blood at the site
Pain-
resulting from swelling and chemical mediators
Loss of function-
resulting from pain and swelling that occurs at the site.
Inflammatory phases
Vascular phase
Delayed phase
Occurs 10 to 15 minutes after injury
Vascular phase
Associated with vasodilation and increased capillary permeability
Vascular phase
Fluid and blood substances move to injured site
Vascular phase
Leukocytes infiltrate inflamed tissue
Delayed phase
Converts arachidonic acid into prostaglandins (causing vasodilation, papillary permeability, and sensation that causes pain)
Cyclooxygenase (COX) enzyme
Cyclooxygenase (COX) enzyme has two forms:
COX-1
COX-2
Protecting lining of the stomach and regulating platelets. Inducing clotting.
COX-1
Trigger inflammation and pain.
COX-2
Anti-inflammatory drug groups (4 major drug groups)
Nonsteroidal anti-inflammatory drugs (NSAIDs)
Corticosteroids
Disease-modifying antirheumatic drugs (DMARDS)
Antigout drugs
Inhibit COX enzyme which increases biosynthesis of prostaglandins- by inhibiting the enzyme it decreases pain.
Action of NSAIDs
Analgesic effect- Primary use is to relieve inflammation and pain
Action of NSAIDs
Antipyretic effect- can decrease fever
Action of NSAIDs
Inhibit platelet aggregation
Action of NSAIDs
Mimic effects of corticosteroids
Action of NSAIDs
Inhibit COX enzyme
Action of NSAIDs
First generation NSAIDS-
Aspirin- anticoagulant. Help prevent MI or stroke
Over the counter NSAIDS- ____
Other NSAIDs require prescription
aspirin, ibuprofen and naproxen
First-generation NSAIDs-
not selective.
When inhibit cox enzyme it inhibits 1 and 2.
Can cause GI upset and bleeding which is why it is required to be taken with food.
Second-generation NSAIDs-
not causing GI upset or bleeding.
Selective COX-2 inhibitors
Oldest anti-inflammatory drug. Goes back from 1899.
Aspirin (acetylsalicylic acid) (ASA)
Aspirin (acetylsalicylic acid) (ASA) action
Anti-inflammatory, antiplatelet, antipyretic effects
Aspirin (acetylsalicylic acid) (ASA) Therapeutic serum salicylate level
15 to 30 mg/dL
Aspirin (acetylsalicylic acid) (ASA) Toxic serum salicylate level Mild toxicity—
Greater than 30 mg/dL
Aspirin (acetylsalicylic acid) (ASA) Toxic serum salicylate level Severe toxicity—
Greater than 50 mg/dL
Inhibiting prostaglandins which decreasing inflammation.
Aspirin (acetylsalicylic acid) (ASA)
Inhibiting both cox 1- decreasing platelet aggregation, given with cardiac, causes.
Aspirin (acetylsalicylic acid) (ASA)
Downside- GI irritation,
Aspirin (acetylsalicylic acid) (ASA)
Upside- aspirin is a weak acid drug it will not cause as much GI upset as normal ibuprofen or cerebrovascular disorders to prevent clotting
Aspirin (acetylsalicylic acid) (ASA)
Prevents cox 2
Aspirin (acetylsalicylic acid) (ASA)
Gives 81 mg maintenance dose to prevent
Aspirin (acetylsalicylic acid) (ASA)
Decrease irritation- enteric coated
Aspirin (acetylsalicylic acid) (ASA)
Increased bleeding with anticoagulants and other NSAIDs
Salicylates drug interaction
Risk for hypoglycemia with oral antidiabetics (Metformin)
Salicylates drug interaction
Increased gastric ulcer risk with glucocorticoids
Salicylates drug interaction
Decreased effects of ACE inhibitors, loop diuretics, probenecid
Salicylates drug interaction
Salicylate (aspirin) effects are decreased by corticosteroids
Salicylates drug interaction
Increase PT, bleeding time, INR, uric acid
Salicylates Labs
Decrease cholesterol, T3 and T4 levels,
Salicylates Labs
Foods containing salicylates
Prunes, raisins, licorice
Certain spices such as curry and paprika
Do not take with other NSAIDs- it will increase risk for side effects
Aspirin Caution
Avoid during the last trimester of pregnancy- can cause premature closure of the ductus arteriosus (allows blood to bypass they lungs and closes right after birth)
Aspirin Caution
Do not give to children with flu or virus symptoms as it may lead to Reye syndrome- swelling of the liver and brain and can become fatal.
Aspirin Caution
Aspirin Side effects
Dizziness, drowsiness, headache, flushing, visual changes, tinnitus, hearing loss, GI distress, ulceration, bleeding, seizures, Reye syndrome
bronchospasm
Early signs of aspirin side effects
Dizziness, Tinnitus, Bronchospasm
Salicylates Assessment
Medical history- GI disorders, try not to increase risk for GI upset
Salicylates Nsg interventions
monitoring salicylate level.
Observe for s/sx of bleeding- dark tarry stools, bleeding gums, petechiae, ecchymosis and purpura
Do not to take aspirin with alcohol or other drugs that are highly protein bound specifically warfarin.
Salicylates Education
Tell dentist if they are on high doses of aspirin bc of increased bleeding, decrease risk of infection.
Salicylates Education
If someone has surgery they need to discontinued at least 7 days before.
Salicylates Education
If they have enteric coated aspirin it cannot be crushed- helps decrease breakdown in stomach.
Salicylates Education
Not administering this to children.
Salicylates Education
Talk to clients about taking aspirin for menstrual cycle.
Salicylates Education
Report changes is LOC, hearing, vision, potential side effect or toxicity at an early level
Salicylates Education
Para-Chlorobenzoic Acid Examples
Indomethacin, sulindac, tolmetin
First classification developed and can cause severe GI distress
Indomethacin
New drugs in classification, do have less adverse reactions.
Sulindac and Tolmetin
Para-Chlorobenzoic Acid Action
Inhibits prostaglandin synthesis
Para-Chlorobenzoic Acid Use
Rheumatoid arthritis, osteoarthritis, gouty arthritis
Para-Chlorobenzoic Acid Side effects/Adverse effects
Dizziness, headache, weakness
GI distress and bleeding
Sodium and water retention- increase in BP
Hypertension
Group of NSAIDS
Para-Chlorobenzoic Acid
First generation NSAIDs- cox 1 and 2 inhibitor
Para-Chlorobenzoic Acid
If Indomethacin does not work can switch to __
Sulindac and Tolmetin
Phenylacetic Acid Derivatives Examples
Ketorolac (Toradol)
Prototype drug.
Good analgesic effects.
Benefit vs opioid.
PO, intranasally, IM and, IV.
Similar side effects to NSAIDs- GI distress
Ketorolac (Toradol)
Phenylacetic Acid Derivatives Action
Inhibits prostaglandin synthesis
Phenylacetic Acid Derivatives Use
Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and pain
No antipyretic effect
Primary use is to relieve inflammation and pain
First generation NSAIDs
Phenylacetic Acid Derivatives
Reducing pain and inflammation in this drug
Phenylacetic Acid Derivatives
Often used for post op and post-partum pain
Phenylacetic Acid Derivatives
Short term pain reliever. Not longer than 5 day use
Phenylacetic Acid Derivatives
When used for postop or postpartum pain they are giving different NSAIDs such as ibuprofen
Phenylacetic Acid Derivatives
Phenylacetic Acid Derivatives Side effects/Adverse effects
Dizziness, drowsiness, Weakness, headache, GI distress, GI bleeding/perforation
Phenylacetic Acid Derivatives- Ketorolac
Is recommended for short-term management of pain
Propionic Acid Derivatives Examples
Ibuprofen (prototype and commonly used in the drug class) & Naproxen
Propionic Acid Derivatives Action
Inhibit prostaglandin synthesis
Propionic Acid Derivatives Use
Pain, osteoarthritis, rheumatoid arthritis
NSAIDs - New group
Propionic Acid Derivatives
Effects like aspirin but stronger and less GI irritability
Propionic Acid Derivatives
S/E similar to salysilates but less chance of GI distress and bleeding
Propionic Acid Derivatives
Give caution to give this with a blood disorder.
Propionic Acid Derivatives
Need to know drug history. ibuprofen and warfarin increases risks for bleeding
Propionic Acid Derivatives
Propionic Acid Derivatives Side effects
Drowsiness, dizziness, headache, confusion, Insomnia, dreams, blurred vision, tinnitus, gastric distress and bleeding, edema
Propionic Acid Derivatives Drug interactions
Increased bleeding with warfarin
Increased effects with phenytoin, sulfonamides, warfarin, cephalosporins
Hypoglycemia with oral hypoglycemics
Ibuprofen Assessment
Medical and drug history
Specific allergies to NSAIDs
Contraindicated with severe renal or liver disease and peptic ulcers. Caution with bleeding disorders.
S/E: GI distress and peripheral edema
Ibuprofen Nsg interventions
Monitor for bleeding, PT INR prolonged- removing NSAID.
Report if GI discomfort
Avoid alcohol, it will cause increase in GI distress.
Ibuprofen Education
Tell dentist about NSAIDs if taking frequently.
Ibuprofen Education
Menstruation- want females to avoid ibuprofen 1-2 days before menstruation.
Ibuprofen Education
To avoid increasing menstrual flow.
Ibuprofen Education
Should be avoided during pregnancy can cause congenital abnormalities and increase in bleeding at delivery.
Ibuprofen Education
For arthritis- it takes a few weeks for steady state to tx symptoms.
Ibuprofen Education
Take with food to decrease GI upset
Ibuprofen Education
Fenamates Examples
Meclofenamate sodium & mefenamic acid
Fenamates Action
Inhibits prostaglandin synthesis
Fenamates Use
Osteoarthritis, rheumatoid arthritis
Fenamates Side effects/Adverse effects
Dizziness, headache, tinnitus, pruritus
GI distress/bleeding, edema
First generation group most oftenly used to treat arthritis- cause GI distress
Fenamates
Oxicams Examples
Meloxicam
Oxicams Action
Inhibits prostaglandin synthesis
Oxicams Use
Osteoarthritis, rheumatoid arthritis
Oxicams Side effects/Adverse effects
Dizziness, headache
GI distress/bleeding, edema
Well-tolerated
Will or can cause GI distress but less severe
Oxicams
Has a long half life
Oxicams
Selective COX-2 Inhibitors Example
Celecoxib (Celebrex)
Selective COX-2 Inhibitors Action
Selectively inhibits COX-2 enzyme without inhibition of COX-1
Selective COX-2 Inhibitors Use
Osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, pain, dysmenorrhea
Selective COX-2 Inhibitors S/E
Dizziness, headache, sinusitis
Peripheral edema, hypertension
2nd generation NSAIDs
Selective COX-2 Inhibitors
Most recently new to drugs
Selective COX-2 Inhibitors
Only one still left is Celebrex
Selective COX-2 Inhibitors
Drug interactions more common due to number of drugs taken
Selective COX-2 Inhibitors- NSAIDs in older adults
Greater incidence of GI distress, ulceration
Selective COX-2 Inhibitors- NSAIDs in older adults
Reduced dose decreases risk of side effects
Selective COX-2 Inhibitors- NSAIDs in older adults
Increase fluid intake for adequate hydration
Selective COX-2 Inhibitors- NSAIDs in older adults
Arthritis reason for older adults
Selective COX-2 Inhibitors- NSAIDs in older adults
Evaluate renal function bc can cause renal toxicity
Selective COX-2 Inhibitors- NSAIDs in older adults
Use the lowest most effective dose possible- go low start slow
Selective COX-2 Inhibitors- NSAIDs in older adults
NSAIDs- hepatotoxic
Selective COX-2 Inhibitors- NSAIDs in older adults
Corticosteroids examples
Prednisone, prednisolone, cortisone, methylprednisolone
Corticosteroids Action
Control inflammation by suppressing or preventing many of the components of the inflammatory process at the injured site
Corticosteroids Use
Arthritic flare-ups
Not the drug of choice for arthritis because of their numerous side effects
Corticosteroids Discontinuation
Taper off over 5-10 days
Short term for arthritic flare ups
Corticosteroids
Avoiding long term use due to side effects- adrenal insufficiency, osteoporosis, infection, hyperglycaemia, fluid and electrolyte imbalance, growth delay in children and peptic ulcer disease.
Corticosteroids
Dose strength and duration is dependent on the pain
Corticosteroids
Disease-Modifying Antirheumatic Drugs Types
Immunosuppressive agents
Immunomodulators
Antimalarials
Disease-Modifying Antirheumatic Drugs Use
Refractory rheumatoid arthritis that does not respond to other tx- invasive way.
Osteoarthritis, ankylosing spondylitis
Psoriatic arthritis, severe psoriasis
Crohn disease, ulcerative colitis
DMARDs
Disease-Modifying Antirheumatic Drugs
Slow or stop inflammatory process associated with rheumatoid arthritis
Disease-Modifying Antirheumatic Drugs
Including drugs that suppress or regulate the immune system
Disease-Modifying Antirheumatic Drugs
Including antimalarial drugs
Disease-Modifying Antirheumatic Drugs
Disease-Modifying Antirheumatic Drugs Side effects
Infection, peripheral edema, hypertension, hypercholesterolemia, headache, fever, chills, insomnia, oral ulcerations, nasopharyngitis, Influenza, sinusitis, GI distress, fatigue, Injection site reaction, Increase risk for infection
Immunosuppressive Agents Example
Methotrexate
Immunosuppressive Agents Action
Suppress inflammatory process
Immunosuppressive Agents Use
Refractory rheumatoid arthritis that does not respond to other anti-inflammatory tx
First type of DMARDs used
Immunosuppressive Agents
Immunomodulators Classifications
Interleukin 1 (IL-1) receptor antagonists
Tumor necrosis factor (TNF) blockers
Immunomodulators Examples
Anakinra & infliximab (remicade)
(Interleukin 1 receptor antagonist)- sydopine that contributes to the inflammation in the synovial joint and destruction.
Antagonist blocks from occurring
Anakinra
TNF blocker tumor necrosis factor contributes to synovitis- inflammation of synovial joint. By blocking it, it blocks from occurring.
Infliximab (remicade)
Immunomodulators Action
Disrupt inflammatory process
Delay disease progression`
Neutralize TNF
Immunomodulators Use
Rheumatoid arthritis, psoriatic arthritis, psoriasis, spondylitis, ulcerative colitis, Crohn disease
Modulating
Immunomodulators
Disrupting inflammatory process and delaying progression of the inflammatory disease
Immunomodulators
Risk for infection
Immunomodulators
Need to have a negative TB test
Immunomodulators