anti-inflammatory drugs Flashcards
Calecoxib
Selective COX-2 inhibitor
Valdecoxib
Selective COX-2 inhibitor
Etoricoxib
Selective COX-2 inhibitor
Nabumetone
Selective COX-2 inhibitor in lower dosage
Meloxicam
Selective COX-2 inhibitor in lower dosage, rheumatoid arthritis, gout, osteorthritis
Etodilac
Selective COX-2 inhibitor in lower dosage
Asprin
(irreversibly binds to COX1) higher dosage non selective
Ibuprofen
higher dosage non selective to COX1 or COX2
Indomethacin
higher dosage non selective to COX1 or COX2
Naproxen
higher dosage non selective to COX1 or COX2
Diclofenac
higher dosage non selective to COX1 or COX2
NSAIDs CNS effect
Headache and tinnitus
NSAIDs Cardiovascular effect
Fluid rentention, hypertension
NSAIDs Hematologic effect
Rare thrombocytopenia
NSAIDs Hepatic effect
Abnormal liver function test
NSAIDs Rashes
all types
NSAIDs Renal effect
chronic analgesic nephropathy
Asprin overdose Sx
Hyperventilation, CNS depression of respiration, bleeding time increase
In Kids due to Asprin usage due to viral infection
Reye’s syndrome
Sx: Acute encephalophathy and fatty liver failure, seen in children after viral infection, nausea, vomiting, change in mental status
Reye’s syndrome
When can you use Aspirin in children ?
Kawasaki Diseases
Low dosage of Asprin (<300 mg)
Decrease platelet aggregation
Medium dosage of Aspirin (300- 2400 mg)
antipyretic and analgesic
(2400 -4000 mg) Asprin (large)
anti-inflammatory
COX2 inhibitors are used for:
rheumatoid artheritis and other inflammation disease
When is COX2 inhibitors preferred to be used?
Patients with history of gastritis or ulcers as COX1 inhibition is less.
COX-2 inibits production of PGI2 so:
unopposed effect of TxA2, increased risk of cardiovascular and cerebrovascular events, so edema and hypertension
Rofecoxib
most prescribed selective cox2 inhibitor, Vioxx, ceoxx, ceeoxx,
Adverse effect of celecoxib
increased risk of thrombosis, sulfa-allergy
Acetaminophen
analgesic, antipyretic, used for mild and moderate pain
What is preferred for children with viral infection?
Acetaminophen
Adverse reaction of acetaminophen?
increase of hepatic enzymes (hepatotoxicity with centrilobular necrosis),
Adverse dose of Acetaminophen
15 g
Antidote for Acetaminophen toxicity
N-acetylcysteine–regenerates glutathione-start within 8-10 hrs, liver transplant may be required.
What happens to APAP?
Oxidized to N-acetyl-p-benzoquinoneimine (highly electrophilic), accumulates and adducts with macromolecular systems and cell function
How does APAP work?
weak COX1 and 2 inactivated peripherally tissues
What does APAP toxicity work?
hepatic necorsis, APAP metabolites depletes glutathione and form toxic tissues
What is glucocorticoids?
anti-inflammatory drugs used for Addison’s disease and asthma, have powerful immunosuppresent actions as well
Prednisone
glucocorticoids
Cortisone
glucocorticoids
Hydrocortisone
glucocorticoids
How does glucocorticoids work?
inhibits PLA2, which suppresses cox-2 syn, so decrease leukotrines and prostaglandin, and upregulates anit-inflamm protein in gene and protein level
Toxicity of glucocorticoids?
adrenal insufficiency and Cushing’s syndrome (osteoporesis due to demineralization)
Sx: buffalo hump, moon facies, truncal obesity, muscle wasting, thin, osteoporsis, adrenocortical atrophy, peptic ulcer, diabetes
Latrogenic Cushing’s syndrome
What happens when you stop glucocorticoids after using a long time?
Adrenal insufficiency
What is the first choice to treat rheumatoid arthritis?
DMARDS: Methotrexate (MTX)
MTX toxicity
myelosuppression (reversible with leucovorin), fatty liver, mucositis, teratogenic (bad pregnancy)
When is MTX used?
Cancers (leukemias, lymphomas, choriocarcinoma, sarcomas), nonneoplastic (abortion, ectopic preg, rheumatoid arthritis)