Pharmacology Flashcards
LTB4
Neutrophil chemotactic agent
LTC4, D4, E4
Increases bronchial tone
PGE2 and PGE2alpha
Increases uterine tone, decreases bronchial tone
TXA2
Increase platelet aggregation, increase vascular tone, increase bronchial tone
PGI2
Decrease platelet aggregation, decrease vascular tone, decrease bronchial tone, decrease uterine tone
Low dose aspirin <300mg/d
decreases platelet aggregation
intermediate dose of aspirin 300-2400mg/d
antipyretic and analgesic
high dose aspirin 2400-400mg/d
anti-inflammatory
stimulates respiratory centers causing hyperventilation and respiratory alkalosis
Aspirin
Irreversibly inhibits COX-1 and COX-2 by covalent acetylation
Aspirin
NSAIDs
Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac
reversibly blocks cyclooxygenase blocking PG syn
NSAIDs
used to close PDA
Indomethacin
Toxicity of NSAIDs
interstitial nephritis, gastric ulcer, renal ischemia
Reversibly inhibits COX2 found in inflammatory cells and vascular endothelium. Spares gastric mucosa
Celecoxib
Used in patient with RA and osetoarthritis who have gastritis or ulcers
Celecoxib
Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally
Acetaminophen
Use instead of aspirin to avoid Reye syndrome
Acetaminophen
N-acetylcysteine
Antidote for Acetaminophen toxicity which regenerates glutathione
Acetaminophen metabolite
NAPQI, depletes glutathione and forms toxic tissue adducts in liver
Pyrophosphate analogs; bind hydroxyapatite in bone, inhibiting osteoclast activity
Bisphosphonates like Alendronate
Clinical use for Bisphosphonates
osteoporosis, hypercalcemia, Paget dx of bone
Advise patients to take this w/ water and remain upright for 30 minutes
Bisphosphonates, can cause corrosive esophagitis
Osetonecrosis of jaw
S/E of bisphosphonate
Used in lymphoma and leukemia to prevent tumor lysis-associated urate nephropathy
Allopurinol
Inhibits Xanthine Oxidase
Allopurinol and Febuxostat
Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
Probenecid
NSAID drugs used for Acute gout
Naproxen and indomethacin
Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing leukocyte chemotaxis and degranulation.
Colchicine
reactivation of latent TB
TNF-alpha inhibitors like Etanercept, Infliximab, adalimumab
used for RA, psoriasis, ankylosing spondylitis
Etanercept
used for IBD, RA, ankylosing spondylitis, psoriasis
Infliximab and adalimumab
Four main actions of NSAIDS
Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol), PGE2, and PGF2alpha
Prostaglandin analog indicated for severe pulmonary hypertension
Epoprostenol (PGI2)
Prostaglandin analog used as 2nd line for erectile dysfunction
Alprostadil (PGE1)
Prostaglandin analog used in pediatrics to maintain patency of ductus arteriosis
Alprostadil (PGE1)
NSAID available orally, IM, IV, nasally, and ophthalmically
Ketoralac
NSAID used mostly for anesthesia and has limited duration (<5 days) due to nephrotoxicity
Ketoralac
Difference between COX 1 and COX 2
COX 1: constitutive, COX 2: inducible during inflammation
COX 2 inhibitors should be used cautiously in patients with
Pre-existing cardiac or renal disease
Two main actions of acetaminophen
Antipyretic and analgesic activity
Inhibitor of lipoxygenase
Zileuton
Major side effect of zileuton that limits its use
Liver toxicity
Two leukotrienes (LTD4) receptor antagonists used in asthma
Zafirlukast and montelukast
NSAID avoided in gout because low doses increases uric acid levels
Aspirin
Side effects of colchicine
Diarrhea, liver toxicity, myelosuppression
Recombinant uricase that enhances uric acid metabolism and indicated for gout refractory to conventional therapy
Pegloticase
DMARDs are slow acting drugs for this indication
Rheumatic diseases
1st line for rheumatoic arthritis for most patients
Low-dose methotrexate
Dose-limiting toxicity of methotrexate
Myelosuppression
A mixture of two agents with one agent active for rheumatic disease and the other for inflammatory bowel disease
Sulfasalazine
Alternative to methotrexate as 1st line for rheumatoid arthritis through inhibition of dihydroorotate dehydrogenase, which leads to decreased pyrimidine synthesis
Leflunomide
Anti-malarial drug used in rheumatoid arthritis
Hydroxychloroquine
Side effect of hydroxychloroquine
Retinopathy
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
This class of agents block acetylcholine receptors at motor endplates and its effects can be reversed by cholinesterase inhibitors
Nondepolarizing blockers
Non-depolarizing neuromuscular blocker with long duration of action and is most likely to cause histamine release
Tubocurarine
Non-depolarizing neuromuscular blocker with short duration of action
Mivacurium
Two non-depolarizing blockers that undergo Hofmann elimination, which is useful for patients with renal and hepatic deficiency
Atracurium, cisatracurium
Non-depolaring neuromuscular blocker with long duration of action that can block muscarinic receptor in the heart
Pancuronium
These drugs strongly potentiate and prolong effect of neuromuscular blockers
Inhalation anesthetics (isoflurane), antibiotics (aminoglycosides, tetracyclines)
Depolarizing blocker that causes muscle relaxation and paralysis and can cause postoperative muscle pain
Succinylcholine
Two life-threatening side effects of succinylcholine
Hyperkalemia, malignant hyperthermia
Drug for treating malignant hyperthermia associated with drug-drug interaction between halogenated anesthetics and depolarizing blocker
Dantrolene
During Phase I depolarizing block this class of agents enhance muscle paralysis, but during Phase II block they may reverse muscle paralysis
Cholinesterase inhibitors
Drug of choice for reversal of non-depolarizing neuromuscular blockade
Neostigmine
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