問題一覧
1
Non opioid
2
Opioid
3
• Most widely used • Frequently prescribed • Often taken without prescription • More than 50 • Have significant unwanted effects • Newer agents have fewer and less serious adverse action
Non-steroidal Anti-inflammatory Drugs
4
• Enzymes that produce PGs 🡪 promote inflammation, pain and fever.
Cyclooxygenase enzymes
5
• 3 major types of effect: ◦ Anti-inflammatory effects • Analgesic effect • Antipyretic effect ◦ Inhibition of arachidonate cyclooxygenase thus inhibition of the production of PGs and TXA2
Non-steroidal Anti-inflammatory Drugs
6
• Others: ◦ Inhibit platelet aggregation except selective COX 2 inhibitors • Gastric irritants • Nephrotoxicity • Hepatotoxicity • Hypertensive complications
Non-steroidal Anti-inflammatory Drugs
7
NSAIDs: Pharmacokinetics Weak organic acid, except
Nabumetone
8
NSAIDs: Pharmacokinetics food does not change their bioavailability, except
Fenoprofen & Piroxicam
9
NSAIDs: Pharmacokinetics Highly protein bound (95% - 99%):
Albumin
10
(Aspirin, Na salicylate, choline Mg++ trisalicylate, salsalate, diflunisal, sulfasalazine)
Salicylic acid derivatives
11
(Indomethacin, Sulindac)
Para-chlorobenzoic acid derivatives or indoles
12
(Phenylbutazone, Azapropazone)
Pyrazolone derivatives
13
(Ibuprofen, Flurbiprofen, Ketoprofen, Fenoprofen, Naproxen, Oxaprozin)
Arylpropionic acid
14
(Mefenamic Acid, Meclofenamic acid)
Fenamates/Anthranilic acids
15
(Piroxicam, Tenoxicam)
Enolic acids/Oxicams
16
(Diclofenac Sodium, Tolmetin, ketorolac)
Heteroaryl/Phenylacetic acids
17
(Nabumetone)
Alkalones
18
Aspirin
19
Pharmacokinetics aspirin
20
Pharmacodynamics aspirin
21
Aspirin unwanted effects 4
Gastric upset, Increases uric acid levels, Glucose intolerance , Salicylism
22
4 Aspirin drug interactions
Warfarin, Spirinolactone, Penicillin, ACE inhibitors
23
2 Aspirin Contraindications
Hemophilia, Gastric & duodenal ulcers
24
Diflunisal
25
Selective COX-2 Inhibitors
26
Paracetamol unwanted effects
27
Paracetamol
28
Corticosteroid drugs
29
DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDS)
30
Colchicine
31
Probenecid & Sulfinpyrazone
32
• Reduce uric acid synthesis by inhibiting xanthine oxidase and increasing uric acid excretion • Absorption: 80%, oral & • Terminal serum t1/2 of 1-2 hours • Given o.d. • Indications: chronic tophaceous gout, uric acid urine (24hrs) > 600-700mg, allergic reactions to probenecid & sulfinyrazone, renal impairment, grossly elevated serum uric acid levels • AE: N/V, diarrhea, peripheral neuritis, necrotizing vasculitis, BM depression, aplastic anemia, hepatic toxicity, interstitial nephritis, allergic skin reaction, cataracts
ALLOPURINOL
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Febuxostat
34
Febuxostat pharmacodynamics
35
Pegloticase
36
Adverse effects Pegloticase
37
Mixed agonist antagonist
38
Nalbuphine mu
Antagonist
39
Nalbuphine kappa
Agonist
40
Naltrexone, Naloxone
Opioid antagonist
41
Opioid antagonist
42
Opioid antagonist
43
Pure agonists
44
Pure agonists
45
Pure agonists
46
Partial/Weak agonist
47
Partial/Weak agonist
48
Kappa
49
Dynorphins
50
Spinal analgesia
K1
51
Supraspinal analgesia
K3
52
Delta
53
associated with supraspinal analgesia
U1
54
sub-serves spinal analgesia, respiratory depression, and gastrointestinal actions
U2
55
• Morphine and other similar pure agonists have greater affinity (CNS and PNS) • ß-endorphines and enkephalins
Mu
56
Opioid Analgesics & Antagonists
57
Opioid Analgesics & Antagonists
58
Opioid Analgesics & Antagonists
59
Opioid Analgesics & Antagonists
60
Opioid Analgesics & Antagonists
61
Interleukin-1 Inhibitors
62
Interleukin-1 Inhibitors
63
• a fully human anti-IL-1ß monoclonal antibody 🡪 provides rapid and sustained pain relief ◦ Dose: 150mg SC
Canakinumab
64
Non-opioid (Nonsteroidal Anti-inflammatory Drugs – NSAIDs) 3
Non-selective COX inhibitors, Selective COX-2 inhibitors, Selective COX-3 inhibitor
65
Opioid (Narcotic analgesics) 4
Pure Agonists, Partial/Weak agonist, Mixed agonist-antagonists, Opioid antagonist
66
Folic antagonist
Methotrexate
67
4.5 days half life Injection site reactions
Etanercept
68
IV infusion nausea, headache, sinusitis, rash
Infliximab
69
CD20 B lymphocytes
Rituximab
70
CD28 to CD80
Abatacept
71
15 minutes IV IM
Parecoxib