Pain

71問 • 1年前

問題一覧

Non opioid

Opioid

• 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

• Enzymes that produce PGs 🡪 promote inflammation, pain and fever.

Cyclooxygenase enzymes

• 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

• Others: ◦ Inhibit platelet aggregation except selective COX 2 inhibitors • Gastric irritants • Nephrotoxicity • Hepatotoxicity • Hypertensive complications

Non-steroidal Anti-inflammatory Drugs

NSAIDs: Pharmacokinetics Weak organic acid, except

Nabumetone

NSAIDs: Pharmacokinetics food does not change their bioavailability, except

Fenoprofen & Piroxicam

NSAIDs: Pharmacokinetics Highly protein bound (95% - 99%):

Albumin

(Aspirin, Na salicylate, choline Mg++ trisalicylate, salsalate, diflunisal, sulfasalazine)

Salicylic acid derivatives

(Indomethacin, Sulindac)

Para-chlorobenzoic acid derivatives or indoles

(Phenylbutazone, Azapropazone)

Pyrazolone derivatives

(Ibuprofen, Flurbiprofen, Ketoprofen, Fenoprofen, Naproxen, Oxaprozin)

Arylpropionic acid

(Mefenamic Acid, Meclofenamic acid)

Fenamates/Anthranilic acids

(Piroxicam, Tenoxicam)

Enolic acids/Oxicams

(Diclofenac Sodium, Tolmetin, ketorolac)

Heteroaryl/Phenylacetic acids

(Nabumetone)

Alkalones

Aspirin

Pharmacokinetics aspirin

Pharmacodynamics aspirin

Aspirin unwanted effects 4

Gastric upset, Increases uric acid levels, Glucose intolerance, Salicylism

4 Aspirin drug interactions

Warfarin, Spirinolactone, Penicillin, ACE inhibitors

2 Aspirin Contraindications

Hemophilia, Gastric & duodenal ulcers

Diflunisal

Selective COX-2 Inhibitors

Paracetamol unwanted effects

Paracetamol

Corticosteroid drugs

DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDS)

Colchicine

Probenecid & Sulfinpyrazone

• 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

Febuxostat

Febuxostat pharmacodynamics

Pegloticase

Adverse effects Pegloticase

Mixed agonist antagonist

Nalbuphine mu

Antagonist

Nalbuphine kappa

Agonist

Naltrexone, Naloxone

Opioid antagonist

Pure agonists

Partial/Weak agonist

Kappa

Dynorphins

Spinal analgesia

Supraspinal analgesia

Delta

associated with supraspinal analgesia

sub-serves spinal analgesia, respiratory depression, and gastrointestinal actions

• Morphine and other similar pure agonists have greater affinity (CNS and PNS) • ß-endorphines and enkephalins

Opioid Analgesics & Antagonists

Interleukin-1 Inhibitors

• a fully human anti-IL-1ß monoclonal antibody 🡪 provides rapid and sustained pain relief ◦ Dose: 150mg SC

Canakinumab

Non-opioid (Nonsteroidal Anti-inflammatory Drugs – NSAIDs) 3

Non-selective COX inhibitors, Selective COX-2 inhibitors, Selective COX-3 inhibitor

Opioid (Narcotic analgesics) 4

Pure Agonists, Partial/Weak agonist, Mixed agonist-antagonists, Opioid antagonist

Folic antagonist

Methotrexate

4.5 days half life Injection site reactions

Etanercept

IV infusion nausea, headache, sinusitis, rash

Infliximab

CD20 B lymphocytes

Rituximab

CD28 to CD80

Abatacept

15 minutes IV IM

Parecoxib

Sporeformers

Tameyra Stefani Al-Suhairy · 44問 · 1年前

Sporeformers