Analgesic Drugs Flashcards
What class of drug is Ibuprofen (Nurofen, Advil, Herron Blue)?
NSAID (non-steroidal anti-inflammatory drug)
What class of drug is Aspirin (Solprin, Astrix)?
Anti-platelet analgesic
What class of drug is Paracetamol (Panadol, Panamax)?
Non-opioid analgesic
What class of drug is Celecoxib (Celebrex)?
NSAID (COX-2 selective inhibitor)
What class of drug is Diclofenac (Voltaren)?
NSAID (non-steroidal anti-inflammatory drug)
What class of drug is Indomethacin (Indocid)?
NSAID (non-steroidal anti-inflammatory drug)
What class of drug is Naproxen (Naprosyn)?
NSAID (non-steroidal anti-inflammatory drug)
What is the mechanism of action of Ibuprofen (Nurofen, Advil, Herron Blue)?
Inhibits prostaglandins (mediators of pain, inflammation and fever) by inhibiting cyclo-oxygenase (COX)
COX is the enzyme responsible for converting arachidonic acid to prostaglandin H2, which is then converted to other prostaglandins, causing pain. There are two isoforms of COX – COX-1 and COX-2
Ibuprofen is a non-selective inhibitor, meaning that it inhibits both COX-1 and COX-2
What is the mechanism of action of Aspirin (Solprin, Astrix)?
Irreversibly binds to COX-1 → prevents thromboxane A2 formation → reduced platelet aggregation
What is the mechanism of action of Paracetamol (Panadol, Panamax)?
Not fully determined.
Mechanisms involved in its analgesic effect may include inhibition of central prostaglandin synthesis and modulation of inhibitory descending serotonergic pathways.
The antipyretic effect is probably due to reduced production of prostaglandins in the hypothalamus.
Paracetamol has negligible anti-inflammatory effects.
What is the mechanism of action of Celecoxib (Celebrex)?
Have analgesic, antipyretic and anti-inflammatory actions
They inhibit synthesis of prostaglandins by inhibiting cyclo-oxygenase (COX). Inhibition of COX-2 results in anti-inflammatory and analgesic action
Although selective COX-2 inhibitors have little or no effect on COX-1 at therapeutic doses, they are still associated with GI adverse effects
What is the mechanism of action of Diclofenac (Voltaren)?
Primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is thought to be inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX)
It also appears to exhibit bacteriostatic activity by inhibiting bacterial DNA synthesis
Diclofenac has a low to moderate preference to block the COX2-isoenzyme (approximately 10-fold) and is said to have, therefore, a somewhat lower incidence of gastrointestinal complaints than noted with indomethacin and aspirin
What is the mechanism of action of Indomethacin (Indocid)?
Indomethacin is a nonselective inhibitor of cyclooxygenase (COX) 1 and 2. Prostaglandins cause uterine contractions in pregnant women.
As it inhibits COX and therefore PG synthesis, indomethacin is an effective tocolytic agent, able to delay premature labour by reducing uterine contractions
In addition, it inhibits motility of neutrophils and also uncouples oxidative phosphorylation in cartilaginous (and hepatic) mitochondria. These additional effects also account for the analgesic and the anti-inflammatory properties
What is the mechanism of action of Naproxen (Naprosyn)?
Naproxen works by reversibly inhibiting both the COX-1 and COX-2 enzymes
What are the side effects of Ibuprofen (Nurofen, Advil, Herron Blue)?
- Active peptic ulcer disease or GI bleeding
- Nausea
- Headaches
- Dizziness
- Problems with blood clotting – increased bleeding
- Fluid and salt retention
- Hypertension
- Diarrhoea
- Can increase bronchospasm (concern for asthmatics)
- IBD may worsen
- Renal impairment
