Analgesics Flashcards

1
Q

NSAIDs: Mechanism of Action

A

Competitive COX 1 and COX-2 inhibitor

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2
Q

NSAIDs: Effects

A

Mild pain relief and anti-inflammatory

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3
Q

NSAIDs: Side Effects

A

Long term use in elderly particularly associated with iatrogenic morbidity and mortality

Major ADRs seen in stomach /GI tract - stomach pain, nausea, heartburn, gastric bleeding, ulceration

Renal ADRs occur in compromised individuals with HRH or hypovolaemia Heart failure Renal disease Hepatic cirrhosis, PGE2 and PGI2 maintain renal blood flow, If reduced by NSAIDs then GFR ↓ - further risk of renal compromise

Vascular
• Risk ↑ bleeding time ↑ bruising haemorrhage
Stevens Johnson Syndrome - Severe examples
• Immune-complex-mediated hypersensitivity disorder
• Compromised hepatic function
• Rash - skin mucous membranes

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4
Q

NSAIDs: Cautions

A

NSAIDs given in combination increase risk of ADRs. NSAIDs together can affect each others PK/PDs due to competition for plasma protein binding sites - many NSAIDs heavily bound - up to 90-99%
e.g. NSAIDs + low dose Aspirin – Compete for COX-1 binding sites - may interfere with cardioprotective action of Aspirin
↑Sulphonylurea - Hypoglycaemia
↑Warfarin – Increased Bleeding
↑Methotrexate – Wide ranging serious ADRs

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5
Q

NSAIDs: Drug Dose

A

Naproxen: 0.5–1 g daily in 1–2 divided doses.
Note: with food

Ibuprofen apply gel 3 times daily

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6
Q

Opioids (Codeine): Mechanism of Action

A

Bind to GPCRs
μ -outward flux of potassium decreses excitability
δ, k – Influx of calcium via channels decresed CAMP synthesis
inhibit the release of Substance P from nerve terminals.
Inhibitory descending pathways from higher centres in the brain.

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7
Q

Opioids (Codeine): Effects

A

Relief of moderate to severe pain

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8
Q

Opioids (Codeine): Side Effects

A

μ - nausea, vomiting constipation
drowsiness miosis
δ – respiratory depression (monitoring required) hypotension
k- dysphoria - pentazocine

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9
Q

Opioids (Codeine): Cautions

A

Overdose (treat with naloxone – opioid receptor antagonist)

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10
Q

Opioids (Codeine): Drug Dose

A

30–60 mg every 4 hours if required.

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11
Q

Paracetamol: Mechanism of Action

A

Weak COX-1 / COX-2 inhibitor weak inhibitor of synthesis of prostaglandins. analgesic effect of paracetamol is central and is due to activation of descending serotonergic pathways

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12
Q

Paracetamol: Effects

A

pain reflex and decrease pyrexia

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13
Q

Paracetamol: Side Effects

A

N&V

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14
Q

Paracetamol: Cautions

A

Single doses > 10 g (20 tablets) potentially fatal Start N-Acetylcysteine iv Methionine by mouth if NAC cannot be given promptly

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15
Q

Paracetamol: Drug Dose

A

max 4g per day - 1g QDS

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