Analgesics

Classification

Analgesics

Opioids/Narcotics Nonopioids or
Nonsteroidal
(NSAIDs)

Definition: Analgesics are drugs that selectively inhibit the perception “sensation”
of pain.
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs(
Pharmacologic Action:
• Analgesic, antipyretic, Anti-inflammatory.
• Most of them inhibit platelet aggregation – prolong bleeding time
- Aspirin is the strongest antiplatelet aggregation
Mechanism of action:
They inhibit cyclooxygenase enzyme.
They are classified into:
A. Non-selective COX Inhibitors:
Include: acetylsalicylic acid (aspirin), ibuprofen, diclofenac, mefenamic acid.
B. Selective COX-2 Inhibitors: Celecoxib, Rofecoxib, Valdecoxib.
Clinical uses:
• Analgesic in headache, toothache and common cold.
• Antipyretic.
• Ant-inflammatory in rheumatoid arthritis.
• Aspirin in small dose used as anti-thrombotic in angina and
myocardial infarction.
Side effects:
 Nausea, vomiting and ulceration.
 Bleeding.
 Hypersensitivity reaction.
 Aspirin causes “Reye's syndrome” in children > 6 years old.
Contraindication:
• Peptic ulcer.
• Allergy.
• Bronchial asthma.
• Renal disease.
• Bleeding tendency (aspirin)
• Aspirin is contraindicated in infant and children < 6 years “Reye's syndrome”
(hyperpyrexia, acidosis, seizures, vomiting, psichiatric disorders, hepatopathy)
Paracetamol:
 Antipyretic analgesic.
 No anti-inflammatory.
 No peptic ulcer.
 No bleeding.
Safe in:
• Children.
• Bronchial asthma.
• Peptic ulcer
• Pregnancy.
Hepatotoxicity: Toxic dose cause hepatic failure. Antidote Acetylcysteine
 Narcotic (Opioids) Analgesics
• Narcotic Analgesics are natural or synthetic substances.
• They have many receptor.
Mechanism of action:
1. Inhibit the nerve cell decrease release of excitatory neurotransmitters.
2. Decrease the release of substance –P.
Include:
 Morphine, pethidine, fentanyl, alfentanil, codeine, tramadol: Analgesics
Dextromethorphan: used as antitussive (cough syrup)
 Diphenoxylate, loperamide: used to treat diarrhea.
Therapeutic uses:
o Analgesic in severe pain e.g., postoperative, cancer, fracture and
myocardial infarction.
o Preanesthetic medication.
o Relief of cough (Dextromethorphan)
o Treatment of diarrhea (Diphenoxylate, loperamide)
Adverse effects:
Respiratory depression, constipation, vomiting, urinary retention,
hypotension, tolerance and dependence (has withdrawal symptoms).
Contraindications:
o Acute respiratory disease (bronchial asthma): it causes depression of
respiratory center and increase of histamine.
o Head injury: it increase intracranial pressure.
o Paralytic ileus: as it causes constipation due to decrease intestinal
peristalsis.
o Benign prostatic hyperplasia (BPH): as it causes urine retention.
o Pregnancy and Labour.
Opioid Antidote: Naloxone.
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