Analgesics - Drugs - Medbullets Step 2/3

Analgesic Drug Introduction
- Analgesic medications can be broken down into the following categories
  - antirheumatic agents
  - muscle relaxants
  - narcotic agonists
  - narcotic agonists-antagonists
  - narcotic antagonists
  - narcotic analgesic combo
  - NSAIDS
  - other analgesics

Analgesic Drug Table

Antirheumatic Agents
Name	Mechanism of Action	Key Indication	Key Toxicity
TNFα Inhibitors
Infliximab	Monoclonal antibody against TNF-alpha (infliximab, adalimumab, certolizumab) Decoy receptor for TNF-alpha (etanercept)	Disease modifying drug for Crohn's, psoriasis, rheumatoid arthritis, ankylosing spondylitis	Opportunistic infection, in particular mycobacterial infection due to TNF destabilization of granulomas
Adalimumab
Etanercept
Gold Preparations
Auranofin	Gold complex	Not commonly used	Gold toxicity Myelosuppression
Aurothioglucose	Gold complex	Not commonly used	Gold toxicity Myelosuppression
Other Antirheumatics
Cyclophosphamide	Alkylating agent - nitrogen mustard type	Hodgkin lymphoma Leukemia RA	Alkylating agent Hemorrhagic cystitis (treat with mesna) Myelosuppression
Azathioprine	Purine synthesis inhibitor	Renal transplant immunosuppresion Autoimmune disease	PTLPD Myelosuppression
Hydroxychloroquine	Lysosomal accumulation/inhibition	Malaria prophylaxi SLE RA	Can excacerbate G6PD deficiency
Methotrexate	Dihydrofolate reductase competitive inhibitor	RA Psoriasis Anti-folate chemotherapy Ectopic pregnancy	Must monitor pregnancy status, extremely toxic to fetus including neural tube defects
Muscle Relaxants
Carbamic Acid Esters
Methocarbamol	Mechanism unknown Potential carbonic anhydrase inhibition	Adjunct for tetanus, muscle spams	Ataxia Seizures
Carisoprodol	Mechanism unknown Central skeletal muscle relaxant	Muscle spams Musculoskeletal pain	Ataxia Seizures
Other
Baclofen	GABA_B receptor activation	Spasticity	CNS depression Respiratory depression
Cyclobenzaprine	Mechanism unkown Muscle relaxant	Muscle spasms	Contraindicated with MAOIs Heart block
Dantrolene	Binds ryanodine receptor Decreases calcium release from the sarcomplasmic reticulum	Neuroleptic malignant syndrome Malignant hyperthermia	Hepatotoxicity CNS depression
Metaxalone	Mechanism unkown CNS depression	Musculoskeletal pain	CNS depression
Orphenadrine	Ach receptor antagonism H₁ receptor blocker (antihistamine) NMDA receptor antagonist Norepinephrine reuptake inhibitor Na+ channel blocker K+ channel blocker	Discontinued in the U.S.	Anticholinergic effects
Tizanidine	Centralα2 agonist (G_icoupled)	Spasticity	Hypotension (α2 agonist)
Diazepam	GABA type A positive modulator	Anxiety Status epilepticus Alcohol withdrawal Seizures Sedative Muscle relaxant	Dependency Abuse potential
Narcotic Agonists
Alfentanil	Opioid analgesic (short acting)	Induction agent for general anesthesia	Respiratory depression Dependency Abuse potential
Codeine	Opioid (μ agonist)	Acute pain
Levorphanol
Oxymorphone
Hydromorphone
Morphine
Oxycodone
Meperidine		Acute pain Sedation
Dextropropoxyphene		Antitussive Mild pain Restless leg syndrome
Methadone	Very long acting opioid (μagonist)	Opioid dependence Chronic pain
Fentanyl	Very potent opioid (μ agonist)	Induction agent Chronic pain
Narcotic Agonists-Antagonists
Buprenorphine	Partial opioid receptor (μ) modulator	Moderate pain Opioid dependence	Respiratory depression Seizures Bradycardia
Butorphanol	Partial agonist/antagonist activity ofμreceptors Competitive antagonis of κ opioid receptors	Anesthesia induction	Seizures CNS depression Anticholinergic effects
Nalbuphine		Anesthesia induction	Seizures CNS depression Anticholinergic effects
Pentozocine	Agonist-antagonist at opioid (μ) receptor	Mild pain Opioid dependence	Hypertension Tachycardia
Buprenorphine/naloxone	Partial opioid receptor (μ) modulator (buprenorphine) μreceptor antagonist (naloxone)	Opioid dependence maintenance therapy	Seizures CNS depression Anticholinergic effects Opiod withdrawal if abused
Narcotic Antagonists
Naloxone	μreceptor antagonist	Acute opioid toxicity	Opioid withdrawal
Narcotic Analgesic Combo
Acetaminophen/oxycodone	μagonist + unknown mechanism of acetaminophen	Acute pain moderate	Respiratory depression Dependency Abuse potential
Acetaminophen/hydrocodone	μagonist + unknown mechanism of acetaminophen	Acute pain moderate	Respiratory depression Dependency Abuse potential
NSAIDS
Salicylates
Aspirin	Irreversible inhibitor of COX-1	Antiplatelet therapy for CAD Pain Antipyretic	Reye's Syndrome in children Tinnitus Mixed metabolic acidosis and respiratory alkalosis
Proprionic Acids
Ibuprofen	COX inhibitor	Mild pain	Gastritis NSAID nephropathy GI bleeding
Naproxen	COX inhibitor	Mild pain	Gastritis NSAID nephropathy GI bleeding
Acetic Acids
Ketorolac	COX inhibitor (competitive)	Mild pain	Gastritis NSAID nephropathy GI bleeding
Indomethicin	COX inhibitor	Patent ductus arteriosus Pain	Gastritis NSAID nephropathy GI bleeding
COX-2 Selective Inhibitors
Celecoxib	COX-2 inhibition	Osteoarthritis	Increased risk of MI, thrombosis in at-risk individuals
Other Analgesics
Acetominophen	Not well characterized	Antipyrretic Mild pain	Hepatotoxicity
Tramadol	Opioid agonist (μ)	Chronic, moderate-severe pain	Hepatotoxicity Seizures Withdrawal symptoms

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