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Advanced Pharmacology Study Guide (NP Level)
1. Drugs for Muscle Spasm and Spasticity
Muscle Spasms
Acute, involuntary muscle contractions due to injury or strain.
Common Agents:
• Cyclobenzaprine (Flexeril) – TCA-like structure; reduces tonic somatic motor activity
• Methocarbamol (Robaxin) – CNS depressant
• Carisoprodol (Soma) – High abuse potential; metabolized to meprobamate
Key Notes:
• Sedating
• Avoid alcohol or CNS depressants
• Caution in elderly
Spasticity
Chronic hypertonia from CNS injury (e.g., MS, CP, spinal cord injury).
Common Agents:
• Baclofen – GABA-B agonist; reduces excitatory neurotransmission
• Tizanidine – Alpha-2 adrenergic agonist; centrally acting
• Diazepam – Benzodiazepine; enhances GABA-A inhibition
• Dantrolene – Direct skeletal muscle relaxant; blocks Ca²⁺ release (used in malignant
hyperthermia)
Key Notes:
• Baclofen: risk of withdrawal seizures
• Tizanidine: hypotension, dry mouth
• Dantrolene: hepatotoxicity
, 2. Opioid Analgesics
Used for moderate to severe pain. Bind to mu, kappa, and delta opioid receptors.
Common Opioids:
• Morphine – Standard; causes histamine release (itching, hypotension)
• Hydromorphone (Dilaudid) – More potent than morphine
• Fentanyl – Very potent; patch for chronic pain
• Oxycodone, Hydrocodone – Often combined with acetaminophen
• Codeine – Prodrug; metabolized to morphine (watch for CYP2D6 variability)
• Methadone – Long half-life; QT prolongation risk
• Meperidine – Risk of seizures (normeperidine metabolite)
Adverse Effects:
• Respiratory depression
• Constipation
• Sedation
• Nausea/vomiting
• Tolerance, dependence, addiction
NP Prescribing Tips:
• Start low, go slow
• Use multimodal pain management
• Monitor for misuse (PDMP, contracts)
• Educate on naloxone availability
3. Opioid Antagonists
Used to reverse opioid effects or treat opioid use disorder.
Common Agents:
• Naloxone (Narcan) – IV/IN; short half-life; emergency reversal
• Naltrexone – PO/IM; long-acting; used for maintenance (OUD, alcohol use disorder)
• Methylnaltrexone – Peripherally acting; treats opioid-induced constipation without
reversing analgesia
Key Notes:
• Naloxone: may cause withdrawal symptoms
• Naltrexone: avoid in acute opioid dependence (can precipitate withdrawal)
• Monitor liver function with naltrexone
, 4. Non-Opioid Centrally Acting Analgesics
Work within the CNS but not through traditional opioid receptors.
Common Agents:
• Tramadol – Weak mu agonist; also inhibits reuptake of serotonin and norepinephrine
• Tapentadol – Stronger SNRI activity than tramadol
Adverse Effects:
• Seizures (esp. tramadol)
• Serotonin syndrome (esp. with SSRIs)
• Less respiratory depression than traditional opioids
Clinical Use:
• Moderate pain when NSAIDs are inadequate
• Good alternative in patients with high opioid misuse risk
5. Drugs for Headache
Migraine Treatment:
Acute (Abortive) Treatment:
• Triptans (sumatriptan, rizatriptan) – 5-HT1B/1D agonists; vasoconstriction and
inhibition of neuropeptide release
• NSAIDs – First-line for mild/moderate attacks
• Ergotamines – Rarely used; more side effects
• Antiemetics (metoclopramide, prochlorperazine) – For nausea
Preventive Treatment:
• Beta-blockers (propranolol)
• Anticonvulsants (topiramate, valproate)
• TCAs (amitriptyline)
• CGRP inhibitors (erenumab, fremanezumab) – Injectable monoclonal antibodies
• Botox – For chronic migraines
Tension Headaches:
• NSAIDs or acetaminophen
• TCAs if chronic