Analgesic & Antimigraine

Butorphanol Dihydroergotamine Fentanyl Meperidine Methadone Morphine Naloxone Propoxyphene Sumatriptan Tramadol .

dependence than full µ receptor agonists Dysphoria Nightmares w/drawal in pts dependent on full opioid agonists AVOID MAOI Potentially fatal . constipation.Butorphanol Opioid analgesic Mixed opioid agonist-antagonist Partial agonist or antagonist @ opioid µ receptors Agonist @ κ receptors @ spinal & supraspinal sites Inhibits spinothalamic pain neurotransmission Moderate-severe pain Admin intranasally ↓ respiratory depression.

V Stiff neck. shoulder.Dihydroergotamine Antimigraine Ergot alkaloid 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors Pial & dural vessel constriction N. extremities Leg weakness Numbness & tingling in fingers & toes Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons Vascular HA Migraine & cluster Injection or nasal spray .

V Constipation AVOID MAOI in past 14d .Fentanyl Opioid analgesic Phenylpiperidine Activates opioid µ receptors Inhibits pain transmission @ spinal & supraspinal sites Chronic pain Breakthrough for cancer pain Transdermal patch Sedation Confusion Respiratory depression Anorexia N.

Meperidine Opioid analgesic Strong opioid agonist Activates opioid receptors Inhibits pain transmission Generalized CNS depression Moderate-severe pain Analgesia during labor Preoperative sedation Lacks antitussive activity Confusion Sedation Constipation N. tremors AVOID MAOI Potentially fatal . convulsions. V Dependence Toxic metabolite CNS excitation.

once per day AVOID MAOI Respiratory depression Constipation Confusion Sedation .Methadone Opioid analgesic Strong opioid agonist Activates opioid receptors Inhibits pain transmission Suppresses opioid w/drawl Sx w/ euphoria or dependence Moderate-severe pain Prevention of opioid abuse Orally.

Morphine Opioid analgesic Strong opioid µ receptor agonist Activates µ receptors ↑ cAMP Opens K & closes Ca channels ↓ release substance P Sedation Confusion Hypotension Constipation Respiratory depression AVOID MAOI w/ 14 d Potentially fata Inhibits pain @ spinal & supraspinal sites Severe pain w/ MI Pulmonary edema Active metabolite Morphine glucuronate .

κ receptors Rapidly reverses effects of opioid agonists Opioid OD.Naloxone Opioid antagonist Opioid receptor antagonist Blocks opioid µ. dependence Short half-life needs repeated doses . δ.

Propoxyphene Opioid analgesic Weak opioid agonist Activates opioid receptors Inhibits pain transmission Mid-moderate pain Combined w/ acetaminophen or aspirin Dizziness Weakness N dependence .

Sumatriptan Antimigraine 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors Pial & dural vessel constriction Dizziness Vertigo Tingling Warm sensation Tight feeling head & chest Coronary vasospasm AVOID MAOI SSRI Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons Vascular HA Migraine & cluster Oral. & subQ . nasal.

Tramadol Analgesic Dual action Activates µ opioid receptors Inhibits neuronal reuptake 5HT & NE ↑ inhibition of pain Moderate pain Chronic pain Naloxone reverses some but NOT all Sx Dizziness HA Constipation Lowers seizure threshold AVOID MAOI ↑ risk seizures w/ high doses Penicillins Phenothiazines .

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