5 Opioid Ag Antag Flashcards
When pain is inhibited v augmented
Inhib: spinal neurons release gaba and glycine or descending pathway releases ne, 5-ht, and endorphins. Augmented by sensitization and wind up
Opioid moa
Binds to receptor, G protein activ, Adenylate cyc inhib/less camp, ca dec and k inc
Mu: ligand, cv resp, cns resp, gi
Endorphins, bradycardia, sedation/euphoria/prolactin/mild hypothermia. Nv, inc biliary p dec peristalsis
Delta receptor: ligand, se
Enkephalins, resp dep, urine ret, itching
Kappa: ligand, se
Dynorphin. Resp dep, sedation/dysphoria/halluc, miosis, diuresis. Antishivering
Mu 1, 2, 3 main differences
1: supraspinal/spinal analgesia, euphoria, bradycardia, less abuse potential. 2: spinal analgesia, resp dep, constip, dependence. Mu3: immune sup
Opioids most to least potent
Su, fent= remi, alfent, dilaudid, morphine, demerol
Early and late se of withdrawal
Early: sweat, insomnia, restless. Late: abd cramp and nv
S.s serotonin syndrome, drug to avoid
Demerol. Hyperthermia, mental status changes, hyperreflexia, sz, death
Mao inhibitors
Phenelzine, isocarbozadid, trancyclopromine
Opioids that cause histamine release
Demerol, morphine, codeine, oxycodone
Pka: highest, lowest
Demerol 8.5 alfentanil 6.5
Highest and lowest unionized percent
89% alfentanil, 7% demerol
Highest and lowest protein binding
Remi and sufentanil 93, morphine 35
Lowest and highest vd
Lowest remi 0.39 highest fentanyl 4
Things that dec opioid hyperalgesia
Ketamine and mag
Methadone moa
Mu agonist, nmda antag, Maoi inhib
What inc with opioid induced skel muscle rigidity
02 consump, PVR, ICP
Buprenorphine: moa, strength, reversal ability, features
Partial mu, greater than morphine, not reversed well. Long duration, can give transdermal
Nalbuphine: moa, analgesia strength, reversal ability, features
Kappa agonist mu antag, sim to morphine, reversible, doesnt inc bp or hr, useful if heart disease
Butorphanol: moa, analgesia strength, reversible, features
Kappa agonist weak mu antag. > than morphine, reversible. Can tx shivering and give intranasal
Narcan: dose, duration, metab
1-4 mcg/kg. 30-40 min. Liver, first pass metab
Narcan se
Pulm edema, tachycardia, dysrhythmias, sudden death, NG
Methylnaltrexone: type of drug, useful when
Quaternary, doesnt reverse resp dep, tx peripheral effects of opioids like constip
