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Analgesics & Muscle Relaxants

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Question
Answer
Analgesics   Pain Killers (Decreases sensation of pain - sense of relief & well-being)  
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Pain   unsatisfactory feeling that makes an emotional drive  
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Opiod receptors   5; Mu (2 subclasses), Kappa, Delta  
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Number of pain pathways from periphery to brain   50  
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Sedation   Affects higher cortical function. (Lead to coma or general anesthesia)  
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Dextromethorphan SE   suppresses cough reflex  
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Morphine Classification   CII  
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Morphine is derived from...   Opium Poppy  
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Opiods   morphine-like substance  
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Narcotics   Opiods & those that induce narcosis  
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Morphine(Avinza, Kadian, MSContin, Duramorph)site of action   spinal cord, midbrain, thalamus, cortex (depresses nocioceptive spinal reflexes in dorsal horn)  
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Morphine (Avinza, Kadian, MSContin, Duramorph) neurotransmitters   Cholinergic, adrenergic, serotonergic, dopaminergic  
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Morphine (Avinza, Kadian, MSContin, Duramorph) onset   Quick: peaks 30-40 minutes after administration  
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Propoxyphene   Darvocet, Darvon  
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Morphine   Avinza, Kadian, MSContin, Duramorph  
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Propoxyphene (Darvocet, Darvon) pain use   mild to mod  
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Propoxyphene (Darvocet, Darvon) Class   CV  
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Propoxyphene (Darvocet, Darvon) SE   Acute & chronic Toxicity, convulsions (difficult to treat)  
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Propoxyphene (Darvocet, Darvon) DI   Increase toxic effects with muscle relaxants & CNS depressants  
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Propoxyphene (Darvocet, Darvon) overdose   Most fatal OD in US b/c it extremely lowers the Sz. threshold. 2nd most common drug cause of death.  
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Meperidine   Demerol  
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Meperidine (Demerol) pain use   mod-severe; perioperative  
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Meperidine (Demerol) vs Morphine   1/6 potency. No pupillary constriction or cough suppression. Less smooth muscle effects  
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Meperidine (Demerol) metabolized by   Liver  
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Meperidine (Demerol) SE   CNS excitation - high doses (Tremor, muscle twitches, Szs.) & Respiratory suppression  
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Meperidine (Demerol) Class   CII  
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Opiates SE   Analgesia, Antianxiety, euphoria, sedation, respiratory depression, depression of cough reflex, pupillary constriction, N/V,endocrine effects (Increases ADH, corticotropin, PRL, GH, gonadotrophic hormones), edema, flushing, orthostasis, constipation,itch  
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Hydromorphone   Dilaudid  
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Hydromorphone (Dilaudid) class   CII  
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Hydromorphone (Dilaudid) Duration   Short Acting  
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Hydromorphone (Dilaudid) SE   Same as Morphine  
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Hydromorphone (Dilaudid) Potency   High w/ IM  
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Fentanyl   Actiq, Duragesic, Fentora  
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Fentanyl (Actiq, Duragesic, Fentora) Class   CII  
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Fentanyl (Actiq, Duragesic, Fentora) Onset   Rapid  
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Fentanyl (Actiq, Duragesic, Fentora) Duration   Short  
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Fentanyl (Actiq, Duragesic, Fentora) Form   No PO b/c doesnt go through the gut b/c its greater lipid soluble)  
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Fentanyl (Actiq, Duragesic, Fentora) SE   Respiratory depression/Apnea (high risk), skeletal muscle rigidity, moderate bradycardia  
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Oxycodone   Oxycontin, Roxicodone, Percocet, Roxicet, Percodan  
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Oxycodone (Oxycontin, Roxicodone, Percocet, Roxicet, Percodan) SE   Fewer than Codeine - more tolerable  
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Oxycodone (Oxycontin, Roxicodone, Percocet, Roxicet, Percodan) vs morphine   slightly higher potency than morphine  
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Oxycodone (Oxycontin, Roxicodone, Percocet, Roxicet, Percodan) Class   CII  
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Oxymorphone   Opana  
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Oxymorphone (Opana) class   CII  
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Oxymorphone (Opana) efficacy   Questionable  
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Oxymorphone (Opana) similar to...   Oxycodone  
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Hydrocodone   Lortab, Lorcet, Vicodin, Vicodin ES, Zydone, Norco  
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Hydrocodone (Lortab, Lorcet, Vicodin, Vicodin ES, Zydone, Norco) abuse   Must abused drug in US  
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Hydrocodone (Lortab, Lorcet, Vicodin, Vicodin ES, Zydone, Norco) similarities   Oxycodone except less euphoria  
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Hydrocodone (Lortab, Lorcet, Vicodin, Vicodin ES, Zydone, Norco) combination   Combined with acetominophen (Be careful of acetominophen toxicity)  
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Hydrocodone (Lortab, Lorcet, Vicodin, Vicodin ES, Zydone, Norco) Class   CIV  
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Codeine SE   Same as morphine  
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Codeine Pain Use   Mild to moderate  
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Codeine Combinations   Aspirin/Acetominophen (CIV) & Pure (CII)  
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Codeine Class   Pure-CII or Combined with Aspirin/Acetominophen (CIV)  
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Nalorphine type of drug   First known morphine antagonist (proof that antagonist are analgesic with less abuse potential)  
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Pentazocin   Talacen, Talwin, Talwin NX  
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Pentazocin (Talacen, Talwin, Talwin NX) Class   CIV  
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Pentazocin (Talacen, Talwin, Talwin NX) type of drug   Kappa receptor agonist & mu receptor antagonist  
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Pentazocin (Talacen, Talwin, Talwin NX) SE   No ADH effect, less GI effects, lowers seizure threshhold, N/V, dysphoria, hallucinations & confusion  
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Nalbuphine   Nubain  
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Nalbuphine (Nubain) class   CII  
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Nalbuphine (Nubain) vs morphine   Equal potency & duration of morphine  
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Nalbuphine (Nubain) type of drug   Mu antagonist and kappa agonist  
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Nalbuphine (Nubain) SE   Less respiratory suppression  
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Butorphanol   Stadol  
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Butorphanol (Stadol) class   CIV  
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Butorphanol (Stadol) type of drug   Potent kappa agonist  
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Butorphanol (Stadol) onset   quick in nasal form  
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Butorphanol (Stadol) abuse potential   High abuse potential  
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Tramadol   Ultram, Ultracet  
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Tramadol (Ultram, Ultracet) type of drug   Mu antagonist, kappa agonist, 5HT-ag  
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Tramadol (Ultram, Ultracet) SE   Sedation, less GI effects, abuse potential, seizures  
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Kertorolac   Toradol  
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Kertorolac (Toradol) type of drug   prostaglandin inhibitor (NSAID)  
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Kertorolac (Toradol) use   Mild to moderate pain - short term  
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Kertorolac (Toradol) vs Codeine   Similar potency  
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Kertorolac (Toradol) CI   Perioperative and obstetrics (premature closure of the PAD in the baby)  
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Naloxone   Narcan  
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Naloxone (Narcan) type of drug   mu, delta, and kappa antagonist  
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Naloxone (Narcan) SE   Opposite of opiates: euphoria, analgesia, mental clouding, respiratory depression, severe withdrawl Sx.  
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Naloxone (Narcan) Half-life   Short (10 minutes)  
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Acetaminophen type of drug   non-prostaglandin synthetase  
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Acetaminophen metabolized & excreted   Liver & Kidney  
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Acetaminophen vs aspirin   Analgesic activity equivalent to aspirin  
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Acetaminophen use   Reduces opiate dose  
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Methadone   Dolophine  
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Methadone (Dolophine) half-life   Long; withdrawl lasts for months  
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Methadone (Dolophine) Class   CII  
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Nucynta type of drug   Dual-action pain inhibition (ascending; mu-opiate agonist. Descending; Inhibits NE reuptake)  
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Nucynta CI   Patients at risk for respiratry depression and MAOIs  
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Tolerance   phenomenon where an organism chronically exposed to a substance becomes progressively less sensitive to it (need higher dose to achieve equal effects)  
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Dependence   Withdrawl syndrome upon cessation of a substance  
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Drugs that reduce opiate use   Antidepressants, anticonvulsants, NSAIDs, Topical/local agents, Muscle relaxants & Antihistamines  
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Muscle spasticity   UMN dz. which relates to the tone of the muscle  
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Muscle spasm   Localized in1 muscle body  
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Dantrolene   Dantrium  
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Dantrolene (Dantrium) Tx use   CP, MNS, malignant hyperthermia  
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Dantrolene (Dantrium) SE   Drowsiness, dizziness, weakness,liver toxicity (chronic), pleural effusion (Chronic)  
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Methocarbamole   Robaxin  
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Methocarbamole (Robaxin) physiology   Depresses muscle spindle affarent activity (spinal cord level)  
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Methocarbamole (Robaxin) Tx for...   Acute muscle spasm, back pain, sprain/strains  
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Methocarbamole (Robaxin) SE   Drowsiness, ataxia & coma (high doses)  
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Diazepam   Valium  
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Diazepam (Valium) physiology   Presynaptic inhibition of motor neuron in spinal cord (increases GABA)  
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Baclofen   Lioresal  
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Baclofen (Lioresal) physiology   Reduces excitatory synaptic influences of motor neuron at spinal and supraspinal level. (blocks asparate and glutamate)  
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Baclofen (Lioresal) Tx.   Chronic muscle spasm, spasticity of MS & spinal cord injury  
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Baclofen (Lioresal) SE   Hyperglycemia  
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Cyclobenzaprine   Flexeril, Amrix  
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Cyclobenzaprine (Flexeril, Amrix) physiology   Acts in midbrain & spinal cord level  
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Cyclobenzaprine (Flexeril, Amrix) Tx.   Spinal cord damage due to ischemia  
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Cyclobenzaprine (Flexeril, Amrix) SE   Very sedating, dry mouth, fatigue, mental confusion  
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Carisoprodol (SOMA) physiology   Blocks interneuron action similar to methocarbamol (less selective); metabolized to sedative with little muscle relaxant.  
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Carisoprodol (SOMA) SE   Very sedating  
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Tizanidine   Zanaflex  
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Tizanidine (Zanaflex) physiology   Alpha agonist; acts in spinal cord  
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Tizanidine (Zanaflex) Tx. for...   Chronic muscular pain, spasticity or MS-related spasticity  
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Tizanidine (Zanaflex) monitor   LFTs  
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Tizanidine (Zanaflex) SE   Sedating (less with given food)  
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Orphenadrine   Norflex  
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Orphenadrine (Norflex) physiology   Acts supraspinally to decrease rigidty  
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Orphenadrine (Norflex) SE   Anticholinergic SE  
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Orphenadrine (Norflex) Tx   Strain, Spain, Low back injury  
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Cholpromazine   Thorazine  
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Cholpromazine (Thorazine) physiology   Depresses system btwn cerebellar & midbrain areas  
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Metaxalone   Skelaxin  
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Metaxalone (Skelaxin) physiology   Similar to methocarbamol  
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Metaxalone (Skelaxin) SE   Least sedating  
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Chlorzoxazone   Parafon Forte  
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Chlorzoxazone (Parafon Forte) physiology   Smooth muscle relaxant  
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