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