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55 Cards in this Set
- Front
- Back
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Levodopa
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- DA precursor
- Metabolized via decarboxylation or O-methylation - Variable accumulation of catecholamines in different areas of the brain - Actions and SE result from metabolites - Rigidity and bradykinesia generally respond better and more promptly than tremor - SE: hypotension, nausea, vomiting, rrhea |
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Carbidopa
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- Peripheral (does not cross BBB) decarboxylase inhibitor
- Administered w/ L-dopa - Can be used to help reduce emesis sx. |
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Selegiline
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- MAOI (selective for MAO-B)
- Prevents metabolism of DA and preserves DA in the BG - Enhances therapeutic efficacy of L-dopa (dose and interval) - Advantage: does not cause potentiation of the effects of catecholamines when administered with sympathomimetic amine (or foods containing tyramine) - Prevents the appearance of MPTP induced Parkinsonism - SE: amphetamine metabolites |
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Rasagiline
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- MAOI (selective for MAO-B)
- Monotherapy tx. for Parkinson's or adjunct for L-dopa - No amphetamine metabolites (unlike selegiline) - Metabolized by CYP1A2 - SE: insomnia, hallucinations, orthostatic hyptotension, serotonin syndrome |
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Entacapone
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- COMT inhibitor (peripheral acting)
- Used in addition to L-dopa (increases F and effectiveness of dose) or carbidopa - Enhances "off" effect of Parkinson's sx. - SE: discoloration of urine, rrhea |
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Tolcapone
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- COMT inihibitor (central AND peripheral effects)
- SE: hepatotoxicity, increased DA stimulation, prolonged dyskinesias, psychotic sx. - Similar to entacapone, but more potent and longer duration |
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Pergolide
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- DA agonist
- Ergot derivative - Produces more unwanted SE than roprinirole and pramipexole; not readily used - Metabolized by P450; inhibits CYP3A4 - SE: nausea, peripheral edema and hypotension |
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Ropinirole
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- DA agonist (D3>D2 receptor)
- Used as monotherapy or w/L-dopa - Delays the onset of "off" periods - Rapid onset, long duration - Metabolized by CYP1A2, 3A4 - SE: excessive sedation, vivid dreams and hallucinations - Also used to tx. restless leg syndroms |
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Pramipexole
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- DA agonist
- D3>D2 receptor - Rapid onset, long duration - Used as a monotherapy (mild Parkinson's) or w/L-dopa - Secondary use = affective sx. - Neuroprotective (scavenges H202) and neurotrophic - SE: dizziness, orthostatic hypotension, drowsiness, hallucinations, twitching, twistinf, narcolepsy, compulsive gambling, hypersexuality, overearting |
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Amantadine
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- Antiviral (influenza A2)
- Used to treat L-dopa induced dyskinesias late in Parkinson's - MOA: may block release of excitatory NMDA receptors, especially those on cholinergic neurons that increase the release of ACh - Transient effects - SE: restlessness, depression, irritability, excitement, hallucinations and confusion |
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Bromocriptine
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- DA agonist
- Ergot derivative - Produces more unwanted SE than roprinirole and pramipexole; not readily used - SE: nausea, peripheral edema and hypotension |
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Trihexyphenidyl
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- Centrally acting antimuscarinic
- Qualitative resembles belladonna alkaloids - More effective at treating tremor than bradykinesia - MOA: modify the action of striatal cholinergic interneurons> influences interaction of direct and indirect pathway neurons - SE: anticholinergic sx., hallucinations, disorientation and delirium - Avoid in pts. w/BPH, GI obst., narrow-angle glaucoma |
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Benztropine
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- Centrally acting antimuscarinic
- Blocks DA reuptake > potentiates the action of L-dopa - SE: antimuscarinic SE and sedation |
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Morphine
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- Opioid analgesic
- Parenteral or oral relief - Metabolized by hepatic conjugation (undergoes first pass) - Primary effects mediated in CNS and gut via mu receptors - Absorbed from GI tract and rectal mucosa |
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Codeine
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- Opioid analgesic
- Undergoes little 1st pass metabolism; oral dose more effective than most other opioids - 10% of dose converted to morphine - Commonly used w/aspirin - Lower potential for abuse |
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Meperidine
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- Opioid analgesic
- Short duration of analgesia (take 1X4 hrs.) - Converted to a convulsant in liver - Less GI SE - Large increase in HR can be seen w/IV adm. - Contraindication = MAOI |
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Propoxyphene
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- Opioid analgesic
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Methadone
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- Opioid analgesic
- Mu agonist - Pharm. profile spectrum identical to morphine (abuse) - Similar potency, but kinetics altered due to plasma protein binding, which yields a longer t1/2 - Can be given at much wider intervals - More effective orally than morphine |
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Buprenorphine
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- Opioid analgesic
- Similar to morphine - 25-50X more potent as an analgesic - Partial mu agonist and kappa antagonist - Tx. for opiate or cocaine addiction? |
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Pentazocine
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- Agonist-antagonist
- Used primarily as an analgesic - Low doses > similar to morphine, but less potent - High doses > anxiety, nightmares, hallucinations - Less potential for abuse, but dependence and abstinence do occur (may precipitate withdrawal sx. in morphine dependent indiv.) - Partial mu antagonist, kappa and sigma agonist? - Use caution when prescribing to cardiac pts. - Formulated w/naloxone to reduce parenteral abuse |
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Diphenoxylate
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- Anti-diarrheal
- A phenylpiperidine - Very insoluble in aqu. solution - Adm. w/atropine (helps deter abuse) - No central effects at effective intestinal doses |
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Fentanyl
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- Opioid analgesic
- Lipophilic - Very potent (80X more than morphine) - IV as anesthetic agent w/droperidol (neuroleptic) - Transdermal patch - Accumulates in body w/cont'd dosing yielding unpredictable effcets - Related compounds used for spinal anesthesia and postoperative analgesia |
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Naloxone
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- Antagonist
- Adm. IV - Undergoes almost complete first pass metabolism - Potent antagonist at mu receptors - Higher doses required to reverse effects of agonist-antagonist opioids on delta and kappa receptors - Very little or no pain effects when adm. to a healthy, drug-free indiv. - Rapidly prod. withdrawal sx. in opioid dep. indiv. - Use: opioid OD; reversal of resp. depression (min.) |
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Dextrometorphan
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- Antitussive (non-opioid)
- D-isomer of codeine analog of levorphanol (L-isomer is a very potent opioid) - Does not prod. analgesia, resp. depressions, dependence, or withdrawal syndrome - Does provide cough suppression (equ. to codeine) - Contraindication: MAOIs |
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Halothane
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- Volatile anesthetic (halogenated hydrocarbon)
- No longer used much b/c of SE (more frequ. used in peds) - Poor analgesic - Highly potent and soluble > slow induction - SE: dose-dep. reduction in art. press and cardiac output, increased intracranial pressure, arrythmias, decreased resp. drive, hepatitis, malignant hyperthermia |
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Isoflurane
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- Volatile anesthetic (halogenated hydrocarbon)
- Musc. relaxant - Airway irritant (more often used for maintenance of anesthesia than induction due to pungent odor) - Higher MAC (lower sol.) than halothane > more rapid induction and recovery - SE: suppresses art. press. and depresses ventilation, incr. cerebral blood flow |
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Enflurane
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- Volatile anesthetic (halogenated hydrocarbon)
- Muscle relaxant - SE: hypotension and respr. depression, increases cerebral blood flow |
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Desflurane
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- Volatile anesthetic (halogenated hydrocarbon)
- Muscle relaxant - Rapid induction - SE: suppresses cardiovascular function, depresses respiratory function and increases cerebral blood flow |
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Sevoflurane
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- Volatile anesthetic (halogenated hydrocarbon)
- Rapid induction and recovery - Not irritating to the airways - Suppresses cardiovascular function, depresses respiratory function, increases cerebral blood flow |
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Nitrous Oxide
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- Volatile anesthetic (halogenated hydrocarbon)
- Poor muscle relaxant - Good analgesic - Cannot induce anesthesia alone w/out hyperbaric cond. - Very insoluble > rapid induction; use w/other vol. anesthetics to induce more rapidly ("second gas effect") - Adm. O2 during cessation to avoid diffusional hypoxia - SE: increases cerebral blood flow/intracranial pressure, neg. inotropic effect on heart, but no cardiovasc. depression |
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Xenon
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- Volatile anesthetic (halogenated hydrocarbon)
- Inert gas - Not avail. in US > $$$ ("perfect anesthetic" - Rapid induction and emergence - No effect on CV or resp. system, no hepatic or renal toxicity |
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Propofol
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- IV anesthetic (incr. TI, reversible, no alveolar barrier)
- Weak analgesic - $ - Rapid induction, awakening > short duration of action (min.) - SE: painful injection (use lg. veins), histamine rel. (rash), severe hypoTN, inhibits resp. activity, blunts chemoreceptor responses to hypercapnia (induces apnea) |
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Etomidate
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- IV anesthetic (incr. TI, reversible, no alveolar barrier)
- Non-barbiturate anesthetic (GABAa effect) - Rapid induction and recovery (short procedures) - Little effect on CV system (except in hypovol. pts.) - SE: pain on injection, invol. muscle movements, postop. nausea and emesis, suppresses adrenocortical function, convulsant (in some pts.) |
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Ketamine
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- IV anesthetic (incr. TI, reversible, no alveolar barrier)
- Dissociative anesthetic (NMDA antagonist)- dissociation btw. thalamus and limbic cortex - Sx: cataleptic state w/nystagmus, hypertonicity and skel. musc. responses, amnesia - Does not induce sleep - Potent analgesic - SE: hypertonicity may result in seizures, stim. CV system, increases cerebral blood flow and ICP, emergent delirium (pseudohallucinations and vivid dreams), resp. depression is less than with most anesthetics, incr. resp. secretions > tx. w/tropane alkaloids - Psych. sx reduced in peds. pts. - Causes bronchodilation > use in asthmatics |
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Neuroletanesthesia
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- IV anesthetic
- Short-lasting - Used in pts. who are esp. sensitive to general anesthesia (i.e geriatrics) - Combo of an opioid and neuroleptic agent (i.e. fentanyl and droperidol) - Sometimes supplemented w/low dose of general anesthetic (greatly reduced chance for adverse effects) |
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Barbiturates
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- Adjunct agent
- Gen. not used as an anesthetic; more often as adjuncts - GABAa facilitation - Rapid onset and recovery - Weak analgesic - Low TI - Common ex: thiopental (lethal injection), thiamylal, methohexital - SE: Arrythmias, CV and resp. depression |
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Dexmedetomidine
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- Adjunct agent
- Acts on imidazoline receptors - Sedation and analgesia; not anesthesia - Poor amnesia - Nausea and dry mouth - SE: decr. in arterial pressure, little resp. depression |
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Analgesics
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- Adjunct agent
- Commonly administered w/most anesthetics part. to assist on post-op recovery - Reduces amt. of gen anesthesia required - SE: resp. and CV depression, opioid-like effects - Common ex: fentanyl, sulfentanil, alfentanil, meperidine, morphine |
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Tranquilizers
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- Adjunct agent
- The "pams" - Common to tranquilize pts. before induction of anesthesia (part. w/irritating agents) - SE: CV and resp. depression are pretty negligible |
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Muscle relaxants
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- Adjunct agent
- Advisable to reduce musc. twitches and other motor activity, anesthetic- induced hypertonicity, or for intubation - SE: malignant hyperthermia (tx. w/neostigmine or erdrophonium) - Common ex: succinylcholine (depol.), pancuroinum (non-depol) |
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Cocaine
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- Ester (broken down fairly quickly)
- Only naturally occurring local anesthetic - Monoamine (NE, epi, DA, serotonin) reuptake inihibition. This contrasts w/amphetamines, which stimulate rel. of DA - CNS: central depression can follow and death is due to rep. failure or vent. arrythmias after high doses - Synpathomimetic: activ. of CNS sympathoexcitation - Topical use in upper resp. passages - SE: seizures and hyperthermia |
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Procaine
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- Ester (broken down fairly quickly)
- Low potency, slow onset and short duration of action - Rarely used today except for infiltration and spinal anesthesia |
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Tetracaine
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- Ester (exceptionally longer lasting due to difficulty in metabolizing)
- Long-lasting and more potent than procaine - Used for topical, spinal and opthalmalogical anesthesia |
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Chloroprocaine
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- Ester (broken down fairly quickly)
- Short-acting w/a rapid onset |
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Benzocaine
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- Ester (exceptionally longer lasting)
- Prolonged surface anesthesia - Very low sol. in water; low pKa (~3.5) means it does not bind to Na receptor very well (does get across membrane) - Topical use |
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Lidocaine
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- Amide (longer lasting due to hepatic metabolism)
- Most widely used of local anesthetics - Gen. more useful tha procaine b/c it can be used for infiltration and surface anesthesia - Vasoconstrictive properties - Least potent of amides |
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Prilocaine
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- Amide (longer lasting due to hepatic metabolism)
- Used in topical cream mixed w/lidocaine - SE: methemoglobinemia (rapidly rev.) |
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Mepivicaine
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- Amide (longer lasting due to hepatic metabolism)
- Properties similar to lidocaine; more rapid onset and more prolonged effect - Used for infiltration, epidural and nerve block anesthesia |
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Bupivicaine
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- Amide (longer lasting due to hepatic metabolism)
- Potent injectable agent w/a long duration of action - More cardiotoxic than lidocaine > arrythmias - Myocardial depr. due to prolonged blockade of Na channels - Used for infiltration, nerve block, spinal and epidural adm. Use @ sites where you don't expect uptake into bloodstream - Convulsion in peds. w/prolonged eposure |
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Ropivacaine
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- Amide
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Ropivacaine
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- Amide
- Slightly less potent than bupiviacaine; less likely to prod. cardiotoxicity - Used for epidural and regional anesthesia |
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Etidocaine
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- Amide
- Action is longer than lidocaine - Used for infiltration and nerve block - SE: cardiac toxicity |
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Dibucaine
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- Amide
- Highly potent w/ long lasting effects - Only used topically |
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Tetrodotoxin
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- Toxin
- Puffer fish toxin - Blocks Na channels prod. a long lasting anesthesia - Highly toxic and not used clinically |
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Saxitoxin
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- Toxin
- Highly toxic and long lasting - Produced by dinoflagellates consumed by shellfish and clams |
