Pharm 1 Final

enicozmo's version from 2015-12-07 01:20


Question Answer
What is a frequency dependent block?A nerve cell that is being stimulated repetitively will have increased opportunity to be blto beblock by local anesthetics. Incr. firing = incr. chances of beingblocked
Which local anesthetic will not be metabolized in CNS? WHY?Amino Ester linked local anestherics; Cerebral spinal fluid lal fluid lacks cholinesterase enzymes.
Procain has what potential rxn?Procaine--> amino ester linked local anaesthetic has PABA as a metabolite--> POTENTIAL ALLERGIC RXN
Signs of local anesthetic drug toxicity?severe CNS depression, possible resulting in respiratory depression and death
Bupivacaine and its toxicity?Dysrhythmia as a sign of CNS toxicity
Lodocaine is actually used to stabilize what?Ventricular dysrhythmia
What may be potential administered to treat bupivicaine toxicitylipid emulsion, intralipid
Amide linked local anesthetics not containing epinephrine can or cannot be autoclaved?CAN be, epi is light sensitive tho and cannot be autoclaved
Who is more toxic bupivacaine or lidocainebupivacaine
Lidocaine is also used as a ____ drug other than a local.anti-arrhythmia drug
Bupivacaine duration?Most long acting anesthetic drug
Levobupivacaine?S/Enantiomer form--> less toxic than bupivacaine
Benzocaine?used topically and for fish anesthesia
Benzodiazepines MOA? (seizure)GABA agonist modulatory (opens channel) not for status epiticulus ENHANCEMENT OF GABA-A activation--> INCR. FREQ. OF CHANNEL OPENING; drug of choice for seizures (emergency tcx &mtc)
Barbiturates MOA ? (seizure)stimulation of GABA; decr. RAS, incr. Cl- decr. Glutamate/NMDA--> Enhancement of GABA-A activation--> prolongs opening of the Cl channel (treatment of acute seizure/mtc therapy)
Phenobarbital side effects? (seizure)auto-induction of CYP450 enzyme in liver; sedation, polyphaagia/incr. appetite, PU/PD and hepatotoxicity
Potassium bromide?use (seizure)emergency tx of seizures and add on for seizure =mtC
Zonanisamide MOA?inhibition of Na+ and T-type Ca Channels; similar to Felbamate, free of major unwanted effects LONG PLASMA HALF-LIFE --> means less frequency of dosing
Fosphenytoin/Phenytoin MOA and effects?MOA--> use dependent block of sodium channels, fosphenytoin is converted to pheytoin CAUSES ENZYME INDUCTION (CYP450 enzyme induced)
Vigabatrin--> MOA and binding?Inhibition of the GABA metabolizing enzyme GABA-T; decr. metabolism & incr. GABA ,forms an irreversible covalent bound--> long acting
Cabamazepine metabolism? (TCA)Hepatic Metabolism, used as neuropathic pain, manic depression, anticonvulsant
3 drugs induce hepatic metabolism (more enzymes released)barbituates, cabamazepine, (FOS-) phenytoin
Descending inhibition is mediated mainly by what endogenous opiod peptides?serotonin (5-HT), NE, adenosine
Opioids CNS side effects?affects of opiods are seen the periphery HUMANS/DOGS--> depression HORSE/CATS--> excitation
Opioid effect on respiration and GIT?does dependent respiratory depression GIT-->incr. sphincter tonus= constipation
Methadone selectivity and receptors (opioids)pure agonist, only mu receptor
Mixed opioid agonists (4)?pentazocine, nalbuphine,nalorphine, buprenorphine
Partial opioid agonist?butorphanol (+++)partial mu receptor and kappa +++
Pentazoncine, nalbuphine and nalorphine have what receptor selectivity?antag of mu, ag/partial agonist of kappa and agonist of delta receptor
Opioid Antagonists of mu,kappa,deltaNaloxone and naltrexone
Buprenorphine given to whom?opioid with decent analgesia GIVE SUBLINGUAL TO CATS
Tramadol?not an opioid!!!! has opioid live activity/affects CENTRAL ACTING ANALGESIC
4 modes of action of Tramadol ?1.Complex interaction at Mu opioid receptor (+ Form) 2. SSRI (+) 3. SNRI reuptake inhibitor (-) 4. M1 antagonist
Alpha-2 Agonists general characteristics?sedation, analgesia, mm relaxant (high doses) Synergism w/opioids local anesthetics, NMDA antagonists
Do NMDA antagonists cause mm. relaxation?No this is why we add alpha-2 to ketamine, tiletamine
Anti-epileptic Drugs not used for standard tx of painGabapentin &pregabalin, voltage gated Ca channels=inhibit NT release
Gabapentin and Pregabalin bind where?alpha2delta1 and alpha2delta2 subunits of voltage gated Ca channels--> inhibit