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154 Cards in this Set
- Front
- Back
Main Drug Classes Used to Rx Glaucoma?
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Cholinomimetics
Beta Blockers |
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Which Cholinomimetics are high yield for Rx-ing Glaucoma?
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Pilocarpine
Echothiopate |
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MOA of Pilocarpine for Glaucoma?
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M-Receptor Agonist--->
contraction of ciliary muscle---> INc flow through Canal of Schlemm |
|
MOA for Echothiophate for glaucoma?
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Organophosphate AChE Inhibitor-->
Inc Outflow |
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Which Beta-Blockers are used for Glaucoma?
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Timolol
|
|
MOA for Timolol for Glaucoma?
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Blocks NE's actions at Ciliary Epithelium--->
Dec production of Aqueous Humor |
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Rx for Closed Angle Glaucoma?
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Surgery
Pre-Op: Cholinomimetics CA Inhibitors and/or Mannitol (dec body volume of water) |
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Drug class straight contraindicated in Closed Angle?
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Antimuscarinics
Alpha 1 agonists |
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Who else can you use for Glaucoma (low yield)? kicker?
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Epi: dec synthesis, SE = stinging; not for closed angle,
Brimonidine (alpha agonist) Latanoprost (PGF-2alpha): inc outflow; SE: darkens iris |
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Difference between Pain Threshold and Tolerance?
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Threshold is where you have the initial perception of pain
Tolerance is your Rxn to pain |
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Morphine's Fxns?
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Analgesia: Inc pain tolerance (you feel it, you just don't care)
Sedation Cough Suppression |
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SE's of Morphine?
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Resp Depression (not good)
CV: minimal on heart, but vasodilates (avoid in head trauma) GI: longitudinal's relax, circular constricts---> CONSTIPATION MIOSIS***via E-W nucleus N&V: stimulates CTZ in area postrema |
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Which is the only Opioid that doesn't cause MIOSIS? why?
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Meperidine
it also blocks M receptors #1 abused by health care professional |
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Which Opioid is the key for Cough Suppression?
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DM
Dextromethorphan |
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Who are the Full Opioid Receptor Agonists?
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Meperidine
Methadone Fantanyl Heroin |
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Key to Meperidine Metabolism?
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Metabolized by P450---> Nomeperidine = SSRI that can cause Serotonin Syndrome (seizures)
|
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Who are the Partial Opioid receptor agonists?
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Codeine
Buprenorphine/Butorphanol |
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Kicker for Buprenorphine?
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Acts as an antagonist in presence of Full agonists, which is Bad Bad for Substance Dependence b/c it precipitates withdrawal, so its contraindicated
|
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Time Out: what are the Opioid receptors? who have we been talking about so far with morphine and all these other guys?
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mu
kappa delta Mu is the guy we've been referring to. Mu is most pharmacologically important |
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Who are the Mixed Opioid Agonists?
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Nalbuphine
Pentazocine |
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What other receptor do Nalbuphine and Pentazocine stimulate? result?
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kappa: spinal analgesia and dysphoria
|
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Issue w/ Nalbuphine and Pentazocine?
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can precipitate withdrawal just like partial agonists
|
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Who are the Opioid Receptor Antagonists/
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Naloxone
Naltrexone |
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Pharm properties for Naloxone and Naltrexone?
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Naloxone: short acting
Naltrexone: long duration, better bioavailability |
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uses for Naloxone?
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IV
Reversal of Resp. Depression Post-op reversal of fentanyl's effects |
|
Uses and administration of Naltrexone?
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PO
Dec craving for alcohol Used after detox in opioid addicts |
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Mech for Naltrexone and booze?
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Alcohol is addicting in part b/c of Enkephalins and Endorphins (endogenous opioids)
Naltrexone blocks these |
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What's up w/ Tolerance and opioids?
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Occurs to all effects
EXCEPT Miosis Constipation (so as you raise dose to combat tolerance they get MORE CONSTIPATED) |
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Rx for Opioid Withdrawal?
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FULL AGONIST (like methadone)
|
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Who are the Opiate-related drugs w/ specific indications? why?
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Loperamide: rx's diarrhea b/c it doesn't cross BBB
Dextromethorphan: Rx's Cough |
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Who is Tramadol? mech?
|
Very weak opioid agonist
Also inhibits 5-HT and NE reuptake |
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Use for Tramadol?
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Chronic Pain
|
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SE of Tramadol?
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Dec seizure threshold
|
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2 High Yield Mechanisms for Anticonvulsants? which drugs for each?
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Dec axonal Conductions by Blocking Fast Na Channels
carbamazepine and phenytoin Inc inhibitory tone by facilitating GABA-mediated hyperpolarization barbs and benzo's |
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DOC for Partial Seizures (simple or complex?
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Valproic Acid
Phenytoin Carbamazepine |
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DOC for Tonic-Clonic (grand mal) Seizures (general)
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Valproic Acid
Phenytoin Carbamazepine |
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DOC for General Absence Seizures?
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Ethosuximide
and Valproid Acid |
|
DOC for Status epilepticus? ly
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Benzo's (lorazepam, diazepam)
Phenytoin (fosphenytoin is better IV cause its water soluble) |
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MOA for Phenytoin?
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blocks axonal Na channels in their Inactive state thus preventing seizure propagation
|
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Pharmacokinetics for Phenytoin?
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Induces cytochrome P450's
Zero-Order Elimination!!! |
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Who are the drugs eliminated via Zero-Order kinetics?
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Phenytoin
Alcohol |
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Main SE for Phenytoin?
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Gingival Hyperplasia!!!
|
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What drugs cause Gingival Hyperplasia?
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Phenytoin
Nifedipine Cyclosporine |
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MOA for Carbamazepine?
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same as phenytoin
blocks Na channels in inactive state |
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Other use for Carbamazepine?
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DOC for Trigeminal Neuralgia
|
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SE kickers for Carbamazepine? hy
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Induces P450 (especially the ones that metabolize sex hormones---> dec efficacy of OCP's)
Inc ADH secretion---> SIADH and dilutional hyponatremia |
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Other drug that can cause SIADH?
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Chlorpropramide (Sulfonylurea)
|
|
When talking about valproic acid, what do clinicians actually prescribe?
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Divalproex Na
|
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MOA of valproic acid? LY
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similar to phenytoin
also inhibits GABA transaminase blocks t-type Ca channels |
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Uses for Valproic Acid?
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all Seizure types
Mania of Bipolar Disorders (soon to be DOC) Migraine Prophylaxis (but not sx rx) |
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SE's of Valproic Acid?
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Inhibits P450s
Hepatotoxic (from toxic metabolite) Pancreatitis**** Teratogen--->Spina Bifida Hepatotoxicity and pancreatitis can kill you |
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What other drugs can cause pancreatitis?
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i don't know, but if there is a question about it, then Valproic Acid is the answer
|
|
MOA for ethosuximide?
LY |
blocks t-type Ca channels and thalamic neurons
|
|
Uses for ethosuximide?
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DOC for absence seizures
|
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General SE for anticonvulsants?
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Dec efficacy of OCP's via induction of P450's
|
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New Anticonvulsants to know?
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Felbamate
Lamotrigine |
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Uses for Felbamate and Lamotrigine
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Broad spectrum
good for Seizure States |
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SE's for Felbamate and Lamotrigine
|
Felbamate:
hepatotoxic Aplastic anemia (100% fatal) Lamotrigine: Stevens-Johnson Syndrome (40% develop rashes. 1% of those are S-J) |
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Why the heck is Felbamate and its hepatotoxicity and aplastic anemia still on the market?
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Last line of defense
used for Lenox-Gusalt Syndrome |
|
Gabapentin uses?
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DOC for Neuropathic pain (except for trigeminal = carba...)
|
|
SE's of Ethosuximide?
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Fatigue
GI HA |
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What drugs can Cause SLE-like reactions?
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Hydralazine
Isoniazid Procainamide quinidine phenytoin |
|
Benzo vs Barb toxicity?
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Barbs have a much narrower therapeutic window before they kill you
So mostly we just use benzo's |
|
MOA for Benzo's
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Potentiate GABA
Inc frequency of Cl channel openings--->membrane hyperpolarization Not GABA mimetic, so need GABA to be present Act through BZ receptors on GABA complex |
|
Different BZ receptors and their activity?
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BZ1: sedation
BZ2: anti-anxiety and impaired cognitive fxn |
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Rx for Benzo and Barb OD?
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Benzo: Flumazenil
Barbs: flumazenil doesn't work, you've just gotta Rx the sx's |
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MOA for Flumazenil?
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Nonspecific BZ receptor antagonist--->reversal of CNS depression seen w/ OD or post-anesthesia
|
|
Examples of Benzo's?
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Alprazolam
Diazepam Lorazepam Midazolam Temazepam Oxazepam |
|
General Uses for Benzo's?
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Anxiety
Panic attacks Muscle relaxation Withdrawal states (ethanol) Status epilepticus (loraz and diaz) Anesthesia amnesia (Midazolam) Sleep Disorders (temaz and oxaz) |
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Rare uses of Barbs?
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Phenobarbital: seizures
Thiopental: induce anesthesia |
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besides killing you (cns depression), what are SE's of barbs?
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induce P450
|
|
Kickers for relationship between benzo's, barb's and booze?
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Cross-tolerance to all 3
Barbs and booze are more likely to be abused Withdrawal of any ---> life threating sx's (tonic-clonic status and DT's) |
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Rx for Barb or Ethanol
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Long acting Benzo
(diazepam>lorazepam> the rest) |
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DDI's for Benzo's and Barbs?
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additive w/ other CNS depressants
Induce P450 of most lipid-soluble drugs (like OCP's) |
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Who are the Non-Benzo's who act like Benzo's?
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Zolpidem
Zaleplon Buspirone |
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MOA for Zolpidem and Zaleplon?
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BZ-1 receptor agonist
|
|
Uses of Zolpidem and Zaleplon?
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Sleep disorders
|
|
MOA for Buspirone?
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No effect on GABA
5-HT-1a partial agonist---> inc 5-HT activity |
|
Use for Buspirone?
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Generalized Anxiety Disorders (have low 5-HT)
Nonsedative |
|
Downside to Buspirone?
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takes 1-2 weeks to take effect
so no good for situational anxiety disorders |
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What is MAC?
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Minimal Alveolar Concentration at which 50% of the population is anesthetized
Measure of potency: ED50 |
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How does lipid solubility affect MAC?
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The more Lipid Soluble the anesthetic, the Lower the MAC and the Greater the Potency
Inc Lipid Solubility = Dec MAC = Inc Potency |
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How does blood solubility affect MAC?
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More Soluble in Blood = Slower Anesthetic onset
|
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How do Blood:Gas Ratios affect Anesthetics?
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High B:G ratio --> Slow onset
High B:G ratio---> Slow recovery Low B:G ratio--->fast onset and recovery |
|
Inhalational Anesthetics I need to know?
|
Nitrous Oxide
Halothane |
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MAC values for Nitrous and Halothane?
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104% for Nitrous
0.8% for Halothane so halothane is much more lipid soluble and much more potent |
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Blood:Gas Ratios for Nitrous and Halothane?
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Nitrous: 0.5
Halothane: 2.3 So halothane is more blood soluble and thus has a slower onset |
|
CV effects of Nitrous and Halothane? significance?
|
Nitrous: minimal
Halothane: sensitizes heart to Catecholamines (Beta 1's can lead to an arrhythmia. Ergo, don't ever put a pt w/ a pheochromocytoma under using halothane |
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SE's for Nitrous? how to prevent?
|
Diffusional Hypoxia
prevent w/ 100% O2 after use |
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SE's for Halothane?
|
Malignant Hyperthermia
Arrhythmias |
|
Who are the IV Anesthetics?
|
Thiopental
Midazolam Propofol Fentanyl Ketamine |
|
Kickers for Thiopental?
|
Barb
Used for induction (not much anymore) Highly lipid soluble Rapid Onset Short Acting due to redistribution? |
|
what is redistribution?
|
Lipid soluble drug get redistributed to tissue (adipose) and thus decrease the duration of the drug
|
|
uses of Midazolam?
|
Anterograde Amnesia
Preop sedation induction Outpatient surgery depresses resp |
|
Use for Propofol?
|
INDUCTION and maintenance
ANTIEMETIC!!! (only anesthetic w/ this property) CNS and cardiac depressant |
|
Uses of Fentanyl?
|
Opiate for induction and maintenance
Depresses resp |
|
MOA for ketamine?
|
Dissociative Anesthetic
NMDA Receptor Antagonist |
|
Uses of Ketamine?
|
Induction
only used in kids cause they don't report... |
|
SE's of Ketamine?
|
Emergent Delirium
Hallucinations (not in kids) CV Stimulation Inc ICP |
|
Types of Local Anesthetics?
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Esters and Amides
|
|
How do you tell the local anesthetics apart?
|
If it has just 1 "i" then its an ester
more than 1 "i" is an amide |
|
So who are the local anesthetic esters and amides?
|
Esters: Procaine, Cocaine, Benzocaine
Amides: Lidocaine, Bupivacaine, Mepivacaine |
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How are Local Anesthetics metabolized?
|
Esters are metabolized by plasma and tissue esterases
Amides are metabolized by liver amidases |
|
MOA for local anestetics?
|
The drug must cross the axonal membrane to fxn
In order to cross the membrane the drug must be in the non-ionized form. In order to be active the drug must be in the ionized form. The active, ionized drug blocks Fast Na channels in the inactive state So there's a lot of stuff having to happen. |
|
How do different nerve fiber differ in sensitivity to Local Anesthetics?
|
The smaller the diameter the more sensitive
AND the higher the firing rate, the more sensitive AND myelinated are more sensitive than unmyelinated |
|
based on the different factors affecting sensitivity what is the Order of Sensitivity for different nerve fibers? Significance?
|
Type B and C > A-delta > A-beta and A-gamma > A-alpha
This means we'll lose the nerves for pain (C's and A-deltas) way before we lose the nerve fibers for motor neurons (A-alphas) |
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How does recovery proceed?
|
in the reverse order of sensitivity. so motors first, pregang ANS fibers last
|
|
How are local anesthetics administered?
|
They're given w/ Alpha-1 agonists (vasoconstrictors) in order to stop the anesthetics from entering the systemic circ
Inc Duration and dec toxicity |
|
SE's of Local Anesthetics?
|
Neurotoxic--->seizures
CV toxic (esp bupivacaine and cocaine) Allergies: esters via PABA formation |
|
Affect of pH on Local Anesthetics? clinical significance?
|
In acidic tissue, the drugs get stuck in the ionized (active) form and can't penetrate the axonal membrane
this occurs clinically in infections. To fix just up the dose |
|
Use of Neuromuscular blocking drugs? why they work?
|
Used for muscle paralysis in surgery or mech. ventilation.
Selective for motor (vs autonomic) nicotinic receptors |
|
2 types of NM blocking drugs?
|
Nondepolarizing (competitive)
Depolarizing (noncompetitive) |
|
MOA for Nondepolarizing NM blocking drugs?
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Nicotinic Antagonists
|
|
Examples of Nondepolarizing NM blocking drugs?
|
D-Tubocurarine
Atracurium Mivacurium -cur- drugs |
|
What do Nondepolarizing NM blocking drugs affect? not affect?
|
Paralysis of face, limbs, resp muslces
No effects on cardiac or smooth muscle No CNS effects |
|
1 reason to use Atracurium
and 1 reason not to use Atracurium? |
It is safe in heptic and renal impairment
It is inactivated to Laudanosine, which can cause seizures |
|
How to cause recovery from Nondepolarizing NM blocking drugs?
|
AChE Inhibitors (neostigmine)
|
|
MOA for Depolarizing NM blocking drugs? phases?
|
Nicotinic AGONIST
Phase 1 = depolarization, FASCICULATION, prolonged depol, flaccid paralysis Phase 2: densensitization |
|
Who are the Depolarizing NM blocking drugs?
How do you reverse them? |
SUCCINYLCHOLINE!
you don't. AChE I's only make Phase 1 worse but will help Phase 2 |
|
Potential SE's of Depolarizing NM blocking drugs
|
MALIGNANT HYPERTHERMIA
hyperK atypical pseudocholinesterase |
|
Who are the Centrally Acting Skeletal Muscle Relaxants? MOA? use?
|
Benzo's
Baclofen both work via GABA receptors Used for spasticity |
|
Rx for malignant hyperthermia?
|
Dantrolene
|
|
What causes malignant hyperthermia?
|
inhalation anesthetics (except nitrous)
Succinylcholine |
|
MOA for Dantrolene?
|
prevents release of Ca from SR of skeletal muscle
|
|
Other uses of Dantrolene?
|
Neuroleptic Malignant Syndrome (toxicity of anti-psychotic drugs)
|
|
Drug types used to Rx Parkinson's?
|
DA receptor agonists
Inc DA Prevent breakdown of DA Block fxn of ACh |
|
Primary Parkinson drug? MOA?
|
Levodopa
prodrug that gets converted by Aromatic AA decarboxylase to DA |
|
How is Levodopa Administered? why?
|
With Carbidopa:
Carbidopa blocks AAAD and doesn't cross the BBB. This keep L-dopa from being converted to DA outside the CNS |
|
SE's of Levodopa?
|
**Peak-dose dyskinesias
On-Off effects **Psychosis (inc DA in mesolimbic) Hypotension (makes post. instability worse) Vomiting (activates CTZ) |
|
Who else can help Levodopa?
|
Tolcapone (entacapone)
Selegiline |
|
MOA for Tolcapone and Entacapone?
|
Inhibit COMT, which is good b/c COMT metabolizes DA
Inc uptake and efficacy |
|
SE's of Tolcapone?
|
Hepatotoxic (not entacapone)
|
|
MOA for Selegiline?
|
MAO-b selective inhibitor
|
|
Why is it good the Selegiline is a selective MAO-b inhibitor?
|
b/c it means there isn't any wine/cheese HTN
|
|
Why is Selegiline almost always given w/ Levodopa?
|
It blocks the metabolism of DA in the CNS
|
|
SE's of Selegiline?
|
one of its metabolites is an amphetamine--->insomnia
|
|
Who are the DA receptor agonists for PD?
|
BROMOCRIPTINE
Pramipexole ropinirole PERGOLIDE |
|
Other uses for Bromocriptine?
|
HyperPRL and Acromegaly since DA suppresses Prolactin and GH
|
|
Kicker for Pergolide?
|
off the market due to causing valvular defects
|
|
What drugs are used to Dec ACh fxn?
|
Benztropine*
Trihexyphenidyl Diphenhydramine* |
|
How do benztropine, diphenhydramine and trihexylphenidyl work?
|
They are Muscarinic blockers and thus block the effects of ACh--->Dec tremors and rigidity but have little effects on bradykinesia
|
|
SE's of the muscarinic blockers?
|
Anti-DUMBELLS
|
|
1 more drug that can be used for PD?
|
Amantidine
|
|
MOA for amantidine?
|
Anti-viral
Blocks M-receptors Inc DA release |
|
SE's of Amantidine?
|
Anti-dumbells
Livedo Reticularis |
|
What is Livedo Reticularis?
|
Purple-ish lower legs
varicose veins to the max Benign and reversile |
|
Rx for essential or familial tremors?
|
beta blockers
|
|
MOA for Sumatriptan?
|
5-HT-1b/1d agonist
causes: vasoconstriction inhibition of trigeminal activation and vasoactive peptide release |
|
Clinical Uses for Sumatriptan?
|
acute migraines (dec PAIN)
cluster HA's |
|
2 big Alzheimer's Drugs?
|
Memantine
Donepezil |
|
MOA for memantine?
|
NMDA receptor ANTAGONIST
helps prevent excitotoxicity |
|
SE's of Memantine?
|
dizzy
confused hallucinations |
|
MOA for Donepezil?
|
AChE I
|
|
SE's of Donepezil?
|
Nausea
Dizzy Insomnia |