anesthetics, analgesics
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- What is the significance of anesthetics with decreased solubility in blood?
- rapid induction and recovery times . Ie. N20
- What is the significance of anesthetics with increased solubility in lipids?
- increased potency = I/ MAC. Ie. Halothane
- Inhaled Anesthetics list them
- halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
- Inhaled Anesthetics What is good about lower solubility?
- the quicker the anesthetic response, and the quicker the recovery
- Inhaled Anesthetics What are these drug's effects?
- myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
- What toxicity mactches the following drugs 1. Halothane 2. Methoxyflurane 3. Enflurane 4. Rare
- 1. Hepatotoxcity 2. Nephrotoxicty 3. Proconvulsant 4. Malignant hyperthermia
- What do barbituates, benzodiazepines, arylcyclohexylamines and narcotic analgesics have in common?
- they are IV anesthetics
- What the pharmacokinetics and uses of thiopental?
- high lipid solubility, rapid entry into brain. Used for induction of anesthesia for short surgical procedures. Terminated by redistribution from brain. Decreased cerebral blood flow
- Give an example of a benzo and what is this class's shortcoming?
- midazolam used for endoscopy. Used with gaseous anesthetics and narcotics. May cause severe post-op respiratory depressio and amnesia
- What does Ketamine (PCP analog and an arylcyclohexylamine) do?
- dissociative anesthetic. Cardiovascular stimulant. Causes disorientation, hallucination, bad dreams. Increases cerebral blood flow.
- How are narcotic analgesics used? Examples?
- Morphone and fentanyl are used with CNS depressant during general anesthesia.
- What is the advantage of propofol
- used for rapid anesthesia induction and short procedures. Less post-op nausea than thiopental
- Local anesthetics Name some esters?
- procaine, cocaine, tetracaine,
- Local anesthetics Name some amides?
- lidocaine, bupivacaine, (amides have two I's in name!)
- Local anesthetics What is the mechanism and clinical use?
- bind receptor and block Na channels. Tertiary amine local anesthetics penetrate membrane in uncharge form, then bind charged form. Use for minor surgical procedures, spinal anesthesia.
- Local anesthetics How do you decide to use ester or amides?
- if allergic to esters, give amides
- Local anesthetics what is the toxicity
- CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine)
- Local anesthetics In infected ________ tissue, anesthetics are charged and cannot penetrate membrane. Therefore, ______ anesthetics are needed.
- acidic; more
- Local anesthetics What is the order of nerve blockade for size and myelination? Which factor predominates?
- small diameter> large diameter. Myelinated fibers> unmyelinated fibers. Size factor predominates
- Local anesthetics what is the order of loss of sensation?
- pain first, then temp, then touch, then pressure
- Local anesthetics Why would you give these drugs with vasoconstrictors?
- to enhance local action
- Opiod analgesics List as many as you can.
- morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
- Opiod analgesics Mechanism: They act as _____ for opiod receptors to modulate synaptic transmission
- agonists
- Opiod analgesics which drugs act at the mu, delta, kappa receptors?
- morphine enkephalin, dynorphin
- Opiod analgesics Clinical use?
- pain, cough supression (dex), diarrhea (loperamide), acute pulmonary edema, methadone maintenance programs
- Opiod analgesics What are the major toxicities?
- addiction, respiratory depression, constipation, miosis, additive CNS depression wth other drugs
- Opiod analgesics Tolerance does not develop to __________and ______
- miosis and constipation
- Opiod analgesics How would you treat toxicity?
- naloxone, naltrexone (opiod R antagonist)
- List three nonaspirin nonselective NSAIDS?
- ibuprofen, naproxen, indomethacin
- What is the mechanism of nonselective NSAIDs?
- reversibly inhibit COX 1 and 2. Blocks PG synthesis
- What are nonselective NSAID clinical use (3As)?
- Antipyretic, analgesic, anti-inflammatory. Indomethacin is used to close a PDA.
- What are common NSAID toxicities?
- renal damage, aplastic anemia, GI distress, ulcers
- Where is cox2 found?
- in inflammatory cells and mediates inflammation and pain
- Why is cox2 inhibition better than cox1?
- cox1 helps to maintain gastric mucosa, thus, should not have the corrosive effects of other NSAIDs on the GI lining (less incidence of ulcers and bleeding)
- Clinical Use of cox2 inhibitors?
- RA and osteoarthritis
- Acetaminophen What is its mechanism and where does it work?
- reversibly inhibits cox, mostly in CNS. Inactivated peripherally.
- Acetaminophen What are its 2 As?
- antipyretic, analgesic but NOT anti-inflammatory.
- Acetaminophen Overdose effects?
- hepatic necrosis, acetaminophen metabolites depletes glutathine and forms toxic tissue adducts in the liver