CNS drugs
Terms
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- partial opioid agonist at mu receptors, agonist at kappa receptors
- butorphanol
- weak opioid agonist that also inhibits 5-HT and NE uptake
- tramadol "tram it all" in
- On opioids, tolerance develops to everything but...
- constipation and miosis
- dec aqueous humor synthesis via vasoconstriction
- alpha agonists -EPI - do NOT use in closed-angle glaucoma -brimonidine
- dec aqueous humor secretion
- B blockers - timolol, betaxolol, carteolol acetazolamide
- inc outflow of aqueous humor
- cholinomimetics (contract ciliary muscle and open trabecular meshwork) -pilocarpine (emergencies) -carbachol -physostigmine -echothiophate PG - latanoprost (PGF2a) The circular ciliary muscle fibers affect zonular fibers in the eye (fibers that suspend the lens in position during accommodation), enabling changes in lens shape for light focusing. When the ciliary muscle contracts, it pulls itself forward and moves the frontal region toward the axis of the eye. This releases the tension on the lens caused by the zonular fibers (fibers that hold or flatten the lens). This release of tension of the zonular fibers causes the lens to become more spherical, adapting to short range focus. The other way around, relaxation of the ciliary muscle causes the zonular fibers to become taut, flattening the lens, increasing long range focus. Contraction and relaxation of the longitudinal fibers, which insert into the trabecular meshwork in the anterior chamber of the eye, cause an increase and decrease in the meshwork pore size, respectively, facilitating and impeding aqueous humour flow into the canal of Schlemm.
- darkens color of iris
- latanoprost
- anticonvulsants with liver toxicity
- carbamazepine valproic acid
- first line for tonic-clonic seizures
- phenytoin carbamazepine valproic acid
- contraindicated in pregnancy (teratogenic)
- phenytoin carbamazepine valproic acid
- first line in pregnant women, kids
- phenoBarbital
- used for trigeminal neuralgia
- carbamazepine
- used for neuropathic pain
- gabapentin
- causes Stevens-Johnson syndrome
- ethosuximide lamotrigine
- used for absence seizures
- ethosuximide (first line) valproic acid
- Prophylaxis for status epilepticus
- Phenytoin
- acute status epilepticus
- BDZ
- induce cyt P450
- phenytoin carbamazepine valproic acid
- causes wt gain
- valproic acid
- causes wt loss
- topiramate
- kidney stones
- topiramate
- agranulocytosis, aplastic anemia
- carbamazepine
- megaloblastic anemia hirsutism SLE-like syndrome gingival hyperplasia
- phenytoin
- mental dulling
- topiramate
- inc Na inactivation
- phenytoin - use dependent blockade, also inhibits glutamate release carbamazepine
- inc GABA-A action
- phenobarbital - inc duration of Cl channel opening (barbiDURATE) BDZ - inc frequency of Cl channel opening (FREnzodiazepine)
- block thalamic T-type Ca channels
- ethosuximide
- BDZs for status epilepticus
- lorazepam diazepam Lora Diaz had epilepsy.
- short-acting BDZs highest addictive potential
- triazolam oxazepam midazolam TOM thumb
- GABA antag to treat BDZ overdose
- flumazenil
- The more lipid-soluble a drug is, the ____ the MAC and the ____ the potency.
- lower higher
- low blood solubility
- rapid induction and recovery
- N2O has _____ blood solubility and _____ lipid solubility.
- low,low fast induction and low potency
- Halothane has ____ blood solubility and _____ lipid solubility.
- high, high high potency, slow induction
- inhaled anesthetics
- halothane "fluranes" N2O
- halothane
- hepatotoxicity
- enflurane
- proconvulsant
- methoxyflurane
- nephrotoxicity
- inhaled anesthetics SE
- malignant hyperthermia inc cerebral BF myocardial and respiratory depression nausea/emesis
- IV anesthetics
- barbiturates - thiopental BDZ - midazolam ketamine opiates - morphine, fentanyl propofol "B B King on OPIATES PROPROses FOOLishly"
- rapid induction, short procedures
- thiopental - DEC cerebral BF propofol
- most common drug for endoscopy
- midazolam (used with inhaled anesthetics and narcotics) may cause sevrer postop resp depression, dec BP, amnesia
- block NMDA Rs
- ketamine PCP analog cardiac stimulant disorientation, hallucination, bad dreams INC cerebral BF
- local anesthetics
- esters - procaine, etc. amides - lidocaine, bupivacaine, etc. can cause CNS excitation, severe CV toxicity (bupivacaine), HTN, hypoTN, arrhythmias (cocaine) except for cocaine, given with vasoC (EPI) to dec bleeding, dec systemic concentration in infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membranes effectively. more anesthetic is needed in these cases. preferentially bind activated Na channels
- order of nerve blockade
- small faster than large myelinated fasted then unmyelinated size factor predominates: 1. small myelinated 2. small unmyelinated 3. large myelinated 4. large unmyelinated
- order of sensory loss
- pain temp touch pressure PTTP
- depolarizing NM blocker
- succinylcholine -can cause hyperCa, hyperK -phase I: prolonged depol, no antidote, cholinesterase inhibitors potentiate blockade -phase 2: repolarized but blocked. use cholinesterase inhibitors
- competitive NM blockers
- tubocurarine, atracurium, pancuronium, etc.
- treat malignant hyperthermia, malignant neuroleptic syndrome
- dantrolene - prevent Ca release from SR
- drugs for Parkinson's
- Bromocriptine, pramipexole, ropinirole - DA agonist Amantadine - inc DA release, can cause ataxia L-dopa/carbidopa - can cause arrhythmias (peripheral conversion), dyskinesia, akinesia Selegiline (MAO-B inhibitor), entacapone, tolcapone (COMT inhibitors) Antimuscarinic - benztropine - helps with tremor and rigidity but not bradykinesia Al Capone hates commies decrease your tremor before you drive your BENZ
- memantine
- NMDA antag used to treat AD SE: confusion, dizziness, hallucinations
- donepezil
- anticholinesterase used to treat AD SE: dizziness, nausea, insomnia
- sumatriptan
- 5-HT1B/1D agonist causes vasoC, inhibition of trigeminal activation and vasoactive peptide release t1/2 less than 2 hrs treat: migraine, cluster headaches SE: coronary vasospasm (don't use in ppl with CAD, Prinzmetal's angina), tingling
- INC cerebral blood flow
- inhaled anesthetics ketamine
- DEC cerebral blood flow
- thiopental
- CV toxicity
- bupivacaine