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88 Cards in this Set
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Epinephrine glaucoma mech, use, toxicities
constraindication |
decreases aqueous humor by alpha agonism production
for open-angle glaucoma toxicities- miadrisis,stinging DO NOT USE WITH CLOSED ANGLE GLAUCOMA |
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Bromonidine mech, use
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alpha agonist
decreases aqueous humor open angle glaucoma |
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3 beta blockers used for glaucoma, mech of action
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timolol, betaxalol, cartelol
decrease aqueous humor secretion |
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Acetazolamide for glaucoma:
helps how? |
decreases aqueous humor secretion (like beta blockers)
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echothiophate mech, use
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indirect ACh agonist
glaucoma |
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what is best cholinomimetic for acute glaucoma emergency, works how?
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pilocarpine
works by contracting ciliary muscle to allow outflow through trabecular meshwork/canal of schlemm |
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2 direct glaucoma cholinomimetics, 2 indirect cholinomimetics, 2 side effects
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direct agonists- pilocarpine, carbachol
indirect agonists- phyostigmine, echothiophate miosis, cyclospasm (contraction of ciliary muscle for accomodation, helps with outflow) |
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Latanoprost mech, use, toxicitiy
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prostaglandin analog
increases outflow for glaucoma (like cholinomimetic) toxicity- browning of iris |
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2 opiates for diarrhea
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loperamide
diphenoxylate |
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3 non-pain uses for opioid analgesics
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cough suppressant (dextromethorphan)
diarrhea (loperamide, duphenoxylate) acute pulmonary edema |
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opioids acts on mostly mu receptors to decrease synaptic transmission, change what ion channels?
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open K+ channels which causes decrease Ca++ channel opening
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opioids act mostly on mu receptors, but can also act on other receptors where?
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opioid receptors are mu, gamma, and kappa.
also has some effect on kappa receptors in dorsal horn |
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tramadol mech, complication
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weak opioid agonist, but also NE and serotonin reuptake inhibitor ("tram it all")
decreases seizure threshold |
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buprenorphine mech, complication
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mu mixed agonist/antagonist
can cause withdrawal in pt on full agonist opioid |
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butorphanol mech, complication
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partial mu agonist
can cause withdrawal in pt on full agonist opioid |
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situation meperedine is preferred?
contraindicated? |
preferred over morphine in labor because more rarely causes seizures
can cause serotonin syndrome with MAOI |
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Naloxone reverses what?
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opioid overdose causing respiratory coma, can cause opioid withdrawal
-may need to be redosed to avoid lapsing back into coma |
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Naltrexone use
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mu agonist used for chronic alcoholism
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main opioid complications
which complications not influenced by tolerance? |
RESPIRATORY DEPRESSION
CNS depression additive with other substances (EtOH, barbiturates, benzos) constipation miosis addiction constipation and miosis not subject to tolerance |
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Nausea, tachycardia, seizures, muscle spasms, HTN, diarrhea, fever, chills, tremors characterize withdrawal of what, when
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opioid withdrawal 3-5 days out.
withdrawal 2-3 days out presents with anxiety, insomnia, GI disturbance, rhinorrhea, myadrisis, diaphoresis |
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NSAIDs attenuate inflammatory pain how?
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by decreasing production of prostaglandins (sensitize to pain and promote inflammation)
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3 first line drugs for tonic-clonic seizures
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Phenytoin
Carbamazepine Valproic acid |
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First line drug for Absence seizure
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Ethosuxamide
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1st line drug for status epilepticus
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Diazepam or Lorazepam
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1st line for trigeminal neuralgia
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carbamazepine
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1st line for epilepsy in pregnant women, children
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phenobarbitol
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1st line for ecclampsia
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MGSO4 (can also use benzodiazepines)
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1st line for parital complex seizures
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carbamazepine
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what are the 4 classic anti-epileptics? 2 toxicities they have in common
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Phenytoin, Carbamazepine, Valproic Acid, Phenobarbitol
hepatotoxicity, induce p-450 |
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the classic antiepileptics cover all the bases: thromboctyopenia, agranulocytosis, anemia, aplastic anemia (deficiency of all). which belongs to which?
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Valproic acid- low platelets
Phenytoin- megaloblastic anemia Carbamazepine- agranulocytosis and aplastic anemia |
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Phenytoin mech, use
toxicities: toxicities: organ hematologic reproductive endocrine MSK Neuro |
blocks Na+ channels (which decreases presynaptic glutamate release)
1st line for tonic-clonic, 1st line status epilepticus prophylaxis toxicities: like all classic drug toxicities, hepatotoxicity and p-450 induction hematologic: megaloblastic anemia Reproductive: teratogen (Fetal Hydrantoin syndrome- anencephaly and hypoplastic nails) Endocrine: hirsutism MSK: SLE-like syndrome, gingival hyperplasia Neuro: ataxia, diplopia |
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1st line for status epilepticus prophylaxis
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phenytoin
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how is phenytoin like procainamide and hydralazine
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can have SLE-like syndrome
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Carbamazepine mech, uses
toxicities: organ hematologic reproductive endocrine MSK Neuro |
Na+ channel blocker
1st line tonic-clonic, partial seizures, 1st line trigeminal neuralgia toxicities: classic carbamazepine toxicities of hepatotoxicity and p-450 induction blood: agranulocytosis aplastic anemia teratogenesis SIADH Steven-Johnson syndrome ataxia, diplopia |
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increases Na+ inactivation and GABA concentration?
uses (3) toxicities: organ hematologic reproductive endocrine Neuro |
Valproid Acid
uses: 1st line tonic-clonic, myoclonic seizures, partial toxicities: organ: hepatotoxicity, p-450 induction, FULMINANT LIVER FAILURE (in kids with polypharmacy usually) hematologic: decreased platelets reproductive: Neural tube defects endocrine: WEIGHT GAIN MSK: Neuro: tremor |
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Phenobarbitol mech, uses
toxicities contraindication |
inc. duration of GABAa Cl- channel opening
1st line pregnant seizures, kids "Makes kids HYPER and STUPID" -can cause paradoxical hyperactivity -decreased mental function normal toxicities- CNS depression, respiratory and cardiac depression. can lead to dependence and tolerance induces p-450 |
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barbiturates are contraindicated in what condition
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porphyria
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blocks thalamic T-type Ca+ channel receptors
use? toxicities |
Ethosuxamide
use- first line for absence seizures toxicities EFGH Ethosuxamide Fatigue GI distress Headache can have small skin rxn-urticaria or Steven-Johnson syndrome |
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3 epileptics that can cause steven-johnson's syndrome
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Ethosuxamide
Carbamazepine Lamotrigine |
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Lamotrigine mech, uses, toxicity
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blocks Na+ channels
partial and clonic-tonic seizures steven-johnsons |
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GABA analog that inhibits HVA Ca++ channels
uses (3) toxicities (2) |
Gabapentin
used for peripheral neuropathy, bipolar disorder, seizures toxicities- sedation, ataxia |
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Topiramate mech, uses, toxicities (3)
organ Neuro Endocrine |
blocks Na+ channels and increases GABA action
partial and tonic-clonic seizures Organ: kidney stones Neuro: mental dulling (think of my teacher) Endocrine: weight loss |
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do benzos, barbiturates, and EtOH bind to same point on GABA-R as GABA?
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no, allosteric site
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what are the short-acting benzodiazepines?
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TOM thumb
Triazolam, Oxazepam, Midazolam |
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traditional epileptic drugs are contraindicated in hepatic failure because they are metabolized by p450. Can use (2)
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Lamotrigine
Valproic Acid |
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Benzodiazepines:
common side effects? be very careful using in what situation? contraindicated in what situation? how affect sleep? |
CNS depression, sedation, some repiratory depression (less than barbs)
careful in heptic damage contraindicated in narrow-angle glaucoma decrease REM sleep |
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night terrors, sleep walking use what class?
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benzos
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Zolpidem, zaleplon, ezopiclone mech, use, 3 toxicities
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act via BZ1 receptor subtype of GABA receptors (not same as benzos)
insomnia (have very rapid onset and metabolism by liver) ataxia, headache, confusion do respond to flumazenil like benzos |
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Inhaled anesthetic general principles:
dereased solubility in blood? increased solubility in lipids? increased arterial-venous concentration gradient in tissue? |
decreased solubility in blood- faster induction and recovery time
increased solubility in lipids- has SLOWER INDUCTION, but HIGHER POTENCY higher conc. gradient in tissue (brain)- more needed to saturate tissues- slower induction |
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benzo mechanism on GABAa-R
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bind allosterically to and increase activity of GABA binding (increae frequency of Cl- channel opening--> more hyperpolarization)
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inhaled anesthetics:
MAC inversely related to? NO high or low MAC? Halothane high or low? |
1/MAC= potency
(MAC is conc. of drug at which 50% of people anesthetized) potency directly proportional to lipid solubility of the drug NO- low lipid solubility and blood solubility- low potency, fast induction and clearance time Halothane- high blood and lipid solubility - slow induction and high potency |
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Halothane
3 common inhaled anesthetic toxicities 1 specific 1 bad |
common= respiratory, myocardial depression, increase in cerebral blood flow
specific= hepatotoxicity bad= Malignant hyperthermia |
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Enflurane
use 3 common toxicities 1 specific |
induce anesthesia
common= myocardial depression, respiratory depression, increased cerebral blood flow specific- seizures |
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Isoflurane
use toxicities (3) |
inhaled anesthetic
myocardial depression, respiratory depression, increased cerebral blood flow |
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Methoxyflurane
3 common toxicities among inhaled anesthetics 1 specific |
myocardial depression, respiratory depression
increased cerebral blood flow specific- nephrotoxicity |
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2 possible toxicities for NO (inhaled)
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megaloblastic anemia
peripheral neuropathy |
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Malignant hyperthermia:
genetic basis? cause treatment |
AD inheritance to have problem
increased Ca++ release from ryanodine receptors treatment- dantrolene (blocks ca++ channels on sracoplasmic reticulum) |
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sevoflurane
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inhaled anesthetic
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Thiopental
use what causes effect termination increased or decrease cerebral blood flow |
intravenous anesthetic, very fast induction
effect terminated by quick redistribution into other tissues DECREASED cerebral blood flow (unlike inhaled anesthetics) |
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inhaled anesthetics inc./dec. cerebral blow flow? cerebral metabolic demand?
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increase cerebral blood flow but decrease metabolic demand
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mneumonic for Intravenous anesthetics
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BB King on OPIATES PROPoses FOOLishly
barbiturates (thiopental) benzodiazepines (midazolam) Ketamine Opiates (morphine, fentanyl) Propofol |
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what is longest acting benzodiazepine?
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clonazepam
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Benzo used in intravenous anesthesia? 2 possible problems
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Midazolam
postoperative respiratory depression decresed BP -use flumazenil |
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2 anesthetic classes that increase cerebral blood flow
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ketamine
inhaled anesthetics |
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Ketamine mech, produces what kind of amnesia?
causes stimulation of what? increases what? |
blocks NMDA receptors
produces DISSOCIATIVE amnesia (disconnection from surroundings) with disorientation, hallucination, nightmares. causes cardiovascular stimulation increased cerebral blood flow |
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2 opiates used as intravenous anesthetics
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morphine
fentanyl (has high tolerance, very addictive and dangerous) use with other anesthetics, no by self |
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Propofol mech, use
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potentiates GABA like barbiturate, but is not one. recovery rate faster than thiopental.
use for fast induction of anesthesia |
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Local anesthetics:
procaine, cocaine, tetracaine, lidocaine, bupivicaine, mepivicaine, ropivacaine 2 classes, which better, how tell difference? |
Amides- better availability, less allergic reactions, metabolized by liver, can tell because have "i" before -caine
Esthers- rapidly degraded by pseudocholiesterase in serum, used only when person has liver damage |
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local anesthetics mechanism?
what factor decreases local anesthetic action? do they like small/large nerves? myelinated/unmyelinated? what is order of loss? touch, pressure, pain, temp |
Na+ channel blockade by going through channel and binding on inside
decreased pH ionizes them, and charged ions cannot pentrate tissue as well like small over large diameter, myelinated over unmyelinated (makes sense that pain lost first because Adelta pain fibers are small and myelinated) 1. pain 2. temp 3. touch 4. pressure |
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local anesthetic toxicity (procaine, lidocaine, etc)
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cardiotoxicity and arrhythmias, CNS excitation, hypo/hypertension
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Succinylcholine mech, use
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depolarizing motor nicotinic receptor blocker
used for neuromuscular paralysis in surgery/mechanical ventilation |
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in Depolarizing muscular nicotinic receptor blockade:
what is antidote for phase 1 (extended depolarization)? what is antidote for phase 2 (repolarization but blocked) |
description of Succinylcholine
phase 1= no antidote (cholinesterase inhibitors exacrerbate) phase 2= cholinesterase inhibitors (ex. neostigmine) |
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Tubocurarine, atracurium, pancuronium, vecuronoium are examples of?
antidote? |
Non-depolarizing Neuromuscular blockers (selective for motor, not autonomic, nicotinic receptors)
cholinestterase inhibitors (ex. neostigmine) |
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entacapone
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COMT inhibitor (prevents L-dopa breakdown, used in Parkinson's)
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tolcapone
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COMT inhibitor (prevents L-dopa breakdown, used in Parkinson's)
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pneumonic for Parkinson's drugs
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BASLA
bromocriptine amantadine L-dopa (and carbidopa) Selegilene (and COMT inhibitors) Antimuscarinics (Benztropine) |
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Bromocriptine mech for parkinson's
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agonize dopamine receptors
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Amantadine:
neuologic use 2 infectious uses what is toxicity? |
increases dopamine release (Parkinson's)
influenza rubella ataxia |
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selegeline mech in parkinson's
possible side effect |
MAOI-B
inhibits dopamine breakdown can exacerbate eperipheral effects of L-dopa (arrhythmias, dyskinesia with extended use) |
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Benztropine for Parkinson's
mech? helps what TRAP symptoms, what not? |
antimuscarinic
HELPS with TREMOR and RIGIDITY doesn't help akinesia |
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difference between L-Dopa and dopamine?
what is mechanism of carbidopa? side effect of peripheral conversion of L-Dopa? |
dopamine can't cross BBB
carbidopa is peripheral dopamine decarboxylase inhibitor peripheral dopamine can cause arrythmias long-term use causes dyskinesia with use and akinesia between uses |
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Memantine mech, use, toxicities (3)
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NMDA receptor antagonist
(helps prevent Ca++ mediated excitotoxicity) for Alzheimers dizziness, confusion, hallucinations |
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Donepizil mech, use
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cholinesterase inhibitor
Alzheimers dizziness, nausea, insomnia |
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galantamine
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cholinesterase inhibitor for Alzheimers
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rivastigmine
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cholisterase inhibitor used for Alzheimers
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Non-psychotic use for haloperidol
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huntington's
(dopamine receptor antagonist) |
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reserpine and tetrabenazine help in Huntington's by
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amine depleting
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Sumatriptan
mech use toxcity and contraindication |
5-HT agonist
causes vasconstriction and inhibits trigeminal activation and release of vasoactive peptides used in migraines, cluster headaches toxicity - vasospasm contraindicated in those with CAD or prinzmetal's angina |
