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98 Cards in this Set
- Front
- Back
Glaucoma drugs: classes and specific drugs
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1. alpha agonists: epinephrine, brimonidine
2. beta blockers: timolol, betaxolol, careolol 3. diuretics: acetazolamide 4. cholinomimetics: direct: carbachol, pilocarpine indirect: physostigmine, echothiophate 5. prostaglandin: latanoprost |
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Glaucoma - Epinephrine
1. mechanism 2. side effects 3. c/i |
1. decrease aq humour synthesis
2. mydriasis, stinging 3. DO NOT USE in closed angle glaucoma |
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Glaucoma - Brimonidine
1. mechanism 2. side effects |
1. alpha-agonist, decreases aq humor synthesis
2. none |
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Glaucoma - Beta blockers
1. mechanism 2. side effects |
1. decrease aq humour secretion
2. none |
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Glaucoma - Acetazolamide
1. mechanism 2. side effects |
1. decrease aq humour secretion by decreasing HCO3-
2. none |
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Glaucoma - Cholinomimetics
1. mechanism 2. side effects |
1. Increase outflow of aq humour, contract ciliary muscle (which produces aq humour) and opens trabecular network into canal of Schlemm
2. miosis, cyclospasm (accomodate) |
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Which glaucoma drug do you use in an emergency?
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Pilocarpine
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Glaucoma - Latanoprost
1. mechanism 2. side effects |
1. Prostaglandin (PGFa2), increase outflow of aq humour
2. Darkens iris (browning) |
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Opioid analgesics - drugs
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Morphine
Fentanyl Codeine Heroin Methadone Meperidine Dextromethorphan |
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Opioid analgesics - mechanism
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Agonist at opioid receptors, mu, delta, kappa
Open K close Ca channels --> decrease synaptic transmission Inhibit release of ACh, NE, 5HT, glutamate, substance P |
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Opioid analgesics - use
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Pain
Cough suppression (dextromethorphan) Diarrhea (loperamide and diphenoxylate) Acute pulmonary edema Maintenance program for addicts (methadone) |
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Which opioid is used for cough suppression?
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Dextromethorphan
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Which opioids are used for diarrhea?
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Loperamide and diphenoxylate
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Which opioids are used for maintenance in drug addicts?
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Methadone
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Toxicity of opioid analgesics
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Tolerance
Respiratory depression Constipation Miosis CNS depression with other drugs |
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What do you treat opioid toxicity with?
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Opioid receptor antagonists:
naltrexone naloxone |
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What do you NOT develop tolerance to when using opioids?
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Miosis
Constipation |
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Butorphanol
Mechanism Use Toxicity |
1. Partial agonist at opioid mu receptors, agonist at kappa
2. Pain, causes less respiratory depression than full agonists 3. Causes withdrawal if on full agonists |
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Which opioid causes less respiratory depression in comparison to other opioids?
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Butorphanol
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Tramadol
1. Mechanism 2. Use 3. Toxicity |
1. Weak opioid agonist, inhibits Serotonin and NE reuptake (works on multiple neurotransmitters)
2. chronic pain 3. decreases seizure threshold |
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Phenytoin
1. Tx's which seizures 2. Mechanism 3. Which drug can be used parenterally? |
1. Simple Partial
Simple Complex Generalized Tonic-Clonic 1st line for Status 2. Increases Na inactivation 3. Fosphenytoin |
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Carbamezapine
1. Tx's which seizures 2. Mechanism |
1. Simple Partial
Simple Complex 1st line for Generalized Tonic-Clonic 2. Increases Na channel inactivation |
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Which drug is 1st line for trigeminal neuralgia?
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Carbamezapine
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Lamotrigine
1. Tx's which seizures 2. Mechanism |
1. PS, PC, GTC
2. Blocks voltage-gated Na channels |
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Gabapentin
1. Tx's which seizures 2. Mechanism |
1. PS, PC, GTC
2. GABA analogue, blocks high voltage activated Ca channels |
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Topiramate
1. Tx's which seizures 2. Mechanism |
1. PS, PC, GTC
2. Blocks Na channels, increases GABA action |
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Phenobarbital
1. Tx's which seizures 2. Mechanism |
1. PS, PC, GTC
2. Increases duration of Cl- channel opening, increases GABA action |
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Which AED is the first line for kids and pregnant women?
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Phenobarbital
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Which drugs are first line for GTC seizures?
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Phenytoin
Carbamezapine Valproic acid |
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Valproic acid
1. Tx's which seizures 2. Mechanism |
1. PS, PC, 1st line for GTC
2. Increase Na inactivation, increase GABA action |
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Which AED is also used for myoclonic seizures?
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Valproic acid
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Ethosuximide
1. Tx's which seizures 2. Mechanism |
1. 1st line for absence seizures
2. Block Ca channels in thalamus |
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Benzo's
1. Tx's which seizures 2. Mechanism |
1. first line for acute status epilepticus
2. increase frequency of Cl- channel opening |
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Tiagabine
1. Tx's which seizures 2. Mechanism |
1. PS, PC
2. inhibit GABA reuptake |
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Vigabatrin
1. Tx's which seizures 2. Mechanism |
1. PS, PC
2. inhibits GABA transaminase, increasing GABA |
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Levetiracetam
1. Tx's which seizures 2. Mechanism |
1. PS, PC, GTC
2. Unknown |
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Which AEDs are first line for status epilepticus?
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Prophylaxis: Phenytoin
Acute: Benzo |
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Which AED is used for seizures in eclampsia?
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Benzo
MgSO4 is first line |
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Benzodiazepine toxicities
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Sedation
Tolerance Dependance |
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Carbamezapine toxicity
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Blood dyscrasias (aplastic anemia and agranulocytosis)
Liver toxicity Teratogenesis Cyt-P450 inducer SIADH Stevens-Johnsons syndrome |
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Ethosuximide toxicity
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"EFGH"
Ethosuximide: Fatigue GI Distress Headaches Stevens-Johnsons syndrome |
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Stevens-Johnsons syndrome
Sx's 3 AEDs that have this SE |
1. Prodrome of malaise and fever
Rapid onset erythematous/purpuric macules (oral, ocular, genital) Epidermal necrosis and sloughing 2. Ethosuximide Carbamezapine Lamotrigine |
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Phenobarbital toxicity
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Sedation
Tolerance/Dependance Cyt-P450 inducer |
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Phenytoin toxicity
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Gingival hyperplasia in kids
Hirsutism Megaloblastic anemia (decreases folate absorption) Teratogenesis (fetal hydantoin syndrome) SLE-like syndrome Cyt-P450 inducer |
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Valproic acid toxicity
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Fatal hepatotoxicty
NTDs/spina bifida in fetus Weight gain C/i in pregnancy |
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Lamotrigine toxicity
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Stevens-Johnsons syndrome
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Gabapentin toxicity
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Sedation
Ataxia |
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Topiramate toxicity
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Sedation
Kidney stone Weight loss |
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Phenytoin is also what type of drug in addition to being an AED?
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Class I antiarrhythmic
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Barbiturates:
1. Examples of drugs 2. Use 3. Toxicites 4. Tx overdose? |
1. Phenobarbital, Thiopental
2. Anxiety, seizures, induction for anesthesia 3. additive CNS depression respiratory/CV depression induction of Cyt-P450 4. symptom management -- assist respiration and increase BP |
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Which AED is c/i in porphyria?
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Barbiturates
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Benzodiazepines
1. use 2. list short-acting drugs 3. toxicity |
1. anxiety, spasticity, epilepticus, detox from EtOH, night terrors, sleep walking, general anesthetic, hypnotic
2. TOM thumb is short Triazolam Oxazepam Midazolam 3. dependance additive CNS depression with EtOH less risk of respiratory depression and coma |
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How do you Tx benzo overdose?
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Flumazenil
GABA receptor antagonist |
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Which benzo's have the highest addictive potential?
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Short acting
Triazolam Oxazepam Midazolam |
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Which 2 AEDs are used for acute status epileptices?
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Diazepam
Lorazepam (Benzo's) |
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How do CNS drugs cross BBB?
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1. soluble in lipid
OR 2. transporter |
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Drugs with decreased solubility in the blood have:
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rapid induction and recovery times
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Drugs with increased solubility in lipids have:
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Increased potency
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Potency of anesthetic drug =
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1/MAC
MAC = minimal alveolar concentration |
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What does a large MAC mean in terms of potency?
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low potency
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MAC
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minimal alveolar concentration at which 50% of population is anesthetized
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Halothane has increased blood and lipid solubility, what does this mean in terms of potency and induction?
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increased blood solubility: slow induction
increased lipid solubility: high potency |
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Mechanism of anesthetic action in lungs
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increases rate and depth of ventilation
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Mechanism of anesthetic action in blood
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increased blood solubility: increase gas required to saturate blood --> slow induction time
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Mechanism of anesthetic action in tissue (i.e. brain)
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increased solubility: increased gas required to saturate tissue --> slower onset of action
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Inhaled anesthetics
1. Drug examples 2. Mechanism 3. Effects 4. Toxicity |
1. Halothane, isoflurane, nitrous oxide
2. unknown 3. myocardial and respiratory depression nausea/emesis increased cerebral blood flow (decreased cerebral metabolic demand) 4. Hepatotoxicity - halothane Nephrotoxicity - methoxyflurane Proconvulsant - enflurane Malignant hyperthermia |
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IV anesthetics (5)
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BBKing on OPIATES PROPoses FOOLishly
Barbiturates Benzodiazepine Ketamine Opiates Propofol |
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Thiopental
1. Potency, lipid solubility, entry time into brain 2. use 3. effect terminated by 4. effect on cerebral blood flow |
IV anesthetic, barbiturate
1. high potency, high lipid solubility, rapid entry 2. induction anesthesia, short surgical procedures 3. redistribution into fat and tissues 4. decreases cerebral blood flow |
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Benzo's
1. use in anesthesia 2. used in conjuction with 3. toxicity |
1. IV anesthetic, midazolam most commonly used for endoscopy
2. gas anesthetics and narcotics 3. severe post-op respiratory depression, amnesia |
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Ketamine
1. analog of 2. blocks which receptors 3. simulates 4. side effects |
1. PCP, dissociative anesthesia
2. NMDA 3. CV system 4. disorientation, hallucination, bad dreams, increases cerebral blood flow |
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Opiates used as IV anesthetics
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Morphine, fentanyl
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Propofol
1. use 2. mechanism |
1. IV rapid induction of anesthesia, short procedures
2. potentiates GABA Less post-op nausea than thiopental |
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Ester local anesthetics
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Procaine, cocaine, tetracaine
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Amide local anesthetics
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lidocaine, mepivacaine, bupivacaine
(amides have 2 I's each) |
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Local anesthetics: mechanism
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block Na channels
binds better to activated Na channels, so most effective in rapidly firing neurons |
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Tertiary local amides penetrate membrane in what form and bind to ion channels in what form?
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penetrate in uncharged
bind in charged form |
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In infected (acidic) tissue, how must local anesthetics be administered differently?
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Alkaline anesthetics are charged and can't penetrate acidic membrane effectively, so must administer more
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Order of nerve blockade in local anesthetics
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small fibers > large fibers
myelinated fibers > unmyelinated Size factor predominates over myelination. |
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Order of sensory loss in local anesthetics
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Pain>temperature>touch>pressure
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Local anesthetics are usually given with what drug and why?
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Vasoconstrictors (epi), they enhance local action
*except cocaine |
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NMJ blockers
1. use 2. selective for which receptor 3. types |
1. muscle paralysis in surgery or mechanical ventilation
3. Motor nicotinic 3. Depol and Non-depol |
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Local anesthesia toxicity
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CNS excitation
Severe CV toxicity (bupivacaine) HTN Hypotension Arrhythmias (cocaine) |
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Succinylcholine
1. class 2. reversal of blockade 3. complications |
1. cholinomimetic, NMJ depolarizing blocker
2. Phase 1: prolonged depol, no antidote Phase 2: repolarized but blocked, can reverse with AChE inhibitor (neostigmine) 3. Hypercalemia, Hypercalcemia |
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Non-depolarizing NMJ blockers
1. examples 2. mechanism 3. reversal of blockade |
1. tubocurarine, atracurium, pancuronium, etc.
2. competitive antagonists for ACh 3. AChE inhibitors (neostigime, edrophonium, etc.) |
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Dantrolene: use and mechanism
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tx for malignant hyperthermia and neuroleptic malignant syndrome
prevents release of Ca from sarcoplasmic reticulum of skeletal muscle |
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Malignant hyperthermia is caused by
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concomitant use of inhalational anesthetics (except N2O) and succinylcholine
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Parkinson's has excess____ activity
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cholinergic
|
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PD drug classes
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1. dopamine agonists - Bromocriptine
2. drugs that increase dopamine - Amantadine, L-dopa/carbidopa 3. prevent dopamine breakdown - Selegiline 4. decrease cholinergic activity - Benztropine |
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PD drugs mnemonic
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"BALSA"
Bromocriptine Amantagine Levodopa/Carbidoma Selegiline Anti-muscarinics |
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Dopamine agonists in PD:
examples side effects |
1. Bromocriptine (ergot), pramipexole, ropinorole (non-ergot, preferred)
2. gambling |
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Amantadine in PD
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Increases dopamine release
also used as antiviral against influenza A toxicity: ataxia |
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Selegiline
1. MOA 2. examples 3. adjunctive to what PD drug 4. toxicity |
1. selective MAO-B inhibitor, which prefers metabolism of dopamine instead of NE or 5-HT
2. Entacapone, tocapone (COMT inhibitors) 3. L-dopa 4. enhance adverse effects of L-dopa |
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Benztropine in PD: MOA
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anti-muscarinic (decreased cholinergic activity), improves tremor and rigidity, but little effect on bradykinesia
"Park your Benz" |
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L-Dopa/carbidopa toxicity
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arrhythmias from peripheral conversion of L-dopa
Long-term: dyskinesia after administration Short-term: akinesia b/w doeses |
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Why is carbidopa given in PD?
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peripheral decarboxylase inhibitor
decreases peripheral side effects of L-dopa and increases bioavailability in brain |
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AD Drugs (2)
1. MOA 2. toxicity |
Memantine
1. NMDA receptor antagonist, helps prevent excitotoxicity mediated by Ca 2. dizziness, confusion, hallucinations Donezapil 1. AChE inihibitor 2. Nausea, dizziness insomnia |
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Huntington's Drugs
1. alterations in NTs 2. drug classes and examples |
1. Increased dopamine, decreased GABA and ACh
2. Reserpine + tetrabenzine - amine depleting Haloperidol - dopamine receptor antagonist |
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Sumatriptan
1. MOA 2. Half-life 3. Use 4. Toxicity 5. c/i in |
1. 5-HT agonist. Causes vasoconstriction, inhibits trigeminal activation and vasoactive peptide release.
2. <2hrs 3. Migraine and cluster HAs 4. Coronary vasospasm, mild tingling 5. CAD, Prinzmetal's angina |