Pharmacology: Neuro(USMLE Step 1) Flash Cards

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Title: Pharmacology: Neuro(USMLE Step 1)
Description: USMLE Step 1 Neuropharmacology
Number of Cards: 388
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Author: phharsh.doc
Created: 2011-12-19
Tags: cns pharmacology
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    • Question
    • Answer
    • Side 3
    • Types of GABA receptors?
    • GABA A: Cl influx
      GABA B: K efflux

      BelKin AC
    • Benzodiazepines: MOA?
      Effect observed on graph
    • 1. Act through BZ-1 + BZ-1 receptors(part of GABA complex)
      2. Potentiate GABA
      3. Increase frequency of opening of GABA channels
      "FRENZODIAZEPINES"
      4. Work on Gamma-subunit of GABA thru BZ-1 and BZ-2
      5. Cl efflux thru GABA produces hyperpolarization-->depression

      BZ-1: Sedation
      BZ-2: Anti-anxiety + impaired cognition


      "LEFT SHIFT OBSERVED ON GRAPH": potentiation
    • Benzodiazepines have/do not have GABA mimetic activity?
    • No GABA mimetic activity

      "BENZOs have NO gaba mimetic activity"
    • Barbiturates have/do not have GABA mimetic activity?
    • Barbiturates have GABA mimetic activity

      BarBs have MiMetic activity.

      "BBM"
    • Benzodiazepines:
      Uses?
    • 1. Sedative
      2. Anxiety
      3. Insomnia
      4. Night terrors
      5. Sleep walking
      6. Anesthesia
      7. Anti-epileptic
      8. Panic phobias
    • Benzodiazepines: Effect on REM sleep?
    • Sedative effect but reduce duration of REM sleep.
    • Benzodiazepines: Drugs and respective uses?
    • 1. Alprazolam: Anxiety

      2. Diazepam:
      i. Anxiety
      ii. Alcohol withdrawal
      iii. Antiseizure
      iv. Pre-op sedation

      3. Lorazepam:
      i. Anxiety
      ii. Anti-seizure
      iii. Pre-op sedation

      4. Oxazepam:
      i. Sleep disorders
      ii. Anxiety

      5. Midazolam:
      i. IV- anesthesia
      ii. Pre-op sedation

      6. Temazepam: Sleep disorders
    • Benzodiazepines: Short T1/2?
    • 1. Triazepam
      2. Oxazepam
      3. Midazolam

      TOM thumb- short (T1/2)
    • Benzodiazepines: Drugs that do not undergo liver metabolism?
    • Oxazepam
      Temazepam
      Lorazepam

      Out The Liver
    • Barbiturates uses?
    • Phenobarbital: seizures
      Thiopental: IV pre-anesthetic medication
    • Barbiturates: Pharmacokinetics?
      C/I: condition?
    • 1. General inducers of cytp450
      2. C/I in porphyrias:
      D-ALA induction

      ** See induction graph **
    • Sedatives: cross tolerance with?
    • Alcohol (ethanol)
      Barbs
      BZDs

      (higher dose required for BZDs in chronic alcoholics)
    • Withdrawal signs for BZDs?
    • 1. Rebound Insomnia
      2. Seizures
      3. Anxiety
    • Withdrawal signs for alcohol/barbs?
    • 1. Anxiety
      2. Agitation
      3. Life-threatening seizures.
    • Alcohol: Withdrawal Management?
    • Supportive
      Long acting BZDs
    • Drug interactions with alcohol/BZs?
    • Additive effects with:
      Additive depression with:
      1. Anesthetics
      2. A/histaminics
      3. Opiates
      4. B-blockers

      Metabolism induction:
      1. OC pills
      2. Carbamazepine
      3. Phenytoin
      4. Warfarin
    • BZs overdose: Rx?
    • Flumazenil

      Flumazenil MOA?
    • Competitive BZ receptor a/agonist
      (No effect on alcohol or barb overdose)
    • Non BZ drugs that act on BZ receptors?
    • 1. Zaleplon
      2. Zolpidem
    • Zolpidem/Zaleplon: MOA?
      Use?
      Advantage for use?
    • MOA: BZ-1 receptor agonist
      (No effect on cognition)

      Use: Sleep disorder

      Advantage: No addiction
      Less abuse liability
      Less tolerance
    • Buspirone:
      MOA?
      Use?
      Advantage of use?
      How long does it take for effect?
    • 1. 5HT-1A partial agonist
      (No effect on GABA)

      Use: Generalized anxiety disorder

      Advantage: Non sedative

      1-2 weeks for effects.
    • Alcohol: MOA for sedation?
    • GABA mimetic activity
    • All alcohols cause ____?
    • Metabolic acidosis

      Acidosis due to?
    • 1. Glycolic acid/Oxalic acid
      2. Formic acid
      3. Acetic acid
      4. Lactic acid
    • Ethyene glycol toxicity?
    • 1. CNS depression
      2. Acidosis
      3. Nephrotoxicity
    • Methanol toxicity?
    • 1. CNS depression
      2. Acidosis
      3. Ocular damage`
    • Ethanol toxicity?
    • 1. CNS depression
      2. Acidosis
      3. Acetaldehyde toxicity

      Acetaldehyde toxicity?
    • 1. NV
      2. Headache
      3. Hypotension
      4. Folate deficiency(inactivation)
      5. Thaimine deficiency(absorption)
    • Drugs that cause disulfiram like effect?
    • 1. Metronidazole
      2. Cefoperazone
      3. Cefotetan
      4. Chlorpropamide
      5. Griseofulvin
      6. Omeprazole
      7. Aripiprazole
      8. Ketoconazole
    • Component in alcohol metabolism responsible for hangover?
    • Acetaldehyde
    • Fetal alcohol syndrome?
      Mechanism of effects?
    • 1. Growth restriction
      2. Midfacial hypoplasia
      3. Microcephaly
      4. Mental retardation

      Mechanism:
      Inhibition of cell migration
    • Fomepizole: MOA?
    • 1. Inhibitor of alcohol dehydrogenase

      (high alcohol levels require hemodialysis)
    • MCC of Mental retardation?
    • Fetal alcohol syndrome
    • Anticonvulsants:
      Drugs and MOA?
    • 1. Block Na channels in inactive state:
      a. Phenytoin
      b. Carbamazepine

      2. Facilitation of GABA:
      a. Barbiturates
      b. benzodiazepines

      3. Block glutamate receptors:
      a. Lamotrigine (AMPA)
      b. Topiramate (AMPA)
      c. Felbamate (NMDA)

      4. Block T-type Ca channels:
      a. Ethosuxamide
      b. Valproic acid
    • DOC for partial seizures?
    • 1. Phenytoin
      2. Carbamazepine
      3. Valproic acid
    • DOC for General- tonic clonic seizures?
    • 1. Phenytoin
      2. Carbamazepine
      3. Valproic acid
    • DOC for absence seizures?
    • 1. Ethosuxamide
      2. Valproic acid
    • DOC for status epilepticus?
    • 1. Lorazepam
      2. Diazepam
      3. Phenytoin
      4. Fosphenytoin
    • Advantages of using fosphenytoin over phenytoin for antiseizure medication?
    • Fosphenytoin- more water soluble
    • Barbiturates not used for Rx of status epilepticus?
    • Prolonged opening of Cl- channels --> hydrops/swelling --> Irreversible neurological damage
    • T-type ca channel blockers?
      L-type ca channel blockers?
    • T-type:
      1. Ethosuxamide
      2. Valproic acid
      3. "Dipines"

      L-type:
      1. Verapamil
      2. Ethosuxamide
    • Phenytoin:
      MOA?
      Uses?
    • MOA:
      1. Blocks axonal sodium channels (in blocked/inactivated state)
      "DOSE DEPENDENT BLOCKING of Na channels"

      2. Inhibits glutamate release

      3. Prevents seizure PROPAGATION


      Uses:
      Seizures: Partial/GTCS
    • Phenytoin: Pharmacokinetics?
    • 1. Variable absorption
      2. Non linear kinetics for absorption
      3. Cytochrome P450 induction
      4. Zero order kinetics for elimination


      **
      1. Increased absorption followed by plateau
      2. Constant elimination independent of concentration of drug in blood

      Therefore requires therapeutic drug monitoring. Tendency to accumulate enough to cause toxicity.
    • Phenytoin: side effects?
    • 1. CNS depression
      2. Hirsutism
      3. Gingival hyperplasia
      4. Megaloblastic anemia
      5. Aplastic anemia
      6. Osteomalacia
      7. Teratogenic effects:
      a. Cleft lip and palate
      b. Microcephaly
      c. Hypoplastic nails/fingers
      d. IUGR
      e. Development delay
      f. Craniofacial feature defects
    • Gingival hyperplasia-

      1. CCBs
      2. Phenytoin
      3. Cyclosporine
    • Fetal hydantoin syndrome?
    • Fetal hydantoin syndrome:
      Phenytoin teratogenicity

      a. Cleft lip and palate
      b. Microcephaly
      c. Hypoplastic nails/fingers
      d. IUGR
      e. Development delay
      f. Craniofacial feature defects
    • Carbamazepine:
      MOA?
      Uses?
    • Blocks inactivated Na channels

      Uses:
      1. Seizures
      2. Bipolar disorders
      3. Trigeminal neuralgia
    • Carbamazepine:
      Pharmacokinetics?
    • Induction of cytochrome P450
    • Carbamazepine:
      Side effects?
    • 1. CNS depression
      2. Megaloblastic anemia
      3. Aplastic anemia (agranulocytosis)
      4. Osteomalacia

      5. SJS/ Exfoliative dermatitis

      6. Dilutional hyponatremia
      (increased ADH secretion)

      7. Teratogenic:
      i. Cleft lip and palate
      ii. Spina bifida

      8. Diplopia
      9. Ataxia
    • Valproic acid: MOA?
    • 1. Block inactivated Na channels
      2. Inhibition of GABA transaminase
      3. Blockade of T-type Ca channel


      "Wall off like a pro" : block everything
    • Valproic acid: Uses?
    • 1. Seizure states(all)
      2. Bipolar mania
      3. Migraines


      Seizure states inclusive of:
      1. Absence seizures
      2. Myoclonic seizures
    • Valproic acid: pharmacokinetics?
    • Inhibits cytochrome P450
    • Antiseizure drugs and effect on P450?
    • Induced by:
      Carbamazepine
      Phenytoin

      Inhibited by:
      Valproic acid
    • Valproic acid: side effects?
    • 1. Hepatotoxicity
      2. Thombocytopenia
      3. Pancreatitis
      4. Alopecia
    • Drugs used in trigeminal neuralgia?
    • 1. Amitryptiline
      2. B-blockers
      3. Carbamazepine
      4. Gabapentin

      Drugs used in trigeminal neuralgia:
      "ABC" and gabapentin
    • Drug used in bipolar disorder and seizures?
    • 1. Carbamazepine
      2. Valproic acid
    • Drug used as IB a/arrhythmic and Seizures?
    • Phenytoin
    • A/seizure drugs causing:
      1. Thromocytopenia
      2. Agranulocytosis
      3. SJS
      4. Pancreatitis
      5. Osteomalacia
      6. Dilutional hyponatremia
      7. Alopecia
      8. Hepatotoxicity
      9. Dilantin embropathy
      10. Ataxia?
    • 1. Thrombocytopenia:
      Valproic acid

      2. Agranulocytosis:
      Phenytoin
      Carbamazepine

      3. SJS:
      i. Lamotrigine
      ii. Felbamate
      iii. Carbamazepine
      iv. Ethosuximide

      4. Pancreatitis:
      Valproic acid

      5. Osteomalacia:
      i. Phenytoin
      ii. Carbamazepine

      6. Dilutional hyponatremia:
      Carbamazepine

      7. Alopecia:
      Valproic acid

      8. Hepatotoxicity:
      i. Valproic acid
      ii. Lamotrigine
      iii. Felbamate

      9. Dilantin embryopathy:
      Phenytoin

      10. Ataxia:
      i. Gabapentin
      ii. Carbamazepine
      iii. Phenytoin
    • A/seizure drug causing"
      "Fizzy Kinky hair"?
    • Valproic acid (alopecia)
    • Antiseizure drug associated with:
      i. Spina bifida
      ii. Cleft lip/palate
      iii. Cleft lip/palate + Spina bifida?
    • Cleft lip/palate: Phenytoin

      Spina bifida: Valproic acid

      Cleft lip/palate + Spina bifida: Carbamazepine
    • Pharmac Drugs inducing pancreatitis?
      (Step 1 relevant)
    • 1. Alcohol
      2. Valproic acid

      3. Didanosine
      4. Zalcitabine
      5. Asparagine
    • Drugs that increase ADH secretion?
      (Step-1 relevant)
    • 1. Antipsychotics
      2. Antidepressants
      3. Anti convulsant: Carbamazepine

      Drug that decreases ADH?
    • Lithium
    • Drugs associated with lupus-like syndrome
    • 1. Phenytoin
      2. Isoniazid
      3. Hydralazine
      4. Procainamide
    • Antiseizure drug also used for migraines?
    • Valproic acid
    • Ethosuximide:
      MOA?
      Use?
    • MOA: T Ca channel blockade in THALAMUS
      Use: Absence seizures
    • Phenytoin/carbamazepine: effect on OC pill effect?
    • Effect mitigated due to P450 induction
    • OC pill effect enhanced by ____(a/seizure drug)
    • Valproate- inhibition of P450
    • Safest antiseizure drug for pregnancy?
    • Phenobarbital
    • Felbamate and lamotrigine: MOA?
    • 1. Block Na channels
      2. Block glutamate receptors

      (felbamate blocks glutamate)
    • Gabapentin: MOA? uses?
    • MOA:
      1. Enhances GABA effects
      2. Blocks Ca channels

      Uses:
      1. Seizures
      GTCS and Partial
      2. Neuropathic pain
    • DOC for seizure(status epilepticus) prophylaxis?
    • Phenytoin
    • DOC for GTCS?
    • Phenytoin
      Carbamazepine
      Valproic acid
    • DOC for Absence seizures?
    • Ethosuximide
    • DOC for Status epilepticus?
    • BZDs-
      Diazepam
      Lorazepam
    • Felbamate: side effects?
    • 1. SJS
      2. Hepatoxicity
      3. Aplastic anemia
    • Lamotrigine: side effects?
    • 1. SJS
      2. Hepatoxicity
      3. Aplastic anemia
    • Anticonvulsants have additive side effects with ______?
    • CNS depressants
    • Antiseizure drug that may predispose to infective endocarditis?
    • Phenytoin
      (gingival hyperplasia-->gingivitis--> septicemia--> infective endocarditis)
    • Antiseizure drug associated with cerebral herniation?
    • Carbamazepine
      (increased ADH--> dilutional hyponatremia--> neuronal hydrops + raised ICT---> herniation)