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1
Q

Bromocriptine

A

Parkinson

  • **Dopamine agonist **
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2
Q

Pramipexole

A

Parkinson

  • **Dopamine agonist **
  • ergot
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3
Q

Ropinirole

A

Parkinson

  • Dopamine agonist
  • non ergot
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4
Q

Amantadine

A

Parkinson

  • **Increase dopamine release **
  • Toxicity
    • ataxia
  • Also used as antiviral against influenza A and rubella
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5
Q

L- Dopa

+

Carbidopa

A

Parkinson

  • Increase dopamine
  • L-dopa: converted to dopamine in CNS
    • can cross BBB
    • converted by dopa decarboxylase in CNS to dopamine
  • Carbidopa: peripheral dopa decarboxylase inhibitor
    • increases bioavailabilty of L-dopa in brain
    • limits peripheral side effects
    • no effect on CNS isde effect
  • Toxicity
    • arrhythmia- increased peripheral formation of catecholamines
    • dyskinesia (following administration)
    • akinesia (between doses)
    • CNS
      • anxiety, agitation, insomnia, confusion, delusions, hallucinations
  • Do not give with vit B6
    • increase coversion of l-dopa to dopamine in periphery
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6
Q

Selegiline

A

Parkinson

  • **Selective MAO- B inhibitor **
    • preferentially metabolizes dopamine
    • increasing availability of dopamine
  • Clinical use
    • adjuctive agent to L-dopa
  • Toxicity
    • may enhance adverse effects of L-dopa
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7
Q

Entacapone

A

Parkinson

  • COMT inhibitor
    • prevent L-dopa degradation
    • increase dopamine availability
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8
Q

Tolcapone

A

Parkinson

  • COMT inhibitors
    • prevent L-dopa degradation
    • increase levaopa availability
    • hepatotoxicity
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9
Q

Benztropine

A

Parkinson

  • **Antimuscarinic **
    • improves tremor, rigidity
    • little effect on bradykinesia
  • Use with drug induced parkinsonism from first generation antipsychotic
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10
Q

Memantine

A

Alzheimer’s Disease

  • NMDA receptor antagonist
    • prevent excitotoxicity
    • mediated by Ca++
  • Toxicity
    • Dizziness
    • Confusion
    • Hallucinations
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11
Q

Donepezil

A

Alzheimer’s

  • **AChE Inhibitors **
  • Toxicity
    • nausea
    • dizziness
    • insomnia
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12
Q

Galantamine

A

Alzheimer’s

  • AChE inhibitors
  • Toxicity
    • nausea
    • dizziness
    • insomnia
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13
Q

Rivastigmine

A

Alzheimer’s

  • AChE inhibitors
  • Toxicity
    • nausea
    • dizziness
    • insomnia
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14
Q

Tetrabenazine

A

Huntington’s

  • Inhibit VMAT
    • limit dopamine vesicle packaging and release
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15
Q

Reserpine

A

Huntington

  • Inhibit VMAT
    • limit dopamine vesicle packaging and release
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16
Q

Haloperidol

A

Huntington

  • **dopamine receptor antagonist **
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17
Q

Sumatriptan

A

Migraine + Cluster Headaches

  • 5-HT agonist
    • inhibits trigeminal nerve activation
    • prevents vasosctive peptide release (substance P + CGPR)
    • induces vasoconstriction
    • half life 2 hours
  • Toxicity
    • coronary vasospasm
      • dont use in CAD or prinzmetal’s angina
    • mild tingling
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18
Q

Succinylcholine

A

Neuromuscular Blocking Drugs

  • Muscle paralysis in surgery or mechanical ventilation
    • Selective for motor nicotinic receptor
  • Depolarizing
    • Binds ACh receptor keeping it depolarized
    • prevents muscle contraction
  • Reversal of blockage
    • phase 1: no antidote, block potentiated by cholinesteraes inhibitors
    • phase 2: antidote = cholinesteraes inhibitors
      • neostigmine
  • Complications
    • hypercalcemia
    • hyperkalemia
      • can lead to arrhythmias in peopel predisposed to hyperkalemia (burns, myopathies, crush injury, denervating injuries or disease)
    • *malignant hyperthermia *
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19
Q

Tubocurarine

Atracurium

Mivacurium

Pancuronium

Vecuronium

Rocuronium

A

Neuromusclar blocking drugs

  • Muscle paralysis in surgery or mechanical ventilation
    • selective for motor and nicotinic receptor
  • Nondepolarizing
    • Competitive ACh receptor antagonist
  • Reversalof blockage
    • neostigmine
    • edrophonium
    • cholinesterase inhibitors
20
Q

Dantrolene

A

Malignant Hyperthermia

  • **Prevent Ca++ release from sarcoplasmic reticulum of skeletal muscle **
  • Malignant Hyperthermia
    • life threatening
    • inherited susceptibility
  • Neuroleptic malignany syndrome
    • toxicity of antipsychotic drugs
21
Q

Procaine

Cocaine

Tetracaine

A

Local anesthetic

  • Ester = “caine”
  • Mechanism
    • block activated Na+ channels
      • specifically inhibit rapidly firing neurons
  • Principle
    • give with vasoconstrictors (epi) to enhance local action
      • decrease bleeding
      • increase anesthesia
      • decrease systemic concentration
    • Infected tissue (acidic)
      • need more anesthetic
        • alkaline are charged adn can’t penetrate membrane
  • Clinical use
    • minor surgical procedures
    • spinal anesthesia
  • toxicity
    • CNS excitation
    • HTN
    • Hypotension
    • Arrhythmias = cocaine
22
Q

Local anesthetic

nerve blockade order

A
  • Small diameter > large diameter
  • Myelinated > unmyelinated
  • Size > Myelination
  • Small myelinated > small unmyelinated > large myelinated > large unmyelinated
  • Order of loss
    • pain > temp > touch > pressure
23
Q

Lidocaine

A

Local anesthetic

  • Amide = two i
  • Mechanism
    • block activated Na+ channels
      • penetrate membrane in uncharged form then bind channel in charged form
      • most effective in rapidly firing neurons
  • Principles
    • give with vasoconstrictors (epi) to enhance local action
      • decrease bleeding
      • increase anesthesia
      • decrease systemic concentration
    • Infected tissue (acidic)
      • need more anesthetic
        • alkaline anesthetics cant penetrate membrane
  • Clinical use
    • minor surgical procedures
    • spinal anesthesia
  • Toxicity
    • CNS excitation
    • HTN
    • Hypotension
24
Q

Mepivacaine

A

Local anesthetic

  • amide = 2 i
  • Mechanism
    • block activated Na+ channels
      • penetrate membrane in uncharged form and bind channel in charged form
      • most effective in rapidly firing neurons
  • Principle
    • give with vasoconstrictors (epi) to enhance local action
      • decrease bleeding
      • increase anesthesia
      • decrease systemic concentration
    • infected tissue (Acidic)
      • need more anesthetic
        • alkaline anesthetics are charged so cant pennetrate membrane
  • Use
    • minor surgical procedures
    • spinal anesthetica
  • Toxicity
    • CNS excitation
    • HTN
    • Hypotension
25
Bupivacaine
local anesthetic * Amide = 2 i * Mechanism * **Block active Na+ channels** * penetrate membrane in uncharged form adn bind ion channel in charged form * most effective in rapidly firing neurons * Principle * give with vasoconstrictors (epi) to enhance local action * decrease bleeding * increase anesthesia * decrease systemic concentration * infected tissue (Acidic) * give more anesthetic * alkaline anesthetics charged and can't penetrate membrane * Use * minor surgeries * spinal anesthesia * Toxicity * CNS excitation * **severe CV toxicity** * HTN * Hypotension
26
Thiopental
IV anesthetic * **Barbituate** * high potency, high lipid solubility * rapid entry into brain * Use * Anesthesia induction * short surgical procedures * characteristics * **rapid redistribution into tissue and fat** * decreases cerebral flow
27
Midazolam
IV anesthetic * **Benzodiazapine** * Use * endoscopy * use with gaseous anesthetics and narcotics * Toxicity * severe postop respiratory depression * decrease BP * give flumazenil * amnesia
28
Ketamine
IV anesthetic * Aka: arylcyclohexamines * PCP analog * **Block NMDA receptor ** * *CV stimulant* * *increase cerebral blood flow * * Toxicity * disorientation * hallucinations * bad dreams
29
Morphine
IV anesthetics * **opioid** * Use * general anesthesia * use with other CNS depressants
30
Fentanyl
IV anesthetics * Opioid * Use * general anesthesia * use with other CNS depressants
31
Proprofol
IV anesthetic * Potentiation GABA * Less postop nausea than thiopental * Use * sedation in ICU * rapid anesthesia induction * short procedures
32
Modafinil
Narcolepsy * Pyschostimulant * non amphetamine * first line * effective * well tolerated * drug abuse is rare
33
Pentazocine Class MOA Use Toxicity
* opioid analgesic * MOA: Partial agonist adn weak antagonist at mu receptors * Use: * effective analgesia with little abuse potential * Toxicity * Used in combo with full opioid agonists --\> competitively inhibit mu receptors and produce antagonist effects reducing analgesic effect * Patient dependent on opioid (morphine) --\> withdrawal symptoms
34
Cyproheptadine - MOA - Use
* MOA * 1st generation histamine antagonist * nonspecific 5-HT1 and 5-HT2 receptor antagonist properties * Use * Serotonin syndrome * Serotonin Syndrome * neuromuscular excitation * hyperreflexia * clonus * myoclonus * rigidity * flushing * diarrhea * seizures * autonomic stimulation * hyperthermia * tachycardia * CV collapse * diaphoresis * tremor * altered mental status * agitation * confusion
35
Phentyoin
* seizure * simple * complex * tonic clonic- first line * status epilepticus- first line * moa * increase Na+ channel inactivation * toxicity * nystagmus * diplopia * ataxia * sedation * gingival hyperplasia * hirsutism * megoblastic anemia * teratogen * fetal hydantoin syndrome * SLE like syndrome * CYP induce * lymphadenopathy * steven johnson syndrome
36
Carbamazepine
* seizures * simple- 1st line * complex- 1st line * tonic clonic- 1st line * trigeminal neuralgia * Bipolar - mood stabilizer * moa * increase Na+ channel ianctivation * toxicity * diplopia * ataxia * blood dyscarasias * agranulocytosis * aplastic anemia * liver toxicity * teratogen * Cyp inducer * SIADH * Steven johnson
37
Lamotrigine
* seizures * simple * complex * tonic-clonic * moa * blocks voltage gated Na+ channels * toxicity * steven johnson syndrome
38
Gabapentin
* seizures * simple * ecomplex * tonic clonic * peripheral neuropathy * postherpetic neuralgia * migraine prophylaxis * bipolar * moa * inhibit high voltage activated Ca++ channels * GABA analog * toxicity * sedation * atazia
39
Topiramate
* seizures * simple * complex * tonic clonic * migraine prevention * moa * block Na+ channels * increase GABA action * toxicity * sedation * mental dulling * kidney stones * weight loss
40
Phenobarbital
* seizures * simple * complex * tonic-clonic * 1st line kids * moa * increase GABA action * increase **duration** fo Cl- openning * toxicity * Respirator and CV depression * can be fatal * Sedation * CNS depression exacerbated by alcohol * tolerance * dependence * CYP inducer
41
Valproic acid
* seizues * simple * complex * tonic clonic- first line * absence * myoclonic seizures * Bipolar --\> mood stabilizer * use if poor kidneys b/c can't give lithum (renal excretion) * moa * increase Na+ channel inactivation * increase GABA concentration * toxicity * GI distress * rare but fatal hepatotoxicity (measure LFT) * teratogen- neural tube defects * spina bifida * tremor * weight gain
42
ethosuximide
* seizures * absence- 1st line * moa * block thalamic t type Ca+ channels * toxicity * GI distres * fatigue * headache * urticaria * steven johnson syndrome
43
Benzodiazepines diazepam lorazepam
* seizures * status epilepticus - 1st line * moa * increase GABA actio * increase **frequency** of Cl- channel openning * toxicity * sedation * do not give with alcohol, barbituatesm, neuroleptics, 1st generation antihistamines * tolerance * dependence
44
Tiagabine
* seizures * simple * complex * moa * inhibit GABA reputake
45
Vigabatrin
* seizures * simple * complex * moa * irreversible inhibit GABA transaminase * increase GABA
46
Levetiracetam
* seizures * simple * complex * tonic-clonic * mechanism * unknown
47
Primidone
* seizures * essential tremors * moa * metabolized into phenobarbital + phenylethylmalonamide (PEMA)

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