Final EXAM Pharmacology

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Final EXAM Pharmacology
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  1. Myoclonic, Atonic, Atypical Absence
    Seizures treatment drug of choice
    Valproic acid
  2. •Blocks calcium ion influx in thalamus;
    blocks T-type calcium ion channels

    •Inhibits Na+/K+ ATPase, depresses the
    cerebral metabolic rate, and inhibits GABA aminotransferase
    •Clinical use– absence seizures
    •Drug of choice for petit mal seizures
    Ethosuximide (Zarontin®)
  3. •ADR: gastric distress (pain, nausea,
    vomiting), dizziness, drowsiness, ataxia, sedation, renal, hepatic, bone marrow
    toxicity
    Ethosuximide
  4. •Structurally
    related to the tricyclic antidepressants
    •Works
    on seizure focus, decreases Na+ influx therefore decreasing repetitive firing
    from seizure focus
    •Clinical
    Use: complex partial seizures, generalized tonic-clonic seizures, mixed seizures, trigeminal
    neuralgia
    Carbamazepine (Tegretol®)
  5. •ADR: dizziness,  diplopia, hyponatremia, unsteadiness, nausea,  skin rash, hepatic dysfunction, vomiting, xerostomia,
    diarrhea, jaundice, aplastic anemia (rare)
    Carbamazepine
  6. •Structurally related to GABA, exact
    mechanism unknown but may alter GABA metabolism or nonsynaptic
    release
    •Clinical use: partial seizures adjunct,
    generalized tonic-clonic seizures, chronic pain control adjunct
    Gabapentin (Neurontin®)
  7. •ADR: somnolence, drowsiness, ataxia,
    headache, tremor, sedation, renal, hepatic and bone marrow toxicity
    Gabapentin
  8. •Secondary agent in epilepsy treatment

    •Bind to GABAA receptor in neuronal membranes to
    increase the efficiency of GABAergic synaptic inhibition, leading to a
    decrease in the firing rate of critical neurons in the brain
    •Clinical Use: Lennox-Gestaut
    Syndrome, Akinetic,
    Absence & Myoclonic Seizures
    Clonazepam (Klonopin®)
  9. •ADR: sedation, tolerance, ataxia,
    drowsiness, dependence, hypersensitivity
    Clonazepam
  10. •Exact mechanism of action unknown, but
    may suppress abnormal neurons, inhibiting the spread and suppressing firing
    from the foci, enhances GABA, suppresses excitatory action of glutamic acid

    •Clinical Use: Tonic-Clonic
    seizures, Simple Partial Seizures
    Phenobarbital (Luminol®)
  11. •ADR: sedation, paradoxical excitement in
    elderly and peds, exfoliative
    dermatitis, megaloblastic anemia, dependence, tolerance,
    withdrawal
    Phenobarbital
  12. •Decreases
    post-tetanic potentiation, decreases Na+ influx during depolarization,
    decreases Ca++
    influx, decreases K+ efflux (slows repolarization), blocks reuptake of GABA
    •Clinical
    Use: Generalized tonic-clonic seizures, complex partial seizures, pre-
    & post-surgical seizure, prophylaxis, status epilepticus
    Phenytoin (Dilantin®)
  13. •ADR: dizziness, drowsiness, ataxia,
    tremors, epigastric
    pain, gingival hyperplasia, hirsutism, hepatitis, coarsening of facial
    features, abnormalities in vitamin D metabolism (chronic use),  diplopia, low folate levels, megaloblastic anemia

    •Fetal Hydantoin Syndrome
    Phenytoin
  14. •Therapeutic serum level : 10-20 mcg/ml

    •DI: Enzyme inducer, may interfere with
    thyroid function test, plasma protein binding site displacement with
    sulfonamides, sulfonylureas, phenylbutazone, isoniazid inhibits metabolism of
    phenytoin
    Phenytoin
  15. •Pro-drug of phenobarbital
    •Decreases post tetanic potentiation,
    decreases spread of seizure focus, may decrease sodium entrance into neurons
    •Clinical Use: Tonic-Clonic
    Seizures, Partial Seizures
    Primidone (Mysoline®)
  16. •ADR:
    drowsiness, sedation, dizziness, ataxia, exfoliative dermatitis, megaloblastic anemia (rare), contraindicated with
    phenobarbital
    Primidone
  17. •Activity related to increased brain
    levels of GABA, may decrease sodium influx and prevent repetitive firing of
    seizure focus

    •Clinical Use: Simple and Complex Absence
    Seizures, Generalized Tonic-Clonic and Partial Seizures in the presence of
    Absence Seizures
    Valproic Acid (Depakote®)
  18. •ADR: 
    nausea, vomiting, abdominal pain, heartburn, fine tremor, weight gain,
    increased appetite, hair loss, idiosyncratic hepatotoxicity, constipation,
    sedation skin rash, weakness, thrombocytopenia

    •Increased incidence of spina
    bifida in offspring of women who took drug during pregnancy
    Valproic Acid
  19. •DI:
    inhibits its own metabolism at low doses, displaces phenytoin from plasma
    protein binding sites, inhibits metabolism of phenobarbital, phenytoin,
    carbamazepine
    Valproic Acid
  20. •Suppresses sustained rapid firing of
    neurons and inactivates sodium channels
    •Clinical Use: Partial Seizures, Myoclonic
    and Absence Seizures in Children
    Lamotrigine (Lamictal®)
  21. •ADR: dizziness, headache, diplopia,
    nausea, somnolence, rash
    Lamotrigine
  22. •Weak inhibitory effect on GABA receptor
    binding and benzodiazepine receptor binding
    •Clinical Use: Partial Seizures, Lennox-Gestaut
    Syndrome (third line agent)
    Felbamate (Felbatol®)
  23. •ADR:
    anorexia, vomiting, insomnia, nausea, dizziness, somnolence, headache, aplastic
    anemia, severe hepatitis
    •DI:
    increases plasma phenytoin and valproic acid levels, decreases levels of
    carbamazepine
    Felbamate
  24. •Blocks the repetitive firing of cultured
    spinal cord neurons, blocking of voltage dependent sodium channels, potentiate
    inhibitory effect of GABA
    •Clinical Use: Partial and Generalized
    Tonic-Clonic
    Seizures
    Topiramate (Topamax®)
  25. •Inhibits reuptake of GABA into
    presynaptic neurons and glial cells

    •Approved as adjunctive therapy in adults
    with partial and generalized tonic-clonic seizures
    Tiagabine (Gabitril®)
  26. •ADR:
    dizziness, lack of energy, somnolence, nausea, nervousness, tremor, generalized
    muscle weakness, difficulty with concentration or attention
    •DI:
    displaced from plasma protein binding sites by naproxen, valproic
    acid and salicylates
    •Caution:
    erythromycin & ketoconazole
    Tiagabine
  27. •With chronic use, the ADR of this drug
    include coarsening of facilal features, hirsutism, and gingival hyperplasia.

    –A) carbamazepine

    –B) ethosuximide

    –C) gapapentin

    –D) phenytoin
  28. –D) phenytoin
  29. •Which drug is most effective against
    absence seizures without the risk of development of excessive sedation and
    tolerance?

    –A) clonazepam

    –B) phenobarbital

    –C) ethosuximide

    –D) felbamate
    –C) ethosuximide
  30. Curare, active crude material •Tubocurarine
    & synthetic derivatives
    Neuromuscular Blocking Agents
  31. Control of ventilation
    Management of convulsions
    Surgical procedures
    Neuromuscular Blocking Agents--Uses
  32. •Non-Depolarizing—blocks
    acetylcholine binding to the nicotinic receptor (antagonist)

    •Depolarizing–
    2 phases of mechanism of action, reacts with the nicotinic receptor to cause
    depolarization  (1), although
    repolarization takes place as long as succinylcholine is present no more
    depolarization can occur (2) (agonist)
    Neuromuscular Blocking Agents
  33. •Compete with acetylcholine at nicotinic receptor site

    •Prototypeis tubocurarine

    •Blockade may be reversed with cholinesterase inhibitors (edrophonium,
    neostigmine, physostigmine)
    Non-Depolarizing Agents
  34. Atracurium  Cisatracurium

    Doxacurium  Metocurine

    Mivacurium  Tubocurarine
    • Non-Depolarizing Agents
    • Isoquinolone Derivatives
  35. Pancuronium  Pipecuronium

    Rocuronium  Vecuronium
    • Non-Depolarizing Agents
    • Steroid Derivatives
  36. •After IV administration, first causes motor weakness, skeletal muscles become flaccid
    and inexcitable

    •Larger muscles more resistant to block and recover more rapidly than smaller muscles

    •Diaphragm is last muscle to be paralyzed

    •Recovery occurs in reverse order
    Non-Depolarizing Agents
  37. •Pancuronium caused a moderate increase in heart rate

    •Vecruonium, pipecruonium, doxacurium, cisatracurium, rocuronium
    –little or no CV effects

    •Tubocurarine, metocurine, mivacurium, atracurium--hypotension
    Non-Depolarizing Agents
  38. •Duration of action 5-10 minutes, due to rapid hydrolysis by plasma cholinesterase

    •Causes various cardiac arrhythmias (esp. bradycardia)

    •Other ADR: hyperkalemia, increase IOP, increase intragastric pressure, muscle pain
    Depolarizing Agents--Succinylcholine
  39. •Diazepam

    •Baclofen

    •Tizanidine

    •Dantrolene

    •Botulinum
    Toxin
    Spasmolytic Agents
  40. •Benzodiazepine
    with antispastic, anxiolytic, hypnotic, anticonvulsant properties

    •Relieves muscle spasms associated with paraplegia and cerebral palsy

    •Potentiates action of GABA resulting in increased neuroal
    inhibition and CNS depression
    Diazepam
  41. •Controlled substance

    •Contraindicated in narrow angle glaucoma

    •Cimetidine, oral contraceptives, disulfiram
    increase effects of diazepam

    •Diazepam may increase serum digoxin concentration

    •Omeprazole may increase diazepam levels and effects
    Diazepam
  42. •GABA-mimetic agent, GABA agonist at GABAB
    receptors

    •As effective as diazepam for reducing spasticity but causes much less sedation

    •Does not reduce general muscle strength

    •Intrathecal administration may be used for patients unresponsive to other medications
    Baclofen
  43. •CI: spasms from rheumatic disorders, stroke, cerebral palsy and parkinson’s
    disease

    •CNS depressants may cause increased sedative effects

    •Epidural morphine may cause hypotension and dyspnea
    Baclofen
  44. •Congener of clonidine

    •Significant alpha 2 adrenoceptor
    agonist effects but reduces spasticity with less hypotension than clonidine

    •ADR: drowsiness, hypotension, dry mouth, asthenia
    Tizanidine
  45. Reduces skeletal muscle strength by interfering with excitation-contraction coupling in
    the muscle fiber– site of action is sarcoplasmic reticulum in skeletal muscle
    (interferes with calcium release)

    Manages malignant hyperthermia (triggered by anesthesia, NMBA
    Dantrolene
  46. •CV:  tachycardia, erratic blood pressure,
    phlebitis

    •RESP:  pleural effusion with pericarditis, pulmonary
    edema (IV)

    •CNS:
    drowsiness, dizziness, weakness, general malaise, fatigue, speech disturbances,
    seizures, HA, insomnia

    •EENT:
    visual disturbances, diplopia, alteration of taste

    •GI:
    D, constipation, dysphagia, abdominal cramps
    Dantrolene--ADR
  47. •Local injection in treatment of generalized spastic disorders due to neurologic
    injury
    Botulinum Toxin
  48. •Carisoprodol

    •Chlorphenesin

    •Chlorzoxazone

    •Cyclobenzaprine

    •Metaxalone

    •Methocarbamol

    •Orphenadrine
    Drugs used for Acute Local Muscle Spasm
  49. •Relief of acute temporary muscle spasm caused by local trauma or strain
    •Many act as sedatives or at the level of the spinal cord or brain stem
    Acute Local Muscle Spasm Agents
  50. •Reversibly block impulse conduction along nerve axons and other membranes that use sodium
    channels as the primary means of action potential generation

    •Work by:
    blocking pain sensation from specific areas of the body

    –blocking sympathetic vasoconstrictor impulses to specific areas of the body
    Local Anesthetics
  51. •Administered by injection into the area of the nerve fibers to be blocked
    •Absorption and distribution more associated with offset of anesthesia rather than onset of
    action
    Local Anesthetics
  52. •Vasoconstrictor substances like epinephrine reduce the amount of systemic absorption from the depot site of injection by reducing blood flow in these areas
    Local Anesthetics
  53. •Use of epinephrine in the spinal cord stimulates alpha 2 receptors, causing a
    decrease in substance P release and reduce sensory neuron firing
    Local Anesthetics
  54. •Benzocaine

    •Bupivacaine

    •Lidocaine

    •Procaine

    •Tetracaine
    Local Anesthetics
  55. Procaine, chloroprocaine
    Short acting Local Anesthetics
  56. Lidocaine, mepivacaine, prilocaine
    Intermediate acting Local Anesthetics
  57. Tetracaine, bupivacaine, etidocaine, ropivacaine
    Long acting Local Anesthetics
  58. •Tachyphylaxis (repeated injections cause a decrease in effectiveness)
    •CNS:sleepiness, lightheadedness, circumoral or tongue numbness, nystagmus,
    muscular twitching, seizures
    ADR/Toxicity of Local Anesthetics
  59. •Peripheral Nervous System:  high concentrations
    demonstrate toxicity to nerve tissue– numbness, tingling, sensory and motor
    deficiency 
    •CV: hypotension, cardiovascular collapse, arrhythmias (bupivacaine is the most cardiotoxic of the local anesthetics)
    •Other ADR: methemoglobinemia (prilocaine),
    allergic reactions
    ADR/Toxicity of Local Anesthetics
  60. •Amide type-
    •Metabolized
    in liver-
    •Mepivacaine, lidocaine,bupivacaine
    •Longduration of action
    •Cross placenta- fetal effects for 24-48 hours after birth
    Local Anesthetics-Amide
  61. •ADR maternal: respiratory depression, urinary retention, nausea, vomiting
    •Can be used to deliver morphine or fentanyl but itch that develops is not relieved
    by diphenhydramine or naloxone, therefore use PCA or other forms of pain relief
    •Commonly used
    Continuous Epidural Block
  62. •Bupivacaine  
    •Chloroprocaine  
    •Etidocaine  
    •Lidocaine 
    •Mepivacaine 
    Ropivacaine
    epidural use
  63. halothane, methoxyflurane, nitrous oxide, enflurane, desflurane, isoflurane, sevoflurane
    Inhaled general anesthetics
  64. etomidate, fentanyl, ketamine, midazolam, propofol, thiopental
    Intravenous general anesthetics
  65. •MOA:
    depress spontaneous and evoked activity of neurons in the brain

    •Increases
    in the inspired anesthetic concentration will increase the rate of induction of
    anesthesia by increasing the rate of transfer into the blood

    •During induction, organs with the highest perfusion will exert the greatest influence
    on the arterial-venous concentration gradient (liver, kidneys, brain, heart)
    Inhaled Anesthetics
  66. Thiopental, propofol, methohexital
    • Barbiturates
    • Intravenous Anesthetics
  67. Midazolam, diazepam, lorazepam
    • Benzodiazepines
    • Intravenous
    • Anesthetics
  68. Fentanyl, morphine
    Opioid
  69. •Produces anesthesia at a rate comparable to that of the ultra short acting barbiturates,
    but renders a much more rapid recovery

    •Mayhave antiemetic properties

    •May be used for both induction and maintenance of anesthesia

    •ADR:apnea, pain at injection site, tremors
    Propofol
  70. •Sedative-hypnotics that readily cross the blood-brain barrier

    •High incidence of anterograde amnesia, may also prolong post-anesthesia recovery
    period
    Benzodiazepines
  71. •Trihexyphenidyl (Artane®)

    •Procyclidine (Kemadrin®)

    •Benztropine (Cogentin®)

    •Biperiden (Akineton®)

    •Diphenhydramine (Benadryl®)
    Anticholinergics
  72. •ADR:  drowsiness, mental slowness, inattention,
    restlessness, confusion, agitation, delusions, hallucinations, mood changes,
    dry mouth, blurry vision, mydriasis, urinary retention, nausea,
    vomiting, constipation, tachycardia, tachypnea, increased IOP, palpitations,
    cardiac arrhythmias
    Anticholinergics
  73. •Inhibitory neurotransmitter that
    will not cross the blood-brain barrier if administered into the periphery

    •Levodopa, an immediate metabolic
    precursor of dopamine will cross the blood brain barrier to be decarboxylated in the brain to dopamine
    Dopamine
  74. •ADR: dystonic movements,
    palpitations, orthostatic hypotension, mental changes, depression, anorexia,
    nausea, vomiting, dry mouth, dysphagia, headache, dizziness, numbness, bruxism
    Levodopa
  75. •is contraindicated in patients with
    psychotic illness or narrow angle glaucoma

    • is not to be administered
    concomitantly with MAO-A inhibitors or within 2 weeks of their withdrawal

    •may exacerbate peptic
    ulcers or malignant melanoma
    Levodopa
  76. •Amantadine (Symmetrel®)

    •Bromocriptine (Parlodel®)

    •Pergolide (Permax®)

    •Pramipexole (Mirapex®)

    •Ropinirole (Requip®)
    Dopamine Agonists
  77. •Prophylactic for influenza A2 virus

    •Increases dopamine release from
    neurons and blocks dopamine reuptake

    •ADR: confusion, ataxia, sleep
    disorders, tremors, hallucination, anorexia, nausea, vomiting, orthostatic
    hypotension, edema, slurred speech, anticholinergic effects
    Amantidine
  78. •Direct dopaminergic agonist

    •Causes
    fewer abnormal involuntary movements than levodopa, but more mental aberrations

    •ADR: nausea,anorexia, vomiting, constipation, dyskinesias, nasal congestion, orthostatic
    hypotension, constipation, headache, fatigue, hallucinations
    Bromocriptine
  79. •Direct acting dopaminergic agonist
    at D1 & D2 receptors

    •As effective as bromocriptine but with a longer duration of
    action

    •ADR  profile similar to that of bromocriptine

    •Tends to lose efficacy over time
    Pergolide
  80. •Non-ergot dopamine agonist with
    affinity for D2, D3, & D4 receptors ( highest affinity is
    for D3)

    •ADR: Nausea, dizziness, somnolence,
    insomnia, constipation, dry mouth, dystonia, dyspepsia

    •Idiopathic Parkinsons Disease
    Pramipexole
  81. •Non-ergot agonist with high
    affinity for D2 & D3 receptors with minimal activity
    for nondopaminergic receptors

    •ADR: similar to pramipexole except that somnolence and
    hallucination are less & orthostatic hypotension and dizziness are greater

    •Ciprofloxacin and ethinyl estradiol may increase levels of ropinirole due to their inhibition of
    cytochrome P-450 enzyme 1A2
    Ropinirole
  82. •Selectively inhibits monoamine oxidase B, inhibiting central dopamine metabolism

    •May delay need for levodopa, slow progression of symptoms, and prolongs
    employability

    •May be used as an adjunct in moderate to advanced disease, to reduce levodopa dose
    and decrease “wearing off” effect of L-dopa
    Selegiline (Eldepryl®)
  83. •ADR: insomnia, dizziness, headache,
    abdominal pain, lightheadedness, confusion, hallucination, benign cardiac
    arrhythmias, dry mouth, nausea, peptic ulcer disease, elevations in liver
    enzymes

    •Avoid in patients with history of
    dementia, frequent falls, & postural hypotension
    Selegiline
  84. •Peripherally active, when administered with levodopa is effective for “wearing off” symptoms

    •Avoid in patients with hepatic impairment

    •ADR: increased dopaminergic side effects (dyskinesias, GI disturbances, dizziness,
    hallucinations), dry mouth, darkening of urine, diarrhea, increased LFTs
    Entacapone (Comtan®)
  85. •Increased risk of CV ADR with
    concurrent administration of non-selective MAO inhibitors

    •DI: may inhibit metabolism of
    epinephrine, isoproterenol, apomorphine, dobutamine, methyldopa, nadolol; chelates iron
    Entacapone
  86. •ADR: similar to entacapone, due to risk of hepatocellular
    injury, monitor ALT/AST levels at baseline, q 2 weeks 1st year of therapy, then q 4 weeks
    for 6 months, then q 8 weeks thereafter

    •If ALT/AST levels increase to high
    normal levels-DC drug (also if jaundice, lethargy, anorexia, clay colored
    stools, pruritis)
    Tolcapone
  87. •Peripheral adverse effects of
    levodopa, including nausea, hypotension, and cardiac arrhythmias can be
    diminished by including which of the following?

    –A) Amantadine

    –B) Bromocriptine

    –C) Carbidopa

    –D) Entacapone
    –C) Carbidopa

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