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Pharmacology > Sedatives, Anxiolytics, Anticonvulsant > Flashcards

Sedatives, Anxiolytics, Anticonvulsant Flashcards

0
Q

Drugs that produce drowsiness and encourage the onset and maintenance of a state of sleep. Involve more pronounced CNS depression than sedation

A

Hypnotics

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1
Q

Drugs that reduce anxiety and exert calming effect

A

Sedatives (anxiolytics)

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2
Q

Major inhibitory neurotransmitter?

A

GABA - Glycine in the spinal cord

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3
Q

Major excitatory neurotransmitters?

A

Glutamate, aspartate (dicarboxylate)

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4
Q

Short acting benzodiazepine, for acute anxiety, anesthesia induction, preoperative sedation. May cause anterograde amnesia. And has additive CNS depression with ethanol

A

Midazolam

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5
Q

Intermediate acting benzodiazepine, for anxiety disorders, insomnia, tranquilizer. With additive CNS depression with ethanol

A

Lorazepam

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6
Q

What abnormal sleep pattern results from use of benzodiazepines?

A

Decreased REM sleep

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7
Q

Long acting benzodiazepine, for anxiety disorder, skeletal muscle relaxation, alcohol withdrawal. May cause anterograde amnesia.

A

Diazepam - binds GABA A receptor subunits to increase frequency of chloride channel opening. Membrane hyperpolarization

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8
Q

Benzodiazepine drug used as a date-rape drug.

A

Flunitrazepam together with Alcohol (most common) and Gamma hydroxybutyrate

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9
Q

Which benzodiazepine has the longest half life?

A

Chlordiazepoxide

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10
Q

Preferred benzodiazepine: anticonvulsant maintenance

A

Clonazepam - intermediate

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11
Q

Preferred benzodiazepine: status epilepticus

A

Lorazepam and diazepam

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12
Q

Preferred benzodiazepine: skeletal muscle relaxation

A

Diazepam - eg. Cerebral palsy

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13
Q

Preferred benzodiazepine: panic disorders and phobias

A

Alprazolam, Clonazepam

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14
Q

Preferred benzodiazepine: insomnia

A

Estrazolam, Flurazepam and Triazolam

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15
Q

Preferred benzodiazepine: anesthesia induction

A

Midazolam and Diazepam

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16
Q

Preferred benzodiazepine: bipolar disorder

A

Clonazepam

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17
Q

Preferred benzodiazepine: alcohol withdrawal

A

Chlordiazepoxide and Diazepam

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18
Q

Antidote for Benzodiazepine toxicity

A

Flumazenil - a competitive BZ receptor antagonist

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19
Q

Ultrashort acting barbiturate, for anesthesia induction and increased ICP. May cause acute intermittent porphyria

A

Thiopental-potent inducer of CYP450 enzymes

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20
Q

Short to intermediate acting barbiturate for insomnia, preoperative sedation

A

Pentobarbital

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21
Q

Long acting barbiturates, for insomnia. Gilbert disease, seizure disorder in children

A

Phenobarbital - bind to GABA A receptor sites. Increases duration of chloride channel opening

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22
Q

Imidazopyridine drug, for insomnia only. Lacks anti-convulsant, anti-anxiety and muscle relaxant

A

Zolpidem - SIMD: Zaleplon and Eszopiclone

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23
Q

Anxiolytic drug for generalized anxiety disorder by partial agonist at 5-HT receptors and possibly D2 receptors

A

Buspirone - no anticonvulsant, no muscle relaxant properties with minimal CNS depressant effects

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24
Q

Effects of Zolpide. Can be reversed with?

A

Flumazenil

25
Q

Cytosolic, NAD+ dependent enzyme, mainly in liver and gut, for metabolism of low to moderate doses of ethanol

A

Alcohol dehydrogenase

Fixed metabolism of ethanol:7-10g/h

26
Q

Responsible for ethanol metabolism at blood levels higher than 100mg/dL

A

Microsomal Ethanol Oxidizing System (MEOS)

27
Q

Blood alcohol concentration that causes impairment of driving ability

A

60-80mg/dL

28
Q

Blood alcohol concentration that causes coma

A

300 to 400mg/dL

29
Q

Blood alcohol concentration that causes respiratory depression and death

A

> 500mg/dL

30
Q

Most common neurologic abnormality in chronic alcoholics

A

Peripheral neuropathy

31
Q

Syndrome associated with alcohol use presenting with ataxia, confusion, paralysis of the extra-ocular muscles

A

Wernicke-Korsakoff syndrome

32
Q

Changes in the brain seen in Wernicke-Korsakoff syndrome.

A

Hemorrhagic necrosis of the mamillary bodies

33
Q

Most common mental retardation syndrome, presents with microcephaly, underdevelopment of midface region associated with heavy consumption of alcohol during the first trimester of pregnancy

A

Fetal alcohol syndrome

34
Q

Drug of choice for alcohol withdrawal syndrome

A

Long acting benzodiazepines

35
Q

Inhibits aldehyde dehydrogenase leading to acetaldehyde accumulation then nausea, headache, flushing and hypotension

A

Disulfiram

36
Q

What Drugs can causes Disulfiram reaction?

A 
Chlorpropamide
Cefoperazone
Cefomandole
Cefotetan
Procarbazine
Metronidazole
37
Q

Treatment for methanol poisoning

A

Ethanol - retards formation of formaldehyde

Fomepizole - inhibitor of alcohol dehydrogenase

38
Q

Refers to finite episode of brain dysfunction resulting from abnormal discharge of cerebral neurons

A

Seizures

39
Q

Type of seizure wherein the consciousness is preserved

A

Simple partial seizures

40
Q

Type of seizure: impaired consciousness

A

Complex partial seizure

41
Q

Type of seizure: involves abrupt loss of consciousness, muscle rigidity and respiratory arrest for less than 1min then followed with jerking of the body muscles, lip and tongue biting, and fecal and urinary incontinence for 2-3mins

A

Generalized tonic-clonic seizure (Grand Mal)

42
Q

Type of seizure: with impaired consciousness (often abrupt onset and brief) begin in childhood and usually cease by age of 20years

A

Absence seizure (Petit Mal)

43
Q

Type of seizure: sudden, brief, shocklike contractions of musculature (myoclonic jerks)

A

Myoclonic seizures

44
Q

Series of seizures (usually tonic-clonic) without recovery of consciousness between attacks. Life-threatening emergency

A

Status epilepticus

45
Q

Anticonvulsant drug for generalized tonic-clonic seizure, partial seizures. Status epilepticus. May cause ataxic diplopia, gingival hyperplasia. Follows zero order kinetic, potent inducer of CYP450

A

Phenytoin - blocks voltage-gated Na channels

46
Q

Drug of choice for Trigeminal neuralgia

A

Carbamazepine

48
Q

Anticonvulsant drug for generalized tonic-clonic seizures, partial seizures, bipolar disorder and trigeminal neuralgia

A

Carbamazepine - blocks voltage gated Na channels and decreases glutamate release

49
Q

Anticonvulsant drug for myoclonic seizure, generalized tonic-clonic seizures and acute mania. May cause Spina bifida. Inhibitor of CYP450

A

Valproic acid - blocks high-frequency firing of neurons modifies amino acid metabolism

50
Q

Anticonvulsant drug for absence seizures. May cause GI distress, lethargy, headache and behavioral changes

A

Ethosuximide - decreases Ca2+ currents in thalamus

51
Q

Anticonvulsant drug for partial seizure, neuropathic pain and migraine. May cause dizziness, sedation, nystagmus, tremor and ataxia

A

Gabapentin - SIMD: Pregabalin, blocks Ca2+ channels, increases GABA release. Inhibits neuronal discharge from seizure foci

52
Q

Anticonvulsant drug for generalized tonic-clonic seizure, partial seizures and juvenile myoclonic epilepsy

A

Levetiracetam - selectively binds synaptic vesicular protein SV2A. Modify synaptic release of glutamate and GABA

53
Q

Anticonvulsant drug for generalized tonic-clonic seizures, absence seizures, partial seizures, Lennox-Gastaut syndrome, West syndrome and migraine. Noted to be the anti-seizure drug with most number of mechanisms of action

A

Topiramate - multiple actions on synaptic function via actions on phosphorylation

54
Q

Drugs of choice: generalized tonic-clonic seizures

A

Valproic acid
Phenytoin
Carbamazepine

55
Q

Drugs of choice: partial seizure

A

Carbamazepine
Lamotrigine
Phenytoin

56
Q

Drugs of choice: absence mal

A

Ethosuximide

Valproic acid

57
Q

Drugs of choice: myoclonic and atypical absence syndromes

A

Valproic acid

58
Q

Drugs of choice: status epilepticus

A

Lorazepam
Diazepam
Phenytoin
Phenobarbital

59
Q

First line for patients with mania, bipolar affective disorder

A

Valproic acid

60
Q

Drug of choice for Trigeminal neuralgia

A

Carbamazepine

Pharmacology (11 decks)

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