GABA System, Sedative-Hypnotic & Anxiolytic Drugs - 28 Flashcards

1
Q

How many types of GABAa subunits have been identified?

A

18

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2
Q

How can you gain region or effect specificity when targeting the GABAa receptor?

A

By targeting specific GABAa receptor sub-types (subunit combos)

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3
Q

What are GABAa receptor subtype selective drugs called?

A

Z-Drugs

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4
Q

Z-Drugs are structurally similar to the barbiturates and benzodiazepines. They bind to the same site as benzos. (Statement 1/Statement 2)

A

S1 - F : S2 - T

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5
Q

What are the Z-drugs known as?

A

Sedative Hypnotics

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6
Q

How do Z-drugs relate to BDZs?

A

Less day-after psychomotor depression : less amnesia effects : more selective for GABAa Alpha-1-subunit

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7
Q

What general effects do Z-drugs have?

A

Shorten sleep latency, prolongs sleep time : (Less likely to change sleep patterns)

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8
Q

What is an example of a Z-Drug? Its half-life? Something interesting about it?

A

Zolpidem (Ambien) : 2.5hrs : Women metabolize it more slowly

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9
Q

How are Z-Drugs metabolized?

A

By P450s

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10
Q

What effect would barbituates in your system have on your metabolization of Zolpidem?

A

It would make the Zolpidem less effective (metabolize faster)

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11
Q

Safety and Adverse effects of Z-drugs:

A

Wakeful behavior/amnesia : Low tolerance when used as directed : Few withdrawal reactions (some with long term use) : NO TOLERANCE TO THERAPEUTIC EFFECTS

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12
Q

What are “centrally acting muscle relaxants”?

A

Drugs that diminish output of nerve impulses to voluntary muscles

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13
Q

What are examples of centrally acting muscle relaxants?

A

Diazepam, Mephenesin, Baclofen (GABAb agonist)

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14
Q

What is Baclofen used for?

A

Trigeminal Neuralgia, MS and spinal cord injury

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15
Q

Why do epilepsy and seizures happen?

A

Excessive excitability of neurons in the CNS

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16
Q

The term “seizure” refers to:

A

A general term referring to all types of epileptic events

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17
Q

The term “convulsion” refers to:

A

Abnormal motor phenomenon

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18
Q

All __________ can be called ____________, but not all _____________ can be called ________________.

A

Convulsions : seizures : seizures : convulsions

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19
Q

If a seizure stays in one part of the brain, it is called a _______________

A

Partial seizure

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20
Q

If a seizure spreads to a larger area of the brain, it is called a ________________.

A

Generalized seizure

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21
Q

What is the difference between seizures and epilepsy?

A

Seizures can be symptoms of an underlying condition due to genetics, trauma, infection, tumor, autoimmune disorders, or pharmacology. :
Epilepsy is a disease defined by recurrent seizures and accompanying increases in electrical neural activity.

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22
Q

How many people are effected by epilepsy?

A

50 million people worldwide (30% without good control)

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23
Q

Partial seizures can be ______________ or _________________.

A

Simple or complex

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24
Q

Simple partial seizures:

A

Effect 1 part of the brain : have a specific disturbance (motor, sensory, speech) : consciousness unimpaired

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25
Q

Complex partial seizures:

A

Effect more than one area of the brain : can induce dreamy/blank/vacant state with automated movements : impairment of consciousness

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26
Q

Generalized seizures can be _______________ or __________________.

A

Convulsive or nonconvulsive

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27
Q

What are the 2 phases of a convulsive seizure?

A

Tonic (flexed) and Clonic (relaxed)

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28
Q

What may happen during a convulsive seizure?

A

Contraction of respiratory muscles (little/no breathing)

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29
Q

What is an example of a non-convulsive seizure?

A

Petit Mal : sudden/brief cessation in activity

30
Q

Basic First aid for Seizures:

A

Cushion head, turn on side, look for ID, loosen neckwear, offer help when it ends

31
Q

Diagnosis and AED selection:

A

Specific antiepileptic drugs for specific seizure disorders : make physiological/neurological assessments over time : EEG Essential

32
Q

What are the primary mechanisms of action for anticonvulsive drugs?

A

Promote GABA activity : Keep Na channels inactivated : Keep Ca channels inactivated

33
Q

What were the negative effects that made Phenobarbital not great as the first anticonvulsant?

A

Induces its own metabolism : tolerance develops to anti-convulsive effects : highly sedating

34
Q

When is phenobarbital used today?

A

Rarely, for partial and general seizures : mostly in children

35
Q

What drugs are used to stop status epilepticus?

A

Diazepam and lorazepam

36
Q

Why are benzos not used as mainstay anticonvulsive therapy?

A

They cause cerebellar toxicity

37
Q

Examples of anticonvulsive drugs that target Na channels:

A

Phenytoin & Carbamazepine

38
Q

Examples of anticonvulsive drugs that target Ca channels:

A

Ethosuximide

39
Q

Examples of anticonvulsive drugs that target both Na and Ca channels:

A

Valproic Acid

40
Q

Action potentials rely on activation of ____________________

A

Voltage gated Na, K, and Ca channels

41
Q

T/F voltage gated channels go from closed to open depending on the membrane potential.

A

F - the go from Closed - Open - Inactive - Closed - Open ………

42
Q

How does Phenytoin work? How is it used? Positive/negative characteristic?

A

Binds “inactive” Na channels and slows recovery : used as mainstay treatment for partial/generalized seizures : Relatively non-sedating/narrow therapeutic window - metabolism saturates (cant break down as expected)

43
Q

Side effects of Phenytoin:

A

Cerebellar toxicity : Gingival hyperplasia : many drug-drug interaction

44
Q

How do Carbamazepines work? How are they used? Negatives to it?

A

Delays Na channel recovery : used for partial complex seizures : cerebellar toxicity - induces P450 - metabolized by P450s

45
Q

How do ethosuximides work? What are they used for? Pros/Cons?

A

Inactivated Ca channels : absence seizures : NO CEREBELLAR TOXICITY - GI distress, headache, dizziness

46
Q

How does Valproic acid work? When is it used?

A

Inactivated Na AND Ca channels and inhibits GABA metabolism : for partial, general, and absence seizures

47
Q

Side effects of Valproic Acid

A

Thrombocytopenia, inhibition of P450

48
Q

What is thrombocytopenia?

A

Deficiency of platelets in the blood (slow blood clotting and bleeding into tissues/bruising)

49
Q

Why is it bad to inhibit P450s?

A

Causes hyperammonemic metabolic disturbance (build up of ammonia) causing hepatotoxicity (liver toxicity)

50
Q

What are the newest anticonvulsant drugs?

A

Lamotrigine and Gabapentin

51
Q

How does Gabapentin work? What is it used for?

A

Increases GABA : partial seizures : dizziness/drowsiness

52
Q

How does Lamotrigine work?

A

Prolongs sodium channel inactivation and blocks glutamate release :

53
Q

What are some “other uses” for antiepileptic drugs?

A

Used to treat Mania and Neuropathic pain (trigeminal neuralgia)

54
Q

What are the common toxicities of antiepileptic drugs?

A

Cerebellar toxicity: ataxia/nystagmus, sedation, drug interactions (induce/inhibit P450s)

55
Q

What are some negative effects that antiepileptic drugs may have on a fetus? Why would someone still take them?

A

Valproic acid has high risk of spina bifida/neural tube defects, oral facial clefts : risk from uncontrolled seizures is greater than risk from AED

56
Q

What things can you do for a woman taking AEDs while pregnant?

A

Use lowest effective dose : use only 1 AED : Supplement folic acid : Supplement Vit K

57
Q

T/F AED are CNS depressants

A

TRUE

58
Q

What are some examples of drugs that will effect metabolism of other drugs through P450 interactions?

A

Phenytoin, carbamazepine, valproic acid, oral contraceptives

59
Q

What are some dental related side effects of AEDs?:

A

Increased incidence of infection : xerostomia : gingival hypertophy :delayed healing : bleeding gums : postop bleeding

60
Q

When does autism become apparent?

A

In the first 3 years

61
Q

Autism affects the development of _________________________.

A

Social and communication skills

62
Q

How prevalent is autism today?

A

1 in 68 - 4:1 male:female

63
Q

What are some examples of comorbid conditions to autism?

A

Anxiety disorder, ADHD, sensory integration dysfunction, immune disorders, neuroinflammation

64
Q

T/F Children with autism will stop progressing indefinitely

A

F - early intervention is key

65
Q

Does autism influence life expectancy?

A

NO - but there is a higher incidence of accidental death

66
Q

What is Asperger syndrome? Characteristics?

A

High functioning autism : normal language development, socially inappropriate, hyper/hyposensitive to sensory input

67
Q

Symptoms of Autism:

A

Lack of pretend play : impaired social interactions : impaired verbal/nonverbal communication : sensitive to change : trouble remaining still : tantrums

68
Q

What are some common medications prescribed for autism?

A

Risperidone, methylphenidate, SSRIs

69
Q

What are some examples of damaging oral habits displayed by some with autism?

A

Bruxism, Self-injurious behavior (picking at gingiva), eating/chewing gravel, pens…

70
Q

What are good approaches when treating autistic patients?

A

Work with the family, adjust expectations, reduce distractions, be sensitive to sound, maintain routine, praise good behavior, may need to sedate.