GABA System, Sedative-Hypnotic & Anxiolytic Drugs - 28

Question 1

How many types of GABAa subunits have been identified?

Answer 1

18

Question 2

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

Answer 2

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

Question 3

What are GABAa receptor subtype selective drugs called?

Answer 3

Z-Drugs

Question 4

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

Answer 4

S1 - F : S2 - T

Question 5

What are the Z-drugs known as?

Answer 5

Sedative Hypnotics

Question 6

How do Z-drugs relate to BDZs?

Answer 6

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

Question 7

What general effects do Z-drugs have?

Answer 7

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

Question 8

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

Answer 8

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

Question 9

How are Z-Drugs metabolized?

Answer 9

By P450s

Question 10

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

Answer 10

It would make the Zolpidem less effective (metabolize faster)

Question 11

Safety and Adverse effects of Z-drugs:

Answer 11

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

Question 12

What are “centrally acting muscle relaxants”?

Answer 12

Drugs that diminish output of nerve impulses to voluntary muscles

Question 13

What are examples of centrally acting muscle relaxants?

Answer 13

Diazepam, Mephenesin, Baclofen (GABAb agonist)

Question 14

What is Baclofen used for?

Answer 14

Trigeminal Neuralgia, MS and spinal cord injury

Question 15

Why do epilepsy and seizures happen?

Answer 15

Excessive excitability of neurons in the CNS

Question 16

The term “seizure” refers to:

Answer 16

A general term referring to all types of epileptic events

Question 17

The term “convulsion” refers to:

Answer 17

Abnormal motor phenomenon

Question 18

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

Answer 18

Convulsions : seizures : seizures : convulsions

Question 19

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

Answer 19

Partial seizure

Question 20

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

Answer 20

Generalized seizure

Question 21

What is the difference between seizures and epilepsy?

Answer 21

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.

Question 22

How many people are effected by epilepsy?

Answer 22

50 million people worldwide (30% without good control)

Question 23

Partial seizures can be ______________ or _________________.

Answer 23

Simple or complex

Question 24

Simple partial seizures:

Answer 24

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

Question 25

Complex partial seizures:

Answer 25

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

Question 26

Generalized seizures can be _______________ or __________________.

Answer 26

Convulsive or nonconvulsive

Question 27

What are the 2 phases of a convulsive seizure?

Answer 27

Tonic (flexed) and Clonic (relaxed)

Question 28

What may happen during a convulsive seizure?

Answer 28

Contraction of respiratory muscles (little/no breathing)

Question 29

What is an example of a non-convulsive seizure?

Answer 29

Petit Mal : sudden/brief cessation in activity

Question 30

Basic First aid for Seizures:

Answer 30

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

Question 31

Diagnosis and AED selection:

Answer 31

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

Question 32

What are the primary mechanisms of action for anticonvulsive drugs?

Answer 32

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

Question 33

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

Answer 33

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

Question 34

When is phenobarbital used today?

Answer 34

Rarely, for partial and general seizures : mostly in children

Question 35

What drugs are used to stop status epilepticus?

Answer 35

Diazepam and lorazepam

Question 36

Why are benzos not used as mainstay anticonvulsive therapy?

Answer 36

They cause cerebellar toxicity

Question 37

Examples of anticonvulsive drugs that target Na channels:

Answer 37

Phenytoin & Carbamazepine

Question 38

Examples of anticonvulsive drugs that target Ca channels:

Answer 38

Ethosuximide

Question 39

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

Answer 39

Valproic Acid

Question 40

Action potentials rely on activation of ____________________

Answer 40

Voltage gated Na, K, and Ca channels

Question 41

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

Answer 41

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

Question 42

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

Answer 42

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)

Question 43

Side effects of Phenytoin:

Answer 43

Cerebellar toxicity : Gingival hyperplasia : many drug-drug interaction

Question 44

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

Answer 44

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

Question 45

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

Answer 45

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

Question 46

How does Valproic acid work? When is it used?

Answer 46

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

Question 47

Side effects of Valproic Acid

Answer 47

Thrombocytopenia, inhibition of P450

Question 48

What is thrombocytopenia?

Answer 48

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

Question 49

Why is it bad to inhibit P450s?

Answer 49

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

Question 50

What are the newest anticonvulsant drugs?

Answer 50

Lamotrigine and Gabapentin

Question 51

How does Gabapentin work? What is it used for?

Answer 51

Increases GABA : partial seizures : dizziness/drowsiness

Question 52

How does Lamotrigine work?

Answer 52

Prolongs sodium channel inactivation and blocks glutamate release :

Question 53

What are some “other uses” for antiepileptic drugs?

Answer 53

Used to treat Mania and Neuropathic pain (trigeminal neuralgia)

Question 54

What are the common toxicities of antiepileptic drugs?

Answer 54

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

Question 55

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

Answer 55

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

Question 56

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

Answer 56

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

Question 57

T/F AED are CNS depressants

Answer 57

TRUE

Question 58

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

Answer 58

Phenytoin, carbamazepine, valproic acid, oral contraceptives

Question 59

What are some dental related side effects of AEDs?:

Answer 59

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

Question 60

When does autism become apparent?

Answer 60

In the first 3 years

Question 61

Autism affects the development of _________________________.

Answer 61

Social and communication skills

Question 62

How prevalent is autism today?

Answer 62

1 in 68 - 4:1 male:female

Question 63

What are some examples of comorbid conditions to autism?

Answer 63

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

Question 64

T/F Children with autism will stop progressing indefinitely

Answer 64

F - early intervention is key

Question 65

Does autism influence life expectancy?

Answer 65

NO - but there is a higher incidence of accidental death

Question 66

What is Asperger syndrome? Characteristics?

Answer 66

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

Question 67

Symptoms of Autism:

Answer 67

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

Question 68

What are some common medications prescribed for autism?

Answer 68

Risperidone, methylphenidate, SSRIs

Question 69

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

Answer 69

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

Question 70

What are good approaches when treating autistic patients?

Answer 70

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