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Pharmacology E5 > Anticonvulsants and Stimulants > Flashcards

Anticonvulsants and Stimulants Flashcards

1
Q

What is the MOA of carbamazepine (Tegretol)?

A

blocks Na channels = blocks propagation of impluses

decreases pre-synaptic transmission

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2
Q

What drug has the following known side effects: aplastic anemia, agranulocytosis, thrombocytopenia, rashes, altered skin pigment, alopecia, hepatoxicity, congestive heart failure, changes in BP?

A

carbamazepine (Tegretol)

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3
Q

Cabamezepine (Tegretol) is a classic inducer of what type(s) of drugs?

A

Dec. warfarin, doxycycline, theophylline and oral contraceptive effectiveness

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4
Q

cabamezepine (Tegretol) increases the hepatotoxicity associated with what medication?

A

acetaminophen

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5
Q

Toxic blood levels of cabamezepine (Tegretol) can occur with simultaneous use of what other drug?

A

erythromycin-type antibiotics (macrolides)

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6
Q

What is the MOA of phenytoin (Dilantin)?

A
  1. Stabilizes neuronal membranes by decreasing the neuronal membrane passage of Na/Ca ions
  2. Interferes with Ca mediated release of NT
  3. Reduces propagation of abnormal impulses in the brain to reduce the frequency of seizures
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7
Q

What medication is associated with the following adverse effects:

  1. megaloblastic anemia
  2. osteoporosis
  3. gingival hyperplasia
  4. hirsutism
A

phenytoin (Dilantin)

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8
Q

How does phenytoin (Dilantin) cause megaloblastic anemia?

A

by interfering with Vit B12 metabolism

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9
Q

How does phenytoin (Dilantin) cause osteoporosis?

A

By creating Vit D and folate deficiencies

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10
Q

What is the first symptom of folate deficiency seen as a result of Dilantin use?

A

oral mucosal ulceration or glossitis

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11
Q

T/F gingival hyperplasia associated with Dilantin use will regress with improved OH and drug termination

A

True

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12
Q

What is a recommended tx procedure to prevent gingival hyperplasia in patients taking Dilantin?

A

carbamazepine is sometimes used before phenytoin to avoid gingival hyperplasia

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13
Q

What are the teratogenic effects of Dilantin and what FDA category is is classified as?

A

Fetal syndrome: includes cleft lip, cleft palate, congenital heart disease

FDA category D

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14
Q

What is the MOA of GABAmimetic agents?

A

release of GABA from presynaptic interneurons = increase GABA fusion w/ presynaptic neurons

inhibit release of ACH from presynaptic neurons

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15
Q

What is the MOA of phenobarbital (Luminal)?

A

reduces Na/K transport along axonal membranes

potentiates inhibitory effects of GABA mediated neurons

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16
Q

What drug can produce hyperactivity in children and increases bleeding time?

A

valproic acid (Depakene)

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17
Q

What is the drug of choice for tx of absence seizures (petit mal)?

A

ethosuximide (Zarontin)

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18
Q

What drug is not effective in treating absence seizures (petit mal)?

A

phenytoin (Dilantin)

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19
Q

What two benzo can be used for tx to seizures?

A

clonazepam (Clonipin): all types of seizures

diazepam (Valium): status epilepticus and local anesthetic induced

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20
Q

When would a person use gabapentin (Neurontin)?

A

partial seizures and tonic-clonic
chronic pain
post-herpetic neuralgia (shingles)

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21
Q

What is a major side effect of gabapentin (Neurontin)?

A

oral mucositis

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22
Q

T/F gabapentin (Neurontin) has many drug interactions

A

False - it has very few since it is not metabolized

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23
Q

What is the MOA of lamotrigine (Lamictal)?

A

inhibit release of glutamate (excitatory amino acid)
inhibits voltage sensitive Na channels
stabilize neuronal membranes
weakly inhibits serotonin receptors

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24
Q

Which anticonvulsants act as hepatic cytochrome P450 inducers?

A

phenytoin (Dilantin)
phenobarbital (Luminal sodium)
carbamazepine (Tegretol)

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25
Q

How does metabolism of anticonvulsants differ based on doses?

A

Low dose = first order

High doses/liver enzyme saturation = zero order

26
Q

T/F anticonvulsants cure epilepsy

A

False - drugs are used for symptomatic tx

27
Q

T/F when adding additional anticonvulsants you must change the metabolism of all anticonvulsants

A

True

28
Q

What drug is able to tx the following conditions:

  1. simple and complex partial seizures
  2. management of bipolar depression
  3. management of chronic pain
  4. Dental: trigeminal neuralgia (tic douloureux)
A

carbamazepine (Tegretol)

29
Q

what are indications for phenytoin (Dilantin) use?

A
  1. simple and complex partial seizures
  2. tonic-clonic seizures
  3. status epilepticus
  4. dental: trigeminal neuralgia
30
Q

What drug has the following indications for use:

  1. anticonvulsant
  2. tonic-clonic seizures
  3. partial seizures
A

phenobarbital (Luminal sodium)

31
Q

What drug is the most common barbiturate used as an anticonvulsant?

A

phenobarbital (Luminal sodium)

32
Q

What are the indications of use for primidone (Mysoline)?

A

partial seizures

tonic-clonic seizures

33
Q

What are the indications of use for Valproates (Depakote)?

A

tonic-clonic seizures (grand mal)

generalized seizures: absence (petit mal), myoclonic

34
Q

What is the first drug of choice for absence (petit mal) seizures? (think children)

A

ethosuximide (Zarontin)

35
Q

What type(s) of seizures can the benzo clonazepam (Clonipin) be used to tx?

A

All types!

36
Q

What are the indications for gabapentin (Neurontin)?

A

partial seizures
tonic-clonic
chronic pain
post-herpetic neuralgia (shingles)

37
Q

What are the indications for lamotrigine (Lamictal)?

A

partial seizures
tonic-clonic
part of tx for bipolar disorder

38
Q

What convulsant is used for provocative dx of epilepsy?

A

pentylenetetrazole (Metrazole)

39
Q

Valium is indicated in what 2 situations?

A
  1. local anesthetic induced seizures in dental office

2. status epilepticus

40
Q

When would a stimulant be used in medicine?

A

antidote for depression: analeptics

reverse respiratory, cardiac and CNS depression

41
Q

What are the 3 primary classes of stimulants?

A

Xanthenes
Centrally acting sympathomimetics
Convulsants

42
Q

What is the main effect of Xanthenes and its tx use?

A

bronchodilators

asthma tx

43
Q

What is the main effect of centrally acting sympathomimetics and its tx indications?

A

amphetamine

tx: hyperkinetic children, diet pills

44
Q

What is the main purpose of convulsant medications?

A

diagnostic

45
Q

What are the common xanthene medications?

A

aminophylline
theophylline
caffeine

46
Q

At what dosages of caffeine are the following structures effected:

  1. cerebral cortex
  2. brain stem
  3. spinal cord
A
  1. 50-200 mg
  2. > 250 mg
  3. 100 mg
47
Q

T/F caffeine and theophylline are equally effective on the CNS?

A

True

48
Q

Theophylline produces (more/less) effects on blood vessels, heart, smooth muscle, diuresis than caffeine does

A

Theophylline produces more than caffeine

Theophylline > Caffeine

49
Q

Theophylline produces (more/less) effects on skeletal muscle than caffeine does

A

Theophylline produces less than caffeine

Theophylline

50
Q

What what dosage does caffeine toxicity occur?

A

300 mg

51
Q

What type of caffeine in take results in physical dependence?

A

5+ cups/day

52
Q

What type of medication can be used to tx acute pulmonary edema and apnea in perterm infants?

A

Xanthenes: increases perfusion, decreases peripheral resistance causing bronchiodilation

53
Q

CNS sympathomimetics increase or decrease the following:

  1. fatigue
  2. mood, motor activity, performance, wakefulness
  3. REM sleep
  4. appetite
  5. satiety center
  6. medullary respiratory center
A
  1. decrease
  2. increase
  3. decrease
  4. decrease
  5. increase
  6. increase
54
Q

What drug type(s) have the following indications of use:

  1. narcolepsy
  2. hyperkinetic syndrome
A

CNS sympathomimetics

55
Q

What is the popular drugs used for the management of children with hyperkinetic disorders?

A

Centrally acting sympathomimetics (amphetamine)

56
Q

Why vasoconstrictors (epinephrine) must be used with caution in dental patients taking CNS sympathomimetics?

A

CNS sympathomimetics block reuptake of dopa and NE

inhibit MAO

Enhances sympathomimetic response of Epi/NE

57
Q

What is the MOA of cocaine?

A

blocks Na/K ATPase reuptake mechanism
dopa and NE remain in synapse
crosses blood brain barrier

58
Q

What 4 things do cocaine clinically increase?

A
  1. sympathetic system responses
  2. peripheral resistance
  3. cardiac output
  4. energy expenditure
59
Q

What is the MOA of pentylenetetrazol (Metrazole)?

A

decreases neuronal recovery time by increasing K+ permeability
used for provocative dx of epilepsy

60
Q

What is the MOA of strychnine?

A

blocks glycine receptors on Renshaw cells (postsynaptic inhibition)

produces generalized convulsion → non-spontaneous, simultaneous tonic convulsion of flexors and extensors

61
Q

What drug causes OD when added to heroin?

A

strychnine (rat poison)

62
Q

What are the effects of nicotine based on dosage level?

A

Low doses: stimulates nicotinic receptors in brainstem and cortex

High doses: tremor, emesis and stimulation of respiratory center

Higher doses: convulsions (can be fatal)

Pharmacology E5 (3 decks)

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