PharmII_Exam2(p1-3) Flashcards

1
Q

Describe focal seizures

A

Neuronal excitation originates at specific cortical sites and potentially spreads to wider areas of the brain.

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2
Q

T/F?

Most seizures are of the focal nature?

A

True

60%

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3
Q

Describe generalized seizures

A

Begin on both sides of the brain at about the same time and can manifest as either full
“grand mal” convulsions or brief staring episodes.

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4
Q

Describe absense seizure (petit mal)

A

Loss of consciousness, stare, eye flicking, usually no motion (<30sec)

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5
Q

Describe myoclonic generalized seizure

A

Brief 1 sec shock like contractions of muscles.

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6
Q

Describe tonic-clonic generalized seizure

A

loss of consciousness, Sustained contractions (tonic) followed by relaxations
(clonic) of muscles throughout the body (1—2min).

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7
Q

Name of disorder associated with Generalized seizures?

A

juvenile myoclonic epilepsy.

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8
Q

MOA of generalized seizures?

A

(reciprocal firing through the thalamus via T-type Ca2+ channels)

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9
Q

Name the three MOA that anti-epileptic drugs work?

A
  1. Prolonging the inactivation of voltage gated Na+ channels
  2. Enhancement of synaptic inhibition by increasing GABA activity
  3. Treating a less common form of epilepsy, generalized absence seizures and myoclonic seizures, is
    accomplished through the inhibition of T-type voltage gated Ca2+ channels.
    Regardless
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10
Q

What condition will occur if you withdraw an anti-epileptic?

A

sudden withdrawal of the drug can cause status epilepticus.

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11
Q

T/F?

COnsciousness is not preserved in simple focal seizure?

A

False. It is preserved.

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12
Q

Name the two MOAs of drugs that treat focal seizures and tonic-clonic seizure?

A
  1. Prolonging Na+ channel inactivation

2. Enhancing GABA activity

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13
Q

Name the MOAs of drugs that treat generalized absence and myoclonic seizures?

A

Target T-Type Calcium channels.

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14
Q

Is there birth defect risk with the use of anti-epileptic drugs?

A
Yes. 
Trimethadione
Paramethadione
Phenytoin
Phenobarbital
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15
Q

Carbamazepine and Phenytoin are 1st line agents for which type of seizures

A

partial seizures and generalized tonicclonic.

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16
Q

Ethosuximide and Valproate are preferred for

A

generalized absence seizures since they are non-sedating.

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17
Q

Clonazepam is highly effective for which seizure?

A

Generalized absence seizure.
Effective for myoclonic as well
Really bad because it causes sedation

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18
Q

Fosphenytoin?

A

More soluble pro-drug (converted to phenytoin in the body)

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19
Q

For phenytoin to work, what is it dependent upon?

A

Voltage dependent

Use dependent.

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20
Q

What does use dependent mean?

A

It only works on an active channel.

Regarding sodium ion channels.

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21
Q

At very low blood levels, which order kinetics does phenytoin follow?

A

First order.

Same percentage of drug is eliminated/ime

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22
Q

When phenytoin is saturated, what order kinetics is followed?

A

Zero order.

Same amt of drug is eliminated per unit time.

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23
Q

What will phenytoin do to warfarrin?

A

It will displace warfarin from albumin binding sites.

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24
Q

How are u supposed to administer an anti-epileptic to a patient?

A

Increase dose slowly to avoid toxicity.

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25
Q

Mephenytoin?

A

a phenytoin cogener with saturable metabolism Nirvanol is the active metabolite

26
Q

Carbamazepine

A

Structurally related to tri-cyclic antidepressants. In addition to its anticonvulsant actions, it can treat bipolar depression.
It locks sodium channels in inactivated state

27
Q

Which drug to you used if patient is hypersensitive to phenytoin?

A

Ethotoin

28
Q

Is it ok to give MAOI in a patient taking carbamezipine?

A

NO!!!
It is structurally similar to imipramine.
If do, will get hpertensive crisis.

29
Q

Oxcarbazepine

A

Similar to carbamazepine but better toxicity profile (less potent, less interactions.

30
Q

Phenobarbital

A

Still among the most commonly used. increases GABA while decreasing Glutamate. Used for partial and
generalized tonic clonic and generalized myoclonic refractory to other agents.

31
Q

Mephobarbital

A

Also a barbiturate used in epilepsy

32
Q

Primidone

A

Metabolized to Phenobarbitol and PEMA. Action is more similsr to phenytoin.

33
Q

Vigabatrin

A

an analog of GABA which reversibly inhibits GABA aminotransferase and promotes the
accumulation of GABA at the synapse thus increasing GABA activity and inhibits high frequency neuronal
firing.

34
Q

What is the worse side effect of vigabatrin?

A

Irreversible visual impairment with long term therapy. 50% o patients experience AE
Causes psychosis

35
Q

Which seizures is vigabatrin used in?

A

Used for partial and tonic-clonic.
Used as adjunctive therapy for refractive cases of these.
and West’s Syndrome.

36
Q

Name two MOA of Lamotrigine

A
  1. Inactivates voltage gated sodium channels.

2. Block voltage gated calcium channels.

37
Q

Which seizures and other condition can Lamotrigine treat?

A
  1. partial seizure and tonic clonic
  2. Absence and myoclonic
  3. Lennox-Gasaut syndrome
    Bipolar disorder.
38
Q

What is a major adverse effect in Lamotrigine?

A

Severe life threatening rashes

39
Q

Felbamate

A

Thought to block NMDA. 3rd line drug for partial seizures or Lennox-Gastaut syndrome. Can
cause aplastic anemia and hepatic failure.

40
Q

Gabapentin

A

GABA + a lipophilic hexane ring but does NOT activate GABA receptors. Binds Ca2+
channels to inhibit glutamate and may alter GABA metabolism and transport. Partial and generalized tonic-clonic and
for neuropathic pain in post herpetic neuralgia (shingles). NOT metabolized (eliminated by kidney unchanged).

41
Q

Pregabalin

A

Also a GABA analog with similar mechanism. Partial seizures, surgical dental pain, diabetic
neuropathies, postherpetic neuralgia, and off label for anxiety.

42
Q

Topiramate

A

Prevents seizure spread, used for partial and generalized tonic-clonic seizures, absence, and
myoclonic. Also TX for Lennox- Gastaut syndrome and West’s syndrome. May reduce efficacy of oral contraceptives
and cause Glaucoma and acute myopia (stop drug).

43
Q

Tiagabine

A

–“Rationally” designed drug that blocks the GABA transporter GAT-1 to

44
Q

Zonisamide

A

Sulfonamide derivative that blocks T-type Ca3+ channels and prolongs Na+ channel
inactivation. Partial, general tonic-clonic, and absence. May cause ataxia, psychosis and speech disturbances.

45
Q

Keppra

A

– Binds synaptic vesicle SV2 protein altering release an glutaminergic and GABAergig
synapses. Partial and secondary tonic-clonic. Little metabolism. Can cause somnolence, asthenia, and dizziness.

46
Q

Ethosuximide
Methusuximide
Phensuximide

A
Particularly effective for absence petit mal) seizures. Efficacious and safe. Can cause
gastric effects (more common) and CNS effects (less common).
47
Q

Valproate

A

Prolongation of Na channel inactivation, reduction of T-type
Ca+ currents, reduces NMDA currents and increased [GABA] in brain. The preferred choice for absence seizures
concomitant with tonic-clonic seizures (Ethosuximide is preferred for absence alone). Also used for bipolar
disorder, migraine headaches, alcohol withdrawal and dementia. It is contraindicated in liver disease and urea cycle disorders.

48
Q

Benzodiazepines

A

effective at non-sedating doses and likely potentiate GABA activity on GABA-A receptor. Used IV
for status epilepticus to quickly reduce seizures. May, however, have a pronounced sedative effect and tolerance may develop within a few months.

49
Q

Acetazolamide

A

a diuretic that inhibits carbonic anhydrase and likely produces a slight acidosis of the brain
or reduces the depolarizing activity of bicarbonate ions. Only use may be for women who have increased seizures
during menstruation.

50
Q

What happens if you overdose on anti-epileptics?

A

U won’t die!!!

51
Q

MOA of benzo?

A

These drugs potentiate GABA at the GABA-A Receptor (except Buspirone and Ramelton)
Increase Frequency of channel opening,
increasing infinity of GABA for receptor

52
Q

What does barb do to gaba receptor

A

Increase mean open time, Increasing the infinity of GABA for receptor,
act directly as agonist

53
Q

Which group of drugs is used for acute anxiety attacks?

A

Benzodiazepines

54
Q

Which group of drugs is used for long term anxiety care?

A

SSRIs
SNRIs
Quetiapen, an atypical antipsychotic is used as an adjunct.

55
Q

T/F?

Benzodiazepines are able to produce cardiovascular/respiratory depression

A

False

One exception is Midazolam.It is able to produce general anesthesia.

56
Q

Can you use benzodiazepines with other CNS depressants like alcohol?

A

NOPE

57
Q

Which receptor does Buspirone act on?

A

5-HT1a

58
Q

Which receptor does Ramelteon act on?

A

Melatonin receptor.

59
Q

Does barb or bdz produce a dose dependent CNS depression?

A

Barbs

60
Q

Name the three non-benzodiazepines?

A

Ambien
Sonata
Lunesta

61
Q

What is the name of the only drug that reverse BDZ overdose

A

Flumenazil.
Used to tx BDZ OD and reverse effects of BDZ and non BDZ used as anesthesia
adjucts. Does not block barbiturate, ethanol, or general anesthetic action. Can precipitate the
rapid development of withdrawal symptoms.

62
Q

Can flumazenil reverse the efffects of barbs?

A

Nope