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PHARMACOLOGY > ANTICONVULSANT 2 > Flashcards

ANTICONVULSANT 2 Flashcards

1
Q

Benzodiazepines are usually used as

A

sedative hypnotics

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2
Q

Give examples of benzodiazepines

A

Lorazepam
Clonazepam
Diazepam
Clorazapate dipotassium
Clobazam
Nitrazepam
Modazolam

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3
Q

Give the metabolism of benzodiazepines

A

Metabolised by CYP3A4 to active metabolites

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4
Q

Give an important PK of the benzodiazepines

A

Half life of 40hrs
Cross the placental barrier and may depress foetal vital functions

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5
Q

Give the MOA od benzodiazepines

A

potentiating the effect of GABA

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6
Q

1) Diazepam is give through which ROA

What is the main clinucal use of diazepam

A

IV or IM , not usually for long term oral due to tolerance

GTC status epilepticus

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7
Q

Continuous seizure activity is termed as

A

status epilepticus

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8
Q

Lorazepam is more effective than diazepam in stafus epilepticus , true or false

A

True

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9
Q

Clonazepam is termed as what acting and is used in

Clonazepam causes

A

long acting
Myoclonic , Absence and Infantile spasms
marked sedation

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10
Q

Clorazepate dipotassium is used as

A

an adjunct in complex partial seizures in adults

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11
Q

The active metabolite of Clobazam is

A

Norclobazam

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12
Q

Tolerance develops for clobazam

A

true

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13
Q

Give general clinical applications of BDzs

A

Anxiolytic
Anticonvulsant
Muscle relaxant
Sleep aid
Pre-ooetative anaesthesia

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14
Q

Give two main limitations of BDzs

A

Marked sedation
Tolerance

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15
Q

Give the toxivity of BDZs

A

1)Sedation , impaired judgement
2) Teratogenic
3) Hypersensivity - rash

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16
Q

Give the DDI of BDZs

A

Additice effects woith other CNS depressants such as alcohol , opoids , TCAs , phenothiazines

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17
Q

Give the structure of Gabapentin

A

GABA molecule covalently bonded to a cyclohexane ring

18
Q

Gabapentin is able to pass through the BBBdue to

A

its high lipid solubility

19
Q

Give the structure of Pregabalin

A

GABA molecule covalently bounded to isobutane

20
Q

Pregabalin and gabapentin moa

A

Bind to a2delta subunits of voltage gated calcium channels thus inhibit calcium entry and inhibits presynaptic release of glutamate

21
Q

Gabapentin PK

A

Not bound to plasma proteins and not metabolised in humans

22
Q

Give the clinucal use of
1) Gabapentin
2Pregabalin

A

Gabapentin - adjunct in partial and GTCS , Bipolar disorder , Migraine , Chronic pain

Pregabalin - partial seizures , painful diabetic peripheral neurppathy , Fibromyalgia , Postherpetic neuralgia , Genaralized anxiety disorder

23
Q

Give the MOA of Vigabatrin

A

A structural analog of GABA that inhibits GABA transaminase used in GABA degradation

24
Q

Vigabatrin is usually reserved for patients with failed alternative therapues due to

A

Progressive and permanent bilateral vision loss

25
Q

Guve the structure lf Tiagabine

A

Its is a derivative of nipecotic acid

26
Q

Give the MOA of Tiagabin

A

Inhibits the GABA transporter GAT-1 prolonging its effects at inhibitory synapses

27
Q

Give the effects of phenytoin carbamezapine and phenobarbital to the haalf life of tiagabine

A

Usually 8hrs but reduced to 2-3 hrs when codaministered with the above drugs

28
Q

Give the effects of Tiagabin and food

A

taken with food to minimoze A/E

29
Q

Tiagabin is mainly excreted via

A

feces

30
Q

Give the moa of Retigabine

A

Opens voltage gated potassium channels thus inhibiting release of glutamate

31
Q

Give the structure of Levetiracetam

A

pyrrolidine

32
Q

Give the MOA of Levetiracetam

A

Binds selectively to SVA2 decreasing release of glutamate

33
Q

Levetiracetam is metabolised in the

A

blood

34
Q

Give the MOA of Perampanel

A

Ingibits AMPA receptors , a type of glutamate receptors

35
Q

Give the Metabolism and DDI of perampanel

A

Extensive hepatic metabolism by CYP3A4
Inducees of CYP3A4 such as Carbamezapine and phenytoin increase clearance

36
Q

Guve the clinical ise of Felbamate

A

Refractory focal seizures
Atonic seizures
Lennox-Gastaut syndrome

37
Q

Felbamate works via

A

Blockade of NMDA receptors
Potentioation of GABA

38
Q

Give the MOA of acetazolamide as an anticonvulsant

A

Its is a carbonic anhydrase inhibitor thus reduces bicarbonate ions which are important in depolarization

39
Q

Give a limitation of acetazolamide

A

Tolerance

40
Q

Give two drugs with the lpwest risk of congenital abnormalities in pregnancy

A

Lamotrigine
Levetiracetam

PHARMACOLOGY (17 decks)

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