ANTICONVULSANT 2

Question 1

Benzodiazepines are usually used as

Answer 1

sedative hypnotics

Question 2

Give examples of benzodiazepines

Answer 2

Lorazepam
Clonazepam
Diazepam
Clorazapate dipotassium
Clobazam
Nitrazepam
Modazolam

Question 3

Give the metabolism of benzodiazepines

Answer 3

Metabolised by CYP3A4 to active metabolites

Question 4

Give an important PK of the benzodiazepines

Answer 4

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

Question 5

Give the MOA od benzodiazepines

Answer 5

potentiating the effect of GABA

Question 6

1) Diazepam is give through which ROA

What is the main clinucal use of diazepam

Answer 6

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

GTC status epilepticus

Question 7

Continuous seizure activity is termed as

Answer 7

status epilepticus

Question 8

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

Answer 8

True

Question 9

Clonazepam is termed as what acting and is used in

Clonazepam causes

Answer 9

long acting
Myoclonic , Absence and Infantile spasms
marked sedation

Question 10

Clorazepate dipotassium is used as

Answer 10

an adjunct in complex partial seizures in adults

Question 11

The active metabolite of Clobazam is

Answer 11

Norclobazam

Question 12

Tolerance develops for clobazam

Answer 12

true

Question 13

Give general clinical applications of BDzs

Answer 13

Anxiolytic
Anticonvulsant
Muscle relaxant
Sleep aid
Pre-ooetative anaesthesia

Question 14

Give two main limitations of BDzs

Answer 14

Marked sedation
Tolerance

Question 15

Give the toxivity of BDZs

Answer 15

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

Question 16

Give the DDI of BDZs

Answer 16

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

Question 17

Give the structure of Gabapentin

Answer 17

GABA molecule covalently bonded to a cyclohexane ring

Question 18

Gabapentin is able to pass through the BBBdue to

Answer 18

its high lipid solubility

Question 19

Give the structure of Pregabalin

Answer 19

GABA molecule covalently bounded to isobutane

Question 20

Pregabalin and gabapentin moa

Answer 20

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

Question 21

Gabapentin PK

Answer 21

Not bound to plasma proteins and not metabolised in humans

Question 22

Give the clinucal use of
1) Gabapentin
2Pregabalin

Answer 22

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

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

Question 23

Give the MOA of Vigabatrin

Answer 23

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

Question 24

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

Answer 24

Progressive and permanent bilateral vision loss

Question 25

Guve the structure lf Tiagabine

Answer 25

Its is a derivative of nipecotic acid

Question 26

Give the MOA of Tiagabin

Answer 26

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

Question 27

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

Answer 27

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

Question 28

Give the effects of Tiagabin and food

Answer 28

taken with food to minimoze A/E

Question 29

Tiagabin is mainly excreted via

Answer 29

feces

Question 30

Give the moa of Retigabine

Answer 30

Opens voltage gated potassium channels thus inhibiting release of glutamate

Question 31

Give the structure of Levetiracetam

Answer 31

pyrrolidine

Question 32

Give the MOA of Levetiracetam

Answer 32

Binds selectively to SVA2 decreasing release of glutamate

Question 33

Levetiracetam is metabolised in the

Answer 33

blood

Question 34

Give the MOA of Perampanel

Answer 34

Ingibits AMPA receptors , a type of glutamate receptors

Question 35

Give the Metabolism and DDI of perampanel

Answer 35

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

Question 36

Guve the clinical ise of Felbamate

Answer 36

Refractory focal seizures Atonic seizures Lennox-Gastaut syndrome

Question 37

Felbamate works via

Answer 37

Blockade of NMDA receptors Potentioation of GABA

Question 38

Give the MOA of acetazolamide as an anticonvulsant

Answer 38

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

Question 39

Give a limitation of acetazolamide

Answer 39

Tolerance

Question 40

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

Answer 40

Lamotrigine Levetiracetam