CNS Pharmacology

Question 1

Typical antipsychotics

Answer 1

• 1st generation dopamine antagonists
• Phenothiazones, Haloperidol, thiothixene

Question 2

Phenothiazones derivatives

Answer 2

Chlorpromazine- aliphatic derivative of phenothiazone

Question 3

Atypical Antipsychotics

1ex

Answer 3

Newer 2nd gen dopamine antagonists

Clozapine

Question 4

Antipsychotic drugs mechanism of action

Answer 4

• Dopamine antagonists
• Block dopamine D2 receptors in dopaminergic pathways
• Some also block 5HT 2 receptors

Question 5

Types of antidepressant drugs for unipolar

Answer 5

Monoamine uptake inhibitors (NE and 5HT) Monoamine oxidase inhibitors (MAOIs)

Question 6

Monoamine uptake inhibitors

Answer 6

Tricyclic antidepressants (TCAs): Amitriptyline Selective serotonin reuptake inhibitors (SSRIs): Prozac (Fluoxetine) Newer Mixed 5-HT & NE reuptake inhibitors (SNRIs): Effexor (Venlafaxine) Cymbalta (Duloxetiene) Norepinephrine reuptake inhibitors: Wellbutrin (Bupropion)

Question 7

Monoamine Oxidase Inhibitors MAOI

Answer 7

Phenelzine Should NOT be used with other antidepressants or autonomic drugs that cause the release of serotonin and catecholamines

Question 8

Monoamine receptor antagonists ie Unipolar

Answer 8

alpha 2 adrenergic receptor blockers Mirtazapine

Question 9

Trazodone AoM Unipolar

Answer 9

Thought to potentiate 5HT activity. Get mixed agonist on receptor subtype Also blocks alpha1 adrenergic receptors

Question 10

St Johns wort AoM Unipolar

Answer 10

Contains hyperforin A weak monoamine uptake inhibitor, activates P450 enzymes and can alter effects of other drugs

Question 11

Lithium

Answer 11

Bipolar Used prophylactically to avoid manic depressive episodes

Question 12

Valproate

Answer 12

Bipolar, antiepileptic drugs

Question 13

Olanzapine for which depression

Answer 13

bipolar, an atypical antipsychotic drug blocks dopamine receptors in hypothalamus and leads to expression of prolactin

Question 14

Sedative Hypnotics 9

Answer 14

Benzodiazepines Barbiturates Chloral hydrate Zolpidem Buspirone Baclofen Diphenyhydramine Ethanol Flumazenil

Question 15

Benzodiazepines and Barbiturates moa

Answer 15

Enhance effect of native GABA on GABA-A receptors (modulators not direct agonists) Barbiturates at higher doses also inhibit AMPA (glutamate) receptors

Question 16

Subclasses of barbiturates 3 how long acting and used for

Answer 16

Long acting- Phenobarbital (antiepileptic) Intermediate acting- Pentobarbital (sleep induction) Short acting- Thiopental, induction anesthetic

Question 17

Benzodiazipines examples and their half lives

Answer 17

Most have active metabolites–> extends functional half-lives Triazolam 1.5 hrs Midazolam 4 hrs Oxazepam 8 hrs Lorazepam 14 hrs *Diazepam 48-100 hrs Flurazepam 100 hrs most eventually get glucuroniated–> secreted by kidneys

Question 18

Chloral Hydrate MoA Used for

Answer 18

Similar action to benzodiazepines Short acting sleep inducer Used for conscious sedation in dentistry, no repetitive doses

Question 19

Zolpidem MOA Used for

Answer 19

Act on GABA receptors (BZ1 receptor site) Not anticonvulsant Tx insomnia

Question 20

Buspirone MOA Used for

Answer 20

Partial agonist at 5HT1A receptors not GABA Tx anxiety

Question 21

Baclofen MOA Used

Answer 21

Agonist of GABA-B Muscle relaxant

Question 22

Diphenyhydramine MOA Used

Answer 22

Block H1 receptors in CNS Sedation

Question 23

Ethanol MOA Used

Answer 23

Multiple targets including GABA-A Sedation

Question 24

Flumazenil MOA Used

Answer 24

GABA-A Bensodiazepine receptor antagonist Reverse sedation

Question 25

Mechanisms of action for antiepileptics

Answer 25

Na+ channel antagonists Ca++ channel antagonists - either acting on channel itself or on a modulatory subunit Glutamate receptor antagonists -AMPA, NMDA Cl- channel agonists

Question 26

Antiepileptic Drugs

Answer 26

Phenobarbital Phenytoin Primidone Carbamazepine Gabapentin Valporic acid (Valporate) Ethosuximide

Question 27

Phenobarbital MoA

Answer 27

GABA-A Receptor Modulator

Question 28

Phenytoin MoA

Answer 28

Nav+ antagonist Often eliminated by zero order kinetics (potential for OD)

Question 29

Primidone MoA

Answer 29

Metabolized to phenobarbital and other active compounds

Question 30

Carbamazepine also used for MOA

Answer 30

Also used for bipolar, trigeminal neuralgia Nav+ antagonist

Question 31

Gabapentin MoA

Answer 31

UK MoA does not bind GABA A or B receptors

Question 32

Valporic acid also used for MoA

Answer 32

Bipolar Inc GABA and block Nav+ and Cav++

Question 33

Ethosuximide MoA

Answer 33

Block Cav++