CNS Pharmacology Flashcards

1
Q

Typical antipsychotics

A
  • 1st generation dopamine antagonists
  • Phenothiazones, Haloperidol, thiothixene
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2
Q

Phenothiazones derivatives

A

Chlorpromazine- aliphatic derivative of phenothiazone

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3
Q

Atypical Antipsychotics

1ex

A

Newer 2nd gen dopamine antagonists

Clozapine

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4
Q

Antipsychotic drugs mechanism of action

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

Types of antidepressant drugs for unipolar

A

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

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6
Q

Monoamine uptake inhibitors

A

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)

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7
Q

Monoamine Oxidase Inhibitors MAOI

A

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

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8
Q

Monoamine receptor antagonists ie Unipolar

A

alpha 2 adrenergic receptor blockers Mirtazapine

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9
Q

Trazodone AoM Unipolar

A

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

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10
Q

St Johns wort AoM Unipolar

A

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

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11
Q

Lithium

A

Bipolar Used prophylactically to avoid manic depressive episodes

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12
Q

Valproate

A

Bipolar, antiepileptic drugs

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13
Q

Olanzapine for which depression

A

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

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14
Q

Sedative Hypnotics 9

A

Benzodiazepines Barbiturates Chloral hydrate Zolpidem Buspirone Baclofen Diphenyhydramine Ethanol Flumazenil

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15
Q

Benzodiazepines and Barbiturates moa

A

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

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16
Q

Subclasses of barbiturates 3 how long acting and used for

A

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

17
Q

Benzodiazipines examples and their half lives

A

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

18
Q

Chloral Hydrate MoA Used for

A

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

19
Q

Zolpidem MOA Used for

A

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

20
Q

Buspirone MOA Used for

A

Partial agonist at 5HT1A receptors not GABA Tx anxiety

21
Q

Baclofen MOA Used

A

Agonist of GABA-B Muscle relaxant

22
Q

Diphenyhydramine MOA Used

A

Block H1 receptors in CNS Sedation

23
Q

Ethanol MOA Used

A

Multiple targets including GABA-A Sedation

24
Q

Flumazenil MOA Used

A

GABA-A Bensodiazepine receptor antagonist Reverse sedation

25
Mechanisms of action for antiepileptics
Na+ channel antagonists Ca++ channel antagonists - either acting on channel itself or on a modulatory subunit Glutamate receptor antagonists -AMPA, NMDA Cl- channel agonists
26
Antiepileptic Drugs
Phenobarbital Phenytoin Primidone Carbamazepine Gabapentin Valporic acid (Valporate) Ethosuximide
27
Phenobarbital MoA
GABA-A Receptor Modulator
28
Phenytoin MoA
Nav+ antagonist Often eliminated by zero order kinetics (potential for OD)
29
Primidone MoA
Metabolized to phenobarbital and other active compounds
30
Carbamazepine also used for MOA
Also used for bipolar, trigeminal neuralgia Nav+ antagonist
31
Gabapentin MoA
UK MoA does not bind GABA A or B receptors
32
Valporic acid also used for MoA
Bipolar Inc GABA and block Nav+ and Cav++
33
Ethosuximide MoA
Block Cav++