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
Q

Mechanisms of action for antiepileptics

A

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
Q

Antiepileptic Drugs

A

Phenobarbital Phenytoin Primidone Carbamazepine Gabapentin Valporic acid (Valporate) Ethosuximide

27
Q

Phenobarbital MoA

A

GABA-A Receptor Modulator

28
Q

Phenytoin MoA

A

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

29
Q

Primidone MoA

A

Metabolized to phenobarbital and other active compounds

30
Q

Carbamazepine also used for MOA

A

Also used for bipolar, trigeminal neuralgia Nav+ antagonist

31
Q

Gabapentin MoA

A

UK MoA does not bind GABA A or B receptors

32
Q

Valporic acid also used for MoA

A

Bipolar Inc GABA and block Nav+ and Cav++

33
Q

Ethosuximide MoA

A

Block Cav++