Central Nervous System Agents

Front 1

Anti-depressants
Serotonin reuptake inhibitors
Mechanism of Action

Back 1

These drugs inhibit the membrane protein pumps that transport released serotonin (5HT) into the neuronal ending for recycling. This results in more serotonin available in the synaptic cleft and an increased stimulation of post-synaptic receptors

Front 2

Anti-depressants-
Serotonin reuptake inhibitors
Interactions:

Back 2

SSRIs are highly plasma protien bound (the amount of binding differs with each individual drug) and so have the potential for drug interactions. They are also metabolized by the cytochrome mixed function oxidase system ( cytochrome 450)-another potential for drug interactions.

Front 3

Anti-depressants-
Serotonin reuptake inhibitors
Adverse effects

Back 3

Rash and skin abnormalities are not uncommon. In addition, these drugs bind to receptors for neurotransmitter substances, such as norepinephrine, acetylcholine, and histamine. Thus, common adverse effects include headache, dizziness, sedation, insomnia, restlessness, tremor, and gastrointestinal dysfunction and decreased libido, weight loss. Cardiovascular effects, such as palpitations, chest pain, and hypotension, may also be seen. Thesse drugs can also cause serotonin syndrome, due to an increased level of serotonin in the CAN. This syndrome is characterized by fever, agitation, confusion, tremors, and cardiovascular abnormalities, which may progress to coma and death.

Front 4

Anti-depressants-
Serotonin reuptake inhibitors
Contraindications

Back 4

SSRIs should not be used in combination with MAO inhibitors or within two weeks of terminating treatment with MAO inhibitors. Treatment after this time should then be initiated cautiosly and dosage increased gradually until optimal response is reached. Conversely, MAO inhibitors should not be introduced within two weeks of cessation of therapy with an SSRI.

Front 5

Anti-depressants-
Serotonin reuptake inhibitors
Treatment of psychiatric patients:

Back 5

SSRIs can cause a manic episode or exacerbate existing mania. They should therefore be used with caution, or not at all, in bipolar or manic patients.

Front 6

Anti-depressants-
Serotonin reuptake inhibitors
List all drug in this category

Back 6

1.Floxetine (Prozac, Sarafen)
2.Flovoxamine A.K.A Flovoxamine maleate (Lovox)
3.Paroxetine hydrocholride (Zoloft)
4.Paroxetine mesylate (Asimia)
5.Sertraline hydrochoride (Zoloft)
6.Venlafaxine hydrochloride (Effexor, Effexor XR)
7. Citalopram (celexa)
8. Escitalopram (Lexapro)

Front 7

Anti-depressants-
Serotonin reuptake inhibitors
Floxetine (Prozac, Sarafen)
Metabolized:

Back 7

Heptic

Front 8

Anti-depressants-
Serotonin reuptake inhibitors
Floxetine (Prozac, Sarafen)
Half life:

Back 8

very long half life (2 days) increases to four with consistant dosing… after drug is with drawn… active drug may remain in plasma for as much as two months

Front 9

Anti-depressants-
Serotonin reuptake inhibitors
Flovoxamine A.K.A Flovoxamine maleate (Lovox)
Half life-

Back 9

shortest of all SSRIs

Front 10

Anti-depressants-
Serotonin reuptake inhibitors
Flovoxamine A.K.A Flovoxamine maleate (Lovox)
Additional uses:

Back 10

obsessive-compulsive disorder(OCD), and has also benn used in the treatment of post-traumatic stress disorder, obesity, bulimia nervosa, scizophrenia, panic disorder, and social anxiety disorder

Front 11

Anti-depressants
-Serotonin reuptake inhibitors
Citalopram (celexa)
Contraindication:

Back 11

has anticonvulsant effects and should be used with caution in patients with a history of seizures.

Front 12

Anti-depressants-
-Serotonin reuptake inhibitors
Escitalopram (Lexapro)
Half life:

Back 12

doubles in patients with reduced liver function

Front 13

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Mechanism of Action:

Back 13

tricyclic antidepressants inhibit reuptake of neurotransmitter into the neuronal ending. The primary neurotransmitters affected are norepinephrine and serotonin.
Inhibition of reuptake occurs immediately, although the clinical benefits of the drug are not seen for four to five weeks. IT is now thought that the major clinical action of these drugs is due to a decrease in beta receptors in an area of the brain called the limbic system (the increased concentration of norepinephrine causes an over stimulation of beta receptors, and leads to a decrease in receptor number or function)

Front 14

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
List all drugs:

Back 14

1. Imipramine (Tofranil, Janimine)
2. Desirpramine (Norpramin, Pertofrane)
3. Amitriptyline (Elavil)
4. Nortriptyline (Aventyl, Pamelor)
5. Doxepin (Adapin, Sinequan)
6.Amoxapine (Ascendin)

Front 15

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Adverse Effects

Back 15

These drugs have very low patient compliance, due to the delayed onset of clinical effects and the prompt onst of adverse effects. Tricyclis are very non specific drugs and therefore have effects at various receptors- in particular they have an afiinity for muscarinic and histamine receptors. This results in constipation, as well as less frequently seen effects, such as palpiations and arrhythmias. Effects on histamine recetptors cause increased sedation.

Front 16

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Interactions:

Back 16

Tricyclics are highly plasma protein bound, so drug interactions with other drugs that bind to plasmsa proteins may cause fluctuations in plasm concentration of the drug and potential toxicity.

Front 17

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Contraindication

Back 17

These drugs are contraindicated with any drug or substance that causes an increase in the levels of catecholamines (eg. Norepinephrine), or serotonin levels

Note: Tricyclis should not be administered within 14 days of treatment with an MAO inhibitor. Doing so could result in a hypertensive crisis, due to radically incrased levels of norepinephrine.

-Tricyclics should not be administered during the acute phase of recovery from a myocardial infarction, or to a patient with glaucoma, becouse of the drug’s antimuscarinic effects.

-Tricyclics are contraindicated in hyperthyroid patients, or those on exogenous thyroid medication, because of the increased sensitivity to catecholamines in these patients.

-Because of the high degree of sedation, operating machinery and driving etc should be done with caution.

Front 18

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Imipramine (Tofranil, Janimine)
Half life:

Back 18

long… but shortend in patients that are hepatically comprimised.

Front 19

Anti-depressants-
Second Line Antidepressants
Tricyclic Anti-depressants
Doxepin (Adapin, Sinequan)
adverse effects:

Back 19

Due to strong anticholinergic actions, the drug can cause changes in heart rate and conduction (producing a “quinidine like effect), possibly leading to heart block and /or arrhythmias. CAN effects, such as headache, drowsiness, autonomic effects, and insomnia may also be seen, as well as seizures. GI disturbances and various other effects may be seen as well.

Front 20

Anti-depressants-
Second Line Antidepressants
Monoamine Oxidase Inhibitors (MOA)
Mech of action:

Back 20

work by inhibiting MAO in a dose dependant manner, which results in a decrease in the rate of metabolism of norepinephrine. This results in more norepinephrine available to be released from the neuron.

Front 21

Anti-depressants-
Second Line Antidepressants
Monoamine Oxidase Inhibitors (MOA)
List all drugs:

Back 21

Phenelzine (Nardil)

Front 22

Anti-depressants-
Second Line Antidepressants
Monoamine Oxidase Inhibitors (MOA)
Adverse effects:

Back 22

: hypertensive crisis;-food interactions: “feel good” foods, such as wine, cheese, chocolate and beans contain a substance called tyramine, which is normally broken down by MAO shortly after ingestion. Without MAO present, the tyramine is absorbed and can enter the noradrenergic neuron and be converted to a false transmitter, octopamine, by enzymes that normally make norepinephrine. Octopamine is packaged wit norepinephrine in the secretory vesicles, and pushes out the norepinephrine, causing a huge release of norepinephrine. If MAO were active in the cell, the norepinephrine would be broken down in the neuron, but it is not, so huge amount of norepinephrine are released.

A serious adverse effect of MAOIs is the development of a hypertensive crisis. Orthostatic hypotension; peripheral edema and swelling of the legs; anticholinergic effects, such as sedation, miosis, confusion, blurred vision, and urinary retention; sexual dysfunction; tremors, insomnia, and fatigue, hematological reaction (anemia, pancytopenia; liver toxicity (rare)

Front 23

Anti-depressants-
Unclassified
Third line antidepressants
Mecanism of action

Back 23

Unknown, but as been shown that bupropion inhibit’s the neuronal uptake

Front 24

Anti-depressants-
Unclassified
Third line antidepressants
List all Drug(s)

Back 24

Bupropion (Wellbutrin, Wellbutrin SR, Zyban)

Front 25

Anti-depressants-
Unclassified
Third line antidepressants
Adverse effects:

Back 25

high potential for causing drug induced seizures if taken with alcohol

Front 26

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
List all drugs:

Back 26

1.Amoxipine (considered a heterocyclic but also a tricyclic)
2. Maprotiline (ludiomil)
3. Nefazadone (serzone)
4. Trazadone (desyrel)

Front 27

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Amoxipine
Uses:

Back 27

a heterocyclic but also a tricyclic

Front 28

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Maprotiline (ludiomil)
Contraindication

Back 28

: patients with cardiovascular disease or hypothyroidism

Front 29

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Nefazadone (serzone)
Metabolism

Back 29

heptic

Front 30

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Nefazadone (serzone)
Uses

Back 30

both a serotonin reuptake inhibitor (SRI) and 5HT2 antagonist., useful for chronic pain.

Front 31

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Nefazadone (serzone)
Adverse effects:

Back 31

: Cases of life-threatening hepatic failure have been reported in patients treated with nefazadone. Therapy should not be initiated in individuals with active liver disease or with elevated baseline serm transaminases. Patients should be advised to be alert for signs and symptoms of liver dysfunction (e.g. jaundice, anorexia, gastrointestinal complaints, malaise, etc.) and to report them to the doctor immediately if they occur.

Front 32

Anti-depressants-
Third line antidepressants
Heterocyclic Antidepressants
Trazadone (desyrel)
Adverse effects:

Back 32

has been shown to cause priapism in young males; causes sedation
Contraindicated: synergism with alcohol and/or barbiturates can produce CNS depression
Mechanism of action: Serotonergic neurons also contain <><2 receptors, called heterocreceptors, which decrease serotonin release. These drugs block heteroreceptors, which results in increased release of 5HT.

Front 33

CNS Agents
Sedative Hypnotics
List Classes of drug

Back 33

Benzodiazepines and barbiturates

Front 34

CNS Agents
Sedative Hypnotics
Mecanism of action

Back 34

These sedative-hypnotic drugs work by augmenting the actions of the inhibitory neurotransmitter GABA. They thus decrease the frequency and amplitude (strength) of neuronal transmission. This results in decreased rate of firing of neurons, decreased mental acuity, relaxation, and eventually sleep.

Front 35

CNS Agents
Sedative Hypnotics
Barbituates
Adverse effects:

Back 35

Respitory Depression; changes in bowel function; sleep changes

Front 36

CNS Agents
Sedative Hypnotics
Barbituates
Interactions

Back 36

Alcohol, opiates, other CNS drugs

Front 37

CNS Agents
Sedative Hypnotics
Barbituates
Classified:

Back 37

CII and CIII

Front 38

CNS Agents
Sedative Hypnotics
Benzodiazepines
Adverse effects

Back 38

: Sedation; difficulty in movement; visual disturbances; changes in bowel and bladder function; skin rash; changes in libido; sleep changes; rebound insomnia

: rarely occur, but include leukopenia, jaundice, hypersensitivity, paradoxial reactions.

Front 39

CNS Agents
Sedative Hypnotics
Benzodiazepines
Paradoxial Reactions:

Back 39

upon withdrawl…hyperexictability, anxiety, excitement, hallucinations, increased muscle spasticity, insomnia, rage and sleep disturbances, If the patient experiences these symptoms during therapy, the drug should be withdrawn

Front 40

CNS Agents
Sedative Hypnotics
Benzodiazepines
Contraindicated:

Back 40

pregnancy Withdrawal should be gradual

Front 41

CNS Agents
Sedative Hypnotics
Benzodiazepines
Classified:

Back 41

CIII and CIV

Front 42

Central Nervous System Agents
Drugs Used for Anxiety
Drug Class:

Back 42

Benzodiazepines

Front 43

Central Nervous System Agents
Drugs Used for Anxiety
Benzodiazepines

Back 43

A. Alprazolam (Xanax)
B. Lorazepam (Ativan)
C .Busirone (Buspar)

Front 44

Central Nervous System Agents
Drugs Used for Anxiety
Benzodiazepines
Alprazolam (Xanax)
Half life:

Back 44

short

Front 45

Central Nervous System Agents
Drugs Used for Anxiety
Benzodiazepines
Alprazolam (Xanax)
Contraindication:

Back 45

antimuscarinic effects and so is contraindicated in patients with narrow angle glaucoma or myasthenia gravis. Pregnancy

Front 46

Central Nervous System Agents
Drugs Used for Anxiety
Benzodiazepines
Lorazepam (Ativan)
Half life:

Back 46

long 3-4 days

Front 47

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders
Drug Class:

Back 47

Benzodiazepine and certain Antihistamines

Front 48

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders
List all drugs:

Back 48

Benzodiazepines
A. Lorazpam (Ativan)
B. Temazepam (Resoril)
C. Triazolam (Halcion)
“The non-benzodiazepine benzodiazepine”
A. Zolpidem (ambien)
Antihistamines
1. Zopiclone

Front 49

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders
Lorazepam(Ativan)
Half life:

Back 49

8 to 10 hours (serum half life)

Front 50

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders
Temazepam (Resoril)
Half life:

Back 50

3 hours (serum)

Front 51

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders
Temazepam (Resoril)
Metabolized:

Back 51

liver

Front 52

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders

“The non-benzodiazepine benzodiazepine”

Zolpidem (ambien)
Mech of aciton

Back 52

: This drug is similar in structure to the benzodiazepines, and, like the benzodiazepines, binds to a receptor (the omega-3 receptor) on the choloride channel, causing a decrease in sensitivity of neuronal membranes to stimulus. It is no considered to be a benzodiazepine, however, and has therfore been termed the “ non…

Front 53

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders

“The non-benzodiazepine benzodiazepine”

Zolpidem (ambien)
Uses:

Back 53

delayed sleep onset type of insomnia

Front 54

Central Nervous System Agents
Drugs used in Therapy of Insomnia and sleep disorders

Antihistamines
Zopiclone
Contraindications:

Back 54

myasthenia gravis and with glaucoma

Front 55

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Contraindications:

Back 55

Alcohol

Front 56

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Tolerance:

Back 56

physically addictive… abrupt withdrawl may lead to life threating siezure called status ellipticus

Front 57

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
List all drug sub groups:

Back 57

1. Sodium Channel Blockers
2. Drugs that mimic the effects of GABA
3. Drugs that affect excitatory neurotransmitter levels
4. Barbiturates and Benzodiazepines as Anticonvulsants
5. Therapy of Status Epirlepticus

Front 58

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
List all drugs:

Back 58

A. Carbamazepine (Tegretol XR, Carbatrol)
B. Phenytoin Sodium (Dilantin Infatab, Dilantin-125)
C. Fosphenytoin (cerebyx)

Front 59

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Carbamazepine (Tegretol XR, Carbatrol)
Adverse Effects:

Back 59

aplastic anemia, sunburn

Front 60

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Carbamazepine (Tegretol XR, Carbatrol
Mechanism of action

Back 60

: antimuscarinic actions (blocks muscarinic receptors for acetylcholine)

Front 61

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Phenytoin Sodium (Dilantin Infatab, Dilantin-125)
Mech of action:

Back 61

blockade of both sodium and potassium channels… primary site of action appears to be the motor cortex, making the drug useful in the tonic phase of grand mal seizures.

Front 62

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Phenytoin Sodium (Dilantin Infatab, Dilantin-125)
Adverse Effects include

Back 62

Osteomalacia due to the effects of the drug on vitamin D
Hypoglycemia; gingival hyperlasia (swelling of gums); CNS effects( nystagmus, ataxia, slurred speech, decreased coordination, and mental confusion.; bone marrow suppression; may produce a characheristic urticaria

Front 63

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Phenytoin Sodium (Dilantin Infatab, Dilantin-125)
Metabolized:

Back 63

involves the enzyme aldehyde dehydrogenase, so it may produce “dusulfiram-like” reactions, particularly with the concurrent administration of ethanol. (liver enzymes) these events are termed (disulfiram-like reactions)

Front 64

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Phenytoin Sodium (Dilantin Infatab, Dilantin-125)
Form:

Back 64

Phenytoin is not administered by rapid Injection

Front 65

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Sodium Channel Blockers
Fosphenytoin (cerebyx)
Uses:

Back 65

may be used for status elipticus. Rapidly injectable

Front 66

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
List all drugs:

Back 66

A. Gabapentin (Neutotin)
B. Vigabatrin (Sabril)
C. Tiagabine (Gabatril)

Front 67

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
Gabapentin (Neutotin)
Mechanism of action:

Back 67

Stucally related to GABA, but mech of action is unknown

Front 68

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
Gabapentin (Neutotin)
Uses:

Back 68

supplemental therapy in control so seizures, and in the therapy of bipolar disorder

Front 69

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
Gabapentin (Neutotin)
Metabolized:

Back 69

Renal excreation (kidney)

Front 70

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
Vigabatrin (Sabril)
Mech of action:

Back 70

increases the amount of available GABA. It is similar in structure to GABA (it is a “structual analog” of GABA), and competes with GABA for binding sites on the enzyme (GABA Transaminase) that metabolises GABA. Thus, it interferes with the metabolism of GABA, reculting in increased levels of available GABA.

Front 71

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that mimic the effects of GABA
Tiagabine (Gabatril)
Mech of action:

Back 71

selectively inhibit’s the neuronal reuptake of GABA. This results in increased levels of GABA available to bind to the GABA receptor.

Front 72

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that affect excitatory neurotransmitter levels
List all drugs

Back 72

A.Valproic acid (Depakene)
B. Lamotrigine (Lamictal)

Front 73

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that affect excitatory neurotransmitter levels
Valproic acid (Depakene)
Adverse effects:

Back 73

liver toxicity: sedation; sodium causes edema

Front 74

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that affect excitatory neurotransmitter levels
Valproic acid (Depakene)
Contraindication:

Back 74

clonzaepam may result in status epilepticus, pregnancy

Front 75

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Drugs that affect excitatory neurotransmitter levels
Lamotrigine (Lamictal)
Adverse effects:

Back 75

skin rash (life threatning)

Front 76

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
List all drugs:

Back 76

A. Phenobarbital
B. Butabarbital
C. Secobarbital

Front 77

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
Phenobarbital-
Uses:

Back 77

pediatric epilepsy

Front 78

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
Butabarbital
Uses:

Back 78

suppression of the spread of seizure activity in the cortex, thatlamus, and limbic systems

Front 79

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
Secobarbital
Form:

Back 79

IV

Front 80

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
Secobarbital
Uses:

Back 80

status elipticus

Front 81

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Barbituates
Secobarbital
Protective effects:

Back 81

protective effects on brain tissue- decreases damage due to lack of oxygen

Front 82

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Benzodiazepines
List Drug(s)

Back 82

Diazepam
Clonazepam

Front 83

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Benzodiazepines
Diazepam
Uses:

Back 83

anxiety, endoscopic surgery as a muslce relaxant; drug of choice for status elipticus.

Front 84

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Barbiturates and Benzodiazepines as Anticonvulsants
Benzodiazepines
Diazepam
Metabolism:

Back 84

metabolized by the liver to active metabolites desmethyldiazepam and oxazepam. Both of these have pharmacological activity and are marketed separatly

Front 85

Central Nervous System Agents
Drugs used in the therapy of seizures (Anticonvulsants)
Therapy of Status Epilepticus
List all drugs

Back 85

1. Drug of Choice - Diazepam
2. IV clonezepam or secobarbital
3. IV fosphenytoin (IV or IM)

Front 86

Central Nervous System Agents
Therapy of ADHD
List all drugs:

Back 86

1. Tricyclic Antidepressants

2. Amphetamines

3. Drug of choice: Methylphenidate (Ritalin, concerta (methyphenidate XR

Front 87

Central Nervous System Agents
Therapy of ADHD
Drug of choice: Methylphenidate
Mech of action:

Back 87

Methylphenidate selectively blocks neuronal reuptake of dopamine in the central nervous system. This results in an increase in central levels of dopamine in the brain stem, which regulates arousal, and the cerebral cortex, which regulates cognitve ability. Levels may also be Increased in the nigrostriatal tract and limbic system, which are involved in the regulation of movement and learning/memory/behavior, respectively.

Front 88

Central Nervous System Agents
Therapy of ADHD
Drug of choice: Methylphenidate
-Adverse effects-

Back 88

Psychologically addictive. Psychological addiction is more likely to occur with parenteral administartion, such as would be seen when the drug is abused.

Front 89

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
List all drugs (first and second line)

Back 89

A. L-dopa aka. Levodopa.. (Dopar, carodopa)
B. Levodopa with carbidopa (Sinemet)
C. Bromocriptine (Parlodel, Ergoset)

Second Line:

D. Tolcapone (Tasmar, Mirapex)
E. Selegiline (Eldepry, Carbex)

Front 90

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Mechanism of action:

Back 90

attempt to normalize the balance between dopamine and acetylcholine- either by increasing dopamine levels or decreasing levels of acetylcholine.

Front 91

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
L-dopa aka. Levodopa.. (Dopar, carodopa)
Adverse Effects:

Back 91

Extrapyramidal effects; hallucinations; behavioural changes

Front 92

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Levodopa with carbidopa (Sinemet)
Uses:

Back 92

: the effects of L-dopa wear off after a period of time. Therapy must then be stopped, and reinstated at a later date. The period of time between therapies is called a drug holiday and gives the tussue time to return to a responsive state.

Front 93

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Bromocriptine (Parlodel, Ergoset)
Mech of action:

Back 93

: Bromocriptine is an agonist at dopamine receptors. It therefore stimulates the receptor and mimics the effects of dopamine.
Adverse effects: psychiatic effects, mimicking schizophrenia. The autonomic (eg. Cardiovascular) effects of the drug are minimal.

Front 94

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Second line:
Tolcapone (Tasmar, Mirapex)
Mech of action:

Back 94

inhibitor of COMT. It thus:
-Decreases the metabolism of dopamine in the synaptic cleft, resulting in increased levels of available dopamine

-Decreases tissue metabolism of L-dopa, so when tolcapone and L-dopa are given ncurrently, greater amounts of L-dopa are presented to the neuron and drug potency is increased

Front 95

Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Second line:
Tolcapone (Tasmar, Mirapex)
Withdrawl

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graduall, as parkinson’s symptoms may reapperar

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Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Second line:
Tolcapone (Tasmar, Mirapex)
Adverse effects:

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Severe liver injury

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Central Nervous System Agents
Parkinson’s Disease
Drugs that increase levels or activity of dopamine
Second line:
Selegiline (Eldepry, Carbex)
Mechanism of action:

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irreversibly inhibits MAOb , resulting in decreased rate of dopamine breakdown within the neuron

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Central Nervous System Agents
Parkinson’s Disease
Angents that decrease levels or activity of Acetycholine
Mechanism of action:

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these drugs block muscarinic receptors and decrease cholinergic activity.

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Central Nervous System Agents
Parkinson’s Disease
Angents that decrease levels or activity of Acetycholine
Therapy:

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Blockade of muscarinic effects in the nigrostraiatal tract, resulting in normalization of acetylcholine/dopamine activity ration

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Central Nervous System Agents
Parkinson’s Disease
Angents that decrease levels or activity of Acetycholine
Contraindications:

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glaucoma (the “angle-closure” type, in particular), obstruction of the lower stomach (pyloric) valve or duodenum, enlarged prostate, obstructed bladder, myashenia gravis, and megacolon

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Central Nervous System Agents
Parkinson’s Disease
Angents that decrease levels or activity of Acetycholine
List all drugs:

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A. Procyclidine (kemadrin)
B. Biperiden (Akineton)
C. Amantadine HCI (symmetrel)

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Central Nervous System Agents
Therapy of Alzheimers Disease
Mechanism of Action:

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These drugs bind to the enzyme acetylcholinesterase. Binding occurs at the site where the enzyme normally binds acetylcholine, and destroys it. The result is more available acetylcholine. Since there are slight differences in structure between acetylcholinesterase in the CNS and the periphery, these drugs are targeted to selectively inhibit CNS Cholinesterase, resulting in decreased adverse effects. Nevertheless, in high doses, toxicity may be seen

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Central Nervous System Agents
Therapy of Alzheimers Disease
Adverse effects:

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Bradycardia (slow heart rate), hypotension (low blood pressure); bowel and/or bladder dysfunciont; Miosis (pinpoint pupils); dyspepsia (upset stomach); difficulty in breathing, muscle weakness, and confusion may also be present; liver toxicity

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Central Nervous System Agents
Therapy of Alzheimers Disease
List all drugs:

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A. Tacrine (cognex)
B. Donezepil

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Central Nervous System Agents
Therapy of Alzheimers Disease
Donezepil (aricept)
Mech of action:

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piperadine-type inhibitor of acetylcholinesterase

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Adverse Effects:

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: incrased prolactin secretion and milk production in both men and women due to the inhibition of dopamine actions at the pituitary; gynecomastia (enlarged breasts), particularly in men; parkinsons like sympoms, due to blockade of dopamine receptors in the substania nigra; neuroleptic malignant syndrome, characterized by severe fever, muscle rigidity, altered mental status (catatonia), and cardiovascular instability (unstable heart rate and blood pressure). This syndrome is similar to the malignant hyperthermia seen with inalation anesthetics and is a life threating condition.

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Mechanism of action:

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Treated with drugs that block dopamine receptors (dopamine antagonists.)

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Phonothiazides
List the 3 classes:

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Aliphatic side chain; piperdine side chain; and piperzine side chain

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Phonothiazides
adverse effects:

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should never be administered with epinephrine( loss of blood pressure)

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Phonothiazides
List Drugs in the aliphatic side chain:

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Promazine; chlorpromazine

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Phonothiazides
aliphatic side chain adverse effects

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autonomic effects, sedation, cardio, extrapyramidal… dry mouth…. Tardive dyskinesia

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Central Nervous System Agents
Therapy of Schizophrenia (Antipsychotics)
Phonothiazides
Piperdine side chain:
List all drugs:

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Thioridazine; mesoridazine;

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
Phonothiazides
Piperdine side chain:
adverse effects:

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cardio toxicity; extrapyramidal higher degree of tardive dyskinesia

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
Phonothiazides
Piperazine side chain:
List all drugs:

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Fluphenazine

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
Phonothiazides
Piperazine side chain:
adverse effects

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sedation, hypotensive

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
List all the drug classes other than the Phenothiazine class:

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Dibenzoxapines; Thioxanthines; buterophenones; Benzisoxazoles; Thienobenzodiazepines; Floourophenylindoles:

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
Dibenzoxaapines:
List drugs in this class

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Loxapine
Clozapine

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Central Nervous System Agents
Therapy of Schizophrenia(Antipsychotics)
Dibenzoxaapines:
Adverse effects:

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agranulocytosis; seizures; lowered other effects than others

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Thioxanthines:
List all drugs in this class:

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Thiothixine
Chloroprothixine

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Thioxanthines:
Adverse effects:

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sedation, extrapyramidal effects, decreased risk of tardive dyskinesia

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Buterophenoes:
List all drugs in this class

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Haloperidol

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Buterophenoes:
adverse effects:

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severe extrapyramidal effects

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Benzisoxazoles:
List drugs in class:

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riperidone

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Thienobenzodiazepines:
List drug(s)

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olanzepine

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Floourophenylindoles:
List drug(s)

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Olanzepine

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Frequently prescibed drugs:

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A. Chlorpromazine (Thorazine, Lagactil)
B. Thioridazine (mellaril)
C. Haolperidol (hadol)
D. Olanzapine (zyprexa)
E. Clozapine (clozaril)
F. Fluphenazine (permitil, prolixin)
G. Loxapine (Loxitane)
H. Quetiapine (seroquel)

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Buterophonones:
halperidol
Uses:

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tourette’s syndrome, mania

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Piperzine side chain:
Fluphenazine
Adverse effects

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high degree of extrapyramidal effects (tardive dyskninesia), particularly in older patients and women… should not be used when confusion and/or agitation are present, particularly in the elderly

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Dibenzoxapines:
Loxapine
Contraindicated:

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CNS depression, such as slcohol induced is present…comatose patients; siezures… caution with cardiovascular disease.

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Quetiapine
Mech of action:

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blocks both serotonin and dopamine receptors. Blocks <><1 receptors

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Quetiapine
Adverse effects:

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does not block muscarinic receptors, so no anticholinergic effects are seen… may cause postural hypotension.

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CNS agents
Therapy of Schizophrenia(Antipsychotics)
Quetiapine
Metabolized:

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metabolized by isoenzyme of liver cytochrome P450, which also metabolizes several other drugs. May cause liver damage.