Pharmacology Test #1 - Cns

Front 1

Schizophrenia

Mechanism of action

Back 1

Dopamine antagonist
-typical antipsychotics
-Atypical antipsychotics

Front 2

Schizophrenia

List the drugs that are a dopamine antagonist typical antipsychotic.

Back 2

Haldol (haloperidol)


o Mechanism: Binds to receptors in all central dopamine pathways
o Effect: Alleviate positive symptoms, hallucinations, delusions
o No effect on: interpersonal withdrawal, loss of drive, flattened affect
o BINDS TO D2 Receptor
 Adverse effects of Conventional antipsychotic
• Dystonia- diskinetic movements due to tonicity
• Akinesia- absent of movement
• Tardive dyskinesia- continual chewing and nose twitching
• Pituitary gland
• Antagonism of peripheral muscarinic receptors
o Dry mouth = cavities

Front 3

Schizophrenia

Haldol - MOA

Effect: __________

Back 3

o Mechanism: Binds to receptors in all central dopamine pathways
o Effect: Alleviate positive symptoms ONLY, hallucinations, delusions
o No effect on: interpersonal withdrawal, loss of drive, flattened affect

Front 4

Schizophrenia

Haldol binds to _______ receptor.

Back 4

D2 Receptor

Front 5

Schizophrenia

Adverse effects of Conventional antipsychotics

Back 5

• Dystonia- diskinetic movements due to tonicity
• Akinesia- absent of movement
• Tardive dyskinesia- continual chewing and nose twitching
• Pituitary gland
• Antagonism of peripheral muscarinic receptors
o Dry mouth = cavities

Front 6

Schizophrenia

List the Atypical antipsychotics

Back 6

Clozaril (clozapine)
Zyprexa (olanzapine)
Risperdal (Risperidone)
Seroquel (quetiapine)
Abilify (ariprazole)

Front 7

Schizophrenia

Clozaril (clozapine) is a ___________ antipsychotic.

MOA- ___________

Effects- __________________

Adverse Effects- ________________

Back 7

o Atypical Antipsychotic
o Mechanism
 Binds to receptors in mesolimbic and mesocortical dopaminergic pathways– more selective than older drugs (Haldol)
 Greater affinity for dopamine receptor subtypes found in these areas, D4 and D3
 Fewer side effects
o Effects: Positive and Negative symptoms
 Binds to serotonin receptor = alleviates negative effects
o Adverse effects:
 Weight gain = leads to non compliance
 Anticholinergic effect
 HYPER-salivation
 1% develop agranulocytosis
 BLOOD COUNT EVERY 2 WEEKS

Front 8

Schizophrenia

Zyprexa

What is unique about zyprexa?
MOA -- ______________
Effects- _______________
Adverse effects- _________________

Back 8

Patient 10x more likely to developo diabetes or exacerbate diabetes
o Mechanism
 Binds to receptors in mesolimbic and mesocortical dopaminergic pathways– more selective than older drugs (Haldol)
 Greater affinity for dopamine receptor subtypes found in these areas, D4 and D3
 Fewer side effects
o Effects: Positive and Negative symptoms
 Binds to serotonin receptor = alleviates negative effects

Adverse effects = same except for
Agranulocytosis
Hypersalivation

Front 9

Schizophrenia

Risperdal
MOA -- ______________
Effects- _______________
Adverse effects- _________________

Back 9

o Mechanism
 Binds to receptors in mesolimbic and mesocortical dopaminergic pathways– more selective than older drugs (Haldol)
 Greater affinity for dopamine receptor subtypes found in these areas, D4 and D3
 Fewer side effects
o Effects: Positive and Negative symptoms
 Binds to serotonin receptor = alleviates negative effects


Adverse effects = same except for
Agranulocytosis
Hypersalivation

Front 10

Schizophrenia

Seroquel

MOA -- ______________
Effects- _______________
Adverse effects- _________________

Back 10

o Mechanism
 Binds to receptors in mesolimbic and mesocortical dopaminergic pathways– more selective than older drugs (Haldol)
 Greater affinity for dopamine receptor subtypes found in these areas, D4 and D3
 Fewer side effects
o Effects: Positive and Negative symptoms
 Binds to serotonin receptor = alleviates negative effects


Adverse effects = same except for
Agranulocytosis
Hypersalivation

Front 11

Schizophrenia

Abilify

Classification
Partial agonist at ____________ and _______________.
Antagonist at __________________.

Indications- ___________, __________________. and __________

Back 11

o Atypical antipsychotics
o Partial agonist at DOPAMINE and SEROTONIN (5 HT 1A)
o Antagonist at serotonin (5-HT 2A)
o Indications = schizophrenia, bipolar and depression

Front 12

Parkinsons

Drugs that work on Parkinsons:
Effects __________________ precursors
Acts as a _________________ receptor ________________
Inhibits __________________________
______ of ________ is gone before symptoms appear

Back 12

 Dopamine precursors
 DOPAMINE receptor agonist
 Inhibitors of dopamine metabolism
 60% of dopamine gone before symptoms appear

Front 13

Parkinsons

Symptoms

Back 13

• #1 = resting tremor
• Postural instability (predispose to falling)
• Rigidity
• Cholinergic hyperactivity
• Dementia
• 1% of Americans above 60

Front 14

Parkinsons

Effects
Under-stimulation of _____________ pathway and under-inhibition of ____________ pathway

Off balance of neurotransmitters
- Decreased ____________
- Normal ________________

Back 14

• Under-stimulation of direct pathway and under-inhibition of indirect pathway
• Off balance of neurotransmitters
o DECREASED – DOPAMINE
o Normal – acetylcholine

Front 15

Parkinsons

Therapy goals

Back 15

• Increase Dopamine
• Suppress acetylcholine actions

Front 16

Parkinsons

Result of low dopamine and normal acetylcholine levels. Can't just give dopamine because _______________.

Levodopa- ______________
Carbidopa- _____________

Back 16

 Can’t just give dopamine
• Dopamine doesn’t cross blood brain barrier BUT levodopa does
• Levodopa metabolized by dopa decarboxylase to dopamine in CNS
• Levodopa metabolized in GI and peripheral tissue before reaching brain
• Carbidopa = dopa decarboxylase inhibitor that does not cross BBB
• Carbidopa/Levodopa = Sinement

Front 17

Parkinsons

Sinement ( _______________ + _________________)

Classification
Adverse effects
Oral Problems

Back 17

• Sinement (Carbidopa + Levodopa)
Dopamine precursors
o Adverse effects- Abnormal involuntary movements of orofacial muscles
o Oral problems – Inflammation, damage to oral structures, movement of anterior teeth, difficult wear dentures
o Dry mouth

Front 18

Parkinsons

Requip

What receptor does it effect?
Adverse effects

Back 18

• Ropinirole (Requip)
o D2 receptor Agonist
o Adverse effects – abnormal involuntary movements, confusion, psychosis and dry mouth

Front 19

Parkinsons

Comtan

Inhibitor of _____________
Inhibits __________________ metabolism

Back 19

o INHIBITOR of COMT***EXAM*** (also tolcapone/tasmar)
o INHIBITs Dopamine metabolism

Front 20

Parkinsons

Azilect (rasgiline)

Inhibits ____________ metabolism
Inhibition of ____________
______________________ inhibition at higher dose.
Should not inhibit __________________

Dental drug interactions: _______________ and __________

Back 20

o Inhibits dopamine metabolism
o Inhibition of MAO-B
o Non-selective MAO inhibition at higher doses
 SHOULD NOT inhibit type-A MAO
o Dental drug interaction: Demerol methadone, tramadol

Front 21

Parkinsons


Dopamine precursors
_______________________

Dopamine receptor agonists
______________________

Inhibitors of dopamine metabolism
______________
_______________

Back 21

Dopamine precursors
Carbidopa/Levodopa = Sinemet

Dopamine receptor agonists
Ropinirole (Requip)

Inhibitors of dopamine metabolism
Rasagiline (Azilect)
Entacapone (Comtan)

Front 22

Schizophrenia


Dopamine antagonists
Typical antipsychotics
• ____________
Atypical antipscyhotics
• _____________
• _____________
• _____________
• _____________
• ______________

Back 22

Dopamine antagonists
Typical antipsychotics
• Haldol
Atypical antipscyhotics
• Clozapine
• Olanzapine (Zyprexa)
• Risperidone (Risperdal)
• Quetiapine (Seroquel)
• Ziprasidone (Geodon)

Front 23

Depression

Use inhibitors of __________________
Use __________________ inhibitors

Results from pathologically decreased ___________ and/or __________

Back 23

o Depression –
 Use inhibitors of Serotonin degradation
 Use serotonin reuptake inhibitors
 Results from: pathologically decreased serotonin and/or norepinephrine NT.
• Take 3 weeks to have an effect

Front 24

Depression

EMSAM (selegiline)

Dosage form

MOA

Back 24

***Monoamine oxidase inhibitors (MAOIs)
o Initial exposure of the drug to the digestive tract is minimized
o 6 mg/24 hr patch
 inhibit MAO in the brain (MAO-B) for antidepressant effect
 preserving MAO-A in the digestive tract to break down tyramine
o 9 mg/24 hr patch and the 12 mg/24 hr patch
 dietary modifications are required
o Dental adverse effects: dry mouth, orthostatic hypotension

Front 25

Depression

What drug is a monoamine oxidase inhibitor?

Adverse effect:
Contraindicated with:
Diet restriction:

Back 25

Selegiline (EMSAM)

• MAO = enzyme that breaks down monoamines
• Adverse effect: brain hemorrhage
• Contraindicated: CVD, epilepsy, bronchitis, HTN, asthma
• Diet restriction: NO FOOD with TYRAMINE

Front 26

Depression

Elavil (amitriptyline)

Classification of drug

MOA:
Adverse Effects
Indications:
Drug interactions:
OVerdose:

Back 26

o Tricyclic Antidepressant
o Mechanism: NE and serotonin reuptake inhibitors
 Also block muscarinic receptors and α1 adrenergic receptors
o Adverse Effects: dry mouth, orthostatic hypotension
o Indications: Depression, anxiety, obsessive-compulsive disorder (OCD)
o Drug interactions of TCA– Increased effects of epinephrine
o Overdose of TCAs- leads to cardiotoxicity, arryhythmias, MIs