Pharmacology Exam 3

Front 1

types of EPS

Back 1

-parkinsonism- anticholinergics (benztropine or diphenhydramine) may help, amantidine, levodopa should not be used
-akathisia- pacing and squirming, use benzos or propranolol
-acute dystonia- spasms, anticholinergics, antihistamines, or benzos help
-tardive dyskinesia- no effective treatment, anticholinergics make worse
-neuroleptic malignant syndrome- rare, dantrolene or bromocriptine may help

Front 2

Chlorpromazine

Back 2

-used for emesis, intractable hiccups, severe itching, and hyperexcitability in children
-low potency traditional- has worse anticholinergic effects (dry mouth, blurry vision, constipation)
-lower affinity for dopamine, and higher affinity for other receptors
-ADE is skin rash
-improves positive symptoms but not cognitive, may make negative symptoms worse

Front 3

Thioridazine

Back 3

-intractable hiccups, severe itching, and hyperexcitability in children
-low potency traditional- has worse anticholinergic effects (dry mouth, blurry vision, constipation)
-lower affinity for dopamine, and higher affinity for other receptors
-improves positive symptoms but not cognitive, may make negative symptoms worse

Front 4

Perphenazine

Back 4

-intractable hiccups, severe itching, and hyperexcitability in children
-high potency traditional- more parkinsonism, akathisia, acute dystonia (EPS)
-higher potency for dopamine than other receptors
-improves positive symptoms but not cognitive, may make negative symptoms worse

Front 5

Fluphenazine

Back 5

-high potency traditional- more parkinsonism, akathisia, acute dystonia (EPS)
-improves positive symptoms but not cognitive, may make negative symptoms worse
-higher potency for dopamine than other receptors

Front 6

Haloperidol

Back 6

-used for tourettes and huntington’s chorea
-high potency traditional- more parkinsonism, akathisia, acute dystonia (EPS)
-improves positive symptoms but not cognitive, may make negative symptoms worse
-higher potency for dopamine than other receptors- high EPS
-high prolactin secretion

Front 7

Clozapine

Back 7

-helps positive and negative and cognitive
-few EPS
-agranulocytosis- use is limited
-high muscarinic affinity (high anticholinergic effects- dry mouth, sedation, blurred vision)
-high alpha 1 blocking- hypotension
-high histamine blocking- high weight gain!

Front 8

Risperidone

Back 8

-high 5HT2A blocking- benefit in regard to positive symptoms
-high alpha 1 blocking- hypotension
-medium histamine blocking and weight gain
-higher prolaction secretion

Front 9

Olanzapine

Back 9

-high muscarinic affinity (high anticholinergic effects- dry mouth, sedation, blurred vision)
-high histamine blocking- high weight gain!

Front 10

Sertindole

Back 10

-withdrawn due to cardiotoxicity

Front 11

Quetiapine

Back 11

-may not have EPS at higher doses
-low 5HT2A

Front 12

Ziprasidone

Back 12

-doesn’t have much weight gain (because little 5HT2C)
-high 5HT2A blocking- benefit in regard to positive symptoms

Front 13

Aripiprazole

Back 13

-partial agonist- even though high DA blocking, less EPS

Front 14

Paliperidone

Back 14

-metabolite of risperidone

Front 15

Serotonergic functions: 1A

Back 15

improves mood

Front 16

Serotonergic functions: 2A

Back 16

causes agitation, OCD, anxiety, insomnia, sexual dysfunction

Front 17

Serotonergic functions: 2C

Back 17

causes anxiety, anorexia

Front 18

Serotonergic functions: 3

Back 18

causes nausea and cramps

Front 19

Serotonergic functions: 4

Back 19

causesa cramps and diarrhea

Front 20

fluoxetine

Back 20

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 21

paroxetine

Back 21

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 22

fluvoxamine

Back 22

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 23

sertraline

Back 23

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 24

citalopram

Back 24

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 25

escitalopram

Back 25

SSRI, competitive inhibition of serotonin transporter, ADEs are N, HA, anxiety, sexual dysfxn

Front 26

amitriptyline

Back 26

TCA, 3 ring fused system, similar efficacy to SSRIs but more ADEs: hypotension, anticholinergic, sedation, cardiotoxicity (slow conduction due to Na channel blockade), suicidal ideation (as with any antidepressant), can get severe hypertension if used with MAOI

Front 27

clomipramine

Back 27

TCA, 3 ring fused system, similar efficacy to SSRIs but more ADEs: hypotension, anticholinergic, sedation, cardiotoxicity (slow conduction due to Na channel blockade), suicidal ideation (as with any antidepressant), can get severe hypertension if used with MAOI

Front 28

imipramine

Back 28

TCA, 3 ring fused system, similar efficacy to SSRIs but more ADEs: hypotension, anticholinergic, sedation, cardiotoxicity (slow conduction due to Na channel blockade), suicidal ideation (as with any antidepressant), can get severe hypertension if used with MAOI

Front 29

desipramine

Back 29

TCA, 3 ring fused system, similar efficacy to SSRIs but more ADEs: hypotension, anticholinergic, sedation, cardiotoxicity (slow conduction due to Na channel blockade), suicidal ideation (as with any antidepressant), can get severe hypertension if used with MAOI

Front 30

MAO A preference

Back 30

5HT

Front 31

MAO B preference

Back 31

for NE, DA, estphenylethylamine

Front 32

phenelzine

Back 32

MAOI
irreversible inhibitor of MAO-A and MAO-B, risk of hypertensive crisis if taken with TCA or high diet of tyramine (get tachycardic, HA, N, V), other ADEs are hypotension, GI, CNS stimulation, and more

Front 33

tranylcypromine

Back 33

MAOI
irreversible inhibitor of MAO-A and MAO-B, risk of hypertensive crisis if taken with TCA or high diet of tyramine (get tachycardic, HA, N, V), other ADEs are hypotension, GI, CNS stimulation, and more

Front 34

moclobemide

Back 34

MAOI
newer reversible inhibitor that is MAO-A selective, risk of hypertensive crisis if taken with TCA or high diet of tyramine (get tachycardic, HA, N, V), other ADEs are hypotension, GI, CNS stimulation, and more

Front 35

selegiline

Back 35

MAOI
irreversible inhibitor that is MAO-B selective at low doses, risk of hypertensive crisis if taken with TCA or high diet of tyramine (get tachycardic, HA, N, V), other ADEs are hypotension, GI, CNS stimulation, and more

Front 36

Trazodone

Back 36

-SARI- serotonin and adrenergic reuptake inhibitor
-is antagonist, but metabolite (m-CPP) is agonist
-ADEs are sedation, orthostatic hypotension, sexual dysfxn (but less anticholinergic and cardiac effects)

Front 37

Nefazodone

Back 37

-SARI- serotonin and andrenergic reuptake inhibitor
-is antagonist, but metabolite (m-CPP) is agonist
-ADEs are liver failure, very sedating (due to histamine antagonist), hypotension (blocking A1)

Front 38

Bupropion

Back 38

-DRI- dopamine and norepinephrine reuptake inhibition
-ADEs are seizures at high doses, anorexia, worsening of psychotic symptoms (due to increasing DA)
-less hypotension, anticholinergic, and cardio effects than TCAs
-also used to treat smoking or nicotine withdrawal

Front 39

Venlafaxine

Back 39

-SNRI- serotonin and norepinephrine reuptake inhibitor
-only 5-HT at low dose, both at high dose
-ADEs are N, dizziness, insomnia, sexual dysfxn (like SSRIs)

Front 40

Duloxetine

Back 40

-SNRI- serotonin and norepinephrine reuptake inhibitor
-100 times more potent than venlafaxine
-inhibits both 5HT and NE at low dose

Front 41

Mirtazapine

Back 41

-is an antagonist at A2 receptor and at most 5HT post-synaptic sites, but not at 5-HT1A (normally A2 blocks release of 5HT, so you facilitate 5HT release) and then (you improve mood by not having inhibitory activity at 1A receptor)
-ADE is sedation!!, increased appetite, and weight gain (does not have same ADEs as most SSRIs)

Front 42

Lithium

Back 42

for chronic (mood stabilizer)
-rapidly absorbed but takes weeks to become effective
-dietary Na will decrease lithium’s effectiveness, while low Na will cause toxicity
-very toxic, therapeutic dose is 0.6-1.4 but toxic over 1.5 (get persistant GI upset)
-best at decreasing risk of suicide
-MOA: competitive inhibitor of inositol monophosphatase (enzyme important in inosital phosphates signaling), and inhibitor of glycogen synthase kinase 3B
-ADEs: GI, tremor, polyuria, hypothyroidism, birth defects

Front 43

Carbamazepine

Back 43

acute and chronic
-ADES are dipolopia and ataxia
-concern about aplastic anemia and agranulocytosis

Front 44

Valproic acid

Back 44

acute and chronic
-also inhibits glycogen synthase kinase 3B
-ADEs are N, V, GI upset
-fine tremor, hepatotoxicity

Front 45

Haloperidol

Back 45

for acute manic phase

Front 46

Lorazepam

Back 46

for acute manic phase

Front 47

cocaine #

Back 47

5

Front 48

amphetamine #

Back 48

5

Front 49

nicotine #

Back 49

4

Front 50

caffeine #

Back 50

1

Front 51

ethanol #

Back 51

3

Front 52

benzo/barb #

Back 52

3

Front 53

heroin #

Back 53

4

Front 54

oxycodone/hydrocodone #

Back 54

3

Front 55

marijuana #

Back 55

2

Front 56

LSD #

Back 56

1

Front 57

ecstasy #

Back 57

1.5

Front 58

ketamine #

Back 58

1.5

Front 59

Orexins/hypocretins

Back 59

-neuropeptides produced in hypothalamus- activity governs arousal and alertness, enhance dopamine reward pathway
-antagonists of orexin receptors increase sleep, may help treat obesity and drug addiction

Front 60

Sildenafil

Back 60

-inhibits 5-phosphodiesterase which then prolongs smooth muscle relaxant effects of cGMP
-high affinity for retina (visual disturbances)
-ADEs are HA, flushing, indigestion, priprism not common
-contra in nitrate patients

Front 61

Tadalafil

Back 61

-may have muscle pain due to PDE11 inhibition

Front 62

papaverine

Back 62

Papaverine- direct smooth muscle relaxant injected into penis

Front 63

phentolamine

Back 63

Phentolamine- A1 antagonist injected into penis

Front 64

yohimbine

Back 64

Yohimbine- A1 antagonist, no efficacy

Front 65

apomorphine

Back 65

Apomorphine- dopamine agonist used for impotence, works but bad ADEs like N, V

Front 66

Disulfiram

Back 66

-for alcohol dependence
-inhibits acetaldehyde dehydrogenase
-if person drinks, have HA, flushing, increased heart rate, N, V

Front 67

Acamprosate

Back 67

-for alcohol dependence
-analog of GABA that modifies signaling, unclear MOA

Front 68

Naltrexone

Back 68

-for alcohol dependence
-opiate receptor antagonist, may reduce craving for alcohol, used as adjunct to psychosocial treatment

Front 69

NRT

Back 69

-for nicotine dependence
-some success when used with treatment programs

Front 70

Bupropion (for use in drug abuse)

Back 70

-for nicotine dependence
-antagonist of nicotinic cholinergic receptors
-reduce severity of nicotine craving and withdrawal, modest efficacy

Front 71

Varenicline

Back 71

-for nicotine dependence
-selective and partial agonist to nicotinic cholinergic receptors
-partial agonist activity reduces craving and withdrawal symptoms, block pleasurable effects
-ADE is N, HA, disturbed sleep, suicidal ideation
-may work better than NRT or bupropion

Front 72

Methadone

Back 72

-for opiate dependence
-full agonist of opiate receptor

Front 73

Buprenorphine

Back 73

-for opiate dependence
-partial agonist of mu and antagonist of kappa opioid receptor
-for maintenance therapy and opiate detox

Front 74

Naltrexone

Back 74

-for opiate dependence
-rapid detox, then 12 months of daily oral to prevent relapse
-success rate low because rapid detox does not cure drug craving

Front 75

Rimonabant

Back 75

-drug on horizon to treat addiction- alcohol and drugs
-antagonist of cannabinoid CB1 receptor
-has approval in Europe for obesity